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11. 发明申请

WO2009100994A1 PIPERIDINE SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：哌啶磺酰胺衍生物
公开(公告)号：WO2009100994A1
公开(公告)日：2009-08-20
申请号：PCT/EP2009/051135
申请日：2009-02-02
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07D211/96 , C07D401/06 , A61K31/54 , A61K31/4545 , A61P25/00
CPC分类号： C07D401/06 , C07D211/96
摘要： The present invention relates to piperidine sulphonamide derivatives of formula (I) wherein Ar 1 , Ar 2 , R 1 , R 2 , m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds may be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
摘要翻译：本发明涉及式（I）的哌啶磺酰胺衍生物，其中Ar1，Ar2，R1，R2，m和n如说明书和权利要求中所定义，或其药学上合适的酸加成盐。式I化合物是食欲蛋白受体拮抗剂，相关化合物可用于治疗睡眠呼吸暂停，发作性睡病，失眠，睡眠不足，时差综合症，昼夜节律障碍或与神经疾病相关的睡眠障碍。

12. 发明申请

WO2018104419A1 NEW ISOXAZOLYL ETHER DERIVATIVES AS GABA A ALPHA5 PAM 审中-公开
公开(公告)号：WO2018104419A1
公开(公告)日：2018-06-14
申请号：PCT/EP2017/081768
申请日：2017-12-07
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BUETTELMANN, Bernd , CECERE, Giuseppe , FASCHING, Bernhard , GROEBKE ZBINDEN, Katrin , HERNANDEZ, Maria-Clemencia , KNUST, Henner , KOBLET, Andreas , PINARD, Emmanuel , THOMAS, Andrew
IPC分类号： C07D413/14 , A61K31/4439 , A61K31/501 , A61P25/28
摘要： The invention provides novel compounds having the general formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X, Y and Z are as described herein, compositions including the compounds and methods of using the compounds.

13. 发明申请

WO2017037146A1 PHENOXYMETHYL DERIVATIVES 审中-公开
标题翻译：苯甲基衍生物
公开(公告)号：WO2017037146A1
公开(公告)日：2017-03-09
申请号：PCT/EP2016/070561
申请日：2016-09-01
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： HERT, Jérôme , 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 , C07D231/12 , C07D231/56 , C07D401/12 , C07D237/14 , C07D407/04 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D249/12 , C07D471/04 , C07D487/04 , C07F7/08 , A61P27/02
CPC分类号： C07D249/08 , A61P27/02 , C07B41/04 , C07C205/04 , C07C255/50 , C07C317/14 , C07D231/12 , C07D231/20 , C07D231/56 , C07D237/14 , C07D249/04 , C07D249/12 , C07D401/12 , C07D403/12 , C07D407/04 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07F7/0812
摘要： The invention provides novel compounds having the general formula (I), wherein R A , R B , R C , R C1 and W are as defined herein, compositions including the compounds and methods of using the compounds.
摘要翻译：本发明提供具有通式（I）的新化合物，其中RA，RB，RC，RC1和W如本文所定义，包括该化合物的组合物和使用该化合物的方法。

14. 发明申请

WO2015197503A1 IMIDAZO[1,2-A]PYRAZIN-1YL-BENZAMIDE COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY 审中-公开
标题翻译：咪达唑[1,2-A]吡嗪-1-基 - 苯甲酰化合物治疗脊髓性肌阵挛
公开(公告)号：WO2015197503A1
公开(公告)日：2015-12-30
申请号：PCT/EP2015/063894
申请日：2015-06-22
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GREEN, Luke , PINARD, Emmanuel , RATNI, Hasane , WILLIAMSON, Patrick
IPC分类号： C07D487/04 , A61K31/519 , A61P21/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides compounds of formula (I) wherein A, X l , X 2 , R 1 , R 2 , R 3 , R 4 and R 5 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of spinal muscular atrophy.
摘要翻译：本发明提供式（I）化合物，其中A，X1，X2，R1，R2，R3，R4和R5如本文所述，以及其药学上可接受的盐。此外，本发明涉及制备式（I）化合物，包含它们的药物组合物及其作为用于治疗脊髓性肌肉萎缩的药物的用途。

