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8143406 |
Process for the manufacture of HI-6 dimethanesulfonate
The invention provides a process for the manufacture of HI 6 dimethanesulfonate comprising contacting an O-protected pyridine aidoxime compound with bis(methylsulphonoxymethyl)ether in a suitable...
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8063036 |
Benzamides and related inhibitors of factor Xa
Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described....
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8053212 |
Non-standard nucleoside analogs with reduced epimerization
This invention relates to nucleoside, nucleotide, and oligonucleotide analogs that incorporate non-standard nucleobase analogs, defined to be those that present a pattern of hydrogen bonds to a...
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8003797 |
Pyridine carboxamide orexin receptor antagonists
The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric...
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7973059 |
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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7947680 |
Adamantyl diamide derivatives and uses of same
The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions...
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7939548 |
Certain chemical entities, compositions, and methods
Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with...
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7932270 |
Certain chemical entities, compositions, and methods
Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with...
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7901559 |
Polyacrylamide gel for electrophoresis, polyacrylamide gel electrophoresis method using the same, method of producing the same, and acrylamide compound
It is intended to provide a method for easily detecting a phosphorylated peptide (protein) in a test sample by using SDS-polyacrylamide gel electrophoresis (SDS-PAGE) which has been conventionally...
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7872029 |
Chalcone and its analogs as agents for the inhibition of angiogenesis and related disease states
The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit...
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7816535 |
Vinyl-phenyl derivatives for inflammation and immune-related uses
The invention relates to compounds of structural formula (Ia): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, X4, X6, X10, R1, Y, Z, L, and n are...
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7728013 |
Method of modulating stress-activated protein kinase system
Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38...
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7560553 |
Use of fuse nicotinamides to promote neurogenesis
The present invention provides a group of compounds found to increase the number of neurons derived from stem cells for use as a therapeutic agent in neurological conditions or diseases. In one...
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7553798 |
Heterocyclic carboxamides with microbiocidal activity
Compounds of the formula (I), in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
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7547782 |
Met kinase inhibitors
The present invention is directed to compounds having the formula I or II: including salts thereof, and methods for using them for the treatment of cancer.
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7544702 |
Bisaryl-sulfonamides
Bisaryl-sulfonamide compounds having the formula wherein Ar, R1, R2, L, B, W, X, Y, and Z, compositions and methods are provided that are useful in the treatment or prevention of a condition or...
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7414060 |
Pyridine-2-carboxyamide derivatives
The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to...
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7371747 |
Cyanoalkylamino derivatives as protease inhibitors
The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical...
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7288124 |
Heteroaromatic binuclear black direct dyes
Disclosed herein are novel heteroaromatic binuclear direct dyes, dye compositions containing these dyes and also a process for dyeing keratin fibers using them. In particular, the invention relates...
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7157580 |
Aminopyrimidine and aminopyridine anti-inflammation agents
Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein
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7135472 |
3-Heterocyclic benzylamide derivatives as potassium channel openers
The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and Het are as defined in the specification,...
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7109220 |
Amino substituted pyridinyl methanone compounds useful in treating kinase disorders
The present invention provides amino substituted pyridinyl methanone compounds; pharmaceutical compositions comprising the compounds and methods of synthesis thereof. The compounds, which are...
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7074742 |
Pyridinyl amides and imides for use as fungicides
Compounds of Formula (I), their N-oxides and agriculturally suitable salts are disclosed which are useful as fungicides formula (I), (II) wherein A is a substituted pyridinyl ring; B is a...
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7034035 |
Fungicidal mono-, bi-, and tri-cycloheteroalkyl amides and their compositions, methods of use and preparation
The present invention relates to compounds of Formula I: wherein: a) represents a 6-membered heterocyclic aromatic ring in which X1 is N and X2, X3 and X4 are each independently CR″; R″ is ind...
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6995162 |
Substituted alkylamine derivatives and methods of use
Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and...
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6949655 |
Acyclic piperidine derivatives
A compound having the formula (I): wherein: each R1, R2, R3 and R4 are independently selected from (C1-C10)-straight or branched alkyl, Ar-substituted- (C1-C10)-straight or branched alkyl,...
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6943180 |
Substituted N-arylsulfonyl-proline derivatives as potent cell adhesion inhibitors
Compounds of formula (I) are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These...
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6936597 |
Prodrugs of anticancer agents employing substituted aromatic acids
Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties;Y1 is...
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6878714 |
Substituted alkylamine derivatives and methods of use
Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically...
