EE03241B1 - Androstenooni derivaat 17ß-N-(2,5-bis(trifluorometüül))fenüülkarbamoüül-4-asa-5a-androst-1-een-3-oon ja selle farmatseutiliselt vastuvõetavad solvaadid - Google Patents
Androstenooni derivaat 17ß-N-(2,5-bis(trifluorometüül))fenüülkarbamoüül-4-asa-5a-androst-1-een-3-oon ja selle farmatseutiliselt vastuvõetavad solvaadidInfo
- Publication number
- EE03241B1 EE03241B1 EE9600130A EE9600130A EE03241B1 EE 03241 B1 EE03241 B1 EE 03241B1 EE 9600130 A EE9600130 A EE 9600130A EE 9600130 A EE9600130 A EE 9600130A EE 03241 B1 EE03241 B1 EE 03241B1
- Authority
- EE
- Estonia
- Prior art keywords
- androst
- phenylcarbamoyl
- aza
- trifluoromethyl
- bis
- 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US12328093A | 1993-09-17 | 1993-09-17 | |
PCT/US1994/010530 WO1995007927A1 (fr) | 1993-09-17 | 1994-09-16 | Derive de l'androstenone |
Publications (1)
Publication Number | Publication Date |
---|---|
EE03241B1 true EE03241B1 (et) | 1999-12-15 |
Family
ID=22407744
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EE9600130A EE03241B1 (et) | 1993-09-17 | 1994-09-16 | Androstenooni derivaat 17ß-N-(2,5-bis(trifluorometüül))fenüülkarbamoüül-4-asa-5a-androst-1-een-3-oon ja selle farmatseutiliselt vastuvõetavad solvaadid |
Country Status (41)
Country | Link |
---|---|
US (2) | US5565467A (fr) |
EP (1) | EP0719278B1 (fr) |
JP (1) | JP2904310B2 (fr) |
KR (1) | KR100364953B1 (fr) |
CN (1) | CN1057771C (fr) |
AP (1) | AP494A (fr) |
AT (1) | ATE162199T1 (fr) |
AU (1) | AU690925B2 (fr) |
BG (1) | BG62363B1 (fr) |
BR (1) | BR1100329A (fr) |
CA (2) | CA2462061A1 (fr) |
CY (2) | CY2219B1 (fr) |
CZ (1) | CZ286069B6 (fr) |
DE (2) | DE10399022I2 (fr) |
DK (1) | DK0719278T3 (fr) |
EE (1) | EE03241B1 (fr) |
ES (1) | ES2113127T3 (fr) |
FI (1) | FI115216B (fr) |
GR (1) | GR3026144T3 (fr) |
HK (1) | HK1004334A1 (fr) |
HR (1) | HRP940563B1 (fr) |
HU (1) | HU220060B (fr) |
IL (1) | IL110978A (fr) |
IS (1) | IS1713B (fr) |
LU (1) | LU91027I2 (fr) |
MY (1) | MY119778A (fr) |
NL (1) | NL300122I2 (fr) |
NO (2) | NO306117B1 (fr) |
NZ (1) | NZ274642A (fr) |
OA (1) | OA10575A (fr) |
PE (1) | PE15095A1 (fr) |
PL (1) | PL180002B1 (fr) |
RO (1) | RO117455B1 (fr) |
RU (1) | RU2140926C1 (fr) |
SA (1) | SA94150231B1 (fr) |
SG (1) | SG52650A1 (fr) |
SI (1) | SI0719278T1 (fr) |
SK (1) | SK281869B6 (fr) |
TW (1) | TW369521B (fr) |
WO (1) | WO1995007927A1 (fr) |
ZA (2) | ZA947118B (fr) |
Families Citing this family (76)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1993023051A1 (fr) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | NOUVEAUX DERIVES 17-ESTER, AMIDE ET CETONE DE 3-OXO-4-AZASTEROIDES UTILISES COMME INHIBITEURS DE 5a-REDUCTASE |
AU5323694A (en) * | 1992-10-06 | 1994-04-26 | Merck & Co., Inc. | 17beta -carboxanilides of 4-aza-5alpha-androstan-3-ones as 5alpha-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 |
EP0724592B1 (fr) * | 1993-10-21 | 1999-01-07 | Merck & Co. Inc. | Inhibiteurs de l'isozyme alpha-reductase 1 de 4-aza-androstane-5 a substitution en position 16 |
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 |
HUP0101809A3 (en) * | 1998-03-11 | 2002-07-29 | Endorech Inc Sainte Foy | Inhibitors of type 5 and type 3 17betha-hydroxysteroid dehydrogenase and methods for their use |
EP1321146A3 (fr) * | 1998-03-11 | 2004-06-02 | Endorecherche Inc. | Inhibiteurs de la 17beta-hydroxysteroide deshydrogénase du type 5 et du type 3 ainsi que leurs méthodes d'utilisation |
US5998427A (en) * | 1998-05-14 | 1999-12-07 | Glaxo Wellcome Inc. | Androstenones |
