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1. 发明申请

WO2010086251A1 AROYLAMINO - AND HETEROAROYLAMINO-SUBSTITUTED PIPERIDINES AS GLYT-1 INHIBITORS 审中-公开
标题翻译：作为GLYT-1抑制剂的α-亚氨基 - 和异丁烯酰胺取代的哌啶
公开(公告)号：WO2010086251A1
公开(公告)日：2010-08-05
申请号：PCT/EP2010/050551
申请日：2010-01-19
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , PINARD, Emmanuel , STALDER, Henri
发明人： KOLCZEWSKI, Sabine , PINARD, Emmanuel , STALDER, Henri
IPC分类号： C07D211/56 , C07D401/04 , C07D401/12 , C07D405/04 , C07D417/10 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/4545
CPC分类号： C07D407/04 , A61K31/451 , C07D211/56 , C07D213/56 , C07D221/20 , C07D401/04 , C07D401/12 , C07D405/04 , C07D417/10
摘要： The present invention relates to a compound of general formula (I) wherein R 1 is hydrogen, lower alkyl, CD 3 , -(CH 2 ) n -CHO, -(CH 2 ) n -O-lower alkyl, -(CH 2 ) n -OH, -(CH 2 ) n -cycloalkyl or is heterocycloalkyl; R 2 is hydrogen, halogen, hydroxy, lower alkyl, di-lower alkyl, -OCH 2 -O-lower alkyl, or lower alkoxy; or the piperidin ring form together with R 2 a spiro ring, selected from 4-aza-spiro[2.5]oct-6-yl; Ar is aryl or heteroaryl, which are optionally substituted by one, two or three substituents, selected from halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cycloalkyl, lower alkoxy, S-lower alkyl, heteroaryl, heterocycloalkyl, or by phenyl optionally substituted by R', and R' is halogen, lower alkyl, lower alkoxy or lower alkoxy substituted by halogen, or is heteroaryl; R is lower alkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, wherein aryl and heteroaryl are optionally substituted by one or two R'; n is 0, 1 2 or 3; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. Furthermore, the present invention relates to pharmaceutical compositions containing the compounds of formula I and to their use in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及通式（I）的化合物，其中R1是氢，低级烷基，CD3， - （CH2）n-CHO， - （CH2）nO-低级烷基， - （CH2）n-OH， - （ CH2）n-环烷基或杂环烷基; R2是氢，卤素，羟基，低级烷基，二低级烷基，-OCH2-O-低级烷基或低级烷氧基; 或哌啶环与R2一起形成选自4-氮杂 - 螺[2.5]辛-6-基的螺环; Ar是芳基或杂芳基，其任选被一个，两个或三个选自卤素，低级烷基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，环烷基，低级烷氧基，S-低级烷基，杂芳基，杂环烷基，或被R'任意取代的苯基，R'是卤素，低级烷基，低级烷氧基或被卤素取代的低级烷氧基，或是杂芳基; R是低级烷基，环烷基，杂环烷基，芳基或杂芳基，其中芳基和杂芳基任选被一个或两个R'取代; n为0，1 2或3; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体。此外，本发明涉及含有式I化合物的药物组合物及其在治疗神经和神经精神障碍中的用途。

2. 发明申请

WO2010094659A1 AMINE OR AMINO ALCOHOLS AS GLYT1 INHIBITORS 审中-公开
标题翻译：胺或氨基醇作为GLYT1抑制剂
公开(公告)号：WO2010094659A1
公开(公告)日：2010-08-26
申请号：PCT/EP2010/051877
申请日：2010-02-16
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , MARTY, Hans-Peter , NARQUIZIAN, Robert , PINARD, Emmanuel , STALDER, Henri
发明人： KOLCZEWSKI, Sabine , MARTY, Hans-Peter , NARQUIZIAN, Robert , PINARD, Emmanuel , STALDER, Henri
IPC分类号： A61P25/28 , A61K31/16 , A61P25/18 , C07C215/30 , C07C215/68 , C07C217/70 , C07C233/43 , C07C237/30 , C07C317/32 , C07D213/30 , C07D213/34 , C07D213/61 , C07D277/28 , C07D305/06 , C07D307/20
CPC分类号： A61K31/16 , C07C215/30 , C07C215/68 , C07C217/70 , C07C233/43 , C07C237/30 , C07C317/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D211/46 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/71 , C07D213/73 , C07D239/26 , C07D277/28 , C07D305/06 , C07D307/12 , C07D307/20 , C07D309/06 , C07D309/12 , C07D333/20 , C07D335/02 , C07D405/12
摘要： The invention relates to the use of compounds of formula (I), wherein the substituents are described in the description and claims, for the preparation of medicaments for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease.
摘要翻译：本发明涉及式（I）化合物的用途，其中取代基在描述和权利要求书中描述，用于制备用于治疗精神病药，记忆障碍和学习功能障碍的药物，精神分裂症，痴呆，注意力缺陷障碍或阿尔茨海默氏病。

