ES2106185T3 - 3-carboxiesteroides 17-beta-sustituidos no saturados. - Google Patents

3-carboxiesteroides 17-beta-sustituidos no saturados.

Info

Publication number
ES2106185T3
ES2106185T3 ES92910992T ES92910992T ES2106185T3 ES 2106185 T3 ES2106185 T3 ES 2106185T3 ES 92910992 T ES92910992 T ES 92910992T ES 92910992 T ES92910992 T ES 92910992T ES 2106185 T3 ES2106185 T3 ES 2106185T3
Authority
ES
Spain
Prior art keywords
group
alkyl group
hydrogen
cycloalkyl
oxygen
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
ES92910992T
Other languages
English (en)
Inventor
Achille Panzeri
Marcella Nesi
Salle Enrico Di
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 and Upjohn 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 and Upjohn SpA filed Critical Pharmacia and Upjohn SpA
Application granted granted Critical
Publication of ES2106185T3 publication Critical patent/ES2106185T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • 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

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)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Details Of Garments (AREA)
  • Ceramic Products (AREA)
  • Dental Preparations (AREA)

Abstract

LA PRESENTE INVENCION SE REFIERE A INHIBIDORES DE LA 5OREDUCTASA ESTEROIDICOS QUE TIENE LA FORMULA (I) EN DONDE Y ES OXIGENO O AZUFRE; R ES UN GRUPO: A) -OR4, EN DONDE R4 ES HIDROGENO O UN GRUPO ALQUILO C1-C6; B) (1) EN DONDE CADA R5 Y R6 ES, INDEPENDIENTEMENTE, HIDROGENO O UN GRUPO ALQUILO C1-C6; C) (2) EN DONDE R7 ES HIDROGENO O UN GRUPO ALQUILO C1-C6 Y W ES UN GRUPO: (I) (3), EN DONDE R8 ES UN GRUPO ALQUILO C1-C6, UN GRUPO CICLOALQUILO C5-C6, UN GRUPO CICLOALQUILALQUILO C6-C9, UN GRUPO FENILO O UN GRUPO BENCILO; O (II) (4), EN DONDE R9 ES UN GRUPO ALQUILO C1-C6 O UN GRUPO CICLOALQUILO C5-C6; O (III) (5), EN DONDE R5 Y R6 SON COMO SE HAN DEFINIDO ARRIBA; (D) (6), EN DONDE CADA R10 Y R11 ES, INDEPENDIENTEMENTE, HIDROGENO O UN GRUPO ALQUILO C1-C6 QUE, TOMADOS JUNTO CON EL ATOMO DE NITROGENO AL QUE ESTAN ENLAZADOS, FORMAN UN ANILLO HETEROMONOCICLICO SATURADO PENTATOMICO O HEXATOMICO QUE OPCIONALMENTE CONTIENE AL MENOS UN HETEROATOMO ADICIONAL SELECCIONADO DEL OXIGENO Y DEL NITROGENO Y N ES UN ENTERO DE 2 A 4; R1 ES HIDROGENO, UN GRUPO ALQUILO C1C6, UN GRUPO CICLOALQUILO C5-C6, UN GRUPO CICLOALQUILALQUILO C6C9 O UN GRUPO ARILO; CADA R2 Y R3 SE SELECCIONA, INDEPENDIENTEMENTE, DEL GRUPO QUE CONSISTE EN HIDROGENO, ALQUILO C1-C6, CICLOALQUILO C5-C6, CICLOALQUILALQUILO C6-C9 O ARILO O R2 Y R3, TOMADOS JUNTO CON EL ATOMO DE NITROGENO AL QUE SE ENCUENTRAN ENLAZADOS, FORMAN UN ANILLO HETEROMONOCICLICO SATURADO PENTATOMICO O HEXATOMICO QUE OPCIONALMENTE CONTIENE AL MENOS UN HETEROATOMO ADICIONAL SELECCIONADO DEL OXIGENO Y DEL NITROGENO Y EL SIMBOLO DE RAYA CONTINUA CON RAYAS DISCONTINUAS ENCIMA REPRESENTA UN ENLACE DOBLE O SENCILLO QUE, CUANDO ES DOBLE, EL HIDROGENO DE LA POSICION 5O NO EXISTE Y LAS SALES FARMACEUTICAMENTE ACEPTABLES DE LOS MISMOS. ANTE LA ACTIVIDAD INHIBIDORA DE LA 5O-REDUCTASA, LOS COMPUESTOS DE LA INVENCION PUEDEN SER UTILES PARA EL TRATAMIENTO DE CONDICIONES ANDROGENODEPENDIENTES.
ES92910992T 1991-05-24 1992-05-22 3-carboxiesteroides 17-beta-sustituidos no saturados. Expired - Lifetime ES2106185T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ITMI911432A IT1259419B (it) 1991-05-24 1991-05-24 Steroidi 3-carbossi 17b - sostituiti insaturi utili come inibitori della testosterone 5 a reduttasi

