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11. 发明申请

WO2004031137A1 CYCLOHEXYL SULPHONE DERIVATIVES AS GAMMA-SECRETASE INHIBITORS 审中-公开
标题翻译：作为GAMMA-SECRETASE抑制剂的CYCLOHEXYL SULPHONE衍生物
公开(公告)号：WO2004031137A1
公开(公告)日：2004-04-15
申请号：PCT/GB2003/004102
申请日：2003-09-25
申请人： MERCK SHARP & DOHME LIMITED , CHURCHER, Ian , HARRISON, Timothy , KERRAD, Sonia , OAKLEY, Paul, Joseph , SHAW, Duncan, Edward , TEALL, Martin, Richard , WILLIAMS, Susannah
发明人： CHURCHER, Ian , HARRISON, Timothy , KERRAD, Sonia , OAKLEY, Paul, Joseph , SHAW, Duncan, Edward , TEALL, Martin, Richard , WILLIAMS, Susannah
IPC分类号： C07C317/14
CPC分类号： C07D213/70 , C07C317/14 , C07C317/18 , C07C317/20 , C07C317/22 , C07C317/24 , C07C317/44 , C07C331/04 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/48 , C07D211/96 , C07D213/71 , C07D213/89 , C07D233/84 , C07D239/38 , C07D249/12 , C07D257/04 , C07D277/36 , C07D285/125 , C07D295/088 , C07D295/26 , C07D307/38 , C07D307/46 , C07D307/52 , C07D307/64 , C07D307/68 , C07D317/46 , C07D333/18 , C07D333/48 , C07D491/08
摘要： Compounds of formula (I) inhibit the processing of APP by gamma-secretase, and hence are useful in treatment of Alzheimer's disease.
摘要翻译：式（I）化合物通过γ-分泌酶抑制APP的加工，因此可用于治疗阿尔茨海默氏病。

12. 发明申请

WO2002081433A1 SULPHONES WHICH MODULATE THE ACTION OF GAMMA SECRETASE 审中-公开
标题翻译：调节伽马秘密行动的磺胺
公开(公告)号：WO2002081433A1
公开(公告)日：2002-10-17
申请号：PCT/GB2001/003778
申请日：2001-08-21
申请人： MERCK SHARP & DOHME LIMITED , HARRISON, Timothy , OAKLEY, Paul, Joseph , TEALL, Martin, Richard
发明人： HARRISON, Timothy , OAKLEY, Paul, Joseph , TEALL, Martin, Richard
IPC分类号： C07C317/14
CPC分类号： C07D233/64 , C07C317/14 , C07C317/18 , C07C317/44 , C07C2601/04 , C07C2601/08 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/088
摘要： Novel sulphones of Formula I are disclosed. The novel compounds modulate the action of gamma secretase, and hence find use in the treatment or prevention of Alzheimer's disease.
摘要翻译：公式I的新型手机被公开。新型化合物调节γ分泌酶的作用，因此可用于治疗或预防阿尔茨海默氏病。

13. 发明申请

WO1995030674A1 MORPHOLINE DERIVATIVES AND THEIR USE AS ANTAGONISTS OF TACHIKININS 审中-公开
标题翻译：吗啉衍生物及其作为TACHIKININS的拮抗剂使用
公开(公告)号：WO1995030674A1
公开(公告)日：1995-11-16
申请号：PCT/GB1995000983
申请日：1995-05-01
申请人： MERCK SHARP & DOHME LIMITED , HAWORTH, Karen, Elizabeth , TEALL, Martin, Richard , SEWARD, Eileen, Mary , SWAIN, Christopher, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： The present invention relates to compounds of formula (I): wherein X is N or CH; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.
摘要翻译：本发明涉及式（I）化合物：其中X是N或CH; 及其药学上可接受的盐和前药。该化合物特别用于治疗疼痛，炎症，偏头痛和呕吐。