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6794396 |
Substituted pyridines useful for inhibiting cholesteryl ester transfer protein activity
A class of substituted pyridines that are useful for inhibiting the activity of cholesteryl ester transfer protein, and have the structural formula (IA), wherein R2, R3, R4, R5, and R6 are defined...
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6787546 |
Heterocycle derivatives and drugs
The object of the invention is to provide an excellent compound as a drug. The invention relates to a heterocyclic compound shown by the following formula:A—B—D—E [1]whereinA is heteroaryl or its o...
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RE38506 |
Potent inducers of terminal differentiation and methods of use thereof
The present invention provides the compound having the structure: wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a...
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6680383 |
Method for making nevirapine
A process for making nevirapine, comprising the following steps: (a) reacting a 2-halo-3-pyridinecarbonitrile of the formula wherein X is a fluorine, chlorine, bromine or iodine atom, preferably...
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6677452 |
Pyridine carboxamide or sulfonamide derivatives and combinatorial libraries thereof
The present invention relates to novel pyridine carboxamide or sulfonamide derivative compounds of the following formula: wherein R1 to R6 have the meanings provided herein. The invention further...
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6656958 |
Substituted pyridine compounds useful for controlling chemical synaptic transmission
The present invention is directed to a series of substituted pyridine compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical...
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6610717 |
Dihydropyridine derivatives
Dihydropyridine derivatives represented by the following formula: analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type...
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6521626 |
Thiocarboxamide derivatives
Compounds of formula (1): whereinR1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic...
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6503928 |
Arylpiperidine and aryl-1,2,5,6-tetrahydropyridine amide derivatives
Compounds of the formula wherein R1, R2, R3, R4, X and n are defined in the specification, are useful for the treatment of anxiety, depression and related CNS disorders, and other related...
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6486183 |
Antivirals
Compounds of formula (I): wherein Rx is cyano or bromo; R1 is halo; R2 is C1-C3 alkyl, and pharmaceutically acceptable salts and prodrugs thereof have activity as antiretrovirals.
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6465471 |
Cinnamic acid derivatives
Compounds of formula (1) are described: in which Het is a heteroaromatic group, Alk1 is an optionally substituted aliphatic or heteroaliphatic chain and R is a carboxylic acid or a derivative...
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6458813 |
Substituted pyridine compounds and methods of use
Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-α, IL-1β, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain a...
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6414157 |
3-Substituted tetrahydropyridopyrimidinone derivatives, method for producing the same, and their use
3-substituted tetrahydropyridopyrimidinone derivatives of the formula (I) wherein the radicals have the meanings given in the Description, to a method for producing said derivatives and, to their...
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6399606 |
Neuroprotective agents and methods related thereto
Neuroprotective agents are disclosed having the following structure: wherein R1, R2, R3, R4 and R5 are as defined herein. Such compounds have utility in the treatment of conditions which benefit...
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6329362 |
Cinnamic acid derivatives
Compounds of formula (1) are described: ##STR1##wherein L1 is a covalent bond or a linker atom or group; R is a carboxylic acid (--CO2 H) or a derivative threof; R6 and R7 which may be the same or...
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6313148 |
Aromatic amine compounds that antagnoize the pain enhancing effects of prostaglandins
Compounds antagonistic of the pain enhancing effects of prostaglandins are disclosed. The compounds comprise an optionally-substituted A ring with a --CH(R3)N(R2)B--R1 and --OD groups positioned in...
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6225316 |
3-phenyl-pyridine-derivatives
The invention relates to compounds of the formula ##STR1##wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1 may be together...
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6197792 |
Tetra-substituted phenyl derivatives and processes for their preparation
Compounds of the general formula (1) ##STR1##wherein: W-- is N--; Y is halogen or an alkyl or --XRa group; X is --O--, --S(O)m -- or --N(Ra)--, where m is zero or an integer 1 or 2; Ra is hyd...
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6187926 |
Process for producing quinolone derivatives
The present invention relates to a process for producing a 4-quinolone derivative, comprising allowing an o-aminoacetophenone derivative to react with a formic acid in an aprotic solvent in the...
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6020335 |
(N-(pyridinylmethyl)-heterocyclic)ylideneamine compounds as nicotinic acetylcholine receptor binding agents
An (N-(pyridinylmethyl)-heterocyclic)ylideneamine compound of the formula ##STR1## wherein R3, A, and B are as described below, and its pharmaceutically acceptable salts and prodrugs. Compounds of...
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6005113 |
Long wavelength dyes for infrared tracing
The invention relates to fluorescent dyes that are substituted or unsubstituted derivatives of 1-(isoindolyl)methylene-isoindole that are bound through both isoindole nitrogens to a boron...
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