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1. 发明申请

WO2003022833A1 PYRIDYLFURANS AND PYRROLES AS RAF KINASE INHIBITORS 审中-公开
标题翻译：吡蚜酮和吡咯作为RAF激酶抑制剂
公开(公告)号：WO2003022833A1
公开(公告)日：2003-03-20
申请号：PCT/EP2002/009945
申请日：2002-09-05
申请人： SMITHKLINE BEECHAM PLC , DEAN, David, Kenneth , NAYLOR, Antoinette , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
发明人： DEAN, David, Kenneth , NAYLOR, Antoinette , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , A61K31/44 , A61K31/505 , C07D405/04 , C07D405/14
摘要： Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.
摘要翻译：化合物及其作为药物的用途，特别是作为用于治疗神经外伤性疾病，癌症，慢性神经变性，疼痛，偏头痛和心脏肥大的Raf激酶抑制剂的用途。

2. 发明申请

WO2003022840A1 PYRIDINE DERIVATIVES AS RAF KINASE INHIBITORS 审中-公开
标题翻译：吡啶衍生物作为RAF激酶抑制剂
公开(公告)号：WO2003022840A1
公开(公告)日：2003-03-20
申请号：PCT/EP2002/009946
申请日：2002-09-05
申请人： SMITHKLINE BEECHAM PLC , BAMFORD, Mark, James , DEAN, David, Kenneth , NAYLOR, Antoinette , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
发明人： BAMFORD, Mark, James , DEAN, David, Kenneth , NAYLOR, Antoinette , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
IPC分类号： C07D405/14
CPC分类号： C07D405/04 , C07D405/14
摘要： Compounds (I) and their use as pharmaceuticals particularly as Raf Kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.
摘要翻译：化合物（I）及其作为药物的用途，特别是用作治疗神经创伤性疾病，癌症，慢性神经变性，疼痛，偏头痛和心脏肥大的Raf激酶抑制剂。

3. 发明申请

WO2003022836A1 NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND THEIR USE AS RAF INHIBITORS 审中-公开
标题翻译：含氮杂环化合物及其作为RAF抑制剂的用途
公开(公告)号：WO2003022836A1
公开(公告)日：2003-03-20
申请号：PCT/EP2002/009942
申请日：2002-09-05
申请人： SMITHKLINE BEECHAM PLC , BAMFORD, Mark, James , DEAN, David, Kenneth , NAYLOR, Antoinette , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
发明人： DEAN, David, Kenneth , NAYLOR, Antoinette , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
IPC分类号： C07D401/14
CPC分类号： C07D451/04 , C07D405/04 , C07D405/14 , C07D409/04
摘要： Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.
摘要翻译：化合物及其作为药物的用途，特别是用作治疗神经创伤性疾病，癌症，慢性神经变性，疼痛，偏头痛和心脏肥大的Raf激酶抑制剂。

4. 发明申请

WO2003022838A1 PYRIDINE SUBSTITUTED FURAN DERIVATIVES AS RAF KINASE INHIBITORS 审中-公开
标题翻译：吡咯啉替代呋喃衍生物作为RAF激酶抑制剂
公开(公告)号：WO2003022838A1
公开(公告)日：2003-03-20
申请号：PCT/EP2002/009944
申请日：2002-09-05
申请人： SMITHKLINE BEECHAM PLC , DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
发明人： DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
IPC分类号： C07D405/04
CPC分类号： C07D405/04 , C07D405/14
摘要： Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH 2 CO, S or NH, or the moiety X-R 1 is hydrogen; Y 1 and Y 2 independently represent CH or N; Ar is a mono- or fused bicyclic aromatic or heteroaromatic group which may be optionally substituted; one of X 1 and X 2 is selected from O, S or NR 11 and the other is CH, wherein R 11 is hydrogen, C 1-6 alkyl, aryl or arylC 1-6 alkyl.
摘要翻译：化合物及其作为药物的用途，特别是用作治疗神经创伤性疾病，癌症，慢性神经变性，疼痛，偏头痛和心脏肥大的Raf激酶抑制剂。其中X为O，CH> 2 为氢; Y1和Y2独立地表示CH或N; Ar是可以任选取代的单或二稠合双环芳族或杂芳族基团; X 1和X 2中的一个选自O，S或NR 11，另一个是CH，其中R 11是氢，C 1-6烷基，芳基或芳基C 1-6烷基。

