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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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 (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US12328093A | 1993-09-17 | 1993-09-17 | |
PCT/US1994/010530 WO1995007927A1 (en) | 1993-09-17 | 1994-09-16 | Androstenone derivative |
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 (et) |
EP (1) | EP0719278B1 (et) |
JP (1) | JP2904310B2 (et) |
KR (1) | KR100364953B1 (et) |
CN (1) | CN1057771C (et) |
AP (1) | AP494A (et) |
AT (1) | ATE162199T1 (et) |
AU (1) | AU690925B2 (et) |
BG (1) | BG62363B1 (et) |
BR (1) | BR1100329A (et) |
CA (2) | CA2462061A1 (et) |
CY (2) | CY2219B1 (et) |
CZ (1) | CZ286069B6 (et) |
DE (2) | DE69407978T2 (et) |
DK (1) | DK0719278T3 (et) |
EE (1) | EE03241B1 (et) |
ES (1) | ES2113127T3 (et) |
FI (1) | FI115216B (et) |
GR (1) | GR3026144T3 (et) |
HK (1) | HK1004334A1 (et) |
HR (1) | HRP940563B1 (et) |
HU (1) | HU220060B (et) |
IL (1) | IL110978A (et) |
IS (1) | IS1713B (et) |
LU (1) | LU91027I2 (et) |
MY (1) | MY119778A (et) |
NL (1) | NL300122I2 (et) |
NO (2) | NO306117B1 (et) |
NZ (1) | NZ274642A (et) |
OA (1) | OA10575A (et) |
PE (1) | PE15095A1 (et) |
PL (1) | PL180002B1 (et) |
RO (1) | RO117455B1 (et) |
RU (1) | RU2140926C1 (et) |
SA (1) | SA94150231B1 (et) |
SG (1) | SG52650A1 (et) |
SI (1) | SI0719278T1 (et) |
SK (1) | SK281869B6 (et) |
TW (1) | TW369521B (et) |
WO (1) | WO1995007927A1 (et) |
ZA (2) | ZA947119B (et) |
Families Citing this family (78)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0641209A4 (en) * | 1992-05-20 | 1995-08-23 | Merck & Co Inc | NEW 17-ESTER, AMID AND KETONE DERIVATIVES OF 3-OXO-4-AZASTEROIDS AS 5-ALPHA REDUCTINE 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 |
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 |
KR100363994B1 (ko) * | 1993-10-21 | 2003-04-10 | 머크 앤드 캄파니 인코포레이티드 | 16-치환된-4-아자-안드로스탄5-알파-리덕타제아이소자임1억제제 |
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 |
AU4701299A (en) * | 1998-06-23 | 2000-01-10 | Stuart R. Adler | Therapeutic applications of estrogenic carboxylic acids |
AU2512800A (en) | 1999-02-03 | 2000-08-25 | Eli Lilly And Company | Alpha1-adrenergic receptor antagonists |
ATE301129T1 (de) | 1999-05-04 | 2005-08-15 | Strakan Int Ltd | Androgen glykoside und die androgenische aktivität davon |
US6645974B2 (en) | 2001-07-31 | 2003-11-11 | Merck & Co., Inc. | Androgen receptor modulators and methods for use thereof |
JP4490689B2 (ja) * | 2001-10-03 | 2010-06-30 | メルク・シャープ・エンド・ドーム・コーポレイション | アンドロゲン受容体調節剤としてのアンドロスタン17β−カルボキサミド類 |
DK1468983T3 (da) * | 2002-01-25 | 2008-01-07 | Asahi Glass Co Ltd | Fremgangsmåde til fremstilling af 2,5-bis(trifluormethyl)nitrobenzen |
EP1743656A3 (en) * | 2002-04-24 | 2007-03-07 | Boehringer Ingelheim Pharma GmbH & Co. KG | Pharmaceutical combination for the treatment of benign prostatic hyperplasia or for the long-term prevention of acute urinary retention |
CA2484173A1 (en) * | 2002-04-30 | 2003-11-13 | Merck & Co., Inc. | 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 |
EP1746998A1 (en) * | 2004-03-22 | 2007-01-31 | Ranbaxy Laboratories, Ltd. | 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 |
JP2008510811A (ja) * | 2004-08-25 | 2008-04-10 | メルク エンド カムパニー インコーポレーテッド | アンドロゲン受容体モジュレーター |
WO2006058781A2 (en) * | 2004-12-03 | 2006-06-08 | Proteosys Ag | Finasteride, dutasteride and related compounds for preventing/treating 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 |
WO2007120263A2 (en) * | 2005-11-10 | 2007-10-25 | 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 |
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 |
US8252947B2 (en) | 2008-04-03 | 2012-08-28 | Harbor Therapeutics, 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 |
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 |
EP2838533B1 (en) | 2012-04-16 | 2017-10-04 | 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 |
WO2014158875A1 (en) * | 2013-03-14 | 2014-10-02 | 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 |
CA2927730A1 (en) | 2013-10-15 | 2015-05-07 | Case Western Reserve University | Compositions and methods of modulating short-chain dehydrogenase activity |
EP2949319A1 (en) | 2014-05-26 | 2015-12-02 | Galenicum Health S.L. | Pharmaceutical compositions comprising an active agent |
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 |
CN113896607B (zh) * | 2015-03-13 | 2024-04-16 | 陶氏环球技术有限责任公司 | 利用包含具有含有磷环的配体的铬络合物的催化剂的烯烃低聚反应方法 |
KR102503428B1 (ko) | 2015-12-22 | 2023-02-24 | 한미약품 주식회사 | 두타스테라이드를 포함하는 경구용 연질 캡슐 제형용 포장재 |
