NZ334277A - 7'alpha'('xi'-aminoalkyl)estratrienes - Google Patents

7'alpha'('xi'-aminoalkyl)estratrienes

Info

Publication number
NZ334277A
NZ334277A NZ334277A NZ33427797A NZ334277A NZ 334277 A NZ334277 A NZ 334277A NZ 334277 A NZ334277 A NZ 334277A NZ 33427797 A NZ33427797 A NZ 33427797A NZ 334277 A NZ334277 A NZ 334277A
Authority
NZ
New Zealand
Prior art keywords
alpha
hydrocarbyl
aminoalkyl
estratrienes
halogen
Prior art date
Application number
NZ334277A
Inventor
Rolf Bohlmann
Dieter Bittler
Josef Heindi
Nikolaus Heinrich
Helmut Hofmeister
Hermann Kunzer
Gerhard Sauer
Christa Hegele-Hartung
Rosemarie Lichtner
Yukishige Nishino
Karsten Parczyk
Martin Schneider
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
Application filed by Schering Ag filed Critical Schering Ag
Priority to NZ507075A priority Critical patent/NZ507075A/en
Publication of NZ334277A publication Critical patent/NZ334277A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids 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
    • C07J53/002—Carbocyclic rings fused
    • C07J53/004—3 membered carbocyclic rings
    • C07J53/008—3 membered carbocyclic rings in position 15/16
    • 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
    • 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
    • A61P5/32—Antioestrogens
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/006—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton spiro-condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids 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
    • C07J53/002—Carbocyclic rings fused

Landscapes

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

Abstract

7 alpha -(xi-Aminoalkyl)-oestratriene derivatives of formula (I) and their acid-addition salts wherein: SK = -(CH2)m-NA-CHB-CHD-(CH2)n-SOx-(CH2)3-E; A = H or 1-5C alkyl and B, D = H; or A+B = (CH2)p and D = H; or A+D = (CH2)q and B = H; E = optionally mono- to perfluorinated ethyl; R3 = H, 1-8C hydrocarbyl or COR3'; R3' = H, 1-8C hydrocarbyl or phenyl; R11 = H, halogen or ONO2; R14, R15a, R15b, R16a and R16b = H, or R14+R15a = a bond or a CH2 bridge, or R15b = Me and R15a = H, or R15a and R15b = Me, or R15b+R16b = a CH2 bridge, or R16a or R16b = halogen, or R16a+R16b = methylidene; and the remaining substituents from R14, R15a, R15b, R16a and R16b = H; R17' = H, alkyl, 2-5C alkenyl, 2-5C alkynyl or CF3, or R17'+R14 = CH2CH2 when R17' is in the alpha position; R17" = H or COR17"'; R17"' = H or hydrocarbyl; m = 4-6, n, x = 0-2, p = 2-5, q = 2-4; provided that, if A+B do not form (CH2)p or A+D do not form (CH2)q then R11, R14, R15a, R15a, R16a and R16b are not all H.
NZ334277A 1996-08-20 1997-08-20 7'alpha'('xi'-aminoalkyl)estratrienes NZ334277A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
NZ507075A NZ507075A (en) 1996-08-20 1997-08-20 Intermediate compounds for preparing 7a-(-aminoalkyl)-estratrienes

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 (1)

Publication Number Publication Date
NZ334277A true NZ334277A (en) 2000-10-27

Family

ID=7804367

Family Applications (1)

Application Number Title Priority Date Filing Date
NZ334277A NZ334277A (en) 1996-08-20 1997-08-20 7'alpha'('xi'-aminoalkyl)estratrienes

