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1. 发明申请

WO1993022303A1 1-PIPERAZINEACETIC DERIVATIVES AS FIBRINOGEN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为纤维蛋白原受体拮抗剂的1-哌嗪衍生物
公开(公告)号：WO1993022303A1
公开(公告)日：1993-11-11
申请号：PCT/EP1993000963
申请日：1993-04-20
申请人： GLAXO GROUP LIMITED , MIDDLEMISS, David , JUDKINS, Brian, David , ELDRED, Colin, David , PORTER, Barry , KELLY, Henry, Anderson
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D295/14
CPC分类号： C07D295/15 , C07D213/74 , C07D295/145
摘要： The invention thus provides the compounds of general formula (I) and salts, solvates and pharmaceutically acceptable derivatives thereof, in which X and X represent CH or are different and represent CH or N; Y , Y , Y and Y represent CH, or Y and Y represent CH and Y and Y represent N, or Y and Y represent CH and Y and Y represent N, or three of Y to Y represent CH and the other represents N; Z represents CH or N; Z represents N or N R ; R represents a hydrogen atom or a hydroxyl, C1-4alkyl or 2,2,2-trifluoroethyl group; R represents a hydrogen atom or, when both X and X represent CH, may also represent a fluorine, chlorine or bromine atom or a C1-4alkyl group; R represents a hydrogen atom or, when both Y and Y represent CH, may also represent a fluorine, chlorine or bromine atom or a C1-4alkyl group; R and R each represent a hydrogen atom; or, when Z represents CH and Z represents N, R may also represent C1-4alkyl; or, when both Z and Z both represent N, R and R may be the same or different, and represent hydrogen or C1-4alkyl; R represents a C1-4alkyl group or phenylC1-3alkyl group; R represents a hydrogen atom; a C1-4alkyl group; a naphthyl group; a thiophene group; an unsubstituted phenyl group; a phenyl group substituted by C1-4alkyl group, C1-4alkoxy, phenylC1-3alkoxy, OH, halogen (where halogen is fluorine, chlorine, bromine or iodine), CF3, unsubstituted phenyl, phenyl substituted by OH, pyridinyl, NR R , NHSO2R , CONR R or CO2R ; a C1-4alkyl group substituted by one or more naphthyl, phenyl, OH or CO2R ; a C2-4alkenyl group substituted by one or more naphthyl, phenyl, OH or CO2R ; or a saturated or unsaturated C5-7cycloalkyl group; and R and R , which may be the same or different represent H or C1-4alkyl or, together with the nitrogen atom to which they are attached, form a saturated 5 to 7 membered ring.
摘要翻译：因此，本发明提供了通式（I）的化合物及其盐，溶剂化物和药学上可接受的衍生物，其中X 1和X 2代表CH或不同并表示CH或N; Y 1，Y 2，Y 3和Y 4表示CH，或Y 1和Y 4表示CH且Y 2和Y 3表示N或Y < 2>和Y 3表示CH且Y 1和Y 4表示N，Y 1至Y 4中的3个表示CH，而另一个表示N; Z 1表示CH或N; Z 2表示N或N + R 6; R 1表示氢原子或羟基，C 1-4烷基或2,2,2-三氟乙基; R 2表示氢原子，或者当X 1和X 2都表示CH时，也可以表示氟，氯或溴原子或C 1-4烷基; R 3表示氢原子，当Y 1和Y 2都表示CH时，也可以表示氟，氯或溴原子或C 1-4烷基; R 4和R 5各自表示氢原子; 或者当Z 1表示CH且Z 2表示N时，R 4也可以表示C 1-4烷基; 或者当Z 1和Z 2均同时表示N时，R 4和R 5可以相同或不同，表示氢或C 1-4烷基; R 6表示C 1-4烷基或苯基C 1-3烷基; R 7表示氢原子; C 1-4烷基; 萘基; 噻吩基; 未取代的苯基; 被C 1-4烷基取代的苯基，C 1-4烷氧基，苯基C 1-3烷氧基，OH，卤素（其中卤素是氟，氯，溴或碘），CF 3，未被取代的苯基，被OH取代的苯基，吡啶基，NR 8 R 9，NHSO 2 R 8，CONR 8 R 9或CO 2 R 8; 被一个或多个萘基，苯基，OH或CO 2 R 8取代的C 1-4烷基; 被一个或多个萘基取代的C 2-4链烯基，苯基，OH或CO 2 R 8; 或饱和或不饱和的C 5-7环烷基; 和R 8和R 9可以相同或不同，表示H或C 1-4烷基，或者与它们所连接的氮原子一起形成饱和的5至7元环。

2. 发明申请

WO1993010091A2 PIPERIDINE ACETIC ACID DERIVATIVES AS INHIBITORS OF FIBRINOGEN-DEPENDENT BLOOD PLATELET AGGREGATION 审中-公开
标题翻译：哌啶乙酸衍生物作为纤维蛋白原依赖性血小板聚集剂的抑制剂
公开(公告)号：WO1993010091A2
公开(公告)日：1993-05-27
申请号：PCT/EP1992002588
申请日：1992-11-10
申请人： GLAXO GROUP LIMITED , PORTER, Barry , ELDRED, Colin, David , KELLY, Henry, Anderson , WHEATCROFT, James, Russell
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D211/26
CPC分类号： C07D401/12 , C07D211/26 , C07D211/58 , C07F9/65583
摘要： The invention relates to acetic acid derivatives of formula (I) and pharmaceutically acceptable derivatives thereof and salts and solvates thereof, in which X?1 and Y1¿, which may be the same or different, represent CH or N; X2 represents CH or, when X1 represents CH, may also represent N; Y2 represents N or, when Y1 represents N, may also represent CH; Z represents N or N+R5; R1 represents a hydrogen atom or a hydroxyl, C¿1-4?alkyl or 2,2,2-trifluoroethyl group; R?2¿ represents a hydrogen atom or, when both X?1 and X2¿ represent CH, may also represent a fluorine, chlorine or bromine atom or a C¿1-4?alkyl group; R?3¿ represents a hydrogen atom or, when both Y?1 and Y2¿ represent N, may also represent a C¿1-4?alkyl or hydroxymethyl group. R?4¿ represents a hydrogen atom or, when Z represents N, R4 may also represent a C¿1-4?alkyl group; R?5¿ represents a C¿1-4?alkyl or phenylC1-4alkyl group; R?6¿ represents a hydrogen atom or a C¿1-4?alkyl group. The compounds inhibit fibrinogen-dependent blood platelet aggregation.
摘要翻译：式（I）的乙酸衍生物，其药学上可接受的衍生物及其盐和溶剂合物。上述式（I）中，X 1和Y 1相同或不同，表示CH或N; X2代表CH，或者当X1代表CH时，它也可以代表N; Y2表示N，或者当Y1表示N时，它也可以表示CH; Z是N或N + R5; R1代表氢原子或羟基，C1-4烷基或2,2,2-三氟乙基; R 2表示氢原子，或者当X 1和X 2都表示CH时，它也可以表示氟，氯或溴原子或C 1-4烷基; R3代表氢原子，或者当Y1和Y2都代表N时，它也可以代表C1-4烷基或羟甲基; R4代表氢原子，或者当Z代表N时，它也可以代表C1-4烷基; R5代表C1-4烷基或C1-4苯基烷基; R6代表氢原子或C1-4烷基。这些化合物抑制纤维蛋白原依赖性血液学血小板聚集。

