Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-04-08
1999-10-05
Clardy, S. Mark
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
548146, 548214, 548452, 548469, 546 17, 5462681, 540467, 540480, 540200, 540484, 530333, 530337, 530342, C07D22120, C07D40106, C07D20910, A61K 31435
Patent
active
059625023
DESCRIPTION:
BRIEF SUMMARY
The subject of the present invention is new derivatives of glutamic acid and of aspartic acid which can be represented by the general formula (I) indicated below: ##STR2## and in which s is 1 or 2, substituents are selected from chloro, fluoro, bromo, trifluoromethyl, linear or branched C.sub.1 -C.sub.4 alkyl, nitro, cyano, and methoxy groups, the 2-naphthyl group, the 2- (or 3-) indolyl group, and the 2- (or 3-) quinolinyl group, ##STR3## in which m and n are selected independently and may assume values of between 1 and 3 provided that the ring formed consists of at least 5 atoms, X and Y are selected independently from (CH--R.sub.3)z, TCH.sub.2 and CH.sub.2 T, where T is 0 (oxygen), or S and in which R.sub.3 is a group selected independently from H, CH.sub.3, and C.sub.2 H.sub.5 and z may assume values of from 0 to 3, provided that the ring formed consists of at least 3 atoms; ##STR4## where z and R.sub.3 have the meanings given above whilst Ad is adamantyl (1- or 2-yl). ##STR5## in which R.sub.4 is a linear or branched alkyl chain containing from 4 to 10 carbon atoms, or a C.sub.5 -C.sub.10 cycloalkyl group, or a linear or branched alkoxyalkyl group containing from 4 to 7 carbon atoms, and R.sub.5 is selected independently from H, an alkyl group, a linear or branched alkoxyalkyl group containing from 1 to 7 carbon atoms, or a C.sub.5 -C.sub.10 cycloalkyl group; ##STR6## in which m, n, X, Y and R.sub.3 have the meanings given above, R.sub.3a, R.sub.3b, and R.sub.3d are H or CH.sub.3, R.sub.3c, and R.sub.3e are 0 (zero), H or CH.sub.3, r.sub.1, raw and r.sub.3 may independently assume whole values of between 0 and 2, containing from 1 to 6 carbon atoms, OH, OCH.sub.3, SH, the benzyloxyl group, the thiomethyl group (CH.sub.3 --S--), or a group selected independently from a cycloalkane group, a heterocyclic group, a mono- or dicyclic aromatic or hydro-aromatic group having up to 10 carbon atoms, unsubstituted or substituted with substituents selected from fluoro, chloro, methyl, ethyl, trifluoromethyl, methoxy, cyano and nitro groups; from: ##STR7## in which R.sub.7 is selected from H and a linear or branched C.sub.1 -C.sub.5 alkyl or alkoxyalkyl group and R.sub.8 is selected from H, a C.sub.1 -C.sub.5 alkyl group and a (CH.sub.2).sub.z -Ar group, where z has the meaning given above and Ar is a phenyl group unsubstituted or mono- or di-substituted with substituents selected from fluoro, chloro, methyl, ethyl, trifluoromethyl and methoxy groups or the 1 (or 2)-naphthyl group; ##STR8## in which z, R.sub.3 and R.sub.7 are selected independently and have the meanings given above, z.sub.1 and z.sub.2 are selected independently and may assume values of between 1 and 4, provided that the ring formed includes between 4 and 10 carbon atoms; ##STR9## in which R.sub.3, R.sub.7, s, z.sub.1 and z.sub.2 have the meanings given above; ##STR10## in which R.sub.3, R.sub.7, S, z.sub.1 and z.sub.2 have the meanings given above; ##STR11## in which R.sub.3, R.sub.7, S, z, z.sub.1 and z.sub.2 have the meanings given above; ##STR12## in which R.sub.3, z.sub.1 and z.sub.2 have the meanings given above; 7) an azadicyclic (orthofused) group, represented by: ##STR13## in which R.sub.3, s, z.sub.1 and z.sub.2 have the meanings given above; 8) a dicyclic azaspiro group represented by: ##STR14## in which R.sub.3, s, z.sub.1 and z.sub.2 have the meanings given above; 9) an azadicyclic group represented by: ##STR15## in which R.sub.3, s, z.sub.1 and z.sub.2 have the meanings given above; 10) an azacycloalkyl group represented by: ##STR16## in which R.sub.3, z.sub.1, z.sub.2 and T have the meanings given above; 11) an aminoalkyl adamantyl group represented by: ##STR17## in which R.sub.3 and z have the meanings given above and Ad is adamantyl (1- or 2-yl).
Some of the compounds according to the invention may be represented better by the general formula (II) indicated below: ##STR18## in which: R.sub.1, R.sub.2, R.sub.3a, R.sub.3b, R.sub.3c, R.sub.3e, s, r.sub.1 and r.sub.2 have the meanings given above, and B is selected independently from
REFERENCES:
Internationakl Search Report PCT/EP (94/02983) Jan. 16, 1995.
J. Med. Chem. 1992, 35, 28-38.
Chemical & Pharmacuetical Bulletin, vol. 36, No. 10, 1988 pp. 3961-3966.
Chemical & Pharmaceutical Bulletin, vol. 36, No. 9, 1988 pp. 3433-3438.
Makovec Francesco
Peris Walter
Rovati Lucio C.
Rovati Luigi A.
Clardy S. Mark
Qazl Sabiha N.
Rotta Research Laboratorium S.p.A.
LandOfFree
Polyamidic acid derivatives with antigastrin activity, a method does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Polyamidic acid derivatives with antigastrin activity, a method , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Polyamidic acid derivatives with antigastrin activity, a method will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1172028