BG103603A - Антигестагенни стероиди с флуорирана 17 алфа-алкилова верига - Google Patents

Антигестагенни стероиди с флуорирана 17 алфа-алкилова верига

Info

Publication number
BG103603A
BG103603A BG103603A BG10360399A BG103603A BG 103603 A BG103603 A BG 103603A BG 103603 A BG103603 A BG 103603A BG 10360399 A BG10360399 A BG 10360399A BG 103603 A BG103603 A BG 103603A
Authority
BG
Bulgaria
Prior art keywords
hydrogen
residue
group
alkyl group
antigestagene
Prior art date
Application number
BG103603A
Other languages
English (en)
Other versions
BG63875B1 (bg
Inventor
Wolfgang Schwede
Arwed Cleve
Ulrich Klar
Guenter Neef
Kristof Chwalisz
Martin Schneider
Ulrike Fuhrmann
Holger Hess-Stumpp
Original Assignee
Schering Aktiengesellschaft
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.)
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Publication date
Application filed by Schering Aktiengesellschaft filed Critical Schering Aktiengesellschaft
Publication of BG103603A publication Critical patent/BG103603A/bg
Publication of BG63875B1 publication Critical patent/BG63875B1/bg

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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
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003Androstane derivatives
    • C07J1/0033Androstane derivatives substituted in position 17 alfa and 17 beta
    • 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
    • A61P15/04Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
    • 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
    • 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
    • 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
    • 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
    • C07J41/0094Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J53/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • C07J53/002Carbocyclic rings fused

Landscapes

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

Abstract

Съединенията имат силна антигестагенна активност и са подходящи за приготвяне на фармацевтични състави. 17 -флуороалкилстероидите са с обща формула@@в която R1 означава метилова или етилова група, R2означава остатък с формула СnFmHo, където n е 2, 3, 4, 5 или 6, m > 1 и m + o = 2n + 1, R3 означавасвободна, етерифицирана или естерифицирана хидроксигрупа, R4 и R5 са водороден атом или заедно означават допълнителна връзка или метиленова група, Stпредставлява стероидна АВС-пръстенна система на отделните формули А, В и С@@в които R6 означава водород С1-С4- с права верига или С3-С4 алкилова група с разклонена верига, или халогенен атом, R7 означава водород С1-С4- с права верига или С3-С4 алкилова група с разклонена верига, или когато St означава А или В стероидна АВС-пръстенна система, освен това R6 и R7 заедно образуват допълнителна връзка, Х означава кислороден атом, хидроксииминогрупа =N OH или два водородни атома, R8 означава остатъкY или арилов остатък, в даден случай многократнозаместен с групата Y, където Y означава водород, халогенен атом, -ОН, -NO2, -N3, -CN, -NR9aR9b, -NHSO2R9, -CO2R9, C1-C10 алкилова, С1-С10 алкокси-, С1-С10 алканоилокси-, бензоилокси, С1-С10 алканоилова, С1-С10 хидроксиалкилова или бензоилова група и R9a и R9b са еднакви или различни и като R9 означават водород или С1-С10 алкилова група. Изобретението се отнася и до физиологично поносими соли на тези стероиди с киселини, когато съдържат остатъка NR9aR9b, и до техни физиологични соли с осно
BG103603A 1997-02-07 1999-07-26 Антигестагенни стероиди с флуорирана 17 алфа-алкилова верига BG63875B1 (bg)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19706061A DE19706061A1 (de) 1997-02-07 1997-02-07 Antigestagen wirksame Steroide mit fluorierter 17alpha-Alkylkette
PCT/EP1998/000752 WO1998034947A1 (de) 1997-02-07 1998-02-09 ANTIGESTAGEN WIRKSAME STEROIDE MIT FLUORIERTER 17α-ALKYLKETTE

Publications (2)

Publication Number Publication Date
BG103603A true BG103603A (bg) 2000-06-30
BG63875B1 BG63875B1 (bg) 2003-04-30

Family

ID=7820508

Family Applications (1)

Application Number Title Priority Date Filing Date
BG103603A BG63875B1 (bg) 1997-02-07 1999-07-26 Антигестагенни стероиди с флуорирана 17 алфа-алкилова верига

Country Status (35)

