发明名称 Pyrazole compound and pharmaceutical use thereof
摘要 The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use:; wherein each symbol is the same as defined in the description.
申请公布号 US8846746(B2) 申请公布日期 2014.09.30
申请号 US201213599665 申请日期 2012.08.30
申请人 Japan Tobacco Inc. 发明人 Miura Tomoya;Ogoshi Yosuke;Ueyama Kazuhito;Motoda Dai;Iwayama Toshihiko;Suzawa Koichi;Nagamori Hironobu;Ueno Hiroshi;Takahashi Akihiko;Sugimoto Kazuyuki
分类号 A01N43/56;A61K31/415;C07D405/14;C07D403/14;C07D403/12;C07D409/12;C07D401/12;C07D413/12;C07D405/12 主分类号 A01N43/56
代理机构 Fitzpatrick, Cella, Harper & Scinto 代理人 Fitzpatrick, Cella, Harper & Scinto
主权项 1. A compound or a pharmaceutically acceptable salt thereof represented by the general formula [Ib]: wherein Ring Cy is (1) C6-10 aryl,(2) C3-8 cycloalkyl or(3) C3-8 cycloalkenyl, n1 is 0, 1, 2, 3 or 4, R1a is (1) a halogen atom,(2) hydroxy,(3) carboxy,(4) a C1-6 alkyl group,(5) a C2-8 alkenyl group,(6) a C2-8 alkynyl group,(7) a C1-6 alkoxy group,(8) a C3-6 cycloalkyl group,(9) a halo C1-6 alkyl group,(10) a hydroxy C1-6 alkyl group,(11) a C1-6 alkoxy C1-6 alkyl group,(12) a halo C1-6 alkoxy C1-6 alkyl group,(13) a C1-6 alkylsulfonyl C1-6 alkyl group,(14) a halo C1-6 alkylsulfonyl C1-6 alkyl group,(15) a halo C1-6 alkylamino C1-6 alkyl group,(16) a C3-6 cycloalkyl C2-6 alkynyl group,(17) a halo C1-6 alkoxy group,(18) a carboxy C1-6 alkoxy group,(19) a C1-6 alkylsulfanyl group,(20) a C1-6 alkylsulfonyl group,(21) a halo C1-6 alkylsulfonyl group,(22) a C1-8 alkylcarbonyl group,(23) a C1-6 alkyloxycarbonyl group,(24) a group represented by the Formula: whereinR5 is (a) a hydrogen atom or(b) a C1-6 alkyl group, andR6 is (a) a C1-6 alkyl group, or(b) a halo C1-6 alkyl group,(25) a saturated heterocyclo C1-6 alkyl group, wherein the saturated heterocycle is a 4-membered to 6-membered saturated heterocycle having 1 to 2 heteroatoms selected from nitrogen, oxygen, and sulfur, or(26) a saturated heterocyclo oxy C1-6 alkyl group, wherein the saturated heterocycle is a 4-membered to 6-membered saturated heterocycle having 1 to 2 heteroatoms selected from nitrogen, oxygen, and sulfur, provided that when n1 is 2, 3 or 4, each R1a is the same or different, R2a is (1) a C1-8 alkyl group,(2) a C3-8 cycloalkyl C1-6 alkyl group,(3) a C6-10 aryl C1-6 alkyl group,(4) a saturated heterocyclo C1-6 alkyl group, wherein the saturated heterocycle is a 4-membered to 6-membered saturated heterocycle having 1 to 2 heteroatoms selected from nitrogen, oxygen, and sulfur,(5) a C3-8 cycloalkyl group,(6) a halo C1-6 alkyl group,(7) a C1-6 alkoxy C1-6 alkyl group,(8) a halo C3-8 cycloalkyl group,(9) a C6-10 aryl group, wherein the C6-10 aryl group is optionally substituted by 1 to 4 substituents selected from the group consisting of: (a) a halogen atom,(b) hydroxy,(c) a C1-6 alkyl group,(d) a C2-8 alkenyl group,(e) a C2-6 alkynyl group,(f) a C1-6 alkoxy group,(g) a halo C1-6 alkyl group,(h) a C1-6 alkoxy C1-6 alkyl group,(i) a halo C1-6 alkoxy group,(j) a hydroxy C1-6 alkoxy group,(k) a C1-6 alkoxy C1-6 alkoxy group,(l) a carboxy C1-6 alkoxy group,(m) a C6-10 aryl C1-6 alkoxy group,(n) a C1-6 alkylsulfanyl C1-6 alkoxy group,(o) a C1-6 alkylsulfonyl C1-6 alkoxy group,(p) a C6-10 aryl C1-6 alkoxy C1-6 alkoxy group,(q) a saturated heterocyclo C1-6 alkoxy group, wherein the saturated heterocycle is a 4-membered to 6-membered saturated heterocycle having 1 to 2 heteroatoms selected from nitrogen, oxygen, and sulfur, and is optionally substituted by 1 to 2 C1-6 alkyl groups,(r) a saturated heterocyclo oxy group, wherein the saturated heterocycle is a 4-membered to 6-membered saturated heterocycle having 1 to 2 heteroatoms selected from nitrogen, oxygen, and sulfur,(s) a C3-8 cycloalkyloxy group,(t) a C1-6 alkoxycarbonyloxy group and(u) a C1-6 alkylsulfonyl group, or(10) a saturated heterocycle group, wherein the saturated heterocycle is a 4-membered to 6-membered saturated heterocycle having 1 to 2 heteroatoms selected from nitrogen, oxygen, and sulfur, and is optionally substituted by 1 to 4 C1-6 alkyl groups, and Ring Cya is a group selected from the group consisting of: (1) a group represented by the Formula: wherein m2 is 1, 2 or 3,m3 is 1, 2 or 3,n3 is 1 or 2,(2) a group represented by the Formula: wherein m4 is 0, 1, 2 or 3,m5 is 0, 1 or 2,provided that the sum of m4 and m5 is 1 or more,(3) a group represented by the Formula: wherein m4 is 0, 1, 2 or 3,m5 is 0, 1 or 2,provided that the sum of m4 and m5 is 1 or more,(4) a group represented by the Formula: wherein m6 is 0, 1 or 2,m7 is 0, 1 or 2,provided that the sum of m6 and m7 is 1 or more,(5) a group represented by the Formula: wherein m6 is 0, 1 or 2,m7 is 0, 1 or 2,provided that the sum of m6 and m7 is 1 or more,(6) a group represented by the Formula: wherein m8 is 1 or 2,m9 is 1 or 2, and(7) a group represented by the Formula: wherein m8 is 1 or 2,m9 is 1 or 2, n2 is 0, 1, 2, 3 or 4, R3a is (1) hydroxy,(2) a C1-6 alkyl group or(3) a hydroxy C1-6 alkyl group,provided that when n2 is 2, 3 or 4, each R3a is the same or different, R3b is (1) hydroxy,(2) a C1-6 alkyl group, which optionally forms a C3-6 cycloalkyl group together with the carbon to which it is attached and the carbon adjacent thereto,(3) a hydroxy C1-6 alkyl group, or(4) when two R3b are attached to the same carbon, they optionally form a C3-6 cycloalkyl group together with the carbon to which they are attached,provided that when n2 is 2, 3 or 4, each R3b is the same or different, and R4b is (1) a hydrogen atom,(2) a C1-6 alkyl group,(3) a carboxy C1-6 alkyl group,(4) a halo C1-6 alkyl group or(5) a C1-6 alkoxy C1-6 alkyl group.
地址 Tokyo JP