IL110979A - Substituted 17beta-anilide-4-aza-5alpha-androstan-3-ones their preparation and pharmaceutical compositions containing them - Google Patents

Substituted 17beta-anilide-4-aza-5alpha-androstan-3-ones their preparation and pharmaceutical compositions containing them

Info

Publication number
IL110979A
IL110979A IL11097994A IL11097994A IL110979A IL 110979 A IL110979 A IL 110979A IL 11097994 A IL11097994 A IL 11097994A IL 11097994 A IL11097994 A IL 11097994A IL 110979 A IL110979 A IL 110979A
Authority
IL
Israel
Prior art keywords
hydrogen
substituted
5alpha
17beta
androstan
Prior art date
Application number
IL11097994A
Other languages
English (en)
Other versions
IL110979A0 (en
Original Assignee
Glaxo 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
Application filed by Glaxo Inc filed Critical Glaxo Inc
Publication of IL110979A0 publication Critical patent/IL110979A0/xx
Publication of IL110979A publication Critical patent/IL110979A/xx

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)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
IL11097994A 1993-09-17 1994-09-16 Substituted 17beta-anilide-4-aza-5alpha-androstan-3-ones their preparation and pharmaceutical compositions containing them IL110979A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US12328093A 1993-09-17 1993-09-17
US13651593A 1993-10-12 1993-10-12

Publications (2)

Publication Number Publication Date
IL110979A0 IL110979A0 (en) 1994-11-28
IL110979A true IL110979A (en) 1999-08-17

Family

ID=26821398

Family Applications (1)

Application Number Title Priority Date Filing Date
IL11097994A IL110979A (en) 1993-09-17 1994-09-16 Substituted 17beta-anilide-4-aza-5alpha-androstan-3-ones their preparation and pharmaceutical compositions containing them

Country Status (19)

Country Link
US (1) US5977126A (de)
EP (2) EP0783001B1 (de)
CN (1) CN1041939C (de)
AT (2) ATE161268T1 (de)
AU (1) AU685167B2 (de)
CA (3) CA2478971C (de)
DE (2) DE69421726T2 (de)
DK (2) DK0719277T3 (de)
ES (2) ES2110260T3 (de)
FI (1) FI961232A7 (de)
GR (2) GR3025717T3 (de)
HU (1) HUT74445A (de)
IL (1) IL110979A (de)
IS (1) IS1726B (de)
NO (1) NO306510B1 (de)
NZ (1) NZ274059A (de)
RU (1) RU2144037C1 (de)
TW (1) TW408127B (de)
WO (1) WO1995007926A1 (de)

Families Citing this family (18)

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TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
USRE39056E1 (en) * 1995-09-15 2006-04-04 Merck & Co, Inc. 4-Azasteroids for treatment of hyperandrogenic conditions
US5935968A (en) * 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
GB9717444D0 (en) * 1997-08-19 1997-10-22 Glaxo Group Ltd Pharmaceutical composition
GB9717428D0 (en) * 1997-08-19 1997-10-22 Glaxo Group Ltd Pharmaceutical composition
PT1955700E (pt) 1999-09-30 2011-05-04 Harbor Biosciences Inc Tratamento terap?utico de doen?as associadas ao receptor de androg?nios
CA2427569C (en) * 2000-11-03 2010-07-27 Matrix Therapeutics Limited Selective glucocorticoid receptor agonists
GB0026876D0 (en) * 2000-11-03 2000-12-20 Glaxo Group Ltd Process
US6645974B2 (en) 2001-07-31 2003-11-11 Merck & Co., Inc. Androgen receptor modulators and methods for use thereof
CA2462456C (en) * 2001-10-03 2010-05-04 Merck & Co., Inc. Androstane 17-beta-carboxamides as androgen receptor modulators
PL372920A1 (en) * 2002-03-13 2005-08-08 Merck & Co,Inc. Fluorinated 4-azasteroid derivatives as androgen receptor modulators
CA2484173A1 (en) * 2002-04-30 2003-11-13 Merck & Co., Inc. 4-azasteroid derivatives as androgen receptor modulators
CU23256A1 (es) * 2003-03-20 2008-01-24 Dalmer Lab Sa EXTRACTO OBTENIDO A PARTIR DE FRUTOS DE ROYSTONEA REGIA UTILIZADO CONTRA LA HIPERPLASIA PROSTáTICA Y LA PROSTATITIS
WO2005105091A1 (en) * 2004-04-28 2005-11-10 Merck & Co., Inc. Fluorinated 4-azasteroids as androgen receptor modulators
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
CN103554213A (zh) * 2012-01-05 2014-02-05 中国药科大学 4-氧杂-雄甾-3-酮-17β-酰胺类衍生物、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
CN103570796A (zh) * 2012-07-24 2014-02-12 重庆医药工业研究院有限责任公司 一种度他雄胺ⅰ型晶的制备方法

Family Cites Families (38)

