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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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6486136 |
Combinations comprising VX478, zidovudine and/or 1592U89 for use in the treatment of HIV
The present invention relates to therapeutic combinations of [3R*(1R*,2S*)]-[3[[(4-aminophenyl)sulphonyl](2-methylpropyl)
-amino]-2-hydroxy-1-phenylmethyl)propyl]carbamic acid, tetrahydro-3-furanyl...
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6479500 |
Agents for alleviating side effects
The present invention provides an agent for alleviating side effects caused by use of an anti-tumor agent, which contains 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimid
i nedione (1)...
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6465484 |
Angiogenesis inhibitors
The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to...
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6465476 |
Immuno-modulator exhibiting antimicrobial and anti-mycrobacterial activities, method for producing the same and pharmaceutical preparation
The present invention pertains to the field of medicine and more precisely relates to a novel immuno-modulator of the following formula which exhibits anti-microbial and anti-mycobacterial...
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6462017 |
Method of reducing side effects of chemotherapy in cancer patients
A method for reducing the severity of chemotherapy side effects in cancer patients by administering thymosin α 1 in conjunction with the administration of a chemotherapy agent to the patient. As...
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6448256 |
Antibiotic prodrugs
The invention relates to prodrugs of N-substituted derivatives of 6-aminouracils, 6-aminoisocytosines, guanines, and 2-aminoadenines. The N-linked substituents include an ester group that is...
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6440984 |
Use of aryl-substituted pyrimidines as insecticidal and acaricidal agents
There are provided compositions and methods comprising compounds of formula I: wherein R 1 , A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.
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6436949 |
Heterocyclically substituted benzamides and their use
Heterocyclically substituted benzamides of the formula I are described, where R 1 , R 2 , R 3 , R 4 , R 5 , X, m and n have the meanings given in the description. The novel compounds are useful...
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6436989 |
Prodrugs of aspartyl protease inhibitors
The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl...
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6436948 |
Method for the treatment of psoriasis and genital warts
The present invention relates to the use of prodrug forms of (−)-(2S,4S)-1-(2-hydroxymethyl-1,3-dioxolan-4-yl)cytosine to treat psoriasis, genital warts and other hyperproliferative keratinocyte...
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6432966 |
Antiviral combinations
The present invention relates to therapeutic combinations comprising (2R,cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-pyr
imidin-2-one (lamivudine) and BMS-200475 which have anti-hepatitis...
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6417219 |
Hetero-substituted cyclic amine metalloprotease inhibitors
The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular,...
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6417191 |
Synergistic combinations of zidovudine, 1592U89 and 3TC
The present invention relates to therapeutic combinations of (1S,4R)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl)-2
-cyclopentene-1-methanol (1592U89), 3′-azido-3′-deoxythymidine...
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6417192 |
Pyrimidinone compounds and pharmaceutical compositions containing them
A group of novel pyrimidone compounds are inhibitors of the enzyme LDL PLA 2 and therefore of use in treating atherosclerosis.
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6417180 |
Zinc finger-reactive antimicrobial compounds
The invention relates to antimicrobial compounds which interact with zinc in a zinc finger of a bacterial DNA polymerase, methods of screening for such compounds, and methods of using such...
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6413968 |
Treatment of myasthenia gravis by cyclic nucleotide phosphodiesterase inhibition
A method of treating myasthenia gravis confined to the eyes iby administering, orally, a therapeutically effective dose the nucleotide (cGMP) phosphodiesterase inhibitor Sildenafil either 100 mg....
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6410546 |
Use of MKC-442 in combination with other antiviral agents
Use of MKC-442 in combination with other antiviral agents for the treatment of patients infected with HIV is disclosed.
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6410554 |
Combination therapy for the treatment of benign prostatic hyperplasia
This invention relates to combination therapy for the treatment of benign prostatic hyperplasia comprising an alpha-1a antagonist and an endothelin antagonist. More specifically, the use of a...
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6403601 |
N-(2-phenyl-4-piperidinybutyl)-5,6,7,8-tetrahydro-1-naphthalenecarboxamides and their use as neurokinin 1 (NK1) and/or neurokinin 2 (NK2) receptor antagonists
Compounds of formula (I), wherein R 2 is a 5,6,7,8-tetrahydronaphth-1-yl group which may be substituted (the remaining groups defined herein), and pharmaceutical compositions containing the...
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6399620 |
Cycloalkyl derivatives as inhibitors of bone resporption and vitronectin receptor antagonists
There are described cycloalkyl derivatives of the formula (I) R 1 —Y—A—B—D—E—F—G (I) in which R 1 , Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and...
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6387898 |
Treatment for CNS injuries
This invention relates to a novel use of imidazole compounds in the treatment of CNS injuries.
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6387915 |
Isoxazole-sulfonamide endothelin antagonists
Isoxazole-sulfonamide endothelin antagonists of formula (I) below having good affinity for endothelin receptors and selectivity for ET A over ET B are described herein. Such compounds are...
