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7342015 |
Indole derivatives
A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder,...
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7300929 |
Mediators of hedgehog signaling pathways, compositions and uses related thereto
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function...
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7291619 |
Melanocortin receptor agonists
The present invention relates to melanocortin receptor agonists of formula (I), which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction
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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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7279491 |
Phenylpiperidines and phenylpyrrolidines
Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
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7265118 |
Regulation of substrate activity
A method for regulating substrate activity in vivo is useful for the treatment of medical disorders such as inflammation, arteriolosclerosis and angiogenesis. The method involves the administration...
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7247631 |
Pegylated interferon alfa-CCR5 antagonist combination HIV therapy
Methods for treating treatment-naive as well as treatment-experienced adult and pediatric patients having HIV-1 infections as well as patients co-infected with HIV-1 and HCV involving administering...
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7241787 |
Substituted N-cycloexylimidazolinones, process for their preparation and their use as medicaments
The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and...
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7223764 |
2,4-bis (trifluoroethoxy)pyridine compound and drug containing the compound
The present invention is directed to a 2,4-bis(trifluoroethoxy)pyridine compound represented by formula (1):
(wherein X 1 represents a fluorine atom or a hydrogen atom) or a salt thereof, and...
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7214679 |
Piperidine/piperazine-type inhibitors of p38 kinase
Compounds of the formula:
wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase.
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RE39608 |
Substituted benzimidazoles and their use as PARP inhibitors
Compounds of the formula Ia or IB
where
A is a saturated or monounsaturated heterocyclic, 4 - to 8-membered ring which contains one or two nitrogen atoms,
and their tautomeric forms,...
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7196080 |
Phenylpyridinecarbonylpiperazinederivative
The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. ...
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7186743 |
Substituted pyrazolyl compounds for the treatment of inflammation
The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating...
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7179813 |
Bicyclic indolyl derivatives and methods for their use as serotonergic agents
Bicyclic indolyl derivatives and compositions containing such compounds are disclosed. Methods of using the bicyclic indolyl derivatives and compositions containing such composition as serotonergic...
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7160886 |
Acylated piperazine derivatives as melanocortin-4 receptor agonists
Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are...
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7153868 |
N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises...
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7125887 |
Pyrrolidine modulators of CCR5 chemokine receptor activity
Pyrrolidine compounds of Formula (I), (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6a , R 6b , R 7 and R 8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor...
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7119086 |
Phenylsulfonyl-1,3-dihydro-2h-indole-2-one derivatives, their preparation and their therapeutic use
The invention relates to compounds of formula:
and also to the salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, with affinity for and selectivity towards...
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7115609 |
Alanyl-piperidine heterocyclic derivatives useful against cardiovascular diseases
Compounds of formula (I)
in which R 1 , R 2 , n and X 1 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.
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7109201 |
Piperazine derivatives, their preparation and uses in therapy
Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed:
in which R a is a group of formula (i)
wherein P 2 is phenyl, naphthyl, heteroaryl or a 5 to 7...
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7101885 |
Piperazinyl-aryloxy and piperazinyl-heteroaryloxy-n-aryl lactams
The present invention relates to compounds of formula I
wherein Ar, Y and G are as defined in the specification, a is 1 to 4, Z and W are carbon or nitrogen and n is 1, 2 or 3; and to...
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RE39265 |
Heteroarylpiperidines, and their use as antipsychotics and analgetics
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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7094779 |
Piperazine oxime dervatives having NK-1 receptor antagonistic activity
The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein:...
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7067518 |
Pyridinyl-methyl-ethyl cyclohexanecarboxamides as serotonergic agents
A compound having 5-HT 1A receptor activity, represented by the chemical formula
wherein:
Ar is 2-methoxyphenyl, 1H-indol-4-yl or 2,3-dihydro-1,4-benzodioxin-5-yl; R 1 is 2-, 3- or...
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7053086 |
4-heteroaryl-3-heteroarylidenyl-2-indolinones and their use as protein kinase inhibitors
The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases...
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7015218 |
Amide compounds and medicinal use thereof
The present invention relates to a compound of the formula
wherein R 1 is substituted aryl, heteroaryl and the like, R 2 and R 3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q...
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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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6936602 |
Benzazepine derivatives, process for the preparation of the same and uses thereof
Compounds of the general formula (I):
or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R 1 is a 5- to 6-membered...
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6900206 |
Indole, azaindole and related heterocyclic sulfonylureido 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 sulfonylureido...
