RU2499795C2 - Антагонисты гистаминовых н3-рецепторов - Google Patents

Антагонисты гистаминовых н3-рецепторов Download PDF

Info

Publication number
RU2499795C2
RU2499795C2 RU2011142654/04A RU2011142654A RU2499795C2 RU 2499795 C2 RU2499795 C2 RU 2499795C2 RU 2011142654/04 A RU2011142654/04 A RU 2011142654/04A RU 2011142654 A RU2011142654 A RU 2011142654A RU 2499795 C2 RU2499795 C2 RU 2499795C2
Authority
RU
Russia
Prior art keywords
pyridin
isopropylpiperazin
phenyl
pharmaceutically acceptable
acceptable salt
Prior art date
Application number
RU2011142654/04A
Other languages
English (en)
Other versions
RU2011142654A (ru
Inventor
Рольф Хольвег
Кнуд Эрик Андерсен
Ян Линди СЁРЕНСЕН
Жан Мари ЛУНДБЕК
Original Assignee
Хай Пойнт Фармасьютикалс, ЛЛС
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Хай Пойнт Фармасьютикалс, ЛЛС filed Critical Хай Пойнт Фармасьютикалс, ЛЛС
Publication of RU2011142654A publication Critical patent/RU2011142654A/ru
Application granted granted Critical
Publication of RU2499795C2 publication Critical patent/RU2499795C2/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/86—Hydrazides; Thio or imino analogues thereof
    • C07D213/87—Hydrazides; Thio or imino analogues thereof in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)

Abstract

Изобретение относится к новым соединениям, которые взаимодействуют с Н3-гистаминовым рецептором и содержат в своей структуре пиридиновое кольцо. Кроме того, изобретение относится к фармацевтической композиции для модуляции Н3-гистаминовых рецепторов, содержащей соединения, описанные выше. Технический результат: описанные соединения являются полезными в лечении ряда заболеваний или состояний, при которых взаимодействия с Н3-гистаминовым рецептором являются благоприятными, таким образом, данные соединения могут найти применение, например, в лечении заболеваний центральной нервной системы, периферической нервной системы, сердечно-сосудистой системы, пульмональной системы, желудочно-кишечного тракта и эндокринной системы. 2 н. и 7 з.п. ф-лы, 216 пр.

Description

Текст описания приведен в факсимильном виде.
Figure 00000001
Figure 00000002
Figure 00000003
Figure 00000004
Figure 00000005
Figure 00000006
Figure 00000007
Figure 00000008
Figure 00000009
Figure 00000010
Figure 00000011
Figure 00000012
Figure 00000013
Figure 00000014
Figure 00000015
Figure 00000016
Figure 00000017
Figure 00000018
Figure 00000019
Figure 00000020
Figure 00000021
Figure 00000022
Figure 00000023
Figure 00000024
Figure 00000025
Figure 00000026
Figure 00000027
Figure 00000028
Figure 00000029
Figure 00000030
Figure 00000031
Figure 00000032
Figure 00000033
Figure 00000034
Figure 00000035
Figure 00000036
Figure 00000037
Figure 00000038
Figure 00000039
Figure 00000040
Figure 00000041
Figure 00000042
Figure 00000043
Figure 00000044
Figure 00000045
Figure 00000046
Figure 00000047
Figure 00000048
Figure 00000049
Figure 00000050
Figure 00000051
Figure 00000052
Figure 00000053
Figure 00000054
Figure 00000055
Figure 00000056
Figure 00000057
Figure 00000058
Figure 00000059
Figure 00000060
Figure 00000061
Figure 00000062
Figure 00000063
Figure 00000064
Figure 00000065
Figure 00000066
Figure 00000067
Figure 00000068
Figure 00000069
Figure 00000070
Figure 00000071
Figure 00000072
Figure 00000073
Figure 00000074
Figure 00000075
Figure 00000076
Figure 00000077
Figure 00000078
Figure 00000079
Figure 00000080
Figure 00000081
Figure 00000082
Figure 00000083
Figure 00000084
Figure 00000085
Figure 00000086
Figure 00000087
Figure 00000088
Figure 00000089
Figure 00000090
Figure 00000091
Figure 00000092
Figure 00000093
Figure 00000094
Figure 00000095
Figure 00000096
Figure 00000097
Figure 00000098
Figure 00000099
Figure 00000100
Figure 00000101
Figure 00000102
Figure 00000103
Figure 00000104
Figure 00000105
Figure 00000106
Figure 00000107
Figure 00000108
Figure 00000109
Figure 00000110
Figure 00000111
Figure 00000112
Figure 00000113
Figure 00000114
Figure 00000115
Figure 00000116
Figure 00000117
Figure 00000118
Figure 00000119
Figure 00000120
Figure 00000121
Figure 00000122
Figure 00000123
Figure 00000124
Figure 00000125
Figure 00000126
Figure 00000127
Figure 00000128
Figure 00000129
Figure 00000130
Figure 00000131
Figure 00000132
Figure 00000133
Figure 00000134
Figure 00000135
Figure 00000136
Figure 00000137
Figure 00000138
Figure 00000139
Figure 00000140
Figure 00000141
Figure 00000142
Figure 00000143
Figure 00000144
Figure 00000145
Figure 00000146
Figure 00000147
Figure 00000148
Figure 00000149
Figure 00000150
Figure 00000151
Figure 00000152
Figure 00000153
Figure 00000154
Figure 00000155
Figure 00000156
Figure 00000157
Figure 00000158
Figure 00000159
Figure 00000160
Figure 00000161
Figure 00000162
Figure 00000163
Figure 00000164
Figure 00000165
Figure 00000166
Figure 00000167
Figure 00000168
Figure 00000169
Figure 00000170
Figure 00000171
Figure 00000172
Figure 00000173
Figure 00000174
Figure 00000175
Figure 00000176
Figure 00000177
Figure 00000178
Figure 00000179
Figure 00000180
Figure 00000181
Figure 00000182
Figure 00000183
Figure 00000184
Figure 00000185
Figure 00000186
Figure 00000187
Figure 00000188
Figure 00000189
Figure 00000190
Figure 00000191
Figure 00000192
Figure 00000193
Figure 00000194
Figure 00000195
Figure 00000196
Figure 00000197
Figure 00000198
Figure 00000199
Figure 00000200
Figure 00000201
Figure 00000202
Figure 00000203
Figure 00000204
Figure 00000205
Figure 00000206
Figure 00000207
Figure 00000208
Figure 00000209
Figure 00000210
Figure 00000211
Figure 00000212

