[go: up one dir, main page]

OA10575A - Androstenone derivative - Google Patents

Androstenone derivative Download PDF

Info

Publication number
OA10575A
OA10575A OA60795A OA60795A OA10575A OA 10575 A OA10575 A OA 10575A OA 60795 A OA60795 A OA 60795A OA 60795 A OA60795 A OA 60795A OA 10575 A OA10575 A OA 10575A
Authority
OA
OAPI
Prior art keywords
compound
formula
solvaté
bis
aza
Prior art date
Application number
OA60795A
Other languages
English (en)
Inventor
Kenneth William Batchelor
Stephen Vernon Frye
Original Assignee
Glaxo Wellcome Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22407744&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=OA10575(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Glaxo Wellcome Inc filed Critical Glaxo Wellcome Inc
Publication of OA10575A publication Critical patent/OA10575A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J3/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005Normal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26Androgens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70Carboxylic 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
    • C07C235/82Carboxylic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0066Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J73/00Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001Steroids 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
    • C07J73/005Steroids 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/04Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12Ortho- 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
    • C07C2603/14Benz[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)
OA60795A 1993-09-17 1996-03-13 Androstenone derivative OA10575A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US12328093A 1993-09-17 1993-09-17

Publications (1)

Publication Number Publication Date
OA10575A true OA10575A (en) 2002-06-25

Family

ID=22407744

Family Applications (1)

Application Number Title Priority Date Filing Date
OA60795A OA10575A (en) 1993-09-17 1996-03-13 Androstenone derivative

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) DE69407978T2 (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 (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0641209A4 (fr) * 1992-05-20 1995-08-23 Merck & Co Inc NOUVEAUX DERIVES 17-ESTER, AMIDE ET CETONE DE 3-OXO-4-AZASTEROIDES UTILISES COMME INHIBITEURS DE 5a-REDUCTASE.
EP0663924B1 (fr) * 1992-10-06 2001-02-14 Merck & Co. Inc. 17-beta-carboxanilides de 4-aza-5-alpha-androstan-3-ones utilises comme inhibiteurs de 5-alpha-reductase
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
TW382595B (en) * 1993-10-15 2000-02-21 Merck & Co Inc Pharmaceutical composition for use in arresting and reversing androgenic alopecia
RO116197B1 (ro) * 1993-10-21 2000-11-30 Merck & Co Inc Derivati de 4-aza-androstan-16-substituiti, compozitie farmaceutica ce ii contine si metoda de tratament
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
US5942519A (en) * 1997-10-28 1999-08-24 Merck & Co., Inc. Prevention of precipitated acute urinary retention
RU2000125533A (ru) * 1998-03-11 2002-10-20 Эндорешерш, Инк. (Ca) Ингибиторы 17-бета-гидроксистероиддегидрогеназ 5 и 3 типа и способы их применения
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
KR20010101931A (ko) 1999-02-03 2001-11-15 피터 지. 스트링거 α1-아드레날린성 수용체 길항제
JP5005127B2 (ja) 1999-05-04 2012-08-22 ストラカン・インターナショナル・リミテッド アンドロゲングリコシド及びそのアンドロゲン作用活性
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
DK1501517T3 (da) * 2002-04-24 2007-06-11 Boehringer Ingelheim Pharma Farmaceutisk kombination til behandling af godartet hyperplasia af prostata eller til langtidsforhindring af akut urinretention
WO2003092588A2 (fr) * 2002-04-30 2003-11-13 Merck & Co., Inc. Derives de 4-azasteroide utilises comme modulateurs du recepteur de l'androgene
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 (fr) * 2004-03-22 2007-01-31 Ranbaxy Laboratories, Ltd. Therapie combinee destinee a reduire les symptomes des voies urinaires
WO2005097127A2 (fr) * 2004-04-02 2005-10-20 Merck & Co., Inc. Methode destinee a traiter des hommes presentant des troubles metaboliques et anthropometriques
EP1784187A4 (fr) * 2004-08-25 2010-08-18 Merck Sharp & Dohme Modulateurs du recepteur de l'androgene
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
CN101146535A (zh) * 2005-03-25 2008-03-19 默克公司 用睾酮补充剂和5α-还原酶抑制剂治疗男性病人的方法
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
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
CA2728889C (fr) 2008-04-03 2016-06-14 Harbor Biosciences, Inc. Formes a l'etat solide d'un produit pharmaceutique
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
WO2012162776A1 (fr) * 2011-06-03 2012-12-06 Eurofarma Laboratórios S.A Composition pharmaceutique pour le traitement de l'hyperplasie bénigne de la prostate
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
WO2013158649A1 (fr) 2012-04-16 2013-10-24 Case Western Reserve University Compositions et méthodes pour moduler l'activité 15-pgdh
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
EP3057973B1 (fr) 2013-10-15 2019-09-04 Case Western Reserve University Compositions comportant un inhibiteur de 15-pdgh pour la cicatrisation de plaies
ES2555485T1 (es) 2014-05-26 2016-01-04 Galenicum Health S.L. Composiciones farmacéuticas que contienen un agente activo
AU2015357489A1 (en) 2014-12-05 2017-07-06 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
ES3037196T3 (en) * 2015-03-13 2025-09-30 Dow Global Technologies Llc Olefin oligomerisation process with a catalyst comprising a chromium complex with a phosphacycle-containing ligand
KR102503428B1 (ko) 2015-12-22 2023-02-24 한미약품 주식회사 두타스테라이드를 포함하는 경구용 연질 캡슐 제형용 포장재
BR112018068686A2 (pt) 2016-03-16 2019-01-15 Hanmi Pharm Ind Co Ltd formulação de compósito de cápsula dura, formulação de compósito de dose fixa e método de preparação da formulação de compósito de cápsula dura
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
CN110573154A (zh) 2017-02-06 2019-12-13 卡斯西部储备大学 调节短链脱氢酶活性的组合物和方法
AU2018325148B2 (en) 2017-09-01 2024-08-01 Jw Pharmaceutical Corporation Solid preparation comprising dutasteride and method for preparing same
KR101996597B1 (ko) 2017-10-13 2019-07-31 주식회사 유유제약 두타스테리드와 타다라필을 용해시킨 경구용 캡슐 제형의 복합제제
WO2019225924A1 (fr) * 2018-05-21 2019-11-28 (주)인벤티지랩 Microparticules comprenant du dutastéride et procédé de préparation associé
KR102281252B1 (ko) 2018-05-21 2021-07-23 (주)인벤티지랩 두타스테라이드를 포함하는 마이크로 입자 및 이의 제조 방법
SG11202105345TA (en) 2018-11-21 2021-06-29 Univ Case Western Reserve Compositions and methods of modulating short-chain dehydrogenase activity
KR20200074759A (ko) 2018-12-17 2020-06-25 동국제약 주식회사 두타스테라이드를 함유하는 고형제제
JP2023527279A (ja) 2020-05-20 2023-06-28 ロデオ・セラピューティクス・コーポレイション 短鎖デヒドロゲナーゼ活性を調節する組成物及び方法
WO2024144084A1 (fr) * 2022-12-26 2024-07-04 주식회사 유영제약 Composition pharmaceutique de dutastéride à dose élevée sous forme de comprimé pour administration hebdomadaire et son procédé de préparation

