AP494A - Androstenone derivative. - Google Patents
Androstenone derivative. Download PDFInfo
- Publication number
- AP494A AP494A APAP/P/1994/000669A AP9400669A AP494A AP 494 A AP494 A AP 494A AP 9400669 A AP9400669 A AP 9400669A AP 494 A AP494 A AP 494A
- Authority
- AP
- ARIPO
- Prior art keywords
- compound
- formula
- testosterone
- mediated disease
- pharmaceutically acceptable
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
- C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/82—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0066—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by a carbon atom forming part of an amide group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
- C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
- C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
- C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
- C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
- C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
- C07C2603/14—Benz[f]indenes; Hydrogenated benz[f]indenes
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12328093A | 1993-09-17 | 1993-09-17 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AP9400669A0 AP9400669A0 (en) | 1994-10-31 |
| AP494A true AP494A (en) | 1996-05-15 |
Family
ID=22407744
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| APAP/P/1994/000669A AP494A (en) | 1993-09-17 | 1994-09-15 | Androstenone derivative. |
Country Status (41)
| Country | Link |
|---|---|
| US (2) | US5565467A (fi) |
| EP (1) | EP0719278B1 (fi) |
| JP (1) | JP2904310B2 (fi) |
| KR (1) | KR100364953B1 (fi) |
| CN (1) | CN1057771C (fi) |
| AP (1) | AP494A (fi) |
| AT (1) | ATE162199T1 (fi) |
| AU (1) | AU690925B2 (fi) |
| BG (1) | BG62363B1 (fi) |
| BR (1) | BR1100329A (fi) |
| CA (2) | CA2462061A1 (fi) |
| CY (2) | CY2219B1 (fi) |
| CZ (1) | CZ286069B6 (fi) |
| DE (2) | DE69407978T2 (fi) |
| DK (1) | DK0719278T3 (fi) |
| EE (1) | EE03241B1 (fi) |
| ES (1) | ES2113127T3 (fi) |
| FI (1) | FI115216B (fi) |
| GR (1) | GR3026144T3 (fi) |
| HK (1) | HK1004334A1 (fi) |
| HR (1) | HRP940563B1 (fi) |
| HU (1) | HU220060B (fi) |
| IL (1) | IL110978A (fi) |
| IS (1) | IS1713B (fi) |
| LU (1) | LU91027I2 (fi) |
| MY (1) | MY119778A (fi) |
| NL (1) | NL300122I2 (fi) |
| NO (2) | NO306117B1 (fi) |
| NZ (1) | NZ274642A (fi) |
| OA (1) | OA10575A (fi) |
| PE (1) | PE15095A1 (fi) |
| PL (1) | PL180002B1 (fi) |
| RO (1) | RO117455B1 (fi) |
| RU (1) | RU2140926C1 (fi) |
| SA (1) | SA94150231B1 (fi) |
| SG (1) | SG52650A1 (fi) |
| SI (1) | SI0719278T1 (fi) |
| SK (1) | SK281869B6 (fi) |
| TW (1) | TW369521B (fi) |
| WO (1) | WO1995007927A1 (fi) |
| ZA (2) | ZA947119B (fi) |
Families Citing this family (78)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2135167A1 (en) * | 1992-05-20 | 1993-11-25 | Donald W. Graham | New 17-ester, amide, and ketone derivatives of 3-oxo-4- azasteroids as 5a-reductase inhibitors |
| US5693810A (en) * | 1992-10-06 | 1997-12-02 | Merck & Co., Inc. | 17 β-carboxanilides of 4-aza-5α-androstan-3-ones as 5α-reductase inhibitors |
| TW408127B (en) * | 1993-09-17 | 2000-10-11 | Glaxo Inc | Androstenones |
| TW382595B (en) * | 1993-10-15 | 2000-02-21 | Merck & Co Inc | Pharmaceutical composition for use in arresting and reversing androgenic alopecia |
| US5547957A (en) * | 1993-10-15 | 1996-08-20 | Merck & Co., Inc. | Method of treating androgenic alopecia with 5-α reductase inhibitors |
| RU2142956C1 (ru) * | 1993-10-21 | 1999-12-20 | Мерк Энд Ко., Инк. | 16-замещенные 4-аза-андростаны, соединения, способы ингибирования, фармацевтическая композиция |
