ES2080297T3 - Derivados 17-g(b)-sustituido-4-aza-5g(a)-androstan-3-ona y procedimiento de preparacion de estos. - Google Patents

Derivados 17-g(b)-sustituido-4-aza-5g(a)-androstan-3-ona y procedimiento de preparacion de estos.

Info

Publication number
ES2080297T3
ES2080297T3 ES91903236T ES91903236T ES2080297T3 ES 2080297 T3 ES2080297 T3 ES 2080297T3 ES 91903236 T ES91903236 T ES 91903236T ES 91903236 T ES91903236 T ES 91903236T ES 2080297 T3 ES2080297 T3 ES 2080297T3
Authority
ES
Spain
Prior art keywords
sub
hydrogen
alkyl
group
substituted
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES91903236T
Other languages
English (en)
Inventor
Achille Panzeri
Salle Enrico Di
Marcella Nesi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Italia SRL
Original Assignee
Pharmacia SpA
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 Pharmacia SpA filed Critical Pharmacia SpA
Application granted granted Critical
Publication of ES2080297T3 publication Critical patent/ES2080297T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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
    • A61P35/00—Antineoplastic agents

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

LA PRESENTE INVENCION SE REFIERE A INHIBIDORES DE 5ALFA-REDUCTASA ESTERODICA QUE TIENEN LA FORMULA (I) DONDE R SUB 1 ES HIDROGENO, UN GRUPO ALQUILO C SUB 1 C SUB 1 UFRE; W ES UN GRUPO (2) DONDE R SUB 2 Y R SUB 3 SE ELIGEN INDEPENDIENTEMENTE ENTRE EL GRUPO FORMADO POR HIDROGENO, ALQUILO C SUB 1 QUILO C SUB 6 ALQUILO, CICLOALQUILO, CICLOALQUILALQUILO Y ARILO PUEDE ESTAR NO-SUSTITUIDO O SUSTITUIDO POR UN SUSTITUTO -OR SUB 4 DONDE R SUB 4 ES HIDROGENO O ALQUILO C SUB 1 ICLOALQUILALQUILO C SUB 6 OS ALQUILO, CICLOALQUILO Y CICLOALQUILALQUILO, PUEDE ESTAR SUSTITUIDO O NO POR UN SUSTITUTO ELEGIDO ENTRE: A) -OR SUB 4 DONDE R SUB 4 ES COMO SE HA DEFINIDO ANTERIORMENTE, Y B) (3) DONDE BIEN R SUB 5 Y R SUB 6 SE ELIGEN INDEPENDIENTEMENTE ENTRE EL GRUPO FORMADO POR HIDROGENO, ALQUILO C SUB 1 QUILO C SUB 1 LO HETEROMONOCICLICO SATURADO PENTALOMICO O HEXATOMICO, CONTENIENDO OPCIONALMENTE AL MENOS UN HETEROATOMO ADICIONAL ELEGIDO ENTRE OXIGENO Y NITROGENO; Y EL SIMBOLO (----) REPRESENTA UN ENLACE SENCILLO ODOBLE, Y SUS SALES FARMACEUTICAMENTE ACEPTABLES. EN VISTA DE SU ACTIVIDAD INHIBIDORA DE 5ALFA-REDUCTASA, LOS COMPUESTOS DE LA INVENCION PUEDEN SER UTILES PARA EL TRATAMIENTO DE CONDICIONES DEPENDIENTES DE ANDROGENOS.
ES91903236T 1990-02-09 1991-02-06 Derivados 17-g(b)-sustituido-4-aza-5g(a)-androstan-3-ona y procedimiento de preparacion de estos. Expired - Lifetime ES2080297T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB909002922A GB9002922D0 (en) 1990-02-09 1990-02-09 17 beta-substituted-4-aza-5 alpha-androstan-3-one derivatives and process for their preparation

Publications (1)

Publication Number Publication Date
ES2080297T3 true ES2080297T3 (es) 1996-02-01

Family

ID=10670693

Family Applications (1)

Application Number Title Priority Date Filing Date
ES91903236T Expired - Lifetime ES2080297T3 (es) 1990-02-09 1991-02-06 Derivados 17-g(b)-sustituido-4-aza-5g(a)-androstan-3-ona y procedimiento de preparacion de estos.

Country Status (26)

