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6617329 |
Aminoquinazolines and their use as medicaments
Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the...
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6613772 |
Substituted 2-aryl-4-amino-chinazolines, method for the production and use thereof as medicaments
Compounds of the formula I in which R 1 , R 2 , R 3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and...
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6566361 |
Azapirone pain treatment
A method of treating pain with acetaminophen comprises the concurrent administration of an azapirone such as buspirone. This combination of agents surprisingly results in a strengthened analgesic...
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6559186 |
Compositions and methods of treatment of sympathetically maintained pain
Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other...
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6500830 |
Conversion of modification D to modification A of doxazosin mesylate
A process for preparing doxazosin mesylate in modification A which comprises dissolving doxazosin with methanesulfonic acid in methanol or a mixture of an aprotic, polar organic solvent and...
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6489333 |
Integrin antagonists
This invention relates to novel heterocycles which are useful as antagonists of the α v β 3 integrin, the α 2b β 3 integrin, and related cell surface adhesive protein receptors, to...
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6479496 |
Methods for treating angina with ranolazine
A sustained release ranolazine formulation contains an intimate mixture of ranolazine and a partially neutralized pH-dependent binder to form a film that is mostly insoluble in aqueous media below...
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6476037 |
L-arginine and phosphodiesterase (PDE) inhibitor synergism
This invention pertains to the discovery that L-arginine and type V phosphodiesterases act synergistically to inhibit vasospasm and/or to induce vasodilation. Methods are provided using...
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6476033 |
Medicaments containing doxazosin mesylate of crystalline modification D
Drugs comprising modification D of doxazosin mesylate are described. They are suitable for treating high blood pressure.
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6423716 |
Nitrogenous heterocyclic compounds
The present invention relates to nitrogen-containing heterocyclic compounds represented by formula (I): wherein W represents 1,4-piperazinediyl, etc.; U represents NR 1 R 2 (wherein R 1 ...
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6407116 |
Nitrogenous fused-ring compounds, process for the preparation of the same, and drugs
A compound represented by the formula: [wherein ring A represents a homocycle optionally having substituents or a nitrogen-containing heterocycle optionally having substituents; D and E are O or...
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6391874 |
Fused heterocyclic compounds as protein tyrosine kinase inhibitors
Substituted heteroaromatic compounds of formula (I) and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for...
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6365590 |
Compounds, compositions and methods for treating erectile dysfunction
Vasoactive compounds are described for the treatment of erectile dysfunction and impotence. The compounds are reaction products of an anionic or negatively charged vasoactive or erection-inducing...
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6344449 |
Modified aminoacids, pharmaceuticals containing these compounds and method for their production
The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R 2 , R 3 , R 4 and R 11 are defined as in claims 1 to 5, their tautomers, their...
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6337332 |
Neuropeptide Y receptor antagonists
Compounds of the structures are useful for treating conditions related to an excess of neuropeptide Y including obesity and circulatory disorders.
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6291455 |
4-anilinoquinazoline derivatives
The invention relates to quinazoline derivatives of formula (I) (wherein: R 1 represents hydrogen or methoxy; R 2 represents methoxy, ethoxy, 2-methoxyethoxy, 3-methoxypropoxy, 2-ethoxyethoxy,...
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6265411 |
Oxindole derivatives
The invention relates to compounds of formula (I), ##STR1## wherein: R 2 represents hydroxy, halogeno, C 1 -3 alkyl, C 1 -3 alkoxy, C 1 -3 alkanoyloxy, trifluoromethyl, cyano, amino, nitro,...
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6251912 |
Substituted quinazoline derivatives
This invention provides compounds of formula 1 having the structure ##STR1## wherein: X, R 1 , R 2 , R 3 , R 4 , Z, X, and n are as defined hereinbefore in the specification, which are useful as...
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6225315 |
Method of treating nitrate-induced tolerance
The present invention relates to methods for treating nitrate-induced tolerance in a mammal by administering a nitrate-induced tolerance treating amount of a compound of formulae (I), (II), (III)...
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6204267 |
Methods of modulating serine/thereonine protein kinase function with quinazoline-based compounds
The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with quinazoline-based compounds. The methods incorporate cells that express...
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6177430 |
Use of α1-adrenoreceptor antagonists in the prevention and treatment of benign prostatic hyperplasia
A method for reducing the extent of or preventing further hyperplasia in BPH in a mammal which comprises administering to said mammal an effective amount of a drug comprising an α 1 ...
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6172072 |
Heterocyclically substituted benzamides and their use in fighting diseases
Heterocyclically substituted benzamides of the formula I ##STR1## are described, where R 1 , R 2 , R 3 , R 4 , R 5 , X, m and n have the meanings given in the description. The novel compounds are...
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6169093 |
Quinoline and quinazoline compounds useful in therapy, particularly in the treatment of benign prostatic hyperplasia
Compounds of formula I, ##STR1## wherein R 1 represents C 1 -4 alkoxy optionally substituted by one or more fluorine atoms; R 2 represents H or C 1 -6 alkoxy optionally substituted by one...
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6166019 |
Piperazinyl pyrimidine dione compounds selective for adrenoceptors
Compounds of Formula I and II and their pharmaceutically acceptable, salts, esters and prodrugs thereof are selective alpha-1D adrenoceptor anatagonists and may be useful for treating disease states.
