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Patent # Description
2016/0244464 SUBSTITUTED BENZENE COMPOUNDS
The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of...
2016/0244463 CONFORMATIONALLY RESTRICTED P13K AND MTOR INHIBITORS
The invention relates to novel phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor compounds of formula (I) and (II), which are...
2016/0244462 6-NITRO-2,3-DIHYDROIMIDAZO[2,1-b]OXAZOLES AND A PROCESS FOR THE PREPARATION THEREOF
The present invention relates to newer generation of triazoles, tetrazoles, isoxazoles, urea and sulphonamide functionalities containing 6-nitro-2,...
2016/0244461 CYCLIC THIENOURACIL-CARBOXAMIDES AND USE THEREOF
The present application relates to novel 2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidine-6-carboxamide derivatives ("thienouracil"-carboxamides), to...
2016/0244460 ANTIVIRAL COMPOUNDS
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of...
2016/0244459 OPIOID KETAL COMPOUNDS AND USES THEREOF
This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): or a pharmaceutically acceptable salts thereof, wherein...
2016/0244458 Crystals of Dispiropyrrolidine Derivatives
Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of ...
2016/0244457 SELECTIVE EFFLUX INHIBITORS AND RELATED PHARMACEUTICAL COMPOSITIONS AND METHODS OF TREATMENT
The present invention provides novel compounds which inhibit cancer-associated transporter proteins, methods of treating or preventing the onset of a...
2016/0244456 PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS
The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2,...
2016/0244455 PYRAZOLOPYRIMIDINYL INHIBITORS OF UBIQUITIN-ACTIVATING ENZYME
Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: ##STR00001## or a pharmaceutically...
2016/0244454 PRODUCTION METHOD OF IMIDAZOLE DERIVATIVES
The present invention provides an advantageous production method of an imidazole derivative, which is suitable for industrial production. Compound (VI) is...
2016/0244453 TREATMENT OF VIRAL AND INFECTIOUS DISEASES USING AN INHIBITOR OF CBP/CATENIN
The present disclosure relates generally to alpha-helix mimetic structures and specifically to alpha-helix mimetic structures that are inhibitors of...
2016/0244452 HETEROCYCLIC COMPOUNDS AND USES THEREOF
Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods...
2016/0244451 SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
Provided is a sulfonamide derivative represented by the following general formula (1) and having an .alpha.4 integrin inhibitory effect with high selectivity...
2016/0244450 BICYCLIC HETEROCYCLES AS FGFR4 INHIBITORS
The present disclosure relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR4 enzyme and are useful in...
2016/0244449 BICYCLIC HETEROCYCLES AS FGFR4 INHIBITORS
The present disclosure relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR3 and/or FGFR4 enzyme and...
2016/0244448 BICYCLIC HETEROCYCLES AS FGFR4 INHIBITORS
The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR4 enzyme and are useful in...
2016/0244447 FLUORINATED TETRAHYDRONAPHTHYRIDINYL NONANOIC ACID DERIVATIVES AND USES THEREOF
The present invention relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present invention also relates to...
2016/0244446 HETEROARYL SYK INHIBITORS
The invention relates to new substituted heteroaryls of formula (1), wherein A is selected from the group consisting of N and CH, D is CH, E is selected from...
2016/0244445 4-Azaindole Derivatives
4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying...
2016/0244444 NOVEL TETRAHYDROPYRIDOPYRIMIDINE COMPOUND OR SALT THEREOF
To provide a compound having an inhibitory activity for an androgen receptor. A tetrahydropyridopyrimidine compound represented by the following general...
2016/0244443 NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
The present invention discloses compounds according to Formula I: ##STR00001## Wherein R.sup.1a, R.sup.1b, R.sup.2, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b,...
2016/0244442 NOVEL DIHYDROPYRIMIDINOISOQUINOLINONES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF...
A compound according to Formula Ia: ##STR00001## wherein L.sub.1, G, and R.sup.1 are as described herein. The present invention relates to novel compounds according...
2016/0244441 2-PHENYL OR 2-HETARYL IMIDAZOL[1,2-a]PYRIDINE DERIVATIVES
The invention relates to compounds of formulas I and II ##STR00001## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, halogen, S-lower alkyl, lower alkoxy...
2016/0244440 PYRIDINE DERIVATIVE AND MEDICAL USE THEREOF
The present invention relates to the field of pharmaceutical chemistry, specifically to a class of compounds containing lactam and derivative thereof, and...
2016/0244439 QUININE COMPOUNDS, AND OPTICAL ISOMERS, PREPARATION METHOD AND MEDICAL USE THEREOF
The present invention discloses a class of quinine compounds and pharmaceutically acceptable salts, solvates, prodrugs or optical isomers thereof. Also...
2016/0244438 PROCESSES FOR PREPARING DIHYDROPYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF
The present invention relates to processes for preparing a dihydropyrimidine derivative having Formula (I) or a tautomer thereof having Formula (Ia), as well...
2016/0244437 SUBSTITUTED PHENYLALANINE DERIVATIVES
The invention relates to substituted phenylalanine derivatives and to processes for preparation thereof, and to the use thereof for production of medicaments...