Country Link
US (1) US5155107A (es)
EP (1) EP0468012B1 (es)
JP (1) JPH04505462A (es)
KR (1) KR920701234A (es)
CN (1) CN1054771A (es)
AT (1) ATE128143T1 (es)
AU (1) AU642215B2 (es)
CA (1) CA2049318A1 (es)
CZ (1) CZ279484B6 (es)
DE (1) DE69113155T2 (es)
DK (1) DK0468012T3 (es)
ES (1) ES2080297T3 (es)
FI (1) FI914723A0 (es)
GB (1) GB9002922D0 (es)
GR (1) GR3017996T3 (es)
HR (1) HRP921221A2 (es)
HU (1) HUT59158A (es)
IE (1) IE910408A1 (es)
IL (1) IL97025A (es)
MY (1) MY105402A (es)
NO (1) NO913923L (es)
NZ (1) NZ237023A (es)
PT (1) PT96699A (es)
RU (1) RU2088589C1 (es)
WO (1) WO1991012261A1 (es)
ZA (1) ZA91918B (es)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CA2084799C (en) 1991-12-17 2003-01-28 Glenn J. Gormley Method of prevention of prostatic carcinoma with 17 beta-n-monosubstituted-carbamoyl-4-aza-5 alpha-androst-1 -en-3-ones
ATE165368T1 (de) * 1991-12-20 1998-05-15 Glaxo Wellcome Inc Inhibitoren von testosteron-5-alpha reductase.
EP0641204B1 (en) * 1992-05-20 2000-08-16 Merck & Co. Inc. 17-ethers and thioethers of 4-aza-steroids
CZ283894A3 (en) * 1992-05-20 1995-09-13 Merck & Co Inc 7beta-substituted 4-aza-5alpha-cholestanones, their use for the preparation of pharmaceutical preparations and pharmaceutical compositions containing thereof
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
CA2135173A1 (en) * 1992-05-20 1993-11-25 Bruce E. Witzel Ester derivatives of 4-aza-steroids
DE69326008T2 (de) * 1992-05-20 2000-03-02 Merck & Co., Inc. 17-amino-substituierte 4-azasteroide als 5-alpha-reductase inhibitoren
ATE195129T1 (de) * 1992-05-20 2000-08-15 Merck & Co Inc 4-azasteroide als 5-alpha-reduktase
JPH07506575A (ja) * 1992-05-21 1995-07-20 アンドルシェルシュ・インコーポレイテッド テストステロン５α−レダクターゼ活性の阻害剤
GB9216329D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives
GB9216280D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa Steroids with a fluorinated acylureidic type side chain
GB9216284D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa Fluorinated 17beta-substituted 4-aza-5alpha-androstane-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
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
US5621104A (en) * 1993-03-24 1997-04-15 Merck & Co., Inc. Substituted 3-phenanthridinone derivatives as 5-alpha-reductase inhibitors
DE69405760T2 (de) * 1993-06-28 1998-04-09 Merck & Co Inc 4-aza-pregnan-5-alpha-reductase isozym 1 inhibitoren
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
GB9415178D0 (en) * 1994-07-28 1994-09-21 Erba Carlo Spa 4-azasteroids with side-chain fluoroketones
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
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
CN1072679C (zh) * 1995-07-30 2001-10-10 重庆医科大学 一种氮杂甾体化合物、制备及其用途
GB9518858D0 (en) * 1995-09-14 1995-11-15 Pharmacia Spa Phenylsubstituted 4-azasteroid fluoroderivatives
AU7078296A (en) * 1995-09-27 1997-04-17 Merck & Co., Inc. Method of preventing androgenetic alopecia with 5-alpha reductase inhibitors
GB9727522D0 (en) 1997-12-31 1998-02-25 Pharmacia & Upjohn Spa Process for preparing carboxamido-4-azasteroids
US6645974B2 (en) * 2001-07-31 2003-11-11 Merck & Co., Inc. Androgen receptor modulators and methods for use thereof
US7605152B2 (en) * 2002-01-15 2009-10-20 Merck & Co., Inc. 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators
KR100503193B1 (ko) * 2002-08-19 2005-07-25 한미약품 주식회사 3-옥소-4-아자-5α-안드로스탄 화합물의 선택적인 제조방법
JP4917889B2 (ja) * 2003-09-25 2012-04-18 テル アヴィヴ ユニヴァーシティ フューチャー テクノロジー ディヴェロップメント エル．ピー． アミロイド関連疾患を処置するための組成物及びその使用方法
EP1746998A1 (en) * 2004-03-22 2007-01-31 Ranbaxy Laboratories, Ltd. Combination therapy for lower urinary tract symptoms
CN100355772C (zh) * 2005-12-28 2007-12-19 天津大学 具有5α－还原酶抑制活性的甾体化合物及其制备方法
WO2023070071A2 (en) * 2021-10-21 2023-04-27 The Board Of Trustees Of The University Of Illinois Small molecule activators of the immune system

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA970692A (en) * 1971-11-08 1975-07-08 Walter Voigt METHODS OF INHIBITING THE ACTIVITY OF TESTOSTERONE 5.alpha.-REDUCTASE
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
US4220778A (en) * 1978-10-30 1980-09-02 G. D. Searle & Co. 8-Aryl-1,2,3,4-tetrahydroisoquinoline and derivatives thereof
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
US4317817A (en) * 1979-08-27 1982-03-02 Richardson-Merrell Inc. Novel steroid 5α-reductase inhibitors
US4396615A (en) * 1981-06-24 1983-08-02 Duke University Method of treating androgen-related disorders
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
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-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
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

Also Published As

Publication number Publication date
FI914723A7 (fi) 1991-10-07
HU913193D0 (en) 1992-01-28
CS9100274A2 (en) 1991-12-17
RU2088589C1 (en) 1997-08-27
WO1991012261A1 (en) 1991-08-22
AU7230791A (en) 1991-09-03
ZA91918B (en) 1991-11-27
NZ237023A (en) 1993-01-27
NO913923D0 (no) 1991-10-07
EP0468012A1 (en) 1992-01-29
KR920701234A (ko) 1992-08-11
EP0468012B1 (en) 1995-09-20
CN1054771A (zh) 1991-09-25
CZ279484B6 (cs) 1995-05-17
FI914723A0 (fi) 1991-10-07
NO913923L (no) 1991-12-06
DE69113155T2 (de) 1996-02-29
CA2049318A1 (en) 1991-08-10
IL97025A (en) 1995-05-26
MY105402A (en) 1994-09-30
GB9002922D0 (en) 1990-04-04
DK0468012T3 (da) 1995-11-06
IL97025A0 (en) 1992-03-29
US5155107A (en) 1992-10-13
ATE128143T1 (de) 1995-10-15
GR3017996T3 (en) 1996-02-29
HUT59158A (en) 1992-04-28
DE69113155D1 (de) 1995-10-26
AU642215B2 (en) 1993-10-14
HRP921221A2 (en) 1995-12-31
PT96699A (pt) 1991-10-31
JPH04505462A (ja) 1992-09-24
IE910408A1 (en) 1991-08-14

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