KR101088239B1 - Ｃｒｆ１ 수용체 길항제로서의 티아졸 피라졸로피리미딘 - Google Patents

Ｃｒｆ１ 수용체 길항제로서의 티아졸 피라졸로피리미딘 Download PDF

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KR101088239B1
KR101088239B1 KR1020097005602A KR20097005602A KR101088239B1 KR 101088239 B1 KR101088239 B1 KR 101088239B1 KR 1020097005602 A KR1020097005602 A KR 1020097005602A KR 20097005602 A KR20097005602 A KR 20097005602A KR 101088239 B1 KR101088239 B1 KR 101088239B1
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mmol
formula
dimethyl
propyl
added
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Korean (ko)
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KR20090052366A (ko
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자오겐 첸
차피크 함도우치 함도우치
에릭 제임스 헴브레
필립 아써 힙스킨드
제이슨 케네쓰 마이어스
타카코 타카쿠와
제임스 리 토쓰
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일라이 릴리 앤드 캄파니
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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
    • 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
    • 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
    • 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
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (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)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1020097005602A 2006-09-20 2007-09-17 Ｃｒｆ１ 수용체 길항제로서의 티아졸 피라졸로피리미딘 Expired - Fee Related KR101088239B1 (ko)

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
KR20090052366A KR20090052366A (ko) 2009-05-25
KR101088239B1 true KR101088239B1 (ko) 2011-11-30

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ID=38924802

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KR1020097005602A Expired - Fee Related KR101088239B1 (ko) 2006-09-20 2007-09-17 Ｃｒｆ１ 수용체 길항제로서의 티아졸 피라졸로피리미딘

Country Status (33)

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
KR101357392B1 (ko) * 2008-10-02 2014-02-03 일라이 릴리 앤드 캄파니 합성 중간체로서의 티아졸릴-피라졸로피리미딘 화합물 및 관련 합성 방법
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
CA3155599A1 (en) 2014-01-21 2015-07-30 Neurocrine Biosciences, Inc. Crf1 receptor antagonists for the treatment of congenital adrenal hyperplasia
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
CN109906222B (zh) 2016-09-07 2023-08-01 加利福尼亚大学董事会 减少p-tau并且改善认知的变构促肾上腺皮质激素释放因子受体1(crfr1)拮抗剂
KR102644781B1 (ko) * 2017-08-14 2024-03-06 스프루스 바이오사이언시스 인코포레이티드 코티코트로핀 방출 인자 수용체 길항제
BR112020002967A2 (pt) * 2017-08-14 2020-08-11 Spruce Biosciences, Inc. antagonistas de receptor de fator de liberação de corticotropina
CN112423747A (zh) * 2018-04-27 2021-02-26 云杉生物科学公司 用于治疗睾丸肾上腺残余瘤和卵巢肾上腺残余瘤的方法
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
MA56226A (fr) 2018-12-07 2022-04-20 Neurocrine Biosciences Inc Antagoniste du récepteur crf1, formulations pharmaceutiques et ses formes solides pour le traitement de l'hyperplasie surrénale congénitale
KR20220052927A (ko) * 2019-07-19 2022-04-28 스프루스 바이오사이언시스 인코포레이티드 선천성 부신 증식증의 치료 방법
CN118252829A (zh) 2019-09-27 2024-06-28 纽罗克里生物科学有限公司 Crf受体拮抗剂及使用方法
ES3039926T3 (en) * 2019-12-04 2025-10-27 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
EP4656192A2 (en) * 2020-08-12 2025-12-03 Spruce Biosciences, Inc. Tildacerfont and derivatives thereof for treating polycystic ovary syndrome
US20240024330A1 (en) 2020-08-26 2024-01-25 Neurocrine Biosciences, Inc. Crf receptor antagonists and methods of use
US12280046B2 (en) 2021-03-19 2025-04-22 Crinetics Pharmaceuticals, Inc. Melanocortin subtype-2 receptor (MC2R) antagonist for the treatment of disease
EP4402142A4 (en) * 2021-11-19 2025-07-23 Spruce Biosciences Inc CRYSTALLINE COMPOSITION OF TILDACERFONT AND ITS METHODS OF USE AND PREPARATION
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

