Claims
- 1. An arylglycinamide derivative of the formula I ##STR73## or the pharmaceutically acceptable salts thereof, wherein Ar denotes unsubstituted or mono- to penta-substituted phenyl, or unsubstituted or mono- or di-substituted naphthyl, in which the substituents of the phenyl and naphthyl independently of each other denote halogen (F, Cl, Br, I), (C.sub.1-4)alkyl, O-(C.sub.1-4)alkyl, CF.sub.3, OCF.sub.3 or NR.sup.9 R.sup.10 (wherein R.sup.9 and R.sup.10 independently of each other denote H, methyl or acetyl);
- R.sup.1 and R.sup.2 together with the N to which they are bound form a 6-membered ring of the formula ##STR74## wherein X denotes N(CH.sub.2).sub.n R.sup.6 ;
- N is 0, 1 or 2,
- R.sup.6 is (C.sub.3-7)cycloalkyl, phenyl or naphthyl, wherein the phenyl may be mono- to tri-substituted by halogen (F, Cl, Br, I), (C.sub.1-4)alkyl, O-(C.sub.1-4)alkyl, CF.sub.3, OCF.sub.3 or NR.sup.9 R.sup.10 (wherein R.sup.9 and R.sup.10 independently of each other denote H, methyl or acetyl);
- R.sup.3 denotes H, (C.sub.1-4)alkyl, unsubstituted or mono- to tri-substituted phenyl, wherein the substituents independently of one another represent halogen (F, Cl, Br, I), (C.sub.1-4)alkyl, O-(C.sub.1-4)alkyl, CF.sub.3, OCF.sub.3 or NR.sup.9 R.sup.10 (wherein R.sup.9 and R.sup.10 independently of one another denote H, methyl or acetyl);
- R.sup.4 denotes (CH.sub.2).sub.m phenyl or (CH.sub.2).sub.m naphthyl, wherein m is 1, 2 or 3 and phenyl may be substituted by 1 to 3 substituents, wherein the substituents independently of one another are halogen (F, Cl, Br, I), (C.sub.1-4)alkyl, O-(C.sub.1-4)alkyl, CF.sub.3, OCF.sub.3 or NR.sup.9 R.sup.10 (wherein R.sup.9 and R.sup.10 independently of one another denote H, methyl or acetyl);
- R.sup.5 denotes H, (C.sub.1-4)alkyl, (C.sub.3-6)cycloalkyl or CH.sub.2 COOH.
- 2. A compound according to claim 1, wherein n is 0, 1 or 2 and R.sup.6 is (C.sub.3-6)cycloalkyl.
- 3. A compound according to claim 1, wherein R.sup.3 is H or methyl.
- 4. A compound according to claim 1, wherein R.sup.4 is (CH.sub.2).sub.m phenyl, wherein m is 1, 2 or 3 and phenyl is unsubstituted or up to tri-substituted.
- 5. A compound according to claim 4, wherein R.sup.4 is (CH.sub.2).sub.1-2 phenyl, wherein the phenyl is substituted by 2 CF.sub.3 groups.
- 6. A compound according to claim 1, wherein R.sup.5 denotes H or (C.sub.1-4)alkyl.
- 7. A compounds according to claim 1, wherein Ar denotes phenyl having 0, 1, 2 or 3 substituents.
- 8. A pharmaceutical preparation comprising a compound according to claim 1.
- 9. A method for treating a neurokinin-mediated disease which comprises administering to a host suffering from such condition a therapeutically effective amount of a compound according to claim 1.
- 10. A process for preparing the compounds of formula I according to claim 1, comprising the step of reacting an acid of formula ##STR75## or the halide or alkylester thereof, with an amine of formula ##STR76##
Priority Claims (2)
Number |
Date |
Country |
Kind |
195 14 112.1 |
Apr 1995 |
DEX |
|
195 19 245.1 |
May 1995 |
DEX |
|
Parent Case Info
This is a continuation of application Ser. No. 08/473,470, filed Jun. 7, 1995 now abandoned.
US Referenced Citations (4)
Foreign Referenced Citations (5)
Number |
Date |
Country |
WO9401402 |
Jul 1993 |
WOX |
WO9410146 |
Nov 1993 |
WOX |
9408983 |
Apr 1994 |
WOX |
WO9526335 |
Mar 1995 |
WOX |
WO9608480 |
Sep 1995 |
WOX |
Non-Patent Literature Citations (3)
Entry |
Chemical Abstracts, vol. 68, No. 3, p. No. 5717, Abstract No. 59230g (1968). |
Chemical Abstracts, vol. 11, No. 13, p. No. 7, Abstract No. 54228t (1972). |
K. Nagarajan et al., "A Novel Displacement Reaction on a .alpha.-Chlorodiphenylacetamides", Tetrahedron Letters, 15, pp. 1387-1390)1967. |
Continuations (1)
|
Number |
Date |
Country |
Parent |
473470 |
Jun 1995 |
|