EA016056B1 - Тиофенпиразолопиримидиновые соединения - Google Patents

Тиофенпиразолопиримидиновые соединения Download PDF

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Publication number
EA016056B1
EA016056B1 EA200970302A EA200970302A EA016056B1 EA 016056 B1 EA016056 B1 EA 016056B1 EA 200970302 A EA200970302 A EA 200970302A EA 200970302 A EA200970302 A EA 200970302A EA 016056 B1 EA016056 B1 EA 016056B1
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EA
Eurasian Patent Office
Prior art keywords
mmol
hexane
reaction
formula
added
Prior art date
Application number
EA200970302A
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English (en)
Russian (ru)
Other versions
EA200970302A1 (ru
Inventor
Чжаогэнь Чэнь
Чафик Амдоучи Амдоучи
Эрик Джеймс Хембр
Филип Артур Хипскинд
Шаоцзюань Цзя
Джеймс Ли Тот
Original Assignee
Эли Лилли Энд Компани
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Application filed by Эли Лилли Энд Компани filed Critical Эли Лилли Энд Компани
Publication of EA200970302A1 publication Critical patent/EA200970302A1/ru
Publication of EA016056B1 publication Critical patent/EA016056B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
EA200970302A 2006-09-20 2007-09-13 Тиофенпиразолопиримидиновые соединения EA016056B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US82627306P 2006-09-20 2006-09-20
PCT/US2007/078352 WO2008036541A1 (en) 2006-09-20 2007-09-13 Thiophene pyrazolopyrimidine compounds

Publications (2)

Publication Number Publication Date
EA200970302A1 EA200970302A1 (ru) 2009-10-30
EA016056B1 true EA016056B1 (ru) 2012-01-30

Family

ID=38988344

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200970302A EA016056B1 (ru) 2006-09-20 2007-09-13 Тиофенпиразолопиримидиновые соединения

Country Status (12)

Country Link
US (1) US8110580B2 (cg-RX-API-DMAC7.html)
EP (1) EP2076515B1 (cg-RX-API-DMAC7.html)
JP (1) JP5184536B2 (cg-RX-API-DMAC7.html)
KR (1) KR101088196B1 (cg-RX-API-DMAC7.html)
CN (1) CN101516886B (cg-RX-API-DMAC7.html)
AU (1) AU2007297481B2 (cg-RX-API-DMAC7.html)
BR (1) BRPI0717070A2 (cg-RX-API-DMAC7.html)
CA (1) CA2662000C (cg-RX-API-DMAC7.html)
EA (1) EA016056B1 (cg-RX-API-DMAC7.html)
ES (1) ES2428543T3 (cg-RX-API-DMAC7.html)
MX (1) MX2009003098A (cg-RX-API-DMAC7.html)
WO (1) WO2008036541A1 (cg-RX-API-DMAC7.html)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US9029411B2 (en) 2008-01-25 2015-05-12 Millennium Pharmaceuticals, Inc. Thiophenes and uses thereof
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
CA2750935A1 (en) 2009-01-30 2010-08-12 Millennium Pharmaceuticals, Inc. Heteroaryls and their use as pi3k inhibitors
WO2012021611A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
EP2603214A4 (en) 2010-08-11 2013-12-18 Millennium Pharm Inc HETEROARYLE AND USES THEREOF
EP2603216A4 (en) 2010-08-11 2013-12-18 Millennium Pharm Inc HETEROARYLE AND USES THEREOF
EP2627181A4 (en) 2010-10-13 2014-03-19 Millennium Pharm Inc HETEROARYLE AND USES THEREOF
ES2606043T3 (es) 2011-07-05 2017-03-17 Lupin Limited Derivados de biarilo como moduladores de nAChR
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
JP6585625B2 (ja) 2014-01-21 2019-10-02 ニューロクライン バイオサイエンシーズ,インコーポレイテッド 先天性副腎皮質過形成の処置のためのcrf1レセプターアンタゴニスト
JP6364967B2 (ja) * 2014-05-30 2018-08-01 東ソー株式会社 ジチエノベンゾジチオフェンの製造方法
EP3238676B1 (en) 2016-04-29 2019-01-02 The Procter and Gamble Company Absorbent core with profiled distribution of absorbent material
CN110997667A (zh) * 2017-08-14 2020-04-10 云杉生物科学公司 促肾上腺皮质激素释放因子受体拮抗剂
EP3628005A4 (en) 2017-08-14 2021-01-20 Spruce Biosciences, Inc. Corticotropin releasing factor receptor antagonists
TW202446384A (zh) 2018-12-07 2024-12-01 美商紐羅克里生物科學有限公司 用於治療先天性腎上腺增生之crf1受體拮抗劑、醫藥配方及其固體形式
CN114502162B (zh) 2019-09-27 2025-03-28 纽罗克里生物科学有限公司 Crf受体拮抗剂及使用方法
US20230065034A1 (en) * 2019-12-04 2023-03-02 Neurocrine Biosciences, Inc. Crf receptor antagonists and methods of use
CN118948857A (zh) 2020-08-12 2024-11-15 云杉生物科学公司 用于治疗多囊卵巢综合征的方法和组合物
US11708372B2 (en) 2021-11-19 2023-07-25 Spruce Biosciences, Inc. Crystalline composition of tildacerfont and methods of use and preparation thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997029109A1 (en) * 1996-02-07 1997-08-14 Janssen Pharmaceutica N.V. Pyrazolopyrimidines as crf receptor antagonists
WO2001023388A2 (en) * 1999-09-30 2001-04-05 Neurogen Corporation AMINO SUBSTITUTED PYRAZOLO[1,5,-a]-1,5-PYRIMIDINES AND PYRAZOLO[1,5-a]-1,3,5-TRIAZINES
WO2005063755A1 (en) * 2003-12-22 2005-07-14 Sb Pharmco Puerto Rico Inc Crf receptor antagonists and methods relating thereto