AU4701299A (en) * | 1998-06-23 | 2000-01-10 | Stuart R. Adler | Therapeutic applications of estrogenic carboxylic acids |
US6410565B1 (en) | 1999-02-03 | 2002-06-25 | Eli Lilly And Company | α1-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 |
AU2002331916B2 (en) * | 2001-10-03 | 2008-07-24 | Merck Sharp & Dohme Corp. | Androstane 17-beta-carboxamides as androgen receptor modulators |
DE60317626T2 (de) * | 2002-01-25 | 2008-10-23 | Asahi Glass Co., Ltd. | Verfahren zur herstellung von 2,5-bis(trifluormethyl)nitrobenzol |
BR0309435A (pt) | 2002-04-24 | 2005-02-15 | Boehringer Ingelheim Pharma | Combinação farmacêutica para o tratamento de hiperplasia prostática benigna ou para a prevenção a longo prazo de retenção urinária aguda |
AU2003223754B2 (en) * | 2002-04-30 | 2007-08-16 | Merck Sharp & Dohme Corp. | 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 (fr) * | 2004-03-22 | 2005-10-06 | Ranbaxy Laboratories Limited | Therapie combinee destinee a reduire les symptomes des voies urinaires |
EP2305352A1 (fr) | 2004-04-02 | 2011-04-06 | Merck Sharp & Dohme Corp. | Inhibiteurs de la 5-alpha-reductase pour le traitement d'hommes aux troubles métaboliques et anthropométriques |
AU2005280334A1 (en) * | 2004-08-25 | 2006-03-09 | Merck Sharp & Dohme Corp. | Androgen receptor modulators |
EP1824495A2 (fr) * | 2004-12-03 | 2007-08-29 | ProteoSys AG | Utilisation de finasteride, dutasteride et de composes associes dans la prevention ou le traitement de troubles neurologiquement associes |
US20060193804A1 (en) * | 2005-02-24 | 2006-08-31 | L'oreal | Haircare use of cyclic amine derivatives |
AU2006229840B2 (en) * | 2005-03-25 | 2010-12-23 | Merck Sharp & Dohme Corp. | Method of treating men with testosterone supplement and 5alpha-reductase inhibitor |
WO2007120263A2 (fr) * | 2005-11-10 | 2007-10-25 | Dr. Reddy's Laboratories Ltd. | Préparation de dutastéride |
EP1897533A1 (fr) * | 2006-09-08 | 2008-03-12 | Revotar Biopharmaceuticals AG | Utilisation de 1,6-Bis[3-(3-carboxyméthylphényl)-4-(2-alpha-D-mannopyranosyl-oxy)-phényl]hexane pour la préparation des compositions cosmétiques. |
EP1946756A1 (fr) * | 2007-01-17 | 2008-07-23 | Revotar Biopharmaceuticals AG | Utilisation d'entacapone dans les compositions cosmétiques, dermatologiques et pharmaceutiques |
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 (fr) | 2007-12-21 | 2009-04-22 | Siegfried Generics International AG | Composition pharmaceutique qui comporte de la dutastéride |
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 |
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 |
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 |
CN102215845A (zh) | 2008-04-03 | 2011-10-12 | 哈博生物科学公司 | 药学试剂的固体形式 |
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 |
WO2011004242A2 (fr) * | 2009-07-09 | 2011-01-13 | Aurobindo Pharma Limited | Procédé amélioré de préparation du dutastéride |
FR2949052B1 (fr) | 2009-08-13 | 2015-03-27 | Oreal | Procede de traitement cosmetique du cuir chevelu. |
EP2468262A1 (fr) | 2010-12-06 | 2012-06-27 | Krka Tovarna Zdravil, D.D., Novo Mesto | Composition pharmaceutique contenant de la dutastéride |
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 |
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 |
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 |
KR101976137B1 (ko) | 2012-01-25 | 2019-05-09 | 한미약품 주식회사 | 두타스테라이드 함유 자가 유화 약물전달 시스템용 조성물 및 이의 제조 방법 |