Claims (9)

1. Соединение, которое выбрано из группы, включающей в себя:
N-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}ацетамид;
N-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}ацетамид;
4-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}морфолин;
N,N-Диизопропил-4-[6-(4-изопропилпиперазин-1-ил)пиридин-3-ил]бензамид;
{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}-(4-метилпиперидин-1-ил)метанон;
{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}морфолин-4-илметанон;
4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]-N,N-диметилбензамид;
{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}пиперидин-1-илметанон;
(4-Гидроксиметилпиперидин-1-ил)-{4-[6-(4-изопропилпиперазин-1-ил)пиридин-3-ил]фенил}-метанон;
{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}-(4-метилпиперазин-1-ил)метанон;
{4-[6-(4-Циклопропилпиперазин-1-ил)пиридин-3-ил]фенил}пиперидин-1-илметанон;
{4-[6-(4-Циклопропилпиперазин-1-ил)пиридин-3-ил]фенил}-(4-метилпиперазин-1-ил)метанон;
{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}-(4-метоксиметилпиперидин-1-ил)-метанон;
{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}диметиламин;
1-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}-4-метилпиперазин;
(1-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}пиперидин-4-ил)метанол;
1-Изопропил-4-[5-(4-пиперидин-1-илметилфенил)пиридин-2-ил]пиперазин;
1-Циклопропил-4-[5-(4-пиперидин-1-илметилфенил)пиридин-2-ил]пиперазин;
или его фармацевтически приемлемая соль.
2. Соединение по п.1, которое представляет собой N-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}ацетамид или его фармацевтически приемлемую соль.
3. Соединение по п.1, которое представляет собой N-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}ацетамид или его фармацевтически приемлемую соль.
4. Соединение по п.1, которое представляет собой 4-{4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]бензил}морфолин или его фармацевтически приемлемую соль.
5. Соединение по п.1, которое представляет собой N,N-Диизопропил-4-[6-(4-изопропилпиперазин-1-ил)пиридин-3-ил]бензамид или его фармацевтически приемлемую соль.
6. Соединение по п.1, которое представляет собой {4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}-(4-метилпиперидин-1-ил)метанон или его фармацевтически приемлемую соль.
7. Соединение по п.1, которое представляет собой {4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]фенил}морфолин-4-илметанон или его фармацевтически приемлемую соль.
8. Соединение по п.1, которое представляет собой 4-[6-(4-Изопропилпиперазин-1-ил)пиридин-3-ил]-N,N-диметилбензамид или его фармацевтически приемлемую соль.
9. Фармацевтическая композиция для модуляции Н3-гистаминовых рецепторов, содержащая соединение по любому из пп.1-8 и фармацевтически приемлемый носитель или эксципиент.
RU2011142654/04A 2005-07-04 2006-06-30 Антагонисты гистаминовых н3-рецепторов RU2499795C2 (ru)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
EP05106038 2005-07-04
EP05106037 2005-07-04
EP05106038.2 2005-07-04
EP05106037.4 2005-07-04
EP05109674 2005-10-18
EP05109674.1 2005-10-18
EP06114615 2006-05-29
EP06114615.5 2006-05-29

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
RU2007147044/04A Division RU2442775C2 (ru) 2005-07-04 2006-06-30 Антагонисты гистаминовых н3-рецепторов

Publications (2)

Publication Number Publication Date
RU2011142654A RU2011142654A (ru) 2013-04-27
RU2499795C2 true RU2499795C2 (ru) 2013-11-27

Family

ID=37198852

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2011142654/04A RU2499795C2 (ru) 2005-07-04 2006-06-30 Антагонисты гистаминовых н3-рецепторов

Country Status (13)

