ZA200500217B - 9-Alpha-substituted estratienes as selectively active estrogen - Google Patents
9-Alpha-substituted estratienes as selectively active estrogen Download PDFInfo
- Publication number
- ZA200500217B ZA200500217B ZA200500217A ZA200500217A ZA200500217B ZA 200500217 B ZA200500217 B ZA 200500217B ZA 200500217 A ZA200500217 A ZA 200500217A ZA 200500217 A ZA200500217 A ZA 200500217A ZA 200500217 B ZA200500217 B ZA 200500217B
- Authority
- ZA
- South Africa
- Prior art keywords
- estra
- triene
- vinyl
- treatment
- diol
- Prior art date
Links
- 229940011871 estrogen Drugs 0.000 title claims description 23
- 239000000262 estrogen Substances 0.000 title claims description 23
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- 238000011282 treatment Methods 0.000 claims description 29
- 150000001875 compounds Chemical class 0.000 claims description 23
- 125000004432 carbon atom Chemical group C* 0.000 claims description 16
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 10
- 210000002307 prostate Anatomy 0.000 claims description 10
- 239000000126 substance Substances 0.000 claims description 10
- 238000000338 in vitro Methods 0.000 claims description 9
- 230000002265 prevention Effects 0.000 claims description 9
- 238000002560 therapeutic procedure Methods 0.000 claims description 9
- 125000000217 alkyl group Chemical group 0.000 claims description 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 8
- 210000000988 bone and bone Anatomy 0.000 claims description 7
- 229910052731 fluorine Inorganic materials 0.000 claims description 7
- 238000001727 in vivo Methods 0.000 claims description 7
- 239000004215 Carbon black (E152) Substances 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 229930195733 hydrocarbon Natural products 0.000 claims description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
- 239000011737 fluorine Substances 0.000 claims description 5
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- 239000000333 selective estrogen receptor modulator Substances 0.000 claims description 5
- 229940095743 selective estrogen receptor modulator Drugs 0.000 claims description 5
- 125000001424 substituent group Chemical group 0.000 claims description 5
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims description 4
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 4
- 229910052794 bromium Inorganic materials 0.000 claims description 4
- 125000005111 carboxyalkoxy group Chemical group 0.000 claims description 4
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- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 3
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- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 3
- 239000000328 estrogen antagonist Substances 0.000 claims description 3
- 125000001072 heteroaryl group Chemical group 0.000 claims description 3
- 229910052739 hydrogen Inorganic materials 0.000 claims description 3
- 239000001257 hydrogen Substances 0.000 claims description 3
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- CPEONABTMRSIKA-UHFFFAOYSA-N 1,4$l^{2}-oxazinane Chemical compound C1COCC[N]1 CPEONABTMRSIKA-UHFFFAOYSA-N 0.000 claims description 2
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- 208000001132 Osteoporosis Diseases 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 150000002154 estra-1,3,5(10)-trienes Chemical class 0.000 claims description 2
- 150000002164 estratrienes Chemical class 0.000 claims description 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
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- 239000000203 mixture Substances 0.000 claims 10
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- 125000004429 atom Chemical group 0.000 claims 3