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6384070 |
Indole derivatives useful as endothelin receptor antagonists
Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R 1 and R 2 are optional substituents and independently represent C 1-6 alkyl, C 2-6 alkenyl, optionally...
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6376503 |
Alpha 1a adrenergic receptor antagonists
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the...
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6376504 |
Phenethyl-5-bromopyridlythiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DBABO) derivatives exhibiting spermicidal activity
Novel phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity as well as anti-viral activity. These novel compounds can be...
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6372751 |
Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
This invention is directed to aryl and heterocyclyl substituted pyrimidine derivatives selected from the following formulae: wherein Z 1 , Z 2 , R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are defined...
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6372719 |
α&ngr β3 integrin antagonists in combination with chemotherapeutic agents
The present invention is directed to compounds of the formula and pharmaceutically acceptable salts and isomers thereof administered in combination with chemotherapeutic agents.
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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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RE37623 |
Enzyme inhibitors, their synthesis, and methods for use
Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula where X is S or Se; Y is H, I, F, Cl, Br, methoxy,...
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6365592 |
Phosphonic and carboxylic acid derivatives as inhibitors of protein tyrosine phosphatase-1B (PTP-1B)
The invention encompasses compounds represented by formula I: as well as compositions and methods of treatment. The compounds are inhibitors of the PTP-1B enzyme.
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6362180 |
Imidazopyridines for the treatment of neurological disorders
Corticotropin releasing factor (CRF) antagonists of formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress...
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6362193 |
Cycloalkenyl substituted compounds
Novel pyridyl or pyrimidinyl substituted cycloalkenyl compounds and compositions for use in therapy.
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6358961 |
Farnesyltransferase inhibiting quinazolinones
This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional...
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6358976 |
Integrin receptor antagonists
This invention relates to novel fused heterocycles which are useful as antagonists of the α v β 3 and related integrin receptors, to pharmaceutical compositions containing such compounds,...
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6352992 |
Endothelin antagonist and beta receptor blocking agent as combined preparations
A combination of endothelin antagonists and beta-receptor blockers is described. The combination is suitable for controlling diseases.
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6350753 |
2-Substituted-4-substituted-1,3-dioxolanes and use thereof
Nucleoside analogues containing a 1,3-dioxolane structure are suitable antiviral agents, particulary for the treatment of the HIV infections in mammals, especially humans. Examples of the...
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6348471 |
Pyrimidyl oxyphenylacetic acid derivatives
The invention relates to novel pyrimidyloxyphenylacetic acid derivatives, to a plurality of processes for their preparation and to their use to fungicides, and also to novel intermediates and to a...
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6344460 |
Propynyl uracils
The present invention provides compounds comprising propynyl uracils having the formula wherein R 1 is hydrogen, chlorine, bromine, iodine, fluorine, —CN, substituted or unsubstituted linear...
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6342499 |
Parasitic and saprophagous mite control in beneficial insects
The present invention provides a method to control parasitic and saprophagous mites on beneficial insects such as honeybees via the application of a parasiticidally or saprophagouscidally effective...
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6342504 |
Aromatic heterocyclic derivatives as enzyme inhibitors
The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof,...
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6340687 |
Substituted tetrahydro-pyrimidine-2(1H)-thione HDL-C elevators useful as antiatherosclerotic agents
Antiatherosclerotic agents are provided having the following structure: wherein: R 1 is hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl...
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6339090 |
Alpha 1A adrenergic receptor antagonists
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the...
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6333333 |
Methods for treating proliferative diseases
Methods are provided for treating proliferative diseases, especially cancers, comprising administering (1) a farnesyl protein transferase inhibitor in conjunction with (2) an antineoplastic agent...
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6329384 |
Endothelin antagonist and renin-angiotensin system inhibitor as a combined preparation
A combination of endothelin antagonists and RAS inhibitor is described. The combination is suitable for controlling diseases.
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6319925 |
O-benzyl oxime ether derivatives and their use in crop protection compositions
##STR1## Oxime ethers of formula (I) in which a) X is an N atom and Y is an oxygen atom or NH, or b) X is CH and Y is an oxygen atom, in which furthermore R 1 is C 1 -C 4 alkyl; R 2 is...
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6300337 |
Acetamide derivative and use thereof
The present Invention relates to a novel acetamide derivative represented by the following Formula 1, which has an inhibition activity for chymotrypsin type proteases and is useful as an inhibitor...
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6297223 |
Uracil reductase inactivatores
Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-fluorouracil and find use particularly in the treatment of cancer. The 5-substituent...
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6294549 |
Method for eliciting an αvβ5 or dual αvβ3/αvβ5 antagonizing effect
A method for eliciting an α v β 5 or dual α v β 3 /α v β 5 antagonizing effect in a mammal which comprises administering to the mammal a therapeutically effective amount of a compound of...
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6294542 |
Pyrimidinone compounds, pharmaceutical compositions containing the compounds and the process for preparing the same
The present invention relates to a novel pyrimidinone compounds and the pharmaceutical acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, thereby, being...
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