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6919350 |
Compositions and methods for reducing respiratory depression and attendant side effects of mu opioid compounds
A method of reducing, treating or preventing drug-mediated respiratory depression, muscle rigidity, or nausea/vomiting in an animal, incident to the administration to said animal of a mixed...
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6916821 |
Methods of treating disorders with Group I mGluR antagonists
mGluR5 antagonists are used for the treatment and prevention of disorders, including Fragile X, autism, mental retardation, schizophrenia and Down's Syndrome. The methods of the invention can be...
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6916830 |
Substituted tetrahydroisoquinolines as C5a receptor modulators
Substituted tetrahydroisoquinolines and related compounds are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly...
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6911457 |
Diabetes imaging probes
The present invention relates to novel imaging probes and methods for using the probes in diagnostic imaging processes and other imaging processes to determine physiological functions.
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6890928 |
Aromatic sulfone hydroxamic acids and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix...
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6890937 |
Aromatic sulfone hydroxamic acid metalloprotease inhibitor
A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix...
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6878723 |
LTA4 hydrolase inhibitors
The invention concerns compounds inhibiting LTA 4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.
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6875775 |
Triphenylalkene derivatives and their use as selective estrogen receptor modulators
The invention provides novel selective estrogen receptor modulator compounds of the general formula:
wherein R1 and R2, which are the same or different are
a) H, halogen, OCH 3 , OH; or...
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6858623 |
Compounds useful as reversible inhibitors of cysteine proteases
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , Het and X are defined herein. The...
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6855324 |
Therapeutic placebo enhancement of commonly-used medications
There is provided a method and associated kit for reducing the normal dosage of a pharmaceutical given to a patient for the treatment of a disorder without substantially reducing its effectiveness....
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6846836 |
N-substituted phenylurea inhibitors of mitochondrial F1F0 ATP hydrolase
Compounds having the formula (I),
are useful as inhibitors of mitochondrial F 1 F 0 ATP hydrolase, wherein R 1 -R 8 , X, A, Z, n and m are defined herein.
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6846830 |
Naphtalene derivatives and their pharmaceutical use
Use of compounds of the formula (I) where A, E, R 1 , R 2 , p and q have the meanings given in the specification are GluR6 antagonists useful for the treatment of disorders of the central nervous...
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6838470 |
Arylpiperidinopropanol and arylpiprazinopropanol derivatives and pharmaceuticals containing the same
A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate:
wherein R 1 to R 4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or...
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6838472 |
Substituted urea retinoid agonists
The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention...
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6825202 |
Arylsulfonyl derivatives with 5-HT6 receptor affinity
This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula (I): wherein Ar, R 1 , R 2 , R 3 or R 4 are as defined in the...
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6821989 |
Method of treating certain cancers using an estrogen agonist/antagonist
The present invention provides methods of treating cancer of the liver, ovarian cancer, a desmoid tumor, glioma, pancreatic cancer, or renal cell carcinoma using an estrogen agonist/antagonist. The...
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6812231 |
Benzamidine derivative
Benzamidine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an effect of inhibiting activated...
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6809093 |
2-substituted heterocyclic compounds
Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds. An example compound has the formula:
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6803370 |
Alpha amino acid derivatives—inhibitors of leukocyte adhesion mediated by VLA-4
Disclosed are certain alpha amino acid compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such...
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6800639 |
Pharmaceutical combination for the treatment of cancer
In accordance with the present invention there is provided a pharmaceutical combination useful for the treatment of cancer comprising at least one active compound of formula (I): and at least...
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6797694 |
Chemical compounds having ion channel blocking activity for the treatment of immune dysfunction
The present invention relates to chemical compounds having inhibitory activity on an intermediate conductance Ca 2+ activated potassium channel (IK Ca ), and the use of such compounds for the...
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6784175 |
Use of substituted 1-amino-5-phenylpentane-3-ol and/or 1-amino-6-phenylhexane-3-ol compounds as medicaments
The use of at least one substituted 1-amino-5-phenylpentane-3-ol and/or 1-amino-6-phenylhexane-3-ol compound and/or one of the enantiomers thereof and/or one of the diastereomers thereof and/or one...
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6780858 |
Antibacterial agents
Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.
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6777424 |
Methods for treating osteoarthritis using an estrogen agonist / antagonist
The present invention provides methods and kits for treating osteoarthritis using an estrogen agonist/antagonist.
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6774135 |
Method of enhancing lysosomal α-galactosidase A
A method of enhancing the activity of lysosomal α-Galactosidase A (α-Gal A) in mammalian cells and for treatment of Fabry disease by administration of 1-deoxy-galactonojirimycin and related...
