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1. 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

2. 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

3. 发明公开

KR20180043837A 페녹시메틸 유도체 审中-公开
公开(公告)号：KR20180043837A
公开(公告)日：2018-04-30
申请号：KR20187009433
申请日：2016-09-01
申请人： HOFFMANN LA ROCHE
发明人： HERT JEROME , HUNZIKER DANIEL , KUEHNE HOLGER , LUEBBERS THOMAS , MARTIN RAINER E , MATTEI PATRIZIO , NEIDHART WERNER , RICHTER HANS , RUDOLPH MARKUS , PINARD EMMANUEL
IPC分类号： C07D249/12 , A61K31/4196 , A61K31/4245 , A61P27/02 , A61P27/06 , C07D403/12 , C07D413/12
CPC分类号： C07D403/12 , C07D231/12 , C07D231/56 , C07D237/14 , C07D249/12 , C07D401/12 , C07D407/04 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07F7/0812
摘要： 본발명은하기화학식 (I)의신규화합물, 상기화합물을포함하는조성물, 및상기화합물의사용방법을제공한다:(I) 상기식에서, R, R, R, R및 W는본원명세서에정의된바와같다.

4. 发明申请

WO2011101304A3 PIPERIDINE DERIVATIVES 审中-公开
标题翻译：哌啶衍生物
公开(公告)号：WO2011101304A3
公开(公告)日：2011-10-20
申请号：PCT/EP2011052101
申请日：2011-02-14
申请人： HOFFMANN LA ROCHE , BAUMANN KARLHEINZ , FLOHR ALEXANDER , GOETSCHI ERWIN , GREEN LUKE , JOLIDON SYNESE , KNUST HENNER , LIMBERG ANJA , LUEBBERS THOMAS , THOMAS ANDREW
发明人： BAUMANN KARLHEINZ , FLOHR ALEXANDER , GOETSCHI ERWIN , GREEN LUKE , JOLIDON SYNESE , KNUST HENNER , LIMBERG ANJA , LUEBBERS THOMAS , THOMAS ANDREW
IPC分类号： C07D401/14 , A61K31/4523 , A61P25/28 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
CPC分类号： C07D471/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04
摘要： The invention relates to compounds of formula (I). Hetaryl I is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; hetaryl II is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N, or is a two membered ring system containing 1 to 4 heteroatoms selected from S, O or N, wherein at least one ring is aromatic in nature; R1 is lower alkyl, lower alkoxy, lower alkyl substituted by halogen, or halogen; R2 is halogen, lower alkyl, lower alkoxy, hydroxy, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy or benzo[1,3]dioxolyl, or is -(CHR)p-phenyl, optionally substituted by halogen, lower alkyl, lower alkoxy, S(O)2-lower alkyl, cyano, nitro, lower alkoxy substituted by halogen, dimethylamino, -(CH2)P-NHC(O)O-Iower alkyl, or lower alkyl substituted by halogen, and R is hydrogen, halogen, hydroxy or lower alkoxy, or is cycloalkenyl or cycloalkyl, optionally substituted by hydroxy or lower alkyl substituted by halogen, or is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N, which is optionally substituted by halogen, lower alkyl, lower alkoxy or dimethylamino, or is O-phenyl, optionally substituted by halogen, or is heterocycloalkyl, optionally substituted by halogen, hydroxy, lower alkyl substituted by halogen or C(O)O-lower alkyl; R3 is hydrogen, lower alkyl, cyano or phenyl; R4 is lower alkoxy, lower alkyl or halogen; p is 0 or 1; n is 0, 1 or 2; if n is 2 then R4 may be the same or different; m is 0, 1 or 2; if m is 2 then R1 may be the same or different; o is 0, 1, 2 or 3, if o is 2 or 3 then R2 may be the same or different; or to pharmaceutically active acid addition salts thereof. The compounds of formula (I) are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ß-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
摘要翻译：本发明涉及式（I）化合物。芳基I是含有1至3个选自O，S或N的杂原子的五或六元杂芳基; 杂芳基II是含有1至3个选自O，S或N的杂原子的五或六元杂芳基，或是含有1至4个选自S，O或N的杂原子的二元环体系，其中至少一个环本质上是芳香的 R1是低级烷基，低级烷氧基，被卤素取代的低级烷基或卤素; R 2为卤素，低级烷基，低级烷氧基，羟基，被卤素取代的低级烷基，被羟基或苯并[1,3]二氧杂环戊烯取代的低级烷基，或为 - （CHR）对 - 苯基，任选被卤素，低级烷基，低级烷氧基，S（O）2-低级烷基，氰基，硝基，被卤素取代的低级烷氧基，二甲基氨基， - （CH2）P-NHC（O）O-低级烷基或被卤素取代的低级烷基，R是氢，卤素，羟基或低级烷氧基，或是任选被羟基或被卤素取代的低级烷基取代的环烯基或环烷基，或是含有1至3个选自O，S或N的杂原子的五或六元杂芳基，其中或任选被卤素取代的O-苯基，或任选被卤素取代的杂环烷基，羟基，被卤素或C（O）O-低级烷基取代的低级烷基， ; R3是氢，低级烷基，氰基或苯基; R4是低级烷氧基，低级烷基或卤素; p为0或1; n为0,1或2; 如果n为2，则R4可以相同或不同; m为0,1或2; 如果m为2，则R1可以相同或不同; o为0,1,2或3，如果o为2或3，则R2可以相同或不同; 或其药物活性的酸加成盐。式（I）化合物是淀粉样蛋白β的调节剂，因此它们可用于治疗或预防与脑中β-淀粉样蛋白沉积相关的疾病，特别是阿尔茨海默病，以及其他疾病如脑淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆和唐氏综合征。

