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1. 发明专利

JP2013056894A Anthranilamide/2-amino-heteroarene carboxamide derivative 审中-公开
标题翻译：苯胺甲酰胺/ 2-氨基异恶唑羧酰胺衍生物
公开(公告)号：JP2013056894A
公开(公告)日：2013-03-28
申请号：JP2012226826
申请日：2012-10-12
申请人： F Hoffmann La Roche Ag , エフ.ホフマン−ラロシュアーゲーF. Hoffmann−La Roche Aktiengesellschaft
发明人： CONTE AURELIA , KUEHNE HOLGER , LUEBBERS THOMAS , MATTEI PATRIZIO , MAUGEAIS CYRILLE , MUELLER WERNER , PFLIEGER PHILIPPE
IPC分类号： C07C237/30 , A61K31/166 , A61K31/192 , A61K31/216 , A61K31/275 , A61K31/381 , A61K31/415 , A61K31/417 , A61K31/425 , A61K31/426 , A61K31/4418 , A61K31/4427 , A61K31/455 , A61K31/4965 , A61K31/50 , A61K31/505 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P43/00 , C07C231/02 , C07C237/32 , C07C237/34 , C07C237/42 , C07C253/30 , C07C255/24 , C07C255/57 , C07C269/06 , C07C271/28 , C07C303/30 , C07C303/40 , C07C309/66 , C07C311/08 , C07D213/61 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/16 , C07D233/64 , C07D237/24 , C07D239/32 , C07D241/28 , C07D261/14 , C07D263/38 , C07D275/02 , C07D277/20 , C07D277/42 , C07D333/38 , C07D401/12 , C07F7/12
CPC分类号： C07D213/82 , C07C237/30 , C07C237/32 , C07C255/25 , C07C255/54 , C07C271/28 , C07C309/66 , C07C311/08 , C07C2601/02 , C07C2601/04 , C07C2601/06 , C07D231/14 , C07D261/18 , C07D275/03 , C07D333/38 , C07D401/12 , C07D403/12 , C07F7/0818
摘要： PROBLEM TO BE SOLVED: To provide novel anthranilamide and 2-amino-heteroarene carboxamide derivatives useful as cholesteryl ester transfer protein (CETP) inhibitors; methods for producing the same; use thereof as pharmaceuticals; and pharmaceutical compositions including the same.SOLUTION: The novel anthranilamide and 2-amino-heteroarene carboxamide derivatives are compounds typified by 5-chloro-N-(4-cyclopentyl-benzyl)-2-isopropylamino-N-[2-(3-trifluoromethyl-phenyl)-ethyl]-benzamide or N-(4-tert-butyl-benzyl)-N-2-(3,4-dichloro-phenyl)-ethyl-2-methylamino-nicotinamide and represented by formula I.
摘要翻译：要解决的问题：提供用作胆固醇酯转移蛋白（CETP）抑制剂的新型邻氨基苯甲酰胺和2-氨基 - 杂芳酰胺酰胺衍生物; 生产方法; 作为药物使用; 和包含其的药物组合物。解决方案：新颖的邻氨基苯甲酰胺和2-氨基 - 杂芳酰胺衍生物是以5-氯-N-（4-环戊基 - 苄基）-2-异丙基氨基-N- [2-（3-三氟甲基 - 苯基） - 乙基] - 苯甲酰胺或N-（4-叔丁基 - 苄基）-N-2-（3,4-二氯 - 苯基） - 乙基-2-甲基氨基 - 烟酰胺，由式I表示。（C）2013，JPO＆INPIT

