CN105873917B - 含有吡啶基部分的非甾体类抗雄激素和选择性雄激素受体调节剂 - Google Patents

含有吡啶基部分的非甾体类抗雄激素和选择性雄激素受体调节剂 Download PDF

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CN105873917B
CN105873917B CN201480069528.2A CN201480069528A CN105873917B CN 105873917 B CN105873917 B CN 105873917B CN 201480069528 A CN201480069528 A CN 201480069528A CN 105873917 B CN105873917 B CN 105873917B
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compound
pyr
group
acetone
androgen
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CN105873917A (zh
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费尔南德·莱伯里
尚卡尔莫汉·辛格
里哈德·拉布雷克
利维乌康斯坦丁·乔巴努
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Endorecherche Inc
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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CN201480069528.2A 2013-12-19 2014-12-16 含有吡啶基部分的非甾体类抗雄激素和选择性雄激素受体调节剂 Expired - Fee Related CN105873917B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361918133P 2013-12-19 2013-12-19
US61/918,133 2013-12-19
US14/567,970 US9682960B2 (en) 2013-12-19 2014-12-11 Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
US14/567,970 2014-12-11
PCT/CA2014/000894 WO2015089634A1 (en) 2013-12-19 2014-12-16 Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety

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CN105873917A CN105873917A (zh) 2016-08-17
CN105873917B true CN105873917B (zh) 2021-08-10

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US (1) US9682960B2 (enExample)
EP (1) EP3083590B1 (enExample)
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Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9682960B2 (en) * 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
TW201630899A (zh) 2015-01-09 2016-09-01 必治妥美雅史谷比公司 作為ｒｏｃｋ抑制劑的環狀脲類
TWI726969B (zh) 2016-01-11 2021-05-11 比利時商健生藥品公司 用作雄性激素受體拮抗劑之經取代之硫尿囊素衍生物
WO2018005533A1 (en) 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Antiproliferative pyrimidine-based compounds
WO2019226213A2 (en) 2018-03-08 2019-11-28 Incyte Corporation AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS
CN108329236B (zh) * 2018-04-04 2020-12-29 盐城师范学院 一种恩杂鲁胺中间体的制备方法
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
US20220306640A1 (en) * 2019-09-06 2022-09-29 Ono Pharmaceutical Co., Ltd. Hydantoin derivative
WO2025103470A1 (zh) * 2023-11-17 2025-05-22 中国药科大学 作为雄激素受体(ar)拮抗剂的化合物及其应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101243052A (zh) * 2005-06-17 2008-08-13 恩多研究公司 螺旋结构12定位的非甾族抗雄激素物质
CN101501005A (zh) * 2006-08-08 2009-08-05 塞诺菲-安万特股份有限公司 芳基氨基芳基-烷基-取代的咪唑烷-2,4-二酮类、其制备方法、包含这些化合物的药物以及其用途
CN102639523A (zh) * 2009-09-11 2012-08-15 拜耳医药股份有限公司 用作抗癌药的取代的(杂芳基甲基)乙内酰硫脲
CN102884057A (zh) * 2010-02-16 2013-01-16 亚拉冈制药公司 雄激素受体调节剂及其用途

