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1. 发明申请

US20130116318A1 Enzyme Inhibitors 有权
标题翻译：酶抑制剂
公开(公告)号：US20130116318A1
公开(公告)日：2013-05-09
申请号：US12957829
申请日：2010-12-01
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
IPC分类号： A61K31/381 , A61K31/27
CPC分类号： C07C237/40 , C07C259/06 , C07C275/24 , C07C311/46 , C07C317/50 , C07C2601/08 , C07C2601/14 , C07D207/416 , C07D209/42 , C07D213/40 , C07D217/02 , C07D217/22 , C07D217/26 , C07D295/185 , C07D295/192 , C07D333/70 , C07D471/04
摘要： Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers:
摘要翻译：式（I）化合物是组蛋白脱乙酰酶活性的抑制剂，可用于治疗例如癌症：

2. 发明授权

US08686032B2 Enzyme inhibitors 有权
标题翻译：酶抑制剂
公开(公告)号：US08686032B2
公开(公告)日：2014-04-01
申请号：US12957829
申请日：2010-12-01
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
IPC分类号： A61K31/381 , A61K31/27 , C07C271/02 , C07C271/06
CPC分类号： C07C237/40 , C07C259/06 , C07C275/24 , C07C311/46 , C07C317/50 , C07C2601/08 , C07C2601/14 , C07D207/416 , C07D209/42 , C07D213/40 , C07D217/02 , C07D217/22 , C07D217/26 , C07D295/185 , C07D295/192 , C07D333/70 , C07D471/04
摘要： Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers:
摘要翻译：式（I）化合物是组蛋白脱乙酰酶活性的抑制剂，可用于治疗例如癌症：

3. 发明申请

US20090291978A1 Enzyme Inhibitors 有权
公开(公告)号：US20090291978A1
公开(公告)日：2009-11-26
申请号：US11918139
申请日：2006-05-04
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
IPC分类号： A61K31/437 , C07D471/02 , C07C229/28 , A61K31/216 , A61K31/192 , C07D217/00 , A61K31/472 , C07D213/72 , A61K31/44 , C07D209/04 , A61K31/404 , C07D333/50 , A61K31/381 , A61P35/00 , A61P25/00 , A61P29/00 , A61P3/10 , A61P37/06
CPC分类号： C07C237/40 , C07C259/06 , C07C275/24 , C07C311/46 , C07C317/50 , C07C2601/08 , C07C2601/14 , C07D207/416 , C07D209/42 , C07D213/40 , C07D217/02 , C07D217/22 , C07D217/26 , C07D295/185 , C07D295/192 , C07D333/70 , C07D471/04
摘要： Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, C(═O)—, —S(═O)2—, —C(—O)O—, —C(O)NR3—, —C(═S)—NR3, —C(═NH)NR3 or —S(═O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L is a divalent radical of formula -(Alk1)m(O)n(Alk2)p— wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or hetero-cyclic radical having 5-13 ring members, AIk1 and AIk2 independently represent optionally substituted divalent C3-C7 cycloalkyl radicals, or optionally substituted straight or branched, C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals which may optionally contain or terminate in an ether (—O—), thioether (—S—) or amino (—NRA-) link wherein RA is hydrogen or optionally substituted C1-C3 alkyl; X represents a bond; —C(═O); or —S(═O)2—; —NR4C(═O)—, —C(═O)NR4—, —NR4C(═O)NR5—, —NR4S(═O)2—, or —S(═O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; z is 0 or 1; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system wherein the radicals R1R2NH—Y-L1-X1—[CH2]z— and HONHCO-[LINKER]- are attached different ring atoms; and -[Linker]- represents a divalent linker radical linking a ring atom in A with the hydroxamic acid group CONHOH, the length of the linker radical, from the terminal atom linked to the ring atom of A to the terminal atom linked to the hydroxamic acid group, is equivalent to that of an unbranched saturated hydrocarbon chain of from 3-10 carbon atoms.

