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1. 发明申请

WO2005116002B1 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 审中-公开
标题翻译： 11-β-羟基类固醇脱氢酶1型抑制剂
公开(公告)号：WO2005116002B1
公开(公告)日：2006-08-24
申请号：PCT/US2005018081
申请日：2005-05-24
申请人： AMGEN INC , BIOVITRUM AB , HENRIKSSON MARTIN , HOMAN EVERT , JOHANSSON LARS , VALLGARDA JERK , WILLIAMS MEREDITH , BERCOT ERIC , FOTSCH CHRISTOPHER H , LI AIWEN , CAI GUOLIN , HUNGATE RANDALL W , YUAN CHESTER CHENGUANG , TEGLEY CHIRSTOPHER , ST JEAN DAVID , HAN NIANHE , HUANG QI , LIU QINGYIAN , BARTBERGER MICHAEL D , MONIZ GEORGE A , FRIZZLE MATTHEW J
发明人： HENRIKSSON MARTIN , HOMAN EVERT , JOHANSSON LARS , VALLGARDA JERK , WILLIAMS MEREDITH , BERCOT ERIC , FOTSCH CHRISTOPHER H , LI AIWEN , CAI GUOLIN , HUNGATE RANDALL W , YUAN CHESTER CHENGUANG , TEGLEY CHIRSTOPHER , ST JEAN DAVID , HAN NIANHE , HUANG QI , LIU QINGYIAN , BARTBERGER MICHAEL D , MONIZ GEORGE A , FRIZZLE MATTHEW J
IPC分类号： C07D277/54 , A61K31/42 , A61K31/426 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P19/10 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , C07D20060101 , C07D263/48 , C07D277/42 , C07D277/60 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/18
CPC分类号： C07D417/06 , C07D263/34 , C07D263/48 , C07D275/03 , C07D277/42 , C07D277/54 , C07D277/60 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/1856
摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): (I) (II), (III), or (IV), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-ß-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-ß-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译：（I），（II），（III）或（IV）的化合物：其中R 1， R 2，R 3，R 4，R 5，R 6，R 6，R 5，R 8，R 8，R 8， R 7，X和Z如本文所定义，并且还涉及包含所述化合物的药物组合物，以及所述化合物用于治疗与人11-β-羟基类固醇相关的病症的方法脱氢酶1型酶和用于制备作用于人类11-β-羟基类固醇脱氢酶1型酶的药物的用途。

2. 发明申请

WO2005116002A2 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 审中-公开
标题翻译： 11-羟基甾体脱氢酶1型抑制剂
公开(公告)号：WO2005116002A2
公开(公告)日：2005-12-08
申请号：PCT/US2005018081
申请日：2005-05-24
申请人： AMGEN INC , BIOVITRUM AB , HENRIKSSON MARTIN , HOMAN EVERT , JOHANSSON LARS , VALLGARDA JERK , WILLIAMS MEREDITH , BERCOT ERIC , FOTSCH CHRISTOPHER H , LI AIWEN , CAI GUOLIN , HUNGATE RANDALL W , YUAN CHESTER CHENGUANG , TEGLEY CHIRSTOPHER , ST JEAN DAVID , HAN NIANHE , HUANG QI , LIU QINGYIAN , BARTBERGER MICHAEL D , MONIZ GEORGE A , FRIZZLE MATTHEW J
发明人： HENRIKSSON MARTIN , HOMAN EVERT , JOHANSSON LARS , VALLGARDA JERK , WILLIAMS MEREDITH , BERCOT ERIC , FOTSCH CHRISTOPHER H , LI AIWEN , CAI GUOLIN , HUNGATE RANDALL W , YUAN CHESTER CHENGUANG , TEGLEY CHIRSTOPHER , ST JEAN DAVID , HAN NIANHE , HUANG QI , LIU QINGYIAN , BARTBERGER MICHAEL D , MONIZ GEORGE A , FRIZZLE MATTHEW J
IPC分类号： A61K31/42 , A61K31/426 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P19/10 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , C07D20060101 , C07D263/48 , C07D277/42 , C07D277/54 , C07D277/60 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/18
CPC分类号： C07D417/06 , C07D263/34 , C07D263/48 , C07D275/03 , C07D277/42 , C07D277/54 , C07D277/60 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/1856
摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): (I) (II), (III), or (IV), wherein R , R , R , R , R , R , R , X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-beta-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-beta-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译：本发明涉及具有式（I），（II），（III）或（IV）：（I）（II），（III）或（IV））的化合物，其中R 1，R 2 R 3，R 4，R 5，R 6，R 7，X 7和Z如本文所定义，并且还涉及包含该化合物的药物组合物，以及使用方法的用于治疗与人类11-β-羟基类固醇脱氢酶1型酶相关的疾病的化合物和用于制备作用于人类11-β-羟基类固醇脱氢酶1型酶的药物。

