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51. 发明申请

WO2002072536A1 UREA DERIVATIVES HAVING VANILLOID RECEPTOR (VR1) ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有VANILLOID受体（VR1）拮抗剂活性的尿素衍生物
公开(公告)号：WO2002072536A1
公开(公告)日：2002-09-19
申请号：PCT/GB2002/001046
申请日：2002-03-07
申请人： SMITHKLINE BEECHAM P.L.C. , RAMI, Harshad, Kantilal , THOMPSON, Mervyn , WYMAN, Paul, Adrian
发明人： RAMI, Harshad, Kantilal , THOMPSON, Mervyn , WYMAN, Paul, Adrian
IPC分类号： C07C275/40
CPC分类号： C07J63/008 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/42 , C07C323/44
摘要： The invention relates to novel compounds having Vanilloid Receptor (VR1) antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders.
摘要翻译：本发明涉及具有香草素受体（VR1）拮抗剂活性的新化合物，其制备方法，含有它们的组合物及其在治疗各种疾病中的用途。

52. 发明申请

WO0006575A3 AZABICYCLIC COMPOUNDS 审中-公开
标题翻译：偶氮化合物
公开(公告)号：WO0006575A3
公开(公告)日：2000-05-18
申请号：PCT/EP9905350
申请日：1999-07-23
申请人： SMITHKLINE BEECHAM PLC , GASTER LARAMIE MARY , HEIGHTMAN THOMAS DANIEL , WYMAN PAUL ADRIAN
发明人： GASTER LARAMIE MARY , HEIGHTMAN THOMAS DANIEL , WYMAN PAUL ADRIAN
IPC分类号： C07D471/04 , C07D471/08 , C07D487/04 , A61K31/4985 , A61K31/551 , A61P25/00 , C07D455/02 , C07D487/08
CPC分类号： C07D471/04 , C07D471/08 , C07D487/04
摘要： The invention relates to novel azabicyclic compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.
摘要翻译：本发明涉及具有药理活性的新型氮杂双环化合物，其制备方法，含有它们的组合物及其在治疗CNS障碍中的用途。

53. 发明申请

WO9850346A2 ACETAMIDE AND UREA DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：乙酰胺和尿酸衍生物，其制备方法及其在治疗CNS疾病中的应用
公开(公告)号：WO9850346A2
公开(公告)日：1998-11-12
申请号：PCT/EP9802263
申请日：1998-04-14
申请人： SMITHKLINE BEECHAM PLC , GASTER LARAMIE MARY , WYMAN PAUL ADRIAN
发明人： GASTER LARAMIE MARY , WYMAN PAUL ADRIAN
IPC分类号： C07C233/29 , C07C271/58 , C07C275/34 , C07C275/36 , C07C275/40 , C07C323/44 , C07D209/08 , C07D213/40 , C07D213/56 , C07D401/06 , C07D401/12 , C07D401/14 , C07C275/32 , A61K31/16 , A61K31/17 , A61K31/395
CPC分类号： C07D213/40 , C07C233/29 , C07C271/58 , C07C275/34 , C07C275/36 , C07C275/40 , C07C323/44 , C07D209/08 , C07D213/56 , C07D401/06 , C07D401/12 , C07D401/14
摘要： Compounds of formula (I), processes for their preparation and their use as CNS agents are disclosed, in which R is a group of formula (i), in which P is phenyl, bicyclic aryl, a 5- to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen and sulphur, or a bicyclic heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen and sulphur; or R is a group of formula (ii); L is a group of formula -Y-C(=V)-DG-, in which Y is -NH-, NR where R is C1-6alkyl, or Y is -CH2- or -O-; V is oxygen or sulphur; D is nitrogen, carbon or a CH group, G is hydrogen or C1-6alkyl providing that D is nitrogen or a CH group, or G together with R forms a group W where W is (CR R )t where t is 2, 3 or 4 and R and R are independently hydrogen or C1-6alkyl or W is (CR R )u-J where u is 0, 1, 2 or 3 and J is oxygen, sulphur, CR =CR , CR =N, =CR O, =CR S or =CR -NR ; B is CH2, oxygen, S(O)p where p is 0, 1 or 2, NR where R6 is hydrogen or C1-6alkyl or B is CR =CR where R and R are independently hydrogen or C1-6alkyl; R and R are independently hydrogen or C1-6alkyl; R is a 5- to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen and sulphur, or R is a group of formula -NR R in which R and R are independently hydrogen, C1-6alkyl or aralkyl; R and R are independently hydrogen, halogen, hydroxy, C1-6alkyl, trifluoromethyl, C1-6alkoxy or aryl, or R together with G forms a group W as defined above; and n is 0, 1, 2, 3 or 4.
摘要翻译：公开了式（I）化合物及其制备方法及其作为CNS剂的用途，其中R a为式（ⅰ）基团，其中P 1为苯基，双环芳基，含有1至3个选自氧，氮和硫的杂原子的7元杂环，或含有1至3个选自氧，氮和硫的杂原子的双环杂环; 或R a是式（ii）的基团; L是式-Y-C（= V）-DG-的基团，其中Y是-NH-，NR5，其中R 5是C 1-6烷基，或Y是-CH 2 - 或-O-; V是氧或硫; D是氮，碳或CH基，G是氢或C 1-6烷基，条件是D是氮或CH基，或G与R b1一起形成基团W，其中W是（CR 16 R 17）其中t是2,3或4，R 16和R 17独立地是氢或C 1-6烷基或W是（CR 16 R 17）其中u是0,1,2 或3，并且J为氧，硫，CR 16 = CR 17，CR 16 = N，= CR 16 O，= CR 16 S或= CR 16 -NR 17 ; B是CH 2，氧，S（O）p，其中p是0,1或2，NR 6，其中R 6是氢或C 1-6烷基或B是CR 7 = CR 8，其中R 7和 R 8独立地是氢或C 1-6烷基; R c和R d独立地是氢或C 1-6烷基; R y是含有1至3个选自氧，氮和硫的杂原子的5至7元杂环，或R y是式-NR e R f的基团，其中R“ e>和R f独立地是氢，C 1-6烷基或芳烷基; R b1和R b2独立地是氢，卤素，羟基，C 1-6烷基，三氟甲基，C 1-6烷氧基或芳基，或者R b与G一起形成如上定义的基团W; n为0,1,2,3或4。

