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7378420 |
Urea derivatives as calcium channel blockers
Derivatives of urea that contain piperazine rings and additional substitution with aromatic groups are effective in ameliorating conditions associated with unwanted calcium ion channel activity.
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7351703 |
Sulfonylamino carboxylic acid N-arylamides as guanylate cyclase activators
The present invention relates to compounds of the formula I
in which A 1 , A 2 , R 2 and R 3 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds for...
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7342018 |
Urokinase inhibitors and uses thereof
The invention relates to the use of derivatives of 3-amidinophenylalanine as urokinase inhibitors for treating malignant tumors and the formation of metastases.
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7332495 |
Aralkyl-ketone piperazine derivatives and their uses as new antalgic or ataractic agent
Arylalkyl ketone piperazine derivatives of the formula:
and pharmaceutical compositions comprising the same. Also disclosed are methods for using the compounds as analgesic and sedative agents....
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7326710 |
Aralkyl formyl-alkyl piperazine derivatives and their uses as a cerebral nerve protective agent
Aralkyl formyl alkyl piperazine derivatives
Pharmaceutical compositions comprising the same, and methods of using them as a neuroprotective agent. Pharmaceutical results indicate that these...
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7294628 |
Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I)
in which:
n is 1 or 2; R 1 represents a halogen atom; a trifluoromethyl radical; a (C...
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7291620 |
N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme...
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7271168 |
Piperazine derivatives having SST1 antagonistic activity
The invention provides compounds of formula ( 1 )
wherein X, R 1 and R 2 are as defined in the specification, their, preparation and to their use in treating, e.g., depression, anxiety and...
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7268140 |
Piperazine derivatives and their use as anti-inflammatory agents
This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of...
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7256194 |
Compounds that inhibit factor Xa activity
The present invention relates to compounds of the Formula
or a pharmaceutically acceptable salt, solvate, hydrate or formulation thereof. These compounds can be used for the inhibition of...
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7220749 |
Nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use
The invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated...
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7214714 |
20-hydroxyeicosatetraenoic acid production inhibitors
A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof
[wherein R 1 represents a substituted morpholino group, a substituted...
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7214681 |
Tri(cyclo) substituted amide compounds
Compounds of Formula (I):
or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
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7214680 |
2-substituted 1-arylpiperazines as tachykinin antagonists and/or serotonin reuptake inhibitors
The present invention relates to piperazine of formula (I)
wherein
R represents halogen, C 1-4 alkyl, trifluoromethoxy or trifluoromethyl; R 1 is trifluoromethyl, C 1-4 alkyl, C 1-4 ...
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7208497 |
Substituted piperazines and diazepanes
A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor....
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7186726 |
Preferentially substituted calcium channel blockers
Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.
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7176207 |
Platelet adenosine diphosphate receptor antagonists
Compounds of the following formula (I):
where A, a, b, R 1 , R 2 , R 3 , R 4 and R 6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical...
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7160874 |
Phenylalanine derivatives
Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
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7109243 |
Inhibitors of cathepsin S
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at...
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7098212 |
Piperazine derivatives
The present invention relates to compounds of the formula I
and the pharmaceutically acceptable forms thereof; wherein X, Y, a, b, c, d, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein....
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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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7078407 |
4-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them
The present invention relates to 4-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them. More particularly, it relates to 4-hydroxycinnamamide derivatives...
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7056524 |
Methods of hydrating mucosal surfaces
A method of hydrating nasal airway surfaces in a subject in need of such treatment comprises topically applying a sodium channel blocker to a nasal airway surface of the subject in an amount...
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7048924 |
Combination antiviral and interleukin-2 therapy for HIV infection
Methods for promoting immunologic control of human immunodeficiency virus (HIV) in an HIV-infected subject are provided. The methods comprise administering to the subject highly active...
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7045524 |
Pleuromutilin derivatives with antimicrobial activity
Pleuromutilin compounds of the formula:
are of use in anti-bacterial therapy.
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7030115 |
N-sulfonylurea apoptosis promoters
Compounds having the formula
are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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7022707 |
Piperazine derivatives
The present invention is a chemical compound of formula (I)
or a pharmaceutically acceptable salts, solvates and esters thereof, wherein R 1 to R 4 , A 1 , A 2 m and n are as described in the...
