ES2422204T3 - Novedosos derivados de imidazolidin-2-ona como moduladores selectivos de receptor de andrógenos (SARMS) - Google Patents
Novedosos derivados de imidazolidin-2-ona como moduladores selectivos de receptor de andrógenos (SARMS)Info
- Publication number
- ES2422204T3 ES2422204T3 ES05800947T ES05800947T ES2422204T3 ES 2422204 T3 ES2422204 T3 ES 2422204T3 ES 05800947 T ES05800947 T ES 05800947T ES 05800947 T ES05800947 T ES 05800947T ES 2422204 T3 ES2422204 T3 ES 2422204T3
- Authority
- ES
- Spain
- Prior art keywords
- 4alkyl
- halogen
- amino
- substituted
- 4alkoxy
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Virology (AREA)
- Reproductive Health (AREA)
- Dermatology (AREA)
- Biomedical Technology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Tropical Medicine & Parasitology (AREA)
- Gynecology & Obstetrics (AREA)
- AIDS & HIV (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Un compuesto de fórmula (I) **Fórmula** R1 es hidrógeno; R2 es alquilo C1-4 o alquilo C1-4 sustituido con halógeno y R3 es carboxi, -C(O)-(C1-4 alcoxi), -C(O)-N(RB)2; en la que cada RB está independientemente seleccionado de hidrógeno, alquilo C1-4 y arilo, a condición de quesi está presente, solo un RB es arilo; en la que el arilo está opcionalmente sustituido con uno o más sustituyentes independientementeseleccionados de halógeno, hidroxi, carboxi, alquilo C1-4, alquilo C1-4 sustituido con halógeno, alcoxi C1-4, alcoxiC1-4 sustituido con halógeno, ciano, nitro, amino, alquil C1-4-amino o di(alquil C1-4)amino; R4 está seleccionado del grupo que consiste en halógeno, hidroxi, carboxi, alquilo C1-4, alquilo C1-4 sustituidocon halógeno, alcoxi C1-4, alcoxi C1-4 sustituido con halógeno, ciano, nitro, amino, alquil C1-4-amino, di(alquil C1-4)amino, -C(O)-(alquilo C1-4), -C(O)-(alcoxi C1-4), -C(O)-N(RA)2, -S(O)0-2-(alquilo C1-4), -SO2-N(RA)2, -N(RA)-C(O)-(alquilo C1-4), -N(RA)-C(O)(alquilo C1-4 sustituido con halógeno) y arilo; en la que cada RA está independientemente seleccionado de hidrógeno o alquilo C1-4; en la que el arilo está opcionalmente sustituido con uno o más sustituyentes independientementeseleccionados de halógeno, hidroxi, carboxi, alquilo C1-4, alquilo C1-4 sustituido con halógeno, alcoxi C1-4, alcoxiC1-4 sustituido con halógeno, ciano, nitro, amino, alquil C1-4-amino o di(alquil C1-4)amino; a es un número entero de 0 a 4; b es 0; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US60915704P | 2004-09-10 | 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 (1)
| Publication Number | Publication Date |
|---|---|
| ES2422204T3 true ES2422204T3 (es) | 2013-09-09 |
Family
ID=36060597
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES05800947T Active ES2422204T3 (es) | 2004-09-10 | 2005-09-09 | Novedosos derivados de imidazolidin-2-ona como moduladores selectivos de receptor de andrógenos (SARMS) |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US7531565B2 (es) |
| EP (1) | EP1791821B1 (es) |
| JP (1) | JP5031568B2 (es) |
| CN (1) | CN101056862B (es) |
| AU (1) | AU2005285035B2 (es) |
| CA (1) | CA2579514A1 (es) |
| ES (1) | ES2422204T3 (es) |
| WO (1) | WO2006031715A2 (es) |
Families Citing this family (41)
| 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 |
| JP5486928B2 (ja) * | 2007-02-26 | 2014-05-07 | 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のサイクリックウレアおよびカルバメートインヒビター |
| JP5451611B2 (ja) * | 2007-07-26 | 2014-03-26 | 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のサイクリックインヒビター |
| AR069207A1 (es) | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| WO2009075835A1 (en) | 2007-12-11 | 2009-06-18 | Vitae Pharmaceutical, 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 |
| JP5490020B2 (ja) * | 2008-01-24 | 2014-05-14 | 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の環状カルバゼート及びセミカルバジドインヒビター |
| JP5734666B2 (ja) * | 2008-02-11 | 2015-06-17 | 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１，３−オキサアゼパン−２−オン及び１，３−ジアゼパン−２−オン阻害剤 |
| US8598160B2 (en) * | 2008-02-15 | 2013-12-03 | Vitae Pharmaceuticals, Inc. | Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| US20110105504A1 (en) * | 2008-03-18 | 2011-05-05 | Vitae Pharmaceuticals ,Inc. | Inhibitors Of 11beta-Hydroxysteroid Dehydrogenase Type 1 |
