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7361682 |
Indole derivatives as H3 inverse agonists
The present invention relates to compounds of formula I:
wherein X, R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof,...
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7323456 |
Carboxylic acid derivatives compounds and agents comprising the compounds as active ingredient
A compound of formula (I)
(wherein all symbols are as defined in the specification) and a salt thereof, and peroxisome proliferator activated receptor regulator comprising thereof as active...
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7319097 |
Compounds
The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the...
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7307074 |
Diazepan derivatives or salts thereof
To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of...
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7291613 |
Inhibitors of p38 kinase
The invention is directed to methods to inhibit p38-α kinase using compounds comprising saturated heterocycles coupled to a fused ring system.
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7241745 |
Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I)
as well as methods for their production, medicaments containing these compounds...
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7223750 |
Derivatives of 5-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, the preparation thereof and the application of same in therapeutics
Compounds complying with the general formula (I)
in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C 1 –C 6...
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7202237 |
Pyridylether derivatives, their preparation and use
The present invention relates to novel pyridylether derivatives which are cholinergic ligands at nicotinic Ach receptors. The compounds of the invention are useful for the treatment of conditions,...
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7115635 |
Benzylpiperidine compound
The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral...
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7115596 |
Thiazole compounds as integrin receptor antagonists derivatives
The present invention relates to a class of compounds represented by the Formula I
or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula...
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7105556 |
Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure
wherein Q is C or N, X 1 is C or N, and R 1 , R 2 , R 2a , R 2b , R 2c , R 3 , Y, A, m, n, X 2 , X 3 and X 4 are as defined herein, which...
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7071184 |
Protease inhibitors
The present invention provides C 1-6 alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin...
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7041675 |
Heterocyclic compounds and their use as PARP inhibitors
The invention relates to compounds of the formula I
and the tautomeric forms, possible enantiomeric and diasteromeric forms thereof, and prodrugs thereof, and use thereof as PARP inhibitors.
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7026310 |
Heteroaryl derivatives and their use as medicaments
The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.
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7022695 |
Thioether-substituted benzamides as inhibitors of Factor Xa
Thioether-substituted benzamide compounds having the formula:
are provided that exhibit exceptionally strong inhibition of Factor Xa in combination with weak hERG binding.
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6992092 |
Anti-diabetic agents
The present invention provides compounds of formula (I)
the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein...
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6984637 |
Cyclic amine derivatives-CCR-3 receptor antagonists
This invention relates to certain cyclic amine derivatives of Formula (I)
that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods...
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6939867 |
β3 agonists and uses thereof
Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with β-adrenergic receptors, such as obesity,...
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6887864 |
Azepane derivatives
This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I)
wherein the symbols are defined in the specification, as...
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6815451 |
1,2,3,4-Tetrahydroisoquinolines derivatives as urotensin II receptor antagonists
The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions....
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6809093 |
2-substituted heterocyclic compounds
Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds. An example compound has the formula:
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6743808 |
4-aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl) 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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6677354 |
Piperdines for use as orexin receptor antagonists
Disclosed are compounds of formula (I): wherein: Y represents a group (CH 2 ) n , wherein n represents 0, 1 or 2; R 1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3...
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6642233 |
1-Phenacyl-3-phenyl-3-(piperidylethyl)piperidine derivatives, process for the preparation thereof and pharmaceutical compositions containing them
The invention relates to the compounds of formula: as well as to the salts thereof with inorganic or organic acids, to solvates thereof and/or to hydrates thereof, which have strong affinity and...
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6613776 |
Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: wherein Z 1 is N, CR a , or CH, and Z 2 is N or CH, provided...
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6583179 |
Substituted aminoalkylamide derivatives as antagonists of follicle stimulating hormone
The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders...
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6509329 |
Cyclic diamine compound with 6-membered ring groups
A cyclic diamine compound of formula (1): wherein A is a single bond or C≡C; X and Y are individually CH or a nitrogen atom; m is 1 or 2; and n is a number of 1 to 5; an acid-addition salt...
