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1. 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。

2. 发明授权

US4728670A Biphenyl hydroxamic acids 失效
标题翻译：联苯异羟肟酸
公开(公告)号：US4728670A
公开(公告)日：1988-03-01
申请号：US870565
申请日：1986-06-04
申请人： Martin F. Haslanger , Ravi K. Varma , Eric M. Gordon
发明人： Martin F. Haslanger , Ravi K. Varma , Eric M. Gordon
IPC分类号： C12N9/99 , A61K31/17 , A61K31/27 , A61P11/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C239/00 , C07C271/08 , C07C275/04 , C07C275/18 , C07C275/64 , C07C325/00 , C07C333/12 , C07C83/10 , A61K31/265
CPC分类号： C07C275/64
摘要： Biphenyl hydroxamic acids are provided having the structure ##STR1## wherein m is 1 to 7, X is S, O or NH, R is H, lower alkyl, aryl, aralkyl or cycloalkyl and R.sup.1 is H, lower alkyl, aryl, aralkyl, cycloalkyl, alkanoyl or aroyl.These compounds are inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
摘要翻译：提供具有以下结构的联苯异羟肟酸，其中m为1至7，X为S，O或NH，R为H，低级烷基，芳基，芳烷基或环烷基，R 1为H，低级烷基，芳基，芳烷基，环烷基，烷酰基或芳酰基。这些化合物是DELTA5-脂肪氧合酶的抑制剂，因此可用作抗过敏剂。

3. 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。

4. 发明授权

US4695586A 7-oxabicyclo(2.2.1)heptane-based derivatives useful as antiinflammatory, antiasthma and antipsoratic agents 失效
标题翻译： 7-氧杂二环（2.2.1）庚烷基衍生物，可用作抗炎，抗哮喘和抗肿瘤药物
公开(公告)号：US4695586A
公开(公告)日：1987-09-22
申请号：US910597
申请日：1986-09-23
申请人： Ravi K. Varma , Sam T. Chao , Eric M. Gordon
发明人： Ravi K. Varma , Sam T. Chao , Eric M. Gordon
IPC分类号： A61K31/34 , A61P37/08 , C07D493/08 , A61K31/557 , C07D307/00
CPC分类号： C07D493/08
摘要： 7-Oxabicyclo(2.2.1)heptane-based N-hydroxy-N-alkyl (or aryl) ureas, carbamic acids and carbamothioic acids are disclosed having the general formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, alkenyl, aryl or aralkyl; R.sub.2 is hydrogen, lower alkyl, aralkyl, alkanoyl or aroyl; R.sub.3 is lower alkyl, alkenyl or alkynyl; A is --CH.sub.2 --CH.dbd.CH-- or a single bond; X is oxygen, sulfur or NH; n is an integer from 1 to 8; and all stereoisomers thereof.These new compounds have been found to simultaneously inhibit the enzymes arachidonic acid cyclooxygenase and arachidonic acid 5-lipoxygenase and are therefore useful as antiinflammatory, antiasthma and antipsoriatic agents.
摘要翻译：公开了具有通式“IMAGE”的7-氧杂双环（2.2.1）庚烷基N-羟基-N-烷基（或芳基）脲，氨基甲酸和氨基甲酸，其中R 1是氢，低级烷基，烯基，芳基或芳烷基 R2是氢，低级烷基，芳烷基，烷酰基或芳酰基; R3是低级烷基，烯基或炔基; A是-CH 2 -CH = CH-或单键; X是氧，硫或NH; n是1至8的整数; 及其所有立体异构体。已经发现这些新化合物同时抑制花生四烯酸环加氧酶和花生四烯酸5-脂氧合酶，因此可用作抗炎，抗哮喘和抗牛皮癣药。

5. 发明授权

US5264455A Sulfur-substituted mevinic acid derivatives 失效
标题翻译：硫取代的维甲酸衍生物
公开(公告)号：US5264455A
公开(公告)日：1993-11-23
申请号：US724272
申请日：1991-07-01
申请人： Ravi K. Varma , Jeffrey O. Saunders , Sam T. Chao , Eric M. Gordon , Dinos P. Santafianos
发明人： Ravi K. Varma , Jeffrey O. Saunders , Sam T. Chao , Eric M. Gordon , Dinos P. Santafianos
IPC分类号： C07C317/46 , C07C323/61 , C07C323/65 , A61K31/35 , A61K31/215 , C07D339/00
CPC分类号： C07C317/46 , C07C323/61 , C07C323/65 , C07C2101/08 , C07C2101/14 , C07C2102/10
摘要： X is hydrogen or --S(O).sub.m --R.sup.1 and Y is hydrogen or S(O).sub.n --R.sup.2, except that X and Y are not both hydrogen, or one of X and Y is --S--alkyl--SH and the other is hydrogen; ##STR2## and the remaining symbols are as defined in the specification.
摘要翻译：其作为细胞选择性HMG-CoA还原酶抑制剂具有活性，因此可用作抗高胆固醇血症药。在上式中，X是氢或-S（O）m -R 1，Y是氢或S（O）n -R 2，不同之处在于X和Y不同时为氢，X和Y之一为-S- 烷基-SH，另一个是氢; ＆lt; IMAGE＆gt;其余符号如说明书中所定义。

