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1. 发明申请

WO2007147834A1 GLYCINE TRANSPORTER INHIBITING COMPOUNDS AND USES IN MEDICINE 审中-公开
标题翻译： GLYCINE运输机抑制化合物和药物用途
公开(公告)号：WO2007147834A1
公开(公告)日：2007-12-27
申请号：PCT/EP2007/056112
申请日：2007-06-20
申请人： GLAXO GROUP LIMITED , COULTON, Steven , GILPIN, Martin, Leonard , PORTER, Roderick, Alan
发明人： COULTON, Steven , GILPIN, Martin, Leonard , PORTER, Roderick, Alan
IPC分类号： C07C323/62 , C07D295/135 , A61K31/166 , A61K31/40 , A61P25/18
CPC分类号： C07C323/62 , C07C2601/08 , C07D295/125 , C07D295/135
摘要： Compounds of formula (I) and salts and solvates thereof are provided: wherein either 1 ) R1, R2, R3 and R4 and all methyl, or 2) R1 and R2 form a pyrrolidinyl group and R3 and R4 are both methyl, or 3) R1 and R2 are both methyl and R3 and R4 together form a cyclopentyl group. Uses in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, such as psychoses, dementia or attention deficit disorder, and processes to make these compounds and pharmaceutical formulations thereof are also disclosed.
摘要翻译：提供式（I）化合物及其盐和溶剂合物：其中1）R1，R2，R3和R4以及全部甲基，或2）R1和R2形成吡咯烷基，R3和R4均为甲基，或3） R1和R2都是甲基，R3和R4一起形成环戊基。还公开了用于制备用于治疗神经和神经精神障碍的药物的用途，例如精神病，痴呆或注意力缺陷障碍，以及制备这些化合物及其药物制剂的方法。

2. 发明申请

WO2006067423A1 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸运输抑制剂
公开(公告)号：WO2006067423A1
公开(公告)日：2006-06-29
申请号：PCT/GB2005/004951
申请日：2005-12-21
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , GILPIN, Martin, Leonard , HARRIS, Andrew, Jonathan , JAXA-CHAMIEC, Albert, Andrzej , LAI, Justine, Yeun, Quai , MARSHALL, Howard, Robert , MACRITCHIE, Jacqueline, Anne , NASH, David, John , PORTER, Roderick, Alan , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , GILPIN, Martin, Leonard , HARRIS, Andrew, Jonathan , JAXA-CHAMIEC, Albert, Andrzej , LAI, Justine, Yeun, Quai , MARSHALL, Howard, Robert , MACRITCHIE, Jacqueline, Anne , NASH, David, John , PORTER, Roderick, Alan , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07C233/78 , A61K31/166 , C07C211/36
CPC分类号： C07C233/78 , C07C235/50 , C07C235/60 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/20 , C07D209/02 , C07D295/13 , C07D307/22
摘要： The present invention relates to compounds of formula (I), or to salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：本发明涉及式（I）化合物或其盐或溶剂化物，其用于制备用于治疗神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍的药物。本发明还包括制备这些化合物及其药物制剂的方法。

3. 发明申请

WO2005049023A1 GLYT1 TRANSPORTER INHIBITORS 审中-公开
标题翻译： GLYT1输送机抑制剂
公开(公告)号：WO2005049023A1
公开(公告)日：2005-06-02
申请号：PCT/EP2004/013052
申请日：2004-11-16
申请人： GLAXO GROUP LIMITED , COULTON, Steven , GILPIN, Martin, Leonard
发明人： COULTON, Steven , GILPIN, Martin, Leonard
IPC分类号： A61K31/445
CPC分类号： C07D295/13 , C07D207/06 , C07D209/44 , C07D209/48 , C07D209/80 , C07D213/06 , C07D215/36 , C07D217/02 , C07D295/027 , C07D295/088 , C07D303/36 , C07D317/68 , C07D333/38 , C07D405/06
摘要： The invention provides a compound of formula (I): or a salt, solvate or a physiologically functional derivative thereof, wherein R1 to R10 are as defined in the specification and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
摘要翻译：本发明提供式（I）化合物或其盐，溶剂化物或生理功能衍生物，其中R 1至R 10如本说明书中所定义和这些化合物的用途。该化合物抑制GlyT1转运蛋白并且可用于治疗某些神经和神经精神障碍，包括精神分裂症。

