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21. 发明授权

US5476944A Derivatives of cyclic phenolic thioethers 失效
标题翻译：环状酚类硫醚的衍生物
公开(公告)号：US5476944A
公开(公告)日：1995-12-19
申请号：US245780
申请日：1994-05-19
申请人： Richard A. Partis , Richard A. Mueller , Francis J. Koszyk , Richard M. Weier
发明人： Richard A. Partis , Richard A. Mueller , Francis J. Koszyk , Richard M. Weier
IPC分类号： C07C323/17 , C07C323/20 , C07C323/22 , C07C323/52 , C07C323/60 , C07D213/40 , C07D307/18 , C07D307/20 , C07D493/04 , C07D213/02 , A61K31/38 , A61K31/44 , C07D335/02
CPC分类号： C07D213/40 , C07C323/17 , C07C323/20 , C07C323/22 , C07C323/52 , C07C323/60 , C07D307/18 , C07D307/20 , C07D493/04 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要： The present invention relates to derivatives of cyclic phenolic thioethers of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, which are inhibitors or stimulators of superoxide generation, and which may also inhibit cyclooxygenase and/or 5-lipoxygenase, to pharmaceutical compositions containing one or more of these compounds in combination with a pharmaceutically-acceptable carrier, and to medical methods of treatment employing these compounds.
摘要翻译：本发明涉及以下化学式的环状酚硫醚衍生物及其药学上可接受的盐，其为抑制剂或超氧化物产生的刺激剂，并且还可以将环氧合酶和/或5-脂氧合酶抑制于含有这些化合物中的一种或多种与药学上可接受的载体组合，以及使用这些化合物的医疗治疗方法。

22. 发明授权

US5451604A Halogenated phenylacetonitrile alkylaminoalkylphenyl compounds as immunosuppressives 失效
标题翻译：卤代苯乙腈烷基氨基烷基苯基化合物作为免疫抑制剂
公开(公告)号：US5451604A
公开(公告)日：1995-09-19
申请号：US97809
申请日：1993-07-26
申请人： Richard A. Mueller , Thomas E. Barta , John P. McKearn , Susan A. Gregory , Richard A. Partis , Francis J. Koszyk
发明人： Richard A. Mueller , Thomas E. Barta , John P. McKearn , Susan A. Gregory , Richard A. Partis , Francis J. Koszyk
IPC分类号： C07C255/42 , A61K31/275 , C07C247/06 , C07C255/35
CPC分类号： C07C255/42 , C07C2101/10
摘要： A class of halogenated phenylacetonitrile alkylaminoalkylphenyl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula ##STR1## wherein m is a number selected from three to five, inclusive; wherein n one or two; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl and phenethyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl and phenethyl; wherein each of R.sup.3 through R.sup.7 is selected from hydrido, fluoro, chloro, bromo, azide, trifluoromethyl, difluorochloromethyl, 1,1-difluoroethyl, 2,2,2-trifluoroethyl, perfluoroethyl and 2,2,2,3-tetrafluoropropyl; with the proviso that at least one of R.sup.3 through R.sup.7 is selected from fluoro and trifluoromethyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类具有免疫抑制特性的卤代苯基乙腈烷基氨基烷基苯基化合物。该类化合物可用于减少移植器官的受体排斥和治疗自身免疫性或炎性疾病。特别感兴趣的化合物具有下式：其中m是选自三至五的数字，包括端值; 其中n个或两个; 其中R1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，叔丁基，异丁基，正戊基，异戊基，环丙基，环丁基，环戊基，环己基，环丙基甲基，环丁基甲基，环戊基甲基，环己基甲基，苄基和苯乙基; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，叔丁基，异丁基，正戊基，异戊基，环丙基，环丁基，环戊基，环己基，环丙基甲基，环丁基甲基，环戊基甲基，环己基甲基，苄基和苯乙基; 其中R3至R7各自选自氢，氟，氯，溴，叠氮化物，三氟甲基，二氟氯甲基，1,1-二氟乙基，2,2,2-三氟乙基，全氟乙基和2,2,2,3-四氟丙基; 条件是R3至R7中的至少一个选自氟和三氟甲基; 或其互变异构体或其药学上可接受的盐。