15. 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。

16. 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。

17. 发明申请

WO2009016087A1 MONOAMIDE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：单酰胺衍生物作为OREXIN受体拮抗剂
公开(公告)号：WO2009016087A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059697
申请日：2008-07-24
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07C233/88 , C07C235/68 , C07C235/78 , C07D277/62 , C07D317/48 , A61K31/167 , A61K31/357 , A61K31/428 , A61P25/20
CPC分类号： C07D405/12 , C07C233/29 , C07C235/38 , C07C235/80 , C07C237/20 , C07C237/22 , C07C251/48 , C07C255/58 , C07C255/60 , C07C271/22 , C07D205/04 , C07D207/12 , C07D209/44 , C07D211/46 , C07D213/56 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/16 , C07D235/26 , C07D277/62 , C07D305/02 , C07D305/08 , C07D307/14 , C07D307/52 , C07D307/79 , C07D317/28 , C07D317/46 , C07D317/66 , C07D319/20 , C07D333/24 , C07D471/04 , C07D487/04 , C07D491/107
摘要： The present invention relates to compounds of formula (I), wherein Ar is aryl or heteroaryl; R 1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, cyano, SO 2 -lower alkyl or hydroxy; R 2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, cyano, S-lower alkyl, SO 2 -lower alkyl, NO 2 or hydroxy; R 3 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, -(CH 2 ) m -O-lower alkyl, lower alkoxy substituted by halogen, 3-hydroxy-oxetan-3-yl, cyano or SO 2 -lower alkyl; or if o is 2, R 3 may form in 3 and 4 position together with the carbon atoms to which they are attached an addional ring with the groups -O-CH 2 -O-, -O-CF 2 -CF 2 -O-, -N=CH-S-, -O-CF 2 -O-, -(CH 2 ) 4 -, -NH-C(O)-NH-, -O-(CH 2 ) 2 - or _(CH 2 ) 2 -O-; R 4 /R 5 are independently from each other hydrogen, -(CR" 2 ) m OH, lower alkyl, lower alkoxy, -NRR', or is -(CH 2 ) 0,1 -heterocycloalkyl, optionally substituted by hydroxy, or R 4 and R 5 are together =O or =N-OH,; R/R' are independently from each other hydrogen, lower alkyl, C(O)H, -(CR" 2 )m-OH, -(CR" 2 )m-NR" 2 , -(CR" 2 ) m -NR"-C(O)-lower alkyl, -(CR" 2 ) m -O-lower alkyl, -(CR" 2 ) m -O-lower alkenyl, -C(O)O-lower alkyl, -C(O)-CR" 2 -NH-C(O)O-lower alkyl, -C(O)-CR" 2 -NR" 2 , or is -(CH 2 ) 0,1 -heterocycloalkyl or -(CH 2 ) 0,1 -furan-2-yl; R" are independently from each other hydrogen, lower alkoxy, phenyl or lower alkyl; n is 1, 2, 3 or 4; o is 1, 2 or 3; p is 1, 2 or 3; m is 1, 2 or 3; or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds of formula (I) may be used for example for the treatment of the sleep disorders, which are sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
摘要翻译：本发明涉及式（I）化合物，其中Ar为芳基或杂芳基; R 1为氢，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，氰基，SO 2 - 低级烷基或羟基; R 2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，氰基，S-低级烷基，SO 2 - 低级烷基，NO 2或羟基; R 3是氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基， - （CH 2）m -O-低级烷基，被卤素取代的低级烷氧基，3-羟基 - 氧杂环丁烷-3-基，氰基或SO 2 - 低级烷基; 或者如果o是2，则R3可以与它们所连接的碳原子一起形成3和4位与-O-CH 2 -O-，-O-CF 2 -CF 2 -O-，-N = CH-S-，-O-CF2-O-， - （CH2）4-，-NH-C（O）-NH-，-O-（CH2）2-或_（CH2） R 4 / R 5彼此独立地为氢， - （CR“2）mOH，低级烷基，低级烷氧基，-NRR'或为任选被羟基取代的 - （CH 2）0,1 - 杂环烷基，或R 4和R 5为一起= O或= N-OH; R / R'彼此独立地为氢，低级烷基，C（O）H， - （CR“2）m -OH， - （CR”2）m -NR“ 2， - （CR“2）m-NR”-C（O） - 低级烷基， - （CR“2）mO-低级烷基， - （CR”2）mO-低级烯基，-C（O）低级烷基，-C（O）-CR“2-NH-C（O）O-低级烷基，-C（O）-CR”2 -NR“2或为 - （CH 2） - （CH 2）0,1 - 呋喃-2-基; R“彼此独立地为氢，低级烷氧基，苯基或低级烷基; n为1,2,3或4; o是1,2或3; p为1,2或3; m为1,2或3; 或其药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。式（I）的化合物可用于例如睡眠呼吸暂停，发作性睡眠，失眠，睡眠睡眠，时差综合征，昼夜节律障碍或与神经疾病相关的睡眠障碍的睡眠障碍。