JP6203820B2 (ja) | 2012-04-16 | 2017-09-27 | ケース ウエスタン リザーブ ユニバーシティ | 15−pgdh活性を調節する組成物および方法 |
WO2014002015A1 (fr) | 2012-06-25 | 2014-01-03 | Ranbaxy Laboratories Limited | Composition pharmaceutique comprenant du dutastéride |
EP2968219B1 (fr) * | 2013-03-14 | 2019-04-24 | Pellficure Pharmaceuticals, Inc. | Nouvelle thérapie pour le carcinome de la prostate |
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 |
AU2014342811B2 (en) | 2013-10-15 | 2019-01-03 | Board Of Regents Of The University Of Texas System | Compositions and methods of modulating short-chain dehydrogenase activity |
ES2555485T1 (es) | 2014-05-26 | 2016-01-04 | Galenicum Health S.L. | Composiciones farmacéuticas que contienen un agente activo |
KR101590072B1 (ko) | 2014-12-23 | 2016-01-29 | 한미약품 주식회사 | 두타스테라이드를 포함하는 자가유화 약물전달 시스템용 조성물 |
BR112017019446A2 (pt) * | 2015-03-13 | 2018-04-24 | Dow Global Technologies Llc | complexo de cromo com um ligante contendo fosfaciclo e catalisador de oligomerizacão de olefina do mesmo |
KR102503428B1 (ko) | 2015-12-22 | 2023-02-24 | 한미약품 주식회사 | 두타스테라이드를 포함하는 경구용 연질 캡슐 제형용 포장재 |
CN109152743B (zh) | 2016-03-16 | 2022-01-07 | 韩美药品株式会社 | 含有度他雄胺和坦索罗辛的硬胶囊复合物及其制备方法 |
KR101716878B1 (ko) | 2016-05-12 | 2017-03-15 | 주식회사 유유제약 | 글리세롤 지방산에스테르유도체 또는 프로필렌글리콜 지방산에스테르유도체를 함유한 두타스테리드와 타다라필의 복합 캡슐제제 조성물 및 이의 제조방법 |
EP3548035A4 (fr) | 2016-11-30 | 2020-07-22 | Case Western Reserve University | Combinaisons d'inhibiteurs de 15-pgdh avec des corcostéroïdes et/ou des inhibiteurs du tnf et leurs utilisations |
US11718589B2 (en) | 2017-02-06 | 2023-08-08 | Case Western Reserve University | Compositions and methods of modulating short-chain dehydrogenase |
BR112020004197A2 (pt) | 2017-09-01 | 2020-09-08 | Jw Pharmaceutical Corporation | preparação sólida compreendendo dutasterida e método para preparar a mesma |
KR101996597B1 (ko) | 2017-10-13 | 2019-07-31 | 주식회사 유유제약 | 두타스테리드와 타다라필을 용해시킨 경구용 캡슐 제형의 복합제제 |
KR102281252B1 (ko) * | 2018-05-21 | 2021-07-23 | (주)인벤티지랩 | 두타스테라이드를 포함하는 마이크로 입자 및 이의 제조 방법 |
WO2019225924A1 (fr) * | 2018-05-21 | 2019-11-28 | (주)인벤티지랩 | Microparticules comprenant du dutastéride et procédé de préparation associé |
BR112021009832A2 (pt) | 2018-11-21 | 2021-08-17 | Case Western Reserve University | composições e métodos de modulação da atividade da desidrogenase de cadeia curta |
KR20200074759A (ko) | 2018-12-17 | 2020-06-25 | 동국제약 주식회사 | 두타스테라이드를 함유하는 고형제제 |
MX2022014637A (es) | 2020-05-20 | 2023-03-03 | Rodeo Therapeutics Corp | Composiciones y metodos para modular la actividad de deshidrogenasas de cadena corta. |
Family Cites Families (79)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
US4191759A (en) * | 1978-04-13 | 1980-03-04 | Merck & Co., Inc. | N-substituted-17β-carbamoylandrost-4-en-3-one 5α 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 |
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 |
IL74365A (en) * | 1984-02-27 | 1990-07-26 | Merck & Co Inc | 17beta-(n-t.-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one and pharmaceutical compositions containing it |
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 |
ATE67503T1 (de) * | 1984-02-27 | 1991-10-15 | Merck & Co Inc | 17-beta-substituierte-4-aza-5-alpha-androstenon und ihre anwendung als 5-alpha-reduktaseinhibitoren. |
GB8505862D0 (en) * | 1985-03-07 | 1985-04-11 | Erba Farmitalia | Steroidic 5alpha-reductase inhibitors |
ATE78827T1 (de) * | 1986-11-20 | 1992-08-15 | 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 |