Country Link
US (2) US8501739B2 (ru)
EP (3) EP2233470B1 (ru)
JP (1) JP5121707B2 (ru)
KR (1) KR101286569B1 (ru)
CN (1) CN103110635A (ru)
AT (1) ATE536344T1 (ru)
AU (1) AU2006264966B2 (ru)
BR (1) BRPI0613564A2 (ru)
CA (1) CA2614116A1 (ru)
ES (1) ES2375929T3 (ru)
MX (1) MX2007015675A (ru)
RU (1) RU2499795C2 (ru)
WO (1) WO2007003604A2 (ru)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030236259A1 (en) * 2002-02-05 2003-12-25 Rolf Hohlweg Novel aryl- and heteroarylpiperazines
RU2499795C2 (ru) 2005-07-04 2013-11-27 Хай Пойнт Фармасьютикалс, ЛЛС Антагонисты гистаминовых н3-рецепторов
GB0525957D0 (en) * 2005-12-21 2006-02-01 Astrazeneca Ab Methods
CA2648036C (en) 2006-03-31 2012-05-22 Janssen Pharmaceutica N.V. Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine h4 receptor
JP2009537596A (ja) * 2006-05-23 2009-10-29 ハイ ポイント ファーマシューティカルズ，リミティド ライアビリティ カンパニー ６−（４−シクロプロピルピペリジン−１−イル）−２’−メチル−［３，４’］−ビピリジン及びその医薬としての使用
CA2659570C (en) 2006-05-29 2015-10-06 High Point Pharmaceuticals, Llc 3-(1,3-benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)-pyridazine, its salts and solvates and its use as histamine h3 receptor antagonist
US9108948B2 (en) 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
WO2007150010A2 (en) 2006-06-23 2007-12-27 Abbott Laboratories Cyclopropyl amine derivatives as histamin h3 receptor modulators
TW200901998A (en) * 2007-03-06 2009-01-16 Astrazeneca Ab Novel 2-heteroaryl substituted benzothiophenes and benzofuranes
WO2008145681A2 (en) * 2007-05-31 2008-12-04 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists and uses thereof
EP2014656A3 (en) * 2007-06-11 2011-08-24 High Point Pharmaceuticals, LLC New heteocyclic h3 antagonists
MX2010008384A (es) * 2008-01-30 2010-11-30 Cephalon Inc Derivados de piridazina substituida, con actividad antagonista de h3 de histamina.
EP3782991A1 (en) 2008-05-14 2021-02-24 The Scripps Research Institute Novel modulators of sphingosine phosphate receptors
US9371311B2 (en) 2008-06-30 2016-06-21 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine derivatives
US8193363B2 (en) 2008-08-29 2012-06-05 Astrazeneca Ab Compounds suitable as precursors to compounds that are useful for imaging amyloid deposits
PE20120061A1 (es) 2008-12-19 2012-02-19 Boehringer Ingelheim Int Derivados de pirimidina como antagonistas del receptor ccr2
AU2010226826A1 (en) 2009-03-18 2011-10-13 Merck Sharp & Dohme Corp. Bicyclic compounds as inhibitors of diacylglycerol acyltransferase
US9186353B2 (en) 2009-04-27 2015-11-17 Abbvie Inc. Treatment of osteoarthritis pain
WO2011034078A1 (ja) * 2009-09-16 2011-03-24 アステラス製薬株式会社 グリシン化合物
SI2513093T1 (sl) 2009-12-17 2014-11-28 Boehringer Ingelheim International Gmbh Novi CCR2 receptorski antagonisti in njihove uporabe
EP2560488B1 (en) 2010-04-23 2015-10-28 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
EP2569294B1 (en) * 2010-05-11 2015-03-11 Sanofi Substituted n-heteroaryl bipyrrolidine carboxamides, preparation and therapeutic use thereof
JP5646736B2 (ja) 2010-05-12 2014-12-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規ｃｃｒ２受容体アンタゴニスト、これらの製造方法、及び薬物としてのこれらの使用
JP2013526507A (ja) 2010-05-12 2013-06-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規ｃｃｒ２受容体アンタゴニスト、その製造方法及び薬物としてのその使用
JP5647339B2 (ja) 2010-05-17 2014-12-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃｃｒ２アンタゴニスト及びこれらの使用
US9018212B2 (en) 2010-05-25 2015-04-28 Boehringer Ingelheim International Gmbh Pyridazine carboxamides as CCR2 receptor antagonists
US8962656B2 (en) 2010-06-01 2015-02-24 Boehringer Ingelheim International Gmbh CCR2 antagonists
WO2012037258A1 (en) 2010-09-16 2012-03-22 Abbott Laboratories Processes for preparing 1,2-substituted cyclopropyl derivatives
JP5786258B2 (ja) 2011-07-15 2015-09-30 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規かつ選択的なｃｃｒ２拮抗薬
WO2013076590A1 (en) 2011-11-23 2013-05-30 Oxygen Healthcare Research Pvt. Ltd Benzothiazine compounds as h3 receptor ligands
US8729263B2 (en) 2012-08-13 2014-05-20 Novartis Ag 1,4-disubstituted pyridazine analogs there of and methods for treating SMN-deficiency-related conditions
SI2964229T1 (sl) 2013-03-06 2020-02-28 Janssen Pharmaceutica Nv Benzoimidazol-2-il pirimidin modulatorji receptorja histamina H4
GB201311953D0 (en) * 2013-07-03 2013-08-14 Redx Pharma Ltd Compounds
US20160184305A1 (en) 2013-07-31 2016-06-30 Novartis Ag 1,4-disubstituted pyridazine quinolne analogs there of and methods for treating smn-deficiency-related conditions
EP3053577A1 (en) * 2015-02-09 2016-08-10 F. Hoffmann-La Roche AG Compounds for the treatment of cancer
JP6884102B2 (ja) 2015-02-09 2021-06-09 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト がんの治療のための化合物
BR112017028492B1 (pt) 2015-07-02 2023-12-26 Centrexion Therapeutics Corporation Citrato de (4-((3r,4r)-3-metoxitetra-hidro-piran-4- ilamino)piperidin-1-il) (5- metil-6-(((2r, 6s)-6-(p-tolil) tetra-hidro-2h-piran-2-il)metilamino)pirimidin-4-il) metanona, seu uso e seu método de preparação, e composição farmacêutica
EP3373935B1 (en) * 2015-11-12 2021-09-01 Merck Sharp & Dohme Corp. Cyanopyridine derivatives as liver x receptor beta agonists, compositions, and their use
IL294124B2 (en) * 2015-12-10 2024-02-01 Ptc Therapeutics Inc Methods for treating Huntington's disease
WO2018165520A1 (en) 2017-03-10 2018-09-13 Vps-3, Inc. Metalloenzyme inhibitor compounds
MX2019014514A (es) 2017-06-05 2020-07-20 Ptc Therapeutics Inc Compuestos para tratar la enfermedad de huntington.
BR112019027717A2 (pt) 2017-06-28 2020-07-28 Ptc Therapeutics, Inc. métodos para tratar a doença de huntington
US11395822B2 (en) 2017-06-28 2022-07-26 Ptc Therapeutics, Inc. Methods for treating Huntington's disease
CA3094703A1 (en) * 2018-03-27 2019-10-03 Ptc Therapeutics, Inc. Compounds for treating huntington's disease
EP3814360B8 (en) 2018-06-27 2024-11-06 PTC Therapeutics, Inc. Heteroaryl compounds for treating huntington's disease
EA202092896A1 (ru) 2018-06-27 2021-04-13 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Гетероциклические и гетероарильные соединения для лечения болезни гентингтона
CN114600165A (zh) 2019-09-17 2022-06-07 波士顿偏振测定公司 用于使用偏振提示表面建模的系统和方法
US12099148B2 (en) 2019-10-07 2024-09-24 Intrinsic Innovation Llc Systems and methods for surface normals sensing with polarization
MX2022005289A (es) 2019-11-30 2022-08-08 Boston Polarimetrics Inc Sistemas y metodos para segmentacion de objetos transparentes usando se?ales de polarizacion.
CN115552486A (zh) 2020-01-29 2022-12-30 因思创新有限责任公司 用于表征物体姿态检测和测量系统的系统和方法
EP4085424A4 (en) 2020-01-30 2024-03-27 Intrinsic Innovation LLC SYSTEMS AND METHODS OF DATA SYNTHESIS FOR TRAINING STATISTICAL MODELS ON DIFFERENT IMAGING MODALITIES INCLUDING POLARIZED IMAGES
WO2021243088A1 (en) 2020-05-27 2021-12-02 Boston Polarimetrics, Inc. Multi-aperture polarization optical systems using beam splitters
WO2022053541A1 (en) * 2020-09-10 2022-03-17 Eracal Therapeutics Ltd. Compounds for use as appetite suppressant
US12020455B2 (en) 2021-03-10 2024-06-25 Intrinsic Innovation Llc Systems and methods for high dynamic range image reconstruction
US12069227B2 (en) 2021-03-10 2024-08-20 Intrinsic Innovation Llc Multi-modal and multi-spectral stereo camera arrays
US11290658B1 (en) 2021-04-15 2022-03-29 Boston Polarimetrics, Inc. Systems and methods for camera exposure control
US11954886B2 (en) 2021-04-15 2024-04-09 Intrinsic Innovation Llc Systems and methods for six-degree of freedom pose estimation of deformable objects
US12067746B2 (en) 2021-05-07 2024-08-20 Intrinsic Innovation Llc Systems and methods for using computer vision to pick up small objects
US11689813B2 (en) 2021-07-01 2023-06-27 Intrinsic Innovation Llc Systems and methods for high dynamic range imaging using crossed polarizers
WO2023034836A1 (en) * 2021-08-30 2023-03-09 Remix Therapeutics Inc. Compounds and methods for modulating splicing
CN114478478B (zh) * 2022-02-18 2023-06-13 厦门大学 N-(1-(6-(取代苯基)哒嗪-3-基)哌啶-3-基)胺/酰胺衍生物及制备方法

