Patent classifications
C07D515/02
Optically active 2-hydroxy tetrahydrothienopyridine derivatives, preparation method and use in manufacture of medicament thereof
Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases.
Furanone derivative
To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): ##STR00001##
wherein A represents COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.
Indoles as respiratory syncytial virus antiviral agents
Indoles having inhibitory activity on RSV replication and having the formula I ##STR00001##
the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
Process for preparation of (2S, 5R)-7-oxo-6-sulphooxy-2-[((3R)-piperidine-3-carbonyl)-hydrazino carbonyl]-1,6-diaza-bicyclo [3.2.1]-octane
A process for preparation of (2S, 5R)-7-oxo-6-sulphooxy-2-[((3R)-piperidine-3-carbonyl)-hydrazino carbonyl]-1,6-diaza-bicyclo[3.2.1]octane is disclosed.
Polymorphs and process for preparation of (2S, 5R)-7-oxo-N-[(2S)-pyrrolidin-2-yl-methyloxy]-6-(sulfooxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide
A process for preparation of compound of Formula (I) is disclosed. The application is also directed to polymorphic forms of the compound of formula (I). ##STR00001##
Substituted triazolopyridines
The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds. ##STR00001##
6-arylamino pyridone carboxamide as MEK inhibitors
The invention provides novel substituted 6-arylamino pyridone carboxamides represented by Formula I, or a pharmaceutically acceptable salt, solvate, poly-morph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans. ##STR00001##
Ring-fused heterocyclic compound
The ring-fused heterocyclic compound or a pharmaceutically acceptable salt thereof according to the present invention has a T-type calcium channel regulatory effect, and is useful, for example, as a medicament for treating and/or preventing pruritus. The present invention provides a ring-fused heterocyclic compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof and the like which has a T-type calcium channel regulatory effect and is useful as a therapeutic and/or preventive agent for pruritus, and the like. ##STR00001##
[wherein, R.sup.1 represents optionally substituted lower alkyl and the like, R.sup.2 represents optionally substituted lower alkyl and the like, R.sup.3 represents the formula (II): ##STR00002##
(wherein, n represents 0 or 1, R.sup.3a represents a hydrogen atom and the like, R.sup.3b represents a hydrogen atom and the like, and R.sup.3c represents a hydrogen atom and the like) and the like, Q represents a hydrogen atom and the like, and W.sup.1 represents a nitrogen atom and the like, W.sup.2 represents a nitrogen atom and the like].