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1. 发明授权

US06617324B1 Substituted pyrazoles as p38 kinase inhibitors 失效
标题翻译：取代的吡唑作为p38激酶抑制剂
公开(公告)号：US06617324B1
公开(公告)日：2003-09-09
申请号：US10114297
申请日：2002-04-02
申请人： Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xi , Ish K. Khanna , Yi Yu
发明人： Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xi , Ish K. Khanna , Yi Yu
IPC分类号： A61K31496
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04
摘要： A class of pyrazole derivatives described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
摘要翻译：一类描述用于治疗p38激酶介导的病症的吡唑衍生物。特别感兴趣的化合物由式IA定义，其中R1，R2，R3和R4如说明书中所述。

2. 发明授权

US6087496A Substituted pyrazoles suitable as p38 kinase inhibitors 失效
标题翻译：适合作为p38激酶抑制剂的取代的吡唑
公开(公告)号：US6087496A
公开(公告)日：2000-07-11
申请号：US283718
申请日：1999-04-01
申请人： Ashok Anantanarayan , Michael Clare , Lifeng Geng , Gunnar J. Hanson , Richard A. Partis , Michael A. Stealey , Richard M. Weier
发明人： Ashok Anantanarayan , Michael Clare , Lifeng Geng , Gunnar J. Hanson , Richard A. Partis , Michael A. Stealey , Richard M. Weier
IPC分类号： A61K31/44 , A61K31/445 , A61K31/5377 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04
CPC分类号： C07D401/04 , C07D401/14
摘要： A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R.sup.1, R.sup.2, Ar.sup.1 and HetAr.sup.2 are as described in the specification.
摘要翻译：描述了一类吡唑衍生物用于治疗p38激酶介导的病症。特别感兴趣的化合物由式I定义：其中R1，R2，Ar1和HetAr2如说明书中所述。

3. 发明授权

US5393764A Cyclic phenolic thioethers 失效
标题翻译：环状酚类硫醚
公开(公告)号：US5393764A
公开(公告)日：1995-02-28
申请号：US107821
申请日：1993-08-25
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 ##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.
摘要翻译： PCT No.PCT / US92 / 03569。 371日期：1993年8月25日 102（e）日期1993年8月25日PCT提交1992年5月5日PCT公布。 WO92 / 19608 PCT出版物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。

4. 发明授权

US5272178A Compounds of cyclic phenolic thioethers which are useful in stimulating and inhibiting superoxide generation 失效
标题翻译：可用于刺激和抑制超氧化物产生的环状酚类硫醚的化合物
公开(公告)号：US5272178A
公开(公告)日：1993-12-21
申请号：US45449
申请日：1993-04-08
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： C07C323/17 , C07C323/20 , C07C323/22 , C07C323/52 , C07C323/60 , C07D213/40 , C07D307/18 , C07D307/20 , C07D493/04 , A61K31/095
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 compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl, phenyl, or hydrogen; R.sup.3 represents hydrogen or alkyl; X represents O, S or (CH.sub.2).sub.m wherein m is 1 or 2; A represents O or S(O).sub.n wherein n is 0, 1, or 2; p is an integer from 0 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl; or NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl, and R.sup.6 is hydrogen, alkyl, heterocyclealkyl, substituted heterocyclealkyl, 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 (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; and the pharmaceutically acceptable salts thereof. The compounds are inhibitors or stimulators of superoxide generation.
摘要翻译：本发明涉及下式的化合物：其中R 1和R 2相同或不同并且独立地代表叔烷基，苯基或氢; R3表示氢或烷基; X表示O，S或（CH 2）m，其中m为1或2; A表示O或S（O）n，其中n为0,1或2; p是0至4的整数; 和R表示烷基; 哦; OR4，其中R4是烷基; 或NR5R6，其中R5是氢或烷基，R6是氢，烷基，杂环烷基，取代的杂环烷基，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NR5R6一起形成可任意取代的杂环; 或（CH 2）t COOR 7，其中t是1至4的整数，并且R 7是氢或烷基; 及其药学上可接受的盐。这些化合物是超氧化物产生的抑制剂或刺激剂。

5. 发明授权

US5244899A Azabicycloalkyl and azatricycloalkyl amides used to treat inflammation, allergy, asthma and skin disorders 失效
标题翻译：用于治疗炎症，过敏，哮喘和皮肤疾病的氮杂双环烷基和氮杂三环烷基酰胺
公开(公告)号：US5244899A
公开(公告)日：1993-09-14
申请号：US921876
申请日：1992-07-29
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 , Y10S514/859 , Y10S514/863 , Y10S514/885 , Y10S514/886
摘要： The compounds of this invention are 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 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 并且p独立地为1〜8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; R3选自氮杂双环烷基氨基，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。

