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41. 发明授权

US4499295A Protease inhibitors 失效
公开(公告)号：US4499295A
公开(公告)日：1985-02-12
申请号：US492842
申请日：1983-05-09
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： C07C69/88 , A61K31/19 , A61K31/235 , A61P43/00 , C07C51/00 , C07C65/01 , C07C65/03 , C07C65/19 , C07C65/21 , C07C65/28 , C07C65/40 , C07C67/00 , C07C69/84 , C07C69/92 , C07D295/02 , C07D295/03 , C12N9/99 , C07C69/76
CPC分类号： C07D295/03 , C07C65/01 , C07C65/19 , C07C65/40
摘要： This invention relates to methods of preventing or reducing the degradation of elastin and other proteins and thereby preventing or retarding the disease states caused by said degradation by administering compounds of the formula: ##STR1## or their pharmacologically acceptable salts.

42. 发明授权

US4469885A Halogenated protease inhibitors 失效
标题翻译：卤化蛋白酶抑制剂
公开(公告)号：US4469885A
公开(公告)日：1984-09-04
申请号：US492843
申请日：1983-05-09
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： A61K31/19 , A61K31/235 , A61P43/00 , C07C45/46 , C07C49/807 , C07C51/00 , C07C63/00 , C07C63/70 , C07C63/74 , C07C65/00 , C07C65/01 , C07C65/32 , C07C67/00 , C07C69/00 , C07C69/76 , C07D263/00 , C07D263/10
CPC分类号： C07D263/10 , C07C45/46 , C07C49/807 , C07C63/70 , C07C63/74 , C07C65/01 , C07C65/32 , Y10S514/825
摘要： This invention relates to novel compounds for preventing or retarding the degradation of elastin or other proteins and therefore preventing or retarding the disease states caused by said degradation, of the formula: ##STR1## or its pharmacologically acceptable salts. The invention also relates to novel methods and intermediates for making the compounds.
摘要翻译：本发明涉及用于预防或延缓弹性蛋白或其它蛋白质降解并因此预防或延缓由所述降解引起的疾病状态的新颖化合物，其具有下式：其药理学上可接受的盐。本发明还涉及制备该化合物的新方法和中间体。

43. 发明授权

US5326907A 2-aminoethanesulfonic acid derivatives of 3,5-disubstituted-4-hydroxyphenolic thioethers 失效
标题翻译： 3,5-二取代-4-羟基苯酚硫醚的2-氨基乙磺酸衍生物
公开(公告)号：US5326907A
公开(公告)日：1994-07-05
申请号：US993329
申请日：1992-12-18
申请人： Richard A. Partis , Richard A. Mueller
发明人： Richard A. Partis , Richard A. Mueller
IPC分类号： C07C323/20 , C07C323/60 , C07C149/00
CPC分类号： C07C323/60 , C07C323/20
摘要： The present invention relates to compounds of the Formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl, halogen, or phenyl; Alk.sup.1 represents straight or branched chain alkylene of 2 to 10 carbon atoms which can optionally be substituted by hydroxy, provided that said hydroxy is not attached to a carbon which is adjacent to sulfur or oxygen, X represents sulfur or oxygen, and Alk.sup.2 represents straight or branched chain alkylene of 1 to 4 carbon atoms; and the pharmaceutically acceptable salts thereof. These compounds are specific 5-lipoxygenase inhibitors and are useful as anti-inflammatory and anti-allergy agents and in the treatment of conditions mediated by 5-lipoxygenase.
摘要翻译：本发明涉及式I（I）的化合物，其中R 1和R 2相同或不同并且独立地代表叔烷基，卤素或苯基; Alk1表示2-10个碳原子的直链或支链亚烷基，其可以任选地被羟基取代，条件是所述羟基不与硫或氧相邻的碳连接，X表示硫或氧，Alk2表示直链或 1至4个碳原子的支链亚烷基; 及其药学上可接受的盐。这些化合物是特异性的5-脂氧合酶抑制剂，可用作抗炎和抗过敏剂，并且用于治疗5-脂氧合酶介导的病症。

