摘要:
The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.
摘要:
The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.
摘要:
The piperidine derivative of the present invention in which the 4-position of the piperidine ring is bonded, via vinylene, to a mono-substituted (—R1) or unsubstituted benzene ring and the 1-position of the piperidine ring has an acyl group [—C(═O)—R4], or a pharmaceutically acceptable salt thereof has an excellent sodium channel inhibition action and an excellent analgesic action and shows a high analgesic effect particularly to neurogenic pain. The present compound is useful as a sodium channel inhibitor of low side effect
摘要:
A compound represented by following general formula (I): wherein, represents a single bond or a double bond; L represents —NH— or the like; X1 represents N or C, provided that in the case where X1 is N, X2 represents C—R and in the case where X1 is C, X2 represents N—R1 or the like; Y's may be either the same or different and represent CH2 or the like; A represents a non-natural sugar residue represented by following general formula: wherein, m represents 0 to 1; represents a single bond or a double bond; X represents O or the like; R3 to R8 may be either the same or different and represent hydroxy group or the like; and B represents a group represented by following general formula: wherein, n and k represent 0 to 5; represents a single bond or a double bond; Z1 to Z16 may be either the same or different and represent CH or the like; R10 and R11 may be either the same or different and represent a lower alkoxy group having 1 to 5 carbon atoms or the like; and R15 represents a hydrogen atom or the like, a pharmaceutically acceptable salt thereof, a prodrug thereof, a hydrate thereof or solvate thereof. Because of having an excellent CNT2 inhibitory activity and showing a high in vivo stability and stable physicochemical properties, the aforesaid compound is useful as a remedy for hyperuricemia.
摘要翻译:由以下通式(I)表示的化合物:其中,表示单键或双键; L表示-NH-等; X1表示N或C,条件是在X1为N的情况下,X2表示C-R,在X1为C的情况下,X2表示N-R1等; Y可以相同或不同,表示CH2等; A表示由以下通式表示的非天然糖残基:其中,m表示0至1; 代表单键或双键; X表示O等; R3至R8可以相同或不同,表示羟基等; 并且B表示由以下通式表示的基团:其中,n和k表示0至5; 代表单键或双键; Z1至Z16可以相同或不同,表示CH等; R 10和R 11可以相同或不同,表示具有1〜5个碳原子的低级烷氧基等; R 15表示氢原子等,其药学上可接受的盐,前药,其水合物或其溶剂合物。 由于具有优异的CNT2抑制活性并且具有高的体内稳定性和稳定的物理化学性质,上述化合物可用作高尿酸血症的补救剂。
摘要:
Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein.As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.
摘要:
Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein.As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.