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1. 发明申请

US20080287547A1 Glycine Transport Inhibitors 失效
标题翻译：甘氨酸运输抑制剂
公开(公告)号：US20080287547A1
公开(公告)日：2008-11-20
申请号：US11718333
申请日：2005-12-21
申请人： Daniel Marcus Bradley , Clive Leslie Branch , Wai Ngor Chan , Steven Coulton , Martin Leonard Gilpin , Andrew Jonathan Harris , Albert Andrzej Jaxa-Chamiec , Justine Yeun Quai Lai , Jacqueline Anne Macritchie , Howard Robert Marshall , David John Nash , Roderick Alan Porter , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
发明人： Daniel Marcus Bradley , Clive Leslie Branch , Wai Ngor Chan , Steven Coulton , Martin Leonard Gilpin , Andrew Jonathan Harris , Albert Andrzej Jaxa-Chamiec , Justine Yeun Quai Lai , Jacqueline Anne Macritchie , Howard Robert Marshall , David John Nash , Roderick Alan Porter , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
IPC分类号： A61K31/166 , A61P25/00 , C07C233/65 , A61P25/18
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。

2. 发明申请

US20090270510A1 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸运输抑制剂
公开(公告)号：US20090270510A1
公开(公告)日：2009-10-29
申请号：US11722213
申请日：2005-12-21
申请人： Daniel Marcus Bradley , Clive Leslie Branch , Wai Ngor Chan , Steven Coulton , Martin Leonard Gilpin , Andrew Jonathan Harris , Justine Yeun Quai Lai , Jacqueline Anne Macritchie , Howard Robert Marshall , David John Nash , Roderick Alan Porter , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
发明人： Daniel Marcus Bradley , Clive Leslie Branch , Wai Ngor Chan , Steven Coulton , Martin Leonard Gilpin , Andrew Jonathan Harris , Justine Yeun Quai Lai , Jacqueline Anne Macritchie , Howard Robert Marshall , David John Nash , Roderick Alan Porter , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
IPC分类号： A61K31/166 , C07C321/10 , C07C233/78 , 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，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

US20080255144A1 Acylated Piperidines as Glycine Transporter Inhibitors 审中-公开
标题翻译：酰化哌啶酮作为甘氨酸转运蛋白抑制剂
公开(公告)号：US20080255144A1
公开(公告)日：2008-10-16
申请号：US11908151
申请日：2006-03-09
申请人： Daniel Marcus Bradley , Clive Leslie Branch , Wai Ngor Chan , Steven Coulton , Anthony William Dean , Paul Martin Doyle , Brian Evans , Martin Leonard Gilpin , Sharon Lisa Gough , Jacqueline Anne Macritchie , Howard Robert Marshall , David John Nash , Roderick Alan Porter , Simon Edward Ward
发明人： Daniel Marcus Bradley , Clive Leslie Branch , Wai Ngor Chan , Steven Coulton , Anthony William Dean , Paul Martin Doyle , Brian Evans , Martin Leonard Gilpin , Sharon Lisa Gough , Jacqueline Anne Macritchie , Howard Robert Marshall , David John Nash , Roderick Alan Porter , Simon Edward Ward
IPC分类号： A61K31/496 , C07D241/04 , C07D405/10 , C07D401/10 , A61P25/18 , C07D401/04 , A61K31/495
CPC分类号： C07D231/12 , C07D209/08 , C07D213/56 , C07D213/74 , C07D295/192 , C07D307/54 , C07D333/24 , C07D405/12 , C07D471/04
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, 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合物：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。

4. 发明申请

US20100216837A1 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸运输抑制剂
公开(公告)号：US20100216837A1
公开(公告)日：2010-08-26
申请号：US11722210
申请日：2005-12-21
申请人： Andrea Bozzoli , Daniel Marcus Bradley , Steven Coulton , Martin Leonard Gilpin , Jacqueline Anne MacRitchie , Roderick Alan Porter , Kevin Michael Thewlis
发明人： Andrea Bozzoli , Daniel Marcus Bradley , Steven Coulton , Martin Leonard Gilpin , Jacqueline Anne MacRitchie , Roderick Alan Porter , Kevin Michael Thewlis
IPC分类号： A61K31/4709 , C07C231/06 , A61K31/166 , C07D215/50 , A61K31/47 , C07D333/06 , A61K31/381 , C07D207/04 , A61K31/40 , A61P25/00
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。

