CN101516886B - 噻吩吡唑并嘧啶化合物 - Google Patents

噻吩吡唑并嘧啶化合物 Download PDF

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Publication number
CN101516886B
CN101516886B CN2007800349472A CN200780034947A CN101516886B CN 101516886 B CN101516886 B CN 101516886B CN 2007800349472 A CN2007800349472 A CN 2007800349472A CN 200780034947 A CN200780034947 A CN 200780034947A CN 101516886 B CN101516886 B CN 101516886B
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China
Prior art keywords
hexane
thiophene
methyl
dimethyl
compound
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Expired - Fee Related
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CN2007800349472A
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English (en)
Chinese (zh)
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CN101516886A (zh
Inventor
陈招根
C·H·哈姆杜迟
E·J·亨布雷
P·A·希普斯金德
贾韶娟
J·L·托特
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Eli Lilly and Co
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Eli Lilly and Co
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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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Addiction (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Cardiology (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)
CN2007800349472A 2006-09-20 2007-09-13 噻吩吡唑并嘧啶化合物 Expired - Fee Related CN101516886B (zh)

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 (2)

Publication Number Publication Date
CN101516886A CN101516886A (zh) 2009-08-26
CN101516886B true CN101516886B (zh) 2012-02-29

Family

ID=38988344

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2007800349472A Expired - Fee Related CN101516886B (zh) 2006-09-20 2007-09-13 噻吩吡唑并嘧啶化合物

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 (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
EP2391619A1 (en) 2009-01-30 2011-12-07 Millennium Pharmaceuticals, Inc. Heteroaryls and their use as pi3k inhibitors
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
SG10201506238SA (en) 2010-08-11 2015-09-29 Millennium Pharm Inc Heteroaryls And Uses Thereof
PE20141044A1 (es) 2010-10-13 2014-09-07 Millennium Pharm Inc Heteroarilos y sus usos
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
LT3096756T (lt) 2014-01-21 2024-08-26 Neurocrine Biosciences, Inc. Crf1 receptoriaus antagonistai, skirti įgimtos antinksčių hiperplazijos gydymui
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
KR102644781B1 (ko) * 2017-08-14 2024-03-06 스프루스 바이오사이언시스 인코포레이티드 코티코트로핀 방출 인자 수용체 길항제
FI3984523T3 (fi) 2018-12-07 2025-10-21 Neurocrine Biosciences Inc Crf1-reseptorin antagonisti, lääkeformulaatioita ja niiden kiinteitä muotoja synnynnäisen lisämunuaisten liikakasvun hoitoon
CA3152590A1 (en) 2019-09-27 2021-04-01 Evan Smith Crf receptor antagonists and methods of use
WO2021113263A1 (en) * 2019-12-04 2021-06-10 Neurocrine Biosciences, Inc. Crf receptor antagonists and methods of use
KR20230043222A (ko) 2020-08-12 2023-03-30 스프루스 바이오사이언시스 인코포레이티드 다낭성 난소 증후군을 치료하기 위한 방법 및 조성물
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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Publication number Priority date Publication date Assignee Title
WO1994013676A1 (en) 1992-12-17 1994-06-23 Pfizer Inc. Pyrrolopyrimidines as crf antagonists
EP0915880B1 (en) 1996-07-24 2007-10-10 Bristol-Myers Squibb Pharma Company Azolo triazines and pyrimidines
DE69736711T2 (de) 1996-08-28 2007-09-20 Pfizer Inc. Substituierte 6,5-heterobicyclische-derivate
US7612067B2 (en) * 2005-03-21 2009-11-03 Eli Lilly And Company Imidazopyridazine compounds

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 (2)

* 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》.2003,第345卷(第5期),620-624. *
MAJOV.J.，etal.FacilePalladium-CatalyzedSynthesisof3-Arylpyrazolo-[1 5a]pyrimidines.《ADVANCED SYNTHESIS AND CATALYSIS》.2003

Also Published As

Publication number Publication date
KR20090053921A (ko) 2009-05-28
WO2008036541A1 (en) 2008-03-27
JP2010504343A (ja) 2010-02-12
AU2007297481B2 (en) 2012-03-08
US20100022560A1 (en) 2010-01-28
MX2009003098A (es) 2009-04-01
JP5184536B2 (ja) 2013-04-17
KR101088196B1 (ko) 2011-11-30
BRPI0717070A2 (pt) 2013-09-24
CA2662000C (en) 2013-01-08
EA016056B1 (ru) 2012-01-30
AU2007297481A1 (en) 2008-03-27
EP2076515A1 (en) 2009-07-08
ES2428543T3 (es) 2013-11-08
CA2662000A1 (en) 2008-03-27
CN101516886A (zh) 2009-08-26
EA200970302A1 (ru) 2009-10-30
EP2076515B1 (en) 2013-07-17
US8110580B2 (en) 2012-02-07

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Termination date: 20160913