54. 发明申请

WO1997034900A1 AZASPIRO DERIVATIVES 审中-公开
标题翻译： AZASPIRO衍生物
公开(公告)号：WO1997034900A1
公开(公告)日：1997-09-25
申请号：PCT/EP1997001405
申请日：1997-03-19
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , WYMAN, Paul, Adrian
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D491/20
CPC分类号： C07D491/20
摘要： Compounds of formula (I) where P is a 5- to 7-membered carbocyclic or heterocyclic ring containing one to four heteroatoms selected from oxygen, nitrogen or sulphur, R is O, S, CH2, C=O, NR CO or NR , D is nitrogen or carbon, E is O, CR R , NR with 5HT1B receptor antagonist activity.
摘要翻译：其中P为含有1-4个选自氧，氮或硫的杂原子的5-至7-元碳环或杂环的式（I）化合物，R 4为O，S，CH 2，C = O， 5 CO或NR 5，D是氮或碳，E是具有5HT1B受体拮抗剂活性的O，CR 18 R 19，NR 20。

55. 发明申请

WO1997017350A1 AZASPIRO DERIVATIVES WITH 5HT1B ACTIVITY 审中-公开
标题翻译：具有5HT1B活性的AZASPIRO衍生物
公开(公告)号：WO1997017350A1
公开(公告)日：1997-05-15
申请号：PCT/EP1996004657
申请日：1996-10-23
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , WYMAN, Paul, Adrian
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D491/20
CPC分类号： C07D491/20
摘要： Compounds of formula (I) in which B is oxygen, CR R or NR where R , R and R are independently hydrogen or C1-6alkyl or B is a group S(O)b where b is 1, 2, or 3; and R is a group -(CH2)p-R where R is OR or SR is hydrogen or C1-6alkyl or R is NR R where R and R are as defined for R ; have been found to exhibit 5TH1B antagonist activity.
摘要翻译：其中B是氧的式（I）化合物，其中R 17，R 18和R 19独立地是氢或C 1-6烷基或B是组S（O）b，其中b为1,2或3; 并且R 6是基团 - （CH 2）p R 15，其中R 15是OR 16或SR 16是氢或C 1-6烷基或R 15是NR 10 R 11 其中R 10和R 11如对R 1所定义; 已被发现表现出5TH1B拮抗剂活性。

56. 发明申请

WO9623769A3 HETEROCYCLIC COMPOUNDS POSSESSING 5HT2C RECEPTOR AHETEROCYCLIC COMPOUNDS POSSESSING 5HT2C RECEPTOR ANTAGONIST ACTIVITY NTAGONIST ACTIVITY 审中-公开
标题翻译：吸收5HT2C受体的异源化合物5HT2C受体拮抗剂活性NTAGONIST活性
公开(公告)号：WO9623769A3
公开(公告)日：1996-10-24
申请号：PCT/EP9600369
申请日：1996-01-24
申请人： SMITHKLINE BEECHAM PLC , GASTER LARAMIE MARY , WYMAN PAUL ADRIAN , MULHOLLAND KEITH RAYMOND , DAVIES DAVID THOMAS
发明人： GASTER LARAMIE MARY , WYMAN PAUL ADRIAN , MULHOLLAND KEITH RAYMOND , DAVIES DAVID THOMAS
IPC分类号： C07D401/12 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/495 , A61K31/535 , A61P25/00 , A61P25/30 , A61P43/00 , C07D209/08 , C07D409/12 , C07D403/12 , C07D413/12
CPC分类号： C07D409/12 , C07D209/08
摘要： The invention relates to heterocyclic families of compounds having pharmacological activity, in particular possessing 5HT2C receptor antagonist activity processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.