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1345880A (en) * 1971-06-18 1974-02-06 Cepbepe Pyridazine derivatives
US3886161A (en) * 1970-12-14 1975-05-27 Sandoz Ag 2-Piperazino-3-cyano-5-phenyl-pyridines
DE2824764A1 (de) * 1978-06-06 1979-12-20 Hoechst Ag Neue pyridylpiperazinderivate und verfahren zu ihrer herstellung
US4251658A (en) * 1977-06-13 1981-02-17 Richter Gedeon Vegyeszeti Gyar Rt. 3-(1-Pyrazolyl)-pyridazine derivatives
US4616014A (en) * 1981-10-22 1986-10-07 Fujisawa Pharmaceutical Co., Ltd. Triazine derivatives, and pharmaceutical compositions comprising the same
EA005160B1 (ru) * 2001-07-12 2004-12-30 Ле Лаборатуар Сервье НОВЫЕ СОЕДИНЕНИЯ ОКТАГИДРО-2H-ПИРИДО[1,2-α]ПИРАЗИНА, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ ПРЕПАРАТЫ, ИХ СОДЕРЖАЩИЕ
WO2005028438A1 (ja) * 2003-09-22 2005-03-31 Banyu Pharmaceutical Co., Ltd. 新規ピペリジン誘導体