14. 发明申请

WO1993024465A1 2/3-(HETEROCYCLIC ALKYL AMINO)-1-(SUBST.-PHENYL-METHOXY)-ETHANES/PROPANES AS TACHYKININ-RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2 / 3-（杂环烷基氨基）-1-（亚苯基 - 甲氧基） - 乙醇/丙酮作为TACHYKININ-RECEPTOR ANTAGONISTS
公开(公告)号：WO1993024465A1
公开(公告)日：1993-12-09
申请号：PCT/GB1993001072
申请日：1993-05-25
申请人： MERCK SHARP & DOHME LIMITED , OWENS, Andrew, Pate , TEALL, Martin, Richard , WILLIAMS, Brian, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D233/54
CPC分类号： C07D249/08 , C07D233/76 , C07D257/04 , C07D271/07
摘要： Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents phenyl or benzhydryl; X and Y each represent H or X and Y together form a group =0; Z is O, S or NR (R is H or C1-6alkyl); R is H, optionally substituted C1-6alkyl, phenyl(C1-4 alkyl), C2-6alkylene, COR , COOR , CONHR , COC1-4alkylNR R , or CONR C1-4alkylCONR R ; R is C1-4alkyl substituted by an optionally substituted aromatic heterocycle; R is H, C1-6alkyl or C2-6alkenyl; R is H, C1-6alkyl or optionally substituted phenyl; R represents optionally substituted phenyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.
摘要翻译：式（I）化合物及其盐和前药，其中Q表示苯基或二苯甲基; X和Y各自表示H或X和Y一起形成基团= 0; Z是O，S或NR 8（R 8是H或C 1-6烷基）; R 1是H，任选取代的C 1-6烷基，苯基（C 1-4烷基），C 2-6亚烷基，COR a，COOR a，CONHR a，COC 1-4烷基NR a R b，，或CONR a C 1-4烷基CONR a R b; R 2是被任选取代的芳族杂环取代的C 1-4烷基; R 3是H，C 1-6烷基或C 2-6烯基; R 4是H，C 1-6烷基或任选取代的苯基; R 5表示任选取代的苯基; q为0,1,2或3; 是用于治疗的速激肽拮抗剂。

