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AR049547A1 - STEROID PROPHARMS WITH ANDROGENIC ACTION - Google Patents

STEROID PROPHARMS WITH ANDROGENIC ACTION

Info

Publication number
AR049547A1
AR049547A1 ARP050102084A ARP050102084A AR049547A1 AR 049547 A1 AR049547 A1 AR 049547A1 AR P050102084 A ARP050102084 A AR P050102084A AR P050102084 A ARP050102084 A AR P050102084A AR 049547 A1 AR049547 A1 AR 049547A1
Authority
AR
Argentina
Prior art keywords
group
hydrogen atom
alkyl
cycloalkyl
atom
Prior art date
Application number
ARP050102084A
Other languages
Spanish (es)
Inventor
Peter Droescher
Walter Elger
Alexander Hillisch
Gudrun Reddersen
Sven Ring
Birgitt Schneider
Ralf Wyrwa
Original Assignee
Schering Ag
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 Schering Ag filed Critical Schering Ag
Publication of AR049547A1 publication Critical patent/AR049547A1/en

Links

Classifications

    • 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
    • C07J41/0038Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an androstane skeleton, including 18- or 19-substituted derivatives, 18-nor derivatives and also derivatives where position 17-beta is substituted by a carbon atom not directly bonded to a further carbon atom and not being part of an amide group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P5/26Androgens
    • 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
    • C07J41/0044Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an estrane or gonane skeleton, including 18-substituted derivatives and derivatives where position 17-beta is substituted by a carbon atom not directly bonded to another carbon atom and not being part of an amide group

