HRP20171805T1 - Derivati 17-hidroksi-17-pentafluoroetil-estra-4,9(10)-dien-11-arila, postupci za njihovu proizvodnju i njihova upotreba za liječenje bolesti - Google Patents

Derivati 17-hidroksi-17-pentafluoroetil-estra-4,9(10)-dien-11-arila, postupci za njihovu proizvodnju i njihova upotreba za liječenje bolesti Download PDF

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HRP20171805T1
HRP20171805T1 HRP20171805TT HRP20171805T HRP20171805T1 HR P20171805 T1 HRP20171805 T1 HR P20171805T1 HR P20171805T T HRP20171805T T HR P20171805TT HR P20171805 T HRP20171805 T HR P20171805T HR P20171805 T1 HRP20171805 T1 HR P20171805T1
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compound according
estra
dien
hydroxy
pentafluoroethyl
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Wolfgang Schwede
Ulrich Klar
Carsten Moeller
Andrea Rotgeri
Wilhelm Bone
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Bayer Intellectual Property Gmbh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • A61K31/567Compounds 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
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    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds 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
    • A61K31/573Compounds 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
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • 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
    • 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
    • A61P5/36Antigestagens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • 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
    • C07J41/0077Normal 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
    • C07J41/0083Normal 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

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  • Diabetes (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Claims (33)

