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6417204 |
Pyridoxine AMD pyridoxal analogues: cardiovascular therapeutics
The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions...
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6413995 |
Cinnamamide derivatives and drug compositions containing the same
The invention relates to cinnamamide derivatives having the following formula wherein R 1 represents a hydroxyl group, a C 1-6 -alkoxy group, an arylalkoxy group or a substituted or...
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6413987 |
Dermal anesthetic agents
The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as...
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6413947 |
Anilide derivative, production and use thereof
This invention is to provide a compound of the formula: wherein R 1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula: wherein the ring A is an...
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6410573 |
2,5-substituted benzolsulfonylureas and thioureas methods for the production thereof use thereof and pharmaceutical preparations containing the same
Novel 2,5-substituted benzolsulfonyl ureas and thioureas of formula (I) as illustrated in the disclosure. The compounds are useful active ingredients for medicaments. The compounds of formula (I)...
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6407120 |
Neuropeptide Y antagonists
The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.
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6407100 |
Fungicidal aromatic oximes
The invention relates to novel compounds of the formula in which R 1 is C 1-4 alkyl and (Y—X) is CH 2 , C 1-2 alkylthio-CH═ or C 1-2 alkyl-ON═ and Z is an aldimino or ketimino group, and...
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6391282 |
Antihistamine sprays and ointments for relief of delayed contact dermatitis
It has been found that certain antihistamines can mediate the delayed dermatitis and in particular that caused by poison ivy and poison sumac or poison oak. Especially useful are antihistamines...
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6391881 |
Thiourea derivatives of dihydropyridine NPY antagonists
A series of antagonists of NPY have been synthesized and are comprised of thiourea linked piperazine and piperidine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1. where Z is NR 7 R 8...
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6387954 |
Alkenyl sulphonamide derivatives
The present invention provides certain alkenyl sulphonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of...
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6387933 |
Insecticidal compositions and insecticidal methods
A pesticidal composition comprising (E)-N 1 -[(6-chloro-3-pyridyl) methyl]-N 2 -cyano-N 1 -methylacetamidine and pyriproxyfen as active ingredients and a carrier, especially, the composition having...
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6387880 |
Transdermal N-&lsqb N-&lsqb 5-&lsqb 4-(aminoiminomethly)phenyl&rsqb -1-oxopentyl&rsqb -L-α-aspartyl&rsqb -L-phenylalainine or its esters and their pharmaceutically acceptable salts
The present invention is for pharmaceutical compositions and a method of use for the transdermal delivery of N-[N-[5-[4-(aminoiminomethyl)phenyl]-1-oxopentyl]-L-α-aspar
tyl]-L-phenylalanine or its...
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6358987 |
Metalloproteinase inhibitors
A compound of formula (I) wherein X is —COOH or —CONHOH Y is a group of formula (ID) or (IE) or a pharmaceutically acceptable salt, hydrate, or solvate thereof. The compounds are inhibitors...
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6355634 |
Aromatic compounds
The invention relates to novel compounds of the formula in which R 1 is C 1-4 alkyl and (Y—X) is CH 2 , C 1-2 alkylthio-CH═ or C 1-2 alkyl-ON═ and Z is an aldimino or ketimino group, and...
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6348479 |
Water-in-oil emulsifier composition
This invention provides a milk lotion, cream or the like which does not undergo oil-water phase separation but remains stable for a long time and, in addition, has a good skin feel with good...
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6342505 |
Use of 4-substituted tetrahydropyridines for making medicines acting on TGF-β1
The invention relates to the use of a compound of formula (I): for the preparation of pharmaceutical compositions for increasing the circulating, cellular and extracellular levels of TGF-β1.
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6340695 |
Rapid onset formulation
Provided herein is a novel enterically-coated pyridoxine HCl and doxylamine succinate rapid onset formulation comprising a disintegrating agent such that the following dissolution profiles are...
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6335352 |
IL-8 receptor antagonists
Novel compounds useful in the treatment of Interleukin-8 mediated diseases, and methods of using them are disclosed.
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6331542 |
Protease inhibitors
The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or...
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6329405 |
Cyclobutene derivatives, their preparation and their therapeutic uses
Compounds of formula (I): ##STR1## {wherein: R 1 and R 2 each represents a variety of organic groups; R 3 and R 4 each represents hydrogen or a variety of organic groups; A represents a...
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6326387 |
Methods and compositions for stimulating neurite growth
The present invention relates to methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compositions comprise a neurotrophic amount of a compound which...
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6323228 |
3-substituted indole angiogenesis inhibitors
3-Substituted indole carbohydrazides having the formula ##STR1## are useful for inhibiting angiogenesis. Also disclosed are angiogenesis-inhibiting compositions and methods of inhibiting...
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6323227 |
Substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides
This invention relates to compounds of formula ##STR1## which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of...
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6319894 |
Complexes and combinations of fetuin with therapeutic agents
There is disclosed a complex and a combination of the glycosylated polypeptide fetuin and a therapeutically active small molecule compound having a net positive charge at physiological pH. The...
