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1. 发明申请

WO2006000324A2 NEW MAO-B INHIBITORS 审中-公开
标题翻译：新MAO-B抑制剂
公开(公告)号：WO2006000324A2
公开(公告)日：2006-01-05
申请号：PCT/EP2005006398
申请日：2005-06-15
申请人： HOFFMANN LA ROCHE , JOLIDON SYNESE , RODRIGUEZ-SARMIENTO ROSA MARIA , THOMAS ANDREW WILLIAM , WOSTL WOLFGANG , WYLER RENE
发明人： JOLIDON SYNESE , RODRIGUEZ-SARMIENTO ROSA MARIA , THOMAS ANDREW WILLIAM , WOSTL WOLFGANG , WYLER RENE
IPC分类号： C07C233/00 , A61K31/165 , A61K31/277 , C07C235/20 , C07C255/54
CPC分类号： C07C255/54 , C07C235/20
摘要： The invention relates to compounds of the general formula (I), wherein R 1 , R 2 are independently from each other hydrogen or C l -C 6 -alkyl; R 3 , R 4 are independently from each other hydrogen or C 1 -C 6 -alkyl; R 5 is halogen, CN, (C 1 -C 6 )-alkyl or (C 1 -C 6 )-alkoxy; n, m or o is 0, 1 or 2; as well as to their pharmaceutically acceptable salts. The compounds may be used for the treatment and prevention of Alzheimer's disease or senile dementia.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1，R 2，2彼此独立地为氢或C 1〜 ç_{6 - 烷基; R 3，R 4，R 4彼此独立地为氢或C 1 -C 6 - 烷基; R 5是卤素，CN，（C 1 -C 6 - ） - 烷基或（C 1 -C 6 - _{6 ） - 烷氧基; n，m或o为0,1或2; 以及它们的药学上可接受的盐。该化合物可用于治疗和预防阿尔茨海默病或老年痴呆。}}

2. 发明申请

WO0240487A3 BENZODIAZEPINE DERIVATIVES AS GABA A RECEPTOR MODULATORS 审中-公开
标题翻译：作为GABA受体调节剂的苯二氮卓衍生物
公开(公告)号：WO0240487A3
公开(公告)日：2002-09-26
申请号：PCT/EP0112887
申请日：2001-11-08
申请人： HOFFMANN LA ROCHE
发明人： MASCIADRI RAFFAELLO , THOMAS ANDREW WILLIAM , WICHMANN JUERGEN
IPC分类号： A61K31/55 , A61K31/5517 , A61P25/00 , A61P25/28 , A61P43/00 , C07D487/14
CPC分类号： C07D487/14
摘要： The present invention relates to compounds of formula (I), wherein R is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, cyano, trifluoromethyl, trifluoromethoxy or lower alkylthio; R is -C(O)O-lower alkyl, isoxazol, 1,2,4-oxadiazol-3-yl or 1,2,4-oxadiazol-5-yl, which rings may be substituted by lower alkyl, trifluoromethyl or cycloalkyl; R is hydrogen, lower alkyl, -(CH2)n-cycloalkyl, -(CH2)n-halogen, -(CH2)n-pyridin-4-yl, or -(CH2)n-phenyl, wherein the phenyl ring may be substituted by one or two substituents selected from the group consisting of lower alkoxy, halogen, -SO2CH3, phenyl, OCF3, nitro, CF3, -NR2, or is -(CH2)n-indolyl, optionally substituted by lower alkyl or lower alkoxy, or is pyrrolidinyl-5-oxo, -C(O)-NR2, -(CH2)n-OH, -(CH2)n-NR2 or -(CH2)n-benzo[1,3]dioxole; R is hydrogen or lower alkyl; and n is 0, 1, 2 or 3; and to their pharmaceutically acceptable acid addition salts. These compounds have a good affinity to the GABA A alpha 5 receptor and they are therefore useful for the treatment of diseases, related to this receptor.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，卤素，低级烷基，低级烷氧基，羟基，氰基，三氟甲基，三氟甲氧基或低级烷硫基; R 2是-C（O）O-低级烷基，异恶唑，1,2,4-恶二唑-3-基或1,2,4-恶二唑-5-基，该环可以被低级烷基取代，三氟甲基或环烷基; （CH 2）n - 卤素， - （CH 2）n - 吡啶-4-基或 - （CH 2）n - 苯基，其中苯基环可以被一个或两个选自低级烷氧基，卤素，-SO 2 CH 3，苯基，OCF 3，硝基，CF 3，-NR 2或是 - （CH 2）n - 吲哚基的取代基取代，任选被低级烷基或低级烷氧基或吡咯烷基-5-氧代-C（O）-NR2， - （CH2）n-OH， - （CH2）n-NR2或 - （CH2）n-苯并[1,3] R是氢或低级烷基; 并且n为0,1,2或3; 及其药学上可接受的酸加成盐。这些化合物对GABA Aα5受体具有良好的亲和力，因此它们可用于治疗与该受体有关的疾病。

