公开(公告)号：EP1937652B1

公开(公告)日：2014-07-30

申请号：EP06816247.8

申请日：2006-10-04

申请人： Aventis Pharmaceuticals Inc.

发明人： ALDOUS, Suzanne C. ,  JIANG, John Ziqi ,  LU, Jinqi ,  MA, Liang ,  MU, Lan ,  MUNSON, Harry Randall ,  SABOL, Jeffrey Stephen ,  THURAIRATNAM, Sukanthini ,  VANDEUSEN, Christopher Loren

IPC分类号： C07D239/28 ,  C07D401/04 ,  C07D403/12 ,  C07D413/04 ,  A61K31/506 ,  A61P11/00

CPC分类号： C07D239/28 ,  C07D401/04 ,  C07D403/12 ,  C07D413/04

公开(公告)号：EP1667988B1

公开(公告)日：2013-04-10

申请号：EP04782722.5

申请日：2004-08-27

申请人： Aventis Pharmaceuticals Inc.

发明人： JACKSON, Sharon ,  NIEDUZAK, Thaddeus, R. ,  REBELLO, Sam, S. ,  LIANG, Guyan ,  CHIANG, Yulin ,  MERRILL, Jean

IPC分类号： C07D311/18 ,  C07D311/46 ,  C07D405/12 ,  C07D407/12

CPC分类号： C07D405/12 ,  C07D311/46 ,  C07D407/12

公开(公告)号：EP2547672A1

公开(公告)日：2013-01-23

申请号：EP11710373.9

申请日：2011-03-15

申请人： Aventis Pharmaceuticals Inc.

发明人： HARRIS, Keith J. ,  AGUIAR, Joacy C. ,  SHUM, Patrick Wai-Kwok ,  ZHAO, Zhicheng ,  POLI, Gregory B. ,  STOKLOSA, Gregory ,  CHOI-SLEDESKI, Yong-Mi ,  REILING, Stephan ,  STEFANY, David ,  GARDNER, Charles

IPC分类号： C07D403/04 ,  A61K31/505 ,  A61P11/00

CPC分类号： C07D403/04

摘要： The present invention is directed to a substituted pyrimidine compound of formula (I) as set forth herein, or an enantiomer thereof, or a prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such a compound. The invention also includes a method of treatment of a patient by the administration of a pharmaceutically effective amount of such a compound. Formula (I), wherein m and n, independently of each other, are selected from the integers 0, 1, 2 or 3; X and Y, independently of each other, are selected from CR
1 R
2 , NR
1 or O, wherein X and Y cannot both be O; or X and Y, taken together with the bond between them, form a phenyl group optionally substituted by one to four R
3 groups; each Z, independently of each other, is CR
1 R
2 ; R
1 , R
2 and R
3 , independently of each other, are selected from the group consisting of H, halogen, aryl, amino, optionally substituted alkyl, optionally substituted alkoxy, and carboxy; wherein optionally substituted alkyl, may be substituted by one to three of the same or different of halogen, carboxy, cyano, hydroxy, amino or aryl.

公开(公告)号：EP2395108A1

公开(公告)日：2011-12-14

申请号：EP11003917.9

申请日：2005-12-01

申请人： Aventis Pharmaceuticals Inc.

发明人： Grueneberg, Dorre ,  Huang, Xi ,  Natesan, Sridaran ,  August, Paul

IPC分类号： C12Q1/68 ,  G01N33/574

CPC分类号： C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158 ,  C12Q2600/178 ,  G01N33/574 ,  G01N33/6893

摘要： The present invention relates to novel and useful methods that predict or monitor a patient's response to a molecule of the taxoid family by measuring the increase or decrease of specific genetic markers, in particular GBP1, as compared to controls. The present invention also provides kits that predict of monitor patient's response to a molecule of the taxoid family by measuring nucleic acid or protein levels of particular genetic markers and comparing their levels to controls or reference markers.

摘要翻译： 本发明涉及新的和有用的方法的确预测或通过测量增加或特定的遗传标记的减少，特别是GBP1，监测患者对紫杉醇类分子的反应与对照相比。 因此，本发明提供试剂盒，并通过预测测量特定遗传标记的核酸或蛋白质水平和它们的水平进行比较来控制或参考标记监控患者对紫杉醇类分子反应。

公开(公告)号：EP0853618B1

公开(公告)日：2011-08-17

申请号：EP96919298.8

申请日：1996-06-07

申请人： Aventis Pharmaceuticals Inc.

发明人： EWING, William, R. ,  BECKER, Michael, R. ,  PAULS, Henry, W. ,  CHENEY, Daniel, L. ,  MASON, Jonathan, Stephen ,  SPADA, Alfred, P. ,  CHOI-SLEDESKI, Yong, Mi

IPC分类号： C07D207/26 ,  A61K31/40 ,  C07D407/12 ,  C07D401/12 ,  A61K31/47 ,  C07D409/14 ,  A61K31/44 ,  C07D207/14 ,  C07D207/40 ,  C07D211/76 ,  A61K31/445 ,  C07D223/12 ,  A61K31/55 ,  C07D409/12 ,  C07D403/12 ,  A61K31/505 ,  C07D205/085 ,  A61K31/395 ,  A61K31/415 ,  C07D401/06 ,  C07D409/06 ,  C07D407/06

CPC分类号： C07D207/273 ,  C07D205/085 ,  C07D207/14 ,  C07D207/416 ,  C07D211/76 ,  C07D223/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14

摘要： The compounds of formula (I) exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula (I), compositions containing compounds of formula (I), and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

公开(公告)号：EP1585525B1

公开(公告)日：2010-11-17

申请号：EP03814050.5

申请日：2003-12-16

申请人： Aventis Pharmaceuticals Inc.

