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1. 发明申请

WO0250061A8 PIPERAZINE DERIVATIVES FOR TREATMENT OF BACTERIAL INFECTIONS 审中-公开
标题翻译：用于治疗细菌感染的哌啶衍生物
公开(公告)号：WO0250061A8
公开(公告)日：2002-07-25
申请号：PCT/GB0105653
申请日：2001-12-19
申请人： SMITHKLINE BEECHAM PLC , DARTOIS CATHERINE GENEVIEVE YV , MARKWELL ROGER EDWARD , MORVAN MARCEL , NADLER GUY MARGUERITE MARIE GE , PEARSON NEIL DAVID
发明人： DARTOIS CATHERINE GENEVIEVE YV , MARKWELL ROGER EDWARD , MORVAN MARCEL , NADLER GUY MARGUERITE MARIE GE , PEARSON NEIL DAVID
IPC分类号： A61K31/496 , A61K31/498 , A61K31/538 , A61K31/5415 , A61P31/04 , C07D401/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D401/14 , A61K31/495
CPC分类号： C07D401/12 , C07D405/12 , C07D409/06 , C07D417/06 , C07D471/04
摘要： Piperazine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man(represented by formula (I).
摘要翻译：哌嗪衍生物及其药学上可接受的衍生物可用于哺乳动物，特别是人类（由式（I）表示）的哺乳动物细菌感染的治疗方法。

2. 发明申请

WO1992006966A1 N-(2-ALKYL-3-MERCAPTOGLUTARYL)-AMINO-DIAZA CYCLOALKANONE DERIVATIVES AND THEIR USE AS COLLAGENASE INHIBITORS 审中-公开
标题翻译： N-（2-烷基-3-甲基戊基）氨基 - 二氮杂环丁酮衍生物及其作为胶原抑制剂的用途
公开(公告)号：WO1992006966A1
公开(公告)日：1992-04-30
申请号：PCT/GB1991001749
申请日：1991-10-09
申请人： BEECHAM GROUP PLC , MARKWELL, Roger, Edward , WARD, Robert, William , RAHMAN, Shahzad, Sharooq
发明人： BEECHAM GROUP PLC
IPC分类号： C07D243/08
CPC分类号： C07D245/02
摘要： Thiol carboxylic acid derivatives, processes for their preparation and their use as collagenase inhibitors are described.
摘要翻译：描述了硫醇羧酸衍生物，其制备方法及其作为胶原酶抑制剂的用途。

3. 发明申请

WO2004058144A2 ANTIBACTERIAL AGENTS 审中-公开
公开(公告)号：WO2004058144A2
公开(公告)日：2004-07-15
申请号：PCT/US2003/040032
申请日：2003-12-17
申请人： GLAXO GROUP LIMITED , AXTEN, Jeffrey, Michael , BROOKS, Gerald , BROWN, Pamela , DAVIES, David , GALLAGHER, Timothy, Francis , MARKWELL, Roger, Edward , MILLER, William, Henry , PEARSON, Neil, David , SEEFELD, Mark
发明人： AXTEN, Jeffrey, Michael , BROOKS, Gerald , BROWN, Pamela , DAVIES, David , GALLAGHER, Timothy, Francis , MARKWELL, Roger, Edward , MILLER, William, Henry , PEARSON, Neil, David , SEEFELD, Mark
IPC分类号： A61K
CPC分类号： C07D401/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D491/04 , C07D497/04 , C07D513/04
摘要： Quinoline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.