4. 发明申请

WO1997010225A1 PYRROLIDINE AND THIAZOLE DERIVATIVES WITH ANTIBACTERIAL AND METALLO-BETA-LACTAMASE INHIBITORY PROPERTIES 审中-公开
标题翻译：具有抗菌和金属 - β-乳酸酶抑制性的吡咯烷和噻唑衍生物
公开(公告)号：WO1997010225A1
公开(公告)日：1997-03-20
申请号：PCT/EP1996004014
申请日：1996-09-09
申请人： SMITHKLINE BEECHAM PLC , GILPIN, Martin, Leonard , PAYNE, David, John , BATESON, John, Hargreaves
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D277/06
CPC分类号： A61K31/40 , C07D207/16 , C07D277/06 , Y02A50/478
摘要： A method of treatment of bacterial infections in humans or animals with comprises administering, in combination with a beta-lactam antibiotic, a therapeutically effective amount of a thiazolidine or proline derivative of formula (I) or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof. Compounds (IA) falling within the scope of formula (I) are also claimed; in formula (I): X is S, S(O)n or CH2; n is 1 or 2; R is hydrogen, a salt forming cation or an in vivo hydrolysable ester-forming group; R1 and R2 are each hydrogen or an organic substituent group; R3 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl(C1-6)alkyl, heterocyclyl or heterocyclyl(C1-6)alkyl; and R4 is hydrogen, or an in vivo hydrolysable acyl group. In compounds (IA) R3 represents (C1-6)alkyl substituted by up to three halogen atoms, aryl, aryl(C1-6)alkyl, heterocyclyl or heterocyclyl(C1-6)alkyl and X is S.
摘要翻译：一种治疗人或动物细菌感染的方法，包括与β-内酰胺抗生素组合施用治疗有效量的式（I）的噻唑烷或脯氨酸衍生物或其药学上可接受的盐，溶剂化物或体内可水解的的酯。属于公式（I）范围内的化合物（IA）也被要求保护; 在式（I）中：X是S，S（O）n或CH 2; n为1或2; R是氢，形成盐的阳离子或体内可水解的酯形成基团; R1和R2各自为氢或有机取代基; （C 2-6）炔基，芳基，芳基（C 1-6）烷基，杂环基或杂环基（C 1-6）烷基，任选被至多三个卤素原子取代的（C 1-6））烷基; R4是氢或体内可水解的酰基。在化合物（IA）中，R 3表示被至多三个卤素原子取代的（C 1-6）烷基，芳基，芳基（C 1-6）烷基，杂环基或杂环基（C 1-6）烷基，X是S.

5. 发明申请

WO1989002441A1 ANTIBIOTIC COMPOUNDS 审中-公开
标题翻译：抗生素化合物
公开(公告)号：WO1989002441A1
公开(公告)日：1989-03-23
申请号：PCT/GB1988000752
申请日：1988-09-16
申请人： BEECHAM GROUP PLC , ATHALYE, Medha , ELSON, Anna , GILPIN, Martin, Leonard , JEFFRIES, Leonard, Richard
发明人： BEECHAM GROUP PLC
IPC分类号： C07K09/00
CPC分类号： C12R1/01 , A61K38/00 , C07K9/008
摘要： Glycopeptide antibiotics MM 45289 and MM 47756 are produced by Amycolatopsis orientalis strain NCIB 12531. They have formula (I), wherein R is hydrogen or chlorine.

