JP5161226B2 - Ｃｒｆ１受容体アンタゴニストとしてのチアゾールピラゾロピリミジン - Google Patents
Ｃｒｆ１受容体アンタゴニストとしてのチアゾールピラゾロピリミジン Download PDFInfo
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- JP5161226B2 JP5161226B2 JP2009529316A JP2009529316A JP5161226B2 JP 5161226 B2 JP5161226 B2 JP 5161226B2 JP 2009529316 A JP2009529316 A JP 2009529316A JP 2009529316 A JP2009529316 A JP 2009529316A JP 5161226 B2 JP5161226 B2 JP 5161226B2
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- 229910000033 sodium borohydride Inorganic materials 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
- 238000000935 solvent evaporation Methods 0.000 description 1
- 238000013222 sprague-dawley male rat Methods 0.000 description 1
- 208000024794 sputum Diseases 0.000 description 1
- 210000003802 sputum Anatomy 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229960002317 succinimide Drugs 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- JRMUNVKIHCOMHV-UHFFFAOYSA-M tetrabutylammonium bromide Chemical compound [Br-].CCCC[N+](CCCC)(CCCC)CCCC JRMUNVKIHCOMHV-UHFFFAOYSA-M 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 150000003557 thiazoles Chemical class 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 150000003852 triazoles Chemical class 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- JAYKPAAGOYELFD-UHFFFAOYSA-N tris(2,4-ditert-butylphenyl)phosphane Chemical compound CC(C)(C)C1=CC(C(C)(C)C)=CC=C1P(C=1C(=CC(=CC=1)C(C)(C)C)C(C)(C)C)C1=CC=C(C(C)(C)C)C=C1C(C)(C)C JAYKPAAGOYELFD-UHFFFAOYSA-N 0.000 description 1
- KRVVVSZNTMFCON-UHFFFAOYSA-L zinc;1,3-thiazole;dibromide Chemical compound [Zn+2].[Br-].[Br-].C1=CSC=N1 KRVVVSZNTMFCON-UHFFFAOYSA-L 0.000 description 1
Classifications
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- 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
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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)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Chemical Kinetics & Catalysis (AREA)
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- Biomedical Technology (AREA)
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- Gynecology & Obstetrics (AREA)
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- Child & Adolescent Psychology (AREA)
- Orthopedic Medicine & Surgery (AREA)
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- Cardiology (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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| 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 |
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| JP2010504344A JP2010504344A (ja) | 2010-02-12 |
| JP2010504344A5 JP2010504344A5 (enExample) | 2010-10-28 |
| JP5161226B2 true JP5161226B2 (ja) | 2013-03-13 |
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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 |
| PT2350079E (pt) | 2008-10-02 | 2012-12-20 | Lilly Co Eli | Compostos tiazolil-pirazolopirimidina como intermediários de síntese e processos de síntese relacionados |
| 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 |
| LT3096756T (lt) * | 2014-01-21 | 2024-08-26 | Neurocrine Biosciences, Inc. | Crf1 receptoriaus antagonistai, skirti įgimtos antinksčių hiperplazijos gydymui |
| 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 |
| 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 |
| BR112020024062A2 (pt) * | 2018-04-27 | 2021-02-09 | Spruce Biosciences, Inc. | métodos para o tratamento de tumores de restos adrenais de testículo e de ovário |
| 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 |
| FI3984523T3 (fi) | 2018-12-07 | 2025-10-21 | Neurocrine Biosciences Inc | Crf1-reseptorin antagonisti, lääkeformulaatioita ja niiden kiinteitä muotoja synnynnäisen lisämunuaisten liikakasvun hoitoon |
| AU2020318970A1 (en) * | 2019-07-19 | 2022-03-03 | Spruce Biosciences, Inc. | Methods of treating congenital adrenal hyperplasia |
| CA3152590A1 (en) | 2019-09-27 | 2021-04-01 | Evan Smith | Crf receptor antagonists and methods of use |
| WO2021113263A1 (en) * | 2019-12-04 | 2021-06-10 | 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 |
| KR20230043222A (ko) * | 2020-08-12 | 2023-03-30 | 스프루스 바이오사이언시스 인코포레이티드 | 다낭성 난소 증후군을 치료하기 위한 방법 및 조성물 |
| US20240024330A1 (en) | 2020-08-26 | 2024-01-25 | Neurocrine Biosciences, Inc. | Crf receptor antagonists and methods of use |
| JP2024510260A (ja) | 2021-03-19 | 2024-03-06 | クリネティックス ファーマシューティカルズ，インク． | 疾患の治療のためのメラノコルチンサブタイプ－２受容体（ｍｃ２ｒ）アンタゴニスト |
| US11708372B2 (en) | 2021-11-19 | 2023-07-25 | Spruce Biosciences, Inc. | Crystalline composition of tildacerfont and methods of use and preparation thereof |
| WO2023091684A1 (en) * | 2021-11-19 | 2023-05-25 | 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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| WO1994013676A1 (en) | 1992-12-17 | 1994-06-23 | Pfizer Inc. | Pyrrolopyrimidines as crf antagonists |
| TR199800792T2 (xx) * | 1996-02-07 | 1998-07-21 | Janssen Pharmaceutica N.V. | CRF resept�r antagonistleri olarak pirazolopirimidinler. |
| 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 |
| EP0915880B1 (en) | 1996-07-24 | 2007-10-10 | Bristol-Myers Squibb Pharma Company | Azolo triazines and pyrimidines |
| DE69736711T2 (de) | 1996-08-28 | 2007-09-20 | Pfizer Inc. | Substituierte 6,5-heterobicyclische-derivate |
| 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 |
| 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 |
| HRP20030822B1 (en) | 2001-03-13 | 2008-01-31 | 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 |
| CA2550948A1 (en) * | 2003-12-22 | 2005-07-14 | Sb Pharmco Puerto Rico Inc. | Crf receptor antagonists and methods relating thereto |
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| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
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| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |