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6018052 |
Fungicidal optically active 1-(mono-or substituted amino)-2-substituted-4,4-disubstituted-2-imidazolin-5-ones and 5- thiones corresponding
Fungicidal 2-imidazolin-5-ones and 2-imidazoline-5-thiones, processes for their preparation, fungicidal compositions containing them and methods of using them to treat or prevent fungal disease in...
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6015900 |
N-aminoalkylfluorenecarboxamides
Disclosed are compounds of formula (I) or the pharmaceutically acceptable salts thereof wherein: ##STR1## G represents a group of the formula (a), (b) or (c) where R a and R b represent hydrogen,...
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6001851 |
HIV protease inhibitors
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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5998379 |
Serine protease inhibitors-proline analogs
The present invention relates to certain substituted oxadiazole, thiadiazole, and triazole peptoids that are useful as inhibitors of serine proteases, in particular human neutrophil elastase....
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5998624 |
Haloisoquinoline carboxamide
Compounds of the invention have the general structure ##STR1## X, Y or Z are, respectively independently, H, F or an isotope thereof, Br or an isotope thereof, I or an isotope thereof, At or an...
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5994507 |
Method for binding albumin and means to be used in the method
A method for binding albumin by contacting an aqueous liquid containing an albumin with an albumin-binding compound is selected from albumin-binding compounds containing the scaffold...
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5977367 |
N-aminoalkyldibenzofurancarboxamides; new dopamine receptor subtype specific ligands
Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R 1 , R 2 , R 3 , R 4 are the same or different and represent hydrogen, C...
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5965562 |
Aroyl-piperidine derivatives
The invention relates to novel N-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-4-(azanaphthoyl
-amino)-piperi dines of the formula ##STR1## wherein X and Y are each independently of the other N and/or...
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5962471 |
Substituted 6- and 7-aminotetrahydroisoquinolinecarboxylic acids
Compounds of the formula I ##STR1## are suitable for the preparation of pharmaceuticals for the prophylaxis and therapy of disorders involving increased activity of matrix-degrading...
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5955471 |
Tetrahydroisoquinolinealkanol derivatives and pharmaceutical compositions containing same
The present invention provides novel 1,2,3,4-tetrahydroisoquinoline carbamate and thiocarbamate derivatives represented by Formula I ##STR1## wherein: X 1 and X 2 are the same or different from...
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5952328 |
Benzothiazo and related heterocyclic group-containing cysteine and serine protease inhibitors
The present invention is directed to novel benzothiazo and related heterocyclic group-containing inhibitors of cysteine or serine proteases. Methods for using the same are also described.
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5948779 |
Substituted condensation products of n-benzyl-3-indenyl acetamides with heterocyclic aldehydes
Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell...
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5948778 |
Difluoro statone antiviral analogs
This invention relates to novel statone antiviral analogs, to the processes and intermediates useful for their preparation and to their use as antiviral agents.
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5936089 |
Dipeptides which promote release of growth hormone
Compounds of formula (I) are growth hormone releasing peptide mimetics which are useful for the treatment and prevention of osteoporosis. ##STR1##
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5904877 |
Trifluoratetrahydroisoquinoline derivatives, and the use thereof in liquid-crystalline mixtures
1,8,8-Trifluoro-5,6,7,8-tetrahydroisoquinoline derivatives, and their use in liquid-crystalline mixtures 1,8,8-Trifluoro-5,6,7,8-tetrahydroisoquinoline derivatives of the formula (I) R 1 (--M 1...
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5885985 |
Guanidine derivatives useful in therapy
Guanidine derivatives of formula I ##STR1## wherein R 8 represents hydrogen, halogen, alkyl C1 to 6, nitro, trifluoromethyl, thioalkyl C1 to 6, hydroxy, alkoxy C1 to 6, or a group selected from...
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5883257 |
N-piperidinyl- and N-tetrahydropyridinyl-2-anthracenecarboxamides: dopamine receptor subtype specific ligands
Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are the same or...
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5863950 |
HIV protease inhibitors
HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well...
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5861412 |
Dihydro-isoquinoline compounds and their use as pharmaceuticals
Compound of general formula I ##STR1## wherein A is a benzo or thieno group; R 1 is (C 4 -6)cycloalkyl, (C 4 -6)cycloalkyl-(C 1 -5)alkyl or ##STR2## R 2 , m, R 3 , R 4 , R and u are defined as...
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5852007 |
Cysteine and serine protease inhibitors containing D-amino acid at the P2 position, methods of making same, and methods of using same
The present invention is directed to (D)-amino acid containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.
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5849917 |
Process for the preparation of isoquinoline compounds
(Z)-1 1-(4-Methoxybenzylidene)-1,2,3,4,5,6,7,8-octahydro-isoquinol
in-2-yl!a lkanones of the formula ##STR1## wherein R is lower alkanoyl, can be produced under specific reaction conditions in a...
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5849732 |
Phenol compound having antioxidative activity and the process for preparing the same
Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R 0 represents H, alkyl or alkyloxy; R 1 represents alkyl; R 2 represents alkyl or alkyloxy; OR 3 represents OH;...
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5846942 |
Cholecystokinin antagonists, their preparation and therapeutic use
Novel cholecystokinin antagonists useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the...
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5847144 |
Process for manufacturing α,α'-diaminoalcohol
A process for the manufacture of the α,α'-diaminoalcohol of formula ##STR1## is via N-protected L-phenylalanine lower alkyl esters, corresponding N-protected α-amino-α'-haloketones, and...
