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1. 发明申请

WO2005077926A3 BENZOFURAN AND BENZOTHIOPHENE DERIVATIVES USEFUL FOR THE TREATMENT OF CARDIOVASCULAR DISEASE 审中-公开
公开(公告)号：WO2005077926A3
公开(公告)日：2005-08-25
申请号：PCT/EP2005/001540
申请日：2005-02-10
申请人： SMITHKLINE BEECHAM CORPORATION , HARLING, John, David , LAMBETH, Paul, Francis , LIVERMORE, David, George
发明人： HARLING, John, David , LAMBETH, Paul, Francis , LIVERMORE, David, George
IPC分类号： C07D333/54
摘要： A compound of formula (I) and pharmaceutically acceptable salts and solvates and hydrolysable esters thereof, where X, X 1 , X 2 , X 3 , X 4 and R, R 2 , R 3 , R 4 are defined as in claim 1. These compounds are activators of the hPPAR receptors and are useful for the treatment of cardiovascular disease.

2. 发明申请

WO2005077926A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2005077926A2
公开(公告)日：2005-08-25
申请号：PCT/EP2005001540
申请日：2005-02-10
申请人： SMITHKLINE BEECHAM CORP , HARLING JOHN DAVID , LAMBETH PAUL FRANCIS , LIVERMORE DAVID GEORGE
发明人： HARLING JOHN DAVID , LAMBETH PAUL FRANCIS , LIVERMORE DAVID GEORGE
IPC分类号： C07D307/79 , C07D307/80 , C07D333/54 , C07D333/56 , C07D417/12 , C07D307/00
CPC分类号： C07D307/79 , C07D307/80 , C07D333/54 , C07D333/56 , C07D417/12
摘要： A compound of formula (I) and pharmaceutically acceptable salts and solvates and hydrolysable esters thereof.
摘要翻译：式（I）的化合物及其药学上可接受的盐和溶剂合物及其可水解的酯。

3. 发明申请

WO2004000762A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2004000762A2
公开(公告)日：2003-12-31
申请号：PCT/EP2003/006416
申请日：2003-06-18
申请人： SMITHKLINE BEECHAM CORPORATION , BESWICK, Paul, John , HARLING, John, David , KLEANTHOUS, Savvas , PATEL, Vipulkumar, Kantibhai , SIMPSON, Juliet
发明人： BESWICK, Paul, John , HARLING, John, David , KLEANTHOUS, Savvas , PATEL, Vipulkumar, Kantibhai , SIMPSON, Juliet
IPC分类号： C07C
CPC分类号： C07D213/74 , C07C217/58 , C07C217/80 , C07C233/18 , C07C255/58 , C07C311/08 , C07C311/29 , C07C323/25 , C07C2601/02 , C07D239/42 , C07D241/20
摘要： A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, .Wherein:R1 and R2 are independently hydrogen or C1-3 alkyl;X represents a bond, CH2 or O;R3 and R4 are independently hydrogen, C1-6 alkyl, OCH3, CF3, allyl or halogen;X1 is CH2, SO2, or CO;R5 is -C1-6 alkyl (optionally substituted by C1-6alkoxy or C1-6alkylthio), -C2-6 alkenyl, -C0-6 alkyl phenyl (wherein the phenyl is optionally substituted by one or more CF3, halogen, C1-3 alkyl, C1-3 alkoxy), -COC1-6 alkyl, SO2C1-6 alkyl ;R6 is phenyl or a 6 membered heteroaryl group containing 1,2 or 3 N atoms wherein the phenyl or heteroaryl group is optionally substituted with 1, 2 or 3 moieties selected from the group consisting of C1-6 alkyl, halogen, -OC1-6 alkyl, -SO2C1-3 alkyl, phenyl (optionally substituted by one or more groups selected from halogen, CF3, C1-3 alkyl, OC1-3 alkyl, acetyl, CN).
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或可水解的酯。其中R 1和R 2独立地是氢或C 1-3烷基; X代表键，CH 2或O; R 3和R 4独立地是氢，C 1-6烷基，OCH 3，CF 3，烯丙基或卤素; X 1是CH 2，SO 2或CO; R 5是-C 1-6烷基（任选被C 1-6烷氧基或C 1-6烷硫基取代），-C 2-6链烯基， C 0-6烷基苯基（其中苯基任选被一个或多个CF 3，卤素，C 1-3烷基，C 1-3烷氧基取代），-COC 1-6烷基，SO 2 C 1-6烷基; R 6是苯基或6元杂芳基含有1,2或3个N原子的基团，其中苯基或杂芳基任选被1,2或3个选自C 1-6烷基，卤素，-OC 1-6烷基，-SO 2 C 1-3烷基，苯基（任选被一个或多个选自卤素，CF 3，C 1-3烷基，OC 1-3烷基，乙酰基，CN的基团取代）。

