CN101528707A - 用作糖皮质激素受体配体的2-[1-苯基-5-羟基或甲氧基-4α-甲基-六氢环戊[f]吲唑-5-基]乙基苯基衍生物 - Google Patents
用作糖皮质激素受体配体的2-[1-苯基-5-羟基或甲氧基-4α-甲基-六氢环戊[f]吲唑-5-基]乙基苯基衍生物 Download PDFInfo
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- CN101528707A CN101528707A CNA2007800392434A CN200780039243A CN101528707A CN 101528707 A CN101528707 A CN 101528707A CN A2007800392434 A CNA2007800392434 A CN A2007800392434A CN 200780039243 A CN200780039243 A CN 200780039243A CN 101528707 A CN101528707 A CN 101528707A
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- ethyl
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- indazole
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Abstract
Description
底物 | MW | 量 | mmol | 当量 |
1 | 164 | 15g | 91.46 | 1.0 |
TMS炔 | 98 | 13g | 132.62 | 1.45 |
iPrMgCl(1.8M THF溶液) | 71.14mL | 128.05 | 1.4 | |
CeCl3 | 246 | 31.6g | 128.05 | 1.4 |
THF | 50+150+45mL |
行 | 试剂 | FW | 量 | mMol |
1 | 炔4 | 308.35 | 9.87gA | 32.0 |
2 | 溴化物5 | 218.02 | 7.67g | 35.2 |
3 | 哌啶 | 85.15 | 6.39mL | 64.0 |
4 | [(烯丙基)PdCl]2 | 365.89 | 58.8mgA | 0.160 |
5 | (t-Bu)3P.HBF4 | 290.13 | 232mgA | 0.800 |
6 | CH3CN | 41.05 | 50mL | |
8 | 甲苯 | 92.14 | 100mL |
Claims (23)
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US85365506P | 2006-10-23 | 2006-10-23 | |
US60/853,655 | 2006-10-23 | ||
US92333707P | 2007-04-13 | 2007-04-13 | |
US60/923,337 | 2007-04-13 | ||
PCT/US2007/022463 WO2008051532A1 (en) | 2006-10-23 | 2007-10-23 | 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydroclopenta[f]indazol-5-yl]ethyl phenyl derivatives as glucocorticoid receptor ligands |
Publications (2)
Publication Number | Publication Date |
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CN101528707A true CN101528707A (zh) | 2009-09-09 |
CN101528707B CN101528707B (zh) | 2012-11-07 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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CN2007800392434A Expired - Fee Related CN101528707B (zh) | 2006-10-23 | 2007-10-23 | 用作糖皮质激素受体配体的2-[1-苯基-5-羟基或甲氧基-4α-甲基-六氢环戊二烯并[f]吲唑-5-基]乙基苯基衍生物 |
Country Status (19)
Country | Link |
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US (1) | US8119681B2 (zh) |
EP (2) | EP2097385B1 (zh) |
JP (1) | JP5271911B2 (zh) |
KR (1) | KR20090068345A (zh) |
CN (1) | CN101528707B (zh) |
AT (1) | ATE538099T1 (zh) |
AU (1) | AU2007309507A1 (zh) |
BR (1) | BRPI0718505A2 (zh) |
CA (1) | CA2667007A1 (zh) |
CO (1) | CO6190517A2 (zh) |
CR (1) | CR10771A (zh) |
EA (1) | EA200970401A1 (zh) |
IL (1) | IL198226A0 (zh) |
MA (1) | MA30870B1 (zh) |
MX (1) | MX2009004385A (zh) |
NO (1) | NO20092004L (zh) |
SV (1) | SV2009003233A (zh) |
TN (1) | TN2009000149A1 (zh) |
WO (2) | WO2008060391A2 (zh) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW200829578A (en) | 2006-11-23 | 2008-07-16 | Astrazeneca Ab | Chemical compounds 537 |
JO2754B1 (en) | 2006-12-21 | 2014-03-15 | استرازينكا ايه بي | Amylendazoleil derivatives for the treatment of glucocorticoid-mediated disorders |
US20100261693A1 (en) * | 2007-10-17 | 2010-10-14 | Ulmann Andre | Method for treating cushing's syndrome |
