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    Alpha-AminoCycloLactam Ligands for G-Protein Coupled Receptors, and Methods of Using Same
    1.
    发明申请
    Alpha-AminoCycloLactam Ligands for G-Protein Coupled Receptors, and Methods of Using Same 审中-公开
    用于G蛋白偶联受体的α-氨基环内酰胺配体及其使用方法

    公开(公告)号：US20130172319A1

    公开(公告)日：2013-07-04

    申请号：US13777938

    申请日：2013-02-26

    申请人： Cambridge Enterprise Limited ,  David J. Grainger ,  David John Fox

    发明人： David J. Grainger ,  David John Fox

    IPC分类号： C07D225/02 ,  C07D211/76 ,  C07D223/12 ,  C07D207/273

    CPC分类号： C07D225/02 ,  C07D207/273 ,  C07D211/76 ,  C07D223/12 ,  C07D487/08

    摘要： The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs).The library contains compounds of general formula (II) wherein: y is any integer from 1 to 8; X is —CO—R1 or —SO2—R1; each R1 is independently selected from an alkyl, haloalkyl, alkenyl, alkynyl, alkylaminoalkyl, alkylaminodialkyl, or charged alkylaminotrialkyl, radical of 1 to 20 carbon atoms; or each R1 is independently selected from oxyalkyl, aminoalkyl, aminodialkyl, or charged aminotrialkyl radical; and wherein the R1 radical has a “key” carbon next to the carbonyl of the carbon amide or the sulfonyl group of the sulfonamide which is di-substituted with the same or different groups selected from: alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl and alkylamino radicals.

    摘要翻译： 本发明涉及产生富含G-蛋白偶联受体类（GPCR）成员的激动剂和拮抗剂的化合物文库。 该文库含有通式（II）的化合物，其中：y为1至8的整数; X是-CO-R 1或-SO 2 -R 1; 每个R 1独立地选自烷基，卤代烷基，烯基，炔基，烷基氨基烷基，烷基氨基二烷基或带电荷的烷基氨基三烷基，1-20个碳原子的基团; 或每个R 1独立地选自烷氧基，氨基烷基，氨基二烷基或带电荷的氨基三烷基; 并且其中所述R 1基团与碳酰胺的羰基相邻的“键”碳或磺酰胺的磺酰基，其被选自以下的相同或不同的基团二取代：烷基，卤代烷基，烷氧基，卤代烷氧基，烯基， 炔基和烷基氨基。

    Anti-inflammatory agents
    4.
    发明授权
    Anti-inflammatory agents 失效
    抗炎剂

    公开(公告)号：US07691845B2

    公开(公告)日：2010-04-06

    申请号：US11573637

    申请日：2005-08-10

    申请人： David J. Grainger ,  David John Fox

    发明人： David J. Grainger ,  David John Fox

    IPC分类号： A61K31/55 ,  C07D223/10 ,  A61P29/00 ,  A61P19/10

    CPC分类号： C07D223/10 ,  A61K31/55

    摘要： The invention provides compounds, compositions and uses of compounds of general formula (I) or (I′), or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder.

    摘要翻译： 本发明提供了用于制备用于治疗炎症性疾病的药物的通式（I）或（I'）化合物或其药学上可接受的盐作为3-氨基己内酰胺衍生物的化合物，组合物和用途。

    Anti-Inflammatory Agents
    5.
    发明申请
    Anti-Inflammatory Agents 审中-公开
    抗炎药

    公开(公告)号：US20090203739A1

    公开(公告)日：2009-08-13

    申请号：US11922283

    申请日：2006-06-14

    申请人： David J. Grainger ,  David John Fox

    发明人： David J. Grainger ,  David John Fox

    IPC分类号： A61K31/45 ,  A61K31/395 ,  C07D207/36 ,  C07D211/86 ,  C07D225/02 ,  A61K31/4015 ,  A61P35/00 ,  A61P19/02 ,  A61P11/06 ,  A61P19/10 ,  A61P9/00 ,  A61P17/06 ,  A61P17/02 ,  A61P31/12 ,  A61P29/00 ,  A61P37/06

