|8633323||Process for preparing bis(thiohydrazide amides)|
Disclosed herein are methods of preparing a bis(thio-hydrazide amides) compounds of the following structural formula: wherein R1, R2, R3, R4, R5, R6 and R13 are defined herein.
|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 solvent to form an intermediate compound, contacting said intermediate...
|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...
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 methods...
|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 composition comprising these compounds, method of treating diseases mediated by...
|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 to heteroaromatic binuclear direct dyes comprising a pyridine nucleu...
|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 ...
|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
|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 cyclin dependent kinase (CDK) inhibitors, can be used to treat or ameliora...
|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 substituted pyridinyl ring; W is C=L or SOn is O or S; R1
|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 w...
|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 pharmaceutically acceptable derivatives thereof, pharmaceutical composit...
|6949655||Acyclic piperidine derivatives|
A compound having the formula (I): wherein: each R1, R2, R3 and R4 are independently selected from (C1-C10)-straight ...
|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 compounds may be formulated into pharmaceutical compositions and are suitable...
|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 m...
|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 acceptable salts thereof, pharmaceutical compositions and methods for p...
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 conditions, such as, fo...
|6833378||Corticotropin releasing factor antagonists|
Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined...
|6800619||Caspase inhibitors and uses thereof|
Described herein are compounds that are useful as caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrog...
The invention concerns amide derivatives of the Formula I wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carb...
|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...
|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  wherein A is heteroaryl or its oxi...
This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor....
|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 i...
|6680383||Method for making nevirapine|
A process for making nevirapine, comprising the following steps: (a) reacting a 2-halo-3-pyridinecarbonitrile of the formula ##STR1## wherein X is a fluorine, chlorine, bromine or iodine atom, preferably chlorine or bromine, with cyclopropylamine, to y...
|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: ##STR1## wherein R1 to R6 have the meanings provided herein. The invention further relates to combinatorial lib...
|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 compositions containing these compounds. Preferred compound...
This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediate...
|6624178||Compounds for the management of aging-related and diabetic vascular complications, process for their preparation and therapeutic uses thereof|
The invention discloses novel compounds of the pyridinium series useful for the management of diabetes and aging-related vascular complications, including kidney disease, nerve damage, atherosclerosis, retinopathy, dermatological disorders and discolorati...
Dihydropyridine derivatives represented by the following formula: ##STR1## analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel, and they are used as therapeutic agen...
|6608060||Inhibitors of p38|
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides...
|6605624||Substituted pyridines useful for inhibiting cholesteryl ester transfer protein activity|
##STR1## 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 de...
|6566527||Process for preparing 1-(6-methylpyridin-3-yl)-2-[4-methylsulphonyl)-phenyl]ethanone|
A five-step process for preparing 1-(6-methylpyridin-3-yl)-2-[4-methylsulfonyl)phenyl]ethanone of formula (I): ##STR1## The process involves the following steps: (a) 4-(methylthio)benzyl alcohol is converted into 4-(methylthio)benzyl chloride; (b) 4-...
The invention concerns amide derivatives of the Formula I ##STR1## wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R2
Compounds of formula (1): ##STR1## wherein R1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Alk1 is an optionally...
|6503928||Arylpiperidine and aryl-1,2,5,6-tetrahydropyridine amide derivatives|
Compounds of the formula ##STR1## 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 conditions suc...
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....
|6465471||Cinnamic acid derivatives|
Compounds of formula (1) are described: ##STR1## 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 thereof. The compounds are able to inhibit ...
|6458957||,-dibromo--chloro-acetophenones as synthons|
This disclosure relates to the use of ,-dibromo--chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-,...
|6458813||Substituted pyridine compounds and methods of use|
Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-, IL-1ଲ, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel com...