Family Cites Families (125)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB753166A (en) 1953-05-22 1956-07-18 Miles Lab Improvements in or relating to substituted piperazines
US2724713A (en) * 1954-03-24 1955-11-22 American Cyanamid Co 1-carbobenzoxypiperazines and process of preparing same
US2993899A (en) * 1958-03-31 1961-07-25 Miles Lab Acetylenically unsaturated piperazine derivatives
US3164598A (en) * 1963-02-01 1965-01-05 American Home Prod Substituted 1, 4-diazabicyclo[4.3.0]nonanes and methods for their preparation
US3309370A (en) * 1964-07-16 1967-03-14 Miles Lab Bicycloalkyl piperazine derivatives and process
GB1293565A (en) * 1969-05-03 1972-10-18 Aspro Nicholas Ltd Aminophthalazines and pharmaceutical compositions thereof
DE2516040C2 (de) * 1974-06-10 1984-12-20 Dr. Karl Thomae Gmbh, 7950 Biberach Benzimidazole, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel
FR2306694A1 (fr) 1975-04-07 1976-11-05 Parcor Derives de la piperazine
GB1545094A (en) * 1976-12-14 1979-05-02 Gist Brocades Nv Piperazine derivatives
US4144346A (en) * 1977-01-31 1979-03-13 Janssen Pharmaceutica N.V. Novel 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles
US4163849A (en) * 1978-03-17 1979-08-07 Merck & Co., Inc. Piperazinylpyrazines
DE3160397D1 (en) 1980-02-22 1983-07-14 Tanabe Seiyaku Co Phenoxyalkane derivative and processes for preparing same
US4339579A (en) * 1980-12-29 1982-07-13 American Home Products Corporation 2,6-Bis-(pyrrolopyrazinyl)pyrazines
US5001125A (en) * 1984-03-26 1991-03-19 Janssen Pharmaceutica N.V. Anti-virally active pyridazinamines
FR2573075B1 (fr) * 1984-09-14 1987-03-20 Innothera Lab Sa Nouvelles (pyridyl-2)-1 piperazines, leur procede de preparation et leur application en therapeutique
DE3526235A1 (de) 1984-11-16 1986-05-22 Bayer Ag, 5090 Leverkusen Fluessigkristallzusammensetzungen
KR860700352A (ko) * 1984-11-27 1986-10-06 후지와라 도미오 2--(1-피페라지닐)-4-치환 페닐퀴놀린 유도체와 그 염의 제조방법
ATE77817T1 (de) 1985-04-30 1992-07-15 Dresden Arzneimittel 3-cyan-pyridine, verfahren zu ihrer herstellung und ihre pharmazeutische verwendung.
US4670505A (en) * 1985-08-23 1987-06-02 Hercules Incorporated Polyacrylate dispersions
PH25772A (en) 1985-08-30 1991-10-18 Novo Industri As Insulin analogues, process for their preparation
DK111387A (da) 1986-03-05 1987-09-06 Otsuka Pharma Co Ltd Carbostyrilderivater og salte deraf, laegemiddel indeholdende saadanne derivater samt fremgangsmaade til fremstilling af derivaterne
DE3609596A1 (de) * 1986-03-21 1987-10-01 Hoechst Ag 2-azolylmethyl-2-aryl-1,3-dioxolane und deren salze, verfahren zu ihrer herstellung, sie enthaltende mittel und ihre verwendung
MY104343A (en) 1987-11-23 1994-03-31 Janssen Pharmaceutica Nv Novel pyridizinamine deravatives
DE3803860A1 (de) 1988-02-09 1989-08-17 Basf Ag N,n'-disubstituierte piperazine
DE3837825A1 (de) 1988-11-08 1990-05-10 Hoechst Ag Neue insulinderivate, ihre verwendung und eine sie enthaltende pharmazeutische zubereitung
ES2058630T3 (es) 1989-03-03 1994-11-01 Dainippon Pharmaceutical Co Derivados de 2-(1-piperazinil)-4-fenilcicloalcanopiridinas, procedimientos de preparacion y composiciones farmaceuticas que los contienen.
GB9012316D0 (en) 1990-06-01 1990-07-18 Wellcome Found Pharmacologically active cns compounds
EP0674627A1 (en) 1992-12-18 1995-10-04 The Wellcome Foundation Limited Pyrimidine, pyridine, pteridinone and indazole derivatives as enzyme inhibitors
DE4308028B4 (de) * 1993-03-13 2012-08-16 Merck Patent Gmbh 1,2,2,2-Tetrafluorethylether und flüssigkristallines Medium
WO1994022846A1 (en) 1993-03-30 1994-10-13 Pfizer Inc. Compounds enhancing antitumor activity of other cytotoxic agents
JP3377826B2 (ja) 1993-05-06 2003-02-17 ヘキスト・アクチェンゲゼルシャフト 液晶組成物に使用するための新規化合物
DE122006000015I1 (de) 1993-06-21 2006-06-29 Novo Nordisk As Asp-B28-Insulinkristalle
HU217684B (hu) 1993-09-17 2000-03-28 Novo Nordisk A/S Acilezett inzulinszármazékok és azokat tartalmazó gyógyszerkészítmények és előállításuk
IL111730A (en) 1993-11-29 1998-12-06 Fujisawa Pharmaceutical Co Piperazine derivatives, processes for their preparation and pharmaceutical preparations containing them
US5504188A (en) 1994-06-16 1996-04-02 Eli Lilly And Company Preparation of stable zinc insulin analog crystals
DE4423044A1 (de) 1994-07-01 1996-01-04 Hoechst Ag 1-(3-Alkyloxiran-2-yl)alkylester mesogener Carbonsäuren und ihre Verwendung in flüssigkristallinen Mischungen
DE4425642A1 (de) 1994-07-20 1996-01-25 Merck Patent Gmbh Partiell fluorierte Benzolderivate
WO1997002245A1 (fr) 1995-07-06 1997-01-23 Japan Tobacco Inc. Derives de benzamidoxime et leur utilisation a des fins medicinales
US6130217A (en) * 1995-09-20 2000-10-10 Pfizer Inc Compounds enhancing antitumor activity of other cytotoxic agents
TR199800827T2 (xx) * 1995-11-09 1999-02-22 Synthelabo 5-HT4, H3 resept�r ligandlar� olarak 5-fenil-3-(piperidin-4-il)-1,3,4-oksadiyazol-2(3H)-on t�revleri.
PL327938A1 (en) 1996-01-17 1999-01-04 Novo Nordisk As Derivatives of 1,2,4-thiadiazine and 1,4-thiazine, their production and application
EP0923580A1 (en) 1996-07-26 1999-06-23 Dr. Reddy's Research Foundation Thiazolidinedione compounds having antidiabetic, hypolipidaemic, antihypertensive properties, process for their preparation and pharmaceutical compositions thereof
UA72181C2 (ru) 1996-08-30 2005-02-15 Ново Нордіск А/С Translated By PlajПРОИЗВОДНЫЕ ГЛЮКАГОНООБРАЗНОГО ПЕПТИДА-1
DZ2376A1 (fr) 1996-12-19 2002-12-28 Smithkline Beecham Plc Dérivés de sulfonamides nouveaux procédé pour leurpréparation et compositions pharmaceutiques les c ontenant.
IL127296A (en) 1996-12-31 2003-01-12 Reddy Research Foundation Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them
WO1997041119A1 (en) 1997-05-02 1997-11-06 Dr. Reddy's Research Foundation Novel antidiabetic compounds having hypolipidaemic, antihypertensive properties, process for their preparation and pharmaceutical compositions containing them
US6613942B1 (en) 1997-07-01 2003-09-02 Novo Nordisk A/S Glucagon antagonists/inverse agonists
WO1999001423A1 (en) 1997-07-01 1999-01-14 Novo Nordisk A/S Glucagon antagonists/inverse agonists
RU2215004C2 (ru) 1997-07-16 2003-10-27 Ново Нордиск А/С Конденсированное производное 1,2,4-тиадиазина, фармацевтическая композиция и способ получения лекарственного препарата
EP0927992A4 (en) 1997-07-17 1999-09-15 Sony Corp MAGNETIC RECORDING MEDIUM AND MAGNETIC RECORDING / REPRODUCING DEVICE COMPRISING SAME
WO1999018077A1 (fr) 1997-10-02 1999-04-15 Eisai Co., Ltd. Derives de pyridine condenses
CA2306082A1 (en) 1997-10-27 1999-05-06 Agouron Pharmaceuticals, Inc. Substituted 4-amino-thiazol-2-y compounds as cdks inhibitors
WO1999019313A1 (en) 1997-10-27 1999-04-22 Dr. Reddy's Research Foundation Novel tricyclic compounds and their use in medicine; process for their preparation and pharmaceutical compositions containing them
US6440961B1 (en) 1997-10-27 2002-08-27 Dr. Reddy's Research Foundation Tricyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them
EP0971917B1 (en) 1997-12-02 2002-02-06 Dr. Reddy's Research Foundation Thiazolidinedione and oxazolidinedione derivatives having antidiabetic, hypolipidaemic and antihypertensive properties
EP0978512A1 (en) 1998-07-29 2000-02-09 Societe Civile Bioprojet Non-imidazole aryloxy (or arylthio) alkylamines as histamine H3-receptor antagonists and their therapeutic applications
JP2002527503A (ja) 1998-10-21 2002-08-27 ノボ ノルディスク アクティーゼルスカブ 新規化合物類、それらの調製及び使用
EP1123292A1 (en) 1998-10-21 2001-08-16 Novo Nordisk A/S New compounds, their preparation and use
JP2002527502A (ja) 1998-10-21 2002-08-27 ノボ ノルディスク アクティーゼルスカブ 新規化合物、それらの調製及び使用
WO2000023425A1 (en) 1998-10-21 2000-04-27 Novo Nordisk A/S New compounds, their preparation and use
AU6325799A (en) 1998-10-21 2000-05-08 Dr. Reddy's Research Foundation New compounds, their preparation and use
US6353018B1 (en) 1998-10-21 2002-03-05 Novo Nordisk A/S Compounds, their preparation and use
EP1338600A1 (en) 1998-12-18 2003-08-27 Novo Nordisk A/S Fused 1,2,4-Thiadiazine derivatives, their preparation and use
WO2000041121A1 (en) 1999-01-07 2000-07-13 Ccrewards.Com Method and arrangement for issuance and management of digital coupons and sales offers
AU3033500A (en) 1999-01-15 2000-08-01 Agouron Pharmaceuticals, Inc. Non-peptide glp-1 agonists
WO2000063191A1 (en) 1999-04-16 2000-10-26 Dr. Reddy's Research Foundation Novel polymorphic forms of an antidiabetic agent: process for their preparation and a pharmaceutical composition containing them
BR0010683A (pt) 1999-04-16 2003-07-01 Reddy Research Foundation Formas polimórficas de um agente antidiabético: processo para seu preparo e composições farmacêuticas contendo o mesmo
WO2000063193A1 (en) 1999-04-16 2000-10-26 Dr. Reddy's Research Foundation Novel polymorphic forms of an antidiabetic agent: process for their preparation and a pharmaceutical composition containing them
AU3957900A (en) 1999-04-20 2000-11-02 Novo Nordisk A/S New compounds, their preparation and use
CA2367356A1 (en) 1999-04-20 2000-10-26 Per Sauerberg New compounds, their preparation and use
WO2000063196A1 (en) 1999-04-20 2000-10-26 Novo Nordisk A/S New compounds, their preparation and use
EP1171438A1 (en) 1999-04-20 2002-01-16 Novo Nordisk A/S Compounds, their preparation and use
AU2935200A (en) 1999-04-30 2000-11-17 Pfizer Products Inc. Compounds for the treatment of obesity
DE19922723A1 (de) 1999-05-18 2000-11-23 Clariant Gmbh Aktivmatrix-Displays mit hohem Kontrast
DE19934799B4 (de) * 1999-07-28 2008-01-24 Az Electronic Materials (Germany) Gmbh Chiral-smektische Flüssigkristallmischung und ihre Verwendung in Aktivmatrix-Displays mit hohen Kontrastwerten
GB9926302D0 (en) 1999-11-05 2000-01-12 Smithkline Beecham Plc Novel compounds
GB9926303D0 (en) 1999-11-05 2000-01-12 Smithkline Beecham Plc Novel compounds
US6602872B1 (en) 1999-12-13 2003-08-05 Merck & Co., Inc. Substituted pyridazines having cytokine inhibitory activity
FR2802206B1 (fr) * 1999-12-14 2005-04-22 Sod Conseils Rech Applic Derives de 4-aminopiperidine et leur utilisation en tant que medicament
BR0017025A (pt) 1999-12-16 2003-01-07 Schering Corp Antagonistas do receptor y5 do neuropeptìdeo y de imidazola substituìda
FI20000480A0 (fi) 2000-03-01 2000-03-01 Orion Yhtymae Oyj Kinoliini- ja naftaleenijohdannaisia alfa-2 antagonisteina
WO2001066534A2 (en) * 2000-03-09 2001-09-13 Abbott Laboratories Cyclic and bicyclic diamino histamine-3 receptor antagonists
TR200400354T4 (tr) 2000-03-31 2004-04-21 Ortho-Mcneil Pharmaceutical, Inc. Fenil ikameli indolizin türevleri ve bunların histamin H3 ligandları olarak kullanımı
AU2001251083A1 (en) 2000-03-31 2001-10-15 Ortho-Mcneil Pharmaceutical, Inc. Method for using 2-aryloxyalkylaminobenzoxazoles and 2-aryloxyalkylaminobenzothiazoles as h3 antagonists
EP1268421B1 (en) 2000-03-31 2009-05-06 Ortho-McNeil Pharmaceutical, Inc. Phenyl-substituted indoles as histamine h3-receptor antagonists
AU2001249679A1 (en) 2000-03-31 2001-10-15 Ortho-Mcneil Pharmaceutical, Inc. Phenyl-substituted imidazopyridines
AU2001249672A1 (en) 2000-03-31 2001-10-15 Ortho-Mcneil Pharmaceutical, Inc. Method for using 2- or 3-aryl substituted imidazo(1,2-a) pyridines as h3 antagonists
MXPA03001268A (es) 2000-08-08 2004-09-06 Johnson & Johnson Ariloxipiperidinas sin imidazol.
US6316475B1 (en) 2000-11-17 2001-11-13 Abbott Laboratories Aminoalkoxybiphenylcarboxamides as histamine-3 receptor ligands and their therapeutic applications
US20030078271A1 (en) 2001-01-31 2003-04-24 Blackburn Thomas P. Use of GAL3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
US20030073672A1 (en) * 2001-09-05 2003-04-17 Breitenbucher J. Guy Method for treating allergies using substituted pyrazoles
IL162859A0 (en) 2002-02-05 2005-11-20 Novo Nordisk As Novel aryl-and heteroarylpiperazines
US20030236259A1 (en) * 2002-02-05 2003-12-25 Rolf Hohlweg Novel aryl- and heteroarylpiperazines
JP2003277755A (ja) 2002-03-26 2003-10-02 Fuji Photo Film Co Ltd 液晶組成物および液晶素子
US6864261B2 (en) * 2002-05-02 2005-03-08 Euro-Celtique S.A. Therapeutic agents useful for treating pain
SE0201544D0 (sv) * 2002-05-17 2002-05-17 Biovitrum Ab Novel compounds and thier use
US6906060B2 (en) * 2002-06-06 2005-06-14 Novo Nordisk A/S Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines
ATE356127T1 (de) 2002-06-06 2007-03-15 Novo Nordisk As Substituierte hexahydropyrrolo(1,2-a)pyrazine, octahydropyrido(1,2-a)pyrazine und decahydropyrazino(1,2-a)azepine
DE10246657A1 (de) * 2002-10-07 2004-04-15 Merck Patent Gmbh Chirales Phenolderivat, dieses enthaltendes Flüssigkristallmedium, Verfahren zur Herstellung eines Flüssigkristallmediums und elektrooptische Flüssigkristallanzeige
US7332508B2 (en) 2002-12-18 2008-02-19 Novo Nordisk A/S Substituted homopiperidine, piperidine or pyrrolidine derivatives
EP1651615B1 (en) 2003-07-29 2010-03-17 High Point Pharmaceuticals, LLC Pyridazinyl- piperazines and their use as histamine h3 receptor ligands
US20050028438A1 (en) * 2003-08-05 2005-02-10 Campana Kimberly A. Plastic lawn edging fabricated by a continuous vacuum forming process
US20070032477A1 (en) * 2003-10-17 2007-02-08 Waer Mark J A Pteridine derivatives useful for making pharmaceutical compositions
JP2007510747A (ja) 2003-11-10 2007-04-26 シンタ ファーマシューティカルズ コーポレーション ピリジン化合物
FR2864080B1 (fr) * 2003-12-23 2006-02-03 Sanofi Synthelabo Derives de 1-piperazine-et-1-homopiperazine-carboxylates, leur preparation et leur application en therapeutique
JP2007217282A (ja) 2004-03-04 2007-08-30 Astellas Pharma Inc 置換ピリミジン誘導体
ATE499364T1 (de) 2004-04-09 2011-03-15 Merck Sharp & Dohme Hemmer der akt aktivität
CA2563895C (en) 2004-04-13 2012-10-16 Synta Pharmaceuticals Corp. Disalt inhibitors of il-12 production
JP5221952B2 (ja) 2004-05-08 2013-06-26 ノバルティス・インターナショナル・ファーマシューティカル・リミテッド ３−アリール−５，６−ジ置換ピリダジン類
CN1956974B (zh) * 2004-05-19 2010-11-24 巴斯福股份公司 2-取代嘧啶及其作为农药的用途
KR20070034524A (ko) 2004-05-28 2007-03-28 버텍스 파마슈티칼스 인코포레이티드 무스카린 수용체 조정자
CA2589106C (en) 2004-11-02 2015-07-21 Northwestern University Pyridazine compounds, compositions and methods and their use in treating inflammatory diseases
ES2343812T3 (es) 2004-12-03 2010-08-10 F. Hoffmann-La Roche Ag Derivados de piperidina 3-sustituidos como antagonistas del receptor h3.
WO2006090273A2 (en) 2005-02-22 2006-08-31 Warner-Lambert Company Llc [1,8]naphthyridin-2-ones and related compounds with keto or hydroxyl linkers for the treatment of schizophrenia
CA2606288A1 (en) 2005-04-18 2006-10-26 Neurogen Corporation Subtituted heteroaryl cb1 antagonists
FR2885615B1 (fr) 2005-05-12 2007-06-22 Servier Lab Nouveaux derives de phenylpyridinylpiperazine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
FR2885616B1 (fr) * 2005-05-12 2007-06-22 Servier Lab Nouveaux derives de phenylpyridinylpiperazine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
RU2499795C2 (ru) 2005-07-04 2013-11-27 Хай Пойнт Фармасьютикалс, ЛЛС Антагонисты гистаминовых н3-рецепторов
EA019115B1 (ru) 2005-07-15 2014-01-30 Олбани Молекьюлар Рисерч, Инк. Арил- и гетероарилзамещенные тетрагидробензазепины и их применение для блокировки обратного захвата норэпинефрина, допамина и серотонина
EP1909797A4 (en) 2005-08-02 2013-02-27 Neurogen Corp DIPIPERAZINYL KETONE AND RELATED ANALOG
SG170785A1 (en) * 2006-03-28 2011-05-30 Transtech Pharma Benzothiazoles having histamine h3 receptor activity
JP2009537596A (ja) * 2006-05-23 2009-10-29 ハイ ポイント ファーマシューティカルズ，リミティド ライアビリティ カンパニー ６−（４−シクロプロピルピペリジン−１−イル）−２’−メチル−［３，４’］−ビピリジン及びその医薬としての使用
CA2659570C (en) * 2006-05-29 2015-10-06 High Point Pharmaceuticals, Llc 3-(1,3-benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)-pyridazine, its salts and solvates and its use as histamine h3 receptor antagonist
EP2014656A3 (en) * 2007-06-11 2011-08-24 High Point Pharmaceuticals, LLC New heteocyclic h3 antagonists

