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7612205 |
Crystals of quinolinecarboxylic acid derivative solvate
A main object is to provide a crystal of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)-me
thyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3
-carboxylic acid acetonitrile...
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7557107 |
Farnesyl protein transferase inhibitors as antitumor agents
Disclosed are novel tricyclic compounds of the formula:
and a pharmaceutically acceptable salts or solvates thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also...
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7501418 |
Fused heterocyclic isoxazoline derivatives and their use as anti-depressants
The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof...
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7462717 |
C6-and C9-substituted chromeno[4,3-c]isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and...
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7312209 |
Acridone inhibitors of IMPDH enzyme
Compounds having the formula (I),
wherein R 3 is selected from H, OH and NH 2 ; R 30 is selected from ═O and ═S; W is —C(═O)—, —S(═O)—, or —S(O) 2 —; or W may be —CH 2...
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7291612 |
Immunomodulatory compounds
The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions...
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7265103 |
Substituted amino isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and...
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7235557 |
Compounds and their uses
This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.
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7226928 |
Methods for the treatment of periodontal disease
The disclosure provides methods for the treatment and prevention of periodontal disease. In preferred embodiments, the invention provides for local treatment of periodontal tissues with a...
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7199128 |
8-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents
The invention provides compounds and salts of Formula I and Formula II:
which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making...
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7169786 |
Isoxazoline derivatives as anti-depressants
The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R 7 , S or O, R 1 , R 2 and R 3 are certain specific substituents, Pir is an...
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7153859 |
Condensed polycyclic compounds
The present invention provides a novel a condensed polycyclic compound useful as a phosphodiesterase 4 inhibitor, which is shown by the formula [I]:
or a pharmaceutically acceptable salt...
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7153849 |
Antidepressant arylpiperazine derivatives of hetrocycle-fused benzodioxans
Compounds of the formula I:
are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
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7115621 |
Chemical compounds
Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents as inhibitors of phosphodiesterase 5 cardiovascular disorders
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7053091 |
17 β-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical...
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6939881 |
Methods for prevention of ulcers and improving physiological performance
Methods for preventing ulcers, such as gastric ulcers, in a horse about to undergo stress that causes gastric ulcers and prior to occurrence of a gastric ulcer condition in the horse involving...
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6936622 |
6-phenylbenzonaphthyridines
Compounds of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in the description, are novel effective PDE3/4 Inhibitors.
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6924289 |
Benzyl(Idene)-lactam derivatives, their preparation and their use as selective (ANT) agonists of 5-HT1A- and/or 5-HT1D receptors
The present invention relates to lactam derivatives of the formula
wherein R 1 , R 2 , R 3 , A, X, Z, n and the dashed line are defined herein, and pharmaceutical compositions thereof, to...
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6924292 |
Furoisoquinoline derivatives, process for producing the same and use thereof
A compound having a partial structure represented by Formula:
or a salt thereof has an excellent phosphodiesterase (PDE) IV-inhibiting effect, and is useful as a prophylactic or therapeutic...
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6875761 |
Certain 1,3-disubstituted isoquinoline derivatives
Condensed pyridine compounds represented by formula (I):
wherein: R 1 and R 3 are, independently, hydrogen, lower alkyl, or lower alkoxy; R 2 represent an amino substituent; ring A is a...
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6815449 |
LK6-A derivatives
Compounds having immunosuppressive activity, cell growth inhibitory activity, anti-tumor activity, etc. are represented by formula I: and pharmaceutically acceptable salts thereof.
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6774129 |
Benzothieno&lsqb 3,2-c&rsqb pyridines as α2 antagonists
The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R 1 is...
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6743794 |
Methods and compounds for inhibiting MRP1
The present invention further relates to a method of inhibiting MRP1 in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound of formula (I).
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6740661 |
Farnesyl protein transferase inhibitors
Disclosed are compounds of the formula: wherein R 13 represents an imidazole ring; R 14 represents a carbamate, urea, amide or sulfonamide group; R 8 represents H when the alkyl chain between...
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6723733 |
Sulfonamide and carbamide derivatives of 6(5H)phenanthridinones and their uses
This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.
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6720332 |
Oxindole derivatives
Oxindole derivatives, specifically pyrrolo[3,2-f]quinoline-2-ones, which are useful as CDK4 inhibitors are described herein. The described invention also includes methods of making such oxindole...
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6699872 |
N-substituted urea inhibitors of farnesyl-protein transferase
Novel halo-N-substituted urea compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras...
