公开(公告)号：EP0923371A1

公开(公告)日：1999-06-23

申请号：EP97934696.0

申请日：1997-08-14

申请人： MOR-RESEARCH APPLICATIONS LTD. ,  YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM

发明人： NOVOGRODSKY, Abraham ,  LEVITZKI, Alexander ,  GAZIT, Aviv

IPC分类号： C07D231 ,  A01N1 ,  A61K31 ,  A61P39 ,  C07C255 ,  C07C317 ,  C07C327 ,  C07D213 ,  C07D277 ,  C07D307

CPC分类号： A61K31/415 ,  A61K31/277 ,  A61K31/427 ,  A61K31/4406

摘要： Compounds useful for countering undesired toxic effects to cells, tissues or organs having formula (I) wherein: Ar is a group of formulae (i) or (ii), n is O or, when Ar has formula (i) above, then n may also be 1, R is CN, -C(S)NH2, -C(O)NHR3 or, when R1 is 4-NO2 and R2 is H or 3-OH, then R may also be a group of formulae (iii), (iv), (v), (vi) where R3 is H, phenyl, phenyl(lower alkyl) or pyridylmethyl; R1 and R2 are each independently H, OH, NO2 or, when R is CN, also CH3, F, or CF3, provided that both R1 and R2 are not simultaneously H.

公开(公告)号：EP0748219B8

公开(公告)日：2005-06-08

申请号：EP95910239.3

申请日：1995-02-09

申请人： Sugen, Inc. ,  YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM

发明人： GAZIT, Aviv ,  LEVITZKI, Alexander ,  APP, Harald ,  TANG, Cho, Peng ,  MCMAHON, Gerald, M.

IPC分类号： A61K31/24 ,  A61K31/42 ,  A61K31/275 ,  A61K31/415 ,  A61K31/495 ,  C07C211/45 ,  C07C255/01 ,  C07D209/18 ,  C07D231/38 ,  C07D241/36 ,  C07C255/41 ,  C07D239/93

CPC分类号： C07D487/04 ,  A61K31/235 ,  A61K31/275 ,  A61K31/277 ,  A61K31/38 ,  A61K31/40 ,  A61K31/415 ,  A61K31/42 ,  A61K31/495 ,  A61K31/502 ,  A61K31/505 ,  A61K31/517 ,  A61K31/535 ,  A61K38/00 ,  C07C229/60 ,  C07C255/36 ,  C07C255/40 ,  C07C255/41 ,  C07C255/66 ,  C07C317/46 ,  C07C327/44 ,  C07D209/18 ,  C07D239/93 ,  C07D239/94 ,  C07D241/42 ,  C07D241/44 ,  C07K14/71 ,  C07K16/2863 ,  C07K2319/32 ,  G01N33/5008 ,  G01N33/5011 ,  G01N33/502 ,  G01N33/5064 ,  G01N33/5091 ,  G01N33/6893 ,  G01N2333/71 ,  G01N2500/04

公开(公告)号：EP0754038A1

公开(公告)日：1997-01-22

申请号：EP95917619.0

申请日：1995-04-20

申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM ,  THE HOSPITAL FOR SICK CHILDREN RESEARCH AND DEVELOPMENT LIMITED PARTNERSHIP

发明人： LEVITZKI, Alexander ,  GAZIT, Aviv ,  ROIFMAN, Chaim

IPC分类号： A61K31

CPC分类号： A61K31/275

摘要： The present invention relates to products and methods useful for treating leukemia, in particular acute lymphoblastomic leukemias. Compounds described herein are effective in inhibiting activities associated with ALL both in vitro and in vivo. Methods for modifying such compounds and screening other compounds are also provided in order to identify additional compounds with similar or better inhibition properties.

公开(公告)号：EP1036067A2

公开(公告)日：2000-09-20

申请号：EP98960526.6

申请日：1998-11-30

申请人： YISSUM RESEARCH DEVELOPMENT COMPANY of the Hebrew University of Jerusalem

发明人： LEVITZKI, Alexander ,  GAZIT, Aviv ,  BANAI, Shmuel ,  GERTZ, David, S. ,  GOLOMB, Gershon

IPC分类号： C07D241/36 ,  C07D471/00 ,  A01N43/58

CPC分类号： C07D409/04 ,  C07D241/42 ,  C07D487/04

摘要： PDGF receptor kinase inhibitory compounds of the quinoxaline family, methods for their synthesis and containment in slow release pharmaceutical preparations, and their use for treatment of proliferative malignant and non-malignant diseases or disorders by local or systemic application. A compound according to the invention includes a tyrphostin of general formula (I), wherein R1 and R2 are each independently selected from the group consisting of alkyl, alkoxy, halogen, nitro and amine and Ar is selected from the group consisting of phenyl, ferrocene, thiophene, furane, pyrrole, indole, thiazole, imidazole and pyridine.

公开(公告)号：EP0731697A1

公开(公告)日：1996-09-18

申请号：EP95904123.0

申请日：1994-11-23

申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM ,  Kupot- Holim Health Insurance Institute of the General Federation of Labour in Eretz-Israel ,  LEVITZKI, Alexander

发明人： LEVITZKI, Alexander ,  NOVOGRODSKY, Abraham ,  GAZIT, Aviv

IPC分类号： A61K31 ,  A61P9 ,  A61P11 ,  A61P17 ,  A61P29 ,  A61P31 ,  A61P37 ,  A61P43 ,  C07C255

CPC分类号： A61K31/275

摘要： SSI thyrphostins are useful in preventing LPS induced toxicity, TNFα induced toxicity, LPS induced increases in TNFα levels, nitric oxide production, and the treatment of septic shock and various immune disorders. Featured are novel compounds and pharmaceutical compositions, both of which may be used in the methods of prevention and/or treatment described herein, as well as methods for making the novel compounds.