23. 发明授权

US5334616A Cyclic phenolic thioethers compounds which are useful in treating allergies and inflammation 失效
标题翻译：可用于治疗过敏和炎症的环状酚类硫醚化合物
公开(公告)号：US5334616A
公开(公告)日：1994-08-02
申请号：US80941
申请日：1993-06-22
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： C07C323/20 , C07C323/52 , C07C323/60 , C07C323/65 , C07D213/40 , C07D307/20 , A61K31/34 , C07D305/04
CPC分类号： C07D213/40 , C07C323/20 , C07C323/52 , C07C323/60 , C07C323/65 , C07D307/20 , C07C2101/08 , C07C2101/14 , C07C2103/66 , C07C2103/74
摘要： The compounds of the present invention comprise substituted phenolic thioethers represented by the formula(I) and the radicals are defined in the claims: ##STR1## The compounds of the present invention are useful in the treatment of local and systemic inflammation and allergy reactions.
摘要翻译：本发明的化合物包括由式（I）表示的取代的酚类硫醚，并且所述基团在权利要求书中定义。本发明的化合物可用于治疗局部和全身炎症和过敏反应。

24. 发明授权

US5298514A Phenolic thioetheramides 失效
标题翻译：酚类硫醚酰胺
公开(公告)号：US5298514A
公开(公告)日：1994-03-29
申请号：US943166
申请日：1992-09-10
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/4468 , A61K31/495 , A61K31/50 , A61P29/00 , A61P37/08 , C07D20060101 , C07D211/16 , C07D211/58 , C07D213/40 , C07D279/12 , C07D295/18 , C07D295/185 , C07D211/72
CPC分类号： C07D213/40 , C07D211/16 , C07D295/185
摘要： The present invention relates to phenolic thioetheramides of the formula ##STR1## wherein R.sup.1 and R.sup.2 are tert-alkyl or phenyl, Alk.sup.1 and Alk.sup.2 are alkylene; X is sulfur or oxygen, m is 0, 1, or 2; and R is ##STR2## wherein R.sup.3 and R.sup.4 are hydrogen or alkyl and Alk.sup.3 is alkylene.
摘要翻译：本发明涉及下式的酚硫醚酰胺，其中R1和R2是叔烷基或苯基，Alk1和Alk2是亚烷基; X是硫或氧，m是0,1或2; 其中R 3和R 4是氢或烷基，而Alk 3是亚烷基。

25. 发明授权

US5280047A 2-(4-substituted)phenylmethylene derivatives and methods of use 失效
标题翻译： 2-（4-取代）苯基亚甲基衍生物和使用方法
公开(公告)号：US5280047A
公开(公告)日：1994-01-18
申请号：US42214
申请日：1993-04-02
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： A61K31/12 , A61K31/215 , A61U31/12
CPC分类号： A61K31/12 , A61K31/215
摘要： The present invention relates to methods of using and pharmaceutical compositions containing compounds of Formula I: ##STR1## wherein R.sup.1 is hydrogen, --COR.sup.4 wherein R.sup.4 is C.sub.1 -C.sub.4 alkyl, or --COOR.sup.5 wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl; R.sup.2 is C.sub.1 -C.sub.4 alkyl, phenyl, or --OR.sup.6 wherein R.sup.6 is C.sub.1 -C.sub.4 alkyl; and R.sup.3 is C.sub.6 -C.sub.8 alkyl, halogen, or NO.sub.2 ; with the proviso that when R.sup.1 is hydrogen, R.sup.2 is C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable carrier. Compounds of Formula I and pharmaceutical compositions containing them are inhibitors of 5-lipoxygenase and are useful in the treatment of conditions mediated by leukotrienes such as inflammation, allergy, hypersensitivity reactions, and proliferative skin diseases such as psoriasis.
摘要翻译：本发明涉及使用含有式I化合物的药物组合物的方法：（*化学结构*）I其中R1是氢，-COR4，其中R4是C1-C4烷基，或-COOR5，其中R5是C1-C4烷基; R2是C1-C4烷基，苯基或-OR6，其中R6是C1-C4烷基; R3为C6-C8烷基，卤素或NO2; 条件是当R1是氢时，R2是C1-C4烷基; 和药学上可接受的载体。式I化合物和含有它们的药物组合物是5-脂氧合酶的抑制剂，并且可用于治疗由白细胞三烯介导的病症，例如炎症，过敏，超敏反应和增殖性皮肤疾病如牛皮癣。

