公开(公告)号：EP1838304B1

公开(公告)日：2009-08-19

申请号：EP05766007.8

申请日：2005-06-09

申请人： Schering Corporation ,  Pharmacopeia, LLC

发明人： ZHU, Zhaoning ,  MCKITTRICK, Brian ,  SUN, Zhong-Yue ,  YE, Yuanzan ,  VOIGT, Johannes H. ,  STRICKLAND, Corey ,  SMITH, Elizabeth M. ,  STAMFORD, Andrew ,  GREENLEE, William J. ,  MAZZOLA, Robert ,  CALDWELL, John ,  CUMMING, Jared ,  WANG, Lingyan ,  WU, Yusheng ,  ISERLOH, Ulrich ,  GUO, Tao ,  LE, Thuy X.H. ,  SAIONZ, Kurt W. ,  BABU, Suresh D. ,  HUNTER, Rachael C. ,  MORRIS, Michelle L. ,  GU, Huizhong ,  QIAN, Gang ,  TADESSE, Dawit

IPC分类号： A61K31/4168 ,  A61K31/4178 ,  C07D233/46 ,  C07D233/88 ,  C07D239/22 ,  C07D271/06 ,  C07D273/00 ,  C07D401/10 ,  C07D403/06 ,  C07D403/12 ,  C07D407/10 ,  C07D409/04 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  A61P9/00 ,  A61P25/00

CPC分类号： C07D233/88 ,  A61K31/4168 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/655 ,  A61K45/06 ,  C07D233/46 ,  C07D233/70 ,  C07D235/02 ,  C07D239/22 ,  C07D239/70 ,  C07D271/07 ,  C07D273/00 ,  C07D295/15 ,  C07D401/04 ,  C07D401/06 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/10 ,  C07D403/12 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D407/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  Y02A50/411

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 antagonist.

公开(公告)号：EP2066316A1

公开(公告)日：2009-06-10

申请号：EP07838156.3

申请日：2007-09-13

申请人： Schering Corporation

发明人： MCKITTRICK, Brian ,  SMITH, Elizabeth M. ,  BENNETT, Chad E. ,  BURNETT, Duane A. ,  KNUTSON, Chad E.

IPC分类号： A61K31/397 ,  C07D471/10 ,  C07D487/10 ,  A61K31/438 ,  A61P29/00

CPC分类号： C07D471/10 ,  C07D487/10

摘要： Disclosed are compounds of formula (I) wherein Z1 is -CH2- or -C(O)-, R4 and R5 are carbon chains (and optionally, together can form a C2 bridge), u and v are independently an integer of 0-3 such that there sum is from 3 to 5, and R2 is heteroaryl, and R1 and R3 are as defined herein. Also disclosed are methods of treating pain using a compound of formula (I).

公开(公告)号：EP2001870A2

公开(公告)日：2008-12-17

申请号：EP07754317.1

申请日：2007-03-28

申请人： Schering Corporation

发明人： CHAN, Tin-Yau ,  MCKITTRICK, Brian ,  PU, Haiyan ,  HONG, Liwu ,  PRONGAY, Andrew ,  XIAO, Li ,  MCCOY, Mark, A.

IPC分类号： C07D403/14 ,  C07D401/14 ,  C07D403/04 ,  A61K31/497

CPC分类号： C07D403/14 ,  C07D401/14 ,  C07D403/04

摘要： Disclosed is a compound of the formula and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating protein kinase mediatied diseases using the compound of formula (1.0). Also disclosed are methods of treating cancer using a compound of formula (1.0). The disclosed methods also include combination therapies wherein the compound of formula (1.0) is administered in combination with at least one addition pharmaceutically active ingredient.

公开(公告)号：EP1896478A2

公开(公告)日：2008-03-12

申请号：EP06784807.7

申请日：2006-06-12

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  MCKITTRICK, Brian ,  STAMFORD, Andrew ,  GREENLEE, William, J. ,  LIU, Xiaoxiang ,  MANDAL, Mihirbaran ,  VOIGT, Johannes, H. ,  STRICKLAND, Corey

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/28

CPC分类号： C07D487/04

摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein j, k, U, W, R, R1, R2, R3, R4, R6, R7 and R7a are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. 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.

