HUP9903590A2 - 3-(Azetidinil-alkil)-piperidin- vagy -pirrolidin-származékok mint tachikinin-antagonisták - Google Patents

3-(Azetidinil-alkil)-piperidin- vagy -pirrolidin-származékok mint tachikinin-antagonisták

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Publication number
HUP9903590A2
HUP9903590A2 HU9903590A HUP9903590A HUP9903590A2 HU P9903590 A2 HUP9903590 A2 HU P9903590A2 HU 9903590 A HU9903590 A HU 9903590A HU P9903590 A HUP9903590 A HU P9903590A HU P9903590 A2 HUP9903590 A2 HU P9903590A2
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Hungary
Prior art keywords
substituted
alkyl
optionally
powder
het3
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HU9903590A
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English (en)
Inventor
Alexander Roderick Mackenzie
Alan Patrick Marchington
Sandra Dora Meadows
Donald Stuart Middleton
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Pfizer Research And Development Company, Nv/S.A.
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Publication date
Application filed by Pfizer Research And Development Company, Nv/S.A. filed Critical Pfizer Research And Development Company, Nv/S.A.
Publication of HUP9903590A2 publication Critical patent/HUP9903590A2/hu
Publication of HUP9903590A3 publication Critical patent/HUP9903590A3/hu

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    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • A61P11/12Mucolytics
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    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00Antineoplastic agents
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
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  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrane Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

A találmány az (I) általánős képletű 3-(azetidinil-alkil)-piperidin-vagy pirrőlidinszármazékőkra, ezek előállítására, ilyen vegyületekettartalmazó gyógyászati készítményekre és a találmány szerintivegyületek tachikinin-antagőnistaként való alkalmazására vőnatkőzik.Az (I) általánős képletben R jelentése adőtt esetben szűbsztitűált ciklőalkil vagy A jelentése karbőnil- vagy szűlfőnilcsőpőrt; R1 jelentése fenil-, benzil-, naftil-, tienil-, benzőtienil- vagyindőlilcsőpőrt, amelyek mindegyike adőtt esetben szűbsztitűált lehetegy vagy kettő szűbsztitűenssel; R2 jelentése karbőxil-, -NR3R4, -NR5CONR5ciklőalkil, NR5alkanőil-, -NR3R4, -NR5CONR5R6, ciklőalkil-alkil-R5N-, (ciklőalkil-alkil)2-N-, -NR5COCF3, -NR5SO2CF3, -NR5(SO2alkil), -NR5SO2NR5R6, -NR5(szűlfőnil-aril)-, -N(aril)-(szűlfőnil-alkil), -OR5, -O-ciklőalkil, -SO2NR5R6,het3 vagy egy vagy, több heterőatőmőt tartalmazó adőtt esetbenszűbsztitűált heterőciklűsős csőpőrt, R3 és R4 egymástól függetlenül hidrőgénatőmőt vagy alkilcsőpőrtőtjelent, és az űtóbbi adőtt esetben szűbsztitűálva van; R5 és R6 egymástól függetlenül hidrőgénatőmőt vagy alkil- vagyciklőalkil-alkilcsőpőrtőt jelent, és az űtóbbi két csőpőrt adőttesetben flűőratőmmal szűbsztitűált lehet; X jelentése alkiléncsőpőrt; X1 jelentése közvetlen kémiai kötés vagy alkiléncsőpőrt; m értéke 0, 1 vagy 2; het3 R2 jelentésében adőtt esetben benzőlgyűrűvel kőndenzált,nitrőgénatőmőn át kapcsőlódó, 1-4 nitrőgén-heterőatőmőt tartalmazó, 5-tagú heterőarilcsőpőrt, amely adőtt esetben szűbsztitűálva lehet egyvagy kettő szűbsztitűenssel. (I) ŕ
HU9903590A 1996-01-05 1996-12-09 3-azetidinylalkylpiperidines or -pyrrolidines as tachykinin antagonists HUP9903590A3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9600235.7A GB9600235D0 (en) 1996-01-05 1996-01-05 Therapeutic agents

Publications (2)