| US5817818A (en) * | 1994-09-16 | 1998-10-06 | Glaxo Wellcome Inc. | Androstenones |
| US6001844A (en) * | 1995-09-15 | 1999-12-14 | Merck & Co., Inc. | 4-Azasteroids for treatment of hyperandrogenic conditions |
| US5872126A (en) * | 1996-09-06 | 1999-02-16 | Merck & Co., Inc. | Methods and compositions for treating preterm labor |
| US5935968A (en) * | 1997-03-17 | 1999-08-10 | Merck & Co., Inc. | Methods for treating polycystic ovary syndrome |
| GB9717428D0 (en) * | 1997-08-19 | 1997-10-22 | Glaxo Group Ltd | Pharmaceutical composition |
| JP2001521000A (ja) * | 1997-10-28 | 2001-11-06 | メルク エンド カムパニー インコーポレーテッド | 誘発性急性閉尿の予防 |
| CN1429104A (zh) * | 1998-03-11 | 2003-07-09 | 内部研究股份有限公司 | 5型和3型17β－羟基类固醇脱氢酶的抑制剂及其用法 |
| EP1321146A3 (en) * | 1998-03-11 | 2004-06-02 | Endorecherche Inc. | Inhibitors of type 5 and 3 17beta-hydroxysteroid dehydrogenase and methods for their use |
| US5998427A (en) * | 1998-05-14 | 1999-12-07 | Glaxo Wellcome Inc. | Androstenones |
| WO1999066915A2 (en) * | 1998-06-23 | 1999-12-29 | Southern Illinois University At Carbondale | Therapeutic applications of estrogenic carboxylic acids |
| AU2512800A (en) * | 1999-02-03 | 2000-08-25 | Eli Lilly And Company | Alpha1-adrenergic receptor antagonists |
| AU777770C (en) | 1999-05-04 | 2005-11-10 | Strakan International Limited | Androgen glycosides and androgenic activity thereof |
| US6645974B2 (en) | 2001-07-31 | 2003-11-11 | Merck & Co., Inc. | Androgen receptor modulators and methods for use thereof |
| US7402577B2 (en) * | 2001-10-03 | 2008-07-22 | Merck & Co., Inc. | Androstane 17-beta-carboxamides as androgen receptor modulators |
| EP1468983B1 (en) * | 2002-01-25 | 2007-11-21 | Asahi Glass Company Ltd. | Process for producing 2,5-bis(trifluoromethyl)nitrobenzene |
| DE60313603T2 (de) * | 2002-04-24 | 2008-01-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmazeutische kombination zur behandlung von benigner prostatahyperplasie oder zur langzeitvorbeugung von akuter harnzurückhaltung |
| US20050131005A1 (en) * | 2002-04-30 | 2005-06-16 | Jiabing Wang | 4-azasteroid derivatives as androgen receptor modulators |
| US7326717B2 (en) * | 2003-05-06 | 2008-02-05 | L'oreal | Pyrimidine n-oxide compounds for stimulating the growth of keratin fibers and/or reducing loss thereof |
| US7022854B2 (en) * | 2003-07-17 | 2006-04-04 | Dr. Reddy's Laboratories, Limited | Forms of dutasteride and methods for preparation thereof |
| US20050059692A1 (en) * | 2003-09-09 | 2005-03-17 | Dr. Reddy's Laboratories Limited | Process for the preparation of 17beta-N-[2,5-bis(trifluoromethyl)phenyl] carbamoyl-4-aza-5-alpha-androst-1-en-3-one |
| WO2005092341A1 (en) * | 2004-03-22 | 2005-10-06 | Ranbaxy Laboratories Limited | Combination therapy for lower urinary tract symptoms |
| EP1734963A4 (en) * | 2004-04-02 | 2008-06-18 | Merck & Co Inc | METHOD FOR TREATING PEOPLE WITH METABOLIC AND ANTHROPOMETRIC DISORDER |
| AU2005280334A1 (en) * | 2004-08-25 | 2006-03-09 | Merck Sharp & Dohme Corp. | Androgen receptor modulators |
| US7998970B2 (en) * | 2004-12-03 | 2011-08-16 | Proteosys Ag | Use of finasteride, dutasteride and related compounds for the prevention or treatment of neurologically-associated disorders |
| US20060193804A1 (en) * | 2005-02-24 | 2006-08-31 | L'oreal | Haircare use of cyclic amine derivatives |
| EP1865955A4 (en) * | 2005-03-25 | 2009-04-15 | Merck & Co Inc | TREATMENT OF MALE-HUMAN HUMANS BY TESTOSTERONE SUPPLEMENTATION ASSOCIATED WITH 5ALPHA-REDUCTASE INHIBITOR |
