IL165321A - Astronomers converted to the alpha-9 position as selectively active estrogens - Google Patents
Astronomers converted to the alpha-9 position as selectively active estrogensInfo
- Publication number
- IL165321A IL165321A IL165321A IL16532104A IL165321A IL 165321 A IL165321 A IL 165321A IL 165321 A IL165321 A IL 165321A IL 16532104 A IL16532104 A IL 16532104A IL 165321 A IL165321 A IL 165321A
- Authority
- IL
- Israel
- Prior art keywords
- oestra
- triene
- vinyl
- diol
- homo
- Prior art date
Links
- 239000000262 estrogen Substances 0.000 title claims description 32
- 229940011871 estrogen Drugs 0.000 title description 30
- 150000002164 estratrienes Chemical class 0.000 title description 5
- -1 trifluoromethylthio, methoxy, ethoxy Chemical group 0.000 claims description 84
- 150000001875 compounds Chemical class 0.000 claims description 48
- 238000011282 treatment Methods 0.000 claims description 35
- 125000004432 carbon atom Chemical group C* 0.000 claims description 23
- 210000002307 prostate Anatomy 0.000 claims description 20
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 16
- 238000002560 therapeutic procedure Methods 0.000 claims description 16
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 14
- 238000004519 manufacturing process Methods 0.000 claims description 14
- 238000000338 in vitro Methods 0.000 claims description 13
- 125000000217 alkyl group Chemical group 0.000 claims description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims description 12
- 210000000988 bone and bone Anatomy 0.000 claims description 10
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 10
- 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
- 201000010099 disease Diseases 0.000 claims description 8
- 229910052731 fluorine Inorganic materials 0.000 claims description 8
- 230000002265 prevention Effects 0.000 claims description 8
- 239000004215 Carbon black (E152) Substances 0.000 claims description 7
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 7
- 229930195733 hydrocarbon Natural products 0.000 claims description 7
- 229920006395 saturated elastomer Polymers 0.000 claims description 7
- 125000003118 aryl group Chemical group 0.000 claims description 6
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- 125000001424 substituent group Chemical group 0.000 claims description 6
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims description 5
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 5
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 5
- 208000007984 Female Infertility Diseases 0.000 claims description 5
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 5
- 229910052794 bromium Inorganic materials 0.000 claims description 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 5
- 125000005111 carboxyalkoxy group Chemical group 0.000 claims description 5
- 239000000460 chlorine Substances 0.000 claims description 5
- 229910052801 chlorine Inorganic materials 0.000 claims description 5
- 229910052736 halogen Inorganic materials 0.000 claims description 5
- 125000005843 halogen group Chemical group 0.000 claims description 5
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- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 206010020718 hyperplasia Diseases 0.000 claims description 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 4
- 125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 claims description 4
- 125000003107 substituted aryl group Chemical group 0.000 claims description 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 3