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

Profármacos de esteroides, composiciones farmacéuticas, que contienen estos compuestos, así como su uso para la preparacion de medicamentos con accion androgénica. Reivindicacion 1: Profármacos de esteroides de la formula general (1), caracterizado porque: n es un numero 0-4; R1 es un radical -SO2NH2 o -NHSO2NH2; en donde R2, R3, y X, X1 son un átomo de hidrogeno, un átomo de halogeno, un grupo nitrilo, un grupo nitro, un grupo alquilo C1-5, un grupo CpF2p+1 con p = 1-3, un grupo OC(O)-R20, COOR20, OR20, C(O)NHR20 u OC(O)NHR21, en donde R20, R21 y R22 son un grupo alquilo C1-5, un grupo cicloalquilo C3-8, un grupo arilo, un grupo alquilenarilo C1-4, un grupo alquilen C1-4-cicloalquilo C3-8 o cicloalquilen C3-8-alquilo C1-4, así como R20 puede ser, además, un hidrogeno; o R2 es un radical -SO2NH2 o -NHSO2NH2; en donde R2, R3, y X, X1 son un átomo de hidrogeno, un átomo de halogeno, un grupo nitrilo, un grupo nitro, un grupo alquilo C1-5, un grupo CpF2p+1 con p = 1-3, un grupo OC(O)-R20, COOR20, OR20, C(O)NHR20 u OC(O)NHR21, en donde R20, R21 y R22 son un grupo alquilo C1-5, un grupo cicloalquilo C3-8, un grupo arilo, un grupo alquilenarilo C1-4, un grupo alquilen C1-4-cicloalquilo C3-8 o cicloalquilen C3-8-alquilo C1-4, así como R20 puede ser, además, un hidrogeno; o R3 es un radical -SO2NH2 o -NHSO2NH2; en donde R2, R3, y X, X1 son un átomo de hidrogeno, un átomo de halogeno, un grupo nitrilo, un grupo nitro, un grupo alquilo C1-5, un grupo CpF2p+1 con p = 1-3, un grupo OC(O)-R20, COOR20, OR20, C(O)NHR20 u OC(O)NHR21, en donde R20, R21 y R22 son un grupo alquilo C1-5, un grupo cicloalquilo C3-8, un grupo arilo, un grupo alquilenarilo C1-4, un grupo alquilen C1-4-cicloalquilo C3-8 o cicloalquilen C3-8-alquilo C1-4, así como R20 también puede ser un hidrogeno; y ESTEROIDE es un sistema cíclico esteroide de acuerdo con las formulas generales (2) a (4), en donde: Y es un átomo de oxígeno o de carbono; R4 es un átomo de hidrogeno, un átomo de halogeno, un grupo metilo, trifluorometilo, hidroxi, tri(alquil C1-6)sililoxi, alcoxi C1-5 o heterocicloalquiloxi C2-5; R7 es un átomo de hidrogeno, un grupo metilo o etilo; R10 es un átomo de hidrogeno, un grupo metilo o etilo; R11 es un átomo de halogeno, un átomo de hidrogeno, un grupo hidroxi, un grupo metoxi, un grupo OC(O)-R20, un grupo metilo o etilo; R12 es un átomo de hidrogeno, un grupo metilo o un grupo etilo; R13 es un átomo de hidrogeno, un grupo metilo, etilo, etinilo, trifluorometilo, pentafluoroetilo; R14 es un átomo de hidrogeno, un grupo OH o un átomo de oxígeno unido a través de un enlace doble; R15 es un grupo hidroxi, tri(alquil C1-6)sililoxi, alcoxi C1-5, un grupo OC(O)-R20 o un grupo heterocicloalquiloxi C2-5; en donde se puede hallar un enlace doble adicional en la posicion 4,5 y cuando Y es un átomo de carbono, se pueden hallar enlaces dobles adicionales en la posicion 1,2 o cuando el radical R14 es un átomo de hidrogeno o un grupo OH, en la posicion 2,3; y sus sales farmacéuticamente aceptables.Steroid prodrugs, pharmaceutical compositions, containing these compounds, as well as their use for the preparation of drugs with androgenic action. Claim 1: Steroid prodrugs of the general formula (1), characterized in that: n is a number 0-4; R1 is a radical -SO2NH2 or -NHSO2NH2; wherein R2, R3, and X, X1 are a hydrogen atom, a halogen atom, a nitrile group, a nitro group, a C1-5 alkyl group, a CpF2p + 1 group with p = 1-3, a group OC (O) -R20, COOR20, OR20, C (O) NHR20 or OC (O) NHR21, where R20, R21 and R22 are a C1-5 alkyl group, a C3-8 cycloalkyl group, an aryl group, a C 1-4 alkylenearyl group, a C 1-8 alkylene-C 3-8 cycloalkyl or C 3-8 cycloalkylene-C 1-4 alkyl group, as well as R 20 may also be a hydrogen; or R2 is a radical -SO2NH2 or -NHSO2NH2; wherein R2, R3, and X, X1 are a hydrogen atom, a halogen atom, a nitrile group, a nitro group, a C1-5 alkyl group, a CpF2p + 1 group with p = 1-3, a group OC (O) -R20, COOR20, OR20, C (O) NHR20 or OC (O) NHR21, where R20, R21 and R22 are a C1-5 alkyl group, a C3-8 cycloalkyl group, an aryl group, a C 1-4 alkylenearyl group, a C 1-8 alkylene-C 3-8 cycloalkyl or C 3-8 cycloalkylene-C 1-4 alkyl group, as well as R 20 may also be a hydrogen; or R3 is a radical -SO2NH2 or -NHSO2NH2; wherein R2, R3, and X, X1 are a hydrogen atom, a halogen atom, a nitrile group, a nitro group, a C1-5 alkyl group, a CpF2p + 1 group with p = 1-3, a group OC (O) -R20, COOR20, OR20, C (O) NHR20 or OC (O) NHR21, where R20, R21 and R22 are a C1-5 alkyl group, a C3-8 cycloalkyl group, an aryl group, a C1-4 alkylenearyl group, a C1-4 alkylene-C3-8 cycloalkyl or C3-8 cycloalkyl-C1-4 alkyl group, as well as R20 may also be a hydrogen; and STEROID is a cyclic steroid system according to general formulas (2) to (4), where: Y is an oxygen or carbon atom; R4 is a hydrogen atom, a halogen atom, a methyl, trifluoromethyl, hydroxy, tri (C1-6 alkyl) silyloxy, C1-5 alkoxy or C2-5 heterocycloalkyloxy group; R7 is a hydrogen atom, a methyl or ethyl group; R10 is a hydrogen atom, a methyl or ethyl group; R11 is a halogen atom, a hydrogen atom, a hydroxy group, a methoxy group, an OC (O) -R20 group, a methyl or ethyl group; R12 is a hydrogen atom, a methyl group or an ethyl group; R13 is a hydrogen atom, a methyl, ethyl, ethynyl, trifluoromethyl, pentafluoroethyl group; R14 is a hydrogen atom, an OH group or an oxygen atom attached through a double bond; R15 is a hydroxy, tri (C1-6 alkyl) silyloxy, C1-5 alkoxy, an OC (O) -R20 group or a C2-5 heterocycloalkyloxy group; where an additional double bond can be found at position 4.5 and when Y is a carbon atom, additional double bonds can be found at position 1.2 or when the radical R14 is a hydrogen atom or an OH group , in position 2,3; and its pharmaceutically acceptable salts.