6. 发明授权

US5189038A Method of stimulating superoxide generation 失效
标题翻译：刺激超氧化物生成的方法
公开(公告)号：US5189038A
公开(公告)日：1993-02-23
申请号：US724680
申请日：1991-07-02
申请人： Richard A. Mueller , Akira Nakao , Richard A. Partis
发明人： Richard A. Mueller , Akira Nakao , Richard A. Partis
IPC分类号： A61K31/10 , A61K31/165 , A61K31/44 , A61K31/495
CPC分类号： A61K31/165 , A61K31/10 , A61K31/44 , A61K31/495
摘要： The present invention is directed to a method of stimulating superoxide generation using phenolic thioethers which stimulate the generation of superoxide.
摘要翻译：本发明涉及一种刺激产生超氧化物的酚类硫醚刺激超氧化物产生的方法。

7. 发明授权

US5064860A Method of inhibiting superoxide generation 失效
标题翻译：抑制超氧化物产生的方法
公开(公告)号：US5064860A
公开(公告)日：1991-11-12
申请号：US579138
申请日：1990-09-07
申请人： Richard A. Mueller , Akira Nakao , Richard A. Partis
发明人： Richard A. Mueller , Akira Nakao , Richard A. Partis
IPC分类号： A61K31/19 , C07C315/02 , C07C317/22 , C07C319/02 , C07C323/20 , C07C323/52 , C07C331/10
CPC分类号： A61K31/19 , C07C315/02 , C07C319/02 , C07C323/52 , C07C331/10
摘要： The present invention relates to a method of inhibiting superoxide generation which comprises administering to a mammal in need of such treatment an amount of a compound of the Formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; Alk.sup.1 represents straight or branched chain alkylene of 1 to 10 carbon atoms, X represents sulfur or oxygen, Alk.sup.2 represents straight or branched chain alkylene of 1 to 4 carbon atoms; and m is 0, 1 or 2; or a pharmaceutically acceptable salt or stereoisomer or geometric isomer thereof, which is effective to inhibit superoxide generation.
摘要翻译：本发明涉及抑制超氧化物产生的方法，其包括向需要这种治疗的哺乳动物施用一定量的式I化合物（I），其中R 1和R 2相同或不同并且独立地表示叔 - 烷基或苯基; Alk1表示1〜10个碳原子的直链或支链亚烷基，X表示硫或氧，Alk2表示1〜4个碳原子的直链或支链亚烷基; m为0,1或2; 或其药学上可接受的盐或立体异构体或几何异构体，其有效抑制超氧化物产生。

8. 发明授权

US5002967A Phenolic thioethers, sulfoxides, and disulfides as inhibitors of 5-lipoxygenase 失效
标题翻译：酚硫醚，亚砜和二硫化物作为5-脂氧合酶的抑制剂
公开(公告)号：US5002967A
公开(公告)日：1991-03-26
申请号：US378687
申请日：1989-07-11
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： A61K31/19 , A61K31/215 , A61K31/34 , A61K31/365
CPC分类号： A61K31/215 , A61K31/19 , A61K31/34 , A61K31/365 , Y10S514/826
摘要： The compounds of the present invention comprise substituted phenolic thioethers, sulfoxides, and disulfides 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 metablic pathway are involved.
摘要翻译：本发明的化合物包括作为5-脂氧合酶的特异性抑制剂的取代的酚类硫醚，亚砜和二硫化物，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形成药剂的其它病症涉及5-脂氧合酶代谢途径。

9. 发明授权

US4711903A 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：US4711903A
公开(公告)日：1987-12-08
申请号：US824984
申请日：1986-01-31
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： A61K38/16 , C07C317/44 , C07C323/20 , C07C323/22 , C07C323/25 , C07C323/52 , C07C323/65 , C07C327/22 , C07C331/10 , C07D257/04 , C07C149/40 , A61K37/10
CPC分类号： C07D257/04 , C07C317/00 , C07C317/44 , C07C323/00 , 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; amd 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; 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。

10. 发明授权

US4692552A Protease inhibitors 失效
标题翻译：蛋白酶抑制剂
公开(公告)号：US4692552A
公开(公告)日：1987-09-08
申请号：US831238
申请日：1986-02-18
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： C07C65/01 , C07C65/19 , C07C65/40 , C07D295/02 , C07D295/03 , C07C65/04 , C07C69/88
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.
摘要翻译：本发明涉及通过给予下式的化合物或其药理学上可接受的盐来预防或减少弹性蛋白和其它蛋白质降解的方法，从而预防或延缓由所述降解引起的疾病状态。

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