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1. 发明申请

US20100137243A1 Oxazolidinone And/Or Isoxazoline As Antibacterial Agents 审中-公开
标题翻译：恶唑烷酮和/或异恶唑啉作为抗菌剂
公开(公告)号：US20100137243A1
公开(公告)日：2010-06-03
申请号：US12128135
申请日：2008-05-28
申请人： Michael Barry Gravestock , Neil James Hales , Michael Lingrad Swaim , Sheila Irene Hauck , Stuart Dennett Mills
发明人： Michael Barry Gravestock , Neil James Hales , Michael Lingrad Swaim , Sheila Irene Hauck , Stuart Dennett Mills
IPC分类号： A61K31/695 , A61K31/4439 , C07D413/14 , A61K31/422 , C07F9/06 , A61K31/675 , C07F7/02
CPC分类号： C07D263/20 , C07D413/10 , C07D413/14
摘要： Compounds of Formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, and compounds as shown in Formula (I) wherein C is for example (D), (E), (F); wherein A and B are independently selected from (i) and (ii); R2a to R3b are independently selected from hydrogen and fluorine; R1a and R1b are independently selected from, for example, hydroxy, —NHC(═W)R4, (a) and (b); wherein W is O or S; R4 is, for example, hydrogen, amino, (1-4C)alkyl; HET-1 is, for example, a C-linked 5-membered heteroaryl ring; HET-2 is, for example, an N-linked 5-membered, fully or partially unsaturated heterocyclic ring; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
摘要翻译：式（I）化合物或其药学上可接受的盐或其体内可水解的酯，以及其中C为（D），（E），（F）的式（I）所示的化合物。其中A和B独立地选自（i）和（ii）; R2a至R3b独立地选自氢和氟; R1a和R1b独立地选自例如羟基，-NHC（= W）R4，（a）和（b）; 其中W是O或S; R4是例如氢，氨基，（1-4C）烷基; HET-1是例如C连接的5元杂芳基环; HET-2是例如N-连接的5元全部或部分不饱和杂环; 作为抗菌剂是有用的; 并描述了其制造方法和含有它们的药物组合物。

2. 发明授权

US07396847B2 Oxazolidinone and/or isoxazoline as antibacterial agents 失效
标题翻译：恶唑烷酮和/或异恶唑啉作为抗菌剂
公开(公告)号：US07396847B2
公开(公告)日：2008-07-08
申请号：US10489266
申请日：2002-09-09
申请人： Michael Barry Gravestock , Neil James Hales , Michael Lingard Swain , Sheila Irene Hauck , Stuart Dennett Mills
发明人： Michael Barry Gravestock , Neil James Hales , Michael Lingard Swain , Sheila Irene Hauck , Stuart Dennett Mills
IPC分类号： A61K31/42 , C07D263/02 , C07D263/00 , C07D261/02
CPC分类号： C07D263/20 , C07D413/10 , C07D413/14
摘要： Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, and compounds as shown in (I) wherein C is for example wherein A and B are independently selected from R2a to R3b are independently selected from hydrogen and fluorine; R1a and R1b are independently selected from, for example, hydroxy, —NHC(═W)R4, wherein W is O or S; R4 is, for example, hydrogen, amino, (1-4C)alkyl; HET-1 is, for example, a C-linked 5-membered heteroaryl ring; HET-2 is, for example, an N-linked 5-membered, fully or partially unsaturated heterocyclic ring; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
摘要翻译：式（I）化合物或其药学上可接受的盐或其体内可水解的酯，和（I）所示的化合物，其中C为例如其中A和B独立地选自R 1， 2 a至R 3 b独立地选自氢和氟; R 1 a和R 1 b独立地选自，例如羟基，-NHC（-W）R 4，其中W是 O或S; R 4是例如氢，氨基，（1-4C）烷基; HET-1是例如C连接的5元杂芳基环; HET-2是例如N-连接的5元全部或部分不饱和杂环; 作为抗菌剂是有用的; 并描述了其制造方法和含有它们的药物组合物。

