专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO1996019451A1 SUBSTITUTED AZETIDIN-2-ONES FOR TREATMENT OF ATHEROSCLEROSIS 审中-公开
标题翻译：用于治疗甲状腺功能亢进症的AZETIDIN-2-ONES
公开(公告)号：WO1996019451A1
公开(公告)日：1996-06-27
申请号：PCT/EP1995005130
申请日：1995-12-20
申请人： SMITHKLINE BEECHAM PLC , HICKEY, Deirdre, Mary, Bernadette , DHANAK, Dashyant , LEACH, Colin, Andrew , IFE, Robert, John , TEW, David, Graham
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D205/09
CPC分类号： C07D205/09
摘要： Compounds of formula (I) in which R and R , which may be the same or different, is each selected from hydrogen, halogen or C(1-8)alkyl; R is aryl or arylC(1-4)alkyl which may be optionally substituted; X is a linker group; Y is an optionally substituted aryl group; and n is 0, 1 or 2; are inhibitors of the enzyme Lp-PLA2 and thereof of use in treating atherosclerosis.
摘要翻译：其中R 1和R 2可以相同或不同的式（I）化合物各自选自氢，卤素或C（1-8）烷基; R 3是可以任选被取代的芳基或芳基C（1-4）烷基; X是连接基团; Y是任选取代的芳基; 且n为0,1或2; 是用于治疗动脉粥样硬化的酶Lp-PLA2及其抑制剂。

2. 发明申请

WO2006000399A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2006000399A1
公开(公告)日：2006-01-05
申请号：PCT/EP2005/006760
申请日：2005-06-21
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , MASON, Andrew, McMurtrie
发明人： BORTHWICK, Alan, David , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , MASON, Andrew, McMurtrie
IPC分类号： C07D401/06
CPC分类号： A61K31/5377 , C07D401/06 , C07D413/14
摘要： Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2, 6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
摘要翻译：式（I）的化合物，其中R 1是2-茚满基，R 2是1-甲基丙基，R 3是选自2,6-二甲基-3-吡啶基或4,6-二甲基-3-吡啶基的基团，R 4表示甲基和R 5 表示氢或甲基，或者R4和R5与它们所连接的氮原子一起代表吗啉代及其药学上可接受的衍生物，其制备方法，含有它们的药物组合物及其在药物中的用途，特别是其用作催产素拮抗剂。

3. 发明申请

WO2003053443A1 SUBSTITUTED DIKETOPIPERAZINES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：替代哌替啶作为氧化蛋白拮抗剂
公开(公告)号：WO2003053443A1
公开(公告)日：2003-07-03
申请号：PCT/EP2002/014823
申请日：2002-12-20
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , HATLEY, Richard, Jonathan , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , LIVERMORE, David, George, Hubert , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , NEROZZI, Fabrizio , SOLLIS, Steven, Leslie , SZARDENINGS, Anna, Katrin , WYATT, Paul, Graham
发明人： BORTHWICK, Alan, David , HATLEY, Richard, Jonathan , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , LIVERMORE, David, George, Hubert , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , NEROZZI, Fabrizio , SOLLIS, Steven, Leslie , SZARDENINGS, Anna, Katrin , WYATT, Paul, Graham
IPC分类号： A61K31/495
CPC分类号： C07D241/08 , A61K38/00 , C07D401/10 , C07D403/06 , C07D413/10 , C07D417/06 , C07K5/06078 , C07K5/06191
摘要： A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of the formula (I)and/or a physiologically acceptable derivative thereof, wherein the substituents have the meaning given in the description. Disclosed are also novel compounds of formula (I) and processes for their preparation.
摘要翻译：一种治疗或预防通过催产素作用介导的疾病或病症的方法，其包括向有需要的哺乳动物施用有效量的式I化合物和/或其生理上可接受的衍生物，其中所述取代基具有给定的含义在说明中。公开了式I的新化合物及其制备方法。

