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6706733 |
Quinolinone derivative formulation and its production method
The problem to be solved by the present invention is to provide a quinolinone derivative formulation, and its production method, having for its active ingredient the β crystal form and/or γ...
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6699877 |
Substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acid derivatives
A substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acid derivative of formula I and salts thereof with pharmaceutically acceptable acids. Also disclosed are methods for making the...
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6699894 |
Methods for treatment of inflammatory bowel disease
Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of inflammatory bowel disease.
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6696442 |
Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof
This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof,...
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6696459 |
Steroid receptor modulator compounds and methods
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds,...
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6696466 |
Methods of treating select neuronal inflammatory disorders using hydroxyalkylquinolines
Methods of treating select mammalian disorders using a leukotriene antagonist are described. The methods involve administering to the mammal a therapeutically effective amount of a compound having...
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6689771 |
Amide derivatives as inhibitors of matrix metalloproteinases, TNF-α, and aggrecanase
The present application describes novel amides and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein these compounds are useful as inhibitors of matrix...
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6686382 |
Sulfonamides and derivatives thereof that modulate the activity of endothelin
Thienyl-, furyl-, pyrrolyl- and phenylsulfonamides, formulations of pharmaceutically-acceptable derivatives thereof and methods for modulating or altering the activity of the endothelin family of...
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6686388 |
Regulators of the hedgehog pathway, 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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6677353 |
Substituted N-phenyl-N-heteroaralkyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer...
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6673801 |
Dihydroxyhexanoic acid derivatives
Dihydroxyhexanoic acid derivatives of the general formula are useful to treat inflammation and other immune disorders.
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6673813 |
Methods for identifying and treating resistant tumors
This invention provides a method of identifying and reversing multidrug resistance in a multidrug resistant tumor comprising administering a multidrug resistance reversing amount of any of the...
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6653322 |
Therapeutic combinations of RAR antagonists and RXR agonists and use thereof
The present invention provides compositions and methods for treating an animal, preferably a human, suffering from or predisposed to a physical disorder by administering an effective amount of a...
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6653309 |
Inhibitors of IMPDH enzyme technical field of the invention
The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions...
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6653302 |
Quinoline and quinazoline compounds useful in therapy
Compounds of formula I, wherein R 1 represents C 1-4 alkoxy optionally substituted by one or more fluorine atoms; R 2 represents H or C 1-6 alkoxy optionally substituted by one or more...
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6653321 |
Naphthylsulfonic acids and related compounds as glucose uptake agonists
Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or...
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6645966 |
Treatment of malaria with farnesyl protein transferase inhibitors
Disclosed is a method of treating Malaria comprising administering an effective amount of an FPT inhibitor to a patient in need of such treatment alone or in combination with an additional...
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6645968 |
Potassium channel openers
Compounds of formula I: are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of...
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6645961 |
Dry granulation formulation for an HIV protease inhibitor
This invention relates to a dry granulation capsule formulation of the HIV protease inhibitor, indinavir sulfate, which is useful in the treatment of AIDS, ARC or HIV infection. Processes for...
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6642254 |
Heterocyclic compounds and their therapeutic use
N-oxides of formula (i) wherein R 1 is CH 3 , CH 2 F, CHF 2 or CF 3 ; R 2 is CH 3 or CF 3 ; R 3 is F, Cl, Br, CN or CH 3 ; and R 4 is H, F, Cl, Br, CN or CH 3 ; and...
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6632840 |
Monoacyl-substituted guanidines, a process for their preparation, their use as a medicament or diagnostic aid, and pharmaceutical compositions containing them
Monoacyl-substituted guanidines of formula III, or a salt or acid thereof, and their use as medicine or diagnostic aid: in which X(2) is
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6632826 |
Carbocyclic HIV protease inhibitors
The present invention is concerned with novel HIV protease Inhibitors of formula I as individual isomers, racemates, non-racemic mixtures or mixtures of diastereoisomers; wherein n, R 1 and R 4...
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6630489 |
Quinoline derivatives as tyrosine kinase inhibitors
The invention concerns quinoline derivatives of formula (I) wherein n is 0-3 and each R 4 , which may be the same or different, is a substituent such as halogeno, hydroxy, amino, nitro,...
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6627642 |
Quinolinone derivative preparations and process for producing the same
The problem to be solved by the present invention is to provide a quinolinone derivative formulation, and its production method, having for its active ingredient the β crystal form and/or γ...
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6620844 |
Method for reducing blood insulin levels by reducing in vivo cathepsin L activity
Methods and compositions are provided for modulating blood insulin levels of animals by targeting the gene and gene products of cathepsins, particularly cathepsins L, K, and S, and especially...
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6617336 |
2-arylquinoline derivatives, preparation and therapeutic use thereof
Compounds of general formula (I) in which: A represents a hydrogen atom, a hydroxyl, a C 1-3 alkoxy group, a hydroxy(C 1-6 alkyl) group, a (C 1-3 alkoxy)(C 1-3 alkyl) group, a thiol, (C 1-6 ...
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6617333 |
Antineoplastic combinations comprising
This invention provides the use of a combination of CCI-779 and EKB-569 in the treatment of neoplasms.