3. 发明授权

US06362191B1 Aminometyl oxooxazolidinyl benzene derivatives 失效
标题翻译：氨基甲基氧代恶唑烷基苯衍生物
公开(公告)号：US06362191B1
公开(公告)日：2002-03-26
申请号：US09485972
申请日：2000-02-18
申请人： Stuart Dennett Mills
发明人： Stuart Dennett Mills
IPC分类号： C07D41110
CPC分类号： C07D413/06 , C07D417/06 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The invention concerns compounds of formula (I), wherein: A is a 5 membered heteroaryl ring, a bicyclic benzo system containing such a 5 membered heteroaryl ring or a bicyclic or tricyclic heteroaryl ring system with at least one bridgehead nitrogen and optionally a further 1-3 heteroatoms chosen from oxygen, sulfur and nitrogen; R1 is, for example, hydroxy, halo, amino, nitro, cyano, carboxy, thiol, C1-4alkanoyloxy, C1-4alkoxycarbonyl, dimethylaminomethyleneaminocarbonyl, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, optionally substituted phenyl, an optionally substituted 5- or 6-membered heteroaryl ring or hydroxyC1-4alkyl; n is 0-6; R2 and R3 are independently hydrogen or fluoro; R4 is, for example, C1-4alkyl; pharmaceutically acceptable salts and in vivo hydrolysable ester thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.
摘要翻译：本发明涉及式（I）化合物，其中：A是5元杂芳基环，含有这种5元杂芳基环的双环苯并系统或具有至少一个桥头烷氮和任选另外1个的桥头烷氮的双环或三环杂芳基环系统 3个选自氧，硫和氮的杂原子; R 1是例如羟基，卤素，氨基，硝基，氰基，羧基，硫醇，C 1-4烷酰氧基，C 1-4烷氧基羰基，二甲基氨基亚甲基氨基羰基，C 1-4烷基，C 2-4链烯基，C 2 4-炔基，C 1-4烷氧基，任选取代的苯基，任选取代的5或6元杂芳基环或羟基C 1-4烷基; n为0-6; R 2和R 3独立地为氢或氟; R 4为例如C 1〜 4个烷基; 其药学上可接受的盐和体内可水解的酯; 其准备过程; 含有它们的药物组合物及其作为抗菌剂的用途。

4. 发明授权

US5728701A Heterocyclic derivatives 失效
标题翻译：杂环衍生物
公开(公告)号：US5728701A
公开(公告)日：1998-03-17
申请号：US820003
申请日：1997-03-18
申请人： Michael Garth Wayne , Michael James Smithers , John Wall Rayner , Alan Wellington Faull , Robert James Pearce , Andrew George Brewster , Richard Eden Shute , Stuart Dennett Mills , Peter William Rodney Caulkett
发明人： Michael Garth Wayne , Michael James Smithers , John Wall Rayner , Alan Wellington Faull , Robert James Pearce , Andrew George Brewster , Richard Eden Shute , Stuart Dennett Mills , Peter William Rodney Caulkett
IPC分类号： C07D213/74 , A61K31/495 , C07D401/04
CPC分类号： C07D213/74
摘要： Compounds of formula I ##STR1## and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.13, M.sup.2, X.sup.1, Z.sup.1, Z.sup.1a, X.sup.2 and A.sup.1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Novel intermediates are also disclosed.
摘要翻译：式I的化合物（I）及其代谢不稳定的酯和酰胺及其药学上可接受的盐，其中R13，M2，X1，Z1，Z1a，X2和A1具有说明书中给出的含义。该化合物可用作纤维蛋白原与糖蛋白IIb / IIIa结合的抑制剂。还公开了新的中间体。

5. 发明授权

US5654298A Amine derivatives 失效
标题翻译：胺衍生物
公开(公告)号：US5654298A
公开(公告)日：1997-08-05
申请号：US685944
申请日：1991-04-16
申请人： Stuart Dennett Mills , Rodney Brian Hargreaves , Bernard Joseph McLoughlin
发明人： Stuart Dennett Mills , Rodney Brian Hargreaves , Bernard Joseph McLoughlin
IPC分类号： A61K31/44 , A61K31/4409 , A61K31/4412 , A61K31/4418 , A61K31/4425 , A61K31/4439 , A61P9/00 , A61P9/06 , C07D213/74 , C07D215/44 , C07D401/04 , C07D471/04 , A01N43/62 , A01N43/40 , C07D211/68 , C07D211/92
CPC分类号： C07D213/74 , C07D215/44 , C07D401/04 , C07D471/04
摘要： This invention concerns novel aminopyridinium compounds of the formula I wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are selected from the following combinations: ##STR1## (a) one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino, or is alkyl, alkenyl, alkoxyalkyl, alkoxy, alkylthio, phenyl, phenylalkyl, cycloalkyl or cycloalkylalkyl; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl or one of the above defined basic groups;R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl, cycloalkylalkyl; and R.sup.3 and R.sup.5 are independently hydrogen, alkyl or alkenyl;(b) R.sup.2 is a basic group as defined above, R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyridine ring, complete a benzene ring; has any of the meanings defined in(a) above; and R.sup.3 is hydrogen, alkyl or alkenyl; and(c) R2 has any of the meanings defined above and R.sup.6 is a group of the formula --NR.sup.7.A-- in which A together with R.sup.1 forms an ethylene, trimethylene or tetramethylene link and R.sup.7 is hydrogen or alkyl; andR.sup.3 and R.sup.5 have, independently, any of the meanings defined in (a) above; and wherein R.sup.4 is hydrogen, cycloalkylalkyl, alkyl, alkenyl, alkynyl or phenylalkyl; and Q is phenyl; or the group Q.N(R.sup.4)-- together constitutes an azaheterocyclic moietyo; Y is a physiologically acceptable anion; and any one or more of said phenyl or benzene moieties may optionally be unsubstituted or bear one or more selected substituents.The invention also includes certain closely related anhydro-base derivatives which, like the formula I compounds, possess beneficial effects on the cardiovascular system. Also included are pharmaceutical compositions and processes for the manufacture of the various novel compounds.
摘要翻译：本发明涉及式I的新型氨基吡啶鎓化合物，其中R 1，R 2，R 3，R 5和R 6选自以下组合：选自氨基，烷基氨基，至多8个碳原子的二烷基氨基，吡咯烷子基，哌啶子基和吗啉代，或烷基，烯基，烷氧基烷基，烷氧基，烷硫基，苯基，苯基烷基，环烷基或环烷基烷基; R2和R6中的另一个是氢，烷基或上述定义的基团之一; R1是烷基，烯基，环烷基，苯基，苯基烷基，环烷基烷基; 并且R 3和R 5独立地是氢，烷基或链烯基; （b）R2是如上定义的碱性基团，R5和R6一起形成亚烷基，或与吡啶环的上述碳原子一起形成苯环; 具有上述（a）中定义的任何含义; 并且R 3是氢，烷基或烯基; 和（c）R 2具有上述定义的任何含义，R 6是式-NR 7 A的基团，其中A与R 1一起形成乙烯，三亚甲基或四亚甲基，R 7为氢或烷基; 和R3和R5独立地具有上述（a）中定义的任何含义; 并且其中R4是氢，环烷基烷基，烷基，烯基，炔基或苯基烷基; Q为苯基; 或基团Q.N（R4） - 一起构成氮杂环基; Y是生理上可接受的阴离子; 并且所述苯基或苯部分中的任何一个或多个可以任选地是未取代的或承载一个或多个选定的取代基。本发明还包括某些密切相关的脱氢基衍生物，其如式I化合物对心血管系统具有有益作用。还包括用于制备各种新型化合物的药物组合物和方法。