1. Spoj s formulom I [image] naznačen time da R1predstavlja ili ostatak Y ili predstavlja fenilni prsten supstituiran jednom ili dva puta s ostatkom Y, Y je odabran iz skupine koja sadrži SR2, S(O)R3, S(O)2R3, S(O)(NH)R3, S(O)(NR4)R3, S(O)2NR9R10, R2predstavlja vodik, C1-C6-alkil, C7-C10-aralkil ili aril, R3predstavlja C1-C6-alkil ili aril, R4predstavlja skupinu S(O)2R6, R6 predstavlja fenil ili 4-metilfenil X označava kisikov atom, NOR7 ili NNHSO2R7, R7je odabran iz skupine koja sadrži vodik, C1-C10-alkil, aril R9, R10su neovisno jedan od drugoga odabrani iz skupine koja sadrži vodik, C1-C10-alkil ili aril ili alternativno predstavljaju, zajedno s dušikovim atomom, 3- do 8-člani, zasićeni ili nezasićeni heterociklički prsten, i njihovi odvojeni stereoizomeri, njihove soli, solvati ili solvati soli, uključujući sve kristalne modifikacije.
2. Spoj prema zahtjevu 1, naznačen time da R1predstavlja ili ostatak Y ili fenilni prsten supstituiran jednom s ostatkom Y, Y je odabran iz skupine koja sadrži SR2, S(O)R3, S(O)2R3, S(O)(NH)R3, S(O)(NR4)R3, S(O)2NR9R10 i R2predstavlja vodik ili C1-C6-alkil, R3predstavlja C1-C6-alkil i X predstavlja kisikov atom, R6predstavlja fenil ili 4-metilfenil i R9, R10neovisno jedan od drugoga predstavljaju vodik ili C1-C6-alkil ili fenil i njihovi odvojeni stereoizomeri, njihove soli, solvati ili solvati soli.
3. Spoj prema zahtjevu 1, naznačen time da R1predstavlja S(O)2R3i X predstavlja O.
4. Spoj prema zahtjevu 3, naznačen time da R3predstavlja C1-C6-alkil.
5. Spoj prema zahtjevu 1, naznačen time da R1predstavlja S(O)(NH)R3i X predstavlja O i njihovi odvojeni stereoizomeri.
6. Spoj prema zahtjevu 5, naznačen time da R3predstavlja C1-C6-alkil i njihovi odvojeni stereoizomeri.
7. Spoj prema zahtjevu 6, naznačen time da R3predstavlja metil i njihovi odvojeni stereoizomeri.
8. Spoj prema zahtjevu 1, naznačen time da R1predstavlja SOR3 i X predstavlja O i njihovi odvojeni stereoizomeri.
9. Spoj prema zahtjevu 8, naznačen time da R3predstavlja C1-C6-alkil i njihovi odvojeni stereoizomeri.
10. Spoj prema zahtjevu 9, naznačen time da R3predstavlja metil i njihovi odvojeni stereoizomeri.
11. Spoj prema zahtjevu 1, naznačen time da R1predstavlja SR2 i X predstavlja O.
12. Spoj prema zahtjevu 11, naznačen time da R2predstavlja vodik.
13. Spoj prema zahtjevu 11, naznačen time da R2predstavlja C1-C6-alkil.
14. Spoj prema zahtjevu 13, naznačen time da R2predstavlja metil.
15. Spoj prema zahtjevu 11, naznačen time da R2predstavlja aril.
16. Spoj prema zahtjevu 15, naznačen time da R2predstavlja fenil.
17. Spoj prema zahtjevu 11, naznačen time da R2predstavlja C7-C10-aralkil.
18. Spoj prema zahtjevu 17, naznačen time da R2predstavlja benzil.
19. Spojevi prema zahtjevu 2, naznačeni time da R2predstavlja metil, etil ili vodik.
20. Spojevi prema zahtjevu 1, naznačeni time da R3predstavlja C1-C6-alkil.
21. Spojevi prema zahtjevu 4, naznačeni time da R3predstavlja metil ili etil.
22. Spojevi prema zahtjevu 1, naznačeni time da R6predstavlja fenil.
23. Spojevi prema zahtjevu 1, naznačeni time da X je kisikov atom.
24. Spojevi prema zahtjevu 1, naznačeni time da Y predstavlja SR2ili S(O)2R3ili S(O)(NH)R3 gdje je R2jednak vodiku, metilu ili etilu i R3je jednak metilu ili etilu.
25. Spojevi prema zahtjevu 1, naznačeni time da Y predstavlja S(O)2R3.
26. Spojevi prema zahtjevu 1 naznačeni time da su (11β,17β)-17-hidroksi-11-[4-(metilsulfanil)fenil]-17-(pentafluoroetil)estra-4,9-dien-3-on; (11β,17β)-11-[4-(etilsulfanil)fenil]-17-hidroksi-17-(pentafluoroetil)estra-4,9-dien-3-on; (11β,17β)-17-hidroksi-11-{4-[(RS)-metilsulfinil]fenil}-17-(pentafluoroetil)estra-4,9-dien-3-on; (11β,17β)-11-[4-(etilsulfonil)fenil]-17-hidroksi-17-(pentafluoroetil)estra-4,9-dien-3-on; (11β,17β)-11-[4-(benzilsulfanil)fenil]-17-hidroksi-17-(pentafluoroetil)estra-4,9-dien-3-on; N-[{4-[(11β,17β)-17-hidroksi-3-okso-17-(pentafluoroetil)estra-4,9-dien-11-il]fenil}(RS)(metil)oksido-λ6-sulfaniliden]-4-metilbenzen sulfonamid; (11β,17β)-17-hidroksi-11-[4-(RS-metilsulfonimidoil)fenil]-17-(pentafluoroetil)estra-4,9-dien-3-on; (11β,17β)-17-hidroksi-11-[4'-(metilsulfanil)bifenil-4-il]-17-(pentafluoroetil)estra-4,9-dien-3-on; (11β,17β)-17-hidroksi-11-[4'-(metilsulfonil)bifenil-4-il]-17-(pentafluoroetil)estra-4,9-dien-3-on; N-[{4'-[(11β,17β)-17-hidroksi-3-okso-17-(pentafluoroetil)estra-4,9-dien-11-il]bifenil-4-il}(RS)(metil)oksido-λ6-sulfaniliden]-4-metilbenzen sulfonamid; (11β,17β)-17-hidroksi-11-[4'-(RS-metilsulfonimidoil)bifenil-4-il]-17-(pentafluoroetil)estra-4,9-dien-3-on; (11β,17β)-17-hidroksi-17-(pentafluoroetil)-11-(4'-sulfanilbifenil-4-il)estra-4,9-dien-3-on; 4'-[(11β,17β))-17-hidroksi-3-okso-17-(pentafluoroetil)estra-4,9-dien-11-il]-N,N-dimetilbifenil-4-sulfonamid; 4-[(11β,17β)-17-hidroksi-3-okso-17-(pentafluoroetil)estra-4,9-dien-11-il]-N,N-dimetilbenzen sulfonamid
27. Spoj prema jednom od prethodnih zahtjeva, naznačena time da je za liječenje i sprječavanje bolesti.
28. Spoj prema jednom od zahtjeva 1-26, naznačena time da je za liječenje i sprječavanje mioma maternice, endometrioze, teškog menstrualnog krvarenja, meningioma, karcinoma dojke ovisnih o hormonima i pritužbi povezanih s menopauzom ili za kontrolu plodnosti i kontracepciju u hitnim slučajevima.
29. Uporaba spoja prema jednom od zahtjeva 1-26, naznačena time da je za proizvodnju medicinskog proizvoda za liječenje i/ili sprječavanje bolesti.
30. Uporaba spoja prema jednom od zahtjeva 1-26, naznačena time da je za proizvodnju medicinskog proizvoda za liječenje i/ili sprječavanje mioma maternice, endometrioze, teškog menstrualnog krvarenja, meningioma, karcinoma dojke ovisnih o hormonima i pritužbi povezanih s menopauzom ili za kontrolu plodnosti i kontracepciju u hitnim slučajevima.
31. Medicinski proizvod naznačen time da sadrži spoj kako je definiran u jednom od zahtjeva 1-26, u kombinaciji s drugom aktivnom tvari.
32. Medicinski proizvod naznačen time da sadrži spoj kako je definiran u jednom od zahtjeva 1-26, u kombinaciji s inertnim, ne-toksičnim, farmaceutski prihvatljivim pomoćnim sredstvom.
33. Medicinski proizvod prema zahtjevima 31 ili 32 naznačen time da je za liječenje i/ili sprječavanje mioma maternice, endometrioze, teškog menstrualnog krvarenja, meningioma, karcinoma dojke ovisnih o hormonima i pritužbi povezanih s menopauzom ili za kontrolu plodnosti i kontracepciju u hitnim slučajevima.
HRP20171805TT 2009-07-20 2017-11-21 Derivati 17-hidroksi-17-pentafluoroetil-estra-4,9(10)-dien-11-arila, postupci za njihovu proizvodnju i njihova upotreba za liječenje bolesti HRP20171805T1 (hr)

