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2. 发明公开

EP0274867A2 Pharmaceutically active compounds 失效
标题翻译： Pharmazutische aktive Verbindungen。
公开(公告)号：EP0274867A2
公开(公告)日：1988-07-20
申请号：EP87310807.0
申请日：1987-12-09
申请人： SCHERING CORPORATION
发明人： Girijavallabhan, Viyyoor Moopil , Pinto, Patrick Anthony , Ganguly, Ashit Kumar , Versace, Richard William
IPC分类号： C07D233/60 , A61K31/415 , C07D277/36 , C07D257/04 , C07D213/70 , C07D257/06 , C07D213/30 , C07D239/54 , C07D233/70 , C07D233/94 , C07D235/06
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 formula
and pharmaceutically acceptable acid addition, basic addition and quarternary amine salts thereof and pharmaceutically acceptable solvates thereof, wherein
each Z is independently tetiary butyl, phenyl, naphthyl or adamantyl; substituted phenyl, wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile. nitro, phenyslsulfonyl, loweralkylsulfonyl, oxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, lower alkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl; 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining members of the ring being at least one carbon, and optionally sulfur or oxygen, wherein the substituents are one or more of carboxyl, hydroxymethyl, lower alkyl, loweralkylcarbonyl or aryl lower alkyl;

X and Y are each independently a bond, -0-,
each Q is independently a divalent substituted or unsubstituted, straigh or branched chain lower alkanediyl, lower alkanediyl-cycloalkaneidyl-lower alkanediyl, lower alkenediyl, lower alkynediyl, phenylene, dihydrofurandiyl, tetrahydrofurandiyl, tetrahydropyrandiyl, or, loweralkanediyl-tetrahydrofurandiyl-loweralkanediyl, wherein the substituents are one or more of hydroxy, epoxy, fluorine, chlorine, azide, or amino; W is a monovalent substituted or unsubstituted aryl group or a heterocyclic single or fused ring containing from 4 to 10 ring atoms, at least one hetero atom of which is a nitrogen atom and the remaining ring atoms being at least one carbon and optionally sulfur or oxygen, wherein the substituents are one or more of hydroxy, oxo amino, carbamoyl, carboxyl, nitrile, nitro, lower alkoxy carbonyl, halogen, sulfamyl, lower alkyl, lower alkylthio, lower alkoxy, hydroxyloweralkyl, lower alkoxycarbonylloweralkyl, amino loweralkyl, carboxyloweralkyl, guanidino, thioureido, lower alkylsulfonylamino, aminocarbonylloweralkyl, allyloxycarbonylmethyl or carbamoyloxyloweralkyl; with the proviso that W cannot be substituted or unsubstituted isoxazolyl, and
W' is divalent W.

The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.
摘要翻译：所公开的发明是由式表示的化合物及其药学上可接受的酸加成，碱加成和季胺盐及其药学上可接受的溶剂化物，其中每个Z独立地为丁基，苯基，萘基或金刚烷基; 取代的苯基，其中取代基是卤素，低级烷氧基，苯氧基，腈，硝基，苯基磺酰基，低级烷基磺酰基，恶唑-2-基，低级烷酰基，苯甲酰基，低级烷氧基羰基，低级烷基，低级烷硫基，苯基，苯基氨基硫代羰基，或低级烷基氨基硫代羰基; 含有至少一个氮的4或6元未取代或取代的杂环，其余的成员为至少一个碳，以及任选的硫或氧，其中取代基是羧基，羟甲基，低级烷基，低级烷基羰基或芳基低级烷基; X和Y各自独立地为键，-O-，各Q独立地为二价取代或未取代的，直链或支链的低级烷二基，低级烷二基 - 环烷烃基 - 低级烷二基，低级烯二基，低级炔二基，亚苯基，二氢呋喃二基，四氢呋喃基，四氢吡喃基或低级烷二基 - 四氢呋喃二基 - 低级烷二基，其中取代基是羟基，环氧基，氟，氯，叠氮化物或氨基中的一个或多个; W是单价取代或未取代的芳基或含有4至10个环原子的杂环单或稠环，其至少一个杂原子是氮原子，剩余的环原子是至少一个碳和任选的硫或氧其中取代基是羟基，氧代氨基，氨基甲酰基，羧基，腈，硝基，低级烷氧基羰基，卤素，氨基磺酰基，低级烷基，低级烷硫基，低级烷氧基，羟基低级烷基，低级烷氧羰基低级烷基，氨基低级烷基，羧基低级烷基，胍基，硫脲基，低级烷基磺酰基氨基，氨基羰基低级烷基，烯丙氧基羰基甲基或氨基甲酰氧基低级烷基; 条件是W不能是取代或未取代的异恶唑基，W'是二价的W.该化合物具有抗病毒活性，抗炎活性，是PAF抑制剂。

