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6924305 |
Diazocine derivatives and their use as tryptase inhibitors
Compounds of the formula I, in which B1, B2, R1, R2, R6, R7, K1 and K2 are as defined in the description are novel effective tryp-tase inhibitors.
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6916831 |
Flavone acetic acid analogs and methods of use thereof
Compounds are described having a structure according to Formula I or Formula II:
wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O...
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6908732 |
Compounds and methods for regulating cell differentiation
The present invention makes available methods and reagents for inhibiting cell growth or promoting cell differentiation comprising contacting the cell with a differeguline in a sufficient amount to...
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6906098 |
Mixed steroidal 1,2,4,5-tetraoxane compounds and methods of making and using thereof
Disclosed herein are mixed steroidal tetraoxanes having the following structural formula 1
wherein n is 0, 1, 2, or 3; R is H; ethanoyl, propanoyl, or benzoyl; R1 is H, methyl, ethyl, or...
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6903129 |
D-proline prodrugs
The invention relates to compounds of formulas
wherein
R 1 and R 2 are independently from each other lower alkoxy, lower alkenyloxy, benzyloxy, hydroxy, —OCH(CH 3 )OC(O)-lower alkyl or...
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6903116 |
Methods of treating cancer using a heat shock factor activity inhibitor
A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an...
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6903131 |
3,4-di-substituted maleimide compounds as CXC chemokine receptor antagonists
Disclosed are compounds of the formula (I)
or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the treatment of chemokine-mediated diseases such as acute and...
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6900227 |
Benzodioxole derivatives
The present invention relates to compounds of the general formula
and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases such...
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6897211 |
Thienodibenzoazulene compounds as tumor necrosis factor inhibitors
The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-α) and...
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6894072 |
Compounds as NS3-serine protease inhibitors of hepatitis C virus
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses...
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6890928 |
Aromatic sulfone hydroxamic acids and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix...
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6887888 |
Soluble compositions of triphenylethylene antiestrogens
Aqueous compositions of nonsteroidal triphenylethylene antiestrogens for pharmaceutical use comprising as a solubility enhancing agent a pharmaceutically acceptable mono- or dicarboxylic acid...
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6887893 |
Methods and compositions for treatment and prevention of tumors, tumor-related disorders and cachexia
Certain cyclooxygenase-2 inhibitors are useful for the treatment and prevention of tumors and tumor-related disorders and cachexia.
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6881733 |
Serotonergic benzofurans
The present invention provides serotonergic benzofurans of Formula (I): where A, R, R 1 , R 2 , R 3 , and R 4 are as described in the specification.
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6878733 |
Formulations for pharmaceutical agents ionizable as free acids or free bases
The present invention features formulations of indolinones which compounds are ionizable as free acids or free bases. The formulation is suitable for parenteral or oral administration, wherein the...
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6872735 |
LFA-1 antagonist compounds
The invention relates to novel compounds having formula (I)
wherein Cy, X, Y, L and R 1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte...
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6867230 |
Hygromycin A derivatives
This invention relates to compounds of the formula
and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R 1 , R 2 , R 3 and R 10 are as defined herein. The...
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6864270 |
Iron binding agents
Composition, article of manufacture for and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a...
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6858227 |
Vitamin E conjugates
Vitamin E conjugates, methods for their preparation, and compositions that include the conjugates. The vitamin E conjugates include a tocopherol moiety covalently coupled through a linker moiety to...
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6852752 |
Urea compounds, compositions and methods of use and preparation
Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptide deformylase (PDF), an enzyme present in prokaryotes and are therefore useful as antimicrobials and antibiotics....
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6852713 |
Lactam derivatives and methods of their use
Lactam derivatives of the general formula
are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.
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6849639 |
Integrin inhibitors and their methods of use
The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated...
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6849622 |
Aliphatic nitrogenous five-membered ring compounds
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]:
wherein
A represents —CH 2 — or —S—, R 1 ...
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6846817 |
Nicotine receptor ligands
The invention provides nicotine receptor agonists of formula I:
wherein R 1 , x, y, and n have any of the values given in the specification, or a pharmaceutically acceptable salt thereof, as...
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6844336 |
4-fluoroalkyl-2h-benzopyrans with anti-estogenic activity
This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I,
in which
Z is a straight-chain or branched-chain alkyl group with up to 5 carbon atoms that is...