3. 发明专利

HRP20060456A2 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 未知
公开(公告)号：HRP20060456A2
公开(公告)日：2007-03-31
申请号：HRP20060456
申请日：2006-12-21
申请人： AMGEN , BIOVITRUM AB
发明人： HENRIKSSON MARTIN , HOMAN EVERT , JOHANSSON LARS , VALLGARDA JERK , WILLIAMS MEREDITH , BERCOT ERIC , FOTSCH CRISTOPHER H , LI AIWEN , CAI GOULIN , HUNGATE RANDALL W , YUAN CHESTER CHENGUANG , TEGLEY CHIRSTOPHER , JEAN DAVID ST , HAN NIANHE , HUANG QI , LIU QINGYIAN , BARTBERGER MICHAEL D , MONIZ GEORGE A , FRIZZLE MATTHEW J
IPC分类号： C07D277/54 , A61K31/42 , A61K31/426 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P19/10 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , C07D20060101 , C07D263/48 , C07D277/42 , C07D277/60 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/18
摘要： The disclosure relates to compounds with the formula (III) wherein R5, R6, R7 are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-hydroxysteroid dehydrogenase type 1 enzyme.

4. 发明专利

CA2568186A1 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 未知
公开(公告)号：CA2568186A1
公开(公告)日：2005-12-08
申请号：CA2568186
申请日：2005-05-24
申请人： BIOVITRUM AB , AMGEN INC
发明人： TEGLEY CHIRSTOPHER , YUAN CHESTER CHENGUANG , HAN NIANHE , HENRIKSSON MARTIN , ST JEAN DAVID , HOMAN EVERT , WILLIAMS MEREDITH , FOTSCH CHRISTOPHER H , BERCOT ERIC , CAI GUOLIN , LI AIWEN , VALLGARDA JERK , JOHANSSON LARS , HUANG QI , LIU QINGYIAN , MONIZ GEORGE A , FRIZZLE MATTHEW J , HUNGATE RANDALL W , BARTBERGER MICHAEL D
IPC分类号： C07D277/54 , A61K31/42 , A61K31/426 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P19/10 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , C07D20060101 , C07D263/48 , C07D277/42 , C07D277/60 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/18
摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-&bgr;-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-&bgr;-hydroxysteroid dehydrogenase type 1 enzyme.

5. 发明专利

NZ552284A Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1 未知
公开(公告)号：NZ552284A
公开(公告)日：2010-01-29
申请号：NZ55228405
申请日：2005-05-24
申请人： AMGEN INC , BIOVITRUM AB
发明人： HENRIKSSON MARTIN , HOMAN EVERT , JOHANSSON LARS , VALLGARDA JERK , WILLIAMS MEREDITH , BERCOT ERIC , FOTSCH CHRISTOPHER H , LI AIWEN , CAI GUOLIN , HUNGATE RANDALL W , YUAN CHESTER CHENGUANG , TEGLEY CHRISTOPHER , ST JEAN DAVID , HAN NIANHE , HUANG QI , LIU QINGYIAN , BARTBERGER MICHAEL D , MONIZ GEORGE A , FRIZZLE MATTHEW J
IPC分类号： A61K31/42 , A61K31/426 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P19/10 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , C07D20060101 , C07D263/48 , C07D277/42 , C07D277/54 , C07D277/60 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/18
摘要： The disclosure relates to compounds with the formula (III) wherein R5, R6, R7 are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-hydroxysteroid dehydrogenase type 1 enzyme.

6. 发明专利

DE602005011795D1 未知
公开(公告)号：DE602005011795D1
公开(公告)日：2009-01-29
申请号：DE602005011795
申请日：2005-05-24
申请人： AMGEN INC , BIOVITRUM AB
发明人： HENRIKSSON MARTIN , HOMAN EVERT , JOHANSSON LARS , VALLGARDA JERK , WILLIAMS MEREDITH , BERCOT ERIC , FOTSCH CHRISTOPHER H , LI AIWEN , CAI GUOLIN , HUNGATE RANDALL W , YUAN CHESTER CHENGUANG , TEGLEY CHIRSTOPHER , ST JEAN DAVID , HAN NIANHE , HUANG QI , LIU QINGYIAN , BARTBERGER MICHAEL D , MONIZ GEORGE A , FRIZZLE MATTHEW J
IPC分类号： C07D277/54 , A61K31/42 , A61K31/426 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P19/10 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , C07D20060101 , C07D263/48 , C07D277/42 , C07D277/60 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/18
摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-&bgr;-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-&bgr;-hydroxysteroid dehydrogenase type 1 enzyme.

