Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-06-19
2000-09-12
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544354, A01N 4360, A61K 31495, C07D24136
Patent
active
061178756
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to new heterobicyclic derivatives.
One object of this invention is to provide the new and useful pyridopyrazine derivatives and pharmaceutically acceptable salts thereof which possess a strong phosphodiesterase IV (PDE IV)-inhibitory activity and a strong inhibitory activity on the production of tumor necrosis factor (TNF).
Another object of this invention is to provide processes for preparation of the pyridopyrazine derivatives and salts thereof.
A further object of this invention is to provide a pharmaceutical composition comprising said pyridopyrazine derivatives or a pharmaceutically acceptable salt thereof.
Still further object of this invention is to provide a use of said pyridopyrazine derivatives or a pharmaceutically acceptable salt thereof as a medicament for prophylactic and therapeutic treatment of PDE-IV and TNF mediated diseases such as chronic inflammatory diseases, specific autoimmune diseases, sepsis-induced organ injury, and the like in human being and animals.
DISCLOSURE OF INVENTION
The object pyridopyrazine derivatives of the present invention are novel and can be represented by the following general formula (I): ##STR2## wherein R.sup.1 is pyridyl(lower)alkyl, N-oxidopyridyl(lower)alkyl or imidazolyl(lower)alkyl, [[[halophenyl](lower)alkenoyl]amino]phenyl, [[pyridyl(lower)alkenoyl]amino]phenyl, [[[N-oxidopyridyl](lower)alkenoyl]amino]phenyl, [[[protected aminopyridyl](lower)alkenoyl]amino]phenyl, [thiazolylcarbonylamino]phenyl which may have pyridyl, naphthyl having lower alkoxy and halogen, [dihalophenyl](lower)alkenyl, [N-oxidopyridyl](lower)alkenyl, [aminopyridyl](lower)alkenyl, [protected aminopyridyl](lower)alkenyl, [carboxypyridyl](lower)alkenyl, [protected carboxypyridyl](lower)alkenyl, [[pyridyl(lower)alkenyl]pyridyl](lower)alkenyl, [[carboxy(lower)alkenyl]pyridyl](lower)alkenyl, [[protected carboxy(lower)alkenyl]pyridyl](lower)alkenyl, [pyridyl(lower)alkenyl]pyridyl, lower alkylbenzothiazolyl or [halopyridylcarbonyl]amino, aminophenyl, [lower alkanoylamino]phenyl or [dihalophenyl](lower)alkenyl, then
The object compound (I) of the present invention can be prepared by the following processes. ##STR3## wherein [[[halophenyl](lower)alkenoyl]amino]phenyl, [[pyridyl(lower)alkenoyl]amino]phenyl, [[[N-oxidopyridyl](lower)alkenoyl]amino]phenyl, [[[protected aminopyridyl](lower)alkenoyl]amino]phenyl, [thiazolylcarbonylamino]phenyl which may have pyridyl or [acylaminopyridyl](lower)alkenyl, [[[halophenyl](lower)alkenoyl]amino]phenyl, [[pyridyl(lower)alkenoyl]amino]phenyl, [[[N-oxidopyridyl](lower)alkenoyl]amino]phenyl, [[[protected aminopyridyl](lower)alkenoyl]amino]phenyl or [thiazolylcarbonylamino]phenyl which may have pyridyl, pyridyl(lower)alkenoyl, [N-oxidopyridyl](lower)alkenoyl, [protected aminopyridyl](lower)alkenoyl or thiazoylcarbonyl which may have pyridyl,
The starting compound (II) of the present invention can be prepared by the following processes. ##STR4## wherein above, aminopyridyl, carboxypyridyl, protected carboxypyridyl, [pyridyl(lower)alkenyl]pyridyl, [carboxy(lower)alkenyl]pyridyl or [protected carboxy(lower)alkenyl]pyridyl, and
Suitable pharmaceutically acceptable salts of the object compound (I) are conventional non-toxic salts and may include a salt with a base or an acid addition salt such as a salt with an inorganic base, for example, an alkali metal salt (e.g., sodium salt, potassium salt, etc.), an alkaline earth metal salt (e.g.., calcium salt, magnesium salt, etc.), an ammonium salt; a salt with an organic base, for example, an organic amine salt (e.g., triethylamine salt, pyridine salt, picoline salt, ethanolamine salt, triethanolamine salt, dicyclohexylamine salt, N,N'-dibenzylethylenediamine salt, etc.); an inorganic acid addition salt (e.g., hydrochloride, hydrobromide, sulfate, phosphate, etc.); an organic carboxylic or sulfonic acid addition salt (e.g., formate, acetate, trifluoroacetate, maleate, tartrate, fumarate, methanesulfonate, benzenesulfonate, toluenesulfonate, etc.); a salt with a basic or acidic
REFERENCES:
patent: 4296114 (1981-10-01), Appleton et al.
Sawada Akihiko
Shimazaki Norihiko
Watanabe Shinya
Fujisawa Pharmaceutical Co. Ltd.
Shah Mukund J.
Truong Tamithom N.
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