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6777418 |
Retinoid compounds (I)
The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical...
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6762182 |
Converting cox inhibition compounds that are not COX-2 selective inhibitors to derivatives that are COX-2 selective inhibitors
A method of altering specificity of cyclooxygenase-inhibiting compounds that have a COOH moiety by changing the various COOH containing compounds, such as indomethacin, into ester derivatives or...
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6743817 |
Substituted fused pyrroleimines and pyrazoleimines
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R 1 and R 2 are defined herein. These compounds are highly selective agonists,...
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6743811 |
Oxazalidinone compounds and methods of preparation and use thereof
Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising...
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6740647 |
Thrombin inhibitors
Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein....
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6716841 |
Nitrogen containing heterobicycles as factor Xa inhibitors
This invention relates generally to nitrogen containing heterobicycles of formulas A and B: which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical...
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6713498 |
Method for treating glaucoma VI
Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the...
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6686363 |
Cyclopropyl containing oxazolidinone antibiotics and derivatives thereof
This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and...
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6673820 |
Aminoheterocyclylamides as pesticides and antiparasitic agents
The invention relates to novel compounds of the general formula: in which R 1 is hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkyl or unsubstituted or mono- to...
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6653309 |
Inhibitors of IMPDH enzyme technical field of the invention
The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions...
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6649649 |
Method of treating colonic adenomas
This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a...
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6605631 |
Ortho-substituted 2-methoxyiminophenyl-N-methylacetamides
Compounds of the general formula I where the index and the substituents have the following meanings: n is 0 or 1 to 4; X is O or S; Y is a five-membered heteroaromatic ring; R 1 is nitro;...
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6558685 |
Method for treating wood against the attack of harmful fungi
A multi-phase suspoemulsion containing as essential components a) 1 to 50% by weight of particular fungicidal benzimidazoles or precursors liberating them as microsuspended solids particles, b) 5...
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6555576 |
Method for treating exercise induced asthma
Methods of treating exercise-induced asthma using a PDE-4 inhibitor are disclosed.
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6555563 |
Heteroaryl substituted amidinyl and imidazolyl compounds and methods employing same for the treatment of inflammation
In accordance with the present invention, there are provided compounds and pharmaceutical compositions useful for the selective inhibition of COX-2 in the presence of COX-1. As a result, invention...
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6552031 |
Synergistic analgesic combination of oxycodone and rofecoxib
Disclosed is a pharmaceutical composition, comprising a combination of a dose of rofecoxib or a pharmaceutically acceptable salt thereof and a dose of oxcodone or a pharmaceutically acceptable salt...
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6552053 |
Controlling attention and memory by altering neuronal carbonic anhydrase activity
The invention provides a method for modulating attentive cognition comprising administering a compound that alters intraneuronal carbonic anhydrase activity thereby affecting establishment of a...
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6537549 |
Cytokine antagonists for the treatment of localized disorders
Cytokine antagonists for use in localized clinical disorders are provided for the treatment and prevention of damage to the optic nerve, other cranial nerves, spinal cord, nerve roots, peripheral...
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6506738 |
Benzimidazolone antiviral agents
The present invention concerns antiviral compounds, their compositions, and use in the treatment of viral infections. More particularly, the invention provides benzimidazolone derivatives for the...
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6506781 |
Oxazole PPAR antagonist
A method is disclosed for rational design of a PPAR, FXR, LXR-alpha, or LXR-beta antagonist comprising chemical modification of a PPAR, FXR, LXR-alpha, or LXR-beta agonist to: a) prevent formation...
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6495551 |
Substituted phenyloxazolidinones and their use as antibiotics
The invention concerns compounds of formula (I), wherein, for example, R 1 is of the formula —NHC(═O)R a wherein R a is (1-4C)alkyl; R 2 and R 3 are independently hydrogen or fluoro; R...
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6492421 |
Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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6472406 |
Sulfonamidomethyl phosphonate inhibitors of beta-lactamase
The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel β-lactamase...
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6469032 |
3-(4′-bromobenzylindenyl)-2-indolinone and analogues thereof for the treatment of disease
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
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6469036 |
Peptidyl heterocyclic ketones useful as tryptase inhibitors
The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment...
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6451828 |
Selective inhibition of glutaminase by bis-thiadiazoles
Compounds are disclosed which efficiently inhibit glutaminase but which have no effect, at higher levels, on various mechanistically and functionally related enzymes. The compounds, which are...
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6441005 |
Oxazolidinone compounds and compositions, and methods of using the same
Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising...
