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7615563 |
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...
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7601744 |
Benzothiadiazolylphenylalkylamine derivatives and methods of their use
The present invention is directed to benzothiadiazolylphenylalkylamine derivatives of formula I:
or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and...
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7585882 |
Phosphodiesterase 4 inhibitors
Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I:
wherein R 1 , R 2 ,...
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7576109 |
1,3,4-oxadiazol-2-ones as PPAR delta modulators and their use thereof
The present invention is directed to 1,3,4-oxadiazolones, compounds of formula I and their pharmaceutically acceptable salts stereoisomers, tautomers, or solvates thereof. Novel compounds include...
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7572820 |
Chemical compounds
This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.
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7553973 |
Pharmaceutical compounds
The instant invention provides compounds of Formula Ia which are leukotriene biosynthesis inhibitors.
Compounds of Formula Ia are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic,...
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7531561 |
GSK-3 inhibitors
Provided are thiadiazolidine compounds of formula I
wherein R 1 is an organic group having at least 8 atoms selected from C or O, which is not linked directly to the N through a —C(O)— and...
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7514459 |
Gamma-secretase inhibitors
Compounds of formula I:
are potent inhibitors of gamma-secretase and hence find use in treatment or prevention of diseases associated with deposition of β-amyloid.
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7465718 |
Ansamycins having improved pharmacological and biological properties
Ansamycins and methods of preparing and using the same are described. At least some of these ansamycins exhibit one or more of improved aqueous formulation ability, chemical stability, and...
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7459473 |
N-linked sulfonamides of N-heterocyclic carboxylic acids or carboxylic acid isosteres
This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including...
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7439242 |
PPARγ modulators
Modulators of PPARγ activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.
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7432293 |
Heterocyclic compounds useful as Nurr-1 activators
The present invention relates to compounds of formula (I): wherein R 1 is hydroxy, C 1-4 alkoxy, amino, C 1-4 alkyl-amino, di C 1-4 alkylamino, benzyloxy or C 2 -C 7 alkanoyl, R 2 is C 1-4 ...
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7419991 |
3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid, compositions, and methods for the use thereof
Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of...
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7402606 |
Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss
Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The...
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7399765 |
Substituted diazabicycloalkane derivatives
Compounds of formula (I)
Z-Ar 1 —Ar 2 (I)
wherein Z is a diazabicyclic...
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7393869 |
Methods of using thiazolidine derivatives to treat cancer or inflammation
Methods of using thiazolidine derivatives of formula (I) to treat cancer, inflammation, or other disorders related to the activities of protein phosphatases PTPN12 or PTPN2 in a mammal are...
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7388006 |
Non-steroidal progesting
The present invention relates to non-steroidal progestins of the general formula (I)
wherein
R 1 and R 2 are independently of each other —H or —F, R 3 is —CH 3 or —CF 3 , and Ar is...
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7378448 |
Diphenylether amide derivatives as opioid receptor antagonists
A compound of the formula (I) wherein the variables X 1 , X 2 , B, D, R 1 to R 7 including R 3′ , p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer,...
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7375123 |
1,2,4-thiadiazole derivatives as melanocortin receptor modulators
The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention...
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7371746 |
1,2,4-Thiadiazole compounds and pests controlling composition containing the same
The present invention relates to a 1,2,4-thiadiazole compound of the formula (I) represented by the formula (1): wherein R 1? represents C3-C7 alkynyl and X represents C4-C7 straight alkylene...
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7365047 |
Use of pentagastrin to inhibit gastric acid secretion or as a diuretic
This invention pertains to the discovery that pentagastrin, when administered in conjunction with a proton pump inhibitor (PPI) is synergistic with the PPI and significantly increases the efficacy...
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7361675 |
1,2,4-thiadiazole compounds and use thereof
1,2,4-Thiadiazole compounds represented by the formula (1) have excellent control activities against harmful arthropods:
wherein R 1 represents C3-C7 alkynyl group optionally substituted one...
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7345095 |
Sulfonamide compounds for the treatment of neurodegenerative disorders
The present invention relates to compounds of the Formula I
wherein R 1 , R 2 , R 3 , m, and n are as defined. Compounds of the Formula I have activity inhibiting production of Aβ-peptide. The...
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7342039 |
Substituted indole oximes
The present invention relates to substituted indole oximes and methods of using them.
