公开(公告)号：EP0617705A1

公开(公告)日：1994-10-05

申请号：EP92925312.0

申请日：1992-11-19

Applicant: YEDA RESEARCH AND DEVELOPMENT COMPANY, LTD.

Inventor： LIDER, Ofer ,  GREENSPOON, Noam ,  HERSHKOVIZ, Rami ,  RONEN, Alon

IPC: A61K31 ,  A61P7 ,  A61P35 ,  A61P37 ,  A61P43 ,  C07C279 ,  C07C323 ,  C07D211 ,  C07K5 ,  A61K38

CPC classification number: C07K5/06026 ,  A61K38/00 ,  C07C279/08 ,  C07C279/12 ,  C07C279/14 ,  C07C323/44 ,  C07D211/60 ,  C07K5/0202 ,  C07K5/06086 ,  Y10S514/822

Abstract: Des analogues RXD non peptidiques inhibent des interactions moléculaires et cellulaires biologiques qui dépendent de la reconnaissance de RXD, X représentant l'un des restes d'amino acides G, E, Y, A ou F. En particulier les succédanés RGD n'ont pas de séquences d'amino acides alpha-naturels et comprennent un groupe guanidino et un groupe terminal carboxyle espacés par une chaîne de 11 atomes, dont au moins 5 sont des atomes de carbone. Les composés empêchent l'adhésion des cellules et sont utiles pour le traitement de divers états pathologiques, par exemple, la thrombose, les maladies autoimmunes, les métastases, les allergies, les réactions hôtes-greffes et empêchent la formation de tissu cicatriciel.

Abstract translation: 非肽RXD类似物抑制依赖于RXD识别的分子和细胞细胞相互作用，其中X代表氨基酸残基G，E，Y，A或F中的一个。特别地，RGD替代物不 的α-天然氨基酸序列并且包含间隔有11个原子链的胍基和羧基端基，其中至少5个是碳原子。 该化合物可防止细胞粘附，并可用于治疗各种疾病状态，例如血栓形成，自身免疫性疾病，转移，变态反应，宿主 - 移植物反应并防止疤痕组织形成。

公开(公告)号：EP1673097A2

公开(公告)日：2006-06-28

申请号：EP04788634.6

申请日：2004-09-08

Applicant: YEDA RESEARCH AND DEVELOPMENT COMPANY, LTD.

Inventor： SCHWARTZ, Michal ,  LIDER, Ofer ,  ROLLS, Asya ,  CAHALON, Liora

IPC: A61K31/7016 ,  A61K31/702

CPC classification number: A61K31/7016 ,  A61K31/702 ,  A61K31/727 ,  A61K31/728 ,  A61K31/737

Abstract: Oligosaccharides, and in particular disaccharides, which are degradation products of chondroitin sulfate proteoglycan are effective for use in treating, inhibiting, or ameliorating the effects of injuries or diseases or disorders that result in or are caused by neuronal degeneration or of disorders resulting in mental and cognitive dysfunction.

公开(公告)号：EP0617705B1

公开(公告)日：1997-09-24

申请号：EP92925312.8

申请日：1992-11-19

Applicant: YEDA RESEARCH AND DEVELOPMENT COMPANY, LTD.

Inventor： LIDER, Ofer ,  GREENSPOON, Noam ,  HERSHKOVIZ, Rami ,  RONEN, Alon

IPC: C07K5/08 ,  C07C279/12 ,  C07C279/14 ,  C07D211/60 ,  C07D211/62 ,  A61K31/155 ,  A61K31/195 ,  A61K31/445

CPC classification number: C07K5/06026 ,  A61K38/00 ,  C07C279/08 ,  C07C279/12 ,  C07C279/14 ,  C07C323/44 ,  C07D211/60 ,  C07K5/0202 ,  C07K5/06086 ,  Y10S514/822

Abstract: Non-peptidic RXD analogues are provided that inhibit biological cellular and molecular interactions which are dependent on RXD recognition, wherein X is one of the amino acid residues G, E, Y, A or F. In particular, RGD surrogates are provided having no sequence of α-natural amino acids and comprising a guanidino and a carboxyl terminal groups spaced by a chain of 11 atoms, at least 5 of which are carbon atoms. The compounds inhibit cell adhesion and are useful for the treatment of several pathological disorders, e.g., thrombosis, autoimmune diseases, metastasis, allergy, host-graft reactions and inhibition of scar tissue formation.

公开(公告)号：EP0652863A1

公开(公告)日：1995-05-17

申请号：EP93918388.0

申请日：1993-07-26

Applicant: YEDA RESEARCH AND DEVELOPMENT COMPANY, LTD.

Inventor： LIDER, Ofer ,  GREENSPOON, Noam ,  HERSHKOVIZ, Rami ,  ALON, Ronen

IPC: A61K38 ,  A61K31 ,  A61P29 ,  A61P35 ,  A61P37 ,  A61P43 ,  C07C237 ,  C07C323 ,  C07K5 ,  C07K7

CPC classification number: C07K7/56 ,  A61K38/00 ,  C07C237/22 ,  C07C323/60 ,  C07K5/0202

Abstract: Non-peptidic Leu-Asp-Val (LDV) surrogates of formula (I), wherein X1 to X5 are the same or different C, N, O or S atoms, at least two of them being C, and the X1-X5 chain may be optionally substituted by radicals selected from halogen, hydrocarbyl, oxo, thioxo, amino and carboxyl, or the X1-X5 chain or part thereof may form part of a heterocyclic ring, and pharmaceutically acceptable salts thereof, inhibit cellular or molecular interactions which depend on recognition of the LDV sequence, and are useful for the treatment of inflammation and disorders involving interference with cell-matrix or cell-cell dependent immune processes, such as autoimmune diseases and allergy, and inhibition of tumour progression and metastasis.