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52 条记录 (耗时 0.041 秒)

    3,4-disubstituted anilines-immunomodulating agents
    42.
    发明授权
    3,4-disubstituted anilines-immunomodulating agents 失效
    3,4-二取代的苯胺 - 免疫调节剂

    公开(公告)号：US5310760A

    公开(公告)日：1994-05-10

    申请号：US89007

    申请日：1993-07-09

    申请人： William N. Washburn ,  Lee H. Latimer ,  Barbara B. Lussier ,  Carl R. Illig ,  Alexander L. Weis

    发明人： William N. Washburn ,  Lee H. Latimer ,  Barbara B. Lussier ,  Carl R. Illig ,  Alexander L. Weis

    IPC分类号： A61K31/165 ,  C07C237/44 ,  C07C233/65

    CPC分类号： A61K31/165 ,  C07C237/44

    摘要： Certain 3,4-disubstituted anilines and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --NH.sub.2 or --NHCH.sub.3 ;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.

    摘要翻译： 提供了通过诱导IL-2合成和随后的IL-2受体表达而模拟IL-1活性的某些3,4-二取代的苯胺及其药学上可接受的盐。 具体地说，本发明提供了式I化合物及其酸加成盐：其中Y是NH 3或SO 2 NH，其中R 4是H; Z是-O-，-NH-，-NR-，-S-或能够与R4氢键合的其它杂原子，以产生优选的构象; R是烷基; R1是-NH2或-NHCH3; R2是H，烷基，环烷基，芳烷基，取代或未取代的芳基或取代或未取代的具有4至5个核碳原子的氮杂环基; 并且R 3是亲脂性部分。

    3,4-disubstituted phenols-immunomodulating agents
    43.
    发明授权
    3,4-disubstituted phenols-immunomodulating agents 失效
    3,4-二取代苯酚 - 免疫调节剂

    公开(公告)号：US5258407A

    公开(公告)日：1993-11-02

    申请号：US816503

    申请日：1991-12-31

    申请人： William N. Washburn ,  Barbara B. Lussier ,  Carl B. Illig ,  Lee H. Latimer

    发明人： William N. Washburn ,  Barbara B. Lussier ,  Carl B. Illig ,  Lee H. Latimer

    IPC分类号： C07C233/75 ,  C07C235/60 ,  C07C235/62 ,  C07C235/64 ,  C07C243/40 ,  C07D239/42 ,  A61K31/165 ,  C07C233/65

    CPC分类号： C07D239/42 ,  C07C233/75 ,  C07C235/60 ,  C07C235/62 ,  C07C235/64 ,  C07C243/40 ,  C07C2103/74 ,  Y10S514/885

    摘要： Certain 3,4-disubstituted phenols and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --OH;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.

    摘要翻译： 提供了通过诱导IL-2合成和随后的IL-2受体表达而模拟IL-1活性的某些3,4-二取代的苯酚及其药学上可接受的盐。 具体地说，本发明提供了式I化合物及其酸加成盐：其中Y是NH 3或SO 2 NH，其中R 4是H; Z是-O-，-NH-，-NR-，-S-或能够与R4氢键合的其它杂原子，以产生优选的构象; R是烷基; R1是-OH; R2是H，烷基，环烷基，芳烷基，取代或未取代的芳基或取代或未取代的具有4至5个核碳原子的氮杂环基; 并且R 3是亲脂性部分。

    Reagents for detecting oxidase positive microorganisms
    44.
    发明授权
    Reagents for detecting oxidase positive microorganisms 失效
    用于检测氧化酶阳性微生物的试剂

    公开(公告)号：US5093239A

    公开(公告)日：1992-03-03

    申请号：US188999

    申请日：1988-05-02

    申请人： Robert T. Belly ,  Lee J. Fleckenstein ,  Drake M. Michno ,  William N. Washburn

    发明人： Robert T. Belly ,  Lee J. Fleckenstein ,  Drake M. Michno ,  William N. Washburn

