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1. 发明申请

WO2005068463A1 DIAZA-SPIROPIPERIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2005068463A1
公开(公告)日：2005-07-28
申请号：PCT/EP2004/014841
申请日：2004-12-30
申请人： F. HOFFMANN-LA ROCHE AG , CECCARELLI, Simona, Maria , JOLIDON, Synese , PINARD, Emmanuel , THOMAS, Andrew, William
发明人： CECCARELLI, Simona, Maria , JOLIDON, Synese , PINARD, Emmanuel , THOMAS, Andrew, William
IPC分类号： C07D471/10
CPC分类号： C07D471/10
摘要： The present invention relates to compounds of formula (I); wherein A-B is -CH 2 -CH 2 -, -CH 2 -O- or -O-CH 2 -; X is hydrogen or hydroxy; R l is aryl, optionally substituted by one or two substituents, selected from the group consisting of halogen, lower alkyl, cyano, CF 3 , -OCF 3 , lower alkoxy, -SO 2 -lower alkyl or by heteroaryl, R 2 is aryl, optionally substituted by one or two substituents, selected from the group consisting of halogen, lower alkyl, CF 3 or lower alkoxy; R 3 is hydrogen or lower alkyl; n is 0, 1 or 2; and to their pharmaceutically active salts. The compounds of formula I may be used in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及式（I）化合物; 其中A-B是-CH 2 -CH 2 - ， - CH 2 -O-或-O-CH 2 - ; X是氢或羟基; R 1是任选被一个或两个选自卤素，低级烷基，氰基，CF 3，-OCF 3，低级烷氧基，-SO 2 - 低级烷基或杂芳基的取代基取代的芳基，R 2是芳基，任选被一个或两个选自卤素，低级烷基，CF 3或低级烷氧基的取代基取代; R 3是氢或低级烷基; n为0,1或2; 和其药物活性盐。式I化合物可用于治疗神经和神经精神障碍。

2. 发明申请

WO2005068462A1 DIAZA-SPIROPIPERIDINE DERIVATIVES AS INHIBITORS OF TRANSPORTER 1 AND GLYCINE TRANSPORTER 2 审中-公开
标题翻译：作为运输车辆1和糖果运输车辆2的抑制剂的DIAZA-螺旋磷酸二氢吡啶衍生物
公开(公告)号：WO2005068462A1
公开(公告)日：2005-07-28
申请号：PCT/EP2004/014840
申请日：2004-12-30
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , PINARD, Emmanuel , THOMAS, Andrew, William
发明人： JOLIDON, Synese , PINARD, Emmanuel , THOMAS, Andrew, William
IPC分类号： C07D471/10
CPC分类号： C07D471/10
摘要： The present invention relates to compounds of formula (I) wherein A-B is CH 2 -CH 2 , -CH 2 -O-, O-CH 2 , CH 2 -S, -S-CH 2 -, CH 2 -C(O)-, C(O)-CH 2 -, .-N(R 4 )-CH 2 - or -CH 2 -N(R 4 )-; R 1 is lower alkyl, lower alkenyl, cycloalkyl, or is aryl, optionally substituted by one or two substituents, selected from the group consisting of halogen, cyano, lower alkyl, CF 3 , OCF 3 or lower alkoxy, or is heteroaryl, optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, CF 3 or lower alkoxy; R 2 is lower alkyl, cycloalkyl, or is aryl, optionally substituted by one or two substituents, selected from the group consisting of halogen, lower alkyl, CF 3 , lower alkoxy, or is heteroaryl, optionally substituted by one or two substituents, selected from the group consisting of halogen, lower alkyl, CF 3 , lower alkoxy, or is heteroaryl, optionally substituted by one or two substituents, selected from the group consisting of halogen, lower alkyl, CF 3, or lower alkoxy; R 3 is hydrogen, lower alkyl or benzyl; R 4 is hydrogen or benzyl; n is 0, 1 or 2; and to pharmaceutically available salts thereof. The compounds of formula I may be used in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及式（I）化合物，其中AB是CH 2 -CH 2，-CH 2 -O-，O-CH 2，CH 2 -S，-S-CH 2 - ，CH 2 -C（O） - ，C（O） -CH 2 - ， - N（R 4）-CH 2 - 或-CH 2 -N（R 4） - ; R 1是低级烷基，低级烯基，环烷基或芳基，任选地被一个或两个选自卤素，氰基，低级烷基，CF 3，OCF 3或低级烷氧基的取代基取代，或者是杂芳基，任选地被一个或两个选自卤素，低级烷基，CF 3或低级烷氧基的取代基取代; R 2是低级烷基，环烷基或芳基，任选被一个或两个选自卤素，低级烷基，CF 3，低级烷氧基或被一个或两个取代基取代的杂芳基取代的取代基取代，选自卤素，低级烷基，CF 3，低级烷氧基或杂芳基，任选被一个或两个选自卤素，低级烷基，CF 3或低级烷氧基的取代基取代; R 3是氢，低级烷基或苄基; R 4是氢或苄基; n为0,1或2; 及其药学上可用的盐。式I化合物可用于治疗神经和神经精神障碍。

