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Patent # Description
2016/0176893 RAPAMYCIN ANALOGUES AND THEIR PHARMACEUTICAL USE
Novel rapamycin analogues and methods for their production with FKBP and/or MIP inhibitory activity with reduced mTOR inhibitory activity with therapeutic...
2016/0176892 BENZIMIDAZOLE DERIVATIVES AND THEIR PHARMACEUTICAL COMPOSITIONS AND USES
The present invention relates to benzimidazole derivatives and their pharmaceutical compositions and uses, specifically to benzimidazole derivatives of Formula...
2016/0176891 Conformationally Restricted 4-Substituted-2,6-dimethylfuro[2,3-d]pyrimidines as Multi-targeted Receptor...
Compounds of Formula I: ##STR00001## and compounds of Formula II: ##STR00002## are provided. Pharmaceutical compositions comprising either the compound of...
2016/0176890 Oral Pharmaceutical Compositions of Buprenorphine and Another Opioid Receptor Agonist
The present invention is directed to oral pharmaceutical compositions of buprenorphine and it pharmaceutically acceptable salts and the use thereof.
2016/0176889 PROCESS FOR PREPARING OXYCODONE COMPOSITIONS
In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone.
2016/0176888 PROCESS FOR PREPARING OXYCODONE COMPOSITIONS
In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone.
2016/0176887 PROCESS FOR THE PREPARATION OF MORPHINAN-6-ONE COMPOUNDS
A process for preparing a compound of formula (3), includes the steps of: (a) providing an aqueous acidic solution including a compound of formula (1) and, as...
2016/0176886 BACTERIOCHLORIN IMIDES
Compound of Formula I: ##STR00001## are described, along with compositions containing the same and methods of use thereof.
2016/0176885 SUBSTITUTED 1,2,3,4,6,8,12,12a-OCTAHYDRO-1,4-METHANODIPYRIDO[1,2-a:1',2'-d]PYRAZINES AND METHODS FOR...
Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): ##STR00001## ...
2016/0176884 Process for Making Beta 3 Agonists and Intermediates
The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are...
2016/0176883 Forms and salts of a dihydropyrrolo[1,2c]imidazolyl aldosterone synthase or aromatase inhibitor
The invention relates to a phosphate salt or a nitrate salt of 4-(R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl-3-fluoro-benzonitrile, especially in...
2016/0176882 TRIAZOLOPYRIMIDINE COMPOUNDS AND USES THEREOF
A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or...
2016/0176881 SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS
The invention relates to besylate salts of the compound of formula (I): ##STR00001## Methods of preparing the salts, and their use as medicaments, in particular...
2016/0176880 SUBSTITUTED IMIDAZO[1,2-A]PYRAZINECARBOXAMIDES AND USE THEREOF
The present application relates to novel substituted imidazo[1,2-a]pyrazinecarboxamides, to processes for preparation thereof, to the use thereof, alone or in...
2016/0176879 Novel Hydroximic Acid Derivative and Medical Application Thereof
The present invention relates to a kind of new hydroximic acid derivatives, in particular, hydroximic acid derivatives of pyrazolopyrimidine and their medical...
2016/0176878 NOVEL PREPARATION OF TETRANITROGLYCOLURIL
An improved method of preparing tetranitroglycoluril (TNGU) via the in situ decomposition of a nitrimino group with elimination of nitrogen without the use of...
2016/0176877 10H-BENZO[G]PTERIDINE-2,4-DIONE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF
The invention relates to 10H-benzo[g]pteridine-2,4-dione derivatives, to the production thereof, and to the use thereof.
2016/0176876 2-SUBSTITUTED IMIDAZO[4,5-D]PHENANTHROLINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER
The present invention provides 2-substituted imidazo[4,5-d]phenanthroline compounds, which are capable of inhibiting proliferation of one or more renal cancer...
2016/0176875 SPIROCYCLIC EBI2 MODULATORS
Provided herein are small molecule Epstein-Barr virus-induced G-protein coupled receptor 2 (EBI2) modulator compounds, compositions comprising the compounds,...
2016/0176874 AZETIDINE AND PIPERIDINE COMPOUNDS USEFUL AS PDE10 INHIBITORS
Azetidine and piperidine compounds of formula (I): ##STR00001## as defined in the specification, compositions containing them, and processes for preparing such...
2016/0176873 HETEROCYCLIC COMPOUND
The present invention provides a heterocyclic compound having a ROR.gamma.t inhibitory action. The present invention relates to a compound represented by the...
2016/0176872 HETEROCYCLIC COMPOUND
The present invention provides a heterocyclic compound having a ROR.gamma.t inhibitory action. The present invention relates to a compound represented by the...
2016/0176871 TGF BETA R ANTAGONISTS
The invention relates generally to compounds that modulate the activity of TGF.beta.R-1 and TGF.beta.R-2, pharmaceutical compositions containing said compounds...
2016/0176870 POLYCYCLIC-CARBAMOYLPYRIDONE COMPOUNDS AND THEIR PHARMACEUTICAL USE
Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (Ia): ##STR00001## ...
2016/0176869 Solid State Forms of Fused Heteroaromatic Pyrrolidinones
Disclosed are chemical entities which are inhibitors of spleen tyrosine kinase (SYK), namely, chemical entities comprising ...
