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6384028 |
N-acylpiperidinylcarbonylaminocarboxylic acids and their use as glycoprotein IIb/IIIa antagonists and fibrinogen-blood platelets binding inhibitors
β-alanine compounds or a pharmaceutically acceptable salt thereof, which is useful as a glycoprotein IIB/IIIa antagonist, inhibitor of blood platelet aggregation and inhibitor of the binding of...
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6369228 |
Aroyl aminoacyl pyrroles for use in the treatment of neuropathic pain
Aroyl aminoacyl pyrroles are pharmaceutically useful in treating neuropathic pain, which includes utility for the treatment of neuropathic pain.
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6362193 |
Cycloalkenyl substituted compounds
Novel pyridyl or pyrimidinyl substituted cycloalkenyl compounds and compositions for use in therapy.
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6358974 |
Isoquinoline derivatives
Compounds of formula (I) wherein: R 1 represents a substituent selected from: a hydrogen or halogen atom; a hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, trifluoromethanesulfonyloxy,...
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6350760 |
Substituted piperidines as melanocortin-4 receptor agonists
Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are...
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6344570 |
Substituted urea derivatives as cell adhesion inhibitors
Compounds of formula (II) where R 1 is in the para or meta position and is (A); R 2 and R 3 are each independently selected from hydrogen, nitro, C 1-6 alkyl, C 3-6 cycloalkyl, C 2-6 alkenyl,...
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6340760 |
Process for the preparation of (S)-N-tert-butyl-1,2,3,4-tetrahydroisoquinoline-3-carboxyamide
A description is given here of a novel process for the synthesis of N-carboxyanhydride of formula VI by reacting (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid with triphosgene in...
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6331545 |
Heterocycyclic piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): ##STR1## or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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6329377 |
Ketomethylene group-containing cysteine and serine protease inhibitors
The present invention is directed to novel ketomethylene group-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.
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6323215 |
Neurotrophic tetrahydroisoquinolines and tetrahydrothienopyridines, and related compositions and methods
This invention provides compounds having the following general structure: ##STR1## This invention also provides pharmaceutical compositions comprising same and methods of using these compositions...
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6307049 |
Heterocyclic 2-substituted ketoamides
The present disclosure describes novel compounds and compositions which are particularly useful for treating hair loss in mammals, including arresting and/or reversing hair loss and promoting hair...
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6303628 |
Bicycliccarbonyl indole compounds as anti-inflammatory/analgesic agents
This invention provides a compound of the following formula: ##STR1## or the pharmaceutically acceptable salts thereof wherein A is C 1 -6 alkylene or --NR 1 --; Z is C(L)R 2 , or SO 2 R 3 ;...
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6303786 |
Processes for making nelfinavir mesylate
HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel...
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6300501 |
Histidine-(N-benzyl glycinamide) inhibitors of protein farnesyl transferase
Inhibitors of protein farnesyl transferase enzymes are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating cancer,...
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6300342 |
Antithrombotic phenylalkyl derivatives
Antithrombotic phenylalkyl derivatives of the formula ##STR1## Exemplary compounds are: (a) 1-[3-(4-amidino-phenyl)propionyl]-6-(4-fluoro-phenylsulphona
mido)-1,2,3,4- tetrahydro-quinoline, ...
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6294551 |
N-linked sulfonamides of heterocyclic thioesters
This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as...
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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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6274593 |
Substituted tetrahydro isoquinolines as modulators of dopamine D3 receptors
The present invention provides compounds of formula (I): ##STR1## which are useful as antipsychotic agents.
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6271236 |
Diaminopyridine-containing thiourea inhibitors of herpes virus
Compounds of the formula ##STR1## wherein R 1 -R 5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms,...
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6265408 |
Sulphonamide derivatives and their use in the treatment of CNS disorders
Sulphonamide compounds according to formula (I) or pharmaceutically acceptable salts thereof: ##STR1## wherein: Ar is naphthyl, phenyl or thienyl optionally substituted by one or more...
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6262074 |
4-Hetaroylpyrazol derivatives and the use thereof as herbicides
Hetaroyl derivatives of the formula I ##STR1## where: R 1 and R 2 are each hydrogen, nitro, halogen, cyano, thiocyanato, hydroxyl, mercapto, C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, C 1 -C 6 ...
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6239126 |
Arylpiperidine and aryl-1,2,5,6-tetra-hydropyridine urea derivatives
Compounds of the formula ##STR1## are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep...
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6231786 |
Fluorinated azoles, and their use in liquid-crystalline mixtures
In the fluorinated azoles of the formula (I) R 1 (--A 1 ) a --T--(A 2 --) b (M--A 3 --) c R 2 (I) the symbols and indices have -the following meanings: T is undirected and is ...
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6228867 |
Antagonists of gonadotropin releasing hormone
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety...
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6218393 |
Anthranilic acid derivatives as multi drug resistance modulators
Anthranilic acids of formula (I): ##STR1## wherein each of R to R 9 is an organic substituent, n is 0 or 1, m is 0 or an integer of 1 to 6, q is 0 or 1, X is a direct bond, O, S, --S--(CH 2 ) p ...
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6214841 |
Antithrombotic compound
This application relates to a novel compound of formula (I) (or a pharmaceutically acceptable salt thereof) as defined herein, processes and Intermediates for its preparation, pharmaceutical...
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6211373 |
Phenyl urea antagonists of the IL-8 receptor
This invention relates to novel compounds of Formula (I), and a novel use of these compounds in treating chemokine mediated diseases, wherein the chemokine binds to an IL-8 a or b receptor....
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6211196 |
Benzyloxy-substituted, fused N-heterocycles, processes for their preparation, and their use as bradykinin receptor antagonists
Benzyloxy-substituted, fused N-heterocycles, because of their ability to act as bradykinin receptor antagonists, have been found to be useful as therapeutics for the treatment and prevention of...
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RE37094 |
Heterocyclic substituted acylaminothiazoles, their preparation and pharmaceutical compositions containing them
Compounds of formula ##STR1## in which R 1 represents H, an alkyl or a substituted alkyl, R 2 represents H or alkyl and R 3 represents an optionally substituted cycloalkyl or an optionally...
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6200957 |
Antagonists of gonadotropin releasing hormone
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety...
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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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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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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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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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6150335 |
Tic-containing opioid dipeptide derivatives useful as analgesics
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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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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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6107316 |
Method for treating protozoal infections
A method for treating protozoal infections is described. The method employs N-acetonylbenzamide compounds provided in an effective amount to inhibit the growth of protozoans. The compounds are...
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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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6100238 |
Indole and tetrahydroisoquinoline containing Alpha-keto oxadiazoles as serine protease inhibitors
The present invention relates to certain substituted oxadiazole nonpeptides, which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated...
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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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6077864 |
Cyclic sulfone derivatives
A compound of the formula ##STR1## wherein n, X, Y and Ar are as defined herein, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration,...
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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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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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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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6025367 |
Sulfonamide derivatives as 5HT.sub.7 receptor antagonists
The invention relates to sulphonamide compounds of formula (I) or a salt thereof having pharmacological activity, processes for their preparation, to compositions containing them and to their use...
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