5. 发明授权

US6022885A Pyrrolidine and thiazole derivatives with antibacterial and . metallo-.beta-lactamase inhibitory properties 失效
标题翻译：吡咯烷和噻唑衍生物具有抗菌和金属β-内酰胺酶抑制特性
公开(公告)号：US6022885A
公开(公告)日：2000-02-08
申请号：US29210
申请日：1998-06-10
申请人： Martin Leonard Gilpin , David John Payne , John Hargreaves Bateson
发明人： Martin Leonard Gilpin , David John Payne , John Hargreaves Bateson
IPC分类号： A61K31/40 , C07D207/16 , C07D277/06 , A61K31/425
CPC分类号： A61K31/40 , C07D207/16 , C07D277/06
摘要： This invention relates to a method of treating bacterial infections in humans or animals comprising administering, in combination with a .beta.-lactam antibiotic, a therapeutically effective amount of a compound of formula (I). ##STR1##
摘要翻译： PCT No.PCT / EP96 / 04014 Sec。 371日期：1998年6月10日 102（e）1998年6月10日PCT PCT 1996年9月9日PCT公布。出版物WO97 / 10225 日本1997年3月20日本发明涉及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）化合物。

6. 发明授权

US6156774A Beta-thiopropionyl-amino acid derivatives and their use as beta-lactamase inhibitors 失效
标题翻译： β-硫代丙酰氨基酸衍生物及其作为β-内酰胺酶抑制剂的用途
公开(公告)号：US6156774A
公开(公告)日：2000-12-05
申请号：US284098
申请日：1999-04-07
申请人： John Hargreaves Bateson , Desmond John Best , Brian Peter Clarke , Martin Leonard Gilpin , David Witty
发明人： John Hargreaves Bateson , Desmond John Best , Brian Peter Clarke , Martin Leonard Gilpin , David Witty
IPC分类号： A61K31/198 , A61K31/341 , A61K31/343 , A61K31/381 , A61K31/403 , A61K31/41 , A61K31/4166 , A61K31/4192 , A61K31/4406 , A61K31/4409 , A61P31/04 , C07C323/60 , C07C327/32 , C07D209/86 , C07D213/30 , C07D307/42 , C07D307/54 , C07D307/91 , C07D333/16 , C07D333/24 , C07D409/06 , A61K31/44 , C07D401/02
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 a in vivo hydrolysable ester-forming group; R.sub.1 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 --Z.sub.p --(CR.sub.8 CR.sub.9).sub.q -- or --(CR.sub.8 CR.sub.9).sub.q --Z.sub.p -- where p is 0 or 1, q is 0 to 3 provided that p+q in C is not 0, R.sub.8 and R.sub.9 are independently hydrogen or (C.sub.1-6)alkyl or together represent oxo and Z is O, NR.sub.10 or S(O).sub.x where R.sub.10 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)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); R.sub.2 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)alkyl; R.sub.3 is hydrogen, (C.sub.1-6)alkyl optionally substituted by up to three halogen atoms, (C.sub.3-7)cycloalkyl, fused aryl(C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl(C.sub.2-6)alkyl, (C.sub.2-6)alkenyl, (C.sub.2-6)alkynyl, aryl, aryl--(CH.sub.2).sub.m --X--(CH.sub.2).sub.n, heterocyclyl or heterocyclyl--(CH.sub.2).sub.m --X--(CH.sub.2).sub.n, where m is 0 to 3, n is 1 to 3 and X is O or S(O).sub.x where x is 0-2 or a bond; R.sub.4 is hydrogen or an in vivo hydrolysable acyl group; and R.sub.5 and R.sub.6 are independently hydrogen and (C.sub.1-6)alkyl or together represent (CH.sub.2).sub.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 antiobiotic.
摘要翻译： PCT No.PCT / EP97 / 05709 Sec。 371日期1999年4月7日 102（e）日期1999年4月7日PCT 1997年10月10日PCT公布。公开号WO98 / 17639 日期：1998年4月30日式（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）链烯基，（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为0-3，n为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-内酰胺抗生素联合施用来治疗人或动物中的细菌感染。

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