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Patent # Description
2016/0318908 NOVEL IMIDAZOLIDINE-2,4-DIONE DERIVATIVES
Imidazolidine-2,4-dione derivatives of formula (I): ##STR00001## These compounds have anti-proliferative activity and are useful for treating pathological states...
2016/0318907 INHIBITORS OF BRUTON'S TYROSINE KINASE
This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds...
2016/0318906 DIHYDRO-HYDANTOIN DERIVATIVES WITH HERBICIDAL ACTIVITY
The invention relates to substituted dihydro-hydantoin derivatives of the formula (I) wherein X, R.sup.a, R.sup.b, R.sup.c, R.sup.1, R.sup.2 and R.sup.3 are as...
2016/0318905 Novel benzimidazole derivatives as EP4 ligands
The present invention relates to novel benzimidazole derivatives of the general formula (I), to processes for their preparation and to their use for preparing...
2016/0318904 SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS
The present invention provides compounds of Formula (I): ##STR00001## or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables...
2016/0318903 THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE
Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described...
2016/0318902 NOVEL IMIDAZOLIDINE-2,4-DIONE DERIVATIVES
Imidazolidine-2,4-dione derivatives of formula (I): ##STR00001## The compounds have anti-proliferative activity and are useful for treating pathological states...
2016/0318901 SUBSTITUTED PIPERIDINYL-TETRAHYDROQUINOLINES
The present application relates to novel substituted piperidinyltetrahydroquinolines, to processes for their preparation, to their use for the treatment and/or...
2016/0318900 2-AMINO-3-ESTER-PYRIDYL OREXIN RECEPTOR ANTAGONISTS
The present invention is directed to 2-amino-3-ester pyridyl compounds which are antagonists of orexin receptors. The present invention is also directed to...
2016/0318899 THIOETHER-PIPERIDINYL OREXIN RECEPTOR ANTAGONISTS
The present invention is directed to thioether-piperidinyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses...
2016/0318898 Processes for the Preparation of Axitinib
Processes for the preparation of Axitinib in good yield (generally greater than 80%) are provided that avoid the use of a palladium-catalyzed coupling reaction.
2016/0318897 AZOLE COMPOUNDS CARRYING AN IMINE-DERIVED SUBSTITUENT
The present invention relates to azole compounds of formula I ##STR00001## wherein the variables are as defined in the claims or the description. The invention also...
2016/0318896 NOVEL PIPERIDINE CARBOXAMIDE COMPOUND, PREPARATION METHOD, AND USAGE THEREOF
The present invention provides a compound of a general formula I, a stereomeride, pharmaceutically acceptable salt or a solvate thereof, a preparation method...
2016/0318895 Inhibitors of 17Beta-Hydroxysteroid Dehydrogenases Type 1 and Type 2
Provided herein are non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 and type 2 (17.beta.-HSD1 and 17.beta.-HSD2) inhibitors, their production and use,...
2016/0318894 Sulfamate Derivative Compounds for Use in Treating or Alleviating Pain
The present invention relates to sulfamate derivative compounds and a composition for treating and/or alleviating pain containing the sulfamate derivative...
2016/0318893 STEREO-SPECIFIC SYNTHESIS OF (13R)-MANOYL OXIDE
The present invention relates to a method for manufacturing enantiomerically pure (13R)-manoyl oxide, said method comprising the steps of contacting...
2016/0318892 PRODRUG COMPOUNDS
A compound of formula (Ia) or (Ib), or a pharmaceutically acceptable salt thereof, Wherein Q, R.sup.2, Ar, A and R.sup.1 are as defined in claim 1. The claimed...
2016/0318891 TONABERSAT PRODRUGS
The invention relates to pharmaceutically active compounds having improved pharmacokinetic properties and being useful for the treatment or prevention of a...
2016/0318890 NOVEL KINASE MODULATORS
The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment,...
2016/0318889 SECOND-ORDER NONLINEAR OPTICAL COMPOUND AND NONLINEAR OPTICAL ELEMENT COMPRISING THE SAME
Problem to Be Solved: to provide a chromophore having a far superior nonlinear optical activity to conventional chromophores and to provide a nonlinear optical...
2016/0318888 CRYSTALLINE FORM OF CABAZITAXEL AND PROCESS FOR PREPARING THE SAME
The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or ...
2016/0318887 AMIDOPHENOXYPROPANOLAMINES
The use of compounds of formula ##STR00001## wherein R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have several meanings, for the treatment of...
2016/0318886 Novel Compound, Organic Cation Transporter 3 Detection Agent, And Organic Cation Transporter 3 Activity Inhibitor
[Problem] The present invention addresses the problem of providing a novel compound. The present invention also addresses the problem of providing an OCT3...
2016/0318885 GAMMA-AMINOBUTYRIC ACID (GABA) ANALOGUES FOR THE TREATMENT OF PAIN AND OTHER DISORDERS
A compound of Formula (1) wherein R.sub.1 represents hydrogen, halo, a C1-C4 alkyl group, a C1-C4 alkylhalide group, a C1-C4 alkoxy-C2-C4 alkyl group, a C2-C4...
2016/0318884 3-(5-CHLORO-2-OXOBENZO[D]OXAZOL-3(2H)-YL) PROPANOIC ACID DERIVATIVES AS KMO INHIBITORS
A compound of formula (I) or a salt thereof are provided: ##STR00001## wherein R.sup.1, X and R.sup.3 are defined in the specification, useful in the treatment...
