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1. 发明申请

WO2004072051A1 ISOXAZOLE COMPOUNDS AS INHIBITORS OF HEAT SHOCK PROTEINS 审中-公开
标题翻译：作为热休克蛋白的抑制剂的异噻唑化合物
公开(公告)号：WO2004072051A1
公开(公告)日：2004-08-26
申请号：PCT/GB2004/000506
申请日：2004-02-09
申请人： VERNALIS (CAMBRIDGE) LIMITED , CANCER RESEARCH TECHNOLOGY LTD , THE INSTITUTE OF CANCER RESEARCH , DRYSDALE, Martin, James , DYMOCK, Brian, William , FINCH, Harry , WEBB, Paul , MCDONALD, Edward , JAMES, Karen, Elizabeth , CHEUNG, Kwai, Ming , MATHEWS, Thomas, Peter
发明人： DRYSDALE, Martin, James , DYMOCK, Brian, William , FINCH, Harry , WEBB, Paul , MCDONALD, Edward , JAMES, Karen, Elizabeth , CHEUNG, Kwai, Ming , MATHEWS, Thomas, Peter
IPC分类号： C07D261/08
CPC分类号： A61K31/541 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07D261/08 , C07D261/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D495/04
摘要： Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: (A), (B) wherein R 1 , is a group of formula (IA): -Ar 1 -(Alk 1 )p-(Z) r -(Alk 2 ) S -Q, wherein in any compatible combination Ar 1 is an optionally substituted aryl or heteroaryl radical, Alk 1 and Alk 2 are optionally substituted divalent C l -C 6 alkylene or C 2 -C 6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, -S-, -(C=O)-, -(C=S)-, -SO 2 -, -C(=O)O-, -C(=O)NR A -, -C(=S)NR A -, - SO 2 NR A -, -NR A C(=O)-, -NR A SO 2 - or -NR A - wherein R A is hydrogen or C l -C 6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R 2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk 1 )p-(Z) r -(Alk 2 ) s -Q wherein Q, Alk 1 , Alk 2 , Z, p, r and s are as defined above in relation to group (IA); and R 3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C 1 -C 6 alkyl, C 1 -C 6 alkenyl, or C 1 -C 6 alkynyl; or a carboxyl, carboxamide, or carboxyl ester group.
摘要翻译：式（A）或（B）的异恶唑是HSP90活性的抑制剂，可用于治疗例如癌症：（A），（B）其中R1是式（IA）的基团：-Ar 1 - （Alk 1）对 - （Z）r-（Alk 2）SQ，其中在任何相容的组合中，Ar 1是任选取代的芳基或杂芳基，Alk 1和Alk 2是任选取代的二价C 1 -C 6亚烷基或C 2 -C 6亚烯基，p，r和s独立地为0或1，Z为-O-，-S-， - （C = O） - ， - （C = S），-SO 2 - ， - C（= O）O-，-C（= O）NR A - ， - C（= S）NR A A - ， - SO 2 NR C（= O） - ， - NR A 2 - 或-NR A A - 其中R A A是氢或C 1 -C 6烷基，Q是氢或任选取代的碳环或杂环基; R2是（i）上述式（IA）的基团或（ii）甲酰胺基团; 或（iii）非芳族碳环或杂环，其中环碳任选被取代，和/或环氮任选地被式 - （Alk 1）对 - （Z）r - （Alk < 其中Q，Alk 1，Alk 2，Z，p，r和s如上文关于组（IA）所定义; 并且R 3是氢，任选取代的环烷基，环烯基，C 1 -C 6烷基，C 1 -C 6烯基或C 1 -C 6炔基; 或羧基，羧酰胺或羧基酯基团。