3. 发明申请

WO2011161008A1 QUINOLIZIDINE AND INDOLIZIDINE DERIVATIVES 审中-公开
标题翻译：喹诺酮和吲哚来啶衍生物
公开(公告)号：WO2011161008A1
公开(公告)日：2011-12-29
申请号：PCT/EP2011/060077
申请日：2011-06-17
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , PINARD, Emmanuel
发明人： KOLCZEWSKI, Sabine , PINARD, Emmanuel
IPC分类号： C07D455/02 , C07D471/04 , A61K31/437 , A61K31/4375 , A61P25/00
CPC分类号： C07D455/02 , C07D471/04
摘要： The present invention relates to a compound of general formula I-A or I-B wherein X is a bond or a CH 2 - group; R 1 , R 2 and R 3 are independently from each other hydrogen, lower alkoxy, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. It has been found that the compounds of general formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and that they have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及通式I-A或I-B的化合物，其中X为键或CH2-基; R 1，R 2和R 3彼此独立地为氢，低级烷氧基，被卤素或S-低级烷基取代的低级烷基; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体。已经发现，通式IA和IB的化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，并且它们对甘氨酸转运蛋白2（GlyT-2）抑制剂具有良好的选择性，适用于治疗神经和神经精神障碍。

4. 发明申请

WO2011095434A1 TETRAHYDRO-PYRAN DERIVATIVES AGAINST NEUROLOGICAL ILLNESSES 审中-公开
标题翻译：四氢吡喃衍生物对抗神经病学
公开(公告)号：WO2011095434A1
公开(公告)日：2011-08-11
申请号：PCT/EP2011/051179
申请日：2011-01-28
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , PINARD, Emmanuel
发明人： KOLCZEWSKI, Sabine , PINARD, Emmanuel
IPC分类号： A61K31/351 , A61K31/4025 , A61K31/439 , A61K31/4412 , A61K31/4433 , C07D309/14 , C07D407/04 , A61P29/00 , A61P25/00
CPC分类号： A61K31/351 , A61K9/2018 , A61K9/4858 , A61K31/4025 , A61K31/439 , A61K31/4412 , A61K31/4433 , C07D309/14 , C07D405/04
摘要： The present invention relates to a compound of general formula (I) wherein X is -O- or -CH 2- ; X' is -O- or -CH 2- ; with the proviso that one of X or X' is always -O- and the other is -CH 2- . It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GIyT-1) and therefore they may be used for the treatment of schizophrenia, psychoses and other neurological conditions, including pain.
摘要翻译：本发明涉及通式（I）的化合物，其中X是-O-或-CH 2 - ; X'是-O-或-CH 2 - ; 条件是X或X'中的一个总是-O-，另一个是-CH 2 - 。已经发现通式（I）的化合物是甘氨酸转运蛋白1（GlyT-1）和因此它们可用于治疗精神分裂症，精神病和其他神经病症，包括疼痛。

