Patent classifications
C07D313/20
Bicyclic compound, production and use thereof
The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: ##STR00001##
wherein, R.sup.1 is a 5- to 6-membered ring group which may be substituted; X.sup.1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X.sup.2 is a bivalent group of 1 to 4 atom; Z.sup.1 is a bivalent cyclic ring group or the like; Z.sup.2 is a bond or the like; and R.sup.2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
Condensed heterocyclic compound
The present invention relates to a condensed heterocyclic compound that has an enteropeptidase inhibitory effect and is useful in the treatment or prevention of obesity, diabetes mellitus, or the like, and a medicament containing the same. Specifically, the present invention relates to a compound represented by the following formula (I) or a salt thereof, and a medicament containing the same [in the formula, each symbol is as defined in the specification]. ##STR00001##
Condensed heterocyclic compound
The present invention relates to a condensed heterocyclic compound that has an enteropeptidase inhibitory effect and is useful in the treatment or prevention of obesity, diabetes mellitus, or the like, and a medicament containing the same. Specifically, the present invention relates to a compound represented by the following formula (I) or a salt thereof, and a medicament containing the same [in the formula, each symbol is as defined in the specification]. ##STR00001##
IMPROVED METHODS AND ENZYMES
Improved methods of making amberketal and amberketal homologues and compositions comprising same, improved squalene-hopene cyclase (SHC) enzymes to be used in said methods, nucleic acid constructs and vectors encoding said enzymes, and host cells expressing said enzymes.
IMPROVED METHODS AND ENZYMES
Improved methods of making amberketal and amberketal homologues and compositions comprising same, improved squalene-hopene cyclase (SHC) enzymes to be used in said methods, nucleic acid constructs and vectors encoding said enzymes, and host cells expressing said enzymes.
Compounds and methods for detection of enzymes that remove formyl, succinyl, methyl succinyl or myristoyl groups from ε-amino lysine moieties
Provided is a compound that comprises the structure: ##STR00001## where SIG is a signaling molecule and R.sup.3 is a formyl, a succinyl, a methyl succinyl, or a myristoyl. Also provided is a kit is provided that comprises the above compound, with instructions for determining the presence of the enzyme. Additionally, a method is provided for determining whether a sample has an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an -amino of a lysine. Also provided is a method of determining whether a molecule inhibits an enzyme that removes a succinyl, a methyl succinyl, a formyl, or a myristoyl moiety from an -amino of a lysine.
Organic electroluminescent compound and organic electroluminescent device comprising the same
The present disclosure relates to an organic electroluminescent compound represented by formula 1 and an organic electroluminescent device comprising the same. By comprising the organic electroluminescent compound of the present disclosure, an organic electroluminescent device having improved driving voltage and/or luminous efficiency characteristics can be provided.
Organic electroluminescent compound and organic electroluminescent device comprising the same
The present disclosure relates to an organic electroluminescent compound represented by formula 1 and an organic electroluminescent device comprising the same. By comprising the organic electroluminescent compound of the present disclosure, an organic electroluminescent device having improved driving voltage and/or luminous efficiency characteristics can be provided.
Inhibitors of nitric oxide synthases (NOS), pharmaceutical products thereof, and methods thereof
The present invention provides NOS inhibitors such as iNOS inhibitors, or a pharmaceutically acceptable salt, ester, prodrug, complex, solvate, hydrate, or isomer thereof, in any crystalline form or in amorphous form. The inhibitors include 1,1 or 1,2 substituted-ethyl carbamimido thioates, cyclic compounds substituted with a carbamimidoyl sulfanylethylphenyl group and a carbamimidoylsulfanyl group, compounds substituted with a carbamimidoyl sulfanylethyl phenylmethyl group, bis-carbamimidoylsulfanylethyl substituted compounds, 2-propoxypyridine derivatives, alkylamine or heteroalkylamine derivatives, n-aminoethyl n-phenyl amine derivatives, and saturated heterocyclic fused benzene derivatives. Pharmaceutical products comprising the NOS inhibitors such as iNOS inhibitors and the applications thereof in prophylaxis and/or treatment of inflammatory diseases, and proliferative diseases such as cancer including gastro-intestinal, colorectal, gynecological, pancreatic, head and neck, esophageal, breast, lung, and central nervous system tumors, among others, are also provided.
Inhibitors of nitric oxide synthases (NOS), pharmaceutical products thereof, and methods thereof
The present invention provides NOS inhibitors such as iNOS inhibitors, or a pharmaceutically acceptable salt, ester, prodrug, complex, solvate, hydrate, or isomer thereof, in any crystalline form or in amorphous form. The inhibitors include 1,1 or 1,2 substituted-ethyl carbamimido thioates, cyclic compounds substituted with a carbamimidoyl sulfanylethylphenyl group and a carbamimidoylsulfanyl group, compounds substituted with a carbamimidoyl sulfanylethyl phenylmethyl group, bis-carbamimidoylsulfanylethyl substituted compounds, 2-propoxypyridine derivatives, alkylamine or heteroalkylamine derivatives, n-aminoethyl n-phenyl amine derivatives, and saturated heterocyclic fused benzene derivatives. Pharmaceutical products comprising the NOS inhibitors such as iNOS inhibitors and the applications thereof in prophylaxis and/or treatment of inflammatory diseases, and proliferative diseases such as cancer including gastro-intestinal, colorectal, gynecological, pancreatic, head and neck, esophageal, breast, lung, and central nervous system tumors, among others, are also provided.