3. 发明申请

WO1993014077A1 PIPERIDINEACETIC ACID DERIVATIVES AS INHIBITORS OF FIBRINOGEN-DEPENDENT BLOOD PLATELET AGGREGATION 审中-公开
标题翻译：作为纤维蛋白依赖性血小板聚集抑制剂的哌啶酸衍生物
公开(公告)号：WO1993014077A1
公开(公告)日：1993-07-22
申请号：PCT/EP1993000100
申请日：1993-01-15
申请人： GLAXO GROUP LIMITED , PORTER, Barry , ELDRED, Colin, David , JUDKINS, Brian, David , KELLY, Henry, Anderson , WHEATCROFT, James, Russell
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D295/14
CPC分类号： C07D409/06 , C07D211/58
摘要： The invention relates to acetic acid derivatives of formula (I) and pharmaceutically acceptable derivatives thereof and salts and solvates thereof, where: X and Y , which may be the same or different, represent CH or N; X represents CH or, when X represents CH, may also represent N; Y represents N or, when Y represents N, may also represent CH; Z represents N or N R ; R represents a hydrogen atom or a hydroxyl, C1-4alkyl or 2,2,2-trifluoroethyl group; R represents a hydrogen atom or, when both X and X represent CH, may also represent a fluorine, chlorine or bromine atom or a C1-4alkyl group; R represents a hydrogen atom or, when both Y and Y represent N, may also represent a C1-4alkyl or hydroxymethyl group; R represents a hydrogen atom or, when Z represents N, R may also represent a C1-4alkyl group; R represents a C1-4alkyl or phenylC1-4alkyl group; R represents a naphthyl group; a thiophenyl group; an unsubstituted phenyl group; a phenyl group substituted by C1-4alkyl, C1-4alkoxy, phenylC1-3alkoxy, OH, halogen, where halogen is fluorine, chlorine, bromine or iodine, CF3, unsubstituted phenyl, phenyl substituted by OH, pyridinyl, NR R , NHSO2R , CONR R or CO2R ; a C1-4alkyl group substituted by one or more naphthyl, phenyl, OH or CO2R ; a C2-4alkenyl group substituted by one or more naphthyl, phenyl, OH or CO2R ; or a saturated or unsaturated C5-7cycloalkyl group; and R and R , which may be the same or different represent H or C1-4alkyl or, together with the nitrogen atom to which they are attached, form a saturated 5 to 7 membered ring. The compounds inhibit fibrinogen dependent blood platelet aggregation.
摘要翻译：本发明涉及式（I）的乙酸衍生物及其药学上可接受的衍生物及其盐和溶剂合物，其中：X 1和Y 1可以相同或不同，表示CH或N; X 2表示CH，或者当X 1表示CH时，也可以表示N; Y 2表示N，或者当Y 1表示N时，也可以表示CH; Z表示N或N + R 5; R 1表示氢原子或羟基，C 1-4烷基或2,2,2-三氟乙基; R 2表示氢原子，或者当X 1和X 2都表示CH时，也可以表示氟，氯或溴原子或C 1-4烷基; R 3表示氢原子，当Y 1和Y 2都表示N时，也可以表示C 1-4烷基或羟甲基; R 4表示氢原子，当Z表示N时，R 4也可以表示C 1-4烷基; R 5表示C 1-4烷基或苯基C 1-4烷基; R 6表示萘基; 噻吩基; 未取代的苯基; 被C 1-4烷基取代的苯基，C 1-4烷氧基，苯基C 1-3烷氧基，OH，卤素，其中卤素是氟，氯，溴或碘，CF 3，未被取代的苯基，被OH取代的苯基，吡啶基，NR 7 R 8，NHSO 2 R 7，CONR 7 R 8或CO 2 R 7; 被一个或多个萘基取代的C 1-4烷基，苯基，OH或CO 2 R 7; 被一个或多个萘基取代的C 2-4链烯基，苯基，OH或CO 2 R 7; 或饱和或不饱和的C 5-7环烷基; R 7和R 8可以相同或不同，表示H或C 1-4烷基，或与它们相连的氮原子一起形成饱和的5至7元环。该化合物抑制纤维蛋白原依赖性血小板聚集。

