TWI799399B - 吡啶并〔3,4-d〕嘧啶衍生物及其藥學上所容許之鹽 - Google Patents

吡啶并〔3,4-d〕嘧啶衍生物及其藥學上所容許之鹽 Download PDF

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TWI799399B
TWI799399B TW106141152A TW106141152A TWI799399B TW I799399 B TWI799399 B TW I799399B TW 106141152 A TW106141152 A TW 106141152A TW 106141152 A TW106141152 A TW 106141152A TW I799399 B TWI799399 B TW I799399B
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Taiwan
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pyrido
pharmaceutically acceptable
acceptable salts
pyrimidine derivatives
pyrimidine
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TW106141152A
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English (en)
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TW201831476A (zh
Inventor
水野剛志
嶋田朋嘉
鵜木元
丸山明伸
佐佐木浩介
横坂卓也
髙橋広
堀江恭平
酒井由里
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日商帝人製藥股份有限公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • 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]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0803Compounds with Si-C or Si-Si linkages
    • C07F7/081Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
TW106141152A 2016-11-28 2017-11-27 吡啶并〔3,4-d〕嘧啶衍生物及其藥學上所容許之鹽 TWI799399B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2016-229969 2016-11-28
JP2016229969 2016-11-28

Publications (2)

Publication Number Publication Date
TW201831476A TW201831476A (zh) 2018-09-01
TWI799399B true TWI799399B (zh) 2023-04-21

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ID=62194988

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Country Status (28)

Country Link
US (1) US11084814B2 (zh)
EP (1) EP3546458B1 (zh)
JP (1) JP6785876B2 (zh)
KR (1) KR102290815B1 (zh)
CN (1) CN110036012B (zh)
AR (1) AR110238A1 (zh)
AU (1) AU2017364807B2 (zh)
BR (1) BR112019010674A2 (zh)
CA (1) CA3043561A1 (zh)
CL (1) CL2019001419A1 (zh)
CO (1) CO2019005514A2 (zh)
CY (1) CY1123850T1 (zh)
DK (1) DK3546458T3 (zh)
ES (1) ES2852123T3 (zh)
HR (1) HRP20210285T1 (zh)
HU (1) HUE053220T2 (zh)
IL (1) IL266312B (zh)
LT (1) LT3546458T (zh)
MX (1) MX2019005803A (zh)
MY (1) MY196497A (zh)
PH (1) PH12019501171A1 (zh)
PL (1) PL3546458T3 (zh)
PT (1) PT3546458T (zh)
SA (1) SA519401827B1 (zh)
SI (1) SI3546458T1 (zh)
TW (1) TWI799399B (zh)
WO (1) WO2018097297A1 (zh)
ZA (1) ZA201902893B (zh)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115942937A (zh) * 2020-08-17 2023-04-07 南京明德新药研发有限公司 嘧啶并环类化合物
CN113636973B (zh) * 2021-09-07 2023-04-07 山东铂源药业股份有限公司 一种4-(6-氨基吡啶-3-基)哌嗪-1-羧酸叔丁酯的工业化制备方法
WO2023155841A1 (zh) * 2022-02-16 2023-08-24 南京明德新药研发有限公司 嘧啶并环类化合物的盐型、晶型
WO2024020419A1 (en) * 2022-07-18 2024-01-25 Iambic Therapeutics, Inc. Aza-quinazoline compounds and methods of use

Citations (2)

* Cited by examiner, † Cited by third party
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WO2014037750A1 (en) * 2012-09-07 2014-03-13 Cancer Research Technology Limited Inhibitor compounds
WO2015128676A1 (en) * 2014-02-28 2015-09-03 Cancer Research Technology Limited N2-phenyl-pyrido[3,4-d]pyrimidine-2,8-diamine derivatives and their use as mps1 inhibitors

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IL162721A0 (en) 2002-01-22 2005-11-20 Warner Lambert Co 2-(Pyridin-2-ylamino)-pyridoÄ2,3-dÜpyrimidin-7-ones
DK2331547T3 (da) 2008-08-22 2014-11-03 Novartis Ag Pyrrolopyrimidinforbindelser som CDK-inhibitorer
JP2012504646A (ja) 2008-10-01 2012-02-23 ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル 選択的サイクリン依存性キナーゼ4/6阻害剤を用いた化学療法化合物に対する造血系の防護
PA8852901A1 (es) 2008-12-22 2010-07-27 Lilly Co Eli Inhibidores de proteina cinasa
WO2012031004A1 (en) 2010-09-01 2012-03-08 Gilead Connecticut, Inc. Pyridinones/pyrazinones, method of making, and method of use thereof
CN104470921B (zh) * 2013-05-17 2017-05-03 上海恒瑞医药有限公司 吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用
CN105682661B (zh) * 2013-08-23 2020-03-27 润新生物公司 某些化学实体、组合物和方法
NZ718820A (en) * 2013-09-30 2017-10-27 Certain Teed Corp Stain repellent and voc eliminating coatings and use thereof
US9828373B2 (en) * 2014-07-26 2017-11-28 Sunshine Lake Pharma Co., Ltd. 2-amino-pyrido[2,3-D]pyrimidin-7(8H)-one derivatives as CDK inhibitors and uses thereof
AR104789A1 (es) 2015-05-29 2017-08-16 Teijin Pharma Ltd Derivado de pirido[3,4-d]pirimidina y sal farmacéuticamente aceptable de éste

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014037750A1 (en) * 2012-09-07 2014-03-13 Cancer Research Technology Limited Inhibitor compounds
WO2015128676A1 (en) * 2014-02-28 2015-09-03 Cancer Research Technology Limited N2-phenyl-pyrido[3,4-d]pyrimidine-2,8-diamine derivatives and their use as mps1 inhibitors

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Publication number Publication date
CA3043561A1 (en) 2018-05-31
MY196497A (en) 2023-04-17
HUE053220T2 (hu) 2021-06-28
CN110036012B (zh) 2022-05-10
AU2017364807B2 (en) 2021-05-13
PL3546458T3 (pl) 2021-06-14
LT3546458T (lt) 2021-05-10
TW201831476A (zh) 2018-09-01
PT3546458T (pt) 2021-02-25
JPWO2018097297A1 (ja) 2019-06-24
BR112019010674A2 (pt) 2019-10-01
AU2017364807A1 (en) 2019-05-16
AR110238A1 (es) 2019-03-13
ZA201902893B (en) 2020-01-29
ES2852123T3 (es) 2021-09-13
DK3546458T3 (da) 2021-02-22
RU2019116137A3 (zh) 2021-08-13
EP3546458A4 (en) 2019-10-09
US20190367510A1 (en) 2019-12-05
CL2019001419A1 (es) 2019-08-30
HRP20210285T1 (hr) 2021-04-02
MX2019005803A (es) 2019-09-10
KR102290815B1 (ko) 2021-08-18
IL266312A (en) 2019-06-30
CY1123850T1 (el) 2022-05-27
RU2019116137A (ru) 2020-11-27
KR20190066631A (ko) 2019-06-13
SA519401827B1 (ar) 2022-07-28
WO2018097297A1 (ja) 2018-05-31
EP3546458A1 (en) 2019-10-02
CO2019005514A2 (es) 2019-07-31
SI3546458T1 (sl) 2021-03-31
JP6785876B2 (ja) 2020-11-18
EP3546458B1 (en) 2021-01-06
PH12019501171A1 (en) 2021-02-08
US11084814B2 (en) 2021-08-10
CN110036012A (zh) 2019-07-19
IL266312B (en) 2021-08-31

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