Assignee: ArQule, Inc.

Location: Woburn, MA
No. of patents: 34

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Number	Title	Issue Date
8178672	Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 MAP kinase An efficient route for the synthesis is of formula (I) of imidazooxazole and imidazothiazole inhibitors of the p38 MAP kinase pathway, useful as therapeutics for disease conditions including inflammation and auto-immune responses is described. ...	05/15/2012
8173808	Substituted naphthalenyl-pyrimidine compounds The present invention relates to substituted naphthalenyl-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted naphthalenyl-pyrimidine compounds and methods of trea...	05/08/2012
8114873	1,4-disubstituted naphthalenes as inhibitors of p38 map kinase Naphthalene-based compounds having linked heterocyclic and aromatic rings capable of inhibiting P38, methods for inhibiting P38 in vivo or in vitro, diagnostics for determining activity in the treatment of P38 and/or cytokine-associated conditions and methods for tr...	02/14/2012
8067459	Lapachone compounds and methods of use thereof The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment ...	11/29/2011
8049005	Substituted tetrahydropyrazolo-pyrido-azepine compounds The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds...	11/01/2011
8039503	Lapachone compounds and methods of use thereof The present invention provides novel tricyclic spiro-oxathiine naphthoquinone derivatives, a synthetic method for making the derivatives, and the use of the derivatives to induce cell death and/or to inhibit proliferation of cancer or precancerous cells. The naphtho...	10/18/2011
7960158	Kinase inhibition models and their uses The present invention provides a c-Met inhibition model. The invention further provides a method to derive inhibition models for other kinases. The kinase inhibition models of the present invention can be used to design or screen for inhibitors for kinases. ...	06/14/2011
7960134	Kinase inhibition models and their uses The present invention provides a c-Met inhibition model. The invention further provides a method to derive inhibition models for other kinases. The kinase inhibition models of the present invention can be used to design or screen for inhibitors for kinases. ...	06/14/2011
7932279	Substituted tetrazole compounds and uses thereof The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole compounds. The present invention provides methods of treating a cell prolife...	04/26/2011
7902354	Lapachone compounds and methods of use thereof The present invention provides novel tricyclic spiro-oxathiine naphthoquinone derivatives, a synthetic method for making the derivatives, and the use of the derivatives to induce cell death and/or to inhibit proliferation of cancer or precancerous cells. The naphtho...	03/08/2011
7902192	Inhibitors of P38 and methods of using the same In general, the present invention relates to compounds capable of inhibiting p38, methods for inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or cytokine activity. ...	03/08/2011
7842718	Heterocyclic sulfonamide inhibitors of beta amyloid production Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt...	11/30/2010
7829560	1,4-disubstituted naphthalenes as inhibitors of P38 MAP kinase 1,4 disubstituted napthylenes, of formula (I), are disclosed. These compounds may be useful in treating cell-proliferative diseases. ...	11/09/2010
7812051	Pharmaceutical compositions of β-lapachone and β-lapachone analogs with improved tumor targeting potential The present invention relates to polymer-modified quinone-containing and carbonyl-containing therapeutic agents, including polymer-modified β-lapachone compounds, and methods of treating cancer by administering the polymer-modified therapeutic agents to a subject. ...	10/12/2010
7790765	Hydroxy sulfonate of quinone compounds and their uses The present invention provides sodium 6-hydroxy-2,2-dimethyl-5-oxo-3,4,5,6-tetrahydro-2H-benzo(h)chromene-6-sulfonate, and its synthesis and uses in the treatment of cancer. ...	09/07/2010
7713969	Compositions and methods for treatment of cancer The present invention relates to pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrroloq...	05/11/2010
7691884	Heterocyclic sulfonamide inhibitors of β amyloid production Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt...	04/06/2010
7671075	Substituted phenylsulfonamide inhibitors of beta amyloid production Compounds of Formula I, wherein R1-R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibit...	03/02/2010
7649013	Methods of protecting against radiation injury Administration of a modulator of cell cycle checkpoint activation, which is preferably β-lapachone, or a pharmaceutically acceptable salt, prodrug, metabolite, analog or derivative thereof, protects normal cells against radiation injury. The invention includes meth...	01/19/2010