US4888336A (en) * | 1987-01-28 | 1989-12-19 | Smithkline Beckman Corporation | Steroid 5-alpha-reductase inhibitors |
US5110939A (en) * | 1987-01-28 | 1992-05-05 | Smithkline Beecham Corporation | Intermediates in the preparation of steriod 5-alpha-reductase inhibitors |
US4814324A (en) * | 1987-03-06 | 1989-03-21 | Merck & Co., Inc. | Sterol inhibitors of testosterone 5α-reductase |
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. |
EP0285382B1 (fr) * | 1987-04-03 | 1994-04-13 | Merck & Co. Inc. | Traitement d'alopécia androgénique avec 17-bêta-n-monosubstitué-carbamoyl-4-aza-5-alpha-androst-1-en-3-ones |
US4910226A (en) * | 1987-04-29 | 1990-03-20 | Smithkline Beckman Corporation | 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 |
ZA883034B (en) * | 1987-04-29 | 1989-03-29 | Smithkline Beckman Corp | 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 |
WO1989011282A1 (fr) * | 1988-05-25 | 1989-11-30 | Smithkline Beckman Corporation | INHIBITEURS DE 5-alpha-REDUCTASE STEROIDE AROMATIQUE |
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 |
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 |
US4946834A (en) * | 1988-12-23 | 1990-08-07 | Smithkline Beecham Corporation | Phosphonic acid substituted steroids as steroid 5α-reductase 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 |
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 |
CA2023157A1 (fr) * | 1989-08-21 | 1991-02-22 | Gary H. Rasmusson | 17 beta-acyl-4-aza-5-alpha-androst-1-ene-3-ones utilsiables comme inhibiteurs de l'alpha-reductase |
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 |
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 |
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 |
US5318961A (en) * | 1990-08-01 | 1994-06-07 | Merrell Dow Pharmaceuticals Inc. | 4-amino-Δ4-steroids and their use as 5α-reductase inhibitors |
NZ239141A (en) * | 1990-08-01 | 1994-04-27 | Merrell Dow Pharma | 4-amino-delta-4,6-steroids; preparatory processes and pharmaceutical compositions |
AU637247B2 (en) * | 1990-08-01 | 1993-05-20 | Merrell Dow Pharmaceuticals Inc. | 4-amino-delta4-steroids and their use as 5alpha-reductase inhibitors |
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 |
US5120847A (en) * | 1990-08-27 | 1992-06-09 | Merck & Co., Inc. | Process for iodinating or brominating the α-methylenic carbon of a secondary amide |
US5061801A (en) * | 1990-09-24 | 1991-10-29 | Merck & Co., Inc. | Intermediate for making 3-oxo-4-aza-androst-1-ene 17β-ketones |
CA2050824A1 (fr) * | 1990-09-24 | 1992-03-25 | John M. Williams | Methode de preparation de 3-oxo-4-azaandrost-1-en-17.beta.-ones |
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 |
IE76452B1 (en) * | 1990-10-29 | 1997-10-22 | Sankyo Co | Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use |
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 |
WO1992018132A1 (fr) * | 1991-04-17 | 1992-10-29 | Merck & Co., Inc. | Association pharmaceutique destinee au traitement de l'hyperplasie prostatique benigne et contenant un inhibiteur de 5 alpha-reductase |
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 |
ES2118222T3 (es) * | 1991-12-20 | 1998-09-16 | Glaxo Wellcome Inc | Inhibidores de 5-alfa-testosterona reductasa. |
JP3164389B2 (ja) * | 1991-12-25 | 2001-05-08 | 三共株式会社 | 4−アザステロイド類 |
DE69326008T2 (de) * | 1992-05-20 | 2000-03-02 | Merck & Co Inc | 17-amino-substituierte 4-azasteroide als 5-alpha-reductase inhibitoren |
WO1993023039A1 (fr) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | 4-aza-5a-androstan ones substituees utilisees en tant qu'inhibitors de la 5a-reductase |