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6613770 |
Quinoline derivatives as NK-2 and NK-3 receptor ligands
A compound, or a solvate or a salt thereof, of formula (I): wherein R is linear or branched alkyl; R 1 represents hydrogen or up to four optional substituents selected from the list consisting...
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6610711 |
4-phenylpiperidines for the treatment of pruritic dermatoses
Novel compounds having general formula (I), and pharmaceutically and veterinarily acceptable salts thereof wherein R 1 , R 2 , R 3 , W, Y 1 , Y 2 , X, n and y are as defined above and processes for...
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6610702 |
Ammonium salts of inositol hexaphosphate, and uses thereof
The present invention comprises compounds, compositions thereof, and methods capable of delivering inositol hexaphospahte (IHP) to the cytoplasm of mammalian cells. In certain embodiments, the...
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6608084 |
Aza-bicycles which modulate the inhibition of cell adhesion
The invention is directed to physiologically active compounds of formula (I) wherein R 1 represents R 3 —Z 3 —, R 3 —L 2 —R 4 —Z 3 —, R 3 —L 3 —Ar 1 —L 4 —Z 3 — or R 3 —L 3...
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6608083 |
Quinoline derivatives(2)
NK 3 receptor antagonists of formula (I): in which: Ar is an optionally substituted phenyl group, or a naphthyl or C 5-7 cycloalkdienyl group, or an optionally substituted single or fused ring...
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6608061 |
Bisaryl compound and medicament for cancer treatment comprising the same
A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar 1 —S—R 1 —S—Ar 2 wherein R 1 ...
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6608085 |
4-quinolinemethanol derivatives as purine receptor antagonists (II)
Use of a compound of formula (I) as defined herein, or a pharmaceutically acceptable salt or prodrug thereof, in the manufacture of a medicament for the treatment or prevention of a disorder in...
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6605615 |
Hydrazones and analogs as cholesterol lowering agents
Hydrazones and hydrazone analogs are provided which are useful as upregulators of LDL receptors and can be used in the treatment of hypercholesterolemia and related disorders and conditions.
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6602884 |
Quinolylpropylpiperidine derivatives, their preparation, and compositions containing them
Quinolylpropylpiperidine derivatives of general formula (I) are described, and are useful as antimicrobial agents. Their preparation is also described.
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6596735 |
Quinoline derivatives useful for inhibiting farnesyl protein transferase
The invention relates to compounds of the formula: and to pharmaceutically acceptable salts and solvates thereof wherein Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , and R 10 have...
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6593340 |
Pharmaceutical compositions containing N-propargylphentermine and related analogs to treat neurodegeneration and/or depression
The present invention relates to N-propargylphentermine and its derivatives and the neuroprotective and anti-depressant activity of such compounds as well as therapeutic methods for such compounds.
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6586441 |
Adenosine receptor ligands and their use in the treatment of disease
The invention relates to cyclic heteroaromatic compounds, containing at least one nitrogen atom, and to their use in the manufacture of medicaments for the treatment of diseases, related to...
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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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6573278 |
Aryl sulfonamides and analogues thereof and their use in the treatment of neurodegenerative diseases
The present invention relates to new aryl ether sulphonamides and analogues, processes for their preparation and their use for the treatment of neurodegenerative disorders, in particular for the...
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6562822 |
Heterocyle carboxamides as antiviral agents
The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
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6559144 |
Bicyclic amino acids
Compounds of the formula I in which X, Y, Z, R 1 , R 2 , R 3 , R 4 , R 5 , R 7 , R 8 , R 11 , m and n have the meanings stated in claim 1, and their physiologically acceptable salts can be...
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6555569 |
Use of heteroaryl substituted N-(indole-2-carbonyl-) amides for treatment of infection
A pharmaceutical composition containing a glycogen phosphorylase inhibitor of Formula I or IA as defined herein is administered to a mammal to treat infection.
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6548521 |
Inhibitors of metazoan parasite proteases
Compositions and methods for treating a patient infected with a metazoan parasite by inhibiting the enzymatic action of the metazoan parasite protease, wherein there is employed at least one...
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6545019 |
Method of modulating microglial activation for the treatment of acute and chronic neurodegenerative disorders
The present invention provides methods of modulating or inhibiting microglia activation comprising the administration of a compound capable of inhibiting 5-LOX, FLAP, attenuating degradation of...
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6545020 |
Farnesyl Protein transferase inhibitors with in vivo radiosensitizing properties
The present invention is concerned with the finding that farnesyl protein transferase inhibitors have radiosensitizing properties which makes them useful for preparing a pharmaceutical composition...
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6541487 |
PDE III inhibitors for treating sexual dysfunction
Compositions that are selective PDE III inhibitors and that are effective to treat sexual dysfunction in males and females, including, but not limited to, erectile dysfunction in males. The...
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6534503 |
Melanocortin receptor-3 ligands to treat sexual dysfunction
Methods for treating sexual dysfunction, such as erectile dysfunction or sexual arousal disorder, with a compound having the generic formula X 1 —X 2 -(D)Phe-Arg-(D)Trp-X 3 . A particularly...
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6531478 |
Amino pyrazole derivatives useful for the treatment of obesity and other disorders
Amino pyrazole derivatives of the formula: which are ligands for the neuropeptide Y, subtype 5 receptor and pharmaceutical compositions containing an amino pyrazole derivative as the active...
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