6. 发明申请

WO2006094840A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2006094840A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/002480
申请日：2006-03-09
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , BROWN, Bethany, Joy , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , STASI, Luigi, Piero
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , BROWN, Bethany, Joy , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , STASI, Luigi, Piero
IPC分类号： C07D295/18 , A61P25/00 , A61K31/495
CPC分类号： C07D295/192
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R 1 , n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
摘要翻译：本发明提供式（I）化合物或其盐或溶剂化物：其中R 1，n，X，Y和Z如说明书中所定义，以及这些化合物的用途。该化合物抑制GlyT1转运蛋白并且可用于治疗某些神经和神经精神障碍，包括精神分裂症。

7. 发明申请

WO1998017639A1 BETA-THIOPROPIONYL-AMINO ACID DERIVATIVES AND THEIR USE AS BETA-LACTAMASE INHIBITORS 审中-公开
标题翻译： β-谷氨酰氨基酸衍生物及其作为β-乳酸酶抑制剂的用途
公开(公告)号：WO1998017639A1
公开(公告)日：1998-04-30
申请号：PCT/EP1997005709
申请日：1997-10-10
申请人： SMITHKLINE BEECHAM PLC , BATESON, John, Hargreaves , BEST, Desmond, John , CLARKE, Brian, Peter , GILPIN, Martin, Leonard , WITTY, David, R.
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07C323/60
CPC分类号： C07D307/91 , C07C323/60 , C07C327/32 , C07D209/86 , C07D213/30 , C07D307/54 , C07D333/16 , C07D333/24 , C07D409/06
摘要： Mercapto amino acid derivatives of formula (I), wherein R is hydrogen, a salt-forming cation of an in vivo hydrolysable ester-forming group; R1 is selected from (a) and (b) in which A is a monocyclic aryl or heteroaryl ring and B is a monocyclic aryl, alicyclic or heterocyclic ring, C and D are independently -Zp-(CR8CR9)q- or -(CR8CR9)q-Zp- where p is 0 or 1, q is 0 to 3 provided that p + q in C is not 0, R8 and R9 are independently hydrogen or (C1-6)alkyl or together represent oxo and Z is O, NR10 or S(O)x where R10 is hydrogen, (C1-6)alkyl or aryl(C1-6)alkyl and x is 0-2, and wherein C and D are linked ortho to one another on each of the rings A and B in formula (b); R2 is hydrogen, (C1-6)alkyl or aryl(C1-6)alkyl; R3 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms, (C3-7)cycloalkyl, fused aryl(C3-7)cycloalkyl, (C3-7)cycloalkyl(C2-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl-(CH2)m-X-(CH2)n, heterocyclyl or heterocyclyl-(CH2)m-X-(CH2)n, where m is 0 to 3, n is 1 to 3 and X is O or S(O)x where x is 0-2 or a bond; R4 is hydrogen or an in vivo hydrolysable acyl group; and R5 and R6 are independently hydrogen and (C1-6)alkyl or together represent (CH2)r, where r is 2 to 5; for use in treatment of bacterial infections in humans or animals by administration in combination with a beta -lactam antibiotic.
摘要翻译：式（I）的巯基氨基酸衍生物，其中R是氢，体内可水解的酯形成基团的成盐阳离子; R1选自（a）和（b），其中A是单环芳基或杂芳基环，B是单环芳基，脂环族或杂环，C和D独立地是-Zp-（CR8CR9）q-或 - （CR8CR9 ）q-Zp-其中p为0或1，q为0至3，条件是C中的p + q不为0，R8和R9独立地为氢或（C1-6）烷基或一起代表氧代，Z为O， NR10或S（O）x，其中R10是氢，（C1-6）烷基或芳基（C1-6）烷基，x是0-2，并且其中C和D在每个环A上彼此原子连接和式（b）中的B; R2是氢，（C1-6）烷基或芳基（C1-6）烷基; R3是氢，任选被至多三个卤素原子取代的（C 1-6）烷基，（C 3-7）环烷基，稠合芳基（C 3-7）环烷基，（C 3-7）环烷基（C 2-6）烷基，（C 2 -6）烯基，（C2-6）炔基，芳基，芳基 - （CH2）mX-（CH2）n，杂环基或杂环基 - （CH2）mX-（CH2）n，其中m是0-3，n是1 至3且X为O或S（O）x，其中x为0-2或键; R4是氢或体内可水解的酰基; 并且R 5和R 6独立地为氢和（C 1-6）烷基或一起代表（CH 2）r，其中r为2至5; 用于通过与β-内酰胺抗生素组合施用来治疗人或动物中的细菌感染。

