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1. 发明申请

WO2010024110A1 OXOTETRAHYDROFURAN-2-YL-BENZIMIDAZOLE DERIVATIVE 审中-公开
标题翻译：氧自由基2-YL-苯并咪唑衍生物
公开(公告)号：WO2010024110A1
公开(公告)日：2010-03-04
申请号：PCT/JP2009/064072
申请日：2009-08-03
申请人： BANYU PHARMACEUTICAL CO.,LTD. , IINO, Tomoharu , ASAI, Masanori , OHNO, Akio , INAMURA, Seiichi , ISHIKAWA, Makoto , OHTAKE, Norikazu
发明人： IINO, Tomoharu , ASAI, Masanori , OHNO, Akio , INAMURA, Seiichi , ISHIKAWA, Makoto , OHTAKE, Norikazu
IPC分类号： C07D405/14 , A61K31/4439 , A61K31/444 , A61K45/00 , A61P3/04 , A61P3/10 , A61P9/10 , A61P13/12 , A61P25/02 , A61P27/02 , A61P43/00
CPC分类号： C07D405/14 , A61K31/4439 , A61K31/444 , A61K38/28 , A61K38/31 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds, which are useful for treatment and/or prevention of diabetes mellitus, diabetes mellitus complications or obesity, since the compounds have glucokinase-activating effects, and are presented in Formula (I): wherein R1 represents a carbamoyl group; R2 represents a lower alkyl group; both of X1 and X2 represent CH, or any one of X1 and X2 represents a nitrogen atom and the other represents CH; a group of represents a group selected from the group consisting of a pyridinyl, a pyrazinyl, a pyrazolyl, a thiadiazolyl, a triazolyl, an isoxazolyl and a thiazolyl group; and k is zero or 1, or relates to pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及可用于治疗和/或预防糖尿病，糖尿病并发症或肥胖症的化合物，因为该化合物具有葡糖激酶活化作用，并且呈现在式（I）中：其中R1表示氨基甲酰基 ; R2表示低级烷基; X1和X2都表示CH，或X1和X2中的任一个表示氮原子，另一个表示CH; 一组表示选自吡啶基，吡嗪基，吡唑基，噻二唑基，三唑基，异恶唑基和噻唑基的基团。且k为0或1，或与其药学上可接受的盐有关。

2. 发明申请

WO2008088692A2 SPIROCHROMANON DERIVATIVES 审中-公开
标题翻译：螺吡喃衍生物
公开(公告)号：WO2008088692A2
公开(公告)日：2008-07-24
申请号：PCT/US2008/000247
申请日：2008-01-08
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , IINO, Tomoharu , JONA, Hideki , KURIHARA, Hideki , NAKAMURA, Masayuki , NIIYAMA, Kenji , SHIBATA, Jun , SHIMAMURA, Tadashi , WATANABE, Hitomi , YAMAKAWA, Takeru , YANG, Lihu
发明人： IINO, Tomoharu , JONA, Hideki , KURIHARA, Hideki , NAKAMURA, Masayuki , NIIYAMA, Kenji , SHIBATA, Jun , SHIMAMURA, Tadashi , WATANABE, Hitomi , YAMAKAWA, Takeru , YANG, Lihu
IPC分类号： A01N43/16
CPC分类号： C07D491/107 , C07D491/20 , C07D519/00
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.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar 1表示由选自苯，吡唑，异恶唑，吡啶，吲哚，1H-吲唑，1H-呋喃并[2,5- 3-c]吡唑，1H-噻吩并[2,3-c]吡唑，苯并咪唑，1,2-苯并异恶唑，咪唑并[1,2-a]吡啶，咪唑并[1,5-a]吡啶和1H-吡唑并[ 3,4-b]吡啶，具有Ar 2，并且任选具有一个或两个以上选自R3的取代基; R 1和R 2各自独立地表示氢原子，卤素原子，氰基，C 2 -C 6烯基，C 1 -C 6烷氧基，C 2 -C 7烷酰基，C 2 -C 7烷氧基羰基，芳烷氧基羰基，氨基甲酰基-C 1 -C 6烷氧基，羧基-C 2 -C 6烯基或-Q 1 -N（R a）-Q 2 -R b的基团; 或任选具有取代基的C1-C6烷基; 或任选具有取代基的芳基或杂环基; 或具有芳基或杂环基的C 1 -C 6烷基或C 2 -C 6烯基; T和U各自独立地表示氮原子或次甲基; V表示氧原子或硫原子。本发明的化合物可用作各种ACC相关疾病的治疗剂。

