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1. 发明申请

US20100173958A1 COMPOUNDS FOR THE INHIBITION OF DGAT1 ACTIVITY 审中-公开
标题翻译：用于抑制DGAT1活性的化合物
公开(公告)号：US20100173958A1
公开(公告)日：2010-07-08
申请号：US12303862
申请日：2007-06-08
申请人： Stuart Norman Lile Bennett , Roger John Butlin , Alleyn Thomas Plowright
发明人： Stuart Norman Lile Bennett , Roger John Butlin , Alleyn Thomas Plowright
IPC分类号： A61K31/4245 , C07D271/07 , A61P3/10
CPC分类号： C07D271/113
摘要： Compounds of formula (I), or salts thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein, for example, R1 is optionally substituted phenyl or naphthyl; Ring A is selected from (3-6C)cycloalkyl, (5-12C)bicycloalkyl and phenyl; n is 0, 1 or 2; R2 is, for example, hydrogen, fluoro, chloro or hydroxy; Ring B is selected from (3-6C)cycloalkyl, (5-12C)bicycloalkyl and phenyl; L1 is a direct bond or a defined linker group and R3 is, for example, hydroxy, carboxy or (1-6C)alkoxycarbonyl; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译：提供抑制乙酰CoA（乙酰辅酶A）：二酰基甘油酰基转移酶（DGAT1）活性的式（I）化合物或其盐，其中，例如，R 1为任选取代的苯基或萘基; 环A选自（3-6C）环烷基，（5-12C）双环烷基和苯基; n为0,1或2; R2是例如氢，氟，氯或羟基; 环B选自（3-6C）环烷基，（5-12C）双环烷基和苯基; L1是直接键或定义的连接基团，R 3是例如羟基，羧基或（1-6C）烷氧基羰基; 以及其制备方法，含有它们的药物组合物及其作为药物的用途。

2. 发明申请

US20090124682A1 Indan-Amide Derivatives with Glycogen Phosphorylase Inhibitory Activity 审中-公开
标题翻译：具有糖原磷酸化酶抑制活性的茚满酰胺衍生物
公开(公告)号：US20090124682A1
公开(公告)日：2009-05-14
申请号：US11883770
申请日：2006-02-02
申请人： Alan Martin Birch , Craig Johnstone , Alleyn Thomas Plowright , Iain Simpson , Paul Robert Owen Whittamore
发明人： Alan Martin Birch , Craig Johnstone , Alleyn Thomas Plowright , Iain Simpson , Paul Robert Owen Whittamore
IPC分类号： A61K31/40 , C07D209/42 , A61P3/10 , A61P3/04 , A61P9/10
CPC分类号： C07D209/42
摘要： A compound of the formula (1) or a pharmaceutically-acceptable salt: (A chemical formula should be inserted here—please see paper copy enclosed herewith) (1) possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.
摘要翻译：式（1）化合物或其药学上可接受的盐：（化学式应插入此处，请参见随附的纸质复制品）（1）具有糖原磷酸化酶抑制活性，因此具有治疗疾病相关的价值具有增加的糖原磷酸化酶活性。描述了制备含有它们的化合物和药物组合物的方法。

3. 发明授权

US08084478B2 Substituted 5- phenylamino- 1, 3, 4-oxadiazol-2-ylcarbonylamino-4-phenoxy-cyclohexane carboxylic acid as inhibitors of acetyl coenzyme A diacylglycerol acyltransferase 失效
标题翻译：取代的5-苯基氨基-1,3,4-恶二唑-2-基羰基氨基-4-苯氧基 - 环己烷羧酸作为乙酰辅酶A二酰基甘油酰基转移酶
公开(公告)号：US08084478B2
公开(公告)日：2011-12-27
申请号：US12302185
申请日：2007-05-29
申请人： Roger John Butlin , Alleyn Thomas Plowright
发明人： Roger John Butlin , Alleyn Thomas Plowright
IPC分类号： A61K31/4245 , C07D271/113
CPC分类号： C07D271/10 , C07D271/113
摘要： Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein R1, R2 and R3 are each independently selected from hydrogen, fluoro, chloro, cyano, trifluoromethyl, trifluoromethoxy and difluoromethoxy; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译：提供了抑制乙酰CoA（乙酰辅酶A）：二酰基甘油酰基转移酶（DGAT1）活性的式（I）化合物或其盐，其中R 1，R 2和R 3各自独立地选自氢，氟，氯，氰基，三氟甲基，三氟甲氧基和二氟甲氧基; 以及其制备方法，含有它们的药物组合物及其作为药物的用途。