2. 发明专利

JP2012246303A Benzamide and heteroarene derivative 审中-公开
标题翻译：苯并恶嗪衍生物
公开(公告)号：JP2012246303A
公开(公告)日：2012-12-13
申请号：JP2012180374
申请日：2012-08-16
申请人： F Hoffmann La Roche Ag , エフ.ホフマン−ラロシュアーゲーF. Hoffmann−La Roche Aktiengesellschaft
发明人： CONTE AURELIA , KUEHNE HOLGER , LUEBBERS THOMAS , MATTEI PATRIZIO , MAUGEAIS CYRILLE , MUELLER WERNER , PFLIEGER PHILIPPE
IPC分类号： C07C233/65 , A61K31/166 , A61K31/415 , A61K31/44 , A61K31/455 , A61K31/505 , A61K31/695 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/04 , A61P9/10 , A61P9/12 , A61P43/00 , C07C233/66 , C07C233/73 , C07D213/81 , C07D213/82 , C07D233/68 , C07D239/28
CPC分类号： C07C233/66 , C07C233/65 , C07C233/73 , C07C2601/02 , C07C2601/04 , C07D213/40 , C07D213/61 , C07D213/81 , C07D213/82 , C07D231/16 , C07D239/28 , C07F7/0818
摘要： PROBLEM TO BE SOLVED: To provide novel benzamide and heteroarene derivatives, methods for producing them, use of them as pharmaceuticals, and pharmaceutical compositions including them.SOLUTION: Compounds represented by formula (I) and pharmaceutically acceptable salts thereof are provided. In the formula: Ris 1-6C alkyl or the like; Ris hydrogen or the like; Ris hydrogen, 1-6C alkyl or the like, Ris hydrogen or the like; A is CRor N, B is CRor N, and D is CRor N where -B=A- and -A=D- are not -N=N-, Ris hydrogen, 1-6C alkyl or the like, and Rand Rare hydrogen or the like; and n is 1, 2, or 3.
摘要翻译：要解决的问题：提供新的苯甲酰胺和杂芳烃衍生物，其制备方法，它们作为药物的用途，以及包括它们的药物组合物。解决方案：提供由式（I）表示的化合物及其药学上可接受的盐。在下式中：R 1 = C 1-6烷基等; R 2 是氢等; 4 是氢，1-6C烷基等，R 4是氢或类似物; A为CR 10 或N，B为CR 11 或N，D为CR 3 或N其中-B = A-和-A = D-不是-N = N-，R 3是氢，1-6C烷基或例如，R 10 和R 11 是氢等; 而且n为1,2或3.版权所有（C）2013，JPO＆INPIT

3. 发明专利

CA2640662C TRIALKYLSILYLBENZYLAMINOCARBOXYINDOLES, INDAZOLES AND INDOLINES AND THEIR USE IN TREATING CETP-MEDIATED DISORDERS 未知
公开(公告)号：CA2640662C
公开(公告)日：2014-04-22
申请号：CA2640662
申请日：2007-01-29
申请人： HOFFMANN LA ROCHE
发明人： CONTE AURELIA , KUEHNE HOLGER , LUEBBERS THOMAS , MATTEI PATRIZIO , MAUGEAIS CYRILLE , MUELLER WERNER , PFLIEGER PHILIPPE
IPC分类号： C07F7/10 , A61K31/695 , C07F7/08
摘要： Compounds of formula (I) their manufacture, pharmaceutical compositions containing them and their use as medicaments in the treatment and /or prophylaxis of diseases mediated by cholesteryl ester transfer protein (CETP).

4. 发明专利

CA2637771C ANTHRANILAMIDE/2-AMINO-HETEROARENE CARBOXAMIDE DERIVATIVES 未知
公开(公告)号：CA2637771C
公开(公告)日：2014-04-22
申请号：CA2637771
申请日：2007-01-29
申请人： HOFFMANN LA ROCHE
发明人： CONTE AURELIA , KUEHNE HOLGER , LUEBBERS THOMAS , MATTEI PATRIZIO , MAUGEAIS CYRILLE , MUELLER WERNER , PFLIEGER PHILIPPE
IPC分类号： C07D213/82 , A61K31/44 , A61P3/00 , C07C237/32 , C07D231/14 , C07D261/18 , C07D275/02 , C07D333/38 , C07D401/12 , C07D403/12
摘要： Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.