    CPC分类号： C07D213/76 ,  A61K31/4015 ,  A61K31/45 ,  C07D207/267 ,  C07D207/50 ,  C07D211/76 ,  C07D225/02

    摘要： The invention provides compounds, pharmaceutical compositions and uses of compounds of general formula (I) or a pharmaceutically acceptable salt thereof, for the preparation of a medicament intended to treat an inflammatory disorder; wherein z X is 1, 2 or 4; X is —CO—Yk—(R1)n or SO2—Yk—(R1)n; k is 0 or 1; Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or is a cycloalkenyl or polycycloalkenyl group; each R1 is independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms (for example of 5 to 20 carbon atoms, of 8 to 20 carbon atoms, of 9 to 20 carbon atoms, of 10 to 18 carbon atoms, of 12 to 18 carbon atoms, of 13 to 18 carbon atoms, of 14 to 18 carbon atoms, of 13 to 17 carbon atoms); or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radical; and n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y (such that n=1 if k=0, such that the R1 group is bonded directly to the carbonyl or sulfonyl group); provided that simultaneously X cannot be an undec-10-en-1-oyl group and z be equal to 1 or 2; or alternatively R1 is selected from a peptido radical having from 1 to 4 peptidic moieties linked together by peptide bonds.

    摘要翻译： 本发明提供化合物，药物组合物和通式（I）化合物或其药学上可接受的盐在制备用于治疗炎症性疾病的药物中的应用; 其中z X为1,2或4; X是-CO-Yk-（R1）n或SO2-Yk-（R1）n; k为0或1; Y是环烷基或聚环烷基（例如金刚烷基，金刚烷甲基，双环辛基，环己基，环丙基）; 或者是环烯基或多环烯基; 每个R 1独立地选自氢或具有1至20个碳原子的烷基，卤代烷基，烷氧基，卤代烷氧基，烯基，炔基或烷基氨基（例如5至20个碳原子，8至20个碳原子，9至20个 碳原子数10〜18，碳原子数12〜18，碳原子数13〜18，碳原子数14〜18，碳原子数13〜17的碳原子数）。 或每个R 1独立地选自氟，氯，溴，碘，羟基，氧烷基，氨基，氨基烷基或氨基二烷基; 并且n是从1到m的任何整数，其中m是环组Y上允许的最大取代数（如果k = 0，则n = 1，使得R1基团直接键合到羰基或磺酰基上 ）; 条件是同时X不能是十一碳-1-烯-1-基，z等于1或2; 或者R1选自具有通过肽键连接在一起的1至4个肽部分的肽基。

    METHODS AND MEANS
    6.
    发明申请
    METHODS AND MEANS 审中-公开
    方法与手段

    公开(公告)号：US20090075872A1

    公开(公告)日：2009-03-19

    申请号：US11577974

    申请日：2005-10-25

    申请人： David J. Grainger

    发明人： David J. Grainger

    IPC分类号： C12Q1/02 ,  A61K38/17 ,  A61P25/28 ,  A61P29/00 ,  A61P19/10 ,  A61P9/00 ,  A61P9/10

    CPC分类号： G01N33/92 ,  G01N2510/00

    摘要： This invention relates to methods and means for the stimulation of phagocytosis and in particular to the phagocytosis of apoptotic cells, and discloses a role for the protein product of the apoE gene (apolipoproteinE) as a regular of apoptotic cell clearance. ApoE mimetics and other compounds which stimulate the clearance of apoptotic cells may be useful in the treatment of a range of disorders. One aspect of the invention provides a method of identifying and/or obtaining a compound for the treatment of a condition associated with decreased endogenous apoE activity in an individual comprising: determining the ingestion of apoptic cells by a macrophage in the presence of a test compound. An increase in apoptic cell ingestion in the presence relative to the absence of test compound may be indicative that the compound may be useful in the treatment of a condition associated with decreased endogenous apoE activity.

    摘要翻译： 本发明涉及刺激吞噬的方法和手段，特别涉及凋亡细胞的吞噬作用，并且公开了apoE基因（载脂蛋白E）的蛋白质产物作为凋亡细胞清除的规则的作用。 刺激凋亡细胞清除的ApoE模拟物和其它化合物可用于治疗一系列疾病。 本发明的一个方面提供了鉴定和/或获得用于治疗与个体内源性apoE活性降低相关的病症的化合物的方法，其包括：在测试化合物的存在下测定巨噬细胞摄入的凋亡细胞。 在相对于不存在测试化合物存在的情况下，凋亡细胞摄取的增加可以指示该化合物可用于治疗与内源性apoE活性降低相关的病症。

    COMPOSITION
    7.
    发明申请
    COMPOSITION 失效
    组成

    公开(公告)号：US20090036486A1

    公开(公告)日：2009-02-05

    申请号：US11833022

    申请日：2007-08-02

    申请人： David J. Grainger ,  David John Fox

    发明人： David J. Grainger ,  David John Fox

    IPC分类号： A61K31/45 ,  A61P29/00

    CPC分类号： C07D211/76

    摘要： The invention relates to the use of 3-(2′,2′-dimethylpropanoylamino)-tetrahydropyridin-2-one for preparing a medicament intended to prevent or treat inflammatory disorders.