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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US6503896B1 (en) 1997-12-24 2003-01-07 Sri International Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use
US6548491B2 (en) 1997-12-24 2003-04-15 Sri International Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use
DE19807791A1 (en) 1998-02-19 1999-08-26 Schering Ag Combination preparation of estrogen with 7-aminoalkyl-estratriene antiestrogen, useful in hormone replacement therapy, e.g. for treatment osteoporosis, Alzheimer's disease and hot flushes
DE19833786A1 (en) * 1998-07-18 2000-01-20 Schering Ag New diphenyl-benzocycloheptene derivatives, are tissue-selective estrogens and antiestrogens useful e.g. for treating osteoporosis or hormone-dependent tumors or in hormone replacement therapy
DE19842123C1 (en) * 1998-09-05 2000-07-13 Schering Ag 11beta-fluoro-7alpha- (14,14,15,15,15-pentafluoro-6-methyl-10-thia-6-azapentadecyl) estra-1,3,5 (10) - triene-3,17beta-diol as crystalline solvate
DE19906159A1 (en) * 1999-02-09 2000-08-10 Schering Ag 16-hydroxyestratrienes as selectively active estrogens
WO2001012622A1 (en) * 1999-08-18 2001-02-22 Schering Aktiengesellschaft Piperidine and pyrrolidine derivatives displaying neuronal activity
GB0000313D0 (en) * 2000-01-10 2000-03-01 Astrazeneca Uk Ltd Formulation
DE10019171A1 (en) * 2000-04-07 2001-10-18 Schering Ag Compositions for use as penetration enhancers in transdermal formulations for highly lipophilic active ingredients
AU2006202187B2 (en) * 2001-11-27 2008-11-06 Bayer Schering Pharma Aktiengesellschaft 17alpah-alkyl-17beta-oxy-estratrienes and intermediate products for their production, uses thereof and pharmaceutical preparations
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
US20040242551A1 (en) * 2003-05-28 2004-12-02 Schering Ag Composition comprising antiprogestins and pure antiestrogens for prophylaxis and treatment of hormone-dependent diseases
TW200617019A (en) 2004-07-27 2006-06-01 Sicor Inc A process for the preparation of 7α-alkylated 19-norsteroids
WO2007060839A1 (en) 2005-11-22 2007-05-31 Sumitomo Chemical Company, Limited Organic sulfur compounds and use thereof as arthropodicides
DE102007023614A1 (en) 2007-05-21 2008-11-27 Bayer Schering Pharma Aktiengesellschaft New amide compounds used for treatment of gynecological diseases e.g. endometriosis, for female fertility control and female hormone replacement therapy, has general formula
DE102007049630A1 (en) 2007-10-11 2009-10-29 Bayer Schering Pharma Aktiengesellschaft New amide compounds used for therapy and/or prophylaxis of gynecological diseases e.g. endometriosis, for female fertility control and female hormone replacement therapy
TW200904329A (en) 2007-05-18 2009-02-01 Sumitomo Chemical Co Organic sulfur compound and its use for controlling harmful arthropod
JP2009001551A (en) 2007-05-18 2009-01-08 Sumitomo Chemical Co Ltd Organic sulfur compound and its use for controlling harmful arthropod
JP5298631B2 (en) 2007-05-18 2013-09-25 住友化学株式会社 Organic sulfur compounds and their use for controlling harmful arthropods
DE102007032800A1 (en) 2007-07-10 2009-01-15 Bayer Schering Pharma Aktiengesellschaft Nonsteroidal progesterone receptor modulators
NZ591955A (en) 2007-10-16 2011-10-28 Repros Therapeutics Inc Trans-clomiphene for diabetes mellitus type 2
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
DE102009034362A1 (en) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-aryl derivatives, process for their preparation and their use for the treatment of diseases
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
DE102009034367A1 (en) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-benzylidene derivatives, process for their preparation and their use for the treatment of diseases
DE102009034366A1 (en) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-methyleneoxyalkylene aryl derivatives, process for their preparation and their use for the treatment of diseases
DE102009034526A1 (en) 2009-07-21 2011-02-10 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-ethynylphenyl derivatives, process for their preparation and their use for the treatment of diseases
DE102009034525A1 (en) 2009-07-21 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluoroethyl-estra-4,9 (10) -diene-11-aryl derivatives, process for their preparation and their use for the treatment of diseases
WO2011092127A1 (en) 2010-01-26 2011-08-04 Bayer Schering Pharma Aktiengesellschaft 14,17-bridged estratriene derivatives comprising heterocyclic bioisosteres for the phenolic a-ring
DE102010007722A1 (en) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesterone receptor antagonist
DE102010007719A1 (en) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesterone receptor antagonist
KR20160088947A (en) 2010-06-16 2016-07-26 앙도르쉐르슈 인코포레이티드 Methods of treating or preventing estrogen-related diseases
DE102010030538A1 (en) 2010-06-25 2011-12-29 Bayer Schering Pharma Aktiengesellschaft 6,7-Dihydro-5H-benzo [7] annulene derivatives, process for their preparation, pharmaceutical preparations containing them and their use for the preparation of medicaments
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DE102011087987A1 (en) 2011-12-08 2013-06-13 Bayer Intellectual Property Gmbh 6,7-Dihydro-5H-benzo [7] annulene derivatives, process for their preparation, pharmaceutical preparations containing them and their use for the preparation of medicaments
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JP6356218B2 (en) * 2013-04-18 2018-07-11 シーアン リーバン ファーマシューティカル テクノロジー シーオー．， エルティーディー．Ｘｉ’Ａｎ Ｌｉｂａｎｇ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏ．， Ｌｔｄ． Of 7-α- [9- (4,4,5,5,5-pentafluoropentylsulfinyl) nonyl] -estradi-1,3,5 (10) -triene-3,17β-diol having antitumor activity Ester derivatives and methods for their preparation
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US10752653B2 (en) 2016-05-06 2020-08-25 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
EP3919502A1 (en) 2016-07-07 2021-12-08 Sage Therapeutics, Inc. 11-substituted 24-hydroxysterols for use in the treatment of nmda related conditions
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Also Published As

Publication number Publication date
BR9711328A (en) 1999-08-17
IL128601A0 (en) 2000-01-31
ZA977482B (en) 1998-02-23
HUP9903106A2 (en) 2000-03-28
CA2263708A1 (en) 1998-02-26
EA001577B1 (en) 2001-06-25
EE04021B1 (en) 2003-04-15
DE59709239D1 (en) 2003-03-06
PL186309B1 (en) 2003-12-31
CZ57999A3 (en) 1999-08-11
SK18899A3 (en) 1999-08-06
EP0920441A1 (en) 1999-06-09
ATE231882T1 (en) 2003-02-15
NO990793L (en) 1999-04-20
KR20000068261A (en) 2000-11-25
TW552267B (en) 2003-09-11
AU4552097A (en) 1998-03-06
EE9900075A (en) 1999-10-15
WO1998007740A1 (en) 1998-02-26
DK0920441T3 (en) 2003-05-26
BG103185A (en) 1999-11-30
UA50792C2 (en) 2002-11-15
AU728843B2 (en) 2001-01-18
EP0920441B1 (en) 2003-01-29
AR009278A1 (en) 2000-04-12
EA199900210A1 (en) 1999-08-26
JP2001503024A (en) 2001-03-06
HUP9903106A3 (en) 2000-05-29
PT920441E (en) 2003-06-30
BG62972B1 (en) 2000-12-29
TR199900432T2 (en) 1999-04-21
PL331863A1 (en) 1999-08-16
IS4976A (en) 1999-02-11
NO315655B1 (en) 2003-10-06
IL128601A (en) 2003-07-31
NO990793D0 (en) 1999-02-19
CN1231670A (en) 1999-10-13
ES2191857T3 (en) 2003-09-16
DE19635525A1 (en) 1998-02-26

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