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41. 发明授权

US06545021B1 Use of substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds for treating hepatitis virus infections 有权
标题翻译：使用取代的-1,5-二脱氧-1,5-亚氨基-D-葡萄糖醇化合物治疗肝炎病毒感染
公开(公告)号：US06545021B1
公开(公告)日：2003-04-08
申请号：US09503945
申请日：2000-02-14
申请人： Richard A. Mueller , Martin L. Bryant , Richard A. Partis
发明人： Richard A. Mueller , Martin L. Bryant , Richard A. Partis
IPC分类号： A61K31445
CPC分类号： A61K31/436 , A61K31/444 , A61K31/445 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61K45/06 , Y10S514/885
摘要： N-Substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds of Formula I are effective in treatment of hepatitis infections, including hepatitis B and hepatitis C. In treating hepatitis infections, the compounds of Formula I may be used alone, or in combination with another antiviral agent selected from among nucleosides, nucleotides, immunomodulators, immunostimulats or various combinations of such other agents.
摘要翻译：式I的N-取代的-1,5-二脱氧-1,5-亚氨基-D-葡萄糖醇化合物在治疗肝炎感染中是有效的，包括乙型肝炎和丙型肝炎。在治疗肝炎感染中，式I化合物可以是或者与选自核苷，核苷酸，免疫调节剂，免疫调节剂或其它药剂的各种组合的另一种抗病毒剂组合使用。

42. 发明授权

US5342838A Phenolic thioetheramides 失效
标题翻译：酚类硫醚酰胺
公开(公告)号：US5342838A
公开(公告)日：1994-08-30
申请号：US164498
申请日：1993-12-09
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 , C07D
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; or ##STR3## wherein Y is CH, N, O, or S; R.sup.6 is hydrogen, alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl or a heterocyclic amine; and R.sup.7 is hydrogen or alkyl. The compounds inhibit 5-lipoxygenase and are useful in the treatment of inflammation and allergic conditions.
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; a）其中R 3和R 4是氢或烷基，Alk 3是亚烷基; 或 b）其中Y是CH，N，O或S; R6是氢，烷基，苯基，取代的苯基，苄基，取代的苄基或杂环胺; 并且R 7是氢或烷基。该化合物抑制5-脂氧合酶，可用于治疗炎症和过敏症状。

43. 发明授权

US5145992A Process and preparation of .alpha.-alkoxy acetic acids and their salts 失效
标题翻译： α-烷氧基乙酸及其盐的制备与制备
公开(公告)号：US5145992A
公开(公告)日：1992-09-08
申请号：US695676
申请日：1991-05-06
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： C07C51/367 , C07C319/20 , C07C323/20
CPC分类号： C07C51/367 , C07C319/20
摘要： A process for producing an .alpha.-alkoxy acetic acids and salts thereof which comprises reacting an alcohol of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 can be hydrogen, alkyl, alkoxy, halo, phenyl, substituted phenyl, or hydroxy; A can be S, O or --CH.sub.2 --; and Alk is straight or branched chain alkylene, with a base in an aprotic solvent, then reacting the resulting alkoxide with a monohaloacetic acid ester to give an alkoxyacetate followed by reaction of the alkoxyacetate with a hydrogen halide, organic acid or Lewis acid in nitromethane to give the corresponding .alpha.-alkoxyacetic acid which then may be recovered or may optionally be converted to the corresponding salt by contracting the .alpha.-alkoxyacetic acid with a base.

44. 发明授权

US5066679A Phenolic thioalkylamides as inhibitors of 5-lipoxygenase 失效
标题翻译：酚硫代烷基酰胺作为5-脂氧合酶的抑制剂
公开(公告)号：US5066679A
公开(公告)日：1991-11-19
申请号：US321034
申请日：1989-03-09
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： A61K31/165
CPC分类号： A61K31/165
摘要： The compounds of the present invention comprise substituted phenolic thioalkylamides 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.
摘要翻译：本发明的化合物包含取代的酚硫代烷基酰胺，其是5-脂氧合酶的特异性抑制剂，因此其可用于治疗局部和全身炎症，变态反应和超敏反应以及其中在5-脂氧合酶中形成的药物的其它病症涉及代谢途径。

45. 发明授权

US5013864A Process for preparation of .alpha.-alkoxy acetic acids and their salts 失效
标题翻译： α-烷氧基乙酸及其盐的制备方法
公开(公告)号：US5013864A
公开(公告)日：1991-05-07
申请号：US447766
申请日：1989-12-08
申请人： Arthur L. Campbell , Richard A. Mueller , John S. Ng , Richard A. Partis
发明人： Arthur L. Campbell , Richard A. Mueller , John S. Ng , Richard A. Partis
IPC分类号： C07C51/367 , C07C59/125 , C07C59/13 , C07C59/66 , C07C319/20 , C07C323/12 , C07C323/20
CPC分类号： C07C323/20 , C07C51/367
摘要： A process for producing an .alpha.-alkoxy acetic acids and salts thereof which comprises reacting an alcohol of the formula R--OH wherein R is alkyl, substituted alkyl, or cycloalkyl, or cycloalkyl alkyl with a base in an aprotic organic solvent to give an alkoxide followed by removal of the organic solvent and reaction of the alkoxide with a salt of a monohaloacetic acid in a polar aprotic solvent such as DMSO to give the corresponding alkoxyacetate salt which then may be recovered or may optionally be converted to the corresponding acid by contacting the alkoxy acetate salt with an acid.

46. 发明授权

US4803294A Process and intermediates for the preparation of halogenated protease inhibitors 失效
标题翻译：用于制备卤化蛋白酶抑制剂的方法和中间体
公开(公告)号：US4803294A
公开(公告)日：1989-02-07
申请号：US114186
申请日：1987-10-29
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： C07C69/76 , C07C69/78
CPC分类号： C07C69/78
摘要： This invention relates to novel intermediate compounds which are useful for producing the halogenated protease inhibitors that are the subject matter of U.S. Pat. No. 4,469,885. In particular, the invention relates to novel methods and intermediates for making said protease inhibitors, the intermediate compounds being of the formula: ##STR1## wherein R.sub.1 is: (a) straight or branched chain lower alkyl having 1-6 carbon atoms; or(b) H;wherein R.sub.6 is:(a) straight or branched chain higher alkyl having 13-25 carbon atoms; or(b) straight or branched chain higher alkenyl having 13-25 carbon atoms;wherein R.sub.5 is:(a) straight or branched chain lower alkyl having 1-6 carbon atoms; or(b) benzyl;wherein R.sub.7 is:(a) straight or branched chain lower alkyl having 1-6 carbon atoms; or(b) H;wherein R.sub.2 is:(a) --Cl, --Br, or --I; or(b) --CF.sub.3.

47. 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。

48. 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。

49. 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。

50. 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。

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