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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Endocrinology (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 (da)
EP (2) EP0783001B1 (da)
CN (1) CN1041939C (da)
AT (2) ATE186733T1 (da)
AU (1) AU685167B2 (da)
CA (3) CA2478971C (da)
DE (2) DE69407422T2 (da)
DK (2) DK0783001T3 (da)
ES (2) ES2110260T3 (da)
FI (1) FI961232A0 (da)
GR (2) GR3025717T3 (da)
HU (1) HUT74445A (da)
IL (1) IL110979A (da)
IS (1) IS1726B (da)
NO (1) NO306510B1 (da)
NZ (1) NZ274059A (da)
RU (1) RU2144037C1 (da)
TW (1) TW408127B (da)
WO (1) WO1995007926A1 (da)

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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
WO2001023405A2 (en) 1999-09-30 2001-04-05 Hollis-Eden Pharmaceuticals, Inc. Therapeutic treatment of androgen receptor driven conditions
GB0026876D0 (en) * 2000-11-03 2000-12-20 Glaxo Group Ltd Process
US20040102425A1 (en) * 2000-11-03 2004-05-27 Barr Alexander Stephen Selective glucocorticoid receptor agonists
US6645974B2 (en) 2001-07-31 2003-11-11 Merck & Co., Inc. Androgen receptor modulators and methods for use thereof
US7402577B2 (en) * 2001-10-03 2008-07-22 Merck & Co., Inc. Androstane 17-beta-carboxamides as androgen receptor modulators
CN1652786A (zh) * 2002-03-13 2005-08-10 麦克公司 作为雄激素受体调节剂的氟代4－氮杂甾体衍生物
JP4516839B2 (ja) * 2002-04-30 2010-08-04 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修飾因子としての４−アザステロイド誘導体
JP2007534757A (ja) * 2004-04-28 2007-11-29 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としてのフッ素付加４−アザステロイド
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

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AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
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
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
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
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.
US4888336A (en) * 1987-01-28 1989-12-19 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
EP0285383B1 (en) * 1987-04-03 1994-03-16 Merck & Co. Inc. Treatment of prostatic carcinoma with 17beta-n-monosubstituted-carbamoyl-4-aza-5alpha-androst-1-en-3-ones
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
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
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
IE76452B1 (en) * 1990-10-29 1997-10-22 Sankyo Co Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use
NZ241979A (en) * 1991-03-20 1996-01-26 Merck & Co Inc Treatment of benign prostatic hyperplasia using 5alpha-reductase inhibitor and an alpha1-adrenergic recepter blocker
IL101245A0 (en) * 1991-03-20 1992-11-15 Merck & Co Inc Pharmaceutical compositions for the treatment of prostatic cancer
AU1893492A (en) * 1991-04-17 1992-11-17 Merck & Co., Inc. Pharmaceutical combination for the treatment of benign prostatic hyperplasia comtaining a 5 alpha-reductase inhibitor
US5304562A (en) * 1991-10-09 1994-04-19 Ciba-Geigy Corporation 17β-substituted Aza-androstane derivatives
EP0547687A1 (en) * 1991-12-18 1993-06-23 Merck & Co. Inc. 17B-N-Substituted adamantyl/norbonanyl carbamoyl-4-aza-5a-and-rost-1-en-3-ones and androstan-3 ones
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
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
JPH07508033A (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 ５α−レダクターゼ阻害剤としての３−オキソ−４−アザステロイドの新規１７−エステル，アミド及びケトン誘導体
WO1993023048A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. 4-azasteroid 5-alpha-reductase inhibitors
WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
EP0641204B1 (en) * 1992-05-20 2000-08-16 Merck & Co. Inc. 17-ethers and thioethers of 4-aza-steroids
WO1993023419A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-CHOLESTAN-ONES AS 5α-REDUCTASE INHIBITORS
EP0649306B1 (en) * 1992-05-20 2001-01-10 Merck & Co. Inc. Ester derivatives of 4-aza-steroids
CA2135057A1 (en) * 1992-05-20 1993-11-25 Bruce E. Witzel 17-amino substituted 4-azasteroid 5a-reductase inhibitors
CA2135056A1 (en) * 1992-05-20 1993-11-25 Donald W. Graham New delta-17 and delta-20 olefinic and saturated 17b-substituted-4-aza-5a-andros-tan-3-ones as 5a-reductase inhibitors
RU2141967C1 (ru) * 1992-05-21 1999-11-27 Андорешерш Инк. ИНГИБИТОРЫ ТЕСТОСТЕРОН 5α-РЕДУКТАЗЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ИНГИБИРОВАНИЯ АКТИВНОСТИ ТЕСТОСТЕРОН 5α-РЕДУКТАЗЫ
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Also Published As

Publication number Publication date
EP0719277A1 (en) 1996-07-03
IL110979A0 (en) 1994-11-28
CN1134155A (zh) 1996-10-23
DK0783001T3 (da) 2000-04-10
FI961232A (fi) 1996-03-15
GR3025717T3 (en) 1998-03-31
HUT74445A (en) 1996-12-30
RU2144037C1 (ru) 2000-01-10
CA2171329C (en) 2004-11-23
US5977126A (en) 1999-11-02
NO306510B1 (no) 1999-11-15
GR3032198T3 (en) 2000-04-27
EP0719277B1 (en) 1997-12-17
CN1041939C (zh) 1999-02-03
ATE161268T1 (de) 1998-01-15
CA2478971A1 (en) 1995-03-23
EP0783001B1 (en) 1999-11-17
TW408127B (en) 2000-10-11
DE69421726T2 (de) 2000-06-29
DK0719277T3 (da) 1998-08-24
IS1726B (is) 1999-09-06
FI961232A0 (fi) 1996-03-15
ES2110260T3 (es) 1998-02-01
AU7798094A (en) 1995-04-03
DE69407422T2 (de) 1998-04-09
ATE186733T1 (de) 1999-12-15
DE69407422D1 (en) 1998-01-29
DE69421726D1 (de) 1999-12-23
CA2478971C (en) 2007-10-23
NZ274059A (en) 1997-12-19
CA2171329A1 (en) 1995-03-23
HU9600643D0 (en) 1996-05-28
ES2140181T3 (es) 2000-02-16
WO1995007926A1 (en) 1995-03-23
NO961085D0 (no) 1996-03-15
EP0783001A1 (en) 1997-07-09
NO961085L (no) 1996-04-22
IS4206A (is) 1995-03-18
AU685167B2 (en) 1998-01-15
CA2449679A1 (en) 1995-03-23
CA2449679C (en) 2007-10-23

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Legal Events

Date Code Title Description
FF Patent granted
KB Patent renewed
KB Patent renewed
MM9K Patent not in force due to non-payment of renewal fees