|Application No.||Application Title||Issue Date|
|20140051675||MODULATORS OF CELLULAR ADHESION|
The present invention provides compounds having formula (I):
|20140051679||KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME|
The present teachings provide a compound represented by Structural Formula (I):
or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof....
|20140045770||OLIGOMER-PROTEASE INHIBITOR CONJUGATES|
The invention provides small molecule drugs 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 administration routes, exhibits characteristics that are different from the...
|20140038821||ISOXAZOLINES FOR CONTROLLING INVERTEBRATE PESTS|
Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof,
|20140031387||LFA-1 INHIBITOR AND METHODS OF PREPARATION AND POLYMORPH THEREOF|
Methods of preparation and purification of a compound of Formula I, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed.
|20140018356||FUSED CYCLOPENTYL ANTAGONISTS OF CCR2|
The present invention comprises compounds of Formula (I).
wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The inve...
|20140005382||NITROGEN-CONTAINING CONDENSED HETEROCYCLIC COMPOUND|
There are provided compounds represented by the following general formula (I) or pharmaceutically acceptable salts of thereof, which have a superior monoacylglycerol acyltransferase 2 inhibitory action:
|20140004243||SALTY TASTE ENHANCER|
The present invention provides a compound having a salty taste enhance activity, and a salty taste enhancer containing the compound, and the like.
The present invention relates to a salty taste enhancer for a food or drink, which contains a...
|20130310419||PYRROLE DERIVATIVES USED AS MODULATORS OF ALPHA7 NACHR|
The present invention is related to pyrrole derivatives of formula I as the modulators of nicotinic acetylcholine receptors particularly the α7 subtype. The invention includes pyrrole derivatives, analogues, their prodrugs, their isotopes, their metabolites, pharmaceut...
|20130296320||NOVEL BICYCLIC COMPOUND OR SALT THEREOF|
Provided is a novel bicyclic compound which has an HSP90 inhibitory effect and a carcinostatic effect. Also provided is a pharmaceutical agent which is based on the HSP90 inhibitory effect and is useful in the prevention and/or treatment of a disease involving HSP90, pa...
|20130289280||NOVEL PHARMACEUTICAL FORMS, AND METHODS OF MAKING AND USING THE SAME|
Crystalline salts, polymorphs, solvates, and hydrates of bicalutamide, 5-fluorouracil, donepezil, anastrozole, nelfinavir, mirtazapine, lansoprazole, and tamsulosin, or derivatives thereof are provided by the subject invention. Methods of making and using the same are a...
|20130252940||c-Met Modulators and Method of Use|
The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazoline...
|20130245025||Compounds that modulate intracellular calcium|
Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other co...
|20130245008||NITROBENZOTHIAZOLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATIONS THEREOF|
The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.
|20130210859||NOVEL CORTISTATIN A ANALOG AND USE THEREOF|
A compound represented by the general formula (M):
|20130203709||ACYLSULFONAMIDES AND PROCESSES FOR PRODUCING THE SAME|
The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, ...
|20130196996||USE OF ISOXAZOLINE COMPOUNDS AND COMPOSITIONS IN BLADDER CANCER|
One embodiment provides a method, comprising treating or preventing at least one disease selected from the group consisting of bladder cancer, weight loss accompanying bladder cancer, bone pain accompanying bladder cancer, bladder cancer carcinoma in-situ (CIS), TA stag...
|20130184222||THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE|
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here....
|20130184258||Compositions Useful as Inhibitors of Voltage-Gated Sodium Channels|
The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of var...
|20130172553||CHIRAL SYNTHESIS OF ISOXAZOLINES, ISOXAZOLINE COMPOUNDS, AND USES THEREOF|
Processes for the chiral syntheses of isoxazolines and intermediates are described. Compounds prepared thereby, and methods of using the compounds are also described....
|20130172384||FATTY ACID SYNTHASE INHIBITORS|
This invention relates to the use of triazolone and triazolethione derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones and triazolethiones in t...
|20130158072||KAPPA OPIOID RECEPTOR BINDING LIGANDS|
Kappa opioid recep-tor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor, such...
|20130157996||TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS|
Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions....
|20130150585||Crystalline Pharmaceutical and Methods of Preparation and Use Thereof|
Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this...
|20130137684||HAEMATOPOIETIC-PROSTAGLANDIN D2 SYNTHASE INHIBITORS|
The present invention generally relates to compounds that inhibit haematopoietic-prostaglandin D2 synthase (H-PGDS), to compositions containing them and to their use in treating or preventing conditions and diseases associated with H-PGDS, such as allergies a...
|20130131321||LIGANDS FOR ANTIBODY AND Fc-FUSION PROTEIN PURIFICATION BY AFFINITY CHROMATOGRAPHY|
The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented ...
|20130131018||SUBSTITUTED ISOQUINOLINES AND THEIR USE AS TUBULIN POLYMERIZATION INHIBITORS|
The present invention relates generally to substituted isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of the...
|20130123242||COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS|
The present invention provides novel compounds represented by formula I:
or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection....
|20130072494||INHIBITORS OF JUN N-TERMINAL KINASE|
The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula:
or a salt or solvate thereof, wherein ring A, Ca, Cb, ...
|20130065882||VLA-4 inhibitory drug|
This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof:
|20130059883||COMPOUNDS AND METHODS|
Disclosed are compounds having the formula:
wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods...
|20130059839||PYRIDYLTHIAZOLE-BASED UREAS AS INHIBITORS OF RHO ASSOCIATED PROTEIN KINASE (ROCK) AND METHODS OF USE|
Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed....
|20130053382||Inhibitors of Phosphoinositide Dependent Kinase 1 (PDK1)|
The instant invention provides for compounds that inhibit PDK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer....
|20130029845||ISOXAZOLINES FOR CONTROLLING INVERTEBRATE PESTS|
Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof,
|20130028843||KALLIKREIN 7 MODULATORS|
The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7....
|20130023660||Carboxamide Compounds and Methods for Using the Same|
Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure
in which R1, R2, R3, R4<...
|20130004518||CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT|
Disclosed are compounds of the formula
or a pharmaceutically acceptable salt or solvate thereof, wherein
|20120330020||METHOD FOR PREPARING TETRAZOLE METHANESULFONIC ACID SALTS, AND NOVEL COMPOUND USED IN SAME|
According to the present invention, a method for preparing tetrazole methanesulfonic acid salts comprises an acylation reaction using a novel 4-iodine-4H-chromene-2-carbothionic acid S-benzothiazole-2-yl ester. The method of the present invention can shorten a reaction ...
|20120309751||TERTIARY 8-HYDROXYQUINOLINE-7-CARBOXAMIDE DERIVATIVES AND USES THEREOF|
New tertiary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof are disclosed.
These compounds are useful as antifungal agents. Specifically, the...
|20120301427||CHEMOKINE RECEPTOR BINDING HETEROCYCLIC COMPOUNDS WITH ENHANCED EFFICACY|
The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optiona...