18. 发明申请

WO2008022938A1 DI-AROMATIC SUBSTITUTED AMIDES AS INHIBITORS FOR GLYT1 审中-公开
标题翻译：作为GLYT1抑制剂的DI-AROMATIC取代的氨基酸
公开(公告)号：WO2008022938A1
公开(公告)日：2008-02-28
申请号：PCT/EP2007/058350
申请日：2007-08-13
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , PINARD, Emmanuel
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , PINARD, Emmanuel
IPC分类号： C07C237/22 , C07C255/57 , C07C271/22 , C07C275/24 , C07D213/40 , C07D213/81 , C07D261/18 , C07D275/02 , C07D279/02 , C07D307/79 , C07D333/20 , C07D333/38 , C07D333/44 , C07D335/18 , A61K31/16
CPC分类号： C07C237/22 , C07C255/57 , C07C271/22 , C07C275/24 , C07C2601/14 , C07D213/40 , C07D213/81 , C07D261/18 , C07D275/02 , C07D279/02 , C07D307/79 , C07D333/20 , C07D333/38 , C07D333/44 , C07D335/18
摘要： The present invention relates to compounds of the general Formula (I) wherein (A) is a 5 or 6-membered aromatic or heteroaromatic ring; R 1 is cycloalkyl or is aryl or heteroaryl, wherein at least one ring is aromatic in nature, unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, -C(O) -lower alkyl, -S(O) 2 -lower alkyl, nitro or cyano; R 2 is hydrogen or lower alkyl; R 3 is hydrogen or lower alkyl; R 4 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or nitro; R 5 is hydrogen, halogen, lower alkyl or lower alkyl substituted by halogen; X is a bond, -(CH 2 ) m -, -CH 2 O- or -CH 2 NH-; The dotted line denotes a bond or not; n is 1 or 2; m is 1, 2 or 3; and pharmaceutically acceptable acid addition salts thereof and 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（A）是5或6元芳族或杂芳族环; R 1是环烷基或芳基或杂芳基，其中至少一个环在本质上是芳族的，未被取代或被1至3个选自以下的取代基取代：卤素，低级烷基，被卤素，低级烷氧基，被卤素取代的低级烷氧基，-C（O） - 低级烷基，-S（O）2 - 低级烷基，硝基或氰基; R 2是氢或低级烷基; R 3是氢或低级烷基; R 4是卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素或硝基取代的低级烷氧基; R 5是氢，卤素，被卤素取代的低级烷基或低级烷基; X是一个键， - （CH 2）2 - ， - CH 2 O-或-CH 2 - NH-; 虚线表示不是键; n为1或2; m为1,2或3; 及其药学上可接受的酸加成盐及其在治疗神经和神经精神障碍中的用途。

