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8158617 |
Fused heterocyclic compound and use thereof
The present invention relates to a serotonin 5-HT2C receptor activator containing a compound represented by the formula wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having...
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8022058 |
Agents for preventing and treating disorders involving modulation of the RyR receptors
The present invention provides novel compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds...
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8012960 |
Heterocyclic aspartyl protease inhibitors
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification;...
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7994160 |
Pyridazine compounds as glycogen synthase kinase 3 inhibitors
Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and...
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7981879 |
HIV integrase inhibitors
Compounds of Formula I are inhibitors of FHV integrase and inhibitors of FHV replication (I), wherein m, n, X, R1, R2, R3, R4, R5, R6, R7; R8, R9 and R10 are defined herein. The compounds are...
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7943607 |
Heteroaryl benzamide derivatives for use as GLK activators in the treatment of diabetes
Compounds of formula (I), wherein R1, R4, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the...
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7879840 |
Agents for preventing and treating disorders involving modulation of the RyR receptors
The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of...
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7718645 |
Substituted bicyclolactam compounds
The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5a, R5b, R5c, R5d, Q, A, Z, and R7 are as described herein; compositions...
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7704990 |
Agents for preventing and treating disorders involving modulation of the RyR receptors
The present invention provides novel compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds...
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7598237 |
7-aryl 1,5-dihydro-4,1-benzoxazepin-2(3H)-one derivatives and their use as progesterone receptor modulators
This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.
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7572783 |
Substituted benzofused heterocycles
The present invention relates to the compounds of Formula I, their preparation and pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful, for...
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7569561 |
2,4-diaminopyrimidines useful for treating cell proliferation diseases
The present invention encompasses compounds of general formula (1) wherein R1 to R6, X and Y are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive...
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7151097 |
Bicyclic pyrazolyl and imidazolyl compounds and uses thereof
Compounds of Formula (I) are described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases linked to the mediation of...
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7122662 |
Tricyclic compound having spiro union
This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated...
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7109233 |
Protease inhibitors
This invention relates in general to certain substituted substituted 1,1,4-1l6-trioxo[1,2]thiazepan-4-ylamides of formula I as defined herein which are protease inhibitors.
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7060698 |
Benzoxazepinone derivatives
The invention relates to benzoxazepinone derivatives of formula wherein R1, R2, R3, R4, and n are as defined in the specification and to a pharmaceutically suitable acid addition salt thereof....
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7030107 |
Fused bicyclic pyridine derivatives as tachykinin receptor antagonists
A novel fused bicyclic pyridine derivative or a salt thereof that acts as a tachykinin receptor antagonist, in particular as an NK1 receptor antagonist, is represented by the following general...
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7026309 |
Fused bicyclic pyridine derivative as tachykinin receptor antagonist
A fused bicyclic pyridine derivative represented by the following general formula (1), or a salt thereof: wherein the rings A and B are each a benzene ring, which may have 1 to 3 substituents (any...
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7014981 |
Benzoindole styryl compounds and their uses in high-density recording media
The invention discloses new benzoindole styryl compounds and its use for a high-density optical recording medium. The invention uses the dyes of the new benzoindole styryl compounds to form the...
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6908934 |
Therapeutic compounds for treating dyslipidemic conditions
Compounds of Formula I and the pharmaceutically acceptable salts and esters thereof, wherein Z is selected from the group consisting of: (a) Formula Ia and(b) Formula Ib are novel LXR agonists and...
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6846833 |
Vitronectin receptor antagonist bicyclic compounds, preparation method and compositions containing same
Compounds of formula (1): wherein: G represents an optionally substituted phenyl or optionally substituted heterocycle, G1 and G2 being N or C,T1 represents —CH2—CH2—, —CH═CH— or ═CH—CH2—, a...
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6613761 |
Benzoxazepine compounds, their production and use
This invention provides new benzoxazepine compounds represented by the formula: [wherein R stands for a lower alkyl group optionally substituted with a hydroxyl group, X stands for an optionally...
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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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6506744 |
Benzazepinone-derivatives
Compounds of formula I as well as pharmaceutically usable salts and esters thereof, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence...
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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 reverse...
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6486315 |
Recrystallization processes
Mercaptoalkanoylamino lactam acids are recrystallized by treatment with an agent that minimizes the formation of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing...
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6455522 |
Cyclic sulfonamide derivatives as metalloproteinase inhibitors
The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic sulfonamide...