4. 发明申请

WO2011110575A1 DERIVATIVES OF 2-[2-(BENZO- OR PYRIDO-) THIAZOLYLAMINO]-6-AMINOPYRIDINE, USEFUL IN THE TREATMENT OF RESPIRATORIC, ALLERGIC OR INFLAMMATORY DISEASES 审中-公开
标题翻译： 2- [2-（苯并或吡啶-2-基）噻唑啉氨基] -6-氨基吡啶的衍生物，用于治疗呼吸道感染，过敏或炎症性疾病
公开(公告)号：WO2011110575A1
公开(公告)日：2011-09-15
申请号：PCT/EP2011/053499
申请日：2011-03-09
申请人： GLAXO GROUP LIMITED , ALDER, Catherine Mary , BALDWIN, Ian Robert , BARTON, Nicholas Paul , CAMPBELL, Amanda Jennifer , CHAMPIGNY, Aurelie Cecile , HARLING, John David , MAXWELL, Aoife Caitriona , SIMPSON, Juliet Kay , SMITH, Ian Edward David , TAME, Christopher John , WILSON, Caroline , WOOLVEN, James Michael
发明人： ALDER, Catherine Mary , BALDWIN, Ian Robert , BARTON, Nicholas Paul , CAMPBELL, Amanda Jennifer , CHAMPIGNY, Aurelie Cecile , HARLING, John David , MAXWELL, Aoife Caitriona , SIMPSON, Juliet Kay , SMITH, Ian Edward David , TAME, Christopher John , WILSON, Caroline , WOOLVEN, James Michael
IPC分类号： C07D417/04 , C07D417/14 , C07D513/04 , A61K31/427 , A61K31/428 , A61P11/00 , A61P19/00 , A61P37/00
CPC分类号： C07D417/04 , C07D417/14 , C07D513/04
摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular Itk activity.
摘要翻译：本发明涉及某些新型化合物。具体地，本发明涉及式（I）的化合物及其盐。本发明的化合物是激酶活性的抑制剂，特别是Itk活性。

