CA2663511C - Thiazole pyrazolopyrimidines as crf1 receptor antagonists - Google Patents

Thiazole pyrazolopyrimidines as crf1 receptor antagonists Download PDF

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Publication number
CA2663511C
CA2663511C CA2663511A CA2663511A CA2663511C CA 2663511 C CA2663511 C CA 2663511C CA 2663511 A CA2663511 A CA 2663511A CA 2663511 A CA2663511 A CA 2663511A CA 2663511 C CA2663511 C CA 2663511C
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CA
Canada
Prior art keywords
mmol
compound according
dimethyl
propyl
pyrazolo
Prior art date
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CA2663511A
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English (en)
French (fr)
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CA2663511A1 (en
Inventor
Zhaogen Chen
Chafiq Hamdouchi Hamdouchi
Erik James Hembre
Philip Arthur Hipskind
Jason Kenneth Myers
Takako Takakuwa
James Lee Toth
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Eli Lilly and Co
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Eli Lilly and Co
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Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CA2663511A1 publication Critical patent/CA2663511A1/en
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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)
  • 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)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA2663511A 2006-09-20 2007-09-17 Thiazole pyrazolopyrimidines as crf1 receptor antagonists Active CA2663511C (en)

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
CA2663511A1 CA2663511A1 (en) 2008-03-27
CA2663511C true CA2663511C (en) 2012-12-04

Family

ID=38924802

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2663511A Active CA2663511C (en) 2006-09-20 2007-09-17 Thiazole pyrazolopyrimidines as crf1 receptor antagonists

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)

Families Citing this family (23)

* 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
TWI432435B (zh) * 2008-10-02 2014-04-01 Lilly Co Eli 作為合成中間物之噻唑基－吡唑并嘧啶化合物及相關合成方法
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
KR20210064407A (ko) * 2014-01-21 2021-06-02 뉴로크린 바이오사이언시즈 인코퍼레이티드 선천성 부신 과형성 치료를 위한 ｃｒｆ1 수용체 길항제
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
EP3510029B1 (en) 2016-09-07 2025-11-05 The Regents of The University of California Allosteric corticotropin-releasing factor receptor 1 (crfr1) antagonists that decrease p-tau and improve cognition
BR112020002967A2 (pt) 2017-08-14 2020-08-11 Spruce Biosciences, Inc. antagonistas de receptor de fator de liberação de corticotropina
TWI803504B (zh) * 2017-08-14 2023-06-01 美商雲杉生物科技股份有限公司 促皮質素釋放因子受體拮抗劑
MX2020011344A (es) * 2018-04-27 2021-02-09 Spruce Biosciences Inc Métodos para tratar tumores en reposo suprarrenales testiculares y de ovarios.
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
PL3984523T3 (pl) 2018-12-07 2026-02-02 Neurocrine Biosciences, Inc. Antagonista receptora crf1, jego formulacje farmaceutyczne i postacie stałe do leczenia wrodzonego przerostu nadnerczy
KR20220052927A (ko) * 2019-07-19 2022-04-28 스프루스 바이오사이언시스 인코포레이티드 선천성 부신 증식증의 치료 방법
US12383536B2 (en) 2019-09-27 2025-08-12 Neurocrine Biosciences, Inc. CRF receptor antagonists and methods of use
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
JP2023537598A (ja) 2020-08-12 2023-09-04 スプルース バイオサイエンシーズ，インク． 多嚢胞性卵巣症候群を処置するための方法および組成物
US20240024330A1 (en) 2020-08-26 2024-01-25 Neurocrine Biosciences, Inc. Crf receptor antagonists and methods of use
BR112023018816A2 (pt) 2021-03-19 2023-10-31 Crinetics Pharmaceuticals Inc Antagonista do receptor de melanocortina subtipo-2 (mc2r) para o tratamento de doença
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

Family Cites Families (10)

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Publication number Priority date Publication date Assignee Title
BR9307646A (pt) 1992-12-17 1999-05-25 Pfizer Pirrolopirimidinas como antagonistas de crf
ES2168237T3 (es) * 1996-02-07 2007-04-01 Neurocrine Biosciences, Inc. Pirazolopirimidinas como antagonistas de receptores de crf.
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
AU747708B2 (en) 1996-07-24 2002-05-23 Du Pont Pharmaceuticals Company Azolo triazines and pyrimidines
PL332040A1 (en) 1996-08-28 1999-08-16 Pfizer Substitution 6,5-heterobicyclic 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
YU23602A (sh) * 1999-09-30 2004-09-03 Neurogen Corporation Amino supstituisani pirazolo /1,5/a/-1,5-pirimidini i pirazolo /1,5-a/-1,3,5-triazini
ES2282401T3 (es) 2001-03-13 2007-10-16 Bristol-Myers Squibb Pharma Company 4-(2-butilamino)-2,7-dimetil-8-(2-metil-6-metoxipirid-3-il) pirazolo - 1,5-a-1,3,5-triazina, sus enantiomeros y sales farmaceuticamente aceptables como ligandos del receptor del factor liberador de croticotropina.
JP4926720B2 (ja) 2003-12-22 2012-05-09 スミスクライン ビーチャム （コーク） リミテッド Ｃｒｆ受容体アンタゴニストおよびそれらに関連する方法

Also Published As

Publication number Publication date
BRPI0717023B8 (pt) 2021-05-25
JP5161226B2 (ja) 2013-03-13
EP2094709A1 (en) 2009-09-02
MY146388A (en) 2012-08-15
ES2350282T3 (es) 2011-01-20
DE602007009305D1 (de) 2010-10-28
MX2009003125A (es) 2009-05-28
EA015179B1 (ru) 2011-06-30
CY1110854T1 (el) 2015-06-10
PT2094709E (pt) 2010-10-04
AR062886A1 (es) 2008-12-10
US20100222339A1 (en) 2010-09-02
NZ575572A (en) 2011-10-28
JP2010504344A (ja) 2010-02-12
HK1132505A1 (en) 2010-02-26
BRPI0717023B1 (pt) 2019-11-19
IL197614A0 (en) 2009-12-24
AU2007297421B2 (en) 2012-03-08
DK2094709T3 (da) 2010-12-06
KR20090052366A (ko) 2009-05-25
CA2663511A1 (en) 2008-03-27
TWI402269B (zh) 2013-07-21
SI2094709T1 (sl) 2011-01-31
BRPI0717023A2 (pt) 2014-03-11
ATE481405T1 (de) 2010-10-15
TW200821312A (en) 2008-05-16
CL2007002693A1 (es) 2008-04-18
US8030304B2 (en) 2011-10-04
HRP20100516T1 (hr) 2010-10-31
WO2008036579A1 (en) 2008-03-27
EP2094709B1 (en) 2010-09-15
UA96458C2 (ru) 2011-11-10
KR101088239B1 (ko) 2011-11-30
MA30798B1 (fr) 2009-10-01
PL2094709T3 (pl) 2011-02-28
EA200970303A1 (ru) 2009-10-30
NO20091489L (no) 2009-04-16
CN101516887B (zh) 2011-11-02
AU2007297421A1 (en) 2008-03-27
IL197614A (en) 2012-10-31
PE20081377A1 (es) 2008-09-18
CR10682A (es) 2009-08-13
RS51545B (sr) 2011-06-30
CN101516887A (zh) 2009-08-26
TN2009000095A1 (en) 2010-08-19

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