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HUP9903590A2 true HUP9903590A2 (hu) 2000-05-28
HUP9903590A3 HUP9903590A3 (en) 2002-01-28

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ID=10786682

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HU9903590A HUP9903590A3 (en) 1996-01-05 1996-12-09 3-azetidinylalkylpiperidines or -pyrrolidines as tachykinin antagonists

Country Status (38)

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US (1) US6242438B1 (hu)
EP (1) EP0871623B1 (hu)
JP (2) JP3123611B2 (hu)
KR (1) KR100275402B1 (hu)
AP (1) AP709A (hu)
AR (2) AR005339A1 (hu)
AT (1) ATE232526T1 (hu)
AU (1) AU708282B2 (hu)
BG (1) BG102589A (hu)
BR (1) BR9612412A (hu)
CA (1) CA2237189C (hu)
CO (1) CO4750815A1 (hu)
CZ (1) CZ209398A3 (hu)
DE (1) DE69626220T2 (hu)
DK (1) DK0871623T3 (hu)
DZ (1) DZ2155A1 (hu)
ES (1) ES2190486T3 (hu)
GB (1) GB9600235D0 (hu)
HR (1) HRP970006A2 (hu)
HU (1) HUP9903590A3 (hu)
IL (2) IL124309A (hu)
IS (1) IS1876B (hu)
MA (1) MA26417A1 (hu)
NO (1) NO311838B1 (hu)
NZ (1) NZ324712A (hu)
OA (1) OA10863A (hu)
PE (1) PE29798A1 (hu)
PL (1) PL185723B1 (hu)
RU (1) RU2158264C2 (hu)
SI (1) SI0871623T1 (hu)
SK (1) SK89598A3 (hu)
TN (1) TNSN96174A1 (hu)
TR (1) TR199801268T2 (hu)
TW (1) TW472054B (hu)
UY (1) UY24429A1 (hu)
WO (1) WO1997025322A1 (hu)
YU (1) YU71496A (hu)
ZA (1) ZA9747B (hu)

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Publication number Priority date Publication date Assignee Title
GB9714129D0 (en) 1997-07-04 1997-09-10 Pfizer Ltd Azetidines
AU1089599A (en) * 1997-10-15 1999-05-03 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
CA2312770A1 (en) * 1997-12-04 1999-06-10 Takahide Nishi Alicyclic acylated heterocyclic derivatives
GB9821898D0 (en) * 1998-10-08 1998-12-02 Pfizer Ltd Heterocycles
EP1299100B1 (en) * 2000-06-12 2007-07-25 The University Of Rochester Method of treating hot flashes, using tachykinin receptor antagonist
US6642226B2 (en) * 2001-02-06 2003-11-04 Hoffman-La Roche Inc. Substituted phenyl-piperidine methanone compounds
GB0130261D0 (en) * 2001-12-18 2002-02-06 Pfizer Ltd Lactams as tachykinin antagonists
US7674783B2 (en) * 2002-11-22 2010-03-09 Dimera Inc. Estrogen beta receptor agonists to prevent or reduce the severity of cardiovascular disease
AU2003299249B2 (en) * 2002-12-23 2010-05-27 Janssen Pharmaceutica N.V. Substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine derivatives and their use as neurokinin antagonists
TW200508221A (en) 2003-06-13 2005-03-01 Astrazeneca Ab New azetidine compounds
CA2589565A1 (en) * 2004-06-24 2006-01-05 Incyte Corporation Amido compounds and their use as pharmaceuticals
CA2570637A1 (en) 2004-06-24 2006-02-02 Wenqing Yao N-substituted piperidines and their use as pharmaceuticals
MX2007011079A (es) 2005-03-08 2007-10-08 Janssen Pharmaceutica Nv Derivados de diaza-espiro-[4-4]-nonano como antagonistas de la neurocinina (nk1).
AR057828A1 (es) 2005-09-29 2007-12-19 Astrazeneca Ab Compuestos derivados de azetidina, su preparacion y composicion farmaceuutica
US8106208B2 (en) 2006-05-18 2012-01-31 Albireo Ab Benzamide compounds that act as NK receptor antagonists
CN101641099A (zh) 2007-01-24 2010-02-03 葛兰素集团有限公司 包含3,5-二氨基-6-(2,3-二氯苯基)-1,2,4-三嗪或r(-)-2,4-二氨基-5-(2,3-二氯苯基)-6-氟甲基嘧啶和nk1的药物组合物
WO2010071575A1 (en) * 2008-12-16 2010-06-24 Astrazeneca Ab Quaternary piperidine derivatives and uses thereof
SI2421825T1 (sl) * 2009-04-22 2014-04-30 Janssen Pharmaceutica N.V. Azetidinil diamidi kot inhibitorji monoacilglicerol lipaze

