KR101088196B1 - 티오펜 피라졸로피리미딘 화합물 - Google Patents

티오펜 피라졸로피리미딘 화합물 Download PDF

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KR101088196B1
KR101088196B1 KR1020097005694A KR20097005694A KR101088196B1 KR 101088196 B1 KR101088196 B1 KR 101088196B1 KR 1020097005694 A KR1020097005694 A KR 1020097005694A KR 20097005694 A KR20097005694 A KR 20097005694A KR 101088196 B1 KR101088196 B1 KR 101088196B1
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mmol
reaction
added
hexanes
formula
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KR20090053921A (ko
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자오겐 첸
차피크 함도우치 함도우치
에릭 제임스 헴브레
필립 아써 힙스킨드
샤오쥬안 지아
제임스 리 토쓰
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일라이 릴리 앤드 캄파니
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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
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
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    • 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
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    • A61P35/00Antineoplastic agents
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    • A61P37/00Drugs for immunological or allergic disorders
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    • 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
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    • 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)
  • 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)
  • Addiction (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Pulmonology (AREA)
  • Hematology (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)
KR1020097005694A 2006-09-20 2007-09-13 티오펜 피라졸로피리미딘 화합물 Expired - Fee Related KR101088196B1 (ko)

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
KR20090053921A KR20090053921A (ko) 2009-05-28
KR101088196B1 true KR101088196B1 (ko) 2011-11-30

Family

ID=38988344

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Application Number Title Priority Date Filing Date
KR1020097005694A Expired - Fee Related KR101088196B1 (ko) 2006-09-20 2007-09-13 티오펜 피라졸로피리미딘 화합물

Country Status (12)

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

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
US9029411B2 (en) 2008-01-25 2015-05-12 Millennium Pharmaceuticals, Inc. Thiophenes and uses thereof
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
WO2012021611A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US8859768B2 (en) 2010-08-11 2014-10-14 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
TW201217365A (en) 2010-08-11 2012-05-01 Millennium Pharm Inc Heteroaryls and uses thereof
TW201307309A (zh) 2010-10-13 2013-02-16 Millennium Pharm Inc 雜芳基化合物及其用途
EP2729455B1 (en) 2011-07-05 2016-09-14 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
RS65839B1 (sr) 2014-01-21 2024-09-30 Neurocrine Biosciences Inc Crf1 receptor antagonisti za tretman kongenitalne adrenalne hiperplazije
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
JP7285222B2 (ja) * 2017-08-14 2023-06-01 スプルース バイオサイエンシズ インコーポレイテッド 副腎皮質刺激ホルモン放出因子受容体拮抗薬
EP4643950A3 (en) 2018-04-27 2026-01-14 Spruce Biosciences, Inc. Methods for treating testicular and ovarian adrenal rest tumors
US20220023266A1 (en) 2018-12-07 2022-01-27 Neurocrine Biosciences, Inc. Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia
JP7623365B2 (ja) 2019-09-27 2025-01-28 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 Crf受容体アンタゴニストおよび使用方法
TW202134241A (zh) * 2019-12-04 2021-09-16 美商紐羅克里生物科學有限公司 Crf受體拮抗劑及使用方法
KR20240023691A (ko) 2020-08-12 2024-02-22 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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005063755A1 (en) 2003-12-22 2005-07-14 Sb Pharmco Puerto Rico Inc Crf receptor antagonists and methods relating thereto

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR19990067704A (ko) 1992-12-17 1999-08-25 디. 제이. 우드, 스피겔 알렌 제이 부신피질자극호르몬 유리인자 길항제로서의 피롤로피리미딘을함유하는 약학 조성물
AU713673B2 (en) * 1996-02-07 1999-12-09 Neurocrine Biosciences Inc. Pyrazolopyrimidines as crf receptor antagonists
HU229024B1 (en) 1996-07-24 2013-07-29 Bristol Myers Squibb Pharma Co Azolo-pyridimidines, pharmaceutical compositions containing the same and use thereof
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
ES2277855T3 (es) * 1999-09-30 2007-08-01 Neurogen Corporation Pirazolo-(1,5-a)-1,5-pirimidinas y pirazolo-(1,5-a)-1,3,5-triazinas amino sustituidas.
EP1869049B1 (en) * 2005-03-21 2009-03-04 Eli Lilly And Company Imidazopyridazine compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005063755A1 (en) 2003-12-22 2005-07-14 Sb Pharmco Puerto Rico Inc Crf receptor antagonists and methods relating thereto

Also Published As

Publication number Publication date
JP2010504343A (ja) 2010-02-12
CN101516886B (zh) 2012-02-29
MX2009003098A (es) 2009-04-01
US8110580B2 (en) 2012-02-07
ES2428543T3 (es) 2013-11-08
CN101516886A (zh) 2009-08-26
AU2007297481A1 (en) 2008-03-27
EA200970302A1 (ru) 2009-10-30
CA2662000C (en) 2013-01-08
CA2662000A1 (en) 2008-03-27
KR20090053921A (ko) 2009-05-28
EP2076515A1 (en) 2009-07-08
JP5184536B2 (ja) 2013-04-17
BRPI0717070A2 (pt) 2013-09-24
WO2008036541A1 (en) 2008-03-27
EA016056B1 (ru) 2012-01-30
AU2007297481B2 (en) 2012-03-08
EP2076515B1 (en) 2013-07-17
US20100022560A1 (en) 2010-01-28

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