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21. 发明授权

US4169202A Process for preparing 4,5-dihydro-4-oxofuran-2-carboxylic acid derivatives 失效
标题翻译：制备4,5-二氢-4-氧代呋喃-2-羧酸衍生物的方法
公开(公告)号：US4169202A
公开(公告)日：1979-09-25
申请号：US912798
申请日：1978-06-05
申请人： Ivo L. Jirkovsky , Dushan Dvornik , Mitchell N. Cayen
发明人： Ivo L. Jirkovsky , Dushan Dvornik , Mitchell N. Cayen
IPC分类号： A61K31/34 , A61K31/341 , A61K31/44 , A61K31/443 , A61P3/06 , C07C33/30 , C07C45/31 , C07D307/00 , C07D307/68 , C07D309/36 , C07D405/00 , C07D405/12
CPC分类号： C07D309/36 , C07C33/30 , C07C45/31 , C07D307/68
摘要： Derivatives of 4,5-dihydro-4-oxofuran-2-carboxylic acid characterized by having two substituents at position 5 and in addition being optionally further substituted at position 3 with a lower alkyl group, as well as esters therefor are disclosed. The foregoing compounds are useful hypolipidemic agents in a mammal. Novel methods for the preparation of these compounds also are disclosed.
摘要翻译：特征在于在5位具有两个取代基，另外任选地在3位被低级烷基取代的PG，1的4,5-二氢-4-氧代呋喃-2-羧酸衍生物，以及其酯是披露上述化合物是哺乳动物中有用的降血脂药。还公开了制备这些化合物的新方法。

22. 发明授权

US4012417A Process for preparing pyrano[3,4-b]indole or thio pyrano[3,4-b]indole derivatives 失效
标题翻译：制备吡喃并{8,3-b {9吲哚或硫代吡喃并{8,3-b {9吲哚衍生物
公开(公告)号：US4012417A
公开(公告)日：1977-03-15
申请号：US555506
申请日：1975-03-05
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
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。

23. 发明授权

US5389671A 4- or 5-(substituted sulfonyl)methyl-3(2H)-furanones 失效
标题翻译： 4-或5-（取代的磺酰基）甲基-3（2H） - 呋喃酮
公开(公告)号：US5389671A
公开(公告)日：1995-02-14
申请号：US197427
申请日：1994-02-16
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 , C07D307/94 , A61K31/34
CPC分类号： C07D307/94 , C07D307/58
摘要： The present invention relates to novel 4- or 5-(substituted sulfonyl) methyl-3(2H)-furanones having the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl containing 1 to 6 branched or straight chain carbon atoms, phenyl, or halogen substituted phenyl; or R.sup.1 and R.sup.2 are joined by 5 to 7 carbon atoms;R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 1 to 6 branched or straight chain carbon atoms or R.sup.3 and R.sup.4 are joined by 4 to 6 carbon atoms;R.sup.5 is alkyl containing 1 to 6 branched or straight chain carbon atoms, phenyl, naphthyl or substituted phenyl wherein the substituent is selected from the group consisting of alkyl containing 1 to 6 branched or straight chain carbon atoms, halogen, methoxy, nitro and acetamide which possess blood-glucose lowering activity and inhibit cholesterol absorption, and which have cytoprotective and antiulcer activity, to processes for preparation thereof, pharmaceutical compositions comprising the same, and to the method of using the same in the reduction of excess glucose and cholesterol and of treatment of ulcers in human beings and animals.
摘要翻译：本发明涉及具有式（I）的新的4-或5-（取代的磺酰基）甲基-3（2H） - 呋喃酮，其中R 1和R 2独立地为含有1至6个支链或直链的烷基碳原子，苯基或卤素取代的苯基; 或R 1和R 2与5至7个碳原子连接; R3和R4独立地为氢，含有1至6个支链或直链碳原子的烷基或R3和R4通过4至6个碳原子连接; R5是含有1至6个支链或直链碳原子的烷基，苯基，萘基或取代的苯基，其中取代基选自含1-6个支链或直链碳原子的烷基，卤素，甲氧基，硝基和乙酰胺，其中具有血糖降低活性和抑制胆固醇吸收，并且其具有细胞保护和抗溃疡活性，其制备方法，包含其的药物组合物及其在减少过量葡萄糖和胆固醇和治疗中的使用方法的人类和动物的溃疡。

