EA200201052A1 - 8β-ГИДРОКАРБИЛЗАМЕЩЕННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ - Google Patents
8β-ГИДРОКАРБИЛЗАМЕЩЕННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯInfo
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- EA200201052A1 EA200201052A1 EA200201052A EA200201052A EA200201052A1 EA 200201052 A1 EA200201052 A1 EA 200201052A1 EA 200201052 A EA200201052 A EA 200201052A EA 200201052 A EA200201052 A EA 200201052A EA 200201052 A1 EA200201052 A1 EA 200201052A1
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- Prior art keywords
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- 229940011871 estrogen Drugs 0.000 title 1
- 239000000262 estrogen Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 238000002360 preparation method Methods 0.000 abstract 3
- 210000004291 uterus Anatomy 0.000 abstract 3
- 241000700159 Rattus Species 0.000 abstract 2
- 210000000988 bone and bone Anatomy 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 150000002164 estratrienes Chemical class 0.000 abstract 2
- 102000015694 estrogen receptors Human genes 0.000 abstract 2
- 108010038795 estrogen receptors Proteins 0.000 abstract 2
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 abstract 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 abstract 1
- 206010030247 Oestrogen deficiency Diseases 0.000 abstract 1
- 206010067572 Oestrogenic effect Diseases 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000005466 alkylenyl group Chemical group 0.000 abstract 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000000969 carrier Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000002552 dosage form Substances 0.000 abstract 1
- 230000001076 estrogenic effect Effects 0.000 abstract 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 1
- 239000012634 fragment Substances 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 210000002307 prostate Anatomy 0.000 abstract 1
- 230000004936 stimulating effect Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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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
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- C07J1/0051—Estrane derivatives
- C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
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- C07J1/0051—Estrane derivatives
- C07J1/0062—Estrane derivatives substituted in position 17 alfa not substituted in position 17 beta
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- 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
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- 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
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Abstract
В заявке описаны новые 8β-замещенные эстратриены общей формулы Iв которой R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, Rи Rимеют указанные в описании значения, а Rобозначает необязательно частично или полностью галогенированный алкильный или алкенильный остаток с прямой или разветвленной цепью, содержащий до 5 атомов углерода, этинил или проп-1-инил, как фармацевтические действующие вещества, которые in vitro обладают более высокой аффинностью к эстрогенным рецепторам в препаратах из предстательной железы крыс по сравнению с аффинностью к эстрогенным рецепторам в препаратах из матки крыс и действие которых in vivo преимущественно направлено на костную ткань, а не на матку, и/или которые обладают ярко выраженным действием в отношении стимуляции экспрессии 5НТ-рецепторов и -переносчиков, к получению таких соединений, к их терапевтическому применению и к фармацевтическим лекарственным формам, содержащим эти новые соединения. В заявке описано далее применение этих соединений для лечения обусловленных эстрогенной недостаточностью заболеваний и состояний, а также применение 8β-замещенного эстратриенового структурного фрагмента в общей структуре соединений, которые обладают избирательностью преимущественно в отношении их эстрогенного действия на костную ткань по сравнению с действием на матку.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10019167A DE10019167A1 (de) | 2000-04-12 | 2000-04-12 | Substituierte Estratriene als selektiv wirksame Estrogene |
