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1. 发明授权

US07276611B2 Process for synthesizing beta-lactamase inhibitor intermediates 失效
标题翻译： β-内酰胺酶抑制剂中间体的合成方法
公开(公告)号：US07276611B2
公开(公告)日：2007-10-02
申请号：US10844243
申请日：2004-05-12
申请人： Michael William Winkley , Anita Wai-Yin Chan , Ivo L. Jirkovsky , Kenneth Alfred Martin Kremer , Joseph Zeldis , Antonia Aristotelevna Nikitenko , Henry Lee Strong , Tarek Mansour , Gulnaz Khafizova , Aranapakam M. Venkatesan
发明人： Michael William Winkley , Anita Wai-Yin Chan , Ivo L. Jirkovsky , Kenneth Alfred Martin Kremer , Joseph Zeldis , Antonia Aristotelevna Nikitenko , Henry Lee Strong , Tarek Mansour , Gulnaz Khafizova , Aranapakam M. Venkatesan
IPC分类号： C07D231/54
CPC分类号： C07D498/04 , C07D487/04
摘要： There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of β-lactamase inhibitors.
摘要翻译：提供了一种制备具有结构式I的双环杂芳基羧醛的方法，其中X和Y在说明书中定义。双环杂芳基羧醛可用作制备β-内酰胺酶抑制剂的中间体。

2. 发明授权

US4492697A 4H-Imidazo[2,3-c]pyrido[2,3-e][1,4]oxazine derivatives 失效
标题翻译： 4H-咪唑并[2,3-c]吡啶并[2,3-e] [1,4]恶嗪衍生物
公开(公告)号：US4492697A
公开(公告)日：1985-01-08
申请号：US523989
申请日：1983-08-16
申请人： Jean A. Gauthier , Ivo L. Jirkovsky
发明人： Jean A. Gauthier , Ivo L. Jirkovsky
IPC分类号： C07D498/04 , C07D498/14 , A61K31/535
CPC分类号： C07D498/04 , C07D498/14
摘要： The invention discloses novel 4H-imidazo[2,3-c]pyrido[2,3-e][1,4]oxazine derivatives, processes for their preparation, pharmaceutical compositions thereof and methods for using the compounds. The compounds of this invention are useful in the treatment of anaphylactic reactions and allergic conditions in a mammal.
摘要翻译：本发明公开了新颖的4H-咪唑并[2,3-c]吡啶并[2,3-e] [1,4]恶嗪衍生物，其制备方法，药物组合物和使用该化合物的方法。本发明的化合物可用于治疗哺乳动物的过敏反应和过敏状况。

3. 发明授权

US4355031A 2,3-Dihydro-3-[4-(substituted)-1-piperazinyl]-1H-isoindol-1-ones 失效
标题翻译： 2,3-二氢-3- [4-（取代的）-1-哌嗪基] -1H-异吲哚-1-酮
公开(公告)号：US4355031A
公开(公告)日：1982-10-19
申请号：US262717
申请日：1981-05-11
申请人： Christopher A. Demerson , Ivo L. Jirkovsky
发明人： Christopher A. Demerson , Ivo L. Jirkovsky
IPC分类号： C07D209/50 , C07D403/04 , A61K31/41 , C07D403/14
CPC分类号： C07D209/50
摘要： Pyrazinoisoindolone derivatives of the formula ##STR1## wherein R.sup.1 is lower alkyl, phenyl, diphenylmethyl, pyridinyl, pyrimidinyl, pyrazinyl or pyrazinyl substituted with a lower alkyl, lower alkoxy or halo; and R.sup.2 is hydrogen, lower alkyl or di(lower)alkylamino(lower)alkyl are useful as antihypertensive agents.
摘要翻译：苯基，二苯基甲基，吡啶基，嘧啶基，吡嗪基或被低级烷基，低级烷氧基或卤素取代的吡嗪基的吡唑并吲哚酮衍生物其中R 1是低级烷基，并且R 2是氢，低级烷基或二（低级）烷基氨基（低级）烷基可用作抗高血压剂。