5. 发明申请

WO2003022837A1 HETEROCYCLE-CARBOXAMIDE DERIVATIVES AS RAF KINASE INHIBITORS 审中-公开
标题翻译：杂环羧酰胺衍生物作为RAF激酶抑制剂
公开(公告)号：WO2003022837A1
公开(公告)日：2003-03-20
申请号：PCT/EP2002/009941
申请日：2002-09-05
申请人： SMITHKLINE BEECHAM P.L.C. , DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
发明人： DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
IPC分类号： C07D405/04
CPC分类号： C07D405/04
摘要： Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine or cardiac hypertrophy.
摘要翻译：化合物及其作为药物的用途，特别是用作治疗神经创伤性疾病，癌症，慢性神经变性，疼痛，偏头痛或心脏肥大的Raf激酶抑制剂。

6. 发明申请

WO2003022832A1 PYRIDYLFURANS AND PYRROLES AS RAF KINASE INHIBITORS 审中-公开
标题翻译：吡咯烷酮和吡咯烷酮作为RAF激酶抑制剂
公开(公告)号：WO2003022832A1
公开(公告)日：2003-03-20
申请号：PCT/EP2002/009943
申请日：2002-09-05
申请人： SMITHKLINE BEECHAM p.l.c. , DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
发明人： DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , A61K31/44 , A61K31/505 , C07D405/04
摘要： Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.
摘要翻译：化合物及其作为药物的用途，特别是用作治疗神经创伤性疾病，癌症，慢性神经变性，疼痛，偏头痛和心脏肥大的Raf激酶抑制剂。

7. 发明申请

WO2002094808A1 IMIDAZOLE-2-CARBOXAMIDE DERIVATIVES AS RAF KINASE INHIBITORS 审中-公开
标题翻译：咪唑-2-羧酰胺衍生物作为RAF激酶抑制剂
公开(公告)号：WO2002094808A1
公开(公告)日：2002-11-28
申请号：PCT/GB2002/002353
申请日：2002-05-20
申请人： SMITHKLINE BEECHAM P.L.C. , DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
发明人： DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/14
摘要： Compounds of formula (I): wherein X is O, CH 2 , S or NH, or the moiety X-R 1 is hydrogen; Y 1 and Y 2 independently represent CH or N; R 1 is hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, aryl, arylC 1-6 alkyl, heterocyclyl, heterocyclylC 1-6 alkyl, heteroaryl, or heteroarylC 1-6 alkyl, any of which except hydrogen may be optionally substituted; R 2 and R 3 independently represent hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, aryl, arylC 1-6 alkyl, heteroaryl, heteroarylC 1-6 alkyl, heterocyclyl, or heterocyclylC 1-6 alkyl, or R 2 and R 3 together with the nitrogen atom to which they are attached form a 4- to 10-membered monocyclic or bicyclic ring; Ar is a group of the formula a) or b), wherein A represents a fused 5- to 7-membered ring optionally containing up to two heteroatoms selected from O, S and NR 5 , wherein R 5 is hydrogen or C 1-6 alkyl, which ring is optionally substituted by up to 2 substituents selected from halogen, C 1-6 alkyl, hydroxy, C 1-6 alkoxy or keto ; R a and R 4 are independently selected from hydrogen, halogen, C 1-6 alkyl, aryl, arylC 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, haloC 1-6 alkyl, arylC 1-6 alkoxy, hydroxy, nitro, cyano, azido, amino, mono- and di- N -)C 1-6 alkylamino, acylamino, arylcarbonylamino, acyloxy, carboxy, carboxy salts, carboxy esters, carbamoyl, mono- and di- N -C 1-6 alkylcarbamoyl, C 1-6 alkoxycarbonyl,aryloxycarbonyl, ureido, guanidino, C 1-6 alkylguanidino, amidino, C 1-6 alkylamidino, sulphonylamino, aminosulphonyl, C 1-6 alkylthio, C 1-6 alkyl sulphinyl or C 1-6 alkylsulphonyl; and one of X 1 and X 2 is N and the other is NR 6 , wherein R 6 is hydrogen, C 1-6 alkyl, or arylC 1-6 alkyl; or pharmaceutically acceptable salts thereof.
摘要翻译：式（I）化合物：其中X是O，CH 2，S或NH，或X-R 1部分是氢; Y1和Y2独立地表示CH或N; R 1是氢，C 1-6烷基，C 3-7环烷基，芳基，芳基C 1-6烷基，杂环基，杂环基C 1-6烷基，杂芳基或杂芳基C 1-6烷基，除氢之外的任何一个可以是任选取代的; R 2和R 3独立地表示氢，C 1-6烷基，C 3-7环烷基，芳基，芳基C 1-6烷基，杂芳基，杂芳基C 1-6烷基，杂环基或杂环基C 1-6烷基，或R 2和R 3 与它们所连接的氮原子一起形成4-至10-元单环或双环; Ar是式a）或b）的基团，其中A表示稠合的5-至7-元环，任选地含有至多两个选自O，S和NR 5的杂原子，其中R 5是氢或 C 1-6烷基，该环任选被至多2个选自卤素，C 1-6烷基，羟基，C 1-6烷氧基或酮的取代基取代; R a和R 4独立地选自氢，卤素，C 1-6烷基，芳基，芳基C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基C 1-6烷基，卤代C 1-6烷基，芳基C 1-6烷氧基，羟基，硝基，氰基，叠氮基，氨基，单 - 和二 - N - C 1-6烷基氨基，酰氨基，芳基羰基氨基，酰氧基，羧基，羧基盐，羧基酯，氨基甲酰基，单 - 和二 - C 1-6烷基氨基甲酰基，C 1-6烷氧基羰基，芳氧基羰基，脲基，胍基，C 1-6烷基胍基，脒基，C 1-6烷基脒基，磺酰基氨基，氨基磺酰基，C 1-6烷硫基，C 1-6烷基亚磺酰基或C 1-6烷基磺酰基; X 1和X 2之一是N，另一个是NR 6，其中R 6是氢，C 1-6烷基或芳基C 1-6烷基; 或其药学上可接受的盐。

