利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

110 条记录 (耗时 0.066 秒)

    MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
    5.
    发明申请
    MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF 有权
    GLUCOCORTICOID受体的调节剂，AP-1和/或NF-kB活性及其用途

    公开(公告)号：US20100063051A1

    公开(公告)日：2010-03-11

    申请号：US12513187

    申请日：2007-10-31

    申请人： Bingwei Vera Yang ,  Lidia M. Doweyko ,  Wayne Vaccaro ,  Tram N. Huynh ,  David R. Tortolani ,  T.G. Murali Dhar

    发明人： Bingwei Vera Yang ,  Lidia M. Doweyko ,  Wayne Vaccaro ,  Tram N. Huynh ,  David R. Tortolani ,  T.G. Murali Dhar

    IPC分类号： A61K31/5377 ,  C07D277/38 ,  C07D417/12 ,  A61K31/426 ,  A61P37/00 ,  A61P29/00

    CPC分类号： C07D211/58 ,  C07C235/36 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D213/75 ,  C07D231/40 ,  C07D233/88 ,  C07D239/42 ,  C07D277/46 ,  C07D277/82 ,  C07D285/08 ,  C07D285/135 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12

    摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R6 and R7 taken together with the carbon atom to which they are both attached are selected from a group other than cycloalkyl; Q is selected from (i) hydrogen, C1-C4 alkyl, and substituted C1-C4 alkyl; or (ii) Q and R6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and MaM are combined with the carbon atom(s) to which they are attached to form a 3- to 7-membered ring containing 1-2 heteroatoms which are independently selected from the group consisting of O, S, SO2, and N which ring may be optionally substituted with 0-2 R5 groups or carbonyl; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and Ma, Za, R1, R2, R3, R4, R6, R7, and R22 are as defined herein. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using said compounds.

    摘要翻译： 提供了新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病，包括具有式（I）结构的炎性和免疫疾病，肥胖症和糖尿病 ），对映体，非对映体，互变异构体，溶剂合物（例如水合物）或其药学上可接受的盐，其中：M选自烷基，取代的烷基，环烷基，芳基，杂环和杂芳基，条件是如果M是烷基 那么R6和R7与它们所连接的碳原子一起选自除环烷基以外的基团; Q选自（i）氢，C 1 -C 4烷基和取代的C 1 -C 4烷基; 或（ii）Q和R 6与它们所连接的碳原子结合形成3-至6-元环烷基; 或（iii）Q和MaM与它们所连接的碳原子一起形成含有1-2个杂原子的3-至7-元环，其独立地选自O，S，SO 2 和N，该环可以任选地被0-2个R5基或羰基取代; Z选自环烷基，杂环基，芳基或杂芳基; 并且Ma，Za，R 1，R 2，R 3，R 4，R 6，R 7和R 22如本文所定义。 还提供了使用所述化合物治疗代谢和炎症或免疫相关疾病或病症的药物组合物和方法。

    N-bisaryl- and n-aryl-cycloakylidenyl-αhydroxy-and α-alkoxy acid amides
    8.
    发明授权
    N-bisaryl- and n-aryl-cycloakylidenyl-αhydroxy-and α-alkoxy acid amides 失效
    N-二芳基 - 和正 - 芳基 - 亚环烷基 - α-羟基和α-烷氧基酰胺

