JP5184536B2 - チオフェンピラゾロピリミジン化合物 - Google Patents

チオフェンピラゾロピリミジン化合物 Download PDF

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JP5184536B2
JP5184536B2 JP2009529307A JP2009529307A JP5184536B2 JP 5184536 B2 JP5184536 B2 JP 5184536B2 JP 2009529307 A JP2009529307 A JP 2009529307A JP 2009529307 A JP2009529307 A JP 2009529307A JP 5184536 B2 JP5184536 B2 JP 5184536B2
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mmol
reaction
hexane
added
ethyl acetate
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JP2010504343A5 (enExample
JP2010504343A (ja
Inventor
チャオゲン・チェン
チャフィク・アムドウチ・アムドウチ
エリック・ジェイムズ・ヘンブル
フィリップ・アーサー・ヒップスカインド
ジア・シャオジュアン
ジェイムズ・リー・トス
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イーライ リリー アンド カンパニー
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • 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
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Addiction (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Anesthesiology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (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)
JP2009529307A 2006-09-20 2007-09-13 チオフェンピラゾロピリミジン化合物 Expired - Fee Related JP5184536B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US82627306P 2006-09-20 2006-09-20
US60/826,273 2006-09-20
PCT/US2007/078352 WO2008036541A1 (en) 2006-09-20 2007-09-13 Thiophene pyrazolopyrimidine compounds

Publications (3)

Publication Number Publication Date
JP2010504343A JP2010504343A (ja) 2010-02-12
JP2010504343A5 JP2010504343A5 (enExample) 2010-11-04
JP5184536B2 true JP5184536B2 (ja) 2013-04-17

Family

ID=38988344

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2009529307A Expired - Fee Related JP5184536B2 (ja) 2006-09-20 2007-09-13 チオフェンピラゾロピリミジン化合物

Country Status (12)

Country Link
US (1) US8110580B2 (enExample)
EP (1) EP2076515B1 (enExample)
JP (1) JP5184536B2 (enExample)
KR (1) KR101088196B1 (enExample)
CN (1) CN101516886B (enExample)
AU (1) AU2007297481B2 (enExample)
BR (1) BRPI0717070A2 (enExample)
CA (1) CA2662000C (enExample)
EA (1) EA016056B1 (enExample)
ES (1) ES2428543T3 (enExample)
MX (1) MX2009003098A (enExample)
WO (1) WO2008036541A1 (enExample)

Families Citing this family (22)

* 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
WO2009094224A1 (en) 2008-01-25 2009-07-30 Millennium Pharmaceuticals, Inc. Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
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
JP2012516329A (ja) 2009-01-30 2012-07-19 ミレニアム ファーマシューティカルズ, インコーポレイテッド Pi3k阻害剤としてのヘテロアリールおよびその使用
EP2603214A4 (en) 2010-08-11 2013-12-18 Millennium Pharm Inc HETEROARYLE AND USES THEREOF
US8859768B2 (en) 2010-08-11 2014-10-14 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9062038B2 (en) 2010-08-11 2015-06-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
MX2013004003A (es) 2010-10-13 2013-10-01 Millenium Pharmaceuticals Inc Heteroarilos y usos de los mismos.
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
KR20210064407A (ko) 2014-01-21 2021-06-02 뉴로크린 바이오사이언시즈 인코퍼레이티드 선천성 부신 과형성 치료를 위한 crf1 수용체 길항제
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
BR112020002967A2 (pt) 2017-08-14 2020-08-11 Spruce Biosciences, Inc. antagonistas de receptor de fator de liberação de corticotropina
TWI803504B (zh) * 2017-08-14 2023-06-01 美商雲杉生物科技股份有限公司 促皮質素釋放因子受體拮抗劑
MX2020011344A (es) 2018-04-27 2021-02-09 Spruce Biosciences Inc Métodos para tratar tumores en reposo suprarrenales testiculares y de ovarios.
PL3984523T3 (pl) 2018-12-07 2026-02-02 Neurocrine Biosciences, Inc. Antagonista receptora crf1, jego formulacje farmaceutyczne i postacie stałe do leczenia wrodzonego przerostu nadnerczy
US12383536B2 (en) 2019-09-27 2025-08-12 Neurocrine Biosciences, Inc. CRF receptor antagonists and methods of use
ES3039926T3 (en) * 2019-12-04 2025-10-27 Neurocrine Biosciences Inc Crf receptor antagonists and methods of use
JP2023537598A (ja) 2020-08-12 2023-09-04 スプルース バイオサイエンシーズ,インク. 多嚢胞性卵巣症候群を処置するための方法および組成物
US11708372B2 (en) 2021-11-19 2023-07-25 Spruce Biosciences, Inc. Crystalline composition of tildacerfont and methods of use and preparation thereof

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR9307646A (pt) 1992-12-17 1999-05-25 Pfizer Pirrolopirimidinas como antagonistas de crf
ES2168237T3 (es) 1996-02-07 2007-04-01 Neurocrine Biosciences, Inc. Pirazolopirimidinas como antagonistas de receptores de crf.
AU747708B2 (en) 1996-07-24 2002-05-23 Du Pont Pharmaceuticals Company Azolo triazines and pyrimidines
PL332040A1 (en) 1996-08-28 1999-08-16 Pfizer Substitution 6,5-heterobicyclic derivatives
YU23602A (sh) * 1999-09-30 2004-09-03 Neurogen Corporation Amino supstituisani pirazolo /1,5/a/-1,5-pirimidini i pirazolo /1,5-a/-1,3,5-triazini
JP4926720B2 (ja) 2003-12-22 2012-05-09 スミスクライン ビーチャム (コーク) リミテッド Crf受容体アンタゴニストおよびそれらに関連する方法
CN101142217B (zh) * 2005-03-21 2010-12-08 伊莱利利公司 咪唑并哒嗪化合物

Also Published As

Publication number Publication date
BRPI0717070A2 (pt) 2013-09-24
CA2662000A1 (en) 2008-03-27
CN101516886B (zh) 2012-02-29
KR101088196B1 (ko) 2011-11-30
EA016056B1 (ru) 2012-01-30
AU2007297481A1 (en) 2008-03-27
EA200970302A1 (ru) 2009-10-30
AU2007297481B2 (en) 2012-03-08
ES2428543T3 (es) 2013-11-08
WO2008036541A1 (en) 2008-03-27
US20100022560A1 (en) 2010-01-28
MX2009003098A (es) 2009-04-01
JP2010504343A (ja) 2010-02-12
CN101516886A (zh) 2009-08-26
KR20090053921A (ko) 2009-05-28
EP2076515A1 (en) 2009-07-08
US8110580B2 (en) 2012-02-07
CA2662000C (en) 2013-01-08
EP2076515B1 (en) 2013-07-17

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