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公开(公告)号：US20100173934A1
公开(公告)日：2010-07-08
申请号：US12294667
申请日：2007-04-04
申请人： Gregory P. Burke , Ronald R. Linnartz , Paul M. J. McSheehy , Richard W. Versace , Markus Wartmann
发明人： Gregory P. Burke , Ronald R. Linnartz , Paul M. J. McSheehy , Richard W. Versace , Markus Wartmann
IPC分类号： A61K31/437 , A61K31/427 , A61P35/00
CPC分类号： A61K31/425 , A61K45/06 , A61K2300/00
摘要： The invention relates to a combination comprising a microtubule active agent; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.
摘要翻译： 本发明涉及包含微管活性剂的组合; 和一种或多种药物活性剂; 包含所述组合的药物组合物; 包括所述组合的治疗方法; 制作所述组合的方法; 以及包括所述组合的商业包装。
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2.发明授权Certain substituted phenoxy-methyl phenyl-methoxy benzenes having antiviral activity 失效某些具有抗病毒活性的取代的苯氧基 - 甲基苯基 - 甲氧基苯
公开(公告)号：US5350772A
公开(公告)日：1994-09-27
申请号：US39532
申请日：1993-03-26
IPC分类号： A61K31/085 , A61K31/09 , A61K31/185 , A61K31/235 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/42 , A61K31/421 , A61P31/00 , C07C43/205 , C07C43/225 , C07C43/23 , C07C69/92 , C07C205/38 , C07C233/25 , C07C255/54 , C07C317/22 , C07C323/19 , C07D213/30 , C07D213/65 , C07D263/12 , C07D263/14 , C07D307/12 , C07D307/28 , C07D307/42 , C07D333/16 , C07C43/220
CPC分类号： C07D213/30 , C07C43/225 , C07C43/23 , C07C69/92 , C07D263/14 , C07D307/12 , C07D307/28 , C07D307/42 , C07D333/16
摘要： A compound represented by formula IAr.sub.1 --O--M--O--Ar.sub.2 Iwherein Ar.sub.1 and Ar.sub.2 are independently substituted phenyl or substituted pyridinyl, the substituents on said phenyl or pyridinyl being independently selected from one, two or three of (C.sub.1 -C.sub.10) alkyl, (C.sub.1 -C.sub.10) alkoxy, halogen, carbamyl, (C.sub.1 -C.sub.10) alkoxycarbonyl, oxazoyl, and (C.sub.1 -C.sub.10) alkyl substituted by halogen, (C.sub.1 -C.sub.10) alkoxy, hydroxy, or (C.sub.1 -C.sub.10) alkoxycarbonyl; M is ##STR1## (C.sub.4 -C.sub.8) alkylene, (C.sub.4 -C.sub.8) alkenylene or (C.sub.4 -C.sub.8)-alkynylene;O is oxygen;or pharmaceutically acceptable salts thereof.as well as pharmaceutical compositions containing the compounds and methods of treating or preventing viral infections, especially picornaviral infections, are disclosed.
摘要翻译： 由式I Ar1-OMO-Ar2I表示的化合物，其中Ar1和Ar2独立地是取代的苯基或取代的吡啶基，所述苯基或吡啶基上的取代基独立地选自（C1-C10）烷基，（C1-C10）烷基中的一个，两个或三个 （C1-C10）烷氧基，羟基或（C1-C10）烷氧基羰基取代的（C1-C10）烷氧基，（C1-C10）烷氧基羰基，恶唑基， M是（C4-C8）亚烷基，（C4-C8）亚烯基或（C4-C8） - 亚炔基; O是氧; 或其药学上可接受的盐。 以及含有化合物的药物组合物和治疗或预防病毒感染，特别是小RNA病毒感染的方法。
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公开(公告)号：US4814442A
公开(公告)日：1989-03-21
申请号：US757047
申请日：1985-07-19
IPC分类号： C07D499/897 , A61K31/43 , A61P31/04 , C07D205/09 , C07D499/86 , C07D499/87 , C07D499/88 , C07F7/18 , C07D499/00 , A61K31/425
CPC分类号： C07F7/186 , C07D205/09 , C07D499/88
摘要： Processes for the production of 6-hydroxyethyl-2-substituted thio penem-3-carboxylates are disclosed as well as novel penems.
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公开(公告)号：US4443373A
公开(公告)日：1984-04-17
申请号：US363710
申请日：1982-03-30
IPC分类号： C07D499/06 , C07D499/88 , C07F7/08 , C07D499/04 , C07D499/00
CPC分类号： C07D499/88 , C07F7/0812 , Y02P20/55
摘要： There is disclosed a process for preparing 6-hydroxyethyl-2-alkylthio penem-3-carboxylates by a multi-step process comprising reacting an azetidinone having a protected hydroxy group at the 5 position with a diester of ketomalonic acid, chlorinating the resulting N-substituted azetidinone, removing the chlorine and OH protecting group, reacting the resulting compound with a silver salt to form a silver thio substituted at the 4 position of the azetidinone, cyclizing with a thiocarbonyl compound, then reacting the resulting penam with a fluoride to form a penam-penem tautomer, reacting the tautomer with a halide or ethylenically unsaturated compound followed by deprotecting the carboxyl at the 3 position to form the final penem product in high yield.
