AR050335A1 - ESTRADIOL PRODUCTS, PHARMACEUTICAL COMPOSITION BASED ON THE COMPOUND AND PREPARATION PROCEDURE FOR THIS - Google Patents

ESTRADIOL PRODUCTS, PHARMACEUTICAL COMPOSITION BASED ON THE COMPOUND AND PREPARATION PROCEDURE FOR THIS

Info

Publication number
AR050335A1
AR050335A1 ARP050102083A ARP050102083A AR050335A1 AR 050335 A1 AR050335 A1 AR 050335A1 AR P050102083 A ARP050102083 A AR P050102083A AR P050102083 A ARP050102083 A AR P050102083A AR 050335 A1 AR050335 A1 AR 050335A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
atom
cycloalkyl
halogen atom
Prior art date
Application number
ARP050102083A
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=34969196&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR050335(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 AR050335A1 publication Critical patent/AR050335A1/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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P15/18—Feminine contraceptives
    • 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
    • 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
    • A61P5/30—Oestrogens

Landscapes

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

Abstract

Prodrogas de estradiol de la formula general (1), un procedimiento para su preparacion, composiciones farmacéuticas que contienen estos compuestos y su uso para preparar medicamentos con efecto estrogeno. Reivindicacion 1: Prodrogas de estradiol de la formula general (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 H, 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 H, o R2 es un radical -SO2NH2 o -NHSO2NH2, donde R2, R3 y X, X1 es un átomo de H, 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 H o R3 es un radical -SO2NH2 o -NHSO2NH2; donde R2, R3 y X, X1 es un átomo de H, 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, u 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 H, y esteroide es un sistema de anillo ABCD esteroide de las formulas generales parciales (2)-(3), donde R5, R6, R8 son, cada uno, un átomo de H y R7 es un átomo de H, un grupo metilo o etilo o R5+R6, R7+R8 o R6+R7 son juntos, una union doble; R9 es un átomo de H, un átomo de halogeno, un grupo hidroxi, un grupo metoxi, un grupo OC(O)-R20, un grupo metilo o un grupo etilo; R10 es un grupo hidroxi, un grupo metoxi, un grupo tri(alquil C1-6)sililoxi, un grupo OC(O)-R20, un grupo heterocicloalquiloxi C2-5 o un grupo Z; R11 es un átomo de H o de halogeno; R12 es un grupo hidroxi, un grupo metoxi, un grupo tri(alquilo C1-6)sililoxi, un grupo OC(O)-R20, un grupo heterocicloalquiloxi C2-5 o un grupo Z; R14 es átomo de H, un grupo metilo, o un grupo etilo; R15 es átomo de H, un grupo hidroxi, un grupo metoxi, un grupo etoxi, un grupo tri(alquilo C1-6)sililoxi, un grupo OC(O)-R20 o un grupo heterocicloalquiloxi C2-5, y sus sales farmacéuticamente aceptables.Prodiges of estradiol of the general formula (1), a process for its preparation, pharmaceutical compositions containing these compounds and their use for preparing drugs with estrogen effect. Claim 1: Estradiol prodrugs of the general 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 an H atom, a halogen atom, a nitrile group, a nitro group, a C1-5 alkyl group, a CpF2p + 1 group, with p = 1-3, an OC group (O) -R20, COOR20, OR20, C (O) NHR20 or OC (O) NH-R21; 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 and R20 alkyl may also be an H, or R2 is a radical -SO2NH2 or -NHSO2NH2, where R2, R3 and X, X1 is an H atom, a halogen atom, a nitrile group, a group nitro, a C1-5 alkyl group, 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 an H or R3 is a radical -SO2NH2 or -NHSO2NH2; where R2, R3 and X, X1 is an H atom, a halogen atom, a nitrile group, a nitro group, a C1-5 alkyl group, a CpF2p + 1 group with p = 1-3, an OC group ( O) -R20, COOR20, OR20, C (O) NHR20 or OC (O) NH-R21; wherein R20, R21 and R22 are a C1-5 alkyl group, a C3-8 cycloalkyl group, or 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 an H, and steroid is a steroid ABCD ring system of the partial general formulas (2) - (3), where R5, R6, R8 are each a H and R7 atom is an H atom, a methyl or ethyl group or R5 + R6, R7 + R8 or R6 + R7 are together, a double bond; R9 is an H atom, a halogen atom, a hydroxy group, a methoxy group, an OC (O) -R20 group, a methyl group or an ethyl group; R10 is a hydroxy group, a methoxy group, a tri (C1-6 alkyl) silyloxy group, an OC (O) -R20 group, a C2-5 heterocycloalkyloxy group or a Z group; R11 is an H or halogen atom; R12 is a hydroxy group, a methoxy group, a tri (C1-6 alkyl) silyloxy group, an OC (O) -R20 group, a C2-5 heterocycloalkyloxy group or a Z group; R14 is an atom of H, a methyl group, or an ethyl group; R15 is an H atom, a hydroxy group, a methoxy group, an ethoxy group, a tri (C1-6 alkyl) silyloxy group, an OC (O) -R20 group or a C2-5 heterocycloalkyloxy group, and their pharmaceutically acceptable salts .