ARP050102084A 2004-05-21 2005-05-20 STEROID PROPHARMS WITH ANDROGENIC ACTION AR049547A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102004025986A DE102004025986A1 (en) 2004-05-21 2004-05-21 Steroid prodrugs with androgenic effects

Publications (1)

Publication Number Publication Date
AR049547A1 true AR049547A1 (en) 2006-08-16

Family

ID=34968657

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050102084A AR049547A1 (en) 2004-05-21 2005-05-20 STEROID PROPHARMS WITH ANDROGENIC ACTION

Country Status (22)

Country Link
EP (1) EP1747229A1 (en)
JP (1) JP2007538026A (en)
CN (1) CN1993375A (en)
AR (1) AR049547A1 (en)
AU (1) AU2005245568A1 (en)
BR (1) BRPI0510136A (en)
CA (1) CA2564963A1 (en)
CR (1) CR8785A (en)
DE (1) DE102004025986A1 (en)
EA (1) EA200602049A1 (en)
EC (1) ECSP067028A (en)
GT (1) GT200500122A (en)
IL (1) IL179293A0 (en)
MX (1) MXPA06013469A (en)
NO (1) NO20065885L (en)
PA (1) PA8633601A1 (en)
PE (1) PE20060271A1 (en)
SV (1) SV2006002123A (en)
TW (1) TW200613317A (en)
UY (1) UY28911A1 (en)
WO (1) WO2005113575A1 (en)
ZA (1) ZA200610769B (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10027887A1 (en) 2000-05-31 2001-12-13 Jenapharm Gmbh Compounds with a sulfonamide group and pharmaceutical compositions containing these compounds
US7534780B2 (en) 2004-05-21 2009-05-19 Bayer Schering Pharma Aktiengesellschaft Estradiol prodrugs
DE102005057224A1 (en) * 2005-11-29 2007-05-31 Bayer Schering Pharma Ag New 9-alpha substituted estratriene derivatives esterified with a sulfamoylphenyl-substituted acid residue, are prodrugs useful as carboanhydrase inhibitors for treating estrogen deficiency disorders
DE102005057408A1 (en) * 2005-11-30 2007-05-31 Bayer Schering Pharma Ag New sulfamoylsulfonate prodrugs e.g. useful for protecting red blood cells from attack by parasites or for hormone replacement therapy, female fertility control or treating hormone-associated diseases
CN101708338B (en) * 2008-12-26 2014-06-04 中国人民解放军军事医学科学院放射与辐射医学研究所 Prodrug containing sterides structures and high dispersion preparation thereof
CN102964417A (en) * 2012-11-30 2013-03-13 华中药业股份有限公司 Synthetic method of 17-hydroxy tetrahydropyran ether steroid
CN107556258B (en) * 2017-08-22 2021-06-04 湖北江田精密化学有限公司 Preparation method of 4-amino-2-chloro-5 (1H-tetrazolyl-5) benzenesulfonamide
EP3533619A1 (en) * 2018-03-02 2019-09-04 Basf Se Heat sensitive recording material and color developer

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH545316A (en) * 1970-07-17 1973-12-15 Hoffmann La Roche Process for the preparation of acyl derivatives
US5001234A (en) * 1987-04-16 1991-03-19 The Upjohn Company Cyclic hydrocarbons with an aminoalkyl sidechain
US5571933A (en) * 1994-11-17 1996-11-05 Duquesne University Of The Holy Ghost Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their use
DE19712488A1 (en) * 1997-03-25 1998-10-01 Knoell Hans Forschung Ev Steroid sulfamates, processes for their preparation and use thereof
DE10027887A1 (en) * 2000-05-31 2001-12-13 Jenapharm Gmbh Compounds with a sulfonamide group and pharmaceutical compositions containing these compounds

Also Published As

Publication number Publication date
MXPA06013469A (en) 2007-01-23
WO2005113575A1 (en) 2005-12-01
TW200613317A (en) 2006-05-01
UY28911A1 (en) 2005-12-30
CA2564963A1 (en) 2005-12-01
ZA200610769B (en) 2008-08-27
PA8633601A1 (en) 2006-07-03
EA200602049A1 (en) 2007-06-29
JP2007538026A (en) 2007-12-27
NO20065885L (en) 2006-12-19
PE20060271A1 (en) 2006-05-25
DE102004025986A1 (en) 2005-12-15
EP1747229A1 (en) 2007-01-31
BRPI0510136A (en) 2007-10-02
CR8785A (en) 2007-02-05
IL179293A0 (en) 2007-03-08
CN1993375A (en) 2007-07-04
GT200500122A (en) 2006-01-24
AU2005245568A1 (en) 2005-12-01
ECSP067028A (en) 2006-12-29
SV2006002123A (en) 2006-02-15

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