4. 发明申请

US20110092547A1 CHEMICAL COMPOUNDS 979 审中-公开
标题翻译：化学化合物979
公开(公告)号：US20110092547A1
公开(公告)日：2011-04-21
申请号：US12673767
申请日：2008-08-15
申请人： Alan Martin Birch , Roger John Butlin , Adrian Liam Gill , Samuel David Groombridge , Alleyn Thomas Plowright , Michael James Waring
发明人： Alan Martin Birch , Roger John Butlin , Adrian Liam Gill , Samuel David Groombridge , Alleyn Thomas Plowright , Michael James Waring
IPC分类号： A61K31/4439 , C07D413/12 , A61P3/10 , A61P3/04
CPC分类号： C07D413/12
摘要： Compounds of formula (I), or pharmaceutically-acceptable salts and/or pro-drugs thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein n is 0 to 3; p is 0 or 1; q is 0 to 2; R1 and R2 are, for example, independently fluoro, chloro, bromo, cyano or (1-4C)alkyl; X is —O—, —S— or —NRa— wherein Ra is hydrogen or (1-4C)alkyl; RA1 and RA2 are, for example, independently hydrogen or (1-4C)alkyl; Ring A is a di-linked ring or ring system chosen from (4-6C)cycloalkane, (7-10C)bicycloalkane and (8-12C)tricycloalkane each optionally substituted, for example, by one substituent selected from (1-4C)alkyl, (1-4C)alkoxy and (1-4C)alkoxy(1-4C)alkyl; or Ring A is phenylene optionally substituted, for example, by up to four substituents selected from fluoro, chloro, bromo, cyano, (1-4C)alkyl, (1-4C)alkoxy and (1-4C)alkoxy(1-4C)alkyl; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译：提供了抑制乙酰辅酶A（乙酰辅酶A）：二酰基甘油酰基转移酶（DGAT1）活性的式（I）化合物或其药学上可接受的盐和/或其前体药物，其中n为0-3; p为0或1; q为0〜2; R 1和R 2例如独立地为氟，氯，溴，氰基或（1-4C）烷基; X是-O - ， - S-或-NRa-，其中R a是氢或（1-4C）烷基; RA1和RA2例如独立地为氢或（1-4C）烷基; 环A是选自（4-6C）环烷烃，（7-10C）双环烷烃和（8-12C）三环烷烃的二联环或环系，每个任选被例如一个选自（1-4C）的取代基取代，烷基，（1-4C）烷氧基和（1-4C）烷氧基（1-4C）烷基; 或环A为任选取代的亚苯基，例如至多四个选自氟，氯，溴，氰基，（1-4C）烷基，（1-4C）烷氧基和（1-4C）烷氧基（1-4C））烷基; 以及其制备方法，含有它们的药物组合物及其作为药物的用途。

5. 发明申请

US20100137397A1 Chemical Compounds 审中-公开
标题翻译：化学化合物
公开(公告)号：US20100137397A1
公开(公告)日：2010-06-03
申请号：US11815418
申请日：2006-02-02
申请人： Alan Martin Birch , Craig Johnstone , Alleyn Thomas Plowright , Iain Simpson , Paul Robert Owen Whittamore
发明人： Alan Martin Birch , Craig Johnstone , Alleyn Thomas Plowright , Iain Simpson , Paul Robert Owen Whittamore
IPC分类号： A61K31/407 , C07D495/04 , A61P3/10 , A61P9/00 , A61P3/04
CPC分类号： C07D495/04
摘要： A compound of the formula (1) or a pharmaceutically-acceptable salt: possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity such as 2 diabetes. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.
摘要翻译：式（1）的化合物或药学上可接受的盐：具有糖原磷酸化酶抑制活性，因此在治疗与糖原磷酸化酶活性增加相关的疾病状态如2型糖尿病中具有价值。描述了制备含有它们的化合物和药物组合物的方法。

6. 发明申请

US20110152297A1 QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS 有权
标题翻译：喹唑啉衍生物作为酪氨酸激酶抑制剂
公开(公告)号：US20110152297A1
公开(公告)日：2011-06-23
申请号：US11884923
申请日：2006-02-24
申请人： Christopher Thomas Halsall , Laurent Francois Andre Hennequin , Alleyn Thomas Plowright , Richard Storey , Kieran Lennon
发明人： Christopher Thomas Halsall , Laurent Francois Andre Hennequin , Alleyn Thomas Plowright , Richard Storey , Kieran Lennon
IPC分类号： A61K31/517 , C07D401/12 , A61P35/00
CPC分类号： C07D401/12
摘要： The invention concerns quinazoline derivatives of the Formula I, or pharmaceutically acceptable salts thereof: wherein each of R1, R2, R3, R4 and m are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula I are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, and, for example, EGFR tyrosine kinase.
摘要翻译：本发明涉及式I的喹唑啉衍生物或其药学上可接受的盐：其中R1，R2，R3，R4和m各自如说明书中所定义; 其准备过程; 含有它们的药物组合物及其在制备用于提供抗增殖作用的药物中的用途。预期式I的喹唑啉衍生物可用于治疗疾病，例如由erbB受体酪氨酸激酶介导的某些癌症，以及例如EGFR酪氨酸激酶。

