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7390799 |
Apoptosis promoters
Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than...
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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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7365063 |
Quinazolinone and benzoxazinone derivatives and uses thereof
Compounds of the formula I:
and pharmaceutically acceptable salts thereof wherein X is N, Y is S, Z is —(CR a R b ) r —, A is —NR 3 , m is 2, n is 1, q is 2, R 2 is optioinally...
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7351708 |
Pyrrolo [2,3-b] pyridine derivatives
The present invention relates to compounds of formula I
wherein R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are...
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7348323 |
Pyrrolo [2,3-c] pyridine derivatives
The present invention relates to compounds of formula I
wherein R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are...
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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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7307079 |
1,3,5-Triazine derivatives as ligands for human adenosine-A3 receptors
The invention relates to a group of novel triazine derivatives which are ligands for human adenosine-A 3 receptors, as well as to pharmaceutical compositions containing a pharmacologically active...
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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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7238688 |
Piperidine compounds
Disclosed are novel compounds of the formula
Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or...
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7179803 |
Method of modulating ion channel functional activity
The present invention relates generally to a method of retarding, reducing or otherwise inhibiting viral functional activity and, more particularly, to a method of reducing, retarding or otherwise...
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7141562 |
Substituted benzoxazinones and uses thereof
Compound of the Formula:
and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO 2 — or —(CR a R b ) r —, n is 1 or 2, R 2 is aryl or...
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7074798 |
Xanthine derivative and DPPIV inhibitor
The present invention provides novel compounds exhibiting an excellent DPPIV inhibition effect. The compounds are represented by the formula:
wherein, m is 0 or 1;
n is 0; R 31 , R 32 , R 33 ,...
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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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7067513 |
Phenylpiperazines
The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D 2 receptor and/or the serotonin reuptake site,...
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7022696 |
Piperazino-derivatives and their use as PDE4 inhibitor
The compounds of formula I
in which R1, R2, R3, A, X, s and R9 have the meanings as given in the description are novel effective PDE4 inhibitors.
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7022687 |
Combination of loteprednol and antihistamines
The present invention relates to a novel combination of a soft steroid, in particular loteprednol, and at least one antihistamine, such as, for example, azelastine and/or levocabastine, for...
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7015221 |
2,4-disubstituted triazine derivatives
This invention concerns the use of the compounds of formula
the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof,...
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6960575 |
Thiazine derivatives
A compound having 3-oxo-3, 4-dihydro-2H-1, 4-thiazine 4-tetrahydropyrazine as a main skeleton. The compound is a chymase inhibitor and is represented by the following formula [I] and salts thereof:...
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6906057 |
Methods for modulating FXR receptor activity
Methods for modulating the activity of the mammalian FXR receptor. The methods include methods of treating a hyper- or hypocholesterolemic mammal comprising contacting the mammal with synthetic...
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6890921 |
Arylsubstituted piperazines useful in the treatment of benign prostatic hyperplasia
This invention relates to a series of arylsubstituted piperazines, of Formula I
pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the...
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6890517 |
Inhalable formulation of a solution containing a tiotropium salt
A liquid, propellant-free pharmaceutical preparation comprising:
(a) a first active substance comprising a tiotropium salt, in a concentration based on tiotropium of between 0.0005% and 5%...
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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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6821965 |
Amidobenzamide derivatives which are useful as cytokine inhibitors
The invention concerns amide derivatives of the Formula (I) wherein R 3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy,...
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6821951 |
Processes for making pharmaceutical oral ECB formulations and compositions
A fluid bed spray process is described where one or more carbohydrates are incorporated into an echinocandin formulation to provide a significant improvement in thermal stability. The carbohydrate...
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6800636 |
Farnesyl protein transferase inhibitors
Disclosed are compounds of the formula: wherein R 8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R 9 represents a carbamate, urea, amide or sulfonamide group; and the...
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6743788 |
Carbamate and oxamide compounds
Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or...
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6713472 |
Thiazine or pyrazine derivatives
A compound which is a chymase inhibitor and which is represented by a formula [I] and salts thereof. In the formula [I], X is R 6 —(A 2 ) n —N, R 1 and R 2 are H, alkyl, cycloalkyl or aryl, R...
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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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6699856 |
Pyrazinones, compositions containing such compounds and methods of use
Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also...
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6656932 |
Benzo thiadiazine matrix metalloproteinase inhibitors
Selective MMP-13 inhibitors are benzo thiadiazines of the Formula or a pharmaceutically acceptable salt thereof, wherein R 2 is hydrogen or alkyl; R 1 and R 3 include hydrogen, alkyl, and...
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6620808 |
Endocrine modulation with positive modulators of AMPA type glutamate receptors
Methods for modulating the endocrine system of a mammal are provided. In the subject methods, a positive allosteric modulator of AMPA receptors of the hypothalamus are administered to the host. The...
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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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6583136 |
Antifungal ethers
The present invention concerns compounds of formula the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein D represents a tetrahydrofuran or...
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6541472 |
Compounds, compositions and methods for preventing and treating pestivirus infection and associated diseases
Triazinoindole derivatives are useful in the prophylaxis and treatment of pestivirus infections and diseases associated with pestivirus infections.
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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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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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6448244 |
Water soluble azoles as broad-spectrum antifungals
The present invention concerns novel water-soluble azole compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof;...
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6436924 |
Antihistamine leukotriene combinations
The invention relates to a pharmaceutical composition for the treatment of allergic rhinitis, vasomotor rhinitis, and allergic conjunctivitis, which comprises (a) a nonsedating antihistamine or a...
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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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6355640 |
Pyrazolopyridine adenosine antagonists
The present invention relates to a novel pyrazolopyridine compound of the following formula: wherein R 1 is aryl, and R 2 is cyclo(lower)alkyl which may have one or more suitable...
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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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6326371 |
Pyrudyl and pyrimidylpiperazine derivatives
The present invention relates to a method for treating a patient suffering from a mental disorder, comprising administering to the patient an effective 5-HT 1A agonistic and 5-HT 2 antagonistic...
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6316438 |
Fused pyridopyridazine inhibitors of cGMP phosphodiesterase
Compounds of the formula ##STR1## are useful as inhibitors of cGMP PDE especially Type 5.
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6313111 |
Substituted 6H-1,3,4-thiadiazine-2-amines, the use thereof as anaesthetising, cardiovascular and hypometabolic agents, and pharmaceutical composition containing them
Substitued 6H-1,3,4-thiadiazin-2-amines of the following general formula: ##STR1## wherein Ar is phenyl optionally substituted with one or more chloro, bromo atoms, C 1 -C 4 alkoxy, or C 1 -C 4 ...
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6299888 |
Azelastine hydrochloride-containing percutaneous preparation having good percutaneous absorbability and reduced skin irritation
The invention relates to azelastine hydrochloride-containing percutaneous preparations which comprises, as base ingredients; hydrocarbon and/or beeswax, and a surfactant.
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6255302 |
1,4-piperazine 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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6225324 |
Antidepressant heterocyclic compounds
Compounds of formula I are useful antidepressant agents ##STR1## demonstrating potent inhibition of 5-HT reuptake. Z is selected from among various phenyl and hetaryl moieties while Y is benzyl or...
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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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