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7585856 |
Resolvins: Biotemplates for novel therapeutic interventions
The present invention is generally drawn to novel isolated therapeutic agents, termed resolvins, generated from the interaction between a dietary omega-3 polyunsaturated fatty acid (PUFA) such as...
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7576072 |
Heterocyclic inhibitors of MEK and methods of use thereof
Disclosed are compounds of the Formula I
and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 and R 9 , W, X, Y and Z are as defined in the specification....
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7514442 |
Trisubstituted 4-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds,...
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7494984 |
Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
The invention encompasses a series of bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the...
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7470695 |
N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds,...
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7452872 |
Formulations and uses of 2-hydroxy-5-phenylazobenzoic acid derivatives
A method of increasing the bioavailability of balsalazide by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of...
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7399760 |
Pyrimidinedione derivatives
Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and...
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7223797 |
Meldonium salts, method of their preparation and pharmaceutical composition on their basis
New salts of Meldonium, the method of their preparation, and pharmaceutical formulation on their basis have been described. The general formula of these salts is X − (CH3)3N+NHCH2CH2COOH where X...
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7214669 |
Tetracycline derivatives and methods of use thereof
A treatment for inhibiting microbial or tumor growth is disclosed, which comprises adding to a subject in need of treatment an effective amount of one or more tetracycline derivatives.
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7169407 |
Carbonyl stress-decreasing agent
The present invention provides agents that decrease carbonyl stress comprising biguanides, such as metoformin. Through oral administration and such, the carbonyl stress-decreasing agents of the...
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7166594 |
Streptogramin derivatives, their preparation and compositions containing them
Group A streptogramin derivatives of general formula (I) in which:
R 1 represents a halogen atom or an azido or thiocyanato radical, R 2 represents a hydrogen atom or a methyl or ethyl...
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7087648 |
Methods for modulating macrophage proliferation using polyamine analogs
Methods for modulating macrophage proliferation in an individual afflicted with or at risk for a macrophage-associated disease are provided. The methods employ a polyamine analog, or salt or...
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7070941 |
Methods and compositions for tagging via azido substrates
The invention provides methods and compositions for azide tagging of biomolecules. In one embodiment of the invention, proteins are tagged by metabolic incorporation of prenylated azido-analog...
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7045495 |
Combination of bryostatin and paclitaxel for treating cancer
This invention provides methods for screening a modulating agent which when combined with antitumor therapeutic agent increases apoptosis in tumor cells. This invention also provides methods for...
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6932985 |
Azide method and composition for controlling deleterious organisms
Disclosed is both a method and composition for controlling deleterious organisms, such as insects, nematodes and weeds by applying a compound comprised of a liquid medium comprising azide and...
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6790841 |
2-hydroxymethylcyclopropylidenemethylpurines and -pyrimidines as antiviral agents
Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of...
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6608048 |
Tricyclic protein kinase inhibitors
This invention provides compounds of Formula (I), where A″, Z, X and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the...
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6593314 |
Neuraminidase inhibitors
The present invention provides compounds of formula Ia and Ib or a pharmaceutically acceptable salt, prodrug, or ester thereof, useful in the inhibition of neuraminidase enzymes from...
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6444638 |
Combinations of PKC inhibitors and therapeutic agents for treating cancers
This invention provides methods for screening a modulating agent which when combined with antitumor therapeutic agent increases apoptosis in tumor cells. This invention also provides methods for...
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6436915 |
Pyrazole compounds
Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle...
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6407081 |
Method for inhibiting cytokine production by cells
The invention concerns a method for inhibiting cytokine production by cells, in particular animal or human cells, and their secretion, which consists in applying on said cells at least an azo...
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6395719 |
Methods for increasing levels of acetylcholine
The present invention is directed to increasing levels of acetylcholine by the administration of 2-aryl-3-aroylbenzo[b]thiophenes.
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6369066 |
Substituted 1,3-oxathiolanes with antiviral properties
This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of the formula (I): wherein; R 1 is hydrogen, and R 2 is cytosine or 5-fluorocytosine; and...
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6297258 |
Substituted 3-cyanoquinolines
This invention provides compounds of formula I having the structure ##STR1## wherein G 1 , G 2 , R 1 , R 4 , Z, n, and X are defined in the specification or a pharmaceutically acceptable salt...
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6297250 |
Pyrimidopyrimidine compounds
A range of dipyridamole analogues useful for inhibiting transport of nucleosides or purines across cell membranes, thereby to potentiate the activity of various cytotoxic antitumor drugs, is...
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6287601 |
Topical nitric oxide donor compositions
Compositions and methods of the topical treatment of equine laminitis are disclosed. In particular, combinations of a fast acting nitric oxide (NO) donor, a sustained acting NO donor and an NSAID...
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6284764 |
Substituted bicyclic derivatives useful as anticancer agents
The invention relates to compounds of the formula 1 ##STR1## and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R 1 , R 3 and R 4 are as defined herein. The invention...
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6271212 |
Prodrug azide compositions and compounds
Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and...
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6251912 |
Substituted quinazoline derivatives
This invention provides compounds of formula 1 having the structure ##STR1## wherein: X, R 1 , R 2 , R 3 , R 4 , Z, X, and n are as defined hereinbefore in the specification, which are useful as...