3. 发明申请

WO2005039591A1 BENZAZEPINE DERIVATIVES AS MAO-B INHIBITORS 审中-公开
标题翻译：苯并噻吩衍生物作为MAO-B抑制剂
公开(公告)号：WO2005039591A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011541
申请日：2004-10-14
申请人： F. HOFFMANN-LA ROCHE AG , 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： A61K31/55
CPC分类号： C07D223/16
摘要： The present invention relates to novel benzazepine derivatives of the following formula: (I) wherein R 1 , R 2 , R 3 , R 4 and R 5 , X, X’, Y and Y’ are as defined in the description and claims, processes for their preparation, pharmaceutical compositions containing said derivatives and their use for the preparation of medicaments useful for the prevention and treatment of diseases in which selective inhibition of monoamine oxidase B activity plays a role or is implicated.
摘要翻译：本发明涉及下式的新的苯并氮杂衍生物：其中R 1，R 2，R 3，R 4和R 5，X，X'，Y和Y '如在说明书和权利要求书中所定义，其制备方法，含有所述衍生物的药物组合物及其用于制备可用于预防和治疗单胺氧化酶B活性的选择性抑制发挥作用的疾病的药物的用途牵连。

4. 发明申请

WO2006000324A3 NEW MAO-B INHIBITORS 审中-公开
公开(公告)号：WO2006000324A3
公开(公告)日：2006-01-05
申请号：PCT/EP2005/006398
申请日：2005-06-15
申请人： F. HOFFMANN-LA ROCHE AG , 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： C07C235/34 , C07C271/12 , A61K31/165 , A61K31/27 , A61P25/28
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.

5. 发明申请

WO2006048146A1 QUINOLINE AS ALLOSTERIC ENHANCERS OF THE GABA-B RECEPTORS 审中-公开
标题翻译：喹啉作为GABA-B受体的独立增强剂
公开(公告)号：WO2006048146A1
公开(公告)日：2006-05-11
申请号：PCT/EP2005/011403
申请日：2005-10-25
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： C07D215/18 , C07D215/20 , C07D491/04 , C07D215/38 , C07D401/04 , A61K31/4738 , A61P25/22
CPC分类号： C07D215/38 , C07D215/18 , C07D215/20 , C07D401/04
摘要： The present invention relates to compounds of formula (I) wherein R 1 to R 6 are as defined as described herein, which compounds are active at the GABA B receptor and can be used for the preparation of medicaments useful in the treatment of CNS disorders comprising anxiety and depression.
摘要翻译：本发明涉及式（I）化合物，其中R 1至R 6如本文所述，其化合物在GABA B上具有活性， / SUB>受体，可用于制备用于治疗包括焦虑和抑郁症的中枢神经系统疾病的药物。