5. 发明专利

BRPI0707703A2 未知
公开(公告)号：BRPI0707703A2
公开(公告)日：2011-05-10
申请号：BRPI0707703
申请日：2007-01-29
申请人： HOFFMANN LA ROCHE
发明人： KUEHNE HOLGER , LUEBBERS THOMAS , MATTEI PATRIZIO , MAUGEAIS CYRILLE , MUELLER WERNER , PFLIEGER PHILIPPE , CONTE AURELIA
IPC分类号： C07C233/65 , A61K31/166 , C07C233/66 , C07C233/73 , C07D213/40 , C07D213/61 , C07D213/81 , C07D213/82 , C07D231/16 , C07D239/28 , C07F7/08
摘要： Compounds of formula I wherein R1, R2, R4, R5, A, B, D and n are as defined, and pharmaceutically acceptable salts thereof, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them.

6. 发明专利

ES2355600T3 TRIALQUILSILILBENCILAMINOCARBOXIINDOLES, INDAZOLES E INDOLINAS Y SU EMPLEO EN EL TRATAMIENTO DE TRASTORNOS MEDIADOS POR CETP. 未知
公开(公告)号：ES2355600T3
公开(公告)日：2011-03-29
申请号：ES07712128
申请日：2007-01-29
申请人： HOFFMANN LA ROCHE
发明人： CONTE AURELIA , KUEHNE HOLGER , LUEBBERS THOMAS , MATTEI PATRIZIO , MAUGEAIS CYRILLE , MUELLER WERNER , PFLIEGER PHILIPPE
IPC分类号： A61K31/695 , A61P9/10 , C07F7/08
摘要： Un compuesto de la fórmula I **(Ver fórmula)** en la que-X-Y- es -CRa=CRc- o -CRa=N- o -CRaRb-CRcRd-, en los que Ra, Rb, Rc y Rd se eligen con independencia entre sí entre el grupo formado por hidrógeno y alquilo C1-C8;R1, R2, R4 y R5 se eligen con independencia entre sí entre el grupo formado por hidrógeno, alquilo C1-C8, alcoxi C1-C8, halógeno y halógeno-alquilo C1-C8;R3es Si(alquilo C1-C6)3; R6se elige entre el grupo formado por hidrógeno y alquilo C1-C8; R7se elige entre el grupo formado por hidrógeno, alquilo C1-C8, hidroxi y halógeno; R8se elige entre el grupo formado por alquilo C1-C8, alquenilo C2-C8, halógeno-alquilo C1-C8, heterociclilo, heteroarilo, que está sin sustituir o sustituido por uno o dos grupos elegidos con independencia entre alquilo C1-C8, alcoxi C1-C8, halógeno-alquilo C1-C8, halógeno-alcoxi C1-C8 y halógeno, fenilo, que está sin sustituir o sustituido por uno o dos grupos elegidos con independencia entre alquilo C1-C8, alcoxi C1-C8, halógeno-alquilo C1-C8, halógeno-alcoxi C1-C8 y halógeno, -OR12, en el que R12 es alquilo C1-C8 o fenilo, que está sin sustituir o sustituido por uno o dos grupos elegidos con independencia entre alquilo C1-C8, alcoxi C1-C8, halógeno-alquilo C1-C8, halógeno-alcoxi C1-C8 y halógeno, -NR13R14, en el que R13 y R14 con independencia entre sí se eligen entre hidrógeno, alquilo C1-C8, y fenilo, que está sin sustituir o sustituido por uno o dos grupos elegidos con independencia entre alquilo C1-C8, alcoxi C1-C8, halógeno-alquilo C1-C8, halógeno-alcoxi C1-C8 y halógeno, y -C(O)-OR15, en el que R15 es hidrógeno o alquilo C1-C8; R9, R10 y R11 con independencia entre sí se eligen entre el grupo formado por hidrógeno, alquilo C1-C8, cicloalquilo, alcoxi C1-C8, halógeno-alquilo C1-C8 y halógeno;nes el número 1, 2 ó 3; y todas sus sales farmacéuticamente aceptables.

