Pyrazole derivatives

Details Pyrazole derivatives Pyrazole derivatives

1995-08-21

1997-09-23

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

544183, C07D25172, C07D25310

Patent

active

056705034

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This invention relates to new heterocylic derivatives and pharmaceutically acceptable salts thereof which are useful as a medicament.


DISCLOSURE OF INVENTION

This invention relates to new heterocyclic derivatives. More particularly, this invention relates to pyrazole derivatives and pharmaceutically acceptable salts thereof which have pharmacological activities, processes for preparation thereof, a pharmaceutical composition comprising the same and a use of the same.
Accordingly, one object of this invention is to provide the new and useful pyrazole derivatives and pharmaceutically acceptable salts thereof which possess a strong inhibitory activity on the production of Interleukin-1 (IL-1) 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 pyrazole derivatives and salts thereof.
A further object of this invention is to provide a pharmaceutical composition comprising said pyrazole derivatives or a pharmaceutically acceptable salt thereof.
Still further object of this invention is to provide a use of said pyrazole derivatives or a pharmaceutically acceptable salt thereof as a medicament for prophylactic and therapeutic treatment of IL-1 and TNF mediated diseases such as chronic inflammatory diseases, specific autoimmune diseases, sepsis-induced organ injury, and the like in human being and animals.
The object pyrazole derivatives of the present invention are novel and can be represented by the following general formula (I): ##STR3## wherein R.sup.1 is aryl which may have suitable substituent(s) or heterocyclic group which may have suitable substituent(s), group which may have suitable substituent(s), cyclo(lower)alkyl-(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl, ar(lower)alkyl which may have suitable substituent(s), ar(lower)alkenyl, bridged tricyclicalkyl, heterocyclic group which may have suitable substituent(s), acyl, or a group of the formula: ##STR4## (in which A is lower alkylene), and R.sup.5 is hydrogen or lower alkyl.
The object compound (I) of the present invention can be prepared by the following processes. ##STR5## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.5 are each as defined above, cyclo(lower)alkyl-(C.sub.1 -C.sub.5)alkyl, aryl which may have suitable substituent(s) or ar(C.sub.1 -C.sub.5)alkyl which may have suitable substituent(s), ##STR6## is lower alkyl, cyclo(lower)alkyl, cyclo(lower)alkyl-(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower alkyl, ar (lower)alkyl which may have suitable substituent(s), ar (lower)alkenyl, bridged tricyclicalkyl, heterocyclic group which may have suitable substituent(s), ##STR7## (in which A is lower alkylene), X.sup.1.crclbar. is anion, and ##STR8## is N-containing heterocyclic group.
The starting compounds or salts thereof can be prepared by the following Processes. ##STR9## are each as defined above, R.sup.9 and X.sup.3 are each a leaving group,
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; triethylamine salt, pyridine salt, picoline salt, ethanolamine salt, triethanolamine salt, dicyclohexylamine salt, N,N'-dibenzylethylenediamine salt, etc.); sulfate, phosphate, etc.); acetate, trifluoroacetate, maleate, tartrate, fumarate, methanesulfonate, benzenesulfonate, toluenesulfonate, etc.); glutamic acid, etc.).
In the above and subsequent descriptions of the present specification, suitable examples and illustration of the various definitions which the present invention intends to include within the scope thereof are explained in detail as follows.
The term "lower" is used to intend a group having 1 to 6 carbon atom(s), unless otherwise provided.
The term "higher" is used to intend

REFERENCES:
patent: 5356897 (1994-10-01), Oku et al.
Ruddle et al; J. Exp. Med.; Oct. 1990; 172, 1193-1200.

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