wherein A is a condensed pyrimidinone or condensed pyridazinone ring; Ar 1 and Ar 2 are independently a ring; Z is a divalent group, or a salt thereof which have an excellent antitumor activity.
摘要翻译:A-Z-Ar 1 -CO-Ar 2的新化合物,其中A是稠合的嘧啶酮或缩合的哒嗪酮环; Ar 1和Ar 2独立地是环; Z是具有优异的抗肿瘤活性的二价基团或其盐。
摘要:
The present invention relates to a compound of the formula: wherein A is halogen, N(O)mR¹R², N ⊕ R¹R²R³·X ⊖ , S(O)nR¹ or S ⊕ (O)mR¹R²·X ⊖ where R¹,R² and R³ are each optionally substituted hydrocarbon or heterocyclic group, X ⊖ is a counter anion; m is an integer of 0 or 1; n is an integer of 0 to 2; R¹ and R² may form a nitrogen-containing or a sulfur-containing heterocyclic ring, which may further form a condensed ring, with the adjacent nitrogen atom or sulfur atom, and these nitrogen-containing or sulfur-containing heterocyclic rings may have substituents, B is O or NR⁴ where R⁴ is hydrogen or an optionally substituted lower alkyl or aryl group, D is 2-methyl-1-propenyl group or isobutyl group, and E is hydrogen, an optionally substituted hydrocarbon or an optionally substituted acyl group; provided that, when A is chlorine, E is an optionally substituted hydrocarbon or acyl excepting dinitrobenzoyl, a salt thereof, production and use thereof. The novel cyclohexanol derivatives of the present invention have angiogenesis inhibiting activity and anti-tumor activity, and they are used as anti-rheumatic agents, therapeutic agents of psoriasis, therapeutic agents of diabetic retinopathy and anti-tumor agents.
摘要翻译:本发明涉及下式化合物:其中A为卤素,N(O)m R 1 R 2,N(R)R 1 R 2 R 3, ,X(=),S(O)nR 1或S((+))(O)m R 1 R 2,X( - ))其中R 1,R 2 >和R 3各自是任选取代的烃或杂环基,X'( - )>是抗衡阴离子; m为0或1的整数; n为0〜2的整数, R 1和R 2可以形成含氮或含硫杂环,其可以与相邻的氮原子或硫原子进一步形成稠环,并且这些含氮或含硫杂环 环可以具有取代基,B是O或NR 4,其中R 4是氢或任选取代的低级烷基或芳基,D是2-甲基-1-丙烯基或异丁基,E是氢, 任选取代的烃或任选取代的酰基; 条件是当A是氯时,E是除二硝基苯甲酰基以外的任选取代的烃或酰基,其盐,其制备和用途。 本发明的新型环己醇衍生物具有血管生成抑制活性和抗肿瘤活性,并且它们用作抗风湿剂,牛皮癣治疗剂,糖尿病性视网膜病变的治疗剂和抗肿瘤剂。
摘要:
Anti-tomor agents comprising novel 3(2H)-pyridazinone derivatives or salts thereof and methods of producing the same are disclosed. Also disclosed is a method for treating or preventing tumors by administering to a mammal a therapeutically effective amount of 4,5-di substituted 3(2H)-pyridazinones and salts thereof.
摘要:
There is disclosed a pharmaceutical composition for inhibiting glutaminase which comprises a imidazole derivative or a salt thereof. This compound selectively inhibits the proliferation of tumor cells, and the composition is useful as an anti-cancer agent. There is also disclosed a novel imidazole derivative having glutaminase inhibitory activity.
摘要:
The present invention relates to a compound of the formula: wherein A is halogen, N(O)mR¹R², N ⊕ R¹R²R³·X ⊖ , S(O)nR¹ or S ⊕ (O)mR¹R²·X ⊖ where R¹,R² and R³ are each optionally substituted hydrocarbon or heterocyclic group, X ⊖ is a counter anion; m is an integer of 0 or 1; n is an integer of 0 to 2; R¹ and R² may form a nitrogen-containing or a sulfur-containing heterocyclic ring, which may further form a condensed ring, with the adjacent nitrogen atom or sulfur atom, and these nitrogen-containing or sulfur-containing heterocyclic rings may have substituents, B is O or NR⁴ where R⁴ is hydrogen or an optionally substituted lower alkyl or aryl group, D is 2-methyl-1-propenyl group or isobutyl group, and E is hydrogen, an optionally substituted hydrocarbon or an optionally substituted acyl group; provided that, when A is chlorine, E is an optionally substituted hydrocarbon or acyl excepting dinitrobenzoyl, a salt thereof, production and use thereof. The novel cyclohexanol derivatives of the present invention have angiogenesis inhibiting activity and anti-tumor activity, and they are used as anti-rheumatic agents, therapeutic agents of psoriasis, therapeutic agents of diabetic retinopathy and anti-tumor agents.
摘要:
The present invention relates to a compound of the formula: wherein R¹ is 2-methyl-1-propenyl group or isobutyl group; R² and R³ are each hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group or R² and R³ may form a ring together with the adjacent nitrogen atom; and the bonding mark ∼ means α-linkage or β-linkage, or a salt thereof. The compound (I) of the present invention has, among others, angiogenesis inhibiting activity, cell-growth inhibiting activity and immune reaction inhibiting activity, thus being useful as medicines, etc.
摘要翻译:本发明涉及下式的化合物:其中R 1为2-甲基-1-丙烯基或异丁基; R 2和R 3各自为氢原子,任选取代的烃残基或任选取代的酰基,或R 2和R 3可以与相邻的氮原子一起形成环; 并且粘合标记是指α-链接或β-连接,或其盐。 本发明的化合物(I)具有血管生成抑制活性,细胞生长抑制活性和免疫反应抑制活性,作为药物等有用。