5. 发明申请

WO2003042207A1 THIAZOLYL SUBSTITUTED TRIAZOLES AS ALK5 INHIBITORS 审中-公开
标题翻译：作为ALK5抑制剂的THIAZOLYL取代三唑类
公开(公告)号：WO2003042207A1
公开(公告)日：2003-05-22
申请号：PCT/EP2002/012892
申请日：2002-11-14
申请人： SMITHKLINE BEECHAM CORPORATION , GASTER, Laramie, Mary , HARLING, John, David , HEER, Jag, Paul , HEIGHTMAN, Thomas, Daniel , PAYNE, Andrew, Hele
发明人： HEIGHTMAN, Thomas, Daniel , PAYNE, Andrew, Hele
IPC分类号： C07D417/04
CPC分类号： C07D417/04 , C07D417/14
摘要： Thiazolyl substituted triazoles of formula (I) wherein R 1 is naphthyl or phenyl optionally substituted with one or more substituents selected from halo, -O-C 1-6 -alkyl, -S-C 1-6 alkyl, C 1-6 alkyl, C 1-6 haloalkyl, -O-(CH 2 ) n -Ph, -S-(CH 2 ) n -Ph, cyano, phenyl, and CO 2 R, wherein R is hydrogen or C 1-6 alkyl, and n is 0, 1, 2 or 3; or R 1 is phenyl fused with an aromatic or non-aromatic cyclic ring of 5-7 members wherein said cyclic ring optionally contains up to three heteroatoms, independently selected from N, O and S, and N may be further optionally substituted by C 1-6 alkyl, and wherein the cyclic ring may be optionally substituted by =O; or R 1 is pyridyl fused with an aromatic or non-aromatic cyclic ring of 5-7 members wherein said cyclic ring optionally contains up to three heteroatoms, independently selected from N, O and S, and N may be further optionally substituted by C 1-6 alkyl, and wherein the cyclic ring may be optionally substituted by =O; R 2 is H, C 1-6 alkyl, C 1-6 alkoxy, phenyl, NH(CH 2 ) n -Ph, NH-C 1-6 alkyl, halo, CN, NO 2 , CONHR and SO 2 NHR; two of X 1 , X 2 and X 3 are N and the other is NR 3 wherein R 3 is hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, -(CH 2 ) p -CN, -(CH 2 ) p -CO 2 H, -(CH 2 ) p -CONHR 4 R 5 , -(CH 2 ) p COR 4 , -(CH 2 ) q (OR 5 ) 2 , -(CH 2 ) p OR 4 , -(CH 2 ) q -CH=CH-CN, -(CH 2 ) q -CH=CH-CO 2 H, -(CH 2 ) P -CH=CH-CONHR 4 R 5 , -(CH 2 ) P NHCOR 7 or -(CH 2 ) P NR 8 R 9 ; R 4 and R 5 are independently hydrogen or C 1-6 alkyl; R 6 is C 1-6 alkyl; R 7 is C 1-7 alkyl, or optionally substituted aryl, heteroaryl, arylC 1-6 alkyl or heteroaryl 1-6 alkyl; R 8 and R 9 are independently selected from hydrogen, C 1-6 alkyl, aryl and arylC 1-6 alkyl; p is 0-4; and q is 1-4and salts and solvates thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.
摘要翻译：式（I）的噻唑基取代的三唑，其中R 1是萘基或任选被一个或多个选自卤素，-O-C 1-6烷基的取代基取代的苯基， -S-C 1-6烷基，C 1-6烷基，C 1-16卤代烷基，-O-（CH-）（S 2）2，-S-（CH 2）s - （CH 2）n - ， - C 6 H 6，氰基，苯基和CO > R 2，其中R是氢或C 1-6烷基，n是0,1,2或3; 或者R 15是与5-7个成员的芳族或非芳族环的稠合的苯基，其中所述环任选地含有最多三个独立地选自N，O和S的杂原子，N可以进一步任选地被C 1-6烷基取代，并且其中环状环可以任选地被= O取代; 或R 15是与5-7个成员的芳族或非芳族环的稠合的吡啶基，其中所述环任选地含有最多三个独立地选自N，O和S的杂原子，N可以进一步任选地被C 1-6烷基取代，并且其中环状环可以任选地被= O取代; R 2是H，C 1-6烷基，C 1-6烷氧基，苯基，NH（CH 2）2 / s >） -Ph，NH-C 1-6烷基，卤素，CN，NO，sb> 2，CONHR和SO 2 < / SB> NHR; X 1 ，X 2 和X 3 中的两个是N，另一个是NR s 3，其中R s > 3 是氢，C 1-6烷基，C 3-7环烷基， - （CH 2 b）（CH 2 S）2， - （CH 2 s）2， - （CH 2 S 2） >） p -CONHR 4 R 5 ， - （CH 2 ） p （ 2 ） - （CH ） p OR 4 ， - （CH 2 ） q -CH = CH-CN， - （CH 2）s - > = CH = CH-CO 2 s H 2 - （CH 2 b）
sb> P NHCOR 7 或 - （CH 2 ） 9 ; R 4和R 15独立地是氢或C 1-6烷基; R 6是C 1-6烷基; R 7是C 1-6烷基或任选取代的芳基，杂芳基，芳基C 1-6烷基或杂芳基-S 1-6 烷基; R 8和R 9独立地选自氢，C 1-6烷基，芳基和芳基，C 1-6烷基， >烷基; p为0-4; 和q是1-4，并且其盐和溶剂化物被公开，以及它们的制备方法

