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7365063 |
Quinazolinone and benzoxazinone derivatives and uses thereof
Compounds of the formula I:
and pharmaceutically acceptable salts thereof wherein X is N, Y is S, Z is —(CR a R b ) r —, A is —NR 3 , m is 2, n is 1, q is 2, R 2 is optioinally...
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7358239 |
Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z...
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7341749 |
Flavopereirine and alstonine combinations in the treatment and prevention of prostate cancer
A method and composition for preventing prostate cancer and/or reducing PSA levels and/or alleviating the symptoms of BPH (Benign Prostatic Hyperplasia) or PIN (prostatic intraepithelial neoplasia)...
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7262189 |
Benzothiazine and benzothiadiazine derivatives, method for preparing same and pharmaceutical compositions containing same
Compounds of formula (I):
wherein:
R 1 represents aryl or heteroaryl, R 2 represents hydrogen, halogen or hydroxy, X represents oxygen or sulphur, Y represents oxygen, sulphur or NR wherein...
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7105511 |
Fluorescent fused-ring triazoles that inhibit cell proliferation and uses thereof
Fused-ring triazole compounds which inhibit proliferation of cells and exhibit a unique and intense fluorescence are provided. Also provided are methods for synthesizing these compounds and methods...
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7084136 |
Drug composition antagonistic to both PGD2/TXA2 receptors
A compound of the formula (I):
wherein A is alkylene optionally having an unsaturated bond; R is —C(═O)—R 1 ; R 1 is hydroxy or the like; m is 0 or 1; p is 0 or 1; X 1 and X 3 are each...
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6943158 |
Diazinopyrimidines
Compounds of formula I are p38 inhibitors:
or a pharmaceutically acceptable salt thereof,
wherein
R 1 is hydrogen or alkyl; R 2 alkyl, haloalkyl, aryl, aralkyl, heteroaryl,...
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6900222 |
Pyrrolidinyl, piperdinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein...
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6884285 |
Delivery system for wood treatment chemicals
A wood treatment concentrate includes, by weight;
(a) 0.1-10% of an active wood treatment chemical, (b) 50-99% of a microemulsion concentrate including:
(i) 0.03-80%, preferably 40-70%, of a...
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6858228 |
Solid oral dosage forms of valsartan
The present invention is concerned with solid oral dosage forms of comprising
a) an active agent selected from valsartan and optionally HCTZ, and b) Pharmaceutically acceptable additives...
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6844338 |
Piperidyindoles as serotonin receptor ligands
A pharmaceutical compound of the formula (I) in which R 1 and R 2 are each hydrogen or C 1-6 alkyl, R 3 is —SR 10 , —SOR 10 , —SO 2 R 10 , —COR 10 , —CH 2 OH or —CONHR 11 , where R...
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6743817 |
Substituted fused pyrroleimines and pyrazoleimines
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R 1 and R 2 are defined herein. These compounds are highly selective agonists,...
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6667306 |
Platelet ADP receptor inhibitors
The invention relates to novel compounds of formula (I) containing fused heterocyclic ring systems which are effective platelet ADP receptor inhibitors: In formula (I), W is carbon or nitrogen,...
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6656932 |
Benzo thiadiazine matrix metalloproteinase inhibitors
Selective MMP-13 inhibitors are benzo thiadiazines of the Formula or a pharmaceutically acceptable salt thereof, wherein R 2 is hydrogen or alkyl; R 1 and R 3 include hydrogen, alkyl, and...
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6642222 |
Pyrano, piperidino, and thiopyrano compounds and methods of use
The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder...
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6635635 |
Benzothiadiazine compounds
Compound of formula (I): wherein: R 1 represents hydroxy, RCO—O— or RCO—NR a —, R 2 represents hydrogen, halogen, or hydroxy, R′CO—O or R′CO—NR′ a —, R and R′, which may...
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6630464 |
Cyclin dependent kinase (CDK)4 inhibitors and their use for treating cancer
Certain derivatives of acridones and benzothiadiazines have been found to have anti-cancer properties by virtue of their specific inhibition of the cyclin D dependant kinase CDK4. These molecules...
