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1. 发明申请

WO2006040038A1 IMIDAZO [1, 5-A]TRIAZOLO[1, 5-D]BENZODIAZEPINE DERIVATIVES FOR THE TREATMENT OF COGNITIVE DISORDERS 审中-公开
标题翻译：咪达唑[1,5-A]三唑并[1,5-D]苯并恶唑衍生物治疗认知障碍
公开(公告)号：WO2006040038A1
公开(公告)日：2006-04-20
申请号：PCT/EP2005/010655
申请日：2005-10-04
申请人： F.HOFFMANN-LA ROCHE AG , KNUST, Henner , STADLER, Heinz , THOMAS, Andrew, William
发明人： KNUST, Henner , STADLER, Heinz , THOMAS, Andrew, William
IPC分类号： A61K31/5517 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/28 , A61P43/00
CPC分类号： A61K31/5517 , C07D487/14
摘要： The present invention is concerned with the use of substituted imidazo [1,5-a] [1,2,4]triazolo[1,5-d] [1,4]benzodiazepine derivatives of the following formula (I); wherein R 1 is halogen, lower alkyl, lower alkynyl, cycloalkyl, lower alkoxy, OCF 3 , -NHR, - NHC(O)R or -NHSO 2 R; R 2 is hydrogen, methyl or aryl, which is unsubstituted or substituted by one or two substituents, selected from the group consisting of halogen or lower alkoxy; R 3 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, lower alkoxy, -O(CH 2 ) n+1 -Olower alkyl, -(CH 2 ) n -aryl, which is optionally substituted by lower alkyl or halogen, heteroaryl, -NHR, -NR 2 , wherein R 2 may be the same or different, or is - NHCH 2 C=-CH, or pyrrolidin-1-one; R is hydrogen, lower alkyl, lower alkyl substituted by halogen, heteroaryl, -(CH2) n O-lower alkyl, -NH-lower alkyl, cycloalkyl or aryl, n is 0, 1, 2 or 3; and with their pharmaceutically acceptable acid addition salts for the manufacture of medicaments for the treatment of cognitive enhance or for the treatment of cognitive disorders, anxiety or schizophrenia. The most preferred indication is Alzheimer's disease.
摘要翻译：本发明涉及下式（I）的取代咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物的用途。其中R

2. 发明申请

WO2006063708A1 TETRACYCLIC IMIDAZO-BENZODIAZEPINES AS GABA RECEPTORS MODULATORS 审中-公开
标题翻译：作为GABA受体调节剂的四氢咪唑并苯并嗪
公开(公告)号：WO2006063708A1
公开(公告)日：2006-06-22
申请号：PCT/EP2005/012993
申请日：2005-12-05
申请人： F.HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , KNUST, Henner , THOMAS, Andrew, William
发明人： BUETTELMANN, Bernd , KNUST, Henner , THOMAS, Andrew, William
IPC分类号： C07D487/14 , A61K31/5517
CPC分类号： C07D487/14
摘要： The present invention is concerned with substituted imidazo [1,5-a] [1,2,4] triazolo [1,5-d] [1,4]benzodiazepine derivatives of the following formula (I) wherein R' is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, nitro, cycloalkyl, -O(CH 2 ) m O(CH 2 ) m OH or -C≡C-R'; R 2 is hydrogen or methyl; R 3 is lower alkyl, lower alkyl substituted by halogen, lower alkenyl, lower alkenyl substituted by halogen, lower alkynyl, -(CH 2 ) n -cycloalkyl, -(CR'R") m CH 3 , or is phenyl, unsubstituted or substituted by halogen, or is pyridinyl or thienyl, unsubstituted or substituted by lower alkyl, or is -(CH 2 ) n -NH-cycloalkyl, lower alkenyl-cycloalkyl, lower alkynyl-(CR'R") m OH, or is lower alkynyl-phenyl, wherein the phenyl ring is unsubstituited or substituted by halogen, CF 3 , lower alkyl or lower alkoxy; R' is hydrogen or lower alkyl; R" is hydrogen, hydroxy or lower alkyl; n is 0, 1 or 2; m is 1, 2 or 3; o is 1 or 2; and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA A α 5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及下式（I）的取代咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物，其中R'是氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素取代的低级烷氧基，硝基，环烷基，-O（CH 2） OH或-C = C-R'; R 2是氢或甲基; R 3是低级烷基，被卤素取代的低级烷基，低级烯基，被卤素取代的低级链烯基，低级炔基， - （CH 2 SO 2）n