5. 发明申请

WO2004013120A8 NOVEL BENZODIOXOLES 审中-公开
标题翻译：新的胆甾醇
公开(公告)号：WO2004013120A8
公开(公告)日：2005-04-14
申请号：PCT/EP0307890
申请日：2003-07-18
申请人： HOFFMANN LA ROCHE
发明人： ALANINE ALEXANDER , BLEICHER KONRAD , GUBA WOLFGANG , HAAP WOLFGANG , KUBE DAGMAR , LUEBBERS THOMAS , PLANCHER JEAN-MARC , ROGERS-EVANS MARK , SCHNEIDER GISBERT , ZUEGGE JOCHEN , ROCHE OLIVIER
IPC分类号： A61K31/36 , C07D317/46 , C07D317/54 , C07D317/62 , C07D317/72 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D417/06 , C07D451/06 , C07D491/10
CPC分类号： C07D317/46 , C07D317/72 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D417/06 , C07D451/06 , C07D491/10
摘要： The present invention relates to compound of formula (I) wherein R , R , R , R , R , R , R , and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases, which are associated with the modulation of CB1 receptors.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和X分别为如在说明书和权利要求书中所定义的，及其药学上可接受的盐。该化合物可用于治疗和/或预防与调节CB1受体相关的疾病。

6. 发明申请

WO2013120921A1 NOVEL PYRROLIDINE DERIVATIVES 审中-公开
标题翻译：新型吡咯烷衍生物
公开(公告)号：WO2013120921A1
公开(公告)日：2013-08-22
申请号：PCT/EP2013052914
申请日：2013-02-14
申请人： HOFFMANN LA ROCHE , BANNER DAVID , HAAP WOLFGANG , LUEBBERS THOMAS , PETERS JENS-UWE
发明人： BANNER DAVID , HAAP WOLFGANG , LUEBBERS THOMAS , PETERS JENS-UWE
IPC分类号： C07D401/14 , A61K31/401 , A61P3/00 , C07D403/06 , C07D405/14 , C07D409/14 , C07D417/08 , C07D417/14
CPC分类号： C07D417/14 , C07D207/10 , C07D401/14 , C07D403/06 , C07D403/08 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/08
摘要： The invention relates to a compound of formula (I) wherein A1 to A3 and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
摘要翻译：本发明涉及式（I）化合物，其中A1至A3和R1至R3如在说明书和权利要求书中所定义。式（I）化合物可以用作药物。

7. 发明申请

WO2007090749A3 BENZAMIDE AND HETEROARENE DERIVATIVES AS CETP INHIBITORS 审中-公开
标题翻译：苯并恶嗪衍生物作为CETP抑制剂
公开(公告)号：WO2007090749A3
公开(公告)日：2007-11-29
申请号：PCT/EP2007050812
申请日：2007-01-29
申请人： HOFFMANN LA ROCHE , FAEH CHRISTOPH , KUEHNE HOLGER , LUEBBERS THOMAS , MATTEI PATRIZIO , MAUGEAIS CYRILLE , PFLIEGER PHILIPPE
发明人： FAEH CHRISTOPH , KUEHNE HOLGER , LUEBBERS THOMAS , MATTEI PATRIZIO , MAUGEAIS CYRILLE , PFLIEGER PHILIPPE
IPC分类号： C07D213/40 , A61K31/4402 , C07D213/82 , C07D233/28 , C07D233/58 , C07D233/60 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D405/12 , C07D213/40 , C07D213/82 , C07D277/28 , C07D333/58 , C07D333/60 , C07D401/12 , C07D409/12 , C07D417/12
摘要： Compounds of formula (I) processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
摘要翻译：式（I）化合物的制备方法，它们作为药物的用途以及包含它们的药物组合物。

