Treatment of parasitic diseases by inhibition of cysteine proteases of papain superfamilyThe present invention relates to compounds and pharmaceutical compositions which inhibit proteases, such as cysteine proteases. In particular, the present invention relates to compounds and pharmaceutical compositions which inhibit cysteine proteases of the papain superfamily. The compounds and pharmaceutical compositions of the present invention are useful for treating diseases, particularly parasitic diseases, which are mediated by such proteases. In particular, the present invention relates to a method of treating malaria by inhibiting the cysteine protease falcipain.Use and be selected from the medicine that following compound is used to suppress l-cysteine hcl anhydrous: 2-[n-(n-benzyloxycarbonyl glycyl)]-2 '-[n '-(n-benzyloxycarbonyl-l-leucyl)] carbohydrazide; (3rs)-and 1-(n-benzyloxycarbonyl-l-leucyl)-3-[n-(4-phenoxy group benzoyl) amino] tetramethyleneimine-4-ketone; (1s)-and n-[2-[1-(n-benzyloxycarbonyl amino)-3-methyl butyl] thiazole-4-base carbonyl]-n '-[n-(2-pyridyl methoxycarbonyl)-l-leucyl)] hydrazides; 1-(n-benzyloxycarbonyl-l-leucylamino)-3-(2-benzyloxy benzenesulfonyl) amino-third-2-ketone; n-[2-(2-benzyloxy phenyl) thiazole-4-base carbonyl]-n '-[n-(3-pyridyl methoxycarbonyl)-l-leucyl] hydrazides; (1s)-and n-[2-[1-(n-benzyloxycarbonyl amino)-3-methyl butyl] thiazole-4-base carbonyl]-n '-[n-(3-pyridyl methoxycarbonyl)-l-leucyl] hydrazides; 1-[n-(4-morpholino formamyl)-l-leucylamino]-3-(4-phenoxyphenylsulfonyhalides base) amino-third-2-ketone; n-[2-(1-naphthyl) thiazole-4-base carbonyl]-n '-[n-(4-is than pyridine ylmethoxy carbonyl)-l-leucyl] hydrazides; n-[2-(2-benzyloxy phenyl) thiazole-4-base carbonyl]-n '-(n-pyrazine carbonyl-l-leucyl) hydrazides; n-[n-(1-benzyl-5-methylimidazole-4-base carbonyl)-l-leucyl]-n '-[2-(1-naphthyl) thiazole-4-base carbonyl] hydrazides; (3rs)-and 3-[n-(3-benzyloxy benzoyl)-l-leucylamino] tetrahydrofuran (thf)-4-ketone; n-[2-[n-cyclopropyl-n-(2-methyl-propyl) amino] thiazole-4-base carbonyl]-n '-[n-(5-methyl-2-ben ji oxazole-4-base carbonyl)-l-leucyl] hydrazides; 1-[3-(2-pyridyl) phenyl kharophen]-3-[n-(2-thiophene carbonyl)-l-leucylamino] third-2-ketone; (3s)-3-[n-(benzothiazole-6-base carbonyl)-l-leucylamino]-1-[3-(2-pyridyl) phenyl kharophen] fourth-2-ketone; n-[2-[n-cyclopropyl-n-(2-methyl-propyl) amino] thiazole-4-base carbonyl]-n '-[n-(7-methoxyl group benzo furans-2-base carbonyl)-l-b-cyclopropyl alanyl] hydrazides; 1-[n-(benzoxazole-5-base carbonyl)-the l-leucylamino]-3-[3-(2-pyridyl) phenyl kharophen] third-2-ketone; 1-[n-[4-[2-(n, n-dimethylamino) oxyethyl group] benzoyl]-the l-leucylamino]-3-[3-(2-pyridyl) phenyl kharophen] third-2-ketone; with n-[2-[n-cyclopropyl-n-(2-methyl-propyl) amino] thiazole-4-base carbonyl]-n '-[n-[5-[2-(n, n-dimethylamino) oxyethyl group] cumarone-2-base carbonyl]-l-β-cyclopropyl alanyl] hydrazides.