2. 发明申请

WO2010150014A1 5R- 5 -DEUTERATED GLITAZONES FOR RESPIRATORY DISEASE TREATMENT 审中-公开
标题翻译：用于呼吸道疾病治疗的5R-5-灭菌玻璃制品
公开(公告)号：WO2010150014A1
公开(公告)日：2010-12-29
申请号：PCT/GB2010/051044
申请日：2010-06-24
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , FINCH, Harry , SAJAD, Mohammed , FORREST, Andrew , VAN NIEL, Monique Bodil
发明人： FINCH, Harry , SAJAD, Mohammed , FORREST, Andrew , VAN NIEL, Monique Bodil
IPC分类号： A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/506 , A61K31/513 , A61K45/06 , A61P11/06 , A61P11/08 , A61P29/00 , C07D417/12
CPC分类号： A61K31/4439 , A61K9/0043 , A61K31/426 , A61K31/427 , A61K31/506 , A61K31/513 , A61K2300/00
摘要： A composition comprising a 5R-5-deuterated glitazone or a salt thereof, in which composition the 5R-5 deuterated glitazone component includes less than 5% by weight in total of 5R-5-protonated glitazone, 5S-5-protonated glitazone and 5S-5- deuterated glitazone. The glitazone may be rosiglitazone or pioglitazone. Compositions may be for pulmonary inhalation for treatment of Pulmonary inflammatory disease.
摘要翻译：包含5R-5-氘代格列酮或其盐的组合物，其中5R-5氘化格列酮酮组分的组合物包含总共5R-5质子化格列酮，5S-5质子化格列酮和5S -5-氘代格列酮。格列酮可以是罗格列酮或吡格列酮。组合物可用于肺部吸入治疗肺炎性疾病。

3. 发明申请

WO2010094956A1 TRIAZOLOPYRIDINE DERIVATIVES AS P38 MAP KINASE INHIBITORS 审中-公开
标题翻译：作为P38 MAP激酶抑制剂的三唑吡啶衍生物
公开(公告)号：WO2010094956A1
公开(公告)日：2010-08-26
申请号：PCT/GB2010/050257
申请日：2010-02-16
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED. , FINCH, Harry , MONTANA, John , VAN NIEL, Monique Bodil , WOO, Chi-Kit , KNIGHT, Jamie , WASZKOWYCZ, Bohdan
发明人： FINCH, Harry , MONTANA, John , VAN NIEL, Monique Bodil , WOO, Chi-Kit , KNIGHT, Jamie , WASZKOWYCZ, Bohdan
IPC分类号： C07D471/04 , A61P11/00 , A61P29/00 , A61K31/4162
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of, inter alia , diseases of the respiratory tract wherein; R 1 is C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and R 3 and R 4 are independently H or C 1 -C 6 alkyl, or R 3 and R 4 taken together with the nitrogen to which they are attached form a 6- membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is -O- or -S(O) P - wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C 3 -C 6 divale nt cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to R 2 NHC(=O)W-; W is a bond, -NH- or -C(R A )(R B ), wherein R A and R B are independently H, methyl, ethyl, amino, hydroxyl or halo; and R 2 is a radical as defined in the claims.
摘要翻译：式（I）化合物是p38MAP激酶的抑制剂，其可用作治疗特别是呼吸道疾病的抗炎剂，其中： R 1是C 1 -C 6烷基，C 3 -C 6环烷基，任选取代的苯基，任选被取代的5-或6-元单环杂芳基，或其中n是1或2的式（II）基团，R 3和R 4是独立地是H或C 1 -C 6烷基，或者R 3和R 4与它们所连接的氮一起形成任选含有另外选自N和O的杂原子的6-元杂环; Y是-O-或-S（O）P-，其中p是0,1或2; A是任选取代的二价亚芳基，或单环或双环亚杂芳基，或具有5或6个环原子的C 3 -C 6二烯基亚环烷基或其中环氮连接至R 2 NHC（= O）的哌啶子基， W-; W是键，-NH-或-C（RA）（RB），其中RA和RB独立地是H，甲基，乙基，氨基，羟基或卤素; 并且R 2是如权利要求中所定义的基团。

