DK0724592T3 - 16-substitueret-4-aza-androstan-5alfa-reduktaseisozym-1-inhibitorer - Google Patents

16-substitueret-4-aza-androstan-5alfa-reduktaseisozym-1-inhibitorer

Info

Publication number
DK0724592T3
DK0724592T3 DK94931961T DK94931961T DK0724592T3 DK 0724592 T3 DK0724592 T3 DK 0724592T3 DK 94931961 T DK94931961 T DK 94931961T DK 94931961 T DK94931961 T DK 94931961T DK 0724592 T3 DK0724592 T3 DK 0724592T3
Authority
DK
Denmark
Prior art keywords
inhibitors
5alfa
androstan
aza
reductase
Prior art date
Application number
DK94931961T
Other languages
Danish (da)
English (en)
Inventor
Philippe L Durette
William K Hagmann
Thomas J Lanza Jr
Gary H Rasmusson
Soumya P Sahoo
Richard L Tolman
Langen Derek Von
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
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Application granted granted Critical
Publication of DK0724592T3 publication Critical patent/DK0724592T3/da

Links

Classifications

    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P5/28—Antiandrogens

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
DK94931961T 1993-10-21 1994-10-21 16-substitueret-4-aza-androstan-5alfa-reduktaseisozym-1-inhibitorer DK0724592T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14115393A 1993-10-21 1993-10-21
PCT/US1994/012071 WO1995011254A1 (en) 1993-10-21 1994-10-21 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Publications (1)

Publication Number Publication Date
DK0724592T3 true DK0724592T3 (da) 1999-08-30

Family

ID=22494410

Family Applications (1)

Application Number Title Priority Date Filing Date
DK94931961T DK0724592T3 (da) 1993-10-21 1994-10-21 16-substitueret-4-aza-androstan-5alfa-reduktaseisozym-1-inhibitorer

Country Status (29)

Country Link
US (4) US5739137A (de)
EP (1) EP0724592B1 (de)
JP (1) JP2862376B2 (de)
KR (1) KR100363994B1 (de)
CN (1) CN1058499C (de)
AT (1) ATE175420T1 (de)
BG (1) BG61978B1 (de)
BR (2) BR9407866A (de)
CA (1) CA2173863C (de)
CY (1) CY2136B1 (de)
CZ (1) CZ292614B6 (de)
DE (1) DE69415824T2 (de)
DK (1) DK0724592T3 (de)
ES (1) ES2125495T3 (de)
FI (1) FI961697A (de)
HK (1) HK1009047A1 (de)
HU (1) HUT74613A (de)
IL (1) IL111357A (de)
LV (2) LV11622B (de)
NO (1) NO308037B1 (de)
NZ (1) NZ275293A (de)
PL (1) PL179611B1 (de)
RO (1) RO116197B1 (de)
RU (1) RU2142956C1 (de)
SK (1) SK281645B6 (de)
TW (1) TW413682B (de)
UA (1) UA44257C2 (de)
WO (1) WO1995011254A1 (de)
ZA (1) ZA948285B (de)

Families Citing this family (27)

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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
EP0724592B1 (de) 1993-10-21 1999-01-07 Merck & Co. Inc. 16-substituierte-4-aza-androstan-5-alpha-reduktase-isozym-i-inhibitoren
US5470976A (en) * 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents
EP0786999A4 (de) * 1994-10-21 1999-01-20 Merck & Co Inc Kombinationstherapie für akne
US5886005A (en) * 1995-01-17 1999-03-23 Merck & Co., Inc. 4-Aza-19-norandrostane derivatives
AU704933B2 (en) * 1995-10-19 1999-05-06 Merck & Co., Inc. 16-substituted-6-aza-steroid 5-alpha-reductase inhibitors
US5872126A (en) * 1996-09-06 1999-02-16 Merck & Co., Inc. Methods and compositions for treating preterm labor
US5945412A (en) * 1996-12-09 1999-08-31 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss
US5935968A (en) * 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
WO1998041509A1 (en) * 1997-03-17 1998-09-24 Merck & Co., Inc. Methods and compositions for treating polycystic ovary syndrome
EP1032400A4 (de) * 1997-10-28 2006-04-12 Merck & Co Inc Vorbeugung der plötzlich auftretenden akuten urinretention
US6187925B1 (en) * 1997-12-23 2001-02-13 Merck & Co., Inc. Intermediates and process for the synthesis of azasteroids
AU3977999A (en) * 1998-05-14 1999-11-29 Merck & Co., Inc. 7beta-methyl-16beta-((4-methylsulfonyl)-phenoxy)-4-aza-5alph a-androst-1-en-3-oneas a 5-alpha-reductase isozyme inhibitor
AR016257A1 (es) * 1998-05-14 2001-06-20 Merck & Co Inc Proceso para la sintesis estereoselectiva de ariloxi-4-aza-5alfa-androstan-3-onas, 16 alfa y 16 beta-sustituidas e insustituidas, e intermediariosobtenidos en dicho proceso.
US6902721B1 (en) 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
JP2002521449A (ja) * 1998-07-29 2002-07-16 メルク エンド カムパニー インコーポレーテッド 三環式化合物
US6268377B1 (en) 1998-09-28 2001-07-31 Merck & Co., Inc. Method for treating androgen-related conditions
US20020198215A1 (en) * 2000-10-23 2002-12-26 Lino Tavares Terazosin transdermal device and methods
US20080125403A1 (en) * 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
JP2008534505A (ja) 2005-03-25 2008-08-28 メルク エンド カムパニー インコーポレーテッド テストステロンサプリメントおよび５アルファ−レダクターゼインヒビターによる男性の治療方法
US20060241696A1 (en) * 2005-04-26 2006-10-26 Stjepan Krco Method of limiting hair loss and promoting hair growth
FR2910002B1 (fr) * 2006-12-13 2009-01-30 Sanofi Aventis Sa Nouveau procede pour l'obtention diastereoselective d'une amine primaire chirale sur un steroide
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
TWI593411B (zh) 2013-04-30 2017-08-01 徐懷山 組合物於製備抑制雄性素受體有關之功能及治療雄性素 受體相關之疾病的藥物之用途

