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
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- 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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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Pain & Pain Management (AREA)
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- Endocrinology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Urology & Nephrology (AREA)
- Anesthesiology (AREA)
- Child & Adolescent Psychology (AREA)
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- Cardiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- 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 |
Publications (3)
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| JP2010504344A JP2010504344A (ja) | 2010-02-12 |
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Families Citing this family (23)
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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 |
| 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 |
| JP6585625B2 (ja) * | 2014-01-21 | 2019-10-02 | 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 | 先天性副腎皮質過形成の処置のためのｃｒｆ１レセプターアンタゴニスト |
| 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 |
| KR102571296B1 (ko) | 2016-09-07 | 2023-08-28 | 더 리전트 오브 더 유니버시티 오브 캘리포니아 | P-tau를 감소시키고 인지를 개선하는 알로스테릭 코르티코트로핀-방출 인자 수용체 1 (crfr1) 길항제 |
| KR20250022913A (ko) | 2017-08-14 | 2025-02-17 | 스프루스 바이오사이언시스 인코포레이티드 | 코티코트로핀 방출 인자 수용체 길항제 |
| MX2019015318A (es) * | 2017-08-14 | 2020-07-20 | Spruce Biosciences Inc | Antagonistas del receptor del factor liberador 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 |
| 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 |
| TW202116324A (zh) * | 2019-07-19 | 2021-05-01 | 美商雲杉生物科技股份有限公司 | 治療先天性腎上腺增生之方法 |
| CN114502162B (zh) | 2019-09-27 | 2025-03-28 | 纽罗克里生物科学有限公司 | Crf受体拮抗剂及使用方法 |
| US20230065034A1 (en) * | 2019-12-04 | 2023-03-02 | 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 |
| MX2023001688A (es) * | 2020-08-12 | 2023-02-22 | Spruce Biosciences Inc | Metodos y composiciones para tratar el sindrome de ovario poliquistico. |
| US20240024330A1 (en) | 2020-08-26 | 2024-01-25 | Neurocrine Biosciences, Inc. | Crf receptor antagonists and methods of use |
| IL305952A (en) | 2021-03-19 | 2023-11-01 | Crinetics Pharmaceuticals Inc | Melanocortin subtype 2 receptor (MC2R) antagonist for disease treatment |
| 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 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
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| ES2128544T3 (es) | 1992-12-17 | 1999-05-16 | Pfizer | Pirrolopirimidinas como antagonistas del crf. |
| WO1997029109A1 (en) * | 1996-02-07 | 1997-08-14 | Janssen Pharmaceutica N.V. | Pyrazolopyrimidines as crf receptor antagonists |
| 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 |
| HU229024B1 (en) | 1996-07-24 | 2013-07-29 | Bristol Myers Squibb Pharma Co | Azolo-pyridimidines, pharmaceutical compositions containing the same and use thereof |
| TR199900389T2 (xx) | 1996-08-28 | 2000-06-21 | Pfizer Inc. | �kame edilmi� 6,5-hetero-bisiklik t�revleri. |
| 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 |
| JP4549630B2 (ja) | 2001-03-13 | 2010-09-22 | ブリストル−マイヤーズ スクイブ ファーマ カンパニー | コルチコトロピン放出因子受容体リガンドとしての、４−（２−ブチルアミノ）−２，７−ジメチル−８−（２−メチル−６−メトキシピリド−３−イル）ピラゾロ−［１，５−ａ］−１，３，５−トリアジン、その鏡像異性体および薬学的に許容できる塩類 |
| NZ547990A (en) * | 2003-12-22 | 2010-04-30 | Smithkline Beecham Cork Ltd | CRF receptor antagonists and methods relating thereto |
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