8. 发明申请

WO2004056369A1 BENZO ‘ D!AZEPINE DERIVATIVES FOR THE TREATMENT OF NEUROLOGICAL DISORDERS 审中-公开
标题翻译：用于治疗神经病的BENZO'D！AZEPINE衍生物
公开(公告)号：WO2004056369A1
公开(公告)日：2004-07-08
申请号：PCT/EP2003/014556
申请日：2003-12-18
申请人： GLAXO GROUP LIMITED , BAMFORD, Mark, James , DEAN, David, Kenneth , SEHMI, Sanjeet, Singh , WILSON, David, Matthew , WITHERINGTON, Jason
发明人： BAMFORD, Mark, James , DEAN, David, Kenneth , SEHMI, Sanjeet, Singh , WILSON, David, Matthew , WITHERINGTON, Jason
IPC分类号： A61K31/55
CPC分类号： C07D223/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04
摘要： The present invention relates to benzazepine derivatives of formula ( I ) wherein: R 1 represents -C 3-7 cycloalkyl optionally substituted by C 1-3 alkyl; having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
摘要翻译：本发明涉及式（I）的苯并氮杂衍生物，其中：R 1表示任选被C 1-3烷基取代的-C 3-7环烷基; 具有药理活性，其制备方法，含有它们的组合物及其在治疗神经和精神疾病中的用途。

