WO2004075840A2 - Selective non-steroidal glucocorticoid receptor modulators - Google Patents

Selective non-steroidal glucocorticoid receptor modulators Download PDF

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Publication number
WO2004075840A2
WO2004075840A2 PCT/US2004/005199 US2004005199W WO2004075840A2 WO 2004075840 A2 WO2004075840 A2 WO 2004075840A2 US 2004005199 W US2004005199 W US 2004005199W WO 2004075840 A2 WO2004075840 A2 WO 2004075840A2
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PCT/US2004/005199
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English (en)
French (fr)
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WO2004075840A9 (en
WO2004075840A3 (en
Inventor
Amjad Ali
Richard Beresis
Steven L. Colletti
Donald W. Graham
James R. Tata
Christopher F. Thompson
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Merck and Co Inc
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Merck and Co Inc
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Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Priority to AT04713398T priority Critical patent/ATE464296T1/de
Priority to DE602004026558T priority patent/DE602004026558D1/de
Priority to US10/544,899 priority patent/US7411073B2/en
Priority to JP2006503780A priority patent/JP4648303B2/ja
Priority to CA002516684A priority patent/CA2516684A1/en
Priority to EP04713398A priority patent/EP1599201B1/en
Priority to AU2004216182A priority patent/AU2004216182B2/en
Publication of WO2004075840A2 publication Critical patent/WO2004075840A2/en
Publication of WO2004075840A3 publication Critical patent/WO2004075840A3/en
Publication of WO2004075840A9 publication Critical patent/WO2004075840A9/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
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    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
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    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

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PCT/US2004/005199 2003-02-25 2004-02-20 Selective non-steroidal glucocorticoid receptor modulators Ceased WO2004075840A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
AT04713398T ATE464296T1 (de) 2003-02-25 2004-02-20 Selektive nichtsteroidale glucocorticoid-rezeptor-modulatoren
DE602004026558T DE602004026558D1 (de) 2003-02-25 2004-02-20 Selektive nichtsteroidale glucocorticoid-rezeptor- modulatoren
US10/544,899 US7411073B2 (en) 2003-02-25 2004-02-20 Selective non-steroidal glucocorticoid receptor modulators
JP2006503780A JP4648303B2 (ja) 2003-02-25 2004-02-20 選択的非ステロイド系糖質コルチコイド受容体調節剤
CA002516684A CA2516684A1 (en) 2003-02-25 2004-02-20 Selective non-steroidal glucocorticoid receptor modulators
EP04713398A EP1599201B1 (en) 2003-02-25 2004-02-20 Selective non-steroidal glucocorticoid receptor modulators
AU2004216182A AU2004216182B2 (en) 2003-02-25 2004-02-20 Selective non-steroidal glucocorticoid receptor modulators

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US45081103P 2003-02-25 2003-02-25
US60/450,811 2003-02-25

Publications (3)

Publication Number Publication Date
WO2004075840A2 true WO2004075840A2 (en) 2004-09-10
WO2004075840A3 WO2004075840A3 (en) 2005-02-03
WO2004075840A9 WO2004075840A9 (en) 2005-08-04

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PCT/US2004/005199 Ceased WO2004075840A2 (en) 2003-02-25 2004-02-20 Selective non-steroidal glucocorticoid receptor modulators

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US (1) US7411073B2 (enExample)
EP (1) EP1599201B1 (enExample)
JP (1) JP4648303B2 (enExample)
AT (1) ATE464296T1 (enExample)
AU (1) AU2004216182B2 (enExample)
CA (1) CA2516684A1 (enExample)
DE (1) DE602004026558D1 (enExample)
WO (1) WO2004075840A2 (enExample)