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6495568 |
Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors
Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line...
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6476054 |
Cyclic amine modulators of chemokine receptor activity
The present invention is directed to cyclic amines of the formula I: (wherein R 1 , R 2 , R 3 , m and n are defined herein) which are useful as modulators of chemokine receptor activity. In...
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6451817 |
Alpha-substituted-1-benzyl-napthyls
This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are α-substituted with ether, thioether, amino, hydrazino, cyano or halo...
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6448243 |
1,4-substituted cyclic amine derivatives
A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: (wherein A, B, C, D, T, Y and Z represent each methine or...
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6444664 |
Method for controlling the plasma level of lipoproteins to treat alzheimeris disease
A compound which is an antagonist of platelet activating factor (PAF-antagonist) or a structurally related compound thereof not having PAF-antagonistic activity can be used for decreasing the...
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6420395 |
Azacyclooctane and heptane derivatives, their preparation and use in therapy
The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen,...
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6358976 |
Integrin receptor antagonists
This invention relates to novel fused heterocycles which are useful as antagonists of the α v β 3 and related integrin receptors, to pharmaceutical compositions containing such compounds,...
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6352981 |
Substituted AZA- and diazacycloheptane and -cyclooctane
Aza- and diazacyclohexane and -cyclooctane compounds of the following formula: Ar 1 —A—B—Ar 2 (I) where Ar 1 , A, B and Ar 2 have the meanings stated in the description have a high...
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6346540 |
1-(1,2-disubstituted pipeidinyl)-4-substituted piperidine derivatives
The present invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1...
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6340681 |
2-benzimidazolylamine compounds as ORL-1-receptor agonists
A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 are independently selected from hydrogen, halo, hydroxy, (C 1 -C 4 )alkyl, halo (C 1 -C 4 )alkyl...
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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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6262046 |
Azetidinylpropylpiperidine derivatives, intermediates and use as tachykinin antagonists
Compounds of the formula (I): ##STR1## where X 1 , A, Ar 1 , X and R are as defined in the specification, and pharmaceutically-acceptable salts thereof, are new, and are useful as tachykinin...
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6251918 |
Aniline derivatives as calcium channel blockers
The present invention provides compounds that block calcium channels having formula (I). The present invention also provides methods of using the compounds of formula (I) to treat stroke, cerebral...
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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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6221858 |
Pyridyl-and pyrimidyl-piperazines in the treatment of substance abuse 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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6191145 |
Orally-active nipecotamide glycolamide esters for the treatment of thrombosis disorders
Orally-active nipecotamide glycolamide ester derivatives of formula (I): ##STR1## are disclosed as useful in treating platelet-mediated thrombotic disorders.
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6191125 |
Small molecule pipecolic acid derivative hair growth compositions and uses
This invention relates to pharmaceutical compositions and methods for treating alopecia and promoting hair growth using pipecolic acid derivatives.
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6169097 |
1-(1,2-Disubstituted piperidinyl)-4-substituted piperidine derivatives
The present invention concerns compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m...
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6107291 |
Azepine or larger medium ring derivatives and methods of use
Selected novel azepine and larger medium ring compounds are effective for prophylaxis and treatment of inflammation, tissue degradation and related diseases. The invention encompasses novel...
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6083949 |
Substituted imidazoles having anti-cancer and cytokine inhibitory activity
Compounds represented by formula I: ##STR1## are disclosed. AR represents an aromatic group containing 6-10 atoms; and ##STR2## represents a 4 to 10 membered non-aromatic heterocycle containing at...
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6075022 |
Methods and compositions for controlling biofouling using thiourea compounds
The present invention relates to a method to inhibit bacteria from adhering to a submergible surface. The method contacts the submergible surface with an effective amount of at least one thiourea...
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6057322 |
Basically-substituted benzoylguanidines, a process for preparing them, their use as a medicament or diagnostic agent, and a medicament containing them
Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also...
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