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：EP1539678A1

公开(公告)日：2005-06-15

申请号：EP03772075.2

申请日：2003-07-30

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

发明人： TAVERAS, Arthur, G. ,  AKI, Cynthia, J. ,  CHAO, Jianping ,  DWYER, Michael ,  CHAO, Jianhua ,  YU, Younong ,  MERRITT, J., Robert ,  BIJU, Purakkattle ,  JAKWAY, James ,  LAI, Gaifa ,  WU, Minglang ,  HECKER, Evan, A. ,  LUNDELL, Daniel ,  FINE, Jay, S.

IPC分类号： C07C237/36 ,  C07C237/44 ,  C07C311/39 ,  C07D207/323 ,  C07D217/24 ,  C07D307/52 ,  C07D307/68 ,  C07D307/81 ,  C07D307/82 ,  C07D307/83 ,  C07D317/46 ,  C07D319/18 ,  C07D333/20 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  A61K31/341 ,  A61K31/36 ,  A61K31/381

CPC分类号： C07C237/30 ,  C07C225/20 ,  C07C237/36 ,  C07C237/44 ,  C07C255/59 ,  C07C311/39 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2602/08 ,  C07D207/335 ,  C07D213/74 ,  C07D217/24 ,  C07D295/26 ,  C07D307/38 ,  C07D307/52 ,  C07D307/68 ,  C07D307/81 ,  C07D307/82 ,  C07D307/83 ,  C07D317/46 ,  C07D319/18 ,  C07D333/20 ,  C07D333/36 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14

摘要： Disclosed are novel compounds of the formula (I)or a pharmaceutically acceptable salt or solvate thereof. Also disclosed is the treatment of chemokine-mediated diseases using compounds of the formula (II)

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：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：EP2041107A1

公开(公告)日：2009-04-01

申请号：EP07810279.5

申请日：2007-07-05

申请人： Schering Corporation ,  PHARMACOPEIA, INC.

发明人： CHAO, Jianhua ,  CZARNIECKI, Michael, F. ,  HE, Zhenmin ,  LAI, Gaifa ,  MERRITT, James, Robert

IPC分类号： C07D307/52 ,  A61K31/341 ,  A61K31/40 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D405/12 ,  C07D307/52 ,  C07D307/56

摘要： Disclosed are novel cyclobutenedione Compounds comprising a cycloclobutenedione ring, a substituted phenyl ring, and a -CH(C2H5)-furan moiety. The phenyl ring and the -CH(C2H5)-furan moiety are each bound to the cyclobutenedione ring through a -NH- moiety. Also disclosed are uses o Compounds for the manufacture of a medicament for treating chemokine mediated diseases (e.g., cancer, COPD, acute and chronic inflammatory disorders, psoriasis, cystic fibrosis, and asthma).

公开(公告)号：EP1551818B1

公开(公告)日：2009-02-04

申请号：EP03781311.0

申请日：2003-10-07

申请人： Schering Corporation ,  Pharmacopeia, 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：EP2097387A2

公开(公告)日：2009-09-09

申请号：EP08714220.4

申请日：2008-02-20

申请人： Schering Corporation ,  Pharmacopeia, Inc.

发明人： ZHU, Zhaoning ,  MCKITTRICK, Brian ,  SUN, Zhong-Yue ,  YE, Yuanzan, C. ,  VOIGT, Johannes, H. ,  STRICKLAND, Corey ,  SMITH, Elizabeth, M. ,  STAMFORD, Andrew ,  GREENLEE, William, J. ,  MAZZOLA, JR., Robert, D. ,  CALDWELL, John ,  CUMMING, Jared, N. ,  WANG, Lingyan ,  WU, Yusheng ,  ISERLOH, Ulrich ,  LIU, Xiaoxiang ,  HUANG, Ying ,  LI, Guoqing ,  PAN, Jianping ,  MISIASZEK, Jeffrey, A. ,  GUO, Tao ,  LE, Thuy X. H. ,  SAIONZ, Kurt, W. ,  BABU, Suresh, D. ,  HUNTER, Rachael, C. ,  MORRIS, Michelle, L. ,  GU, Huizhong ,  QIAN, Gang ,  TADESSE, Dawit ,  LAI, Gaifa ,  DUO, Jingqi ,  QU, Chuanxing ,  SHAO, Yuefei

IPC分类号： C07D233/88 ,  C07D239/22 ,  C07D401/06 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/14 ,  C07D495/10 ,  C07D401/10 ,  C07D417/10 ,  A61K31/513 ,  A61P25/28

CPC分类号： C07D233/88 ,  A61K31/4168 ,  A61K31/4178 ,  C07D239/22 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/10 ,  C07D417/14 ,  C07D495/10

摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, -C(=S)-, -S(O)-, -S(O)2-, -C(=O)-, -O-, -C(R6)(R7)-, -N(R5)- or -C(=N(R5))-; X is -O-, -N(R5)- or -C(R6)(R7)-; provided that when X is -O-, U is not -O-, -S(O)-, -S(O)2-, -C(=O)- or -C(=NR5)-; U is a bond, -S(O)-, -S(O)2-, -C(O)-, -O-, -P(O)(OR15)-, -C(=NR5)-, -(C(R6)(R7))b- or -N(R5)-; wherein b is 1 or 2; provided that when W is -S(O)-, -S(O)2-, -O-, or -N(R5)-, U is not -S(O)-, -S(O)2-, -O-, or -N(R5)-; provided that when X is -N(R5)- and W is -S(O)-, -S(O)2-, -O-, or -N(R5)-, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula (I). Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.