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5807883 |
2-oxoindoline derivative
Disclosed is a 2-oxoindoline derivative represented by the formula (I): ##STR1## wherein Ring A represents a benzene ring which is substituted in the 5-position or 6-position by a lower alkyl group...
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5807868 |
Isoquinoline derivatives as therapeutic agents
Tetrahydroisoquinoline compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof, in which: R 1 represents one or more substituents selected from H, halo, hydroxy, alkyl...
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5795907 |
Gastin and CCK receptor ligands
Compounds of formula (Ia), (Ib), or (Ic), wherein A represents a group having two fused rings, or a group of formula (Id), R 1 (m) represents up to 6 substituents, K represents --O--, --S--, --CH 2...
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5789594 |
Dimeric naphthylisoquinoline alkaloids and synthesis methods thereof
The present invention provides methods of preparing dimeric naphthylisoquinoline alkaloids by coupling together two monomeric naphthylisoquinoline alkaloids, each of which may be the same or...
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5786482 |
Dimeric arylisoquinoline alkaloids and synthesis method thereof
The present invention provides a method of preparing dimeric arylisoquinoline alkaloids by coupling two isoquinoline building blocks, which may be the same or different, together with a symmetrical...
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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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5776963 |
3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility
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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5763609 |
Certain pyrrolo pyridine-3-carboxamides; a new class of gaba brain receptor ligands
Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R 1 , R 2 , R 3 , R 4 are the same or different and represent hydrogen, C...
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5763613 |
Monomeric naphthylisoquinoline alkaloids and synthesis methods thereof
The present invention provides methods of preparing monomeric naphthylisoquinoline alkaloids, including the antiparasitic korupensamines and related compounds, as well as non-korupensamines and...
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5744607 |
Basic derivatives of glutamic acid and aspartic acid as gastrin or cholecystokinin antagonists
The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R 1 is selected from the group consisting of unsubstituted, mono- or...
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5741799 |
Heterocyclic thrombin inhibitors
Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R 1 , R 2 , R 3 , G, G x , R 6 ', Ra, Xa, R 6 , Rb, R 3 , p, Q, A and R 4 are as defined herein.
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5739134 |
N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2h-benzopyran, dihydrobenzodioxin, benzodioxole, dihydrobenzodioxepin, or tetrahydrobenzoxepin)carboxamide derivatives
N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal...
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5726184 |
Tetralin compounds with improved MDR activity
The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical...
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5714518 |
HIV protease inhibitors and methods of making the same
HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well...
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5712273 |
Amino acid derivatives, processes for the manufacture thereof and pharmaceutical compositions (II) containing these compounds
The invention relates to new amino acid derivatives of general formula I R 1 -R 11 --A 1 --B (I) and the pharmaceutically acceptable salts thereof, wherein group B...
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5698698 |
Process for preparation of N-tert.butyl-decahydro-2- 2(R)-hydroxy-4-phenyl-3(S)-phthalimidobutyl!-( 4aS,8aS)-isoquinoline-3(S)-carboxamide
The invention relates to a process for the preparation of N-tert.butyl-decahydro-2- 2(R)-hydroxy-4-phenyl-3(S)-phthalimidobutyl!-(4a S,8aS)-isoquinoline-3(S)-carboxamide of the formula ##STR1## as...
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5693803 |
Process for making HIV protease inhibitors
Intermediates of structural formula ##STR1## can be made by reacting a primary or secondary amine with glycosidol or an activated derivative thereof. The process and intermediates are useful for...
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5691337 |
Oxy-phenyl-(phenyl)glycinolamides with heterocyclic substituents
Oxy-phenyl-(phenyl)glycinolamides with heterocyclic substituents are prepared by reaction of the corresponding oxyphenylcarboxylic acids with heterocyclic substituents with phenylglycinol. The new...
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5679687 |
Irreversible HIV protease inhibitors, compositions containing same and process for the preparation thereof
The present invention relates to novel compounds of formula (I) which have inhibitory activity against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and...
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5663174 |
Aromatic sulfonamide derivatives, their use as enzyme inhibitors and pharmaceutical compositions containing them
Aromatic sulfonamide derivatives, particularly benzenesulfonamide, 4-fluorobenzenesulfonamide, 5-chloro-1-naphthalenesulfonamide and 5-isoquinolinesulfonamide derivatives are provided that inhibit...
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5663449 |
Intermediate compounds in the synthesis of heteroarylpiperidines, pyrrolidines and piperazines
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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5659033 |
N-aminoalkylfluorenecarboxamides; a new class of dopamine receptor subtype specific ligands
Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein: G represents a group of the formula ##STR2## where R a and R b represent hydrogen, or...
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5654319 |
N-[(4-heteroaryl-1-piperidinyl)alkyl]-2,3-naphthalimides 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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5652369 |
Amino acid derivatives
Compounds of the formula ##STR1## wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and --N(R 7 )--CH(R 8 )(R 9 ) are as claimed herein or their pharmaceutically acceptable acid addition salts inhibit...
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5652368 |
1,2,3,4-tetrahydroquinoline 2,3,4-trione-3 or 4-oximes
Disclosed herein are substituted or unsubstituted 1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oximes or pharmaceutically acceptable salts thereof that have high binding to the glycine receptor...
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5646121 |
Pseudopeptides with antiviral activity
The present invention relates to novel pseudopeptides with antiviral activity of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to a process...
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