8. 发明专利

ES2318503T3 INHIBIDORES DE 11-BETA-HIDROXIESTEROIDE DESHIDROGENASA DE TIPO 1. 未知
公开(公告)号：ES2318503T3
公开(公告)日：2009-05-01
申请号：ES05756354
申请日：2005-05-24
申请人： AMGEN INC , BIOVITRUM AB
发明人： HENRIKSSON MARTIN , HOMAN EVERT , JOHANSSON LARS , VALLGARDA JERK , WILLIAMS MEREDITH , BERCOT ERIC
IPC分类号： C07D277/54 , A61K31/42 , A61K31/426 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P19/10 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , C07D20060101 , C07D263/48 , C07D277/42 , C07D277/60 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/18
摘要： Un compuesto de fórmula general (III)** ver fórmula** en la que R5 es fenilo-(CR 10a R 10a ) 1-3- opcionalmente sustituido; y en la que R 10a se selecciona independientemente de H, metilo, fluoro o R 10a y R 10a pueden combinarse conjuntamente formando un anillo cicloalquilo C3-6; R 6 se selecciona de alquilo C 1-8, alcoxi C 1-8, cicloalquilo C 3-10, heterociclilo, cicloalquil C 3-10-alquilo C 1-8, CNalquilo C 1-8, arilo, arilalquilo C 1-8; heterociclilalquilo C 1-8 y haloalquilo; R 7 se selecciona de -NR 8 R 9 , halo, alquilo C1-8, -(CR 8 R 9 )n-OR 8 , -S-alquilo C1-8, cicloalquilo C3-10, heterociclilo, cicloalquil C 3-10-alquilo C 1-8, cianoalquilo C 1-8, arilo, arilalquilo C 1-8, heterociclilalquilo C 1-8, heterociclil-C (O)-alquilo C 1-8, heterociclil-SO 2-alquilo C 1-8, haloalquilo C 1-8, R 8 R 9 N-alquilo C 1-8, HO-alquilo C 1-8, -C(O)cicloalquilo C3-10, -C(O)-haloalquilo C1-8, -(CR 8 R 9 )n-Y-(CR 8 R 9 )n-heterociclilo y -(CR 8 R 9 )n-Y-(CR 8 R 9 )n-C(O)- R 8 (en los que n is 0-5, Y es NR 10 , O o S); en los que cualquier residuo arilo, alquilo, heterociclilo o cicloalquilo está opcionalmente sustituido con uno o más de -alquilo C1-8, -halo, -OH, -OR 10 , -alquil C1-8-SO2-, -SO 2-arilo, -C(O)-(CR 8 R 9 )n-carbamato, -C(O)-O-alquilo C 1-8, -C(O)-alquilo C1-8, -C(O)-(CR 8 R 9 )n-C(O)-NR 8 R 9 , -C(O)-(CR 8 R 9 ) n-NR 8 -C(O)-alquilo C 1-8, -C(O)-(CR 8 R 9 )n-NR 8 R 9 , -C(O)-cicloalquilo C 3-10, -C(O)-arilo, -C(O)-(CR 8 R 9 ) n-heterociclilo, -alquil C1-8-OR 8 , -C(O)-haloalquilo C1-8 o -C(O)-(CR 8 R 9 )n-arilo, en los que cualquier residuo arilo, alquilo, cicloalquilo o heterociclilo está opcionalmente sustituido independientemente con uno o más de alquilo C 1-8, arilo, halógeno, -NR 10 R 10 , haloalquilo C 1-8, HO-alquilo C 1-8, R 8 R 9 N-alquilo C 1-8, alquil C 1-8-OR 10 , -OR 10 , cicloalquilo C 3-10 o alquil C 1-8-sulfonilo, -O-(CR 8 R 9 ) n-heterociclilo, -O-(CR 8 R 9 ) n-C(O)- NR 8 R 9 , -O-(CR 8 R 9 )n-NR 8 R 9 , -Y-(CR 8 R 9 )n-NR 8 -C(O)-alquilo C1-8, -Y-(CR 8 R 9 )n-heterociclilo, -O-(CR 8 R 9 )nNR 8 R 9 o alquil C1-8-SO2; en los que R 8 y R 9 se seleccionan cada uno independientemente de hidrógeno, alquilo C 1-8, alcoxi C 1-8, -NR 10 R 10 , -S-alquilo C1-8, arilo y heterociclilo; cualquier alquilo, alcoxi, heterociclilo o arilo puede estar sustituido con uno a tres sustituyentes seleccionados de halo, alquilo C 1-8 no sustituido, alcoxi C 1-8 no sustituido, tioalcoxi C 1-8 no sustituido y arilalquilo C 1-4 no sustituido; en los que R 10 se selecciona independientemente de hidrógeno, alquilo C1-8, aril C1-8-alquilo, alcoxi C1-8, -Salquilo C1-8, heterociclilo y arilo; cualquier heterociclilo o arilo puede estar sustituido con uno a tres sustituyentes seleccionados de halo, alquilo C1-8 no sustituido, alcoxi C1-8 no sustituido, tioalcoxi C1-8 no sustituido y arilalquilo C1-4 no sustituido; o R 6 y R 7 forman junto con el átomo de carbono unido a los mismos un cicloalquilo C3-10 saturado, parcialmente insaturado o insaturado, o un heterociclilo C 4-14 saturado, parcialmente insaturado o insaturado; en los que el cicloalquilo o el heterociclilo puede estar opcionalmente sustituido con uno o más de alquilo C1-8, arilo, haloalquilo C1-8, arilalquilo C1-8, cicloalquilo C3-10, -OR 8 , =O, =NR 8 , =N-OR 8 , -NR 8 R 9 , -SR 8 , -halo, -OC(O)R 8 , -C(O)R 8 , -CO2R 8 , -CONR 8 R 9 , -OC(O)NR 8 R 9 , -NR 9 C(O)R 8 , NR 8 C(O)NR 8 R 9 , -NR 8 SO2NR 8 R 9 ), -NR 8 CO2R 9 , -NHC (NH 2)=NH, -NR 8 C(NH 2=NH), -NHC(NH 2)NR 8 , -S(O)R 8 , -SO 2R 8 , -SO 2NR 8 R 9 , -NR 8 SO 2R 9 , -CN y -NO 2; y sales, solvatos, hidratos, isómeros geométricos, tautómeros, isómeros ópticos y N-óxidos de los mismos farmacéuticamente aceptables, con la condición de que: cuando R 6 = R 7 = metilo, entonces R 5 no sea fenilo ni 4-yodofenilo, R 6 = R 7 = fenilo, entonces R 5 no sea fenilo y R 6 y R 7 se combinan formando un anillo de ciclopropilo, entonces R 5 no sea n-butilo, ciclohexilo, bencilo, fenilo o naftilo.

