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51. 发明申请

WO1995001170A2 USE OF PHENETHANOLAMINE DERIVATIVES IN THE TREATMENT OF GASTROINTESTINAL DISORDERS 审中-公开
标题翻译：苯乙醇胺衍生物在治疗胃肠疾病中的应用
公开(公告)号：WO1995001170A2
公开(公告)日：1995-01-12
申请号：PCT/EP1994002106
申请日：1994-06-29
申请人： GLAXO GROUP LIMITED , STORER, Richard , FOXTON, Michael, Walter , HARTLEY, Charles, David , GREEN, Richard, Howard , TRAVERS, Stuart
发明人： GLAXO GROUP LIMITED
IPC分类号： A61K31/165
CPC分类号： A61K31/195 , A61K31/135
摘要： The use of compounds of formula (I) in which: R is hydrogen, methyl or hydroxymethyl; R is substituted alkyl; R and R are each hydrogen, halogen, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkyl, nitro, haloalkyl group, or substituted alkyl; X is oxygen or sulphur; and Ar is optionally substituted phenyl or naphtyl; and pharmaceutically acceptable salts thereof in the treatment of gastrointestinal disorders is described.
摘要翻译：式（I）化合物的用途，其中：R 0是氢，甲基或羟甲基; R 1是取代的烷基; R 2和R 3各自为氢，卤素，羟基，烷氧基，羧基，烷氧基羰基，烷基，硝基，卤代烷基或取代的烷基; X是氧或硫; 和Ar是任选取代的苯基或萘基; 和其药学上可接受的盐在治疗胃肠道疾病中的用途。

52. 发明申请

WO1995000503A1 PROCESS FOR THE PREPARATION OF N-ACETYL NEURAMINIC ACID DERIVATIVES 审中-公开
标题翻译：制备N-乙酰神经氨酸衍生物的方法
公开(公告)号：WO1995000503A1
公开(公告)日：1995-01-05
申请号：PCT/EP1994001940
申请日：1994-06-15
申请人： GLAXO GROUP LIMITED , SEARLE, Andrew, David , WILLIAMSON, Christopher
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D309/28
CPC分类号： C07D309/28 , Y02P20/55
摘要： A method for the preparation of 5-acetamido-4-amino-2,3,4,5-tetradeoxy-D &cir& _-glycero-D &cir& _-galacto-non-2-enopyranosonic acid is described.
摘要翻译：描述了制备5-乙酰氨基-4-氨基-2,3,4,5-四脱氧-D-半乳糖 - 甘油基-D-半乳糖 - 非-2-吡喃糖酸的方法。

53. 发明申请

WO1994029476A1 PROCESS FOR THE PREPARATION OF N-ACETYLNEURAMINIC ACID 审中-公开
标题翻译：制备N-乙酰氨基酸的方法
公开(公告)号：WO1994029476A1
公开(公告)日：1994-12-22
申请号：PCT/EP1994001860
申请日：1994-06-08
申请人： GLAXO GROUP LIMITED , DAWSON, Michael, John , NOBLE, David , MAHMOUDIAN, Mahmoud
发明人： GLAXO GROUP LIMITED
IPC分类号： C12P19/26
CPC分类号： C12N9/88 , C12P19/26
摘要： A method for the preparation of N-acetyl-D-neuraminic acid (NANA) from N-acetyl-D-glucosamine (NAG) is described.
摘要翻译：描述了从N-乙酰基-D-葡糖胺（NAG）制备N-乙酰基-D-神经氨酸（NANA）的方法。

54. 发明申请

WO1994008560A1 RANITIDINE CHEWABLE TABLETS 审中-公开
公开(公告)号：WO1994008560A1
公开(公告)日：1994-04-28
申请号：PCT/EP1993002763
申请日：1993-10-11
申请人： GLAXO GROUP LIMITED , BYE, Alan , EVANS, Jill , HUCKLE, Paul, Derrick , LACEY, Laurence, Francis , RUE, Peter, John
发明人： GLAXO GROUP LIMITED
IPC分类号： A61K09/00
CPC分类号： A61K9/0056 , A61K31/34 , A61K31/341 , Y10S514/974
摘要： The present invention provides a chewable ranitidine tablet comprising ranitidine, or a physiologically acceptable salt thereof, a chewable base selected from sucrose, glucose, lactose, maltose, or a mixture thereof, a flavouring and, optionally, an intense sweetener and a process for its preparation.
摘要翻译：本发明提供了包含雷尼替丁或其生理学上可接受的盐，选自蔗糖，葡萄糖，乳糖，麦芽糖或其混合物的可咀嚼碱的咀嚼雷尼替丁片，调味剂和任选的强甜味剂及其制备方法制备。