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6313153 |
Compositions and methods for treating nephritis and inhibiting TGF -β related conditions using pyridylacrylamide derivatives
The present invention relates to an agent for treating nephritis and a TGF-β inhibiting agent comprising as an effective ingredient a pyridylacrylamide derivative represented by the following...
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6313150 |
α-substituted phenylacetic acid derivative, its production and agricultural fungicide containing it
An α-substituted phenylacetic acid derivative useful as an agricultural fungicide, represented by general formula (I), or a salt thereof, a process for producing the same, an intermediate for the...
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6306859 |
N-substituted imide derivatives with serotonergic activity
Compounds of the Formula (I) ##STR1## wherein R 2 , Y, X and n are as defined in the specification which compounds are useful in the treatment of disorders associated with serotonergic...
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6306873 |
Substituted β-thiocarboxylic acids
This invention relates to compounds of general formula (I): ##STR1## in which Ar is a group selected from: ##STR2## A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and...
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6303639 |
Propanolamine derivatives substituted by heterocyclic radicals, processes for their preparation, pharmaceuticals comprising these compounds and their use
Substituted propanolamine derivatives and pharmaceutically tolerated salts and physiologically functional derivatives thereof are described. Also described are compounds of formula (I), ##STR1## in...
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6303641 |
Cyanoamidines as cell proliferation inhibitors
Compounds of the following formula are used for inhibiting cell proliferation: ##STR1## wherein R, R1, Q, X are as defined in the specification.
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6300352 |
Pyridine derivatives and pharmaceutical compositions containing them
The invention relates to novel pyridyl derivatives, their use as medicaments, pharmaceutical formulations containing them and methods for their preparation.
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6297264 |
Trisubstituted phenyl derivatives and process for their preparation
Compounds of the general formula (1) ##STR1## are described wherein W is a N--, and Z and L are described in the specifications. These compounds are phosphodiesterase type IV inhibitors and are...
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6291491 |
Amide derivatives as β 3 agonists
Amide derivatives are selective β 3 adrenergic receptor agonists with very little β 1 and β 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and...
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6288071 |
1-ethylene-2-alkylene-1,4-cyclohexadiene pesticides
Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in...
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6284777 |
Carbohydrazide protease inhibitors
The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or...
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6277846 |
Use of platelet activating factor antagonists as anti-pruritic agents
The invention relates to a method for treating pruritus by administering a therapeutically effective amount of a PAF antagonist to a mammal afflicted with pruritus. The PAF antagonists may, for...
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6277865 |
Piperididinyl and N-amidinopiperidinyl derivatives
This invention is directed to a compound of formula I which is useful for inhibiting the activity of Factor Xa, by combining said compound with a composition containing Factor Xa. The present...
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6277849 |
N-sulphonyl and N-sulphinyl amino acid amides as microbiocides
The invention relates to novel pesticidally active compounds of the general formula I ##STR1## as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and ...
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6274606 |
Methods of treating central nervous system disorders with aryl substituted olefinic amine compounds
Patients susceptible to or suffering from central nervous system disorders (e.g., Alzheimer's disease, Parkinson's disease, Tourette's syndrome, attention deficit disorder or schizophrenia) are...
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6268384 |
Compounds possessing neuronal activity
The present invention relates to compounds, methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compounds and the compositions and methods that...
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6268354 |
Pharmaceutical composition for antagonizing CCR5 comprising anilide derivative
This invention is to provide a pharmaceutical composition for antagonizing CCR5 which comprises a compound of the formula: ##STR1## wherein R 1 is an optionally substituted 5- to 6-membered ring;...
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6268379 |
Substituted aryl hydroxamic acids as metalloproteinase inhibitors
The present application describes novel substituted aryl hydroxamic acids of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing...
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6265446 |
Hydrazine derivatives
Hydrazine derivatives of the formula ##STR1## wherein R 1 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R 2 represents...
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6262104 |
Diarylalkenylamine derivatives
Compounds, or solvates or salts thereof, of formula (I): ##STR1## selective delta opioid agonists and antagonists and may be of therapeutic utility as analgesics, immunosuppressants to prevent...
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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...
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6258851 |
Metalloproteinase inhibitors
Compounds of formula (I), wherein A, B, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 are as defined in the specification, are matrix metalloproteinase inhibitors. ##STR1##
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6251917 |
Benzamidoaldehydes and their use as cysteine protease inhibitors
Compounds of the formula ##STR1## where R 1 , R 2 , R 3 , X and n are as defined in the description, are inhibitors of cysteine protease.
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6248744 |
Method for the treatment of pain, including chronic and female specific pain
Patients susceptible to, or suffering from chronic and/or female-specific pain are treated by administering an effective amount of a metanicotine-based compound.
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6245774 |
Tri-substituted phenyl or pyridine derivatives
Compounds of general formula (1) are described: ##STR1## wherein W-- is (1) C(Y)-- where Y is a halogen atom, or an alkyl or --XR a group where X is --O--, --S(O) m -- [where m is zero...
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6239148 |
N-substituted azaheterocyclic carboxylic acids and esters thereof
The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to...
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