Anti-tumour agentsThe invention concerns anti-tumour agents of formula (I) wherein each of R, R and R has the meanings defined in the specification including hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, amino, (1-4C)alkylamino and (1-4C)alkoxy; each of R and R is (1-4C)alkyl; each of R and R is hydrogen or (1-4C)alkyl; X is oxygen; m is 1 or 2 and each R is as defined in the specification; each of Y and Y is halogeno, (1-4C)alkanesulphonyloxy, benzenesulphonyloxy or phenyl-(1-4C)alkanesulphonyloxy; or a pharmaceutically-acceptable salt thereof; provided that at least one of R, R and R is other than hydrogen; a process for their preparation, pharmaceutical compositions containing them and their use in the production of an anti-proliferative effect.The antineoplastic agent shown in the formula i or its pharmaceutically acceptable salt: wherein: r 1be hydrogen, (1-4c) alkyl, (3-4c) alkenyl, (3-4c) alkynyl, the alkyl of hydroxyl-(1-4c), (1-4c) alkyl of alkoxyl group-(1-4c), amino-(1-4c) alkyl, (1-4c) alkyl of alkylamino-(1-4c), two-((1-4c) alkyl) amino-(1-4c) alkyl, tetramethyleneimine-1-base (1-4c) alkyl, the alkyl of piperidino-(1-position only)-(1-4c), the alkyl of morpholino-(1-4c), the alkyl of piperazine-1-base-(1-4c), the alkyl of 4-(1-4c) alkylpiperazine-1-base-(1-4c), the alkyl of carboxyl-(1-4c), (1-4c) alkyl of carbalkoxy-(1-4c), the alkyl of formamyl-(1-4c), the alkyl of n-(1-4c) alkyl-carbamoyl-(1-4c), n, the alkyl of n-two-((1-4c) alkyl) formamyl-(1-4c), amino, (1-4c) alkylamino, (3-4c) chain enamino, (3-4c) alkynes amino, two-((1-4c) alkyl) amino, two-((3-4c) alkenyl) amino, two-((3-4c) alkynyl) amino, tetramethyleneimine-1-base, piperidino-(1-position only), morpholino, piperazine-1-base, 4-(1-4c) alkylpiperazine-1-base, the alkylamino of hydroxyl-(2-4c), (1-4c) alkylamino of alkoxyl group-(2-4c), amino-(2-4c) alkylamino, (1-4c) alkylamino of alkylamino-(2-4c), two-((1-4c) alkyl) amino-(2-4c) alkylamino, the alkylamino of tetramethyleneimine-1-base-(2-4c), the alkylamino of piperidino-(1-position only)-(2-4c), the alkylamino of morpholino-(2-4c), the alkylamino of