专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US08389279B2 α-aminocyclolactam ligands for G-protein coupled receptors, and methods of using same 失效
标题翻译： 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：US08389279B2
公开(公告)日：2013-03-05
申请号：US13193274
申请日：2011-07-28
申请人： David J. Grainger , David John Fox
发明人： David J. Grainger , David John Fox
IPC分类号： A61K31/55 , A61K31/439 , A61P9/12 , A61P9/10 , A61P11/06 , A61P3/04 , A61P37/06 , C12N5/07
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 (I) wherein y is any integer from 1 to 8; z is any integer from 0 to 8 with the proviso that y and z cannot simultaneously be 1; X is —CO—(Y)k—(R1)n or SO2—(Y)k—(R1)n; k is 0 or 1 Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or Y is a cycloalkenyl or polycycloalkenyl group; each R1 is independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl, alkylamino, alkylaminoalkyl, alkylaminodialkyl, charged alkylaminotrialkyl or charged alkylcarboxylate radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl, aminodialkyl, charged aminotrialkyl, or carboxylate radical; and n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y; or alternatively R1 may be selected from a peptido radical, for example having from 1 to 4 peptidic moieties linked together by peptide bonds (for example a peptido radical of 1 to 4 amino acid residues).
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（I）的化合物，其中y为1至8的整数; z是0至8的任何整数，条件是y和z不能同时为1; X是-CO-（Y）k-（R1）n或SO2-（Y）k-（R1）n; k是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Y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，烷基氨基，烷基氨基烷基，烷基氨基二烷基，带电荷的烷基氨基三烷基或带电荷的烷基羧酸根。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，氨基二烷基，带电荷的氨基三烷基或羧酸根; n为1〜m的整数，m为环基Y上允许的最大取代数; 或者R1可以选自肽基，例如具有通过肽键连接在一起的1至4个肽部分（例如1至4个氨基酸残基的肽基）。

2. 发明申请

US20130172319A1 Alpha-AminoCycloLactam Ligands for G-Protein Coupled Receptors, and Methods of Using Same 审中-公开
标题翻译：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。

3. 发明授权

US08063106B2 ApoE mimetic agents 失效
标题翻译： ApoE模拟剂
公开(公告)号：US08063106B2
公开(公告)日：2011-11-22
申请号：US12064117
申请日：2006-08-09
申请人： David J. Grainger , David John Fox
发明人： David J. Grainger , David John Fox
IPC分类号： A01N37/18 , A01N37/52 , A61K31/16 , A61K31/155 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00 , C07C277/00 , C07C279/00
CPC分类号： C07K7/02 , A61K31/00 , A61K38/06 , A61K38/07
摘要： The invention provides low molecular weight apoE mimetic agents suitable for preparing a medicament to treat autoimmune, inflammatory or neurodegenerative disease, (X)a-L-(X)b(Formula (I)) wherein each X is a (potentially different) chemical moiety bearing a positive charge at physiological pH a and b are, independently, numbers between 3 and 6; and L is a linker.
摘要翻译：本发明提供适用于制备治疗自身免疫性，炎性或神经变性疾病的药物的低分子量apoE模拟剂（X）aL-（X）b（式（I）），其中每个X是（可能不同的）化学部分轴承生理pH a和b的正电荷分别为3和6之间; 而L是连接体。

4. 发明授权

US07691845B2 Anti-inflammatory agents 失效
标题翻译：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。

5. 发明申请

US20090203739A1 Anti-Inflammatory Agents 审中-公开
标题翻译：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。

6. 发明申请

US20090036486A1 COMPOSITION 失效
标题翻译：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。

7. 发明申请

US20080194541A1 Anti-Inflammatory Agents 失效
标题翻译：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。

8. 发明授权

US08076323B2 Anti-inflammatory agents 失效
标题翻译：抗炎剂
公开(公告)号：US08076323B2
公开(公告)日：2011-12-13
申请号：US12877041
申请日：2010-09-07
申请人： David J. Grainger , David John Fox
发明人： David J. Grainger , David John Fox
IPC分类号： A61K31/55 , A61K31/455 , A61K31/40
CPC分类号： C07D223/12 , A61K31/4015 , A61K31/45 , A61K31/55 , C07D207/267 , C07D207/273 , C07D211/76
摘要： The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(1′-methylcyclohexylcarbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2—; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alklylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radical.
摘要翻译：本发明提供了通式（I）的化合物及其盐的化合物，药物组合物及其用途，用于制备治疗炎症性疾病但不包括（S）-3-（1'-甲基环己基羰基氨基） - 己内酰胺：其中z是1,2,3或4; A是-CO-或-SO 2 - ; Q是直链或支链烷基，烯基，炔基，烷氧基，烷氧基，氨基烷基，烷基氨基，烷基氨基烷基，卤代烷基，芳基或取代的芳基; T1和T2一起构成由n个另外的碳原子组成的环烷基，环烯基或多环烷基，其中n在2和7之间; 并且与由T1和T2生成的环中与碳原子键合的每个氢原子可以独立地被基团R 1取代，其中R 1独立地选自烷基，卤代烷基，烷氧基，卤代烷氧基，烯基，炔基或烷基氨基至20个碳原子; 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。

9. 发明授权

US08008288B2 Anti-inflammatory A-aminocyclolactam compounds 失效
标题翻译：抗炎A-氨基环内酰胺化合物
公开(公告)号：US08008288B2
公开(公告)日：2011-08-30
申请号：US11573851
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： C07D453/06 , C07D487/08 , A61K31/439 , A61K31/55
CPC分类号： A61K31/55 , A61K31/439 , C07D451/14
摘要： The invention provides compounds, compositions, and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, for the preparation of a medicament intended to treat an inflammatory disorder wherein y is any integer from 1 to 8; z is any integer from 1 to 8; with the proviso that y and z cannot both equal 1; X is —C —(Y)k—(R1)n or SO2—(Y)k—(R1)n; k is 0 or 1; Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or Y is a cycloalkenyl or polycycloalkenyl group.
摘要翻译：本发明提供了通式（I）化合物或其药学上可接受的盐的化合物，组合物和用途，用于制备旨在治疗炎性病症的药物，其中y为1至8的整数; z为1〜8的整数; 条件是y和z不能都等于1; X是-C（Y）k-（R1）n或SO2-（Y）k-（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Y是环烯基或多环烯基。

10. 发明授权

US08497261B2 3-aminocaprolactam compounds for treating inflammatory disorders 失效
标题翻译：用于治疗炎症性疾病的3-氨基己内酰胺化合物
公开(公告)号：US08497261B2
公开(公告)日：2013-07-30
申请号：US12726311
申请日：2010-03-17
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 a cycloalkyl or polycycloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or is a cycloalkenyl or polycycloalkenyl group.
摘要翻译：本发明提供了用于制备用于治疗炎性病症的药物的通式（I）化合物或其药学上可接受的盐的化合物，组合物和用途，其为3-氨基己内酰胺衍生物：其中X为-CO-Y- （R1）n或SO2-Y-（R1）n; Y是环烷基或多环烷基（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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式