3. 发明申请

WO2006063732A1 THIENO-PYRIDINE DERIVATIVES AS GABA-B ALLOSTERIC ENHANCERS 审中-公开
标题翻译：三苯基吡啶衍生物作为GABA-B无菌增强剂
公开(公告)号：WO2006063732A1
公开(公告)日：2006-06-22
申请号：PCT/EP2005/013194
申请日：2005-12-09
申请人： F.HOFFMANN-LA ROCHE AG , MALHERBE, Parichehr , MASCIADRI, Raffaello , NORCROSS, Roger, David , RATNI, Hasane , THOMAS, Andrew, William
发明人： MALHERBE, Parichehr , MASCIADRI, Raffaello , NORCROSS, Roger, David , RATNI, Hasane , THOMAS, Andrew, William
IPC分类号： C07D495/04 , A61K31/435 , A61P25/00 , C07D495/14
CPC分类号： C07D495/04 , C07D495/14
摘要： The present invention relates to compounds of formula (I), Wherein R 1 to R 5 are as defined in the specification which compounds are active on the GABA B receptor and can be used for the manufacture of medicaments useful for treating CNS disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1至R 5如本说明书中所定义，其化合物在GABA B上具有活性， / SUB>

4. 发明申请

WO2006045429A1 HALOGEN SUBSTITUTED BENZODIAZEPINE DERIVATIVES 审中-公开
标题翻译：卤素取代的苯甲酸衍生物
公开(公告)号：WO2006045429A1
公开(公告)日：2006-05-04
申请号：PCT/EP2005/010907
申请日：2005-10-11
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , THOMAS, Andrew, William
发明人： KNUST, Henner , THOMAS, Andrew, William
IPC分类号： C07D487/14 , A61K31/55 , A61P25/00
CPC分类号： C07D487/14
摘要： The invention relates to halogen substituted imidazo [1,5-a] [1,2,4] triazolo [1,5d] [1,4]benzodiazepine derivatives of formula (I), and to their pharmaceutically acceptable acid addition salts. The compounds may be used for the treatment of cognitive enhancer, cognitive disorders, anxiety, Alzheimer's disease and schizophrenia.
摘要翻译：本发明涉及式（I）的卤素取代的咪唑并[1,5-a] [1,2,4]三唑并[1,5d] [1,4]苯并二氮杂衍生物及其药学上可接受的酸加成盐。该化合物可用于治疗认知增强剂，认知障碍，焦虑，阿尔茨海默病和精神分裂症。

5. 发明申请

WO2006045430A1 IMIDAZO-BENZODIAZEPINE DERIVATIVES 审中-公开
标题翻译：咪唑 - 苯二酮衍生物
公开(公告)号：WO2006045430A1
公开(公告)日：2006-05-04
申请号：PCT/EP2005/010908
申请日：2005-10-11
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , THOMAS, Andrew, William
发明人： KNUST, Henner , THOMAS, Andrew, William
IPC分类号： C07D487/14 , A61K31/55
CPC分类号： C07D487/14
摘要： The present invention is concerned with substituted imidazo [1,5-a] [1,2,4] triazolo [1,5d] [1,4]benzodiazepine derivatives of formula (I) wherein R 1 is hydrogen, halogen, lower alkyl, lower alkynyl, cycloalkyl, heterocycloalkyl, benzyl, cyano, lower alkoxy, OCF 3 , -NHR, -NHC(O)R or -NHSO 2 R; R 2 is lower alkyl substituted by halogen; R 3 is hydrogen, methyl or aryl; R is lower alkyl, cycloalkyl or aryl; and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders, anxiety, schizophrenia or Alzheimer's disease.
摘要翻译：本发明涉及式（I）的取代的咪唑并[1,5-a] [1,2,4]三唑并[1,5d] [1,4]苯并二氮杂衍生物，其中R 1，卤素，低级烷基，低级炔基，环烷基，杂环烷基，苄基，氰基，低级烷氧基，OCF 3，-NHR，-NHC（O）R或-NHSO 2， / SUB> R等 R 2是被卤素取代的低级烷基; R 3是氢，甲基或芳基; R是低级烷基，环烷基或芳基; 和其药学上可接受的酸加成盐。已经发现，这类化合物显示出对GABA A a5受体结合位点的高亲和力和选择性，并且可用作认知增强剂或用于治疗认知障碍，焦虑，精神分裂症或阿尔茨海默病。

