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8183236 |
Compounds with HIV-1 integrase inhibitory activity and use thereof as anti-HIV/AIDS therapeutics
Pharmacophore models to be used in drug design and discovery are provided. An in silico protocol and in vitro assays are presented. Compounds and their pharmaceutically acceptable salts with HIV-1...
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8183251 |
Hydantoin compounds and pharmaceutical compositions thereof
The invention provides compounds of formula (I): wherein R1 and R2 are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for...
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8183238 |
Bicyclic and tricyclic compounds as KAT II inhibitors
Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits...
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8178542 |
Methods and compositions for treating pain
The present application relates to compounds and methods for treating pain, incontinence and other conditions.
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8178540 |
Pyrimidylmethyl-sulfonamide compounds
The present invention relates to novel pyrimidylmethyl-sulfonamide compounds and to their N-oxides, their agriculturally acceptable salts and their veterinarily acceptable salts and also to...
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8178548 |
Anti-infective agents and uses thereof
This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such...
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8178547 |
Heterocyclic antiviral compounds
Compounds having the formula I wherein A, R1, R2, R3, R4a, R4b, R4c, R5, R6, R7a, R7b, Ar1, Rc, Rd, Re, Rf, X, n and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also...
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8163793 |
Proline derivatives
The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
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8143057 |
Chelating agents and highly luminescent and stable chelates and their use
This invention relates to a group of novel chelating agents, novel chelates, biomolecules labeled with said chelates or chelating agents as well as solid supports conjugated with said chelates,...
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8138196 |
Antifungal wallboards and building materials and methods for the production thereof
The present invention relates to, inter alia, methods for the treatment of wallboards and the treated wallboards. In particular, the invention relates to the treatment of wallboards with a...
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8133886 |
Heterobicyclic carboxamides as inhibitors for kinases
The invention relates to novel compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the...
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8129377 |
6-(pyridinyl)-4-pyrimidone derivates as tau protein kinase 1 inhibitors
A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R1 represents a C1-C12 alkyl; R2 represents a hydrogen atom or...
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8106063 |
Pyrimidyl sulphone amide derivatives as chemokine receptor modulators
A compound of formula (I), pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof for the treatment of asthma, allergic rhinitis, COPD, inflammatory bowel disease,...
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8106062 |
Calcium channel blockers
The present invention is directed in part towards methods of modulating the function of calcium channels with dihydropyrimidine, dihydropyrimidone, dihydropyrimidinethione, and dihydropyridine...
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8088769 |
Cyanopyrimidinones
The invention relates to novel cyanopyrimidinones, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory.
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8080552 |
Pyrimidyl derivatives as protein kinase inhibitors
Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above...
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RE43029 |
Process for preparing a creatine heterocyclic acid salt and method of use
This invention relates to a process for the synthesis and method of use of an effective amount of a creatine heterocyclic acid salt for the regulation athletic function in humans.
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8063044 |
Pyrazole derivatives
This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to...
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8058276 |
Heterobicyclic carboxamides as inhibitors for kinases
The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and...
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8058279 |
Insecticidal pyrimidinyl aryl hyrdrazones
Pyrimidinyl aryl hydrazones are effective at controlling insects.
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8048885 |
Organic compounds
The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical...
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8026247 |
Bicyclic amides as kinase inhibitors
The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a...
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8017620 |
Dutpase inhibitors
Deoxyuridine derivatives of the formula where R1 is H or various substituents;D is —NHCO—, —CONH—, —O—, —C(═O)—, —CH═CH, —C≡C—, —NR5—;R4 is hydrogen or various substituents;R5 is H, C1-C4 alk...
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8008313 |
Methods of using diaminopyrimidine P2X3 and P2X2/3 receptor modulators for treatment of respiratory and gastrointestinal diseases
Methods for treating respiratory and gastrointestinal diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective...
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8008307 |
Heteroaryl compounds useful as inhibitors of E1 activating enzymes
This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for...
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8003643 |
Inhibitors of Akt activity
The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is...