    IPC分类号： C12Q1/04 ,  C07C235/66 ,  C07C235/74 ,  C07C271/48 ,  C07C311/08 ,  C07C317/32 ,  C12Q1/26

    CPC分类号： C07C235/66 ,  C07C235/74 ,  C07C271/48 ,  C07C311/08 ,  C07C317/32 ,  C12Q1/26 ,  C07C2103/28 ,  C07C2103/40

    摘要： Compounds and reagents containing the compounds are disclosed for detecting oxidase positive organisms. The compounds have the structureCOUP--LINK).sub.n RwhereinCOUP-- represents a radical that couples with an oxidized primary aromatic amine and releases --LINK--R;--LINK-- represents a divalent radical that undergoes intramolecular cyclization and release of --R upon release by COUP--;n represents zero or one;--R represents a monovalent radical that forms a detectable species in the form of a colorimetric dye or fluorescent compound upon release from --LINK--; wherein --R is selected from the group consisting of: ##STR1## wherein W represents hydrogen; halogen; hydroxy; substituted or unsubstituted carbonamido; sulfonamido; sulfonyl; ureido or amino;R.sup.1 and R.sup.2 each independently represent hydrogen, halogen, alkyl, alkoxy, carboxy, sulfo, cyano, nitro, carboxylic acid ester, carbonyl, sulfonyl, carbonamido, sulfonamido, alkylsulfonyl, arylsulfonyl; andR.sup.3 and R.sup.4 each independently represent halogen, nitro, sulfonamido, sulfonyl, carbonamido, carbonyl, cyano, alkylsulfonyl, arylsulfonyl;R.sup.6 represents H, CH.sub.3 or C.sub.2 H.sub.5 ;X.sub.5 represents --O--, --S-- or ##STR2## and R.sup.5 represents H, alkyl, cycloalkyl or aryl.The reagnets containg also a hydrogen donating primary amine.

    NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS AND METHODS
    49.
    发明申请
    NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS AND METHODS 审中-公开
    非基因麦芽宁浓度HORMONE受体-1拮抗剂和方法

    公开(公告)号：US20090011994A1

    公开(公告)日：2009-01-08

    申请号：US12141228

    申请日：2008-06-18

    申请人： Philip D. Stein ,  Sharon N. Bisaha ,  Saleen Ahmad ,  Khehyong Ngu ,  William N. Washburn

    发明人： Philip D. Stein ,  Sharon N. Bisaha ,  Saleen Ahmad ,  Khehyong Ngu ,  William N. Washburn

    IPC分类号： A61K38/22 ,  A61K31/4965 ,  C07D241/18 ,  A61K31/497 ,  A61P3/04 ,  A61P3/10 ,  A61K31/60 ,  C07D401/04 ,  A61K31/675

    CPC分类号： C07D241/18 ,  C07D401/12

    摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are defined herein.Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.

    摘要翻译： 本申请提供化合物，包括其中R 1，R 2，R 3，R 8和R 9在本文中定义的根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式。 另外，本申请提供含有至少一种根据式I的化合物和任选的至少一种另外的治疗剂的药物组合物。 最后，本申请提供了通过施用治疗有效剂量的根据式I的化合物治疗患有MCHR-1调节的疾病或病症例如肥胖，糖尿病，抑郁或焦虑的患者的方法。

    3,4-disubstituted phenols-immunomodulating agents
    50.
    发明授权
    3,4-disubstituted phenols-immunomodulating agents 失效
    3,4-二取代苯酚 - 免疫调节剂

    公开(公告)号：US5466715A

    公开(公告)日：1995-11-14

    申请号：US208396

    申请日：1994-03-08

    申请人： William N. Washburn ,  Barbara B. Lussier ,  Carl R. Illig ,  Lee H. Latimer

    发明人： William N. Washburn ,  Barbara B. Lussier ,  Carl R. Illig ,  Lee H. Latimer

    IPC分类号： C07C233/75 ,  C07C235/60 ,  C07C235/62 ,  C07C235/64 ,  C07C243/40 ,  C07D239/42 ,  A61K31/165 ,  A61K31/16

    CPC分类号： C07D239/42 ,  C07C233/75 ,  C07C235/60 ,  C07C235/62 ,  C07C235/64 ,  C07C243/40 ,  C07C2103/74

    摘要： Certain 3,4-disubstituted phenols and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --OH;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety selected from the group consisting of substituted C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.16 cycloalkyl and 2,4-di-t-pentylphenyl.

    摘要翻译： 提供了通过诱导IL-2合成和随后的IL-2受体表达而模拟IL-1活性的某些3,4-二取代的苯酚及其药学上可接受的盐。 具体地，本发明提供式I化合物及其酸加成盐：其中Y为NHSO 2或SO 2 NH，其中R 4为H; Z是-O-，-NH-，-NR-，-S-或能够与R4氢键合的其它杂原子，以产生优选的构象; R是烷基; R1是-OH; R2是H，烷基，环烷基，芳烷基，取代或未取代的芳基或取代或未取代的具有4至5个核碳原子的氮杂环基; 并且R 3是选自取代的C 1 -C 10烷基，C 3 -C 16环烷基和2,4-二 - 叔戊基苯基的亲脂性部分。