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6423840 |
Inhibitors of interleukin-1β converting enzyme
The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural ...
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6403578 |
Bicyclic fibrinogen antagonists
This invention relates to compounds of the formulae: whereinA1 is O, S, N—R1 or CHR1;A4 is N—R4 or CHR4;R2 is a sidechain containing an acid or ester group;R1, R4 and R5 are substituents such as ...
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6353099 |
Substituted ureas as cell adhesion inhibitors
Compounds of Formula I are antagonists of VLA-4 and/or α4β7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be f...
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6352982 |
4,1-benzoxazepines, their analogues, and their use as somatostatin agonists
The present invention provides a compound of the formula: wherein ring A is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; ring B is an optionally substituted...
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6340752 |
Deprotection and recrystallization processes
Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the...
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6204261 |
Inhibitors of interleukin-1β Converting enzyme inhibitors
The present invention relates to pyradazino[1,2-a][1,2]diazepine-1-carboxamide compounds of formula: ##STR1##which compounds are inhibitors of interleukin-1beta converting enzyme.
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6162913 |
Preparation of [4S-(4α,7α,10aβ)]-4-amino-octahydro-5-oxo-7H-pyrido[2,1 -b] [1,3]thiazepine-7-carboxylic acid, methyl ester and salts thereof via novel disulfides
N-protected-L-homocysteine disulfide of the formula ##STR1## or an activated form thereof is reacted with (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester to give the disulfide intermediate of...
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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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6114522 |
Process of production of 4-substituted-3-halogeno-1,4-benzoxazepine derivative and salts thereof
A process for producing 4-substituted-3-halogeno-1,4-benzoxazepin derivative or the salt thereof comprising: deprotonizing a benzoxazepine derivative having the formula (II): ##STR1## with a base;...
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6110909 |
Benzoxazepine compounds, their production and use as lipid lowering agents
This invention provides new benzoxazepine compounds represented by the formula: ##STR1## [wherein R stands for a lower alkyl group optionally substituted with a hydroxyl group, X stands for an...
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6069114 |
2-amino-4-bicycloamino-1,3,5-Triazines, their preparation, and their use as herbicide and plant growth regulators
Compounds of the formula (I) and their salts ##STR1## in which R1 to R6, Y1, to Y2, Y3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be...
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6008214 |
Bicyclic compounds
This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, which are effective for inhibiting platelet aggregation and bone resorption,...
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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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5770594 |
Naphthyl-benzoxazepines or -benzothiazepines as squalene synthetase inhibitors
This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents and antiatheroscierosis agents.
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5726306 |
4,1-benzoxazepin derivatives and their use
N-containing, condensed heterocyclic compounds and salts thereof are disclosed which are useful for inhibiting squalene synthetase and fungal growth, and which are useful for treating or preventing...
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5698691 |
Condensed cyclic compounds and their use
Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula ##STR1## wherein R1 is hydrogen or an optionally substituted hydrocarbon group; R2 is hydrogen,...
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5677298 |
Benzoxazepine-2-one compounds and their use
Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula (I) ##STR1## wherein R1 stands for H or an optionally substituted hydrocarbon group; R2 and R3...
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5674865 |
Nonpeptidyl integrin inhibitors having specificity for the GPIIb IIIa
A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPIIb IIIa receptor and is...
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5672599 |
Compounds containing a fused bicycle ring
Compounds of the formula ##STR1## wherein X is O or S--(O)t ; n is one; m is zero or one; Y is CH2, O, or S--(O)t provided that Y is O or S--(O)t only when m is one; and A is ##STR2## are dual...
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5654294 |
Spiro lactam dual action inhibitors
Compounds of the formula ##STR1## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular...
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5646276 |
Diazepine containing dual action inhibitors
Compounds of the formula ##STR1## wherein X1 is ##STR2## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being...
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5635502 |
Mercaptoacetylamide bicyclic lactam derivatives useful as inhibitors of enkephalinase and ACE
The present invention relates to certain novel mercaptoacetylamide bicyclic lactam derivatives useful as inhibitors of enkephalinase and of ACE.These mercaptoacetylamide bicyclic lactam derivatives...
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5627278 |
Process for preparing compounds containing a fused bicyclic ring
A process for preparing compounds of the formula ##STR1## wherein X is O or S; n is one or two; m is zero or one; Y is CH2, O, or S provided that Y is O or S only when m is one; and A is ##STR2##...
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