Family Cites Families (79)

* Cited by examiner, † Cited by third party
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
EP0314199B1 (fr) * 1984-02-27 1991-09-18 Merck & Co. Inc. 4-Aza-5-alpha-androsténones substituées en position 17 bêta et leur utilisation comme inhibiteurs de 5-alpha-réductase
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
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors
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
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.
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
EP0285383B1 (fr) * 1987-04-03 1994-03-16 Merck & Co. Inc. Traitement des carcinomes prostatiques avec des 17-bêta-n-monosubstitué-carbamoyl-4-aza-5-alpha-androst-1-en-ones
DE3888994T2 (de) * 1987-04-03 1994-11-03 Merck & Co Inc Behandlung von androgener Alopecia mit 17-beta-n-mono-substituierten-carbamoyl-4-aza-5-alpha-androst-1-en-3-onen.
US4910226A (en) * 1987-04-29 1990-03-20 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
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
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
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
US4937237A (en) * 1988-12-23 1990-06-26 Smithkline Beckman Corporation Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -reductase
US5026882A (en) * 1988-12-23 1991-06-25 Smithkline Beecham Corporation Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase
US4882319A (en) * 1988-12-23 1989-11-21 Smithkline Beckman Corporation Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-α-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 (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
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
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
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
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
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
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
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
CA2050824A1 (fr) * 1990-09-24 1992-03-25 John M. Williams Methode de preparation de 3-oxo-4-azaandrost-1-en-17.beta.-ones
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
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
SK137994A3 (en) * 1992-05-20 1995-04-12 Merck & Co Inc 7-beta-substituted-4-aza-5-alpha-cholestan-ons their using for production of pharmaceutical agent and pharmaceutical agent containing them
EP0641209A4 (fr) * 1992-05-20 1995-08-23 Merck & Co Inc NOUVEAUX DERIVES 17-ESTER, AMIDE ET CETONE DE 3-OXO-4-AZASTEROIDES UTILISES COMME INHIBITEURS DE 5a-REDUCTASE.
AU668180B2 (en) * 1992-05-20 1996-04-26 Merck & Co., Inc. 17-ethers and thioethers of 4-aza-steroids
AU668181B2 (en) * 1992-05-20 1996-04-26 Merck & Co., Inc. Ester derivatives of 4-aza-steroids
US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
CA2135055A1 (fr) * 1992-05-20 1993-11-25 Bruce E. Witzel Inhibiteurs de la 4-azasteroide-5-alpha-reductase
CA2135057A1 (fr) * 1992-05-20 1993-11-25 Bruce E. Witzel Inhibiteurs de la 4-azasteroide 5a-reductase a substituant sur le groupement amine en 17
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
AU676478B2 (en) * 1992-05-20 1997-03-13 Merck & Co., Inc. New delta-17 and delta-20 olefinic and saturated 17beta- substituted-4-aza-5alpha-androstan-3-ones as 5alpha- reductase inhibitors
GB9210880D0 (en) * 1992-05-21 1992-07-08 Smithkline Beecham Corp Compounds
PL175591B1 (pl) * 1992-05-21 1999-01-29 Endorecherche Inc Środek farmaceutyczny do hamowania 5alfa-reduktazy testosteronowej
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
EP0663924B1 (fr) * 1992-10-06 2001-02-14 Merck & Co. Inc. 17-beta-carboxanilides de 4-aza-5-alpha-androstan-3-ones utilises comme inhibiteurs de 5-alpha-reductase
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
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