Family Cites Families (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3797494A (en) 1969-04-01 1974-03-19 Alza Corp Bandage for the administration of drug by controlled metering through microporous materials
US3742951A (en) 1971-08-09 1973-07-03 Alza Corp Bandage for controlled release of vasodilators
US4191775A (en) 1977-12-15 1980-03-04 Imperial Chemical Industries Limited Amide derivatives
EP0100172B1 (en) 1982-07-23 1987-08-12 Imperial Chemical Industries Plc Amide derivatives
DE3333240A1 (de) 1983-09-12 1985-03-28 Schering AG, 1000 Berlin und 4709 Bergkamen Mittel zur transdermalen applikation von arzneimittelwirkstoffen
US4568343A (en) 1984-10-09 1986-02-04 Alza Corporation Skin permeation enhancer compositions
US4816258A (en) 1987-02-26 1989-03-28 Alza Corporation Transdermal contraceptive formulations
US5064654A (en) 1989-01-11 1991-11-12 Ciba-Geigy Corporation Mixed solvent mutually enhanced transdermal therapeutic system
US5071644A (en) 1990-08-07 1991-12-10 Mediventures, Inc. Topical drug delivery with thermo-irreversible gels
US5411981A (en) 1991-01-09 1995-05-02 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
FR2693461B1 (fr) 1992-07-08 1994-09-02 Roussel Uclaf Nouvelles phénylimidazolidines substituées, leur procédé de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant.
FR2671348B1 (fr) 1991-01-09 1993-03-26 Roussel Uclaf Nouvelles phenylimidazolidines, leur procede de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant.
FR2694290B1 (fr) 1992-07-08 1994-09-02 Roussel Uclaf Nouvelles phénylimidazolidines éventuellement substituées, leur procédé 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
DE69531998T2 (de) 1994-12-22 2004-07-22 Ligand Pharmaceuticals, Inc., San Diego Steroidrezeptor-modulator verbindungen und methoden
US5656651A (en) 1995-06-16 1997-08-12 Biophysica Inc. Androgenic directed compositions
FR2741342B1 (fr) 1995-11-22 1998-02-06 Roussel Uclaf Nouvelles phenylimidazolidines fluorees ou hydroxylees, procede, intermediaires de preparation, application comme medicaments, nouvelle utilisation et compositions pharmaceutiques
FR2742749B1 (fr) 1995-12-22 1998-02-06 Roussel Uclaf Nouvelles phenylimidazolidines comportant notamment un radical nitrooxy ou carbonyloxy, procede et intermediaires de preparation, application comme medicaments, nouvelles utilisations et compositions pharmaceutiques
US6071957A (en) 1996-11-27 2000-06-06 The University Of Tennessee Research Corporation Irreversible non-steroidal antagonist compound and its use in the treatment of prostate cancer
US7759520B2 (en) 1996-11-27 2010-07-20 University Of Tennessee Research Foundation Synthesis of selective androgen receptor modulators
US6160011A (en) 1997-05-30 2000-12-12 The University Of Tennessee Research Corporation Non-steroidal agonist compounds and their use in male hormone therapy
TR200002784T2 (tr) 1998-03-11 2000-12-21 Endorecherche, Inc Tip 5 ve tip 3 17beta-Hidroksisteroid dehidrojenaz inhibitörleri ve bunların kullanımı için metodlar
US6184249B1 (en) 1998-12-18 2001-02-06 Biophysica, Inc. Androgen receptor suppressors in the therapy and diagnosis of prostate cancer, alopecia and other hyper-androgenic syndromes
JP2003508397A (ja) 1999-08-27 2003-03-04 リガンド・ファーマシューティカルズ・インコーポレイテッド アンドロゲンレセプターモジュレーターとしての８−置換−６−トリフルオロメチル−９−ピリド［３，２−ｇ］キノリン化合物
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
US7001911B2 (en) 2000-06-28 2006-02-21 Bristol-Myers Squibb Company Fused cyclic modulators of nuclear hormone receptor function
AU2001288213B2 (en) 2000-06-28 2005-04-14 Bristol-Myers Squibb Company Selective androgen receptor modulators and methods for their identification, design and use
US20040077605A1 (en) 2001-06-20 2004-04-22 Salvati Mark E. Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
JP2002088073A (ja) 2000-09-08 2002-03-27 Yamanouchi Pharmaceut Co Ltd 抗アンドロゲン剤
DK1319007T3 (da) 2000-09-19 2006-06-19 Bristol Myers Squibb Co Kondenserede heterocykliske succinimidforbindelser og analoger deraf, modulatorer af nukleær hormonreceptorfunktion
US7803970B2 (en) 2002-02-28 2010-09-28 University Of Tennessee Research Foundation Multi-substitued selective androgen receptor modulators and methods of use thereof
US7405234B2 (en) 2002-05-17 2008-07-29 Bristol-Myers Squibb Company Bicyclic modulators of androgen receptor function
DE10322108B4 (de) 2003-05-09 2008-12-11 Bayer Schering Pharma Aktiengesellschaft Antiandrogene Pyrrolidine mit tumorhemmender Wirksamkeit
EP1634874A4 (en) 2003-06-12 2008-04-02 Chugai Pharmaceutical Co Ltd imidazolidine
ES2291906T3 (es) 2003-06-13 2008-03-01 Janssen Pharmaceutica N.V. Derivados de tiazolina como moduladores selectivos del receptor del androgeno (sarms).