15. 发明申请

WO2010007382A1 BENZAZEPINE DERIVATIVES AND THEIR USE AS HSTAMINE H3 ANTAGONISTS 审中-公开
标题翻译：苯并吖庚因衍生物及其作为HSTAMINE H3拮抗剂的用途
公开(公告)号：WO2010007382A1
公开(公告)日：2010-01-21
申请号：PCT/GB2009/001774
申请日：2009-07-17
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED. , POONI, Parminder, Kaur , MERCHANT, Kevin, John , KERR, Catrina , CROSBY, Stuart, Richard , OKAWA, Tomohiro , SASAKI, Mitsuru , GOTOU, Mika , SHOWELL, Graham, Andrew , TEALL, Martin, Richard
发明人： POONI, Parminder, Kaur , MERCHANT, Kevin, John , KERR, Catrina , CROSBY, Stuart, Richard , OKAWA, Tomohiro , SASAKI, Mitsuru , GOTOU, Mika , SHOWELL, Graham, Andrew , TEALL, Martin, Richard
IPC分类号： C07D223/16 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , A61K31/55 , A61P25/18
CPC分类号： C07D403/12 , C07D223/16 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要： A compound having the formula (1) wherein: R1 is a group selected from C 3-8 cycloalkyl, C 1-6 alkyl, C 1-6 alkylene-C 3-8 cycloalkyl, each of which groups may optionally be substituted with C 1-6 alkyl, halogen, haloC 1-6 alkyl or OR15, or R1 is heterocyclyl, optionally substituted with C 1-6 alkyl, haloC 1-6 alkyl or OR15; n is 0, 1, 2, 3 or 4, the alkylene group -(CH 2 ) n - formed thereby being optionally substituted with a group selected from C 1-4 alkyl, C 3-8 cycloalkyl and arylsulfonyl; A is a group selected from -N(R2)CO-, -CON(R2)-, -OC(O)-, -C(O)O-, -CO-, -C(R2)(OR3)-, -C(=N-O-R3)-, - C(=CR2R3)-, -C 3-8 cycloalkylene-, -C(R2)(haloC 1-6 alkyl)-, C 1-4 alkylene and -C(OR3)(haloC 1-6 alkyl)-; R2 and R3 are each independently selected from H, C 1-6 alkyl, and C 3-8 cycloalkyl, or, when A is -N(R2)CO- and X is absent, R2 may form, together with the adjacent nitrogen atom and Z, an N-containing heterocyclyl group, which may optionally be substituted; X is absent or is C 1-4 alkylene or C 2-4 alkenylene, each of which may optionally be substituted with one or more C 1-4 alkyl groups, OR16, halogen or haloC 1-6 alkyl; Z is selected from aryl, heteroaryl, C 3-8 cycloalkyl, and heterocyclyl, each of which may optionally be substituted by a group selected from -Y-aryl, -Y-heteroaryl, -Y-C 3-8 cycloalkyl and -Y-heterocyclyl, or, when X is present, Z may be H, or, when X is absent and A is -C(R2)(OR3)- or -N(R2)CO-, Z may be H, or, when A is -N(R2)CO- and X is absent, Z may form, together with the adjacent nitrogen atom and R2, an N-containing heterocyclyl group which may optionally be substituted, wherein, when A is -CO-, Z is linked to X or A via a carbon atom and wherein, when A is -N(R2)CO- and Z is H, R1 is C 3-8 cycloalkyl; and Y represents a bond, C 1-6 alkylene, CO, NR14, COC 2-6 alkenylene, O, SO 2 or NHCOC 1-6 alkylene; wherein said cycloalkyl, aryl, heteroaryl and heterocyclyl groups Z may be optionally substituted by one or more substituents which may be the same or different, and which are selected from halogen, haloC 1-6 alkyl, hydroxy, cyano, nitro, =O, -R4, -CO 2 R4, -COR4, -NR5R6, -C 1-6 alkyl-NR5R6, -C 3-8 cycloalkyl-NR5R6, - CONR12R13, -NR12COR13, -NR5SO 2 R6, -OCONR5R6, -NR5CO 2 R6, -NR4CONR5R6 or -SO 2 NR5R6- SHR8, -alkyl-OR8, -SOR8, -OR9, -SO 2 R9, -OSO 2 R9, -alkyl-SO 2 R9, -alkyl-CONHR9, -alkyl-SONHR9, -alkyl-COR10, -CO-alkyl-R10, -O-alkyl-R11 (wherein R4, R5 and R6 independently represent hydrogen, C 1-6 alkyl, -C 3-8 cycloalkyl, -C 1-6 alkylene-C 3-8 cycloalkyl, aryl, heterocyclyl or heteroaryl, wherein R8 represents C 1-6 alkyl, wherein R9 represents C 1-6 alkyl or aryl, wherein R10 represents aryl, wherein R11 represents C 3-8 cycloalkyl or aryl, R12, R13, R14, R15 and R16 each independently represent H or C 1-6 alkyl, and wherein -NR5R6 and -NR12R13 may represent a nitrogen containing heterocyclyl group); wherein said R4, R5, R6 R8, R9, R11 and R11 groups may be optionally substituted by one or more substituents which may be the same or different, and which are selected from the group consisting of halogen, hydroxy, C 1-6 alkyl, C 1-6 alkoxy, cyano, amino, =O or trifluoromethyl; and wherein substituents of Z selected from -Y-aryl, -Y-heteroaryl, -Y-C 3-8 cycloalkyl and -Y-heterocyclyl may be optionally substituted by one or more substituents selected from =O, hydroxy, cyano, nitro, halogen, haloC 1-6 alkyl and C 1-6 alkyl; and wherein, when A is C 1-4 alkylene, said cycloalkyl, aryl, heteroaryl or heterocyclyl group Z (such as a heterocyclyl group Z) is substituted at least with hydroxy, CF 3 , or =0; and wherein, when A is CON(R2) n is 1; or a pharmaceutically acceptable salt or ester thereof, provided that: when A is -CO-, R1 is CH 3 , C 3-8 cycloalkyl-substituted C 1-6 alkylene or n-butyl, n is 0 and X is -CH 2 CH 2 -, Z is not N-benzyl substituted 4-piperidinyl, N-(3-fluorobenzyl)-substituted 4-piperidinyl or N-acetyl substituted 4-piperidinyl; when A is -OC(O)-, R1 is cyclobutyl, n is 0 and X is -CH 2 CH 2 -, Z is not H; when A is -OC(O)-, R1 is n-propyl, n is 0 and X is -CH 2 -, Z is not H; and when A is -CO-, R1 is CH 3 , n is 0 and X is CH 2 , Z is not H.
摘要翻译：具有式（1）的化合物，其中：R 1是选自C 3-8环烷基，C 1-6烷基，C 1-6烷氧基， C 1-6亚烷基-C 3-8环烷基，其中每个基团可以任选地被C 1-6烷基，卤素，C 1-6烷氧基，卤代C 1-6烷基或OR 15，或R 1为杂环基，任选被C 1-6烷基，卤代C 1-6烷基或OR 15取代 ; n是0,1,2,3或4，由此形成的亚烷基 - （CH 2）n - 被任选地被选自C 1 -C 4 - 1-4烷基，C 3-8环烷基和芳基磺酰基; A是选自-N（R 2）CO-，-CON（R 2） - ，-OC（O） - ，-C（O）O - ， - CO-，-C（R 2）（OR 3） - 的基团，（= NO-R 3） - ， - C（= CR 2 R 3） - ， - C 3-8亚环烷基 - ， - C（R 2）（卤代C 1-6 - 烷基） - ，C 1-4亚烷基和-C（OR 3）（卤代C 1-6烷基） - ; R 2和R 3各自独立地选自H，C 1-6烷基和C 3-8环烷基，或者当A是-N（R 2）CO-时，和 X不存在时，R2可与相邻的氮原子和Z一起形成任选被取代的含N杂环基; X不存在或为C 1-4亚烷基或C 2-4亚烯基，其各自可任选被一个或多个C 1-4亚芳基取代，烷基，OR 16，卤素或卤代C 1-6烷基; Z选自芳基，杂芳基，C 3-8环烷基和杂环基，其各自可任选被选自-Y-芳基，-Y-杂芳基，-YC _{3-8 或= 0; 并且其中当A是CON（R2）时，n是1; 条件是：当A是-CO-时，R 1是CH 3 3，C 3-8环烷基取代的C 1 -6亚烷基或正丁基，n为0且X为-CH 2 CH 2 - ，Z不是N-苄基取代的4-哌啶基， N-（3-氟苄基） - 取代的4-哌啶基或N-乙酰基取代的4-哌啶基; 当A是-OC（O） - 时，R 1是环丁基，n是0且X是-CH 2 CH 2 - ，Z不是H; 当A是-OC（O） - 时，R 1是正丙基，n是0且X是-CH 2 - ，Z不是H; 当A是-CO-时，R1是CH 3，n是0且X是CH 2，Z不是H.}

