EA033861B1 - Пиразины в качестве модуляторов gpr6 - Google Patents

Пиразины в качестве модуляторов gpr6 Download PDF

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Publication number
EA033861B1
EA033861B1 EA201691632A EA201691632A EA033861B1 EA 033861 B1 EA033861 B1 EA 033861B1 EA 201691632 A EA201691632 A EA 201691632A EA 201691632 A EA201691632 A EA 201691632A EA 033861 B1 EA033861 B1 EA 033861B1
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EA
Eurasian Patent Office
Prior art keywords
piperidin
isopropylamino
pyrazine
chloro
cyano
Prior art date
Application number
EA201691632A
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English (en)
Russian (ru)
Other versions
EA201691632A1 (ru
Inventor
Марк Э. Адамс
Джейсон В. Браун
Стефен Хичкок
Мария Хопкинс
Шота Кикучи
Бетти Лэм
Холгер Моненскейн
Холли Рейчард
Хойкай Сунь
Original Assignee
Такеда Фармасьютикал Компани Лимитед
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Publication of EA201691632A1 publication Critical patent/EA201691632A1/ru
Publication of EA033861B1 publication Critical patent/EA033861B1/ru

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    • 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
    • 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

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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)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EA201691632A 2014-02-14 2015-02-13 Пиразины в качестве модуляторов gpr6 EA033861B1 (ru)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
EA201691632A1 EA201691632A1 (ru) 2017-02-28
EA033861B1 true EA033861B1 (ru) 2019-12-03

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EA201691632A EA033861B1 (ru) 2014-02-14 2015-02-13 Пиразины в качестве модуляторов gpr6

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US (2) US10000468B2 (enExample)
EP (1) EP3105216B1 (enExample)
JP (1) JP6484640B2 (enExample)
KR (1) KR20160122215A (enExample)
CN (1) CN106103421B (enExample)
AU (1) AU2015218402B2 (enExample)
BR (1) BR112016018418A2 (enExample)
CA (1) CA2939382A1 (enExample)
CL (1) CL2016002043A1 (enExample)
CR (1) CR20160428A (enExample)
DO (1) DOP2016000211A (enExample)
EA (1) EA033861B1 (enExample)
EC (1) ECSP16074207A (enExample)
ES (1) ES2702205T3 (enExample)
GE (2) GEAP201814266A (enExample)
IL (1) IL247140B (enExample)
MA (1) MA39337B1 (enExample)
MX (1) MX369857B (enExample)
MY (1) MY184366A (enExample)
PE (1) PE20170245A1 (enExample)
PH (1) PH12016501613B1 (enExample)
UA (1) UA117779C2 (enExample)
WO (1) WO2015123533A1 (enExample)
ZA (1) ZA201606077B (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA117779C2 (uk) * 2014-02-14 2018-09-25 Такеда Фармасьютікал Компані Лімітед Піразини як модулятори gpr6
KR102218333B1 (ko) 2016-06-07 2021-02-22 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
SG11201908820VA (en) 2017-03-23 2019-10-30 Jacobio Pharmaceuticals Co Ltd Novel heterocyclic derivatives useful as shp2 inhibitors
CN110520127B (zh) * 2017-03-26 2023-05-16 武田药品工业株式会社 作为gpr6的调节剂的经哌啶基取代的杂芳族羧酰胺和经哌嗪基取代的杂芳族羧酰胺
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
WO2021222858A1 (en) * 2020-04-30 2021-11-04 Oregon Health & Science University Antagonists of gpr39 protein
WO2026032256A1 (zh) * 2024-08-06 2026-02-12 上海齐鲁制药研究中心有限公司 单环类gpr6反向激动剂及其用途

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WO2002098864A1 (en) * 2001-06-01 2002-12-12 F. Hoffmann-La Roche Ag Pyrimidine, triazine and pyrazine derivatives as glutamate receptors
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
WO2005079802A1 (en) * 2004-02-12 2005-09-01 Merck & Co., Inc. Bipyridyl amides as modulators of metabotropic glutamate receptor-5
US20060199828A1 (en) * 2005-03-04 2006-09-07 Georg Jaeschke Pyrazine-2-carboxyamide derivatives
WO2014028479A1 (en) * 2012-08-13 2014-02-20 Envoy Therapeutics, Inc. Quinoxaline derivatives as gpr6 modulators

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KR20060037409A (ko) 2003-07-30 2006-05-03 제논 파마슈티칼스 인크. 피페라진 유도체 및 그의 치료제로서의 용도
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4159331A (en) * 1978-05-05 1979-06-26 The Upjohn Company Antihypertensive 4-aminoquinolines
WO2002098864A1 (en) * 2001-06-01 2002-12-12 F. Hoffmann-La Roche Ag Pyrimidine, triazine and pyrazine derivatives as glutamate receptors
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
WO2005079802A1 (en) * 2004-02-12 2005-09-01 Merck & Co., Inc. Bipyridyl amides as modulators of metabotropic glutamate receptor-5
US20060199828A1 (en) * 2005-03-04 2006-09-07 Georg Jaeschke Pyrazine-2-carboxyamide derivatives
WO2014028479A1 (en) * 2012-08-13 2014-02-20 Envoy Therapeutics, Inc. Quinoxaline derivatives as gpr6 modulators

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LACIVITA ENZA; LEOPOLDO MARCELLO: "SELECTIVE AGENTS FOR SEROTONIN(2C)(5-HT2C) RECEPTOR", CURRENT TOPICS IN MEDICINAL CHEMISTRY, BENTHAM SCIENCE PUBLISHERS LTD.HILVERSUM, NL, vol. 6, no. 18, 1 January 2006 (2006-01-01), NL, pages 1927 - 1970, XP009085750, ISSN: 1568-0266, DOI: 10.2174/156802606778522168 *

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CR20160428A (es) 2017-04-04
MX2016010529A (es) 2016-10-31
GEAP201814266A (en) 2018-05-10
MA39337A1 (fr) 2017-10-31
AU2015218402A1 (en) 2016-09-15
ES2702205T3 (es) 2019-02-27
JP2017509601A (ja) 2017-04-06
CL2016002043A1 (es) 2017-02-17
IL247140B (en) 2020-02-27
ZA201606077B (en) 2018-11-28
ECSP16074207A (es) 2017-09-29
AU2015218402B2 (en) 2019-07-11
PE20170245A1 (es) 2017-03-30
MY184366A (en) 2021-04-01
US20170174659A1 (en) 2017-06-22
JP6484640B2 (ja) 2019-03-13
MX369857B (es) 2019-11-25
CN106103421A (zh) 2016-11-09
US20180258073A1 (en) 2018-09-13
PH12016501613A1 (en) 2017-02-06
US10000468B2 (en) 2018-06-19
BR112016018418A2 (pt) 2017-08-08
UA117779C2 (uk) 2018-09-25
KR20160122215A (ko) 2016-10-21
CN106103421B (zh) 2019-04-09
EP3105216A1 (en) 2016-12-21
MA39337B1 (fr) 2019-11-29
EA201691632A1 (ru) 2017-02-28
GEP20186893B (en) 2018-09-10
WO2015123533A1 (en) 2015-08-20
PH12016501613B1 (en) 2021-10-01
DOP2016000211A (es) 2016-10-16
CA2939382A1 (en) 2015-08-20
EP3105216B1 (en) 2018-10-10
IL247140A0 (en) 2016-09-29
US10273225B2 (en) 2019-04-30

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