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7019003 |
Peptide deformylase inhibitors
Novel PDF inhibitors and novel methods for their use are provided.
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7001905 |
Substituted diarylamines as MEK inhibitors
Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C 1-6 alkoxy, or NR 6 OR 7 ; X is OR 12 , NR 13 R 12 , or NR 14 ; inhibitors of MEK and...
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6989383 |
Method of treating cancer
The present invention relates to methods of treating cancer using a combination of a compound which is an antineoplastic agent and a compound which is a inhibitor of prenyl-protein transferase,...
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6984652 |
Gyrase inhibitors
Compounds comprising an indazolyl group and a thiazolyl group, preferably 7-substituted 3-(thiazol-2-yl)-1H-indazole compounds in which the indazolyl group and a thiazolyl group are each...
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6982256 |
Tolerance of 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine in intravenous administration
The invention relates to new formulations for improving the local tolerance of intravenously administered 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-b
enzoylguanidine or one of the...
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6974817 |
Sulfonic acid derivatives
A compound of the formula
or the pharmaceutically acceptable salt thereof; wherein X, Y, a, b, c, d, R 1 , R 2 , R 3 and R 5 are as defined above useful to treat inflammation and other...
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6967196 |
Sulfonamide compounds and uses thereof
In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the...
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6951862 |
Calcium channel blockers comprising two benzhydril moieties
Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.
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6949553 |
Aliphatic compounds, their synthesis method, and utilization of the same
The present invention relates to aliphatic compounds of the formula I, or stereoisomers thereof, or their pharmaceutically acceptable salts:
wherein A represents an optionally substituted CH 3...
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6943168 |
Calcium channel inhibitors comprising benzhydril spaced from piperazine
Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.
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6936600 |
Sorbitol dehrydrogenase inhibitors
This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I,
wherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to...
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6916816 |
Phenanthryl piperazinyl dicarboxylic acids as selective NMDA receptor modulating agents
Disclosed are compounds of formula (I) wherein: L is (a) optionally substituted by replacement of one or more of the hydrogen atoms on the phenanthrene ring system by one or more groups other than...
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6916812 |
Alpha-aminoamide derivatives as melanocortin agonists
Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the...
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6903092 |
Naphthamide neurokinin antagonists for use as medicaments
Compounds having the general formula
wherein R 1 , R 2 , R 3 , R 4 , R 5 , X 1 and X 2 are as defined in the specification, methods of using such compounds for the treatment of diseases and...
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6897218 |
Nitric oxide donors based on metallic centers
A metal complex of a piperazineNONOate derivative of the formula:
wherein a) R 1 and R 2 independently represent hydrogen, linear or branched (C 1 -C 4 ) alkyl, optionally substituted by 1...
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6897209 |
Labelled factor XIIIa substrates
A complex of a radiometal or paramagnetic metal ion with a metal chelating agent such as a diaminedioxime has attached thereto a substituent of formula (Y) m -A-NHR) k can function as a substrate...
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6878712 |
Amides as inhibitors for pyruvate dehydrogenase
A compound of formula (I):
wherein:
Ring A is a nitrogen linked mono or bicyclic heterocyclic ring as defined within; R 1 and R 2 are independently C 1-3 alkyl optionally substituted...
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6878707 |
Carboxamides useful as inhibitors of microsomal triglyceride transfer protein and of apolipoprotein b secretion
Compounds of formula (I) wherein R 2 —C, R 3 —C, R 4 —C or R 5 —C may be replaced by N; and wherein n is 1, 2 or 3; R 1 is aryl, heteroaryl or (aryl or heteroaryl)-lower alkoxy; R 2 , R 3...
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6878706 |
Cyanamides useful as reversible inhibitors of cysteine proteases
Compounds according to the following formula (I):
wherein the variables Q and R 1 to R 6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F,...
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6869943 |
Sorbitol dehydrogenase inhibitors
This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I,
wherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to...
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6861435 |
Urokinase inhibitors
The invention relates to the compounds of general formula (I), that are present with respect to R 1 as racemates as well as L- or D-configured compounds and as E/Z mixtures as well as E or Z...
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6849622 |
Aliphatic nitrogenous five-membered ring compounds
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]:
wherein
A represents —CH 2 — or —S—, R 1 ...
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6844366 |
Sulfonamide hydroxamates
This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for...
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