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1. 发明授权

US06441012B1 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US06441012B1
公开(公告)日：2002-08-27
申请号：US09744331
申请日：2001-01-23
申请人： David R Brittain , Craig Johnstone , Michael S Large , Gareth M Davies
发明人： David R Brittain , Craig Johnstone , Michael S Large , Gareth M Davies
IPC分类号： C07D26358
CPC分类号： C07D263/58 , C07D413/04
摘要： Compound of formula (I) wherein: A is a bicyclic heteroaryl, optionally substituted with one or more substituents; B is linker group connecting group A to group D and comprising a 3 or 4 atom linker where each atom is independently selected from carbon, oxygen, nitrogen and sulphur and is optionally subsituted with one or more C1-6 alkyl groups or two of such adjacent alkyl substituents may form a ring; C is aryl or a mono or bicyclic heteroaryl, each of which can be optionally substituted; D is an aryl or heteroaryl, both of which are optionally substituted R1 is hydrogen, C1-5 alkyl, C1-3 alkanoyl or C1-3 alkoxycarbonyl; R2 to R5 are each independently selected from hydrogen, C1-6 alkyl, aryl and heteroaryl containing up to 2 heteroatoms chosen from oxygen, sulphur and nitrogen, the aryl and heteroaryl optionally substituted with C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-4 alkoxy, C1-4 alkanoyl, C1-6 alkylamino, C1-4alkylC1-6alkyoxyl, C1-6alkylaminoC1-6alkyl, nitro, cyano, halogeno, trifluoromethyl, hydroxy, (CH2)pOH where p is 1 or 2, —CO2Ra, and —CONRaRb, where Ra and Rb are independently selected from hydrogen and C1-6 alkyl or two of R2 to R5 can be taken together to form a 3 to 7 membered ring; R6 is an acidic functional group; r and s are each independently 0 or 1 with the proviso that r and s cannot both be 0; or a pharmaceutically acceptable salt or in vivo hydrolysable derivative thereof.
摘要翻译：式（I）的化合物，其中：A是任选被一个或多个取代基取代的二环杂芳基; B是连接基团A与D组并且包含3或4个原子连接体的连接基团，其中每个原子独立地选自碳，氧，氮和硫，并且任选被一个或多个C 1-6烷基取代或两个相邻的烷基取代基可以形成环; C是芳基或单或双环杂芳基，其各自可任选被取代; D是芳基或杂芳基，它们都是任选取代的R 1是氢，C 1-5烷基，C 1-3烷酰基或C 1-3烷氧基羰基; R 2至R 5各自独立地选自氢，C 1-6烷基，芳基和含有至多2个选自氧，硫和氮的杂原子的杂芳基，芳基和杂芳基任选被C 1-6烷基，C 2-6烯基， 6-炔基，C 1-4烷氧基，C 1-4烷酰基，C 1-6烷基氨基，C 1-4烷基C 1-6烷氧基，C 1-6烷基氨基C 1-6烷基，硝基，氰基，卤代，三氟甲基，羟基，（CH 2）p OH其中p为1或2 ，-CO 2 R a和-CONR a R b，其中R a和R b独立地选自氢和C 1-6烷基，或者R 2至R 5中的两个可以一起形成3至7元环; R6是酸性官能团; r和s各自独立地为0或1，条件是r和s不能都是0; 或其药学上可接受的盐或体内可水解的衍生物。