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6583155 |
Method for treating allergies using substituted pyrazoles
A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
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6569852 |
Coatings and soaks for medical prosthetic devices comprising taurinamide derivatives and carboxylic acids and/or salts thereof
The present invention relates to a method of inhibiting or preventing infection and blood coagulation in or near a medical prosthetic device after the device has been inserted in a patient by...
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6541469 |
CRF receptor antagonists and methods relating thereto
CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded...
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6485745 |
Solid oral dosage forms of valsartan
The present invention is concerned with solid oral dosage forms of comprising a) an active agent selected from valsartan and optionally HCTZ , and b) Pharmaceutically acceptable additives suitable...
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6436927 |
IL-8 receptor antagonists
The present invention involves certain 8-ureido and 8-thioureido, 1,2-benzothiazines, 1,2,4-benzothioxazines and 1,2,4-benzothiodiazines useful in the treatment of disease states mediated by the...
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6329367 |
Fused 1,2,4-thiadiazine derivatives, their preparation and use
The present invention relates to 4H-thieno[3,2-e]-1,2,4-thiadiazine derivatives of the general formula: ##STR1## wherein X, Y, R 1 , R 2 and R 3 are defined in the description, compositions...
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6329366 |
Pharmaceutical compounds
A pharmaceutical compound of the formula ##STR1## in which R 1 and R 2 are each hydrogen, halo, cyano or methyl, the dotted line represents an optional double bond, ##STR2## where R 4 and R 5...
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6316441 |
Brinzolamide and brimonidine for treating glaucoma
Methods and compositions for treating ocular conditions which find their etiology in compromised ocular blood flow with brinzolamide and brimonidine are disclosed.
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6271264 |
Polymers containing spirobicyclic ammonium moieties as bile acid sequestrants
The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises administering a therapeutically effective...
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6242442 |
Brinzolamide and brimonidine for treating ocular conditions
Methods and compositions for treating ocular conditions which find their etiology in compromised ocular blood flow with brinzolamide and brimonidine are disclosed.
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6242441 |
Use of brinzolamide to prevent visual field loss
Methods for preventing or slowing visual field loss are disclosed.
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6242440 |
Synergistic compositions comprising an oxathiazine and a benzothiophene-2-carboxamide-S,S-dioxide
This invention relates to synergistic compositions of oxathiazines and benzothiophene-2-carboxamide-S,S-dioxides for use as fungicidal preservatives in the protection of materials, such as...
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6225310 |
Fused 1,2,4-thiadiazine derivatives, their preparation and use
1,2,4-Thiadiazine and 1,4-thiazine derivates represented by formula (I): ##STR1## wherein A, B, D, R 1 , R 2 , R 3 and R 4 are defined in the description, compositions thereof and methods for...
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6197766 |
Insecticidal dihydrooxadiazine compounds
Insecticidal dihydrooxadiazine compounds having the formula: ##STR1## wherein X is O, N or S; R is a substituted or unsubstituted phenyl or C 4 -C 5 heterocyclic group; R 2 , R 3 , R 4 ,...
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6121278 |
Di-n-heterocyclic compounds, methods, and compositions for inhibiting parp activity
A compound of formula I: ##STR1## or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein: Y represents the atoms necessary...
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6071904 |
Process for manufacturing ophthalmic suspensions
Ophthalmic suspensions containing brinzolamide or brinzolamide and a beta-blocker and processes for manufacturing the suspensions are disclosed.
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6011034 |
Insecticidal dihydrooxadiazine compounds
Insecticidal dihydrooxadiazine compounds having the formula: ##STR1## wherein X is O or S; R is a substituted or unsubstituted phenyl or heterocyclic group; R 1 is halogen, haloalkyl or...
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6004948 |
Derivatives of benzosulphonamides as inhibitors of the enzyme cyclooxygenase II
Compounds of the formula (I) in which A is oxygen, sulphur or NH; B is a group of the formula (IIa) or (IIb); and the other variables have the meaning given in claim 1, may be used as inhibitors of...
