1,2-DI-substituted piperidine derivative, hair growth promoter a

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514326, 514330, 514252, 5142355, 544130, 544160, 546189, 546275, 546278, 546281, 546298, 546301, 546323, 546321N, 546326, C07D21122, A61K 706

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060573376

ABSTRACT:
A 1,2-di-substituted piperidine derivative or a salt thereof expressed by the following Formula (I): ##STR1## wherein one of A and B is a hydrocarbon group of C.sub.1-30 expressed by R.sup.1 and the other is --(CH.sub.2)n-NR.sup.2 R.sup.3 ; Y is --CO--, --CONR.sup.5 -- or --COO--; Z is --O--, --OCO--, --OCONR.sup.6 -- or --NR.sup.6 --; R.sup.2 and R.sup.3 individually represent a hydrogen a lower alkyl, a phenyl or a benzyl group, or together represent a heterocycle having 3-7 members; --NR.sup.5 --(CH.sub.2)n-NR.sup.2 R.sup.3 and --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 of --(Y).sub.1 --A and --Z--B may be the following Group W: ##STR2## wherein ring E is a heterocycle of 6 or 7 members including two nitrogen atoms and R.sup.2 is a hydrogen, a lower alkyl, a phenyl or a benzyl group; R.sup.4 is a hydrogen, a halogen, a lower alkyl, a lower acyl, a nitro, a cyano, a lower alkoxycarbonyl, a carbamoyl, a lower alkylcarbamoyl, a lower alkylamino, a lower acylamino, a lower alkoxy or a lower acyloxy group; each of R.sup.5 and R.sup.6 is a hydrogen, a lower alkyl, a lower acyl, a lower alkylcarbamoyl group, or a part of said ring E; l is 0 or 1; m is an integer of 2-5; and n is an integer of 0-5. The 1,2-di-substituted piperidine derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in human.

REFERENCES:
patent: 3133061 (1964-05-01), Kirchner
patent: 3332949 (1967-07-01), Kirchner
patent: 4873236 (1989-10-01), Engel
Shapiro et al. "Antihypertensive Agents. I. Dialkylaminoalkoxyalkylpiperidines and Pyrrolidines," Journal of the American Chemical Society, vol. 80, 1958, pp. 2743-2745, Jun.
Werbel et al. "N-Momno-and N,N-Dialkyl-N'-1-naphthylalkylenediamines," Journal of Medicinal Chemistry, vol. 6, No. 6, 1963 pp. 637-646, Nov.

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