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6011059 |
Acyl guanidine sodium/proton exchange inhibitors and method
Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure ##STR1## wherein n is 1 to 5; X is N or C--R 5 wherein R 5 is H, halo, alkenyl, alkynyl,...
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6004992 |
Aminocarboxylic acid fluorobutenyl esters
The present invention relates to novel fluorobutenyl aminocarboxylates of the formula (I) R--CO--O--CH 2 --CH 2 --CXCF 2 (I) in which X represents hydrogen or halogen and R...
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5990131 |
Heterocyclic thioesters and ketones
This invention relates to neurotrophic low molecular weight, small molecule heterocyclic thioesters and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the...
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5985860 |
System for transdermal delivery of pain relieving substances
Compositions for pain relieving non-steroidal anti-inflammatory drugs and/or medicaments such as ibuprofen, methotrexate, capsaicin, diphenhydramine, aspirin, methyl-nicotinate and other...
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5977160 |
Methods for reducing risk of repeat myocardial infarction and increasing survival in heart attack victims
The invention involves a method for treating a human survivor of a heart attack and provides further improvement in survival following the heart attack by the early initiation and long-term...
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5977159 |
Medical use of an ace-inhibitor for treatment of dyspeptic symptoms
A method for the prophylaxis and treatment of dyspeptic symptoms of unknown origin using ACE-inhibitors and a pharmaceutical peparation comprising these compounds.
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5972636 |
ATP-dependent protease and use of inhibitors for same in the treatment of cachexia and muscle wasting
The ATP-ubiquitin-dependent process has been shown to be responsible for the excessive protein degradation which occurs in conditions or disease states in which there is severe loss of body mass...
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5972892 |
Topical composition containing a substance P antagonist
The invention relates to a therapeutic composition for topical application containing at least one product with an irritant side effect and a substance P antagonist for reducing or even eliminating...
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5969156 |
Crystalline [R- (R*,R*)]-2-(4-Dfluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)- 3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt (atorvastatin)
Crystalline forms of atorvastatin and hydrates thereof are useful hypolipidemic and hypocholesterolemic agents.
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5965565 |
Piperidines promote release of growth hormone
The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R 1 , R 1a , R...
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5958966 |
Treatment of aberrant cellular states with biomodulators
Biomodulators, which regulate cellular differentiation and proliferation, as well as methods of use thereof, e.g., for treating various conditions, e.g., cancer, senescence, immunological disorders...
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5958937 |
Pharmaceutical formulations of poorly water soluble camptothecin analogues and NMP
A- and/or B-ring substituted camptothecin derivatives, which are poorly water soluble (less than 5 micrograms per milliliter of water), are highly lipophilic camptothecin derivatives (HLCD) and are...
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5942538 |
Benzamidoxime derivatives, method for preparation thereof and fungicide for agricultural and horticultural use
The present invention relates to benzamidoxime derivatives represented by the formula I!; ##STR1## wherein R 1 is unsubstituted or substituted C 1 -C 4 alkyl, unsubstituted or substituted C 2 ...
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5942537 |
Method of inhibiting the transport of L-glutamate to treat CNS disorders
A method of inhibiting the transport of a neurotransmitter away from the synapse comprising contacting a neurotransmitter transporter with a compound having the structure ##STR1## wherein ##STR2##...
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5939437 |
CCK and gastrin receptor ligands
Compounds of formula (I) and their pharmaceutically active salts are gastrin and CCK receptor ligands, where Ar is a monocyclic aromatic group, R 1 is halo, amino, nitro, cyano, sulphamoyl,...
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5935967 |
Pharmaceutical formulations of highly lipophilic camptothecin derivatives
Pharmaceutical formulations of highly lipophilic, poorly water soluble derivatives of Camptothecin are disclosed. The formulations include an effective amount of the HLCD dissolved or suspended in...
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5935997 |
O-thiocarbamoyl-aminoalkanol compounds, their pharmaceutically useful salts and process for preparing the same
The present invention relates to O-thiocarbamoyl-aminoalkanol compound represented by the following structural formula (VI), (VIII) and (IX) which are a racemic or enantiomerically enriched and...
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5935990 |
Substituted pyrrolyl compounds for the treatment of inflammation
A class of pyrrolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein R 1 , R...
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5935988 |
Tolerability of pharmaceutically active β-amino acids
The present invention relates to mixtures of α-amino acids and/or derivatives thereof and cyclopentane-β-amino acids and/or derivatives thereof, dipeptides of the abovementioned α-amino acids...
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5935924 |
Treatment of congestive heart failure
A mammal with congestive heart failure is treated by administering to the mammal an effective amount of growth hormone. Treatment results in increased left ventricular cystolic pressure, increased...
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5935954 |
Compounds with improved multi-drug resistance activity
The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical...
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5932567 |
Thrombin inhibitors
Thrombin inhibitors of the formula ##STR1## where R 1 , A, B and D have the meaning indicated in the description, and intermediates for the preparation thereof are described. The compounds I are...
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5932575 |
Cardiac diseases improving agents
This invention relates to cardiac diseases improving agents substantially free from antagonistic action to type 1 receptor of angiotensin II which participates to hypotensive action. Particularly,...
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5932595 |
Matrix metalloprotease inhibitors
The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of...