Publications (1)

Publication Number Publication Date
ES2106185T3 true ES2106185T3 (es) 1997-11-01

Family

ID=11359980

Family Applications (1)

Application Number Title Priority Date Filing Date
ES92910992T Expired - Lifetime ES2106185T3 (es) 1991-05-24 1992-05-22 3-carboxiesteroides 17-beta-sustituidos no saturados.

Country Status (26)

Country Link
US (1) US5212166A (es)
EP (2) EP0517047A1 (es)
JP (1) JP3226919B2 (es)
CN (1) CN1035055C (es)
AT (1) ATE155792T1 (es)
AU (1) AU655280B2 (es)
CA (1) CA2087953A1 (es)
CZ (1) CZ281309B6 (es)
DE (1) DE69221074T2 (es)
DK (1) DK0540717T3 (es)
ES (1) ES2106185T3 (es)
FI (1) FI930277A0 (es)
HU (1) HUT64083A (es)
ID (1) ID954B (es)
IE (1) IE921634A1 (es)
IL (1) IL101947A (es)
IT (1) IT1259419B (es)
MX (1) MX9202438A (es)
MY (1) MY131089A (es)
NO (1) NO930244L (es)
NZ (1) NZ242850A (es)
RU (1) RU2104283C1 (es)
TW (1) TW213467B (es)
WO (1) WO1992020700A1 (es)
YU (1) YU52992A (es)
ZA (1) ZA923758B (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU4291993A (en) * 1992-04-30 1993-11-29 Smithkline Beecham Corporation 17alpha and 17beta -substituted estra-1,3,5(10)-triene-3-carboxylic acid
US5683995A (en) * 1992-11-18 1997-11-04 Smithkline Beecham Corporation 17 substituted acyl-3-carboxy 3,5-diene steroidals as α-reductase inhibitors
US5641765A (en) * 1992-11-18 1997-06-24 Smithkline Beecham Corporation 17-αand 17-βsubstituted acyl-3-carboxy-3,5-dienes and use in inhibiting 5-α-reductase
ES2185666T3 (es) * 1993-09-03 2003-05-01 Smithkline Beecham Corp Formulacion estabilizada para comprimidos.
GB9324371D0 (en) * 1993-11-26 1994-01-12 Erba Carlo Spa Side chain fluoro substituted 3-carboxysteroids
US5430157A (en) * 1993-12-13 1995-07-04 Eli Lilly And Company Reduced phenanthrenes
GB9402041D0 (en) * 1994-02-03 1994-03-30 Smithkline Beecham Corp Compounds
US5714480A (en) * 1994-03-31 1998-02-03 Smithkline Beecham Corporation Treating cardiovascular disease with steroidal 5-alpha-reductase inhibitors
WO1995028413A1 (en) * 1994-04-15 1995-10-26 Smithkline Beecham Corporation 17β-SUBSTITUTED 3-CARBOXY STEROIDS THAT INHIBIT 5-α-REDUCTASE
GB9415183D0 (en) * 1994-07-28 1994-09-21 Erba Carlo Spa 3-carboxysteroids with a fluorinated side-chain
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
US6372712B1 (en) 1998-05-22 2002-04-16 The Board Of Trustees Of The Leland Stanford Jr. University Synthetic bifunctional molecules containing a drug moiety and presenter protein ligand
WO2001021642A1 (de) * 1999-09-22 2001-03-29 Aventis Pharma Deutschland Gmbh 4-benzylaminochinoline konjugaten mit gallensaeure und ihre heteroanalogen, verfahren zu ihrer herstellung, diese verbindungen enthaltende arzneimittel und deren anwendung
EP2671508B1 (en) 2005-04-28 2020-09-16 Proteus Digital Health, Inc. Pharma-informatics system
US9062126B2 (en) 2005-09-16 2015-06-23 Raptor Pharmaceuticals Inc. Compositions comprising receptor-associated protein (RAP) variants specific for CR-containing proteins and uses thereof
ES2919563T3 (es) 2009-02-20 2022-07-27 Enhanx Biopharm Inc Sistema de administración de medicamentos a base de glutatión
KR20180114970A (ko) 2009-05-06 2018-10-19 라보라토리 스킨 케어, 인크. 활성제-칼슘 포스페이트 입자 복합체를 포함하는 피부 전달 조성물 및 이들을 이용하는 방법