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3886161A (en) * 1970-12-14 1975-05-27 Sandoz Ag 2-Piperazino-3-cyano-5-phenyl-pyridines
GB1345880A (en) * 1971-06-18 1974-02-06 Cepbepe Pyridazine derivatives
US4251658A (en) * 1977-06-13 1981-02-17 Richter Gedeon Vegyeszeti Gyar Rt. 3-(1-Pyrazolyl)-pyridazine derivatives
DE2824764A1 (de) * 1978-06-06 1979-12-20 Hoechst Ag Neue pyridylpiperazinderivate und verfahren zu ihrer herstellung
US4616014A (en) * 1981-10-22 1986-10-07 Fujisawa Pharmaceutical Co., Ltd. Triazine derivatives, and pharmaceutical compositions comprising the same
EA005160B1 (ru) * 2001-07-12 2004-12-30 Ле Лаборатуар Сервье НОВЫЕ СОЕДИНЕНИЯ ОКТАГИДРО-2H-ПИРИДО[1,2-α]ПИРАЗИНА, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ ПРЕПАРАТЫ, ИХ СОДЕРЖАЩИЕ
WO2005028438A1 (ja) * 2003-09-22 2005-03-31 Banyu Pharmaceutical Co., Ltd. 新規ピペリジン誘導体