4. 发明申请

WO1997021676A1 AZETIDINONE COMPOUNDS FOR THE TREATMENT OF ATHEROSCLEROSIS 审中-公开
标题翻译：用于治疗甲状腺功能亢进症的AZETIDINONE化合物
公开(公告)号：WO1997021676A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996005588
申请日：1996-12-04
申请人： SMITHKLINE BEECHAM PLC , HICKEY, Deirdre, Mary, Bernadette , DHANAK, Dashyant , IFE, Robert, John , LEACH, Colin, Andrew , TEW, David, Graham
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D205/09
CPC分类号： C07D401/14 , C07D205/09 , C07D413/06 , C07D413/12 , C07D417/12
摘要： Azetidinone compounds of formula (I) in which inter alia: R is CR R -X -Y or (CH2)pX (CH2)qY ; R and R which may be the same or different is each selected from hydrogen and C(1-6)alkyl, or R and R may be linked together to form the residue of a C(3-7)cycloalkyl ring; X is a linker group and Y is optionally substituted C(1-12)alkyl C(2-12)alkynyl, C(2-12)alkynyl, C(3-7)-cycloalkylC(1-8) alkyl or an optionally substituted heteroaryl group; and X is a heteroaryl group and Y is an optionally substituted aryl group, p is an integer from 1 to 6, q is 0 or an integer from 1 to 6; are inhibitors of the phospholipase A2 enzyme Lp PLA2 and are of use in therapy, for instance in treating atherosclerosis.
摘要翻译：式（I）的氮杂环丁酮化合物，其中特别是：R 0是CR 4 R 5 -X 1 -X 1或（CH 2）p X 2（CH 2）q Y 2 ; R 4和R 5可以相同或不同，各自选自氢和C（1-6）烷基，或者R 4和R 5可以连接在一起形成残基 C（3-7）环烷基环; X 1是连接基团，Y 1是任选取代的C（1-12）烷基C（2-12）炔基，C（2-12）炔基，C（3-7） - 环烷基C（1- 8）烷基或任选取代的杂芳基; 并且X 2是杂芳基，Y 2是任选取代的芳基，p是1至6的整数，q是0或1-6的整数; 是磷脂酶A2酶Lp PLA2的抑制剂，并且可用于治疗，例如治疗动脉粥样硬化。

5. 发明申请

WO1997021675A1 MONOCYCLIC BETA-LACTAME DERIVATIVES FOR TREATMENT OF ATHEROSCLEROSIS 审中-公开
标题翻译：用于治疗甲状腺功能亢进的单克隆抗体衍生物
公开(公告)号：WO1997021675A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996005587
申请日：1996-12-04
申请人： SMITHKLINE BEECHAM PLC , HICKEY, Deirdre, Mary, Bernadette , DHANAK, Dashyant , IFE, Robert, John , LEACH, Colin, Andrew , TEW, David, Graham
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D205/09
CPC分类号： C07D405/12 , C07D205/08 , C07D205/09
摘要： Compounds of formula (I) are prodrugs of the corresponding compounds in which CO2R is CO2H. These are inhibitors of the phospholipase A2 enzyme Lp-PLA2 and of use in treating atherosclerosis.
摘要翻译：式（I）化合物是其中CO 2 R 3是CO 2 H的相应化合物的前药。这些是磷脂酶A2酶Lp-PLA2的抑制剂，用于治疗动脉粥样硬化。

6. 发明申请

WO1992004330A1 SUBSTITUTED IMIDAZOLES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：取代的咪达唑他们的制剂和药物组合物
公开(公告)号：WO1992004330A1
公开(公告)日：1992-03-19
申请号：PCT/GB1991001546
申请日：1991-09-10
申请人： SMITH KLINE & FRENCH LABORATORIES LIMITED , HICKEY, Deirdre, Mary, Bernadette , COOPER, David, Gwynn , WHITTAKER, Caroline, Marie
发明人： SMITH KLINE & FRENCH LABORATORIES LIMITED
IPC分类号： C07D233/64
CPC分类号： C07D233/64 , C07D233/84 , C07D235/02 , C07D403/06 , C07D405/04 , C07D405/12 , C07D409/04 , C07F9/6506
摘要： Substituted 4,5-diaryl-1-carboxyalkylimidazoles, of structure (I), in which each group Ar is the same or different and is optionally substituted phenyl or optionally substituted heteroaryl or, when both groups Ar are phenyl they can be linked by a bond; R is hydrogen, alkyl, alkoxy, alkyl, optionally substituted phenyl, phenyl alkyl in which the phenyl group is optionally substituted, alkylCHO or alkylCH(OR )(OR ) in which each group R and R is alkyl, or together form an ethane 1,2-diyl or propane 1,3-diyl group; n is 2 to 6 and m is 0 to 6; R , R , R and R are the same or different and are each hydrogen or alkyl; AB is a bond, -C=C-, -CH=CH-, S, O, SPh or OPh; and X is CO2H or a group hydrolysable to CO2H, 5-tetrazolyl, SO3H, P(O)(OR)2, P(O)(OH)2, or P(O)(R)(OR) in which R is hydrogen or alkyl, or a pharmaceutically acceptable salt thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, inter alia, in the treatment of cardiovascular disorders.
摘要翻译：结构（I）的取代的4,5-二芳基-1-羧基烷基咪唑，其中每个基团Ar相同或不同，并且是任选取代的苯基或任选取代的杂芳基，或者当两个基团Ar是苯基时，它们可以通过键; R是氢，烷基，烷氧基，烷基，任选取代的苯基，苯基任选取代的苯基烷基，烷基CHO或烷基CH（OR 1）（OR 2），其中每个基团R 1和R 2是烷基，或一起形成乙烷1,2-二基或丙烷1,3-二基; n为2〜6，m为0〜6; R 3，R 4，R 5和R 6相同或不同，各自为氢或烷基; AB是键，-C = C-，-CH = CH-，S，O，SPh或OPh; 并且X是CO 2 H或可水解成CO 2 H，5-四唑基，SO 3 H，P（O）（OR）2，P（O）（OH）2或P（O）（R）氢或烷基，或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在治疗中的用途，尤其用于治疗心血管疾病。