| JP5538365B2 (ja) | 2008-05-01 | 2014-07-02 | 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の環状阻害剤 |
| US8242111B2 (en) * | 2008-05-01 | 2012-08-14 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1 |
| CL2009001058A1 (es) | 2008-05-01 | 2010-09-10 | Vitae Pharmaceuticals Inc | Compuestos derivados de oxazinas sustituidas, inhibidores de la 11b-hidroxiesteroide deshidrogenasa de tipo-1; composicion farmaceutica; y uso del compuesto para inhibir la actividad de 11b-hsd1, como en el tratamiento de la diabetes, dislipidemia, hipertension, obesidad, cancer, glaucoma, entre otras. |
| PL2300461T3 (pl) * | 2008-05-01 | 2013-09-30 | Vitae Pharmaceuticals Inc | Cykliczne inhibitory dehydrogenazy 11beta-hydroksysteroidów 1 |
| EP2687525B1 (en) | 2008-07-25 | 2015-09-23 | Boehringer Ingelheim International GmbH | Cyclic inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| CA2729998A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CA2729993A1 (en) | 2008-07-25 | 2010-01-28 | 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 |
| WO2010089303A1 (en) | 2009-02-04 | 2010-08-12 | Boehringer Ingelheim International Gmbh | CYCLIC INHIBITORS OF 11 β-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 |
| UA109255C2 (ru) | 2009-04-30 | 2015-08-10 | Берінгер Інгельхайм Інтернешнл Гмбх | Циклические ингибиторы 11бета-гидроксистероиддегидрогеназы 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 |
| 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 |
| AU2011212813B2 (en) | 2010-02-04 | 2014-10-23 | Radius Health, Inc. | Selective androgen receptor modulators |
| ME02474B (me) | 2010-05-12 | 2017-02-20 | Radius Health Inc | Terapijski režimi |
| US8648192B2 (en) | 2010-05-26 | 2014-02-11 | Boehringer Ingelheim International Gmbh | 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives |
| JP5860042B2 (ja) | 2010-06-16 | 2016-02-16 | 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 | 置換５、６及び７員複素環、そのような化合物を含有する医薬及びそれらの使用 |
| 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 |
| 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 |
| CN113811333B (zh) | 2019-05-14 | 2024-03-12 | 诺维逊生物股份有限公司 | 靶向抗癌核激素受体的化合物 |
| TW202131930A (zh) | 2019-11-13 | 2021-09-01 | 美商諾維雪碧歐公司 | 抗癌核荷爾蒙受體標靶化合物 |
| US11834458B2 (en) | 2021-03-23 | 2023-12-05 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| US12006314B2 (en) | 2021-05-03 | 2024-06-11 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
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 |
| 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 |
| 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. |
| 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 |
| US7371743B2 (en) * | 2004-02-28 | 2008-05-13 | Boehringer Ingelheim International Gmbh | Carboxylic acid amides, the preparation thereof and their use as medicaments |
| DE102004009835A1 (de) * | 2004-02-28 | 2005-09-15 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Carbonsäureamide, deren Herstellung und deren Verwendung als Arzneimittel |
-
2005
- 2005-09-09 WO PCT/US2005/032381 patent/WO2006031715A2/en active Application Filing
- 2005-09-09 JP JP2007531421A patent/JP5031568B2/ja not_active Expired - Fee Related
- 2005-09-09 ES ES05800947T patent/ES2422204T3/es active Active
- 2005-09-09 US US11/223,187 patent/US7531565B2/en active Active
- 2005-09-09 AU AU2005285035A patent/AU2005285035B2/en not_active Ceased
- 2005-09-09 CA CA002579514A patent/CA2579514A1/en not_active Abandoned
- 2005-09-09 EP EP05800947.3A patent/EP1791821B1/en not_active Not-in-force
- 2005-09-09 CN CN2005800381110A patent/CN101056862B/zh not_active Expired - Fee Related
-
2009
- 2009-03-30 US US12/413,873 patent/US7968580B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP1791821A2 (en) | 2007-06-06 |
| WO2006031715A3 (en) | 2006-07-20 |
| WO2006031715A2 (en) | 2006-03-23 |
| US7531565B2 (en) | 2009-05-12 |
| CN101056862B (zh) | 2013-03-13 |
| US20090215848A1 (en) | 2009-08-27 |
| CA2579514A1 (en) | 2006-03-23 |
| JP2008512492A (ja) | 2008-04-24 |
| JP5031568B2 (ja) | 2012-09-19 |
| EP1791821B1 (en) | 2013-06-05 |
| US7968580B2 (en) | 2011-06-28 |
| US20060063819A1 (en) | 2006-03-23 |
| AU2005285035B2 (en) | 2012-03-22 |
| CN101056862A (zh) | 2007-10-17 |
| AU2005285035A1 (en) | 2006-03-23 |
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