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6894052 |
Diarylalkylpiperazines active on the lower urinary tract
Disclosed herein are novel compounds and methods for the treatment of disorders of the lower urinary tract. The novel compounds are diarylalkylpiperazine derivatives. The methods comprise the...
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6855714 |
1-alkyl-2-aryl-benzimidazole derivatives, their use for the production of pharmaceutical agents as well as pharmaceutical preparations that contain these derivatives
The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R 1 , R 2 , R 3 , A, B and Y have the meanings that are indicated in the description and the...
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6838461 |
N-(indolcarbonyl-)piperazine derivatives
Compounds of the formula I
in which R 1 , R 2 , R 4 and R 5 have the meanings indicated in claim 1 , are potent 5-HT 2A antagonists and are suitable for the treatment of psychoses,...
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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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6762186 |
Substituted imidazoles as dual histamine H1 and H3 agonists or antagonists
The present invention discloses novel substituted imidazole compounds which have H 3 receptor antagonist or dual histamine-H 1 and H 3 receptor antagonist activity as well as methods for...
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6747030 |
Piperazine derivatives as 5-HT1B antagonists
Piperazine derivatives of formula(1), processes for their preparation, pharmaceutical compositions containing them in the treatment of CNS and other disorders and in their use in therapy as 5-HT...
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6743795 |
3-nitropyridine derivaives and the pharmaceutical compositions containing said derivatives
The present invention relates to novel 3-nitropyridine derivatives, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the same as active ingredients. Methods of...
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6723742 |
Substituted 3,5-diphenyl-1,2,4-triazoles and their use as pharmaceutical metal chelators
The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R 1 -R 5 are as defined in the description. The compounds have useful pharmaceutical properties and are...
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6723723 |
Heterocyclic derivatives as inhibitors of factor Xa
The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, of formula (I) wherein: A is an optionally substituted 5- or 6-membered monocyclic aromatic ring...
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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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6686370 |
Triazospiro compounds having nociceptin receptor affinity
Disclosed are compounds of the formula (I) wherein A, R 1 , R 2 , R 3 , R 4 and X 1 are as disclosed herein. The compounds have affinity for the ORL1 receptor and are useful in the treatment...
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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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6632828 |
Substituted imidazole neuropeptide Y Y5 receptor antagonists
Compounds of the formula I or a pharmaceutically acceptable salt, solvate or N-oxide thereof, wherein X is ═CH— or ═N—; Y is H, halogen, trihaloalkyl, alkyl, alkenyl, cycloalkyl,...
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6610707 |
Heterocyclic compounds as inhibitors of rotomase enzymes
Compounds of the formula: wherein R 1 , Y, W, A and R 2 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal...
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6602874 |
Heterocyclic carboxamides
A compound of the formula wherein X, Y, Z, R 2 and R 3 are as defined above, useful in treating or preventing migraine, depression and other disorders for which a 5-HT 1 , agonist or...
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6596745 |
Method for treating fibrotic diseases with azolium chroman compounds
Provided is a method of treating or ameliorating hypertension in an animal comprising administering an effective amount of a compound of formula I:
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6586418 |
Thrombin or factor Xa inhibitors
This invention relates generally to heteroaryl-phenyl substituted compounds that are inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical...
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6573262 |
Composition and antiviral activity of substituted indoleoxoacetic piperazine derivatives
The invention comprises substituted indoleoxoacetic piperazine derivatives of general Formula I, compositions thereof and their use as antiviral agents, and particularly for treating HIV infection.
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6566376 |
Diphenyl-piperidine derivative
The invention provides compounds of general formula (I) wherein R 1 , R 2 , R 3 , R 4 , A, Q, U, V, W, X, Y and n are as defined in the specification, processes for their preparation,...
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6548520 |
Substituted imidazoles having anti-cancer and cytokine inhibitory activity
The present invention is related to novel 2-alkyl substituted imidazoles of formula (I) useful for the treatment of CSBP kinase mediated diseases.
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6521623 |
N,N'-disubstituted benzimidazolone derivatives with affinity at the serotonin and dopamine receptors
A compound of formula (I) wherein: R 1 is C 1 -C 6 -alkyl substituted by a group selected from OH, C 1 -C 6 -alkoxy, —OCONHC 1 -C 6 -alkyl, —OCONHC 1 -C 6 -alkyl, —NHSO 2 C 1 -C 6 -alkyl,...
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