7. 发明申请

WO2006000759A1 SUBSTITUTED DIKETOPIPERAZINES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：替代哌替啶作为氧化蛋白拮抗剂
公开(公告)号：WO2006000759A1
公开(公告)日：2006-01-05
申请号：PCT/GB2005/002448
申请日：2005-06-21
申请人： GLAXO GROUP LIMITED , BORTHWICK, Alan, David , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , MASON, Andrew McMurtrie , POLLARD, Derek, Roland , SOLLIS, Steven
发明人： BORTHWICK, Alan, David , HICKEY, Deirdre, Mary, Bernadette , LIDDLE, John , MASON, Andrew McMurtrie , POLLARD, Derek, Roland , SOLLIS, Steven
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D403/06 , C07D413/06
摘要： Compounds of formula (I); wherein R 1 is 2-indanyl, R 2 is 1-ethylpropyl, R 3 is a heterocyclic group optionally substituted by one or more C 1-6 alkyl groups, R 4 represents methyl and R 5 represents hydrogen or methyl and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
摘要翻译：式（I）化合物; 其中R 1是2-二氢化茚基，R 2是1-乙基丙基，R 3是任选地被一个或多个C 1 - SUB> 1-6个烷基，R 4代表甲基，R 5表示氢或甲基，其药学上可接受的衍生物被描述为它们的制剂，含有它们的药物组合物及其在医药中的用途，特别是其作为催产素拮抗剂的用途。

8. 发明申请

WO1997041099A1 AZETIDINONE DERIVATIVES FOR THE TREATMENT OF ATHEROSCLEROSIS 审中-公开
标题翻译：用于治疗甲状腺功能亢进症的AZETIDINONE衍生物
公开(公告)号：WO1997041099A1
公开(公告)日：1997-11-06
申请号：PCT/EP1997002286
申请日：1997-04-28
申请人： SMITHKLINE BEECHAM PLC , HICKEY, Deirdre, Mary, Bernadette , LEACH, Colin, Andrew , IFE, Robert, John , DHANAK, Dashyant
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D205/09
CPC分类号： C07D205/08 , C07D205/09 , C07D205/095
摘要： Compounds of formula (I) in which inter alia X is a linker group A-B in which A is bond, CH2O, CO, CONR , COO, CONR CO, or CONR O in which R is hydrogen or C(1-6)alkyl and B is (CH2)pCO(CH2)q in which p is an integer from 1 to 8, preferably 3 to 5, and q is 0 or an integer from 1 to 8, preferably 0, 1 or 2, such that p + q = 1 to 12, preferably 5 to 8, more preferably 5; are inhibitors of the enzyme Lp PLA2 and therefore of use in therapy, in particular, treating atherosclerosis.
摘要翻译：式（I）的化合物，其中特别是X是其中A是键的连接基团AB，CH 2 O，CO，CONR 6，COO，CONR 6 CO或CONR 6 O，其中R 6 >为氢或C（1-6）烷基，B为（CH 2）pCO（CH 2）q，其中p为1至8，优选3至5的整数，q为0或1至8的整数，优选为0,1或2，使得p + q = 1至12，优选5至8，更优选5; 是Lp PLA2酶的抑制剂，因此用于治疗，特别是治疗动脉粥样硬化。