2016/0176868 BICYCLIC-PYRIMIDINEDIONE COMPOUNDS
The present invention provides novel bicyclic pyrimidinedione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions...
2016/0176867 MODIFIED BET-PROTEIN-INHIBITING DIHYDROQUINOXALINONES AND DIHYDROPYRIDOPYRAZINONES
The present invention relates to BET protein-inhibitory, especially BRD4-inhibitory, dihydroquinoxalinones and dihydropyridopyrazinones of the general formula...
2016/0176866 4-AMINO-6-(2,6-DICHLOROPHENYL)-2-(PHENYLAMINO)-PYRIDO[2,3-d]PYRIMIDIN-7(8H- )-ONE DERIVATIVES, SYNTHESIS AND...
The present invention is related to 4-amino-6-(2,6-dichlorophenyl)-2-(phenylamino)-pyrido[2,3-d]pyrimidin-7(8- H)-one derivatives, to the preparation of such...
2016/0176865 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant...
2016/0176864 NOVEL TRICYCLIC COMPOUNDS AS ANTICANCER AGENTS
The present invention is directed to tricyclic compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using...
2016/0176863 8-AZABICYCLO[3.2.1]OCTANE COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS
The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, A, and G are defined in the ...
2016/0176862 1-(PIPERAZIN-1-YL)-2-([1,2,4]TRIAZOL-1-YL)-ETHANONE DERIVATIVES
The invention relates to compounds of Formula (I) ##STR00001## wherein X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as described in the description;...
2016/0176861 HYDROXY CONTAINING FXR (NR1H4) MODULATING COMPOUNDS
The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the...
2016/0176860 INHIBITORS OF LC3/ATG3 INTERACTION AND THEIR USE IN THE TREATMENT OF CANCER
The present inventors discovered that the molecule pyridinylthiazolamine (PTA) specifically prevents the protein-protein interaction of hLC3 with hAtg3 in...
2016/0176859 High-Throughput Assay for Identifying Small Molecules that Modulate AMP-activated Protein Kinase (AMPK)
The present invention provides an in vitro method for identifying a compound that modulates adenosine monophosphate-activated protein kinase (AMPK) for the...
2016/0176858 OXAZOLE OREXIN RECEPTOR ANTAGONISTS
The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole...
2016/0176857 3,5-DIAMINOPYRAZOLE KINASE INHIBITORS
Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula I, that are useful for modulating regulated-in-COPD kinase activity, and...
2016/0176856 Compositions and Methods for the Treatment of Norovirus Infection
Compositions and methods for the treatment of norovirus infection are disclosed.
2016/0176855 Novel Sterically Hindered Cyclic Amines
The invention relates to compounds of the formula (1) in which R.sub.1 and R.sub.2 respectively are a sterically hindered cyclic amine and their use as...
2016/0176854 Imidazolecarboxamides and Their Use as FAAH Inhibitors
A compound having a structure selected from the following: ##STR00001## or a pharmaceutically acceptable salt thereof. The compound may be used as an inhibitor...
2016/0176853 Benzocyanine Compounds
Compounds useful as labels with properties comparable to known fluorescent compounds. The compounds are conjugated to proteins and nucleic acids for biological...
2016/0176852 CYANINE COMPOUNDS
Compounds used as labels with properties comparable to known fluorescent compounds. The compounds can be conjugated to proteins and nucleic acids for...
2016/0176851 ANTAGONISTS OF PROSTAGLANDIN EP3 RECEPTOR
Provided herein are antagonists of prostaglandin EP3 receptor, processes to make said antagonists, and methods comprising administering said antagonists to a...
2016/0176850 AXL INHIBITORS
Compounds of the general formula (I): ##STR00001## processes for the preparation of these compounds, compositions containing these compounds, and the uses of...
2016/0176849 N-CYANOMETHYLAMIDES AS INHIBITORS OF JANUS KINASE
The present invention relates to compounds of general formula (1) that are inhibitors of Janus Kinase (JAK), a family of tyrosine kinases that are involved in...
2016/0176848 INDOLIZINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
Compounds of formula (I) wherein Ra, Rb, Rc, Rd, T, R3, R4, R5, X, Y and Het are as defined in the description. ##STR00001## Medicinal products containing the...
2016/0176847 SOVAPREVIR POLYMORPHS AND METHODS OF MANUFACTURE THEREOF
The disclosure provides crystalline Sovaprevir forms. The crystalline forms of Sovaprevir comprise a Form A polymorph, a Form B polymorph, a Form C polymorph,...
2016/0176846 CONJUGATES AND ASSOCIATED METHODS OF PRODUCING THEM FOR THE PREVENTION OR TREATMENT OF NICOTINE ADDICTION
The present invention relates in part to chemical compounds, and methods for producing these compounds. The compounds may also be incorporated into...
2016/0176845 PROCESS FOR THE PREPARATION OF A DIARYLTHIOHYDANTOIN COMPOUND
Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer. ...
2016/0176844 PROCESSES FOR THE PREPARATION OF A DIARYLTHIOHYDANTOIN COMPOUND
Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer. ...
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