24. 发明授权

US5236941A 5-(2-hydroxy-1-arylethylidene)- and 5-(2-oxo-1-arylethylidene)-2,4-thiazolidinediones and derivatives thereof 失效
标题翻译： 5-（2-羟基-1-芳乙炔基） - 和5-（2-氧代-1-芳基亚乙基）-2,4-噻唑烷二酮及其衍生物
公开(公告)号：US5236941A
公开(公告)日：1993-08-17
申请号：US906331
申请日：1992-06-30
申请人： Arie Zask , Ivo L. Jirkovsky
发明人： Arie Zask , Ivo L. Jirkovsky
IPC分类号： C07D277/20 , C07D277/34
CPC分类号： C07D277/20
摘要： 5-(2-Hydroxy-1-phenyl (or-1-naphthalenyl)ethylidene) and 5-(2-oxo-1-phenyl (or 1-naphthalenyl)ethylidene)-2,4-thiazolidinediones and derivatives thereof are useful in lowering blood glucose levels in a hyperglycemic laboratory animal model and are thus useful in the treatment of diabetes mellitus.
摘要翻译： 5-（2-羟基-1-苯基（或-1-萘基）亚乙基）和5-（2-氧代-1-苯基（或1-萘基）亚乙基）-2,4-噻唑烷二酮类及其衍生物可用于降低高血糖实验室动物模型中的血糖水平，因此可用于治疗糖尿病。

25. 发明授权

US4307092A 1-Oxo-5H-pyrimido[2,1-C]benzoxazine-2-carboxylic acid esters 失效
标题翻译： 1-氧代-5H-嘧啶并[2,1-C]苯并恶嗪-2-羧酸酯
公开(公告)号：US4307092A
公开(公告)日：1981-12-22
申请号：US173507
申请日：1980-07-22
申请人： Jean A. Gauthier , Ivo L. Jirkovsky
发明人： Jean A. Gauthier , Ivo L. Jirkovsky
IPC分类号： C07D265/36 , C07D498/04 , C07D513/04 , A61K31/495 , A61K31/505 , C07D487/04
CPC分类号： C07D513/04 , C07D265/36
摘要： This invention discloses novel 1-oxo-5H-pyrimidol[2,1-c][1,4]benzoxa(or thia)zinc-2-carboxylic acid lower alkyl esters, derivatives thereof, process 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1-氧代-5H-嘧啶并[2,1-c] [1,4]苯并恶唑（或硫杂）锌-2羧酸低级烷基酯及其衍生物，其制备方法，其药物组合物和使用化合物的方法。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。

26. 发明授权

US4244958A Hypolipidemic derivatives of 4,5-dihydro-4-oxofuran-2-carboxylic acid 失效
标题翻译： 4,5-二氢-4-氧代呋喃-2-羧酸的降血脂衍生物
公开(公告)号：US4244958A
公开(公告)日：1981-01-13
申请号：US38028
申请日：1979-05-10
申请人： Ivo L. Jirkovsky , Dushan Dvornik , Mitchell N. Cayen
发明人： Ivo L. Jirkovsky , Dushan Dvornik , Mitchell N. Cayen
IPC分类号： C07C29/42 , C07C45/31 , C07D307/68 , C07D309/36 , A61K31/34 , A61K31/445 , C07D213/55
CPC分类号： C07D309/36 , C07C29/42 , C07C45/31 , C07D307/68
摘要： Derivatives of 4,5-dihydro-4-oxofuran-2-carboxylic acid characterized by having two substituents at position 5 and in addition being optionally further substituted at position 3 with a lower alkyl group, as well as esters therefor are disclosed. The foregoing compounds are useful hypolipidemic agents in a mammal. Novel methods for the preparation of these compounds also are disclosed.
摘要翻译：特征在于在5位具有两个取代基，另外在3位任选进一步被低级烷基取代的4,5-二氢-4-氧代呋喃-2-羧酸的衍生物及其酯。上述化合物是哺乳动物中有用的降血脂药。还公开了制备这些化合物的新方法。

27. 发明授权

US4189490A 2-Substituted-3-methyl-.gamma.-pyrone tricyclic derivatives 失效
标题翻译： 2-取代的3-甲基-γ-吡喃酮三环衍生物
公开(公告)号：US4189490A
公开(公告)日：1980-02-19
申请号：US7058
申请日：1979-01-29
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 , C07D493/04 , C07D495/04 , C07F5/02 , C07D257/10 , A61K31/35 , C07D405/04 , C07D493/14
CPC分类号： C07D493/04 , C07D311/22 , C07D335/06 , C07D495/04 , C07F5/022
摘要： Compounds of formula I ##STR1## in which R.sup.1 is hydrogen, halogen, nitro, trifluoromethyl, lower alkyl or lower alkoxy; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydroxy, 1H-tetrazol-5-yl or COOR.sup.4 wherein R.sup.4 is hydrogen or lower alkyl, and X is O, S, SO or SO.sub.2, are disclosed. The compounds of formula I are useful for treating allergic conditions. Methods for the preparation and use of the compounds are disclosed.
摘要翻译：式I的化合物其中R 1是氢，卤素，硝基，三氟甲基，低级烷基或低级烷氧基; R2是氢或低级烷基; R3是羟基，1H-四唑-5-基或COOR4，其中R4是氢或低级烷基，X是O，S，SO或SO2。式I化合物可用于治疗过敏性疾病。公开了制备和使用化合物的方法。

