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7615549 |
Substituted pyrrolidinones, their manufacture and their use as medicaments
The present invention relates to new substituted pyrrolidinones of general formula
wherein A, X, B and R 1 to R 9 are as defined above, or a tautomer or salt thereof, particularly the...
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7569561 |
2,4-diaminopyrimidines useful for treating cell proliferation diseases
The present invention encompasses compounds of general formula (1)
wherein
R 1 to R 6 , X and Y are defined as in claim 1 , which are suitable for the treatment of diseases...
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7566778 |
(Pyrido/thieno)-[f]-oxazepine-5-one derivatives
The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I
wherein R 1 , R 2 and R 3 are independently H or (C 1-4 )alkyl; Ar represents a...
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7550453 |
2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof
The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.
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7361648 |
Heterocyclylakylamines as muscarinic receptor antagonists
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I:
wherein X, Y, and Z are O, S or NR 5 , and the other...
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7314930 |
Process for preparing dibenzothiazepine derivatives
A process for preparing a dibenzothiazepine derivative such as dibenzo[b,f][1,4]thiazepin-11-one employable as a starting material for the preparation of...
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7307073 |
Benzoxazepines derivatives and their use as AMPA receptor stimulators
The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO 2 ; R 1 , R 2 , R 3 and R 4 are independently selected from H, (C 1-4 )alkyl,...
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7294622 |
Lactams and uses thereof
Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid β protein production and...
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7279582 |
Retroviral protease inhibiting compounds
A compound of the formula:
is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
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7229984 |
Dibenzoxazepinone derivatives and uses thereof
Compounds of the Formula I:
wherein m, n, k, A, X, Y, Z, Ar, R 1 , R 2 , R 3 , and R 4 are as defined herein. The compounds are useful as 5-HT6 receptor antagonists. Also provided are...
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7214793 |
Method of preparing 10H-dibenzo[b,f][11,4]thiazepin-11-one
Disclosed is a method of preparing 10H-dibenzo[b,f][1,4]thiazepin-11-one, including reacting dithiosalicylic acid with 1-chloro-2-nitrobenzene in a basic aqueous solution in the presence or absence...
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7208487 |
Compounds, compositions and methods
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
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7205292 |
CGRP receptor antagonists
The present invention is directed to compounds of Formula I and Formula II: (where variables R1, R2, R3, R4, R6, A, B, G, J, W, X and Y are as defined herein) useful as antagonists of CGRP...
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7157442 |
Antibacterial compound
The present invention relates to a compound of formula (I) (wherein R 1 and R 2 represent an aryl group, a heterocyclic group, an alkyl group, an alkenyl group and the like which are optionally...
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7109233 |
Protease inhibitors
This invention relates in general to certain substituted substituted 1,1,4-1l 6 -trioxo[1,2]thiazepan-4-ylamides of formula I
as defined herein which are protease inhibitors.
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7045621 |
Process for producing dibenzothiazepine derivatives
A process for preparing a dibenzothiazepine derivative such as dibenzo[b,f] [1,4]thiazepin-11-one employable as a starting material for the preparation of...
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7015212 |
Thiazepine inhibitors of HIV-1 integrase
The present invention discloses non-catechol compounds, such as thiazolothiazepines, and analogs and derivatives thereof, which are anti-integrase inhibitors. The compounds, which are useful as...
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7009047 |
Ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenylpropanoate], processes for its preparation and its use
The present invention relates to ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate], the preparation of ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate] from...
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6924277 |
Cyclized benzamide neurokinin antagonists for use in therapy
Compounds having the general formula
wherein R 1a , R 1b , R 1c , X 1 , X 2 , R 2 , R 3 , R 4 , R 5 , R 6 , n, Y and Z are as defined in the specification, methods of using such compounds for...
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6921759 |
Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV...
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6919328 |
Tricyclic compounds with NOS activity
The present invention provides novel tricyclic compounds, compositions comprising these compounds and methods of using these compounds as neuroprotectants. In particular, the compounds of the...
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6916807 |
Triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula
wherein said ring X is a 5-7 membered heterocyclic ring, and wherein...
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6900201 |
N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trio
ne metalloproteinase inhibitors of the formula
wherein ring X is a 5-7 membered heterocyclic ring,...
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6864250 |
N-acylated lipophilic amino acid derivatives
Compounds of structural Formula (I) where A is a lipophilic group including an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group...