16. 发明申请

WO2007054739A1 TETRAHYDROINDOLE DERIVATIVES FOR TREATMENT OF ALZHEIMER'S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的四氢吡啶衍生物
公开(公告)号：WO2007054739A1
公开(公告)日：2007-05-18
申请号：PCT/GB2006/050368
申请日：2006-11-03
申请人： MERCK SHARP & DOHME LIMITED , BURKAMP, Frank , CHECKSFIELD, Graham, David , FLETCHER, Stephen, Robert , LEWIS, Stephen, John , MCIVER, Edward, Giles , OAKLEY, Paul, Joseph , TEALL, Martin, Richard
发明人： BURKAMP, Frank , CHECKSFIELD, Graham, David , FLETCHER, Stephen, Robert , LEWIS, Stephen, John , MCIVER, Edward, Giles , OAKLEY, Paul, Joseph , TEALL, Martin, Richard
IPC分类号： C07D209/30 , C07D209/42 , C07D209/08 , C07D405/04 , C07D231/56 , C07D209/86 , C07D401/04 , A61K31/403 , A61K31/404 , A61K31/416 , A61P25/28
CPC分类号： C07D209/30 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/42 , C07D209/86 , C07D231/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译：公开了式（I）的四氢吲哚衍生物：这些化合物调节γ-分泌酶的活性，因此可用于治疗或预防阿尔茨海默病。

17. 发明申请

WO2004089911A1 PYRAZOLE DERIVATIVES AS GAMMA-SECRETASE INHIBITORS USEFUL IN THE TREATMENT OF ALZHEIMER’S DISEASE 审中-公开
标题翻译：用作治疗阿尔茨海默病的GAMMA-分泌酶抑制剂的吡唑衍生物
公开(公告)号：WO2004089911A1
公开(公告)日：2004-10-21
申请号：PCT/GB2004/001452
申请日：2004-04-01
申请人： MERCK SHARP & DOHME LIMITED , BETTATI, Michela , CHAMBERS, Mark, Stuart , HUNT, Peter, Alan , JONES, Philip , MACLEOD, Angus, Murray , SZEKERES, Helen, Jane , TEALL, Martin, Richard
发明人： BETTATI, Michela , CHAMBERS, Mark, Stuart , HUNT, Peter, Alan , JONES, Philip , MACLEOD, Angus, Murray , SZEKERES, Helen, Jane , TEALL, Martin, Richard
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , C07D401/04 , C07D401/06 , C07D409/12
摘要： The compounds of formula (I): inhibit gamma-secretase and hence are of utility in the treatment or prevention of Alzheimer's disease.
摘要翻译：式（I）化合物：抑制γ-分泌酶，因此可用于治疗或预防阿尔茨海默氏病。