| EP1945615A2 (en) * | 2005-11-10 | 2008-07-23 | Dr. Reddy's Laboratories Ltd. | Preparation of dutasteride |
| EP1897533A1 (en) * | 2006-09-08 | 2008-03-12 | Revotar Biopharmaceuticals AG | Use of 1,6-Bis [3-(3-carboxymethylphenyl)-4-(2-alpha -D-mannopyranosyl-oxy)-phenyl] hexane for the preparation of cosmetic compositions |
| EP1946756A1 (en) * | 2007-01-17 | 2008-07-23 | Revotar Biopharmaceuticals AG | Use of entacapone in cosmetic, dermatological and pharmaceutical compositions |
| FR2920309B1 (fr) | 2007-08-28 | 2010-05-28 | Galderma Res & Dev | Utilisation de travoprost pour traiter la chute des cheveux |
| US20090076057A1 (en) * | 2007-09-13 | 2009-03-19 | Protia, Llc | Deuterium-enriched dutasteride |
| EP2050436A1 (en) | 2007-12-21 | 2009-04-22 | Siegfried Generics International AG | Pharmaceutical composition containing dutasteride |
| AR070313A1 (es) | 2008-01-03 | 2010-03-31 | Gador Sa | Un procedimiento para preparar una forma solida y cristalina de dutasteride, una forma polimorfica del compuesto (forma iii) y una composicion farmaceutica que incluye dicha forma |
| FR2929117B1 (fr) | 2008-03-28 | 2010-05-07 | Oreal | Utilisation de l'association du 2,4-diaminopyrimidine 3-n-oxyde et du madecassosside et/ou du terminoloside pour induire et/ou stimuler la croissance de ces fibres keratiniques humaines et/ou freiner leur chute |
| FR2929118B1 (fr) | 2008-03-28 | 2010-05-07 | Oreal | Utilisation de l'association de madecassoside et/ou de terminoloside et d'une arginine pour induire et/ou stimuler la croissance de ces fibres keratiniques humaines et/ou freiner leur chute |
| AU2009231589B2 (en) | 2008-04-03 | 2013-11-07 | Neurmedix, Inc. | Solid state forms of a pharmaceutical |
| US20100048598A1 (en) * | 2008-08-21 | 2010-02-25 | Sateesh Kandavilli | Topical compositions comprising 5-alpha reductase inhibitors |
| CN101759762B (zh) * | 2008-11-06 | 2013-03-20 | 天津金耀集团有限公司 | 4ad在制备度他雄胺中的应用 |
| US8563728B2 (en) * | 2009-07-09 | 2013-10-22 | Aurobindo Pharma Ltd. | Process for the preparation of Dutasteride |
| FR2949052B1 (fr) | 2009-08-13 | 2015-03-27 | Oreal | Procede de traitement cosmetique du cuir chevelu. |
| EP2468262A1 (en) | 2010-12-06 | 2012-06-27 | Krka Tovarna Zdravil, D.D., Novo Mesto | Pharmaceutical composition comprising dutasteride |
| BRPI1103204A2 (pt) * | 2011-06-03 | 2014-02-25 | Eurofarma Lab S A | Composição farmacêutica para o tratamento de hiperplasia prostática benigna |
| HU230730B1 (hu) | 2011-06-30 | 2017-12-28 | Richter Gedeon Nyrt | Eljárás (5alfa,17béta)-N-[2,5-bisz-(trifluormetil)-fenil]-3-oxo-4-aza-5-androszt-1-én-17-karbonsavamid előállítására |
| CN103059098B (zh) * | 2011-10-24 | 2015-04-01 | 成都国为医药科技有限公司 | 一种度他雄胺的制备方法 |
| US9622981B2 (en) | 2011-11-17 | 2017-04-18 | Mylan Inc. | Liquid-filled hard gel capsule pharmaceutical formulations |
| CN102382165B (zh) * | 2011-12-02 | 2014-05-07 | 华润赛科药业有限责任公司 | 一种度他雄胺的制备方法 |
| CN102532236B (zh) * | 2012-01-05 | 2014-04-16 | 中国药科大学 | 甾体类5α-还原酶抑制剂、其制备方法及其医药用途 |
| CN103554210A (zh) * | 2012-01-05 | 2014-02-05 | 中国药科大学 | 甾体类5α-还原酶抑制剂、其制备方法及其医药用途 |
| KR101976137B1 (ko) | 2012-01-25 | 2019-05-09 | 한미약품 주식회사 | 두타스테라이드 함유 자가 유화 약물전달 시스템용 조성물 및 이의 제조 방법 |
| US9790233B2 (en) | 2012-04-16 | 2017-10-17 | Case Western Reserve University | Compositions and methods of modulating 15-PGDH activity |
| WO2014002015A1 (en) | 2012-06-25 | 2014-01-03 | Ranbaxy Laboratories Limited | Pharmaceutical composition comprising dutasteride |
| CA2902335C (en) * | 2013-03-14 | 2021-09-14 | Pellficure Pharmaceuticals, Inc. | Novel therapy for prostate carcinoma |
