CN101056862B - 作为选择性雄激素受体调节剂（sarms）的咪唑烷-2-酮衍生物 - Google Patents

作为选择性雄激素受体调节剂（sarms）的咪唑烷-2-酮衍生物 Download PDF

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Publication number
CN101056862B
CN101056862B CN2005800381110A CN200580038111A CN101056862B CN 101056862 B CN101056862 B CN 101056862B CN 2005800381110 A CN2005800381110 A CN 2005800381110A CN 200580038111 A CN200580038111 A CN 200580038111A CN 101056862 B CN101056862 B CN 101056862B
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phenyl
methyl
oxo
alkyl
acid
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Expired - Fee Related
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CN2005800381110A
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Chinese (zh)
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CN101056862A (zh
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J·C·兰特
Z·隋
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/32—One oxygen atom
    • C07D233/34—Ethylene-urea
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16—Masculine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN2005800381110A 2004-09-10 2005-09-09 作为选择性雄激素受体调节剂（sarms）的咪唑烷-2-酮衍生物 Expired - Fee Related CN101056862B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US60915704P 2004-09-10 2004-09-10
US60/609,157 2004-09-10
PCT/US2005/032381 WO2006031715A2 (en) 2004-09-10 2005-09-09 Novel imidazolidin-2-one derivatives as selective androgen receptor modulators (sarms)

Publications (2)

Publication Number Publication Date
CN101056862A CN101056862A (zh) 2007-10-17
CN101056862B true CN101056862B (zh) 2013-03-13

Family

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CN2005800381110A Expired - Fee Related CN101056862B (zh) 2004-09-10 2005-09-09 作为选择性雄激素受体调节剂（sarms）的咪唑烷-2-酮衍生物

Country Status (8)

Country Link
US (2) US7531565B2 (https=)
EP (1) EP1791821B1 (https=)
JP (1) JP5031568B2 (https=)
CN (1) CN101056862B (https=)
AU (1) AU2005285035B2 (https=)
CA (1) CA2579514A1 (https=)
ES (1) ES2422204T3 (https=)
WO (1) WO2006031715A2 (https=)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006055184A2 (en) 2004-11-16 2006-05-26 Janssen Pharmaceutica N.V. Novel heterocycle derivatives useful as selective androgen receptor modulators (sarms)
US7709516B2 (en) * 2005-06-17 2010-05-04 Endorecherche, Inc. Helix 12 directed non-steroidal antiandrogens
CA2678577A1 (en) * 2007-02-26 2008-09-04 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
JP5470557B2 (ja) * 2007-07-26 2014-04-16 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１型の阻害剤の合成
AR069207A1 (es) * 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
US8440658B2 (en) 2007-12-11 2013-05-14 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
TW200934490A (en) * 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
WO2009094169A1 (en) * 2008-01-24 2009-07-30 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2714532A1 (en) * 2008-02-11 2009-08-20 Vitae Pharmaceuticals, Inc. 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
US8598160B2 (en) * 2008-02-15 2013-12-03 Vitae Pharmaceuticals, Inc. Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
WO2009117109A1 (en) * 2008-03-18 2009-09-24 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
EP2291370B1 (en) 2008-05-01 2013-11-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5696037B2 (ja) 2008-05-01 2015-04-08 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
US8242111B2 (en) * 2008-05-01 2012-08-14 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1
RU2531272C2 (ru) 2008-05-01 2014-10-20 Вайтаи Фармасьютиклз, Инк. Циклические ингибиторы 11бета-гидроксистероид-дегидрогеназы 1
WO2010010157A2 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1
NZ590495A (en) 2008-07-25 2012-10-26 Vitae Pharmaceuticals Inc Dihydropyridin-phenyl-3-oxazinan-2-ones as inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2323994A1 (en) 2008-07-25 2011-05-25 Boehringer Ingelheim International GmbH Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
GB2463514C (en) * 2008-09-11 2018-09-26 Galapagos Nv Imidazolidine compounds and uses therefor
JP5679997B2 (ja) 2009-02-04 2015-03-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
TW201039034A (en) * 2009-04-27 2010-11-01 Chunghwa Picture Tubes Ltd Pixel structure and the method of forming the same
GEP20156309B (en) * 2009-04-30 2015-07-10 Vitae Pharmaceuticals Inc Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8680093B2 (en) 2009-04-30 2014-03-25 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8927539B2 (en) 2009-06-11 2015-01-06 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1 based on the 1,3-oxazinan-2-one structure
EP2448928B1 (en) 2009-07-01 2014-08-13 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
TW201124138A (en) * 2009-09-02 2011-07-16 Valletta Health B V Imidazole-4-carboxylic acid for use in treating a disease related to extracellular reactive oxygen species
WO2011056737A1 (en) 2009-11-05 2011-05-12 Boehringer Ingelheim International Gmbh Novel chiral phosphorus ligands
AU2011212813B2 (en) 2010-02-04 2014-10-23 Radius Health, Inc. Selective androgen receptor modulators
HUE030072T2 (en) 2010-05-12 2017-04-28 Radius Health Inc Therapeutic prescriptions
EP2576570A1 (en) 2010-05-26 2013-04-10 Boehringer Ingelheim International GmbH 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives
WO2011159760A1 (en) 2010-06-16 2011-12-22 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
WO2011161128A1 (en) 2010-06-25 2011-12-29 Boehringer Ingelheim International Gmbh Azaspirohexanones as inhibitors of 11-beta-hsd1 for the treatment of metabolic disorders
RU2434851C1 (ru) * 2010-07-22 2011-11-27 Александр Васильевич Иващенко Циклические n, n'-диарилтиомочевины или n, n'-диарилмочевины - антагонисты андрогенных рецепторов, противораковое средство, способ получения и применения
US9133182B2 (en) 2010-09-28 2015-09-15 Radius Health, Inc. Selective androgen receptor modulators
WO2012059416A1 (en) 2010-11-02 2012-05-10 Boehringer Ingelheim International Gmbh Pharmaceutical combinations for the treatment of metabolic disorders
EP2788330A1 (en) * 2011-12-05 2014-10-15 Novartis AG Cyclic urea derivatives as androgen receptor antagonists
MX389702B (es) 2016-06-22 2025-03-20 Ellipses Pharma Ltd Compuestos para usarse en el tratamiento de cancer de mama que expresa el receptor de androgenos (ar+).
CA3099155A1 (en) 2018-05-14 2019-11-21 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
CA3138197A1 (en) 2019-05-14 2020-11-19 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
EP4058464A1 (en) 2019-11-13 2022-09-21 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
MX2023011241A (es) 2021-03-23 2023-10-03 Nuvation Bio Inc Compuestos dirigidos a receptores de hormonas nucleares contra el cancer.
JP2024516024A (ja) 2021-05-03 2024-04-11 ニューベイション・バイオ・インコーポレイテッド 抗がん核内ホルモン受容体標的化化合物