摘要翻译： 公开了通过多步法制备6-羟乙基-2-烷硫基半胱胺-3-羧酸盐的方法，包括使5位具有被保护的羟基的氮杂环丁酮与酮缩醇酸的二酯反应，氯化得到的N- 取代的氮杂环丁酮，除去氯和OH保护基团，使所得化合物与银盐反应，形成在氮杂环丁酮的4位被取代的硫代硫酸酯，用硫代羰基化合物环化，然后使所得的penam与氟化物反应形成 双氯吡啶互变异构体，使互变异构体与卤化物或烯属不饱和化合物反应，然后在3位上脱羧保护羧基，以高产率形成最终的penem产物。
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公开(公告)号：US4851423A
公开(公告)日：1989-07-25
申请号：US940125
申请日：1986-12-10
IPC分类号： C07D249/08 , A61K31/075 , A61K31/095 , A61K31/12 , A61K31/15 , A61K31/165 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/435 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/443 , A61K31/496 , A61K31/505 , A61K31/52 , A61P7/02 , A61P29/00 , A61P31/12 , C07C45/00 , C07C49/00 , C07C67/00 , C07C313/00 , C07C317/24 , C07C317/26 , C07C317/44 , C07C323/12 , C07C323/20 , C07C323/22 , C07C323/25 , C07C323/36 , C07C323/41 , C07C323/47 , C07C323/65 , C07D213/30 , C07D213/69 , C07D213/70 , C07D233/54 , C07D233/56 , C07D233/58 , C07D233/60 , C07D233/61 , C07D233/64 , C07D233/84 , C07D233/90 , C07D233/91 , C07D233/94 , C07D235/06 , C07D235/12 , C07D235/26 , C07D235/28 , C07D239/54 , C07D257/04 , C07D257/06 , C07D263/32 , C07D277/24 , C07D277/36 , C07D295/08 , C07D295/092 , C07D307/20 , C07D405/04 , C07D405/06 , C07D413/06 , C07D413/12 , C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04 , C07D493/04 , C07D521/00
CPC分类号： C07D213/30 , C07D213/69 , C07D213/70 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/90 , C07D233/94 , C07D235/06 , C07D235/26 , C07D235/28 , C07D239/54 , C07D249/08 , C07D257/04 , C07D257/06 , C07D277/36 , C07D295/088 , C07D307/20 , C07D405/06 , C07D413/06 , C07D413/12 , C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04 , C07D493/04
摘要： The disclosed invention is compounds represented by the formulaZ--X--Q--Y--W, IZ--X--Q--Y--W'--Y--Q--X--Z IIand pharmaceutically acceptable acid addition salts and quarternary amine salts thereof, whereinZ is phenyl, naphthyl or adamantyl; substituted phenyl wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, methylsulfonyl, isoxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, loweralkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl; 5 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen and one carbon in the ring, wherein the substituents are one or more of carboxyl, hydroxymethyl, loweralkyl, loweralkylcarbonyl or aryl lower alkyl; or tertiary butyl;X and Y are each independently a bond, -O-, ##STR1## Q is a divalent substituted or unsubstituted straight or branched chain lower alkanediyl, -lower alkanedinyl- cycloalkanediyl- lower alkanediyl-, lower alkendiyl, lower alkynediyl, phenylene, tetrahydrofurandiyl or tetrahydropyrandiyl;W is a monovalent substituted or unsubstituted aromatic heterocyclic single or fused ring containing from 5 to 10 ring atoms, at least one hetero atom of which is a nitrogen atom, wherein the substituents are hydroxy, amino, carbamoyl, carboxyl, nitrile, nitro, oxo, lower alkoxy carbonyl, halogen, sulfamyl, lower alkyl, lower alkylthio, lower alkoxy, hydroxyloweralkyl, lower alkoxycarbonylloweralkyl, amino loweralkyl, carboxyloweralkyl, guanidino, thioureido, lower alkylsulfonylamino, aminocarbonylloweralkyl, allyloxycarbonylmethyl or carbamoyloxylowralkyl; andW' is divalent W.The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.
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公开(公告)号：US4559333A
公开(公告)日：1985-12-17
申请号：US585314
申请日：1984-03-01
IPC分类号： C07D205/09 , C07D499/88 , C07F7/18 , C07D499/00 , A61K31/425
CPC分类号： C07D205/09 , C07D499/88 , C07F7/1804
摘要： There is disclosed 2-(hydrazonoalkylthio)penems and their pharmaceutically acceptable salts and esters and their use as antibacterials.
摘要翻译： 公开了2-（亚肼基烷硫基）penem及其药学上可接受的盐和酯及其作为抗菌剂的用途。
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公开(公告)号：US4503064A
公开(公告)日：1985-03-05
申请号：US576499
申请日：1984-02-02
IPC分类号： C07D205/09 , C07D233/54 , C07D409/12 , C07D499/88 , C07F7/08 , C07F7/18 , C07D499/00 , A61K31/425
CPC分类号： C07D233/64 , C07D205/09 , C07D409/12 , C07D499/88 , C07F7/0812 , C07F7/0818 , C07F7/1804
摘要： There is disclosed 2-(oximinoalkylthio)penems and their pharmaceutically acceptable salts and esters and their use as antibacterials.