3. 发明申请

WO03099763A8 N-ACYLAMINOBENZENE DERVATIVES AS SELECTIVE MONOAMINE OXIDASE B INHIBITORS 审中-公开
标题翻译：作为选择性单胺氧化酶B抑制剂的N-亚氨基苯甲酸衍生物
公开(公告)号：WO03099763A8
公开(公告)日：2004-03-18
申请号：PCT/EP0305297
申请日：2003-05-20
申请人： HOFFMANN LA ROCHE
发明人： JOLIDON SYNESE , RODRIGUEZ SARMIENTO ROSA MARIA , THOMAS ANDREW WILLIAM , WYLER RENE
IPC分类号： A61P3/00 , A61K31/15 , A61K31/167 , A61K31/216 , A61K31/275 , A61P3/04 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P29/00 , A61P43/00 , C07C231/02 , C07C233/15 , C07C233/25 , C07C233/33 , C07C233/60 , C07C235/16 , C07C237/04 , C07C237/22 , C07C243/14 , C07C243/28 , C07C255/19 , C07C255/23 , C07C255/25 , C07C255/58 , C07C259/06 , C07C323/41
CPC分类号： C07C259/06 , C07C233/15 , C07C233/25 , C07C233/33 , C07C233/60 , C07C235/16 , C07C237/04 , C07C237/22 , C07C243/14 , C07C243/28 , C07C255/19 , C07C255/23 , C07C255/25 , C07C323/41 , C07C2601/02
摘要： This invention relates to N-acylamino aryl derivatives of the general formula (I), wherein R is halogen, halogen-(C1-C6)-alkyl, cyano, C1-C6-alkoxy or halogen-(C1-C6)-alkoxy; R , R , R and R independently from each other are selected from the group consisting of hydrogen, (C1-C6)-alkyl, halogen, halogen-(C1-C6)-alkyl, hydroxy, C1-C6-alkoxy or -CHO; R is hydrogen or C1-C3-alkyl; R , R independently from each other are selected from the group consisting of hydrogen, C1-C6-alkyl, C1-C6-alkoxy or -COO(C1-C6)alkyl; or R and R form together with the C-atom to which they are attach a C3-C7-cycloalkyl ring; R is -CO-NR R ; -COO(C1-C6)-alkyl, -CN, -NR2 or -NHC(O)R; R and R independently from each other are selected from the group consisting of hydrogen, C1-C6-alkyl, NH2 or hydroxy; R is hydrogen or C1-C6-alkyl; n is 0, 1, 2 or 3. X is -CHRO, -OCHR, -CH2S-, -SCH2-, -CH2CH2-, -CH=CH- or -C=C-; and to pharmaceutically active acid addition salts thereof. It has been found that the compounds of general formula (I) are selective monoamine oxidase B inhibitors and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B inhibitors, for example for the treatment of Alzheimer's disease or senile dementia.
摘要翻译：本发明涉及通式（I）的N-酰基氨基芳基衍生物，其中R 1是卤素，卤素 - （C 1 -C 6） - 烷基，氰基，C 1 -C 6 - 烷氧基或卤素 - （C 1 -C 6）烷氧基; R 21，R 22，R 23和R 24彼此独立地选自氢，（C 1 -C 6） - 烷基，卤素，卤素 - （C 1 -C 6） - 烷基，羟基，C 1 -C 6 - 烷氧基或-CHO; R 3是氢或C 1 -C 3 - 烷基; R 4，R 5彼此独立地选自氢，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基或-COO（C 1 -C 6）烷基; 或R 4和R 5与它们所连接的C-C原子一起形成C 3 -C 7 - 环烷基环; R 6是-CO-NR 7 R 8; -COO（C 1 -C 6） - 烷基，-CN，-NR 2或-NHC（O）R; R 7和R 8彼此独立地选自氢，C 1 -C 6 - 烷基，NH 2或羟基; R是氢或C 1 -C 6 - 烷基; n是0,1,2或3.X是-CHRO，-OCHR，-CH 2 S - ， - CH 2 - ， - CH 2 CH 2 - ， - CH = CH-或-C = C-; 及其药物活性的酸加成盐。已经发现通式（I）的化合物是选择性单胺氧化酶B抑制剂，因此它们可用于治疗由单胺氧化酶B抑制剂介导的疾病，例如用于治疗阿尔茨海默氏病或老年痴呆症。

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