19. 发明申请

WO2007147770A3 SUBSTITUTED PHENYL METHANONE DERIVATIVES 审中-公开
公开(公告)号：WO2007147770A3
公开(公告)日：2007-12-27
申请号：PCT/EP2007/055871
申请日：2007-06-14
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger , PINARD, Emmanuel
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger , PINARD, Emmanuel
IPC分类号： C07D205/04 , C07D207/06 , C07D211/16 , C07D407/10 , A61K31/445 , A61P25/18
摘要： The present invention relates to compounds of the general formula (i), wherein R 1 is -OR 1 ' , heterocycloalkyl, aryl or heteroaryl, which are unsubstituted or substituted by lower alkyl or halogen; R1' is lower alkyl, lower alkyl substituted by halogen, or is -(CH 2 ) o -cycloalkyl; R 2 is -S(O) 2 -lower alkyl, -S(O) 2 NH-lower alkyl, NO 2 or CN; R 3 is aryl or heteroaryl, which are unsubstituted or substituted by one to three substituents, selected from the group consisting of lower alkyl, lower alkoxy, CN, NO 2 , halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, aryl or sulfonamide; X is a bond, -CH 2 -, -NH-, -CH 2 O- or -OCH 2 -; n is 1 or 2; m is 1 or 2; o is 0 or 1; to pharmaceutically acceptable acid addition salts thereof, to pharmaceutical compositions containing them and their use in the treatment of neurological and neuropsychiatric disorders. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1).

20. 发明申请

WO2006072436A1 [4-(HETEROARYL) PIPERAZIN-1-YL]-(2,5-SUBSTITUTED -PHENYL)METHANONE DERIVATIVES AS GLYCINE TRANSPORTER 1 (GLYT-1) INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS 审中-公开
标题翻译：作为用于治疗神经病学和神经病学疾病的甘氨酸运输1（GLYT-1）抑制剂的[4-（异丁基）哌嗪-1-基] - （2,5-取代的苯基）甲酮衍生物
公开(公告)号：WO2006072436A1
公开(公告)日：2006-07-13
申请号：PCT/EP2005/014082
申请日：2005-12-28
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger, David , PINARD, Emmanuel
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger, David , PINARD, Emmanuel
IPC分类号： A61K31/427 , A61K31/433 , A61P25/28 , C07D277/42 , C07D277/56 , C07D417/12 , C07D285/12 , C07D285/08
CPC分类号： C07D285/08 , C07D277/42 , C07D277/56 , C07D285/135 , C07D417/12
摘要： The present invention relates to compounds of the general formula (I) wherein R 1 is-OR 1’ ,-SR 1’ or is a heterocycloalkyl group; R 1’ is lower alkyl, lower alkyl substituted by halogen or is -(CH 2 ) n -cycloalkyl; R 2 is-S(O) 2 -lower alkyl, -S(O) 2 NH-lower alkyl, NO 2 or CN; X 1 is CR 3 or N; X 2 is CR 3’ or N; R 3 /R 3’ are independently from each other hydrogen, halogen, lower alkyl, CN, NO 2 ,-S(O) 2 -phenyl, -S(O) 2 -lower alkyl, -S(O) 2 -pyridin-2, 3 or 4-yl, phenyl, optionnally substituted by one or two substituents selected from the group consisting of NO 2 or halogen, or is lower alkyl substituted by halogen or is -C(O)-lower alkyl; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1). They may be used in the treatment of schizophrenia.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1是 - 或 - 1'， - SR 1'或其是杂环烷基 R 1是低级烷基，被卤素取代的低级烷基或是 - （CH 2 CH 2）n - 环烷基; R 2是-S（O）2 - 低级烷基，-S（O）2 NH-低级烷基，NO 2 或CN; X 1是CR 3或N; X 2是CR 3或N; R 3和R 3彼此独立地为氢，卤素，低级烷基，CN，NO 2，-S（O） -S（O）2 - 低级烷基，-S（O）2 - 吡啶基-2,3或4-基 - ，苯基，其选自一个或两个选自NO 2或卤素的取代基，或被卤素取代的低级烷基或-C（O） - 低级烷基; n为0,1或2; 及其药学上可接受的酸加成盐。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。它们可用于治疗精神分裂症。

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