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- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
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- 229940046836 anti-estrogen Drugs 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- IWWREKZBZRBKBM-SSGTUYFUSA-N C[C@@]12CCC[C@H]1[C@@H]3C[C@@H](C4=C([C@H]3CC2)C=CC(=C4)NS(=O)(=O)O)O Chemical compound C[C@@]12CCC[C@H]1[C@@H]3C[C@@H](C4=C([C@H]3CC2)C=CC(=C4)NS(=O)(=O)O)O IWWREKZBZRBKBM-SSGTUYFUSA-N 0.000 claims 1
- 206010030247 Oestrogen deficiency Diseases 0.000 claims 1
- ZIDUOJGQZYFKEM-DABHTEOTSA-N [(8S,9R,13R,14S,16R)-9-ethenyl-13-methyl-3-(sulfoamino)-7,8,11,12,14,15,16,17-octahydro-6H-cyclopenta[a]phenanthren-16-yl]sulfamic acid Chemical compound C1CC2=CC(NS(O)(=O)=O)=CC=C2[C@]2(C=C)[C@@H]1[C@@H]1C[C@@H](NS(O)(=O)=O)C[C@@]1(C)CC2 ZIDUOJGQZYFKEM-DABHTEOTSA-N 0.000 claims 1
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- 102100029951 Estrogen receptor beta Human genes 0.000 description 3
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 3
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- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 3
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 3
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- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
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Classifications
-
- 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
- C07J1/0055—Estrane derivatives not substituted in position 17
-
- 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
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- A61K31/565—Compounds 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
-
- 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
- C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
- C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Epidemiology (AREA)
- Gynecology & Obstetrics (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Transplantation (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Pregnancy & Childbirth (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10226326A DE10226326A1 (de) | 2002-06-11 | 2002-06-11 | 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200500217B true ZA200500217B (en) | 2006-03-29 |
Family
ID=29723144
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200500217A ZA200500217B (en) | 2002-06-11 | 2006-01-10 | 9-Alpha-substituted estratienes as selectively active estrogen |
Country Status (29)
| Country | Link |
|---|---|
| EP (1) | EP1517914B1 (es) |
| JP (1) | JP4615998B2 (es) |
| KR (1) | KR101006612B1 (es) |
| CN (1) | CN1293090C (es) |
| AR (1) | AR040188A1 (es) |
| AT (1) | ATE303397T1 (es) |
| AU (1) | AU2003242683B9 (es) |
| BR (1) | BR0312140A (es) |
| CA (1) | CA2486495C (es) |
| CR (1) | CR10289A (es) |
| CU (1) | CU23414B7 (es) |
| DE (2) | DE10226326A1 (es) |
| DK (1) | DK1517914T3 (es) |
| EA (1) | EA008442B1 (es) |
| EC (1) | ECSP055530A (es) |
| ES (1) | ES2248770T3 (es) |
| HK (1) | HK1081203A1 (es) |
| HR (1) | HRP20050009B1 (es) |
| IL (1) | IL165321A (es) |
| MX (1) | MXPA04012491A (es) |
| NO (1) | NO329563B1 (es) |
| PE (1) | PE20040613A1 (es) |
| PL (1) | PL209910B1 (es) |
| RS (1) | RS50878B (es) |
| TW (1) | TWI286140B (es) |
| UA (1) | UA78062C2 (es) |
| UY (1) | UY27844A1 (es) |
| WO (1) | WO2003104253A2 (es) |
| ZA (1) | ZA200500217B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10027887A1 (de) | 2000-05-31 | 2001-12-13 | Jenapharm Gmbh | Verbindungen mit einer Sulfonamidgruppe und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| EP1689410B1 (en) * | 2003-11-26 | 2008-05-21 | Bayer Schering Pharma Aktiengesellschaft | 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 |
| US7534780B2 (en) | 2004-05-21 | 2009-05-19 | Bayer Schering Pharma Aktiengesellschaft | Estradiol prodrugs |
