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)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Child & Adolescent Psychology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Pulmonology (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)
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)

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

Families Citing this family (21)

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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
EP2250160B1 (en) 2008-01-25 2015-11-11 Millennium Pharmaceuticals, Inc. Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
WO2010090716A1 (en) 2009-01-30 2010-08-12 Millennium Pharmaceuticals, Inc. Heteroaryls and their use as 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
US9062038B2 (en) 2010-08-11 2015-06-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
UY33554A (es) 2010-08-11 2012-02-29 Millennium Pharm Inc Heteroarilos y usos de los mismos
WO2012021615A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
BR112013009166A2 (pt) 2010-10-13 2016-07-26 Millennium Pharm Inc heteroarilas e uso das mesmas.
US8946432B2 (en) 2011-07-05 2015-02-03 Lupin Limited Biaryl derivatives as nAChR modulators
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
CN106102740A (zh) 2014-01-21 2016-11-09 纽罗克里生物科学有限公司 治疗先天性肾上腺增生的crf1受体拮抗剂
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
WO2019036503A1 (en) 2017-08-14 2019-02-21 Spruce Biosciences, Inc. CORTICOTROPIN RELEASE FACTOR RECEPTOR ANTAGONISTS
CA3064445A1 (en) * 2017-08-14 2019-02-21 Spruce Biosciences, Inc. Corticotropin releasing factor receptor antagonists
EP3984523B1 (en) 2018-12-07 2025-09-03 Neurocrine Biosciences, Inc. Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia
WO2021062246A1 (en) 2019-09-27 2021-04-01 Neurocrine Biosciences, Inc. Crf receptor antagonists and methods of use
AR120649A1 (es) * 2019-12-04 2022-03-09 Neurocrine Biosciences Inc Antagonistas del receptor de crf y métodos de uso
EP4175572A4 (en) 2020-08-12 2024-03-27 Spruce Biosciences, Inc. Methods and compositions for treating polycystic ovary syndrome
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

Family Cites Families (4)

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Publication number Priority date Publication date Assignee Title
ES2128544T3 (es) 1992-12-17 1999-05-16 Pfizer Pirrolopirimidinas como antagonistas del crf.
ES2294800T3 (es) 1996-07-24 2008-04-01 Bristol-Myers Squibb Pharma Company Azolo triazinas y pirimidinas.
BR9711970A (pt) 1996-08-28 1999-08-24 Pfizer Derivados 6,5-substitu¡do-heterobic¡clicos
DK1869049T3 (da) * 2005-03-21 2009-05-18 Lilly Co Eli Imidazopyridazinforbindelser

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

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