公开(公告)号：EP1458676A2

公开(公告)日：2004-09-22

申请号：EP02792429.9

申请日：2002-12-19

申请人： SCHERING CORPORATION

发明人： ZHU, Zhaoning ,  MAZZOLA, Robert, Jr. ,  GUO, Zhuyan ,  LAVEY, Brian J. ,  SINNING, Lisa ,  KOZLOWSKI, Joseph ,  MCKITTRICK, Brian ,  SHIH, Neng-Yang

IPC分类号： C07C259/08 ,  C07C69/743 ,  C07D215/14 ,  C07D277/44 ,  C07D233/22 ,  A61K31/16 ,  A61K31/215 ,  A61K31/415 ,  A61K31/47 ,  A61P19/02

CPC分类号： C07D213/30 ,  C07C62/34 ,  C07C69/757 ,  C07C235/40 ,  C07C255/54 ,  C07C259/08 ,  C07C279/08 ,  C07C311/29 ,  C07C317/22 ,  C07C323/19 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07D213/40 ,  C07D213/73 ,  C07D213/74 ,  C07D215/06 ,  C07D215/14 ,  C07D215/18 ,  C07D215/233 ,  C07D215/26 ,  C07D215/38 ,  C07D219/02 ,  C07D221/16 ,  C07D233/60 ,  C07D233/64 ,  C07D251/10 ,  C07D277/24 ,  C07D277/64 ,  C07D311/04 ,  C07D311/58 ,  C07D317/08 ,  C07D317/64 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  Y02P20/582

摘要： This invention relates to compounds of the Formula (I):(Chemical formula should be inserted here as it appears on abstract in paper form)(I)or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-alpha or combinations thereof.

摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或异构体，其可用于治疗由MMP，TNF-α或其组合介导的疾病或病症。

公开(公告)号：EP2417135A1

公开(公告)日：2012-02-15

申请号：EP10714399.2

申请日：2010-04-05

申请人： Schering Corporation

发明人： HO, Ginny, D. ,  SMITH, Elizabeth, M. ,  KISELGOF, Eugenia, Y. ,  BASU, Kallol ,  TAN, Zheng ,  MCKITTRICK, Brian ,  TULSHIAN, Deen

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P3/04 ,  A61P3/10 ,  A61P25/00

CPC分类号： C07D471/04

摘要： The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.

公开(公告)号：EP2185522A1

公开(公告)日：2010-05-19

申请号：EP08795013.5

申请日：2008-08-04

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  GREENLEE, William, J. ,  CALDWELL, John, P. ,  MAZZOLA, Robert, D. ,  MCKITTRICK, Brian ,  BENNETT, Chad, E. ,  HUANG, Xianhai ,  JOSIEN, Hubert, B. ,  BURNETT, Duane, A.

IPC分类号： C07D217/24 ,  C07D487/04 ,  C07D498/04

CPC分类号： C07D487/04 ,  C07D217/24 ,  C07D498/04

摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明提供了一类作为γ分泌酶调节剂的新型杂环化合物，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法以及方法 使用这些化合物或药物组合物治疗，预防，抑制或改善一种或多种与中枢神经系统有关的疾病。

公开(公告)号：EP1773822B1

公开(公告)日：2009-06-17

申请号：EP05773671.2

申请日：2005-07-14

申请人： Schering Corporation

发明人： SU, Jing ,  MCKITTRICK, Brian ,  TANG, Haiqun ,  SASIKUMAR, Thavalakulamgara, K. ,  QIANG, Li

IPC分类号： C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D487/08

CPC分类号： C07D487/08 ,  C07D277/26 ,  C07D277/28 ,  C07D333/20 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

摘要： The present invention discloses compounds of formula (I) wherein m, n, p, R1, R2 and X, are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

公开(公告)号：EP2061462A2

公开(公告)日：2009-05-27

申请号：EP07838180.3

申请日：2007-09-13

申请人： Schering Corporation

发明人： HARRIS, Joel, M. ,  NEUSTADT, Bernard, R. ,  SOROTA, Stephen, C. ,  STAMFORD, Andrew, W. ,  TULSHIAN, Deen ,  MCKITTRICK, Brian

IPC分类号： A61K31/438 ,  A61K45/06 ,  A61K31/444 ,  A61K31/495 ,  A61K31/497 ,  A61K31/513 ,  A61P29/00 ,  A61P25/02 ,  A61P3/10 ,  A61P3/06

CPC分类号： A61K31/438 ,  A61K31/444 ,  A61K31/495 ,  A61K31/497 ,  A61K31/513 ,  A61K45/06

摘要： Disclosed is a method of treating a disease or condition (e.g., pain, diabetes or disorders of lipid metabolism) comprising administering an azetidine derivative of the formula (I) selected from the group consisting of the compounds defined by Tables 1, 2, 3a, 3b, 3c, 3d and 4a.

公开(公告)号：EP1940828A2

公开(公告)日：2008-07-09

申请号：EP06817385.5

申请日：2006-10-25

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  STAMFORD, Andrew, W. ,  MCKITTRICK, Brian

IPC分类号： C07D409/04 ,  C07D487/04 ,  C07D498/04 ,  A61K31/395 ,  A61P9/00 ,  A61P25/28 ,  A61P31/18 ,  A61P33/02

CPC分类号： C07D409/04 ,  C07D487/04

摘要： Disclosed are compounds of the formula I Chemical formula should be inserted here as it appears on the abstract in paper form. or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 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. 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.