9. 发明申请

WO2004089373A1 4- (4-(HETEROCYCLYLALKOXY}PHENYL)-1-(HETEROCYCLYL-CARBONYL)PIPERIDINE DERIVATIVES AND RELATED COMPOUNDS AS HISTAMINE H3 ANTAGONISTS FOR THE TREATMENT OF NEUROLOGICAL DISEASES SUCH AS ALZHEIMER’S 审中-公开
标题翻译： 4-（4-（间苯二甲氧基）苯基）-1-（杂环碳酰氯）哌啶衍生物及相关化合物作为治疗神经病变的组胺H3拮抗剂，如阿尔茨海默氏病
公开(公告)号：WO2004089373A1
公开(公告)日：2004-10-21
申请号：PCT/EP2004/003985
申请日：2004-04-08
申请人： GLAXO GROUP LIMITED , BAMFORD, Mark, James , DEAN, David, Kenneth , WILSON, David, Matthew
发明人： BAMFORD, Mark, James , DEAN, David, Kenneth , WILSON, David, Matthew
IPC分类号： A61K31/4545
CPC分类号： C07D401/06 , C07D211/22 , C07D211/46 , C07D401/14 , C07D405/06
摘要： The present invention provides, in a first aspect, a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein: R 1 represents -C 1-6 alkyl-O-C 1-6 alkyl, -C 3-8 cycloalkyl, aryl, heterocyclyl, heteroaryl and other groups; X represents a bond, O, CO, OCH 2 , CH 2 O or SO 2 ; Z represents CO, CONR 10 or SO 2 ; R 10 represents hydrogen, C 1-6 alkyl, -C 3-8 cycloalkyl, aryl, heterocyclyl, heteroaryl; A represents a single or a double bond; m and n independently represent 0, 1 or 2; R 2 represents hydrogen, C 1-6 alkyl or C 1-6 alkoxy; R 3 represents halogen, C 1-6 alkyl, hydroxy, C 1-6 alkoxy, cyano, amino, -COC 1-6 alkyl, -SO 2 C 1-6 alkyl or trifluoromethyl; R 4 represents -(CH 2 ) q -NR 11 R 12 or a group of formula (i) wherein all the other substituents are as defined in claim 1. Compounds of formula (I) and their pharmaceutically acceptable salts have affinity for and are antagonists and/or inverse agonists of the histamine H3 receptor and are believed to be of potential use in the treatment of neurological diseases including Alzheimer's disease.
摘要翻译：本发明在第一方面提供式（I）化合物或其药学上可接受的盐，其中：R 1表示-C 1-6烷基-O- C 1-6烷基，-C 3-8环烷基，芳基，杂环基，杂芳基和其它基团; X表示键，O，CO，OCH 2，CH 2 O或SO 2; Z表示CO，CONR 10或SO 2; R 10表示氢，C 1-6烷基，-C 3-8环烷基，芳基，杂环基，杂芳基; A表示单键或双键; m和n独立地表示0,1或2; R 2表示氢，C 1-6烷基或C 1-6烷氧基; R 3表示卤素，C 1-6烷基，羟基，C 1-6烷氧基，氰基，氨基，-COC 1-6烷基，-SO 2 C 1-6烷基或三氟甲基; R 4表示 - （CH 2）q -NR 11 R 12或式（i）的基团，其中所有其它取代基如权利要求1中所定义。式（I）化合物及其药学上可接受的盐对组胺H3受体具有亲和力并且是拮抗剂和/或反向激动剂，并被认为可用于治疗包括阿尔茨海默病在内的神经疾病。

10. 发明申请

WO2006125665A1 SUBSTITUTED PIPERIDINE ANTAGONIST OF HI RECEPTOR TO BE USED FOR THE TREATMENT OF RHINITIS 审中-公开
标题翻译：用于治疗RHINITI的HI受体的替代哌啶拮抗剂
公开(公告)号：WO2006125665A1
公开(公告)日：2006-11-30
申请号：PCT/EP2006/005053
申请日：2006-05-23
申请人： GLAXO GROUP LIMITED , BAMFORD, Mark, James , DEAN, David, Kenneth , HANCOCK, Ashley, Paul , WILSON, David, Matthew
发明人： BAMFORD, Mark, James , DEAN, David, Kenneth , HANCOCK, Ashley, Paul , WILSON, David, Matthew
IPC分类号： C07D401/14 , A61K31/435 , A61P37/00 , A61P29/00
CPC分类号： C07D211/46 , C07D401/14
摘要： The present invention relates to the compound, (I) and salts thereof, processes for its preparation, to compositions containing it and to its use in the treatment of various disorders, such as allergic rhinitis.
摘要翻译：本发明涉及化合物（I）及其盐，其制备方法，含有它的组合物及其在治疗各种疾病如过敏性鼻炎中的用途。

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