Patent
Quinazoline derivatives as medicaments
Sarvajit Chakravarty,Sundeep Dugar,John J. Perumattam,George F. Schreiner,David Y. Liu,John A. Lewicki +5 more
TLDR
In this article, a method to inhibit TGF-β and/or p38-α kinase using compounds of formula (1) or the pharmaceutically acceptable salts thereof was proposed.Abstract:
The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of formula (1) or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar' is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.read more
Citations
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Tyrosine kinase inhibitors
TL;DR: In this article, the imidazo[1,2-a]pyrimidine derivatives are used for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET.
Patent
Pyrazole compounds useful as protein kinase inhititors
David Bebbington,Jean-Damien Charrier,Golec Julian M C,Jeremy Green,David Kay,Ronald Knegtel,Andrew Miller,Ronald Tomlison,Pan Li +8 more
TL;DR: In this article, the pyrazole compounds of formula (IV) were described for protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzehimer's disease.
Patent
Compositions useful as inhibitors of protein kinases
TL;DR: In this article, a compound of formula I: or a pharmaceutically acceptable salt or mixtures thereof is presented. And the authors provide a method of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
Patent
Quinazoline derivatives as angiogenesis inhibitors
Stokes Elaine Sophie Elizabeth,Darren Mckerrecher,Laurent Francois Andre Hennequin,Patrick Ple +3 more
TL;DR: In this paper, the use of compounds of formula (I), wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1-3 heteroatoms selected independently from O, N and S, was discussed.
Patent
c-Met modulators and methods of use
Lynne Canne Bannen,Diva Sze-Ming Chan,Jeff Chen,Lisa Esther Dalrymple,Timothy Patrick Forsyth,Tai Phat Huynh,Vasu Jammalamadaka,Richard George Khoury,James W. Leahy,Morrisson B. Mac,Grace Mann,Larry W. Mann,John M. Nuss,Jason Jevious Parks,Craig Stacy Takeuchi,Yong Wang,Wie Xu +16 more
TL;DR: In this article, the authors provide compounds for modifying protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion.
References
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Journal ArticleDOI
TGF-beta signal transduction.
TL;DR: The transforming growth factor beta (TGF-beta) family of growth factors control the development and homeostasis of most tissues in metazoan organisms and mutations in these pathways are the cause of various forms of human cancer and developmental disorders.
Journal ArticleDOI
The integrin alpha v beta 6 binds and activates latent TGF beta 1: a mechanism for regulating pulmonary inflammation and fibrosis.
John S. Munger,Xiaozhu Huang,Hisaaki Kawakatsu,Mark J. D. Griffiths,Stephen L. Dalton,Jianfeng Wu,Jean-Francois Pittet,Naftali Kaminski,Chrystelle Garat,Michael A. Matthay,Daniel B. Rifkin,Dean Sheppard +11 more
TL;DR: In this article, Latency-Aged Peptide (LAP) was shown to be a ligand for the integrin alpha v beta 6 and that alpha-v beta 6-expressing cells induce spatially restricted activation of TGF beta 1.
Journal ArticleDOI
TGFβ signals through a heteromeric protein kinase receptor complex
Jeffrey L. Wrana,Liliana Attisano,Juan M. Cárcamo,A Zentella,Jacqueline Doody,Marikki Laiho,Xiao-Fan Wang,Joan Massagué +7 more
TL;DR: It is shown that the type II receptor requires both its kinase activity and association with another TGF beta-binding protein, the type I receptor, to signal growth inhibition and early gene responses.
Journal ArticleDOI
Thrombospondin-1 Is a Major Activator of TGF-β1 In Vivo
Susan E. Crawford,Susan E. Crawford,Veronica Stellmach,Joanne E. Murphy-Ullrich,Solange M. F. Ribeiro,Jack Lawler,Richard O. Hynes,Gregory P. Boivin,Noel P. Bouck +8 more
TL;DR: It is shown that thrombospondin-1 is responsible for a significant proportion of the activation of TGF-beta1 in vivo, and lung and pancreatic abnormalities reverted toward wild type when pups were treated with a peptide derived from thromBospondIn1 that could activate T GF- beta1.