26. 发明授权

US5198435A Azabicycloalkyl and azatricycloalkyl amides 失效
标题翻译：偶氮二环烷基和氮杂环烷基酰胺
公开(公告)号：US5198435A
公开(公告)日：1993-03-30
申请号：US669543
申请日：1991-03-14
申请人： Richard A. Mueller , Richard A. Partis , James R. Deason
发明人： Richard A. Mueller , Richard A. Partis , James R. Deason
IPC分类号： C07D295/185 , C07D453/02
CPC分类号： C07D295/185 , C07D453/02
摘要： The compounds of this invention are bicyclic, tricyclic, azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided than n+m+p is equal to or less than 10; x is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group consisting of a bicycloalkylamino, tricycloalkylamino, azabicycloalkyl, azatricycloalkyl, azabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino. The compounds are useful as anti-inflammatory and anti-allergy agents.
摘要翻译：本发明的化合物是由下式表示的双环，三环，氮杂双环和氮杂三环酰胺：其中：R 1和R 2是由卤素，苯基，取代的苯基和取代的苯基组成的组中相同或不同的成员其中n，m和p独立地为n + m + p等于或小于10提供的1至8的整数; x是硫代，亚磺酰基或磺酰基; Alk是直链或支链低级亚烷基; R 3选自二环烷基氨基，三环烷基氨基，氮杂双环烷基，氮杂环烷基，氮杂双环烷基氨基，氮杂三环烷基氨基或二环烷基氨基。该化合物可用作抗炎和抗过敏剂。

27. 发明授权

US5157053A Bicycloalky, tricycloalkyl, azabicycloalkyl, and azatricycloalkyl thio amides used to treat inflammation, allergy, asthma and skin disorders 失效
标题翻译：用于治疗炎症，过敏，哮喘和皮肤疾病的双环烷基，三环烷基，氮杂双环烷基和氮杂三环烷基硫代酰胺
公开(公告)号：US5157053A
公开(公告)日：1992-10-20
申请号：US600342
申请日：1990-10-19
申请人： Richard A. Mueller , Richard A. Partis , James R. Deason
发明人： Richard A. Mueller , Richard A. Partis , James R. Deason
IPC分类号： C07D295/185 , C07D453/02
CPC分类号： C07D295/185 , C07D453/02 , Y10S514/826 , Y10S514/863 , Y10S514/864 , Y10S514/886
摘要： The compounds of this invention are bicyclic, tricyclic, azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; x is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group-consisting of a bicycloalkylamino, tricycloalkylamino, azabicycloalkyl, azatricycloalkyl, aszabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino, The compounds are useful as anti-inflammatory and anti-allergy agents.
摘要翻译：本发明的化合物是由下式表示的双环，三环，氮杂双环和氮杂三环酰胺：其中：R 1和R 2是由卤素，苯基，取代的苯基和取代的苯基组成的组中相同或不同的成员其中n，m和p独立地为1至8的整数，条件是n + m + p等于或小于10; x是硫代，亚磺酰基或磺酰基; Alk是直链或支链低级亚烷基; R3选自二环烷基氨基，三环烷基氨基，氮杂双环烷基，氮杂环烷基，二氮杂环烷基氨基，氮杂环烷基氨基或二环烷基氨基。该化合物可用作抗炎和抗过敏剂。