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6756370 |
Piperidine alcohols
The invention relates to compounds of formula (I), wherein R 1 , R 2 and A have the meanings given in claim 1, are potent 5-HT 2A antagonists and are suitable for treating psychoses,...
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6750229 |
Methods for treating skin pigmentation
This invention relates to methods and compositions for bringing about changes in skin pigmentation. More particularly, this invention relates to compounds which affect melanogenesis and can be used...
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6740337 |
Bioavailable dosage form of isotretinoin
The present invention relates to a bioavailable pharmaceutical composition of 13-cis vitamin A acid (also known as 13-cis retinoic acid and isotretinoin) and a process for preparing the same....
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6734202 |
Fungicidal mixtures
The invention relates to a novel fungicidal composition comprising a fungicidally acceptable carrier and/or surface active agent together with, and synergistically effective amounts of (a) at...
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6734177 |
Certain salts of discodermolide acid, pharmaceutical compositions containing them and their use in treating tumors
The present invention relates to certain salts of discodermolide acid, pharmaceutical compositions containing said salts, the use of said salts in treating tumors and to a process for making said...
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6734196 |
Substituted pyridine or piperidine compounds
The invention relates to a compound of formula (I): wherein: A represents pyridine, pyridinium or piperidine R 1 , R 2 , R 3 and R 4 are as defined in the description R 5 represents hydrogen,...
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6730671 |
Compounds useful as reversible inhibitors of cathespin S
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are...
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6723711 |
Propanoic acid derivatives that inhibit the binding of integrins to their receptors
A compound of the structure A method for the inhibition of the binding of α 4 β 1 integrin to its receptors, for example VCAM-1(vascular cell adhesion molecule-1) and fibronectin;...
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6720340 |
Nicotine receptor agonists in stem cell and progenitor cell recruitment
The present invention features methods for recruitment of bone marrow-derived stem cells (e.g., endothelial cell precursors, hematopoietic stem cells) by administration of nicotine or other...
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6720336 |
4,4-biarylpiperidine derivatives
The present invention relates to compounds of the formula I, wherein Z 1 , Z 2 , R 1 , R 2 and R 3 are defined as in the specification, pharmaceutical compositions containing such compounds...
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6713492 |
N-acyloxylated cycloalkyl compounds, composition containing the same and methods of use therefor
Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C 4 or C 5 cycloalkyl which...
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6710056 |
Amidinophenylpyruvic acid derivatives
An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood...
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6703406 |
2,6-disubstituted piperidines as modulators of nicotinic acetylcholine receptor mediated neurotransmitter release, uptake and storage
Compounds used for treating dependence on or withdrawal from a drug of abuse, for an eating disorder or for a CNS disease or pathology having the following formulas:
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6696469 |
Cyclobutenedione compounds
Compounds of formula (I): wherein: X represents a heterocycle bonded to the remainder of the molecule by a nitrogen atom of the heterocycle, or an —NR 2 R 3 group wherein R 2 represents...
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6689794 |
Aromatic sulfone hydroxamates and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known...
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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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6683093 |
Aromatic sulfone hydroxamic acids and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamates (also known as aromatic sulfone hydroxamic acids) and salts thereof that, inter alia, tend to inhibit matrix metalloproteinase (also...
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6676950 |
Neurokinin receptor antagonists and methods of use thereof for inhibiting HIV infection
Compositions and methods are provided which may be used to advantage for the treatment of HIV infection. More specifically, neurokinin receptor antagonists and methods for administration to inhibit...
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6676968 |
Release-regulating preparations comprising biphenyldiamine derivatives
A medicinal composition containing one or more compounds selected from the compounds represented by the following formula (I), salts of these compounds, solvates of these compounds and solvates of...
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6670378 |
Method of treating Parkinson's disease
A method of preventing the development of dyskinesias in patients being treated for Parkinson's Disease requires the administration of a pharmacologically effective amount of a substituted...
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6660749 |
Inhibition of glycolipid biosynthesis
Methods for treating lipid storage diseases using compounds that inhibit glucosyltransferase enzymes are disclosed herein. The invention relates to the treatment of lipid storage disease with...
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6653324 |
Stabilization of wood substrates
The invention relates to a method of protecting wood against light-induced degradation by treatment with an impregnation which penetrates the surface of the wood comprising a) water without an...
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6649614 |
Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent for treatment of depression or anxiety
The present invention relates to the treatment of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and an antidepressant or...
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6642256 |
Piperidine derivatives as subtype selective N-Methyl-D-Aspartate antagonists
Described are piperidines of Formula I and pharmaceutically acceptable salts thereof. The compounds of Formula I are antagonists of NMDA receptor channel complexes useful for treating cerebral...
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