    摘要翻译： 本发明涉及3-（2'，2'-二甲基丙酰基氨基） - 四氢吡啶-2-酮在制备用于预防或治疗炎症性疾病的药物中的用途。

    Anti-Inflammatory Agents
    8.
    发明申请
    Anti-Inflammatory Agents 失效
    抗炎药

    公开(公告)号：US20080194541A1

    公开(公告)日：2008-08-14

    申请号：US11573637

    申请日：2005-08-10

    申请人： David J. Grainger ,  David John Fox

    发明人： David J. Grainger ,  David John Fox

    IPC分类号： A61K31/55 ,  C07D223/10 ,  A61P29/00 ,  A61P19/10

    CPC分类号： C07D223/10 ,  A61K31/55

    摘要： The invention provides compounds, compositions and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder wherein X is —CO—Y—(R1)n or SO2—Y—(R1)n; and Y is 0 cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or is 0 cycloalkenyl or polycycloalkenyl group.

    摘要翻译： 本发明提供了用于制备治疗炎症性疾病的药物的化合物，组合物和通式（I）化合物或其药学上可接受的盐，其为3-氨基己内酰胺衍生物，其中X为-CO-Y-（ n 1或n 2 - （R 1）） - - - - （R 1） ; 和Y为0环烷基或聚环烷基（例如金刚烷基，金刚烷甲基，双环辛基，环己基，环丙基）; 或是0个环烯基或多环烯基。

    Prevention and treatment of cardiovascular pathologies
    9.
    发明授权
    Prevention and treatment of cardiovascular pathologies 失效
    预防和治疗心血管病变

    公开(公告)号：US06251920B1

    公开(公告)日：2001-06-26

    申请号：US09082643

    申请日：1998-05-21

    申请人： David J. Grainger ,  James C. Metcalfe ,  Peter L. Weissberg

    发明人： David J. Grainger ,  James C. Metcalfe ,  Peter L. Weissberg

    IPC分类号： A61K31445

    CPC分类号： A61K9/0024 ,  A61K31/00 ,  A61K31/135 ,  A61K31/138 ,  A61K31/337 ,  A61K31/38 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/407 ,  A61K31/715 ,  C07K14/71 ,  C07K16/22 ,  C07K2317/73 ,  G01N2800/32 ,  G01N2800/324

    摘要： A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): wherein Z is C═O or a covalent bond; Y is H or O(C1-C4)alkyl, R1 and R2 are individually (C1-C4)alkyl or together with N are a saturated heterocyclic group, R3 is ethyl or chloroethyl, R4 is H or together with R3 is —CH2—CH2— or —S—, R5 is I, O(C1-C4)alkyl or H and R6 is I, O(C1-C4)alkyl or H with the proviso that when R4, R5, and R6 are H, R3 is not ethyl; or a pharmaceutically acceptable salt thereof, effective to activate or stimulate production of TGF-beta to treat and/or prevent conditions such as atherosclerosis, thrombosis, myocardial infarction, and stroke is provided. Useful compounds include idoxifene and salts thereof. Further provided is a method for identifying a compound that is a TGF-beta activator or production stimulator is provided. Another embodiment of the invention is an assay or kit to determine TGF-beta in vitro. Also provided is a therapeutic method comprising inhibiting smooth muscle cell proliferation associated with procedural vascular trauma employing the administration of tamoxifen or structural analogs thereof, including compounds of formula (I).

    摘要翻译： 一种治疗或预​​防心血管病变的方法，其通过给予式（I）化合物：其中Z为C = O或共价键; Y是H或O（C1-C4）烷基，R1和R2分别是（C1-C4）烷基或与N一起是饱和杂环基，R3是乙基或氯乙基，R4是H或与R3一起是-CH2- CH2-或-S-，R5是I，O（C1-C4）烷基或H，R6是I，O（C1-C4）烷基或H，条件是当R4，R5和R6是H时，R3是 不是乙基; 提供有效激活或刺激TGF-β的产生以治疗和/或预防诸如动脉粥样硬化，血栓形成，心肌梗死和中风的病症的药学上可接受的盐或其药学上可接受的盐。 有用的化合物包括异昔芬及其盐。 还提供了鉴定作为TGF-β激活剂或生产刺激剂的化合物的方法。 本发明的另一个实施方案是用于在体外测定TGF-β的测定或试剂盒。 还提供了一种治疗方法，其包括使用给予他莫昔芬或其结构类似物（包括式（I）的化合物）来抑制与程序性血管创伤相关的平滑肌细胞增殖。