摘要:
The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.
摘要:
A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents -CH2-O-, -CH=CH- or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
摘要:
[Problem] To provide a compound that is useful as an agent in the prevention and treatment of circulatory system, nervous system, metabolic, reproductive system, and gastrointestinal diseases. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I):
[wherein, Z represents formula (II-1), (II-2), or (II-3),
wherein m and n are 0, 1, or 2, Y represents CR 3 or N, R 1 represents a C 1-6 alkyl, C 3-8 cycloalkyl, etc., R 2 represents phenyl or a heteroaryl, etc., R 3 and R 4 each independently represent a hydrogen atom, a C 1-6 alkyl, etc., M 1 , M 2 , M 3 , and M 4 each independently represent a hydrogen atom, a C 1-6 alkyl, etc.]
摘要:
[PROBLEMS] To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases. [MEANS FOR SOLVING PROBLEMS] The compound, which is for use as an active ingredient, is represented by the formula (I):
[wherein R 1 represents optionally halogenated C 1-6 alkyl, etc.; R 2 represents, e.g., a group represented by the formula (II-1) or (II-4)
(wherein W represents C 1-6 alkylene, etc. and R represents C 1-6 alkyl, etc.); R 3 represents hydrogen, C 1-6 alkyl, etc.; X represents -O-, -NH-, etc.; and Y 1 , Y 2 , Y 3 , and Y 4 each independently represents -CH-, -N-, etc.].
摘要:
The invention relates to compounds of a general formula (I): wherein A1 is selected from the following formula (aa1); R1 is a lower alkenyl group or a lower alkynyl group; R2 is a phenyl, pyridyl or thienyl group; R5 and R6 are a hydrogen atom, a lower alkyl group or a hydroxy-lower alkyl group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要:
The present invention relates to the crystalline forms of 2-allyl-1-[6-(I-hydroxy-1 methylethyl)pyridin-2-yl]-6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one or a salt thereof, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.
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 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 Formula [I]:
or a pharmaceutically acceptable salt or ester thereof, wherein R 1 and R 2 , which may be the same or different, are each a hydrogen atom, a lower alkyl group, a cycloalkyl group, or the like; R 3 and R 4 , which may be the same or different, are each a hydrogen atom, a lower alkyl group, NR a R b , a phenyl group, a lower alkyl group substituted with a phenyl group, a 4- to 7-membered aliphatic heterocyclic group, a lower alkyl group substituted with a 4- to 7-membered aliphatic heterocyclic group, a 5- or 6-membered aromatic heterocyclic group, a lower alkyl group substituted with a 5- or 6-membered aromatic heterocyclic group, or the like; and R 5 is a hydrogen atom, a cyano group, a halogen atom, or a lower alkyl group.
摘要翻译:本发明涉及由式[I]表示的化合物或其药学上可接受的盐或酯,其中R 1和R 2可以相同或不同,分别为氢原子,低级烷基, 环烷基等; R 3和R 4可以相同或不同,分别为氢原子,低级烷基,NR a R b,苯基,被苯基取代的低级烷基,4-至7- 被4至7元脂族杂环基取代的低级烷基,5或6元芳族杂环基,被5或6元芳族杂环基取代的低级烷基, 或类似物; R 5为氢原子,氰基,卤素原子或低级烷基。
摘要:
The present invention is directed at obtaining a high yield of a target substance and simultaneously securing high productivity. A reaction apparatus 10 has: a main flow channel 12 having an inner diameter of 3 mm, in which a raw material M 1 flows; an introduction flow channel 14 in which a raw material M 2 that causes a chemical reaction with the raw material M 1 flows; and five branch introduction flow channels 16a to 16e which are branched from the introduction flow channel 14 and introduce the raw material M 2 to the main flow channel 12, at predetermined introduction points 12o to 12s in the main flow channel 12. Here, in the main flow channel 12, the flow channel lengths of the flow channels 12b to 12d between adjacent introduction points 12p to 12s are not longer than those of the flow channels 12a to 12c between the next previous adjacent introduction points 12o to 12r in a flow direction of the raw material M 1 . At least one length of the flow channels 12b to 12d between the adjacent introduction points 12p to 12s is shorter than lengths of the flow channels 12a to 12c between previous adjacent introduction points 12o to 12r in the flow direction of the raw material M 1 .