| CN103254268A (zh) * | 2013-05-16 | 2013-08-21 | 寿光市富康化学工业有限公司 | 一种制备度他雄胺的工艺 |
| BR102013020508B1 (pt) | 2013-08-12 | 2021-01-12 | Ems S/A. | Forma de dosagem que compreende um inibidor de esteroide 5-alfa-redutase e um bloqueador alfa, processo para a preparaçãode uma forma de dosagem e uso da forma de dosagem |
| EP3057973B1 (en) | 2013-10-15 | 2019-09-04 | Case Western Reserve University | Compositions comprising a 15-pgdh inhibitor for the healing of wounds |
| ES2555485T1 (es) | 2014-05-26 | 2016-01-04 | Galenicum Health S.L. | Composiciones farmacéuticas que contienen un agente activo |
| WO2016090373A1 (en) | 2014-12-05 | 2016-06-09 | Case Western Reserve University | Compositions and methods of modulating s-nitrosylation |
| KR101590072B1 (ko) | 2014-12-23 | 2016-01-29 | 한미약품 주식회사 | 두타스테라이드를 포함하는 자가유화 약물전달 시스템용 조성물 |
| CN107592863B (zh) * | 2015-03-13 | 2021-09-10 | 陶氏环球技术有限责任公司 | 具有含有磷环的配体的铬络合物和由其得到的烯烃低聚反应催化剂 |
| KR102503428B1 (ko) | 2015-12-22 | 2023-02-24 | 한미약품 주식회사 | 두타스테라이드를 포함하는 경구용 연질 캡슐 제형용 포장재 |
| KR101968754B1 (ko) | 2016-03-16 | 2019-04-12 | 한미약품 주식회사 | 두타스테라이드 및 탐수로신 함유 경질 캡슐 복합제 및 그 제조방법 |
| KR101716878B1 (ko) | 2016-05-12 | 2017-03-15 | 주식회사 유유제약 | 글리세롤 지방산에스테르유도체 또는 프로필렌글리콜 지방산에스테르유도체를 함유한 두타스테리드와 타다라필의 복합 캡슐제제 조성물 및 이의 제조방법 |
| US11690847B2 (en) | 2016-11-30 | 2023-07-04 | Case Western Reserve University | Combinations of 15-PGDH inhibitors with corticosteroids and/or TNF inhibitors and uses thereof |
| WO2018145080A1 (en) | 2017-02-06 | 2018-08-09 | Case Western Reserve University | Compositions and methods of modulating short-chain dehydrogenase activity |
| KR102490397B1 (ko) | 2017-09-01 | 2023-01-26 | 제이더블유중외제약 주식회사 | 두타스테라이드를 포함하는 고형 제제 및 이의 제조방법 |
| KR101996597B1 (ko) | 2017-10-13 | 2019-07-31 | 주식회사 유유제약 | 두타스테리드와 타다라필을 용해시킨 경구용 캡슐 제형의 복합제제 |
| WO2019225924A1 (ko) * | 2018-05-21 | 2019-11-28 | (주)인벤티지랩 | 두타스테라이드를 포함하는 마이크로 입자 및 이의 제조 방법 |
| KR102281252B1 (ko) | 2018-05-21 | 2021-07-23 | (주)인벤티지랩 | 두타스테라이드를 포함하는 마이크로 입자 및 이의 제조 방법 |
| CR20210328A (es) | 2018-11-21 | 2021-12-02 | Univ Case Western Reserve | Composiciones y métodos para modular la actividad de deshidrogenasas de cadena corta |
| KR20200074759A (ko) | 2018-12-17 | 2020-06-25 | 동국제약 주식회사 | 두타스테라이드를 함유하는 고형제제 |
| KR20230053551A (ko) | 2020-05-20 | 2023-04-21 | 로데오 테라퓨틱스 코포레이션 | 단쇄 데히드로게나아제 활성을 조절하는 조성물 및 방법 |
| WO2024144084A1 (ko) * | 2022-12-26 | 2024-07-04 | 주식회사 유영제약 | 주 1회 투여를 위한 정제 형태의 고함량 두타스테리드 약제학적 조성물 및 이의 제조방법 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0484094A2 (en) * | 1990-10-29 | 1992-05-06 | Sankyo Company Limited | Azasteroid compounds for the treatment of prostatic hypertrophy, their preparation and use |
Family Cites Families (78)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4191759A (en) * | 1978-04-13 | 1980-03-04 | Merck & Co., Inc. | N-substituted-17β-carbamoylandrost-4-en-3-one 5α reductase inhibitors |
| AU527030B2 (en) * | 1978-04-13 | 1983-02-10 | Merck & Co., Inc. | 4-aza-17-substituted-5a-androstan-3-ones |
| US4377584A (en) * | 1978-04-13 | 1983-03-22 | Merck & Co., Inc. | 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors |
| US4220775A (en) * | 1979-03-15 | 1980-09-02 | Merck & Co., Inc. | Preparation of 4-aza-17-substituted-5α-androstan-3-ones useful as 5α-reductase inhibitors |
| US4317817A (en) * | 1979-08-27 | 1982-03-02 | Richardson-Merrell Inc. | Novel steroid 5α-reductase inhibitors |
| DK465481A (da) * | 1980-11-21 | 1982-05-22 | Hoffmann La Roche | Fremgangsmaade til fremstilling af d-homostemoider |
