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21. 发明授权

US3944584A Steroidal (16.alpha.,17-d)cyclohexenes 失效
标题翻译：甾体（16（60,17-d）环己烯
公开(公告)号：US3944584A
公开(公告)日：1976-03-16
申请号：US546647
申请日：1975-02-03
申请人： Sam T. Chao , Christopher M. Cimarusti , Ravi K. Varma
发明人： Sam T. Chao , Christopher M. Cimarusti , Ravi K. Varma
IPC分类号： A61K8/63 , A61P29/00 , C07J53/00 , C07J5/00
CPC分类号： C07J53/002 , Y10S514/861 , Y10S514/863
摘要： A series of novel steroidal[ 16.alpha., 17-d]cyclohexenes having a 9-fluoro group is disclosed herein for use as anti-inflammatory agents.
摘要翻译：本文公开了一系列具有9-氟基团的新型甾族化合物[16α，17-d]环己烯用作抗炎剂。

22. 发明授权

US5089523A Fluorinated derivatives of mevinic acids 失效
标题翻译：微生物的氟化衍生物
公开(公告)号：US5089523A
公开(公告)日：1992-02-18
申请号：US521880
申请日：1990-05-11
申请人： Ravi K. Varma , Sam T. Chao
发明人： Ravi K. Varma , Sam T. Chao
IPC分类号： A61K31/215 , A61K31/22 , A61K31/351 , A61K31/355 , A61P1/16 , A61P3/06 , A61P9/10 , A61P35/00 , A61P43/00 , C07C69/63 , C07C69/675 , C07C69/732 , C07D309/30
CPC分类号： C07D309/30 , C07C69/732 , C07C2102/28
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salts and tautomeric mixtures thereof possess activity as HMg-CoA reductase inhibitors, thus making them useful as antihypercholesterolemic agents. In the above formula,Z is ##STR2## R.sup.1 and R.sup.2 are each independently fluoro or hydrogen, except that at least one of R.sup.1 and R.sup.2 is fluoro;R.sup.3 is hydrogen, alkyl, cycloalkyl, aryl or arylalkyl; andR.sup.4 is hydrogen, alkyl, ammonium, alkylammonium, or alkali metal.

23. 发明授权

US4906667A Phenyl hydroxamic acids including a hetero-containing substituent 失效
标题翻译：苯基异羟肟酸，包括含杂原子的取代基
公开(公告)号：US4906667A
公开(公告)日：1990-03-06
申请号：US203527
申请日：1988-05-23
申请人： Ravi K. Varma , Eric M. Gordon , Martin F. Haslanger
发明人： Ravi K. Varma , Eric M. Gordon , Martin F. Haslanger
IPC分类号： C07C259/10
CPC分类号： C07C259/10 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Phenyl hydroxamic acids are disclosed having the general formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein X is NR, oxygen, sulfur, ##STR2## or a single bond, and Y is NR, oxygen, sulfur, ##STR3## or a single bond, where R can be hydrogen or lower alkyl, g can be 1 or 2, and with the proviso that at least one of X and Y is other than a single bond; Z is aryl, aralkyl or cycloalkyl; R.sub.1 is hydrogen, substituted or unsubstituted lower alkyl, cycloalkyl, lower alkenyl or aryl; R.sub.2 is hydrogen, lower alkyl, aroyl or acyl; m is 0 to 4 carbon atoms; and, n is 0 to 4 carbon atoms further providing that if one of X or Y is oxygen, the other of X or Y must be oxygen and further that when X and Y are oxygen Z cannot be aralalkyl.These new compounds have been found to be inhibitors or arachidonic acid 5-lipoxygenase and are therefore useful as antiallergy agents and antipsoriatics.
摘要翻译：公开了具有通式为“IMAGE”或其药学上可接受的盐的苯基异羟肟酸，其中X是NR，氧，硫，或单键，Y是NR，氧，硫，单键，其中R可以是氢或低级烷基，g可以是1或2，条件是X和Y中的至少一个不是单键; Z是芳基，芳烷基或环烷基; R 1是氢，取代或未取代的低级烷基，环烷基，低级烯基或芳基; R2是氢，低级烷基，芳酰基或酰基; m为0〜4个碳原子; 并且n为0至4个碳原子，条件是如果X或Y中的一个为氧，X或Y中的另一个必须为氧，此外，当X和Y为氧时，Z不能为芳烷基。已经发现这些新化合物是抑制剂或花生四烯酸5-脂氧合酶，因此可用作抗过敏剂和抗牛皮癣剂。

