Patentscope RSS feed

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

>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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
>> Read More

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.
>> Read More

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.
>> Read More

PHARMACEUTICAL COMPOSITIONS CONTAINING PENTAFLUOROBENZENESULFONAMIDE DERIVATIVES AND NOVEL PENTAFLUOROBENZENESULFONAMIDE DERIVATIVES (Sun, 20 Aug 2006)

>> Read More

ARYLSULFONANILIDE UREA DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME (Wed, 05 Jul 2006)

>> Read More

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.
>> Read More

CXCR3 antagonists (Fri, 28 Jul 2006)
Patent 526622 Disclosed are compounds of formula (I), wherein: A4 is N, X is -C(O)-, -CH2- or a bond, R1 and R2 are independently H or alkyl, R3 is hydroxyl, alkoxy, amino, alkylamino, dialkylamino, heteroalkyl, heterocyclyl, acylamino, amidino, guanidine, ureido, cyano, heteroaryl, -CONR9R10 or -CO2R11, R4 is alkyl, heteroalkyl, heteroaryl, aryl, heteroarylalkyl, heteroarylheteroalkyl, arylalkyl or arylheteroalkyl, R14 is optionally substituted aryl or heteroaryl, Q is -C(O)-, and L is alkylene. The compounds are used for the manufacture of medicaments for the treatment of inflammatory or immune conditions.
>> Read More

CXCR3 antagonists (Thu, 19 Dec 2002)
Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.
>> Read More

THERAPEUTIC MODULATION OF PPAR (GAMMA) ACTIVITY (Thu, 22 Sep 2005)
Modulators of PPAR.gamma. activity are used in methods of treating and/or preventing conditions such as osteoporosis, Alzheimer's disease, psoriasis and acne, and cancer.
>> Read More

Bicyclic sulfonamide compounds as sodium channel inhibitors (Thu, 18 Dec 2014)
The present invention provides compounds of Formula I, embedded image and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.
>> Read More

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.
>> Read More

Substituted pyrido[2,3-d]pyrimidines and methods for their use (Thu, 14 Nov 2002)
Compounds having the formula: embedded image wherein A4 is N and X is —C(O)— or —CH2—, are provided, which are useful as modulators of a chemokine receptor and for treatment of inflammatory and immunoregulatory disorders and diseases. Pharmaceutical compositions and methods of using these compounds for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes, are also provided.
>> Read More

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.
>> Read More