- 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 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 3
- 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
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 3
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- OWJDVMRCRYHKOJ-YNUHATHGSA-N (8s,9r,13r,14s,16r)-9-ethenyl-3-methoxy-13-methyl-7,8,11,12,14,15,16,17-octahydro-6h-cyclopenta[a]phenanthren-16-ol Chemical compound C1C[C@]2(C=C)C3=CC=C(OC)C=C3CC[C@H]2[C@@H]2C[C@@H](O)C[C@]21C OWJDVMRCRYHKOJ-YNUHATHGSA-N 0.000 claims description 2
- 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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- 125000003342 alkenyl 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
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
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- 229930195735 unsaturated hydrocarbon Natural products 0.000 claims description 2
- NWBMAMPWLYWTPL-LODQPUINSA-N (7r,8s,9r,13r,14s,16r)-9-ethenyl-7-fluoro-13-methyl-7,8,11,12,14,15,16,17-octahydro-6h-cyclopenta[a]phenanthrene-3,16-diol Chemical compound C([C@H]1F)C2=CC(O)=CC=C2[C@]2(C=C)[C@@H]1[C@@H]1C[C@@H](O)C[C@@]1(C)CC2 NWBMAMPWLYWTPL-LODQPUINSA-N 0.000 claims 1
- LXLNOGZWGYFWQV-MFWBVCSQSA-N (8S,9R,13S,14S,16R)-9-ethenyl-17-fluoro-13-methyl-7,8,11,12,14,15,16,17-octahydro-6H-cyclopenta[a]phenanthrene-3,16-diol Chemical compound FC1[C@]2(C)[C@@H](C[C@H]1O)[C@@H]1CCC=3C=C(C=CC3[C@]1(CC2)C=C)O LXLNOGZWGYFWQV-MFWBVCSQSA-N 0.000 claims 1
- LXZXJPTVLPPCAL-BSDMPUNLSA-N (8s,9r,13r,14s,16r)-13-methyl-9-[(z)-prop-1-enyl]-7,8,11,12,14,15,16,17-octahydro-6h-cyclopenta[a]phenanthrene-3,16-diol Chemical compound C1CC2=CC(O)=CC=C2[C@]2(\C=C/C)[C@@H]1[C@@H]1C[C@@H](O)C[C@@]1(C)CC2 LXZXJPTVLPPCAL-BSDMPUNLSA-N 0.000 claims 1
- NJQITWAKELCMAY-DABHTEOTSA-N (8s,9r,13r,14s,16r)-9-ethenyl-13-methyl-7,8,11,12,14,15,16,17-octahydro-6h-cyclopenta[a]phenanthrene-3,16-diol Chemical compound C1CC2=CC(O)=CC=C2[C@]2(C=C)[C@@H]1[C@@H]1C[C@@H](O)C[C@@]1(C)CC2 NJQITWAKELCMAY-DABHTEOTSA-N 0.000 claims 1
- VWAHIVOFRSQMGC-OBJCFNGXSA-N (8s,9s,13r,14s,16r)-13-methyl-9-propyl-7,8,11,12,14,15,16,17-octahydro-6h-cyclopenta[a]phenanthrene-3,16-diol Chemical compound C1CC2=CC(O)=CC=C2[C@]2(CCC)[C@@H]1[C@@H]1C[C@@H](O)C[C@@]1(C)CC2 VWAHIVOFRSQMGC-OBJCFNGXSA-N 0.000 claims 1
- ZKGGIOCJNCBSDH-KNOXWWKRSA-N C(C)(=O)O[C@H]1C[C@H]2[C@@H]3CCC[C@@]3(C)CC[C@@]2(C=2C=CC(=CC12)O)C=C Chemical compound C(C)(=O)O[C@H]1C[C@H]2[C@@H]3CCC[C@@]3(C)CC[C@@]2(C=2C=CC(=CC12)O)C=C ZKGGIOCJNCBSDH-KNOXWWKRSA-N 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
- 230000001363 autoimmune Effects 0.000 claims 1
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- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Epidemiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Transplantation (AREA)
- Urology & Nephrology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10226326A DE10226326A1 (de) | 2002-06-11 | 2002-06-11 | 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene |
| PCT/EP2003/006172 WO2003104253A2 (de) | 2002-06-11 | 2003-06-11 | 9-alpha-substituierte estratriene als selektiv wirksame estrogene |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL165321A true IL165321A (en) | 2009-08-03 |
Family
ID=29723144
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL165321A IL165321A (en) | 2002-06-11 | 2004-11-22 | Astronomers converted to the alpha-9 position as selectively active estrogens |
Country Status (28)
| Country | Link |
|---|---|
| EP (1) | EP1517914B1 (enExample) |
| JP (1) | JP4615998B2 (enExample) |
| KR (1) | KR101006612B1 (enExample) |
| CN (1) | CN1293090C (enExample) |