18. 发明申请

WO2004013090A1 SYNTHESIS OF CYCLOHEXANONE DERIVATIVES 审中-公开
标题翻译：环己酮衍生物的合成
公开(公告)号：WO2004013090A1
公开(公告)日：2004-02-12
申请号：PCT/GB2003/003224
申请日：2003-07-30
申请人： MERCK SHARP & DOHME LIMITED , MERCK & CO., INC. , BRANDS, Karel, Marie, Joseph , DAVIES, Antony, John , OAKLEY, Paul, Joseph , SCOTT, Jeremy, Peter , SHAW, Duncan, Edward , TEALL, Martin, Richard
发明人： BRANDS, Karel, Marie, Joseph , DAVIES, Antony, John , OAKLEY, Paul, Joseph , SCOTT, Jeremy, Peter , SHAW, Duncan, Edward , TEALL, Martin, Richard
IPC分类号： C07C315/04
CPC分类号： C07C315/04 , C07C2601/14 , C07C317/24 , C07C317/44
摘要： A novel process for preparing cyclohexanones (1) is described. The products are useful as gamma-secretase inhibitors, or as intermediates in the synthesis of other gamma-secretase inhibitors.
摘要翻译：描述了一种制备环己酮（1）的新方法。该产品可用作γ-分泌酶抑制剂，或作为合成其它γ-分泌酶抑制剂的中间体。

19. 发明申请

WO0138326A3 IMIDAZO-PYRIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：咪达唑啶衍生物作为GABA受体的配体
公开(公告)号：WO0138326A3
公开(公告)日：2002-05-10
申请号：PCT/GB0004451
申请日：2000-11-22
申请人： MERCK SHARP & DOHME , CRAWFORTH JAMES MICHAEL , GOODACRE SIMON CHARLES , HALLETT DAVID JAMES , HARRISON TIMOTHY , OWENS ANDREW PATE , ROWLEY MICHAEL , TEALL MARTIN RICHARD
发明人： CRAWFORTH JAMES MICHAEL , GOODACRE SIMON CHARLES , HALLETT DAVID JAMES , HARRISON TIMOTHY , OWENS ANDREW PATE , ROWLEY MICHAEL , TEALL MARTIN RICHARD
IPC分类号： A61K31/437 , A61K31/444 , A61P1/08 , A61P3/04 , A61P15/00 , A61P21/00 , A61P23/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P27/16 , A61P43/00 , C07B61/00 , C07D471/04
CPC分类号： C07D471/04
摘要： A class of 3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a -NH- linkage, are selective ligands for GABAA receptors, in particular having high affinity for the alpha 2 and/or alpha 3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
摘要翻译：一类3-苯基咪唑并[1,2-a]吡啶衍生物，其通过任选取代的被氧原子连接或桥连的芳基或杂芳基在苯环的间位取代或-NH-键是GABA A受体的选择性配体，特别是对其α2和/或α3亚基具有高亲和力，因此有益于治疗和/或预防中枢神经系统疾病，包括焦虑和抽搐。

20. 发明申请

WO1994015903A1 3,3 DIPHENYL PROP-2-YL AMINO ACID DERIVATIVES AND THEIR USE AS TACHYKININ ANTAGONISTS 审中-公开
标题翻译： 3,3 DIPHENYL PROP-2-YL氨基酸衍生物及其作为TACHYKININ ANTAGONISTS的用途
公开(公告)号：WO1994015903A1
公开(公告)日：1994-07-21
申请号：PCT/GB1993002592
申请日：1993-12-17
申请人： MERCK SHARP & DOHME LIMITED , TEALL, Martin, Richard , WILLIAMS, Brian, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07C229/14
CPC分类号： C07C229/14
摘要： Compounds of formula (I), or a salt or prodrug thereof, wherein R represents H, C1-4alkyl or CH2COOH; R represents H or C1-4alkyl, with the proviso that R and R are not both H; R and R each independently represent H, C1-6alkyl, C2-6alkenyl, C1-6alkoxy, halo or trifluoromethyl; A , A , A and A each independently represent H, C1-6alkyl, C1-6alkenyl, C1-6alkoxy, halo or trifluoromethyl; and A and A each independently represent H or C1-4alkyl are tachykinin antagonists useful as medicaments.
摘要翻译：式（I）化合物或其盐或前药，其中R 1表示H，C 1-4烷基或CH 2 COOH; R 2表示H或C 1-4烷基，条件是R 1和R 2不同时为H; R 3和R 4各自独立地表示H，C 1-6烷基，C 2-6烯基，C 1-6烷氧基，卤素或三氟甲基; A 1，A 2，A 3和A 4各自独立地表示H，C 1-6烷基，C 1-6烯基，C 1-6烷氧基，卤素或三氟甲基; 并且A 5和A 6各自独立地表示H或C 1-4烷基是用作药物的速激肽拮抗剂。

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