3. 发明公开

EP0345827A1 Process for the production of penem compounds 失效
标题翻译： Verfahren zur Herstellung von Penem-Verbindungen。
公开(公告)号：EP0345827A1
公开(公告)日：1989-12-13
申请号：EP89113483.5
申请日：1983-11-21
申请人： SCHERING CORPORATION
发明人： Girijavallabhan, Viyyoor Moopil , Ganguly, Ashit Kumar , Pinto, Patrick Anthony , Versace, Richard William , McCombie, Stuart Walter
IPC分类号： C07D499/00 , A61K31/43
CPC分类号： C07D233/64 , C07D205/09 , C07D409/12 , C07D499/88 , C07F7/0812 , C07F7/0818 , C07F7/186 , Y02P20/55
摘要： Compounds of the general formula XII having valuable antibacterial activity
are provided in which G is 1-hydroxyethyl, Rg is chosen from the group

and
摘要翻译：提供具有有价值的抗菌活性的通式XII的化合物，其中G是1-羟乙基，R g选自 f

4. 发明公开

EP0123650A1 Penems, pharmaceutical compositions containing them, and process for their preparation 有权
标题翻译：青霉烯，含有它们的进程的药物组合物及其制备。
公开(公告)号：EP0123650A1
公开(公告)日：1984-10-31
申请号：EP84810146.5
申请日：1984-03-26
申请人： SCHERING CORPORATION
发明人： Giryavallabhan, Vyyoor Moopil , Ganguly, Ashit Kumar , Pinto, Patrick Anthony , Versace, Richard William
IPC分类号： C07D499/00 , A61K31/43
CPC分类号： C07D499/88
摘要： This invention relates to novel 6-(hydroxy- alkyl)-2-cyclo-aliphaticalkylthio) penems having the general formula:
wherein G is hydroxyloweralkyl,
wherein: R 1 , R 2 , R 3 , R 4 and X are various groups.
These compounds have antibacterial activity.

5. 发明授权

EP0110280B1 Process for the production of penem compounds 有权
标题翻译：一种制备青霉烯化合物的方法。
公开(公告)号：EP0110280B1
公开(公告)日：1994-10-12
申请号：EP83111615.7
申请日：1983-11-21
申请人： SCHERING CORPORATION
发明人： Girijavallabhan, Viyyoor Moopil , Ganguly, Ashit Kumar , Pinto, Patrick Anthony , Versace, Richard William , McCombie, Stuart Walter
IPC分类号： C07D499/04 , C07D205/08 , C07F7/08 , A61K31/43
CPC分类号： C07D233/64 , C07D205/09 , C07D409/12 , C07D499/88 , C07F7/0812 , C07F7/0818 , C07F7/186 , Y02P20/55

6. 发明授权

EP0146730B1 Process for the production of penems 有权
标题翻译：生产骨髓的方法
公开(公告)号：EP0146730B1
公开(公告)日：1990-07-11
申请号：EP84113163.4
申请日：1984-11-02
申请人： SCHERING CORPORATION
发明人： Girijavallabhan, Viyyoor Moopil , Ganguly, Ashit Kumar , Pinto, Patrick Anthony , Versace, Richard William
IPC分类号： C07D499/00
CPC分类号： C07D205/09 , C07D499/88 , C07F7/0818 , C07F7/186 , Y02P20/55

7. 发明授权

EP0080162B1 2-(Fluoroalkylthio)substituted penems, processes for preparing them, and pharmaceutical compositions containing them 有权
标题翻译： 2-（氟代烷基）取代基，制备它们的方法和含有它们的药物组合物
公开(公告)号：EP0080162B1
公开(公告)日：1986-07-09
申请号：EP82110612.7
申请日：1982-11-18
申请人： SCHERING CORPORATION
发明人： Girijavallabhan, Vivyoor Moopil , Mc Combie, Stuart Walter , Ganguly, Ashit Kumar , Pinto, Patrick Anthony , Versace, Richard William
IPC分类号： C07D499/00 , A61K31/43
CPC分类号： C07F7/186 , C07D205/09 , C07D499/88

8. 发明公开

EP0146730A1 Process for the production of penems 有权
标题翻译：一种制备青霉烯类过程。
公开(公告)号：EP0146730A1
公开(公告)日：1985-07-03
申请号：EP84113163.4
申请日：1984-11-02
申请人： SCHERING CORPORATION
发明人： Girijavallabhan, Viyyoor Moopil , Ganguly, Ashit Kumar , Pinto, Patrick Anthony , Versace, Richard William
IPC分类号： C07D499/00
CPC分类号： C07D205/09 , C07D499/88 , C07F7/0818 , C07F7/186 , Y02P20/55
摘要： Improved processes for the production of 6-hydroxyethyl-2-substituted thio penem-3-carboxylates which eliminate the step of using a silver reagent are disclosed.

