BG103185A - 7 alpha -(epsilon -aminoalkyl)-estratrines, method for their preparation, pharmaceutical preparations containing them and their application for the preparation of medicamentous forms - Google Patents

7 alpha -(epsilon -aminoalkyl)-estratrines, method for their preparation, pharmaceutical preparations containing them and their application for the preparation of medicamentous forms

Info

Publication number
BG103185A
BG103185A BG103185A BG10318599A BG103185A BG 103185 A BG103185 A BG 103185A BG 103185 A BG103185 A BG 103185A BG 10318599 A BG10318599 A BG 10318599A BG 103185 A BG103185 A BG 103185A
Authority
BG
Bulgaria
Prior art keywords
residue
atom
hydrogen atom
group
mean
Prior art date
Application number
BG103185A
Other languages
Bulgarian (bg)
Other versions
BG62972B1 (en
Inventor
Rolf Bohlmann
Dieter Bittler
Josef Heindi
Nikolaus Heinrich
Helmut Hofmeister
Hermann Kunzer
Gerhard Sauer
Christa Hegelehartung
Rosemarie Lichtner
Yukishige Nishino
Karsten Parczyk
Martin Schneider
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.)
Filing date
Publication date
Application filed by Schering Aktiengesellschaft filed Critical Schering Aktiengesellschaft
Publication of BG103185A publication Critical patent/BG103185A/en
Publication of BG62972B1 publication Critical patent/BG62972B1/en

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Classifications

    • 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
    • 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
    • C07J53/0043 membered carbocyclic rings
    • C07J53/0083 membered carbocyclic rings in position 15/16
    • 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
    • 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
    • A61P5/32Antioestrogens
    • 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
    • C07J41/0072Normal 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
    • 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
    • C07J43/006Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton spiro-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)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The compoundns can be applied for the preparation ofmedicamentous forms designed for tumour and hormonal therapy. Theyshow very strong antistrogenous effect. Part of them are pureantiestrogens, and another part have partial estrogenous effect.The substituted 7-( -aminoalkyl)-estratrines have the formulawhere the side chain SK means a residue with the formula- -(CH2)m- -N- -CH- -(CH2)n--(CH2)3--EA B Dwhere m has the value of 4, 5 or 6, n - 0, 1 or 2, x - 0, 1 or 2,A means hydrogen atom or C1-5-alkyl group, B and D are always ahydrogen atom, or C1-5-alkyl group, B & D are always a hydrogenatom, or A & B together mean alkylene group --(CH2)p--c, p iw 2,34or 5 and D is hydrogen atom, or A & D together mean alkylene group-(CH2)q-- c, q is 2, 3 or 4 and B means hydrogen atom and E isunsubstituted or one or five times fluorinated ethyl residue, orthe end substitutent --(CH2)-2-E-- of the side chain is optionallysubstituted by a substituted aryl and heteroaryl residue which isbound directly or by means of mono- di- or trimethylene group tothe sulphur atom, R3 means hydrogen atom, carbon residue with upto 8 carbon atoms or residue with the formulaR3'-C(O)-,where R3' is hydrogen or carbon atom with up to 8 carbon atoms oris phenyl residue, R11 is hydrogen, halogen atom or onenitrooxygroup -O-NO2, R14, R15, R16 & R16 always mean hydrgoenatom or R14 & R15 mean additional bond or methylene bridge, or R15means methylene group and R15 means hydrogen atom, or R15 & R15are alway a methylene group, or R15 and R16 together formmethylene bridge, or R16 or R16 means halgen atom or R16 togethermean methylidene group and the customary substitutents R14m R15,R15, R16 and R16 are always hydrogen atom, R17' means hydrogenatom in - or - position means C1-5-alkyl, C2-5-alkylene orC2-5-alkynyl group or is trifluoromethyl group and R17" ishydrogen atom or residue with formulaR17''' --C(O)--in which R17''' is hydrogen atom or carbon residue with up to 8carbon atoms, or when R17' is in - position, R17', together withR14 form ethanol bridge provided that A & B simultaneously do notmean -(CH2)p or A & D togehter do not mean -(CH2)q, at least onesubstituent of R11, R14, R15, R16 & R16 is not a hydrogen atom.The invention also relates to the physiologically aceptableadjunctive salts of the compounds with organic and inorganicacids.42 claims
BG103185A 1996-08-20 1999-02-16 7 alpha-(epsilon-aminoalkyl)-estratrines, method for their preparation, pharmaceutical preparations containing them and their application for the preparation of medicamentous forms BG62972B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19635525A DE19635525A1 (en) 1996-08-20 1996-08-20 New 7-alpha-(xi-aminoalkyl)- oestratriene derivatives
PCT/EP1997/004517 WO1998007740A1 (en) 1996-08-20 1997-08-20 7α-(κ-AMINOALKYL)ESTRATRIENES, PROCESS FOR PREPARING THE SAME, PHARMACEUTICAL PREPARATIONS CONTAINING SAID 7α-(κ-AMINOALKYL)ESTRATRIENES AND THEIR USE FOR PREPARING MEDICAMENTS

Publications (2)

Publication Number Publication Date
BG103185A true BG103185A (en) 1999-11-30
BG62972B1 BG62972B1 (en) 2000-12-29

Family

ID=7804367

Family Applications (1)