4. 发明申请

US20100004250A1 PTERIDINE DERIVATIVES AS POLO-LIKE KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER 审中-公开
标题翻译：作为类似于激素治疗癌症的类激酶抑制剂的哌替啶衍生物
公开(公告)号：US20100004250A1
公开(公告)日：2010-01-07
申请号：US12447011
申请日：2007-09-25
申请人： Oliver James Philips , Julie Mathilde Thibaud , Carl Leslie North , David Festus Moffat , Sanjay Ratilal Patel
发明人： Oliver James Philips , Julie Mathilde Thibaud , Carl Leslie North , David Festus Moffat , Sanjay Ratilal Patel
IPC分类号： A61K31/4985 , C07D401/14 , A61P35/00 , C07D475/00
CPC分类号： C07D475/00
摘要： Compounds of formula (I) are inhibitors of Polo-like kinases (PLKs), and are useful, inter alia, in the treatment of proliferative diseases: wherein R1 is hydrogen, or a (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl group; R2 is hydrogen, or an optionally substituted (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl group; R3 and R3′ are independently selected from hydrogen, —CN, hydroxyl, halogen, optionally substituted (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl, —NR6R7 or C1-C4 alkoxy, wherein R6 and R7 are independently hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted mono- or bi-cyclic carbocyclic or heterocyclic ring or ring system having up to 12 ring atoms; T is a radical of formula (II) R4R5CH—NH—Y-L1-X1— (II) Wherein R4 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R5 is the side chain of a natural or non-natural alpha amino acid; and the linker radical —Y-L1-X1 is as defined in the claims.
摘要翻译：式（I）化合物是Polo样激酶（PLK）的抑制剂，尤其可用于治疗增殖性疾病：其中R1是氢或（C1-C6）烷基，（C2-C6）烷基，烯基，（C 2 -C 6）炔基或（C 3 -C 6）环烷基; R 2是氢或任选取代的（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 2 -C 6）炔基或（C 3 -C 6）环烷基; R 3和R 3'独立地选自氢，-CN，羟基，卤素，任选取代的（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 2 -C 6）炔基或（C 3 -C 6）环烷基，-NR 6 R 7或 C 1 -C 4烷氧基，其中R 6和R 7独立地为氢或任选取代的（C 1 -C 6）烷基; 环A是具有至多12个环原子的任选取代的单环或双环碳环或杂环或环系; T是式（II）的基团R4R5CH-NH-Y-L1-X1-（II）其中R4是羧酸基（-COOH）或可被一种或多种细胞内酯酶水解成的酯基羧酸基; R5是天然或非天然α氨基酸的侧链; 并且连接基自由基-Y-L1-X1如权利要求中所定义。

5. 发明授权

US07939666B2 Enzyme inhibitors 有权
标题翻译：酶抑制剂
公开(公告)号：US07939666B2
公开(公告)日：2011-05-10
申请号：US11918139
申请日：2006-05-04
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Moffat , Kenneth William John Baker , Alistair David Graham Donald
IPC分类号： C07D471/02 , C07D217/00 , C07D213/72 , C07D209/04 , C07D333/50 , C07C229/28
CPC分类号： C07C237/40 , C07C259/06 , C07C275/24 , C07C311/46 , C07C317/50 , C07C2601/08 , C07C2601/14 , C07D207/416 , C07D209/42 , C07D213/40 , C07D217/02 , C07D217/22 , C07D217/26 , C07D295/185 , C07D295/192 , C07D333/70 , C07D471/04
摘要： Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers.
摘要翻译：式（I）化合物是组蛋白脱乙酰酶活性的抑制剂，可用于治疗例如癌症。

6. 发明申请

US20050171134A1 4,5-Disubstituted-2-aminopyrimidines 审中-公开
标题翻译： 4,5-二取代-2-氨基嘧啶
公开(公告)号：US20050171134A1
公开(公告)日：2005-08-04
申请号：US11090474
申请日：2005-03-25
申请人： Jeremy Davis , David Festus Moffat
发明人： Jeremy Davis , David Festus Moffat
IPC分类号： A61K31/505 , A61P9/00 , A61P9/10 , A61P9/14 , A61P17/06 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D239/42 , C07D401/12 , C07D403/12 , C07D521/00 , A61K31/506 , C07D43/02
CPC分类号： C07D239/42 , A61K31/505 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12
摘要： Pyrimidines of formla (1) are described: wherein R1 is a —XR6 group; R2 and R3 which may be the same or different is each a hydrogen or halogen atom or a group selected from an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, —OH, —OR10 [where R10 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group) —SH, —NO2, —CN, —SR10, —COR10, S(O)R10, —SO2R8, —SO2N(R8)(R9), —CO2R8, —CON(R8)(R9), —CSN(R8)(R9), —NH2 or substituted amino group; R4 is a X1R11 group where X1 is a covalent bond or a —C(R12)(R13)— [where each of R12 and R13 is a hydrogen or halogen atom or a hydroxyl, alkyl or haloalkyl group] or —C(O)— group and R11 is an optionally substituted phenyl, thienyl, thiazolyl or indolyl group; R5 is a halogen atom or an alkynyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective KDR kinase and/or FGFr kinase inhibitors and are of use in the prophylaxis and treatment of disease states associated with angiogenesis
摘要翻译：描述了formla（1）的嘧啶：其中R 1是-XR 6 C 6; R 2和R 3可以相同或不同，各自为氢或卤素原子或选自任选取代的脂族，脂环族，杂脂肪族，杂环脂族， OH，-OR 10 [其中R 10是任选取代的脂族，脂环族，杂脂族，杂脂族，芳族或杂芳族基团）-SH，-NO 2， -CON，-SR 10，-COR 10，S（O）R 10，-SO 2，（R 9），-SO 2 N（R 8）， - CO 2， -CON（R 8）（R 9），-CSN（R 8），R 8，（R 9），-NH 2或取代的氨基; R 4是其中X 1是共价键或C（R（R 1））的X 1，R 11，（R 13） - [其中R 12和R 12各自为氢或卤素原子或羟基，烷基或卤代烷基]或-C（O） - 基，R 11是任选取代的苯基，噻吩基，噻唑基或吲哚基; R 5是卤素原子或炔基; 及其盐，溶剂合物，水合物和N-氧化物。这些化合物是选择性KDR激酶和/或FGFr激酶抑制剂，并且可用于预防和治疗与血管发生相关的疾病状态

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