6. 发明申请

WO2005094828A1 4- (SULFANYL-PYRIMIDIN-4-YLMETHYL) -MORPHOLINE DERIVATIVES AND RELATED COMPOUNDS AS GABA RECEPTOR LIGANDS FOR THE TREATMENT OF ANXIETY, DEPRESSION AND EPILEPSY 审中-公开
标题翻译： 4-（SULFANYL-吡啶基-4-甲基乙基） - 吗啉衍生物及相关化合物作为GABA受体配体，用于治疗放射性疾病，恶化和恶化
公开(公告)号：WO2005094828A1
公开(公告)日：2005-10-13
申请号：PCT/EP2005/001814
申请日：2005-02-22
申请人： F. HOFFMANN-LA ROCHE AG , MALHERBE, Pari , MASCIADRI, Raffaello , PRINSSEN, Eric , SPOOREN, Will , THOMAS, Andrew, William
发明人： MALHERBE, Pari , MASCIADRI, Raffaello , PRINSSEN, Eric , SPOOREN, Will , THOMAS, Andrew, William
IPC分类号： A61K31/506
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-; R 1 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; R 2 is hydrogen, lower alkyl or cycloalkyl; R 3 /R 4 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, -NR 2 , -CONR 2 , -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; R 5 is hydrogen or lower alkyl; and to pharmaceutically suitable acid addition salts thereof. It has been found that the compounds are active on the GABA B 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.
摘要翻译：本发明涉及其中X为-S-或-NH-的式（I）化合物; R 1是烷基，烯基，芳基烷基，芳基烯基或芳基-O-烷基，其中芳基任选被一个或多个选自下列的取代基取代：低级烷基，低级烷氧基，卤素或低级卤代烷基 ; R 2是氢，低级烷基或环烷基; R 3 / R 4可以与它们所连接的N-原子一起形成非芳族5,6或7元环，除了N-原子外，还可以含有一个另外的杂原子，该杂原子选自的O，S或N，并且其中所述环任选被羟基，低级烷基，低级烷氧基，-NR 2，-CONR 2，-CO-低级烷基或苄基取代; 或者可以与它们所连接的N-原子一起形成含有至少两个环的杂环体系，并且可以含有一个或两个选自N或O的另外的原子， R是氢或低级烷基; R 5是氢或低级烷基; 和其药学上合适的酸加成盐。已经发现这些化合物对GABA B受体有活性，因此可用于治疗焦虑，抑郁，癫痫，精神分裂症，认知障碍，痉挛和骨骼肌僵硬，脊髓损伤，多发性硬化，肌萎缩性侧索硬化，脑性麻痹，神经性疼痛和与可卡因和尼古丁相关的渴望，精神病，恐慌症，创伤后应激障碍或胃肠疾病。

7. 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。

8. 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。

9. 发明申请

WO2004014856A1 2,3-DIHYDRO-ISOINDOL-1-ONES WITH MAO-B INHIBITING ACTIVITY 审中-公开
标题翻译： 2,3-DIHYDRO-ISOINDOL-1-ONES与MAO-B抑制活性
公开(公告)号：WO2004014856A1
公开(公告)日：2004-02-19
申请号：PCT/EP2003/008456
申请日：2003-07-31
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： C07D209/46
CPC分类号： C07D471/04 , C07D209/46
摘要： 2,3 Dihydro-isoindol-1-one derivatives, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them, for the prevention and treatment of diseases which are mediated by monoamine oxidase B inhibitors.
摘要翻译： 2,3二氢 - 异吲哚-1-酮衍生物，其制备方法，它们作为药物的用途和包含它们的药物组合物，用于预防和治疗由单胺氧化酶B抑制剂介导的疾病。

10. 发明申请

WO2003099763A1 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：WO2003099763A1
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005297
申请日：2003-05-21
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： C07C233/25
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 1 is halogen, halogen-(C 1 -C 6 )-alkyl, cyano, C 1 -C 6 -alkoxy or halogen-(C 1 -C 6 )-alkoxy; R 21 , R 22 , R 23 and R 24 independently from each other are selected from the group consisting of hydrogen, (C 1 -C 6 )-alkyl, halogen, halogen-(C 1 -C 6 )-alkyl, hydroxy, C 1 -C 6 -alkoxy or -CHO; R 3 is hydrogen or C 1 -C 3 -alkyl; R 4 , R 5 independently from each other are selected from the group consisting of hydrogen, C 1- C 6 -alkyl, C 1 -C 6 -alkoxy or -COO(C 1 -C 6 )alkyl; or R 4 and R 5 form together with the C-atom to which they are attach a C 3 -C 7 -cycloalkyl ring; R 6 is -CO-NR 7 R 8 ; -COO(C 1 -C 6 )-alkyl, -CN, -NR 2 or -NHC(O)R; R 7 and R 8 independently from each other are selected from the group consisting of hydrogen, C 1- C 6 -alkyl, NH 2 or hydroxy; R is hydrogen or C 1 -C 6 -alkyl; n is 0, 1, 2 or 3. X is -CHRO, -OCHR, -CH 2 S-, -SCH 2 -, -CH 2 CH 2 -, -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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