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7368445 |
Fused pyrazole derivatives as TGF-β signal transduction inhibitors for the treatment of fibrosis and neoplasms
The disclosed invention is directed to compounds of the formula: Formula (I) and methods of using these compounds.
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7329652 |
Diaminotriazole compounds useful as protein kinase inhibitors
The present invention relates to inhibitors of protein kinases, particularly to inhibitors of JAK2 and JAK3. The invention also provides pharmaceutical compositions comprising the compounds of the...
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7304052 |
Substituted homopiperidinyl benzimidazole analogues as fundic relaxants
The present invention relates to compounds of formula (I)
their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle...
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7279469 |
Diaminotriazoles useful as inhibitors of protein kinases
The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the...
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7273882 |
Aminoacetamide acyl guanidines as β-secretase inhibitors
There is provided a series of substituted acyl guanidines of Formula (Ik)
or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R 2 , R 3 , R 4 , R 5 , R 25 , R 26 and R 27...
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7265102 |
Substituted pyrazoles
Substituted pyrazoles of general formula
methods of manufacturing them, compositions containing them, and methods of using them to, for example, treat autoimmune diseases mediated by cathepsin...
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7125877 |
Benzimidazole derivatives
This invention provides compounds which are represented by a general formula [I]
[in which X stands for hydrogen or halogen; B stands for halogen, cyano or optionally fluorine-substituted lower...
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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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7071182 |
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or...
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7049307 |
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or...
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7041668 |
Substituted benzimidazole compounds and their use for the treatment of cancer
The present invention discloses and claims benzimidazole compounds of formula (I):
in which A is aryl or heteroaryl; R 1 is selected from optionally substituted alkyl, alkoxy, aryl or...
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7030150 |
Benzimidazole compounds and antiviral uses thereof
The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion...
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7001901 |
Tetrazolylpropionamides as inhibitors of Aβ protein production
This invention relates to novel tetrazolyl-propionamides in which the amide group comprises an aminoazepinone, and related structures, of Formula (I):
or pharmaceutically acceptable salt...
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6953793 |
Substituted pyrazoles
Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.
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6906090 |
Compositions and methods for treating mycobacterial diseases
The invention provides the use of certain isatin and oxindole derivatives in the preparation of a medicament for use in the treatment of mycobacterial disease.
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6894041 |
Oxazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
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6887865 |
N-heterocyclic derivatives as NOS inhibitors
N-Heterocyclic derivatives of the formula (I):
are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these...
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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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6869945 |
Pyrrolyl-and imidazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
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6861432 |
Piperazine derivatives that destabilize androgen receptors
This invention relates to new piperazine derivatives of general formula I,
in which V, W, n, R, R′, i, j, Y and Z have the meaning that is indicated in the description.
The compounds...
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6828315 |
1-Amino triazoloc4,3-a&excl quinazoline-5-ones and/or -5-thiones inhibiting phosphodiesterase IV
The present invention relates to triazolo[4,3-a]quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the...
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6720317 |
Inhibitors of factor Xa
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating...
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6710042 |
Human NK3 receptor-selective antagonist compounds, method for obtaining them and pharmaceutical compositions containing them
Compounds of formula (I) are useful as human NK 3 receptor antagonists.
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6696437 |
Heterocyclically substituted benzimidazoles, the production and application thereof
The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.
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6667303 |
Aryl substituted 1,4-diazepanes and method of use thereof
Aryl substituted 1,4-diazepanes are provided such as derivatives of 6-(1,4-diazepan-1-yl)benzo[cd]indol-2(1H)-one, 6-(1,4-diazepan-1-yl)acenaphthylen-1(2H)-one and...
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6627624 |
Aryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 , are variables defined...
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6613781 |
Heterocyclylaklylindole or -azaindole compounds as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor
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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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6365584 |
Arylysulphonamide-substituted benzimidazoles having tryptase-inhibiting activity
Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are:...
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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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6251921 |
Antithrombotic diamines
This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of...
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6133291 |
N-(imidazolylalkyl)substituted cyclic amines as histamine-H.sub.3 agonists or antagonists
The present invention discloses novel N(imidazolylalkyl)-substituted cyclic amine compounds which have excellent histamine-H 3 receptor antagonist activity as well as methods for preparing such...
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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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6100279 |
Imidazoylalkyl substituted with a five, six or seven membered heterocyclic ring containing one nitrogen atom
Disclosed are compounds of Formula I ##STR1## or pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable...
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6096746 |
Indazole compound containing a monocyclic amine structure
An indazole compound having a piperazinyl moiety in the structure thereof, which is a 5-HT 4 receptor agonist which is useful in the treatment of digestive tract disorders.
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6030992 |
Methods of treating or preventing sleep apnea
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6025333 |
Treatment of CNS tumors with metalloprotease inhibitors
The present invention relates to genes and their encoded proteins which regulate neurite growth and the diagnostic and therapeutic use of such proteins (termed herein neurite growth regulatory...
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6022868 |
Substituted azacyclic or azabicyclic compounds
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5994347 |
For a process for treatment of anxiety and tension
A process for the treatment of anxiety and tension, which comprises administering to a patient in need therefor an anxiolytically effective amount of a compound of the formula ##STR1## wherein X is...
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5972975 |
Substituted 2-aminopyridines as inhibitors of nitric oxide synthase
Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders....
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5952354 |
Tris carbamic acid esters: inhibitors of cholesterol absorption
Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are...
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5939437 |
CCK and gastrin receptor ligands
Compounds of formula (I) and their pharmaceutically active salts are gastrin and CCK receptor ligands, where Ar is a monocyclic aromatic group, R 1 is halo, amino, nitro, cyano, sulphamoyl,...
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5932568 |
6-methoxy-1H-benzotriazole-5-carboxamide derivatives and pharmaceutical compositions containing them
6-Methoxy-1H-benzotriazole-5-carboxamide derivatives which are represented by the formula (I) below: ##STR1## in which R 1 stands for ethyl or cyclopropylmethyl group, R 2 stands for hydrogen...
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5872134 |
5-HT4 receptor antagonists
The use of a compound of formula (I) or a pharmaceutically acceptable salt thereof for the treatment of artrial arrhythmia, stroke or CNS disorders X--CO--CH 2 --Z ...
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5869481 |
Anticonvulsive 1-ar(alk)ylimidazolin-2-ones and process for making
Compounds having anticonsulive activity, of the formula 1 ##STR1## in which X is hydrogen, a C 1 -4 -alkyl, C 1 -4 alkoxy, trifluoromethyl, or halogen residue, R 1 and R 2 are independently of...
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5869478 |
Sulfonamido substituted benzopyran derivatives
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5830909 |
Angiotensin (AII) antagonists as inhibitors of the growth of adipose tissue
The invention is a method of using Angiotensin (AII) Antagonists as inhibitors of the growth of adipose tissue, reducing adipocyte growth and body weight gain.
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5776927 |
Methionine sulfone and S-substituted cysteine sulfone derivatives as enzyme inhibitors
This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The...
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5773434 |
Facilitation of AMPA receptor-mediated synaptic transmission in brain as a treatment for schizophrenia
Psychotic symptoms are treated by the administration of drugs which amplify the ability of natural stimulators of AMPA receptors to enhance the mediation of excitatory synaptic response. What is...
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