2. 发明授权

US06344570B1 Substituted urea derivatives as cell adhesion inhibitors 失效
标题翻译：取代的脲衍生物作为细胞粘附抑制剂
公开(公告)号：US06344570B1
公开(公告)日：2002-02-05
申请号：US09554224
申请日：2000-07-11
申请人： David R Brittain , Craig Johnstone
发明人： David R Brittain , Craig Johnstone
IPC分类号： C07D31748
CPC分类号： C07D405/12 , C07C275/34 , C07D317/12 , C07D407/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (II) where R1 is in the para or meta position and is (A); R2 and R3 are each independently selected from hydrogen, nitro, C1-6alkyl, C3-6cycloalkyl, C2-6alkenyl, C2-6alkynyl, C1-4alkoxyl, C1-6alkylamino, C1-6dialkylamino, C1-6akylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, amino, cyano, halogeno, trifluoromethyl, —CO2R12 and —CONR12R13, where R12 and R13 are independently selected from hydrogen or C1-6alkyl, or R2 and R3 together with the phenyl to which they are attached form a 9 or 10 membered bicyclic ring system; R4 is C1-4alkyl; R5 is selected from hydrogen and C1-4alkyl; R6 is selected from C1-6alkyl, C1-4alkyl(C4-6)cycloalkyl, C1-6alkyl(C1-6)alkoxyl, C1-6alkylS(C1-6)alkyl, C1-4alkylsulphonyl(C1-4)alkyl; (B) where q is an integer from 1 to 6 and R14 is halogeno; R7 is selected from C1-6alkyl, C1-8alkoxylcarbonyl, C2-6alkenyl, 1,3-benzodioxol-5-yl and aryl each optionally substituted by one or more substituents selected from C1-4alkoxy, C1-6alkyl, cyano, halogeno, and trifluoromethyl; R8 is aryl, heteroaryl, a bicyclic heteroaryl ring system linked to the nitrogen via a ring carbon or a 9 or 10 membered bicyclic ring system linked to the nitrogen via a ring carbon and each ring is optionally substituted with up to two substituents, which may be the same or different, and are selected from C1-6alkyl, C1-4alkoxy, C1-4alkylthio, C1-6alkylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, hydroxy, —CO2H, —(CH2)pOH where p is 1 or 2, cyano, halogeno, and trifluoromethyl; R9 and R10 are each independently selected from hydrogen and C1-4alkyl or R8 and R9 together with the nitrogen to which they are attached form a dihydroindolyl, or a dihidroquinolinyl group; R11 is selected from carboxyl, tetrazolyl, alkyl sulphonylcarbamyl, sulfo and sulfino; Y is oxygen, sulphur or sulfonyl; m is 0 or 1; and n is 0 or an integer from 1 to 4 with the proviso that when m and n cannot both be 0 and when m is 1, n is 0; or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof. The compounds inhibit the interaction of vascular cell-adhesion molecule-1 and fibronectin with integrin very late antigen 4 (&agr;4&bgr;1). They have therapeutic applications such as in multiple sclerosis, rheumatoid arthritis, asthma, coronary artery disease and psoriasis.
摘要翻译：其中R1为对位或间位且为（A）的式（II）化合物; R 2和R 3各自独立地选自氢，硝基，C 1-6烷基，C 3-6环烷基，C 2-6烯基，C 2-6炔基，C 1-4烷氧基，C 1-6烷基氨基，C 1-6二烷基氨基，C 1-6烷基C 1-4烷氧基，C 1-6烷基氨基C 1- 6烷基，氨基，氰基，卤代，三氟甲基，-CO 2 R 12和-CONR 12 R 13，其中R 12和R 13独立地选自氢或C 1-6烷基，或者R 2和R 3与它们所连接的苯基一起形成9或10元双环环系; R4是C1-4烷基; R5选自氢和C 1-4烷基; R 6选自C 1-6烷基，C 1-4烷基（C 4-6）环烷基，C 1-6烷基（C 1-6）烷氧基，C 1-6烷基S（C 1-6）烷基，C 1-4烷基磺酰基（C 1-4）烷基; （B）其中q是1至6的整数，R 14是卤素; R 7选自C 1-6烷基，C 1-8烷氧基羰基，C 2-6烯基，1,3-苯并间二氧杂环戊烯-5-基和各自任选被一个或多个选自C 1-4烷氧基，C 1-6烷基，氰基，卤代和三氟甲基 R 8是芳基，杂芳基，通过环碳与氮连接的双环杂芳基环系统，或通过环碳与氮连接的9或10元双环体系，并且每个环任选被至多两个取代基取代，选自C 1-6烷基，C 1-4烷氧基，C 1-4烷硫基，C 1-6烷基C 1-4烷氧基，C 1-6烷基氨基C 1-6烷基，羟基，-CO 2 H， - （CH 2）p OH，其中p为1或2 ，氰基，卤代和三氟甲基; R9和R

3. 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。

4. 发明授权

US07572826B2 Thiophene-carboxamide derivatives and their use as inhibitors of the enzyme IKK-2 失效
标题翻译：噻吩 - 甲酰胺衍生物及其作为IKK-2酶抑制剂的用途
公开(公告)号：US07572826B2
公开(公告)日：2009-08-11
申请号：US10542326
申请日：2004-01-13
申请人： Alan Wellington Faull , Craig Johnstone , Andrew David Morley , Jeffrey Philip Poyser
发明人： Alan Wellington Faull , Craig Johnstone , Andrew David Morley , Jeffrey Philip Poyser
IPC分类号： A61K31/381 , C07D333/36
CPC分类号： C07D409/12 , C07D333/38 , C07D333/44 , C07D413/12
摘要： The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明涉及式（I）的噻吩甲酰胺，其中A，R 1，R 2，R 3，R 4，R 5和X如说明书中所定义，其制备中使用的方法和中间体，含有它们的药物组合物及其在治疗中的用途。