摘要翻译： 公开了2-（肟基烷硫基）penem及其药学上可接受的盐和酯及其作为抗菌剂的用途。
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8.发明授权5R,6S,8R-2-(1-Methyl-2-imidazolylmethy lthio)-6-(1-hydroxyethyl)penem-3-carboxylic acid 失效5R，6S，8R-2-（1-甲基-2-咪唑基甲硫基）-6-（1-羟乙基）青霉烯-3-羧酸
公开(公告)号：US4435412A
公开(公告)日：1984-03-06
申请号：US458511
申请日：1983-01-17
IPC分类号： C07D205/09 , C07D233/54 , C07D409/12 , C07D499/88 , C07F7/08 , C07F7/18 , C07D501/36 , A61K31/425
CPC分类号： C07D233/64 , C07D205/09 , C07D409/12 , C07D499/88 , C07F7/0812 , C07F7/0818 , C07F7/1804 , Y02P20/55
摘要： There is disclosed the antibacterial 5R,6S,8R-2-(1-methyl-2-imidazolylmethylthio)-6-(1-hydroxyethyl)penem-3-carboxylic acid, its pharmaceutically acceptable salts and esters as well as compositions containing them and methods for their use.
摘要翻译： 公开了抗菌5R，6S，8R-2-（1-甲基-2-咪唑基甲硫基）-6-（1-羟乙基）青霉烯-3-羧酸，其药学上可接受的盐和酯以及含有它们的组合物， 使用方法
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公开(公告)号：US5449782A
公开(公告)日：1995-09-12
申请号：US287325
申请日：1994-08-08
IPC分类号： A61K31/085 , A61K31/09 , A61K31/185 , A61K31/235 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/42 , A61K31/421 , A61P31/00 , C07C43/205 , C07C43/225 , C07C43/23 , C07C69/92 , C07C205/38 , C07C233/25 , C07C255/54 , C07C317/22 , C07C323/19 , C07D213/30 , C07D213/65 , C07D263/12 , C07D263/14 , C07D307/12 , C07D307/28 , C07D307/42 , C07D333/16 , C07D213/55 , C07D213/56 , C07D493/04
CPC分类号： C07D213/30 , C07C43/225 , C07C43/23 , C07C69/92 , C07D263/14 , C07D307/12 , C07D307/28 , C07D307/42 , C07D333/16
摘要： A compound represented by formula IAr.sub.1 --O--M--O--AR.sub.2 Iwherein Ar.sub.1 and Ar.sub.2 are independently substituted phenyl or substituted pyridinyl, the substituents on said phenyl or pyridinyl being independently selected from one, two or three of (C.sub.1 -C.sub.10)alkyl, (C.sub.1 -C.sub.10) alkoxy, halogen, carbamyl, (C.sub.1 -C.sub.10) alkoxycarbonyl, oxazoyl, and (C.sub.1 -C.sub.10) alkyl substituted by halogen, (C.sub.1 -C.sub.10) alkoxy, hydroxy, or (C.sub.1 -C.sub.10) alkoxycarbonyl; ##STR1## M is (C.sub.4 -C.sub.8) alkylene, (C.sub.4 -C.sub.8) alkenylene or (C.sub.4 -C.sub.8)-alkynylene;O is oxygen;or pharmaceutically acceptable salts thereof.as well as pharmaceutical compositions containing the compounds and methods of treating or preventing viral infections, especially picornaviral infections, are disclosed.
摘要翻译： 由式I Ar1-OMO-AR2I表示的化合物，其中Ar1和Ar2独立地为取代的苯基或取代的吡啶基，所述苯基或吡啶基上的取代基独立地选自（C1-C10）烷基，（C1- （C1-C10）烷氧基，羟基或（C1-C10）烷氧基羰基取代的（C1-C10）烷氧基，（C1-C10）烷氧基羰基，恶唑基， M是（C 4 -C 8）亚烷基，（C 4 -C 8）亚烯基或（C 4 -C 8） - 亚炔基; O是氧; 或其药学上可接受的盐。 以及含有化合物的药物组合物和治疗或预防病毒感染，特别是小RNA病毒感染的方法。
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公开(公告)号：US4690922A
公开(公告)日：1987-09-01
申请号：US626820
申请日：1984-07-02
IPC分类号： C07D499/897 , A61K31/43 , A61P31/04 , C07D499/88 , C07D521/00 , C07D499/00 , A61K31/425
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D499/88
摘要： This invention relates to 2-(heterocycloalkylthio)penems wherein the nitrogen of the heterocyclic ring is connected to the alkyl group, and to their use as antibacterial agents.
摘要翻译： 本发明涉及2-（杂环烷硫基）青霉烯，其中杂环的氮与烷基连接，并用作抗菌剂。
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