JP2005533053A5 - - Google Patents
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- Publication number
- JP2005533053A5 JP2005533053A5 JP2004511321A JP2004511321A JP2005533053A5 JP 2005533053 A5 JP2005533053 A5 JP 2005533053A5 JP 2004511321 A JP2004511321 A JP 2004511321A JP 2004511321 A JP2004511321 A JP 2004511321A JP 2005533053 A5 JP2005533053 A5 JP 2005533053A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- amino
- carbon atoms
- aralkyl
- 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.)
- Granted
Links
- 125000004432 carbon atom Chemical group C* 0.000 claims description 13
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 12
- -1 trifluoromethylthio, methoxy, ethoxy Chemical group 0.000 claims description 11
- 125000000217 alkyl group Chemical group 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 8
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 8
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 6
- 229920006395 saturated elastomer Polymers 0.000 claims description 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 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
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 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
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 4
- 125000005111 carboxyalkoxy group Chemical group 0.000 claims description 4
- 229910052801 chlorine Inorganic materials 0.000 claims description 4
- 239000000460 chlorine Substances 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 229910052731 fluorine Inorganic materials 0.000 claims description 4
- 239000011737 fluorine Substances 0.000 claims description 4
- 229910052740 iodine Inorganic materials 0.000 claims description 4
- 239000011630 iodine Substances 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
- 125000001424 substituent group Chemical group 0.000 claims description 4
- 125000003107 substituted aryl group Chemical group 0.000 claims description 4
- 125000002252 acyl 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
- 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 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 229930195734 saturated hydrocarbon Natural products 0.000 claims description 2
- 229930195735 unsaturated hydrocarbon Natural products 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 1
- 150000002154 estra-1,3,5(10)-trienes Chemical class 0.000 claims 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2005533053A JP2005533053A (ja) | 2005-11-04 |
| JP2005533053A5 true JP2005533053A5 (https=) | 2006-01-19 |
| JP4615998B2 JP4615998B2 (ja) | 2011-01-19 |
Family
ID=29723144
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004511321A Expired - Fee Related JP4615998B2 (ja) | 2002-06-11 | 2003-06-11 | 選択的活性エストロゲンとしての9−α置換のエストラトリエン |
Country Status (28)
| Country | Link |
|---|---|
| EP (1) | EP1517914B1 (https=) |
| JP (1) | JP4615998B2 (https=) |
| KR (1) | KR101006612B1 (https=) |
| CN (1) | CN1293090C (https=) |
| AR (1) | AR040188A1 (https=) |
| AT (1) | ATE303397T1 (https=) |
| AU (1) | AU2003242683B9 (https=) |
| BR (1) | BR0312140A (https=) |
| CA (1) | CA2486495C (https=) |
| CR (1) | CR10289A (https=) |
| CU (1) | CU23414B7 (https=) |
| DE (2) | DE10226326A1 (https=) |
| DK (1) | DK1517914T3 (https=) |
| EA (1) | EA008442B1 (https=) |
| EC (1) | ECSP055530A (https=) |
| ES (1) | ES2248770T3 (https=) |
| HR (1) | HRP20050009B1 (https=) |
| IL (1) | IL165321A (https=) |
| MX (1) | MXPA04012491A (https=) |
| NO (1) | NO329563B1 (https=) |
| PE (1) | PE20040613A1 (https=) |
| PL (1) | PL209910B1 (https=) |
| RS (1) | RS50878B (https=) |
| TW (1) | TWI286140B (https=) |
| UA (1) | UA78062C2 (https=) |
| UY (1) | UY27844A1 (https=) |
| WO (1) | WO2003104253A2 (https=) |
| ZA (1) | ZA200500217B (https=) |
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 |
| ES2307064T3 (es) * | 2003-11-26 | 2008-11-16 | Bayer Schering Pharma Aktiengesellschaft | Prevencion y tratamiento de enfermedades cardiacas hipertensivas por los estrogenos selectivos 8beta-vinil-estra-1,3,5(10)-trien-3,17beta-diol y 17beta-fluor-9alfa-vinil-estra-1,3,5(10)-trien-3,16alfa-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 |
| EA018330B1 (ru) * | 2008-02-13 | 2013-07-30 | Байер Интеллекчуал Проперти Гмбх | Система доставки лекарственного средства со стабилизирующим эффектом |
| 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 |
| JP2021535183A (ja) * | 2018-09-07 | 2021-12-16 | トラスティーズ・オヴ・ダートマス・カレッジ | C19骨格およびステロイドならびにそれらの使用および製造方法 |
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 |
| DE50014299D1 (de) * | 1999-11-02 | 2007-06-14 | Bayer Schering Pharma Ag | 18-nor-steroide als selektiv wirksame estrogene |
| BR0109983A (pt) * | 2000-04-12 | 2003-02-25 | Schering Ag | Estratrienos substituìdos por 8.beta-hidrocarbila como estrogênios seletivamente eficientes |
-
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 AT AT03757065T patent/ATE303397T1/de active
- 2003-06-11 DK DK03757065T patent/DK1517914T3/da active
- 2003-06-11 AU AU2003242683A patent/AU2003242683B9/en not_active Ceased
- 2003-06-11 KR KR1020047020133A patent/KR101006612B1/ko not_active Expired - Fee Related
- 2003-06-11 ES ES03757065T patent/ES2248770T3/es not_active Expired - Lifetime
- 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 PL PL373090A patent/PL209910B1/pl not_active IP Right Cessation
- 2003-06-11 BR BR0312140-2A patent/BR0312140A/pt not_active IP Right Cessation
- 2003-06-11 TW TW092115863A patent/TWI286140B/zh not_active IP Right Cessation
- 2003-06-11 UY UY27844A patent/UY27844A1/es not_active Application Discontinuation
- 2003-06-11 EA EA200401544A patent/EA008442B1/ru not_active IP Right Cessation
- 2003-06-11 CN CNB038135027A patent/CN1293090C/zh not_active Expired - Fee Related
- 2003-06-11 HR HRP20050009AA patent/HRP20050009B1/hr not_active IP Right Cessation
- 2003-06-11 CA CA2486495A patent/CA2486495C/en not_active Expired - Fee Related
- 2003-06-11 RS YUP-1070/04A patent/RS50878B/sr unknown
- 2003-06-11 AR ARP030102079A patent/AR040188A1/es active IP Right Grant
- 2003-06-11 MX MXPA04012491A patent/MXPA04012491A/es active IP Right Grant
- 2003-06-11 WO PCT/EP2003/006172 patent/WO2003104253A2/de not_active Ceased
- 2003-06-11 JP JP2004511321A patent/JP4615998B2/ja 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 NO NO20050127A patent/NO329563B1/no not_active IP Right Cessation
- 2005-01-10 EC EC2005005530A patent/ECSP055530A/es unknown
-
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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