6. 发明申请

WO2012035055A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2012035055A1
公开(公告)日：2012-03-22
申请号：PCT/EP2011/065921
申请日：2011-09-14
申请人： GLAXO GROUP LIMITED , BARTON, Nicholas Paul , CAMPOS, Sebastien Andre , CARR, Robin Arthur , HARLING, John David , SMITH, Ian Edward David
发明人： BARTON, Nicholas Paul , CAMPOS, Sebastien Andre , CARR, Robin Arthur , HARLING, John David , SMITH, Ian Edward David
IPC分类号： C07D417/12 , C07D417/14 , C07D513/04 , A61K31/506 , A61K31/5377 , A61K31/445 , A61K31/496
CPC分类号： C07D513/04 , A61K31/445 , A61K31/496 , A61K31/506 , A61K31/5377 , C07D417/12 , C07D417/14
摘要： The invention is directed to certain novel compounds. Specifically, the invention directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular Itk activity.
摘要翻译：本发明涉及某些新型化合物。具体地，本发明涉及式（I）化合物及其盐。本发明的化合物是激酶活性的抑制剂，特别是Itk活性。

7. 发明申请

WO2007059952A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2007059952A2
公开(公告)日：2007-05-31
申请号：PCT/EP2006/011218
申请日：2006-11-22
申请人： GLAXO GROUP LIMITED , CAMUS, Laure , CHUDASAMA, Reshma , DAY, Caroline, Jane , DESHMUKH, Deepali , GLEASON, John, Gerald , HARLING, John, David , LEE, Chao-Pin , SAKLATVALA, Paula , SENGER, Stefan , VALLANCE, Sarah , WATSON, John , WATSON, Nigel, Stephen , YOUNG, Robert, John , YUAN, Barbara
发明人： CAMUS, Laure , CHUDASAMA, Reshma , DAY, Caroline, Jane , DESHMUKH, Deepali , GLEASON, John, Gerald , HARLING, John, David , LEE, Chao-Pin , SAKLATVALA, Paula , SENGER, Stefan , VALLANCE, Sarah , WATSON, John , WATSON, Nigel, Stephen , YOUNG, Robert, John , YUAN, Barbara
CPC分类号： C07D409/14 , C07D403/04 , C07D403/14
摘要： The invention relates to chemical entities of formula (I): and/or pharmaceutically acceptable derivative(s) thereof. The invention also relates to processes for the preparation of compounds of formula (I), pharmaceutical compositions containing compounds of formula (I) and to the use of compounds of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
摘要翻译：本发明涉及式（I）的化学实体：和/或其药学上可接受的衍生物。本发明还涉及制备式（I）化合物的方法，包含式（I）化合物的药物组合物和式（I）化合物在医药中的用途，特别是在改善临床病症方面指示因子Xa抑制剂。