55. 发明申请

WO1994004486A1 CHEMICAL PROCESS FOR PREPARING AN OPTICALLY ACTIVE AMINODIOL 审中-公开
标题翻译：用于制备光学活性氨基酸的化学方法
公开(公告)号：WO1994004486A1
公开(公告)日：1994-03-03
申请号：PCT/EP1993002219
申请日：1993-08-19
申请人： GLAXO GROUP LIMITED , TAPOLCZAY, David, Joszef , MEERHOLZ, Clive, Alwin , TURNBULL, John, Peter , HALTER, Bernard, Charles , SCHILLING, Mark, Brian
发明人： GLAXO GROUP LIMITED
IPC分类号： C07C233/81
CPC分类号： C07C215/42 , C07C211/27 , C07C217/52 , C07C233/74 , C07C233/81 , C07C2601/08 , C07C2601/10 , C07D209/52
摘要： A process is claimed for preparing [1S(1 alpha , 2 beta , 4 beta )]-4-amino-2-hydroxymethyl-1-cyclopentanol from cis-4-((R)-benzoylamino)-2-cyclopentenecarboxylic acid, methyl ester in five steps. The invention also describes a number of novel intermediates useful in the synthesis of [1S(1 alpha , 2 beta , 4 beta )]-4-amino-2-hydroxymethyl-1-cyclopentanol.
摘要翻译：要求从顺式-4 - （（R） - 苯甲酰氨基）-2-环戊烯甲酸制备[1S（1α，2β，4β）] -4-氨基-2-羟甲基-1-环戊醇的方法，酯五步。本发明还描述了许多可用于合成[1S（1α，2β，4β）] -4-氨基-2-羟甲基-1-环戊醇的新型中间体。

56. 发明申请

WO1993014084A2 PIPERIDINE DERIVATIVES 审中-公开
标题翻译：哌啶衍生物
公开(公告)号：WO1993014084A2
公开(公告)日：1993-07-22
申请号：PCT/EP1993000101
申请日：1993-01-15
申请人： GLAXO GROUP LIMITED , COOPER, Anthony, William, James , HAGAN, Russell, Michael
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： The present invention relates to the novel piperidine derivatives of formula (I) wherein R represents phenyl optionally substituted by one or two C1-4alkyl, C1-4alkoxy, trifluoromethyl groups or halogen atoms; R represents hydrogen, hydroxy or C1-4alkoxy; R represents hydrogen or C1-4alkyl; R represents hydrogen, C1-4alkyl or C1-4alkoxy; R represents hydrogen, a C1-4alkyl, trifluoromethyl or cyano group, or a halogen atom; n represents zero, 1 or 2; and pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their medical use. The invention also relates to the use of tachykinin antagonists, including NKA, NKB and substance P, acting at the NK2 receptor in the treatment of anxiety disorders.
摘要翻译：本发明涉及式（I）的新型哌啶衍生物，其中R 1表示任选被一个或两个C 1-4烷基，C 1-4烷氧基，三氟甲基或卤素原子取代的苯基; R 2表示氢，羟基或C 1-4烷氧基; R 3表示氢或C 1-4烷基; R 4表示氢，C 1-4烷基或C 1-4烷氧基; R 5表示氢，C 1-4烷基，三氟甲基或氰基或卤素原子; n表示0，1或2; 及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其医疗用途。本发明还涉及作用于NK2受体的速激肽拮抗剂，包括NKA，NKB和物质P在治疗焦虑症中的用途。

57. 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。

58. 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.