WO1993023051A1 (fr) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | NOUVEAUX DERIVES 17-ESTER, AMIDE ET CETONE DE 3-OXO-4-AZASTEROIDES UTILISES COMME INHIBITEURS DE 5a-REDUCTASE |
WO1993023040A1 (fr) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | 17-ethers et thioethers de 4-aza-steroides |
WO1993023420A1 (fr) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | NOUVEAUX 4-AZA-5α-ANDROSTANE-3-ONES SUBSTITUES EN POSITION 7β EN TANT QU'INHIBITEURS DE LA 5α-REDUCTASE |
AU672978B2 (en) * | 1992-05-20 | 1996-10-24 | Merck & Co., Inc. | 4-azasteroid 5-alpha-reductase inhibitors |
WO1993023041A1 (fr) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | Derives ester de 4-aza-steroides |
HUT71484A (en) * | 1992-05-20 | 1995-11-28 | Merck & Co Inc | Process for producing of 7beta-substituted-4-aza-5alpha-cholestan-ones as 5-alpha-reductase inhibitors and pharmaceuticals compositions containing them |
CA2135056A1 (fr) * | 1992-05-20 | 1993-11-25 | Donald W. Graham | Nouveaux 17b-a substituant-4-aza-5a-andros-tan-3-ones olefiniques en delta-17 et delta-20 et satures, servant d'inhibiteurs de la 5a-reductase |
UA35589C2 (uk) * | 1992-05-21 | 2001-04-16 | Андорешерш Інк. | ІНГІБІТОРИ ТЕСТОСТЕРОН 5-<font face="Symbol">a</font>-РЕДУКТАЗИ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ ТА СПОСІБ ІНГІБУВАННЯ АКТИВНОСТІ ТЕСТОСТЕРОН 5-<font face="Symbol">a</font>-РЕДУКТАЗИ |
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 |
AU5323694A (en) * | 1992-10-06 | 1994-04-26 | Merck & Co., Inc. | 17beta -carboxanilides of 4-aza-5alpha-androstan-3-ones as 5alpha-reductase inhibitors |
IL107611A0 (en) * | 1992-11-18 | 1994-02-27 | Smithkline Beecham Corp | Steroid compounds and pharmaceutical compositions containing them |
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 ZA ZA947118A patent/ZA947118B/xx unknown
- 1994-09-15 ZA ZA947119A patent/ZA947119B/xx unknown
- 1994-09-15 AP APAP/P/1994/000669A patent/AP494A/en active
- 1994-09-16 CN CN94193410A patent/CN1057771C/zh not_active Expired - Lifetime
- 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 KR KR1019960701363A patent/KR100364953B1/ko not_active IP Right Cessation
- 1994-09-16 DE DE10399022C patent/DE10399022I2/de active Active
- 1994-09-16 AT AT94929828T patent/ATE162199T1/de active
- 1994-09-16 SG SG1996007353A patent/SG52650A1/en unknown
- 1994-09-16 DE DE69407978T patent/DE69407978T2/de not_active Expired - Lifetime
- 1994-09-16 CA CA002462061A patent/CA2462061A1/fr not_active Abandoned
- 1994-09-16 RO RO96-00537A patent/RO117455B1/ro unknown
- 1994-09-16 AU AU78751/94A patent/AU690925B2/en not_active Expired
- 1994-09-16 PL PL94313492A patent/PL180002B1/pl unknown
- 1994-09-16 RU RU96108410A patent/RU2140926C1/ru active
- 1994-09-16 EE EE9600130A patent/EE03241B1/xx unknown
- 1994-09-16 IL IL11097894A patent/IL110978A/en active Protection Beyond IP Right Term
- 1994-09-16 ES ES94929828T patent/ES2113127T3/es not_active Expired - Lifetime
- 1994-09-16 EP EP94929828A patent/EP0719278B1/fr not_active Expired - Lifetime
- 1994-09-16 DK DK94929828T patent/DK0719278T3/da active
- 1994-09-16 WO PCT/US1994/010530 patent/WO1995007927A1/fr active IP Right Grant
- 1994-09-16 JP JP7509391A patent/JP2904310B2/ja not_active Expired - Lifetime
- 1994-09-16 HR HR940563A patent/HRP940563B1/xx not_active IP Right Cessation
- 1994-09-16 CA CA002170047A patent/CA2170047C/fr not_active Expired - Lifetime