8. 发明申请

WO1997048683A1 SUBSTITUTED BENZAMIDE DERIVATIVES AND THEIR USE AS ANTICONVULSANTS 审中-公开
标题翻译：替代苯扎林衍生物及其作为抗生素的用途
公开(公告)号：WO1997048683A1
公开(公告)日：1997-12-24
申请号：PCT/EP1997003131
申请日：1997-06-13
申请人： SMITHKLINE BEECHAM PLC , HARLING, John, David , ORLEK, Barry, Sidney , THOMPSON, Mervyn
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D217/04
CPC分类号： C07D223/16 , A61K31/472 , C07D209/44 , C07D217/04 , C07D401/12
摘要： The invention relates to substituted benzamido-heterocyclic compounds of general formula (I) having an alkoxy substituent at the C2 position of the benzamido group and various substituents at positions C4 and C5, being optionally substituted on the N atom of the heterocyclic system, and where the unsaturated ring of the heterocyclic system is a 5, 6, 7 or 8-membered ring. Also to the use of these compounds as anticonvulsants in certain medical conditions, and to processes for making them.
摘要翻译：本发明涉及在苯甲酰氨基的C2位具有烷氧基取代基的通式（I）的取代苯甲酰氨基 - 杂环化合物和位置C4和C5上的各种取代基，任选在杂环体系的N原子上取代，并且其中杂环体系的不饱和环是5,6,7或8元环。还涉及在某些医疗条件下使用这些化合物作为抗惊厥药，以及制备它们的方法。

9. 发明申请

WO1997010210A1 TRICYCLIC PYRROLIDINE DERIVATIVES AS CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译：三氯吡啶衍生物作为钙通道拮抗剂
公开(公告)号：WO1997010210A1
公开(公告)日：1997-03-20
申请号：PCT/EP1996003990
申请日：1996-09-09
申请人： SMITHKLINE BEECHAM PLC , HARLING, John, David , ORLEK, Barry, Sidney
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D209/70
CPC分类号： C07D209/70
摘要： Compounds of formula (I) wherein A represents (CH2)n in which one -CH2- moiety may be optionally replaced by O, -C(CH3)2 or -OC(CH3)2; and n is 1, 2 or 3; R represents hydrogen, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-4alkyl, benzyl or 4-methoxybenzyl; R represents a substituent selected from one or more of: a hydrogen or halogen atom, or a hydroxy, C1-4alkyl, C1-4alkoxy, amino, mono-or di-C1-4alkylamino, trifluoromethyl, trifluoromethoxy, cyano, nitro, formyl, C1-4alkynoyl, or C alkoxycarbonyl group or a group R R NCO- wherein R and R each independently represents a hydrogen atom or a C1-4alkyl group or R R N forms a 5-7 membered heterocyclic ring; m represents 1, 2, 3, or 4; Ar represents phenyl optionally substituted by 1 to 3 substituents selected from one or more of: halo, C1-4alkyl, C1-4alkoxy, C1-2alkylenedioxy, trifluoromethyl, trifluoromethoxy, CN, NO2, amino, mono- or di-alkylamino, optionally substitued benzoyl or a group Ph(Alk )rY(Alk )s- wherein Ph is optionally substituted phenyl, Y is oxygen or a bond, Alk and Alk each independenlty represents C1-4 alkyl which may be straight or branched and r and s are independently zero or 1, provided that the length of the chain (Alk )rY(Alk )s does not exceed 5 atoms; or Ar represents an optionally substituted unsaturated monocyclic heteroaryl ring system containing 5 or 6 ring members, or an optionally substituted, unsaturated or partially saturated bicyclic aryl or heteroaryl ring system containing 8-10 ring members; and salt thereof are neuronal calcium channel antagonists useful in the treatment of ischaemic conditions e.g. stroke.
摘要翻译：其中A表示（CH 2）n的式（I）化合物，其中一个-CH 2 - 部分可以任选被O，-C（CH 3）2或-OC（CH 3）2取代; n为1,2或3; R 1表示氢，C 1-6烷基，C 3-6环烷基，C 3-6环烷基C 1-4烷基，苄基或4-甲氧基苄基; R 2表示选自以下的一个或多个的取代基：氢或卤素原子，或羟基，C 1-4烷基，C 1-4烷氧基，氨基，单 - 或二-C 1-4烷基氨基，三氟甲基，三氟甲氧基，氰基，硝基，甲酰基，C 1-4炔酰基或C 1-4烷氧基羰基或R 3 R 4 NCO-基团，其中R 3和R 4各自独立地表示氢原子或C 1-4烷基基团或R 3 R 4形成5-7元杂环; m表示1,2,3或4; Ar表示任选被1至3个选自以下的取代基取代的苯基：卤素，C 1-4烷基，C 1-4烷氧基，C 1-2亚烷基二氧基，三氟甲基，三氟甲氧基，CN，NO 2，氨基，单 - 或二 - 烷基氨基，任选取代苯甲酰基或基团Ph（Alk 1）rY（Alk 2）s - ，其中Ph是任选取代的苯基，Y是氧或键，Alk 1和Alk 2各自独立地表示C 1-4烷基其可以是直链或支链，并且r和s独立地为0或1，条件是链（Alk 1）rY（Alk 2）s的长度不超过5个原子; 或Ar表示含有5或6个环成员或含有8-10个环成员的任选取代的不饱和或部分饱和的双环芳基或杂芳基环系的任选取代的不饱和单环杂芳基环系统; 其盐是可用于治疗缺血性病症的神经元钙通道拮抗剂，例如，行程。