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6852713 |
Lactam derivatives and methods of their use
Lactam derivatives of the general formula
are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.
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6828439 |
Compounds, composition, and methods for photodynamic therapy
Disclosed are novel compounds, compositions, and methods that are particularly useful in photodynamic therapy. In particular, the inventive compounds, compositions, and methods relate to the...
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6815463 |
Laulimalide derivatives
Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.
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6806267 |
Apoptosis-inducing compounds
The present invention relates to pyrrolobenzoxazepines, pyrrolobenzthiazepines and related compounds having the ability to induce apoptosis, to pharmaceutical compositions comprising these...
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6767907 |
4-aryl-1-(indanmethyl dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl) piperidines tetrahydropyridines or piperazines
4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH 2 and...
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6686349 |
Substituted tetracyclic pyrroloquinolone derivatives useful as phosphodiesterase inhibitors
The invention relates to novel tetracyclic pyrroloquinolone derivatives of the formula (I) or (II): wherein all variables are as herein defined, pharmaceutical compositions containing the...
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6667301 |
Heterocyclylalkylamines as muscarinic receptor antagonists
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR 5 , and the other...
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6656911 |
Serine protease inhibitors
The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for...
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6635759 |
Luminescent 4-trifluoromethyl 1-2-quinolones with long wave UV absorption and the use thereof
The invention relates to a substituted 4-trifluoromethyl carbostyril according to formula (I) and is characterised in that the 4-trifluoromethyl carbostyril is provided with an absorption maximum...
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6610697 |
Substituted 2-aryl-3-(heteroaryl)-imidazo&lsqb 1,2-a&rsqb pyrimidines, and related pharmaceutical compositions and methods
This invention relates to a series of imidazopyrimidines of Formula I, and pharmaceutical compositions containing them. The compounds of the invention inhibit the production of a number of...
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6544978 |
Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions...
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6541466 |
Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions...
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6537987 |
4,1-benzoxazepines or 4,1-benzothiazepines and their use as squalene synthetase inhibitors
This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents,...
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6503897 |
Antibacterial agents
Compounds of formula (I) are antibacterial agents wherein: R 3 and R 4 , taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated...
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6489320 |
5, 5-disubstituted-1, 5-dihydro-4, 1-benzoxazepin-2 (3H)-ones useful as HIV reverse transcriptase inhibitors
The present invention relates to benzoxazepinones of formula I: or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV...
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6472529 |
Retroviral protease inhibiting compounds
A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
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6472384 |
Antimicrobial compounds
The present invention relates to ester, ether and N-alkylcarbamoyl derivatives of compound (Ia) and pharmaceutically acceptable salts thereof. These compounds exhibit excellent antibacterial...
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6468996 |
Substituted hetero-polycyclic compounds as PPARα and PPAR&ggr activators
The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the...
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6444809 |
Therapeutic heterocycles
Compounds of formula I wherein G, J, L, M, m and D have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of...
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6416922 |
Azomethine dye precursor, image-forming material, and image-forming method
The present invention related to an azomethine dye precursor represented by the following general formula (1) and the image-forming material and image-forming method using the azomethine dye...
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6399598 |
Diheterocyclic metalloprotease inhibitors
The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptacle salt, or biohydrolyzable amide,...
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6297232 |
Triazolo[4,5-D]pyrimidinyl derivatives and their use as medicaments
The invention relates to triazolo[4,5-d]pyrimidin-3-yl derivatives which are useful in the treatment of platelet aggregation disorders.
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6218394 |
4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophene-methyl) piperazines
4-Aryl-1-(indanmethyl, dihydrobenzofuramethyl or dihydrobenzothiophenemethyl) piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I) ##STR1## wherein one of X and Y is CH 2...
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6140320 |
5,5-disubstituted-1,5-dihydro-4,1-benzoxazepin-2 (3H)-ones useful as HIV reverse transcriptase inhibitors
The present invention relates to benzoxazepinones of formula I: ##STR1## or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of...
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5972237 |
Use of heterocyclic compounds as activators for inorganic peroxy compounds
Heterocyclic compounds I R 1 --X--L (I) where L is a cyclic carbamate residue, a lactonoxy residue or a lactam residue, X is an...
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5965553 |
Squalene synthetase inhibitors
This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents,...
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