公开(公告)号：EP1694659B1

公开(公告)日：2008-08-27

申请号：EP04814266.5

申请日：2004-12-16

申请人： Schering Corporation ,  Pharmacopeia Drug Discovery, Inc.

发明人： BIJU, Purakkattle, J. ,  TAVERAS, Arthur, G. ,  YU, Younong ,  ZHENG, Junying ,  CHAO, Jianhua ,  AKI, Cynthia, J. ,  FINE, Jay ,  LUNDELL, Daniel ,  PRIESTLEY, Tony ,  REGGIANI, Angelo ,  MERRITT, J., Robert ,  BALDWIN, John, J.

IPC分类号： C07D285/10 ,  C07D417/12 ,  C07D417/14 ,  A61K31/433 ,  A61K31/4436

CPC分类号： C07D285/10 ,  C07D285/06 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel compounds of Formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of Formula (IA).

摘要翻译： 公开了式（IA）的新化合物及其药学上可接受的盐和溶剂化物。 包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。 包含取代基B的基团的例子包括芳基和杂芳基。 还公开了治疗趋化因子介导的疾病例如癌症，血管生成，血管生成性眼病，肺部疾病，多发性硬化症，类风湿性关节炎，骨关节炎，中风和局部缺血再灌注损伤，疼痛（例如急性疼痛，急性和慢性 炎症性疼痛和神经性疼痛）使用式（IA）的化合物。

公开(公告)号：EP1313725B1

公开(公告)日：2007-04-11

申请号：EP01968188.1

申请日：2001-08-28

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

发明人： NJOROGE, F., George ,  VIBULBHAN, Bancha ,  COOPER, Alan, B. ,  GUZI, Timothy ,  RANE, Dinanath, F. ,  MINOR, Keith, P. ,  DOLL, Ronald, J. ,  GIRIJAVALLABHAN, Viyyoor, Moopil ,  SANTHANAM, Bama ,  PINTO, Patrick, A. ,  ZHU, Hugh, Y. ,  KEERTIKAR, Kartik, M. ,  ALVAREZ, Carmen, S. ,  BALDWIN, John, J. ,  LI, Ge ,  HUANG, Chia-Yu ,  JAMES, Ray, A. ,  BISHOP, Robert, W. ,  WANG, James ,  DESAI, Jagdish, A.

IPC分类号： C07D401/06 ,  C07D401/04 ,  C07D401/14 ,  C07D221/16 ,  A61K31/435 ,  A61P35/00

CPC分类号： C07D231/12 ,  C07D221/16 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14

摘要： The present invention discloses novel tricyclic compounds represented by the formula (1.0), a prodrug thereof, or a pharmaceutically acceptable salt or solvate of the compound or of said prodrug useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising such compounds their preparation as well as methods of using them to treat proliferative diseases such as cancer.

公开(公告)号：EP1694659A1

公开(公告)日：2006-08-30

申请号：EP04814266.5

申请日：2004-12-16

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

发明人： BIJU, Purakkattle, J. ,  TAVERAS, Arthur, G. ,  YU, Younong ,  ZHENG, Junying ,  CHAO, Jianhua ,  AKI, Cynthia, J. ,  FINE, Jay ,  LUNDELL, Daniel ,  PRIESTLEY, Tony ,  REGGIANI, Angelo ,  MERRITT, J., Robert ,  BALDWIN, John, J.

IPC分类号： C07D285/10 ,  C07D417/12 ,  C07D417/14 ,  A61K31/433 ,  A61K31/4436

CPC分类号： C07D285/10 ,  C07D285/06 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel compounds of Formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of Formula (IA).

公开(公告)号：EP1381590B1

公开(公告)日：2007-06-20

申请号：EP02739172.1

申请日：2002-04-15

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

发明人： TAVERAS, Arthur, G. ,  AKI, Cynthia, J. ,  BOND, Richard, W. ,  CHAO, Jianping ,  DWYER, Michael ,  FERREIRA, Johan, A. ,  CHAO, Jianhua ,  YU, Younong ,  BALDWIN, John, J. ,  KAISER, Bernd ,  LI, Ge ,  MERRITT, J., Robert ,  NELSON, Kingsley, H. ,  ROKOSZ, Laura, L.

IPC分类号： C07C237/30 ,  C07C255/59 ,  C07C225/20 ,  C07D213/74 ,  C07D307/52 ,  C07D333/36

CPC分类号： C07D231/38 ,  C07C225/20 ,  C07C237/30 ,  C07C255/59 ,  C07C2601/04 ,  C07D213/74 ,  C07D307/52 ,  C07D333/36

摘要： There are disclosed compounds of Formula (I) or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.

