EA019206B1 - Пиразиновые соединения в качестве ингибиторов фосфодиэстеразы 10 - Google Patents

Пиразиновые соединения в качестве ингибиторов фосфодиэстеразы 10 Download PDF

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Publication number
EA019206B1
EA019206B1 EA201100748A EA201100748A EA019206B1 EA 019206 B1 EA019206 B1 EA 019206B1 EA 201100748 A EA201100748 A EA 201100748A EA 201100748 A EA201100748 A EA 201100748A EA 019206 B1 EA019206 B1 EA 019206B1
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EA
Eurasian Patent Office
Prior art keywords
benzo
pyrazin
phenyl
yloxy
imidazol
Prior art date
Application number
EA201100748A
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English (en)
Russian (ru)
Other versions
EA201100748A1 (ru
Inventor
Дженнифер Р. Аллен
Мэтью П. Борбо
Нинг Чен
Эсса Ху
Роксан Кунц
Шэннон Румфельт
Original Assignee
Амген Инк.
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Publication date
Application filed by Амген Инк. filed Critical Амген Инк.
Publication of EA201100748A1 publication Critical patent/EA201100748A1/ru
Publication of EA019206B1 publication Critical patent/EA019206B1/ru

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    • 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
    • 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
    • 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
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Addiction (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EA201100748A 2008-11-14 2009-11-16 Пиразиновые соединения в качестве ингибиторов фосфодиэстеразы 10 EA019206B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11456708P 2008-11-14 2008-11-14
US16621209P 2009-04-02 2009-04-02
PCT/US2009/064637 WO2010057121A1 (en) 2008-11-14 2009-11-16 Pyrazine compounds as phosphodiesterase 10 inhibitors

Publications (2)

Publication Number Publication Date
EA201100748A1 EA201100748A1 (ru) 2011-10-31
EA019206B1 true EA019206B1 (ru) 2014-01-30

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201100748A EA019206B1 (ru) 2008-11-14 2009-11-16 Пиразиновые соединения в качестве ингибиторов фосфодиэстеразы 10

Country Status (30)

Country Link
US (4) US8053438B2 (enExample)
EP (1) EP2364308B1 (enExample)
JP (1) JP5746972B2 (enExample)
KR (1) KR20110083746A (enExample)
CN (1) CN102300860B (enExample)
AR (1) AR074358A1 (enExample)
AU (1) AU2009313768B2 (enExample)
BR (1) BRPI0922095A2 (enExample)
CA (1) CA2742993C (enExample)
CL (1) CL2011001094A1 (enExample)
CO (1) CO6382157A2 (enExample)
CR (1) CR20110326A (enExample)
CY (1) CY1113680T1 (enExample)
DK (1) DK2364308T3 (enExample)
EA (1) EA019206B1 (enExample)
ES (1) ES2397218T3 (enExample)
HR (1) HRP20130054T1 (enExample)
IL (1) IL212687A0 (enExample)
MA (1) MA32889B1 (enExample)
MX (1) MX2011005100A (enExample)
NZ (1) NZ592508A (enExample)
PE (1) PE20110581A1 (enExample)
PL (1) PL2364308T3 (enExample)
PT (1) PT2364308E (enExample)
RS (1) RS52598B (enExample)
SI (1) SI2364308T1 (enExample)
SM (1) SMT201200061B (enExample)
TN (1) TN2011000221A1 (enExample)
TW (1) TWI396689B (enExample)
WO (1) WO2010057121A1 (enExample)

