Pyridine and pyridazine derivatives, processes for the productio

Details Pyridine and pyridazine derivatives, processes for the productio Pyridine and pyridazine derivatives, processes for the productio

1997-08-11

1998-07-28

Rotman, Alan L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514252, 544238, 544360, 544364, 546187, 546194, A01N 4340

Patent

active

057863717

DESCRIPTION:

BRIEF SUMMARY
It is known that compounds which carry a basic and an acidic group are capable of inhibiting the aggregation of blood platelets when the basic and the acidic group in the compounds are at a very specific distance from one another (Drugs of the Future 19 (8), 757 (1994). Compounds with an anti-aggregatory action on blood platelets are described in the patent specifications WO 93/14077, EP0537980 A1, EP0542363 A2, WO 94/22834 and WO 94/22835.
The present invention concerns new pyridine and pyridazine derivatives, processes for the production thereof as well as pharmaceutical agents containing these substances.
It was now surprisingly found that pyridine and pyridazine derivatives which additionally carry a carboxylic acid group effectively inhibit the aggregation of blood platelets and can thus be used to treat a wide range of diseases that are due to thromboembolytic events such as stroke, myocardial infarction or arterial occlusive diseases as well as inflammations, osteoporosis or tumour diseases.
The present invention concerns compounds of the general formula I ##STR2## in which R.sup.1 denotes hydrogen, lower alkyl, lower alkenyl, cycloalkyl, cycloalkenyl, an optionally substituted monocyclic or bicyclic aryl, an optionally substituted hetaryl, an optionally substituted arylalkyl or one of the groups ##STR3## W denotes nitrogen or -->CR.sup.5, X,Y,Z independently of one another denote nitrogen or a group -->CH and in the case that W denotes the group -->CR.sup.5 and X denotes the group -->CH, Y cannot be the --CH group tert.-butyloxycarbonyl or benzyloxycarbonyl, or together with the nitrogen atom to which they are bound form a five or six-membered heterocyclic ring,
In all cases lower alkyl should represent a straight-chained or branched C.sub.1 -C.sub.6 alkyl group such as e.g. methyl, ethyl, propyl, isopropyl, butyl, isobutyl, pentyl or hexyl in particular methyl, ethyl, propyl, isobutyl and pentyl.
Lower alkenyl denotes unsaturated residues with 3-6 carbon atoms such as allyl, but-2-enyl, hexa-2,4-dienyl but above all allyl.
Cycloalkyl denotes an optionally substituted 3-7-membered ring such as a cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl ring in particular a cyclopropyl, cyclopentyl and cyclohexyl ring. These cycloalkyl residues can be substituted once or twice by a C.sub.1 -C.sub.6 alkyl group preferably a methyl, ethyl or isopropyl group as well as by hydroxy, methoxy, benzyloxy, amino, methylamino, dimethylamino or benzylamino groups or by chlorine or bromine.
Cycloalkenyl denotes an optionally substituted cyclopentenyl, cyclohexenyl or cycloheptenyl ring. These rings can be substituted once or twice by a C.sub.1 -C.sub.6 alkyl group preferably a methyl, ethyl or isopropyl group as well as by chlorine, bromine or hydroxy, methoxy, benzyloxy, amino, methylamino, dimethylamino or benzylamino groups.
If the residues R.sup.3 and R.sup.4 form a heterocyclic ring together with the nitrogen atom to which they are bound then this is a saturated or unsaturated 5-6-membered ring such as a pyrrolidine, piperidine, morpholine or pyrroline ring.
The carbocyclic and heterocyclic rings can be optionally substituted once or twice by C.sub.1 -C.sub.6 alkyl groups, preferably a methyl, ethyl or isopropyl groups as well as by chlorine, bromine or hydroxy, methoxy, benzyloxy, amino, methylamino, dimethylamino or benzylamino groups.
Aryl usually denotes a phenyl residue which is optionally substituted once or several times.
Hetaryl usually denotes a pyridine, pyridazine, pyrrole, thiophene, furan or imidazole ring which is substituted once or several times.
Bicyclic aryl usually denotes an indane or naphthalene residue which is optionally substituted once or several times, preferably a naphthalene residue.
Aryl, bicyclic aryl and hetaryl residues can be optionally substituted once or several times by C.sub.1 -C.sub.6 alkyl groups, preferably a methyl, ethyl or isopropyl group as well as by chlorine, bromine, fluorine or hydroxy, alkoxy such as e.g. methoxy, benzyloxy, acetyloxy, carb

Affiliated with

Also associated with

Rating

Pyridine and pyridazine derivatives, processes for the productio does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Pyridine and pyridazine derivatives, processes for the productio, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pyridine and pyridazine derivatives, processes for the productio will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-23913