8. 发明申请

WO2007000392A3 CHLORO-SUBSTITUTED GUANIDINES 审中-公开
标题翻译：氯取代的瓜氨酸
公开(公告)号：WO2007000392A3
公开(公告)日：2007-04-05
申请号：PCT/EP2006063267
申请日：2006-06-16
申请人： HOFFMANN LA ROCHE , ALANINE ALEXANDER , GOBBI LUCA CLAUDIO , KOLCZEWSKI SABINE , LUEBBERS THOMAS , PETERS JENS-UWE , STEWARD LUCINDA
发明人： ALANINE ALEXANDER , GOBBI LUCA CLAUDIO , KOLCZEWSKI SABINE , LUEBBERS THOMAS , PETERS JENS-UWE , STEWARD LUCINDA
IPC分类号： C07D239/84 , A61K31/517 , A61P25/18 , A61P25/24
CPC分类号： C07D239/42 , C07D403/12 , C07D405/12
摘要： The present invention relates to compounds of formula wherein R 1 is hydrogen or halogen; R 2 is lower alkyl; R 3 is hydrogen, lower alkyl, -(CH 2 ) n -cycloalkyl, -(CH 2 ) n -phenyl optionally substituted by halogen, or is lower alkyl substituted by halogen, or is -(CH 2 ) n -heterocyclyl, -(CH 2 ) n N-di-lower alkyl, -(CH 2 ) n NHC(O)-lower alkyl, adamantly or -(CH 2 ) n -O-lower alkyl; n is 0, 1, 2 or 3; and pharmaceutically acceptable acid addition salts and tautomers thereof. It has been found that the compounds of formula I have a good activity on the 5-HT 5A receptor. Therefore, the invention provides the use of a compound of formula I or a pharmaceutically acceptable salt thereof for the treatment of diseases, related to this 15 receptor.
摘要翻译：本发明涉及下式的化合物：其中R 1是氢或卤素; R 2是低级烷基; R 3是氢，低级烷基， - （CH 2 SUB）n - 环烷基， - （CH 2 SUB）任选被卤素取代的苯基或被卤素取代的低级烷基，或为 - （CH 2）n - 杂环基， - （（C 1 -C 4）（CH 2）n C（O） - （CH 2）n C（O） - （CH 2）低级烷基，金刚烷基或 - （CH 2）n -O-低级烷基; n是0,1,2或3; 及其药学上可接受的酸加成盐和互变异构体。已经发现式I化合物对5-HT 5A受体具有良好的活性。因此，本发明提供了式I化合物或其药学上可接受的盐在治疗与该受体有关的疾病中的用途。

9. 发明申请

WO2006066747A8 4-AMINOPIPERIDINE DERIVATIVES 审中-公开
标题翻译： 4-氨基哌啶衍生物
公开(公告)号：WO2006066747A8
公开(公告)日：2006-09-28
申请号：PCT/EP2005013292
申请日：2005-12-12
申请人： HOFFMANN LA ROCHE , BOEHRINGER MARKUS , HUNZIKER DANIEL , KUHN BERND , LOEFFLER BERND MICHAEL , LUEBBERS THOMAS , RICKLIN FABIENNE
发明人： BOEHRINGER MARKUS , HUNZIKER DANIEL , KUHN BERND , LOEFFLER BERND MICHAEL , LUEBBERS THOMAS , RICKLIN FABIENNE
IPC分类号： C07D211/58 , A61K31/4468 , A61K31/45 , C07D211/60 , C07D277/04
CPC分类号： C07D211/58 , C07D211/60 , C07D277/04
摘要： The present invention relates to compounds of the formula (I), wherein R 1 and R 2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/ or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, non-insulin dependent diabetes mellitus and/or impaired glucose tolerance, obesity, and/or metabolic syndrome or ß-cell protection.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 2如在说明书和权利要求书中所定义，及其药学上可接受的盐。所述化合物可用于治疗和/或预防与DPP-IV相关的疾病，例如糖尿病，非胰岛素依赖性糖尿病和/或葡萄糖耐量异常，肥胖症和/或代谢综合征或β细胞保护。

10. 发明专利

AU2016316717B2 Phenoxymethyl derivatives 未知
公开(公告)号：AU2016316717B2
公开(公告)日：2021-02-18
申请号：AU2016316717
申请日：2016-09-01
申请人： HOFFMANN LA ROCHE
发明人： HERT JEROME , HUNZIKER DANIEL , KUEHNE HOLGER , LUEBBERS THOMAS , MARTIN RAINER E , MATTEI PATRIZIO , NEIDHART WERNER , RICHTER HANS , RUDOLPH MARKUS , PINARD EMMANUEL
IPC分类号： C07D403/12 , A61P27/02 , C07D231/12 , C07D231/56 , C07D237/14 , C07D249/12 , C07D401/12 , C07D407/04 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07F7/08
摘要： The invention provides novel compounds having the general formula (I), wherein R

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