6. 发明授权

US5753659A Heterocyclic compouds 失效
标题翻译：杂环化合物
公开(公告)号：US5753659A
公开(公告)日：1998-05-19
申请号：US458180
申请日：1995-06-02
申请人： Stuart Dennett Mills
发明人： Stuart Dennett Mills
IPC分类号： C07D213/74 , A61K31/495
CPC分类号： C07D213/74
摘要： A compound of the general formula (M.sup.1).sub.n --Q--(M.sup.2).sub.1-n --L--A I wherein: n is 0 or 1; M.sup.1 is an amino group; Q is an aromatic heterocyclic group containing a basic nitrogen atom; M.sup.2 is an imino group; L is a template group; and A is an acidic group, or an ester or amide derivative thereof, or a sulphonamide group; and pharmaceutically acceptable salts and pro-drugs thereof, for use in the treatment of a disease in which platelet aggregation mediated by the binding of adhesion molecules to GPIIb-IIIa is involved. Novel compounds are also disclosed.
摘要翻译：通式（M1）n-Q-（M2）1-n-L-A的化合物，其中n为0或1; M1是氨基; Q是含有碱性氮原子的芳香族杂环基; M2是亚氨基; L是模板组; A是酸性基团，或其酯或酰胺衍生物或磺酰胺基团; 和其药学上可接受的盐和前药，用于治疗由粘附分子与GPIIb-IIIa的结合介导的血小板聚集的疾病。还公开了新的化合物。

7. 发明授权

US5652242A Heterocyclic derivatives 失效
标题翻译：杂环衍生物
公开(公告)号：US5652242A
公开(公告)日：1997-07-29
申请号：US457538
申请日：1995-06-01
申请人： Michael Garth Wayne , Michael James Smithers , John Wall Rayner , Alan Wellington Faull , Robert James Pearce , Andrew George Brewster , Richard Eden Shute , Stuart Dennett Mills , Peter William Rodney Caulkett
发明人： Michael Garth Wayne , Michael James Smithers , John Wall Rayner , Alan Wellington Faull , Robert James Pearce , Andrew George Brewster , Richard Eden Shute , Stuart Dennett Mills , Peter William Rodney Caulkett
IPC分类号： C07D213/74 , A61K31/495 , C07D401/04
CPC分类号： C07D213/74
摘要： Compounds of formula I ##STR1## and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.13, M.sup.2, X.sup.1, Z.sup.1, Z.sup.1a, X.sup.2 and A.sup.1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Novel intermediates are also disclosed.
摘要翻译：式I的化合物（I）及其代谢不稳定的酯和酰胺及其药学上可接受的盐，其中R13，M2，X1，Z1，Z1a，X2和A1具有说明书中给出的含义。该化合物可用作纤维蛋白原与糖蛋白IIb / IIIa结合的抑制剂。还公开了新的中间体。

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