NZ211145A - 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions - Google Patents

4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions

Info

Publication number
NZ211145A
NZ211145A NZ211145A NZ21114585A NZ211145A NZ 211145 A NZ211145 A NZ 211145A NZ 211145 A NZ211145 A NZ 211145A NZ 21114585 A NZ21114585 A NZ 21114585A NZ 211145 A NZ211145 A NZ 211145A
Authority
NZ
New Zealand
Prior art keywords
androst
aza
alpha
ones
pharmaceutical compositions
Prior art date
Application number
NZ211145A
Other languages
English (en)
Inventor
G H Rasmusson
G F Reynolds
Original Assignee
Merck & Co 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=27078980&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NZ211145(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of NZ211145A publication Critical patent/NZ211145A/xx

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C62/00—Compounds having carboxyl groups bound to carbon atoms of rings other than six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C62/30—Unsaturated compounds
    • C07C62/38—Unsaturated compounds containing keto groups
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • 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
    • C07C2603/16—Benz[e]indenes; Hydrogenated benz[e]indenes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
NZ211145A 1984-02-27 1985-02-18 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions NZ211145A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US58406284A 1984-02-27 1984-02-27
US58406184A 1984-02-27 1984-02-27

Publications (1)

Publication Number Publication Date
NZ211145A true NZ211145A (en) 1988-10-28

Family

ID=27078980

Family Applications (1)

Application Number Title Priority Date Filing Date
NZ211145A NZ211145A (en) 1984-02-27 1985-02-18 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions

Country Status (16)

Country Link
EP (1) EP0155096B1 (instruction)
JP (1) JPH0193600A (instruction)
KR (1) KR900001206B1 (instruction)
AU (4) AU584321B2 (instruction)
CA (1) CA1314541C (instruction)
CY (1) CY1553A (instruction)
DE (2) DE3584172D1 (instruction)
DK (1) DK166704B1 (instruction)
ES (1) ES8702430A1 (instruction)
GR (1) GR850483B (instruction)
HK (1) HK63090A (instruction)
IE (2) IE58058B1 (instruction)
IL (1) IL74365A (instruction)
NL (1) NL930005I2 (instruction)
NZ (1) NZ211145A (instruction)
PT (1) PT80010B (instruction)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5494914A (en) * 1992-05-21 1996-02-27 Endorecherche Inhibitors for testosterone 5α-reductase activity

Families Citing this family (76)