公开(公告)号：EP0748219B1

公开(公告)日：2005-04-06

申请号：EP95910239.3

申请日：1995-02-09

申请人： Sugen, Inc. ,  YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM

发明人： GAZIT, Aviv ,  LEVITZKI, Alexander ,  APP, Harald ,  TANG, Cho, Peng ,  MCMAHON, Gerald, M.

IPC分类号： A61K31/24 ,  A61K31/42 ,  A61K31/275 ,  A61K31/415 ,  A61K31/495 ,  C07C211/45 ,  C07C255/01 ,  C07D209/18 ,  C07D231/38 ,  C07D241/36 ,  C07C255/41 ,  C07D239/93

CPC分类号： C07D487/04 ,  A61K31/235 ,  A61K31/275 ,  A61K31/277 ,  A61K31/38 ,  A61K31/40 ,  A61K31/415 ,  A61K31/42 ,  A61K31/495 ,  A61K31/502 ,  A61K31/505 ,  A61K31/517 ,  A61K31/535 ,  A61K38/00 ,  C07C229/60 ,  C07C255/36 ,  C07C255/40 ,  C07C255/41 ,  C07C255/66 ,  C07C317/46 ,  C07C327/44 ,  C07D209/18 ,  C07D239/93 ,  C07D239/94 ,  C07D241/42 ,  C07D241/44 ,  C07K14/71 ,  C07K16/2863 ,  C07K2319/32 ,  G01N33/5008 ,  G01N33/5011 ,  G01N33/502 ,  G01N33/5064 ,  G01N33/5091 ,  G01N33/6893 ,  G01N2333/71 ,  G01N2500/04

摘要： The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described. The invention also relates to the use of the disclosed compounds in the treatment of disorders, including cancer, diabetes, hemangioma and Kaposi's sarcoma, which are related to vasculogenesis and angiogenesis.

公开(公告)号：EP1180034A1

公开(公告)日：2002-02-20

申请号：EP00930818.0

申请日：2000-05-19

申请人： HADASIT MEDICAL RESEARCH SERVICES & DEVELOPMENT LIMITED ,  YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM

发明人： MISHANI, Eyal ,  BONASERA, Thomas ,  ORTU, Giuseppina ,  ROZEN, Yulia ,  GAZIT, Aviv ,  LEVITZKI, Alexandra

IPC分类号： A61K31/517 ,  A61P17/06 ,  A61P35/00 ,  C07D239/94

CPC分类号： C07D239/94 ,  A61K51/0459

摘要： A radiolabeled compound of formula (I): is described R1 and R2 are each independently selected from the group consisting of hydrogen, alkyl, hydroxy, alkoxy, halo, haloalkyl, carboxy, carbalkoxy and salts thereof; and A, B, C and D are each independently selected from the group consisting of a hydrogen and an electon withdrawing group, provided that at least one of A, B, C and D is [18] fluorine.

公开(公告)号：EP1161417A1

公开(公告)日：2001-12-12

申请号：EP00908883.2

申请日：2000-03-13

申请人： HSC Research and Development Limited Partnership ,  Yissum Research Development Company of the Hebrew University of Jerusalem

发明人： ROIFMAN, Chaim, M. ,  GAZIT, Aviv ,  LEVITZKI, Alexander

IPC分类号： C07C323/60 ,  C07D277/74 ,  A61K31/277 ,  A61K31/428 ,  A61P35/02

CPC分类号： C07D277/74 ,  C07C323/60

摘要： Compounds of general formula (I), wherein R1 is H or C1 to C3 alkyl; R2 is aryl or -(CH2)n-aryl and n is 1 to 4; R3 is H or CH3; and R4 is substituted or unsubstituted phenyl, pyridyl, thiophene, furan, indole, pyrrole, thiazole or imidazole are described, as well as methods for treating cell proliferative disorders and neoplastic disorders.

公开(公告)号：EP1228072B1

公开(公告)日：2005-09-28

申请号：EP00973192.8

申请日：2000-11-02

申请人： Yissum Research Development Company of the Hebrew University of Jerusalem

发明人： LEVITZKI, Alexander ,  GAZIT, Aviv ,  BANAI, Shmuel ,  GERTZ, David, S. ,  GOLOMB, Gershon ,  BOEHMER, Frank, D. ,  WALTENBERGER, Johannes

IPC分类号： C07D487/14 ,  A61K31/4188 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D487/04

摘要： A preparation of a tyrphostin including a compound of a general formula (Compound I) or (Compound II), wherein, for (Compound I), the preparation is enriched either for R6 at position 6 or for R6 at position 7, or, for (Compound II), the preparation is enriched either for R6 at position 6 or for R6 at position 8.

公开(公告)号：EP1161417B1

公开(公告)日：2003-12-03

申请号：EP00908883.2

申请日：2000-03-13

申请人： HSC Research and Development Limited Partnership ,  Yissum Research Development Company, of The Hebrew University of Jerusalem

发明人： ROIFMAN, Chaim, M. ,  GAZIT, Aviv ,  LEVITZKI, Alexander

IPC分类号： C07C323/60 ,  C07D277/74 ,  A61K31/277 ,  A61K31/428 ,  A61P35/02

CPC分类号： C07D277/74 ,  C07C323/60

摘要： Compounds of general formula (I), wherein R1 is H or C1 to C3 alkyl; R2 is aryl or -(CH2)n-aryl and n is 1 to 4; R3 is H or CH3; and R4 is substituted or unsubstituted phenyl, pyridyl, thiophene, furan, indole, pyrrole, thiazole or imidazole are described, as well as methods for treating cell proliferative disorders and neoplastic disorders.