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6699864 |
Substituted phenyl-piperazine derivatives, their preparation and use
The present invention provides compounds of the formula: wherein R 1 -R 8 , X, Y, Z, n and m are defined in the application. The compounds of the invention have affinity for the 5-HT 1A receptor.
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6693112 |
Compounds for enhancing chemotherapy
The present invention provides 2,3-dihydro-1H-pyrrolo[2,3-b]quinolin-4-ylamines, of the formula: or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , and R 7 are as defined...
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6677349 |
Sulfonamide and sulfamide substituted imidazoquinolines
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain sulfonamide or sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and...
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6645966 |
Treatment of malaria with farnesyl protein transferase inhibitors
Disclosed is a method of treating Malaria comprising administering an effective amount of an FPT inhibitor to a patient in need of such treatment alone or in combination with an additional...
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6638929 |
Tricyclic protein kinase inhibitors
This invention provides compounds of formula 1, having the structure which are useful as inhibitors of protein tyrosine kinase and are antiproliferative agents.
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6638935 |
Heteroary1 derivatives and their use as medicaments
The invention relates to novel pyridine derivatives of formula 1, to their preparation and to their use as medicaments, in particular for treating tumors
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6608078 |
Antibacterial chiral 8-(substituted piperidino)-benzo &lsqb i,j&rsqb quinolizines, processes, compositions and methods of treatment
The present invention relates to optically pure 8-(substituted piperidino)-benzo[i,j]quinolizines, their isomers, derivatives, salts, pseudopolymorphs, polymorphs prodrugs and hydrates thereof, to...
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6566362 |
Benzo&lsqb f&rsqb naphthyridine derivatives, their preparation and compositions containing them
Benzo[f]naphthyridine derivatives of formula (I): benzo[f]naphthyridine derivatives and benzo[f]naphthyridine esters of formula (IVa): aminoquinoline derivatives of formula (X): processes for...
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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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6548506 |
Benzo&lsqb 1,8&rsqb naphthyridine derivatives, their preparation and pharmaceutical compositions which comprise them
Novel 1,8-benzo-naphthyridine derivatives of general formula (I): which are useful as antimicrobial agents.
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6541483 |
Acridone-derived compounds useful as antineoplastic and antiretroviral agents
The present invention relates to several novel acridone-derived compounds of of formula (I) or (II). These compounds are potent anti-viral agents, useful in the treatment of viral diseases, such as...
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6476025 |
Phenylphennanthridines with PDE-IV inhibiting activity
Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51, R6, R13 and R20 have the meaning indicated in the description, are novel active bronchial therapeutics
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6469006 |
Antiviral indoleoxoacetyl piperazine derivatives
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl...
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6469021 |
Non-peptide antagonists of GLP-1 receptor and methods of use
Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical...
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6462047 |
Carboline derivatives as cGMP phosphodiesterase inhibitors
Compounds of general structural formula (I) wherein A represents a 5- or 6-membered heteroaryl group containing at least one heteroatom selected from the group consisting of oxygen, nitrogen, and...
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6451809 |
Oxo-pyridoimidazole-carboxamides: GABA brain receptor ligands
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof where R 1 -R 4 and A are defined herein, which compounds are highly selective agonists,...
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6410541 |
Compounds useful for inhibition of farnesyl protein transferase
Novel compounds of the formula: are disclosed. In Formula 1.0 a represents N or NO, R 1 and R 3 are halo, R 2 and R 4 are independently H or halo provided that at least one is H, X is C, CH...
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6387905 |
Compounds useful for inhibition of farnesyl protein transferase
Novel compounds of the formula: are disclosed. Compounds of Formula 1.0 are represented by the compounds of formulas: wherein R 1 , R 3 and R 4 are each independently selected from halo. Also...
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6365588 |
Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: to a biological...
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6323206 |
Chemokine receptor antagonists and methods of use therefor
Disclosed is a method of treating a subject with a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to the subject a therapeutically...
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6300331 |
Naphthalimidobenzamide derivatives
The present invention relates to a naphthalimidobenzamide derivative represented by the following formula (1): ##STR1## (wherein, R 1 represents a hydrogen atom, etc., Y represents a hydrogen...
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6277854 |
Tricyclic antitumor farnesyl protein transferase inhibitors
The invention relates to compounds of the formula ##STR1## wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , Y, A, B, X, a, b, c, d, v, and w are as described herein. The compounds of...
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6255306 |
4-indole derivatives as serotonin agonists and antagonists
The present invention relates to compounds of the formula ##STR1##
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