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Patent # Description
2016/0257695 SYNTHESIS OF SUBSTITUTED SALICYLALDEHYDE DERIVATIVES
Among other things, the present invention encompasses methods of synthesizing salicylaldehyde derivatives comprising the steps of: a) providing salicylaldehyde...
2016/0257694 ORIDONIN FUNCTIONALIZED SELENIUM NANOPARTICLES AND METHOD OF PREPARATION THEREOF
The present invention relates to an oridonin functionalized selenium nanoparticle, method of preparing and use thereof for anti-cancer and anti-inflammatory...
2016/0257693 Crystalline Forms of Therapeutic Compounds and Uses Thereof
Described herein is certain crystalline forms of Compound 5, as well as pharmaceutical compositions employing the crystalline forms. Also provided are...
2016/0257692 TETRAHYDROQUINOLINE COMPOSITIONS AS BET BROMODOMAIN INHIBITORS
The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases,...
2016/0257691 PYRIMIDO-PYRIDAZINONE COMPOUNDS AND METHODS OF USE THEREOF
The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in...
2016/0257690 TGF-Beta Inhibitors
Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the...
2016/0257689 SALTS AND PROCESSES OF PREPARING A PI3K INHIBITOR
The present application provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)- ...
2016/0257688 Process for Synthesis of Lactams
Methods for the synthesis of lactams are presented whereby a carboxylic acid of the formula HOOC--OR--NH-LG, wherein OR is an organic moiety and LG is a...
2016/0257687 PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS
The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic...
2016/0257686 Purinone Derivatives as Tyrosine Kinase Inhibitors
The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR,...
2016/0257685 KAPPA OPIOID RECEPTOR EFFECTORS AND USES THEREOF
The present invention is a selective kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder...
2016/0257684 NITROGEN CONTAINING COMPOUNDS AND THEIR USE
Compound of Formula (I), its preparation and use in preventing or treating bacterial infection is disclosed. Formula (I) ##STR00001##
2016/0257683 CHROMOPHORES FOR THE DETECTION OF VOLATILE ORGANIC COMPOUNDS
Aromatic diimide chromophores and methods for using the chromophores for the detection of volatile organic compounds are described. The chromophores are able...
2016/0257682 AZAINDAZOLE COMPOUNDS AS INHIBITORS OF T790M CONTAINING EGFR MUTANTS
This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes...
2016/0257681 Protein Kinase C Inhibitors and Uses Thereof
This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and...
2016/0257680 ISOTOPICALLY LABELED TRIAZOLOPYRIDINE 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are...
2016/0257679 NEW 1-(4-PYRIMIDINYL)-1H-PYRROLO[3,2-c]PYRIDINE DERIVATIVES AS NIK INHIBITORS
The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of ...
2016/0257678 NOVEL COMPOSITIONS, USES AND METHODS FOR MAKING THEM
Generally, the present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce...
2016/0257677 LARGE SUBSTITUTENT, NON-PHENOLIC OPIOIDS AND METHODS OF USE THEREOF
8-Substituted-2,6-methano-3-benzazocines of general structure ##STR00001## are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and...
2016/0257676 Aminoisoquinoline Derivatives as Protein Kinase Inhibitors
The present invention provides novel aminoisoquinoline compounds as defined in the specification, compositions thereof use of these compounds as protein kinase...
2016/0257675 COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISORDERS
The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog...
2016/0257674 KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at...
2016/0257673 4,6-DI- AND 2,4,6-TRISUBSTITUTED QUINAZOLINE DERIVATIVES USEFUL FOR TREATING VIRAL INFECTIONS
This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R.sub.2 is hydrogen, NR'R'', C.sub.1-7 alkyl,...
2016/0257672 FUNCTIONALIZED FURAN-2-SULFONAMIDES EXHIBITING ENDOTHELIAL LIPASE INHIBITION
The present invention relates to pharmaceutical compositions comprising furan-2-sulfonamide derivatives. The present invention further relates to methods of...
2016/0257671 SHIP1 MODULATORS AND METHODS RELATED THERETO
Compounds of formula (I): ##STR00001## where ##STR00002## n, R.sup.1, R.sup.4a, R.sup.4b, R.sup.5, R.sup.7 and R.sup.8 are defined herein, or pharmaceutically...
2016/0257670 Inhibitors of the Renal Outer Medullary Potassium Channel
The present invention provides compounds of Formula I ##STR00001## and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1)...
2016/0257669 SPECIFIC TARGETING OF RNA EXPANDED REPEAT SEQUENCES
The present invention provides small molecule compounds that can form covalent adducts with specific sequences of RNA, such as the hairpin loop r(CUG).sup.exp...