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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
EP12194455.7A EP2623510B1 (de) 2009-07-20 2010-07-07 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-derivate, verfahren zu ihrer herstellung und ihre verwendung zur behandlung von krankheiten

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HRP20171805T1 true HRP20171805T1 (hr) 2017-12-29

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HRP20130558AT HRP20130558T1 (hr) 2009-07-20 2013-06-18 Derivat 17-hidroksi-17-pentafluoretil-estra-4,9(10)-dien-11-arila, postupci za njegovu proizvodnju i njegova uporaba za lijeäśenje bolesti
HRP20171805TT HRP20171805T1 (hr) 2009-07-20 2017-11-21 Derivati 17-hidroksi-17-pentafluoroetil-estra-4,9(10)-dien-11-arila, postupci za njihovu proizvodnju i njihova upotreba za liječenje bolesti
HRP20191049TT HRP20191049T1 (hr) 2009-07-20 2019-06-12 (11beta, 17beta)-17-hidroksi-11-[4-(metilsulfonil)fenil]-17-(pentalfuorometil)estra-4,9-dien-3-on za uporabu za liječenje bolesti

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HRP20130558AT HRP20130558T1 (hr) 2009-07-20 2013-06-18 Derivat 17-hidroksi-17-pentafluoretil-estra-4,9(10)-dien-11-arila, postupci za njegovu proizvodnju i njegova uporaba za lijeäśenje bolesti

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HRP20191049TT HRP20191049T1 (hr) 2009-07-20 2019-06-12 (11beta, 17beta)-17-hidroksi-11-[4-(metilsulfonil)fenil]-17-(pentalfuorometil)estra-4,9-dien-3-on za uporabu za liječenje bolesti

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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
DE102009034366A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-methylenoxyalkylenaryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102009034362A1 (de) * 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102009034368A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-acyloxyalkylenphenyl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
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