JP5031568B2 - 選択的アンドロゲン受容体モジュレーター（ｓａｒｍｓ）としての新規なイミダゾリジン−２−オン誘導体 - Google Patents
選択的アンドロゲン受容体モジュレーター（ｓａｒｍｓ）としての新規なイミダゾリジン−２−オン誘導体 Download PDFInfo
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- JP5031568B2 JP5031568B2 JP2007531421A JP2007531421A JP5031568B2 JP 5031568 B2 JP5031568 B2 JP 5031568B2 JP 2007531421 A JP2007531421 A JP 2007531421A JP 2007531421 A JP2007531421 A JP 2007531421A JP 5031568 B2 JP5031568 B2 JP 5031568B2
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- lower alkyl
- acid
- phenyl
- methyl
- halogen
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- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
- UGZADUVQMDAIAO-UHFFFAOYSA-L zinc hydroxide Chemical compound [OH-].[OH-].[Zn+2] UGZADUVQMDAIAO-UHFFFAOYSA-L 0.000 description 1
- 229940007718 zinc hydroxide Drugs 0.000 description 1
- 229910021511 zinc hydroxide Inorganic materials 0.000 description 1
Classifications
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Virology (AREA)
- Reproductive Health (AREA)
- Dermatology (AREA)
- Biomedical Technology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Gynecology & Obstetrics (AREA)
- Molecular Biology (AREA)
- Urology & Nephrology (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2008512492A JP2008512492A (ja) | 2008-04-24 |
| JP2008512492A5 JP2008512492A5 (enExample) | 2012-07-12 |
| JP5031568B2 true JP5031568B2 (ja) | 2012-09-19 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| JP2007531421A Expired - Fee Related JP5031568B2 (ja) | 2004-09-10 | 2005-09-09 | 選択的アンドロゲン受容体モジュレーター（ｓａｒｍｓ）としての新規なイミダゾリジン−２−オン誘導体 |
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| Country | Link |
|---|---|
| US (2) | US7531565B2 (enExample) |
| EP (1) | EP1791821B1 (enExample) |
| JP (1) | JP5031568B2 (enExample) |
| CN (1) | CN101056862B (enExample) |
| AU (1) | AU2005285035B2 (enExample) |
| CA (1) | CA2579514A1 (enExample) |
| ES (1) | ES2422204T3 (enExample) |
| WO (1) | WO2006031715A2 (enExample) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101103003A (zh) | 2004-11-16 | 2008-01-09 | 詹森药业有限公司 | 用作选择性雄激素受体调节剂(sarms)的新的杂环衍生物 |
| US7709516B2 (en) * | 2005-06-17 | 2010-05-04 | Endorecherche, Inc. | Helix 12 directed non-steroidal antiandrogens |
| WO2008106128A2 (en) * | 2007-02-26 | 2008-09-04 | Vitae Pharmaceuticals, Inc. | CYCLIC UREA AND CARBAMATE INHIBITORS OF 11β -HYDROXYSTEROID DEHYDROGENASE 1 |
| EP2183229B1 (en) * | 2007-07-26 | 2012-04-18 | Vitae Pharmaceuticals, Inc. | Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 |
| AR069207A1 (es) * | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| CA2708303A1 (en) | 2007-12-11 | 2009-06-18 | Vitae Pharmaceuticals, Inc. | Cyclic urea inhibitors of 11.beta.-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 |
| EP2252598A2 (en) * | 2008-02-11 | 2010-11-24 | Vitae Pharmaceuticals, Inc. | 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CA2715290A1 (en) * | 2008-02-15 | 2009-08-20 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| EP2274287B1 (en) * | 2008-03-18 | 2016-03-09 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 |
| WO2009134384A1 (en) * | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| ES2421537T3 (es) * | 2008-05-01 | 2013-09-03 | Vitae Pharmaceuticals Inc | Inhibidores cíclicos de la 11beta-hidroxiesteroide deshidrogenasa 1 |
| US8592410B2 (en) | 2008-05-01 | 2013-11-26 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11BETA-hydroxysteroid dehydrogenase 1 |
| WO2009134392A1 (en) | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| JP5777030B2 (ja) | 2008-07-25 | 2015-09-09 | 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の阻害剤 |
| ES2432150T3 (es) | 2008-07-25 | 2013-12-02 | Boehringer Ingelheim International Gmbh | Inhibidores cíclicos de la 11 beta-hidroxiesteroide deshidrogenasa 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 |
| CA2744946A1 (en) | 2009-02-04 | 2010-08-12 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| 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 |
