PATENTSCOPE: EN_ALL:nmr AND PA:amgen

BISAMIDE SARCOMERE ACTIVATING COMPOUNDS AND USES THEREOF (Fri, 22 Mar 2019)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
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INHIBITORS OF KRAS G12C AND METHODS OF USING THE SAME (Fri, 15 Mar 2019)
Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
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MACROCYCLIC COMPOUNDS THAT INHIBIT MCL-1 PROTEIN (Fri, 08 Mar 2019)
Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
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COMPOUNDS THAT INHIBIT MCL-1 PROTEIN (Fri, 22 Feb 2019)
Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
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KRAS G12C INHIBITORS AND METHODS OF USING THE SAME (Fri, 30 Nov 2018)
Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
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PHARMACEUTICAL COMPOSITION COMPRISING BISPECIFIC ANTIBODY CONSTRUCTS FOR IMPROVED STORAGE AND ADMINISTRATION (Fri, 09 Nov 2018)
The present invention provides an improved pharmaceutical composition for storage and administration comprising (a) a bispecific antibody construct comprising a first domain binding to a target cell surface antigen and a second domain binding to a second antigen, wherein the bispecific antibody construct is present at a concentration in the range from about 0.5 μg/ml to 20 mg/ml, (b) a preservative at a concentration effective to inhibit the growth of microbes, and (c) a diluent wherein bispecific antibody construct is stable and recoverable.
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COMPOUNDS THAT INHIBIT MCL-1 PROTEIN (Fri, 05 Oct 2018)
Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (I), or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
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METHODS DIRECTED TO CRYSTALLINE BIOMOLECULES (Fri, 21 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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LOW PH PHARMACEUTICAL COMPOSITION COMPRISING T CELL ENGAGING ANTIBODY CONSTRUCTS (Fri, 10 Aug 2018)
The present disclosure provides a low pH pharmaceutical composition comprising (a) an antibody constructs comprising a first domain binding to a target cell surface antigen, a second domain binding to a second antigen and preferably a third domain, which is a specific Fc modality, (b) at least one buffer agent, (c) at least one saccharide, and (d) at least one surfactant; and wherein the pH of the pharmaceutical composition is in the range of 3.5 to 6.
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BENZISOTHIAZOLE, ISOTHIAZOLO[3,4-B]PYRIDINE, QUINAZOLINE, PHTHALAZINE, PYRIDO[2,3-D]PYRIDAZINE AND PYRIDO[2,3-D]PYRIMIDINE DERIVATIVES AS KRAS G12C INHIBITORS FOR TREATING LUNG, PANCREATIC OR COLORECTAL CANCER (Fri, 29 Jun 2018)
Provided herein are benzisothiazol, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives and related compounds as KRAS G12C inhibitors for treating e.g. lung cancer, pancreatic cancer or colorectal cancer.
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BICYCLIC THIAZINE AND OXAZINE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE (Fri, 22 Jun 2018)
The present disclosure provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I): (Formula (I)) wherein variables X, Y, R2, R3, R4, R5, R6, and n of Formula (I) are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ 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, and other central nervous system conditions.
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GASTRO-RETENTIVE MODIFIED RELEASE DOSAGE FORMS FOR OPROZOMIB AND PROCESS TO MAKE THEREOF (Fri, 22 Jun 2018)
This disclosure features gastro-retentive (GR) modified release pharmaceutical dosage forms (e.g., solid dosage forms, e.g., tablets, e.g., bilayer tablets) that are useful for the oral administration of oprozomib, or a pharmaceutically acceptable salt thereof, to a human or animal subject as well as methods of making and using the dosage forms.
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THIAZINE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE (Fri, 22 Jun 2018)
The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: (see Formula I structure) wherein variables R1, R1', R2, R2', R3, R4, R5, R6, R7, and b of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ 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, and other central nervous system conditions.
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OXAZINE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE (Fri, 22 Jun 2018)
The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: (insert Formula I structure) wherein variables W, X, Y, R2, R2', R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to beta amyloid (Aβ) 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, and other central nervous system conditions.
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1,4-THIAZINE DIOXIDE AND 1,2,4-THIADIAZINE DIOXIDE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE (Fri, 22 Jun 2018)
The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R2, R2', R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ 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, and other central nervous system conditions.
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CYCLOPROPYL FUSED THIAZINE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE (Fri, 22 Jun 2018)
The present disclosure 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 A, R1, R2, R2', R3, R4, and R5 of Formula (I) are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ 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, and other central nervous system conditions.
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HETEROARYL-SUBSTITUTED TRIAZOLES AS APJ RECEPTOR AGONISTS (Fri, 01 Jun 2018)
Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
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TRIAZOLE FURAN COMPOUNDS AS AGONISTS OF THE APJ RECEPTOR (Fri, 01 Jun 2018)
Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula (I) and Formula (II) have the following structures: (I); (II). Intermediates (V) are also claimed.
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ALKYL SUBSTITUTED TRIAZOLE COMPOUNDS AS AGONISTS OF THE APJ RECEPTOR (Fri, 25 May 2018)
Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: (I), (II) where the definitions of the variables are provided herein.
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TRIAZOLE PYRIDYL COMPOUNDS AS AGONISTS OF THE APJ RECEPTOR (Fri, 25 May 2018)
Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the structures where the definitions of the variables are provided herein.
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