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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28Antiandrogens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0066Normal 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)
  • Ceramic Products (AREA)
  • Dental Preparations (AREA)
  • Details Of Garments (AREA)
  • Medicines Containing Plant Substances (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 (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ252866A (en) * 1992-04-30 1996-09-25 Smithkline Beecham Corp 17-acyl-estra-1,3,5(10)-triene-3-carboxylic acids; precursors
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
ATE227122T1 (de) * 1993-09-03 2002-11-15 Smithkline Beecham Corp Stabilisierte tablettenformulierung
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
DE69942578D1 (de) 1998-05-22 2010-08-26 Univ R Bifunktionelle moleküle sowie darauf basierende therapien.
EP3827747A1 (en) 2005-04-28 2021-06-02 Otsuka Pharmaceutical Co., Ltd. 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
NZ616673A (en) 2009-02-20 2014-08-29 To Bbb Holding B V Glutathione-based drug delivery system
ES2942923T3 (es) 2009-05-06 2023-06-07 Laboratory Skin Care Inc Composiciones de administración dérmica que comprenden complejos de agente activo-partículas de fosfato de calcio y métodos de uso de las mismas

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US4910226A (en) * 1987-04-29 1990-03-20 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
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
AU655280B2 (en) 1994-12-15
US5212166A (en) 1993-05-18
EP0540717B1 (en) 1997-07-23
TW213467B (es) 1993-09-21
ITMI911432A0 (it) 1991-05-24
YU52992A (sh) 1995-03-27
RU2104283C1 (ru) 1998-02-10
CN1067057A (zh) 1992-12-16
ATE155792T1 (de) 1997-08-15
FI930277A (fi) 1993-01-22
HU9300176D0 (en) 1993-04-28
EP0540717A1 (en) 1993-05-12
DE69221074T2 (de) 1997-11-13
MX9202438A (es) 1992-11-01
MY131089A (en) 2007-07-31
IE921634A1 (en) 1992-12-02
IT1259419B (it) 1996-03-18
DE69221074D1 (de) 1997-09-04
ID954B (id) 1996-09-25
CA2087953A1 (en) 1992-11-25
CN1035055C (zh) 1997-06-04
JPH06500342A (ja) 1994-01-13
EP0517047A1 (en) 1992-12-09
IL101947A (en) 1996-01-19
NZ242850A (en) 1994-01-26
NO930244D0 (no) 1993-01-25
DK0540717T3 (da) 1997-08-18
FI930277A0 (fi) 1993-01-22
AU1778192A (en) 1992-12-30
ITMI911432A1 (it) 1992-11-24
NO930244L (no) 1993-01-27
CZ281309B6 (cs) 1996-08-14
ZA923758B (en) 1993-01-27
HUT64083A (en) 1993-11-29
JP3226919B2 (ja) 2001-11-12
WO1992020700A1 (en) 1992-11-26
CZ26593A3 (en) 1993-11-17

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