Ontogen Corporation

Other

Adnan M Mjalli

Sepehr Sarshar

Xiaodong Cao

Farid Bakir

Chengzhi Zhang

Sepehar Sarshar

Todd Kevin Jones

Edmund J Moran

Kristen Lee Arienti

Kevin Michael Short

Rachel Denise Kimmich

James Christopher Mason

Protein tyrosine phosphatase-inhibiting compounds

The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganism, eukaryoic cells, whole animals and human being. R' and R' are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'' is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.

Modulators of proteins with phosphotyrosine recognition units

A solid support template for solid phase synthesis of amino group containing compounds is provided that comprises amino-ketone core compounds of the general formula:

Amino-ketone solid support templates

Compounds of formula A are disclosed: ##STR1## wherein R.sup.1 is aralkyl or cycloalkyl; R.sup.2 is cycloalkylmethyl, alkyl, or aralkyl;

Piperazines as inhibitors of fructose-1,6-bisphosphatase (FBPase)

There are disclosed methods useful for the inhibition of inducible nitric oxide synthase by the adminstration of a compound of the formula I:. when R.sub.2 is H then R.sub.1 is selected from the group consisting of:

Naphthalenedione nitric oxide synthase (NOS) inhibitors

The present invention relates to polysubsituted imidazole having formula 1 ##STR1## These compounds are useful for restoring the sensitivity of multidrug resistant cells to cancer chemotherapeutic agents.

Imidazole derivatives as MDR modulators

The present invention provides novel protein tyrosine phosphatase modulating compounds having an aryl acrylic acid structure, compositions comprising the compounds, and methods of making and using the same.

Aryl acrylic acid derivatives useful as protein tyrosine phosphatase

The present invention relates to imidazole derivatives having formula 1 ##STR1## wherein: R.sub.1 is selected from the group consisting of: mono-,di-,and tri-substituted phenyl or thienyl, the substituents are selected from the group consisting of:

Imidazole derivatives useful as modulators of multi drug resistances

Modulators of proteins with phosphotryrosine recognition units

There are disclosed methods useful for the inhibition of inducible nitric oxide synthase by the adminstration of a compound of the Formula I: ##STR1## to a patient in need of such inhibition such as hypotension, inflammation, autoimmune diseases and septic shock and the like.

Nitric oxide synthase (NOS) inhibitors

This invention relates to compounds of Formula 1 which are pharmacologically useful for the treatment of cancer through sensitization of multi-drug resistant cancer cells to chemotherapeutic agents. ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are, respectively hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, substituted aryl.

Growing community of inventors

Louisville, KY, United States of America

Adnan M Mjalli