4. 发明申请

WO1996012486A1 USE OF [R-(Z)]-ALPHA-(METHOXYIMINO)-ALPHA-(1-AZABICYCLO [2.2.2] OCT-3-YL) ACETONITRILE TO REDUCE AMYLOID BETA A4 FORMATION IN ALZHEIMER'S DISEASE 审中-公开
标题翻译：使用[R-（Z）] - ALPHA-（甲氧基亚氨基）-ALPHA-（1-氮杂双环[2.2.2] OCT-3-YL）乙酰胆碱降低阿尔茨海默病中Aβ形成的淀粉样蛋白
公开(公告)号：WO1996012486A1
公开(公告)日：1996-05-02
申请号：PCT/EP1995004082
申请日：1995-10-17
申请人： SMITHKLINE BEECHAM P.L.C. , MARKWELL, Roger, Edward , HAWKINS, Julie , GRAY, Carol, Wendy
发明人： SMITHKLINE BEECHAM P.L.C.
IPC分类号： A61K31/435
CPC分类号： A61K31/439
摘要： A method of enhancing amyloid precursor protein processing along a non-amyloidogenic pathway in patients suffering from, or at risk of developing, Alzheimer's disease and a method of treatment or prophylaxis of Alzheimer's disease by reducing beta A4 production in patients suffering from, or at risk of developing, Alzheimer's disease comprising administering to the patient an effective, non-toxic amount of an acetonitrile compound, use of the compound in preparation of a medicament for use in the method and a composition for use in the method.
摘要翻译：在患有或有发展中的阿尔茨海默氏病的患者中，通过降低患有或处于危险中的患者中的βA4产生来治疗或预防阿尔茨海默氏病的患者，沿着非淀粉样蛋白生成途径增强淀粉样前体蛋白质加工的方法的发展中的阿尔茨海默氏病包括向患者施用有效的无毒量的乙腈化合物，所述化合物在制备用于该方法的药物中的用途以及用于该方法的组合物。

5. 发明申请

WO2003087098A1 NITROGEN-CONTAINING BICYCLIC HETEROCYCLES FOR USE AS ANTIBACTERIALS 审中-公开
标题翻译：含氮的双环杂环化合物作为抗生素使用
公开(公告)号：WO2003087098A1
公开(公告)日：2003-10-23
申请号：PCT/EP2002/005708
申请日：2002-05-24
申请人： SMITHKLINE BEECHAM P.L.C. , BROOKS, Gerald , DAVIES, David, Thomas , JONES, Graham, Elgin , MARKWELL, Roger, Edward , PEARSON, Neil, David
发明人： BROOKS, Gerald , DAVIES, David, Thomas , JONES, Graham, Elgin , MARKWELL, Roger, Edward , PEARSON, Neil, David
IPC分类号： C07D471/04
CPC分类号： C07D401/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07D491/04 , C07D513/04
摘要： Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives hereof useful in methods of treatment of bacterial infections in mammals, particularly man.
摘要翻译：环己烷和环己烯衍生物及其药学上可接受的衍生物可用于哺乳动物，特别是人的细菌感染治疗方法。

6. 发明申请

WO2002096907A1 BICYCLIC NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES FOR USE AS ANTIBACTERIALS 审中-公开
标题翻译：用作抗菌剂的含二氧化氮的杂环衍生物
公开(公告)号：WO2002096907A1
公开(公告)日：2002-12-05
申请号：PCT/EP2002/005709
申请日：2002-05-24
申请人： SMITHKLINE BEECHAM P.L.C. , DARTOIS, Catherine, Genevieve, Yvette , MARKWELL, Roger, Edward , MADLER, Guy, Marguerite, Marie, Gerard , PEARSON, Neil, David
发明人： DARTOIS, Catherine, Genevieve, Yvette , MARKWELL, Roger, Edward , MADLER, Guy, Marguerite, Marie, Gerard , PEARSON, Neil, David
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
摘要翻译：哌啶衍生物及其药学上可接受的衍生物可用于哺乳动物，特别是人的细菌感染治疗方法。

7. 发明申请

WO1993009136A1 PHOSPHONOPEPTIDES WITH COLLAGENASE INHIBITING ACTIVITY 审中-公开
标题翻译：具有胶原抑制活性的磷酸化酶
公开(公告)号：WO1993009136A1
公开(公告)日：1993-05-13
申请号：PCT/GB1992001903
申请日：1992-10-16
申请人： SMITHKLINE BEECHAM PLC , HUNTER, David, James , MARKWELL, Roger, Edward , WARD, Robert, William
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07K05/06
CPC分类号： C07K5/06191 , A61K38/00
摘要： Phosphorus derivatives having structure (I), processes for their preparation and their use as collagenase inhibitors.
摘要翻译：具有结构（I）的磷衍生物，其制备方法及其作为胶原酶抑制剂的用途。

