Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-05-31
1996-09-03
Datlow, Philip I.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540543, 540576, 540587, A61K 3155, C07D22320, C07D49804, C07D49810
Patent
active
055523994
ABSTRACT:
This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. ##STR1## wherein: R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; C.sub.1-6 alkyl substituted with hydroxy, C.sub.1-6 alkyloxy, carboxyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkyloxycarbonyl or aryl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9, R.sup.10, R.sup.11 or R.sup.12 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)-amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxy-carbonyl; R.sup.7 and R.sup.8 are each independently hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or R.sup.7 and R.sup.8 taken together may form mono- or di(cyano)methylene, or together with the carbon atom to which they are attached form a carbonyl or a spiro substituent; or R.sup.7 and R.sup.8 taken together may form methylene; R.sup.13 is hydrogen, C.sub.1-6 alkyl, or trifluoromethyl; R.sup.14 is hydrogen, C.sub.1-6 alkyl, cyano, or trifluoromethyl; n is zero to 6. These compounds were tested as mCPP-antagonists in rats. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.
REFERENCES:
patent: 4039558 (1977-08-01), Van der Burg et al.
Evenson, Moffett. "O-Carbamoyl Oximes as Potential Analgesics," J. Heterocyclic Chem., 17, 351 (1980).
Andr es-Gil Jos e I.
Fern andez-Gadea Francisco J.
Gil-Lopetegui Pilar
Meert Theo F.
Sipido Victor K.
Bottino Anthony
Datlow Philip I.
Janssen Pharmaceutica N.V.
Metz Charles J.
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