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6200979 |
Methods of administering CRF antagonists
Substituted pyrrazoles of the formula ##STR1## wherein R 1 , R 2 , R 3 , X, Y, Z and A are as defined herein with reference to formula I; pyrazoles and pyzazolopyrimidines of the formula ##STR2##...
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6197771 |
Glutamate (ampa/kainate) receptor antagonists: N-substituted fused azacycloalkylquinoxalinediones
Novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones represented by the formula: ##STR1## or a pharmaceutically acceptable salt thereof, are disclosed, wherein the formula variables R...
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6197801 |
Injectable pharmaceutical composition for treatment and reversal of erectile dysfunction
An injectable pharmaceutical composition for treatment of erectile dysfunction. The composition includes prostaglandin E-1, and optionally further includes levsin and/or additional vasodilators...
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6197784 |
Process for controlling and destroying pathogenic small creatures, in particular insects and worms
Small creatures from the group of insects and worms which are pathogenic to humans, animals and plants can be controlled effectively by applying or introducing an aqueous percarboxylic acid...
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6194421 |
Inhibitors of metazoan parasite proteases
Compositions and methods are disclosed for treating a patient infected with a metazoan parasite by inhibiting the enzymatic action of the metazoan parasite protease, wherein there is employed at...
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6194468 |
Hair growth stimulants
A hair growth stimulant comprising p-menthane-3,8-diol and at least one substance from the group of a blood circulation promoter, a 5α-reductase inhibitor, an antihistaminic, a cell activator, an...
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6191144 |
Method of using angiotensin converting enzyme inhibitor to stimulate angiogenesis
The present invention is directed to the use of a group of ACE inhibitors to stimulate angiogenesis in mammals or in mammalian tissue in vitro. Specifically, the present invention is directed to...
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6187789 |
Substituted isoquinolines as ultra short acting neuromuscular blockers
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6184228 |
Anti-sickling agents: selection methods and effective compounds
The present invention is directed to a method for selecting compounds for use in treating sickle cell disease in a patient. The method comprises the steps of selecting a first set of HbS ligands...
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6180645 |
Annelated dihydropyridines and the use thereof for preparing pharmaceutical preparations
A compound of formula I ##STR1## wherein A denotes a benzo, indolo or thieno group; R 1 denotes thienyl or the group ##STR2## wherein R 7 , R 8 and R 9 independently of one another may...
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6177443 |
4,5,6,7-tetrahydro-thieno[3, 2-C]pyridine derivatives, their preparation and use
The present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier or diluent and a compound of formula I ##STR1## wherein A together with the double bond...
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RE37029 |
N-[(3-heteroaryl-1-pyrrolidinyl)-alkyl]phthalimides and related compounds and their therapeutic utility
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a...
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6174901 |
Substituted pyridine and pyridazine compounds and methods of use
Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-α, IL-1β, IL-6 and/or IL-8 mediated diseases, and other maladies,...
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6172081 |
Tetrahydroisoquinoline 3-carboxamide derivatives
Tetrahydroisoquinoline 3-carboxamide derivatives of formula ##STR1## and pharmaceutically acceptable salts thereof wherein: X is (a) CH 2 ; (b) S (c) O; or (d) C(CH 3 ) 2 ; R 1 ...
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6172085 |
Cyclic ether compounds as sodium channel modulators
A compound of the formula: ##STR1## wherein R 1 and R 2 each represents hydrogen, lower alkyl which may be substituted or acyl; R 3 , R 4 and R 5 each represents lower alkyl which may be...
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6166041 |
2-heteroaryl and 2-heterocyclic benzoxazoles as PDE IV inhibitors for the treatment of asthma
Novel compounds which are effective PDE IV inhibitors are disclosed. The present invention is directed to compounds having the general formula I ##STR1## wherein: X is a halogen; Q is --CH 2 ...
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6166037 |
Pyrrolidine and piperidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine and piperidine compounds of the formula I: ##STR1## (wherein R 1 , R 2 , R 3 , R 4a , R 4b , R 4c , R 4d , R 4e , R 4f , R 4g , R 4h , m, n, x and y...
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6162812 |
Pharmaceutical compositions containing HIV protease inhibitors and methods of their use
HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These...
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6153608 |
Isoquinoline derivatives and drugs
The invention relates to a compound of the following general formula [I] or a medicinally acceptable salt thereof, or a solvate thereof, ##STR1## wherein R 1 represents alkyl, alkenyl, alkynyl,...
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6143762 |
Tetrahydroisoquinoline derivatives and their pharmaceutical use
Compounds of formula (I), wherein R 1 represents a substituent selected from: a hydrogen or halogen atom; a hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, trifluoromethanesulfonyloxy, C...
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6140339 |
Monomeric and dimeric arylisoquinoline alkaloids and derivatives thereof
The present invention provides new monomeric derivatives of the C-8'-7 linked naphthylisoquinoline alkaloid dioncophylline D. The invention also provides new C-4 substituted monomeric...
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6140340 |
Derivatives of 2-[3-phenyl-2-propenyl]-1,2,3,4-tetrahydro isoquinoline, their process and their use as fungicides
Derivatives of 2-[3-phenyl-2-propenyl]-1,2,3,4-tetrahydro-isoquinoline compounds of the formula in all their possible stereoisomer forms as well as their mixtures ##STR1## wherein X is nitrogen or...
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6136826 |
Peripheral vasodilating agent containing piperidine derivative as active ingredient
The present invention relates to novel peripheral vasodilating agents characterized by each containing as an active ingredient, a piperidine derivative or pharmaceutically acceptable salt thereof...
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6130238 |
3-(cyclohexanoheteroarylidenyl)-2-indolinone protein tyrosine kinase inhibitors
The present invention relates to novel 3-(cyclohexanoheteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity...