44. 发明授权

US5310745A Antiviral compounds 失效
标题翻译：抗病毒化合物
公开(公告)号：US5310745A
公开(公告)日：1994-05-10
申请号：US929325
申请日：1992-08-13
申请人： Richard A. Partis , Francis J. Koszyk , Richard A. Mueller
发明人： Richard A. Partis , Francis J. Koszyk , Richard A. Mueller
IPC分类号： C07D211/46 , C07D401/06 , C07D491/04 , A61K31/445
CPC分类号： C07D401/06 , C07D211/46 , C07D491/04
摘要： A method of inhibiting lentivirus is disclosed which comprises mammalian host susceptible to said lentivirus with a virally inhibitory effective amount of an O-acylated derivative of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aroyl derivatives in which from one to four of the free hydroxyl groups are O-acylated with carboxylic alkanoyl radicals selected from the group consisting of .omega.,.omega.,.omega.-trifluoroalkanoyl having from three to eight carbon atoms, carboxylic cycloalkanoyl groups having from four to eight carbon atoms and carboxylic acyclic alkanoyl groups having from two to ten carbon atoms, wherein the N-aroyl groups contain from 7 to 14 carbon atoms, the N-acyl groups contain from 4 to 8 carbon atoms and the N-alkyl groups contain from 1 to 14 carbon atoms.
摘要翻译：公开了一种抑制慢病毒的方法，其包括对所述慢病毒敏感的哺乳动物宿主，其具有病毒抑制有效量的1,5-二脱氧-1,5-亚氨基-D-葡萄糖醇的O-酰化衍生物及其N-烷基，N 酰基和N-芳酰基衍生物，其中1至4个游离羟基与选自具有3至8个碳原子的ω，ω，ω-三氟烷酰基的羧基烷酰基进行O-酰化，羧基环烷酰基具有4至8个碳原子和具有2至10个碳原子的羧酸非环烷酰基，其中N-芳酰基含有7至14个碳原子，N-酰基含有4至8个碳原子，烷基含有1至14个碳原子。

45. 发明授权

US5250567A Cyclic phenolic thioethers 失效
标题翻译：环状酚类硫醚
公开(公告)号：US5250567A
公开(公告)日：1993-10-05
申请号：US903832
申请日：1992-06-24
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
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): ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents O, S, or CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl and R.sup.6 is hydrogen, alkyl, heterocyclealkyl in which the hetercyclic ring may optionally be substituted; cycloalkyl; substituted cycloalkyl; phenyl; substituted phenyl; phenylalkyl; or substituted phenylalkyl; or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or R is (CH.sub.2).sub.t COOR.sup.7 wherein t is an integer from 1 to 4 and R.sup.7 is hydrogen or alkyl of 1 to 4 carbon atoms; and the pharmaceutically acceptable salts and stereoisomers or geometric isomers thereof. The compounds of the present invention are 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式（I）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; R3表示氢或烷基; X表示 - （CH 2）w B-（CH 2）y - ，其中B表示O，S或CH 2，w和y各自独立地为0至3的整数，条件是w + y的和等于或小于3; A表示O或S（O）n，其中n为0,1或2; p是1至4的整数; 和R表示烷基; 哦; OR4，其中R4是1-4个碳原子的烷基; NR5R6其中R5是氢或烷基，R6是氢，烷基，杂环烷基，其中杂环可以被任选取代; 环烷基取代的环烷基; 苯基; 取代的苯基; 苯基烷基; 或取代的苯基烷基; 或NR5R6一起形成可任选被取代的杂环; 或R为（CH 2）t COOR 7，其中t为1至4的整数，且R 7为氢或1至4个碳原子的烷基; 及其药学上可接受的盐和立体异构体或几何异构体。本发明的化合物是5-脂氧合酶的抑制剂，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。

46. 发明授权

US5147893A Cyclic phenolic thioethers 失效
标题翻译：循环酚醛树脂
公开(公告)号：US5147893A
公开(公告)日：1992-09-15
申请号：US697849
申请日：1991-05-09
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
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): ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; or (CH.sub.2).sub.t COOR.sup.7 wherein t is an integer from 1 to 4 and R.sup.7 is hydrogen or alkyl of 1 to 4 carbon atoms; and the pharmaceutically acceptable salts and stereoisomers or geometric isomers thereof. The compounds of the present invention are 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.

47. 发明授权

US5144037A 1,5-dideoxy-1,5-imino-d-glucitol derivatives 失效
标题翻译： 1,5-二脱氧-1,5-亚氨基-d-葡萄糖醇衍生物
公开(公告)号：US5144037A
公开(公告)日：1992-09-01
申请号：US639613
申请日：1991-01-10
申请人： Richard A. Partis , Francis J. Koszyk , Richard A. Mueller
发明人： Richard A. Partis , Francis J. Koszyk , Richard A. Mueller
IPC分类号： A61K31/445 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P31/12 , C07D211/46 , C07D401/06 , C07D405/06 , C07D409/06 , C07D491/04 , C07D491/056
CPC分类号： C07D401/06 , C07D211/46 , C07D405/06 , C07D409/06 , C07D491/04
摘要： Antiviral O-acylated derivatives of 1,5-dideoxy-1,5-imino-D-glucitol are disclosed that contain an N-alkyl or N-aroyl radical in which from one to four of the free hydroxyl groups are O-acylated with carboxylic alkanoyl radicals selected from the group consisting of .omega.,.omega.,.omega.-trifluoro alkanoyl having from three to eight carbon atoms, carboxylic cycloalkanoyl groups having from four to eight carbon atoms and carboxylic acyclic alkanoyl groups having from two to ten carbon atoms, wherein the N-aroyl radical is selected from the group consisting of p-decylbenzoyl, 3-(p-chlorophenoxy)propanoyl, 2-(acetyloxy)benzoyl, [1,1'-biphenyl]-4-ylcarbonyl, 2-thiopheneacetyl, trans-3-furanacryloyl, 3-methoxyphenylacetyl and 3-(trifluoromethyl)benzoyl, and wherein the N-alkyl contains from one to fourteen carbon atoms, provided that when N-alkyl contains from one to five carbon atoms the O-acylated groups are .omega.,.omega.,.omega.-trifluoro alkanoyl or carboxylic cycloalkanoyl.
摘要翻译：公开了1,5-二脱氧-1,5-亚氨基-D-葡萄糖醇的抗病毒O-酰化衍生物，其含有N-烷基或N-芳酰基，其中一至四个游离羟基与O- 选自具有3至8个碳原子的ω，ω，ω-三氟烷酰基，具有4至8个碳原子的羧基环烷酰基和2至10个碳原子的羧酸非环烷酰基的羧基烷酰基，其中 N-芳酰基选自对 - 癸基苯甲酰基，3-（对氯苯氧基）丙酰基，2-（乙酰氧基）苯甲酰基，[1,1'-联苯] -4-基羰基，2-噻吩乙酰基， 3-呋喃丙酰基，3-甲氧基苯乙酰基和3-（三氟甲基）苯甲酰基，其中N-烷基含有1至14个碳原子，条件是当N-烷基含有1至5个碳原子时，O-酰化基团为ω， ω，ω-三氟烷酰基或羧基环烷酰基。

