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1. 发明授权

US4801610A Phenolic ester derivatives as elastase inhibitors 失效
标题翻译：酚酯衍生物作为弹性蛋白酶抑制剂
公开(公告)号：US4801610A
公开(公告)日：1989-01-31
申请号：US58467
申请日：1987-06-05
申请人： Masateru Miyano , James R. Deason
发明人： Masateru Miyano , James R. Deason
IPC分类号： A61K31/22 , A61K31/265 , A61K31/35
CPC分类号： A61K31/22 , A61K31/265 , A61K31/35
摘要： Phenolic esters of the general formula I ##STR1## are useful for the prevention, management or alleviation of elastase mediated diseases or conditions.
摘要翻译：通式I的酚酯可以用于预防，治疗或缓解弹性蛋白酶介导的疾病或病症。

2. 发明授权

US4683241A Phenolic ester derivatives as elastase inhibitors 失效
标题翻译：酚酯衍生物作为弹性蛋白酶抑制剂
公开(公告)号：US4683241A
公开(公告)日：1987-07-28
申请号：US612193
申请日：1984-05-21
申请人： Masateru Miyano , James R. Deason
发明人： Masateru Miyano , James R. Deason
IPC分类号： A61K31/22 , A61K31/265 , A61K31/35
CPC分类号： A61K31/22 , A61K31/265 , A61K31/35
摘要： Phenolic esters of the general formula I ##STR1## are useful for the prevention, management or alleviation of elastase mediated diseases or conditions.
摘要翻译：通式I的酚酯可以用于预防，治疗或缓解弹性蛋白酶介导的疾病或病症。

3. 发明授权

US5225444A Disubstituted 4-hydroxyphenylthio anilides 失效
标题翻译：二取代的4-羟基苯基硫代酰苯胺
公开(公告)号：US5225444A
公开(公告)日：1993-07-06
申请号：US750810
申请日：1991-08-27
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： C07C317/44
CPC分类号： C07C317/44
摘要： The compounds of this invention are anilides 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 hydrogen or lower alkyl; and R.sub.4 is phenyl or substituted phenyl. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.
摘要翻译：本发明的化合物是由下式表示的酰苯胺：其中：R 1和R 2是由卤素，苯基，取代的苯基和取代的苯基和基团组成的组中相同或不同的成员，其中n，m和p是独立地为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是氢或低级烷基; 并且R 4是苯基或取代的苯基。本发明的化合物可用于治疗炎症，过敏和超敏反应以及免疫系统的其它病症。

4. 发明授权

US5071876A Novel disubstituted 4-hydroxyphenylthio anilides 失效
标题翻译：新型二取代的4-羟基苯基硫代酰苯胺
公开(公告)号：US5071876A
公开(公告)日：1991-12-10
申请号：US558965
申请日：1990-07-27
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： C07C317/44
CPC分类号： C07C317/44 , Y10S514/825 , Y10S514/826 , Y10S514/863 , Y10S514/886 , Y10S514/887
摘要： The compounds of this invention are anilides 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 hydrogen or lower alkyl; and R.sub.4 is phenyl or substituted phenyl. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.
摘要翻译：本发明的化合物是由下式表示的酰苯胺：其中：R 1和R 2是由卤素，苯基，取代的苯基和取代的苯基和基团组成的组中相同或不同的成员，其中n，m和p是独立地为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是氢或低级烷基; 并且R 4是苯基或取代的苯基。本发明的化合物可用于治疗炎症，过敏和超敏反应以及免疫系统的其它病症。

5. 发明授权

US4950684A 2,2-di-substituted benzopyran leukotriene-D.sub.4 antagonists 失效
标题翻译： 2,2-二取代苯并吡喃白三烯-D4拮抗剂
公开(公告)号：US4950684A
公开(公告)日：1990-08-21
申请号：US196996
申请日：1988-05-20
申请人： Francis J. Koszyk , James R. Deason
发明人： Francis J. Koszyk , James R. Deason
IPC分类号： A61K31/35 , A61K31/352 , A61P29/00 , A61P37/08 , C07D311/22 , C07D311/58
CPC分类号： C07D311/22 , C07D311/58
摘要： This invention relates to novel compounds having a 2,2-di-substituted chromanonyl (benzopyran) ring structure which are antagonists of leukotriene D.sub.4 (LTD.sub.4) and the slow reacting substance of anaphylaxis (SRS-A). The compounds of this invention are useful as pharmaceutical agents to prevent or alleviate the symptoms associated with LTD.sub.4, such as allergic reactions and inflammatory conditions.