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6844346 |
Chromogenic substrates of sialidase and methods of making and using the same
The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and...
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6841576 |
Anti-hypertensive composition and methods of treatment
Pharmaceutical compositions for the treatment of hypertension comprising an effective anti-hypertensive amount of at least one compound in association with a pharmaceutically acceptable,...
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6838478 |
Amino acid derivatives and their use as thrombin inhibitors
There is provided compounds of formula I,
wherein R 1 , R 2 , R 3 , R x , Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like...
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6838477 |
Lactacystin analogs
Described herein are compounds related to lactacystin and lactacystin β-lactone, pharmaceutical compositions containing the compounds, and methods of use.
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6838479 |
Amidine inhibitors of serine proteases
Inhibitors of serine proteases are provided having formula (I)
wherein X, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. In particular, the compounds bind to factor VIIa, tissue...
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6835742 |
Synergistic effect of amlodipine and atorvastatin on cholesterol crystal formation inhibition and aortic endothelial cell nitric oxide release
The combination of the antihypertensive calcium channel blocker amlodipine and lipid-lowering agent atorvastatin inhibits free cholesterol crystallization in atherosclerotic-like membranes. In...
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6835726 |
Pyrimidine derivatives
Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.
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6828318 |
2-adamantylethylamines and their use in the treatment of conditions generally associated with abnormalities in glutamatergic transmission
Compounds of formula (1): wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are independently selected from hydrogen, alkyl, aryl and non-aromatic heterocyclic groups, or each of one or more pair(s)...
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6825217 |
Carbinols for the treatment of neuropathic dysfunction
Compositions and methods are provided for treating neuropathic pain or neuropathic dysfunction that include the administration of an effective amount of a defined carbinol or a pharmaceutically...
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6825228 |
Benzothiophene compounds having antiinfective activity
Benzothiophene compounds such as are DNA binding compounds exhibiting antibacterial activity.
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6803370 |
Alpha amino acid derivatives—inhibitors of leukocyte adhesion mediated by VLA-4
Disclosed are certain alpha amino acid compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such...
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6790463 |
Uses of targeted oxidative therapeutic formulation in arteriosclerosis
The use of a pharmaceutical formulation in treating coronary arteriosclerosis and a two-component pharmaceutical formulation. The pharmaceutical formulation contains peroxidic species or reaction...
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6787559 |
Sulfonamide compounds
This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for...
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6784167 |
17-beta-hydroxysteroid dehydrogenase-II inhibitors
17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R 4 )(R 6 )Y are oriented cis to each other; W represents O...
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6784173 |
Aromatic dicarboxylic acid derivatives
Compounds of formula I wherein A, R 1 and R 2 are defined in the specification. These compounds are useful as HDAC inhibitors. Also disclosed are methods of making and using said compounds.
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6777433 |
Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates
The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods...
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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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6759412 |
Acylated 6,7,8,9-tetrahydro-5H-benzocycloheptenyl amines and their use as pharmaceutical agents
The present invention relates to compounds according to the general formula (I), wherein R 1 -R 4 have the meanings given in the description, A is CH 2 , CHOH or CH—(C 1 -C 3 -alkyl), B, C...
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6756396 |
Ethylene glycol esters as photoactive agents
New compounds useful in photodynamic therapy are of the formula and their 1,4-diene isomers and the metallated and/or labeled and/or conjugated forms thereof wherein each R 1 is independently...
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6750213 |
Estrogen receptor modulators
The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen...
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6747054 |
EP4 receptor selective agonists in the treatment of osteoporosis
This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I, wherein R 2 , X, Z and Q are as defined in the specification. This invention is also directed to...
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6743810 |
Indol-3-yl derivatives
Indol-3-yl derivatives of the general formula I in which A, B, X, R 1 , R 2 , R 3 , R 4 , R 5 , n and m are as defined in patent claim 1 , and their physiologically acceptable salts or solvates...
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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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6734204 |
Serotonin potentiation by oleamide analogs
Analogs related to oleamide are employed for potentiating the 5-HT 2A and 5-HT 1A responses to serotonin (5-HT). With respect to the potentiation of the 5-HT 2A receptor response, it is...
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6734206 |
3-oxa-8-azaprostaglandin analogs as agents for lowering intraocular pressure
The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective...
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