| EP0314199B1 (en) * | 1984-02-27 | 1991-09-18 | Merck & Co. Inc. | 17 beta-substituted-4-aza-5 alpha-androstenones and their use as 5 alpha-reductase inhibitors |
| NZ211145A (en) * | 1984-02-27 | 1988-10-28 | Merck & Co Inc | 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions |
| US4760071A (en) * | 1984-02-27 | 1988-07-26 | Merck & Co., Inc. | 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors |
| US5049562A (en) * | 1984-02-27 | 1991-09-17 | Merck & Co., Inc. | 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors |
| GB8505862D0 (en) * | 1985-03-07 | 1985-04-11 | Erba Farmitalia | Steroidic 5alpha-reductase inhibitors |
| DE3780778T2 (de) * | 1986-11-20 | 1993-01-14 | Merck & Co Inc | Topisches arzneimittel enthaltend 17-beta-methoxy-carbonyl-4-methyl-4-aza-5-alpha-androst-1-en-3-one. |
| US4845104A (en) * | 1986-11-20 | 1989-07-04 | Merck & Co., Inc. | Oxidized analogs of 17β-N-monosubstituted-carbamoyl-4-aza-5-α-androstan-3-ones |
| US5110939A (en) * | 1987-01-28 | 1992-05-05 | Smithkline Beecham Corporation | Intermediates in the preparation of steriod 5-alpha-reductase inhibitors |
| US4888336A (en) * | 1987-01-28 | 1989-12-19 | Smithkline Beckman Corporation | Steroid 5-alpha-reductase inhibitors |
| US4814324A (en) * | 1987-03-06 | 1989-03-21 | Merck & Co., Inc. | Sterol inhibitors of testosterone 5α-reductase |
| EP0285382B1 (en) * | 1987-04-03 | 1994-04-13 | Merck & Co. Inc. | Treatment of androgenic alopecia with 17beta-n-monosubstituted-carbamoyl-4-aza-5alpha-androst-1-en-3-ones |
| DE3888378T2 (de) * | 1987-04-03 | 1994-09-29 | Merck & Co Inc | Behandlung von Prostatacarcinoma mit 17-beta-n-monosubstituierten-Carbamoyl-4-aza-5-alpha-Androst-1-en-3-onen. |
| ZA883034B (en) * | 1987-04-29 | 1989-03-29 | Smithkline Beckman Corp | Steroid 5-alpha-reductase inhibitors |
| US5041433A (en) * | 1987-04-29 | 1991-08-20 | Smithkline Beecham Corporation | 11-keto or hydroxy 3,5-diene steroids as inhibitors of steriod 5-α-reductase |
| US4910226A (en) * | 1987-04-29 | 1990-03-20 | Smithkline Beckman Corporation | Steroid 5-alpha-reductase inhibitors |
| NZ225100A (en) * | 1987-06-29 | 1991-09-25 | Merck & Co Inc | Reaction of steroids (including 4-azasteroids) with a silylating agent in the presence of a quinone to introduce a delta' double bond and silylated intermediates |
| US4954446A (en) * | 1988-05-25 | 1990-09-04 | Smithkline Beecham Corporation | Aromatic steroid 5-α-reductase inhibitors |
| JP2675418B2 (ja) * | 1988-05-25 | 1997-11-12 | スミスクライン・ベックマン・コーポレイション | 芳香族ステロイド５‐α‐レダクターゼ抑制剤 |
| US5237061A (en) * | 1988-10-31 | 1993-08-17 | Merck & Co., Inc. | Methods of synthesizing benign prostatic hypertropic agents and their intermediates |
| US4882319A (en) * | 1988-12-23 | 1989-11-21 | Smithkline Beckman Corporation | Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase |
| US4970205A (en) * | 1988-12-23 | 1990-11-13 | Smithkline Beecham Corporation | Sulfonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase |
| US4946834A (en) * | 1988-12-23 | 1990-08-07 | Smithkline Beecham Corporation | Phosphonic acid substituted steroids as steroid 5α-reductase inhibitors |
| US5026882A (en) * | 1988-12-23 | 1991-06-25 | Smithkline Beecham Corporation | Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase |
| US4937237A (en) * | 1988-12-23 | 1990-06-26 | Smithkline Beckman Corporation | Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -reductase |
| US4966898A (en) * | 1989-08-15 | 1990-10-30 | Merrell Dow Pharmaceuticals Inc. | 4-substituted 17β-(cyclopropylamino)androst-5-en-3β-ol and related compounds useful as C17-20 lyase inhibitors |