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CA2746307C (en) * 2008-12-17 2013-11-19 Amgen Inc. Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors
BRPI1008498B8 (pt) 2009-02-05 2021-05-25 Takeda Pharmaceuticals Co compostos de piridazinona úteis como inibidores da fosfodiesterase 10a, composição farmacêutica, e, uso de um composto
JP5739415B2 (ja) 2009-05-12 2015-06-24 ブリストル−マイヤーズ スクウィブ カンパニー (S)−7−([1,2,4]トリアゾロ[1,5−a]ピリジン−6−イル)−4−(3,4−ジクロロフェニル)−1,2,3,4−テトラヒドロイソキノリンの結晶形態およびその使用
CN102595902B (zh) * 2009-05-12 2015-04-29 阿尔巴尼分子研究公司 7-([1,2,4]三唑并[1,5-a]吡啶-6-基)-4-(3,4-二氯苯基)-1,2,3,4-四氢异喹啉及其用途
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JP6106603B2 (ja) 2011-01-11 2017-04-05 スノビオン プハルマセウトイカルス インコーポレイテッド ヘテロアリール化合物及びその使用方法
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US9657015B2 (en) 2014-07-31 2017-05-23 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
CN104649882A (zh) * 2015-02-11 2015-05-27 南通恒盛精细化工有限公司 一种磷酸二酯酶抑制剂的中间体制备工艺
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WO2017047602A1 (ja) * 2015-09-18 2017-03-23 科研製薬株式会社 ビアリール誘導体及びそれを含有する医薬
CN112979661B (zh) * 2018-01-19 2022-05-17 苏州信诺维医药科技股份有限公司 杂环化合物、制备方法及其在医药上的应用
CN109020977B (zh) * 2018-10-26 2020-11-13 安庆奇创药业有限公司 一种Acalabrutinib的制备方法
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CN113929598A (zh) * 2021-11-24 2022-01-14 上海吉奉生物科技有限公司 一种(s)-2-叔丁氧羰基氨基-3-(4,4-二氟环己基)丙酸的合成方法
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Publication number Priority date Publication date Assignee Title
RU2632900C2 (ru) * 2010-11-19 2017-10-11 Лиганд Фармасьютикалс Инкорпорейтед Гетероциклические амины и их применение

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WO2010057121A1 (en) 2010-05-20
AR074358A1 (es) 2011-01-12
RS52598B (sr) 2013-04-30
EP2364308B1 (en) 2012-10-24
CN102300860A (zh) 2011-12-28
TW201030006A (en) 2010-08-16
US8053438B2 (en) 2011-11-08
HK1161251A1 (en) 2012-08-24
HRP20130054T1 (hr) 2013-02-28
TWI396689B (zh) 2013-05-21
SI2364308T1 (sl) 2013-01-31
US8247418B2 (en) 2012-08-21
CO6382157A2 (es) 2012-02-15
EA201100748A1 (ru) 2011-10-31
PT2364308E (pt) 2013-01-08
CA2742993C (en) 2015-01-20
IL212687A0 (en) 2011-07-31
US8329700B2 (en) 2012-12-11
PL2364308T3 (pl) 2013-03-29
PE20110581A1 (es) 2011-09-03
US20120277209A1 (en) 2012-11-01
CN102300860B (zh) 2014-08-27
US20110160202A1 (en) 2011-06-30
JP5746972B2 (ja) 2015-07-08
NZ592508A (en) 2013-04-26
AU2009313768B2 (en) 2013-01-10
TN2011000221A1 (en) 2012-12-17
DK2364308T3 (da) 2013-02-04
US20110160182A1 (en) 2011-06-30
MX2011005100A (es) 2011-05-30
KR20110083746A (ko) 2011-07-20
BRPI0922095A2 (pt) 2019-09-24
AU2009313768A1 (en) 2010-05-20
JP2012508776A (ja) 2012-04-12
MA32889B1 (fr) 2011-12-01
CR20110326A (es) 2011-07-28
CY1113680T1 (el) 2016-06-22
CL2011001094A1 (es) 2011-11-11
US20100137278A1 (en) 2010-06-03
EP2364308A1 (en) 2011-09-14
CA2742993A1 (en) 2010-05-20
ES2397218T3 (es) 2013-03-05
SMT201200061B (it) 2013-01-14

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