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
Contreras J.-M. et al. Journal of Medicinal Chemistry, 1999, vol.42, no.4, pp.730-741, tables. Parrot I et al, Synthesis, 1999, no.7, pp.1163-1168, table 2, compound 1. Klauschenz E et al, European Journal of Medicinal Chemitry, 1994, vol.29, no.3, pp.175-184, table 1, compound 61. Contreras J.-M. et al, Journal of Medicinal Chemistry, 2001, vol.44, no.17, pp.2707-2718, tables. Brown D. J. et al, Australian Journal of Chemistry, 1981, vol.34, no.11, pp.2423-2429, table 1. Database Beilstein, BRN 4870130 1991, abstract. Database Beilstein, BRN 6398075 1988, abstract. Coppola G.M. et al. Journal of Heterocyclic Chemistry, 1980, vo.17, no.7, pp.1479-1482, compound 7C. Werbel L.M. et al. Journal of Heterocyclic Chemistry, 1979, vol.16, no.5, pp.881-894, compounds 13, 22, 30, 32. Database Beilstein, BRN 4182175 1991, abstract. Database Beilstein, Citation No. 5688187, BRN 4807006 1989, abstract. Steck E.A. et al. Journal of Heterocyclic Chemistry, 1975, vol.12, no.5, pp.1009-1013, page 1011 *
Kawaguchi K et al, European Journal of Pharmacology, 1999, vol.364, no.2-3, pp.99-105, compound BW619C89. Tafesse L et al, Bioogranic & Medicinal Chemistry Letters, 2004, vol.14, no.22, pp.5513-5519, scheme 2, compound 6. Haugwitz R.D. et al, Journal of Medicinal Chemistry, 1982, vol.25, no.8, pp.969-974, table 1, compound 16. Levay В et al. Journal of Physical Chemistry. A Molecules, Spectroscopy, Kinetics, Environment and General Theory, 2004, vol.108, pp.1753-1756, compound 3. Adam I et al, Synlett, 2004, no.11, pp.2031-2033, table 1, compound 6c, 6d. *
Lumma W.C. et al. Journal of Medicinal Chemistry, 1978, vol.21, no.6, pp.536-542, table 1, compound 3p. *
Rival Y et al. Journal of Medicinal Chemistry, 1998, vol.41, pp.311-317, compound 11. *