4. 发明申请

WO1993008181A1 CYCLOHEXANEACETIC ACID DERIVATIVES AS INHIBITORS OF FIBRINOGEN-DEPENDENT BLOOD PLATELET AGGREGATION 审中-公开
标题翻译：作为纤维蛋白依赖性血小板聚集抑制剂的环己烷酸衍生物
公开(公告)号：WO1993008181A1
公开(公告)日：1993-04-29
申请号：PCT/EP1992002340
申请日：1992-10-12
申请人： GLAXO GROUP LIMITED , PORTER, Barry , ELDRED, Colin, David , KELLY, Henry, Anderson
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D295/14
CPC分类号： C07D213/78 , C07D211/34 , C07D239/42 , C07D295/155
摘要： The invention relates to cyclohexaneacetic acid derivatives of formula (I) and salts and solvates thereof, in which X?1, X2 and Y1¿, which may be the same or different, represent CH or N; Y2 represents N or, when Y1 represents N, may also represent CH; R1 represents a hydrogen atom or a hydroxyl, C¿1-4? alkyl or 2,2,2-trifluoroethyl group; R?2¿ represents a hydrogen atom or, when both X?1 and X2¿ represent CH, may also represent a fluorine, chlorine or bromine atom or a phenyl or C¿1-4? alkyl group; R?3¿ represents a hydrogen atom or, when both Y?1 and Y2¿ represent N, may also represent a C¿1-4? alkyl or hydroxymethyl group. The compounds inhibit fibrinogen-dependent blood platelet aggregation.

5. 发明申请

WO1997049699A1 PIPERIDINE ACETIC ACID DERIVATIVES AND THEIR USE IN THE TREATMENT OF THROMBOTIC DISORDERS 审中-公开
标题翻译：哌啶酸酸衍生物及其在治疗血栓性疾病中的应用
公开(公告)号：WO1997049699A1
公开(公告)日：1997-12-31
申请号：PCT/EP1997003196
申请日：1997-06-19
申请人： GLAXO GROUP LIMITED , ALLEN, David, George , ELDRED, Colin, David , JUDKINS, Brian, David , MITCHELL, William, Leonard
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D413/14 , C07D453/02
摘要： The invention relates to compounds of formula (I) or a salt, solvate, or physiologically functional derivative thereof, in which X represents either CH2-CH2 or CH=CH; Y represents a group (a) or (b); R represents SO2Me or CONH2, and R represents SO2Me, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in medicine, particularly in the treatment of thrombotic disorders.
摘要翻译：本发明涉及式（I）化合物或其盐，溶剂合物或生理功能衍生物，其中X表示CH 2 -CH 2或CH = CH; Y代表（a）或（b）组; R 0表示SO 2 Me或CONH 2，R 1表示SO 2 Me，其制备方法，含有这些化合物的药物组合物及其在医药中的用途，特别是治疗血栓形成障碍。

6. 发明申请

WO1996020192A1 PIPERIDINEACETIC ACID DERIVATIVES USEFUL AS FIBRINOGEN ANTAGONIST AGENT 审中-公开
标题翻译：作为纤维蛋白原拮抗剂代谢物使用的哌啶酸衍生物
公开(公告)号：WO1996020192A1
公开(公告)日：1996-07-04
申请号：PCT/EP1995005043
申请日：1995-12-21
申请人： GLAXO GROUP LIMITED , ALLEN, David, George , ELDRED, Colin, David , MITCHELL, William, Leonard
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D401/14
CPC分类号： C07D401/14
摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof, in which: X represents either CH2-CH2 or CH=CH, and Y represents a hydrogen atom or a phenylmethyl group, wherein the phenyl group is optionally substituted by one or more halogen atoms. Compounds of formula (I) inhibit blood platelet aggregation.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的衍生物，其中：X表示CH 2 -CH 2或CH = CH，Y表示氢原子或苯甲基，其中苯基任选被一个或更多个卤素原子。式（I）化合物抑制血小板聚集。

