AU2001273945A1 - 8beta-substituted-11beta-pentyl- and 11beta-hexyl-estra-1,3,5(10)-triene derivatives - Google Patents

8beta-substituted-11beta-pentyl- and 11beta-hexyl-estra-1,3,5(10)-triene derivatives

Info

Publication number
AU2001273945A1
AU2001273945A1 AU2001273945A AU7394501A AU2001273945A1 AU 2001273945 A1 AU2001273945 A1 AU 2001273945A1 AU 2001273945 A AU2001273945 A AU 2001273945A AU 7394501 A AU7394501 A AU 7394501A AU 2001273945 A1 AU2001273945 A1 AU 2001273945A1
Authority
AU
Australia
Prior art keywords
sup
8beta
11beta
substituted
compounds
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
AU2001273945A
Inventor
Nico Braeuer
Karl-Heinrich Fritzemeier
Christa Hegele-Hartung
Alexander Hillisch
Olaf Peters
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Pharma AG
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
Priority claimed from DE10019167A external-priority patent/DE10019167A1/en
Application filed by Schering AG filed Critical Schering AG
Publication of AU2001273945A1 publication Critical patent/AU2001273945A1/en
Abandoned legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P5/30—Oestrogens
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    • A61P5/00—Drugs for disorders of the endocrine system
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0062—Estrane derivatives substituted in position 17 alfa not substituted in position 17 beta
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0074—Esters
    • 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

Abstract

This invention describes the new 8beta-substituted estratrienes of general formula I in which R<SUP>2</SUP>, R<SUP>3</SUP>, R<SUP>6</SUP>, R<SUP>6'</SUP>, R<SUP>7</SUP>, R<SUP>7'</SUP>, R<SUP>9</SUP>, R<SUP>11</SUP>, R<SUP>11'</SUP>, R<SUP>12</SUP>, R<SUP>14</SUP>, R<SUP>15</SUP>, R<SUP>15'</SUP>, R<SUP>16</SUP>, R<SUP>16'</SUP>, R<SUP>17</SUP>, R<SUP>17'</SUP> have the meanings that are indicated in the description, and R<SUP>8 </SUP>means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of an 8beta-substituted estratriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bones rather than the uterus.
AU2001273945A 2000-04-12 2001-04-12 8beta-substituted-11beta-pentyl- and 11beta-hexyl-estra-1,3,5(10)-triene derivatives Abandoned AU2001273945A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
DE10019167 2000-04-12
DE10019167A DE10019167A1 (en) 2000-04-12 2000-04-12 New 8 beta-substituted 11 beta-(pentyl or hexyl)-estra-1,3,5(10)-triene derivatives, are ovary-selective estrogen receptor ligands useful e.g. as female or male contraceptives or for treating ovarian carcinoma
US20737000P 2000-05-26 2000-05-26
US60207370 2000-05-26
PCT/EP2001/004289 WO2001077138A1 (en) 2000-04-12 2001-04-12 8β-SUBSTITUTED-11β-PENTYL- AND 11β-HEXYL-ESTRA-1,3,5(10)-TRIENE DERIVATIVES

Publications (1)

Publication Number Publication Date
AU2001273945A1 true AU2001273945A1 (en) 2001-10-23

Family

ID=26005365

Family Applications (3)

Application Number Title Priority Date Filing Date
AU2001258341A Ceased AU2001258341B2 (en) 2000-04-12 2001-04-12 8beta-hydrocarbyl-substituted estratrienes for use as selective estrogens
AU5834101A Pending AU5834101A (en) 2000-04-12 2001-04-12 8ss-hydrocarbyl-substituted estratrienes for use as selective estrogens
AU2001273945A Abandoned AU2001273945A1 (en) 2000-04-12 2001-04-12 8beta-substituted-11beta-pentyl- and 11beta-hexyl-estra-1,3,5(10)-triene derivatives

Family Applications Before (2)

Application Number Title Priority Date Filing Date
AU2001258341A Ceased AU2001258341B2 (en) 2000-04-12 2001-04-12 8beta-hydrocarbyl-substituted estratrienes for use as selective estrogens
AU5834101A Pending AU5834101A (en) 2000-04-12 2001-04-12 8ss-hydrocarbyl-substituted estratrienes for use as selective estrogens

Country Status (26)

Country Link
US (3) US7378404B2 (en)
EP (2) EP1272504B1 (en)
JP (2) JP3828423B2 (en)
CN (1) CN100453549C (en)
AT (2) ATE302790T1 (en)
AU (3) AU2001258341B2 (en)
BG (1) BG107173A (en)
BR (1) BR0109983A (en)
CA (1) CA2406177C (en)
CZ (1) CZ20023382A3 (en)
DE (1) DE50112561D1 (en)
DK (2) DK1272504T3 (en)
EA (1) EA006299B1 (en)
EE (1) EE200200589A (en)
ES (2) ES2245694T3 (en)
HK (1) HK1057219A1 (en)
HR (1) HRP20020892B1 (en)
HU (1) HUP0300335A2 (en)
IL (2) IL152248A0 (en)
MX (1) MXPA02010066A (en)
NO (2) NO20024907L (en)
NZ (1) NZ543724A (en)
PL (1) PL207488B1 (en)
PT (1) PT1272504E (en)
SK (1) SK14632002A3 (en)
WO (2) WO2001077138A1 (en)

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DE10226326A1 (en) * 2002-06-11 2004-01-15 Schering Ag 9-alpha-substituted estratrienes as selective estrogens
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DE10318896A1 (en) * 2003-04-22 2004-11-25 Schering Ag 8beta-vinyl-11beta- (omega-substituted) alkyl-estra-1,3,5 (10) -trienes
PT1689410E (en) * 2003-11-26 2008-08-18 Bayer Schering Pharma Ag Prevention and treatment of hypertensive heart diseases by the selective estrogens 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol and 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-diol
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DE102005057224A1 (en) * 2005-11-29 2007-05-31 Bayer Schering Pharma Ag New 9-alpha substituted estratriene derivatives esterified with a sulfamoylphenyl-substituted acid residue, are prodrugs useful as carboanhydrase inhibitors for treating estrogen deficiency disorders
EP2014672A1 (en) * 2007-07-12 2009-01-14 Bayer Schering Pharma Aktiengesellschaft 8-beta-substituted estratrienes as selectively active estrogens
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