公开(公告)号：EP1874768A2

公开(公告)日：2008-01-09

申请号：EP06758426.8

申请日：2006-04-20

申请人： SMITHKLINE BEECHAM CORPORATION

发明人： SEEFELD, Mark, Andrew ,  ROUSE, Meagan, B. ,  HEERDING, Dirk, A.

IPC分类号： C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02 ,  A01N43/42 ,  A61K31/44

CPC分类号： C07D471/04

摘要： Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.

摘要翻译： 本发明的是新的1H-咪唑并[4,5-c]吡啶-2-基化合物，这些化合物作为蛋白激酶B活性抑制剂的用途以及治疗癌症和关节炎。

公开(公告)号：EP1863808A1

公开(公告)日：2007-12-12

申请号：EP06738759.7

申请日：2006-03-17

申请人： Transform Pharmaceuticals, Inc.

发明人： ALMARSSON, Orn ,  HICKEY, Magali, Bourghol ,  PETERSON, Matthew

IPC分类号： C07D471/02 ,  A61K31/44

CPC分类号： C07D498/04

摘要： The invention provides novel gaboxadol forms. These forms include salts, hydrates, solvates, and polymorphs of gaboxadol. The invention also provides novel compositions comprising these novel soluble forms and a suitable carrier. The invention also provides related methods of treatment. Compositions and methods of the invention of the invention have a number of uses, including the treatment or prevention of sleep disorders.

公开(公告)号：EP1737862A4

公开(公告)日：2007-11-28

申请号：EP05737039

申请日：2005-04-21

申请人： EISAI R&D MAN CO LTD

发明人： MIYAZAWA SHUHEI ,  HARADA HITOSHI ,  FUJISAKI HIDEAKI ,  KUBOTA ATSUHIKO ,  KODAMA KOTARO ,  NAGAKAWA JUNICHI ,  WATANABE NOBUHISA ,  OKETANI KIYOSHI

IPC分类号： C07D471/04 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4745 ,  A61P1/04 ,  A61P1/06 ,  A61P31/04 ,  C07D471/02

CPC分类号： A61K31/444 ,  C07D471/04

摘要： A compound represented by the following general formula (1), or a salt or hydrate thereof: wherein R1 represents a C1-C6 alkyl group or C2-C6 alkynyl group which may be substituted, or a phenyl group which may be substituted, R2 represents a hydrogen atom or a C1-C6 alkyl group, R3 represents methyl or ethyl group, R4 represents a C1-C6 alkyl group, R5 represents a hydrogen atom, provided that a compound wherein R1 is a C1-C6 alkyl group unsubstituted or substituted with a halogen atom and R2 is a hydrogen atom is excluded.

摘要翻译： 下述通式（1）表示的化合物或其盐或水合物，式中，R1表示可以被取代的C1-C6烷基或C2-C6炔基或可以被取代的苯基，R2表示 氢原子或C 1 -C 6烷基，R 3表示甲基或乙基，R 4表示C 1 -C 6烷基，R 5表示氢原子，条件是其中R 1为未被取代或被 卤素原子和R2是氢原子。

公开(公告)号：EP1838152A2

公开(公告)日：2007-10-03

申请号：EP06718998.5

申请日：2006-01-19

申请人： NEUROGEN CORPORATION

发明人： HAN, Bingsong ,  GAO, Yang ,  XIE, Linghong

IPC分类号： A01N43/58 ,  A01N43/60 ,  A01N43/90 ,  A01N43/42 ,  A61K31/50 ,  A61K31/495 ,  A61K31/519 ,  A61K31/44 ,  C07D237/26 ,  C07D237/28 ,  C07D487/00 ,  C07D471/00 ,  C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D513/04

摘要： Compounds of Formula I and Formula II are provided, as are methods for their preparation. The variables Y, Z1, Z2, Z3, R4, R5, R6, R7, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).

公开(公告)号：EP1836203A2

公开(公告)日：2007-09-26

申请号：EP06718423.4

申请日：2006-01-13

申请人： NEUROGEN CORPORATION

发明人： CALDWELL, Timothy M. ,  CHENARD, Bertrand ,  HODGETTS, Kevin

IPC分类号： C07D471/02 ,  C07D215/38 ,  C07D215/44 ,  C07D401/00 ,  C07D403/00 ,  C07D409/00 ,  C07D239/02 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00 ,  C07D495/00 ,  C07D497/00 ,  A01N43/58 ,  A01N43/60 ,  A01N43/54 ,  A01N43/42 ,  A61K31/50 ,  A61K31/45 ,  A61K31/501 ,  A61K31/505 ,  A61K31/47

CPC分类号： C07D471/04 ,  C07D417/14

摘要： Heteroaryl substituted quinolin-4-ylamine analogues of Formula (I) are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

公开(公告)号：EP1789055A2

公开(公告)日：2007-05-30

申请号：EP05810363.1

申请日：2005-09-15

申请人： JANSSEN PHARMACEUTICA N.V.

