|6576664||Inhibitors of aggrecanase and matrix metalloproteinases for the treatment of arthritis|
This invention relates to molecules which inhibit metalloproteinases, including aggrecanase, and the production of tumor necrosis factor (TNF). In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation and inhibitors...
|6573297||(2-substituted oxyphenyl)alkanamide derivative, hair growth promoter and external composition for skin using the same|
A (2-substituted oxyphenyl)alkanamide derivative or a salt thereof expressed by the following Formula (I): ##STR1## wherein one of A and B is a hydrocarbon group of C3-30 expressed by R1 and the other is --(CH2)n-NR2
|6562944||Amide library formation using a "by-product-free" activation/coupling sequence|
Disclosed is an improved method for preparing an activated carboxylic acid in the form of a pentafluorophenyl ester, an improved method for making a carboxamide from a pentaflourophenyl ester, and a carboxamide and carboxamide library prepared using both ...
This invention describes the new, nonsteroidal gestagens of general formula I ##STR1## in which A, B, Ar1, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds ...
|6518036||Method of permanent fluorescent assay|
A method for performing a peroxidase-based assay by reacting a peroxidase enzyme with a soluble organic p-hydroxyphenyl-containing compound having the formula: ##STR1## wherein Q is a linear or branched 1-12 heteroatom alkyl wherein the heteroatoms a...
This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: ##STR1##...
|6506937||Substituted benzenesulfonylureas and -thioureas-processes for their preparation and their use as pharmaceuticals|
Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro) (mercapto)alk(oxy)yl, E is O or S; Y is --[CR(3)2 ]n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alky...
Propanolamine derivatives represented by the following formula (I): ##STR1## These derivatives may be 댣 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria ac...
|6469210||Process for the preparation of phenylalkanoic acid amides and intermediates therefor|
A process for producing a phenylalkanoic acid amide of the formula  ##STR1## by reacting a carboxylic acid of the formula  ##STR2## with a dehydrating agent to produce an oxazolinone compound of the formula  ##STR3## and then reacting the ox...
|6458523||Hydroquinone derivatives as scavengers for oxidized developer|
New compounds of the formula I ##STR1## are described, wherein n is >1; X is O or NR4 ; L is a n-valent linking group defined in claim 1 and R1 is H, halogen, C1 -C25 -alkyl, C3 -C25 -alkenyl, u...
|6376524||Triphenyl compounds as interleukin-4 antagonists|
Triphenyl compounds of the formulae I, II, and VI: ##STR1## methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are compounds are interleukin-4 antagonists; and are useful for the treatment of asth...
|6369248||Fragrance precursor compounds|
Compounds having formula (I) in which n is 1, 2 or 3 and R1 to R6 represent, independently, branched or unbranched, substituted or unsubstituted alkyl-, alkenyl-, alkinyl-, cycloalkyl-, cycloalkenyl- or aromatic-radicals or hydrogen ...
|6313088||8-[(2-hydroxy-4-methoxy benzoyl) amino]-octanoic acid compositions for delivering active agents|
Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well....
|6310247||7-aryl-6(Z)-heptatrienoic acid retinamides|
Novel trienoic retinoid compounds of ##STR1## with apoptotic activity useful for the prevention and treatment of cancer....
|6310246||Fluorovinloxyacetamides, process for preparing same and herbicidal composition comprising same|
Herbicidal fluorovinyloxyacetamide compounds of formula (I) are useful for protecting crops from weeds: ##STR1## wherein: R1 is a phenyl group optionally having one or more substituents selected from the group consisting of C1-6 alky...
|6288265||Phloroglucidic acid and derivatives as antibacterial agents|
A series of phloroglucide derivatives are synthesized, which possess potent antibacterial activities. They include unsymmetrical phloroglucide analogs, phloroglucides attached to cephalosporins at the C-3' position, and 7-(phloroglucidamido)cephalosporins...
|6265611||Hydroxymandelic acid amides of phenolic amines|
The present invention relates to hydroxymandelic acid amides of phenolic amines which can be used as antioxidants or as free-radical scavengers, particularly in the cosmetic or dermatological field, in foods and in cosmetic and dermatological compositions...
|6262123||Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them|
Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(4) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective component, for the prophylaxis and treatment of infarction...
|6218426||Non-peptide GnRH agents|
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and are defined variables: ##STR1## Such compounds and their pharmaceutically acceptabl...
|6090981||Substituted benzenesulfonylureas and -thioureas--process for their preparation and their use as pharmaceuticals|
Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(ozy)yl, E is O or S; Y is --[CR(3)2 ]n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or ...