2016/0257668 Factor XIa Inhibitors
The present invention provides a compound of Formula (I) ##STR00001## and pharmaceutical compositions comprising one or more said compounds, and methods for...
2016/0257667 SYNTHESIS OF INTERMEDIATES IN THE PREPARATION OF ALK INHIBITOR
The present disclosure provides a method for preparing a compound of formula XVII, comprising: (1) contacting a compound of formula XIV with a compound of...
2016/0257666 MODULATORS OF RESISTANT ANDROGEN RECEPTOR
The present invention provides compounds useful as modulators, agonists or antagonists of androgen receptor (AR), compositions thereof, and methods of making...
2016/0257665 SUBSTITUTED AZINES AS PESTICIDES
The invention relates to compounds of the general formula (I), wherein the variable have the meanings as indicated in the claims, or a physiologically...
2016/0257664 NOVEL COMPOUNDS
The present invention is directed to crystalline forms of a compound which has retinoid-related orphan receptor gamma (ROR.gamma.) modulator activity,...
2016/0257663 CRYSTALLINE SOLVATE FORMS OF CABAZITAXEL
The present invention relates to new crystalline forms of Cabazitaxel of formula (I). Specifically, the present invention provides four new crystalline solvate...
2016/0257662 KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE
Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDMIA,...
2016/0257661 1,4-CYCLOHEXYLAMINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
The invention relates to a process for the synthesis of Cariprazine, an antipsychotic compound useful in the treatment of positive and negative symptoms...
2016/0257660 THIADIAZOLIDINEDIONES AS GSK-3 INHIBITORS
The present invention relates to new thiadiazolidinediones of formula (I), or any pharmaceutically acceptable salt, solvate or prodrug thereof, and its use in...
2016/0257659 POLYMERIZABLE COMPOUND, POLYMERIZABLE COMPOSITION, POLYMER, AND OPTICALLY ANISOTROPIC PRODUCT
This invention provides a polymerizable compound represented by formula (I), a polymerizable composition containing the polymerizable compound and a...
2016/0257658 2-ACYLAMINOTHIAZOLES FOR THE TREATMENT OF CANCER
The present invention relates to inhibitors of the oncogenic protein kinase ALK of formula (I) as herein described and pharmaceutical compositions thereof. The...
2016/0257657 SMALL MOLECULE INHIBITORS OF THE NUCLEAR TRANSLOCATION OF ANDROGEN RECEPTOR FOR THE TREATMENT OF...
A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I: ...
2016/0257656 HETEROCYCLIC COMPOUNDS AND METHODS FOR THEIR USE
The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT.sub.2) receptor. More particularly the invention...
2016/0257655 DESIGN AND SYNTHESIS OF NOVEL INHIBITORS OF ISOPRENOID BIOSYNTHESIS (ISPF)
Antibacterial and antimalarial IspF inhibitor compounds and compositions are described. Methods include administering described compounds and compositions to...
2016/0257654 CANNABINOID RECEPTOR MEDIATING COMPOUNDS
A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CB.sub.1 receptor mediating scaffold and (ii) a second therapeutic scaffold.
2016/0257653 Benzazepine Dicarboxamide Compounds
This invention relates to novel benzazepine dicarboxamide compounds of the formula ##STR00001## wherein R.sup.1 to R.sup.4 are as defined in the description and...
2016/0257652 ANTIDIABETIC TRICYCLIC COMPOUNDS
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may...
2016/0257651 NOVEL COMPOUND WITH ANTIBACTERIAL ACTIVITY
A compound represented by the general formula (I) or a salt thereof having a potent antibacterial activity against bacteria that have acquired resistance to...
2016/0257650 MONOARYLATION OF AROMATIC AMINES
The present invention relates to a selective process for performing the Hartwig-Buchwald coupling of biphenyl derivatives.
2016/0257649 DUAL FUNCTION MOLECULES FOR HISTONE DEACETYLASE INHIBITION AND ATAXIA TELANGIECTASIA MUTATED ACTIVATION AND...
Dual function compounds are provided that may be inhibitors of histone deacetylase (HDAC) and activators of ataxia telangiectasia mutated (ATM). Pharmaceutical...
2016/0257648 OXINDOLE INHIBITORS OF TYROSINE KINASE
The present invention relates to new oxindole inhibitors of tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof. ##STR00001##
2016/0257647 POLYTHIOLS WITH CARBAMATE GROUPS
The present invention discloses polythiol compositions containing sulfur-containing compounds with carbamate groups, and to methods for producing such...
2016/0257646 METHOD FOR SYNTHESISING A MERCAPTAN BY ADDING HYDROGEN SULFIDE TO AN OLEFIN
The invention relates to a method for synthesising a mercaptan from a terminal olefin and hydrogen sulphide which comprises the following consecutive steps:...
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