- 1994-09-16 NZ NZ274642A patent/NZ274642A/en not_active IP Right Cessation
- 1994-09-16 HU HU9600656A patent/HU220060B/hu unknown
- 1994-09-16 SK SK347-96A patent/SK281869B6/sk unknown
- 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 NO NO961080A patent/NO306117B1/no not_active IP Right Cessation
- 1996-03-15 FI FI961231A patent/FI115216B/fi 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/CY2004002I2/el unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
EE03241B1 (et) | Androstenooni derivaat 17ß-N-(2,5-bis(trifluorometüül))fenüülkarbamoüül-4-asa-5a-androst-1-een-3-oon ja selle farmatseutiliselt vastuvõetavad solvaadid | |
FI944310A0 (fi) | Heteroaryyliamino- ja heteroaryylisuolfonamidosubstituoituja 3-bentsyyliaminometyylipiperidiinejä ja vastaavia yhdisteitä | |
NO307254B1 (no) | 1,2,4-oksadiazolderivater og parasittbekjempningsmiddel inneholdende samme | |
FI944624A0 (fi) | 4-aryyliaminobentsopyraani- ja niiden kaltaisia yhdisteitä | |
ZA976222B (en) | N-(4-aryl-thiazol-2-yl)-sulphonamide derivatives and their use. | |
DK0853617T3 (da) | 2,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinylderivater | |
AU6636598A (en) | Novel 3,4-dialkoxyphenyl derivatives and the use thereof | |
DE69431965T2 (de) | Wirkstoff gegen fettsucht | |
AU7978794A (en) | 3,17-dihydroxy-3,7,16 and/or 17-methyl-androst-5-ene compounds, derivatives thereof, and their use | |
NO954767D0 (no) | 4-amino-17 delser som C17-20-lyase- og 5 | |
PT811593E (pt) | Agentes insecticidas e acaricidas 1,4-diaril-2-fluor-2-buteno | |
HU9502863D0 (en) | 7-azabicyclo-[2.2.1]-heptane and -heptene derivatives as analgesics and anti-inflammatory agents | |
FI934624A0 (fi) | Enantiomera cis-3-(4,6-dihydroxikroman-3-ylmetyl)bensoesyror | |
AU7075694A (en) | Novel cross-linking agents and use thereof | |
AU6871696A (en) | N-(1-isopropyl-2-methyl-1-propenyl)heteroaryloxyacetamides and the use thereof as herbicides | |
ITMI920870A1 (it) | Poliestereimmide trmotropica, procedimento per la sua preparazione e suo impiego | |
BR9510289A (pt) | Monômetros de ciclohexan-1-of 3,3-dissubstituido e compostos relacionados | |
NO306672B1 (no) | N,N-dietyl-8,8-dipropyl-2-azaspiro[4,5]decan-2-propanamindimaleat, farmasöytisk blanding omfattende forbindelsen samt anvendelse derav | |
NO944024D0 (no) | 1,2-dihydro-2-okso-pyridin | |
KR950007960U (ko) | 회전의자 | |
FI931050A0 (fi) | Monitor | |
DK0707579T3 (da) | Piperidinylsubstituerede methanoanthracener som D1/D2-antagonister og 5 HT2-serotanin-antagonister | |
AU4707093A (en) | Pyridyl-substituted 1,3-oxazolidine derivatives and their use as pest-control agents | |
NO942212D0 (no) | 13,14-dihydro-PGF2 | |
AU4659793A (en) | Anorectic epinephrine derivatives |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
KB4A | Valid patent at the end of a year |
Effective date: 20021231 |
|
KB4A | Valid patent at the end of a year |
Effective date: 20031231 |
|
KB4A | Valid patent at the end of a year |
Effective date: 20041231 |
|
GB1A | Change in the ownership or in the address of the owner | ||
KB4A | Valid patent at the end of a year |
Effective date: 20051231 |
|
KB4A | Valid patent at the end of a year |
Effective date: 20061231 |
|
KB4A | Valid patent at the end of a year |
Effective date: 20071231 |
|
KB4A | Valid patent at the end of a year |
Effective date: 20081231 |
|
KB4A | Valid patent at the end of a year |
Effective date: 20091231 |
|
KB4A | Valid patent at the end of a year |
Effective date: 20101231 |