piperazine-1-base-(2-4c), the alkylamino of 4-(1-4c) alkylpiperazine-1-base-(2-4c), (2-4c) alkanoyl amido, (2-4c) alkylamino of alkanoyl amido-(2-4c), the alkylamino of carboxyl-(1-4c), (1-4c) alkylamino of carbalkoxy-(1-4c), the alkylamino of formamyl-(1-4c), the alkylamino of n-(1-4c) alkyl-carbamoyl-(1-4c), n, the alkylamino of n-two-((1-4c) alkyl) formamyl-(1-4c), hydroxyl, (1-4c) alkoxyl group, the alkoxyl group of hydroxyl-(2-4c), (1-4c) alkoxyl group of alkoxyl group-(2-4c), amino (2-4c) alkoxyl group, (1-4c) alkoxyl group of alkylamino-(2-4c), two-((1-4c) alkyl) amino-(2-4c) alkoxyl group, the alkoxyl group of tetramethyleneimine-1-base-(2-4c), the alkoxyl group of piperidino-(1-position only)-(2-4c), the alkoxyl group of morpholino-(2-4c), the alkoxyl group of the alkoxyl group of piperazine-1-base-(2-4c) or 4-(1-4c) alkylpiperazine-1-base-(2-4c); r 2be hydrogen, (1-4c) alkyl, (3-4c) alkenyl, (3-4c) alkynyl, the alkyl of hydroxyl-(1-4c), (1-4c) alkyl of alkoxyl group-(1-4c), amino-(1-4c) alkyl, (1-4c) alkyl of alkylamino-(1-4c), two-((1-4c) alkyl) amino-(1-4c) alkyl, tetramethyleneimine-1-base (1-4c) alkyl, the alkyl of piperidino-(1-position only)-(1-4c), the alkyl of morpholino-(1-4c), the alkyl of piperazine-1-base-(1-4c), the alkyl of 4-(1-4c) alkylpiperazine-1-base-(1-4c), the alkyl of carboxyl-(1-4c), (1-4c) alkyl of carbalkoxy-(1-4c), the alkyl of formamyl-(1-4c), the alkyl of n-(1-4c) alkyl-carbamoyl-(1-4c), n, the alkyl of n-two-((1-4c) alkyl) formamyl-(1-4c), amino, (1-4c) alkylamino, (3-4c) chain enamino, (3-4c) alkynes amino, two-((1-4c) alkyl) amino, two-((3-4c) alkenyl) amino, two-((3-4c) alkynyl) amino, tetramethyleneimine-1-base, piperidino-(1-position only), morpholino, piperazine-1-base, 4-(1-4c) alkylpiperazine-1-base, the alkylamino of hydroxyl-(2-4c), (1-4c) alkylamino of alkoxyl group-(2-4c), amino-(2-4c) alkylamino, (1-4c) alkylamino of alkylamino-(2-4c), two-((1-4c) alkyl) amino-(2-4c) alkylamino, the alkylamino of tetramethyleneimine-1-base-(2-4c), the alkylamino of piperidino-(1-position only)-(2-4c), the alkylamino of morpholino-(2-4c), the alkylamino