4. 发明授权

US4105778A Fused .gamma.-pyrone-2-carboxylic acid derivatives and process therefor 失效
标题翻译：熔融{65-吡喃-2-羧酸衍生物及其方法
公开(公告)号：US4105778A
公开(公告)日：1978-08-08
申请号：US831448
申请日：1977-09-08
申请人： Adolph H. Philipp , Ivo L. Jirkovsky
发明人： Adolph H. Philipp , Ivo L. Jirkovsky
IPC分类号： C07D311/22 , C07D335/06 , C07D491/04 , C07D493/04 , C07D495/04 , A61K31/38
CPC分类号： C07D491/04 , C07D311/22 , C07D335/06 , C07D493/04 , C07D495/04
摘要： Compounds of formula 1 ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different selected from the group consisting of hydrogen, halogen, nitro, trifluoromethyl, lower alkyl and lower alkoxy, or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4 together form a CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 chain and R.sup.3 and R.sup.4, R.sup.1 and R.sup.4 and R.sup.1 and R.sup.2, respectively, are as defined above, R.sup.5 is hydrogen, lower alkyl or a radical of formula --Alk--OR.sup.6 wherein Alk is an alkylene selected from the group consisting of CR.sup.7 R.sup.8, CR.sup.7 R.sup.8 CR.sup.9 R.sup.10, CR.sup.7 R.sup.8 CR.sup.9 R.sup.10 CR.sup.11 R.sup.12 and CR.sup.7 R.sup.8 CR.sup.9 R.sup.10 CR.sup.11 R.sup.12 CR.sup.13 R.sup.14 wherein each of R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is hydrogen or lower alkyl and R.sup.6 is hydrogen or lower alkyl; R.sup.15 is hydrogen or lower alkyl; X is O, S, SO or SO.sub.2 ; Y is O or NR.sup.16 wherein R.sup.16 is hydrogen or lower alkyl, are disclosed. The compounds of formula 1 are useful for treating allergic conditions and for treating microbial infections. Methods for the preparation and use of said compounds are disclosed.
摘要翻译：其中R 1，R 2，R 3和R 4相同或不同，选自氢，卤素，硝基，三氟甲基，低级烷基和低级烷氧基，或R 1和R 2，R 2和R 3的式I化合物或R3和R4一起形成CH 2 CH 2 CH 2 CH 2链，并且R 3和R 4，R 1和R 4以及R 1和R 2分别如上所定义，R 5是氢，低级烷基或式-Alk-OR 6基团，其中Alk是亚烷基选自由CR7R8，CR7R8CR9R10，CR7R8CR9R10CR11R12和CR7R8CR9R10CR11R12CR13R14组成的组，其中R7，R8，R9，R10，R11，R12，R13和R14各自为氢或低级烷基，R6为氢或低级烷基; R 15是氢或低级烷基; X是O，S，SO或SO 2; Y是O或NR16，其中R16是氢或低级烷基。式1的化合物可用于治疗过敏性病症和治疗微生物感染。公开了制备和使用所述化合物的方法。

5. 发明授权

US4070371A Derivatives of 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid 失效
标题翻译： 1,3,4,9-四氢吡喃{8,3-b {9吲哚-1-乙酸）的衍生物
公开(公告)号：US4070371A
公开(公告)日：1978-01-24
申请号：US749631
申请日：1976-12-13
申请人： Christopher A. Demerson , Leslie G. Humber , Thomas A. Dobson , Ivo L. Jirkovsky
发明人： Christopher A. Demerson , Leslie G. Humber , Thomas A. Dobson , Ivo L. Jirkovsky
IPC分类号： C07D311/76 , C07D405/04 , C07D409/04 , C07D491/04 , C07D491/052 , C07D495/04 , H01L29/73
CPC分类号： C07D405/04 , C07D311/76 , C07D409/04 , C07D491/04 , C07D491/052 , C07D495/04 , H01L29/73
摘要： Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus bearing a substituent in position 1, said substituent incorporating an acid, ester or amide function therein, are disclosed. The nucleus is further substituted at position 1 and may be optionally substituted at positions 3, 4, 5, 6, 7, 8, and 9. The derivatives are useful antiinflammatory, analgesic, antibacterial and antifungal agents and methods for their preparation and use are also disclosed.
摘要翻译：其特征在于具有在位置1具有取代基的1,3,4,9-四氢吡喃并[3,4-b]吲哚或1,3,4,9-四氢噻喃并[3,4-b]吲哚核，所述公开了其中包含酸，酯或酰胺官能团的取代基。核在第1位被进一步取代，并且可以在3,4,5,6,7,8和9位任选被取代。该衍生物是有用的抗炎，镇痛，抗菌和抗真菌剂，其制备和使用方法是也披露。

