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8481547 Substituted benzothiazole and benzoxazole derivatives useful as inhibitors of DPP-1  
The present invention is directed to substituted benzothiazole and benzoxazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions...
8476274 Biaryl spiroaminooxazoline analogues as Alpha2C adrenergic receptor modulators  
In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such...
8470776 Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof  
The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present...
8450313 2,3-diaryl- or heteroaryl-substituted 1,1,1-trifluoro-2-hydroxypropyl compounds  
The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl...
8450304 4-azetidinyl-1-heteroaryl-cyclohexanol antagonists of CCR2  
The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, and R4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the...
8445522 Substituted 2-(4-pyridyl)benzoxazoles, and compositions thereof, for use in arthropod pest control  
Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a...
8445480 CETP inhibitors derived from benzoxazole arylamides  
Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for...
8436028 CETP inhibitors derived from benzoxazole arylamides  
Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing...
8431572 2-oxo-3-benzylbenzoxazol-2-one derivatives and related compounds as met kinase inhibitors for the treatment of tumours  
Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein,...
8426455 Prophylactic and/or therapeutic agent for hyperlipidemia  
The present invention provides a therapeutic agent for hyperlipidemia having an excellent effect of lowering the cholesterol and triglyceride level in blood plasma. The present invention relates...
8394816 Methods of using [3.2.0] heterocyclic compounds and analogs thereof in treating Waldenstrom's Macroglobulinemia  
Disclosed are methods of treating Waldenstrom's Macroglobulinemia comprising administering to the animal, a therapeutically effective amount of a heterocyclic compound of Formula I.
8394794 Therapeutic compounds  
The invention provides compounds of Formula (I) and (IV): as described herein, as well as salts thereof. The compounds have anti-cancer properties and/or chemosensitization properties.
8394799 Compounds that inhibit HIF-1 activity, the method for preparation thereof and the pharmaceutical composition containing them as an effective component  
Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer...
8377981 CBI derivatives subject to reductive activation  
A unique class of N-acyl O-amino phenol prodrugs of CBI-TMI and CBI-indole2 were synthesized and shown to be prodrugs, subject to reductive activation by nucleophilic cleavage of a weak N—O bond,...
8354397 Mediators of hedgehog signaling pathways, compositions and uses related thereto  
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function...
8354400 Benzoxazole compounds and methods of use  
The present invention provides benzoxazole compounds and pharmaceutically acceptable salts thereof and pharmaceutical compositions including the same. The present invention further provides...
8338477 Tetracycline derivatives with reduced antibiotic activity and neuroprotective benefits  
The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack...
8338469 Compounds and compositions as channel activating protease inhibitors  
The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate...
8334290 CETP inhibitors  
Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or...
8334311 Indoline anti-cancer agents  
Indoline compounds having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders are provided.
8324213 Biaryl-spiroaminooxazoline analogues as alpha 2C adrenergic receptor modulators  
In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such...
8318728 Compounds and compositions for treating chemical warfare agent-induced injuries  
Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
8318787 Prodrugs of (3,5-bis(4-fluorophenyl)tetrahydro-1H-oxazolo[3,4-C]oxazol-7A-yl)methanol and derivatives thereof  
A prodrug that has a prodrug moiety that degrades into a compound having the general Formula I with R3 being an alcoholic moiety can be useful in therapies for neurodegenerative diseases as well...
8309543 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...
8304409 Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use  
The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated...
8293774 Optically active (R)-aryloxypropionic acid amides and herbicidal composition comprising same  
The present invention relates to an optically active (R)-aryloxypropionic acid amide compound which has high selectivity and safety for protecting a crop such as rice, wheat, barley and soy bean,...
8293775 Benzoxazolone derivatives, processes for preparing them and their uses  
The present invention relates to benzoxazolone derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, in the treatment of movement...
8277688 Aluminum alloy coated pigments and corrosion-resistant coatings  
This invention relates to galvanic aluminum alloy powder-pigments coated with a semi-conducting corrosion inhibiting oxide and the process for preparing said coated powder-pigments in combination...
8268812 Use of oxazolidinone-quinoline hybrid antibiotics for the treatment of anthrax and other infections  
The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological...
8263632 Aminopyridine derivatives having Aurora A selective inhibitory action  
The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is 0 or CH2; R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl,...
8262938 Active aluminum rich coatings  
Chromate-free corrosion-inhibiting coating compositions comprising film-forming binders and galvanic aluminum alloy powders prepared in an oxygen (oxidizing), nitrogen (inert) or nitrogen-hydrogen...
8247398 Zinc complexes of natural amino acids for treating elevated copper caused toxicities  
The present invention relates to the use of zinc complexes of natural amino acids, especially L-arginine, L-lysine, L-ornithine, and other natural amino acids, in a molar ratio of about 1:2...
8242128 1,3-benzoxazolyl derivatives as kinase inhibitors  
The invention relates to compounds of formula 1, the production and use thereof as a medicament for the treatment of diseases, particularly tumours and/or diseases caused, mediated or propagated...
8236837 Tricyclic compound and pharmaceutical use thereof  
The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof...
8222277 Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use  
The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing...
8217044 Spiroindolinone pyrrolidines  
There are provided compounds of the formula wherein X, Y and R1 to R8 are as described herein and the enantiomers and pharmaceutically acceptable salts and esters thereof which compounds have...
8202861 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...
8173689 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling  
Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions...
8168663 Pharmaceutically acceptable salt of 6-carboxy-2-(3,5 dichlorophenyl)-benzoxazole, and a pharmaceutical composition comprising the salt thereof  
Kinetic stabilization of the native state of transthyretin is an effective mechanism for preventing protein misfolding. Because transthyretin misfolding plays an important role in transthyretin...
8163753 2,3-dihydro-6-nitroimidazo (2,1-b) oxazole compounds for the treatment of tuberculosis  
The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or...
8163785 Pyrazolo[5,1b]oxazole derivatives as CRF-1 receptor antagonists  
There are described 4-difluoromethoxyphenyl pyrazolo[5.1-b]oxazole derivatives of Formula I: which are useful as corticotropin releasing factor (CRF) receptor antagonists and as pharmaceuticals.
8158664 Antimicrobial and radioprotective compounds  
The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which...
8119624 Fused phenyl amido heterocyclic compounds  
The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein:Ring A is (4-12)-membered heterocyclyl;Ring B is a fused benzene ring...
8110589 Ectoparasiticide composition and a method for exterminating extoparasites  
An ectoparasiticide composition for animals including etoxazole as an active ingredient, a UV absorber and a phenol antioxidant, and a method for exterminating ectoparasites using the composition....
8106080 Compositions and methods for enhancing nitric oxide delivery  
The present invention is directed to compounds, combinations, compositions and methods for enhancing nitric oxide (NO) delivery to target sites, and in particular to muscle, both normal and...
8106052 Luminescence-based methods and probes for measuring cytochrome P450 activity  
The present invention provides methods, compositions, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their...
8093241 Acid amide derivatives, process for their production and pesticides containing them  
The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl...
8088760 Benzoxazole carboxamide inhibitors of poly(ADP-ribose)polymerase (PARP)  
A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of...
8080567 EP2 receptor agonists  
A compound of formula (III): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20alkyl group; L′ is a single bond, —O— or —C(═O)—;...
8071593 2-oxo-3-benzylbenzoxazol-2-one derivatives and related compounds as Met kinase inhibitors for the treatment of tumours  
Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein,...