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6509356 |
1-(4-(Substituted alkoxy)benzyl)naphthalene compounds having estrogen inhibitory activity
A class of substituted benzylnaphthylene compounds of the structure where R 1 and R 2 are independently hydrogen, alkyl of one to six carbon atoms, acyl of two to six carbon atoms, or...
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6509368 |
Use of catechol derivatives as proteinase inhibitors
Use of catechol derivatives of the general formula I wherein R 1 to R 5 are as defined according to claim 1 , as protease inhibitors.
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6506775 |
Substituted benzylaminopiperidine compounds
The invention provides a compound of formula (I): and its pharmaceutically acceptable salts, wherein R is halo C 2 -C 8 alkenyl or halo C 2 -C 8 alkynyl; R 1 is hydrogen, halo or C 1 -C 6 ...
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6500818 |
Naphthalenecarboxamides as tachykinin receptor antagonists
Compounds having the following formula wherein L, M, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X 1 and X 2 are as defined in the specification, pharmaceutically-acceptable salt thereof, useful for...
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6495569 |
Imidazolidine compounds
Disclosed are novel compounds and a method of treating inflammatory diseases. The method comprises administering to an individual in need an effective amount of an imidazolidine compound...
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6489354 |
3-alkyl substituted pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1 , R 2 , R 3 , R 4c , R 4d , and R 4f are defined herein) which are useful as modulators of chemokine...
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6486178 |
Indane derivatives
The present invention provides medicines for treating cardiac insufficiency which contain as an active ingredient indane derivatives of formula (I) wherein R 1 represents hydrogen atom, nitro...
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6476048 |
Substituted phenanthridinones and methods of use thereof
This invention provides a novel class of substituted 6(5H)phenanthridinone compounds. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable...
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6476054 |
Cyclic amine modulators of chemokine receptor activity
The present invention is directed to cyclic amines of the formula I: (wherein R 1 , R 2 , R 3 , m and n are defined herein) which are useful as modulators of chemokine receptor activity. In...
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6469011 |
Benzenesulfonamide compounds useful as TXA2 and 5-HT2 receptor antagonists
Compound of formula (I): which is useful as a TXA 2 and 5-HT 2 receptor antagonist and pharmaceutical compositions containing the same.
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6458807 |
Methods for treating vascular dementia
The invention describes novel methods for treating and preventing dementia caused by vascular diseases; dementia associated with Parkinson's disease; Lewy Body dementia; AIDS dementia; mild...
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6455544 |
Use of cholinesterase inhibitors to treat disorders of attention
The present invention provides novel methods of treating disorders of attention or improving attention in humans by administering an effective amount of a cholinesterase inhibitor.
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6455531 |
Hydroxamic acid derivatives
Compounds having therapeutic utility are of the formula wherein NB 2 is heterocycloalkyl and R 1 and R 2 are each various substituents or a cyclic group.
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6451817 |
Alpha-substituted-1-benzyl-napthyls
This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are α-substituted with ether, thioether, amino, hydrazino, cyano or halo...
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6444685 |
N-(4-sulfonylaryl)Cyclylamine 2-hydroxyethylamines as beta-3 adrenergic receptor agonists
This invention provides compounds of Formula I having the structure wherein R 1 , R 2 , R 3 , R 4 , W, X, and Y are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which...
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6444688 |
Compounds and compositions with nitrogen-containing non-basic side chains
The instant invention provides compounds of formula I wherein R 1 is OH, O—C(O)—(C 1 -C 6 alkyl), O—C(O)—O(C 1 -C 6 alkyl), O—C(O)—Ar, or O—C(O)—O—Ar; R 2 is H, OH, O(C 1...
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6436961 |
Pharmaceutical agents for the treatment of emesis
The present invention relates to a novel process for preparing and resolving 3-amino-2-phenylpiperidine and for synthesizing from the enantiomers of such compound certain pharmaceutically active...
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6429229 |
Keto acid salts and amine derivatives, and their use for preparing medicines
The invention concerns the use of compounds of general formula (I): (X) n1 ,Y,(Z) n2 wherein n1 and n2 represent 0 or 1; X represents a natural amino acid, in particular an amino acid selected...
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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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6413986 |
&lsqb 1-indanon-2-yl&rsqb methylpiperidines
Novel [[(aminocarbonyloxy)-1-indan]-2-yl]methylpiperidines of the formula wherein R is hydrogen, loweralkyl, or a group of the formula R 1 is hydrogen or a group of the formula W, X and Y are...
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6391892 |
Naphthyl pharmaceutical compounds
The present invention provides a compound of formula I wherein R 1 is H, OH, halo, OCO(C 1 -C 6 alkyl), OCO(aryl), OSO 2 (C 4 -C 6 alkyl), OCOO(C 1 -C 6 alkyl), OCOO(aryl), OCONH(C 1 -C 6 ...
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6384053 |
α-substituted-1-benzyl-napthyls
This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are α-substituted with ether, thioether amino, cyano or halo that are...
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6380220 |
Derivatives from piperidine-keto acid, their preparation and use
Piperidineketocarboxylic acid derivatives of the general formula I and their tautomeric and isomeric forms, and physiologically tolerable salts thereof, where the variables have the meanings...
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6376516 |
Noscapine and noscapine derivatives, useful as anticancer agents
Compounds such as formula (I) are useful in the treatment of tumor cells and the treatment of cancer.
