CN101516887B - 作为crf1受体拮抗剂的噻唑吡唑并嘧啶类 - Google Patents

作为crf1受体拮抗剂的噻唑吡唑并嘧啶类 Download PDF

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Publication number
CN101516887B
CN101516887B CN2007800351453A CN200780035145A CN101516887B CN 101516887 B CN101516887 B CN 101516887B CN 2007800351453 A CN2007800351453 A CN 2007800351453A CN 200780035145 A CN200780035145 A CN 200780035145A CN 101516887 B CN101516887 B CN 101516887B
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thiazole
dimethyl
formula
pyrazolo
compound
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CN101516887A (zh
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Z·陈
C·H·哈姆杜迟
E·J·亨布雷
P·A·希普斯金德
J·K·迈尔斯
高赤贵子
J·L·托特
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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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P15/06—Antiabortive agents; Labour repressants
    • 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
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    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
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    • 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
    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
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    • 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
    • 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Anesthesiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN2007800351453A 2006-09-20 2007-09-17 作为crf1受体拮抗剂的噻唑吡唑并嘧啶类 Active CN101516887B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US82626406P 2006-09-20 2006-09-20
US60/826,264 2006-09-20
PCT/US2007/078605 WO2008036579A1 (en) 2006-09-20 2007-09-17 Thiazole pyrazolopyrimidines as crf1 receptor antagonists

Publications (2)

Publication Number Publication Date
CN101516887A CN101516887A (zh) 2009-08-26
CN101516887B true CN101516887B (zh) 2011-11-02

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CN2007800351453A Active CN101516887B (zh) 2006-09-20 2007-09-17 作为crf1受体拮抗剂的噻唑吡唑并嘧啶类

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Country Link
US (1) US8030304B2 (enExample)
EP (1) EP2094709B1 (enExample)
JP (1) JP5161226B2 (enExample)
KR (1) KR101088239B1 (enExample)
CN (1) CN101516887B (enExample)
AR (1) AR062886A1 (enExample)
AT (1) ATE481405T1 (enExample)
AU (1) AU2007297421B2 (enExample)
BR (1) BRPI0717023B8 (enExample)
CA (1) CA2663511C (enExample)
CL (1) CL2007002693A1 (enExample)
CR (1) CR10682A (enExample)
CY (1) CY1110854T1 (enExample)
DE (1) DE602007009305D1 (enExample)
DK (1) DK2094709T3 (enExample)
EA (1) EA015179B1 (enExample)
ES (1) ES2350282T3 (enExample)
HR (1) HRP20100516T1 (enExample)
IL (1) IL197614A (enExample)
MA (1) MA30798B1 (enExample)
MX (1) MX2009003125A (enExample)
MY (1) MY146388A (enExample)
NO (1) NO20091489L (enExample)
NZ (1) NZ575572A (enExample)
PE (1) PE20081377A1 (enExample)
PL (1) PL2094709T3 (enExample)
PT (1) PT2094709E (enExample)
RS (1) RS51545B (enExample)
SI (1) SI2094709T1 (enExample)
TN (1) TN2009000095A1 (enExample)
TW (1) TWI402269B (enExample)
UA (1) UA96458C2 (enExample)
WO (1) WO2008036579A1 (enExample)

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EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
CA2739422C (en) * 2008-10-02 2013-03-12 Eli Lilly And Company Thiazolyl-pyrazolopyrimidine compounds as synthetic intermediates and related synthetic processes
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
PT3096756T (pt) * 2014-01-21 2024-08-26 Neurocrine Biosciences Inc Antagonistas do recetor crf1 para o tratamento da hiperplasia adrenal congénita
PL236355B1 (pl) * 2015-04-02 2021-01-11 Celon Pharma Spolka Akcyjna Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3
CA3039026A1 (en) 2016-09-07 2018-03-15 The Regents Of The University Of California Allosteric corticotropin-releasing factor receptor 1 (crfr1) antagonists that decrease p-tau and improve cognition
AU2018318990B2 (en) * 2017-08-14 2023-01-05 Spruce Biosciences, Inc. Corticotropin releasing factor receptor antagonists
BR112020002967A2 (pt) * 2017-08-14 2020-08-11 Spruce Biosciences, Inc. antagonistas de receptor de fator de liberação de corticotropina
WO2019210266A1 (en) * 2018-04-27 2019-10-31 Spruce Biosciences, Inc. Methods for treating testicular and ovarian adrenal rest tumors
CN109134481B (zh) * 2018-08-07 2021-05-14 中山大学 一种取代吡咯色原酮类化合物或其药学上可接受的盐及其制备方法和应用
TWI714231B (zh) * 2018-09-04 2020-12-21 美商美國禮來大藥廠 2,6-二胺基吡啶化合物
MA54395A (fr) 2018-12-07 2022-03-16 Neurocrine Biosciences Inc Antagoniste du récepteur crf1, formulations pharmaceutiques et formes solides correspondantes pour le traitement de l'hyperplasie surrénalienne congénitale
EP3986416A4 (en) * 2019-07-19 2023-06-28 Spruce Biosciences, Inc. Methods of treating congenital adrenal hyperplasia
US12383536B2 (en) 2019-09-27 2025-08-12 Neurocrine Biosciences, Inc. CRF receptor antagonists and methods of use
EP4069697B1 (en) * 2019-12-04 2025-07-16 Neurocrine Biosciences, Inc. Crf receptor antagonists and methods of use
GR1010096B (el) * 2020-07-02 2021-10-08 Uni-Pharma Κλεων Τσετης Φαρμακευτικα Εργαστηρια Αβεε, Πυραζολο[1,5-a]πυριμιδινες με δραση αναστολης της αυτοταξινης
WO2022036123A1 (en) 2020-08-12 2022-02-17 Spruce Biosciences, Inc. Methods and compositions for treating polycystic ovary syndrome
US20240024330A1 (en) 2020-08-26 2024-01-25 Neurocrine Biosciences, Inc. Crf receptor antagonists and methods of use
EP4308553A4 (en) 2021-03-19 2025-01-22 Crinetics Pharmaceuticals, Inc. Melanocortin subtype-2 receptor (mc2r) antagonist for the treatment of disease
KR20240109274A (ko) * 2021-11-19 2024-07-10 스프루스 바이오사이언시스 인코포레이티드 틸다서폰트의 결정질 조성물 및 이의 사용 및 제조 방법
US11708372B2 (en) 2021-11-19 2023-07-25 Spruce Biosciences, Inc. Crystalline composition of tildacerfont and methods of use and preparation thereof
WO2023163945A1 (en) * 2022-02-23 2023-08-31 Crinetics Pharmaceuticals, Inc. Treatment of congenital adrenal hyperplasia and polycystic ovary syndrome
WO2025188842A1 (en) * 2024-03-08 2025-09-12 Spruce Biosciences, Inc. Amorphous solid dispersion of tildacerfont formulations