2016/0318883 INTEGRATED PRODUCTION OF UREA AND MELAMINE
Disclosed is a process for the integrated production of urea and melamine. A urea production zone produces a urea synthesis stream comprising urea, water and...
2016/0318882 TRIAZOLES AS KV3 INHIBITORS
Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related...
2016/0318881 PROCESS FOR THE PREPARATION OF SUBSTITUTED PHENOXYPHENYL KETONES
The present invention relates to a process for the preparation of the ketone compounds (IA) ##STR00001## and their use as intermediates for the preparation of...
2016/0318880 SUBSTITUTED [1,2,4]TRIAZOLE AND IMIDAZOLE COMPOUNDS
The present invention relates to compounds of the formula I ##STR00001## and the N-oxides and the salts thereof for combating phytopathogenic fungi, and to the...
2016/0318879 PREPARATION OF PYRIMIDINE INTERMEDIATES USEFUL FOR THE MANUFACTURE OF MACITENTAN
The present invention relates to a new synthetic intermediate, namely the compound of formula I-2 ##STR00001## or a salt thereof. Said compound of formula I-2 or...
2016/0318878 METHODS TO TREAT LYMPHOPLASMACYTIC LYMPHOMA
The present invention provides compounds of any one of Formulae (A), (I-11), (II), and (V) (e.g., compounds of Formula (A-1)-(A-18)), and methods for treating...
2016/0318877 PROCESS FOR MAKING HYDROXYLATED CYCLOPENTYLPYRIMIDINE COMPOUNDS
The invention provides processes for preparing a compound of formula I ##STR00001## and salts thereof, wherein R.sup.1 is defined herein, and compounds and ...
2016/0318876 PHTHALAZINE DERIVATIVES
Compounds of the formula I ##STR00001## in which R.sup.1, X and n have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter...
2016/0318875 PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF ENZALUTAMIDE
The present invention provides processes for the preparation of enzalutamide.
2016/0318874 PROCESS FOR THE REGIOSELECTIVE SYNTHESIS OF PYRAZOLES
A process is described for the synthesis of pyrazoles having general formula (I) ##STR00001## which comprises the steps of mixing a compound having general...
2016/0318873 POLYMORPHIC FORMS OF IVABRADINE HYDROCHLORIDE
Stable crystalline Form II and stable crystalline Form III of ivabradine hydrochloride and processes for their preparation are disclosed.
2016/0318872 6-SUBSTITUTED AND 7-SUBSTITUTED MORPHINAN ANALOGS AND THE USE THEREOF
The application is directed to compounds of Formula I or II: and pharmaceutically acceptable salts and solvates thereof, wherein R', R'', R''' R.sup.1,...
2016/0318871 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which...
2016/0318870 RORy MODULATORS
Described are ROR.gamma. modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The...
2016/0318869 Heterocyclic Compounds for the Treatment of Neurological and Psychological Disorders
Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety...
2016/0318868 METHOD OF PRODUCING 2-AMINONICOTINIC ACID BENZYL ESTER DERIVATIVES
The present invention provides a method of producing a 2-aminonicotinic acid benzyl ester derivative at a high yield and with a high purity. By reacting a...
2016/0318867 METHOD FOR PRODUCING 5-HYDROXYPIPERIDINE-2-CARBOXYLIC ACID
A method for producing (2S,5S)/(2R,5R)-5-hydroxypiperidine-2-carboxylic acid represented by formula (10) below: ##STR00001## the method including removing the...
2016/0318866 SUBSTITUTED BIPIPERIDINYL DERIVATIVES
The invention relates to novel substituted bipiperidinyl derivatives, to processes for their preparation, to their use for the treatment and/or prevention of...
2016/0318865 TRICYCLIC LACTAM DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS
Compounds of the formula (I) useful as 11-Beta Hydroxysteroid Dehydrogenase Inhibitors ##STR00001##
2016/0318864 4-(PIPERRAZIN-1-YL)-PYRROLIDIN-2-ONE COMPOUNDS AS MONOACYLGLYCEROL LIPASE (MAGL) INHIBITORS
The present invention aims to provide a compound having an MAGL inhibitory action, and useful as a prophylactic or therapeutic agent for neurodegenerative...
2016/0318863 CATALYST FOR SYNTHESIZING ETHYLENIMINE AS WELL AS PREPARATION METHOD AND APPLICATION THEREOF
The present invention relates to a catalyst for synthesizing ethylenimine as well as a preparation method and application thereof. The related catalyst...
2016/0318862 SYNTHESIS OF DELTA 12-PGJ3 AND RELATED COMPOUNDS
In one aspect, the present invention provides novel derivatives of .DELTA..sup.12-PGJ.sub.3 and modular synthetic pathways to obtaining ...
2016/0318861 NOVEL PRODRUGS OF DITHIOL MUCOLYTIC AGENTS
Provided are mucolytic compounds that are more effective, and/or absorbed less rapidly from mucosal surfaces, and/or are better tolerated as compared to...
2016/0318860 OXIDATION OF 2-MERCAPTOETHANOL
The present invention relates to a process for the preparation of bis-(2-hydroxyethyl)-disulfide by oxidizing 2-mercaptoethanol with oxygen in a reaction...
2016/0318859 FLORFENICOL SYNTHESIZING METHOD
The present invention discloses a new florfenicol synthesizing method. The method synthesizes florfenicol products meeting requirements of the Drug...
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