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7399778 |
Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole
Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia:
wherein, R 1 is lower alkyl, substituted lower alkyl, phenyl, substituted...
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7141680 |
Aromatic compounds possessing antifungal or antibacterial activity
The present invention provides novel compounds possessing antibacterial, and/or antifungal activities. Pharmaceutical compositions containing these compounds, methods of making and methods for...
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7132543 |
Para-phenylenediamine derivatives containing a disubstituted pyrrolidinyl group bearing a cationic radical, and use of the same for dyeing keratin fibers
The present disclosure relates to a novel a para-phenylenediamine derivative substituted with a pyrrolidinyl group of formula (I) and the addition salts thereof. The present disclosure also relates...
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7078528 |
Biimidazole diamide anion binding agents
Biimidazole diamide compounds that are useful for binding anions such as sulfate are described, along with the use thereof for purposes such as extracting anions from a waste stream and/or...
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6906199 |
Process for preparing distamycin derivatives
It is described a process for preparing, in high yields and purity and without the need of carrying out several steps and/or isolating many intermediates which could lead to undesired by-products,...
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6903221 |
Method for producing β-ketoenol esters
The invention relates to a method for producing β-ketoenol esters of the general formula (Ia) or (Ib), wherein Ar, R a and R b are defined as in claim 1 . The inventive method is characterized...
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6753316 |
Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents
Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each...
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6683189 |
Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from...
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6673940 |
Compositions and methods relating to cyclic compounds that undergo nucleotide base pair-specific interactions with double-stranded nucleic acids
The design, synthesis, and use of cyclic compounds, including cyclic polyamides, is described. Such compounds comprise at least two polymer portions, one of which comprises at least three molecular...
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6555692 |
Preparation and use of bifunctional molecules having DNA sequence binding specificity
Novel small molecule polyamides that specifically bind with subnanomolar affinity to a predetermined sequence with potential use in molecular biology and human medicine are described. The designed...
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6472537 |
Polyamides for binding in the minor groove of double stranded DNA
The invention encompasses improved polyamides for binding to specific nucleotide sequences in the minor groove of double stranded DNA. The 3-hydroxy-N-methylpyrrole/N-methylpyrrole carboxamide pair...
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5719240 |
Compounds containing cyclic amidine and uretdione groups, a process for their preparation and the use thereof
A compound containing cyclic amidine groups and uretdione groups, having the formula: ##STR1## wherein X is O or NR 2 , R is the hydrocarbon radical of isophorone diisocyanate: ##STR2## R 1 is a...
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5698563 |
Bis- hydrazones!
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises bis(guanylhydrazone) of...
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5470834 |
Sulfoximine and suldodiimine matrix metalloproteinase inhibitors
Novel sulfoximine and sulfodiimine matrix metalloproteinase inhibitors of the formula, ##STR1## wherein: R 1 is selected from the group consisting of lower-alkyl, hydroxy lower-alkyl, amino...
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5290670 |
Silver halide photographic elements
An infrared sensitive silver halide photographic element which contains an infrared-absorbing dye represented by the following formula ##STR1## wherein: R 1 and R 2 each independently represents...
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5258357 |
Carboxamides, their preparation and their use as herbicides
Carboxamides of the formulae Ia to Ic ##STR1## where X is oxygen or sulfur; R 1 is hydrogen or substituted or unsubstituted cycloalkyl or alkyl; R 2 is hydroxy, alkoxy, cyanoalkyl,...
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5242939 |
Anilide derivatives with angiotensin II antagonist properties
This invention relates to anilide derivatives of Formula I ##STR1## which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of hypertension, heart...
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5235057 |
Aminodiol derivatives
The invention relates to compounds of the formula ##STR1## in which R 1 and R 2 are identical or different and are hydrogen or aralkyl, R 3 is alkyl, cycloalkyl or cycloalkylalkyl, R 4 and R 5 ...
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5233029 |
Elaiophylin derivatives and a process for the preparation thereof
The invention relates to elaiophylin derivatives of the formula I, II and III ##STR1## in which the substituents R(1), R(2), R(3) and R(3)' have the specified meanings. The compounds have...
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5212291 |
Anthracycline derivatives as solubilized pro-drugs
The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine,...
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5212316 |
Ethers and thioethers having therapeutical activity, their preparation and pharmaceutical compositions containing them
Compounds of formula I ##STR1## wherein Ar is an optionally substituted phenyl ring; B is a single bond, a group --(CH 2 OCH 2 ) n being n=or 2, a a 2,4-disubstituted-1,3-dioxolane ring or a...
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5187290 |
Acylaminoalkanoyl urethanes or thiourethanes
Compounds of the formula ##STR1## wherein Z is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inbitition activity and...
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5183810 |
Imidazole angiotensin II antagonists incorporating a substituted benzyl element
Substituted imidazoles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists. ##STR1##
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5116835 |
Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof
Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof. The present invention relates to compounds of the formula I...
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5116827 |
Quinolinecarboxylic acid derivatives as solubilized pro-drugs
The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine,...
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5114961 |
2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists
The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R 4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at...
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5084465 |
Antifungal carbinols
Antifungal carbinols, particularly α-styryl carbinols, and the corresponding epoxy carbinols are provided. These carbinol compounds have the formula: ##STR1## or a pharmaceutically or...
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5077283 |
Solubilized imidazole pro-drugs
The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine,...
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5075301 |
Furan derivatives useful for the treatment of gastro-intestinal disorders
A furan derivative and a pharmaceutically acceptable salt thereof having gastrointestinal enterokinetic activity which is expected to be used in a broad spectrum of diseases associated with...