of piperazine-1-base-(2-4c), the alkylamino of 4-(1-4c) alkylpiperazine-1-base-(2-4c), (2-4c) alkanoyl amido, (2-4c) alkylamino of alkanoyl amido-(2-4c), the alkylamino of carboxyl-(1-4c), (1-4c) alkylamino of carbalkoxy-(1-4c), the alkylamino of formamyl-(1-4c), the alkylamino of n-(1-4c) alkyl-carbamoyl-(1-4c), n, the alkylamino of n-two-((1-4c) alkyl) formamyl-(1-4c), hydroxyl, (1-4c) alkoxyl group, the alkoxyl group of hydroxyl-(2-4c), (1-4c) alkoxyl group of alkoxyl group-(2-4c), amino (2-4c) alkoxyl group, (1-4c) alkoxyl group of alkylamino-(2-4c), two-((1-4c) alkyl) amino-(2-4c) alkoxyl group, the alkoxyl group of tetramethyleneimine-1-base-(2-4c), the alkoxyl group of piperidino-(1-position only)-(2-4c), the alkoxyl group of morpholino-(2-4c), the alkoxyl group of the alkoxyl group of piperazine-1-base-(2-4c) or 4-(1-4c) alkylpiperazine-1-base-(2-4c); r 3be hydrogen, (1-4c) alkyl, (3-4c) alkenyl, (3-4c) alkynyl, the alkyl of hydroxyl-(1-4c), (1-4c) alkyl of alkoxyl group-(1-4c), amino-(1-4c) alkyl, (1-4c) alkyl of alkylamino-(1-4c), two-((1-4c) alkyl) amino-(1-4c) alkyl, tetramethyleneimine-1-base (1-4c) alkyl, the alkyl of piperidino-(1-position only)-(1-4c), the alkyl of morpholino-(1-4c), the alkyl of piperazine-1-base-(1-4c), the alkyl of 4-(1-4c) alkylpiperazine-1-base-(1-4c), the alkyl of carboxyl-(1-4c), (1-4c) alkyl of carbalkoxy-(1-4c), the alkyl of formamyl-(1-4c), the alkyl of n-(1-4c) alkyl-carbamoyl-(1-4c), n, the alkyl of n-two-((1-4c) alkyl) formamyl-(1-4c), amino, (1-4...
항종양제본 발명은 하기 화학식 I의 항종양제 또는 이것의 약학적으로 허용 가능한 염, 이들을 제조하는 방법, 이들을 함유하는 약학 조성물 및 항증식 효과의 발생에 이들을 사용하는 방법에 관한 것이다. 화학식 I상기 식 중, R1, R2 및 R3은 각각 수소, (C1∼C4)알킬, (C3∼C4)알케닐, (C3∼C4)알키닐, 아미노, (C1∼C4)알킬아미노 및 (C1∼C4)알콕시를 비롯한 명세서에 정의된 의미를 가지고, R4 및 R5는 각각 (C1∼C4)알킬이며, R6 및 R7은 각각 수소 또는 (C1∼C4)알킬이고, X는 산소이며, m은 1 또는 2이고, R8은 각각 명세서에 정의된 바와 같으며, Y1 및 Y2는 각각 할로게노, (C1∼C4)알칸설포닐옥시, 벤젠설포닐옥시 또는 페닐-(C1∼C4)알칸설포닐옥시이고, 단 R1, R2 및 R3 중 하나 이상은 수소 이외의 것이다. 