Also Published As

Publication number Publication date
DE10399022I2 (de) 2012-09-13
KR100364953B1 (ko) 2003-04-08
PE15095A1 (es) 1995-06-04
CZ74596A3 (en) 1996-09-11
HUT73850A (en) 1996-09-30
CA2170047A1 (fr) 1995-03-23
NL300122I2 (nl) 2003-09-01
CY2004002I2 (el) 2009-11-04
WO1995007927A1 (fr) 1995-03-23
CZ286069B6 (cs) 2000-01-12
ES2113127T3 (es) 1998-04-16
BG100410A (bg) 1996-09-30
US5846976A (en) 1998-12-08
MY119778A (en) 2005-07-29
CA2170047C (fr) 2004-11-09
NO306117B1 (no) 1999-09-20
EP0719278A1 (fr) 1996-07-03
US5565467A (en) 1996-10-15
ZA947119B (en) 1995-05-26
AP9400669A0 (en) 1994-10-31
AU7875194A (en) 1995-04-03
DE69407978T2 (de) 1998-05-07
IL110978A (en) 1999-01-26
CN1131424A (zh) 1996-09-18
BG62363B1 (bg) 1999-09-30
RO117455B1 (ro) 2002-03-29
DE69407978D1 (de) 1998-02-19
IL110978A0 (en) 1994-11-28
HRP940563A2 (en) 1997-02-28
FI961231A0 (fi) 1996-03-15
JP2904310B2 (ja) 1999-06-14
SI0719278T1 (sl) 1998-06-30
LU91027I2 (fr) 2004-04-28
FI115216B (fi) 2005-03-31
EP0719278B1 (fr) 1998-01-14
DK0719278T3 (da) 1998-09-14
GR3026144T3 (en) 1998-05-29
HK1004334A1 (en) 1998-11-20
ATE162199T1 (de) 1998-01-15
FI961231L (fi) 1996-03-15
CN1057771C (zh) 2000-10-25
SK281869B6 (sk) 2001-08-06
AU690925B2 (en) 1998-05-07
HU220060B (hu) 2001-10-28
AP494A (en) 1996-05-15
JPH09502731A (ja) 1997-03-18
TW369521B (en) 1999-09-11
CY2219B1 (en) 2003-04-18
EE03241B1 (et) 1999-12-15
CY2004002I1 (el) 2009-11-04
HRP940563B1 (en) 2000-10-31
ZA947118B (en) 1995-05-26
NO961080D0 (no) 1996-03-15
CA2462061A1 (fr) 1995-03-23
IS4205A (is) 1995-03-18
NO2003003I2 (no) 2007-06-11
IS1713B (is) 1998-12-30
PL313492A1 (en) 1996-07-08
NL300122I1 (nl) 2003-06-02
SA94150231B1 (ar) 2005-05-04
NZ274642A (en) 1997-11-24
RU2140926C1 (ru) 1999-11-10
NO961080L (no) 1996-03-15
BR1100329A (pt) 2000-06-13
PL180002B1 (pl) 2000-11-30
SK34796A3 (en) 1996-07-03
DE10399022I1 (de) 2004-01-15
HU9600656D0 (en) 1996-05-28
SG52650A1 (en) 1998-09-28

Similar Documents

Publication Publication Date Title
OA10575A (en) Androstenone derivative
HK1004334B (en) Androstenone derivative
EP0783001B1 (fr) Androsténones
US5998427A (en) Androstenones
JP3824636B2 (ja) アンドロステノン
US5817818A (en) Androstenones
WO1996030391A1 (fr) 6-azacholesten-3-ones substituees