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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- C07D487/00—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
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- 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
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Landscapes
- 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)
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2010504344A JP2010504344A (ja) | 2010-02-12 |
| JP2010504344A5 JP2010504344A5 (https=) | 2010-10-28 |
| JP5161226B2 true JP5161226B2 (ja) | 2013-03-13 |
Family
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| JP2009529316A Active JP5161226B2 (ja) | 2006-09-20 | 2007-09-17 | 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 |
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| EP (1) | EP2094709B1 (https=) |
| JP (1) | JP5161226B2 (https=) |
| KR (1) | KR101088239B1 (https=) |
| CN (1) | CN101516887B (https=) |
| AR (1) | AR062886A1 (https=) |
| AT (1) | ATE481405T1 (https=) |
| AU (1) | AU2007297421B2 (https=) |
| BR (1) | BRPI0717023B8 (https=) |
| CA (1) | CA2663511C (https=) |
| CL (1) | CL2007002693A1 (https=) |
| CR (1) | CR10682A (https=) |
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| MA (1) | MA30798B1 (https=) |
| MX (1) | MX2009003125A (https=) |
| MY (1) | MY146388A (https=) |
| NO (1) | NO20091489L (https=) |
| NZ (1) | NZ575572A (https=) |
| PE (1) | PE20081377A1 (https=) |
| PL (1) | PL2094709T3 (https=) |
| PT (1) | PT2094709E (https=) |
| RS (1) | RS51545B (https=) |
| SI (1) | SI2094709T1 (https=) |
| TN (1) | TN2009000095A1 (https=) |
| TW (1) | TWI402269B (https=) |
| UA (1) | UA96458C2 (https=) |
| WO (1) | WO2008036579A1 (https=) |
Families Citing this family (23)
| 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 |
| WO2010039678A1 (en) * | 2008-10-02 | 2010-04-08 | 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 |
| WO2015112642A1 (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 |
| 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 |
| EA202090321A1 (ru) * | 2017-08-14 | 2020-09-24 | Спрюс Биосайнсес, Инк. | Антагонисты рецептора кортикотропин-рилизинг фактора |
| CN118845788A (zh) | 2017-08-14 | 2024-10-29 | 云杉生物科学公司 | 促肾上腺皮质激素释放因子受体拮抗剂 |
| EP4438124A3 (en) | 2018-04-27 | 2024-12-18 | 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 |
| CA3121920A1 (en) | 2018-12-07 | 2020-06-11 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia |
| 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 |
| JP7623365B2 (ja) | 2019-09-27 | 2025-01-28 | 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 | Ｃｒｆ受容体アンタゴニストおよび使用方法 |
| 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 |
| BR112023002497A2 (pt) * | 2020-08-12 | 2023-05-02 | Spruce Biosciences Inc | Métodos e composições para tratamento da síndrome dos ovários policísticos |
| JP2023540223A (ja) | 2020-08-26 | 2023-09-22 | 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 | Ｃｒｆ受容体アンタゴニストおよび使用方法 |
| 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 |
| MX2024006064A (es) * | 2021-11-19 | 2024-05-30 | Spruce Biosciences Inc | Composicion cristalina de tildacerfont y metodos de uso y preparacion de la misma. |
| 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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| ATE177101T1 (de) | 1992-12-17 | 1999-03-15 | Pfizer | Pyrrolopyrimidine als crf antagonisten |
| JP3356291B2 (ja) * | 1996-02-07 | 2002-12-16 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Ｃｒｆレセプター拮抗薬としてのピラゾロピリミジン類 |
| HU228962B1 (en) | 1996-07-24 | 2013-07-29 | Bristol Myers Squibb Pharma Co | Azolo triazines, pharmaceutical compositions containing them and use of the compounds |
| IL127871A0 (en) * | 1996-07-24 | 1999-10-28 | Du Pont Pharm Co | Azolo triazines and pyrimidines |
| IL127566A0 (en) | 1996-08-28 | 1999-10-28 | Pfizer | 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 |
| WO2000059908A2 (en) * | 1999-04-06 | 2000-10-12 | Du Pont Pharmaceuticals Company | Pyrazolopyrimidines as crf antagonists |
| EP1218381B1 (en) | 1999-09-30 | 2006-12-06 | Neurogen Corporation | AMINO SUBSTITUTED PYRAZOLO¬1,5-a|-1,5-PYRIMIDINES AND PYRAZOLO¬1,5-a|-1,3,5-TRIAZINES |
| BR0208357A (pt) | 2001-03-13 | 2004-06-29 | Bristol Myers Squibb Pharma Co | Composto, composição farmacêutica, método de antagonização de um receptor de fator de liberação de corticotropina (crf), método de tratamento de disfunção, método de triagem de ligantes, método de detecção de receptores de crf, método de inibição da ligação de crf, artigo industrializado e usos do composto |
| CA2550948A1 (en) * | 2003-12-22 | 2005-07-14 | Sb Pharmco Puerto Rico Inc. | Crf receptor antagonists and methods relating thereto |
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