하기 화학식 I의 항종양제 또는 이것의 약학적으로 허용 가능한 염: 화학식 I [이미지] 상기 식 중, R1은 수소, (C1∼C4)알킬, (C3∼C4)알케닐, (C3∼C4)알키닐, 히드록시-(C1∼C4)알킬, (C1∼C4)알콕시-(C1∼C4)알킬, 아미노-(C1∼C4)알킬, (C1∼C4)알킬아미노- (C1∼C4)알킬, 디-[(C1∼C4)알킬]아미노-(C1∼C4)알킬, 피롤리딘-1-일-(C1∼C4)알킬, 피페리디노-(C1∼C4)알킬, 모르폴리노-(C1∼C4)알킬, 피페라진-1-일-(C1∼C4)알킬, 4-(C1∼C4)알킬피페라진-1-일-(C1∼C4)알킬, 카르복시-(C1∼C4)알킬, (C1∼C4)알콕시카르보닐-(C1∼C4)알킬, 카르바모일-(C1∼C4)알킬, N-(C1∼C4)알킬카르바모일- (C1∼C4)알킬, N,N-디-[(C1∼C4)알킬]카르바모일-(C1∼C4)알킬, 아미노, (C1∼C4)알킬아미노, (C3∼C4)알케닐아미노, (C3∼C4)알키닐아미노, 디-[(C1∼C4)알킬]아미노, 디-[(C3∼C4)]알케닐]아미노, 디-[(C3∼C4)알키닐]아미노, 피롤리딘-1-일, 피페리디노, 모르폴리노, 피페라진-1-일, 4-(C1∼C4)알킬피페라진-1-일, 히드록시-(C2∼C4)알킬아미노, (C1∼C4)알콕시-(C2∼C4)알킬아미노, 아미노-(C2∼C4)알킬아미노, (C1∼C4)알킬아미노-(C2∼C4)알킬아미노, 디-[(C1∼C4)알킬]아미노-(C2∼C4)알킬아미노, 피롤리딘-1-일-(C2∼C4)알킬아미노, 피페리디노-(C2∼C4)알킬아미노, 모르폴리노- (C2∼C4)알킬아미노, 피페라진-1-일-(C2∼C4)알킬아미노, 4-(C1∼C4)알킬피페라진-1-일-(C2∼C4)알킬아미노, (C2∼C4)알카노일아미노, (C2∼C4)알카노일아미노-(C2∼C4)알킬아미노, 카르복시-(C1∼C4)알킬아미노, (C1∼C4)알콕시카르보닐-(C1∼C4)알킬아미노, 카르바모일-(C1∼C4)알킬아미노, N-(C1∼C4)알킬카르바모일-(C1∼C4)알킬아미노, N,N-디-[(C1∼C4)알킬]카르바모일-(C1∼C4)알킬아미노, 히드록시, (C1∼C4)알콕시, 히드록시-(C2∼C4)알콕시, (C1∼C4)알콕시-(C2∼C4)알콕시, 아미노-(C2∼C4)알콕시, (C1∼C4)알킬아미노-(C2∼C4)알콕시, 디-[(C1∼C4)알킬]아미노-(C2∼C4)알콕시, 피롤리딘 -1-일-(C2∼C4)알콕시, 피페리디노-(C2∼C4)알콕시, 모르폴리노-(C2∼C4)알콕시, 피페라진-1-일-(C2∼C4)알콕시 또는 4-(C1∼C4)알킬피페라진-1-일-(C2∼C4)알콕시이고, R2는 수소, (C1∼C4)알킬, (C3∼C4)알케닐, (C3∼C4)알키닐, 히드록시-(C1∼C4)알킬, (C1∼C4)알콕시-(C1∼C4)알킬, 아미노-(C1∼C4)알킬, (C1∼C4)알킬아미노- (C1∼C4)알킬, 디-[(C1∼C4)알킬]아미노-(C1∼C4)알킬, 피롤리딘-1-일-(C1∼C4)알킬, 피페리디노-(C1∼C4)알킬, 모르폴리노-(C1∼C4)알킬, 피페라진-1-일-(C1∼C4)알킬, 4-(C1∼C4)알킬피페라진-1-일-(C1∼C4)알킬, 카르복시-(C1∼C4)알킬, (C1∼C4)알콕시카르보닐-(C1∼C4)알킬, 카르바모일-(C1∼C4)알킬, N-(C1∼C4)알킬카르바모일- (C1∼C4)알킬, N,N-디-[(C1∼C4)알킬]카르바모일-(C1∼C4)알킬, 아미노, (C1∼C4)알킬아미노, (C3∼C4)알케닐아미노, (C3∼C4)알키닐아미노, 디-[(C1∼C4)알킬]아미노, 디-[(C3∼C4)알케닐]아미노, 디-[(C3∼C4)알키닐]아미노, 피롤리딘-1-일, 피페리디노, 모르폴리노, 피페라진-1-일, 4-(C1∼C4)알킬피페라진-1-일, 히드록시-(C2∼C4)알킬아미노, (C1∼C4)알콕시-(C2∼C4)알킬아미노, 아미노-(C2∼C4)알킬아미노, (C1∼C4)알킬아미노-(C2∼C4)알킬아미노, 디-[(C1∼C4)알킬]아미노-(C2∼C4)알킬아미노, 피롤리딘-1-일-(C2∼C4)알킬아미노, 피페리디노-(C2∼C4)알킬아미노, 모르폴리노- (C2∼C4)알킬아미노, 피페라진-1-일-(C2∼C4)알킬아미노, 4-(C1∼C4)알킬피페라진-1-일-(C2∼C4)알킬아미노, (C2∼C4)알카노일아미노, (C2∼C4)알카노일아미노-(C2∼C4)알킬아미노, 카르복시-(C1∼C4)알킬아미노, (C1∼C4)알콕시카르보닐-(C1∼C4)알킬아미노, 카르바모일-(C1∼C4)알킬아미노, N-(C1∼C4)알킬카르바모일-(C1∼C4)알킬아미노, N,N-디-[(C1∼C4)알킬]카르바모일-(C1∼C4)알킬아미노, 히드록시, (C1∼C4)알콕시, 히드록시-(C2∼C4)알콕시, (C1∼C4)알콕시-(C2∼C4)알콕시, 