9. 发明专利

TNSN06372A1 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 未知
公开(公告)号：TNSN06372A1
公开(公告)日：2008-02-22
申请号：TNSN06372
申请日：2006-11-14
申请人： AMGEN INC , BIOVITRUM AB
发明人： VALLGARDA JERK , WILLIAMS MEREDITH , BERCOT ERIC , FOTSCH CHRISTOPHER H , LI AIWEN , CAI GUOLIN , HUNGATE RANDALL W , YUAN CHESTER CHENGUANG , TEGLEY CHIRSTOPHER , ST JEAN DAVID , HAN NIANHE , HUANG QI , LIU QINGYIAN , BARTBERGER MICHAEL D , MONIZ GEORGE A , FRI , HENRIKSSON MARTIN , JOHANSSON LARS , HOMAN EVERT
IPC分类号： A61K31/42 , A61K31/426 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P19/10 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , C07D20060101 , C07D263/48 , C07D277/54
摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): (I) (II), (III), or (IV), wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11- -hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11- -hydroxysteroid dehydrogenase type 1 enzyme.

10. 发明专利

MY148480A INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 未知
公开(公告)号：MY148480A
公开(公告)日：2013-04-30
申请号：MYPI20052347
申请日：2005-05-24
申请人： AMGEN INC , BIOVITRUM AB
发明人： HENRIKSSON MARTIN , HUNGATE RANDY W , YUAN CHESTER CHENGUANG , TEGLEY CHRIS , JEAN DAVID ST , HAN NIANHE , HUANG QI , LIU QINGYIAN , BARTBERGER MICHAEL , HOMAN EVERT , JOHANSSON LARS , VALLGAARDA JERK , WILLIAMS MEREDITH , BERCOT ERIC , FOTSCH CHRIS , LI AIWEN , CAI GUOLIN
IPC分类号： C07D277/54 , A61K31/42 , A61K31/426 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P19/10 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/12 , C07D20060101 , C07D263/48 , C07D277/42 , C07D277/60 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/18
摘要： THE PRESENT INVENTION RELATES TO COMPOUNDS WITH THE FORMULA (?), (??), (???) OR (?V): WHEREIN R¹, R², R³, R?,R?, R?, R?, X AND Z ARE AS DEFINED HEREIN, AND ALSO TO PHARMACEUTICAL COMPOSITIONS COMPRISING THE COMPOUNDS, AS WELL AS METHODS OF USE OF THE COMPOUNDS FOR TREATMENT OF DISORDERS ASSOCIATED WITH HUMAN 11-?- HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME AND FOR THE PREPARATION OF A MEDICAMENT WHICH ACTS ON THE HUMAN 11-?-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME.

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