Family Cites Families (6)

* 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
US4910226A (en) * 1987-04-29 1990-03-20 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
US5041433A (en) * 1987-04-29 1991-08-20 Smithkline Beecham Corporation 11-keto or hydroxy 3,5-diene steroids as inhibitors of steriod 5-α-reductase
US5032586A (en) * 1989-08-24 1991-07-16 Smithkline Beecham Corporation 7-keto or hydroxy 3,5-diene steroids as inhibitors of steroid 5-alpha reductase
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
DK0567271T3 (da) * 1992-04-20 1998-02-16 Sankyo Co Steroidderivater til behandling af prostatahypertrofi, fremgangsmåde til fremstilling heraf og anvendelser heraf

Also Published As

Publication number Publication date
HU9300176D0 (en) 1993-04-28
CZ281309B6 (cs) 1996-08-14
TW213467B (es) 1993-09-21
MX9202438A (es) 1992-11-01
JPH06500342A (ja) 1994-01-13
NO930244L (no) 1993-01-27
NZ242850A (en) 1994-01-26
CZ26593A3 (en) 1993-11-17
AU1778192A (en) 1992-12-30
WO1992020700A1 (en) 1992-11-26
US5212166A (en) 1993-05-18
ZA923758B (en) 1993-01-27
NO930244D0 (no) 1993-01-25
ITMI911432A1 (it) 1992-11-24
ITMI911432A0 (it) 1991-05-24
DE69221074T2 (de) 1997-11-13
IT1259419B (it) 1996-03-18
MY131089A (en) 2007-07-31
DE69221074D1 (de) 1997-09-04
CA2087953A1 (en) 1992-11-25
HUT64083A (en) 1993-11-29
AU655280B2 (en) 1994-12-15
ATE155792T1 (de) 1997-08-15
CN1067057A (zh) 1992-12-16
RU2104283C1 (ru) 1998-02-10
FI930277A7 (fi) 1993-01-22
EP0540717B1 (en) 1997-07-23
ID954B (id) 1996-09-25
IL101947A (en) 1996-01-19
EP0540717A1 (en) 1993-05-12
DK0540717T3 (da) 1997-08-18
FI930277A0 (fi) 1993-01-22
IE921634A1 (en) 1992-12-02
JP3226919B2 (ja) 2001-11-12
EP0517047A1 (en) 1992-12-09
CN1035055C (zh) 1997-06-04
YU52992A (sh) 1995-03-27

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