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1617806A4 (en) * 2003-04-23 2006-11-02 Merck & Co Inc SELECTIVE SPIROCYCLIC GLUCOCORTICOID RECEPTOR MODULATORS
WO2006138373A2 (en) 2005-06-14 2006-12-28 Bristol-Myers Squibb Company MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
WO2008051532A1 (en) * 2006-10-23 2008-05-02 Merck & Co., Inc. 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydroclopenta[f]indazol-5-yl]ethyl phenyl derivatives as glucocorticoid receptor ligands
JP2009506077A (ja) * 2005-08-26 2009-02-12 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 非ステロイド性抗アンドロゲン剤
WO2009054925A1 (en) * 2007-10-23 2009-04-30 Merck & Co., Inc. Process for making glucocorticoid receptor ligands
EP2268630A4 (en) * 2008-02-26 2011-03-09 Merck Sharp & Dohme HEXAHYDROCYCLOPENTYL [F] INDAZOLCARBOXYL ACID AMIDES AND THEIR DERIVATIVES AS SELECTIVE MODULATORS OF THE GLUCOCORTICOID RECEPTOR
EP2482659A4 (en) * 2009-09-08 2013-03-27 Merck Sharp & Dohme HEXAHYDROCYCLOPENTA [F] INDAZOL-5-YL ETHANOLS AND DERIVATIVES THEREOF AS SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS
EP2493302A4 (en) * 2009-10-30 2013-04-24 Merck Sharp & Dohme HEXAHYDROCYCLOPENTYL- [F-] INDAZOLE-PYRIDYL 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
WO2018191283A1 (en) * 2017-04-11 2018-10-18 Oric Pharmaceuticals, Inc. Glucocorticoid receptor modulators
WO2020076999A1 (en) * 2018-10-10 2020-04-16 Oric Pharmaceuticals, Inc. Glucocorticoid receptor modulators
WO2020152193A1 (en) 2019-01-22 2020-07-30 Akribes Biomedical Gmbh Selective glucocorticoid receptor modifiers for treating impaired skin wound healing
CN112771046A (zh) * 2018-07-20 2021-05-07 格吕伦塔尔有限公司 其他被取代的三唑并喹喔啉衍生物
US12496304B2 (en) 2019-01-22 2025-12-16 Akribes Biomedical Gmbh Selective glucocorticoid receptor modifiers for treating impaired skin wound healing

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1467730A4 (en) * 2002-01-22 2010-03-10 Univ California Non-steroid ligands for the glucocorticoid receptor, compositions and uses thereof
CA2481320A1 (en) * 2002-04-11 2003-10-23 Merck & Co., Inc. 1h-benzo[f]indazol-5-yl derivatives as selective glucocorticoid receptor modulators
TW201422590A (zh) 2012-09-07 2014-06-16 Abbvie Inc 雜環核激素受體調節劑
WO2014094357A1 (en) 2012-12-21 2014-06-26 Abbvie Inc. Heterocyclic nuclear hormone receptor modulators

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4349559A (en) 1981-02-19 1982-09-14 Sterling Drug Inc. Anti-inflammatory spiro-2H-indene-[2,3']-3H-pyrazolo[4",5":7',6']naphtho[2,1-b]pyran-1,3-dione derivatives
WO2003086294A2 (en) 2002-04-11 2003-10-23 Merck & Co., Inc. 1h-benzo[f]indazol-5-yl derivatives as selective glucocorticoid receptor modulators

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3932388A (en) * 1974-04-22 1976-01-13 Schering Corporation -Azido-4,6-pregnadieno(3,2-c)pyrazoles, processes for their preparation and intermediates useful therein
US4307102A (en) 1981-02-19 1981-12-22 Sterling Drug Inc. Phenanthro[2,3-c]pyrazole
EP0058841B1 (en) 1981-02-19 1984-12-12 Sterling Drug Inc. Phenylpyrazole compounds useful as anti-inflammatory agents and preparation thereof
US4349558A (en) 1981-02-19 1982-09-14 Sterling Drug Inc. Anti-inflammatory 8H-phenanthro-[2,3-c]pyrazole derivatives
EP1467730A4 (en) * 2002-01-22 2010-03-10 Univ California Non-steroid ligands for the glucocorticoid receptor, compositions and uses thereof
US20050245588A1 (en) 2002-09-20 2005-11-03 Amjad Ali Octahydro-2-h-naphtho[1,2-f]indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4349559A (en) 1981-02-19 1982-09-14 Sterling Drug Inc. Anti-inflammatory spiro-2H-indene-[2,3']-3H-pyrazolo[4",5":7',6']naphtho[2,1-b]pyran-1,3-dione derivatives
WO2003086294A2 (en) 2002-04-11 2003-10-23 Merck & Co., Inc. 1h-benzo[f]indazol-5-yl derivatives as selective glucocorticoid receptor modulators

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
"Recent Advances in Glucocorticoid Receptor Action", 2002, SPRINGER-VERLAG: BERLIN-HEIDELBERG
COGHLAN, M.J. ET AL.: "Annual Reports in Medicinal Chemistry", vol. 37, 2002, ACADEMIC PRESS, pages: 167 - 176

