发明名称 Heteroaryl quinazoline derivatives
摘要 Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc.; (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: ; (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).
申请公布号 US8846700(B2) 申请公布日期 2014.09.30
申请号 US201314021639 申请日期 2013.09.09
申请人 MSD K.K. 发明人 Iino Tomoharu;Ohno Akio;Otake Norikazu;Suga Takuya;Asai Masanori
分类号 A61K31/517 主分类号 A61K31/517
代理机构 代理人 Cocuzzo Anna L.;Fitch Catherine D.
主权项 1. A compound represented by a formula (I): wherein the A ring represents a pyrazinyl group, which may have one or two substituent groups selected from the group consisting of lower alkyl, lower alkoxy, halogen, hydroxy, and C3-7 cycloalkyl, wherein the alkyl substituent group may have 1-3 identical or different substituent groups selected from the group consisting of lower alkoxy groups, halogen atoms and hydroxy groups; the B ring represents a 5- or 6-membered heteroaryl group having 1-3 identical or different hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms; R represents a substituent group selected from the group consisting of lower alkyl, lower alkoxy, halogen, hydroxy and lower alkyl having 1-3 identical or different substituent groups selected from the group consisting of: lower alkoxy groups, halogen atoms or hydroxy groups; k represents an integer of from 0 to 3; R1 denotes a group represented by a formula (II-1), (II-2), (II-3) or II-4): wherein R11 and R12 each independently represent hydrogen, lower alkyl or C3-7 cycloalkyl, or R11 and R12, together with the nitrogen atom to which they are bound, constitute a 4- to 7-membered nitrogen-containing aliphatic ring (which may be substituted with 1-3 identical or different halogen atoms), or any carbon atom of (CH2)m, together with R11 or R12, may constitute a 4- to 7-membered nitrogen-containing aliphatic ring; any carbon atom in (CH2)m may be substituted with a lower alkyl group; the nitrogen atom to which R11 and R12 are bound may form N-oxide; and m represents an integer of from 2 to 6, a group represented by a formula (II-2) —O—(CH2)n—R13  (II-2)wherein: R13 represents lower alkoxy, hydroxy or carboxyl; n represents an integer of from 1 to 6; upon R13 being lower alkoxy, the lower alkoxy, together with any carbon atom of (CH2)n, may form a 5- to 7-membered aliphatic rings; and any carbon atom in (CH2)n may be substituted with a lower alkyl group, a group represented by a formula (II-3) wherein R14 and R15 are synonymous with the above R11 and R12; p represents an integer of from 2 to 6; and R3 represents a hydrogen atom or a lower alkyl group, or a group represented by a formula (II-4) wherein: R16 and R17 are synonymous with the above R11 and R12; q represents an integer of from 2 to 6; and R4 represents a hydrogen atom or a lower alkyl group, R2 is a group selected from the group consisting of: lower alkyl, lower alkoxy, halogen, hydroxy, cyano, carboxyl, alkoxycarbonyl, N-alkylcarbamoyl, N,N-dialkylcarbamoyl, lower alkylsulfonyl and lower alkyl having 1-3 identical or different substituents independently selected from lower alkoxy groups, halogen atoms, hydroxy groups, cyano groups, carboxyl groups, alkoxycarbonyl groups, N-alkylcarbamoyl groups, N,N-dialkylcarbamoyl groups or lower alkylsulfonyl groups, and r represents an integer of from 0 to 3,or a pharmaceutically acceptable salt thereof.
地址 Tokyo JP