Also Published As

Publication number Publication date
EP2386554A1 (en) 2011-11-16
JP2009500372A (ja) 2009-01-08
US8846677B2 (en) 2014-09-30
WO2007003604A3 (en) 2007-06-21
ATE536344T1 (de) 2011-12-15
RU2011142654A (ru) 2013-04-27
CN103110635A (zh) 2013-05-22
CA2614116A1 (en) 2007-01-11
BRPI0613564A2 (pt) 2011-01-18
EP2233470B1 (en) 2011-12-07
WO2007003604A2 (en) 2007-01-11
US20120232078A1 (en) 2012-09-13
KR20080032069A (ko) 2008-04-14
AU2006264966A1 (en) 2007-01-11
US20090312309A1 (en) 2009-12-17
EP2233470A1 (en) 2010-09-29
AU2006264966B2 (en) 2013-02-21
KR101286569B1 (ko) 2013-07-23
MX2007015675A (es) 2008-02-20
US8501739B2 (en) 2013-08-06
JP5121707B2 (ja) 2013-01-16
EP1902028A2 (en) 2008-03-26
ES2375929T3 (es) 2012-03-07

Similar Documents

Publication Publication Date Title
RU2499795C2 (ru) Антагонисты гистаминовых н3-рецепторов
RU2433128C2 (ru) Новые пиримидиновые производные и их применение в терапии, а также применение пиримидиновых производных в изготовлении лекарственного средства для предупреждения и/или лечения болезни альцгеймера
RU2386630C2 (ru) Соединения и композиции в качестве ингибиторов протеинтирозинкиназы
RU2436776C2 (ru) ДИАРИЛАМИН-СОДЕРЖАЩИЕ СОЕДИНЕНИЯ, КОМПОЗИЦИИ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРОВ с-КIT
RU2452738C2 (ru) Соединения, модулирующие активность c-fms и/или c-kit, и их применения
JP2014511869A5 (ru)
RU2010110640A (ru) Соединения и композиции 5-(4-(галогеналкокси)фенил)пиримидин-2-амина в качестве ингибиторов киназ
RU2427573C2 (ru) Новые производные бензимидазола в качестве ингибиторов ваниллоидного рецептора 1 (vr1)
RU2008127491A (ru) Применение антагониста cb1 для лечения побочных эффектов и негативных симптомов шизофрении
JP2016517878A5 (ru)
RU2006137716A (ru) Ингибиторы гистондеацетилазы
RU2003131964A (ru) Производные 4-(фенил-пиперазинил-метил)-бензамида и их применение для лечения боли, тревоги или желудочно-кишечных расстройств
JP2009513575A5 (ru)
JP2007534687A5 (ru)
JP2013512900A5 (ru)
UY29389A1 (es) Derivados sustituidos del ácido1-((4-((((3,3-dimetil-2-oxo-2,3-dihidro-1h-indol-1-il)carbonil)amino)metil)piperidin-1-il)metil)ciclobutanocarboxílico, sales farmaceuticamente aceptables, composiciones que los contienen y aplicaciones.
JP2009516685A5 (ru)
RU2005109561A (ru) Новые производные аминоиндазолов в качестве лекарственных средств и содержащие их фармацевтические композиции
NZ591427A (en) P38 map kinase inhibitors
JP2019507179A5 (ru)
RU2005121897A (ru) Производные аминоиндазолов и их применение в качестве ингибиторов киназ
JP2013510876A5 (ru)
RU2008120850A (ru) Соединения и композиции в качестве ингибиторов протеинкиназ
RU2009101911A (ru) Производные пиридина и пиразина в качестве ингибиторов mnk-киназы
MX2010006260A (es) Composiciones orales de abt-263 para tratar cancer.

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20160701