| AR (1) | AR040188A1 (enExample) |
| AT (1) | ATE303397T1 (enExample) |
| AU (1) | AU2003242683B9 (enExample) |
| BR (1) | BR0312140A (enExample) |
| CA (1) | CA2486495C (enExample) |
| CR (1) | CR10289A (enExample) |
| CU (1) | CU23414B7 (enExample) |
| DE (2) | DE10226326A1 (enExample) |
| DK (1) | DK1517914T3 (enExample) |
| EA (1) | EA008442B1 (enExample) |
| EC (1) | ECSP055530A (enExample) |
| ES (1) | ES2248770T3 (enExample) |
| HR (1) | HRP20050009B1 (enExample) |
| IL (1) | IL165321A (enExample) |
| MX (1) | MXPA04012491A (enExample) |
| NO (1) | NO329563B1 (enExample) |
| PE (1) | PE20040613A1 (enExample) |
| PL (1) | PL209910B1 (enExample) |
| RS (1) | RS50878B (enExample) |
| TW (1) | TWI286140B (enExample) |
| UA (1) | UA78062C2 (enExample) |
| UY (1) | UY27844A1 (enExample) |
| WO (1) | WO2003104253A2 (enExample) |
| ZA (1) | ZA200500217B (enExample) |
Families Citing this family (9)
| 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 |
| EP2252261A2 (en) * | 2008-02-13 | 2010-11-24 | Bayer Schering Pharma Aktiengesellschaft | 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 |
| WO2010057594A1 (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 |
| CA3109978A1 (en) * | 2018-09-07 | 2020-03-12 | Trustees Of Dartmouth College | C19 scaffolds and steroids and methods of use and manufacture thereof |
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 |
| EP1226155B1 (de) * | 1999-11-02 | 2007-05-02 | Bayer Schering Pharma AG | 18-nor-steroide als selektiv wirksame estrogene |
| AU5834101A (en) * | 2000-04-12 | 2001-10-23 | Schering Ag | 8ss-hydrocarbyl-substituted estratrienes for use as selective estrogens |
-
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 AU AU2003242683A patent/AU2003242683B9/en not_active Ceased
- 2003-06-11 UY UY27844A patent/UY27844A1/es not_active Application Discontinuation
- 2003-06-11 AT AT03757065T patent/ATE303397T1/de active
- 2003-06-11 EA EA200401544A patent/EA008442B1/ru not_active IP Right Cessation
- 2003-06-11 TW TW092115863A patent/TWI286140B/zh not_active IP Right Cessation
- 2003-06-11 ES ES03757065T patent/ES2248770T3/es not_active Expired - Lifetime
- 2003-06-11 WO PCT/EP2003/006172 patent/WO2003104253A2/de not_active Ceased
- 2003-06-11 HR HRP20050009AA patent/HRP20050009B1/hr not_active IP Right Cessation
- 2003-06-11 RS YUP-1070/04A patent/RS50878B/sr unknown
- 2003-06-11 BR BR0312140-2A patent/BR0312140A/pt not_active IP Right Cessation
- 2003-06-11 DE DE50301116T patent/DE50301116D1/de not_active Expired - Lifetime
- 2003-06-11 EP EP03757065A patent/EP1517914B1/de not_active Expired - Lifetime
- 2003-06-11 KR KR1020047020133A patent/KR101006612B1/ko not_active Expired - Fee Related
- 2003-06-11 JP JP2004511321A patent/JP4615998B2/ja not_active Expired - Fee Related
- 2003-06-11 DK DK03757065T patent/DK1517914T3/da active
- 2003-06-11 CN CNB038135027A patent/CN1293090C/zh not_active Expired - Fee Related
- 2003-06-11 PL PL373090A patent/PL209910B1/pl not_active IP Right Cessation
- 2003-06-11 MX MXPA04012491A patent/MXPA04012491A/es active IP Right Grant
- 2003-06-11 AR ARP030102079A patent/AR040188A1/es active IP Right Grant
- 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
- 2005-01-10 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
-
2008
- 2008-09-16 CR CR10289A patent/CR10289A/es not_active Application Discontinuation
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Legal Events
| Date | Code | Title | Description |
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| KB | Patent renewed | ||
| MM9K | Patent not in force due to non-payment of renewal fees |