摘要翻译： 公开了可用于治疗趋化因子介导的疾病如急性和慢性炎症性疾病和癌症的具有下式的化合物或其药学上可接受的盐或溶剂合物。

公开(公告)号：EP1492772A1

公开(公告)日：2005-01-05

申请号：EP03711214.1

申请日：2003-02-25

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

发明人： ZHU, Hugh, Y. ,  NJOROGE, F., George ,  COOPER, Alan, B. ,  GUZI, Timothy, J. ,  RANE, Dinanath, F. ,  MINOR, Keith, P. ,  DOLL, Ronald, J. ,  GIRIJAVALLABHAN, Viyyoor, Moopil ,  SANTHANAM, Bama ,  PINTO, Patrick, A. ,  VIBULBHAN, Bancha ,  KEERTIKAR, Kartik, M. ,  ALVAREZ, Carmen, S. ,  BALDWIN, John, J. ,  LI, Ge ,  HUANG, Chia-Yu ,  JAMES, Ray, A. ,  BISHOP, W., Robert ,  WANG, James J-S ,  Desai, Jagdish A

IPC分类号： C07D221/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D521/00 ,  A61K31/47 ,  A61K31/50 ,  A61K31/444 ,  A61K31/445 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61P35/00

CPC分类号： C07D231/12 ,  C07D221/16 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14

摘要： Disclosed are novel tricyclic compounds represented by the formula (1.0) and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising compounds of formula 1.0. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

公开(公告)号：EP0819121B1

公开(公告)日：2007-05-30

申请号：EP96912469.2

申请日：1996-04-03

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

发明人： AFONSO, Adriano ,  BALDWIN, John, J. ,  DOLL, Ronald, J. ,  LI, Ge ,  MALLAMS, Alan, K. ,  NJOROGE, F., George ,  RANE, Dinanath, F. ,  READER, John, C. ,  ROSSMAN, Randall, R.

IPC分类号： C07D221/16 ,  A61K31/435 ,  C07D401/04 ,  C07D491/04 ,  C07D405/12 ,  C07D401/12

CPC分类号： C07D401/04 ,  C07D221/16 ,  C07D401/12 ,  C07D491/04

摘要： Novel compounds of Formula (1.0) are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of formula (1.0) to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.

公开(公告)号：EP1697354A1

公开(公告)日：2006-09-06

申请号：EP04814856.3

申请日：2004-12-20

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

发明人： TAVERAS, Arthur, G. ,  ZHENG, Junying ,  BIJU, Purakkattle, J. ,  YU, Younong ,  CHAO, Jianhua ,  FINE, Jay ,  LUNDELL, Daniel ,  PRIESTLEY, Tony ,  REGGIANI, Angelo ,  MERRITT, J., Robert ,  BALDWIN, John, J. ,  LAI, Gaifa ,  WU, Minglang

IPC分类号： C07D417/12 ,  C07D275/02 ,  C07D417/14 ,  A61K31/427 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D275/03 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel compounds of the formula (IA): and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

公开(公告)号：EP1140909B1

公开(公告)日：2005-07-06

申请号：EP99965906.3

申请日：1999-12-22

申请人： Schering Corporation ,  Pharmacopeia Drug Discovery, Inc.

发明人： COOPER, Alan, B. ,  DOLL, Ronald, J. ,  FERREIRA, Johan, A. ,  GANGULY, Ashit ,  GIRIJAVALLABHAN, Viyyoor, M. ,  TAVERAS, Arthur, G. ,  CHAO, Jianping ,  BALDWIN, John, J. ,  HUANG, Chia-Yu ,  LI, Ge

IPC分类号： C07D403/12 ,  C07D401/14 ,  C07D241/04 ,  A61K31/496 ,  A61P35/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D241/04 ,  C07D249/08 ,  C07D401/14 ,  C07D403/12

摘要： Novel compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl-protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel aminooxyamide compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.

公开(公告)号：EP1551818A1

公开(公告)日：2005-07-13

申请号：EP03781311.0

申请日：2003-10-07

申请人： Pharmacopeia Drug Discovery, Inc.

发明人： TAVERAS, Arthur, G. ,  CHAO, Jianhua ,  BIJU, Purakkattle, J. ,  YU, Younong ,  FINE, Jay, S. ,  HIPKIN, William ,  AKI, Cynthia, J. ,  MERRITT, J., Robert ,  LI, Ge ,  BALDWIN, John, J. ,  LAI, Gaifa ,  WU, Minglang ,  HECKER, Evan, A.

IPC分类号： C07D285/10 ,  C07D417/12 ,  C07D417/14 ,  A61K31/433 ,  A61K31/4436

CPC分类号： C07D285/10 ,  C07D417/02 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel compounds of the formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula (IA).

公开(公告)号：EP1891017A1

公开(公告)日：2008-02-27

申请号：EP05758425.2

申请日：2005-06-13

申请人： Pharmacopeia Drug Discovery, Inc.

发明人： LETOURNEAU, Jeffrey, John ,  PARADKAR, Vidyadhar ,  OHLMEYER, Michael, H., J. ,  DILLARD, Lawrence, W. ,  BALDWIN, John, J. ,  RIVIELLO, Christopher, Mark ,  WONG, Angela ,  RONG, Yajing

IPC分类号： C07D235/30 ,  C07D403/12 ,  C07D215/38 ,  C07D405/12 ,  C07D401/12 ,  A61K31/4184 ,  A61P35/00

摘要： Nitrogen heterocycle biaryls having a carboxylate terminus are useful for treating endometriosis, osteoporosis, restenosis following angioplasty, rheumatoid arthritis, cancer, macular degeneration and obesity. Compounds of formula: (I) are disclosed. A representative example is : (II)

摘要翻译： 具有羧酸酯末端的氮杂环联芳基化合物可用于治疗子宫内膜异位症，骨质疏松症，血管成形术后的再狭窄，类风湿性关节炎，癌症，黄斑变性和肥胖症。 式（I）化合物被公开。 一个具有代表性的例子是：（二）