5. 发明申请

US20090062351A1 Benzoyl amino pyridyl carboxylic acid derivatives useful as glucokinase (glk) activators 审中-公开
标题翻译：可用作葡萄糖激酶（glk）激活剂的苯甲酰氨基吡啶羧酸衍生物
公开(公告)号：US20090062351A1
公开(公告)日：2009-03-05
申请号：US10579782
申请日：2004-12-02
申请人： Peter William Rodney Caulkett , Craig Johnstone , Darren McKerrecher , Kurt Gordon Pike
发明人： Peter William Rodney Caulkett , Craig Johnstone , Darren McKerrecher , Kurt Gordon Pike
IPC分类号： A61K31/44 , C07D213/72 , A61P3/00
CPC分类号： C07D213/80
摘要： A compound of Formula (I): Formula (I) wherein: R1 is selected from hydrogen and C1-4alkyl; R2 is selected from: R4—C(R5aR5b)—, R4═C(R6)— and R7aC(R7b)═C(R6)—; R3X— is selected from methyl, methoxymethyl and; R4 is selected from (optionally substituted) C1-4alkyl, phenyl, C3-6cycloalkyl and heteroaryl; R5a and R5b are independently selected from hydrogen, fluoro and C1-4alkyl; R6 is selected from hydrogen and C1-4alkyl; R7a and R7b are optionally substituted C1-4alkyl; or a salt, pro-drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.
摘要翻译：式（I）的化合物：式（I）其中：R 1选自氢和C 1-4烷基; R2选自：R4-C（R5aR5b） - ，R4-C（R6） - 和R7aC（R7b）-C（R6） - ; R3X-选自甲基，甲氧基甲基和 R 4选自（任选取代的）C 1-4烷基，苯基，C 3-6环烷基和杂芳基; R5a和R5b独立地选自氢，氟和C1-4烷基; R6选自氢和C 1-4烷基; R7a和R7b是任选取代的C 1-4烷基; 或其盐，前药或溶剂化物。还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。

6. 发明申请

US20080312207A1 Compounds 审中-公开
标题翻译：化合物
公开(公告)号：US20080312207A1
公开(公告)日：2008-12-18
申请号：US10588315
申请日：2005-02-15
申请人： Craig Johnstone , Darren McKerrecher , Kurt Gordon Pike
发明人： Craig Johnstone , Darren McKerrecher , Kurt Gordon Pike
IPC分类号： A61K31/397 , C07D417/12 , A61K31/496 , C07D277/20 , A61K31/426 , C07D413/12 , A61K31/454 , A61K31/422 , C07D405/12 , A61K31/4155 , C07D403/12
CPC分类号： C07D213/75 , C07D231/40 , C07D241/20 , C07D263/48 , C07D277/46 , C07D285/135 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/04 , C07D417/12
摘要： Compounds of Formula (I) wherein: R1 is methyl; R2 is selected from —C (O) NR4R5, SO2NR4R5, S (O) pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C) alkyl and HET-2; R5 is hydrogen or (1-4C) alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them and processes for their preparation are also described.
摘要翻译：式（I）的化合物，其中：R 1是甲基; R2选自-C（O）NR4R5，SO2NR4R5，S（O）pR4和HET-2; HET-1是5-或6-元，任选取代的C连接的杂芳基环; HET-2是4-，5-或6-元C-或N-连接的任选取代的杂环基环; R 3选自卤素，氟甲基，二氟甲基，三氟甲基，甲基，甲氧基和氰基; R4选自例如氢，任选取代的（1-4C）烷基和HET-2; R5是氢或（1-4C）烷基; 或R 4和R 5与它们所连接的氮原子一起可以形成由HET-3定义的杂环基环系统; HET-3是例如任选取代的N-连接的，4,5或6元饱和或部分不饱和的杂环基环; p是（每次出现时独立）0,1或2; m为0或1; n为0,1或2; 条件是当m为0时，n为1或2; 或其盐，前药或溶剂化物。还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。