5. 发明申请

WO2010020548A1 GLYT1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： GLYT1受体拮抗剂
公开(公告)号：WO2010020548A1
公开(公告)日：2010-02-25
申请号：PCT/EP2009/060316
申请日：2009-08-10
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , NARQUIZIAN, Robert , PINARD, Emmanuel
发明人： KOLCZEWSKI, Sabine , NARQUIZIAN, Robert , PINARD, Emmanuel
IPC分类号： C07D405/04 , A61P25/18 , A61P25/28 , A61K31/40 , A61K31/4025 , C07D305/08 , C07D231/14 , C07D241/42 , C07D319/18 , C07D333/54 , C07D498/08 , C07D295/13 , C07D491/107
CPC分类号： C07D305/08 , C07D231/14 , C07D241/42 , C07D295/033 , C07D319/18 , C07D333/54 , C07D491/107 , C07D498/16
摘要： The present invention relates to a compound of the general formula (I) wherein R 1 /R 2 are independently from each other lower alkyl, or form together with the N-atom to which they are attached a heterocyclic group, selected from pyrrolidine, piperidine, piperazine, 4-methyl-piperazine, 4-cyclopropyl-piperazine, thiomorpholine, morpholine, 1-(3-oxa-8-aza- bicyclo[3.2.1]oct-8-yl or 1-(2-oxa-6-aza-spiro[3.3]hept-6-yl; X is a bond, -CH 2 - or -O-; Ar 1 is aryl or heteroaryl, which are unsubstituted or substituted by one or two substituents selected from halogen, lower alkyl, lower alkoxy, or lower alkyl substituted by halogen; Ar 2 is aryl or heteroaryl, which are unsubstituted or substituted by one, two or three substituents selected from halogen, lower alkyl, lower alkoxy, hydroxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, benzyl or phenyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to their corresponding enantiomers and/or optical isomers thereof. It has surprisingly been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GIyT-1), and that they have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1 / R 2彼此独立地为低级烷基，或与它们所连接的N-原子一起形成杂环基，其选自吡咯烷，哌啶，哌嗪，4-甲基 - 哌嗪，4-环丙基 - 哌嗪，硫代吗啉，吗啉，1-（3-氧杂-8-氮杂 - 双环[3.2.1]辛-8-基或1-（2-氧杂-6-氮杂 - 螺[3.3]庚-6-基; X是键，-CH 2 - 或-O-; Ar 1是未取代的或被一个或两个选自卤素，低级烷基，低级烷氧基，或被卤素取代的低级烷基; Ar 2是未取代的或被1,2或3个选自卤素，低级烷基，低级烷氧基，羟基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，S 或低级烷基，苄基或苯基;或药学上可接受的酸加成盐，与外消旋混合物或其相应的能力其分子量和/或光学异构体。惊奇地发现通式（I）的化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，并且它们对甘氨酸转运蛋白2（GlyT-2）抑制剂具有良好的选择性。

6. 发明申请

WO2011161006A1 AMIDO-TROPANE DERIVATIVES 审中-公开
标题翻译： AMIDO-TROPANE衍生物
公开(公告)号：WO2011161006A1
公开(公告)日：2011-12-29
申请号：PCT/EP2011/060073
申请日：2011-06-17
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , PINARD, Emmanuel
发明人： KOLCZEWSKI, Sabine , PINARD, Emmanuel
IPC分类号： C07D451/02 , A61K31/46 , A61P25/00
CPC分类号： C07D451/02 , A61K9/2018 , A61K9/2054 , A61K9/4858 , A61K9/4866
摘要： The present invention relates to a compound of general formula (I) wherein R 1 , R 2 and R 3 are independently from each other hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1), and that they have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. The compounds may be used in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1，R 2和R 3彼此独立地为氢，低级烷基，低级烷氧基，环烷基，被卤素或S-低级烷基取代的低级烷基; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体。已经发现通式（I）的化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，并且它们对甘氨酸转运蛋白2（GlyT-2）抑制剂具有良好的选择性。该化合物可用于治疗神经和神经精神障碍。