6. 发明授权

US4923891A Leukotriene LTD.sub.4 and LTB.sub.4 antagonists 失效
标题翻译：白三烯LTD4和LTB4拮抗剂
公开(公告)号：US4923891A
公开(公告)日：1990-05-08
申请号：US241265
申请日：1988-09-09
申请人： James R. Deason , Michael A. Stealey , Richard M. Weier
发明人： James R. Deason , Michael A. Stealey , Richard M. Weier
IPC分类号： C07D317/30 , A61K31/335 , A61K31/357 , A61K31/385 , A61K31/39 , A61P29/00 , A61P37/08 , C07D327/04 , C07D339/06
CPC分类号： C07D327/04 , C07D339/06
摘要： This invention encompasses compounds of Formula I ##STR1## and the pharmaceutically acceptable salts and geometrical and optical isomers thereof wherein:X, Y, and Z are each independently O or S with S optionally oxidized to S=O;Alk is straight or branched chain alkylene or hydroxyalkylene containing 1-6 carbon atoms;R.sub.1 is hydrogen or lower alkyl;n is 0 to 5;R.sub.2 is hydrogen, lower alkyl, cycloalkyl, --(CH.sub.2).sub.n --CO.sub.2 R.sub.1, phenyl, phenyl substituted with halo, lower alkyl or lower alkoxy; andAr is 5,6,7,8-tetrahydro-1-naphthalenyl, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, or lower alkanoyl.This invention is in the field of pharmaceutical agents which act as leukotriene D.sub.4 (LTD.sub.4) antagonists and includes embodiments which act as leukotriene B.sub.4 (LTD.sub.4) antagonists.

7. 发明授权

US4808729A Leukotriene LTD.sub.4 and LTB.sub.4 antagonists 失效
标题翻译：白三烯LTD4和LTB4拮抗剂
公开(公告)号：US4808729A
公开(公告)日：1989-02-28
申请号：US100685
申请日：1987-09-24
申请人： James R. Deason , Michael A. Stealey , Richard M. Weier
发明人： James R. Deason , Michael A. Stealey , Richard M. Weier
IPC分类号： C07D327/04 , C07D339/06 , C07D339/02
CPC分类号： C07D339/06 , C07D327/04
摘要： The invention encompasses compounds of Formula I ##STR1## and the pharmaceutically acceptable salts and geometrical and optical isomers thereof wherein:X, Y, and Z are each independently O or S with S optionally oxidized to S.dbd.O;Alk is alkylene or hydroxyalkylene containing 1-6 carbon atoms;R.sub.1 is hydrogen or lower alkyl;n is 0 to 5;R.sub.2 is hydrogen, lower alkyl, cycloalkyl, --(CH.sub.2).sub.n --CO.sub.2 R.sub.1, phenyl, phenyl substituted with halo, lower alkyl or lower alkoxy; andAr is 5,6,7,8-tetrahydro-1-naphthalenyl, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, or lower alkanoyl. The compounds are useful as anti-allergy agents and anti-inflammatory agents.
摘要翻译：本发明包括式I的化合物及其药学上可接受的盐和几何和旋光异构体，其中：X，Y和Z各自独立地为O或S，S任选被氧化成S = O; Alk是含有1-6个碳原子的亚烷基或羟基亚烷基; R1是氢或低级烷基; n为0〜5; R 2是氢，低级烷基，环烷基， - （CH 2）n -CO 2 R 1，苯基，被卤素，低级烷基或低级烷氧基取代的苯基; 和Ar为5,6,7,8-四氢-1-萘基，苯基或被低级烷基，羟基，低级烷氧基或低级烷酰基取代的苯基。该化合物可用作抗过敏剂和抗炎剂。

