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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Plant Substances (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 (28)

Country Link
US (4) US5739137A (cs)
EP (1) EP0724592B1 (cs)
JP (1) JP2862376B2 (cs)
KR (1) KR100363994B1 (cs)
CN (1) CN1058499C (cs)
AT (1) ATE175420T1 (cs)
BG (1) BG61978B1 (cs)
BR (2) BR9407866A (cs)
CA (1) CA2173863C (cs)
CY (1) CY2136B1 (cs)
CZ (1) CZ292614B6 (cs)
DE (1) DE69415824T2 (cs)
DK (1) DK0724592T3 (cs)
ES (1) ES2125495T3 (cs)
FI (1) FI961697A7 (cs)
HU (1) HUT74613A (cs)
IL (1) IL111357A (cs)
LV (2) LV11622B (cs)
NO (1) NO308037B1 (cs)
NZ (1) NZ275293A (cs)
PL (1) PL179611B1 (cs)
RO (1) RO116197B1 (cs)
RU (1) RU2142956C1 (cs)
SK (1) SK281645B6 (cs)
TW (1) TW413682B (cs)
UA (1) UA44257C2 (cs)
WO (1) WO1995011254A1 (cs)
ZA (1) ZA948285B (cs)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
HUT74613A (en) * 1993-10-21 1997-01-28 Merck & Co Inc 16-substituted-4-aza-androstane derivatives as 5-alpha-reductase isozyme 1 inhibitors and pharmaceutical compositions containing the same
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
JPH10508586A (ja) * 1994-10-21 1998-08-25 メルク エンド カンパニー インコーポレーテッド 組み合わせ式アクネ治療方法
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
CA2283098A1 (en) * 1997-03-17 1998-09-24 Merck & Co., Inc. Methods and compositions for treating polycystic ovary syndrome
US5935968A (en) * 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
JP2001521000A (ja) * 1997-10-28 2001-11-06 メルク エンド カムパニー インコーポレーテッド 誘発性急性閉尿の予防
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.
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
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
CA2338298A1 (en) * 1998-07-29 2000-02-10 Merck & Co., Inc. Tricyclic compounds
US6268377B1 (en) 1998-09-28 2001-07-31 Merck & Co., Inc. Method for treating androgen-related conditions
WO2002054996A2 (en) * 2000-10-23 2002-07-18 Euro Celtique Sa Terazosin transdermal device and methods
WO2002092092A1 (fr) * 2001-05-15 2002-11-21 Taisho Pharmaceutical Co., Ltd. Composition liquide contenant du minoxidil
EP1734963A4 (en) * 2004-04-02 2008-06-18 Merck & Co Inc METHOD FOR TREATING PEOPLE WITH METABOLIC AND ANTHROPOMETRIC DISORDER
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
RU2364402C1 (ru) * 2008-04-28 2009-08-20 Государственное образовательное учреждение высшего профессионального образования Московская медицинская академия им. И.М. Сеченова Федерального агентства по здравоохранению и социальному развитию (ГОУВПО ММА им. И.М. Сеченова Росздрава) Способ лечения больных хроническим простатитом
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
TWI522102B (zh) 2013-04-30 2016-02-21 長庚醫療財團法人 組合物於製備治療或預防性治療痤瘡的藥物之用途