10. 发明申请

WO1995026327A1 SUBSTITUTED CYCLOALKYLAMINE DERIVATIVES AND THEIR USE AS CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译：取代的环丙基胺衍生物及其作为钙通道拮抗剂的用途
公开(公告)号：WO1995026327A1
公开(公告)日：1995-10-05
申请号：PCT/EP1995000964
申请日：1995-03-14
申请人： SMITHKLINE BEECHAM PLC , BROWN, Thomas, Henry , HARLING, John, David , ORLEK, Barry, Sidney
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07C217/52
CPC分类号： C07C225/20 , C07C217/52 , C07C323/26 , C07C2601/08
摘要： The use of a compound of formula (I), wherein X represents O, S, C=O or a bond; p and q independently represent 0-4; R and R each independently represent hydrogen, C1-6alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-4alkyl; n is 1, 2, 3 or 4; and Ar represents phenyl optionally substituted by 1 to 3 substituents selected from: halo, C1-4alkyl, C1-4alkoxy, C1-2alkylenedioxy, trifluoromethyl, trifluoromethoxy, CN, NO2, amino, mono- or di- alkylamino and Ph(Alk )rY(Alk )s- where Ph is optionally substituted phenyl, Y is a bond, oxygen or a carbonyl group, Alk and Alk independently represent C1-4alkyl which may be straight or branched and r and s are independently 0 or 1, provided that the length of (Alk )rY(Alk )s does not exceed 5 atoms, and pharmaceutically acceptable salts thereof; in the manufacture of a medicament for the treatment of a disorder wherein a clacium channel antagonist is indicated, e.g. ischaemic stroke. Certain novel compounds within formula (I) are also claimed.
摘要翻译：使用式（I）化合物，其中X表示O，S，C = O或键; p和q独立地表示0-4; R 1和R 2各自独立地表示氢，C 1-6烷基，C 3-6环烷基或C 3-6环烷基C 1-4烷基; n为1,2,3或4; 并且Ar表示任选被1至3个选自以下的取代基取代的苯基：卤素，C 1-4烷基，C 1-4烷氧基，C 1-2亚烷基二氧基，三氟甲基，三氟甲氧基，CN，NO 2，氨基，单 - 或二 - 烷基氨基，Ph（Alk < >）rY（Alk 2）s - 其中Ph是任选取代的苯基，Y是键，氧或羰基，Alk 1和Alk 2独立地表示可以是直链或支链的C 1-4烷基， r和s独立地为0或1，条件是（Alk 1）rY（Alk 2）s的长度不超过5个原子，及其药学上可接受的盐; 在制备用于治疗其中指示藻酸盐通道拮抗剂的病症的药物中，例如，缺血性中风。还要求公式（I）中的某些新化合物。

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