9. 发明公开

EP0118875A1 6-(Hydroxyalkyl)-2-(heteroarylalkylthio)-penems, pharmaceutical compositions containing them, and processes for their preparation 有权
标题翻译： 6-（羟烷基）-2-（heteroarylalkylthio）-Peneme，含有它们的它们的制备方法的药物组合物。
公开(公告)号：EP0118875A1
公开(公告)日：1984-09-19
申请号：EP84102429.2
申请日：1984-03-07
申请人： SCHERING CORPORATION
发明人： Girijavallabhan, Viyyoor Moopil , Ganguly, Ashit Kumar , Pinto, Patrick Anthony , Versace, Richard William
IPC分类号： C07D499/00 , A61K31/43
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D499/88
摘要： Compounds of the general formula
In which G is hydroxyloweralkyl;

R 1 is chosen from various substituents;
n is 1 to 4;
Q is the group
in which X is =N- or
and R is chosen from various substituents; and their pharmaceutically acceptable salts and esters. Various processes for their preparation are disclosed. The compounds have antibacterial activity.
摘要翻译：通式其中G为hydroxyloweralkyl的化合物; [R <1>由各种取代基选择; n是1至4; Q为基团其中X是= N-或= @ - ，其中至少一个是= @ - ，并且R选自各种取代基选择; 及其药学上可接受的盐和酯。各种其制备方法是游离缺失盘。所述化合物具有抗菌活性。

10. 发明公开

EP0274867A3 Pharmaceutically active compounds 失效
标题翻译：药物活性化合物
公开(公告)号：EP0274867A3
公开(公告)日：1990-11-14
申请号：EP87310807.0
申请日：1987-12-09
申请人： SCHERING CORPORATION
发明人： Girijavallabhan, Viyyoor Moopil , Pinto, Patrick Anthony , Ganguly, Ashit Kumar , Versace, Richard William
IPC分类号： C07D233/60 , A61K31/415 , C07D277/36 , C07D257/04 , C07D213/70 , C07D257/06 , C07D213/30 , C07D239/54 , C07D233/70 , C07D233/94 , C07D235/06
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 formula
and pharmaceutically acceptable acid addition, basic addition and quarternary amine salts thereof and pharmaceutically acceptable solvates thereof, wherein
each Z is independently tetiary butyl, phenyl, naphthyl or adamantyl; substituted phenyl, wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile. nitro, phenyslsulfonyl, loweralkylsulfonyl, oxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, lower alkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl; 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining members of the ring being at least one carbon, and optionally sulfur or oxygen, wherein the substituents are one or more of carboxyl, hydroxymethyl, lower alkyl, loweralkylcarbonyl or aryl lower alkyl;
X and Y are each independently a bond, -0-,
each Q is independently a divalent substituted or unsubstituted, straigh or branched chain lower alkanediyl, lower alkanediyl-cycloalkaneidyl-lower alkanediyl, lower alkenediyl, lower alkynediyl, phenylene, dihydrofurandiyl, tetrahydrofurandiyl, tetrahydropyrandiyl, or, loweralkanediyl-tetrahydrofurandiyl-loweralkanediyl, wherein the substituents are one or more of hydroxy, epoxy, fluorine, chlorine, azide, or amino; W is a monovalent substituted or unsubstituted aryl group or a heterocyclic single or fused ring containing from 4 to 10 ring atoms, at least one hetero atom of which is a nitrogen atom and the remaining ring atoms being at least one carbon and optionally sulfur or oxygen, wherein the substituents are one or more of hydroxy, oxo amino, carbamoyl, carboxyl, nitrile, nitro, lower alkoxy carbonyl, halogen, sulfamyl, lower alkyl, lower alkylthio, lower alkoxy, hydroxyloweralkyl, lower alkoxycarbonylloweralkyl, amino loweralkyl, carboxyloweralkyl, guanidino, thioureido, lower alkylsulfonylamino, aminocarbonylloweralkyl, allyloxycarbonylmethyl or carbamoyloxyloweralkyl; with the proviso that W cannot be substituted or unsubstituted isoxazolyl, and W' is divalent W. The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.

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