Cited By (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7662846B2 (en) 2003-04-23 2010-02-16 Merck Sharp & Dohme Corp. Selective spirocyclic glucocorticoid receptor modulators
EP1617806A4 (en) * 2003-04-23 2006-11-02 Merck & Co Inc SELECTIVE SPIROCYCLIC GLUCOCORTICOID RECEPTOR MODULATORS
WO2006138373A2 (en) 2005-06-14 2006-12-28 Bristol-Myers Squibb Company MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
US7888381B2 (en) 2005-06-14 2011-02-15 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity, and use thereof
JP2009506077A (ja) * 2005-08-26 2009-02-12 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 非ステロイド性抗アンドロゲン剤
US7645885B2 (en) 2005-08-26 2010-01-12 The Regents Of The University Of California Non-steroidal antiandrogens
EP1916896A4 (en) * 2005-08-26 2010-08-11 Univ California NOT STEROID-antiandrogens
US8119681B2 (en) 2006-10-23 2012-02-21 Merck Sharp & Dohme Corp. 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta [ƒ]indazole-5-YL]ethyl phenyl derivatives as glucocorticoid receptor ligands
WO2008051532A1 (en) * 2006-10-23 2008-05-02 Merck & Co., Inc. 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydroclopenta[f]indazol-5-yl]ethyl phenyl derivatives as glucocorticoid receptor ligands
WO2008060391A3 (en) * 2006-10-23 2008-09-25 Merck & Co Inc 2- [l-phenyl-5-hydr0xy-4alpha-methyl-hexahydr0cycl0penta[f] indaz0l-5-yl] ethyl phenyl derivatives as glucocorticoid receptor ligands
WO2009054925A1 (en) * 2007-10-23 2009-04-30 Merck & Co., Inc. Process for making glucocorticoid receptor ligands
EP2268630A4 (en) * 2008-02-26 2011-03-09 Merck Sharp & Dohme HEXAHYDROCYCLOPENTYL [F] INDAZOLCARBOXYL ACID AMIDES AND THEIR DERIVATIVES AS SELECTIVE MODULATORS OF THE GLUCOCORTICOID RECEPTOR
US8338472B2 (en) 2008-02-26 2012-12-25 Merck Sharp & Dohme Corp. Hexahydrocyclopentyl[F]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor modulators
EP2482659A4 (en) * 2009-09-08 2013-03-27 Merck Sharp & Dohme HEXAHYDROCYCLOPENTA [F] INDAZOL-5-YL ETHANOLS AND DERIVATIVES THEREOF AS SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS
EP2493302A4 (en) * 2009-10-30 2013-04-24 Merck Sharp & Dohme HEXAHYDROCYCLOPENTYL- [F-] INDAZOLE-PYRIDYL 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
WO2018191283A1 (en) * 2017-04-11 2018-10-18 Oric Pharmaceuticals, Inc. Glucocorticoid receptor modulators
CN112771046A (zh) * 2018-07-20 2021-05-07 格吕伦塔尔有限公司 其他被取代的三唑并喹喔啉衍生物
CN112771046B (zh) * 2018-07-20 2023-09-19 格吕伦塔尔有限公司 其他被取代的三唑并喹喔啉衍生物
US11981677B2 (en) 2018-07-20 2024-05-14 Grünenthal GmbH Further substituted triazolo quinoxaline derivatives
WO2020076999A1 (en) * 2018-10-10 2020-04-16 Oric Pharmaceuticals, Inc. Glucocorticoid receptor modulators
WO2020152193A1 (en) 2019-01-22 2020-07-30 Akribes Biomedical Gmbh Selective glucocorticoid receptor modifiers for treating impaired skin wound healing
US12496304B2 (en) 2019-01-22 2025-12-16 Akribes Biomedical Gmbh Selective glucocorticoid receptor modifiers for treating impaired skin wound healing

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US20060074120A1 (en) 2006-04-06
WO2004075840A9 (en) 2005-08-04
WO2004075840A3 (en) 2005-02-03
ATE464296T1 (de) 2010-04-15
EP1599201A4 (en) 2007-01-24
EP1599201A2 (en) 2005-11-30
EP1599201B1 (en) 2010-04-14
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