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7998968 |
Substituted pyrimidines and [1,2, 4] triazoles and the use thereof for treating prophylaxis, cardiovascular diseases, metabolic diseases and/or central nervous system diseases
A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the...
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7998959 |
Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same
The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of ...
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7989465 |
4,6-disubstituted pyrimidines useful as kinase inhibitors
The present invention provides 4,6-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable salts and compositions thereof, and methods of using the same. The...
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7981899 |
Use of compatible solutes for inhibiting the release of ceramides
Disclosed are the use of compatible solutes for inhibiting the release of ceramides or for the prophylaxis and protection of human skin against premature skin aging and for the prophylaxis and...
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7976852 |
Compositions and methods for cancer immunotherapy
The invention relates to immunotherapeutic compounds and to methods for stimulating an immune response in a subject individual at risk for developing cancer, diagnosed with a cancer, in treatment...
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7968559 |
Methods of using 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds
Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders:
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7964620 |
Imidazole derivatives
The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3, R4, X, Y and R are described hereinabove, or a pharmaceutically acceptable salt thereof. The invention also...
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7959945 |
Dispersible bosentan tablet
The invention relates to dispersible tablets comprising the compound 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2
-(pyrimidin-2-yl)-pyrimidin-4-yl]-benzenesulfonamide.
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7960393 |
Pyrimidine derivatives useful for the treatment of diseases mediated by CRTH2
The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine derivative of...
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7956070 |
Piperidines as chemokine modulators (CCR)
Compounds of formula (I): are modulators of chemokine (for example CCR3) activity (for use in, for example, treating asthma).
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7947734 |
Substituted para-trifluoromethyl phenylate compounds and its preparation and use thereof
The invention relates to substituted para-trifluoromethyl phenyl ether compounds and its preparation and use thereof especially. The substituted para-trifluoromethyl phenyl ether compounds of the...
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7935710 |
Microbicidal pyrimidine or triazine for preventing sexual HIV transmission
The present invention concerns the microbicidal activity of certain pyrimidine or triazine containing non-nucleoside reverse transcriptase inhibitors. The compounds of the present invention inhibit...
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7901701 |
Methods for producing dried pesticide compositions
Disclosed are compositions and methods related to powder and granular emulsifiable concentrate pesticide formulations. As disclosed, emulsions from non-aqueous based liquid or solvent soluble...
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7893072 |
Trp-p8 active compounds and therapeutic treatment methods
Compounds of the disclosure provide compositions, which are effective for prophylaxis and treatment of diseases or disorders, such as cell-proliferation, angiogenesis, or apoptosis mediated...
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7888361 |
Tyrosine kinase inhibitors containing a zinc binding moiety
The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said...
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7879839 |
Potassium channel inhibitors
The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
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7875616 |
Use of tyrosine kinase inhibitor to treat diabetes
The invention relates to the use of a c-Abl-, PDGF-R-, or c-kit- tyrosine kinase inhibitor, e.g. 4-(4-methylpiperazin-1...
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7875622 |
Methods and compositions for treating pulmonary hypertension and related diseases and disorders
Methods of treating pulmonary hypertension are disclosed. Particular methods comprise the administration of a tryptophan hydroxylase inhibitor and at least one other active pharmaceutical...
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7875644 |
1-acyldihydropyrazole derivatives
Compounds of the formula (I), in which R1, R2, R3a, R3b, R3c and R3d have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter...
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7868012 |
Sulfamides as endothelin receptor antagonists for the treatment of cardiovascular diseases
The invention relates to novel sulfamic acid amides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including...
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7858644 |
EP4 receptor antagonists
Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(═O), S(═O)2, or NRN1, where RN1 is selected ...
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7858632 |
Diaminopyrimidines as P2X3 and P2X2/3 antagonists
Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a...
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7855194 |
Pyrimidine, quinazoline, pteridine and triazine derivatives
This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention...
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7855212 |
Pyridinyl acetonitriles
The present invention is related to pyridinyl acetonitriles as well as to pharmaceutical formulations containing such pyridinyl acetonitriles. Said pyridinyl acetonitriles are modulators of the...
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