* Cited by examiner, † Cited by third party
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US5151429A (en) * 1984-02-27 1992-09-29 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 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
US5120742A (en) * 1984-02-27 1992-06-09 Merck & Co., Inc. 17 β-acyl-4-aza-5 α-androst-1-ene-3-ones as 5 α-reductase inhibitors
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
US5571817A (en) * 1984-02-27 1996-11-05 Merck & Co., Inc. Methods of treating androgenic alopecia with finasteride [17β-N-mono-substituted-carbamoyl-4-aza-5-α-androst-1-en-ones]
JPS62201896A (ja) * 1986-02-28 1987-09-05 Shiseido Co Ltd 多毛症治療剤
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
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
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
US5084574A (en) * 1988-04-18 1992-01-28 Merck & Co., Inc. Dehydrogenation process
US5116983A (en) * 1988-04-18 1992-05-26 Merck & Co., Inc. Dehydrogenation process intermediates
US5237061A (en) * 1988-10-31 1993-08-17 Merck & Co., Inc. Methods of synthesizing benign prostatic hypertropic agents and their intermediates
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
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
US5162332A (en) * 1990-06-20 1992-11-10 Merck & Co., Inc. Selected 17 β-polyaroyl-4-aza-5 α-androst-1-en-3-ones as steroidal reductase inhibitors
US5151430A (en) * 1990-06-20 1992-09-29 Merck & Co., Inc. Specific 17β-thiobenzoyl-4-aza-5α-androst-1-en-3-ones as antiandrogen 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
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
US5091380A (en) * 1990-06-28 1992-02-25 Merck & Co., Inc. N-monosubstituted adamantyl/norbornanyl 17β-carbamides of 3-carboxy-androst-3,5-dienes as testosterone 5α-reductase inhibitors
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
CA2050824A1 (en) * 1990-09-24 1992-03-25 John M. Williams Process for making 3-oxo-4-aza-androst-1-ene 17-.beta.-ketones
US5061801A (en) * 1990-09-24 1991-10-29 Merck & Co., Inc. Intermediate for making 3-oxo-4-aza-androst-1-ene 17β-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
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
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
WO1993013124A1 (en) * 1991-12-20 1993-07-08 Glaxo Inc. Inhibitors of 5-alpha-testosterone reductase
EP0567271B1 (en) * 1992-04-20 1997-07-02 Sankyo Company Limited Steroid derivatives for the treatment of prostatic hypertrophy, their preparation and uses
US5698720A (en) * 1992-04-20 1997-12-16 Sankyo Company, Limited Steroid derivatives
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
ES2148229T3 (es) * 1992-05-20 2000-10-16 Merck & Co Inc Eteres y tioeteres en la posicion 17 de 4-aza-esteroides.
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
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
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
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
EP0641208B1 (en) * 1992-05-20 2000-08-02 Merck & Co. Inc. 4-azasteroid 5-alpha-reductase inhibitors
US5610162A (en) * 1992-05-20 1997-03-11 Merck & Co., Inc. Ester derivatives of 4-aza-steroids
AU4251993A (en) * 1992-05-20 1993-12-13 Merck & Co., Inc. Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors
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
US5302589A (en) * 1992-08-07 1994-04-12 Glaxo, Inc. Heterocyclic inhibitors of 5-α-testosterone reductase
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
US5468860A (en) * 1992-11-19 1995-11-21 Merck & Co., Inc. New finasteride processes
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
AU6413594A (en) * 1993-03-24 1994-10-11 Merck & Co., Inc. Substituted 3-phenanthridinone derivatives as 5alpha-reductase inhibitors
CA2166090C (en) * 1993-06-24 2006-01-24 Zoltan Tuba Novel process for preparing 17.beta.-substituted 4-azaandrostane derivatives
ATE158301T1 (de) * 1993-06-28 1997-10-15 Merck & Co Inc 4-aza-pregnan-5-alpha-reductase isozym 1 inhibitoren
US5438061A (en) * 1993-07-16 1995-08-01 Merck & Co., Inc. 7-substituted-δ4-6-azasteroid derivatives as 5α-reductase inhibitors
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US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
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ATE175420T1 (de) * 1993-10-21 1999-01-15 Merck & Co Inc 16-substituierte-4-aza-androstan-5-alpha- reduktase-isozym-i-inhibitoren
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US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
US5595996A (en) * 1994-10-25 1997-01-21 Merck & Co., Inc. 7-substituted 4-aza cholanic acid derivatives and their use
US5656613A (en) * 1995-01-04 1997-08-12 Merck & Co., Inc. Treatment of hyperandrogenic conditions
GB0026876D0 (en) * 2000-11-03 2000-12-20 Glaxo Group Ltd Process
WO2003020311A1 (fr) * 2001-08-28 2003-03-13 Fujisawa Pharmaceutical Co., Ltd. Remedes contre les maladies de la peau
RS92304A (sr) 2002-04-24 2006-10-27 Boehringer Ingelheim Pharma Gmbh. & Co.Kg. Farmaceutska kombinacija za lečenje benigne hiperplazije prostate ili za sprečavanje dugotrajnog akutnog zadržavanja mokraće
HU227117B1 (en) 2002-05-10 2010-07-28 Richter Gedeon Nyrt Process for dehydrogenation of aza-androstane compounds
CN1314241C (zh) * 2002-09-27 2007-05-02 华为技术有限公司 在城域网相同虚容器映射通道内传送不同用户数据的方法
KR100508019B1 (ko) 2003-07-19 2005-08-17 한미약품 주식회사 고순도 1-안드로스텐 유도체의 제조 방법
US7998970B2 (en) 2004-12-03 2011-08-16 Proteosys Ag Use of finasteride, dutasteride and related compounds for the prevention or treatment of neurologically-associated disorders
EP2050436A1 (en) 2007-12-21 2009-04-22 Siegfried Generics International AG Pharmaceutical composition containing dutasteride
CN104292293B (zh) * 2014-09-17 2016-04-06 广东众生药业股份有限公司 一种度他雄胺杂质i的制备方法

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US3285918A (en) * 1962-04-18 1966-11-15 Norman J Doorenbos 1', 4', 5', 6'-tetrahydropyrimidino[a-4, 3]-4-aza-5-cholestene
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
KR830000085B1 (ko) * 1978-04-13 1983-02-08 제임스 에프. 너우톤 5α-환원효소 억제제로서 유용한 4-아자-17-치환-5α-안드로스탄-3-온류의 제조방법
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
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5494914A (en) * 1992-05-21 1996-02-27 Endorecherche Inhibitors for testosterone 5α-reductase activity

Also Published As

Publication number Publication date
AU584321B2 (en) 1989-05-25
EP0155096A2 (en) 1985-09-18
KR900001206B1 (ko) 1990-02-28
DK85985A (da) 1985-10-22
JPH0541638B2 (instruction) 1993-06-24
PT80010B (pt) 1987-09-18
PT80010A (en) 1985-03-01
IE922862L (en) 1985-08-27
DK166704B1 (da) 1993-06-28
NL930005I2 (nl) 1993-09-16
DE3584172D1 (de) 1991-10-24
KR850006185A (ko) 1985-10-02
AU2748192A (en) 1993-03-18
AU626293B2 (en) 1992-07-30
CY1553A (en) 1991-03-22
AU3313589A (en) 1989-08-10
ES8702430A1 (es) 1987-01-01
AU651741B2 (en) 1994-07-28
JPH0193600A (ja) 1989-04-12
AU3916785A (en) 1985-09-05
DE3573429D1 (en) 1989-11-09
IE58058B1 (en) 1993-06-16
IE850476L (en) 1985-08-27
HK63090A (en) 1990-08-17
AU7083591A (en) 1991-07-11
CA1314541C (en) 1993-03-16
GR850483B (instruction) 1985-06-26
IL74365A (en) 1990-07-26
EP0155096A3 (en) 1986-07-02
ES540705A0 (es) 1987-01-01
NL930005I1 (nl) 1993-04-01
EP0155096B1 (en) 1989-10-04
DK85985D0 (da) 1985-02-26
IL74365A0 (en) 1985-05-31

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