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7179825 |
Retinoic acid mimetic anilides
The present invention is concerned with compounds of formula
the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents...
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7060721 |
Imidazole compounds and medicinal use thereof
Imidazole compounds represented by general formula (I):
wherein each symbol is as defined in the specification, and salts thereof, and a pharmaceutical composition containing same are provided....
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6875765 |
Arylsulfonamide ethers, and methods of use thereof
The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1β converting enzyme and other cysteine proteases in the ICE family are...
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6743929 |
Sulfonylalkanoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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6620826 |
Endothelin receptor antagonists
Novel N-phenyl imidazole derivatives, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
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6515133 |
Pharmaceutical compositions containing certain diarylimidazole derivatives
Certain diaryl imidazoles act as partial agonists or antagonists for NPY receptors, in particular NPY 5 receptors. They are of use, for example in treating loss of appetite. Such compounds bear...
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6384220 |
Para-aryl or heterocyclic substituted phenyl glucokinase activators
Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.
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6359061 |
Amide compound libraries
Amide compounds of formula (I), combinatorial libraries of amide compounds and methods of preparing the same are provided. Libraries of the invention are useful for screening in biological assays...
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6319939 |
Retinoic acid mimetic anlides
The present invention is concerned with compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X...
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6265590 |
Nα-2-(4-nitrophenylsulfonyl)ethoxycarbonyl-amino acids
Protected amino acid derivatives of general formula (I) ##STR1## and methods for the prepatation of the derivatives are provided.
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6242474 |
Aromatic ring derivatives
Novel aromatic ring derivatives represented by formula (I) or their pharmaceutical acceptable salts are provided. ##STR1## wherein Nu represents a 5- or 6-membered aromatic ring; ch 1 and ch 2 ...
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6008372 |
Substituted dinaphthylmethyl and diheteroarylmethylacetyl histidine inhibitors of protein farnesyltransferase
Substituted histidine compounds of formula (I) are described as well as methods for the preparation and pharamaceutical compositions of same, which are useful as inhibitors of protein...
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5965588 |
Sulfonylalkanoylamino hydroxyethylamimo sulfonamides useful as retroviral protease inhibitors
Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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5959120 |
Acetate ester compounds
The present invention provides an acetate ester compound of formula (III), ##STR1## a process for synthesizing compound (III), and a process for using that compound to prepare a pyrazolone...
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5792784 |
Coupling product obtained from histamine and an amino acid
The invention relates to a pseudo-dipeptide product obtained by coupling between histamine or methyl-substituted histamine and an amino-acid having formula ##STR1## wherein A is a radical selected...
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5733882 |
Retroviral protease inhibitors
The present invention provides compounds, more particularly dipeptide analogs, which bind to retroviral proteases. These compounds are inhibitors of retroviral proteases and are useful for treating...
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5616788 |
N.sub.α -2-(4-Nitrophenylsulfonyl) ethoxycarbonyl-amino acids
Protected amino acid derivatives of the general formula ##STR1## wherein R 1 represents hydrogen atom, and R 2 represents hydrogen, methyl, isopropyl, 1-methylpropyl, 2-methylpropyl,...
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5545838 |
Diol sulfonamide and sulfinyl renin inhibitors
Compounds of the formula ##STR1## wherein Z is SO or SO 2 possess renin inhibition activity and are useful in treating hypertension and other diseases where the reduction of the levels of...
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5541213 |
Propenoic acid derivatives diazole propenoic acid compounds which have useful pharmaceutical utility
A novel propenoic acid derivative which exhibits adenosine A1 antagonism is defined by the general formula (I): ##STR1## (wherein A represents an aromatic ring; R 1 represents aryl or the like; R...
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5504212 |
Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to...
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5439927 |
Imidazoyl-β-oxo-β-benzenepropanethiomide derivative, compositions and method of use thereof
The β-oxo-β-benzenepropanethioamide derivative of the present invention has potassium channel opening action and is useful for treatment of hypertension, asthma, hypersensitive colon syndrome,...
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5373017 |
Imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
Compounds characterized generally as imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension....
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5356921 |
Imidazolylphenol compounds, pharmaceutical compositions containing them, and processes for preparing such compounds and compositions
3- and 4-(1H-imidazol-1-yl)phenol compounds corresponding to the formula I ##STR1## in which R 1 represents NH 2 or CH 3 , R 2 represents H or CH 3 , X represents O or S, Y represents H, OH or...
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5346907 |
Amino acid analog CCK antagonists
Analogs of CCK-tetrapeptides, which analogs have the formula ##STR1## wherein A, B, D, R 1 , R 2 , R 3 , and R 4 are specifically defined, having activity as CCK antagonists, useful in the...
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5332833 |
β-oxo-β-benzenepropanethioamide compounds
The β-oxo-β-benzenepropanethioamide derivative of the present invention has potassium channel opening action and is useful for treatment of hypertension, asthma, hypersensitive colon syndrome,...
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5302610 |
Renal-selective biphenylmethyl imidazole angiotensin II antagonists for treatment of hypertension
Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs...
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5298647 |
Aromatic compounds of amide structure derived from aminobenzoic acids, hydroxy-benzoic acids, cinnamic acids, urocanic acids and benzimidazoles, absorbing UVB and/or UVA
Aromatic compounds absorbing UVB and/or UVA, substituted with an amide function, selected from the group consisting of ##STR1## whose variable substituents are as defined in the specification, e.g....