发明人： ZHU, Bin ,  WETTSTEIN, Joseph ,  PETTY, Margaret

IPC分类号： A61K31/55 ,  A61P25/28

CPC分类号： A61K31/538 ,  A61K31/542 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554

摘要： The invention relates to the use of compound of Formula (I) in treating patients for inflammatory or neuropathic pain as well as various symptoms of multiple schlerosis.

公开(公告)号：EP1085943B1

公开(公告)日：2009-11-25

申请号：EP99923278.8

申请日：1999-05-20

申请人： Aventis Pharmaceuticals Inc.

发明人： STEIN,David T. ,  BAUM, Stephen, A.

IPC分类号： B01J19/00 ,  B01L3/00 ,  B01L11/00 ,  B01L9/00 ,  G01N33/53 ,  G01N33/543

CPC分类号： B82Y30/00 ,  B01J19/0046 ,  B01J2219/00286 ,  B01J2219/0031 ,  B01J2219/00317 ,  B01J2219/00319 ,  B01J2219/00322 ,  B01J2219/00461 ,  B01J2219/00468 ,  B01J2219/00475 ,  B01J2219/00497 ,  B01J2219/005 ,  B01J2219/00502 ,  B01J2219/00522 ,  B01J2219/00527 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00596 ,  B01J2219/00668 ,  B01J2219/00675 ,  B01J2219/00689 ,  B01J2219/0072 ,  B01J2219/00722 ,  B01J2219/00725 ,  B01L2300/0819 ,  B01L2300/0829 ,  C40B40/06 ,  C40B40/10 ,  C40B50/14 ,  C40B60/14 ,  G01N33/543

摘要： A three-dimensional (3D) array of solid-phase supports is adapted to provide parallel synthesis of a library of molecules with 3D diversity. Individual locations in the 3D array may be assigned to selected molecules in the library such that molecules may be synthesized at and retrieved from such locations. Also, the supports include aperture walls in stacked plates; the supports may be suspended within stacked plate apertures; the 3D array includes discrete supports arranged in columns in one or more wells; the supports include tube inner walls or may be suspended in tubes, the tubes being secured in stacked, two-dimensional (2D) frameworks; or the supports include beads contained in porous enclosures having non-porous side walls and being secured in stacked, 2D frameworks. A support transfer device enables transfer of solid-phase supports used in a 3D array. Such apparatus includes: a rack of rods sized to be inserted through supports and a mechanism to prevent supports from coming off the rack; tubes connected to a vacuum manifold to suction supports one Z plane at a time; or a transfer block having recesses to receive one or more supports and at least one gate withholding supports from passing through the gate when in a closed position. A method of 3D synthesis includes: a) functionalizing solid-phase supports; b) placing supports in a 3D array; and c) performing parallel synthesis with 3D diversity. At least one unique R1 group member may be assigned to each Z plane.

公开(公告)号：EP1501797B1

公开(公告)日：2009-08-05

申请号：EP03733867.0

申请日：2003-04-23

申请人： Aventis Pharmaceuticals Inc.

发明人： ALKAN, Sefik, S. ,  DINERSTEIN, Robert, J. ,  SUBRAMANIAM, Arun ,  HRIB, Nicholas, J. ,  JURCAK, John, G.

IPC分类号： C07D209/42 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D401/14 ,  C07D405/14 ,  A61K31/40 ,  A61P11/06 ,  A61P37/08 ,  A61P31/04

CPC分类号： C07D401/12 ,  A61K31/40 ,  A61K31/405 ,  C07D209/42 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12

摘要： This invention discloses and claims substituted 3-amino-2-carboxylic acid indole and benzo(b)thiophene derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. In preferred embodiments of this invention it is also disclosed and claimed that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.

公开(公告)号：EP1581486B1

公开(公告)日：2009-07-29

申请号：EP03779081.3

申请日：2003-09-18

申请人： Aventis Pharmaceuticals Inc.

发明人： LI, Zhuyin, Julie ,  MEHDI, Shujaath

IPC分类号： C12Q1/48

CPC分类号： C12Q1/48

摘要： Provided herein is a novel and useful method for determining whether a compound or agent decreases or inhibits the activity of a poly(ADP-ribose)-polymerase (PARP).

公开(公告)号：EP1687642B1

公开(公告)日：2009-01-14

申请号：EP04790957.7

申请日：2004-10-07

申请人： CENTELION ,  Aventis Pharmaceuticals Inc.

发明人： NESBIT, Mark ,  SPADA, Alfred, P. ,  HE, Wei ,  MYERS, Michael, R.

IPC分类号： G01N33/74 ,  G01N33/50

CPC分类号： A61K31/498 ,  G01N33/5011 ,  G01N2333/71

摘要： This invention is directed to potent inhibitors of protein tyrosine kinase alone or in synergistic combination with antiangiogenic or chemotherapeutic agents for the abrogation of mature vasculature within chemotherapeutic refractory tumors, pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cell proliferation, and particularly treatment of brain cancer, ovarian cancer, pancreatic cancer prostate cancer, and human leukemias, such as CML, AML or ALL.