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N-(PURIN-6-YL)-(2-PYRIDINYL-QUINOLIN-3-YL)-METHANEAMINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM (Mon, 17 May 2010)

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Methods directed to crystalline biomolecules (Thu, 20 Sep 2018)
Disclosed herein are methods of preparing a composition comprising crystalline biomolecules, for example, crystalline antibodies. In exemplary embodiments, the method comprises forming a fluidized bed of crystalline biomolecules using, for example, a counter-flow centrifuge to exchange buffer and/or to concentrate the crystalline biomolecules in a solution. Also provided are methods of detecting crystalline biomolecules and/or amorphous biomolecules in a sample.
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METHODS DIRECTED TO CRYSTALLINE BIOMOLECULES (Thu, 20 Sep 2018)
Disclosed herein are methods of preparing a composition comprising crystalline biomolecules, for example, crystalline antibodies. In exemplary embodiments, the method comprises forming a fluidized bed of crystalline biomolecules using, for example, a counter-flow centrifuge to exchange buffer and/or to concentrate the crystalline biomolecules in a solution. Also provided are methods of detecting crystalline biomolecules and/or amorphous biomolecules in a sample.
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HYDRATE, CRYSTALLINE HYDRATE AND CRYSTALLINE ANHYDRATE FORMS OF N-((1S)-1-(7-FLUORO-2-(2-PYRIDINYL)-3-QUINOLINYL)ETHYL)-9H-PURIN-6-AMINE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND METHODS FOR TREATING CANCER. (Thu, 12 Nov 2015)
Provided herein are novel hydrate and anhydrate forms of N-((1S)-1-(7-fluoro-2-(2-pyridinyl)-3-quinolinyl)ethyl)-9H-purin-6-amine. Also provided herein are pharmaceutical compositions containing the forms, and methods for using such compositions for treating cancer.
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Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use (Thu, 18 Feb 2016)
The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: embedded image wherein variables A4, A5, A6, A8, and each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
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Heterocyclic compounds as MDM2 inhibitors for the treatment of cancer (Thu, 21 Aug 2014)
The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, embedded image wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
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Piperidinone derivatives as MDM2 inhibitors for the treatment of cancer (Thu, 19 May 2016)
The present invention provides MDM2 inhibitor compounds of Formula I, embedded image wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
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Polymorphic forms and co-crystals of a c-Met inhibitor (Thu, 02 Feb 2017)
Provided herein are novel polymorphic forms and co-crystals of a compound useful in the treatment, prevention, or amelioration of cancer. In particular, the invention provides polymorphs and co-crystals of 6-{(1R)-1-[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl}-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one, which is an inhibitor of c-Met.
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PHARMACEUTICAL COMPOSITIONS CONTAINING PENTAFLUOROBENZENESULFONAMIDE DERIVATIVES AND NOVEL PENTAFLUOROBENZENESULFONAMIDE DERIVATIVES (Sun, 20 Aug 2006)

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Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use (Thu, 17 Sep 2015)
The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II. embedded image
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ARYLSULFONANILIDE UREA DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME (Wed, 05 Jul 2006)

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Processes of making and crystalline forms of a MDM2 inhibitor (Thu, 11 Dec 2014)
The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.
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Quinolinyl and benzothiazolyl modulators (Thu, 03 Sep 2009)
Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPARγ. In particular, the compounds of the invention modulate the function of PPARγ. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.
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QUINOLONE BASED COMPOUNDS EXHIBITING PROLYL HYDROXYLASE INHIBITORY ACTIVITY, COMPOSITIONS AND USES THEREOF (Wed, 27 Aug 2008)
This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.
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Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, and compositions, and uses thereof (Thu, 23 Sep 2010)
This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.
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QUINOLONE BASED COMPOUNDS EXHIBITING PROLYL HYDROXYLASE INHIBITORY ACTIVITY, AND COMPOSITIONS, AND USES THEREOF (Thu, 21 Jun 2007)
This invention relates to new quinolone based compounds of Formula I (see formula I) that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIP levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.
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ALKYNYL ALCOHOLS AS KINASE INHIBITORS (Thu, 14 Apr 2011)
Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.
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ALKYNYL ALCOHOLS AS KINASE INHIBITORS (Wed, 30 Dec 2009)
Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.
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Alkynyl alcohols as kinase inhibitors (Thu, 13 Jan 2011)
Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.
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Antibacterial agents (Thu, 25 Nov 2004)
Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.
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