|6075141||N -, -dimethyl-3,5-dialkoxybenzylcarbonyl amino acid 3,4-dihydro-3-hydroxy-4-oxo-1,2,3-benzotriazin-3-yl and pentafluorophenyl esters|
This invention provides Ddz-amino acid pentafluorophenyl esters and Ddz-amino acid 3,4-dihydro-3-hydroxy-4-oxo-1,2,3-benzotriazine (ODhbt) esters and their side-chain protected derivatives. Preferred esters and derivatives are crystalline solids. The inve...
|6054457||Benzamide derivatives and their use as vasopressin antagonists|
This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R1 is aryl optionally substituted with lower alkoxy, etc., R2 is lower...
|6034266||Gem-difluoro derivative of phenylacetamide and phenylacetic acid and their pharmaceutical uses|
The present invention refers to novel gem-difluoro compounds of formula: ##STR1## wherein: R1 can be hydrogen, acyl or acyl substituted; R2 is hydrogen, lower alkyl, lower alkyl substituted, nitro, halogen, methylenedioxy, trifl...
|6031133||Synthetic techniques and intermediates for polyhydroxy, dienyl lactones and mimics thereof|
Synthetic methods for lactone-containing compounds such as the discodermolides are provided, as are compounds which mimic the chemical and/or biological activity thereof, and methods and intermediates useful in their preparation....
|6025349||Phenyl.-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, a process for their preparation, their use as a medicament or diagnostic agent, and also a medicament containing them|
Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, a process for their preparation, their use as a medicament or diagnostic agent, and also a medicament containing them. Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl g...
|6019957||Non-steroidal radiolabeled agonist/antagonist compounds and their use in prostate cancer imaging|
The present invention relates to a radiolabeled non-steroidal compound having the formula: ##STR1## where R1, R2, and R3, are the same or different and are a radioactive or nonradioactive halogen, a nitro, a cyano, a ...
|5977399||Iminooxymethyleneanilides, preparation thereof and intermediates therefor, and compositions containing them|
Iminooxymethyleneanilides of the formula I ##STR1## where the substituents and the index have the following meanings: R is hydrogen, unsubst. or subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, alkylcarbonyl or alkoxycarbonyl; ...
|5948418||Sulfur-based amides and bis-amides useful against skin disorders|
Novel sulfhydryl group-containing amides and disulfide group-containing bis-amides useful for treating or preventing an abnormal biological condition or a disease, and/or improving the texture or appearance of the skin, as well as compositions containing ...
|5942644||Precursors for the production of chiral vicinal aminoalcohols|
The disclosure describes new compositions of matter useful for the preparation of optically-active vicinal aminoalcohols. The compositions are chiral ଲ-hydroxycarboxamides, ଲ-hydroxyhydraxides, and ଲ-hydroxyhydroxamic acids....
|5935978||Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic- or heteroatom-containing linking group|
This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical c...
|5929120||Guainidino, formamidino, amino and related compounds for inhibiting osteoclast-mediated bone resorption|
Compounds of the following general structure X--Y--Z-Aryl-A--B, ##STR1## which inhibit osteoclast mediated bone resorption....
|5922771||Benzocycloalkene compounds, their production and use|
A compound of the formula ##STR1## wherein R1 and R2 independently represent H or an optionally substituted hydrocarbon group; R3 represents an optionally substituted hydrocarbon group; R4 represents H or a...
|5880156||Substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing them|
Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them Benzoylguanidines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4) are as defined in...
|5855629||Alkoxy acetic acid derivatives|
This invention provides alkoxy acetic acid derivatives of general formula I: ##STR1## wherein R is the residue of an amine, an aminoalcohol or a polyol linked to the or each --CHR'--CO-- moiety via an amide or ester linkage; R' is hydrogen or a C
|5856519||Chiral auxilary for stereoselective alkylations|
This invention relates to a method for the stereoselective synthesis of a 2-aryloxycarboxylic acid using a chiral auxiliary to enhance the stereoselectivity of the alkylation of the -halo acid with an aryloxy group....
|5847005||Benzamidoxime derivatives, process production thereof, and agrohorticultural bactericide|
The present invention relates to benzamidoxime derivatives represented by the formula I!; ##STR1## wherein R1 is unsubstituted or substituted C1 -C4 alkyl, unsubstituted or substituted C2 -C4 a...
Alkylbenzoylguanidines of the formula I ##STR1## in which A, R1, R2 and R3 have the given meanings, and their physiologically harmless salts exhibit antiarrhythmic properties and act as inhibitor of the cellular Na
|5801195||Immunotherapeutic aryl amides|
Novel aryl amides are inhibitors of tumor necrosis factor and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide....
|5780668||X-ray opaque dental materials|
X-ray opaque esters or amides of iodosubstituted benzoic acid according to formula I and polymers and dental materials produced therefrom. ##STR1## R1 =hydrogen or C1 to C3 alkyl, preferably H or CH3 ; R
|5773476||Methods and compositions for inhibiting cell proliferative disorders|
The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers charcterized by over-activity or inappropriate activity HE...