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101103022A (zh) * 2004-02-28 2008-01-09 贝林格尔·英格海姆国际有限公司 用作xa抑制剂的新的羧酸酰胺

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2329276A1 (fr) * 1975-10-29 1977-05-27 Roussel Uclaf Nouvelles imidazolidines substituees, procede de preparation, application comme medicament et compositions les renfermant
TW521073B (en) * 1994-01-05 2003-02-21 Hoechst Marion Roussel Inc New optionally substituted phenylimidazolidines, their preparation process, their use as anti-androgenic agent and the pharmaceutical compositions containing them
FR2715402B1 (fr) * 1994-01-05 1996-10-04 Roussel Uclaf Nouvelles phénylimidazolines éventuellement substituées, leur procédé et des intermédiaires de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant.
FR2724169B1 (fr) * 1994-09-06 1997-01-03 Roussel Uclaf Nouvelles phenylimidazolidines eventuellement substituees, leur procede et des intermediaires de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant
US7371743B2 (en) * 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101103022A (zh) * 2004-02-28 2008-01-09 贝林格尔·英格海姆国际有限公司 用作xa抑制剂的新的羧酸酰胺

Also Published As

Publication number Publication date
WO2006031715A2 (en) 2006-03-23
AU2005285035A1 (en) 2006-03-23
JP5031568B2 (ja) 2012-09-19
ES2422204T3 (es) 2013-09-09
EP1791821B1 (en) 2013-06-05
WO2006031715A3 (en) 2006-07-20
CA2579514A1 (en) 2006-03-23
US7968580B2 (en) 2011-06-28
US20090215848A1 (en) 2009-08-27
AU2005285035B2 (en) 2012-03-22
JP2008512492A (ja) 2008-04-24
US20060063819A1 (en) 2006-03-23
CN101056862A (zh) 2007-10-17
US7531565B2 (en) 2009-05-12
EP1791821A2 (en) 2007-06-06

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