2016/0244436 NOVEL FUNCTIONALIZED 5-(PHENOXYMETHYL)-1,3-DIOXANE ANALOGS EXHIBITING CYTOCHROME P450 INHIBITION AND THEIR...
Pharmaceutical compositions described in this document comprise 5-(phenoxymethyl)-1,3-dioxane analogs having a disease-modifying action in the treatment of...
2016/0244435 EXPANDED THERAPEUTIC POTENTIAL IN NITROHETEROARYL ANTIMICROBIALS
Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to imidazole,...
2016/0244434 P2X4 RECEPTOR ANTAGONIST
The present invention relates to a compound represented by the following general formula (II), wherein, in the formula, R.sup.1a to R.sup.6a represent hydrogen...
2016/0244433 N-HETARYL(THIO)CARBONYL-2-(BENZOCYCLOALKEN-1-YL)CYCLAMINES AND THEIR USE AS FUNGICIDES
The present invention relates to fungicidal N-hetarylcarbonyl-2-(benzocycloalken-1-yl)piperidines or pyrrolidines of formula (I), and their thiocarbonyl...
2016/0244432 FUSED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTCIAL COMPOSITION, AND USES THEREOF
Disclosed are a fused heterocyclic compound, a preparation method therefor, a pharmaceutical composition, and uses thereof. The fused heterocyclic compound is...
2016/0244431 Inhibitors of Metallo-Beta-Lactamase (MBL) Comprising a Zinc Chelating Moiety
Compounds according to formula I are provided: A-L-B wherein A represents a lipophilic chelating moiety which is selective for Zn.sup.2+ions; L is a covalent...
2016/0244430 Processes for preparing ASK1 inhibitors
The present disclosure provides processes for the preparation of a compound of formula: ##STR00001## which exhibits apoptosis signal-regulating kinase ("ASK1")...
2016/0244429 Substituted Piperazine Compounds And Methods Of Use Thereof
Provided herein are novel piperazine compounds and pharmaceutical compositions thereof comprising the piperazine compounds for inhibiting serotonin reuptake...
2016/0244428 EFFICIENT PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE (S)-BINOL COMPLEX
Object of the present invention is an improved process for the preparation of Esomeprazole (S)-BINOL complex which is a key intermediate for the synthesis of...
2016/0244427 PROCESS FOR THE PREPARATION OF 3-(3-CHLORO-1H-PYRAZOL-1-YL)PYRIDINE
3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by coupling 3-bromopyridine with commercially available 3-aminopyrazole, purifying the...
2016/0244426 CARBAMATE/UREA DERIVATIVES
The invention relates to compound of the formula I ##STR00001## or a salt thereof, wherein the substituents are as defined in the specification; to its...
2016/0244425 A PROCESS FOR THE PREPARATION OF OLOPATADINE AND SYLIL INTERMEDIATES THEREOF
The present invention refers to a new "one-pot" process for the preparation of olopatadine via intermediates of formula (III). ##STR00001##
2016/0244424 NEW PI3K/AKT/MTOR INHIBITORS AND PHARMACEUTICAL USES THEREOF
The invention relates to new PI3K/AKT/m TOR inhibitors and their use for the prevention and/or the treatment of a disease selected from the group consisting...
2016/0244423 CHROMENE DERIVATIVES SUBSTITUTED BY ALKOXIDE AS INHIBITORS OF THE TCR-NCK INTERACTION
The present invention relates to a group of compounds of formula (I) containing a chromene nucleus: ##STR00001## and that present the capacity to inhibit the...
2016/0244422 METHOD OF PRODUCING BERAPROST
An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d...
2016/0244421 Derivative of Butylphthalide and Preparation Method and Use Thereof
(-)-(S)-3-(3'-hydroxy)-butylphthalide (a compound shown by Formula I) and an ester formed of the same and an acid are proved by experiments to be applicable to...
2016/0244420 A CRYSTALLINE ANHYDROUS FORM OF CABAZITAXEL, PROCESS FOR THE PREPARATION AND PHARMACEUTICAL COMPOSITIONS THEREOF
The present invention relates to a new anhydrous crystalline form of Cabazitaxel of formula (I), designated as form H. A further object of the present...
2016/0244419 METHOD FOR PREPARING GLYCIDOL USING GLYCEROL AND GLYCIDOL OBTAINED THEREBY
A method for preparing glycidol using glycerol includes mixing glycerol with urea in the presence of at least one zinc-based catalyst selected from the group...
2016/0244418 DERIVATIVES OF SOBETIROME
Ester derivatives of sobetirome with enhanced CNS distribution are disclosed.
2016/0244417 CATHEPSIN CYSTEINE PROTEASE INHIBITORS
This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and...
2016/0244416 (2R,4R)-5-(5'-CHLORO-2'-FLUOROBIPHENYL-4-YL)-2-HYDROXY-4-[(5-METHYLOXAZOLE- -2-CARBONYL)AMINO]PENTANOIC ACID
In one aspect, the invention relates to a compound of the structure: ##STR00001## or a pharmaceutically acceptable salt thereof, and a crystalline form of this...
2016/0244415 SUBSTITUTED URACILS AS CHYMASE INHIBITORS
Substituted uracil derivatives of formula (I), processes for their preparation, their use alone or in combinations for the treatment and/or prophylaxis of...
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