PATENTSCOPE: EN_ALL:nmr AND PA:celgene

PROCESSES FOR THE PREPARATION OF CIS-4 [2-{(3S.4R)-3-FLUOROOXAN-4-YL]AMINO)-8-(2,4,6-TRICHLOROANILINO)-9H-PURIN-9-YL]-1-METHYLCYCLOHEXANE-1-C ARBOXAMIDE (Fri, 12 Apr 2019)
Provided herein are processes for the preparation of cis-4-[2-{[(3S,4R) -3-fluorooxan-4-yl]amino} -8-(2,4,6-trichloroanilino)-9H-purin-9- yl]-l -methylcyclohexane-1 - carboxamide, alternatively named (ls,4s)-4-(2-(((3S,4R)-3-fluorotetrahydro-2H-pyran-4-yl)amino)-8- ((2,4,6-trichlorophenyl)amino)-9H-purin-9-yl)-l-methylcyclohexane-l- carboxamide, or a salt, solvate, hydrate, or isotopologue thereof.
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PROCESSES FOR PREPARATION OF (S)-TERT-BUTYL 4,5-DIAMINO-5-OXOPENTANOATE (Fri, 01 Mar 2019)
Provided are processes for the preparation of (S)-tert-butyl 4,5-diamino-5-oxopentanoate, or a salt, solvate, hydrate, enantiomer, mixture of enantiomers, or isotopologue thereof. Also provided are solid forms of various intermediates and products obtained from the processes.
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ANTIPROLIFERATIVE COMPOUNDS AND METHODS OF USE THEREOF (Fri, 18 Jan 2019)
Provided herein is 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile, or an enantiomer, a mixture of enantiomers, a tautomer, or a pharmaceutically acceptable salt thereof, and methods for treating, preventing or managing multiple myeloma using such compounds. Also provided are pharmaceutical compositions comprising the compounds, and methods of use of the compositions.
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COMPOSITIONS AND METHODS OF USE OF 2-(4-CHLOROPHENYL)-N-((2-(2,6-DOXOPIPERIDIN-3-YL)-1-OXOISOINDOLIN-5-YL) METHYL) -2,2-DIFLUOROACETAMIDE (Fri, 04 Jan 2019)
Provided herein are formulations and methods of use of 2-(4-chlorophenyl)-N-((2-(2,6- dioxopiperidin-3-yl)-l-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide or a stereoisomer or mixture of stereoisomers, pharmaceutically acceptable salt, tautomer, prodrug, solvate, hydrate, co-crystal, clathrate, or polymorph thereof.
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SPHINGOSINE 1 PHOSPHATE RECEPTOR AGONISTS FOR NEUROPROTECTION (Fri, 16 Nov 2018)
Methods of treating conditions for which S1P-mediated neuroprotection is medically indicated, comprising administering to a subject in need thereof an agonist of the sphingosine 1-phosphate receptor (S1P receptor); such as a compound having the following structure (See Formula 1): or a pharmaceutically acceptable salt,stereoisomer, homolog, hydrate or solvate thereof.
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NOVEL GLP-1 RECEPTOR MODULATORS (Fri, 02 Nov 2018)
Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as products containing such compounds, and methods of their use and synthesis. Such compounds have the structure of Formula (I) below: (I) or pharmaceutically acceptable salts thereof, wherein A, J, W1, Y, Z, R1, R2, R3 and R4 are as defined herein.
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THERAPEUTIC COMPOUNDS (Fri, 26 Oct 2018)
The present embodiments related to substituted heterocyclic derivative therapeutic compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are use for the treatment of diseases mediated by aberrant cell signalling, such as inflammatory disorders, cancer and neoplastic disease. Particular compounds described herein exhibit selective inhibitory activity against CBP compared with BRD4.
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KDM4 INHIBITORS (Fri, 05 Oct 2018)
The present disclosure relates generally to compounds and methods for inhibiting the enzymatic activity of lysine demethylase 4 (KDM4) and treating cancer. Provided herein are substituted pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibiting lysine demethylase 4. Furthermore, the subject compounds and compositions are useful for the treatment of breast cancer and the like.
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MK2 INHIBITORS, SYNTHESIS THEREOF, AND INTERMEDIATES THERETO (Fri, 21 Sep 2018)
The present invention provides methods of preparing a MK2 inhibitor, and intermediates related thereto.
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9,10,11,12-TETRAHYDRO-8H-[1,4]DIAZEPINO[5',6':4,5]THIENO[3,2-F]QUINOLIN-8-ONE COMPOUNDS AND USES THEREOF (Fri, 21 Sep 2018)
The present invention provides compounds, compositions thereof, and methods of using the same.