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
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
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
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
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
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
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]
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
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-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
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
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
CA2084798A1 (en) * 1991-12-17 1993-06-18 Glenn J. Gormley Method of preventing prostatic carcinoma with 17beta -acyl-4-aza-5.- androst-1-ene-3-ones
GB2264494A (en) * 1992-02-25 1993-09-01 Merck & Co Inc 17b-n-monosubstituted carbamoyl-11-oxo-4-aza-5-a-androst-1-en-3-one testosterone-5-alpha reductase inhibitors
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
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
HUT71484A (en) * 1992-05-20 1995-11-28 Merck & Co Inc Process for producing of 7beta-substituted-4-aza-5alpha-cholestan-ones as 5-alpha-reductase inhibitors and pharmaceuticals compositions containing them
WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
TW239145B (cs) * 1992-05-21 1995-01-21 Endorech Inc
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
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
US5380728A (en) * 1993-02-10 1995-01-10 Merck & Co., Inc. Aldehyde metabolite of 17β-N-monosubstituted-carbamoyl-4-aza-5α-a
US5407944A (en) * 1993-02-19 1995-04-18 Goldman; Boris E. Compositions and methods for promoting hair growth
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
HUT74613A (en) * 1993-10-21 1997-01-28 Merck & Co Inc 16-substituted-4-aza-androstane derivatives as 5-alpha-reductase isozyme 1 inhibitors and pharmaceutical compositions containing the same
US5525608A (en) * 1994-04-20 1996-06-11 Merck & Co., Inc. 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors
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
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
US5910497A (en) 1999-06-08
AU8086194A (en) 1995-05-08
ES2125495T3 (es) 1999-03-01
US6204273B1 (en) 2001-03-20
US5739137A (en) 1998-04-14
LV12316B (en) 1999-11-20
PL179611B1 (pl) 2000-10-31
BG100516A (bg) 1996-11-29
JPH09511213A (ja) 1997-11-11
TW413682B (en) 2000-12-01
CY2136B1 (en) 2002-06-21
CN1136318A (zh) 1996-11-20
FI961697L (fi) 1996-04-18
CZ292614B6 (cs) 2003-11-12
CA2173863C (en) 2003-05-13
KR100363994B1 (ko) 2003-04-10
HUT74613A (en) 1997-01-28
JP2862376B2 (ja) 1999-03-03
CZ122896A3 (en) 1997-01-15
CN1058499C (zh) 2000-11-15
KR960705839A (ko) 1996-11-08
BG61978B1 (bg) 1998-11-30
UA44257C2 (uk) 2002-02-15
RO116197B1 (ro) 2000-11-30
BR1100217A (pt) 1999-11-09
WO1995011254A1 (en) 1995-04-27
LV11622B (en) 1997-06-20
EP0724592B1 (en) 1999-01-07
CA2173863A1 (en) 1995-04-27
SK49696A3 (en) 1996-10-02
DE69415824D1 (de) 1999-02-18
HU9601037D0 (en) 1996-06-28
AU680063B2 (en) 1997-07-17
DE69415824T2 (de) 1999-08-05
LV12316A (lv) 1999-07-20
IL111357A (en) 2001-01-28
FI961697A0 (fi) 1996-04-18
SK281645B6 (sk) 2001-06-11
BR9407866A (pt) 1996-10-29
IL111357A0 (en) 1994-12-29
HK1009047A1 (en) 1999-05-21
US5719158A (en) 1998-02-17
ATE175420T1 (de) 1999-01-15
NZ275293A (en) 1998-02-26
PL314039A1 (en) 1996-08-05
FI961697A7 (fi) 1996-04-18
RU2142956C1 (ru) 1999-12-20
EP0724592A1 (en) 1996-08-07
NO961575D0 (no) 1996-04-19
NO308037B1 (no) 2000-07-10
ZA948285B (en) 1995-06-19
NO961575L (no) 1996-04-19
LV11622A (lv) 1996-12-20

Similar Documents

Publication Publication Date Title
DE69415824D1 (de) 16-substituierte-4-aza-androstan-5-alpha-reduktase-isozym-i-inhibitoren
GEP20094660B (en) Pyran-2-ones and 5,6-dihydropyran-2-ones useful for treating hyperplasia and other diseases
DE69417925D1 (de) 7-substituierte-4-aza-steroid-derivate als 5-alpha-reductase-hemmer
ATE143942T1 (de) Carbonsäurederivate als 5-alpha-reduktase- inhibitor
EP0641208A4 (en) 4-AZASTEROIDS AS 5-ALPHA REDUCTASE.
EP1266658A3 (en) Use of betulinic acid derivatives for the treatment and prevention of melanoma
RU94046057A (ru) Ингибиторы активности тестостерон 5 альфа -редуктазы, фармкомпозиция, способ подавления активности, тестостерон 5 альфа -редуктазы
HU9600976D0 (en) Method of treating androgenic alopecia with 5-alpha reductase inhibitors
WO2000007576A3 (en) INHIBITORS OF TYPE 3 3α-HYDROSTEROID DEHYDROGENASE
DE69326008D1 (de) 17-amino-substituierte 4-azasteroide als 5-alpha-reductase inhibitoren
NZ332096A (en) Alpha-hydroxylic acid derivatives their production and use in treating conditions requiring endothelin inhibition
ATE198274T1 (de) 17 beta-aryl-4-aza-steroidderivate
ES2160842T3 (es) Derivados de esteroides 17-alquil-4-aza-7-sustituidos.
BR9203266A (pt) Composto,formulacao farmaceutica,processo para inibir 5alfa-reductase,processos para tratar hiperplasia benigna da prostata,seborreia e alopecia androgenica