아미노-(C2∼C4)알콕시, (C1∼C4)알킬아미노-(C2∼C4)알콕시, 디-[(C1∼C4)알킬]아미노-(C2∼C4)알콕시, 피롤리딘 -1-일-(C2∼C4)알콕시, 피페리디노-(C2∼C4)알콕시, 모르폴리노-(C2∼C4)알콕시, 피페라진-1-일-(C2∼C4)알콕시 또는 4-(C1∼C4)알킬피페라진-1-일-(C2∼C4)알콕시이며, R3은 수소, (C1∼C4)알킬, (C3∼C4)알케닐, (C3∼C4)알키닐, 히드록시-(C1∼C4)알킬, (C1∼C4)알콕시-(C1∼C4)알킬, 아미노-(C1∼C4)알킬, (C1∼C4)알킬아미노- (C1∼C4)알킬, 디-[(C1∼C4)알킬]아미노-(C1∼C4)알킬, 피롤리딘-1-일-(C1∼C4)알킬, 피페리디노-(C1∼C4)알킬, 모르폴리노-(C1∼C4)알킬, 피페라진-1-일-(C1∼C4)알킬, 4-(C1∼C4)알킬피페라진-1-일-(C1∼C4)알킬, 카르복시-(C1∼C4)알킬, (C1∼C4)알콕시카르보닐-(C1∼C4)알킬, 카르바모일-(C1∼C4)알킬, N-(C1∼C4)알킬카르바모일- (C1∼C4)알킬, N,N-디-[(C1∼C4)알킬]카르바모일-(C1∼C4)알킬, 아미노, (C1∼C4)알킬아미노, (C3∼C4)알케닐아미노, (C3∼C4)알키닐아미노, 디-[(C1∼C4)알킬]아미노, 디-[(C3∼C4)알케닐]아미노, 디-[(C3∼C4)알키닐]아미노, 피롤리딘-1-일, 피페리디노, 모르폴리노, 피페라진-1-일, 4-(C1∼C4)알킬피페라진-1-일, 히드록시-(C2∼C4)알킬아미노, (C1∼C4)알콕시-(C2∼C4)알킬아미노, 아미노-(C2∼C4)알킬아미노, (C1∼C4)알킬아미노-(C2∼C4)알킬아미노, 디-[(C1∼C4)알킬]아미노-(C2∼C4)알킬아미노, 피롤리딘-1-일-(C2∼C4)알킬아미노, 피페리디노-(C2∼C4)알킬아미노, 모르폴리노 -(C2∼C4)알킬아미노, 피페라진-1-일-(C2∼C4)알킬아미노, 4-(C1∼C4)알킬피페라진-1-일-(C2∼C4)알킬아미노, (C2∼C4)알카노일아미노, (C2∼C4)알카노일아미노-(C2∼C4)알킬아미노, 카르복시-(C1∼C4)알킬아미노, (C1∼C4)알콕시카르보닐-(C1∼C4)알킬아미노, 카르바모일-(C1∼C4)알킬아미노, N-(C1∼C4)알킬카르바모일-(C1∼C4)알킬아미노, N,N-디-[(C1∼C4)알킬]카르바모일-(C1∼C4)알킬아미노, 히드록시, (C1∼C4)알콕시, 히드록시-(C2∼C4)알콕시, (C1∼C4)알콕시-(C2∼C4)알콕시, 아미노-(C2∼C4)알콕시, (C1∼C4)알킬아미노-(C2∼C4)알콕시, 디-[(C1∼C4)알킬]아미노-(C2∼C4)알콕시, 피롤리딘 -1-일-(C2∼C4)알콕시, 피페리디노-(C2∼C4)알콕시, 모르폴리노-(C2∼C4)알콕시, 피페라진-1-일-(C2∼C4)알콕시 또는 4-(C1∼C4)알킬피페라진-1-일-(C2∼C4)알콕시이고, R4는 (C1∼C4)알킬이며, R5는 (C1∼C4)알킬이고, R6은 수소 또는 (C1∼C4)알킬이며, R7은 수소 또는 (C1∼C4)알킬이고, X는 산소이며, m은 1 또는 2이고, R8은 각각 수소, 할로게노, 히드록시, (C1∼C4)알콕시, (C2∼C4)알케닐옥시, (C2∼C4)알키닐옥시, (C1∼C4)알킬, (C3∼C4)알케닐, (C3∼C4)알키닐, 아미노, (C1∼C4)알킬아미노, 디-[(C1∼C4)알킬]아미노, 시아노, (C2∼C4)알카노일아미노, 카르복시, (C1∼C4)알콕시카르보닐, 카르바모일, N-(C1∼C4)알킬카르바모일 또는 N,N-디-[(C1∼C4)알킬]카르바모일이며, Y1은 할로게노, (C1∼C4)알칸설포닐옥시, 벤젠설포닐옥시 또는 페닐-(C1∼C4)알칸설포닐옥시이고, Y2는 할로게노, (C1∼C4)알칸설포닐옥시, 벤젠설포닐옥시 또는 페닐-(C1∼C4)알칸설포닐옥시이며, R1, R2 또는 R3에서 임의의 헤테로시클릭기는 1 개, 2 개 또는 3 개의 (C1∼C4)알킬 치환체에 의해 임의로 치환되고, Y1 및 Y2가 벤젠설포닐옥시 또는 페닐-(C1∼C4)알칸설포닐옥시인 경우 Y1 또는 Y2에서 임의의 페닐기는 할로게노, 니트로, 시아노, 트리플루오로메틸, 히드록시, 아미노, (C1∼C4)알킬, (C1∼C4)알콕시, (C1∼C4)알킬아미노 및 디-[(C1∼C4)알킬]아미노 중에서 선택된 1 개, 2 개 또는 3 개의 치환체에 의해 임의로 치환되며, 단 R1, R2 및 R3 중 하나 이상은 수소 이외의 것이다.