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9040538 Pyrimidines as novel therapeutic agents  
The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers,...
9040697 Process for the production of moxonidine  
4,6-dichloro-2-methyl-5-(1-acyl-2-imidazolin-2-yl)-aminopyri midine is reacted with methanol in the presence of a non-ionic organic base, and moxonidine is obtained directly from the reaction mixture.
9024033 Anti-malarial agents  
The present invention is related to a use of aminopyridine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to...
9023656 Reactive mass labels  
A mass label for labelling and detecting a biological molecule by mass spectroscopy, which label comprises the following structure: X-L-M wherein X is a mass marker moiety comprising the following...
8993752 Neprilysin inhibitors  
In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These...
8980888 Pyrazole derivative  
It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative...
8969365 Thiopyrimidinecarboxamides as CXCR1/2 modulators  
There is disclosed a pyrimidinecarboxamide compound useful as a pharmaceutical agent, synthetic processes, and pharmaceutical compositions which include the pyrimidinecarboxamide compound. More...
8962642 5-cyano-4- (pyrrolo [2,3B] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors  
The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
8933090 1-aza-bicyclo[3.3.1]nonanes  
The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as...
8916555 3,5-diaminopyrazole kinase inhibitors  
Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also...
8901301 Pyrrolo[2,3-]pyridine kinase inhibitors  
Propane-1-sulfonic acid {2,4-difluoro-3-[5-(2-methoxy-pyrimidin-5-yl)-1H-pyrrolo[2,3 -b]pyridine-3-carbonyl]-phenyl}-amide, propane-1-sulfonic acid...
8859769 Processes for preparing ticagrelor intermediate, 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine  
Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate,...
8859573 Pyrimidinone and pyridinone compounds for use in the treatment of diseases or conditions mediated by Lp-PLA2  
The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases...
8859529 Compounds for the treatment of inflammatory disorders  
This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or...
8846913 Neprilysin inhibitors  
In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3—R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof....
8846689 Substituted pyrimidines for the treatment of diseases such as cancer  
The present invention encompasses compounds of general formula (1) wherein A, B, X, R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive...
8835461 Substituted 3-hydroxy-4-pyridone derivative  
This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having...
8829015 Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide  
Crystalline forms of 4-methyl-N-3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phen yl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.
8822448 Pyrazoloquinoline compound  
The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding...
8809343 Pyrimidine derivative, preparation method and use thereof  
A pyrimidine derivative and the preparation method and use thereof. The said pyrimidine derivative is a diaryl pyrimidine derivative or a diaryl benzo pyrimidine derivative which has the structure...
8796451 Crystalline pharmaceutical  
New crystalline forms of lopinavir are disclosed.
8791131 Imidazo[1,5]naphthyridine compounds, their pharmaceutical use and compositions  
The present invention is directed to compounds of Formula (I), and to salts thereof, their synthesis, and their use as PI3-Kα inhibitors and/or PI3-Kα/mTOR dual inhibitors.
8791114 Dihydropyrazoles  
Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the...
8748411 Antineoplastic compounds and pharmaceutical compositions thereof  
Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the...
8748433 β3 adrenergic receptor agonists  
The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of...
8735579 Benzamides, production thereof, and use thereof as medicaments  
Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the...
8729265 Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives  
The present invention relates to a method of making pyrimidines of formula (III) said method comprising reacting a compound of formula (I) with an oxygen, sulfur or nitrogen nucleophile of formula...
8703759 Fused heterocyclic compounds as ion channel modulators  
The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In...
8691816 Pyrrole inhibitors of S-nitrosoglutathione reductase as therapeutic agents  
The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
8685974 Thienylpyri(mi)dinylazole  
Thienylpyri(mi)dinylazole of the formula (I) in which R1 to R8 and X1 have the meanings given in the description, and agrochemically active salts, to their use and to methods and compositions for...
8658659 Substituted oxazole derivatives and their use as tyrosine kinase inhibitors  
The present invention relates to novel compounds selected from substituted oxazole derivatives of formula (I) that selectively modulate, regulate, and/or inhibit signal transduction mediated by...
8653266 Process for the production of etravirine  
A novel process for the preparation of Etravirine comprises the condensing of ethyl cyanoacetate with N-cyanophenylguanidine to obtain an —OH compound of formula (II), which is further converted...
8623860 Azetidine derivatives, pharmaceutical compositions and uses thereof  
The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
8614320 Preparation of aminopyrimidine compounds  
A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with...
8609852 Thiazolyl mGluR5 antagonists and methods for their use  
The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or...
8598360 Apoptosis signal-regulating kinase inhibitors  
The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”)...
8598364 Oligomer-protease inhibitor conjugates  
The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of...
8586536 Neprilysin inhibitors  
In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds...
8580805 Pyrimidine carboxamide derivatives  
The invention relates to a compound of the formula wherein the substituents are as defined herein, and a pharmaceutically acceptable salt of the compound of formula (1). The compounds of formula...
8569322 Lamivudine oxalate and preparation method thereof  
Lamivudine oxalate, preparation method and crystalline forms thereof are disclosed. A preparation method of Lamivudine is also disclosed.
8552196 Apoptosis signal-regulating kinase inhibitors  
The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”)...
8546374 Amino-tetrazoles analogues and methods of use  
A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and...
8530489 5-cyano-4-(pyrrolo [2,3B] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors  
The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
8524726 Amido derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors  
The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate...
8518885 Heterocyclic peptide ketoamides  
A novel class of peptide α-ketoamides useful for selectively inhibiting calpains, selectively inhibiting cysteine proteases, and generally inhibiting all cysteine proteases, having the formula...
8518916 Heterocyclic derivatives as M-GLU5 antagonists  
This invention relates to novel heterocyclic compounds having selective affinity for the mGlu5 subtype of metabotropic receptors, pharmaceutical compositions thereof and uses for such compounds...
8512820 Organic ionic phenylpyrimidine compounds and displays formed thereof  
Ionic mesogenic compounds of formula (I) can be used to form liquid crystal displays, such as ferroelectric liquid crystal displays, having enhanced anti-image sticking properties. The mesogenic...
8507485 Cyclic compound having pyrimidinylalkylthio group  
A method of treating a disease associated with angiogenesis by administering a therapeutically effective amount of a compound represented by the formula (1) or a salt thereof wherein the ring X...
8481731 Compounds, pharmaceutical composition and methods relating thereto  
New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein X1, X2,...
8476287 3-hydroxy-5-arylisothiazole derivative  
[Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the...