US20100228036A1 (en) * | 2007-10-23 | 2010-09-09 | Qinghao Chen | Process for making glucocorticoid receptor ligands |
TWI445705B (zh) | 2008-05-20 | 2014-07-21 | Astrazeneca Ab | 經苯基及苯并二基取代之吲唑衍生物 |
WO2010138421A1 (en) * | 2009-05-27 | 2010-12-02 | Merck Sharp & Dohme Corp. | HEXAHYDROCYCLOPENTYL[f]INDAZOLE REVERSED AMIDES AND DERIVATIVES AS SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS |
WO2010141247A1 (en) | 2009-06-02 | 2010-12-09 | Merck Sharp & Dohme Corp. | Hexahydrocyclopentyl[∫]indazole 5-hydroxymethyl ethanols and derivatives thereof as selective glucocorticoid receptor modulators |
EP2482659A4 (en) * | 2009-09-08 | 2013-03-27 | Merck Sharp & Dohme | HEXAHYDROCYCLOPENTA [F] INDAZOLE 5-YLE ETHANOLS AND DERIVATIVES THEREOF AS SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS |
EP2493303A4 (en) * | 2009-10-30 | 2013-06-26 | Merck Sharp & Dohme | 2- [1-PHENYL-5-HYDROXY-4A-SUBSTITUTED HEXAHYDROCYCLOPENTA [F] INDAZOL-5-YL] ETHYLPHENYL DERIVATIVES AS GLUCOCORTICOID RECEPTOR LIGANDS |
CN104135859B (zh) | 2011-12-28 | 2017-06-27 | 全球血液疗法公司 | 取代的苯甲醛化合物及其用于增加组织氧合的方法 |
WO2013102145A1 (en) | 2011-12-28 | 2013-07-04 | Global Blood Therapeutics, Inc. | Substituted heteroaryl aldehyde compounds and methods for their use in increasing tissue oxygenation |
US9604999B2 (en) | 2013-03-15 | 2017-03-28 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
SG11201507453VA (en) | 2013-03-15 | 2015-10-29 | Global Blood Therapeutics Inc | Compounds and uses thereof for the modulation of hemoglobin |
US9458139B2 (en) | 2013-03-15 | 2016-10-04 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
US9422279B2 (en) | 2013-03-15 | 2016-08-23 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
US8952171B2 (en) | 2013-03-15 | 2015-02-10 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
JP6463327B2 (ja) | 2013-03-15 | 2019-01-30 | グローバル ブラッド セラピューティクス インコーポレイテッド | ヘモグロビンの修飾のための化合物及びその使用 |
US10266551B2 (en) | 2013-03-15 | 2019-04-23 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
US10100043B2 (en) | 2013-03-15 | 2018-10-16 | Global Blood Therapeutics, Inc. | Substituted aldehyde compounds and methods for their use in increasing tissue oxygenation |
US20140274961A1 (en) | 2013-03-15 | 2014-09-18 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
JP6426694B2 (ja) | 2013-03-15 | 2018-11-21 | グローバル ブラッド セラピューティクス インコーポレイテッド | ヘモグロビンの修飾のための化合物及びその使用 |
US9802900B2 (en) | 2013-03-15 | 2017-10-31 | Global Blood Therapeutics, Inc. | Bicyclic heteroaryl compounds and uses thereof for the modulation of hemoglobin |
EA201992707A1 (ru) | 2013-11-18 | 2020-06-30 | Глобал Блад Терапьютикс, Инк. | Соединения и их применения для модуляции гемоглобина |
DK3102208T4 (da) | 2014-02-07 | 2024-08-26 | Global Blood Therapeutics Inc | Krystallinsk polymorph af den frie base af 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyd |