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5932520 |
Use of pyrrole compounds as antifouling agents
There is provided a method for controlling or combatting the attachment of a fouling organism to an underwater surface which comprises contacting said organism with an antifouling-effective amount...
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5929114 |
Arylthio compounds
Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O,...
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5922761 |
Methods for in vivo reduction of iron levels and compositions useful therefor
In accordance with the present invention, there are provided methods for the in vivo reduction of free iron ion levels in a mammalian subject. The present invention employs a scavenging approach...
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5919774 |
Pyrroles as sPLA.sub.2 inhibitors
A class of novel pyrroles is disclosed together with the use of such compounds for inhibiting sPLA 2 mediated release of fatty acids for treatment of conditions such as septic shock.
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5914351 |
Anti-viral aromatic hydrazones
Compounds of the formula ##STR1## wherein Q is a hydrazone derivative; R 1 is hydrogen, halogen, alkyl or alkoxy; R 2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl,...
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5905077 |
Inhibitors of HIV protease useful for the treatment of AIDS
The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
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5900419 |
Formulations and compositions of poorly water soluble camptothecin derivatives
A- and/or B-ring substituted camptothecin derivatives, which are poorly water soluble (less than 5 micrograms per milliliter of water), are highly lipophilic camptothecin derivatives (HLCD) and are...
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5891904 |
Use of inhibitors of phosphodiesterase IV
The invention relates to the use of inhibitors of phosphodiesterase IV for the modulation of the motility and peristalsis of the hollow organs of the urogenital and gastrointestinal tract.
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5889040 |
Composition for increasing protein concentration in a mammal
The present invention is based in part upon the discovery that the use of pyruvate in enteral formulations, in combination with an anabolic protein composition, produces a synergistic effect in...
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5889041 |
Method for treating an inflammatory pathological condition
The present invention relates to a method for treating an inflammatory pathological condition in a patient in need thereof, comprising administering on empty stomach an anti-inflammatory effective...
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5886022 |
Substituted cycloalkanecarboxylic acid derivatives as matrix metalloprotease inhibitors
Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have...
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5886043 |
Substituted 4-biarylbutyric acid derivatives as matrix metalloprotease inhibitors
Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have...
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5883107 |
Arginine mimic derivatives as enzyme inhibitors
The present invention provides peptide aldehydes having an azetidinyl, prolyl or pipecolyl group as part of the peptide backbone and an arginine mimic group such as an amidinopiperidine or...
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5877203 |
Treatment for atherosclerosis and other cardiovascular and inflammatory diseases
Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of...
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5869067 |
Bi-aromatic compounds and pharmaceutical and cosmetic compositions
The present invention relates to new aromatic compounds, to their preparation and to their use in human and veterinary medicine and in cosmetic compositions.
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5866600 |
Method for treating an inflammatory condition with prevention of secretive activity of gastric secretive level
A method for treating an inflammatory pathological condition with simultaneous prevention of a secretive activity on gastric secretion comprising the step of administering a subject in need thereof...
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5863903 |
Use of hydroxy alkyl piperidine and pyrrolidine compounds to treat diabetes
The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.
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5863913 |
Aromatic compound and pharmaceutical composition
An aromatic compound of the formula (I): ##STR1## specifically, for example, 3- (4-carboxyphenyl)methyl!valeramido!-4-dimethylaminobenzoic acid 4'-methylpiperazide, or a salt thereof, and a...
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5863950 |
HIV protease inhibitors
HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well...
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5861434 |
Compositions containing L-carnitine or an acyl L-carnitine in combination with an ace-inhibitor for the treatment of cardiovascular disorders and a method for treating cardiovascular disorders
Compositions containing (a) L-carnitine, an acyl L-carnitine, or a pharmacologically acceptable salt thereof in combination with (b) an ACE-inhibitor are useful for treating cardiovascular...
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5859042 |
Five membered heterocyclic compounds
The instant invention is related to 5-membered heterocyclic compounds and pharmaceutical compositions which possess inhibitory activity on 5 alpha-reductase.
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5852047 |
Pharmaceutical product comprising a salicylate of an esterifiable ace-inhibitor
Salicylates of esterifiable ACE-inhibitors, especially captopril-S-aspirinate, and processes for their preparation are described. Such compounds are useful as analgesics, in the process of...
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5852051 |
Dipeptide p-amidinobenzylamides with N-terminal sulfonyl or aminosulfonyl radicals
Compounds of the formula I ##STR1## in which R 1 , A and B have the meanings stated in the description, and the preparation thereof are described. The novel compounds are suitable for controlling...
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5846966 |
Combinations of hydroxy-substituted azetidinone compounds and HMG CoA Reductase Inhibitors
Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar 1 and Ar 2 are aryl or R 4 -substituted aryl; Ar 3 ...
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5834032 |
Compositions and methods for treating diabetes
Compositions and methods are useful for alleviating symptoms of diabetes in mammals. Some of the compositions include a zinc salt and cyclo-Hispro, and optionally contain arachidonic acid....
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5830869 |
Thiadiazole amide MMP inhibitors
The present invention provides novel thiadiazole amide derivatives represented by formula I ##STR1## The compounds of the present invention inhibit various enzymes from the matrix metalloproteinase...
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