Back to results
US 4,971,957 AGranted
Carboxamide compounds, processes for preparing the same and a pharmaceutical composition containing the same
AssigneeOtsuka Pharmaceutical Factory, Inc.
InventorsKazuhiko Tsutsumi, Eiji Uesaka, Kayoko Shinomiya, Yoshihiko Tsuda, Yauso Shoji, Atsushi Shima
Life of this patent
Estimating the term…
Abstract
Novel carboxamide compounds represented by the general formula (I) possess excellent activities for lowering lipids and thus they are useful as agents for treating and preventing various diseases (hyperlipidemia) such as hypercholesterolemia, hypertriglyceridemia, hyperphospholipidemia, hyperlipacidemia, and the like.
Claims5
A carboxamide compound represented by the general formula (I), ##STR66## wherein R.sup.1 and R.sup.2 are each:
- a hydrogen atom;
- a lower alkyl group;
- a phenyl group which may have 1 to 3 substituents selected from the group consisting of a halogen atom, a carbamoyl group, an N-(lower alkyl)carbamoyl group, an N-(cycloalkyl)carbamoyl group, an N-(phenyl)carbamoyl group which may have halogen atoms, lower alkoxy groups or lower alkyl groups as substituents on the phenyl ring, an N-(phenyl-lower alkyl)carbamoyl group, a lower akanoyl group, a benzoyl group, an N,N-di(lower alkyl)amino group, a phenylthio group, a lower alkylthio group, a lower alkylsulfinyl group, a phenylsulfinyl group, a 4-phenylpiperazinylcarbonyl group, a 4-(phenyl-lower alkyl)piperazinylcarbonyl group, a piperidinylcarbonyl group and a sulfamoyl group;
- a lower alkoxycarbonyl-lower alkyl group;
- a pyridyl group which may have 1 to 3 substituents selected from the group consisting of a halogen atom, a lower alkoxy group and a lower alkoxycarbonyl group;
- an N-phenylamino group;
- a naphthyl group which may have halogen atoms as substituents;
- a pyrimidinyl group;
- an isoxazolyl group which may have lower alkyl groups as substituents;
- or
- an N-phthalazinylamino group;
- further, R.sup.1 and R.sup.2 together with the adjacent nitrogen atom bonded thereto form a heterocyclic group consisting of an indolin-1-yl group, a 1,2,3,4-tetrahydroquinolin-1-yl group which may have halogen atoms as substituents, 1,2,3,4-tetrahydroisoquinolin-2-yl group, a 2,3-dihydro-4H-1,4-benzoxazin-4-yl group which may have a phenyl group at the 2- or 3-position in the benzoxazine ring, and a phenothiazin-10-yl group which may have halogen atoms as substituents in the benzene ring;
- provided that, R.sup.1 and R.sup.2 are not hydrogen atoms at the same time;
- and when any one of R.sup.1 and R.sup.2 is a lower alkyl group, then the other is a phenyl group having a halogen atom and a benzoyl group as substituents;
- or when any one of R.sup.1 and R.sup.2 is a phenyl group having a halogen atom as a substituent, then the other is a lower alkoxycarbonyl-lower alkyl group;
- further, when any one of R.sup.1 and R.sup.2 is a phenyl group, then the other is an N-phenylamino group;
- R.sup.3 is a lower alkyl group;
- and
- X is an oxygen atom or a sulfur atom.
16 more elements
Dependencies are inferred from the claim text.