| US4966897A (en) * | 1989-08-15 | 1990-10-30 | Merrell Dow Pharmaceuticals Inc. | 4-substituted 17β-(cyclopropyloxy)androst-5-en-3β-ol and related compounds useful as C17-20 lyase inhibitors |
| CA2023157A1 (en) * | 1989-08-21 | 1991-02-22 | Gary H. Rasmusson | 17 beta-acyl-4-aza-5 alpha-androst-1-ene-3-ones as 5 alpha-reductase inhibitors |
| US5032586A (en) * | 1989-08-24 | 1991-07-16 | Smithkline Beecham Corporation | 7-keto or hydroxy 3,5-diene steroids as inhibitors of steroid 5-alpha reductase |
| US5021575A (en) * | 1989-11-13 | 1991-06-04 | Merck & Co., Inc. | Method for introducing a 1,2 double bond into azasteroids |
| US5100917A (en) * | 1989-12-29 | 1992-03-31 | Merrell Dow Pharmaceuticals Inc. | Novel a-nor-steroid-3-carboxylic acid derivatives |
| GB9002922D0 (en) * | 1990-02-09 | 1990-04-04 | Erba Carlo Spa | 17 beta-substituted-4-aza-5 alpha-androstan-3-one derivatives and process for their preparation |
| US5098908A (en) * | 1990-06-20 | 1992-03-24 | Merck & Co., Inc. | 17β-hydroxybenzoyl-4-aza-5α-androst-1-en-3-ones as testosterone reductase inhibitors |
| US5061802A (en) * | 1990-06-20 | 1991-10-29 | Merck & Co. Inc. | 17β-aminobenzoyl-4-aza-5α-androst-1-en-3-ones as benign prostatic hypertrophy agents |
| EP0462664A3 (en) * | 1990-06-20 | 1992-11-25 | Merck & Co. Inc. | Specific 17beta-thiobenzoyl-4-aza-5alpha-androst-1-en-3-ones as antiandrogenic agents |
| EP0462662A3 (en) * | 1990-06-20 | 1992-08-19 | Merck & Co. Inc. | 17beta-n-monosubstituted adamantyl/norbornanyl carbamoyl-4-aza-5alpha-androst-1-en-3-ones and androstan-3-ones |
| EP0462665A3 (en) * | 1990-06-20 | 1993-06-30 | Merck & Co. Inc. | Selected 17beta-polyaroyl-4-aza-5alpha-androst-1-en-3-ones as steroidal reductase inhibitors |
| AU637247B2 (en) * | 1990-08-01 | 1993-05-20 | Merrell Dow Pharmaceuticals Inc. | 4-amino-delta4-steroids and their use as 5alpha-reductase inhibitors |
| NZ239141A (en) * | 1990-08-01 | 1994-04-27 | Merrell Dow Pharma | 4-amino-delta-4,6-steroids; preparatory processes and pharmaceutical compositions |
| US5318961A (en) * | 1990-08-01 | 1994-06-07 | Merrell Dow Pharmaceuticals Inc. | 4-amino-Δ4-steroids and their use as 5α-reductase inhibitors |
| US5120847A (en) * | 1990-08-27 | 1992-06-09 | Merck & Co., Inc. | Process for iodinating or brominating the α-methylenic carbon of a secondary amide |
| US5091534A (en) * | 1990-08-27 | 1992-02-25 | Merck & Co., Inc. | Trialkylsilyl trifluoromethanesulfonate mediated α-methylenic carbon functionalization of 4-AZA-5α-androstan-3-one steroids |
| US5061801A (en) * | 1990-09-24 | 1991-10-29 | Merck & Co., Inc. | Intermediate for making 3-oxo-4-aza-androst-1-ene 17β-ketones |
| CA2050824A1 (en) * | 1990-09-24 | 1992-03-25 | John M. Williams | Process for making 3-oxo-4-aza-androst-1-ene 17-.beta.-ketones |
| US5061803A (en) * | 1990-09-24 | 1991-10-29 | Merck & Co., Inc. | Process for making 17-beta alkanoyl 3-oxo-4-aza-5-α-androst-1-enes |
| IL101243A (en) * | 1991-03-20 | 1999-12-22 | Merck & Co Inc | Pharmaceutical preparations for the treatment of benign prostatic hyperplasia containing steroid history |
| IL101245A0 (en) * | 1991-03-20 | 1992-11-15 | Merck & Co Inc | Pharmaceutical compositions for the treatment of prostatic cancer |
| AU1893492A (en) * | 1991-04-17 | 1992-11-17 | Merck & Co., Inc. | Pharmaceutical combination for the treatment of benign prostatic hyperplasia comtaining a 5 alpha-reductase inhibitor |