57. 发明申请

WO1996023783A1 INDOLE DERIVATIVES AS 5-HT RECEPTOR ANTAGONIST 审中-公开
标题翻译：作为5-HT受体拮抗剂的吲哚衍生物
公开(公告)号：WO1996023783A1
公开(公告)日：1996-08-08
申请号：PCT/EP1996000368
申请日：1996-01-26
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , WYMAN, Paul, Adrian , MULHOLLAND, Keith, Raymond , DAVIES, David, Thomas , DUCKWORTH, David, Malcom , FORBES, Ian, Thomson , JONES, Graham, Elgin
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/14
摘要： The invention relates to heterocyclic compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders such as anxiety.
摘要翻译：本发明涉及具有药理活性的杂环化合物，其制备方法，含有它们的组合物及其在治疗CNS疾病如焦虑症中的用途。

58. 发明申请

WO1996011934A1 TRICYCLIC SPIRO COMPOUNDS PROCESS FOR THEIR PREPARATION AND THEIR USE AS 5HT1D RECEPTOR ANTAGONISTS 审中-公开
标题翻译：其制备及其作为5HT1D受体拮抗剂的TRICYCLIC SPIRO化合物方法
公开(公告)号：WO1996011934A1
公开(公告)日：1996-04-25
申请号：PCT/EP1995003945
申请日：1995-10-05
申请人： SMITHKLINE BEECHAM PLC , WYMAN, Paul, Adrian , GASTER, Laramie, Mary , JENNINGS, Andrew, John
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D491/107
CPC分类号： C07D491/10 , C07D495/10
摘要： Novel amide derivatives of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.
摘要翻译：公开了式（I）的新型酰胺衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。

59. 发明申请

WO1995006637A1 INDOLE AND INDOLINE DERIVATIVES AS 5HT1D RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为5HT1D受体拮抗剂的吲哚和吲哚衍生物
公开(公告)号：WO1995006637A1
公开(公告)日：1995-03-09
申请号：PCT/EP1994002663
申请日：1994-08-09
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , DUCKWORTH, David, Malcolm , JENKINS, Sarah, Margaret , WYMAN, Paul, Adrian
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D209/08
CPC分类号： C07D401/10 , C07D209/08 , C07D409/06 , C07D413/10
摘要： Novel indole and indoline derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.
摘要翻译：公开了新型吲哚和二氢吲哚衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。

60. 发明申请

WO1994017071A1 TRICYCLIC HETEROCYCLIC COMPOUNDS AS 5-HT4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为5-HT4受体拮抗剂的三聚杂环化合物
公开(公告)号：WO1994017071A1
公开(公告)日：1994-08-04
申请号：PCT/GB1994000172
申请日：1994-01-28
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , WYMAN, Paul, Adrian
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D491/052
CPC分类号： C07D491/04
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X1-(CH2)x-X2 and the aromatic carbon atoms to which they are attached form a 5-7 membered ring wherein X1 is O or S; X2 is O, S, NRs or NRsCO wherein Rs is hydrogen or C1-6 alkyl; or one of X1 and X2 is O, S or CH2 and the other is CH2; x is 1, 2 or 3; R1 and R2 together are Q-CH2-CH2, Q-CH = CH, or Q-CH = N where Q is linked either to the R1 or the R2 substitution position and Q is O, S or NRt wherein Rt is hydrogen or C1-6 alkyl; R3 is hydrogen, halo, C1-6 alkyl, C1-6 alkoxy or amino; R4 and R4 are independently hydrogen or C1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中X1-（CH2）x-X2和它们所连接的芳族碳原子形成5-7元环，其中X1是O或S; X 2是O，S，NR或NRsCO，其中R 5是氢或C 1-6烷基; 或X 1和X 2中的一个为O，S或CH 2，另一个为CH 2; x为1,2或3; R1和R2一起是Q-CH2-CH2，Q-CH = CH或Q-CH = N，其中Q连接到R1或R2取代位置，Q是O，S或NRt，其中Rt是氢或C1 -6烷基; R3是氢，卤素，C1-6烷基，C1-6烷氧基或氨基; R 4'和R 4'独立地是氢或C 1-6烷基; Y是O或NH; Z为亚式（a），（b）或（c）及其作为药物用于治疗胃肠道疾病，心血管疾病和CNS疾病的用途。

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