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6436971 |
Use of PDE 4-specific inhibitors to reduce the severity of a bacterial infection after a respiratory viral infection
This invention relates to a method for the prophylaxis of or reducing the severity of post-viral bacterial infection by administering a PDE 4-specific inhibitor prior to or during the course of a...
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6419934 |
TNF modulators for treating neurological disorders associated with viral infection
A method for inhibiting the action of TNF for treating neurological conditions in a human by administering a TNF antagonist for reducing the inflammation of neuronal tissue of said human, or for...
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6369108 |
Method for treating COPD
A method for treating COPD is disclosed comprising administering compounds of Formula (I) wherein the terms R 1 , R 3 , X, X 2 and Z are herein defined.
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6358942 |
Phenyloxazolidinones having a c-c bond 4-8 membered heterocyclic rings
A compound of Formula (I): or pharmaceutical acceptable salts thereof wherein X is NR 1 ; R 1 is H, C 1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R 1 is —(CH 2 ) h...
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6352985 |
Benzimidazole compounds
A benzimidazole compound represented by the formula (I): wherein R 3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl...
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6348032 |
Method of inhibiting neoplastic cells with benzimidazole derivatives
A method for inhibiting neoplasia, particularly cancerous and precancerous lesions by exposing the affected cells to benzimidazole derivatives.
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6339100 |
Methods for inhibiting mastocytosis
A method of preventing or treating in a subject mastocytosis which comprises administering to the subject a therapeutically effective amount of a compound having the structure: or a...
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6329373 |
Metalloproteinase inhibitors
A compound of formula (I) ##STR1## wherein X is a --CONHOH group and the R groups are defined in the claims. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation...
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6319933 |
Azole derivatives
The present invention is directed to new 1-(1H-1,2,4-triazol-1-yl)butan-2-ol derivatives of the formula (I), ##STR1## and pharmaceutically acceptable salts thereof wherein Q, R, X, Y and Z are the...
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6316441 |
Brinzolamide and brimonidine for treating glaucoma
Methods and compositions for treating ocular conditions which find their etiology in compromised ocular blood flow with brinzolamide and brimonidine are disclosed.
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6306890 |
Esters derived from indolealkanols and novel amides derived from indolealkylamides that are selective COX-2 inhibitors
A compound of the formula ##STR1## where: n, and X are as defined in the specification, and the compound possesses selectivity for inhibition of cyclooxygenase-2.
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6288061 |
Imidazole derivatives
The present invention relates to the imidazole derivative of the following formula (I) ##STR1## wherein R 1 is hydrogen, optionally substituted alkyl and the like, R 2 is hydrogen, optionally...
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6258851 |
Metalloproteinase inhibitors
Compounds of formula (I), wherein A, B, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 are as defined in the specification, are matrix metalloproteinase inhibitors. ##STR1##
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6242442 |
Brinzolamide and brimonidine for treating ocular conditions
Methods and compositions for treating ocular conditions which find their etiology in compromised ocular blood flow with brinzolamide and brimonidine are disclosed.
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6239175 |
Carbamoyloxy derivatives of mutiline and their use as antibacterials
Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R 1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is...
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6235762 |
2-aryl-Δ2-1,3,4-(oxa and thia)diazoline insecticidal and acaricidal agents
The present invention relates to 2-aryl-Δ 2 -1,3,4-(oxa and thia)diazoline compounds having the structural formula ##STR1## and compositions and methods comprising those compounds for the control...
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6225329 |
Modulators of protein tyrosine phosphatases (PTPases)
The present invention provides novel compounds of Formula 1, compositions containing these compounds, methods of their use, and methods of their manufacture, where such compounds are...
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6225327 |
Compounds which inhibit human conjunctival mast cell degranulation for treating ocular allergic-type complications
Composition and methods for treating ocular allergic reactions are disclosed. In particular, the invention is directed to compounds which inhibit human conjunctival mast cell degranulation.
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6211197 |
Prostaglandin receptor ligands
Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed. The compounds are represented by formula II: Ar 1 --W--Ar 2 ...
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6211209 |
Method of inhibiting connective tissue degradation
The present invention provides a method of inhibiting connective tissue degradation that comprises administering to a patient having a condition in which connective tissue is degraded a...
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6194418 |
Substituted aminosalicyclic acid amides with fungicidal effect and intermediate products for production thereof
The invention relates to novel substituted aminosalicylamides, to a plurality of processes for their preparation and to their use as fungicides, and also to novel intermediates and to a plurality...
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6191152 |
2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives having an effect on the C.N.S. and the heart
The invention refers to novel 2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives of formula (I) having an influence on the heart and the central nervous system, furthermore pharmaceutical...
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6187799 |
Inhibition of raf kinase activity using aryl ureas
Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
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