| DE102005057224A1 (de) | 2005-11-29 | 2007-05-31 | Bayer Schering Pharma Ag | Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| US20110052699A1 (en) * | 2008-02-13 | 2011-03-03 | Adrian Funke | Drug delivery system with stabilising effect |
| EP2143432A1 (en) | 2008-07-11 | 2010-01-13 | Bayer Schering Pharma AG | 9-alpha estratriene derivatives as ER-beta selective ligands for the prevention and treatment of intestinal cancer |
| CA2744127A1 (en) * | 2008-11-21 | 2010-05-27 | Bayer Schering Pharma Aktiengesellschaft | Drug delivery system |
| EP3185881B1 (en) | 2014-08-26 | 2022-03-09 | Betanien Hospital | Methods, agents and compositions for treatment of inflammatory conditions |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2336432A1 (de) * | 1973-07-13 | 1975-01-30 | Schering Ag | 3.17.18-trihydroxy-1.3.5(10)-oestratriene |
| US6154158A (en) * | 1998-06-30 | 2000-11-28 | Qualcomm Incorporated | Digital-to-analog converter D.C. offset correction comparing converter input and output signals |
| DE19906159A1 (de) * | 1999-02-09 | 2000-08-10 | Schering Ag | 16-Hydroxyestratriene als selektiv wirksame Estrogene |
| DK1226155T3 (da) * | 1999-11-02 | 2007-09-10 | Bayer Schering Pharma Ag | 18-nor-steroider som selektivt virksomme östrogener |
| CN100453549C (zh) * | 2000-04-12 | 2009-01-21 | 舍林股份公司 | 作为具选择活性的雌激素的8β-烃基取代的雌三烯 |
-
2002
- 2002-06-11 DE DE10226326A patent/DE10226326A1/de not_active Ceased
-
2003
- 2003-06-10 PE PE2003000575A patent/PE20040613A1/es not_active Application Discontinuation
- 2003-06-11 RS YUP-1070/04A patent/RS50878B/sr unknown
- 2003-06-11 MX MXPA04012491A patent/MXPA04012491A/es active IP Right Grant
- 2003-06-11 BR BR0312140-2A patent/BR0312140A/pt not_active IP Right Cessation
- 2003-06-11 EP EP03757065A patent/EP1517914B1/de not_active Expired - Lifetime
- 2003-06-11 JP JP2004511321A patent/JP4615998B2/ja not_active Expired - Fee Related
- 2003-06-11 PL PL373090A patent/PL209910B1/pl not_active IP Right Cessation
- 2003-06-11 WO PCT/EP2003/006172 patent/WO2003104253A2/de active IP Right Grant
- 2003-06-11 TW TW092115863A patent/TWI286140B/zh not_active IP Right Cessation
- 2003-06-11 AR ARP030102079A patent/AR040188A1/es active IP Right Grant
- 2003-06-11 ES ES03757065T patent/ES2248770T3/es not_active Expired - Lifetime
- 2003-06-11 CN CNB038135027A patent/CN1293090C/zh not_active Expired - Fee Related
- 2003-06-11 AU AU2003242683A patent/AU2003242683B9/en not_active Ceased
- 2003-06-11 EA EA200401544A patent/EA008442B1/ru not_active IP Right Cessation
- 2003-06-11 AT AT03757065T patent/ATE303397T1/de active
- 2003-06-11 UY UY27844A patent/UY27844A1/es not_active Application Discontinuation
- 2003-06-11 DE DE50301116T patent/DE50301116D1/de not_active Expired - Lifetime
- 2003-06-11 DK DK03757065T patent/DK1517914T3/da active
- 2003-06-11 KR KR1020047020133A patent/KR101006612B1/ko not_active IP Right Cessation
- 2003-06-11 CA CA2486495A patent/CA2486495C/en not_active Expired - Fee Related
- 2003-11-06 UA UAA200500212A patent/UA78062C2/uk unknown
-
2004
- 2004-11-22 IL IL165321A patent/IL165321A/en not_active IP Right Cessation
- 2004-12-10 CU CU20040282A patent/CU23414B7/es not_active IP Right Cessation
-
2005
- 2005-01-05 HR HRP20050009AA patent/HRP20050009B1/hr not_active IP Right Cessation
- 2005-01-10 EC EC2005005530A patent/ECSP055530A/es unknown
- 2005-01-10 NO NO20050127A patent/NO329563B1/no not_active IP Right Cessation
-
2006
- 2006-01-10 ZA ZA200500217A patent/ZA200500217B/en unknown
- 2006-01-27 HK HK06101276A patent/HK1081203A1/xx not_active IP Right Cessation
-
2008
- 2008-09-16 CR CR10289A patent/CR10289A/es not_active Application Discontinuation
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