7. 发明申请

WO1992009600A1 BENZOFURAN AND BENZTHIOPHENE DERIVATIVES 审中-公开
标题翻译：苯并呋喃和苯并噻吩衍生物
公开(公告)号：WO1992009600A1
公开(公告)日：1992-06-11
申请号：PCT/GB1991002114
申请日：1991-11-28
申请人： GLAXO GROUP LIMITED , ROSS, Barry, Clive , SCOPES, David, Ian, Carter , CARDWELL, Kevin, Stuart , ELDRED, Colin, David , MIDDLEMISS, David , JACK, Torquil, Iain, MacLean , DOWLE, Michael, Dennis , MONTANA, John, Gary , SHAH, Pritom
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D405/06
CPC分类号： C07D307/82 , C07D405/06 , C07D405/10 , C07D405/14
摘要： The invention provides compounds of general formula (I) or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein Q represents an oxygen or sulphur atom; R represents a hydrogen atom or a halogen atom or a group selected from C1-6alkyl, C2-6alkenyl, fluoroC1-6alkyl, -CHO, -CO2H, C1-6alkoxy, or -COR ; Ar represents the group (a); R represents a group selected from C1-6alkyl, C2-6alkenyl, C1-6alkoxy or the group -NR R ; R represents a group selected from -CO2H, -NHSO2CF3 or a C-linked tetrazolyl group; R and R , which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a C1-6alkyl group; Het represents the group (b); X represents N or CH; Y represents N or CR ; Z represents N or CR ; R represents a hydrogen atom or a C1-6alkyl, C2-6alkenyl or a C1-6alkylthio group; R represents a halogen atom or a group selected from cyano, nitro, C1-6alkyl, C2-6alkenyl, fluoroC1-6alkyl, -(CH2)mR , -(CH2)nCOR , or -(CH2)pNR COR ; R represents a hydroxy or C1-6alkoxy group; R represents a hydrogen atom or a group selected from hydroxy, C1-6alkyl, C1-6alkoxy, phenyl, phenoxy or the group -NR R ; R represents a hydrogen atom or a C1-6alkyl group; R represents a hydrogen atom or a group selected from C1-6alkyl, C1-6alkoxy, phenyl, phenoxy or the group -NR R ; R and R , which may be the same or different, each independently represent a hydrogen atom or a C1-4alkyl group or -NR R forms a saturated heterocyclic ring which has 5 or 6 ring members and may optionally contain in the ring one oxygen atom; m represents an integer from 1 to 4; n represents zero or an integer from 1 to 4; and p represents an integer from 1 to 4; with the proviso that at least one of X, Y and Z is a nitrogen atom, and with the further proviso that when X is N at least one of Y and Z is N and when Y is N at least one of X and Z is N. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.
摘要翻译：本发明提供通式（I）的化合物或其生理上可接受的盐，溶剂合物或代谢不稳定的酯，其中Q表示氧或硫原子; R 1表示氢原子或卤素原子或选自C 1-6烷基，C 2-6烯基，氟C 1-6烷基，-CHO，-CO 2 H，C 1-6烷氧基或-COR 2的基团。 Ar表示组（a）; R 2表示选自C 1-6烷基，C 2-6烯基，C 1-6烷氧基或-NR 14 R 13基团。 R 3表示选自-CO 2 H，-NHSO 2 CF 3或C连接的四唑基的基团; R 4和R 5可以相同或不同，各自独立地表示氢原子或卤素原子或C1-6烷基; Het代表组（b）; X表示N或CH; Y表示N或CR 7; Z表示N或CR 7; R 6表示氢原子或C 1-6烷基，C 2-6烯基或C 1-6烷硫基; R 7表示卤素原子或选自氰基，硝基，C 1-6烷基，C 2-6烯基，氟C 1-6烷基， - （CH 2）m R 8， - （CH 2）n COR 9或 - （ CH2）PNR <10> COR <11>; R 8表示羟基或C 1-6烷氧基; R 9表示氢原子或选自羟基，C 1-6烷基，C 1-6烷氧基，苯基，苯氧基或基团-NR 12 R 13的基团。 R 10表示氢原子或C 1-6烷基; R 11表示氢原子或选自C 1-6烷基，C 1-6烷氧基，苯基，苯氧基或基团-NR 12 R 13的基团。 R 12和R 13可以相同或不同，各自独立地表示氢原子或C 1-4烷基或-NR 12 R 13形成饱和杂环，其具有5或6个环成员，并且可以任选地在环中含有一个氧原子; m表示1〜4的整数， n表示0或1至4的整数; p表示1〜4的整数，条件是X，Y和Z中的至少一个是氮原子，另外条件是当X是N时，Y和Z中的至少一个是N，当Y是N时，X和Z中的至少一个是该化合物可用于治疗或预防与认知障碍相关的高血压和疾病。