| GB9115676D0 (en) * | 1991-07-19 | 1991-09-04 | Erba Carlo Spa | Process for the preparation of 17 beta substituted-4-aza-5 alpha-androstan-3-one derivatives |
| US5304562A (en) * | 1991-10-09 | 1994-04-19 | Ciba-Geigy Corporation | 17β-substituted Aza-androstane derivatives |
| US5543406A (en) * | 1991-12-20 | 1996-08-06 | Glaxo Wellcome, Inc. | Inhibitors of 5-α-testosterone reductase |
| JP3164389B2 (ja) * | 1991-12-25 | 2001-05-08 | 三共株式会社 | ４−アザステロイド類 |
| EP0646007B1 (en) * | 1992-05-20 | 1997-08-13 | Merck & Co. Inc. | NEW DELTA-17 AND DELTA-20 OLEFINIC AND SATURATED 17$g(b)-SUBSTITUTED-4-AZA-5$g(a)-ANDROSTAN-3-ONES AS 5$g(a)-REDUCTASE INHIBITORS |
| DE69329856D1 (de) * | 1992-05-20 | 2001-02-15 | Merck & Co Inc | Ester derivate von 4-aza-steroiden |
| EP0641204B1 (en) * | 1992-05-20 | 2000-08-16 | Merck & Co. Inc. | 17-ethers and thioethers of 4-aza-steroids |
| AU675225B2 (en) * | 1992-05-20 | 1997-01-30 | Merck & Co., Inc. | 17-amino substituted 4-azasteroid 5alpha-reductase inhibitors |
| CA2135167A1 (en) * | 1992-05-20 | 1993-11-25 | Donald W. Graham | New 17-ester, amide, and ketone derivatives of 3-oxo-4- azasteroids as 5a-reductase inhibitors |
| WO1993023039A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors |
| RU94046044A (ru) * | 1992-05-20 | 1996-10-10 | Мерк Энд Ко. | Новые 7 бета -замещенные 4-аза- 5 альфа -холестан-оны в качестве ингибиторов 5 альфа -редуктазы, фармацевтическая композиция на их основе, способ ее получения |
| US5710275A (en) * | 1992-05-20 | 1998-01-20 | Merck & Co., Inc. | 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors |
| ATE195129T1 (de) * | 1992-05-20 | 2000-08-15 | Merck & Co Inc | 4-azasteroide als 5-alpha-reduktase |
| WO1993023053A1 (en) * | 1992-05-21 | 1993-11-25 | Endorecherche Inc. | INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY |
| GB9210880D0 (en) * | 1992-05-21 | 1992-07-08 | Smithkline Beecham Corp | Compounds |
| GB9216284D0 (en) * | 1992-07-31 | 1992-09-16 | Erba Carlo Spa | Fluorinated 17beta-substituted 4-aza-5alpha-androstane-3-one derivatives |
| GB9216329D0 (en) * | 1992-07-31 | 1992-09-16 | Erba Carlo Spa | 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives |
| HU212459B (en) * | 1992-10-02 | 1996-06-28 | Richter Gedeon Vegyeszet | Process for producing new 17-beta-substituted 4-aza-androstane-derivatives and pharmaceutical compositions containing them |
| US5278159A (en) * | 1992-10-06 | 1994-01-11 | Merck & Co., Inc. | Aryl ester derivatives of 3-oxo-4-aza-androstane 17-β-carboxylates as 5-α-reductase inhibitors |
| US5693810A (en) * | 1992-10-06 | 1997-12-02 | Merck & Co., Inc. | 17 β-carboxanilides of 4-aza-5α-androstan-3-ones as 5α-reductase inhibitors |
| AP9300589A0 (en) * | 1992-11-18 | 1994-01-31 | Smithkline Beecham Corp | Novel 17a and 17b substituted acyl-3-carboxy 3,5-diene steroidal compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to inhibit steroid 5-a-reductase. |
| AP459A (en) * | 1992-12-18 | 1996-02-14 | Glaxo Wellcome Inc | Substituted 6-azaandrostenones. |
| US5380728A (en) * | 1993-02-10 | 1995-01-10 | Merck & Co., Inc. | Aldehyde metabolite of 17β-N-monosubstituted-carbamoyl-4-aza-5α-a |
| US5438061A (en) * | 1993-07-16 | 1995-08-01 | Merck & Co., Inc. | 7-substituted-δ4-6-azasteroid derivatives as 5α-reductase inhibitors |
| TW408127B (en) * | 1993-09-17 | 2000-10-11 | Glaxo Inc | Androstenones |
-
1994
- 1994-09-03 TW TW083108127A patent/TW369521B/zh active
- 1994-09-13 IS IS4205A patent/IS1713B/is unknown
- 1994-09-14 MY MYPI94002449A patent/MY119778A/en unknown
- 1994-09-15 PE PE1994250737A patent/PE15095A1/es not_active Application Discontinuation