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CN1205009A (zh) * 1996-02-07 1999-01-13 詹森药业有限公司 吡唑并嘧啶类化合物
CN1225637A (zh) * 1996-07-24 1999-08-11 杜邦药品公司 吡咯并三嗪和嘧啶化合物
CN1509196A (zh) * 2001-03-13 2004-06-30 ����˹�ж�-����˹˹����ҩƷ��˾ 作为促肾上腺皮质素释放因子受体配体的4－(2－丁基氨基)－2 ,7－二甲基－8－(2－甲基－6－甲氧基吡啶－3－基)吡唑并[1,5－α]－1,3,5－三嗪,它的对映异构体及可药用盐
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CN1205009A (zh) * 1996-02-07 1999-01-13 詹森药业有限公司 吡唑并嘧啶类化合物
CN1225637A (zh) * 1996-07-24 1999-08-11 杜邦药品公司 吡咯并三嗪和嘧啶化合物
CN1509196A (zh) * 2001-03-13 2004-06-30 ����˹�ж�-����˹˹����ҩƷ��˾ 作为促肾上腺皮质素释放因子受体配体的4－(2－丁基氨基)－2 ,7－二甲基－8－(2－甲基－6－甲氧基吡啶－3－基)吡唑并[1,5－α]－1,3,5－三嗪,它的对映异构体及可药用盐
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Chen Chen,et al..Design of 2,5-Dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and Structure-Activity Relationships of a Series of Potent and Orally Active Corticotropin-Releasing Factor Receptor Antagonists.《Journal of Medicinal Chemistry》.2004,第47卷(第19期),第4787-4798页. *
ChenChen et al..Design of 2
Liqi He,et al..4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2,4-dichlorophenyl)-pyrazolo[1,5-a]-1,3,5-triazine: A Potent, Orally Bioavailable CRF1 Receptor Antagonist.《Journal of Medicinal Chemistry》.2000,第43卷(第3期),第451页表1. *
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NO20091489L (no) 2009-04-16
MY146388A (en) 2012-08-15
MX2009003125A (es) 2009-05-28
BRPI0717023B1 (pt) 2019-11-19
KR20090052366A (ko) 2009-05-25
CL2007002693A1 (es) 2008-04-18
US8030304B2 (en) 2011-10-04
IL197614A (en) 2012-10-31
DK2094709T3 (da) 2010-12-06
CY1110854T1 (el) 2015-06-10
JP2010504344A (ja) 2010-02-12
AU2007297421A1 (en) 2008-03-27
ES2350282T3 (es) 2011-01-20
US20100222339A1 (en) 2010-09-02
PT2094709E (pt) 2010-10-04
EA200970303A1 (ru) 2009-10-30
TN2009000095A1 (en) 2010-08-19
AU2007297421B2 (en) 2012-03-08
DE602007009305D1 (de) 2010-10-28
HK1132505A1 (en) 2010-02-26
CN101516887A (zh) 2009-08-26
PL2094709T3 (pl) 2011-02-28
NZ575572A (en) 2011-10-28
EP2094709B1 (en) 2010-09-15
UA96458C2 (ru) 2011-11-10
AR062886A1 (es) 2008-12-10
CA2663511A1 (en) 2008-03-27
RS51545B (sr) 2011-06-30
SI2094709T1 (sl) 2011-01-31
ATE481405T1 (de) 2010-10-15
KR101088239B1 (ko) 2011-11-30
TWI402269B (zh) 2013-07-21
CR10682A (es) 2009-08-13
PE20081377A1 (es) 2008-09-18
JP5161226B2 (ja) 2013-03-13
BRPI0717023B8 (pt) 2021-05-25
WO2008036579A1 (en) 2008-03-27
BRPI0717023A2 (pt) 2014-03-11
EA015179B1 (ru) 2011-06-30
MA30798B1 (fr) 2009-10-01
TW200821312A (en) 2008-05-16
IL197614A0 (en) 2009-12-24
CA2663511C (en) 2012-12-04
HRP20100516T1 (hr) 2010-10-31
EP2094709A1 (en) 2009-09-02

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