摘要:
The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, wherein each substituent is defined in the specification. The present invention also relates to a pharmaceutical composition containiing an effective amount of the compound of formula (I) and a pharmaceutically effective carrier. The present invention further relates to methods of treatment of diseases associated with calcium release-activated calcium channels, diseases associated with IL-2 production, and methods of treatment of allergic, inflammatory or auto-immune diseases.
摘要:
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4═CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).
摘要翻译:药物,特别是具有钙释放依赖性钙通道抑制作用的药物组合物,特别是含有上述化合物作为活性成分的钙释放依赖性钙通道抑制剂的下述通式(I)表示的吡唑衍生物, (在该式中,每个符号具有以下含义:B:亚苯基,含氮,二价饱和环基或可被Alk,X:-NR 1取代的单环,二价杂芳族环基团 其中R 1,R 2,R 3,R 3,R 3,R 3, -NR 2 - , - SO 2 - , - SO 2 - , - SO 2 - , - SO 2 - , - SO 2 - 可以具有一个或多个取代基的一个 - 二环或三环稠合杂芳基,其可以具有一个或多个 取代基;可具有一个或多个取代基的环烷基;可具有一个或多个取代基的含氮饱和环基团 ents 可以具有一个或多个取代基的低级烯基; 可以具有一个或多个取代基的低级炔基; 或Alk,其可以具有一个或多个取代基)。
摘要:
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4═CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).
摘要翻译:药物,特别是具有钙释放依赖性钙通道抑制作用的药物组合物,特别是含有上述化合物作为活性成分的钙释放依赖性钙通道抑制剂的下述通式(I)表示的吡唑衍生物, (在该式中,每个符号具有以下含义:B:亚苯基,含氮,二价饱和环基或可被Alk,X:-NR 1取代的单环,二价杂芳族环基团 其中R 1,R 2,R 3,R 3,R 3,R 3, -NR 2 - , - SO 2 - , - SO 2 - , - SO 2 - , - SO 2 - , - SO 2 - 可以具有一个或多个取代基的一个 - 二环或三环稠合杂芳基,其可以具有一个或多个 取代基;可具有一个或多个取代基的环烷基;可具有一个或多个取代基的含氮饱和环基团 ents 可以具有一个或多个取代基的低级烯基; 可以具有一个或多个取代基的低级炔基; 或Alk,其可以具有一个或多个取代基)。
摘要:
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: D: pyrazolyl which may have 1 to 3 substituents selected from the group consisting of -Alk, -lower alkenyl, -lower alkynyl, -halogeno-lower alkyl, -Alk-cycloalkyl, -Alk-O-Alk, -cycloalkyl, —O-Alk, —COOH, —COO-Alk and -Hal, n: 0 or 1, B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4═CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).
摘要:
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: D: pyrazolyl which may have 1 to 3 substituents selected from the group consisting of -Alk, -lower alkenyl, -lower alkynyl, -halogeno-lower alkyl, -Alk-cycloalkyl, -Alk-O-Alk, -cycloalkyl, —O-Alk, —COOH, —COO-Alk and -Hal, n: 0 or 1, B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4═CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).
摘要:
The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, wherein each substituent is defined in the specification. The present invention also relates to a pharmaceutical composition containing an effective amount of the compound of formula (I) and a pharmaceutically effective carrier.The present invention further relates to methods of treatment of diseases associated with calcium release-activated calcium channels, diseases associated with IL-2 production, and methods of treatment of allergic, inflammatory or auto-immune diseases.
摘要:
Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof [wherein each symbol has the following meaning; X: O, S, NR1, CO, NR1CO, CONR1, C═N—OR1 or a bond, Y: a lower alkylene group which may be substituted by OR1 or —NHR1, or a bond, Z: O, NR2 or a bond, A: H, or a lower alkyl which may have a substituent, a —CO-lower alkyl which may have a substituent, an aryl which may have a substituent, a heteroaryl which may have a substituent, a cycloalkyl which may have a substituent or a nitrogen-containing saturated heterocyclic group which may have a substituent, B: an aryl which may have a substituent or a heteroaryl group which may have a substituent, R1, R2: H, a lower alkyl or a —CO-lower alkyl group].
摘要:
A nitrogen-containing six-membered heterocyclic compound having substituents —X—A—R3, —N(R1)-(Ph substituted by R2), and —CONH2, a salt thereof, a prodrug thereof, and a Syk inhibitor containing the same as an active ingredient. (In the formula, A: a (substituted) lower alkylene, a (substituted) arylene, or the like; X: NR4, CONR4, NR4CO, O, or S; R1, R4: H, a lower alkyl, —CO-lower alkyl, or —SO2-lower alkyl; R2: H, a (substituted) lower alkyl, —O-lower alkyl, —S-lower alkyl, —O-aryl, nitro, cyano, or the like; R3: —CO2H, —CO2-lower alkyl, -lower alkylene-CO2H, —NH2, -alkylene-NH2 or the like.
摘要翻译:具有取代基-XAR 3,-N(R 1) - (Ph被R 2取代的)的含氮六元杂环化合物和-CONH 2,其盐,其前药和 含有与活性成分相同的Syk抑制剂。 (式中,A:(取代的)低级亚烷基,(取代的)亚芳基等; X:NR 4,CONR 4,NR 4 CO,O或S; R 1 R 4:H,低级烷基,-CO-低级烷基或-SO 2 - 低级烷基; R 2:H,(取代的)低级烷基,-O-低级烷基,-S-低级 烷基,-O-芳基,硝基,氰基等; R 3:-CO 2 H,-CO 2 - 低级烷基, - 低级亚烷基-CO 2 H,-NH 2, - 亚烷基-NH 2等。
摘要:
To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with α-form crystal and β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenyleth-yl)amino]ethyl]acetanilide. The α-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The β-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the α-form crystal.
摘要:
To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-[(3-carbamimidoylphenylamino)methyl]-3-[4-(4-methyl-1,4-diazepan-1-yl)benzoylamino]benzoic acid and 3-hydroxy-4′-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide or a salt thereof is an effective ingredient.