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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
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
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
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
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
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
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
US4859681A (en) * 1984-02-27 1989-08-22 Merck & Co., Inc. 17 α-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-reductase inhibitors
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]
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
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
EP0285382B1 (de) * 1987-04-03 1994-04-13 Merck & Co. Inc. Behandlung von androgener Alopecia mit 17-bêta-n-mono-substituierten-carbamoyl-4-aza-5-alpha-androst-1-en-3-onen
US5116983A (en) * 1988-04-18 1992-05-26 Merck & Co., Inc. Dehydrogenation process intermediates
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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
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WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
WO1993023419A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-CHOLESTAN-ONES AS 5α-REDUCTASE INHIBITORS
CA2135167A1 (en) * 1992-05-20 1993-11-25 Donald W. Graham New 17-ester, amide, and ketone derivatives of 3-oxo-4- azasteroids as 5a-reductase inhibitors
AU4258493A (en) * 1992-05-21 1993-12-13 Endorecherche Inc. Inhibitors of testosterone 5alpha-reductase activity
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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
EP0724592B1 (de) * 1993-10-21 1999-01-07 Merck & Co. Inc. 16-substituierte-4-aza-androstan-5-alpha-reduktase-isozym-i-inhibitoren
US5525608A (en) * 1994-04-20 1996-06-11 Merck & Co., Inc. 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors
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US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents

Also Published As

Publication number Publication date
RU2142956C1 (ru) 1999-12-20
UA44257C2 (uk) 2002-02-15
ZA948285B (en) 1995-06-19
CZ292614B6 (cs) 2003-11-12
LV12316A (lv) 1999-07-20
EP0724592B1 (de) 1999-01-07
ATE175420T1 (de) 1999-01-15
AU680063B2 (en) 1997-07-17
ES2125495T3 (es) 1999-03-01
US5719158A (en) 1998-02-17
KR960705839A (ko) 1996-11-08
CN1058499C (zh) 2000-11-15
US6204273B1 (en) 2001-03-20
DE69415824D1 (de) 1999-02-18
FI961697A0 (fi) 1996-04-18
SK49696A3 (en) 1996-10-02
FI961697A (fi) 1996-04-18
WO1995011254A1 (en) 1995-04-27
CA2173863C (en) 2003-05-13
BG61978B1 (bg) 1998-11-30
US5739137A (en) 1998-04-14
BG100516A (en) 1996-11-29
PL314039A1 (en) 1996-08-05
LV11622B (en) 1997-06-20
TW413682B (en) 2000-12-01
CZ122896A3 (en) 1997-01-15
DE69415824T2 (de) 1999-08-05
NO961575D0 (no) 1996-04-19
JP2862376B2 (ja) 1999-03-03
RO116197B1 (ro) 2000-11-30
NZ275293A (en) 1998-02-26
NO961575L (no) 1996-04-19
EP0724592A1 (de) 1996-08-07
NO308037B1 (no) 2000-07-10
JPH09511213A (ja) 1997-11-11
US5910497A (en) 1999-06-08
HK1009047A1 (en) 1999-05-21
CY2136B1 (en) 2002-06-21
KR100363994B1 (ko) 2003-04-10
AU8086194A (en) 1995-05-08
SK281645B6 (sk) 2001-06-11
BR1100217A (pt) 1999-11-09
HU9601037D0 (en) 1996-06-28
BR9407866A (pt) 1996-10-29
PL179611B1 (pl) 2000-10-31
LV11622A (lv) 1996-12-20
LV12316B (en) 1999-11-20
CN1136318A (zh) 1996-11-20
CA2173863A1 (en) 1995-04-27
HUT74613A (en) 1997-01-28
IL111357A (en) 2001-01-28
IL111357A0 (en) 1994-12-29

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