CA2516684A1 - Selective non-steroidal glucocorticoid receptor modulators - Google Patents

Selective non-steroidal glucocorticoid receptor modulators Download PDF

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Publication number
CA2516684A1
CA2516684A1 CA002516684A CA2516684A CA2516684A1 CA 2516684 A1 CA2516684 A1 CA 2516684A1 CA 002516684 A CA002516684 A CA 002516684A CA 2516684 A CA2516684 A CA 2516684A CA 2516684 A1 CA2516684 A1 CA 2516684A1
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group
independently selected
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CA002516684A
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English (en)
French (fr)
Inventor
Amjad Ali
Richard Beresis
Steven L. Colletti
Donald W. Graham
James R. Tata
Christopher F. Thompson
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Merck Sharp and Dohme LLC
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/04Antipruritics
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/06Antipsoriatics
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
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    • A61P17/00Drugs for dermatological disorders
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    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/06Antihyperlipidemics
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    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
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    • AHUMAN NECESSITIES
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
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    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • A61P35/00Antineoplastic agents
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D409/04Heterocyclic 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Anesthesiology (AREA)
  • Communicable Diseases (AREA)
  • Child & Adolescent Psychology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
CA002516684A 2003-02-25 2004-02-20 Selective non-steroidal glucocorticoid receptor modulators Abandoned CA2516684A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US45081103P 2003-02-25 2003-02-25
US60/450,811 2003-02-25
PCT/US2004/005199 WO2004075840A2 (en) 2003-02-25 2004-02-20 Selective non-steroidal glucocorticoid receptor modulators

Publications (1)

Publication Number Publication Date
CA2516684A1 true CA2516684A1 (en) 2004-09-10

Family

ID=32927681

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002516684A Abandoned CA2516684A1 (en) 2003-02-25 2004-02-20 Selective non-steroidal glucocorticoid receptor modulators

Country Status (8)

Country Link
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)

Families Citing this family (17)

* 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
CA2522946A1 (en) 2003-04-23 2004-11-04 Merck & Co., Inc. Selective spirocyclic glucocorticoid receptor modulators
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
WO2007025303A2 (en) * 2005-08-26 2007-03-01 The Regents Of The University Of California Non-steroidal antiandrogens
WO2008060391A2 (en) 2006-10-23 2008-05-22 Merck & Co., Inc. 2- [l-phenyl-5-hydr0xy-4alpha-methyl-hexahydr0cycl0penta[f] indaz0l-5-yl] ethyl phenyl derivatives as glucocorticoid receptor ligands
JP2011500804A (ja) * 2007-10-23 2011-01-06 メルク・シャープ・エンド・ドーム・コーポレイション グルココルチコイド受容体リガンドの製造方法
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
WO2011053574A1 (en) * 2009-10-30 2011-05-05 Merck Sharp & Dohme Corp. 2- [1-PHENYL-5-HYDROXY-4a-SUBSTITUTED-HEXAHYDROCYCLOPENTA [F] INDAZOL-5-YL] ETHYL PHENYL DERIVATIVES AS GLUCOCORTICOID RECEPTOR LIGANDS
TW201118073A (en) * 2009-10-30 2011-06-01 Merck Sharp & Dohme Hexahydrocyclopentyl [F] indazole pyridyl ethanols and derivatives thereof 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
WO2018191283A1 (en) * 2017-04-11 2018-10-18 Oric Pharmaceuticals, Inc. Glucocorticoid receptor modulators
US10981918B2 (en) 2018-07-20 2021-04-20 Grünenthal GmbH Further substituted triazolo quinoxaline derivatives
US20220079924A1 (en) * 2018-10-10 2022-03-17 Oric Pharmaceuticals, Inc. Glucocorticoid receptor modulators
CA3123490A1 (en) 2019-01-22 2020-07-30 Akribes Biomedical Gmbh Selective glucocorticoid receptor modifiers for treating impaired skin wound healing

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* 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
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
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
CA2481320A1 (en) * 2002-04-11 2003-10-23 Merck & Co., Inc. 1h-benzo[f]indazol-5-yl derivatives as selective glucocorticoid receptor modulators
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

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Publication number Publication date
WO2004075840A2 (en) 2004-09-10
JP4648303B2 (ja) 2011-03-09
JP2006518752A (ja) 2006-08-17
AU2004216182A1 (en) 2004-09-10
DE602004026558D1 (de) 2010-05-27
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
AU2004216182B2 (en) 2008-11-20
US7411073B2 (en) 2008-08-12

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