3. 发明申请

WO2007011811A1 SPIROCHROMANONE DERIVATIVES AS ACETYL COENZYME A CARBOXYLASE (ACC) INHIBITORS 审中-公开
标题翻译：甲氧基酮衍生物作为乙酰丙酮羧酸酶（ACC）抑制剂
公开(公告)号：WO2007011811A1
公开(公告)日：2007-01-25
申请号：PCT/US2006/027546
申请日：2006-07-14
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , YAMAKAWA, Takeru , JONA, Hideki , NIIYAMA, Kenji , YAMADA, Koji , IINO, Tomoharu , OHKUBO, Mitsuru , IMAMURA, Hideaki , KUSUNOKI, Jun , YANG, Lihu
发明人： YAMAKAWA, Takeru , JONA, Hideki , NIIYAMA, Kenji , YAMADA, Koji , IINO, Tomoharu , OHKUBO, Mitsuru , IMAMURA, Hideaki , KUSUNOKI, Jun , YANG, Lihu
IPC分类号： C07D491/10 , C07D495/10 , A61K31/438 , A61P3/00 , A61P35/00 , A61P31/00
CPC分类号： C07D491/10 , C07D495/10
摘要： The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.
摘要翻译：本发明涉及可用作各种ACC相关疾病的治疗剂的式（I）化合物或其药学上可接受的盐或酯。

4. 发明申请

WO2007011809A1 SPIROCHROMANONE DERIVATIVES AS ACETYL COENZYME A CARBOXYLASE (ACC) INHIBITORS 审中-公开
标题翻译：乙腈衍生物作为乙酰丙酮羧酸酶（ACC）抑制剂
公开(公告)号：WO2007011809A1
公开(公告)日：2007-01-25
申请号：PCT/US2006/027543
申请日：2006-07-14
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , YAMAKAWA, Takeru , JONA, Hideki , NIIYAMA, Kenji , YAMADA, Koji , IINO, Tomoharu , OHKUBO, Mitsuru , IMAMURA, Hideaki , SHIBATA, Jun , KUSUNOKI, Jun , YANG, Lihu
发明人： YAMAKAWA, Takeru , JONA, Hideki , NIIYAMA, Kenji , YAMADA, Koji , IINO, Tomoharu , OHKUBO, Mitsuru , IMAMURA, Hideaki , SHIBATA, Jun , KUSUNOKI, Jun , YANG, Lihu
IPC分类号： C07D491/10 , C07D497/10 , A61K31/438 , A61P3/00 , A61P35/00 , A61P31/00
CPC分类号： C07D491/10 , C07D495/10
摘要： The invention relates to a compound of a formula (I): , or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.
摘要翻译：本发明涉及可用作各种ACC相关疾病的治疗剂的式（I）的化合物或其药学上可接受的盐或酯。