48. 发明授权

US5019597A Bicycloalkyl tricycloalkyl, azabicycloalkyl and azatricycoalkyl amides 失效
标题翻译：双环烷基三环烷基，氮杂双环烷基和吖嗪基烷基酰胺
公开(公告)号：US5019597A
公开(公告)日：1991-05-28
申请号：US79731
申请日：1987-07-30
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 , A61K31/165 , C07C321/00
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 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, 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1至8的整数，条件是n + m + p等于或小于10; X是硫基，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。

49. 发明授权

US5003072A 1,5-dideoxy-1,5-imino-D-glucitol derivatives 失效
标题翻译： 1,5-二脱氧-1,5-亚氨基-D-葡萄糖醇衍生物
公开(公告)号：US5003072A
公开(公告)日：1991-03-26
申请号：US418091
申请日：1989-10-12
申请人： Richard A. Partis , Francis J. Koszyk , Richard A. Mueller
发明人： Richard A. Partis , Francis J. Koszyk , Richard A. Mueller
IPC分类号： A61K31/445 , A61P31/12 , C07D211/46 , C07D401/06 , C07D491/04 , C07D491/056
CPC分类号： C07D401/06 , C07D211/46 , C07D491/04 , Y10S514/885
摘要： O-acylated derivatives of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aryl derivatives in which from one to four of the free hydroxyl groups are acylated with acyl groups having from one to eight carbon atoms and in which the N-alkyl and N-acyl substituents contain from four to fourteen carbon atoms and the N-aryl substituents contain from seven to fourteen carbon atoms are disclosed, provided that when N-aryl is benzyloxycarbonyl, the O-acyl groups contain four to eight carbon atoms.

50. 发明授权

US4981853A Heterocyclic amides 失效
标题翻译：杂环酰胺
公开(公告)号：US4981853A
公开(公告)日：1991-01-01
申请号：US436526
申请日：1989-11-14
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： A61K31/495 , C07C319/02 , C07C323/20 , C07C323/52 , C07C331/10 , C07D207/16 , C07D295/18 , C07D295/185
CPC分类号： C07D295/185 , C07C319/02 , C07C323/00 , C07C331/10 , C07D207/16
摘要： The compounds of this invention are heterocyclic 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 q, r and t are independently an integer of from 1 to 8 provided that q+r+t is equal to or less than 10; Y is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene, and R.sub.3 is a heterocyclic amine represented by the formula: ##STR3## wherein R.sub.4 is selected from the group consisting of hydrogen, lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, carboxyl or carboxyloweralkyl; X is selected from the group consisting of N-R.sub.4, O and CH.sub.2 ; m is 2 or 3; n is 2 or 3 when X is O or N-R.sup.4, and n is 1 to 3 when X is CH.sub.2 ; p is 0 to 2; and the pharmaceutically acceptable salts thereof. The compounds are anti-inflammatory and anti-allergy agents.
摘要翻译：本发明的化合物是由下式表示的杂环酰胺：其中：R 1和R 2是由卤素，苯基，取代的苯基和基团组成的组中相同或不同的成员，其中q，r和t 独立地为1〜8的整数，条件是q + r + t等于或小于10; Y是硫代，亚磺酰基或磺酰基; Alk是直链或支链低级亚烷基，R3是下式表示的杂环胺：其中R 4选自氢，低级烷基，苯基，取代的苯基，苄基，取代的苄基，羧基或羧基低级烷基 ; X选自N-R 4，O和CH 2; m为2或3; 当X为O或N-R 4时，n为2或3，X为CH 2时n为1至3; p为0〜2; 及其药学上可接受的盐。这些化合物是抗炎和抗过敏剂。

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