8. 发明申请

WO2007147839A1 GLYCINE TRANSPORTER INHIBITING COMPOUNDS AND USES IN MEDICINE 审中-公开
标题翻译：甘氨酸转运蛋白抑制化合物和药物用途
公开(公告)号：WO2007147839A1
公开(公告)日：2007-12-27
申请号：PCT/EP2007/056120
申请日：2007-06-20
申请人： GLAXO GROUP LIMITED , COULTON, Steven , GILPIN, Martin, Leonard , PORTER, Roderick, Alan
发明人： COULTON, Steven , GILPIN, Martin, Leonard , PORTER, Roderick, Alan
IPC分类号： C07C235/50 , C07C235/60 , C07D295/12 , A61K31/166
CPC分类号： C07C235/60 , C07D295/13
摘要： Compounds of formula (I) and salts and solvates thereof are provided: wherein R1 and R2 are both methyl, or R1 and R2 form a pyrrolidinyl group. Uses in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, such as psychoses, dementia or attention deficit disorder, and processes to make these compounds and pharmaceutical formulations thereof are also disclosed.
摘要翻译：提供式（I）化合物及其盐和溶剂合物：其中R1和R2均为甲基，或R1和R2形成吡咯烷基。还公开了用于治疗神经和神经精神障碍的药物的用途，例如精神病，痴呆或注意力缺陷障碍，以及制备这些化合物及其药物制剂的方法。

9. 发明申请

WO2006067414A3 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸运输抑制剂
公开(公告)号：WO2006067414A3
公开(公告)日：2006-09-08
申请号：PCT/GB2005004937
申请日：2005-12-21
申请人： GLAXO GROUP LTD , BOZZOLI ANDREA , BRADLEY DANIEL MARCUS , COULTON STEVEN , GILPIN MARTIN LEONARD , MACRITCHIE JACQUELINE ANNE , PORTER RODERICK ALAN , THEWLIS KEVIN MICHAEL
发明人： BOZZOLI ANDREA , BRADLEY DANIEL MARCUS , COULTON STEVEN , GILPIN MARTIN LEONARD , MACRITCHIE JACQUELINE ANNE , PORTER RODERICK ALAN , THEWLIS KEVIN MICHAEL
IPC分类号： C07C233/78 , A61K31/166 , A61K31/381 , A61K31/47 , C07C211/29 , C07C211/36 , C07D215/50 , C07D333/20 , C07D409/12
CPC分类号： C07C211/36 , C07C211/29 , C07C229/34 , C07C233/78 , C07C271/22 , C07C2601/08 , C07D215/50 , C07D295/13 , C07D333/20 , C07D409/12
摘要： The present invention relates to compounds of formula (I), or salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：本发明涉及式（I）化合物或其盐或溶剂合物，其用于制备用于治疗神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍的药物。本发明还包括制备这些化合物及其药物制剂的方法。

10. 发明申请

WO2006067417A1 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸运输抑制剂
公开(公告)号：WO2006067417A1
公开(公告)日：2006-06-29
申请号：PCT/GB2005/004943
申请日：2005-12-21
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , GILPIN, Martin, Leonard , HARRIS, Andrew, Jonathan , LAI, Justine, Yeun, Quai , MARSHALL, Howard, Robert , MACRITCHIE, Jacqueline, Anne , NASH, David, John , PORTER, Roderick, Alan , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , GILPIN, Martin, Leonard , HARRIS, Andrew, Jonathan , LAI, Justine, Yeun, Quai , MARSHALL, Howard, Robert , MACRITCHIE, Jacqueline, Anne , NASH, David, John , PORTER, Roderick, Alan , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07C233/78 , A61K31/166 , C07C211/27
CPC分类号： C07C235/60 , C07C211/27 , C07C233/78 , C07C235/50 , C07C323/62
摘要： The present invention relates to compounds of Formula (I), or salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：本发明涉及式（I）化合物或其盐或溶剂合物，它们在制备用于治疗神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍的药物中的用途。本发明还包括制备这些化合物及其药物制剂的方法。

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