파파인 상과의 시스테인 프로테아제 저해에 의한 기생충질환의 치료본 발명은 프로테아제, 예를 들어 시스테인 프로테아제를 저해하는 화합물 및 제약 조성물에 관한 것이다. 구체적으로, 본 발명은 파파인 상과의 시스테인 프로테아제를 저해하는 화합물 및 제약 조성물에 관한 것이다. 본 발명의 화합물 및 제약 조성물은 상기 프로테아제에 의해 매개되는 질환, 특히 기생충 질환 치료용으로 유용하다. 특히, 본 발명은 시스테인 프로테아제인 팔시파인 저해에 의한 말라리아 치료 방법에 관한 것이다. 2-[N-(N-벤질옥시카르보닐글리시닐)]-2'-[N'-(N-벤질옥시카르보닐-L-루이시닐)]카르보히드라지드, (3RS)-1-(N-벤질옥시카르보닐-L-루이시닐)-3-[N-(4-페녹시벤조일)아미노]피롤리딘-4-온, (1S)-N-[2-[1-(N-벤질옥시카르보닐아미노)-3-메틸부틸]티아졸-4-일카르보닐]-N'-[N-(2-피리디닐메톡시카르보닐)-L-루이시닐]히드라지드, 1-(N-벤질옥시카르보닐-L-루이시닐아미노)-3-(2-벤질옥시페닐술포닐)아미노프로판-2-온, N-[2-(2-벤질옥시페닐)티아졸-4-일카르보닐]-N'-[N-(3-피리디닐메톡시카르보닐)-L-루이시닐]히드라지드, (1S)-N-[2-[1-(N-벤질옥시카르보닐아미노)-3-메틸부틸]티아졸-4-일카르보닐]-N'-[N-(3-피리디닐메톡시카르보닐)-L-루이시닐]히드라지드, 1-[N-(4-모르폴리노카르바모일)-L-루이시닐아미노]-3-(4-페녹시페닐술포닐)아미노-프로판-2-온, N-[2-(1-나프틸)티아졸-4-일카르보닐]-N'-[N-(4-피리디닐메톡시카르보닐)-L-루이시닐]히드라지드, N-[2-(2-벤질옥시페닐)티아졸-4-일카르보닐]-N'-(N-피라진카르보닐-L-루이시닐)히드라지드, N-[N-(1-벤질-5-메틸이미다졸-4-일카르보닐)-L-루이시닐]-N'-[2-(1-나프틸)티아졸-4-일카르보닐]히드라지드, (3RS)-3-[N-(3-벤질옥시벤조일)-L-루이시닐아미노]테트라히드로푸란-4-온, N-[2-[N-시클로프로필-N-(2-메틸프로필)아미노]티아졸-4-일카르보닐]-N'-[N-(5-메틸-2-페닐옥사졸-4-일카르보닐)-L-루이시닐]히드라지드, 1-[3-(2-피리디닐)페닐아세틸아미노]-3-[N-(2-티오펜카르보닐)-L-루이시닐아미노]프로판-2-온, (3S)-3-[N-(벤조티아졸-6-일카르보닐)-L-루이시닐아미노]-1-[3-(2-피리디닐)페닐아세틸아미노]부탄-2-온, N-[2-[N-시클로프로필-N-(2-메틸프로필)아미노]티아졸-4-일카르보닐]-N'-[N-(7-메톡시벤조푸란-2-일카르보닐)-L-b-시클로프로필알라닐]히드라지드, 1-[N-(벤즈옥사졸-5-일카르보닐)-L-루이시닐아미노]-3-[3-(2-피리디닐)페닐아세틸아미노]프로판-2-온, 1-[N-[4-[2-(N,N-디메틸아미노)에톡시]벤조일]-L-루이시닐아미노]-3-[3-(2-피리디닐)페닐아세틸아미노]프로판-2-온, 및 N-[2-[N-시클로프로필-N-(2-메틸프로필)아미노]티아졸-4-일카르보닐]-N'-[N-[5-[2-(N,N-디메틸아미노)에톡시]벤조푸란-2-일카르보닐]-L-β-시클로프로필알라닐]히드라지드 로 이루어진 군으로부터 선택된 화합물의 시스테인 프로테아제 저해용 약물의 제조에 있어서의 용도. 