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HETEROARYL COMPOUNDS USEFUL AS MK2 INHIBITORS (Fri, 21 Sep 2018)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
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FORMS AND COMPOSITIONS OF A MK2 INHIBITOR (Fri, 21 Sep 2018)
The present invention provides solid forms of an MK2 inhibitor, compositions thereof, and methods of using the same.
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DEUTERATED ANALOGS OF MK2 INHIBITORS AND USES THEREOF (Fri, 21 Sep 2018)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
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SOLID FORMS OF 3-(5-AMINO-2-METHYL-4-OXO-4H-QUINAZOLIN-3-YL)-PIPERIDINE-2,6-DIONE, AND THEIR PHARMACEUTICAL COMPOSITIONS AND USES (Fri, 14 Sep 2018)
Solid forms comprising 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)- piperidine-2,6-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed.
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METHODS FOR MEASURING SMALL MOLECULE AFFINITY TO CEREBLON (Fri, 10 Aug 2018)
A complex comprises a CRBN having a europium-anti-his antibody on the N-terminus of the CRBN, and a Cy5-conjugated small molecule, wherein the Cy5-conjugated small molecule binds the CRBN, and uses thereof for identifying therapeutic compounds.
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METHODS FOR TREATING HEMATOLOGICAL CANCER AND THE USE OF BIOMARKERS AS A PREDICTOR FOR RESPONSIVENESS TO TREATMENT COMPOUNDS (Fri, 10 Aug 2018)
A method for predicting the responsiveness of a patient having a hematological cancer to a treatment compound, comprising obtaining a biological sample from the patient having the hematological cancer; determining the expression level of one, two, three, four, five, or more genes; and comparing the expression level of the one, two, three, four, five, or more genes in the biological sample with a reference expression level of the same genes, wherein the treatment compound is 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)- piperidine-2,6-dione (lenalidomide), 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)- piperidine-2,6-dione (Compound A), or a stereoisomer, pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or a polymorph thereof.
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3-(1-OXO-4-((4-((3-OXOMORPHOLINO) METHYL)BENZYL)OXY)ISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE AND ISOTOPOLOGUES THEREOF (Fri, 03 Aug 2018)
Provided are 4'-arylmethoxy isoindoline compounds, e.g., 3-(l-oxo-4-((4-((3- oxomorpholino)methyl)benzyl)oxy)isoindolin-2-yl)piperidine-2,6-dione, or an isotopologue thereof, or an enantiomer or a mixture of enantiomers thereof. Pharmaceutical compositions comprising and methods for using the compounds are also disclosed.
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BROMODOMAIN AND EXTRA-TERMINAL PROTEIN INHIBITOR COMBINATION THERAPY (Fri, 04 May 2018)
The present disclosure relates generally to compositions and methods of treating neoplastic diseases or cancers, such as glioblastoma and non-Hodgkin's lymphomas, or other cancers in which the subject suffers from an advance solid tumor, comprising a combination of, or administering a combination of, a bromodomain and extra-terminal protein BET inhibitor and at least on echemotherapeutic agent, which does not inhibit BET directly. The BET inhibitor/chemotherapeutic agent combination, or combination therapy, can yield syngergistic effects, thereby increasing the effectiveness of the cancer treatment as compared with the administration of either the BET inhibitor or the chemotherapeutic agent alone.
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BROMODOMAIN INHIBITOR (Fri, 27 Apr 2018)
Described herein is the bromodomain inhibitor 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one, including crystalline forms, amorphous forms, solvates, and hydrates thereof, as well as pharmaceutical compositions that include this bromodomain inhibitor. In some embodiments the pharmaceutical composition comprises 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one that has been processed by micronization or spray dried dispersion. In some embodiments, the pharmaceutical composition further comprises at least one polymer. In some embodiments, the pharmaceutical compositions comprises a solid polymer matrix comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one and at least one polymer. Pharmaceutical compositions comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one are useful for the treatment of cancer or neoplastic disease.
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DIMETHYLAMINOETHANOL SALT OF A GLP-1 RECEPTOR MODULATOR (Fri, 06 Apr 2018)
Crystalline 2-hydroxy-N,N-dimethylethanaminium 1 -(2-(5-(tert-butyl) -thiophene-2-carboxamido)-3-(4-(5-(4'-ethyl-[1,1'-bi(cyclohexan)]-3- en-4-yl)pyrimidin-2-yl)phenyl)propanoyl)azetidine-3-carboxylate salt, and methods related to synthesis and therapeutic use of the same.
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