5. 发明申请

WO2008088689A1 SUBSTITUTED SPIROCHROMANONE DERIVATIVES AS ACC INHIBITORS 审中-公开
标题翻译：作为ACC抑制剂的替代螺吡喃酮衍生物
公开(公告)号：WO2008088689A1
公开(公告)日：2008-07-24
申请号：PCT/US2008/000223
申请日：2008-01-08
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , IINO, Tomoharu , JONA, Hideki , SHIBATA, Jun , SHIMAMURA, Tadashi , YAMAKAWA, Takeru , YANG, Lihu
发明人： IINO, Tomoharu , JONA, Hideki , SHIBATA, Jun , SHIMAMURA, Tadashi , YAMAKAWA, Takeru , YANG, Lihu
IPC分类号： C07D491/10 , A61K31/438 , A61P3/00
CPC分类号： C07D519/00 , C07D491/10
摘要： The invention relates to a compound of a general formula (I): wherein Ar 1 represents a group formed from an aromatic ring selected from a group consisting of indole, benzimidazole and 1,2-benzisoxazole, having R 3 and R 4 , and optionally having a substituent selected from a group consisting of a halogen atom, a hydroxyl group, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a hydroxy-C1-C6 alkyl group, a cyclo-C3-C6 alkyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group and carbamoyl group; R 1 represents a phenyl group optionally substituted with a carboxyl group, a tetrazolyl group optionally substituted with a C2-C7 alkanoyloxy-C1-C6 alkyl group, a pyridyl group optionally substituted with a C1-C6 alkyl group or a carboxyl group, a dihydro-1,2,4-triazolyl group optionally substituted with an oxo group, or a dihydro-1,2,4-oxadiazolyl group optionally substituted with an oxo group; R 2 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group, or a C1-C6 alkoxy group; and R 3 and R 4 each independently represent a hydrogen atom, a halogen atom, nitro group, a cyclo-C3-C6 alkyl group, a carbamoyl group optionally substituted with a C1-C6 alkyl or cyclo-C3-C6 alkyl group, a C1-C6 alkoxy group optionally substituted with a hydroxyl group, or a C1-C6 alkyl group optionally substituted with a hydroxyl group. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar 1表示由选自吲哚，苯并咪唑和1,2-苯并异恶唑的芳环形成的基团，其中R 并且任选地具有选自卤素原子，羟基，C 1 -C 6烷基，卤代C 1 -C 6烷基的取代基， C 1 -C 6烷基，羟基-C 1 -C 6烷基，环-C 3 -C 6烷基，C 1 -C 6烷氧基，卤代-C 1 -C 6烷氧基和氨基甲酰基; R 1表示任选被羧基取代的苯基，任选被C 2 -C 7烷酰氧基-C 1 -C 6烷基取代的四唑基，任选被C 1 -C 6烷基取代的吡啶基或任选被氧代基取代的羧基，二氢-1,2,4-三唑基或任选被氧代基取代的二氢-1,2,4-恶二唑基; R 2表示氢原子，卤素原子，C 1 -C 6烷基或C 1 -C 6烷氧基; R 3和R 4各自独立地表示氢原子，卤原子，硝基，环-C 3 -C 6烷基，任选被 C 1 -C 6烷基或环-C 3 -C 6烷基，任选被羟基取代的C 1 -C 6烷氧基或任选被羟基取代的C 1 -C 6烷基。本发明的化合物可用作各种ACC相关疾病的治疗剂。