6. 发明授权

US4060619A 1,4-Dihydro-4-oxo-benzothiopyrano (4,3-b)pyridine-2-carboxylates and derivatives 失效
标题翻译： 1,4-二氢-4-氧代 - 苯并噻喃并（4,3-b）吡啶-2-羧酸酯及其衍生物
公开(公告)号：US4060619A
公开(公告)日：1977-11-29
申请号：US649113
申请日：1976-01-14
申请人： Adolf H. Philipp , Ivo L. Jirkovsky
发明人： Adolf H. Philipp , Ivo L. Jirkovsky
IPC分类号： C07D311/22 , C07D335/06 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/14 , A61K31/435
CPC分类号： C07D491/04 , C07D311/22 , C07D335/06 , C07D493/04 , C07D495/04
摘要： Compounds of formula 1 ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different selected from the group consisting of hydrogen, halogen, nitro, trifluoromethyl, lower alkyl and lower alkoxy, or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4 together form a CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 chain and R.sup.3 and R.sup.4, R.sup.1 and R.sup.4 and R.sup.1 and R.sup.2, respectively, are as defined above, R.sup.5 is hydrogen, lower alkyl or a radical of formula -Alk-OR.sup.6 wherein Alk is an alkylene selected from the group consisting of CR.sup.7 R.sup.8, CR.sup.7 R.sup.8 CR.sup.9 R.sup.10, CR.sup.7 R.sup.8 CR.sup.9 R.sup.10 CR.sup.11 R.sup.12 and CR.sup.7 R.sup.8 CR.sup.9 R.sup.10 CR.sup.11 R.sup.12 CR.sup.13 R.sup.14 wherein each of R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is hydrogen or lower alkyl and R.sup.6 is hydrogen or lower alkyl; R.sup.15 is hydrogen or lower alkyl; X is O, S, SO or SO.sub.2 ; and Y is O or NR.sup.16 wherein R.sup.16 is hydrogen or lower alkyl, are disclosed. The compounds of formula 1 are useful for treating allergic conditions and for treating microbial infections. Methods for the preparation and use of said compounds are disclosed.
摘要翻译：式1的化合物其中R 1，R 2，R 3和R 4相同或不同，选自氢，卤素，硝基，三氟甲基，低级烷基和低级烷氧基，或R 1和R 2，R 2和R 3 或R3和R4一起形成CH 2 CH 2 CH 2 CH 2链，并且R 3和R 4，R 1和R 4以及R 1和R 2分别如上所定义，R 5是氢，低级烷基或式-Alk-OR 6基团，其中Alk是亚烷基选自由CR7R8，CR7R8CR9R10，CR7R8CR9R10CR11R12和CR7R8CR9R10CR11R12CR13R14组成的组，其中R7，R8，R9，R10，R11，R12，R13和R14各自为氢或低级烷基，R6为氢或低级烷基; R 15是氢或低级烷基; X是O，S，SO或SO 2; 并且Y是O或NR 16，其中R 16是氢或低级烷基。式1的化合物可用于治疗过敏性病症和治疗微生物感染。公开了制备和使用所述化合物的方法。

7. 发明授权

US3939178A Certain pyrano [3,4-b]indoles and thiopyrano[3,4-b]indoles 失效
标题翻译：某些吡喃糖[8,3-b] {9吲哚和噻虫啉{8,3-b {9吲哚
公开(公告)号：US3939178A
公开(公告)日：1976-02-17
申请号：US289714
申请日：1972-09-15
申请人： Christopher A. Demerson , Leslie G. Humber , Thomas A. Dobson , Ivo L. Jirkovsky
发明人： Christopher A. Demerson , Leslie G. Humber , Thomas A. Dobson , Ivo L. Jirkovsky
IPC分类号： C07D311/76 , C07D405/04 , C07D409/04 , C07D491/04 , C07D495/04 , H01L29/73 , C07D493/04
CPC分类号： C07D405/04 , C07D311/76 , C07D409/04 , C07D491/04 , C07D491/052 , C07D495/04 , H01L29/73
摘要： Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus bearing a substituent in position 1, said substituent incorporating an acid, ester or amide function therein, are disclosed. The nucleus is further substituted at position 1 and may be optionally substituted at positions 3, 4, 5, 6, 7, 8, and 9. The derivatives are useful antiinflammatory, analgesic, antibacterial and antifungal agents and methods for their preparation and use are also disclosed.
摘要翻译：其特征在于具有在位置1具有取代基的1,3,4,9-四氢吡喃并[3,4-b]吲哚或1,3,4,9-四氢噻喃并[3,4-b]吲哚核，所述公开了其中包含酸，酯或酰胺官能团的取代基。核在第1位被进一步取代，并且可以在3,4,5,6,7,8和9位任选被取代。该衍生物是有用的抗炎，镇痛，抗菌和抗真菌剂，其制备和使用方法是也披露。