8. 发明申请

WO1992017444A1 THIOL-CARBOXYLIC ACID DERIVATIVES AS COLLAGENASE INHIBITORS 审中-公开
标题翻译：作为COLLAGENASE抑制剂的THIOL-羧酸衍生物
公开(公告)号：WO1992017444A1
公开(公告)日：1992-10-15
申请号：PCT/GB1992000612
申请日：1992-04-06
申请人： SMITHKLINE BEECHAM PLC , MARKWELL, Roger, Edward , WARD, Robert, William , RATCLIFFE, Steven, John
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07C327/32
CPC分类号： C07C327/32 , C07C323/60
摘要： A compound of formula (I) or a salt, solvate or hydrate thereof in which, R1 is -OH; alkoxy; aryloxy or aralkyloxy; -NR6R7, where each of R6 and R7 is independently hydrogen or alkyl, or R6 and R7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an additional oxygen, sulphur or optionally substituted nitrogen atom in the ring; or a group (II) where R8 is hydrogen; alkyl optionally substituted by -OH, alkoxy, -NR6R7, guanidine, -CO2H, CONH2, SH, or S-alkyl; or -CH2-Ar where Ar is optionally substituted aryl; and R9 is alkoxy; OH; or -NR6R7; R2 is hydrogen; or acyl, such as (a) or (b)-, where Z is optionally substituted aryl; R3 is C3-6 alkyl; R4 is -(CH2)nNR10R11, -(CH2)nNHCOR12, -(CH2)nNR13C(=NR14)NR10R11, -(CH2)nCONH(CH2)qNR10R11 or -(CH2)n-R15 where n is an integer from 1 to 6, and q is an integer from 2 to 4, and each of R10 and R11 is independently hydrogen or alkyl, or R10 and R11 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom or an optionally substituted second nitrogen atom in the ring, R12 is alkyl, alkoxy, aralkyloxy or -(CH2)mNR10R11, where m is 1 or 2, R13 is hydrogen or alkyl, R14 is hydrogen or alkyl or R14 and R10 together with the nitrogen atoms to which they are bonded form an optionally substituted 5-, 6- or 7-membered ring, and R15 is an optionally substituted piperidyl ring; and R5 is hydrogen, alkyl, -CH2-(CH2)nOR16, -CH2-(CH2)n-OCOR17 or (III) where n is an integer from 1 to 6, R16, R17 and R18 are independently hydrogen or C1-6 alkyl, and R19 is hydroxy, -O-C1-6alkyl or NR10R11 where R10 and R11 are as defined for R4, for use in the treatment of collagenolytic conditions.
摘要翻译：式（I）化合物或其盐，溶剂化物或水合物，其中R 1为-OH; 烷氧基; 芳氧基或芳烷氧基; -NR6R7，其中R6和R7各自独立地为氢或烷基，或R6和R7与它们所键合的氮原子一起形成具有另外的氧，硫或任选取代的5-，6-或7-元环环中的氮原子; 或其中R8为氢的基团（II）; 任选被-OH，烷氧基，-NR 6 R 7，胍，-CO 2 H，CONH 2，SH或S-烷基取代的烷基; 或-CH 2 -Ar，其中Ar是任选取代的芳基; 且R 9为烷氧基; 哦; 或-NR 6 R 7; R2是氢; 或酰基，例如（a）或（b） - ，其中Z是任选取代的芳基; R3是C3-6烷基; R4是 - （CH2）nNR10R11， - （CH2）nNHCOR12， - （CH2）nNR13C（= NR14）NR10R11， - （CH2）nCONH（CH2）qNR10R11或 - （CH2）n -R15，其中n是从1到 6，q为2〜4的整数，R 10和R 11分别独立地为氢或烷基，或R 10和R 11与它们所键合的氮原子一起形成5-，6-或7-元环在环中具有任选的氧或硫原子或任选取代的第二氮原子，R 12是烷基，烷氧基，芳烷氧基或 - （CH 2）m NR R 10 R 11，其中m是1或2，R 13是氢或烷基，R 14是氢或烷基或R 14和R 10与它们所键合的氮原子一起形成任选取代的5-，6-或7-元环，R 15是任选取代的哌啶基环; 其中n为1至6的整数，R 16，R 17和R 18独立地为氢或C 1-6烷基，-CH 2 - （CH 2）nOR 16，-CH 2 - 烷基，R 19为羟基，-O-C 1-6烷基或NR 10 R 11，其中R 10和R 11如R4所定义，用于治疗胶原溶解条件。

