Abstract: 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.
Abstract: The present invention provides labeled synthetic libraries of random oligomers and methods and apparatus for generating labeled synthetic oligomer libraries. Each member of such a library is labeled with a unique identifier tag that specifies the structure or sequence of the oligomer. In a preferred embodiment of the present invention the identifier tag is a microchip that is pre-encoded or encodable with information that is related back to a detector when the identifier tag is pulsed with electromagnetic radiation.
Abstract: 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.
Type:
Grant
Filed:
October 16, 1995
Date of Patent:
June 23, 1998
Assignee:
Ontogen Corporation
Inventors:
Adnan M. M. Mjalli, Xiaodong Cao, Edmund J. Moran
Abstract: Methods and apparatus for the generation of chemical libraries are described. The preferred embodiments include a reaction block which uses replaceable reaction chambers supported in the block. Each reaction block is fitted with four sets of 12 reaction chambers, and has fittings that facilitate robotic manipulation. The reaction chambers are preferably fitted with a frit. An s-shaped trap tube snaps into a fitting on the bottom of each reaction chamber. The trap tube runs into a drain tube. The reaction block is fitted with gas (preferably N.sub.2) lines and a septum seal such that gas pressurization empties the reaction chambers into the drain tubes. The drain tubes are arranged so as to mate directly with a standard 96 well microtiter plate for the collection of material. A docking station provides for secure registration of the reaction blocks, and provides for introduction of gases and liquids into the reaction blocks.
Abstract: 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:(i) substituted C.sub.1-6 alkyl, substituted C.sub.2-6 alkyloxy, wherein the substituents are selected from the group consisting of hydrogen or C.sub.1-6 alkoxy;(ii) C.sub.1-11 CO.sub.2 R.sub.5, trans-CH.dbd.CHCO.sub.2 R.sub.5, wherein R.sub.5 is C.sub.1-11 alkyl, or phenyl C.sub.1-11 alkyl;R.sub.2 and R.sub.3 are mono-, di, and tri-substituted phenyl wherein the substituents are independently selected from:(i) halo;(ii) C.sub.1-6 alkyl-amino, or di(C.sub.1-6 alkyl)amino, and R.sub.4 is hydrogen.These compounds are useful for restoring the sensitivity of multidrug resistant cells to cancer chemotherapeutic agents.
Abstract: Y--X--C(R').dbd.C(R")COOR'" (A1)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, microorganisms, eukaryoic cells, whole animals and human beings. 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.
Abstract: 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.
Type:
Grant
Filed:
August 9, 1996
Date of Patent:
March 3, 1998
Assignee:
Ontogen Corporation
Inventors:
Adnan M. M. Mjalli, Sepehar Sarshar, Chengzhi Zhang
Abstract: 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.
Abstract: Methods and apparatus for the generation of chemical libraries are described. The preferred embodiments include a reaction block which uses replaceable reaction chambers supported in the block. Each reaction block is fitted with four sets of 12 reaction chambers, and has fittings that facilitate robotic manipulation. The reaction chambers are preferably fitted with a frit. An s-shaped trap tube snaps into a fitting on the bottom of each reaction chamber. The trap tube runs into a drain tube. The reaction block is fitted with gas (preferably N.sub.2) lines and a septum seal such that gas pressurization empties the reaction chambers into the drain tubes. The drain tubes are arranged so as to mate directly with a standard 96 well microtiter plate for the collection of material. A docking station provides for secure registration of the reaction blocks, and provides for introduction of gases and liquids into the reaction blocks.