4. 发明申请

WO2010086638A1 DIMERIC PYRROLOPYRIMIDINEDIONE AND ITS USE IN THERAPY OF RESPIRATORY DISEASES 审中-公开
标题翻译：二甲基吡咯啉二酮及其在呼吸道疾病治疗中的应用
公开(公告)号：WO2010086638A1
公开(公告)日：2010-08-05
申请号：PCT/GB2010/050092
申请日：2010-01-22
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , EDWARDS, Christine , KULAGOWSKI, Janus , FINCH, Harry
发明人： EDWARDS, Christine , KULAGOWSKI, Janus , FINCH, Harry
IPC分类号： C07D519/00 , A61K31/519 , A61P11/00
CPC分类号： C07D519/00
摘要： The compound of formula (I) is an inhibitor of human neutrophil elastase, useful for inhalation treatment of pulmonary inflammation.
摘要翻译：式（I）化合物是人嗜中性粒细胞弹性蛋白酶抑制剂，可用于肺部炎症的吸入治疗。

5. 发明申请

WO2009013444A1 TETRAHYDROPYRROLOPYRIMIDINEDIONES AND THEIR USE AS HUMAN NEUTROPHIL ELASTASE INHIBITORS 审中-公开
标题翻译：四氢吡咯并嘧啶及其作为人类中性粒细胞抑制剂的用途
公开(公告)号：WO2009013444A1
公开(公告)日：2009-01-29
申请号：PCT/GB2007/002825
申请日：2007-07-25
申请人： ARGENTA DISCOVERY LIMITED , RAY, Nicholas, Charles , FINCH, Harry , EDWARDS, Christine , O'CONNOR, Elizabeth
发明人： RAY, Nicholas, Charles , FINCH, Harry , EDWARDS, Christine , O'CONNOR, Elizabeth
IPC分类号： C07D487/04 , A61K31/519 , A61P11/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) and multimers thereof are inhibitors of human neutrophil elastase activity, and of utility in the treatment of, e.g., COPD : wherein all the substituents are as defined in claim 1.
摘要翻译：式（I）化合物及其多聚体是人中性粒细胞弹性蛋白酶活性的抑制剂，并且在治疗例如COPD中有用：其中所有取代基如权利要求1所定义。

6. 发明申请

WO2008099186A1 HETEROCYCLIC DERIVATIVES AS M3 MUSCARINIC RECEPTORS 审中-公开
标题翻译：杂环衍生物作为M3肌肉接受体
公开(公告)号：WO2008099186A1
公开(公告)日：2008-08-21
申请号：PCT/GB2008/000519
申请日：2008-02-14
申请人： ARGENTA DISCOVERY LIMITED , AVITABILE, Barbara, Giuseppina , FINCH, Harry , KNIGHT, Jamie, David , NADIN, Alan, John , RAY, Nicholas, Charles
发明人： AVITABILE, Barbara, Giuseppina , FINCH, Harry , KNIGHT, Jamie, David , NADIN, Alan, John , RAY, Nicholas, Charles
IPC分类号： C07D471/08 , A61K31/439 , A61P11/00 , A61P9/00 , A61P1/00
CPC分类号： C07D471/08
摘要： This invention relates to M3 antagonists of formula (I) wherein R 2 , R 4 , R 5 , R 6 , W, V, A, D, X, t, u and v are as defined herein; pharmaceutical compositions containing them; methods for their preparation; and their use in the treatment of diseases where enhanced M3 receptor activation is implicated.
摘要翻译：本发明涉及式（I）的M3拮抗剂，其中R 2，R 4，R 5，R 5，R 5， R 6，W，V，A，D，X，t，u和v如本文所定义; 含有它们的药物组合物其制备方法; 以及它们在治疗与M3受体激活有关的疾病时的用途。