8. 发明授权

US5219883A 2,2-di-substituted benzopyran leukotriene-D.sub.4 antagonists 失效
标题翻译： 2,2-二取代苯并吡喃白三烯-D4拮抗剂
公开(公告)号：US5219883A
公开(公告)日：1993-06-15
申请号：US790976
申请日：1991-11-12
申请人： Francis J. Koszyk , James R. Deason
发明人： Francis J. Koszyk , James R. Deason
IPC分类号： C07D311/22 , C07D311/58
CPC分类号： C07D311/58 , C07D311/22
摘要： This invention relates to LTD.sub.4 antagonists of the formula: ##STR1## or pharmaceutically acceptable salts thereof, wherein R.sup.1 is methyl, phenyl, ##STR2## wherein X.sub.1 and X.sub.2 may be the same or different and are members of the group consisting of hydrogen, --Cl, --Br, --CF.sub.3, --NH.sub.2, --NO.sub.2, or alkyl of 1-3 carbon atoms; m is 1 to 9; n is 1 to 5; V is --CH(OH)--, or --CH.sub.2 --; W is hydrogen or alkyl of 1-6 carbon atoms; Y is hydrogen or --COCH.sub.3 provided that when W is hydrogen Y is not hydrogen; both Z moieties are --CHO, --COOR.sup.2, --COR.sup.3, --CH(OR.sup.4)--CH.sub.2 OR.sup.4, or CH.sub.2 OR.sup.4 with the exception that when one Z moiety of Formula I is COOR.sup.2, the other Z moiety may be COR.sup.3 ;R.sup.2 is hydrogen, a pharmaceutically acceptable cation, straight or branched chain alkyl having 1-6 carbon atoms, --CH.sub.2 --CH(OR.sup.5)--CH.sub.2 --OR.sup.5, CH(CH.sub.2 OR.sup.5).sub.2 with the proviso that when Z is --COOR.sup.2, the R.sup.2 substituent in one --COOR.sup.2 moiety may be the same or different from the R.sup.2 substituent in the other COOR.sup.2 moiety;R.sup.3 is --NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8 may be the same or different and are members of the group comprising hydrogen or alkyl having 1-6 carbon atoms;R.sup.4 is hydrogen, or --C(O)--R.sup.6 ;R.sup.5 is hydrogen, benzyl-, or alkyl or 1-3 carbon atoms; andR.sup.6 is alkyl of 1-6 carbon atoms.
摘要翻译：本发明涉及下式的LTD4拮抗剂或其药学上可接受的盐，其中R 1是甲基，苯基，其中X 1和X 2可以相同或不同，并且是下列成员：的氢，-Cl，-Br，-CF 3，-NH 2，-NO 2或1-3个碳原子的烷基; m为1〜9; n为1至5; V是-CH（OH） - 或-CH 2 - ; W是氢或1-6个碳原子的烷基; Y是氢或-COCH 3，条件是当W是氢时，Y不是氢; 两个Z部分都是-CHO，-COOR 2，-COR 3，-CH（OR 4）-CH 2 OR 4或CH 2 OR 4，除了当式I的一个Z部分是COOR 2时，另一个Z部分可以是COR 3; R2是氢，可药用阳离子，具有1-6个碳原子的直链或支链烷基，-CH2-CH（OR5）-CH2-OR5，CH（CH2OR5）2，条件是当Z是-COOR2时，R2 一个-COOR 2部分中的取代基可以与其它COOR 2部分中的R 2取代基相同或不同; R 3是-NR 7 R 8，其中R 7和R 8可以相同或不同，并且是包含氢或具有1-6个碳原子的烷基的基团的成员; R4是氢或-C（O）-R6; R5是氢，苄基或烷基或1-3个碳原子; R6是1-6个碳原子的烷基。

9. 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。

10. 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。

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