8. 发明授权

US5118675A Quinoxaline phosphono-amino acids 失效
标题翻译：喹喔啉膦酰氨基酸
公开(公告)号：US5118675A
公开(公告)日：1992-06-02
申请号：US656894
申请日：1991-02-15
申请人： Ivo L. Jirkovsky , Reinhardt B. Baudy , Lynne P. Greenblatt
发明人： Ivo L. Jirkovsky , Reinhardt B. Baudy , Lynne P. Greenblatt
IPC分类号： C07F9/6509
CPC分类号： C07F9/650994
摘要： The compounds of the formula: ##STR1## in which Q is the quinoxaline nucleus; m is one of the integers 0, 1 or 2; n is one of the integers 1,2 or 3; or a pharmaceutically acceptable salt, alkyl ester or ##STR2## where R.sup.3 and R.sup.4 are, independently, hydrogen, nitro, halo or methoxy, are NMDA antagonists useful in the treatment and prevention of central nervous system related pathological conditions resulting from overstimulation by excitatory amino acids.
摘要翻译：下式的化合物：其中Q是喹喔啉核; m是整数0,1或2之一; n是整数1,2或3之一; 或其药学上可接受的盐，烷基酯或者其中R 3和R 4独立地为氢，硝基，卤素或甲氧基的NMDA拮抗剂是可用于治疗和预防由兴奋性氨基过度刺激引起的中枢神经系统相关病理状况的NMDA拮抗剂酸。

9. 发明授权

US5010102A Anti-ulcer 5-(2-substituted ethenyl)-3(2H)-furanones 失效
标题翻译：抗溃疡5-（2-取代乙烯基）-3（2H） - 呋喃酮
公开(公告)号：US5010102A
公开(公告)日：1991-04-23
申请号：US572533
申请日：1990-08-23
申请人： Steven W. Felman , Ivo L. Jirkovsky , Kevin A. Memoli
发明人： Steven W. Felman , Ivo L. Jirkovsky , Kevin A. Memoli
IPC分类号： C07D307/58 , C07D405/06 , C07D409/06
CPC分类号： C07D405/06 , C07D307/58 , C07D409/06
摘要： A compound of the formula: ##STR1## in which R is alkyl, phenyl or halophenyl; R.sup.2 is substituted phenyl having from 1 to 3 substiuents selected from halo, alkyl, alkylthio, alkylsulfonyl, cyano, trifluoromethyl, or R.sup.2 is pyridinyl, pyrazinyl, quinolinyl, N-alkylpyrrolyl, thienyl, benzothienyl, or furyl; and n is 1 or 2, are cytoprotective anti-ulcer agents.
摘要翻译：下式的化合物：其中R是烷基，苯基或卤代苯基; R 2是具有1至3个选自卤素，烷基，烷硫基，烷基磺酰基，氰基，三氟甲基或R 2的取代苯基，其为吡啶基，吡嗪基，喹啉基，N-烷基吡咯基，噻吩基，苯并噻吩基或呋喃基; n为1或2，为细胞保护性抗溃疡剂。

10. 发明授权

US4916241A Inhibition of bone loss by 4-substituted-5-hydroxy-2(5H)-furanones 失效
标题翻译：通过4-取代-5-羟基-2（5H） - 呋喃酮抑制骨丢失
公开(公告)号：US4916241A
公开(公告)日：1990-04-10
申请号：US205147
申请日：1988-06-06
申请人： Marshall A. Hayward , Joseph P. Sabatucci , Ivo L. Jirkovsky , Yvon Lefebvre
发明人： Marshall A. Hayward , Joseph P. Sabatucci , Ivo L. Jirkovsky , Yvon Lefebvre
IPC分类号： C07D307/60 , C07D407/06
CPC分类号： C07D407/06 , C07D307/60
摘要： This invention relates to 4-substituted-5-hydroxy-2(5H)-furanones, to the process for their preparation, to pharmaceutical compositions containing said 4-substituted-5-hydroxy-2(5H)-furanones and to the use of said 4-substituted-5-hydroxy-2(5H)-furanones for modifying the balance between bone production and bone resorption in a host animal, including man.
摘要翻译：本发明涉及4-取代-5-羟基-2（5H） - 呋喃酮，其制备方法涉及含有所述4-取代-5-羟基-2（5H） - 呋喃酮的药物组合物，以及使用所述4-取代-5-羟基-2（5H） - 呋喃酮用于改变包括人在内的宿主动物的骨产生和骨吸收之间的平衡。

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