- 1994-09-15 AP APAP/P/1994/000669A patent/AP494A/en active
- 1994-09-15 ZA ZA947119A patent/ZA947119B/xx unknown
- 1994-09-15 ZA ZA947118A patent/ZA947118B/xx unknown
- 1994-09-16 ES ES94929828T patent/ES2113127T3/es not_active Expired - Lifetime
- 1994-09-16 HR HR940563A patent/HRP940563B1/xx not_active IP Right Cessation
- 1994-09-16 CA CA002462061A patent/CA2462061A1/en not_active Abandoned
- 1994-09-16 JP JP7509391A patent/JP2904310B2/ja not_active Expired - Lifetime
- 1994-09-16 SK SK347-96A patent/SK281869B6/sk unknown
- 1994-09-16 SG SG1996007353A patent/SG52650A1/en unknown
- 1994-09-16 SI SI9430130T patent/SI0719278T1/xx unknown
- 1994-09-16 CZ CZ1996745A patent/CZ286069B6/cs not_active IP Right Cessation
- 1994-09-16 RO RO96-00537A patent/RO117455B1/ro unknown
- 1994-09-16 WO PCT/US1994/010530 patent/WO1995007927A1/en active IP Right Grant
- 1994-09-16 DE DE69407978T patent/DE69407978T2/de not_active Expired - Lifetime
- 1994-09-16 DK DK94929828T patent/DK0719278T3/da active
- 1994-09-16 AT AT94929828T patent/ATE162199T1/de active
- 1994-09-16 CN CN94193410A patent/CN1057771C/zh not_active Expired - Lifetime
- 1994-09-16 EE EE9600130A patent/EE03241B1/xx unknown
- 1994-09-16 PL PL94313492A patent/PL180002B1/pl unknown
- 1994-09-16 CA CA002170047A patent/CA2170047C/en not_active Expired - Lifetime
- 1994-09-16 KR KR1019960701363A patent/KR100364953B1/ko not_active IP Right Cessation
- 1994-09-16 IL IL11097894A patent/IL110978A/en active Protection Beyond IP Right Term
- 1994-09-16 EP EP94929828A patent/EP0719278B1/en not_active Expired - Lifetime
- 1994-09-16 AU AU78751/94A patent/AU690925B2/en not_active Expired
- 1994-09-16 HU HU9600656A patent/HU220060B/hu unknown
- 1994-09-16 NZ NZ274642A patent/NZ274642A/en not_active IP Right Cessation
- 1994-09-16 DE DE10399022C patent/DE10399022I2/de active Active
- 1994-09-16 RU RU96108410A patent/RU2140926C1/ru active
- 1994-10-10 SA SA94150231A patent/SA94150231B1/ar unknown
-
1995
- 1995-03-16 US US08/405,120 patent/US5565467A/en not_active Expired - Lifetime
-
1996
- 1996-03-08 BG BG100410A patent/BG62363B1/bg unknown
- 1996-03-13 OA OA60795A patent/OA10575A/en unknown
- 1996-03-15 FI FI961231A patent/FI115216B/fi not_active IP Right Cessation
- 1996-03-15 NO NO961080A patent/NO306117B1/no not_active IP Right Cessation
- 1996-08-22 US US08/708,167 patent/US5846976A/en not_active Expired - Lifetime
-
1997
- 1997-04-23 BR BR1100329-4A patent/BR1100329A/pt active IP Right Grant
-
1998
- 1998-02-12 GR GR980400317T patent/GR3026144T3/el unknown
- 1998-04-20 HK HK98103307A patent/HK1004334A1/xx not_active IP Right Cessation
-
2001
- 2001-01-03 CY CY0100002A patent/CY2219B1/xx unknown
-
2003
- 2003-03-07 NO NO2003003C patent/NO2003003I2/no unknown
- 2003-03-31 NL NL300122C patent/NL300122I2/nl unknown
- 2003-06-18 LU LU91027C patent/LU91027I2/fr unknown
-
2004
- 2004-07-26 CY CY200400002C patent/CY2004002I1/el unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0484094A2 (en) * | 1990-10-29 | 1992-05-06 | Sankyo Company Limited | Azasteroid compounds for the treatment of prostatic hypertrophy, their preparation and use |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AP494A (en) | Androstenone derivative. | |
| EP0719277B1 (en) | Androstenones | |
| EP0674651B1 (en) | Substituted 6-azaandrostenones | |
| US5998427A (en) | Androstenones | |
| US5708001A (en) | Substituted 6-azaandrostenones | |
| US5817818A (en) | Androstenones | |
| JP3824636B2 (ja) | アンドロステノン | |
| WO1996030391A1 (en) | Substituted 6-azacholesten-3-ones |