6. 发明授权

US5177104A 6-.alpha.-hydroxy derivatives of mevinic acids 失效
标题翻译： 6-（ALPHA） - 甲氧基衍生物
公开(公告)号：US5177104A
公开(公告)日：1993-01-05
申请号：US503576
申请日：1990-04-03
申请人： Ravi K. Varma , Sam T. Chao , Eric M. Gordon
发明人： Ravi K. Varma , Sam T. Chao , Eric M. Gordon
IPC分类号： A61K31/22 , A61K31/365 , A61P3/06 , A61P9/10 , A61P43/00 , C07C69/013 , C07C69/03 , C07C69/675 , C07C69/732 , C07D309/30
CPC分类号： C07D309/30 , C07C69/732 , Y10S514/824
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof have been found to possess activity as cell-selective HMG-CoA reductase inhibitors, thus making them useful as antihypercholesterolemic agents. In the above formula, ##STR2## R.sup.1 is hydrogen, alkyl, cycloalkyl, aryl or arylalkyl; and R.sup.2 is hydrogen, alkyl, ammonium, or alkali metal.

7. 发明授权

US4695585A 7-oxabicyclo(2.2.1)heptane analogs useful as inhibitors of 5-lipoxygenase and cyclooxygenase 失效
标题翻译：可用作5-脂氧合酶和环氧合酶抑制剂的7-氧杂二环（2.2.1）庚烷类似物
公开(公告)号：US4695585A
公开(公告)日：1987-09-22
申请号：US910583
申请日：1986-09-23
申请人： Ravi K. Varma , Eric M. Gordon
发明人： Ravi K. Varma , Eric M. Gordon
IPC分类号： A61K31/34 , A61P11/08 , A61P29/00 , A61P37/08 , C07D493/08 , C07D307/00
CPC分类号： C07D493/08 , Y10S514/826 , Y10S514/863
摘要： A compound of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy, alkoxy or aryloxy; R.sub.2 is hydrogen, hydroxy, alkoxy or aryloxy; or wherein R.sub.1 and R.sub.2 taken together is an aromatic ring; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is lower alkyl, substituted alkyl, alkenyl or alkynyl; X is amino, alkylamino, alkanoylamino, oxygen or a single bond; A is CH.sub.2 --CH.dbd.CH or a single bond; and n is an integer from 0 to 9, with the proviso that when A is a single bond, n is an integer from 1 to 9 including all stereoisomers thereof.These new compounds have been found to simultaneously inhibit the arachidonic acid enzymes 5-lipoxygenase and cyclooxygenase and as such are useful, for example, as antiinflammatory agents.
摘要翻译：式IMA的化合物，其中R 1是氢，羟基，烷氧基或芳氧基; R2是氢，羟基，烷氧基或芳氧基; 或其中R 1和R 2一起为芳环; R3是氢或低级烷基; R4是低级烷基，取代的烷基，烯基或炔基; X是氨基，烷基氨基，烷酰基氨基，氧或单键; A是CH 2 -CH = CH或单键; 且n为0至9的整数，条件是当A为单键时，n为1至9的整数，包括其所有立体异构体。已经发现这些新化合物同时抑制花生四烯酸5-脂氧合酶和环氧合酶，因此可用作例如抗炎剂。

