PE20170084A1 - Derivados de 17-hidroxi-17-pentafluoroetil-estra-4-9(10)-dien-11-arilo como antagonistas de progesterona y procedimientos para su preparacion - Google Patents

Derivados de 17-hidroxi-17-pentafluoroetil-estra-4-9(10)-dien-11-arilo como antagonistas de progesterona y procedimientos para su preparacion

Info

Publication number
PE20170084A1
PE20170084A1 PE2016002208A PE2016002208A PE20170084A1 PE 20170084 A1 PE20170084 A1 PE 20170084A1 PE 2016002208 A PE2016002208 A PE 2016002208A PE 2016002208 A PE2016002208 A PE 2016002208A PE 20170084 A1 PE20170084 A1 PE 20170084A1
Authority
PE
Peru
Prior art keywords
estra
pentafluoroethyl
hydroxy
dien
aryl
Prior art date
Application number
PE2016002208A
Other languages
English (en)
Inventor
Wilhelm Bone
Andrea Rotgeri
Wolfgang Schwede
Ulrich Klar
Carsten Moller
Original Assignee
Bayer Ip Gmbh
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=43383964&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20170084(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Ip Gmbh filed Critical Bayer Ip Gmbh
Publication of PE20170084A1 publication Critical patent/PE20170084A1/es

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • 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
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P5/36—Antigestagens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • 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
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings

Abstract

La presente invencion se refiere a derivados de 17-hidroxi-17-pentafluoroetil-estra-4,9(10)-dien-11-arilo de formula (I), sus estereoisomeros, sales, solvatos, solvatos de las sales, en donde: R1 es un radical Y o un anillo fenilo mono- o disustituido con Y; Y es SR2, S(O)R3, entre otros; R2 es H, alquilo C1-C6, entre otros; R3 es alquilo C1-C6 o arilo; X es O, NRO7 o NNHSO2R7; R7 es H, alquilo C1-C10 o arilo. Son compuestos preferidos: (11?, 17?)-17-hidroxi-11-[4-(metilsulfanil)fenil]-17-(pentafluoroetil)estra-4,9-dien-3-ona; (11?, 17?)-11-[4-(etilsulfanil)fenil]-17-hidroxi-17-(pentafluoroetil)estra-4,9-dien-3-ona; entre otros. Estos compuestos tienen accion antagonista de progesterona siendo utiles en el tratamiento o prevencion de fibroides uterinos, endometriosis, entre otros
PE2016002208A 2009-07-20 2010-07-07 Derivados de 17-hidroxi-17-pentafluoroetil-estra-4-9(10)-dien-11-arilo como antagonistas de progesterona y procedimientos para su preparacion PE20170084A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102009034362A DE102009034362A1 (de) 2009-07-20 2009-07-20 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten

Publications (1)

Publication Number Publication Date
PE20170084A1 true PE20170084A1 (es) 2017-03-30

Family

ID=43383964

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2012000076A PE20121085A1 (es) 2009-07-20 2010-07-07 Derivados de 17-hidroxi-17-pentafluoroetil-estra-4,9 (10)-dien-11-arilo, procedimientos para su preparacion y su uso para el tratamiento de enfermedades
PE2016002208A PE20170084A1 (es) 2009-07-20 2010-07-07 Derivados de 17-hidroxi-17-pentafluoroetil-estra-4-9(10)-dien-11-arilo como antagonistas de progesterona y procedimientos para su preparacion

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2012000076A PE20121085A1 (es) 2009-07-20 2010-07-07 Derivados de 17-hidroxi-17-pentafluoroetil-estra-4,9 (10)-dien-11-arilo, procedimientos para su preparacion y su uso para el tratamiento de enfermedades

Country Status (48)

Country Link
US (4) US20120149670A1 (es)
EP (4) EP3252069B1 (es)
JP (3) JP5795312B2 (es)
KR (2) KR101687853B1 (es)
CN (1) CN102482317B (es)
AR (1) AR077491A1 (es)
AU (1) AU2010275849B2 (es)
BR (1) BR112012001344B8 (es)
CA (1) CA2768407C (es)
CL (1) CL2012000166A1 (es)
CO (1) CO6491067A2 (es)
CR (2) CR20170091A (es)
CU (1) CU20120012A7 (es)
CY (3) CY1114260T1 (es)
DE (1) DE102009034362A1 (es)
DK (3) DK2623510T3 (es)
DO (2) DOP2012000015A (es)
EA (2) EA021946B1 (es)
EC (2) ECSP12011616A (es)
ES (3) ES2648292T3 (es)
GT (1) GT201200012A (es)
HK (1) HK1171456A1 (es)
HN (1) HN2012000137A (es)
HR (3) HRP20130558T1 (es)
HU (2) HUE043757T2 (es)
IL (1) IL216967B (es)
IN (1) IN2012DN00598A (es)
JO (2) JO3009B1 (es)
LT (2) LT3252069T (es)
MA (1) MA33445B1 (es)
ME (2) ME03400B (es)
MX (2) MX2012000930A (es)
MY (1) MY179447A (es)
NO (1) NO2623510T3 (es)
NZ (2) NZ623417A (es)
PE (2) PE20121085A1 (es)
PL (3) PL2432798T3 (es)
PT (3) PT2623510T (es)
RS (1) RS52811B (es)
SG (3) SG177519A1 (es)
SI (3) SI2623510T1 (es)
TN (1) TN2012000028A1 (es)
TR (1) TR201908600T4 (es)
TW (1) TWI505830B (es)
UA (1) UA106502C2 (es)
UY (1) UY32791A (es)
WO (1) WO2011009531A2 (es)
ZA (1) ZA201201222B (es)

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DE102009034367A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-benzyliden-Derivate, Verfahren zu deren Herstellung und deren Verwendung zur Behandlung von Krankheiten
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KR101687853B1 (ko) 2016-12-19
UA106502C2 (uk) 2014-09-10
WO2011009531A3 (de) 2011-04-28
PL2432798T3 (pl) 2013-08-30
RS52811B (en) 2013-10-31
MX2012000930A (es) 2012-03-26
HUE043757T2 (hu) 2019-09-30
HRP20171805T1 (hr) 2017-12-29
JP2017105813A (ja) 2017-06-15
US20120094969A1 (en) 2012-04-19
ES2416461T3 (es) 2013-08-01
IN2012DN00598A (es) 2015-06-12
ES2648292T3 (es) 2017-12-29
SG10201811830PA (en) 2019-02-27
LT2623510T (lt) 2017-12-11
EP2432798B1 (de) 2013-04-03
ZA201201222B (en) 2022-11-30
MY179447A (en) 2020-11-06
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