24. 发明授权

US4673685A Hydroximic acids of 7-oxabicycloheptane substituted ethers and thioethers useful in the treatment of thrombotic disease 失效
标题翻译：可用于治疗血栓性疾病的7-氧杂双环庚烷取代的醚和硫醚的羟基酸
公开(公告)号：US4673685A
公开(公告)日：1987-06-16
申请号：US888671
申请日：1986-07-23
申请人： Ravi K. Varma , Eric M. Gordon , Ligaya M. Simpkins
发明人： Ravi K. Varma , Eric M. Gordon , Ligaya M. Simpkins
IPC分类号： A61K31/34 , A61K31/44 , A61P1/04 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/08 , A61P17/00 , A61P25/04 , A61P29/00 , A61P37/08 , A61P43/00 , C07D493/08 , A61K31/557 , C07D307/00
CPC分类号： C07D493/08
摘要： Hydroximic acids of 7-oxabicycloheptane substituted ether and thioether prostaglandin analogs are provided having the structural formula ##STR1## wherein Y is O or ##STR2## and including all stereoisomers thereof. The compounds are inhibitors of prostaglandin and biosynthesis and as such are useful, for example, as anti-allergy and antiinflammatory agents and also as antipsoriatic agents.
摘要翻译：提供7-氧杂双环庚烷取代醚和硫醚前列腺素类似物的羟基酸，其具有结构式为其中Y为O或者IMA的结构式，并且包括其所有立体异构体。这些化合物是前列腺素和生物合成的抑制剂，因此可用作例如抗过敏和抗炎剂，也可用作抗牛皮癣药。

25. 发明授权

US4529547A 17-(substituted thio)-17-(substituted dithio)androstenes 失效
标题翻译： 17-（取代的硫代）-17-（取代的二硫）雄甾烯
公开(公告)号：US4529547A
公开(公告)日：1985-07-16
申请号：US622508
申请日：1984-06-20
申请人： Ravi K. Varma
发明人： Ravi K. Varma
IPC分类号： A61K31/565 , A61P29/00 , C07J31/00 , C07J1/00
CPC分类号： C07J31/003
摘要： Topical antiinflammatory activity is by steroids having the formula ##STR1## and the 1,2-dehydro derivatives thereof wherein R.sub.1 and R.sub.2 are the same or different and each is alkyl, aryl, arylalkyl or cycloalkyl;R.sub.3 is carbonyl or .beta.-hydroxymethylene;R.sub.4 is hydrogen or halogen; andR.sub.5 is hydrogen, methyl or fluorine.
摘要翻译：局部抗炎活性是具有式“IMAGE”的类固醇和其中R1和R2相同或不同并且各自为烷基，芳基，芳烷基或环烷基的1,2-脱氢衍生物; R3是羰基或β-羟基亚甲基; R4是氢或卤素; R5是氢，甲基或氟。

26. 发明授权

US4528138A 16-Keto-17-substituted thia-17-alkyl(or alkenyl or alkynyl) androstenes 失效
标题翻译： 16-酮17取代的硫杂-17-烷基（或烯基或炔基）雄甾烯
公开(公告)号：US4528138A
公开(公告)日：1985-07-09
申请号：US622509
申请日：1984-06-20
申请人： Ravi K. Varma , Donald S. Karanewsky
发明人： Ravi K. Varma , Donald S. Karanewsky
IPC分类号： A61K31/565 , A61P29/00 , C07J31/00 , C07J1/00
CPC分类号： C07J31/003
摘要： Antiinflammatory activity is exhibited by steroids having the formula ##STR1## and the 1,2-dehydro derivative thereof, wherein R.sub.1 is alkyl, mono-, di- or trifluoroalkyl, ##STR2## aryl or alkylthioalkyl, wherein R.sub.6 is alkyl or aryl and m is 1, 2, 3 or 4;R.sub.2 is ##STR3## wherein R.sub.7, R.sub.8 and R.sub.9 are each independently hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.3 is carbonyl or .beta.-hydroxymethylene;R.sub.4 is hydrogen or halogen;R.sub.5 is hydrogen, methyl or fluorine; andn is 0, 1 or 2;with the proviso that if R.sub.1 is alkylthioalkyl, n is 0.
摘要翻译：抗炎活性由具有下式的类固醇及其1,2-脱氢衍生物显示，其中R 1为烷基，单 - ，二 - 或三氟烷基，芳基或烷硫基烷基，其中R 6为烷基或芳基，m 是1，2，3或4; R 2是，其中R 7，R 8和R 9各自独立地是氢或1至4个碳原子的烷基; R3是羰基或β-羟基亚甲基; R4是氢或卤素; R5是氢，甲基或氟; 且n为0,1或2; 条件是如果R1是烷硫基烷基，n是0。

