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US 5,399,570 AGranted
Aspartic acid derivatives, and their use for inhibiting platelete aggregation
AssigneeCassella Aktiengesellschaft
InventorsOtmar Klingler, Gerhard Zoller, Melitta Just, Bernd Jablonka
Life of this patent
Estimating the term…
Abstract
Aspartic acid derivatives of the formula ##STR1## in which X denotes, for example, ##STR2## and R denotes, for example, cyclohexylamino, have useful pharmacological properties.
Claims10
Aspartic acid derivatives of the general formula I ##STR19## in which X denotes ##STR20## A denotes --(CH.sub.2).sub.m --, --O-- or a direct bond, k=2 or 3
- m denotes a number from 0 to 4
- R denotes ##STR21## R.sup.1 denotes hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, phenyl, where the C.sub.1 -C.sub.6 alkyl, the C.sub.3 -C.sub.8 cycloalkyl or the phenyl is unsubstituted or mono- or di-substituted by identical or different radicals selected from the group consisting or hydroxyl, carboxyl, C.sub.1 -C.sub.4 alkoxycarbonyl, phenylmethoxycarbonyl, carboxamido, C.sub.1 -C.sub.4 alkylaminocarbonyl, amine, mercapto, C.sub.1 -C.sub.4 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, imidazolyl, indolyl, pyrrolidinyl, hydroxypyrrolidinyl, halogen, phenyl or phenoxy, each of which is unsubstituted or monosubstituted or di-substituted by hydroxyl, C.sub.1 -C.sub.4 alkyl, halogen, nitro or trifluoromethyl;
- R.sup.2 and R.sup.3 independently of one another denote hydrogen or R.sup.1 ;
- R.sup.4 denotes the radical of an amine acid selected from the group consisting of Aad, Abu, .beta.Abu, ABz, 2ABz, .epsilon.Aca, Ach, Acp, Adpd, Ahb, Aib, .beta.Aib, Ala, .beta.Ala, .DELTA.Ala, Alg, All, Ama, Amt, Ape, Apm, Apr, Arg, Asn, Asp, Asa, Aze, Azi, Bai, Bph, Can, Cit, Cys, (Cys).sub.2, Cyta, Daad, Dab, Dadd, Dap, Dapm, Dasu, Dien, Dpa, Dtc, Fel, Gln, Glu, Gly, Guy, hAla, hArg, hCys, hGln, hGlu, IIis, hIle, hLeu, hLys, hMet, hPhe, hPro, hScr, hThr, hTrp, hTyr, Hyl, Hyp, 3Hyp, Ile, Ise, Iva, KVn, Lant, Lcn, Leu, Lsg, Lys, .beta.Lys, .DELTA.Lys, Met, Mim, Min, nArg, Nle, Nva, Oly, Orn, Pan, Pec, Pen, Phe, Phg, Pic, Pro, .DELTA.Pro, Pse, Pys, Pyr, Pza, Oin, Ros, Sar, Sec, Sem, Ser, Thi, .beta.Thi, Thr, Thy, Thx, Tia, Tle, Tly, Trp, Trta, Tyr, Val, Tbg, Npg, Chg, Cha, Thia, 2,2-diphenylaminoacetic acid, 2- (tolyl)-2-phenylaminoacetic acid, 2-(p-chlorophenyl) aminoacetic acid, or of a dipeptide thereof, in which the peptide bond can also be reduced to --NH--CH.sub.2 --, and their physiologically tolerable salts.
1 more element
p (4-N-Amidinopiperidinyloxy)benzoyl-L-aspartyl-L-valine.
Dependencies are inferred from the claim text.