AR049108A1 - PHENYL ESTERES AMINOSULFONIL OR AMINOSULFONILAMINO SUBSTITUTED AS PRODUCTS OF ESTRIOL OR STEROL - Google Patents

PHENYL ESTERES AMINOSULFONIL OR AMINOSULFONILAMINO SUBSTITUTED AS PRODUCTS OF ESTRIOL OR STEROL

Info

Publication number
AR049108A1
AR049108A1 ARP050102085A ARP050102085A AR049108A1 AR 049108 A1 AR049108 A1 AR 049108A1 AR P050102085 A ARP050102085 A AR P050102085A AR P050102085 A ARP050102085 A AR P050102085A AR 049108 A1 AR049108 A1 AR 049108A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
cycloalkyl
hydrogen
hydrogen atom
Prior art date
Application number
ARP050102085A
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34969311&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR049108(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Ag filed Critical Schering Ag
Publication of AR049108A1 publication Critical patent/AR049108A1/en

Links

Classifications

    • 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
    • C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P5/26—Androgens
    • 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
    • A61P5/30—Oestrogens
    • 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
    • A61P5/34—Gestagens

Abstract

Se refiere a procedimiento para su preparacion, composiciones farmacéuticas que contienen estos compuestos y su uso para preparar medicamentos con efecto estrogeno. Reivindicacion 1: Prodrogas de estriol y esterol de la formula (1), caracterizadas porque: n es un numero de 0 a 4; R1 es un radical -SO2NH2 o -NHSO2NH2, donde R2, R3, y X, X1 es 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 o OC(O)NH-R21, 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 alquileno-C1-4-cicloalquilo-C3-8 o cicloalquileno-C3-8-alquilo-C1-4; y R20 puede ser además, un hidrogeno, o R2 es un radical -SO2NH2 o -NHSO2NH2, donde R2, R3, y X, X1 es 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 o OC(O)NH-R21, 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 alquileno-C1-4-cicloalquilo-C3-8 o cicloalquileno-C3-8-alquilo-C1-4; y R20 puede ser, además, un hidrogeno; o R3 es un radical -SO2NH2 o -NHSO2NH2, donde R2, R3, y X, X1 es 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 o OC(O)NH-R21, 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 alquileno-C1-4-cicloalquilo-C3-8 o cicloalquileno-C3-8-alquilo-C1-4; y R20 puede ser, además, un hidrogeno; y Esteroide es un sistema de anillo ABCD esteroide de las formulas generales parciales (2) a (5), donde, R4, R16, R17 pueden ser un grupo hidroxi, un grupo tri(alquil-C1-6)sililoxi, un grupo OC(O)-R20; un grupo heterocicloalquiloxi-2-5 o un grupo Y; y R15 puede ser un átomo de hidrogeno, un grupo hidroxi, un grupo tri(alquil-C1-6)sililoxi, un grupo OC(O)-R20, un grupo heterocicloalquiloxi-C2-5 o un grupo Y; y sus sales farmacéuticamente aceptables.It refers to the process for its preparation, pharmaceutical compositions containing these compounds and their use to prepare drugs with estrogen effect. Claim 1: Estriol and sterol prodrugs of the formula (1), characterized in that: n is a number from 0 to 4; R1 is a radical -SO2NH2 or -NHSO2NH2, where R2, R3, and X, X1 is a hydrogen atom, a halogen atom, a nitrile group, a nitro group, a C1-5 alkyl group, a CpF2p + group 1, with p = 1-3, an OC (O) -R20, COOR20, OR20, C (O) NHR20 or OC (O) NH-R21 group, where R20, R21 and R22 are a C1-5 alkyl group , a C 3-8 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; and R20 may also be a hydrogen, or R2 is a radical -SO2NH2 or -NHSO2NH2, where R2, R3, and X, X1 is a hydrogen atom, a halogen atom, a nitrile group, a nitro group, a group C1-5 alkyl, a CpF2p + 1 group, with p = 1-3, an OC (O) -R20, COOR20, OR20, C (O) NHR20 or OC (O) NH-R21 group, 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 cycloalkylene group -C1-4 alkyl; and R20 may also be a hydrogen; or R3 is a radical -SO2NH2 or -NHSO2NH2, where R2, R3, and X, X1 is a hydrogen atom, a halogen atom, a nitrile group, a nitro group, a C1-5 alkyl group, a CpF2p group +1, with p = 1-3, an OC (O) -R20, COOR20, OR20, C (O) NHR20 or OC (O) NH-R21 group, where R20, R21 and R22 are a C1-alkyl group 5, a C 3-8 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; and R20 may also be a hydrogen; and Steroid is a steroid ABCD ring system of partial general formulas (2) to (5), where, R4, R16, R17 can be a hydroxy group, a tri (C1-6 alkyl) silyloxy group, an OC group (O) -R20; a heterocycloalkyloxy-2-5 group or a Y group; and R15 may be a hydrogen atom, a hydroxy group, a tri (C1-6 alkyl) silyloxy group, an OC (O) -R20 group, a heterocycloalkyloxy-C2-5 group or a Y group; and its pharmaceutically acceptable salts.