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KR0173172B1 (ko) 1992-12-17 1999-02-01 알렌 제이. 스피겔 Crf 길항제로서의 피롤로피리미딘
DK0915880T3 (da) 1996-07-24 2008-02-11 Bristol Myers Squibb Pharma Co Azolotriaziner og pyrimidiner
JP3621706B2 (ja) 1996-08-28 2005-02-16 ファイザー・インク 置換された6,5―ヘテロ―二環式誘導体
CN101142217B (zh) * 2005-03-21 2010-12-08 伊莱利利公司 咪唑并哒嗪化合物

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997029109A1 (en) * 1996-02-07 1997-08-14 Janssen Pharmaceutica N.V. Pyrazolopyrimidines as crf receptor antagonists
WO2001023388A2 (en) * 1999-09-30 2001-04-05 Neurogen Corporation AMINO SUBSTITUTED PYRAZOLO[1,5,-a]-1,5-PYRIMIDINES AND PYRAZOLO[1,5-a]-1,3,5-TRIAZINES
WO2005063755A1 (en) * 2003-12-22 2005-07-14 Sb Pharmco Puerto Rico Inc Crf receptor antagonists and methods relating thereto

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MAJO V.J. ET AL.: "Facile Palladium-Catalyzed Synthesis of 3-Arylpyrazolo-[1,5a]pyrimidines" ADVANCED SYNTHESIS AND CATALYSIS, WILEY, WEINHEIM, DE, vol. 345, no. 5, May 2003 (2003-05), pages 620-624, XP002468036 ISSN: 1615-4169 page 1, paragraph 2 page 622; table 2; compound 6E *

Also Published As

Publication number Publication date
AU2007297481B2 (en) 2012-03-08
US8110580B2 (en) 2012-02-07
KR20090053921A (ko) 2009-05-28
JP2010504343A (ja) 2010-02-12
EA200970302A1 (ru) 2009-10-30
CN101516886B (zh) 2012-02-29
KR101088196B1 (ko) 2011-11-30
MX2009003098A (es) 2009-04-01
EP2076515B1 (en) 2013-07-17
AU2007297481A1 (en) 2008-03-27
JP5184536B2 (ja) 2013-04-17
ES2428543T3 (es) 2013-11-08
WO2008036541A1 (en) 2008-03-27
BRPI0717070A2 (pt) 2013-09-24
EP2076515A1 (en) 2009-07-08
US20100022560A1 (en) 2010-01-28
CA2662000C (en) 2013-01-08
CN101516886A (zh) 2009-08-26
CA2662000A1 (en) 2008-03-27

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM BY KZ KG MD TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AZ TJ RU