7. 发明申请

WO2011023667A1 CARBOCYCLIC GLYT1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： CARBOCYCLIC GLYT1受体拮抗剂
公开(公告)号：WO2011023667A1
公开(公告)日：2011-03-03
申请号：PCT/EP2010/062281
申请日：2010-08-24
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , PINARD, Emmanuel
发明人： KOLCZEWSKI, Sabine , PINARD, Emmanuel
IPC分类号： C07C233/79 , C07C235/62 , C07C323/62 , C07D205/04 , C07D207/06 , C07D211/08 , C07D307/06 , C07D335/02 , C07D487/10 , C07D295/135 , A61K31/166 , A61K31/397 , A61K31/40 , A61K31/4453 , A61K31/495
CPC分类号： A61K31/166 , A61K31/397 , A61K31/40 , A61K31/4453 , A61K31/495 , A61K31/5375 , C07C233/79 , C07C235/62 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/06 , C07D207/10 , C07D207/12 , C07D211/38 , C07D211/46 , C07D295/12 , C07D295/20 , C07D309/14 , C07D335/02 , C07D487/10
摘要： The present invention relates to the use of a compound of general formula (I) wherein R 1 /R 2 are independently from each other hydrogen, lower alkyl, -CH 2 ) o -cycloalkyl for o being 0 or 1, or are benzyl or heterocycloalkyl; or R 1 and R 2 are together with the N-atom to which they are attached a ring containing -(CH 2 ) 3 -, -(CH 2 ) 4 -, -(CH 2 ) 5 -, -(CH 2 ) 2 -O-(CH 2 ) 2 -, -(CH 2 ) 2 -S-(CH 2 ) 2 -, -(CH 2 ) 2 -NR-(CH 2 ) 2 -, -(CH 2 ) 2 -C(O)-(CH 2 ) 2 -, -(CH 2 ) 2 -CF 2 -(CH 2 ) 2 -, -CH 2 -CHR-(CH 2 ) 2 , -CHR-(CH 2 ) 3 , CHR-(CH 2 ) 2 -CHR-, or is the ring 2,6-diaza-spiro[3.3]heptane-2-carboxylic acid tert-butyl ester and R is hydroxy, halogen, cycloalkyl, or C(O)O-lower alkyl; X is -(CH 2 ) 4 -, -(CH 2 ) 3 -, -(CH 2 ) 2 - or -CH 2 -; R 3 is S-lower alkyl, CF 3 , OCHF 2 , lower alkoxy, lower alkyl, phenyl, cycloalkyl or halogen; R 4 is CF 3 , lower alkoxy, lower alkyl, halogen and n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers thereof for the manufacture of a medicament for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1 / R 2彼此独立地是O，O或1的氢，低级烷基，-CH 2）o - 环烷基，或者是苄基或杂环烷基; （CH 2）3 - ， - （CH 2）4 - ， - （CH 2）5 - ， - （CH 2）2 -O-（CH 2）） - ， - （CH 2）2 -S-（CH 2）2 - ， - （CH 2）2 -NR-（CH 2）2 - ， - （CH 2）2 -C（O） - （CH 2）2 -CF 2 - （CH 2）2 - ， - CH 2 -CHR-（CH 2）2，-CHR-（CH 2）3，CHR-（CH 2）2 -CHR-，或环2,6-二氮杂 - 螺[3.3]庚烷-2-羧酸叔丁酯，R是羟基，卤素，环烷基或C（O）O-低级烷基; X是 - （CH 2）4 - ， - （CH 2）3 - ， - （CH 2）2 - 或-CH 2 - ; R3是S-低级烷基，CF3，OCHF2，低级烷氧基，低级烷基，苯基，环烷基或卤素; R4为CF3，低级烷氧基，低级烷基，卤素，n为1或2; 或其药学上可接受的酸加成盐，或其相应的对映体和/或光学异构体，用于制备用于治疗精神病，疼痛，记忆功能障碍和学习，注意力缺陷，精神分裂症，痴呆症或阿尔茨海默病。

8. 发明申请

WO2005014563A1 PIPERAZINE WITH OR-SUBSTITUTED PHENYL GROUP AND THEIR USE AS GLYT1 INHIBITORS 审中-公开
标题翻译：具有或取代的苯基的哌嗪及其作为GLYT1抑制剂的用途
公开(公告)号：WO2005014563A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008633
申请日：2004-08-02
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
IPC分类号： C07D295/192
CPC分类号： C07D239/42 , C07D213/85 , C07D241/20 , C07D251/42 , C07D257/04 , C07D263/32 , C07D271/06 , C07D295/192 , C07D309/12
摘要： The invention relates to compounds of formula (I) wherein the substituents are described in claim 1. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译：本发明涉及式（I）化合物，其中取代基描述于权利要求1中。该化合物可用于治疗基于甘氨酸摄取抑制剂的疾病，例如精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆症和认知过程受损的其他疾病，如注意力缺陷障碍或阿尔茨海默病。