US20050124625A1 (en) 2003-10-21 2005-06-09 Salvati Mark E. Piperazine derivatives and their use as modulators of nuclear hormone receptor function
US7256208B2 (en) 2003-11-13 2007-08-14 Bristol-Myers Squibb Company Monocyclic N-Aryl hydantoin modulators of androgen receptor function
KR101536701B1 (ko) 2004-01-07 2015-07-14 앙도르쉐르슈 인코포레이티드 헬릭스 12 배향형 스테로이드계 약학 제품
CA2564953A1 (en) 2004-05-03 2005-11-24 Janssen Pharmaceutica N.V. Novel indole derivatives as selective androgen receptor modulators (sarms)
CN101248069A (zh) 2004-05-17 2008-08-20 阿卡蒂亚药品公司 雄激素受体调节剂及用其治疗疾病的方法
AU2005251781C1 (en) 2004-06-07 2008-02-21 University Of Tennessee Research Foundation Selective androgen receptor modulators and methods of use thereof
KR101332889B1 (ko) * 2005-05-13 2013-11-26 더 리전트 오브 더 유니버시티 오브 캘리포니아 디아릴히단토인 화합물
AU2007245022A1 (en) 2006-03-29 2007-11-08 The Regents Of The University Of California Diarylthiohydantoin compounds
US20090227571A1 (en) 2005-07-01 2009-09-10 Ligand Pharmaceuticals Incorporated Androgen Receptor Modulator Compounds and Methods
BRPI0715160A2 (pt) * 2006-08-08 2013-06-11 Sanofi Aventis imidazolidina-2,4-dionas substituÍdas por arilamimoaril-alquil-, processo para preparÁ-las, medicamentos compeendendo estes compostos, e seu uso
WO2008044033A1 (en) 2006-10-11 2008-04-17 Astrazeneca Ab Amide derivatives
FR2912132A1 (fr) 2007-02-05 2008-08-08 Aventis Pharma Sa Procede de preparation de sulfanylamides et sulfinamidines fluores et leurs utilisation
WO2008124000A2 (en) 2007-04-02 2008-10-16 Ligand Pharmaceuticals Incorporated Thiazole derivatives as androgen receptor modulator compounds
US9284345B2 (en) 2007-04-12 2016-03-15 Endorecherche, Inc. 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators
TWI557111B (zh) 2007-10-26 2016-11-11 加州大學董事會 二芳基乙內醯脲類化合物
WO2009079412A2 (en) 2007-12-14 2009-06-25 Ardea Biosciences Inc. Reverse transcriptase inhibitors
AR071069A1 (es) 2008-03-26 2010-05-26 Takeda Pharmaceutical Derivados sustituidos de pirazol y su uso para la prevencion o el tratamiento de cancer
EP2416657A4 (en) 2009-04-09 2012-09-05 Medivation Prostate Therapeutics Inc COMPOUNDS COMPRISING SUBSTITUTED DI-ARYLHYDANTOIDS AND DI-ARYLTHIOHYDANTOINES AND METHODS OF USE THEREOF
US8741951B2 (en) 2009-04-10 2014-06-03 CNR—Consiglio Nazionale Delle Ricerche Non-steroidal compounds for androgen receptor modulation
WO2010143803A2 (en) 2009-06-08 2010-12-16 Industry Foundation Of Chonnam National University New nicotinamide derivatives with anti-androgen effects, processes of preparing, and antiandrogens comprising the same
WO2011008543A2 (en) 2009-06-29 2011-01-20 University Of Delaware Pan-antagonists for the androgen receptor and androgen receptor mutants associated with anti-androgen withdrawal
EP2531029B1 (en) 2010-02-04 2016-10-19 Radius Health, Inc. Selective androgen receptor modulators
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
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
US9139565B2 (en) 2010-09-28 2015-09-22 Georgia Tech Research Corporation Histone deacetylase (HDAC) inhibitors targeting prostate tumors and methods of making and using thereof
EA201390598A1 (ru) 2010-10-22 2013-08-30 Астеллас Фарма Инк. Антагонист мутантного андрогенного рецептора
ES2541295T3 (es) 2011-04-21 2015-07-17 Orion Corporation Carboxamidas que modulan el receptor de andrógenos
BR112014001751A2 (pt) 2011-07-27 2017-02-14 Novartis Ag derivados de pirazolina e seu uso como moduladores seletivos do receptor de estrogênio
AR088082A1 (es) 2011-10-13 2014-05-07 Lilly Co Eli Moduladores selectivos del receptor androgeno
FI20116033A7 (fi) 2011-10-18 2013-04-19 Juha Pulkkinen Uudet ei-steroidiset yhdisteet androgeenireseptorin muuntelijoina
WO2013067142A1 (en) 2011-11-02 2013-05-10 Medivation Technologies, Inc. Compounds and treatment methods
UY34646A (es) 2012-03-02 2013-10-31 Novartis Ag Compuestos de espirohidantoína y su uso como moduladores selectivos del receptor de andrógenos
US20150057452A1 (en) 2012-04-04 2015-02-26 Catylix, Inc. Selective androgen receptor modulators
CN104341396A (zh) * 2013-08-08 2015-02-11 上海医药集团股份有限公司 二芳基乙内酰脲衍生物、其制备方法、药物组合物和应用
US9682960B2 (en) * 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101243052A (zh) * 2005-06-17 2008-08-13 恩多研究公司 螺旋结构12定位的非甾族抗雄激素物质
CN101501005A (zh) * 2006-08-08 2009-08-05 塞诺菲-安万特股份有限公司 芳基氨基芳基-烷基-取代的咪唑烷-2,4-二酮类、其制备方法、包含这些化合物的药物以及其用途
CN102639523A (zh) * 2009-09-11 2012-08-15 拜耳医药股份有限公司 用作抗癌药的取代的(杂芳基甲基)乙内酰硫脲
CN102884057A (zh) * 2010-02-16 2013-01-16 亚拉冈制药公司 雄激素受体调节剂及其用途

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