27. 发明授权

US4488995A Androstene-17.beta.-alkylthiomethyl ethers 失效
标题翻译：雄甾烯-17β-烷硫基甲基醚
公开(公告)号：US4488995A
公开(公告)日：1984-12-18
申请号：US577444
申请日：1984-02-06
申请人： Ravi K. Varma
发明人： Ravi K. Varma
IPC分类号： C07J1/00 , C07J31/00 , C07J7/00
CPC分类号： C07J1/0048 , C07J1/0011 , C07J1/0022 , C07J1/0037 , C07J31/006
摘要： Antiinflammatory activity is exhibited by steroids having the structural formula ##STR1## or a 1,2-dihydro derivative thereof, wherein R is alkyl;R.sub.1 is hydrogen, alkyl, alkenyl, alkynyl, or aryl;R.sub.2 is carbonyl or .beta.-hydroxymethylene;R.sub.3 is hydrogen or halogen; andR.sub.4 is hydrogen, methyl or fluorine.
摘要翻译：抗炎活性由结构式为“IMAGE”的类固醇或其1,2-二氢衍生物表现，其中R为烷基; R1是氢，烷基，烯基，炔基或芳基; R2是羰基或β-羟基亚甲基; R3是氢或卤素; R4是氢，甲基或氟。

28. 发明授权

US4481144A 17-Substituted thia-17-alkyl(or alkenyl or alkynyl)androstenes 失效
标题翻译： 17-取代的硫杂-17-烷基（或烯基或炔基）雄甾烯
公开(公告)号：US4481144A
公开(公告)日：1984-11-06
申请号：US576668
申请日：1984-02-03
申请人： Ravi K. Varma
发明人： Ravi K. Varma
IPC分类号： C07J31/00 , C07J5/00
CPC分类号： C07J31/003
摘要： Antiinflammatory activity is exhibited by steroids having the formula ##STR1## and the 1,2-dehydro derivatives thereof, wherein R is hydrogen, alkyl, or aryl;R.sub.1 is hydrogen, alkyl, ##STR2## alkylthio, alkoxy, fluoro, hydroxyalkyl, cyanoalkyl, alkoxycarbonyl-(CH.sub.2).sub.p -, mono-, di- or trifluoromethyl, or ##STR3## wherein p is 0, 1, 2, 3 or 4, Y.sub.1 is alkyl or aryl, and Y.sub.2 and Y.sub.3 are the same or different and each is hydrogen or alkyl;R.sub.2 is alkyl, alkenyl or alkynyl;R.sub.3 is carbonyl or .beta.-hydroxymethylene;R.sub.4 is hydrogen or halogen;R.sub.5 is hydrogen, methyl or fluorine; andn is 0, 1 or 2.
摘要翻译：具有式“IMAGE”的类固醇及其1,2-脱氢衍生物表现出抗炎活性，其中R为氢，烷基或芳基; R1是氢，烷基，烷硫基，烷氧基，氟，羟基烷基，氰基烷基，烷氧基羰基 - （CH2）p-，单 - ，二 - 或三氟甲基或其中p是0,1,2,3或 4，Y1是烷基或芳基，Y2和Y3相同或不同，各自是氢或烷基; R2是烷基，烯基或炔基; R3是羰基或β-羟基亚甲基; R4是氢或卤素; R5是氢，甲基或氟; n为0,1或2。