| WO2011002910A1 (en) | 2009-07-01 | 2011-01-06 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| WO2011028112A1 (en) * | 2009-09-02 | 2011-03-10 | Valletta Health B.V. | Imidazole-4-carboxylic acid for use in treating a disease related to extracellular reactive oxygen species |
| JP5750449B2 (ja) | 2009-11-05 | 2015-07-22 | 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 | 新規キラルリンリガンド |
| EP2531029B1 (en) | 2010-02-04 | 2016-10-19 | Radius Health, Inc. | Selective androgen receptor modulators |
| WO2011143469A1 (en) | 2010-05-12 | 2011-11-17 | Radius Health,Inc | Therapeutic regimens |
| WO2011149822A1 (en) | 2010-05-26 | 2011-12-01 | Boehringer Ingelheim International Gmbh | 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives |
| EP2582698B1 (en) | 2010-06-16 | 2016-09-14 | 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 |
| BR112013007685B1 (pt) | 2010-09-28 | 2021-11-09 | Radius Pharmaceuticals, Inc | Compostos moduladores de receptor andrógeno seletivos, composição farmacêutica compreendendo os referidos compostos, método de identificação de um composto capaz de modular um receptor andrógeno, usos de um composto ou da composição e processo para a preparação de um composto |
| EA201300522A1 (ru) | 2010-11-02 | 2013-11-29 | Бёрингер Ингельхайм Интернациональ Гмбх | Фармацевтические комбинации для лечения метаболических нарушений |
| CN104105690A (zh) * | 2011-12-05 | 2014-10-15 | 诺华股份有限公司 | 作为雄激素受体拮抗剂的环状尿素衍生物 |
| JP7221699B2 (ja) | 2016-06-22 | 2023-02-14 | エリプセス ファーマ エルティーディー | Ａｒ＋乳癌の治療方法 |
| EA202092436A1 (ru) | 2018-05-14 | 2021-05-04 | Нувейшн Био Инк. | Противораковые соединения, нацеливающие на ядерные гормональные рецепторы |
| CA3138197A1 (en) | 2019-05-14 | 2020-11-19 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| US11952349B2 (en) | 2019-11-13 | 2024-04-09 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| IL306010A (en) | 2021-03-23 | 2023-11-01 | Nuvation Bio Inc | Anticancer compounds against the nuclear hormone receptor |
| 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 |
Family Cites Families (6)
| 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 |
| 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 |
| 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 |
| DE102004009835A1 (de) * | 2004-02-28 | 2005-09-15 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Carbonsäureamide, deren Herstellung und deren Verwendung als Arzneimittel |
| US7371743B2 (en) | 2004-02-28 | 2008-05-13 | Boehringer Ingelheim International Gmbh | Carboxylic acid amides, the preparation thereof and their use as medicaments |
-
2005
- 2005-09-09 EP EP05800947.3A patent/EP1791821B1/en not_active Expired - Lifetime
- 2005-09-09 JP JP2007531421A patent/JP5031568B2/ja not_active Expired - Fee Related
- 2005-09-09 CN CN2005800381110A patent/CN101056862B/zh not_active Expired - Fee Related
- 2005-09-09 US US11/223,187 patent/US7531565B2/en active Active
- 2005-09-09 WO PCT/US2005/032381 patent/WO2006031715A2/en not_active Ceased
- 2005-09-09 CA CA002579514A patent/CA2579514A1/en not_active Abandoned
- 2005-09-09 AU AU2005285035A patent/AU2005285035B2/en not_active Ceased
- 2005-09-09 ES ES05800947T patent/ES2422204T3/es not_active Expired - Lifetime
-
2009
- 2009-03-30 US US12/413,873 patent/US7968580B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JP2008512492A (ja) | 2008-04-24 |
| US7968580B2 (en) | 2011-06-28 |
| CN101056862B (zh) | 2013-03-13 |
| ES2422204T3 (es) | 2013-09-09 |
| CN101056862A (zh) | 2007-10-17 |
| CA2579514A1 (en) | 2006-03-23 |
| EP1791821B1 (en) | 2013-06-05 |
| WO2006031715A3 (en) | 2006-07-20 |
| WO2006031715A2 (en) | 2006-03-23 |
| AU2005285035B2 (en) | 2012-03-22 |
| US7531565B2 (en) | 2009-05-12 |
| US20060063819A1 (en) | 2006-03-23 |
| AU2005285035A1 (en) | 2006-03-23 |
| EP1791821A2 (en) | 2007-06-06 |
| US20090215848A1 (en) | 2009-08-27 |
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