6. 发明申请

WO2008088688A1 SUBSTITUTED SPIROCHROMANONE DERIVATIVES AS ACC INHIBITORS 审中-公开
标题翻译：作为ACC抑制剂的替代螺吡喃酮衍生物
公开(公告)号：WO2008088688A1
公开(公告)日：2008-07-24
申请号：PCT/US2008/000221
申请日：2008-01-08
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , IINO, Tomoharu , JONA, Hideki , SHIBATA, Jun , SHIMAMURA, Tadashi , YAMAKAWA, Takeru , YANG, Lihu
发明人： IINO, Tomoharu , JONA, Hideki , SHIBATA, Jun , SHIMAMURA, Tadashi , YAMAKAWA, Takeru , YANG, Lihu
IPC分类号： C07D491/10 , A61K31/438 , A61P3/00 , C07D495/04
CPC分类号： C07D519/00 , C07D491/10
摘要： The invention relates to a compound of a general formula (I): (I) wherein Ar 1 represents a group formed from an aromatic ring selected from a group consisting of indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; R 1 and R 2 each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(R a )-Q2-R b ; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; R 3 and R 4 each represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-C6 alkyl group, a carbamoyl group optionally substituted with a C1-C6 alkyl or cyclo-C3-C6 alkyl group, or a group of -N(R e )R f ; an optionally-substituted C2-C7 alkanoyl, C1-C6 alkoxy, C2-C7 alkoxycarbonyl, cyclo-C3-C6 alkyloxycarbonyl, C1-C6 alkylsulfonyl, C1-C6 alkylthio, cyclo-C3-C6 alkyloxy, cyclo-C3-C6 alkyl-C1-C6 alkoxy, cyclo-C3-C6 alkylsulfonyl, cyclo-C3-C6 alkylthio or cyclo-C3-C6 alkyl-C1-C6 alkylthio group; or an optionally-substituted C1-C6 alkyl group; T and U each 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.
摘要翻译：本发明涉及通式（I）的化合物：（I）其中Ar 1表示由选自吲哚，1H-吲唑，2H-吲唑的芳环形成的基团，1H-噻吩并[2,3-c]吡唑，1H-吡唑并[3,4-b]吡啶，苯并[b]呋喃，苯并咪唑，苯并恶唑，1,2-苯并异恶唑和咪唑并[1,2-a] ; R 1和R 2各自表示氢原子，卤素原子，氰基，C 2 -C 6烯基，C 1 -C 6烷氧基，卤代 C1-C6烷氧基，环-C3-C6烷氧基，C2-C7烷酰基，卤代-C2-C7烷酰基，C2-C7烷氧基羰基，卤代-C2-C7烷氧基羰基， C 3 -C 6烷氧基羰基，芳烷氧基羰基，氨基甲酰基-C 1 -C 6烷氧基，羧基-C 2 -C 6烯基或-Q 1 -N（R a a O） [R ^{b'/ SUP>; 任选取代的C 1 -C 6烷基，芳基或杂环基; 或具有芳基或杂环基的C 1 -C 6烷基或C 2 -C 6烯基; R 3和R 4各自表示氢原子，卤素原子，硝基，环-C 3 -C 6烷基，任选被C1取代的氨基甲酰基 -C 6烷基或环-C 3 -C 6烷基，或-N（R e）O的基团。任选取代的C 2 -C 7烷酰基，C 1 -C 6烷氧基，C 2 -C 7烷氧基羰基，环C 3 -C 6烷氧基羰基，C 1 -C 6烷基磺酰基，C 1 -C 6烷硫基，环C 3 -C 6烷氧基，环C 3 -C 6烷基 - C 1 -C 6烷氧基，环-C 3 -C 6烷基磺酰基，环-C 3 -C 6烷硫基或环-C 3 -C 6烷基-C 1 -C 6烷硫基; 或任选取代的C 1 -C 6烷基; T和U各自表示氮原子或次甲基; V表示氧原子或硫原子。本发明的化合物可用作各种ACC相关疾病的治疗剂。}

7. 发明公开

EP2120569A2 SPIROCHROMANON DERIVATIVES 有权
标题翻译：螺旋色素衍生物
公开(公告)号：EP2120569A2
公开(公告)日：2009-11-25
申请号：EP08705516.6
申请日：2008-01-08
申请人： Merck & Co., Inc. , BANYU PHARMACEUTICAL CO., LTD.
发明人： IINO, Tomoharu , JONA, Hideki , KURIHARA, Hideki , NAKAMURA, Masayuki , NIIYAMA, Kenji , SHIBATA, Jun , SHIMAMURA, Tadashi , WATANABE, Hitomi , YAMAKAWA, Takeru , YANG, Lihu
IPC分类号： A01N43/16 , A61K31/35
CPC分类号： C07D491/107 , C07D491/20 , C07D519/00
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.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar 1表示由选自苯，吡唑，异恶唑，吡啶，吲哚，1H-吲唑，1H-呋喃并[2,1- 1H-噻吩并[2,3-c]吡唑，苯并咪唑，1,2-苯并异恶唑，咪唑并[1,2-a]吡啶，咪唑并[1,5-a]吡啶和1H-吡唑并[ 3,4-b]吡啶，其具有Ar 2，并且任选地具有一个或两个或更多个选自R 3的取代基; R 1和R 2各自独立地表示氢原子，卤素原子，氰基，C 2 -C 6烯基，C 1 -C 6烷氧基，C 2 -C 7烷酰基，C 2 -C 7烷氧基羰基，芳烷氧基羰基，氨基甲酰基-C1-C6烷氧基，羧基-C2-C6链烯基或-Q1-N（Ra）-Q2-Rb的基团; 或任选具有取代基的C1-C6烷基; 或任选具有取代基的芳基或杂环基团; 或具有芳基或杂环基的C1-C6烷基或C2-C6烯基; T和U各自独立地表示氮原子或次甲基; V代表氧原子或硫原子。本发明的化合物可用作各种ACC相关疾病的治疗剂。