发明人： CONNOLLY, Peter, J. ,  JOHNSON, Sigmond, G. ,  PANDEY, Niranjan, B. ,  MIDDLETON, Steven, A.

IPC分类号： A61K31/535 ,  A61K31/44 ,  C07D413/00 ,  C07D471/02

CPC分类号： C07D497/04 ,  C07D513/04

摘要： The present invention is directed to novel thiazolopyridines, pharmaceutical compositions thereof, and the use thereof as inhibitors of ATP-protein kinase interactions. The thiazolopyridine compounds have the following formula (I).

公开(公告)号：EP1541146B1

公开(公告)日：2006-12-20

申请号：EP05001922.3

申请日：2001-04-24

申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD.

发明人： Aronhime, Judith ,  Leonov, David ,  Meszaros-Sos, Erzebet ,  Salyi, Szaboles ,  Szabo, Csaba ,  Zavurov, Shlomo

IPC分类号： A61K31/44 ,  C07D471/02 ,  A61P43/00 ,  C07D471/04 ,  C07D235/00 ,  C07D221/00

CPC分类号： C07D471/04 ,  A61K31/44

公开(公告)号：EP1496836A4

公开(公告)日：2006-03-22

申请号：EP03716466

申请日：2003-03-12

申请人： MERCK & CO INC

发明人： EGBERTSON MELISSA ,  LANGFORD H MARIE ,  MELAMED JEFFREY Y ,  WAI JOHN S ,  HAN WEI ,  PERLOW DEBBIE S ,  ZHUANG LINGHANG ,  EMBREY MARK

IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61K31/541 ,  A61K31/549 ,  A61K45/00 ,  A61P31/18 ,  A61P43/00 ,  C07D471/02

CPC分类号： C07D471/04

公开(公告)号：EP1560488A2

公开(公告)日：2005-08-10

申请号：EP03783156.7

申请日：2003-11-04

申请人： SMITHKLINE BEECHAM CORPORATION

发明人： AXTEN, Jeffrey, Michael ,  GALLAGHER, Timothy, Francis ,  MILLER, William, Henry ,  SEEFELD, Mark, Antony

IPC分类号： A01N43/64 ,  A01N43/42 ,  A61K31/53 ,  A61K31/44 ,  A61K31/47 ,  C07D215/20 ,  C07D215/36 ,  C07D471/02 ,  C07D253/00

CPC分类号： C07D471/04 ,  C07D413/12 ,  C07D513/04

摘要： Quinoline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.

摘要翻译： 喹啉和萘啶衍生物用于治疗哺乳动物，特别是人的细菌感染。

公开(公告)号：EP1314726A4

公开(公告)日：2005-07-13

申请号：EP01958508

申请日：2001-08-27

申请人： YAMANOUCHI PHARMA CO LTD

发明人： KAZAMI J ,  WATANABE M ,  HIRATA T

IPC分类号： A61K31/4375 ,  A61K31/44 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4741 ,  A61K31/503 ,  A61K31/519 ,  A61K31/5383 ,  A61P31/04 ,  C07D215/36 ,  C07D215/48 ,  C07D401/14 ,  C07D471/02 ,  C07D471/04 ,  C07D471/14 ,  C07D487/02 ,  C07D498/06

CPC分类号： A61K31/4741 ,  A61K31/4375 ,  A61K31/4709 ,  C07D215/48 ,  C07D401/14 ,  C07D471/04

摘要： Ester or amide derivatives represented by the following general formula (I) which have an antibacterial effect on Helicobacter pylori or pharmaceutically acceptable salts thereof. In particular, ester or amide derivatives of 3-alkyl-3-oxo-1,4-dihydroquinoline-2-carboxylic acids represented by the following general formulae (I') and (I') or pharmaceutically acceptable salts thereof. In said formula (I), X1 to X4 independently represent each C or N; Y represents O or NH; R1 represents C1 to C6 alkyl; R2 represents C?1 to C10¿ alkyl, etc.; R3 represents hydrogen, C1 to C6 alkyl, etc.; and R4 to R7 are the same or different and each represents hydrogen, halogeno, C1 to C6 alkyl, etc.