6. 发明申请

WO2004026825A1 PYRROLIDONE DERIVATIVES AS MAOB INHIBITORS 审中-公开
标题翻译：吡咯烷酮衍生物作为MAOB抑制剂
公开(公告)号：WO2004026825A1
公开(公告)日：2004-04-01
申请号：PCT/EP2003/010356
申请日：2003-09-18
申请人： F.HOFFMANN-LA ROCHE AG
发明人： IDING, Hans , JOLIDON, Synese , KRUMMENACHER, Daniela , RODRIGUEZ-SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WIRZ, Beat , WOSTL, Wolfgang , WYLER, Rene
IPC分类号： C07D207/26
CPC分类号： C07D207/273 , C07D207/277
摘要： Racemic or enantiomerically pure 4-pyrrolidino derivatives of the formula (I), processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of a disease which is mediated by a monoamine oxidase B inhibitor, in particular Alzheimer's disease and senile dementia.
摘要翻译：式（I）的外消旋或对映体纯的4-吡咯烷子基衍生物，其制备方法，包含所述衍生物的药物组合物及其在预防和治疗由单胺氧化酶B抑制剂介导的疾病，特别是阿尔茨海默病疾病和老年痴呆症。

7. 发明申请

WO2003106380A2 FLUOROBENZAMIDES 审中-公开
公开(公告)号：WO2003106380A2
公开(公告)日：2003-12-24
申请号：PCT/EP2003/006008
申请日：2003-06-07
申请人： F.HOFFMANN-LA ROCHE AG
发明人： JOLIDON, Synese , RODRIGUEZ SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WYLER, Rene
IPC分类号： C07C
CPC分类号： C07C235/52 , C07C235/48 , C07C235/50 , C07C255/30
摘要： The present invention is concerned with fluorobenzamide derivatives of the general formula Wherein R 1 is hydrogen, (C 1 -C 6 )-alkyl or hydroxy-( C1 -C 6 )-alkyl; R 2 is (C 1 -C 6 )-alkyl, -CO-NR 8 R 9 , -(CH 2 ) n -NR 8 R 9 , -(CH 2 ) P -OR 8 , or -(CH 2 ) n -CN; R 3 is selected from hydrogen, halogen, halogen-(C 1 -C 6 )-alkyl, cyano, C 1 -C 6 -alkoxy or halogen-(C 1 -C 6 )-alkoxy; R 4 , R 5 , R 6 and R 7 are hydrogen or fluoro, and at least one of R 4 , R 5 , R 6 and R 7 is fluoro; R 8 and R 9 independently from each other are hydrogen or (C 1 -C 6 )-alkyl; m is 1, 2 or 3; n is 0, 1, 2 or 3; and p is 1 or 2; as well as their pharmaceutically acceptable salts. The compounds of general formula I are selective monoamine oxidase B inhibitors and therefore they are suitable for the treatment of Alzheimer's disease or senile dementia.
摘要翻译：本发明涉及通式的氟代苯甲酰胺衍生物，其中R 1是氢，（C 1 -C 6） - 烷基或羟基 - （C 1 -C 6） - 烷基; R 2是（C 1 -C 6） - 烷基，-CO-NR 8 R 9 - ， - （CH 2）n -NR 8 R 9 - ，（CH 2）P-OR 8 ，或 - （CH 2）n-CN; R 3选自氢，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 4，R 5，R 6和R 7是氢或氟，R 4，R 5，R 6和R 7中的至少一个是氟 ; R 8和R 9彼此独立地是氢或（C 1 -C 6） - 烷基; m为1,2或3; n为0,1,2或3; p为1或2; 以及它们的药学上可接受的盐。通式I的化合物是选择性单胺氧化酶B抑制剂，因此它们适用于治疗阿尔茨海默病或老年痴呆症。