7501430	RAF inhibitors and their uses The present invention provides imidazooxazole and imidazothiazole compounds and their synthesis. The compounds of the present invention are capable of inhibiting the activity of RAF kinase, such as B-RAFV600E. The compounds are useful for the treatment of...	03/10/2009
7361691	Method of treating cancers using β-lapachone or analogs or derivatives thereof Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint activator, which is preferably β-lapachone, or a derivative or analog thereof, combined with an oncogenic kinase modulator, preferably imatinib. This combination of the cell cyc...	04/22/2008
7307079	1,3,5-Triazine derivatives as ligands for human adenosine-A3 receptors The invention relates to a group of novel triazine derivatives which are ligands for human adenosine-A3 receptors, as well as to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingre...	12/11/2007
7166622	Substituted phenylsulfonamide inhibitors of beta amyloid production Compounds of Formula I, wherein R1–R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs ther...	01/23/2007
7074824	Pharmaceutical compositions containing beta-lapachone, or derivatives or analogs thereof, and methods of using same Beta-lapachone, which is poorly soluble in most pharmaceutically acceptable solvents, has demonstrated significant antineoplastic activity against human cancer lines. The present invention overcomes this significant limitation by teaching novel pharmaceutical compos...	07/11/2006
7034110	Method of identifying chemical compounds having selected properties for a particular application A method for obtaining compounds having selected properties for a particular application by forming base modules having at least two structural diversity elements from the reaction of a first compound having at least one structural diversity element and a first reac...	04/25/2006
6962944	Pharmaceutical compositions containing beta-lapachone, or derivatives or analogs thereof, and methods of using same Beta-lapachone, which is poorly soluble in most pharmaceutically acceptable solvents, has demonstrated significant antineoplastic activity against human cancer lines. The present invention overcomes this significant limitation by teaching novel pharmaceutical compos...	11/08/2005
6878742	Heterocyclic sulfonamide inhibitors of beta amyloid production Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable...	04/12/2005
6878557	Logically ordered arrays of compounds and methods of making and using the same A method for constructing an array of synthetic molecular constructs, by forming a plurality of molecular constructs having a scaffold backbone of a chemical molecule comprising a linear, branched or cyclic organic compound having at least atoms of carbon, nitrogen,...	04/12/2005
6753449	Cleavable linker for solid phase synthesis Cleavable alkene-containing linkers and supports useful for the solid phase synthesis of chemical compounds, and combinatorial libraries of compounds, are disclosed. Also disclosed are methods of making and using the linkers and supports. ...	06/22/2004
6497820	Rapid method for separation of small molecules using reverse phase high performance liquid chromatography Disclosed is a rapid method for the separation of small organic compounds using gradient reverse phase HPLC. The method achieves a run time of one minute or less and a resolution with a peak production of at least 1 peak/2 seconds. The method is also able...	12/24/2002
6452050	Synthesis and use of ଱-ketoamide derivatives and arrays The invention is based on new methods for making and using compounds and arrays of novel ଱-ketoamides, and the arrays and compounds made by these methods. These novel compounds are potential inhibitors of proteolytic enzymes, particularly cysteine p...	09/17/2002
6358750	Spiro[pyrrolidine-2,3'-oxindole] compounds and method of use The invention provides spiro[pyrrolidine-2,3'-oxindole] compounds and libraries of these compounds produced by the stereo- and regio-selective reaction of variously substituted isatins, ଱-amino acids, and dipolarophiles (e.g., trans-chalcones, acryl...	03/19/2002
6271195	Aminimide-containing molecules and materials as molecular recognition agents The design and synthesis of novel aminimide-based molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful i...	08/07/2001
6114540	Spiro[pyrrolidine-2,3'-oxindole] compounds and methods of use The invention provides spiro[pyrrolidine-2,3'-oxindole] compounds produced by the stereo- and regio-selective reaction of variously substituted isatins, ଱-amino acids, and dipolarophiles (e.g., trans-chalcones, acrylate esters, or vinyl oxindoles)....	09/05/2000

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Assignee: ArQule, Inc.