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6191124 |
Methanol derivatives for treatment of retroviral infections especially HIV infections
The present invention relates to compounds of formula (I) which are imidazo[2,1-b]benzothiazole-3-methanol and imidazo[2,1-b]thiazole-5-methanol derivatives useful for inhibiting a retrovirus in a...
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6140317 |
Pyrrolopyrimidines and processes for their preparation
There are described compounds of formula I ##STR1## wherein R 1 and R 2 are as defined in the description, Q is heterocyclyl boned via a ring nitrogen atom and having the formula IA ##STR2##...
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6113920 |
Pharmaceutical compositions
A pharmaceutical composition and a method of inhibiting human immunodeficiency virus (HIV) is disclosed which comprises administering to an HIV infected patient a homogenous combination of...
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6107291 |
Azepine or larger medium ring derivatives and methods of use
Selected novel azepine and larger medium ring compounds are effective for prophylaxis and treatment of inflammation, tissue degradation and related diseases. The invention encompasses novel...
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6103730 |
Amine substituted compounds
Compounds and pharmaceutical compositions, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, have the formula: CORE MOIETY--(R) j In these...
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6045827 |
Treatment of equine laminitis
Compositions and methods of the topical treatment of equine laminitis are disclosed. In particular, combinations of a fast acting nitric oxide (NO) donor, a sustained acting NO donor and an NSAID...
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6001824 |
Butyryl-tyrosinyl spermine, analogs thereof and methods of preparing and using same
The present invention provides a compound having the structure: ##STR1## wherein R 1 is a saturated or unsaturated linear or branched chain alkyl group, or a cholestanyl group; wherein R 2 is a...
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5958932 |
Substitutes O.sup.6 -benzylguanines, compositions, and methods of using same
The present invention provides AGT inactivating compounds such as substituted O 6 -benzylguanines of the formula ##STR1## wherein, for example, R 1 is amino, hydroxy, or alkylamino, R 2 is...
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5866571 |
9-substituted 2-(2-n-alkoxyphenyl)-purin-6-ones
9-Substituted 2-(2-n-alkoxyphenyl)purin-6-ones are prepared by cyclizing correspondingly substituted imidazoles and derivatizing the purines thus obtained. The 9-substituted 2 ...
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5861405 |
S-substituted 1,3,7-trialkyl-xanthine derivatives
The present invention provides 8-substituted 1,3,7-trialkylxanthines useful as A 2 -selective adenosine receptor antagonists and compositions comprising such compounds. Examples of the...
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5861396 |
Purin-6-one derivatives
Purin-6-one derivatives are prepared by acylating appropriately substituted imidazole carboxamides and then cyclizing to give the purines. The purin-6-one derivatives are suitable as active...
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5856322 |
Unsaturated hydroxyalkylquinoline acids as leukotriene antagonists
Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and...
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5849769 |
N-arylalkyl-N-heteroarylurea and guandine compounds and methods of treating HIV infection
A method for treating HIV which comprises a compound of the formula ##STR1## wherein A is ##STR2## and Z i is O, Se, NR a or C(R a ) 2 , and Z ii is --O or (O) 2 ; wherein R 1 , R 2 ,...
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5807861 |
Amine substituted xanthinyl compounds
A method for treating a disease caused by an undesirable cell response mediated by a proliferative intracellular signaling pathway is provided wherein an effective amount of a compound is...
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5770595 |
Oxime substituted therapeutic compounds
Oxime-substituted compounds are preferably cyclic or heterocyclic compounds. The oxime-substituted compounds and pharmaceutical compositions thereof have the formula: CORE MOIETY--(R) j including...
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5728687 |
Antitumour compositions containing taxane derivatives
Pharmaceutical compositions having therapeutic synergy comprising taxol or Taxotere or analogues thereof combined with at least one therapeutically useful substance for treating neoplastic diseases.
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5710160 |
Diphenyl pyridyl ethane derivatives as PDE IV inhibitors
The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the...
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5616578 |
Method of treating human immunodeficiency virus infection using a cyclic protease inhibitor in combination with a reverse transcriptase inhibitor
This invention relates to a method of treating human immunodeficiency virus (HIV) infection in a mammal comprising administering to the mammal a therapeutically effective amount of a combination...
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5491146 |
Hydroxylated erythro-hydroxynonyladenines and related analogs
This invention discloses various analogs of erythro-hydroxynonyladenine (EHNA) which have been modified by the addition of hydroxy groups or other moieties at the #8 or #9 carbon atoms of the...
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5420122 |
3-pyrrolidinylthio-1-azabicyclo-[3.2.0]hept-2-ene-2-carboxylic acid compounds
Novel 3-pyrrolidinylthio-1-azabicyclo[3.2.0]hept-2-ene-2-carboxyli
c acid compounds and processes for their preparation are disclosed. These novel compounds have antimicrobial activity, and are...
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5387747 |
Triazolopyrimidine derivatives which are angiotensin II receptor antagonists, their methods of preparation and pharmaceutical compositions in which they are present
The present invention relates to the derivatives of the formula ##STR1## and their tautomeric forms, as well as their addition salts, and to their use in therapeutics, especially for the treatment...
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