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6372760 |
Stabilized composition comprising antidementia medicament
The present invention provides a stable composition of an antidementia medicament. Specifically, it is a stabilized composition of an antidementia medicament comprising an antidementia medicament...
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6372764 |
Pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1 , R 2 , R 3 , R 4c , R 4d , and R 4f are defined herein) which are useful as modulators of chemokine...
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6365602 |
N-substituted naphthalene carboxamides as neurokinin-receptor antagonists
A compound of formula I wherein: R is alkyl; R 1 is optionally substituted phenyl 2-oxo-tetrahydro-1(2H)-pyrimidinyl, or 2-oxo-1-piperidinyl; R 2 is hydrogen, alkoxy, alkanoyloxy,...
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6362201 |
3-cyclopropyl and 3-cyclobutyl pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1 , R 2 , R 3 , R 4c , R 4d , and R 4f are defined herein) which are useful as modulators of chemokine...
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6358978 |
Substituted benzimidazoles
Compounds of formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NFκB is involved.
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6355632 |
Naphthyl compounds, intermediates, compositions, and methods
The present invention provides pharmaceutically active compounds formula I wherein R 1 is —H, —OH, —O(C 1 -C 4 alkyl), —OCOC 6 H 5 , —OCO(C 1 -C 6 alkyl), or —OSO 2 (C 2 -C 6 ...
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6329399 |
Antifungal amine derivatives and processing for producing the same
Novel amine derivatives having an excellent antimycotic effect represented by general formula (1) below and salts thereof are provided. ##STR1## [in the formula (1, R 1 represents a C 1 -5 alkyl...
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6329395 |
Neuropeptide Y5 receptor antagonists
Compounds of the formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein a and b are 0-2, provided that the sum is 0-3; ##STR2## X is --O--, --S--, --SO--, --SO 2 --,...
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6326372 |
Lactam and cyclic urea derivatives useful as alpha 1a adrenoceptor antagonists
Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also...
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6316467 |
Elevation of HDL cholesterol by 4-[(Aminothioxomethyl)-hydrazono]-N-(substituted)-4-arylbutanamides
Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the "good" cholesterol and as such may be useful for treating diseases such as atherosclerosis. These...
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6303627 |
Inhibitors of serotonin reuptake
This invention provides compounds and a method for the inhibition of serotonin reuptake in mammals.
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6303593 |
3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: ##STR1## (wherein R 1 , R 2 , R 3 , R 4c , R 4d , and R 4f are defined herein) which are useful as modulators of...
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6294537 |
Compounds which are specific antagonists of the human NK3 receptor and their use as medicinal products and diagnostic tools
A method for treating diseases which involve interaction of neurokinin B with NK 3 receptors in humans. The method comprises administering a therapeutically effective amount of a NK 3 antagonist...
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6291478 |
Compounds of the benzylaminodiacetamide family, compositions comprising them, preparation process and uses
The present application relates to novel compounds belonging to the benzylaminodiacetamide family which have good anti-irritant and soothing properties. The invention also relates to their use in a...
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6288085 |
Piperidine derivatives for treating psychoses
The present invention relates to certain novel piperidine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy,...
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6284775 |
3-[4-(1-substituted-4-piperazinyl)butyl]-4-thiazolidinone and related compounds
There are disclosed compounds of the formula, ##STR1## where n is 0, 1 or 2; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy,...
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6281228 |
Heterocyclic inhibitors of microsomal triglyceride transfer protein and method
Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including...
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6277866 |
1-benzyl-4[(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl]methylpiperidine
The present invention provides a novel compound useful as a medicament, an acetylcholinesterase inhibitor, and an agent for preventing, treating and improving various kinds of senile dementia,...
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6262079 |
Prevention and treatment of cardiovascular pathologies
A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): ##STR1## wherein Z is CO or a covalent bond; Y is H or O(C 1 -C 4 )alkyl, R 1 and...
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6262060 |
Azacycloalkane derivatives, preparation and therapeutic application
The invention relates to azacycloalkane derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to methods for the treatment of hyperglycaemia, diabetes,...
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6221866 |
Indanyl-substituted benzenecarboxamides, processes for their preparation, their use as a medicament, and pharmaceutical formulations containing them
in which R(1) to R(8) have the meanings stated in the claims, act on the Kv1.5 potassium channel, and inhibit a potassium current, referred to as "ultra-rapidly activating delayed rectifier," in...
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6197791 |
N-hdroxy-2-(alkyl, aryl, or heteroaryl, sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors
Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases...
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6197789 |
Prevention and treatment of cardiovascular pathologies with tamoxifen analogues
A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): ##STR1## wherein Z is CO or a covalent bond; Y is H or O(C 1 -C 4 )alkyl, R 1 and...
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6193993 |
Suppository containing an antidementia medicament
The present invention provides a rectum applicable preparation containing an antidementia medicament, wherein the antidementia medicament is incorporated a triglyceride of a fatty acid and/or a...
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6190695 |
Pharmaceutical composition containing osteogenesis-promoting substance
This invention provides a pharmaceutical composition comprising a non-peptide osteogenesis-promoting substance and a polyethylene glycol or a derivative thereof, which can be advantageously used as...
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6177447 |
Deoxynojirimycin derivatives and their uses as glucosylceramidase inhibitors
Deoxynojirimycin derivatives containing a large hydrophobic moiety, such as cholesterol or adamantame-methanol, linked through a spacer, such as pentamethylene, to the nitrogen atom of...
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