8. 发明申请

WO1997049698A1 PIPERIDINE ACETIC ACID DERIVATIVES AND THEIR USE IN THE TREATMENT OF THROMBOTIC DISORDERS 审中-公开
标题翻译：哌啶酸酸衍生物及其在治疗血栓性疾病中的应用
公开(公告)号：WO1997049698A1
公开(公告)日：1997-12-31
申请号：PCT/EP1997003194
申请日：1997-06-19
申请人： GLAXO GROUP LIMITED , ALLEN, David, George , ELDRED, Colin, David , JUDKINS, Brian, David , MITCHELL, William, Leonard , SCOPES, David, Ian, Carter
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D413/14 , C07D453/02
摘要： The invention relates to compounds of formula (I) or a salt, solvate, or physiologically functional derivative thereof, in which: X is CH2-CH2, CH=CH, or CC; Y is hydrogen, C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, C1-6 haloalkyl, C1-6 hydroxyalkyl, aryl, hetaryl, arylC1-4alkyl, or hetarylC1-4alkyl, wherein the aryl and hetaryl groups are optionally substituted by halo, nitro, C1-6 alkyl, C1-6haloalkyl, hydroxy, C1-6 alkoxy, cyano, -C(O)nR , -NR S(O)nR , -C(O)NR R , or -NR R , wherein R and R are independently selected from hydrogen, C1-4 alkyl and C1-4 haloalkyl, and n is 0, 1, or 2; Z is piperidinyl, piperazinyl, or quinuclidinyl; ring B is a 5- or 6-membered aromatic heterocycle fused to ring A and is optionally substituted by a group -L-R wherein: L is a bond, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, S(O)n, C(O)n, or CONR , wherein n is 0, 1, or 2, and R is selected from hydrogen, C1-4 alkyl, and C1-4 haloalkyl; and R is C1-6 alkyl, C4-7 cycloalkyl, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 alkoxy, cyano, -NR R , aryl or hetaryl, wherein R and R are independently selected from hydrogen, C1-6 alkyl and C1-6 haloalkyl, or together with the nitrogen to which they are bonded form a piperidinyl, morpholino, or pyrolidinyl group, and the aryl and hetaryl groups are optionally substituted by halo, nitro, C1-4 alkyl, hydroxy, C1-4 alkoxy, cyano, -C(O)NR R or -NR R wherein R and R are as defined for R and R above, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in medicine, particularly in the treatment of thrombotic disorders.
摘要翻译：本发明涉及式（I）化合物或其盐，溶剂化物或生理功能衍生物，其中：X为CH 2 -CH 2，CH = CH或CC; Y是氢，C 1-6烷基，C 1-6烯基，C 1-6炔基，C 1-6卤代烷基，C 1-6羟烷基，芳基，杂芳基，芳基C 1-4烷基或杂芳基C 1-4烷基，其中芳基和杂芳基是任选的被卤素，硝基，C 1-6烷基，C 1-6卤代烷基，羟基，C 1-6烷氧基，氰基，-C（O）n R 1，-NR 1 S（O）n R 2，-C （O）NR 1 R 2或-NR 1 R 2，其中R 1和R 2独立地选自氢，C 1-4烷基和C 1-4卤代烷基，和 n为0,1或2; Z是哌啶基，哌嗪基或奎宁环基; 环B是与环A稠合的5或6元芳族杂环，并且任选地被基团-LR取代，其中：L是键，C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基，C 1-6 卤代烷氧基，S（O）n，C（O）n或CONR 3，其中n为0,1或2，R 3选自氢，C 1-4烷基和C 1-4卤代烷基 ; 和R为C 1-6烷基，C 4-7环烷基，C 1-6卤代烷基，C 1-6卤代烷氧基，C 1-6烷氧基，氰基，-NR 4 R 5，芳基或杂芳基，其中R 4和 R 5独立地选自氢，C 1-6烷基和C 1-6卤代烷基，或与它们键合的氮一起形成哌啶基，吗啉代或吡咯烷基，芳基和杂芳基任选被卤素，硝基，C 1-4烷基，羟基，C 1-4烷氧基，氰基，-C（O）NR 6 R 7或-NR 6 R 7其中R 6和R 7 >如上述R 4和R 5所定义，其制备方法，含有这些化合物的药物组合物及其在医药中的用途，特别是治疗血栓形成障碍。