MA41841A (fr) | 2015-03-30 | 2018-02-06 | Global Blood Therapeutics Inc | Composés aldéhyde pour le traitement de la fibrose pulmonaire, de l'hypoxie, et de maladies auto-immunes et des tissus conjonctifs |
ES2865334T3 (es) | 2015-08-13 | 2021-10-15 | Corcept Therapeutics Inc | Método de diagnóstico diferencial de síndrome de Cushing dependiente de ACTH |
EP3383392A1 (en) | 2015-12-04 | 2018-10-10 | Global Blood Therapeutics, Inc. | Dosing regimens for 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde |
KR102197526B1 (ko) | 2016-01-19 | 2020-12-31 | 코어셉트 쎄라퓨틱스 인코포레이티드 | 이소성 쿠싱 증후군의 감별 진단 |
TWI752307B (zh) | 2016-05-12 | 2022-01-11 | 美商全球血液治療公司 | 新穎化合物及製造化合物之方法 |
TWI778983B (zh) | 2016-10-12 | 2022-10-01 | 美商全球血液治療公司 | 包含2-羥基-6-((2-(1-異丙基-1h-吡唑-5-基)吡啶-3-基)甲氧基)-苯甲醛之片劑 |
US10195214B2 (en) | 2017-03-01 | 2019-02-05 | Corcept Therapeutics, Inc. | Concomitant administration of glucocorticoid receptor modulators and CYP3A inhibitors |
EP3860975B1 (en) | 2018-10-01 | 2023-10-18 | Global Blood Therapeutics, Inc. | Modulators of hemoglobin for the treatment of sickle cell disease |
US20220227729A1 (en) | 2019-05-21 | 2022-07-21 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
WO2021242912A1 (en) | 2020-05-27 | 2021-12-02 | Corcept Therapeutics Incorporated | Concomitant administration of glucocorticoid receptor modulator relacorilant and paclitaxel, a dual substrate of cyp2c8 and cyp3a4 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6846839B1 (en) * | 1995-06-07 | 2005-01-25 | Sugen, Inc. | Methods for treating diseases and disorders related to unregulated angiogenesis and/or vasculogenesis |
US6831093B2 (en) | 2002-01-22 | 2004-12-14 | The Regents Of The University Of California | Non-steroidal ligands for the glucocorticoid receptor, compositions and uses thereof |
DE60335869D1 (de) * | 2002-04-11 | 2011-03-10 | Merck Sharp & Dohme | 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren |
US7411073B2 (en) * | 2003-02-25 | 2008-08-12 | Merck & Co., Inc. | Selective non-steroidal glucocorticoid receptor modulators |
JP4739191B2 (ja) * | 2003-04-23 | 2011-08-03 | メルク・シャープ・エンド・ドーム・コーポレイション | 選択的スピロ環式グルココルチコイド受容体調節物質 |
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WO2008060391A2 (en) | 2008-05-22 |
BRPI0718505A2 (pt) | 2013-11-12 |
AU2007309507A1 (en) | 2008-05-02 |
WO2008051532A1 (en) | 2008-05-02 |
MX2009004385A (es) | 2009-05-22 |
CO6190517A2 (es) | 2010-08-19 |
SV2009003233A (es) | 2009-10-19 |
EA200970401A1 (ru) | 2009-10-30 |
IL198226A0 (en) | 2009-12-24 |
JP2010507663A (ja) | 2010-03-11 |
CR10771A (es) | 2009-05-25 |
TN2009000149A1 (en) | 2010-10-18 |
WO2008060391A3 (en) | 2008-09-25 |
CA2667007A1 (en) | 2008-05-02 |
EP2091922B1 (en) | 2011-12-21 |
EP2097385A1 (en) | 2009-09-09 |
EP2097385B1 (en) | 2012-08-01 |
JP5271911B2 (ja) | 2013-08-21 |
EP2091922A2 (en) | 2009-08-26 |
MA30870B1 (fr) | 2009-11-02 |
US20100311709A1 (en) | 2010-12-09 |
ATE538099T1 (de) | 2012-01-15 |
US8119681B2 (en) | 2012-02-21 |
KR20090068345A (ko) | 2009-06-26 |
CN101528707B (zh) | 2012-11-07 |
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