Citations (2)

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PL191271B1 (pl) * 1996-02-07 2006-04-28 Neurocrine Biosciences Inc Pochodna pirazolopirymidyny i jej zastosowanie oraz kompozycja farmaceutyczna
EA006626B1 (ru) * 1996-07-24 2006-02-24 Дюпон Фармасьютикалз Компани Азолопиримидины, фармацевтическая композиция и способ лечения
CZ299451B6 (cs) * 1996-07-24 2008-07-30 Bristol-Myers Squibb Pharma Company [1,5-a]-Pyrazolo-1,3,5- triaziny jejich použití afarmaceutické kompozice na jejich bázi
CA2263566C (en) 1996-08-28 2003-09-09 Pfizer Inc. Substituted 6,5-hetero-bicyclic derivatives
EP1040831A3 (en) * 1999-04-02 2003-05-02 Pfizer Products Inc. Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death
AU4203500A (en) 1999-04-06 2000-10-23 Du Pont Pharmaceuticals Company Pyrazolopyrimidines as crf antagonists
CN1377355A (zh) 1999-09-30 2002-10-30 纽罗杰有限公司 氨基取代的吡唑并[1,5－a]－1,5－嘧啶和吡唑并[1,5－a]－1,3,5－三嗪

Patent Citations (2)

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WO2002072202A1 (en) 2001-03-13 2002-09-19 Bristol-Myers Squibb Pharma Company 4-(2-butylamino)-2,7-dimethyl-8-(2-methyl-6-methoxypyrid-3-yl) pyrazolo-[1,5-a]-1,3,5-triazine, its enantiomers and pharmaceutically acceptable salts as corticotropin releasing factor receptor ligands
WO2005063755A1 (en) 2003-12-22 2005-07-14 Sb Pharmco Puerto Rico Inc Crf receptor antagonists and methods relating thereto

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PL2094709T3 (pl) 2011-02-28
MY146388A (en) 2012-08-15
TWI402269B (zh) 2013-07-21
IL197614A0 (en) 2009-12-24
HRP20100516T1 (hr) 2010-10-31
PT2094709E (pt) 2010-10-04
BRPI0717023B1 (pt) 2019-11-19
JP5161226B2 (ja) 2013-03-13
EP2094709A1 (en) 2009-09-02
CR10682A (es) 2009-08-13
MA30798B1 (fr) 2009-10-01
US8030304B2 (en) 2011-10-04
RS51545B (sr) 2011-06-30
TW200821312A (en) 2008-05-16
WO2008036579A1 (en) 2008-03-27
HK1132505A1 (en) 2010-02-26
TN2009000095A1 (en) 2010-08-19
CA2663511A1 (en) 2008-03-27
CA2663511C (en) 2012-12-04
CN101516887B (zh) 2011-11-02
PE20081377A1 (es) 2008-09-18
BRPI0717023B8 (pt) 2021-05-25
DE602007009305D1 (de) 2010-10-28
ATE481405T1 (de) 2010-10-15
KR20090052366A (ko) 2009-05-25
BRPI0717023A2 (pt) 2014-03-11
DK2094709T3 (da) 2010-12-06
CY1110854T1 (el) 2015-06-10
EA015179B1 (ru) 2011-06-30
NZ575572A (en) 2011-10-28
SI2094709T1 (sl) 2011-01-31
CL2007002693A1 (es) 2008-04-18
EP2094709B1 (en) 2010-09-15
CN101516887A (zh) 2009-08-26
JP2010504344A (ja) 2010-02-12
MX2009003125A (es) 2009-05-28
AU2007297421A1 (en) 2008-03-27
NO20091489L (no) 2009-04-16
AU2007297421B2 (en) 2012-03-08
ES2350282T3 (es) 2011-01-20
US20100222339A1 (en) 2010-09-02
AR062886A1 (es) 2008-12-10
IL197614A (en) 2012-10-31
UA96458C2 (ru) 2011-11-10
EA200970303A1 (ru) 2009-10-30

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