    公开(公告)号：US07166746B2

    公开(公告)日：2007-01-23

    申请号：US10522077

    申请日：2003-07-23

    申请人： Clemens Lamberth ,  Martin Zeller ,  Tibor Goegh

    发明人： Clemens Lamberth ,  Martin Zeller ,  Tibor Goegh

    IPC分类号： C07C233/58 ,  A01N37/18

    CPC分类号： C07C235/36 ,  C07C215/64 ,  C07C215/74 ,  C07C217/74 ,  C07C217/80 ,  C07C235/38 ,  C07C2601/14 ,  C07F7/1804

    摘要： The invention relates to N-bisaryl- and N-aryl-cycloalkylidenyl-a-hydroxy- and a-alkoxy acetic acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, C1–C12alkyl; C2–C12alkenyl; C2–C12alkynyl; C1–C12haloalkyl; R2 is hydrogen; optionally substituted alkyl; or optionally substituted alkynyl; R3 is optionally substituted aryl or optionally substituted heteroaryl; A is an optionally substituted saturated or unsaturated C3–C8-cycloalkylidene, optionally substituted phenylidene or optionally substituted saturated or unsaturated heterocyclylidene bridge, R4 and R5 are each independently hydrogen or an organic radical, and R6 is hydrogen; tri-C1–C4alkyl-silyl; di-C1–C4alkyl-phenylsilyl; C1–C4alkyl-diphenylsilyl; triphenylsilyl; optionally substituted alkyl; optionally substituted alkenyl or optionally substituted alkynyl. The compounds possess plant-protecting properties and are suitable for protecting plants against infestation by phytopathogenic microorganism, especially fungi.

    摘要翻译： 本发明涉及通式（I）的N-双芳基 - 和N-芳基 - 环丙烯基-α-羟基 - 和α-烷氧基乙酰胺，其包括其旋光异构体和这些异构体的混合物，其中R 1 氢，C 1 -C 12烷基; C 2 -C 12链烯基; C 2 -C 12炔基; C 1 -C 12卤代烷基; R 2是氢; 任选取代的烷基; 或任选取代的炔基; R 3是任选取代的芳基或任选取代的杂芳基; A是任选取代的饱和或不饱和C 3 -C 8 - 亚烷基，任选取代的亚苯基或任选取代的饱和或不饱和杂环亚烷基桥，R 4 >和R 5各自独立地为氢或有机基团，并且R 6为氢; 三-C 1 -C 4烷基 - 甲硅烷基; 二-C 1 -C 4烷基 - 苯基甲硅烷基; C 1 -C 4烷基 - 二苯基甲硅烷基; 三苯基甲硅烷基; 任选取代的烷基; 任选取代的烯基或任选取代的炔基。 该化合物具有植物保护性质，适用于保护植物免受植物病原微生物特别是真菌感染。

    Alpha acyloxyacetamides for kallikrein and urokinase inhibition
    9.
    发明申请
    Alpha acyloxyacetamides for kallikrein and urokinase inhibition 审中-公开
    α酰氧基乙酰胺，用于激肽释放酶和尿激酶抑制

    公开(公告)号：US20040044075A1

    公开(公告)日：2004-03-04

    申请号：US10448447

    申请日：2003-05-29

    申请人： Genzyme Corporation

    发明人： Mark M. Staveski ,  Scott F. Sneddon

    IPC分类号： A61K031/24

    CPC分类号： C07D405/12 ,  C07C235/34 ,  C07C235/36 ,  C07C235/38 ,  C07C237/30 ,  C07C255/57 ,  C07C323/25 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/18 ,  C07D215/12 ,  C07D239/38 ,  C07D317/58 ,  C07D495/04

    摘要： Disclosed herein is a compound represented by Structural Formula (I): 1 R1 is a substituted or unsubstituted aryl group or alkyl group; R2 is a substituted or unsubstituted aryl group or cycloalkyl group; Ar is a substituted or unsubstituted aryl group; X is a nullCH2null, nullOnull, nullSnull or nullCOnull; m is an integer from zero to two; n is an integer from 0-2 when X is nullOnull, nullSnull and 1-2 when X is nullCH2null or nullCOnull. Also disclosed are methods of inhibiting kallikrein activity or urokinase activity in subject in need of such inhibition by administering a compound represented by Structural Formula (I).

    摘要翻译： 本文公开了由结构式（I）表示的化合物：R 1是取代或未取代的芳基或烷基; R2是取代或未取代的芳基或环烷基; Ar是取代或未取代的芳基; X是-CH 2 - ， - O - ， - S-或-CO-; m是从零到二的整数; 当X是-CH 2 - 或-CO-时，当X是-O - ， - S-和1-2时，n是0-2的整数。 还公开了通过施用由结构式（I）表示的化合物来抑制需要这种抑制的受试者的激肽释放酶活性或尿激酶活性的方法。