7. 发明专利

DE602007011398D1 TRIALKYLSILYLBENZYLAMINOCARBOXYINDOLE, INDAZOLE UND INDOLINE UND IHRE VERWENDUNG ZUR BEHANDLUNG VON CETP-VERMITTELTEN ERKRANKUNGEN 未知
公开(公告)号：DE602007011398D1
公开(公告)日：2011-02-03
申请号：DE602007011398
申请日：2007-01-29
申请人： HOFFMANN LA ROCHE
发明人： CONTE AURELIA , KUEHNE HOLGER , LUEBBERS THOMAS , MATTEI PATRIZIO , MAUGEAIS CYRILLE , MUELLER WERNER , PFLIEGER PHILIPPE
IPC分类号： A61K31/695 , A61P9/10 , C07F7/08

8. 发明专利

CA2754176A1 2,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS 未知
公开(公告)号：CA2754176A1
公开(公告)日：2010-09-30
申请号：CA2754176
申请日：2010-03-23
申请人： HOFFMANN LA ROCHE
发明人： HUNZIKER DANIEL , LERNER CHRISTIAN , MUELLER WERNER , OBST SANDER ULRIKE , PFLIEGER PHILIPPE , WALDMEIER PIUS
IPC分类号： C07D213/63 , A61K31/536 , A61K31/5415 , A61P3/10 , C07C255/53 , C07D235/26 , C07D263/58 , C07D265/36 , C07D285/14 , C07D317/46 , C07D317/54 , C07D401/12 , C07D413/12 , C07D455/02 , C07D498/04
摘要： The present invention relates to compounds of formula (I), wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically 5 acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.

9. 发明专利

AU2007213831B2 Benzamide and heteroarene derivatives 未知
公开(公告)号：AU2007213831B2
公开(公告)日：2010-07-01
申请号：AU2007213831
申请日：2007-01-29
申请人： HOFFMANN LA ROCHE
发明人： KUEHNE HOLGER , CONTE AURELIA , MUELLER WERNER , MAUGEAIS CYRILLE , PFLIEGER PHILIPPE , MATTEI PATRIZIO , LUEBBERS THOMAS
IPC分类号： C07C233/65 , A61K31/166 , A61K31/4402 , A61K31/4409 , A61K31/455 , A61K31/506 , C07C233/66 , C07C233/73 , C07D213/40 , C07D213/61 , C07D213/81 , C07D213/82 , C07D231/16 , C07D239/28 , C07F7/08
摘要： Compounds of formula I wherein R1, R2, R4, R5, A, B, D and n are as defined, and pharmaceutically acceptable salts thereof, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them.

10. 发明专利

DE60320529T2 未知
公开(公告)号：DE60320529T2
公开(公告)日：2009-06-10
申请号：DE60320529
申请日：2003-01-27
申请人： HOFFMANN LA ROCHE
发明人： MATTEI PATRIZIO , MUELLER WERNER , NEIDHART WERNER , NETTEKOVEN MATTHIAS HEINRICH , PFLIEGER PHILIPPE
IPC分类号： A61K31/4709 , A61K31/365 , A61K31/4725 , A61K31/5377 , A61K31/55 , A61K45/00 , A61P1/14 , A61P3/04 , A61P3/10 , A61P9/00 , A61P13/12 , A61P19/02 , A61P43/00 , C07D215/42 , C07D215/46 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12
摘要： Compounds of general formula Ias well as pharmaceutically acceptable salts and esters thereof, are potent inhibitors of neuropeptide Y and can be used in the form of pharmaceutical preparations for the treatment or prevention of various disease states and related morbidities including obesity.

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