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7615569 |
Inhibitors of ion channels
Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly,...
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7615542 |
Dioxolane thymine and combinations for use against 3TC/AZT resistant strains of HIV
The present invention relates to the use of a dioxolane thymine compound according to the chemical structure of Formula (I): where R 1 is H, an acyl group, a C 1 -C 20 alkyl or ether group, a...
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7612093 |
Compositions of treating hepatitis virus infections with N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination therapy
Provided are methods and compositions for treating hepatitis virus infections in mammals, especially humans. The methods comprise (1) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol...
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7608618 |
Urea or thiourea substituted 1,4-pyrazine compounds useful as anti-cancer agents and for inhibiting Chk1
Compounds of the formula
wherein: Y′ is O or S, W′ is
optionally substituted,
Z′ is selected from the group consisting of
wherein Q′ is OR 7 and R 7 is C 1-3 alkyleneC 3-8...
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7605137 |
Combination therapy comprising cloretazine
This invention provides a method for treating tumor in a subject comprising administering to the subject an effective amount of: (1) VNP40101M, or its equivalent; and (2) a nucleoside, or a...
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7601730 |
Carboxylic acid derivatives, their preparation and use
Carboxylic acid derivatives
where R—R 6 , X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling...
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7592353 |
Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
Disclosed are compounds of formula (I):
wherein R 1 and R 4 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are...
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7582647 |
Carboxylic acid derivatives, their preparation and use
Carboxylic acid derivatives
where R—R 6 , X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling...
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7569575 |
Synthesis of locked nucleic acid derivatives
The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α- L -oxy-LNA, amino-LNA, α- L -amino-LNA, thio-LNA, α- L -thio-LNA, seleno-LNA and...
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7566724 |
Glycine derivative and use thereof
The compounds of the disclosure, for example, the compound represented by the formula:
has excellent therapeutic and prophylactic effects against inflammatory bowel disease. Further, they are...
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7563788 |
Substituted Imidazo[1,2-a]pyridines as Antibacterial Agents
Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable...
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7560483 |
Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require...
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7560467 |
Indazolo-tetrahydropyrimidine-carboxamide derivative kinase inhibitors
The present invention relates to indazolo-tetrahydropyrimidine-carboxamide derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such...
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7557138 |
5-phenoxyalkoxypsoralens and methods for selective inhibition of the voltage gated Kv1.3 potassium channel
Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects,...
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7544692 |
Polymorphic and other crystalline forms of cis-FTC
Solid phases of (−)-cis-FTC, which are designated herein as amorphous (−)-FTC and Forms II and III (−)-cis-FTC) are provided that can be distinguished from Form I (−)-cis-FTC by X-ray...
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7531536 |
Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula IIIa:
wherein R 1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl,...
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7528142 |
Aminopyrimidines useful as kinase inhibitors
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of...
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7517889 |
2,6-substituted-4-monosubstitutedamino-pyrimidine as prostaglandin D2 receptor antagonists
The present invention is directed to a compound of Formula (I)
wherein Cy 1 , Cy 2 , L 1 , L 2 , and R 1 are as defined herein, a pharmaceutical composition comprising a pharmaceutically...
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7511051 |
Cidofovir peptide conjugates as prodrugs
Cidofovir-based compounds having an amino acid, dipeptide or tripeptide attached to a cidofovir or cyclic cidofovir framework. The compounds show enhanced oral bioavailability and increased binding...
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7511027 |
Method of treating hepatitis delta virus infection
A method for the treatment for hepatitis delta infection in a host, that includes administering an effective amount of a nucleoside or a nucleoside analog that suppresses the expression of the...
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7495006 |
2′ and 3′-substituted cyclobutyl nucleoside analogs for the treatment of viral infections and abnormal cellular proliferation
Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and...
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7482439 |
Caprazene as novel compound and derivatives thereof, and caprazol as novel compound and derivatives thereof
Caprazene and caprazol could be synthesized by hydrolysis of a caprazamycin. There could be synthesized a caprazene-1′″-amide derivative of the formula (II)
and a caprazene-1′″-ester...