7. 发明申请

US20080280874A1 Phenoxy Benzamide Compounds with Utility in the Treatment of Type 2 Diabetes and Obesity 审中-公开
标题翻译：苯氧基苯甲酰胺化合物在治疗2型糖尿病和肥胖中的应用
公开(公告)号：US20080280874A1
公开(公告)日：2008-11-13
申请号：US11665163
申请日：2005-10-11
申请人： Craig Johnstone , Darren Mckerrecher , Kurt Gordon Pike , Michael James Waring
发明人： Craig Johnstone , Darren Mckerrecher , Kurt Gordon Pike , Michael James Waring
IPC分类号： A61K31/397 , C07D231/10 , A61P3/10 , A61K31/415
CPC分类号： C07D213/80 , C07D231/40 , C07D403/12
摘要： Compounds of Formula (I): wherein: R1 is methoxymethyl; R2 is selected from —C(O)NR4R5, —SO2NR4R5, —S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro-drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.
摘要翻译：式（I）的化合物：其中：R 1是甲氧基甲基; R 2选自-C（O）NR 4 R 5，-SO 2 NR 2， 4个，5个，-S（O）4个S 4和4个HET-2; HET-1是5-或6-元，任选取代的C连接的杂芳基环; HET-2是4-，5-或6-元C-或N-连接的任选取代的杂环基环; R 3选自卤素，氟甲基，二氟甲基，三氟甲基，甲基，甲氧基和氰基; R 4选自例如氢，任选取代的（1-4C）烷基和HET-2; R 5是氢或（1-4C）烷基; 或R 4和R 5与它们所连接的氮原子一起可以形成由HET-3定义的杂环基环系; HET-3是例如任选取代的N-连接的，4,5或6元饱和或部分不饱和的杂环基环; p是（每次出现时独立）0,1或2; m为0或1; n为0,1或2; 条件是当m为0时，n为1或2; 或其盐，前药或溶剂化物。还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。

8. 发明申请

US20080207636A1 Compounds Effecting Glucokinase 失效
标题翻译：影响葡萄糖激酶的化合物
公开(公告)号：US20080207636A1
公开(公告)日：2008-08-28
申请号：US12024561
申请日：2008-02-01
申请人： Scott Boyd , Peter William Rodney Caulkett , Rodney Brian Hargreaves , Suzanne Saxon Bowker , Roger James , Clifford David Jones , Darren McKerrecher , Michael Howard Block , Craig Johnstone
发明人： Scott Boyd , Peter William Rodney Caulkett , Rodney Brian Hargreaves , Suzanne Saxon Bowker , Roger James , Clifford David Jones , Darren McKerrecher , Michael Howard Block , Craig Johnstone
IPC分类号： A61K31/496 , C07D277/20 , A61K31/426 , A61K31/433 , A61P3/10 , A61K31/4436 , A61K31/415 , C07D231/10 , C07D213/02 , A61P3/04 , C07D285/12 , C07D295/00
CPC分类号： C07D213/75 , A61K31/165 , A61K31/195 , A61K31/425 , A61K31/445 , C07D213/82 , C07D213/85 , C07D231/40 , C07D233/48 , C07D237/20 , C07D237/24 , C07D239/42 , C07D241/20 , C07D241/26 , C07D261/14 , C07D277/46 , C07D277/56 , C07D277/82 , C07D285/135 , C07D307/66 , C07D401/04 , C07D403/04 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).
摘要翻译：本发明涉及式（I）化合物或其盐，溶剂合物或前体药物的用途，其中R 1，R 2，R 3， N和m如说明书中所述，在制备用于治疗或预防通过葡萄糖激酶（GLK）如2型糖尿病介导的疾病状况的药物中的描述。本发明还涉及一组新的式（I）化合物和制备式（I）化合物的方法。

9. 发明申请

US20070015819A1 Novel compounds 失效
标题翻译：新型化合物
公开(公告)号：US20070015819A1
公开(公告)日：2007-01-18
申请号：US11516225
申请日：2006-09-06
申请人： Alan Faull , Craig Johnstone , Andrew Morley , Jeffrey Poyser
发明人： Alan Faull , Craig Johnstone , Andrew Morley , Jeffrey Poyser
IPC分类号： A61K31/381 , C07D333/38 , C07D333/32 , A61K31/55 , A61K31/541 , A61K31/5377 , A61K31/454 , A61K31/453
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D333/38 , C07D409/04 , C07D409/10 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/12 , C07D487/08 , C07D491/08
摘要： The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明涉及式（I）的噻吩甲酰胺，其中A，R 1，R 2，R 3，n和X分别为在其制备中使用的说明书，方法和中间体中定义，含有它们的药物组合物及其在治疗中的用途。

10. 发明授权

US07125896B2 Thiophene carboxamide compounds as inhibitors of enzyme IKK-2 失效
标题翻译：噻吩甲酰胺化合物作为酶IKK-2的抑制剂
公开(公告)号：US07125896B2
公开(公告)日：2006-10-24
申请号：US10484569
申请日：2002-07-19
申请人： Alan Faull , Craig Johnstone , Andrew Morley , Philip Jeffrey Poyser
发明人： Alan Faull , Craig Johnstone , Andrew Morley , Philip Jeffrey Poyser
IPC分类号： A61K31/4436 , C07D409/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D333/38 , C07D409/04 , C07D409/10 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/12 , C07D487/08 , C07D491/08
摘要： The invention relates to thiophene carboxanmides of formula (I), wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明涉及式（I）的噻吩甲酰胺，其中A，R 1，R 2，R 3，n和X分别为在其制备中使用的说明书，方法和中间体中定义，含有它们的药物组合物及其在治疗中的用途。

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