7. 发明申请

WO2008096128A1 OXAZOLE AND THIAZOLE DERIVATIVES AND THEIR USES 2 审中-公开
标题翻译：奥扎唑和噻唑衍生物及其用途2
公开(公告)号：WO2008096128A1
公开(公告)日：2008-08-14
申请号：PCT/GB2008/000406
申请日：2008-02-06
申请人： ARGENTA DISCOVERY LTD , FINCH, Harry , RAY, Nicholas, Charles , BULL, Richard, James , BRAVO, Jose, Antonio , AVITABILE, Barbara, Giuseppina
发明人： FINCH, Harry , RAY, Nicholas, Charles , BULL, Richard, James , BRAVO, Jose, Antonio , AVITABILE, Barbara, Giuseppina
IPC分类号： C07D263/32 , A61K31/421 , A61P11/06
CPC分类号： C07D263/32
摘要： Compounds of formula (I): wherein A, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 8 are as defined in the Specification are useful in the treatment of diseases where enhanced M3 receptor activation is implicated, such as respiratory tract diseases.
摘要翻译：式（I）化合物：其中A，X，R 1，R 2，R 3，R 4， >，R 5，R 6和R 8如本说明书中所定义，可用于治疗增强M3受体活化的疾病牵连，如呼吸道疾病。

8. 发明申请

WO2008096126A1 COMBINATION OF A MUSCARINIC RECEPTOR ANTAGONIST AND A BETA-2-ADRENOCEPTOR AGONIST 审中-公开
标题翻译：麦考受体拮抗剂与β-2-ADRENOCEPTOR AGONIST的组合
公开(公告)号：WO2008096126A1
公开(公告)日：2008-08-14
申请号：PCT/GB2008/000404
申请日：2008-02-06
申请人： ARGENTA DISCOVERY LTD , ASTRAZENECA AB , FINCH, Harry , WILEY, Katherine , DIXON, John
发明人： FINCH, Harry , WILEY, Katherine , DIXON, John
IPC分类号： A61K31/421 , A61K31/428 , A61K31/167 , A61P11/06
CPC分类号： A61K31/167 , A61K31/421 , A61K31/428 , A61K2300/00
摘要： The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a selected muscarinic receptor antagonist selected, and a second active ingredient which is a β 2 -adrenoceptor agonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.
摘要翻译：本发明提供药物产品，试剂盒或组合物，其包含选择的选择的毒蕈碱受体拮抗剂的第一活性成分和作为治疗用的β2 - 肾上腺素能受体激动剂的第二活性成分呼吸系统疾病如慢性阻塞性肺疾病和哮喘。