9. 发明申请

WO1991015506A1 PHOSPHONOPEPTIDES WITH COLLAGENASE INHIBITING ACTIVITY 审中-公开
标题翻译：具有胶原抑制活性的磷酸化酶
公开(公告)号：WO1991015506A1
公开(公告)日：1991-10-17
申请号：PCT/GB1991000529
申请日：1991-04-05
申请人： BEECHAM GROUP P.L.C. , MARKWELL, Roger, Edward , RAHMAN, Shahzad, Sharooq , WARD, Robert, William
发明人： BEECHAM GROUP P.L.C.
IPC分类号： C07K05/06
CPC分类号： C07K5/06191 , A61K38/00 , C07F9/4006
摘要： Azalactam derivatives processes for their preparation and their use as collagenase inhibitors having structure (I).
摘要翻译：内酰胺衍生物的制备方法及其作为具有结构（I）的胶原酶抑制剂的用途。

10. 发明申请

WO1986006068A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO1986006068A1
公开(公告)日：1986-10-23
申请号：PCT/GB1986000205
申请日：1986-04-11
申请人： BEECHAM GROUP P.L.C. , MARKWELL, Roger, Edward , SMITH, Stephen, Allan
发明人： BEECHAM GROUP P.L.C.
IPC分类号： C07D217/22
CPC分类号： C07D217/24 , C07D217/22
摘要： Compounds of general formula (I) wherein: R1 and R2 are independently hydrogen, C1-6 alkyl or together are a group X which is C3-6 polymethylene optionally interrupted by O, S or NR6 wherein R6 is hydrogen or C1-6 alkyl; R3 is phenyl, optionally substituted by one or more substituents selected from halogen, CF3, nitro, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C2-7 alkanoyl, carboxyl, C1-6 alkoxycarbonyl, cyano, CONR7R8 wherein R7 and R8 are selected from hydrogen or C1-6 alkyl or together are a group X; NR9 R10 wherein R9 and R10 are selected from hydrogen, C1-6 alkyl, C2-7 alkanoyl or C1-6 alkylsulphonyl or together are a group X; SO2NR11R12 wherein R11 and R12 are selected from hydrogen or C1-6 alkyl or together are a group X; or S(O)mR13 wherein m is 1 or 2 and R13 is C1-6 alkyl; R4 and R5 are independently selected from hydrogen, C1-6 alkyl, cyano, amino, aminocarbonyl, or aminocarbamoyl optionally substituted by one or two C1-6 alkyl groups or together are a group X, halogen, CF3, nitro, C1-6 alkoxy, C1-6 alkylthio, C2-7 alkanoyloxy or hydroxy, or together are methylenedioxy or C3-5 polymethylene; are of value in the prophylaxis and treatment of allergic and inflammatory disorders.
摘要翻译：通式（I）的化合物，其中：R 1和R 2独立地为氢，C 1-6烷基或一起为基团X，其为任选被O，S或NR 6中断的C 3-6的多亚甲基，其中R 6为氢或C 1-6烷基; R3是任选被一个或多个选自卤素，CF 3，硝基，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，C 2-7烷酰基，羧基，C 1-6烷氧基羰基，氰基，CONR 7 R 8的取代基取代的苯基，其中 R 7和R 8选自氢或C 1-6烷基或一起为基团X; NR 9 R 10，其中R 9和R 10选自氢，C 1-6烷基，C 2-7烷酰基或C 1-6烷基磺酰基或一起为基团X; SO 2 NR 11 R 12其中R 11和R 12选自氢或C 1-6烷基或一起为基团X; 或S（O）m R 13，其中m为1或2，R 13为C 1-6烷基; R 4和R 5独立地选自氢，C 1-6烷基，氰基，氨基，氨基羰基或任选被一个或两个C 1-6烷基取代的氨基氨基甲酰基，或一起是基团X，卤素，CF 3，硝基，C 1-6烷氧基 C 1-6烷硫基，C 2-7烷酰氧基或羟基，或一起为亚甲二氧基或C 3-5亚甲基; 在预防和治疗过敏性和炎症性疾病中具有价值。

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