9. 发明申请

WO2004072034A1 PIPERIDINE-BENZENESULFONAMIDE DERIVATIVES 审中-公开
标题翻译：哌嗪 - 苯甲酰胺衍生物
公开(公告)号：WO2004072034A1
公开(公告)日：2004-08-26
申请号：PCT/EP2004/001211
申请日：2004-02-10
申请人： F. HOFFMANN-LA ROCHE AG , ALBERATI-GIANI, Daniela , CECCARELLI, Simona, Maria , PINARD, Emmanuel , STALDER, Henri
发明人： ALBERATI-GIANI, Daniela , CECCARELLI, Simona, Maria , PINARD, Emmanuel , STALDER, Henri
IPC分类号： C07D211/58
CPC分类号： C07D413/12 , C07D211/58 , C07D401/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/14
摘要： The present invention relates to compounds of the general formula (I) wherein R 1 is lower alkyl, -(CH 2 ) n -aryl, unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, lower alkoxy, -OCF 3 , halogen, -NR’R” or trifluoromethyl, or heteroaryl; R 2 is lower alkyl, -(CH 2 ) n -aryl, unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen, trifluoromethyl, nitro, cyano, -NR’R”, hydroxy, or by a heteroaryl group, or is heteroaryl, unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl or halogen; R 3 is heteroaryl or is aryl, unsubstituted or substituted by halogen or lower alkyl; R 4 is hydrogen or hydroxy; A is -S(O) 2 -or-C(O)-; X,Y are independently from each other -CH 2 - or -O-, with the proviso that X and Y are not simultaneously -O; R’R” are independently from each other hydrogen, lower alkyl or -C(O)-lower alkyl; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds may be used for the treatment of psychoses, pain, disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer’s disease.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1为低级烷基， - （CH 2）n - 芳基，未取代或被一个或两个选自以下的取代基取代：低级烷基，低级烷氧基，-OCF 3，卤素，-NR'R“或三氟甲基或杂芳基; R 2是低级烷基， - （CH 2）n - 芳基，未取代或被一个或两个取代基取代，所述取代基选自低级烷基，低级烷氧基，卤素，三氟甲基，硝基，氰基，-NR'R“，羟基或杂芳基，或是未被取代或被一个或两个选自低级烷基或卤素的取代基取代的杂芳基; R 3是杂芳基或未被取代或被卤素或低级烷基取代的芳基; R 4是氢或羟基; A是-S（O）2 - 或-C（O） - ; X，Y彼此独立地为-CH 2 - 或-O-，条件是X和Y不同时为-O; R'R“彼此独立地为氢，低级烷基或-C（O） - 低级烷基; n为0,1或2;以及其药学上可接受的酸加成盐。该化合物可用于治疗精神病记忆障碍，学习障碍，精神分裂症，痴呆等认知过程受损的疾病，如注意力缺陷障碍或阿尔茨海默病。