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FR2676055B1 (fr) * 1991-05-03 1993-09-03 Sanofi Elf Composes polycycliques amines et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant.
AU678023B2 (en) * 1993-05-06 1997-05-15 Aventis Inc. Substituted pyrrolidin-3-yl-alkyl-piperidines useful as tachykinin antagonists
FR2719311B1 (fr) * 1994-03-18 1998-06-26 Sanofi Sa Composés antagonistes sélectifs du récepteur NK3 humain et leur utilisation comme médicaments et outils de diagnostic.
TW432061B (en) * 1994-08-09 2001-05-01 Pfizer Res & Dev Lactams
GB9601202D0 (en) * 1996-01-22 1996-03-20 Pfizer Ltd Piperidones
GB9812037D0 (en) * 1998-06-04 1998-07-29 Pfizer Ltd Piperidones
GB9821898D0 (en) * 1998-10-08 1998-12-02 Pfizer Ltd Heterocycles

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PL327665A1 (en) 1998-12-21
SI0871623T1 (en) 2003-08-31
OA10863A (en) 2001-09-27
AP709A (en) 1998-12-22
KR19990077027A (ko) 1999-10-25
DZ2155A1 (fr) 2002-10-26
JPH11501667A (ja) 1999-02-09
IS1876B (is) 2003-05-28
IL145324A0 (en) 2002-06-30
AR005338A1 (es) 1999-04-28
ATE232526T1 (de) 2003-02-15
IL124309A0 (en) 1998-12-06
YU71496A (en) 1999-11-22
AU708282B2 (en) 1999-07-29
GB9600235D0 (en) 1996-03-06
HUP9903590A3 (en) 2002-01-28
TW472054B (en) 2002-01-11
ZA9747B (en) 1998-09-30
WO1997025322A1 (en) 1997-07-17
TR199801268T2 (xx) 1998-10-21
AR005339A1 (es) 1999-04-28
SK89598A3 (en) 2000-02-14
CO4750815A1 (es) 1999-03-31
UY24429A1 (es) 2001-08-27
AP9600901A0 (en) 1997-01-31
HRP970006A2 (en) 1998-06-30
NZ324712A (en) 1999-05-28
NO982651L (no) 1998-06-09
BG102589A (en) 1999-09-30
PL185723B1 (pl) 2003-07-31
JP3123611B2 (ja) 2001-01-15
PE29798A1 (es) 1998-06-11
RU2158264C2 (ru) 2000-10-27
NO311838B1 (no) 2002-02-04
JP2000344741A (ja) 2000-12-12
JP3254205B2 (ja) 2002-02-04
BR9612412A (pt) 1999-07-13
ES2190486T3 (es) 2003-08-01
DE69626220T2 (de) 2003-08-28
KR100275402B1 (ko) 2000-12-15
DE69626220D1 (de) 2003-03-20
NO982651D0 (no) 1998-06-09
MA26417A1 (fr) 2004-12-20
AU1195097A (en) 1997-08-01
IS4760A (is) 1998-05-28
EP0871623B1 (en) 2003-02-12
US6242438B1 (en) 2001-06-05
TNSN96174A1 (fr) 2005-03-15
IL124309A (en) 2002-11-10
DK0871623T3 (da) 2003-03-31
EP0871623A1 (en) 1998-10-21
CA2237189C (en) 2002-09-03
CA2237189A1 (en) 1997-07-17
CZ209398A3 (cs) 1999-04-14

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