9. 发明申请

WO1997041098A1 AZETIDINONE DERIVATIVES FOR THE TREATMENT OF ATHEROSCLEROSES 审中-公开
标题翻译：用于治疗角质层的AZETIDINONE衍生物
公开(公告)号：WO1997041098A1
公开(公告)日：1997-11-06
申请号：PCT/EP1997001898
申请日：1997-04-15
申请人： SMITHKLINE BEECHAM PLC , LEACH, Colin, Andrew , HICKEY, Deirdre, Mary, Bernadette , IFE, Robert, John , DHANAK, Dashyant , THEOBALD, Colin
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D205/09
CPC分类号： C07D405/12 , C07D205/09
摘要： Selected compounds of formula (I) in which: R is hydrogen or a corresponding pharmaceutically acceptable ester or a pharmaceutically acceptable salt thereof; R and R which may be the same or different is each selected from hydrogen or optionally substituted C(1-6)alkyl; X is a group X'(CH2)m in which X' is CO, CONR , COO, CONR CO, CONHO or CH2O in which R is hydrogen or C(1-6)alkyl and m is 0 or an integer from 1 to 12; or a C(1-12)alkylene chain optionally interrupted by X'; and Y is an optionally substituted aryl group; having the absolute configuration (4R,SS); are inhibitors of the enzyme Lp-PLA2 and thereof of use in treating atherosclerosis.
摘要翻译：选择的式（I）化合物，其中：R 1是氢或相应的药学上可接受的酯或其药学上可接受的盐; R 2和R 3可以相同或不同，各自选自氢或任选取代的C（1-6）烷基; X是X'是其中X'是CO，CONR 4，COO，CONR 4 CO，CONHO或CH 2 O的基团X'（CH 2）m，其中R 4是氢或C（1-6）烷基， m为0或1〜12的整数; 或任选地被X'中断的C（1-12）亚烷基链; Y为任选取代的芳基; 具有绝对构型（4R，SS）; 是用于治疗动脉粥样硬化的酶Lp-PLA2及其抑制剂。

10. 发明申请

WO1997002242A1 AZETIDINONE DERIVATIVES FOR THE TREATMENT OF ATHEROSCLEROSIS 审中-公开
标题翻译：用于治疗甲状腺功能亢进症的AZETIDINONE衍生物
公开(公告)号：WO1997002242A1
公开(公告)日：1997-01-23
申请号：PCT/EP1996002765
申请日：1996-06-20
申请人： SMITHKLINE BEECHAM PLC , DHANAK, Dashyant , HICKEY, Deirdre, Mary, Bernadette , IFE, Robert, John , LEACH, Colin, Andrew , TEW, David, Graham
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D205/08
CPC分类号： C07D401/12 , C07D205/085 , C07D205/095 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Azetidinone compounds of formule (I) in which: R and R , which may be the same or different, is each selected from hydrogen, halogen or C(1-8)alkyl; R and R which may be the same or different is each selected from hydrogen, C(1-6)alkyl, C(2-6)alkenyl, aryl, aryl(C1-4)alkyl and heteroaryl(C1-4)alkyl each of which may be optionally substituted or R and R may be linked together to form the remainder of a (C3-7)cycloalkyl ring; X is a linker group; Y is an optionally substituted aryl group; Z is oxygen and R is C(1-8)alkyl, C(3-8)cycloalkyl, C(3-8)cycloalkylC(1-6)alkyl, heteroaryl, heteroaryl(C1-4)alkyl, aryl, or aryl(C1-4)alkyl, each of which may be optionally substituted or Z is S(O)n in which n is 0, 1 or 2 and R is C(1-8)alkyl, C(3-8)cycloalkyl, C(3-8)cycloalkylC(1-6)alkyl, aryl, aryl(C1-4)alkyl, heteroaryl, or heteroaryl(C1-4)alkyl, each of which may be optionally substituted are inhibitors of the enzyme Lp PLA2 and are of use in therapy, in particular treating atherosclerosis.
摘要翻译：式（I）的氮杂环丁酮化合物，其中：R 1和R 2可以相同或不同，各自选自氢，卤素或C（1-8）烷基; R 4和R 5可以相同或不同，各自选自氢，C（1-6）烷基，C（2-6）烯基，芳基，芳基（C1-4）烷基和杂芳基（ C 1-4）烷基，其各自可以是任选取代的，或者R 4和R 5可以连接在一起形成其余的（C 3-7）环烷基环; X是连接基团; Y是任选取代的芳基; Z是氧，R 3是C（1-8）烷基，C（3-8）环烷基，C（3-8）环烷基C（1-6）烷基，杂芳基，杂芳基（C 1-4）烷基，芳基或芳基（C 1-4）烷基，其各自可以任选被取代，或Z是S（O）n，其中n是0,1或2，R 3是C（1-8）烷基，C（ 3-8）环烷基，C（3-8）环烷基C（1-6）烷基，芳基，芳基（C1-4）烷基，杂芳基或杂芳基（C1-4）烷基，其各自可以任选被取代为抑制剂的酶Lp PLA2，并且可用于治疗，特别是治疗动脉粥样硬化。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式