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5032590 |
Substituted hydroxylamines
Substituted hydroxylamines of the formula ##STR1## in which R 1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia...
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5015656 |
Organic compounds and their use as pharmaceuticals
A pharmaceutical compound of the formula ##STR1## in which R 1 , R 2 and R 3 independently are hydrogen, hydroxy, halo, nitro, amino, C 2 -5 acylamino, C 1 -4 alkyl, --CHO, --CH 2 OH, --CH 2 OC...
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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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4992421 |
Luteinizing hormone releasing hormone antagonist
The present invention relates to novel luteinizing hormone releasing hormone antagonists ##STR1## The invention also relates to pharmaceutical compositions containing such compounds and to the use...
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4985451 |
Elaiophylin derivatives, the use thereof as pharmaceuticals, and pharmaceuticals containing them
The invention relates to elaiophylin derivatives of the formula I, II and III ##STR1## in which the substituents R(1), R(2), R(3) and R(3)' have the specified meanings. The compounds have...
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4929744 |
Process for preparing heteroaromatic methyl)-2,2'-bi-1H-imidazoles
This invention relates to a process for preparing (aryl) or heteroaromatic methyl)-2,2'-1H-biimidazoles. Reacting an appropriate alpha-brominated or alpha-chlorinated, substituted or...
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4900838 |
Acylation products of bis(2-imidazolin-2-ylhydrazones) of 9,10-anthracenedicarboxaldehyde
N-acylated derivatives of bis(2-imidazolin-2-ylhydrazones) of 9,10-anthracenedicarboxaldehyde, useful as anti-cancer agents against certain strains in mice, are disclosed and described, including...
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4898977 |
Processes for the preparation of 5-amino-4-hydroxyvaleric acid derivatives
The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R 1 represents hydrogen, optionally...
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4889868 |
Bis-imidazolinoamino derivatives as antiallergy compounds
This invention relates to chemical compounds which possess valuable therapeutic activity particularly as lipoxygenase and phospholipase C inhibitors and as platelet-activating factor receptor...
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4875928 |
Substituted azolylcyclopropyl-azolylmethyl-carbinol derivatives
Substituted azolylcyclopropyl-azolylmethyl-carbinol derivatives of the formula ##STR1## in which Ar is optionally substituted aryl or optionally substituted heteroaryl, R is hydrogen, alkyl,...
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4868270 |
Heterocycle sulfone oligomers and blends
High thermal stabilities are achievable in linear or multidimensional sulfone, solvent resistant oligomers by incorporating oxazole, thiazole, or imidazole linkages into the oligomer backbone....
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4851387 |
5-substituted amino-4-hydroxy-pentanoic acid derivatives and their use
A 5-substituted amino-4-hydroxy-pentanoic acid derivative having the formula: ##STR1## wherein R 1 is a hydrogen atom or an N-protecting group, R 2 , R 3 and R 5 may be any of a variety of...
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4839375 |
(Aryl or heteroaromatic methyl)-2,2'-bi-1H-imidazoles and their use as anti-hypertensive agents
This invention relates to novel (aryl or heteroaromatic methyl)-2,2'-1H-biimidazoles; to a process for their production comprising of reacting an appropriate alpha-brominated or alpha-chlorinated,...
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4820691 |
Amino acid 1,2-diketo derivatives as renin inhibitors
Compounds of the formula ##STR1## are disclosed. These compounds interevene in the conversion of angiotensin to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.
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4816475 |
1,3,5-trithian derivatives and pharmaceutical compositions
An anti-arteriosclerotic or anti-hyperlipemic 1,3,5-trithiane derivative according to the formula (I): ##STR1## a pharmaceutical composition containing the same, and a process for producing the same.
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4788190 |
2,4,4-tri- and 2,2,4,4-tetra substituted-1,3-dioxolane antifungal, antiallergy compounds
Novel 1,3-dioxolane compounds useful as antifungal and antiallergy agents and represented by the formula ##STR1## wherein Ar is thienyl, pyridyl, biphenyl, phenyl or phenyl substituted by one or...
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4775406 |
Salts of 1-phenylimidazole-5-carboxylic acids, composition containing them, and their use as growth regulators
The salts of 1-phenylimidazole-5-carboxylic acids substituted in the phenyl ring, of the general formula (I) ##STR1## exhibit a good plant growth-regulating activity. In the general formula the...
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4737510 |
Bioactive metabolites from the caribbean sponge agelas coniferin
Novel bioactive metabolites from the Caribbean sponge Agelas coniferin are disclosed. These compounds are generically referred to as halopyrroles. They exhibit antiviral and antibacterial...
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4691021 |
Aminoalkyl hydantoins and glycidyl derivatives thereof
Novel aminoalkyl hydantoins and glycidyl derivatives thereof are prepared from previously unknown 3-(amidoalkyl) hydantoins.
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4684736 |
Bisimidazolium salts
The invention relates to bisimidazolium salts whose imidazole moieties are linked to each other through a bridge in the 1-position and which contain, in the 3-position, fibre-reactive groups formed...
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4668799 |
Anti-hepatitis and anti-cirrhotic 1,3-dithiol-2-ylidene derivatives, and pharmaceutical compositions therefor
A 1,3-dithiol-2-ylidene derivative of the formula: ##STR1## wherein each of R and R 1 which may be the same or different, is a lower alkyl group, a lower alkenyl group, a cycloalkyl group, a lower...
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