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7342031 |
Thiadiazole compound and use thereof
The thiadiazole compound represented by the formula (A):
wherein R 1 represents a C1-C7 alkyl group, a C3-C7 alkenyl group, a C3-C7 alkynyl group and the like; R2 represents a C1-C4 alkyl...
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7338956 |
Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals
The present invention relates to acylamino-substituted heteroaromatic compounds of formula I,
wherein R 1 , R 2 , R 3 , R 4 and R 5 and X are as defined herein, to pharmaceutical compositions...
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7319107 |
1,2,4-thiadiazolium derivatives as melanocortin receptor modulators
The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present...
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7288556 |
Antiproliferative 1,2,3-thiadiazole compounds
This invention is directed to methods of using compounds having the structure:
and including stereoisomers, solvates, and pharmaceutically acceptable salts thereof, wherein each of R 1 , R 2 ,...
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7285554 |
Pyrazole derivative
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in...
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7273879 |
Thiadiazole compounds and use thereof
A thiadiazole compound of the formula (A):
wherein R 1 represents methyl, C3-C7 alkenyl, C2-C7 alkoxyalkyl, C2-C7 alkylthioalkyl, C4-C7 alkoxyalkoxyalkyl, C4-C7 alkylthioalkoxyalkyl, phenyl...
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7241759 |
Benzo[1,2,5]thiadiazole compounds
Certain amidophenyl-sulfanylamino-benzo[1,2,5]thiadiazole compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
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7214701 |
Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising
(a) compounds of the formula (I)
in which W, X, Y, Z, A, B, D and G...
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7205321 |
Peroxisome proliferator activated receptor alpha agonists
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is selected from the group...
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7186738 |
Antibacterial oxalidinones
Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl,...
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7183299 |
Tetrazoyl oxime derivative and agricultural chemical containing the same as active ingredient
The present invention provides a tetrazoyloxime derivative which is less likely to cause chemical injury to useful plants and is also superior in chemical efficacy to a conventional hetero...
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7166622 |
Substituted phenylsulfonamide inhibitors of beta amyloid production
Compounds of Formula I,
wherein R 1 –R 8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these...
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7157482 |
Antibacterial 1,3-oxazolidin-2-one derivatives
Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N—HET is for example triazolyl substituted with R 1 ; R 1 is for example...
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7157476 |
Aminofurazan compounds useful as protein kinase inhibitors
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
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7157079 |
Combined tumor suppressor gene therapy and chemotherapy in the treatment of neoplasms
In one embodiment, this invention provides methods of treating mammalian cancer or hyperproliferative cells, said method comprising contacting said cells with a tumor suppressor protein or tumor...
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7157078 |
Devices and methods for eliminating termite colonies
This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing
a) a termiticide selected...
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7144911 |
Anti-inflammatory medicaments
Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein...
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7144899 |
Thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure Formula (I): wherein u is CH or N; Q is 1)—N(R 25 )CH(R 30 )—...
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7141591 |
1,2,4-oxadiazole derivatives as hPPAR alpha agonists
A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof wherein: X 1 is O or S; X 2 is O or S; n is 1–3, One of Y and Z is N, and the other is...
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7115612 |
Arylsulfonamides as antiviral agents
The present invention relates to novel sulphonamides of the general formula (I)
in which the substituents R 1 , R 2 , R 3 , R 4 and A and X are as defined in claim 1 and other claims, and...
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7105556 |
Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure
wherein Q is C or N, X 1 is C or N, and R 1 , R 2 , R 2a , R 2b , R 2c , R 3 , Y, A, m, n, X 2 , X 3 and X 4 are as defined herein, which...
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7049331 |
1,2,4-thiadiazole derivatives as melanocortin receptor modulators
The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention...
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7045532 |
ACE-2 modulating compounds and methods of use thereof
ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include...
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7037914 |
Carboxylic acid derivative and a pharmaceutical composition containing the derivative as active ingredient
A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I)
(wherein all symbols are as defined in the specification), a non-toxic acid...
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7030119 |
Method for treating chronic pain using MEK inhibitors
The invention features a method for treating chronic pain using a compound of formula (I).
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7012085 |
1,3 disubstituted pyrrolidines as α-2-adrenoceptor antagonists
The invention provides compounds of formula (I) wherein R 0 , R 1 , R 2 and A are as defined in the description, and the preparation thereof. The compounds of formula (I) have high affinity as α...
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