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6153617 |
Irreversible bicyclic inhibitors of tyrosine kinases
The invention provides compounds of Formula I ##STR1## that are irreversible inhibitors of tyrosine kinases. Also provided is a method of treating cancer, restenosis, atherosclerosis,...
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6140334 |
Polymorphic form of doxazosin mesylate (form III)
A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of...
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6136848 |
Flavone derivative and medicine comprising the same
This invention relates to a flavone derivative represented by the formula (1) or a salt thereof, and also to a medicine containing the same. ##STR1## wherein A represents H, halogen, phenyl,...
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6127373 |
Method of treating tourette's syndrome and obsessive compulsive disorder
A method for treating Tourette's syndrome, obsessive compulsive disorder, chronic motor or vocal tic disorder in a mammal, including a human, comprising administering to said mammal an effective...
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6124306 |
Thioalkyl alpha substituted pyrimidine compounds
The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula I ##STR1## and pyrimidine-thioalkyl and alkylethers of Formula I, where R 4 is selected from the group...
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6037346 |
Local administration of phosphodiesterase inhibitors for the treatment of erectile dysfunction
A method is provided for treating erectile dysfunction in a mammalian male individual. The method involves the local administration of a phosphodiesterase inhibitor or a pharmaceutically acceptable...
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6030973 |
Heterocyclic compounds having antidiabetic hypolipidemia and antihypertensive properties, process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their analogues, their stereoisomers, their polymorphs, their pharmaceutically acceptable...
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5977110 |
Substituted cyclohexylamines as central nervous systems agents
Substituted cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents...
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5948799 |
Method for improving morbidity and/or mortality
This invention relates to a method for reducing morbidity and/or mortality in a mammal with congestive heart failure due to non-ischemic etiology comprising administering amlodipine or a...
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5942545 |
Composition and method for treating penile erectile dysfunction
A composition for the topical transdermal administration to the penis is based on prostaglandin E 1 . The composition is non-irritating and effective for relieving erectile impotence or other...
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5935962 |
Use of α.sub.1 -adrenoreceptor antagonists in the prevention and treatment of cancer
A method for treating or preventing a cancer in a mammal which comprises administering to said mammal an amount of a drug, comprising an α 1 -adrenoreceptor antagonist or pharmaceutically...
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5932574 |
Quinazoline derivatives
The invention concerns quinazoline derivatives of formula wherein n is 1, 2 or 3 and each R 2 is independently halogeno; and R 1 is di- (1-4C)alkyl!amino-(2-4C)alkoxy,...
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5912247 |
Quinazoline compound and anti-tumor agent containing said compound as an active ingredient
A quinazoline compound of the formula (I): ##STR1## wherein Z means a group of the formula: ##STR2## (X is CH 2 , CHOH, CHOCH 3 , or O, and n is 1 to 3), or a group of the formula: ##STR3## (A is H...
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5874438 |
2,2'-bridged bis-2,4-diaminoquinazolines
The present invention relates to 2,2'-bridged bis-2,4-diaminoquinazolines of the general formula (I): ##STR1## in which the indicated substituents are as defined in the description. The invention...
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5837708 |
Sulphonamides
Compounds of the formula ##STR1## wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders...
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5830909 |
Angiotensin (AII) antagonists as inhibitors of the growth of adipose tissue
The invention is a method of using Angiotensin (AII) Antagonists as inhibitors of the growth of adipose tissue, reducing adipocyte growth and body weight gain.
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5821246 |
Aniline derivatives
The invention concerns aniline derivatives of formula I ##STR1## wherein m is 1, 2 or 3, n is 0, 1, 2 or 3, Q is phenyl or naphthyl or a 5- or 6-membered heteroaryl moiety containing 1, 2 or 3...
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5814630 |
Quinazoline compounds
The invention concerns quinazoline compounds of the formula I ##STR1## wherein Q 1 is a 5- or 6-membered heteroaryl moiety and Q 1 optionally bears up to 3 substituents; wherein m is 1 or 2...
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5798362 |
Quinazolinyl-amino derivatives having α-antagonist activity
New qunazolinyl-amino derivatives useful as α 1 -adrenoreceptor blockers are described. These compounds can be used as therapeutic agents for treating afflictions and diseases related to...
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5783576 |
Benzoyl guanidine derivatives, the preparation thereof and their use in pharmaceutical compositions
New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.
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5773444 |
Quinazolines as inhibitors of endothelin converting enzyme
Novel quinazoline inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated...
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5760029 |
Spirocycle integrin inhibitors
This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspi ro- 4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are...
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5753641 |
Method of treatment for benign prostatic hyperplasia
Disclosed is an improved treatment for men with benign prostatic hyperplasia (BPH), involving combination therapy of a 5α-reductase inhibitor, e.g. a 17β-substituted 4-azasteroid, a...
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5747490 |
Alpha 1b adrenergic receptor antagonists
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1b adrenergic receptor antagonists. These compounds display...
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5739127 |
2,4'-bridged bis-2,4-diaminoquinazolines
The present invention provides 2,4'-bridged bis-2,4-diaminoquinazolines of the general formula (I): ##STR1## in which the indicated substituents are as defined in the description. The invention...
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5707999 |
Use of alfuzosin or terazosin in the treatment of premature ejaculation
The method of use of the α-1 blockers, alfuzosine and terazosine, in the treatment of premature ejaculation is disclosed.
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