8. 发明授权

US5049577A 2-pyrrolidone substituted dihydroxy alkanoic, alkenoic and alkynoic acids, compositions and HMG-CoA reductase inhibition therewith 失效
标题翻译： 2-吡咯烷酮取代的二羟基链烷酸，链烯酸和炔酸，组合物和HMG-CoA还原酶抑制
公开(公告)号：US5049577A
公开(公告)日：1991-09-17
申请号：US471461
申请日：1990-01-29
申请人： Ravi K. Varma , Eric M. Gordon , Sam T. Chao
发明人： Ravi K. Varma , Eric M. Gordon , Sam T. Chao
IPC分类号： C07D207/26 , C07D209/96
CPC分类号： C07D207/26 , C07D209/96
摘要： Antihypercholesterolemic activity has been discovered in compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein: Z is ##STR2## X is lower alkyl, lower alkenyl, or lower alkenyl; R.sup.1 is hydrogen, alkyl, alkenyl, aryl, alkylaryl, or substituted aryl having one or more substituents; andone of R.sup.2 and R.sup.3 is hydrogen and the other is hydrogen, alkyl, alkenyl, aryl, alkylaryl or alkenyl aryl; or R.sup.2 and R.sup.3 are both lower alkyl; or R.sup.2 and R.sup.3 together complete a substituted or unsubstituted hydrocarbon ring that is cycloalkyl or cycloalkenyl with substituents as defined in the specification.
摘要翻译：抗高血胆固醇活性已经在下式化合物及其药学上可接受的盐中发现，其中：Z是低级烷基，低级链烯基或低级链烯基; R1是氢，烷基，烯基，芳基，烷基芳基或具有一个或多个取代基的取代的芳基; R2和R3中的一个是氢，另一个是氢，烷基，烯基，芳基，烷基芳基或烯基芳基; 或R 2和R 3均为低级烷基; 或者R 2和R 3一起完成取代或未取代的烃环，其是具有如说明书中定义的取代基的环烷基或环烯基。

9. 发明授权

US4782085A Arylhydroxamates and use thereof in treating allergies 失效
标题翻译：芳基羟基化合物及其在治疗过敏中的用途
公开(公告)号：US4782085A
公开(公告)日：1988-11-01
申请号：US78437
申请日：1987-07-27
申请人： Ravi K. Varma , Eric M. Gordon
发明人： Ravi K. Varma , Eric M. Gordon
IPC分类号： C07C69/76 , C07D213/56 , C07C81/00 , C07C83/10
CPC分类号： C07C69/76 , C07D213/56
摘要： Arylhydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkyl, or aralkyl;R.sup.2 is hydrogen, lower alkyl, aryl, cycloalkyl, alkanoyl or aroyl;m is 2 to 8; andZ is ##STR2## wherein R.sup.3 is OH, COOH ##STR3## These compounds are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
摘要翻译：提供了具有结构的芳基羟基化合物，其中R 1是氢，低级烷基，芳基，低级烯基，环烷基或芳烷基; R2是氢，低级烷基，芳基，环烷基，烷酰基或芳酰基; m为2〜8; Z是其中R 3是OH，COOH，这些化合物可用作DELTA5-脂肪氧合酶的抑制剂，因此可用作抗过敏剂。

10. 发明授权

US4707494A 7-oxabicyclo(2.2.1)heptane compounds useful in the treatment of inflammation 失效
标题翻译：可用于治疗炎症的7-氧杂二环（2.2.1）庚烷化合物
公开(公告)号：US4707494A
公开(公告)日：1987-11-17
申请号：US900564
申请日：1986-08-26
申请人： Ravi K. Varma , Carl P. Ciosek , Eric M. Gordon
发明人： Ravi K. Varma , Carl P. Ciosek , Eric M. Gordon
IPC分类号： A61K31/34 , A61P25/04 , A61P29/00 , C07D493/08 , A61K31/557 , C07D307/00
CPC分类号： C07D493/08
摘要： 7-Oxabicyclo(2.2.1)heptane analogs are disclosed having the general formula ##STR1## wherein R.sub.1 is lower alkyl, alkenyl, substituted alkenyl or alkynyl; R.sub.2 is lower alkyl, alkenyl or alkynyl; A is --CH.sub.2 --CH.dbd.CH-- or a single bond; X is --CH.sub.2, --CH(CH.sub.3) or --C(CH.sub.3).sub.2 ; n is an integer from 0 to 9, with the proviso that when A is a single bond, n is an integer from 1 to 9; including all stereoisomers.These new compounds have been found to be inhibitors of arachidonic acid cyclooxygenase and are therefore useful as antiinflammatory antipyretic and analgesic agents.
摘要翻译：公开了具有通式为“IMAGE”的7-氧杂双环（2.2.1）庚烷类似物，其中R 1是低级烷基，烯基，取代的链烯基或炔基; R2是低级烷基，烯基或炔基; A是-CH 2 -CH = CH-或单键; X是-CH 2，-CH（CH 3）或-C（CH 3）2; n为0〜9的整数，条件是当A为单键时，n为1〜9的整数，包括所有立体异构体。已经发现这些新化合物是花生四烯酸环氧合酶的抑制剂，因此可用作抗炎解热和止痛剂。

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