9. 发明申请

WO1997043300A1 ADENOSINE DERIVATIVES 审中-公开
标题翻译：腺苷衍生物
公开(公告)号：WO1997043300A1
公开(公告)日：1997-11-20
申请号：PCT/EP1997002403
申请日：1997-05-13
申请人： GLAXO GROUP LIMITED , ELLIS, Frank , SWANSON, Stephen , COUSINS, Richard, Peter, Charles , COX, Brian , PENNELL, Andrew, Michael, Kenneth , ELDRED, Colin, David
发明人： GLAXO GROUP LIMITED
IPC分类号： C07H19/16
CPC分类号： C07H15/04 , C07H19/16
摘要： A compound of formula (I) wherein R represents phenyl optionally substituted by one or more substituents selected from halogen, C1-3alkyl, trifluoromethyl, nitro, cyano, -CO2R , -CONR R , -COR , -SOR , -SO2R , -SO3H, -SO2NR R , -OR , -NHSO2R , -NHCOR and -NR R ; R represents a C1-6alkyl or C3-6alkenyl group; R represents C1-3alkyl; R and R may each independently represent hydrogen or C1-3alkyl or, when -NR R is directly attached to said phenyl, R and R together with the nitrogen atom may form a 5- or 6- membered heterocyclic ring optionally containing a second heteroatom selected from oxygen or nitrogen, which second nitrogen heteroatom may optionally be further substituted by hydrogen or C1-3alkyl; R represents C1-3alkyl; and salts and solvates thereof.
摘要翻译：式（I）化合物，其中R 1表示任选被一个或多个选自卤素，C 1-3烷基，三氟甲基，硝基，氰基，-CO 2 R a，-CONR a R a，，-COR a，-SOR c，-SO 2 R c，-SO 3 H，-SO 2 NR a R b，-OR a，-NHSO 2 R c，-NHCOR a和 -NR - [R的; R 2表示C 1-6烷基或C 3-6烯基; R 3表示C 1-3烷基; R a和R b可各自独立地表示氢或C 1-3烷基，或当-NR a R a直接连接到所述苯基时，R a和R b与氮原子可以形成任选地含有选自氧或氮的第二杂原子的5-或6-元杂环，该第二氮杂原子可以任选地被氢或C 1-3烷基进一步取代; R c表示C 1-3烷基; 及其盐和溶剂合物。

10. 发明申请

WO1998057980A1 PEPTIDES AND COMPOUNDS THAT BIND TO THE IL-5 RECEPTOR 审中-公开
标题翻译：与IL-5受体结合的肽和化合物
公开(公告)号：WO1998057980A1
公开(公告)日：1998-12-23
申请号：PCT/GB1997001618
申请日：1997-06-16
申请人： GLAXO GROUP LIMITED , BARRETT, Ronald, William , ENGLAND, Bruce, Padon , SCHATZ, Peter, Joseph , SLOAN, Derek, Dean , CHEN, Min-Jia
发明人： GLAXO GROUP LIMITED
IPC分类号： C07K07/08
CPC分类号： C40B40/02 , A61K38/00 , C07K7/08 , C07K14/7155 , C12N15/1037
摘要： Described are peptides and peptide mimetics that bind to the IL-5 receptor. Such peptides and peptide mimetics are useful in methods for treating disorders that involve improper production of or response to IL-5 and or the production and accumulation of eosinophils, such as asthma, as well as in diagnostic methods employing labeled peptides and peptide mimetics.
摘要翻译：描述了结合IL-5受体的肽和肽模拟物。这样的肽和肽模拟物可用于治疗涉及IL-5的不适当产生或应答以及嗜酸性粒细胞（例如哮喘）的产生和积累以及使用标记肽和肽模拟物的诊断方法的疾病的方法。

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