WO2017160106A2 (ko) | 2016-03-16 | 2017-09-21 | 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 |
WO2018102552A1 (en) | 2016-11-30 | 2018-06-07 | Case Western Reserve University | Combinations of 15-pgdh inhibitors with corcosteroids and/or tnf inhibitors and uses thereof |
CN118480009A (zh) | 2017-02-06 | 2024-08-13 | 卡斯西部储备大学 | 调节短链脱氢酶活性的组合物和方法 |
EP3677253A4 (en) | 2017-09-01 | 2020-11-04 | JW Pharmaceutical Corporation | SOLID PREPARATION INCLUDING DUTASTERIDE AND RELATED PREPARATION PROCESS |
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 |
CA3120858A1 (en) | 2018-11-21 | 2020-05-28 | Case Western Reserve University | Compositions and methods of modulating short-chain dehydrogenase activity |
KR20200074759A (ko) | 2018-12-17 | 2020-06-25 | 동국제약 주식회사 | 두타스테라이드를 함유하는 고형제제 |
CN116507626A (zh) | 2020-05-20 | 2023-07-28 | 罗迪奥治疗公司 | 调节短链脱氢酶活性的组合物和方法 |
WO2024144084A1 (ko) * | 2022-12-26 | 2024-07-04 | 주식회사 유영제약 | 주 1회 투여를 위한 정제 형태의 고함량 두타스테리드 약제학적 조성물 및 이의 제조방법 |
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 |
US4191759A (en) * | 1978-04-13 | 1980-03-04 | Merck & Co., Inc. | N-substituted-17β-carbamoylandrost-4-en-3-one 5α reductase inhibitors |
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 |
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 |
NZ211145A (en) * | 1984-02-27 | 1988-10-28 | Merck & Co Inc | 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions |
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 |
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 (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 |
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 |
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 |
AU627466B2 (en) * | 1988-05-25 | 1992-08-27 | Smithkline Beckman Corporation | Aromatic steroid 5-alpha-reductase inhibitors |
US4954446A (en) * | 1988-05-25 | 1990-09-04 | Smithkline Beecham Corporation | Aromatic steroid 5-α-reductase inhibitors |
US5237061A (en) * | 1988-10-31 | 1993-08-17 | Merck & Co., Inc. | Methods of synthesizing benign prostatic hypertropic agents and their intermediates |
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 |
US4970205A (en) * | 1988-12-23 | 1990-11-13 | Smithkline Beecham Corporation | Sulfonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase |
US4882319A (en) * | 1988-12-23 | 1989-11-21 | Smithkline Beckman Corporation | Phosphonic 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 |
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 (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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 (en) * | 1991-04-17 | 1992-10-29 | 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 |
ATE165368T1 (de) * | 1991-12-20 | 1998-05-15 | Glaxo Wellcome Inc | Inhibitoren von testosteron-5-alpha reductase. |
JP3164389B2 (ja) * | 1991-12-25 | 2001-05-08 | 三共株式会社 | 4−アザステロイド類 |
JPH07508038A (ja) * | 1992-05-20 | 1995-09-07 | メルク エンド カンパニー インコーポレーテッド | 4−アザステロイドの17−エーテル及びチオエーテル |
WO1993023050A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | NEW DELTA-17 AND DELTA-20 OLEFINIC AND SATURATED 17β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS |
DE69329856D1 (de) * | 1992-05-20 | 2001-02-15 | Merck & Co Inc | Ester derivate von 4-aza-steroiden |
JPH07508034A (ja) * | 1992-05-20 | 1995-09-07 | メルク エンド カンパニー インコーポレーテッド | 17−アミノ置換4−アザステロイド5α−レダクターゼ阻害剤 |
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 |
US5710275A (en) * | 1992-05-20 | 1998-01-20 | Merck & Co., Inc. | 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors |
EP0641209A4 (en) * | 1992-05-20 | 1995-08-23 | Merck & Co Inc | NEW 17-ESTER, AMID AND KETONE DERIVATIVES OF 3-OXO-4-AZASTEROIDS AS 5-ALPHA REDUCTINE INHIBITORS. |
AU4251993A (en) * | 1992-05-20 | 1993-12-13 | Merck & Co., Inc. | Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors |
US5620986A (en) * | 1992-05-20 | 1997-04-15 | Merck & Co., Inc. | 17 urea, thiourea, thiocarbamyl and carbamyl4-azasteroid 5-reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders |
GB9210880D0 (en) * | 1992-05-21 | 1992-07-08 | Smithkline Beecham Corp | Compounds |
KR950701527A (ko) * | 1992-05-21 | 1995-04-28 | 라브리 페르낭 | 테스토스테론 5α 환원효소 활성 저해제(INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY) |
GB9216329D0 (en) * | 1992-07-31 | 1992-09-16 | Erba Carlo Spa | 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives |
GB9216284D0 (en) * | 1992-07-31 | 1992-09-16 | Erba Carlo Spa | Fluorinated 17beta-substituted 4-aza-5alpha-androstane-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 |
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