| US20737000P | 2000-05-26 | 2000-05-26 | |
| PCT/EP2001/004290 WO2001077139A1 (de) | 2000-04-12 | 2001-04-12 | 8.beta.-hydrocarbyl-substituierte estratriene als selektiv wirksame estrogene |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200201052A1 true EA200201052A1 (ru) | 2003-04-24 |
| EA006299B1 EA006299B1 (ru) | 2005-10-27 |
Family
ID=26005365
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200201052A EA006299B1 (ru) | 2000-04-12 | 2001-04-12 | 8β-ГИДРОКАРБИЛЗАМЕЩЕННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US7378404B2 (ru) |
| EP (2) | EP1272504B1 (ru) |
| JP (2) | JP3828423B2 (ru) |
| CN (1) | CN100453549C (ru) |
| AT (2) | ATE363487T1 (ru) |
| AU (3) | AU5834101A (ru) |
| BG (1) | BG107173A (ru) |
| BR (1) | BR0109983A (ru) |
| CA (1) | CA2406177C (ru) |
| CZ (1) | CZ20023382A3 (ru) |
| DE (1) | DE50112561D1 (ru) |
| DK (2) | DK1272504T3 (ru) |
| EA (1) | EA006299B1 (ru) |
| EE (1) | EE200200589A (ru) |
| ES (2) | ES2245694T3 (ru) |
| HR (1) | HRP20020892B1 (ru) |
| HU (1) | HUP0300335A2 (ru) |
| IL (2) | IL152248A0 (ru) |
| MX (1) | MXPA02010066A (ru) |
| NO (2) | NO325337B1 (ru) |
| NZ (1) | NZ543724A (ru) |
| PL (1) | PL207488B1 (ru) |
| PT (1) | PT1272504E (ru) |
| SK (1) | SK14632002A3 (ru) |
| WO (2) | WO2001077138A1 (ru) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU5834101A (en) * | 2000-04-12 | 2001-10-23 | Schering Ag | 8ss-hydrocarbyl-substituted estratrienes for use as selective estrogens |
| DE10027887A1 (de) | 2000-05-31 | 2001-12-13 | Jenapharm Gmbh | Verbindungen mit einer Sulfonamidgruppe und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| DE10039199A1 (de) * | 2000-08-10 | 2002-02-21 | Schering Ag | Kombinationspräparate aus einem ERß selektiven Estrogen und einem SERM oder Antiestrogen |
| GB0020498D0 (en) | 2000-08-18 | 2000-10-11 | Sterix Ltd | Compound |
| DE10151363A1 (de) * | 2001-10-17 | 2003-05-08 | Schering Ag | Somatotrope Therapie |
| DE10226326A1 (de) * | 2002-06-11 | 2004-01-15 | Schering Ag | 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene |
| ES2315455T3 (es) * | 2003-03-27 | 2009-04-01 | Pantarhei Bioscience B.V. | Uso de estrogenos para el tratamiento de infertilidad en maniferos machos. |
| DE10318896A1 (de) * | 2003-04-22 | 2004-11-25 | Schering Ag | 8beta-Vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene |
| PL1689410T3 (pl) * | 2003-11-26 | 2008-10-31 | Bayer Schering Pharma Ag | Sposób zapobiegania i leczenia nadciśnieniowych chorób serca za pomocą selektywnych estrogenów: 8ß-winylo-estra-1,3,5(10)-trien-3,17ß-diolu i 17ß-fluoro-9a-winylo-estra-1,3,5(10)-trien-3,16a-diolu |
| US7534780B2 (en) | 2004-05-21 | 2009-05-19 | Bayer Schering Pharma Aktiengesellschaft | Estradiol prodrugs |
| DE102005057225A1 (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 |
| 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 |
| EP2014672A1 (en) * | 2007-07-12 | 2009-01-14 | Bayer Schering Pharma Aktiengesellschaft | 8-beta-substituted estratrienes as selectively active estrogens |
| WO2009101021A2 (en) * | 2008-02-13 | 2009-08-20 | Bayer Schering Pharma Aktiengesellschaft | Estradiol-containing drug delivery system |
| CN102006857B (zh) * | 2008-02-13 | 2013-06-26 | 拜耳先灵医药股份有限公司 | 具有稳定作用的药物递送系统 |
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| FR2743E (fr) * | 1902-01-11 | 1904-12-15 | Adolphe Ernest Pointe | Panification augmentant le rendement et la digestibilité |
| JPS454059Y1 (ru) * | 1967-11-04 | 1970-02-25 | ||
| JPS454060Y1 (ru) * | 1967-12-11 | 1970-02-25 | ||
| US3501530A (en) * | 1968-02-27 | 1970-03-17 | American Cyanamid Co | Substituted naphthalenones,naphthalenediones and d-homo - beta - nor estra-1,3,5(10),9(11)-tetraenes |
| US3681407A (en) * | 1969-06-18 | 1972-08-01 | American Cyanamid Co | 3-methoxy 8{62 -methylestra 1,3,5(10),9(11)-tetraene-17{62 -carboxylic acid lower alkyl ester and intermediates in the preparation thereof |
| US3806546A (en) * | 1969-06-18 | 1974-04-23 | American Cyanamid Co | Steroid-like compounds and method of synthesis |
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