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7482356 |
Bicyclic pyrazolone cytokine inhibitors
The present invention relates to 6,7-dihydro-5H-pyrazolo[1,2α]pyrazol-1-ones which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or...
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7482355 |
Pyrimidine derivatives as modulators of chemokine receptor activity
Compounds of formula (1), pharmaceutically acceptable salts, solvates and in vivo hydrolysable esters thereof, have activity as pharmaceuticals, in particular as modulators of chemokine receptor...
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7473695 |
4-imidazolin-2-one compounds
The present invention relates to a compound of the formula [I]:
wherein G 1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula:
...
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7470686 |
Method of inhibiting the expression and/or the activity of JNK
The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said...
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7470672 |
Compositions and methods of reducing tissue levels of drugs when given as orotate derivatives
This invention is in the field of chemical restructuring of pharmaceutical agents known to cause tissue toxicity as a side effect, by producing their orotate derivatives. More particularly, it...
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7465736 |
Azole methylidene cyanide derivatives and their use as protein kinase modulators
An azole derivative of formula (I)
a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of...
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7465735 |
5-Phenypyrimidines their preparation compositions comprising them and their use
5-Phenylpyrimidines, their preparation, compositions comprising them and their use 5-Phenylpyrimidines of the formula I
in which the substituents and the index are as defined below:
R 1 ,R 2 ...
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7452898 |
Phosphonate compounds
The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and...
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7452879 |
Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms...
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7419983 |
Gonadotropin-releasing hormone receptor antagonists and methods related thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ...
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7402588 |
Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of...
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7378446 |
Compound having anti-HCV activity and process for producing the same
The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its...
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7368456 |
Methods, compositions, and kits for organ protection during systemic anticancer therapy
Methods, compositions, and kits are presented for local tissue protection during systemic administration of anticancer therapeutic agents.
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7368455 |
6,7-Dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines
The present invention relates to 2-(4-fluorophenyl)-3-(2-phenoxy-pyrimidin-4-yl)-6,7-dihydro-
5H-pyrazolo-[1,2-a]pyrazol-1-one, including all enantiomeric and diasteriomeric forms and...
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7364752 |
Solid dispersion pharamaceutical formulations
A pharmaceutical composition is disclosed which comprises a solid dispersion of an HIV protease inhibitor in a water soluble carrier, such as PEG, having enhanced bioavailability and improved...
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7361654 |
Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity...
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7358239 |
Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z...
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7354928 |
Small molecule inhibitors targeted at Bcl-2
The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-X L . In particular, the present invention provides non-peptide cell permeable small...
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7345046 |
Heteroaryl-fused pyrimidinyl compounds as anticancer agents
Heteroaryl-fused pyrimidinyl compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the...
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7345039 |
Enhancement of effectiveness of 5-fluorouracil in treatment of tumor metastases and cancer
Tumor growth and metastases in cancer patients are inhibited by administration of a combination therapy including effective amounts of 5-Fluorouracil and a methylol transfer agent such as...
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7335657 |
Cytokine inhibitors
Disclosed are compounds of formula (I)
Where Ar 1 , X, Y, Q, W, R 3 , R 4 , R 5 , R 6 and R y are defined herein. The compounds of the invention inhibit production of cytokines involved in...
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7317014 |
Bio-active pyrimidine molecules
The present invention relates to novel derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their...
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7312209 |
Acridone inhibitors of IMPDH enzyme
Compounds having the formula (I),
wherein R 3 is selected from H, OH and NH 2 ; R 30 is selected from ═O and ═S; W is —C(═O)—, —S(═O)—, or —S(O) 2 —; or W may be —CH 2...
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7294627 |
Chemical compounds
Compounds of formula (I)
in which R 1 , R 2 , R 3 and R 4 , have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.
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7291642 |
Bradykinin-B1 antagonists, process for their preparation and their use as medicaments
The present invention provides bradykinin-B1 antagonists of the formula
in which A, Ar, G, Q, R 1 and R 4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and...
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7288544 |
Pyrimidine compounds useful as N-type calcium channel antagonists
Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when...
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7273862 |
Aminoalkyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z...
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7265115 |
Diazabicyclic CNS active agents
Compounds of formula I:
or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.
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