Patent
Substituted beta-alanine derivatives as cell adhesion inhibitors
Philippe L. Durette,William K. Hagmann,Ihor E. Kopka,Malcolm MacCoss,Sander G. Mills,Richard A. Mumford,Plato A. Magriotis +6 more
TLDR
The β-Alanine derivatives of formula (I) are antagonists of VLA-4 and/or α4β7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies as discussed by the authors.Abstract:
β-Alanine derivatives of formula (I) are antagonists of VLA-4 and/or α4β7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.read more
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Human serum albumin linkers and conjugates thereof
TL;DR: In this article, a human serum albumin (HSA) linker and HSA linker with binding, diagnostic, and therapeutic agents conjugated thereto is presented, which is useful in reducing tumor cell proliferation, e.g., for therapeutic therapeutic applications.
Patent
Compounds, pharmaceutical compositions and methods for use in treating metabolic disorders
Michelle Akerman,Jonathan B. Houze,Daniel C.-H. Lin,Jiwen Liu,Jian Luo,Julio C. Medina,Wei Qiu,Reagan Jeffrey D,Michael J. Schmitt,Yingcai Wang,Rajiv Sharma,Stephen J. Shuttleworth,Ying Sun,Jian Zhang,Liusheng Zhu,Zhihua Ma,Jinqian Liu +16 more
TL;DR: In this article, the authors present compounds useful for modulating insulin levels in a subject and that have the general formula Q-L1-P-L2-M-X-L3-A wherein the definitions of the variables Q, L1, P, L2, M, X, L3 and A are provided.
Patent
Conformationally constrained 3-(4-hydroxy-phenyl)-substituted-propanoic acids useful for treating metabolic disorders
Michelle Akerman,Sean P. Brown,Jonathan B. Houze,Jinqian Liu,Jiwen Liu,Zhihua Ma,Julio C. Medina,Wei Qiu,Michael J. Schmitt,Rajiv Sharma,Yingcai Wang,Liusheng Zhu +11 more
TL;DR: In this paper, the general formula I: (F) where the definitions of the variables Q, L1,,, L2, M, X, L3, and A are provided.
Patent
Non-peptidyl inhibitors of VLA-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases
TL;DR: In this paper, partial Formula (1.0.1.2) and partial Formula 1.9.0) are described, wherein A is for example aryl, heteroaryl or heterocyclyl, Y is preferably -C(C(=O)-; B is independently selected from a group of moieties, the most preferred of which are those of partial formulas, and E is a single bond; oxygen; 1,1-cyclopropyl; C(CH3)2; CF2; or a bridging moiety of partial
Patent
Bicyclic carboxylic acid derivatives useful for treating metabolic disorders
Rajiv Sharma,Michelle Akerman,Mario G. Cardozo,Jonathan B. Houze,An-Rong Li,Jinqian Liu,Jiwen Liu,Zhihua Ma,Julio C. Medina,Michael J. Schmitt,Ying Sun,Yingcai Wang,Zhongyu Wang,Liusheng Zhu +13 more
TL;DR: In this paper, compositions and methods for using the compounds for preparing medicaments and for treating metabolic disorders such as, for instance, type II diabetes are disclosed, where the variables are provided herein.
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Patent
Inhibitors of interleukin-1β converting enzyme
Guy W. Bemis,Golec Julian M C,Lauffer David J,Mullican Michael D,Murcko Mark A,David J. Livingston +5 more
TL;DR: In this paper, a class of compounds which are inhibitors of interleukin-1β converting enzyme (ICE) are described and compared with specific structural and physicochemical features.
Patent
Cell adhesion inhibitors
Steven P. Adams,Ko-Chung Lin,Wen-Cherng Lee,Castro Alfredo C,Zimmerman Craig N,Hammond Charles E,Yu-Sheng Liao,Cuervo Julio Hernan,Juswinder Singh +8 more
TL;DR: In this article, the authors present novel compounds that are useful for inhibition and prevention of cell adhesion and cell-adhesion-mediated pathologies, which are particularly well-suited for treatment of many inflammatory and autoimmune diseases.
Patent
CS-1 peptidomimetics, compositions and methods of using the same
TL;DR: In this article, a cyclic peptide that inhibits the binding between the VLA-4 receptor expressed on inflammatory leukocytes and the fibronectin CS-1 peptide expressed on endothelial cells that are involved in immunoinflammatory disease states was proposed.
Patent
Heterocyclic amide compounds as cell adhesion inhibitors
Philippe L. Durette,William K. Hagmann,Malcolm MacCoss,Sander G. Mills,Richard A. Mumford,Gail Van Riper,Jack A. Schmidt,Nancy J. Kevin +7 more
TL;DR: In this paper, compounds of formula (I) are formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
Patent
Process to inhibit binding of the integrin α4 62 1 to VCAM-1 or fibronectin and linear peptides therefor
TL;DR: In this paper, an isolated and purified cyclic peptide of from 5 to about 13 residues modeled after a portion of the CS1 peptide was used to selectively inhibit the binding of α4 β 1 integrin to a protein such as VCAM-1, fibronectin or invasin.