28. 发明授权

US4188389A 1,2,3,4-Tetrahydropyrrolo(1,2-A)pyrazines 失效
标题翻译： 1,2,3,4-四氢吡咯（1,2-A）吡嗪
公开(公告)号：US4188389A
公开(公告)日：1980-02-12
申请号：US957602
申请日：1978-11-03
申请人： Ivo L. Jirkovsky
发明人： Ivo L. Jirkovsky
IPC分类号： C07D207/32 , C07D207/325 , C07D487/04 , A61K31/495
CPC分类号： C07D207/325 , C07D487/04
摘要： 1,2,3,4-tetrahydropyrrolo(1,2-a)pyrazine derivatives characterized by having a lower alkyl, cyclo(lower)alkyl, phenyl or substituted phenyl at position 1 of the nucleus and optionally further substituted at position 2 of the nucleus with a lower alkyl, cyclo(lower)alkyl, phenyl(lower)alkylene or 2-(indole-3-yl)ethyl are disclosed. The derivatives are useful antidepressant agents. Methods for their preparation also are disclosed.
摘要翻译： 1,2,3,4-四氢吡咯并（1,2-a）吡嗪衍生物，其特征在于在核的位置1具有低级烷基，环（低级）烷基，苯基或取代的苯基，并任选地在公开了具有低级烷基，环（低级）烷基，苯基（低级）亚烷基或2-（吲哚-3-基）乙基）的核。衍生物是有用的抗抑郁剂。还公开了其制备方法。

29. 发明授权

US4177284A 2-Substituted-3-methyl-.gamma.-pyrone tricvclic derivatives and process therefor 失效
标题翻译： 2-取代的3-甲基-γ-吡喃酮三氯代衍生物及其制备方法
公开(公告)号：US4177284A
公开(公告)日：1979-12-04
申请号：US855538
申请日：1977-11-28
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 , C07D493/04 , C07D495/04 , C07F5/02 , A61K31/38
CPC分类号： C07D493/04 , C07D311/22 , C07D335/06 , C07D495/04 , C07F5/022
摘要： Compounds of formula I ##STR1## in which R.sup.1 is hydrogen, halogen, nitro, trifluoromethyl, lower alkyl or lower alkoxy; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydroxy, 1H-tetrazol-5-yl or COOR.sup.4 wherein R.sup.4 is hydrogen or lower alkyl, and X is O, S, SO or SO.sub.2, are disclosed. The compounds of formula I are useful for treating allergic conditions. Methods for the preparation and use of the compounds are disclosed.
摘要翻译：式I的化合物其中R 1是氢，卤素，硝基，三氟甲基，低级烷基或低级烷氧基; R2是氢或低级烷基; R3是羟基，1H-四唑-5-基或COOR4，其中R4是氢或低级烷基，X是O，S，SO或SO2。式I化合物可用于治疗过敏性疾病。公开了制备和使用化合物的方法。

30. 发明授权

US4021451A Process for preparing polycyclic heterocycles having a pyran ring 失效
标题翻译：制备具有吡喃环的多环杂环的方法
公开(公告)号：US4021451A
公开(公告)日：1977-05-03
申请号：US584086
申请日：1975-06-05
申请人： Thomas A. Dobson , Leslie G. Humber , Christopher A. Demerson , Ivo L. Jirkovsky
发明人： Thomas A. Dobson , Leslie G. Humber , Christopher A. Demerson , Ivo L. Jirkovsky
IPC分类号： C07D333/24 , C07D491/052
CPC分类号： C07D491/052
摘要： A process applicable to the preparation of a wide variety of novel polycyclic heterocycles having a newly-formed pyran ring is disclosed. According to the process an aromatic nucleus bearing an ethanol group, for example, 3,4-dimethoxyphenethyl alcohol, is condensed with an aldehyde or ketone or a protected aldehyde or ketone, for example, aminoactaldehyde diethyl acetal, in the presence of an acid catalyst to afford the polycyclic heterocycle, for example, 6,7-dimethoxy-1-isochromanmethylamine. The new heterocycles so formed are useful for preparing derivatives having antiinflammatory, antibacterial or antifungal activities.
摘要翻译：公开了一种适用于制备具有新形成的吡喃环的多种新型多环杂环的方法。根据该方法，在酸催化剂存在下，将带有乙醇基团的芳香族核，例如3,4-二甲氧基苯乙醇与醛或酮或被保护的醛或酮，例如氨基甲醛二乙基缩醛缩合得到多环杂环，例如6,7-二甲氧基-1-异苯并二氢吡喃甲胺。如此形成的新的杂环可用于制备具有抗炎，抗菌或抗真菌活性的衍生物。

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