10. 发明申请

WO2005023261A1 1-BENZOYL-PIPERAZINE DERIVATIVES AS GLYCINE UPTAKE INHIBITORS FOR THE TREATMENT OF PSYCHOSES 审中-公开
标题翻译：作为用于治疗心脏病的甘油摄取抑制剂的1-苯甲酰基哌嗪衍生物
公开(公告)号：WO2005023261A1
公开(公告)日：2005-03-17
申请号：PCT/EP2004/009699
申请日：2004-08-31
申请人： F. HOFFMANN-LA ROCHE AG , ALBERATI-GIANI, Daniela , JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
发明人： ALBERATI-GIANI, Daniela , JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
IPC分类号： A61K31/496
CPC分类号： C07D295/16 , A61K31/495 , A61K31/496 , C07D213/56 , C07D213/69 , C07D213/74 , C07D233/64 , C07D239/26 , C07D239/42 , C07D241/12 , C07D251/42 , C07D251/48 , C07D257/04 , C07D263/32 , C07D277/30 , C07D295/185 , C07D309/04 , C07D309/20 , C07D333/24 , C07D409/12
摘要： The invention relates to compounds of formula (I) wherein Ar is substituted aryl or unsubstituted or substituted 6-membered heteroaryl, containing one, two or three nitrogen atoms, and wherein the aryl and the heteroaryl groups may be substituted by one or more substituents selected from the group consisting of hydroxy, halogen, CN, (C 1 C 6 )-alkyl, (C 1 -C 6 )-alkyl substituted by halogen, (C 1 -C 6 )-alkoxy, (C 1 -C 6 )-alkoxy substituted by halogen, NR 7 R 8 , C(O)R 9 or SO 2 R 10 ; R 1 is hydrogen or (C 1 -C 6 )-alkyl; R 2 is halogen, (C 1 -C 6 ) -alkyl, (C 2 -C 6 ) -alkenyl, wherein a hydrogen atom may be replaced by CN, C(O)-R 9 or (C 1 -C 6 )-alkyl, or is (C 2 -C 6 )alkynyl, (C 1 -C 6 )-alkyl substituted by halogen, -(CH 2 ) n -(C 3 -C 7 )-cycloalkyl, -(CH 2 ) n -heterocycloalkyl, -C(O)-R 9 , -(CH 2 ) n -aryl or -(CH 2 ) n -5 or -6membered heteroaryl containing one, two or three heteroatoms, selected from the group consisting of oxygen, sulphur or nitrogen wherein aryl, cycloalkyl, heterocycloalkyl and heteroaryl are unsubstituted or substituted by one or more substituents selected from the group consisting of hydroxy, halogen, (C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkyl substituted by halogen or (C 1 -C 6 ) alkoxy; R 3 , R 4 and R 6 independently from each other are hydrogen, hydroxy, halogen, (C 1 -C 6 )-alkyl or (C 1 -C 6 )-alkoxy; R 5 is NO 2 , CN, C(O)R 9 , SO 2 R 10 or NR 11 R 12 ; R 7 and R 8 independently from each other are hydrogen or (C 1 -C 6 )-alkyl; the other substituents are defined in the claims; and to pharmaceutically acceptable acid addition salts thereof for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译：本发明涉及式（I）化合物，其中Ar是含有一个，两个或三个氮原子的取代的芳基或未取代或取代的6元杂芳基，其中芳基和杂芳基可以被一个或多个选自由羟基，卤素，CN，（C 1 -C 6） - 烷基，被卤素取代的（C 1 -C 6） - 烷基，（C 1 -C 6） - 烷氧基，被卤素取代的（C 1 -C 6） - 烷氧基，NR 7 R 8，C（O）R 9或SO 2 R 10; R 1是氢或（C 1 -C 6） - 烷基; R 2是卤素，（C 1 -C 6） - 烷基，（C 2 -C 6） - 烯基，其中氢原子可以被CN，C（O）-R 9或（C 1 -C 6） - 烷基或（C 2 -C 6）炔基，被卤素， - （CH 2）n - （C 3 -C 7） - 环烷基， - （CH 2）n - 杂环烷基，-C（O）-R 含有一个，两个或三个选自氧，硫或氮的杂原子的（CH 2）n - 芳基或 - （CH 2）n-5或 - （CH 2）n-5或-6元杂芳基，其中芳基，环烷基，杂环烷基和杂芳基是未取代的或被一个或多个选自羟基，卤素，（C 1 -C 6） - 烷基，被卤素或（C 1 -C 6）烷氧基取代的（C 1 -C 6） R 3，R 4和R 6彼此独立地是氢，羟基，卤素，（C 1 -C 6） - 烷基或（C 1 -C 6） - 烷氧基; R 5是NO 2，CN，C（O）R 9，SO 2 R 10或NR 11 R 12; R 7和R 8彼此独立地是氢或（C 1 -C 6） - 烷基; 其它取代基在权利要求中限定; 以及其药学上可接受的酸加成盐，用于治疗精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆和其他认知过程受损的其他疾病，如注意力缺陷障碍或阿尔茨海默病。

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