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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
US4760071A (en) * 1984-02-27 1988-07-26 Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
US5049562A (en) * 1984-02-27 1991-09-17 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors
EP0271219B1 (de) * 1986-11-20 1992-07-29 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
EP0285383B1 (de) * 1987-04-03 1994-03-16 Merck & Co. Inc. Behandlung von Prostatacarcinoma mit 17-beta-n-monosubstituierten-Carbamoyl-4-aza-5-alpha-Androst-1-en-3-onen
ZA883034B (en) * 1987-04-29 1989-03-29 Smithkline Beckman Corp Steroid 5-alpha-reductase inhibitors
US5084574A (en) * 1988-04-18 1992-01-28 Merck & Co., Inc. Dehydrogenation process
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
US5021575A (en) * 1989-11-13 1991-06-04 Merck & Co., Inc. Method for introducing a 1,2 double bond into azasteroids
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
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
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
US5304562A (en) * 1991-10-09 1994-04-19 Ciba-Geigy Corporation 17β-substituted Aza-androstane derivatives
EP0547687A1 (de) * 1991-12-18 1993-06-23 Merck & Co. Inc. 17-Beta-substituierte Adamantyl/Norbornanyl Carbamoyl-4-Aza-5-Alpha-Androsta-1-En-3-Onen und Androstan-3-Onen
JP3164389B2 (ja) * 1991-12-25 2001-05-08 三共株式会社 ４−アザステロイド類
US5215894A (en) * 1992-02-25 1993-06-01 Merck & Co., Inc. Biological process for producing 17β-N-monosubstituted carbamoyl-11-oxo-4-aza-5-α-androst-3-one testosterone-5-α reductase inhibitors
WO1993023038A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. 17-AMINO SUBSTITUTED 4-AZASTEROID 5α-REDUCTASE INHIBITORS
DE69313114T2 (de) * 1992-05-20 1998-03-19 Merck & Co Inc NEUE DELTA-17 UND DELTA-20 UNGESÄTIGTE UND GESATIGTE 17--g(b)-SUBSTITUIERTE-4-AZA-5-g(a)-ANDROSTAN-3-ON VERBINDUNGEN ALS INHIBITOREN VON 5-ALPHA-REDUCTASE
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
ATE195129T1 (de) * 1992-05-20 2000-08-15 Merck & Co Inc 4-azasteroide als 5-alpha-reduktase
AU674145B2 (en) * 1992-05-20 1996-12-12 Merck & Co., Inc. New 17-ester, amide, and ketone derivatives of 3-oxo-4-azasteroids as 5a-reductase inhibitors
JPH07508039A (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−アザステロイドのエステル誘導体
WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
US5536727A (en) * 1992-05-20 1996-07-16 Merck & Co., Inc. 17-Ethers and thioethers of 4-aza-steroids
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
GB9210880D0 (en) * 1992-05-21 1992-07-08 Smithkline Beecham Corp Compounds
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
DE69329933T2 (de) * 1992-10-06 2001-07-19 Merck & Co., Inc. 17-beta-carboxanilid derivate von 4-aza-5-alpha-androstan-3-one als 5-alpha-reduktase-hemmende arzneimittel
US5468860A (en) * 1992-11-19 1995-11-21 Merck & Co., Inc. New finasteride processes
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5512555A (en) * 1994-07-21 1996-04-30 Merck & Co., Inc. Method of treating sweat-related conditions using finasteride, epristeride and a cholestan-3-one

Also Published As

Publication number Publication date
CN1041939C (zh) 1999-02-03
IL110979A0 (en) 1994-11-28
DK0783001T3 (da) 2000-04-10
CA2171329C (en) 2004-11-23
CA2478971A1 (en) 1995-03-23
EP0783001B1 (de) 1999-11-17
ES2110260T3 (es) 1998-02-01
ATE161268T1 (de) 1998-01-15
DE69421726D1 (de) 1999-12-23
ES2140181T3 (es) 2000-02-16
DE69421726T2 (de) 2000-06-29
ATE186733T1 (de) 1999-12-15
TW408127B (en) 2000-10-11
US5977126A (en) 1999-11-02
DE69407422D1 (en) 1998-01-29
GR3025717T3 (en) 1998-03-31
NO306510B1 (no) 1999-11-15
AU7798094A (en) 1995-04-03
WO1995007926A1 (en) 1995-03-23
CA2478971C (en) 2007-10-23
CA2449679A1 (en) 1995-03-23
EP0783001A1 (de) 1997-07-09
FI961232A0 (fi) 1996-03-15
EP0719277B1 (de) 1997-12-17
IS4206A (is) 1995-03-18
NZ274059A (en) 1997-12-19
HUT74445A (en) 1996-12-30
DE69407422T2 (de) 1998-04-09
CA2171329A1 (en) 1995-03-23
FI961232L (fi) 1996-03-15
EP0719277A1 (de) 1996-07-03
GR3032198T3 (en) 2000-04-27
AU685167B2 (en) 1998-01-15
CN1134155A (zh) 1996-10-23
CA2449679C (en) 2007-10-23
NO961085L (no) 1996-04-22
HU9600643D0 (en) 1996-05-28
RU2144037C1 (ru) 2000-01-10
FI961232A7 (fi) 1996-03-15
DK0719277T3 (da) 1998-08-24
IS1726B (is) 1999-09-06
NO961085D0 (no) 1996-03-15

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