29. 发明授权

US4427592A Androstene-17-dithioketals 失效
标题翻译：雄甾烯-17-二硫酮缩酮
公开(公告)号：US4427592A
公开(公告)日：1984-01-24
申请号：US462164
申请日：1983-04-07
申请人： Ravi K. Varma , Donald S. Karanewsky
发明人： Ravi K. Varma , Donald S. Karanewsky
IPC分类号： A61K31/565 , A61P29/00 , C07J1/00 , C07J31/00 , C07J41/00
CPC分类号： C07J41/0038 , C07J1/0011 , C07J31/003
摘要： Topical antiinflammatory activity is exhibited by steroids having the formula ##STR1## and the 1,2-dehydro, and 6,7-dehydro derivatives thereof, wherein one of R.sub.1 and R.sub.2 is alkyl, aryl, arylalkyl, or cycloalkyl, and the other is alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, mono-, di- or trifluoroalkyl, cyanoalkyl, alkanoylalkyl or ##STR2## wherein n is 1, 2, 3 or 4 and Y.sub.1 and Y.sub.2 are the same or different and each is hydrogen or alkyl;R.sub.3 is hydrogen, hydroxy, alkoxy, aryloxy, oxo, methylene, alkylthio, arylthio, alkanoyl, alkanoyloxy, or fluorine;R.sub.4 is carbonyl, .beta.-hydroxymethylene or .beta.-acetyloxymethylene;R.sub.5 is hydrogen or halogen; andR.sub.6 is hydrogen, methyl, hydroxy, alkanoyl, alkanoyloxy or halogen.
摘要翻译：具有式“IMAGE”的类固醇及其1,2-二氢和6,7-脱氢衍生物可表现出局部抗炎活性，其中R1和R2之一为烷基，芳基，芳基烷基或环烷基，另一个为链烯基，取代的烯基，炔基，取代的炔基，单 - ，二 - 或三氟烷基，氰基烷基，烷酰基烷基或其中n为1,2,3或4，并且Y 1和Y 2相同或不同，各自为氢或烷基 ; R3是氢，羟基，烷氧基，芳氧基，氧代，亚甲基，烷硫基，芳硫基，烷酰基，烷酰氧基或氟; R4是羰基，β-羟基亚甲基或β-乙酰氧基亚甲基; R5是氢或卤素; R 6为氢，甲基，羟基，烷酰基，烷酰氧基或卤素。

30. 发明授权

US4265815A 17-(Substituted thio)androst-4-ene[16,17,-b]-[1,4]benzodioxin-3-ones 失效
标题翻译： 17-（取代的硫代）雄甾-4-烯[16,17，-b] - [1,4]苯并二恶英-3-酮
公开(公告)号：US4265815A
公开(公告)日：1981-05-05
申请号：US135823
申请日：1980-03-31
申请人： Ravi K. Varma
发明人： Ravi K. Varma
IPC分类号： A61K31/58 , A61P29/00 , C07J31/00 , C07J71/00 , C07J1/00
CPC分类号： C07J71/0005 , C07J31/003
摘要： Steroids having the formula ##STR1## are useful intermediates for the preparation of novel antiinflammatory agents having the formula ##STR2## In the above formulas, X is S, ##STR3## R.sub.1 is alkyl, aryl, arylalkyl or acyloxyalkyl; R.sub.2 is fluoro, chloro, bromo or iodo (all R.sub.2 groups are the same);R.sub.3 is hydrogen, fluoro, chloro, bromo or iodo;R.sub.4 is carbonyl, or .beta.-hydroxymethylene;R.sub.5 is hydrogen, methyl or fluorine; andR.sub.6 is chloro, bromo, alkoxy, aryloxy, alkylthio, or arylthio.
摘要翻译：具有式的类固醇是制备具有下式的新型抗炎剂的有用中间体：在上式中，X为S，R 1为烷基，芳基，芳基烷基或酰氧基烷基; R2是氟，氯，溴或碘（所有的R2基都相同）; R3是氢，氟，氯，溴或碘; R4是羰基或β-羟基亚甲基; R5是氢，甲基或氟; 并且R 6是氯，溴，烷氧基，芳氧基，烷硫基或芳硫基。

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