Country Link
US (4) US6316432B1 (bg)
EP (1) EP0970103B1 (bg)
JP (1) JP4324249B2 (bg)
KR (1) KR100511815B1 (bg)
CN (2) CN1246865A (bg)
AR (1) AR010887A1 (bg)
AT (1) ATE216397T1 (bg)
AU (1) AU742834B2 (bg)
BG (1) BG63875B1 (bg)
BR (1) BR9807667A (bg)
CA (1) CA2280041C (bg)
CL (1) CL2004001191A1 (bg)
CZ (1) CZ296328B6 (bg)
DE (2) DE19706061A1 (bg)
DK (1) DK0970103T3 (bg)
EA (1) EA003092B1 (bg)
EE (1) EE03831B1 (bg)
ES (1) ES2175673T3 (bg)
HK (1) HK1040718B (bg)
HU (1) HUP0000968A3 (bg)
ID (1) ID22643A (bg)
IL (1) IL131226A (bg)
IS (1) IS2190B (bg)
MY (1) MY118508A (bg)
NO (1) NO313554B1 (bg)
NZ (1) NZ336989A (bg)
PL (1) PL191808B1 (bg)
PT (1) PT970103E (bg)
SI (1) SI0970103T1 (bg)
SK (1) SK283155B6 (bg)
TR (1) TR199901855T2 (bg)
TW (1) TW499434B (bg)
UA (1) UA66783C2 (bg)
WO (1) WO1998034947A1 (bg)
ZA (1) ZA98985B (bg)

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ATE216397T1 (de) 2002-05-15
PL191808B1 (pl) 2006-07-31
MY118508A (en) 2004-11-30
US20020045774A1 (en) 2002-04-18
ZA98985B (en) 1999-08-03
HUP0000968A2 (hu) 2000-10-28
IL131226A0 (en) 2001-01-28
CN1246865A (zh) 2000-03-08
SK283155B6 (sk) 2003-03-04
WO1998034947A1 (de) 1998-08-13
TR199901855T2 (xx) 2000-04-21
US20050080060A1 (en) 2005-04-14
NO993811L (no) 1999-10-04
EA199900644A1 (ru) 2000-04-24
CA2280041A1 (en) 1998-08-13
DE19706061A1 (de) 1998-08-13
IL131226A (en) 2004-12-15
NO313554B1 (no) 2002-10-21
ID22643A (id) 1999-12-02
BG63875B1 (bg) 2003-04-30
JP4324249B2 (ja) 2009-09-02
IS5147A (is) 1999-08-04
NZ336989A (en) 2001-04-27
SK103899A3 (en) 2000-05-16
US6806263B2 (en) 2004-10-19
US6316432B1 (en) 2001-11-13
BR9807667A (pt) 2000-02-15
PT970103E (pt) 2002-09-30
CN1324802A (zh) 2001-12-05
EP0970103B1 (de) 2002-04-17
CA2280041C (en) 2007-10-23
HK1040718A1 (en) 2002-06-21
AU742834B2 (en) 2002-01-10
DK0970103T3 (da) 2002-07-22
EE9900339A (et) 2000-02-15
EE03831B1 (et) 2002-08-15
DE59803856D1 (de) 2002-05-23
JP2001510479A (ja) 2001-07-31
HK1040718B (zh) 2005-12-09
ES2175673T3 (es) 2002-11-16
CZ280599A3 (cs) 2000-01-12
PL334878A1 (en) 2000-03-27
TW499434B (en) 2002-08-21
US20030134834A1 (en) 2003-07-17
UA66783C2 (en) 2004-06-15
KR20000070835A (ko) 2000-11-25
EP0970103A1 (de) 2000-01-12
AU6100598A (en) 1998-08-26
AR010887A1 (es) 2000-07-12
CN1202120C (zh) 2005-05-18
KR100511815B1 (ko) 2005-09-05
CZ296328B6 (cs) 2006-02-15
IS2190B (is) 2007-01-15
SI0970103T1 (en) 2002-10-31
NO993811D0 (no) 1999-08-06
US7148213B2 (en) 2006-12-12
CL2004001191A1 (es) 2005-03-28
HUP0000968A3 (en) 2001-03-28
EA003092B1 (ru) 2002-12-26
US6503895B2 (en) 2003-01-07

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