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6127380 |
4-aminoalkoxy-1H-benzoimidazoles
This invention relates to D 2 dopaminergic compounds of the formula ##STR1## wherein: R 1 is hydrogen, trifluoromethyl, pentafluoroethyl, heptafluoropropyl, straight-chain or branched alkyl group...
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6127381 |
Isoquinoline compound melanocortin receptor ligands and methods of using same
The invention relates to melanocortin receptor ligands and methods of using the ligands to alter or regulate the activity of a melanocortin receptor. The invention further relates to...
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6124277 |
Antithrombotic agents
This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.
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6121283 |
Apo B-secretion/MTP inhibitory amides
This invention is directed to compounds of formula (I) or the stereoisomers, pharmaceutically acceptable salts and hydrates thereof. The compounds are Apo B/MTP inhibitors and are useful in the...
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6121293 |
Benzothiophene compounds, compositions, and methods
The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions...
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6117874 |
Benzopyran and benzo-fused compounds, their preparation and their use as leukotriene B.sub.4 (LTB.sub.4 ) antagonists
This invention relates to novel benzopyran and other benzo-fused leukotriene B 4 (LTB 4 ) antagonists and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing...
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6114328 |
Isoxazoline and isoxazole fibrogen receptor antagonists
This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to...
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6114367 |
Isoxazoline compounds as inhibitors of TNF release
This invention relates to isoxazoline compounds which are inhibitors of tumor necrosis factor (TNF). The isoxazoline compounds are useful for inhibiting TNF in a mammal in need thereof and in the...
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6110933 |
Amino acid derivatives and their use as phospholipase A.sub.2 inhibitor
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6110934 |
Substituted benzamide derivatives and their use as anticonvulsants
This invention relates to substituted benzamido-heterocyclic compounds of general formula (I) having an alkoxy substituent at the C2 position of the benzamido group and various substituents at...
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6107308 |
Piperidine derivatives
The present invention is directed to a piperidine derivative represented by the following formula (1) or a salt thereof: ##STR1## wherein R 1 , R 2 , and R 3 individually represent hydrogen atoms,...
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6100276 |
Isatin derivatives as acetylcholinesterase inhibitors and analgesics
This application relates to compounds of the formula ##STR1## wherein R, X and Y are defined within, which compounds are useful for the treatment of memory dysfunction characterized by decreased...
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6093729 |
Substituted bicyclic heteroaroylguanidines, a process for their preparation, their use as a medicament or a diagnostic agent, and a medicament containing them
Substituted bicyclic heteroaroylguanidines, a process for their preparation, their use as a medicament or a diagnostic agent, and a medicament containing them are described, as are the...
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6077849 |
Antidiabetic agents
Compounds of formula I: ##STR1## as well as tautomers, pharmaceutically acceptable salts, hydrates, prodrugs and reduced forms are disclosed. The compounds are useful for the treatment and...
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6066672 |
Amino compounds and angiotensin IV receptor agonists
The present invention provides an amino compound represented by Formula: ##STR1## wherein X is CH 2 NH or CONH, Y is CH 2 NH or CONH with the proviso that X and Y are not CONH at the same time; Z...
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6066650 |
Inhibitors of microsomal triglyceride transfer protein and method
Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the...
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6060488 |
Benzothiophenes for treating estrogen deficiency
This invention is related to novel benzothiophene compounds of formula I: ##STR1## where R, R 1 , R 2 , X and m are as defined in the specification, which are useful for the inhibition of the...
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6046191 |
Combination
The invention relates to the co-administration of an inhibitor of induced nitric oxide synthase and an inhibitor of cyclooxygenase-2 for the treatment of inflammation and inflammatory disorders.
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6046210 |
Tetrahydroisoquinoline derivatives as modulators of dopamine D.sub.3 receptors
This invention relates to compounds of formula (I): ##STR1## which are useful as modulators of D 3 receptors, in particular in the treatment of psychoses.
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6043253 |
Fused piperidine substituted arylsulfonamides as β3-agonists
Fused piperidine substituted arylsulfonamides are β 3 adrenergic receptor agonists with very little β 1 and β 2 adrenergic receptor activity and as such the compounds are capable of...
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6043263 |
(2,3-dihydrobenzofuranyl)-thiazoles as phosphodiesterase inhibitors
The invention relates to compounds of the formula (I), wherein R1, R2, R3, R4, R5 and n have the meanings cited in the description said compounds being new effective bronchial therapeutic agents.
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6040340 |
Implantation rates after in vitro fertilization, treatment of infertility and early pregnancy loss with a nitric oxide donor alone or in combination with progesterone, and a method for contraception with nitric oxide inhibitors
A method is provided for the improvement of implantation rates and/or pregnancy rates in a female mammal, comprising administering to a female mammal in whom pregnancy is desired an effective...
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6040314 |
Bicyclic isothiourea derivatives useful in therapy
There are provided novel compounds of formula I ##STR1## wherein D represents alkyl C1 to 6; T represents a C 3 -5 saturated or unsaturated alkylene chain substituted by --(CH 2 ) m -- NXY;...
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6034096 |
Compounds with anti-inflammatory and immunosuppressive activities
The present invention provides medicinal compounds that are characterized by a cyclic moiety (A) linked through a carboxamido group (more specifically, a carbamate group or a urea group) to another...
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6034094 |
Pharmaceutically useful 3,4-dihydroisoquinoline
The invention relates to the use of carbocyclically and heterocycally fused dihydroyridines as cerebroprotective agents, as agents for treating chronic inflammatory processes and as agents for...
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6030985 |
Amidine derivatives with nitric oxide synthetase activities
The present invention relates to methods and compositions useful for treating and preventing conditions in which inhibition of nitric oxide synthetase is beneficial. These conditions include...
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