ARP050102085A 2004-05-21 2005-05-20 PHENYL ESTERES AMINOSULFONIL OR AMINOSULFONILAMINO SUBSTITUTED AS PRODUCTS OF ESTRIOL OR STEROL AR049108A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102004025985A DE102004025985A1 (en) 2004-05-21 2004-05-21 Estriol and estetrol prodrugs

Publications (1)

Publication Number Publication Date
AR049108A1 true AR049108A1 (en) 2006-06-28

Family

ID=34969311

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050102085A AR049108A1 (en) 2004-05-21 2005-05-20 PHENYL ESTERES AMINOSULFONIL OR AMINOSULFONILAMINO SUBSTITUTED AS PRODUCTS OF ESTRIOL OR STEROL

Country Status (11)

Country Link
EP (1) EP1747231A1 (en)
JP (1) JP2007538027A (en)
AR (1) AR049108A1 (en)
DE (1) DE102004025985A1 (en)
GT (1) GT200500120A (en)
PA (1) PA8633801A1 (en)
PE (1) PE20060314A1 (en)
SV (1) SV2006002122A (en)
TW (1) TW200612962A (en)
UY (1) UY28910A1 (en)
WO (1) WO2005113576A1 (en)

Families Citing this family (7)

* 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
DE102004025966A1 (en) * 2004-05-21 2005-12-15 Schering Ag 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
CN100396693C (en) * 2006-11-08 2008-06-25 浙江大学 Preparation method of 1,4-dipregnene-16-beta-methyl-17-alpha-21-bihydroxy object
CN102079771B (en) * 2010-12-10 2012-10-03 郑州大学 Estrogen amino-acid ester compound with antitumor activity as well as synthetic method thereof

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1238739A (en) * 1958-08-04 1960-08-19 Chimiotherapie Lab Franc Process for the preparation of water-soluble testosterone derivatives
FR8290M (en) * 1968-12-31 1970-11-09 Rech Chimiques Et Ind Mar Lab
US5001234A (en) * 1987-04-16 1991-03-19 The Upjohn Company Cyclic hydrocarbons with an aminoalkyl sidechain
US5116828A (en) * 1989-10-26 1992-05-26 Nippon Zoki Pharmaceutical Co., Ltd. Pharmaceutical composition for treatment of osteoporosis
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
US6953785B2 (en) * 2000-04-24 2005-10-11 Kyowa Hakko Kogyo Co., Ltd. Estra-1,3,5(10)-triene derivatives
DE10027887A1 (en) * 2000-05-31 2001-12-13 Jenapharm Gmbh Compounds with a sulfonamide group and pharmaceutical compositions containing these compounds
GB0015876D0 (en) * 2000-06-28 2000-08-23 Novartis Ag Organic compounds
GB0316290D0 (en) * 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
TWI331154B (en) * 2003-11-12 2010-10-01 Solvay Pharm Gmbh Novel 17-hydroxysteroid dehydrogenase type i inhibitors
DE102004025966A1 (en) * 2004-05-21 2005-12-15 Schering Ag Estradiol prodrugs

Also Published As

Publication number Publication date
WO2005113576A1 (en) 2005-12-01
SV2006002122A (en) 2006-05-09
PE20060314A1 (en) 2006-05-25
EP1747231A1 (en) 2007-01-31
TW200612962A (en) 2006-05-01
PA8633801A1 (en) 2006-03-24
DE102004025985A1 (en) 2005-12-15
UY28910A1 (en) 2005-12-30
JP2007538027A (en) 2007-12-27
GT200500120A (en) 2006-01-24

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