Assignee: Rigel Pharmaceuticals, Inc.

Location: South San Francisco, CA
No. of patents: 172

Number	Title	Issue Date
8178671	Methods of treating or preventing autoimmune diseases with 2, 4-pyrimidinediamine compounds The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases tha...	05/15/2012
8168636	Polycyclic heteroaryl substituted triazoles useful as Axl inhibitors Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditio...	05/01/2012
8163902	Prodrugs of 2,4-pyrimidinediamine compounds and their uses The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a ...	04/24/2012
8158621	Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases tha...	04/17/2012
8148525	2,4-pyrimidinediamine compounds and their uses The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a...	04/03/2012
8129390	Carboxamide, sulfonamide and amine compounds and methods for using the same Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, ...	03/06/2012
8119809	AMPK-activating heterocycloalkyloxy(hetero)aryl carboxamide, sulfonamide and amine compounds and methods for using the same Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, ...	02/21/2012
8101627	Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses The present invention provides stereoisomers and stereoisomeric mixtures of 3-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular...	01/24/2012
8097630	Pinane-substituted pyrimidinediamine derivatives useful as Axl inhibitors Pinane-substituted pyrimidinediamine derivatives and pharmaceutical compositions containing the derivatives are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the derivatives in treating diseases or...	01/17/2012
8053434	Kinase inhibitors and their uses The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropria...	11/08/2011
8044054	Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses The present invention provides stereoisomers and stereoisomeric mixtures of 3-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular...	10/25/2011
8032346	System and method for high-content oncology assay The present invention provides an apparatus, system, method and computer program and computer program product for analyzing cellular samples. One embodiment of the apparatus and method provides a multiparameter assay that provides information with respect to cell pr...	10/04/2011
8030483	Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses The present invention provides stereoisomers and stereoisomeric mixtures of 3-amino carbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellula...	10/04/2011
8012965	Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseas...	09/06/2011
8012955	N-substituted-heterocycloalkyloxybenzamide compounds and methods of use The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R	09/06/2011
8008501	Quinoline compounds and their uses The present invention provides quinoline compounds that inhibit the IgE receptor signaling cascade that leads to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, i...	08/30/2011
7989448	Prodrugs of 2,4-pyrimidinediamine compounds and their uses The present disclosure provides compounds of the following formula, and methods of using the compounds to inhibit cellular degranulation and to treat diseases associated therewith. ...	08/02/2011
7962290	Identification of pharmacophores from co-crystals of spleen tyrosine kinase (SYK) and SYK ligands The invention comprises for methods of identifying pharmacophores based on the spleen tyrosine kinase (SYK) protein or fragment thereof. The invention further provides methods of identifying SYK inhibitors using pharmacophores that are identified from co-crystals of...	06/14/2011
7947698	Compositions and methods for inhibition of the JAK pathway The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful. ...	05/24/2011
7935693	Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as Axl inhibitors Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating ...	05/03/2011
7915293	Ubiquitin ligase inhibitors This invention describes compounds useful as ubiquitin ligase inhibitors. The compounds of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. The invention also provides for pharmaceutical composition...	03/29/2011
7915273	Compositions and methods for inhibition of the JAK pathway The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful. ...	03/29/2011
7906644	2,4-pyrimidinediamine compounds and their uses The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a...	03/15/2011
7884119	Triazole derivatives useful as Axl inhibitors Triazole derivatives and pharmaceutical compositions containing the derivatives are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the derivatives in treating diseases or conditions associated with ...	02/08/2011
7884111	2,4-pyrimidinediamine compounds and uses as anti-proliferative agents The present invention provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferative diseases such as tumorigenic cance...	02/08/2011
7879856	Diaminothiazoles useful as Axl inhibitors Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activi...	02/01/2011
7872096	Methods for cyclizing synthetic polymers The invention provides methods and compositions for production of a cyclic polymer in a cell free system. In general, the methods of the invention involve ligating first and second recombinant intein domains to a linear synthetic polymer to form a compound containin...	01/18/2011
7872000	Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as Axl inhibitors Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in t...	01/18/2011
7868013	Cycloalkyl substituted pyrimidinediamine compounds and their uses The present disclosure provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancer...	01/11/2011
7863286	Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses The present invention provides stereoisomers and stereoisomeric mixtures of 3-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular...	01/04/2011
7863222	shRNA library As noted above, certain aspects of this disclosure relate to a library of nucleic acid vectors, as well as a method for making the same. In certain embodiments, the library of nucleic acid vectors comprises: a plurality of nucleic acid molecules of the following for...	01/04/2011
7858633	Cycloalkyl substituted pyrimidinediamine compounds and their uses The present disclosure provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancer...	12/28/2010
7851480	Spiro 2,4-pyrimidinediamine compounds and their uses The present invention provides methods of treating or preventing autoimmune diseases with spiro 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseas...	12/14/2010
7834024	Compositions and methods for inhibition of the JAK pathway The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful. ...	11/16/2010
7825116	N2, N4-bis-aryl-5-fluoro-2,4-pyrimidinediamines The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases tha...	11/02/2010
7820819	2,4-pyrimidinediamine compounds and their uses The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a...	10/26/2010
7812029	Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases tha...	10/12/2010
7803939	2,4-pyrimidinediamine compounds and their uses The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a...	09/28/2010
7781182	Ubiquitin ligase assay The invention relates to assays for measuring ubiquitin ligase activity and for identifying modulators of ubiquitin ligase enzymes. ...	08/24/2010
7776847	Benzisothiazoles useful for treating or preventing HCV infection The present invention relates to benzisothiazoles and pharmaceutical compositions thereof that inhibit replication and/or proliferation of HCV virus. The present invention also relates to the use of the benzisothiazoles and pharmaceutical compositions comprising the...	08/17/2010

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Assignee: Rigel Pharmaceuticals, Inc.