CN106103421B - Gpr6的吡嗪调节剂 - Google Patents

Gpr6的吡嗪调节剂 Download PDF

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Publication number
CN106103421B
CN106103421B CN201580013589.1A CN201580013589A CN106103421B CN 106103421 B CN106103421 B CN 106103421B CN 201580013589 A CN201580013589 A CN 201580013589A CN 106103421 B CN106103421 B CN 106103421B
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pyrazine
piperidin
isopropylamino
base
cyano
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CN106103421A (zh
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M·E·阿达姆斯
J·W·布朗
S·希驰库克
菊地正太
B·兰姆
H·蒙内斯切因
H·理查德
孙会凯
M·霍普金森
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Takeda Pharmaceutical Co Ltd
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Takeda Chemical Industries Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or 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
    • C07D401/02—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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
CN201580013589.1A 2014-02-14 2015-02-13 Gpr6的吡嗪调节剂 Active CN106103421B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461940294P 2014-02-14 2014-02-14
US61/940,294 2014-02-14
PCT/US2015/015841 WO2015123533A1 (en) 2014-02-14 2015-02-13 Pyrazines modulators of gpr6

Publications (2)

Publication Number Publication Date
CN106103421A CN106103421A (zh) 2016-11-09
CN106103421B true CN106103421B (zh) 2019-04-09

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US (2) US10000468B2 (https=)
EP (1) EP3105216B1 (https=)
JP (1) JP6484640B2 (https=)
KR (1) KR20160122215A (https=)
CN (1) CN106103421B (https=)
AU (1) AU2015218402B2 (https=)
BR (1) BR112016018418A2 (https=)
CA (1) CA2939382A1 (https=)
CL (1) CL2016002043A1 (https=)
CR (1) CR20160428A (https=)
DO (1) DOP2016000211A (https=)
EA (1) EA033861B1 (https=)
EC (1) ECSP16074207A (https=)
ES (1) ES2702205T3 (https=)
GE (2) GEP20186893B (https=)
IL (1) IL247140B (https=)
MA (1) MA39337B1 (https=)
MX (1) MX369857B (https=)
MY (1) MY184366A (https=)
PE (1) PE20170245A1 (https=)
PH (1) PH12016501613B1 (https=)
UA (1) UA117779C2 (https=)
WO (1) WO2015123533A1 (https=)
ZA (1) ZA201606077B (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20160122215A (ko) * 2014-02-14 2016-10-21 다케다 야쿠힌 고교 가부시키가이샤 Gpr6의 피라진 조절제
EA202092441A1 (ru) 2016-06-07 2021-05-21 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
KR20240026521A (ko) 2017-03-23 2024-02-28 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
MX390512B (es) * 2017-03-26 2025-03-20 Takeda Pharmaceuticals Co Carboxamidas heteroaromáticas sustituidas con piperidinilo y piperazinilo como moduladores de gpr6.
JOP20180057A1 (ar) * 2017-06-15 2019-01-30 Takeda Pharmaceuticals Co مركبات رابع هيدروبيريدو بيرازين والتي تعمل كمعدلات gpr6
CN112839935A (zh) 2018-09-26 2021-05-25 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
CN115996908B (zh) * 2020-04-30 2026-04-24 俄勒冈健康科学大学 Gpr39蛋白的拮抗剂

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CN1364167A (zh) * 1999-02-26 2002-08-14 阿瑞那制药公司 G蛋白偶联受体6的小分子调节剂
WO2004054617A1 (ja) * 2002-12-13 2004-07-01 Kyowa Hakko Kogyo Co., Ltd. 中枢疾患の予防および／または治療剤
CN1512988A (zh) * 2001-06-01 2004-07-14 - 用作谷氨酸受体的嘧啶、三嗪和吡嗪衍生物
CN1933838A (zh) * 2004-02-12 2007-03-21 默克公司 作为代谢型谷氨酸受体－5调节剂的联吡啶酰胺

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KR20160122215A (ko) * 2014-02-14 2016-10-21 다케다 야쿠힌 고교 가부시키가이샤 Gpr6의 피라진 조절제

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US4159331A (en) * 1978-05-05 1979-06-26 The Upjohn Company Antihypertensive 4-aminoquinolines
CN1364167A (zh) * 1999-02-26 2002-08-14 阿瑞那制药公司 G蛋白偶联受体6的小分子调节剂
CN1512988A (zh) * 2001-06-01 2004-07-14 - 用作谷氨酸受体的嘧啶、三嗪和吡嗪衍生物
WO2004054617A1 (ja) * 2002-12-13 2004-07-01 Kyowa Hakko Kogyo Co., Ltd. 中枢疾患の予防および／または治療剤
CN1933838A (zh) * 2004-02-12 2007-03-21 默克公司 作为代谢型谷氨酸受体－5调节剂的联吡啶酰胺

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US20170174659A1 (en) 2017-06-22
GEP20186893B (en) 2018-09-10
PH12016501613B1 (en) 2021-10-01
IL247140A0 (en) 2016-09-29
IL247140B (en) 2020-02-27
CL2016002043A1 (es) 2017-02-17
EP3105216A1 (en) 2016-12-21
DOP2016000211A (es) 2016-10-16
AU2015218402A1 (en) 2016-09-15
EA201691632A1 (ru) 2017-02-28
ZA201606077B (en) 2018-11-28
US10000468B2 (en) 2018-06-19
PE20170245A1 (es) 2017-03-30
EP3105216B1 (en) 2018-10-10
MX2016010529A (es) 2016-10-31
ES2702205T3 (es) 2019-02-27
GEAP201814266A (en) 2018-05-10
MY184366A (en) 2021-04-01
MA39337A1 (fr) 2017-10-31
PH12016501613A1 (en) 2017-02-06
ECSP16074207A (es) 2017-09-29
US20180258073A1 (en) 2018-09-13
UA117779C2 (uk) 2018-09-25
WO2015123533A1 (en) 2015-08-20
EA033861B1 (ru) 2019-12-03
JP2017509601A (ja) 2017-04-06
CR20160428A (es) 2017-04-04
CN106103421A (zh) 2016-11-09
US10273225B2 (en) 2019-04-30
KR20160122215A (ko) 2016-10-21
MX369857B (es) 2019-11-25
MA39337B1 (fr) 2019-11-29
AU2015218402B2 (en) 2019-07-11
JP6484640B2 (ja) 2019-03-13
CA2939382A1 (en) 2015-08-20
BR112016018418A2 (pt) 2017-08-08

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