28. 发明授权

US5030638A Method of antiviral enhancement 失效
标题翻译：抗病毒增强方法
公开(公告)号：US5030638A
公开(公告)日：1991-07-09
申请号：US554494
申请日：1990-07-19
申请人： Richard A. Partis , Richard A. Mueller
发明人： Richard A. Partis , Richard A. Mueller
IPC分类号： A61K31/445 , A61P31/12 , A61P43/00 , C07D211/46
CPC分类号： A61K31/445
摘要： A method for providing enhanced antiviral activity with N-alkyl derivatives of 1,5-dideoxy-1,5-imino-D-glucitol is disclosed which comprises selectively increasing the alkyl chain length to at least 5 carbon atoms and up to about 10 carbon atoms to thereby improve the spectrum of enzyme inhibitory activity and the in vivo half life.

29. 发明授权

US4847305A Phenolic thioethers as inhibitors of 5-lipoxygenase 失效
标题翻译：酚硫醚作为5-脂氧合酶的抑制剂
公开(公告)号：US4847305A
公开(公告)日：1989-07-11
申请号：US194769
申请日：1988-05-23
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： A61K31/10 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C317/22 , C07C323/20 , C07C331/10
CPC分类号： A61K31/10 , C07C317/22 , C07C323/20 , C07C331/10
摘要： The compounds of the present invention comprise substituted phenolic thioether derivatives that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.

30. 发明授权

US4755524A Novel phenolic thioethers as inhibitors of 5-lipoxygenase 失效
标题翻译：新型酚类硫醚作为5-脂氧合酶的抑制剂
公开(公告)号：US4755524A
公开(公告)日：1988-07-05
申请号：US1259
申请日：1987-01-15
申请人： Richard A. Mueller , Richard A. Partis , James R. Deason
发明人： Richard A. Mueller , Richard A. Partis , James R. Deason
IPC分类号： C12N9/99 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/395 , A61K31/41 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C313/00 , C07C317/14 , C07C317/22 , C07C317/28 , C07C317/44 , C07C323/12 , C07C323/20 , C07C323/22 , C07C323/25 , C07C323/31 , C07C323/52 , C07C323/65 , C07C327/22 , C07C331/08 , C07C331/10 , C07D257/04 , C07C149/40 , A61K37/10
CPC分类号： C07D257/04 , C07C317/44 , C07C323/20 , C07C323/22 , C07C323/25 , C07C323/52 , C07C323/65 , C07C327/22 , C07C331/10
摘要： The compounds of the present invention comprise substituted phenolic thioethers represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different and independently represent tert-alkyl or phenyl; A represents methylene or methylene substituted by alkyl, dialkyl or hydroxy, provided that when A includes hydroxymethylene, the hydroxymethylene group is not adjacent to a heteroatom; B represents sulfur, sulfoxide, sulfone, oxygen, --NH-- or nitrogen substituted by alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl; C represents methylene or methylene substituted by alkyl; R.sub.3 represents CO.sub.2 H, CO.sub.2 -alkyl or a tetrazole group; m is 0 or 1, n is 2, 3 or 4 and p is 1, 2 or 3; and the pharmaceutically acceptable salts thereof. The compounds of the present invention are specific inhibitors of 5-lipoxygenase and, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
摘要翻译：本发明的化合物包括由下式表示的取代的酚类硫醚：其中：R 1和R 2相同或不同并且独立地代表叔烷基或苯基; A表示亚烷基或被烷基，二烷基或羟基取代的亚甲基，条件是当A包括羟基亚甲基时，羟基亚甲基不与杂原子相邻; 苯基，苄基，取代的苯基或取代的苄基取代的硫，亚砜，砜，氧，-NH-或氮。 C表示亚烷基或被烷基取代的亚甲基; R3表示CO 2 H，CO 2 - 烷基或四唑基; m为0或1，n为2,3或4，p为1,2或3; 及其药学上可接受的盐。本发明的化合物是5-脂氧合酶的特异性抑制剂，因此可用于治疗局部和全身炎症，变态反应和过敏反应以及涉及5-脂氧合酶代谢途径中形成的药物的其它病症。

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