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5250517 |
Renin inhibiting compounds
Compounds which are amino acid derivatives and have the formula ##STR1## in which R 1 is hydrogen or methyl, R 2 is ethyl, propyl or imidazol-4-yl, R 3 is isobutyl, cyclohexylmethyl or benzyl,...
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5246958 |
Antihypertensive thiocarbamoylascetonitrile compounds
Disclosed are antihypertensive pharmaceutical compositions and compounds which include the thiocarbamoylacetonitrile having the formula: ##STR1## wherein: R 1 is selected from the group consisting...
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5236928 |
Imidazole derivatives bearing acidic functional groups at the 5-position, their compositions and methods of use as angiotensin II antagonists
There are disclosed substituted imidazole derivatives of Formula I bearing acidic functional groups which are useful as angiotensin II antagonists. ##STR1##
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5223489 |
Amino acid derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same
A compound of the formula: ##STR1## wherein R 1 is lower alkyl optionally substituted aryl; or amino optionally substituted; and R 2 is hydrogen or lower alkyl; or R 1 and R 2 are taken...
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5214206 |
Aminosulfonyl urea ACAT inhibitors
The present invention provides pharmaceutically useful compounds which are aminosulfonyl urea compounds which are ACAT inhibitors rendering them useful in controlling blood cholesterol levels,...
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5198426 |
Renin inhibitors containing C-terminal dihydroxy amides
The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, glaucoma and diseases caused by...
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5179117 |
Antihypercholesterolemic 2-substituted imidazoles
The compounds of the described invention are potent ACAT inhibitors and are useful in pharmaceutical compositions for the treatment of atherosclerosis and have the formulas: ##STR1## when Q is a...
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5175181 |
Imidazolyl/imidazolylalkyl-N-terminal amino hydroxy
Non-peptidyl compounds characterized generally as imidazolyl/imidazolylalkyl-N-terminal amino hydroxy β-amino acid derivatives are useful as renin inhibitors for treatment of hypertension....
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5138067 |
Lipid derivatives
Lipid derivatives represented by the formula: ##STR1## wherein R 1 is alkyl or alkylcarbamoyl; R 2 is lower alkyloxy, lower alkylcarbamoyloxy, lower alkylcarbonylamino, lower...
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5135914 |
Substituted derivatives of 3-amino-2-hydroxypropionic acid as inhibitors of renin
Novel substituted derivatives of 3-amino-2-hydroxypropionic acid are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as renin inhibitors...
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5096700 |
Halogenated aminohexanoates and aminobutyrates antimicrobial agents
The subject invention involves halogenated amino acid derivatives useful as antimicrobial agents having the structure: ##STR1## wherein --R is hydrogen or 2-aminoethyl; --R' is hydroxy, alkoxy,...
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5032577 |
Peptidylaminodiols
A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH; U is CH 2 or NR 2 , provided that when W is CHOH then U is CH 2 ; R 1 is loweralkyl,...
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5030738 |
Synthesis of antiulcer compounds
To synthesize molecules with antiulcer action, specifically ranitidine, niperotidine and cimetidine, having the formula: ##STR1## wherein R 1 is hydrogen or together with R 2 represents the rest...
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5013861 |
Ester substituted aminoalkanoylureido amino and imino acid and ester compounds
Compounds of the formula ##STR1## are disclosed. These compounds are useful as intermediates in the preparation of pharmaceutically active products.
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4980366 |
Amide, sulfonamide, urea, carbamate, thiocarbamate, and thiourea derivatives of 4'hydroxybenzylamine having anti-inflammatory and analgesic activity
Novel 4'-hydroxybenzylamine derivatives of the formula ##STR1## pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma,...
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4945098 |
Novel propane-1,3-diol derivatives and use
A derivative of 2-methylenepropane-1,3-diol of the general formula I ##STR1## where O--A 1 and O--A 2 , which can be the same or different, each represents O, O--C(O), O--C(O)NH, O--C(S)NH or...
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4925856 |
Aldoxime-substituted imidazolium derivatives useful in the treatment of poisoning by phosphorus-containing chemicals
A therapeutically effective class of low toxicity aldoxime-substituted functionalized imidazolium compounds and compositions is disclosed which is effective in the treatment of living species...
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4895834 |
Renin inhibitors III
The invention concerns novel renin-inhibitory peptides which are useful for treating renin associated hypertension, hyperaldosternoism, and congestive heart failure. Processes for preparing the...
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4892952 |
Substituted heteroaralkyl, heteroaralkenyl or halomethyl fungicides
Compounds of the formula: ##STR1## wherein R is phenyl or phenyl substituted with 1 to 4 of the same or different substituents selected from fluoro, chloro, bromo, iodo, lower alkyl and...
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4880781 |
Renin inhibitory peptides containing an N-alkyl-histidine moiety
The present invention provides novel renin-inhibiting peptides and novel processes and intermediates for the preparation of both novel and known renin-inhibiting peptide analogs. Such inhibitors...
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4855439 |
Process for the preparation of cimetidine
A new and simple process for the preparation of crystalline cimetidine (N-cyano-N'-methyl-N"-{2/(5-methyl-1H-imidazole-4-yl)methylt
hio/ethyl}guan idine) is described, wherein cimetidine is...
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4826815 |
Renin inhibiting compounds
The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is hydrogen; loweralkyl; arylalkyl; Or 10 wherein R 10 is hydrogen or loweralkyl; NR 11 R 12 wherein R 11 ...
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4812463 |
Alkanesulfonamides as antiglaucoma agents
Alkane sulfonamides with an electron withdrawing function β to the sulfonamide group are topically effective carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure...
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