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5985871 |
Benzoxazine compounds for enhancing synaptic response
Compounds having a certain benzoxazine ring system and their precursors are disclosed which are useful for enhancing synaptic responses mediated by AMPA receptors. Also disclosed are methods for...
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5929114 |
Arylthio compounds
Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O,...
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5929072 |
1H-2,1,3-benzothiadiazine-2,2-dioxide compounds or derivatives thereof
A pharmaceutical compound having the formula: ##STR1## in which n is 1 or 2, m is 1 or 2, p is 1 to 6, q is 0 or 1 to 3, R 1 and R 2 are each hydrogen or C 1 -4 alkyl, R 3 , R 4 and R 5 ...
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5925641 |
Farnesyltransferase inhibitor
The present invention relates to a farnesyltransferase inhibitor and an antitumor agent comprising, as an active ingredient, a piperazinedione derivative represented by formula (I): ##STR1##...
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5889002 |
Fused 1,2,4-thiadiazine and fused 1,4-thiazine derivatives, their preparation and use
1,2,4-Thiadiazine and 1,4-thiazine derivatives represented by the formula ##STR1## wherein A, B, D, R 1 , R 2 , R 3 and R 4 are defined in the description, compositions thereof and methods for...
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5792764 |
Pyrido-1,2,4-thiadiazine and pyrido-1,4-thiazine derivatives, their preparation and use
Pyrido-1,2,4-thiadiazine and pyrido-1,4-thiazine derivatives represented by the formula ##STR1## wherein A, B, D, R 1 , R 2 , R 3 and R 4 are defined in the description, compositions thereof and...
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5744478 |
Thiazolo 3,2-a! quinoline and thiazolo 3,2-a! naphthyridine derivatives
The present invention relates to new thiazolo 3,2-a!quinoline and thiazolo 3,2-a!naphthyridine derivatives of the general formula (I) ##STR1## in which R 1 , R 2 , Z and X have the meaning...
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5728693 |
Arthropodicidal oxadiazine-thiadiazine-or triazine-carboxanilides
Arthropodicidal compounds, compositions and use of compounds having the formula ##STR1##
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5698553 |
Benzylpiperidine derivatives
A benzylpiperidine compound of formula I ##STR1## in which R 1 is H, Hal or nitro, R 2 is a benzyl group, which is unsubstituted or substituted by Hal on the aromatic portion, in the 2-, 3- or...
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5646139 |
Antimicrobial carbapenem quinolones
Compounds of Structure: ##STR1## as well as their pharmaceutically-acceptable salts and biohydrolyzable esters, and hydrates thereof, are effective antiinfective agents, useful in treating and...
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5627179 |
Magnesium salt of 3-isopropyl-2, 1, 3-benzothiadiazin -4-one 2,2-dioxide, its preparation and its use for controlling undesirable plant growth
Solid, non-hygroscopic magnesium salt of 3-isopropyl-2,1,3-benzothiadiazin-4-ones 2,2-dioxide (I), processes for its preparation, solid formulations, in particular granules, which contain this...
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5620970 |
Topical ophthalmic carbonic anhydrase inhibitor formulations
The present invention is directed to topical ophthalmic formulations of carbonic anhydrase inhibitors and polyethoxylated derivatives of castor oil. Methods for using the formulations for treating...
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5589477 |
Pyrimidine derivatives and drugs
The object of the present invention is to obtain new class of compounds which have improving effect on learning and memory disorders with good selectivity in central nervous system and little side...
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5583101 |
Use of nitrogen oxide species and adducts to inhibit skeletal muscle contraction
A method for inhibiting or relaxing skeletal muscle contractions which comprises contacting said skeletal muscle with a skeletal muscle relaxing amount, and a method for the treatment of disease...
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5580889 |
Insecticidal nitromethyl or niteoimino-heteromethyl-heterocyclics
Novel insecticides of the formula ##STR1## in which n is 0 or 1, X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R 9 variously...
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