7. 发明申请

US20090275620A1 SUBSTITUTED 5- PHENYLAMINO- 1, 3, 4-OXADIAZOL-2-YLCARBONYLAMINO-4-PHENOXY-CYCLOHEXANE CARBOXYLIC ACID AS INHIBITORS OF ACETYL COENZYME A DIACYLGLYCEROL ACYLTRANSFERASE 失效
标题翻译：取代的5-苯基氨基亚磺酰基-1,3,4-氧杂双环-2-甲基亚氨基-4-羟基 - 环己烷羧酸作为乙酰苯胺的一种抑制剂二乙酰胆碱酯酶
公开(公告)号：US20090275620A1
公开(公告)日：2009-11-05
申请号：US12302185
申请日：2007-05-29
申请人： Roger John Butlin , Alleyn Thomas Plowright
发明人： Roger John Butlin , Alleyn Thomas Plowright
IPC分类号： A61K31/4245 , C07D271/10
CPC分类号： C07D271/10 , C07D271/113
摘要： Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein R1, R2 and R3 are each independently selected from hydrogen, fluoro, chloro, cyano, trifluoromethyl, trifluoromethoxy and difluoromethoxy; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译：提供了抑制乙酰CoA（乙酰辅酶A）：二酰基甘油酰基转移酶（DGAT1）活性的式（I）化合物或其盐，其中R 1，R 2和R 3各自独立地选自氢，氟，氯，氰基，三氟甲基，三氟甲氧基和二氟甲氧基; 以及其制备方法，含有它们的药物组合物及其作为药物的用途。

8. 发明申请

US20090197926A1 BENZIMIDAZOLES AND THEIR USE FOR THE TREATMENT OF DIABETES 审中-公开
标题翻译：苯并咪唑及其用于治疗糖尿病的用途
公开(公告)号：US20090197926A1
公开(公告)日：2009-08-06
申请号：US12303512
申请日：2007-06-06
申请人： Alan Martin Birch , Roger John Butlin , Alleyn Thomas Plowright
发明人： Alan Martin Birch , Roger John Butlin , Alleyn Thomas Plowright
IPC分类号： A61K31/4245 , C07D413/04 , A61P3/00
CPC分类号： C07D413/04 , C07D413/14
摘要： Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein: R1 is selected from optionally substituted phenyl, cyclopentyl, cyclohexyl and 5- or 6-membered heteroaryl; L1 is a direct bond or a linker selected from, for example, —O—, —OCH2— and —CH2O—; R2 is selected from, for example, (3-6C)cycloalkyl, (5-12C)bicycloalkyl, phenyl and a 4, 5- or 6-membered saturated, partially or fully unsaturated heterocyclyl ring; wherein R2 is substituted by defined substituents and R6 is selected from, for example, hydrogen, fluoro and chloro; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译：提供了抑制乙酰CoA（乙酰辅酶A）：二酰基甘油酰基转移酶（DGAT1）活性的式（I）化合物或其盐，其中：R 1选自任选取代的苯基，环戊基，环己基和5-或6-元杂芳基; L1是直接键或选自例如-O - ， - OCH 2 - 和-CH 2 O-的连接基团; R2选自例如（3-6C）环烷基，（5-12C）双环烷基，苯基和4,5或6元饱和，部分或完全不饱和的杂环基环; 其中R 2被定义的取代基取代，并且R 6选自例如氢，氟和氯; 以及其制备方法，含有它们的药物组合物及其作为药物的用途。

9. 发明授权

US08735410B2 Quinazoline derivatives as tyrosine kinase inhibitors 有权
标题翻译：喹唑啉衍生物作为酪氨酸激酶抑制剂
公开(公告)号：US08735410B2
公开(公告)日：2014-05-27
申请号：US11884923
申请日：2006-02-24
申请人： Christopher Thomas Halsall , Laurent Francois Andre Hennequin , Alleyn Thomas Plowright , Richard Storey , Kieran Lennon
发明人： Christopher Thomas Halsall , Laurent Francois Andre Hennequin , Alleyn Thomas Plowright , Richard Storey , Kieran Lennon
IPC分类号： A01N43/54 , A61K31/517
CPC分类号： C07D401/12
摘要： The invention concerns quinazoline derivatives of the Formula I, or pharmaceutically acceptable salts thereof: wherein each of R1, R2, R3, R4 and m are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula I are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, and, for example, EGFR tyrosine kinase.
摘要翻译：本发明涉及式I的喹唑啉衍生物或其药学上可接受的盐：其中R1，R2，R3，R4和m各自如说明书中所定义; 其准备过程; 含有它们的药物组合物及其在制备用于提供抗增殖作用的药物中的用途。预期式I的喹唑啉衍生物可用于治疗疾病，例如由erbB受体酪氨酸激酶介导的某些癌症，以及例如EGFR酪氨酸激酶。

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