9. 发明申请

WO2007068929A1 CYCLIC AMINE DERIVATIVES AND THEIR USES 审中-公开
标题翻译：循环胺衍生物及其用途
公开(公告)号：WO2007068929A1
公开(公告)日：2007-06-21
申请号：PCT/GB2006/004675
申请日：2006-12-14
申请人： ARGENTA DISCOVERY LTD. , FINCH, Harry , RAY, Nicholas, Charles , BODIL VAN NIEL, Monique , SMITH, Phillip
发明人： FINCH, Harry , RAY, Nicholas, Charles , BODIL VAN NIEL, Monique , SMITH, Phillip
IPC分类号： C07C271/38 , C07C217/52 , C07C219/24 , C07D311/86 , C07D333/24 , A61K31/27 , A61K31/381 , A61K31/14 , A61K31/216 , A61K31/352 , A61P11/00
CPC分类号： C07C271/38 , C07C217/52 , C07C219/24 , C07C2602/42 , C07D311/86 , C07D333/24
摘要： Compounds of formula (I) have muscarinic M3 receptor modulating activity; formula (I) wherein R 1 is C 1 -C 6 -alkyl or a hydrogen atom; and R 2 is a hydrogen atom or a group -R 5 , or a group, -Z-Y-R 5 , or a group -Z-NR 9 R 10 , or a group -Z-N(R 9 )C(O)R 11 ; and R 3 is a lone pair, or C 1 -C 6 -alkyl; R 4 is selected from one of the groups of formula (a), (b), (c) or (d); formulae (a), (b), (c), (d), Z is a C 1 -C 16 -alkylene, C 2 -C 16 -alkenylene or C 2 -C 16 -alkynylene group; Y is a bond or oxygen atom; R 5 is an C 1 -C 6 -alkyl, aryl, arylalkyl; aryl-fused-cycloalkyl, aryl-fused- heterocycloalkyl, heteroaryl, aryl(C 1 -C 8 -alkyl)-, heteroaryl(C 1 -C 8 -alkyl)-, cycloalkyl or heterocycloalkyl group; R 6 is C 1 -C 6 -alkyl or a hydrogen atom; R 7a and R 7b are a C 1 -C 6 - alkyl group or halogen; n and m are independently 0, 1 , 2 or 3; R 8a and R 8b are independently selected from the group consisting of aryl, aryl-fused-heterocycloalkyl, heteroaryl, C 1 -C 6 -alkyl, cycloalkyl and hydrogen; R 8c is -OH, C 1 -C 6 -alkyl, hydroxy-C 1 -C 6 -alkyl, or a hydrogen atom; R 8d is C 1 -C 6 -alkyl or a hydrogen atom; R 9 and R 10 are independently a hydrogen atom, C 1 -C 6 -alkyl, aryl, aryl-fused-heterocycloalkyl, aryl- fused-cycloalkyl, heteroaryl, aryl(C 1 -C 6 -alkyl)-, or heteroaryl(C 1 -C 6 -alkyl)- group; or R 9 and R 10 together with the nitrogen atom to which they are attached form a heterocyclic ring of 4-8 atoms, optionally containing a further nitrogen or oxygen atom; R 11 is C 1 -C 6 -alkyl or a hydrogen atom; Ar 1 is aryl, heteroaryl or cycloalkyl; Ar 2 are independently aryl, heteroaryl or cycloalkyl; and Q is an oxygen atom, -CH 2 -, -CH 2 CH 2 - or a bond.
摘要翻译：式（I）化合物具有毒蕈碱M3受体调节活性; 式（I）其中R 1是C 1 -C 6 - 烷基或氢原子; 和R 2是氢原子或基团-R 5或基团-ZYR 5或基团-Z-NR 或者是基团-ZN（R 9）C（O）R 11; 且R 3是一对或C 1 -C 6 - 烷基; R 4选自式（a），（b），（c）或（d）中的一个：式（a），（b），（c），（d），Z是C 1 -C 16 - 亚烷基，C 2 -C 16 - 亚烯基或C 2 -C 16 - 亚炔基; Y是键或氧原子; R 5是C 1 -C 6 - 烷基，芳基，芳基烷基; 芳基 - 稠合环烷基，芳基 - 稠合 - 杂环烷基，杂芳基，芳基（C 1 -C 8 - 烷基） - ，杂芳基（C 1 -C 12 - -C≡8烷 - 烷基） - ，环烷基或杂环烷基; R 6是C 1 -C 6 - 烷基或氢原子; R 7a和R 7b是C 1 -C 6 - 烷基或卤素; n和m独立地为0,1,2或3; R 8a和R 8b独立地选自芳基，芳基 - 稠合 - 杂环烷基，杂芳基，C 1 -C 3 烷基，环烷基和氢; R 8c是-OH，C 1 -C 6 - 烷基，羟基-C 1 -C 3 > 6个 - 烷基或氢原子; R 8是C 1 -C 6 - 烷基或氢原子; R 9和R 10独立地是氢原子，C 1 -C 6 - 烷基，芳基，芳基 - 杂芳基（C 1 -C 6 - 烷基） - 或杂芳基（C 1 -C 6 - 烷基） - 杂芳基（C 1 -C 6 - -C 6 -C 6 - 烷基） - 基; 或R 9和R 10与它们所连接的氮原子一起形成4-8个原子的杂环，任选地含有另外的氮或氧原子; R 11是C 1 -C 6 - 烷基或氢原子; Ar 1是芳基，杂芳基或环烷基; Ar 2独立地是芳基，杂芳基或环烷基; 和Q是氧原子，-CH 2 - ， - CH 2 CH 2 - 或键。