59. 发明申请

WO1993006084A1 BENZANILIDE DERIVATIVES AS 5-HT1D ANTAGONISTS 审中-公开
标题翻译：苯扎林衍生物作为5-HT1D拮抗剂
公开(公告)号：WO1993006084A1
公开(公告)日：1993-04-01
申请号：PCT/EP1992002136
申请日：1992-09-14
申请人： GLAXO GROUP LIMITED , OXFORD, Alexander, William , MITCHELL, William, Leonard , BRADSHAW, John , CLITHEROW, John, Watson
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D213/56
CPC分类号： C07D213/56
摘要： The invention provides compounds of general formula (I) or a physiologically acceptable salt or solvate thereof wherein R1 represents a hydrogen atom, a halogen atom or a group selected from C¿1-6?alkyl and C1-6alkoxy; R?2¿ represents a pyridinyl group optionally substituted by one or two substituents selected from halogen atoms, C¿1-6?alkyl, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, C1-6alkoxy, hydroxy, -CN, -NO2, -CO2R?6, -COR6, -CONR6R7¿ and -(CH¿2?)mOC(O)C1-4alkyl; R?3¿ represents the group (a); R?4 and R5¿, which may be the same or different, each independently represents a hydrogen atom or a halogen atom or a group selected from hydroxy, C¿1-6?alkoxy and C1-6alkyl; R?6, R7 and R8¿, which may be the same or different, each independently represents a hydrogen atom or a C¿1-6?alkyl group; and m represents zero or an integer from 1 to 3. The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.

60. 发明申请

WO1993001174A1 THIAZOLIDINE DERIVATIVES AND THEIR USE AS ANTI-VIRAL COMPOUNDS 审中-公开
标题翻译：噻唑烷衍生物及其作为抗病毒化合物的用途
公开(公告)号：WO1993001174A1
公开(公告)日：1993-01-21
申请号：PCT/EP1992001494
申请日：1992-07-03
申请人： GLAXO GROUP LIMITED , KITCHIN, John , HOLMES, Duncan, Stuart , HUMBER, David, Cedric , STORER, Richard , DOLAN, Simon, Charles , HANN, Michael, Menteith , MCMEEKIN, Peter , MURRAY-RUST, Peter , PATEL, Binakumari , WEINGARTEN, Gordon, Gad
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D217/06
CPC分类号： C07D417/12 , C07D277/06 , C07D417/14
摘要： The present invention provides compounds of formula (I), wherein R is hydrogen, alkyl or CH2alkyl where the alkyl portion is substituted by OH; A represents either a group CHR CHR OH or a group (II), where R is hydrogen, alkyl, cycloalkylalkyl or Aralkyl, R is hydrogen, alkyl, cycloalkylalkyl, aralkyl, CHR CONR R (where R is hydrogen, alkyl, cycloalkylalkyl or Aralkyl, R is hydrogen or methyl and R is hydrogen, alkyl optionnally substituted by one or two hydroxyl groups, aryl, heteroaryl, cycloalkylalkyl, Aralkyl wherein the alkyl portion is optionnally substituted by hydroxymethyl, or Hetalkyl) or CHR NHCOR (where R is alkyl, cycloalkylalkyl or an aralkyl), R is alkoxy or NR R (where R is hydrogen or methyl and R is hydrogen, alkyl, aryl, aralkyl or cycloalkylalkyl); X is a group -CHR (CHR )r(CHR )sCHR -, where R and R are hydrogen, r is 1, s is zero and R is hydroxyl or hydroxymethyl, or R and R are hydrogen, r and s are 1 and R and R are each hydrogen or hydroxyl provided that at least one of R and R is hydroxyl, or one of R and R is hydrogen and the other is hydroxymethyl and r and s are zero; useful in chemotherapy, particularly of viral infections.
摘要翻译：本发明提供式（I）化合物，其中R 1是氢，烷基或C 2烷基，其中烷基部分被OH取代; A代表基团CHR 21 CHR 22 OH或基团（II），其中R 21是氢，烷基，环烷基烷基或芳烷基，R 22是氢，烷基，环烷基烷基，芳烷基，CHR 24 R CONR 25 R 26（其中R 24是氢，烷基，环烷基烷基或芳烷基，R 25是氢或甲基，R 26是氢，烷基选择性地被一个或两个羟基取代，芳基，杂芳基，环烷基烷基，芳烷基，其中烷基部分选择性地被羟甲基或Hetalkyl取代）或CHR 24 NHCOR 27（其中R 27是烷基，环烷基烷基或芳烷基），R 23是烷氧基或NR 28 R 29（其中R 28是氢或甲基，R 29是氢，烷基，芳基，芳烷基或环烷基烷基）; X是基团-CHR 30（CHR 31）r（CHR 32）s CHR 33，其中R 30和R 33是氢，r是1，s是0，R 31是羟基或羟甲基，或R 30和R 33是氢，r和s是1，R 31和R 32各自是氢或羟基，条件是R 31中至少有一个且R 32为羟基，R 30和R 33之一为氢，另一个为羟甲基，r和s为0; 可用于化疗，特别是病毒感染。

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