8. 发明公开

EP1910375A1 SPIROCHROMANONE DERIVATIVES AS ACETYL COENZYME A CARBOXYLASE (ACC) INHIBITORS 有权
标题翻译：螺吡喃衍生物乙酸乙酯 - 羧基酶
公开(公告)号：EP1910375A1
公开(公告)日：2008-04-16
申请号：EP06787451.1
申请日：2006-07-14
申请人： Merck & Co., Inc. , BANYU PHARMACEUTICAL CO., LTD.
发明人： YAMAKAWA, Takeru , JONA, Hideki , NIIYAMA, Kenji , YAMADA, Koji , IINO, Tomoharu , OHKUBO, Mitsuru , IMAMURA, Hideaki , SHIBATA, Jun , KUSUNOKI, Jun , YANG, Lihu
IPC分类号： C07D491/10 , C07D497/10 , A61K31/438 , A61P3/00 , A61P35/00 , A61P31/00
CPC分类号： C07D491/10 , C07D495/10
摘要： The invention relates to a compound of a formula (I): , or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.

9. 发明公开

EP2111406A1 SUBSTITUTED SPIROCHROMANONE DERIVATIVES AS ACC INHIBITORS 有权转让
标题翻译：取代SPIROCHROMANON衍生物作为ACC抑制剂
公开(公告)号：EP2111406A1
公开(公告)日：2009-10-28
申请号：EP08713050.6
申请日：2008-01-08
申请人： Merck & Co., Inc. , BANYU PHARMACEUTICAL CO., LTD.
发明人： IINO, Tomoharu , JONA, Hideki , SHIBATA, Jun , SHIMAMURA, Tadashi , YAMAKAWA, Takeru , YANG, Lihu
IPC分类号： C07D491/10 , A61K31/438 , A61P3/00 , C07D495/04
CPC分类号： C07D519/00 , C07D491/10
摘要： The invention relates to a compound of a general formula (I): (I) wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; R1 and R2 each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl 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; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; R3 and R4 each represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-C6 alkyl group, a carbamoyl group optionally substituted with a C1-C6 alkyl or cyclo-C3-C6 alkyl group, or a group of -N(Re)Rf; an optionally-substituted C2-C7 alkanoyl, C1-C6 alkoxy, C2-C7 alkoxycarbonyl, cyclo-C3-C6 alkyloxycarbonyl, C1-C6 alkylsulfonyl, C1-C6 alkylthio, cyclo-C3-C6 alkyloxy, cyclo-C3-C6 alkyl-C1-C6 alkoxy, cyclo-C3-C6 alkylsulfonyl, cyclo-C3-C6 alkylthio or cyclo-C3-C6 alkyl-C1-C6 alkylthio group; or an optionally-substituted C1-C6 alkyl group; T and U each 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.

10. 发明公开

EP2221301A1 HETEROARYLOXY QUINAZOLINE DERIVATIVE 有权转让
标题翻译：杂原子氧基喹唑啉衍生物
公开(公告)号：EP2221301A1
公开(公告)日：2010-08-25
申请号：EP08849029.7
申请日：2008-11-10
申请人： Banyu Pharmaceutical Co., Ltd.
发明人： ASAI, Masanori , IINO, Tomoharu , SUGA, Takuya , OHNO, Akio , OHTAKE, Norikazu
IPC分类号： C07D401/14 , A61K31/517 , A61K38/22 , A61K38/28 , A61K45/00 , A61P3/10 , A61P9/10 , A61P13/12 , A61P25/00 , A61P27/00 , A61P43/00 , C07D417/14 , C07D513/04
CPC分类号： C07D401/14 , A61K31/517 , A61K38/28 , C07D403/14 , C07D417/14 , C07D513/04 , A61K2300/00
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.; R 1 represents a group of a formula:

(wherein R 11 and R 12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.;
R 2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).
摘要翻译：公开了具有葡糖激酶活化作用并可用于治疗糖尿病，肥胖症等药物领域的下式的化合物及其药学上可接受的盐（其中环A表示任选具有更低级的吡唑基烷基等;环B表示杂芳基; R表示低级烷基等; R 1表示下式的基团：（其中R 11和R 12各自独立地表示氢原子等; m表示整数 2〜6）等; R 2表示低级烷基等; r表示0〜3的整数; k表示0〜4的整数。

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