8. 发明申请

WO2003106380A3 FLUOROBENZAMIDES SUITABLE FOR THE TREATMENT OF ALZHEIMER’S DISEASE OR SENILE DEMENTIA 审中-公开
公开(公告)号：WO2003106380A3
公开(公告)日：2003-12-24
申请号：PCT/EP2003/006008
申请日：2003-06-07
申请人： F.HOFFMANN-LA ROCHE AG
发明人： JOLIDON, Synese , RODRIGUEZ SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WYLER, Rene
IPC分类号： C07C233/83
摘要： The present invention is concerned with fluorobenzamide derivatives of the general formula, wherein R 1 is hydrogen, (C 1 -C 6 )-alkyl or hydroxy-( C1 -C 6 )-alkyl; R 2 is (C 1 -C 6 )-alkyl, -CO-NR 8 R 9 , -(CH 2 ) n -NR 8 R 9 , -(CH 2 ) P -OR 8 , or -(CH 2 ) n -CN; R 3 is selected from hydrogen, halogen, halogen-(C 1 -C 6 )-alkyl, cyano, C 1 -C 6 -alkoxy or halogen-(C 1 -C 6 )-alkoxy; R 4 , R 5 , R 6 and R 7 are hydrogen or fluoro, and at least one of R 4 , R 5 , R 6 and R 7 is fluoro; R 8 and R 9 independently from each other are hydrogen or (C 1 -C 6 )-alkyl; m is 1, 2 or 3; n is 0, 1, 2 or 3; and p is 1 or 2; as well as their pharmaceutically acceptable salts. The compounds of general formula (I) are selective monoamine oxidase B inhibitors and therefore they are suitable for the treatment of Alzheimer's disease or senile dementia.

9. 发明授权

EP1542970B1 PYRROLIDONE DERIVATIVES AS MAOB INHIBITORS 有权
标题翻译：吡咯烷酮衍生物THAN MAO-B抑制剂
公开(公告)号：EP1542970B1
公开(公告)日：2010-06-30
申请号：EP03750564.1
申请日：2003-09-18
申请人： F.HOFFMANN-LA ROCHE AG
发明人： IDING, Hans , JOLIDON, Synese , KRUMMENACHER, Daniela , RODRIGUEZ-SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WIRZ, Beat , WOSTL, Wolfgang , WYLER, Rene
IPC分类号： C07D207/26 , C07D401/04
CPC分类号： C07D207/273 , C07D207/277
摘要： Racemic or enantiomerically pure 4-pyrrolidino derivatives of the formula (I), processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of a disease which is mediated by a monoamine oxidase B inhibitor, in particular Alzheimer's disease and senile dementia.

10. 发明授权

EP1725239B1 4-(SULFANYL-PYRIMIDIN-4-YLMETHYL)-MORPHOLINE DERIVATIVES AND RELATED COMPOUNDS AS GABA RECEPTOR LIGANDS FOR THE TREATMENT OF ANXIETY, DEPRESSION AND EPILEPSY 有权
标题翻译： 4-（4- sulfanylpyrimidine基甲基）吗啉衍生物及相关化合物AS GABA受体配体用于焦虑，抑郁和癫痫治疗
公开(公告)号：EP1725239B1
公开(公告)日：2007-07-18
申请号：EP05707562.4
申请日：2005-02-22
申请人： F.HOFFMANN-LA ROCHE AG
发明人： MALHERBE, Pari , MASCIADRI, Raffaello , PRINSSEN, Eric , SPOOREN, Will , THOMAS, Andrew, William
IPC分类号： A61K31/506 , C07D239/38 , A61P25/22 , A61P25/24 , A61P25/08
CPC分类号： C07D239/38 , C07D239/42 , C07D401/06 , C07D403/06 , C07D413/06 , C07D471/14 , C07D491/10
摘要： The present invention relates to compounds of Formula (I) wherein X is -S- or -NH-; R1 is alkyl, alkenyl, arylalkyl, arylalkenyl or aryl-O-alkyl, wherein the aryl groups are optionally substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen or lower halogen-alkyl; R2 is hydrogen, lower alkyl or cycloalkyl; R3/R4 may form together with the N-atom to which they are attached a non aromatic5, 6 or 7 membered ring, which may contain in addition to the N-atom one additional heteroatom selected from the group consisting of O, S or N, and wherein the ring is optionally substituted by hydroxy, lower alkyl, lower alkoxy, -NR2, -CONR2, -CO-lower alkyl or benzyl; or may form together with the N-atom to which they are attached a heterocyclic ring system, containing at least two rings and which may contain one or two additional heretoatoms, selected from the group consisting of N or O; R is hydrogen or lower alkyl; R5 is hydrogen or lower alkyl; and to pharmaceutically suitable acid addition salts thereof. It has been found that the compounds are active on the GABAB receptor and therefore useful for the treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, psychosis, panic disorder, posttraumatic stress disorders or gastro-intestinal disorders.

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