ARP050102083A 2004-05-21 2005-05-20 ESTRADIOL PRODUCTS, PHARMACEUTICAL COMPOSITION BASED ON THE COMPOUND AND PREPARATION PROCEDURE FOR THIS AR050335A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102004025966A DE102004025966A1 (en) 2004-05-21 2004-05-21 Estradiol prodrugs

Publications (1)

Publication Number Publication Date
AR050335A1 true AR050335A1 (en) 2006-10-18

Family

ID=34969196

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050102083A AR050335A1 (en) 2004-05-21 2005-05-20 ESTRADIOL PRODUCTS, PHARMACEUTICAL COMPOSITION BASED ON THE COMPOUND AND PREPARATION PROCEDURE FOR THIS

Country Status (11)

Country Link
EP (1) EP1747230A1 (en)
JP (1) JP2007538025A (en)
AR (1) AR050335A1 (en)
DE (1) DE102004025966A1 (en)
GT (1) GT200500121A (en)
PA (1) PA8633701A1 (en)
PE (1) PE20060359A1 (en)
SV (1) SV2006002121A (en)
TW (1) TW200613315A (en)
UY (1) UY28909A1 (en)
WO (1) WO2005113574A1 (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
DE102004025985A1 (en) * 2004-05-21 2005-12-15 Schering Ag Estriol and estetrol prodrugs
US7534780B2 (en) 2004-05-21 2009-05-19 Bayer Schering Pharma Aktiengesellschaft Estradiol prodrugs
DE102005057225A1 (en) * 2005-11-29 2007-05-31 Bayer Schering Pharma Ag New 8-beta-substituted estratriene derivatives esterified with a sulfamoylphenyl-substituted acid residue, are prodrugs useful as carboanhydrase inhibitors for treating estrogen deficiency disorders
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
CN105636592A (en) * 2013-07-11 2016-06-01 伊万斯彻有限公司 Pro-drug forming compounds
CN115368427B (en) * 2022-08-17 2024-02-13 南宁师范大学 Estradiol selenocyanate compound and preparation method and application thereof

Family Cites Families (11)

* 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
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
JPWO2001081364A1 (en) * 2000-04-24 2004-01-08 協和醗酵工業株式会社 Estra-1,3,5 (10) -triene derivative
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
DE102004025985A1 (en) * 2004-05-21 2005-12-15 Schering Ag Estriol and estetrol prodrugs

Also Published As

Publication number Publication date
UY28909A1 (en) 2005-12-30
GT200500121A (en) 2006-01-30
PA8633701A1 (en) 2006-07-03
WO2005113574A1 (en) 2005-12-01
SV2006002121A (en) 2006-02-15
EP1747230A1 (en) 2007-01-31
JP2007538025A (en) 2007-12-27
DE102004025966A1 (en) 2005-12-15
TW200613315A (en) 2006-05-01
PE20060359A1 (en) 2006-05-25

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