Application Number Title Priority Date Filing Date
BG103185A BG62972B1 (en) 1996-08-20 1999-02-16 7 alpha-(epsilon-aminoalkyl)-estratrines, method for their preparation, pharmaceutical preparations containing them and their application for the preparation of medicamentous forms

Country Status (29)

Country Link
EP (1) EP0920441B1 (en)
JP (1) JP2001503024A (en)
KR (1) KR20000068261A (en)
CN (1) CN1231670A (en)
AR (1) AR009278A1 (en)
AT (1) ATE231882T1 (en)
AU (1) AU728843B2 (en)
BG (1) BG62972B1 (en)
BR (1) BR9711328A (en)
CA (1) CA2263708A1 (en)
CZ (1) CZ57999A3 (en)
DE (2) DE19635525A1 (en)
DK (1) DK0920441T3 (en)
EA (1) EA001577B1 (en)
EE (1) EE04021B1 (en)
ES (1) ES2191857T3 (en)
HU (1) HUP9903106A3 (en)
IL (1) IL128601A (en)
IS (1) IS4976A (en)
NO (1) NO315655B1 (en)
NZ (1) NZ334277A (en)
PL (1) PL186309B1 (en)
PT (1) PT920441E (en)
SK (1) SK18899A3 (en)
TR (1) TR199900432T2 (en)
TW (1) TW552267B (en)
UA (1) UA50792C2 (en)
WO (1) WO1998007740A1 (en)
ZA (1) ZA977482B (en)

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DE19906159A1 (en) * 1999-02-09 2000-08-10 Schering Ag 16-hydroxyestratrienes as selectively active estrogens
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DE10019171A1 (en) * 2000-04-07 2001-10-18 Schering Ag Compositions for use as penetration enhancers in transdermal formulations for highly lipophilic active ingredients
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DE10159217A1 (en) 2001-11-27 2003-06-05 Schering Ag 17alpha-alkyl-17ß-oxy-estratrienes and intermediates for their preparation, use of 17alpha-alkyl-17ß-oxy-estratriene for the preparation of medicaments and pharmaceutical preparations
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JP2009001551A (en) 2007-05-18 2009-01-08 Sumitomo Chemical Co Ltd Organic sulfur compound and its use for controlling harmful arthropod
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JP5558358B2 (en) 2007-10-16 2014-07-23 レプロス セラピューティクス インコーポレイティド TRANS-clomiphene for metabolic syndrome
DE102007058747A1 (en) 2007-12-05 2009-06-10 Bayer Schering Pharma Aktiengesellschaft Nonsteroidal progesterone receptor modulators
EP2070941A1 (en) 2007-12-14 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Stereoselective synthesis of selective estrogen receptor down-regulators
EP2070909A1 (en) 2007-12-15 2009-06-17 Bayer Schering Pharma AG Non-steroidal progesterone receptor modulators
DE102008057230A1 (en) 2008-11-11 2010-05-12 Bayer Schering Pharma Aktiengesellschaft Synergistic pharmaceutical combination with an estrogen receptor antagonist and a progestin
JP5212350B2 (en) 2008-12-24 2013-06-19 住友化学株式会社 Halogen-containing organic sulfur compounds and uses thereof
EP2258375A1 (en) 2009-06-04 2010-12-08 Bayer Schering Pharma Aktiengesellschaft 17B-alkyl-17alpha-oxy-estratrienes
DE102009034368A1 (en) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-acyloxyalkylenephenyl derivatives, process for their preparation and their use for the treatment of diseases
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Also Published As

Publication number Publication date
IL128601A0 (en) 2000-01-31
AU4552097A (en) 1998-03-06
ZA977482B (en) 1998-02-23
ES2191857T3 (en) 2003-09-16
BR9711328A (en) 1999-08-17
SK18899A3 (en) 1999-08-06
EE9900075A (en) 1999-10-15
DK0920441T3 (en) 2003-05-26
KR20000068261A (en) 2000-11-25
ATE231882T1 (en) 2003-02-15
CA2263708A1 (en) 1998-02-26
NO315655B1 (en) 2003-10-06
NO990793L (en) 1999-04-20
NZ334277A (en) 2000-10-27
PL186309B1 (en) 2003-12-31
DE19635525A1 (en) 1998-02-26
TR199900432T2 (en) 1999-04-21
JP2001503024A (en) 2001-03-06
PL331863A1 (en) 1999-08-16
DE59709239D1 (en) 2003-03-06
IS4976A (en) 1999-02-11
EA199900210A1 (en) 1999-08-26
NO990793D0 (en) 1999-02-19
TW552267B (en) 2003-09-11
EP0920441A1 (en) 1999-06-09
HUP9903106A3 (en) 2000-05-29
IL128601A (en) 2003-07-31
EE04021B1 (en) 2003-04-15
AR009278A1 (en) 2000-04-12
UA50792C2 (en) 2002-11-15
EA001577B1 (en) 2001-06-25
EP0920441B1 (en) 2003-01-29
WO1998007740A1 (en) 1998-02-26
CZ57999A3 (en) 1999-08-11
BG62972B1 (en) 2000-12-29
HUP9903106A2 (en) 2000-03-28
PT920441E (en) 2003-06-30
AU728843B2 (en) 2001-01-18
CN1231670A (en) 1999-10-13

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