摘要:
The present invention relates to a compound represented by Formula [I]: wherein X is O, S, NH or CH2; Y1, Y2, Y3, Y4 and Y5, which may be identical or different, are each CH or N; however, at least one of Y1, Y2, Y3, Y4 and Y5 is N; Z1 and Z2, which may be identical or different, are each CH or N; n is an integer from 1 to 3; R1 is a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group; R2 and R3, which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aromatic heterocyclic ring, or the like; and R4 is a hydrogen atom, a lower alkyl group, a C3-C6 cycloalkyl group or the like, or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.
摘要翻译:本发明涉及由式[I]表示的化合物:其中X是O,S,NH或CH 2; Y 1,Y 2,Y 3,Y 4和Y 5, 其可以相同或不同,各自为CH或N; 然而,Y 1,Y 2,Y 3,Y 4和Y 3中的至少一个, 5 SUB>是N; Z 1和Z 2可以相同或不同,各自为CH或N; n为1〜3的整数, R 1是C 3 -C 8环烷基,C 6 -C 10环烷基,C 6 -C 15环烷基, 芳基,脂族杂环或芳族杂环,或双环脂族饱和烃基; R 2和R 3可以相同或不同,分别为氢原子,低级烷基,低级烯基,C 3, C 1 -C 8环烷基,C 6 -C 10芳基,芳族杂环等; 和R 4是氢原子,低级烷基,C 3 -C 6环烷基等,或药学上可接受的 盐或酯,以及对Cdk4和/或Cdk6的选择性抑制剂或含有该化合物或其药学上可接受的盐或酯的抗癌剂。
摘要:
The present invention relates to a compound represented by Formula [I]: wherein X is O, S, NH or CH2; Y1, Y2, Y3, Y4 and Y5, which may be identical or different, are each CH or N; however, at least one of Y1, Y2, Y3, Y4 and Y5 is N; Z1 and Z2, which may be identical or different, are each CH or N; n is an integer from 1 to 3; R1 is a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group; R2 and R3, which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aromatic heterocyclic ring, or the like; and R4 is a hydrogen atom, a lower alkyl group, a C3-C6 cycloalkyl group or the like, or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.
摘要:
The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-a]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.
摘要:
The present invention relates to a compound represented by the formula (I): wherein R1 represents a hydrogen atom or the like; R2 represents lower alkyl or the like; R3 and R4 represent lower alkyl or the like; R5 represents phenyl or the like; R6 represents a hydrogen atom or the like; m is an integer of from 0 to 2; p is an integer of from 1 to 4; and q is an integer of from 1 to 5, or a pharmaceutical acceptable salt thereof, and a DGAT 1 inhibitor comprising the compound.
摘要:
The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-b]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3: R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a machine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.
摘要:
The present invention relates to a compound represented by a formula (I): wherein R1 represents a halogen atom or the like; R2 represents a hydrogen atom or the like; R3 and R4 each independently represents lower alkyl; R5 represents phenyl or the like; R6 represents a halogen atom or the like; m is an integer of from 0 to 2; p is an integer of from 1 to 4; and q is an integer of from 1 to 5 as an inhibitor of DGAT1 and its use for the treatment of hyperlipidemia etc.
摘要翻译:本发明涉及由式(I)表示的化合物:其中R1表示卤素原子等; R2表示氢原子等; R 3和R 4各自独立地表示低级烷基; R5表示苯基等; R6表示卤素原子等; m为0〜2的整数; p是1至4的整数; q为1〜5的整数,作为DGAT1的抑制剂及其用于治疗高脂血症等。
摘要:
An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
摘要:
This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X−signifies an anion].
摘要翻译:本发明涉及具有选择性毒蕈碱M 3受体拮抗作用,副作用小,适用于吸入治疗的化合物,并且可用作通式(I)的呼吸系统疾病的治疗剂; [其中A表示由式(a 0 SUB>)或(b 0>)表示的组; Ar表示任选取代的芳基或杂芳基; B 1和B 2表示脂族烃; R 1表示氟取代的环烷基; R 2,R 3和R 4表示低级烷基,单键或与B 1连接的亚烷基,或 R 2和R 3结合起来表示亚烷基; R 5和R 7表示氢,低级烷基或键合到B 2的单键或亚烷基; R 6表示氢,低级烷基或以-N(R 8)R 9表示的基团; 和X - 表示阴离子]。
摘要:
This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X− signifies an anion].
摘要:
The present invention relates to a compound represented by the Formula [I]: Wherein: the A ring is a 5-membered aromatic heterocyclic group containing at least one hetero atom selected from a nitrogen atom, and the like; A1 and A2, are each a nitrogen atom, and the like; X2, X3, X4, and X5 are all carbon atoms, or alternatively any one of X2, X3, X4, and X5 is a nitrogen atom and the rest are all carbon atoms; R1 is a hydrogen atom, or the like; R2, R3, R4, and R5, are each a hydrogen atom, or the like; R6 and R6′, are each a hydrogen atom, and the like; R7 is an aryl group and the like; and R8 is an amino group or a hydroxy group, or a pharmaceutically acceptable salt or ester thereof.
摘要翻译:本发明涉及由式[I]表示的化合物:其中:A环是含有至少一个选自氮原子的杂原子的5元芳族杂环基等; A 1和A 2分别是氮原子等; X 2,X 3,X 4和X 5都是碳原子,或者任意一个 X 2,X 3,X 4和X 5是氮原子,其余全部是碳 原子 R 1是氢原子等; R 2,R 3,R 4和R 5各自为氢原子等 ; R 6和R 6'各自为氢原子等; R 7是芳基等; 并且R 8是氨基或羟基,或其药学上可接受的盐或酯。