10. 发明申请

WO2011098801A1 INFLAMMATORY DISEASE TREATMENT 审中-公开
标题翻译：炎症性疾病治疗
公开(公告)号：WO2011098801A1
公开(公告)日：2011-08-18
申请号：PCT/GB2011/050226
申请日：2011-02-09
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , FINCH, Harry , FOX, Craig
发明人： FINCH, Harry , FOX, Craig
IPC分类号： A61K31/192 , A61P29/00
CPC分类号： A61K31/192 , A61K9/0073
摘要： Compounds of formula (I) are useful in the treatment of inflammatory disease wherein at least 95% by weight of the said compound of formula (I) is in the stereoconfiguration shown in formula (IA) and less than 5% by weight is in the stereoconfiguration shown in formula (IB) in which formulae (I), (IA) and (IB): R is CH 3 - or hydrogen; X 1 is -OR 1 , -S(O) n R 2 or -NR 3 R 4 and X 2 is-OH; or X 1 and X 2 taken together represent a radical *-OC(O)NH-** or *-C(O)N(H)O-** wherein the bond marked * is attached to the carbon to which W and R are attached, and the bond marked ** is attached to the carbonyl carbon; R 1 and R 2 are independently C 1-6 alkyl optionally substituted with one or more halogen atoms; C 1-6 alkoxyalkyl; or aryl R 3 and R 4 are independently hydrogen; C 1-6 alkyl; aryl; a group -C(R a )=C(R b )-C(=O)-Ar a wherein R a and R b are independently hydrogen or C 1-6 alkyl and Ar a is aryl; or a group -Ar b -C(=O)-Ar c wherein Ar b and Ar c are aryl; or -C(=O)O-R c wherein R c is an aryl or C 1-6 alkyl; or R 3 and R 4 taken together with the nitrogen to which they are attached form a saturated ring of 3 to 7 ring members or an unsaturated ring of 5 to 7 ring members; n is 0,1 or 2; W is a group which when linked to the -C(R)(X 1 )C(=O)X 2 results in a compound (I) having PPARγ agonist activity.
摘要翻译：式（I）化合物可用于治疗炎性疾病，其中至少95重量％的所述式（I）化合物为式（IA）所示的立体构型，小于5重量％为其中式（I），（IA）和（IB）：R是CH 3或氢的式（IB）所示的立体构型; X1为-OR1，-S（O）nR2或-NR3R4，X2为-OH; 或X 1和X 2一起表示基团* -OC（O）NH - **或* -C（O）N（H）O - **，其中标记*的键连接到W和R为并且标记为**的键连接到羰基碳上; R1和R2独立地为任选被一个或多个卤素原子取代的C 1-6烷基; C 1-6烷氧基烷基; 或芳基R 3和R 4独立地为氢; C 1-6烷基芳基; 基团-C（Ra）= C（Rb）-C（= O）-Ara，其中R a和R b独立地是氢或C 1-6烷基，Ara是芳基; 或Arb-C（= O）-Arc基团，其中Arb和Arc为芳基; 或-C（= O）O-Rc，其中R c是芳基或C 1-6烷基; 或者R 3和R 4与它们所连接的氮一起形成3至7个环成员的饱和环或5至7个环成员的不饱和环; n为0,1或2; W是与-C（R）（X1）C（= O）X2连接的基团，得到具有PPAR 3的化合物（I）激动剂活性。

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