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1. 发明授权

US08138197B2 Spirochromanon derivatives 有权
标题翻译：螺二色素衍生物
公开(公告)号：US08138197B2
公开(公告)日：2012-03-20
申请号：US12518466
申请日：2008-01-08
申请人： Tomoharu Iino , Hideki Jona , Hideki Kurihara , Masayuki Nakamura , Kenji Niiyama , Jun Shibata , Tadashi Shimamura , Hitomi Watanabe , Takeru Yamakawa , Lihu Yang
发明人： Tomoharu Iino , Hideki Jona , Hideki Kurihara , Masayuki Nakamura , Kenji Niiyama , Jun Shibata , Tadashi Shimamura , Hitomi Watanabe , Takeru Yamakawa , Lihu Yang
IPC分类号： A61K31/438 , C07D221/20
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-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[ 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-a]吡啶，其具有Ar 2，并且任选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-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。

2. 发明申请

US20090270436A1 SPIROCHROMANON DERIVATIVES 有权
标题翻译：螺吡喃衍生物
公开(公告)号：US20090270436A1
公开(公告)日：2009-10-29
申请号：US12518466
申请日：2008-01-08
申请人： Tomoharu Iino , Hideki Jona , Hideki Kurihara , Masayuki Nakamura , Kenji Niiyama , Jun Shibata , Tadashi Shimamura , Hitomi Watanabe , Takeru Yamakawa , Lihu Yang
发明人： Tomoharu Iino , Hideki Jona , Hideki Kurihara , Masayuki Nakamura , Kenji Niiyama , Jun Shibata , Tadashi Shimamura , Hitomi Watanabe , Takeru Yamakawa , Lihu Yang
IPC分类号： A61K31/438 , C07D401/14 , A61P3/00 , A61P35/00 , A61P31/00
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 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[ 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[ 具有Ar 2且任选具有一个或两个以上选自R 3：R 1和R 2的取代基的3,4-b]吡啶各自独立地表示氢原子，卤素原子，氰基，C 2 -C 6烯基， C1-C6烷氧基，C2-C7烷酰基，C2-C7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; 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机组; 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

US20090131464A1 SPIROCHROMANONE DERIVATIVES AS ACETYL COENZYME A CARBOXYLASE (ACC) INHIBITORS 有权
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：US20090131464A1
公开(公告)日：2009-05-21
申请号：US11988588
申请日：2006-07-14
申请人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
发明人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
IPC分类号： A61K31/438 , A61P3/00
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. 发明授权

US07410976B2 Spirochromanone derivatives 有权
标题翻译：螺二色酮衍生物
公开(公告)号：US07410976B2
公开(公告)日：2008-08-12
申请号：US11487029
申请日：2006-07-14
申请人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
发明人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
IPC分类号： A61K31/438 , C07D491/107
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。

5. 发明授权

US07935712B2 Spirochromanone derivatives as acetyl coenzyme A carboxylase (ACC) inhibitors 有权
标题翻译：螺吡色酮衍生物作为乙酰辅酶A羧化酶（ACC）抑制剂
公开(公告)号：US07935712B2
公开(公告)日：2011-05-03
申请号：US11988588
申请日：2006-07-14
申请人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
发明人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
IPC分类号： A01N43/42 , A61K31/44 , A61K31/535
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。

6. 发明申请

US20070021453A1 Novel spirochromanone derivatives 有权
标题翻译：新型螺二色酮衍生物
公开(公告)号：US20070021453A1
公开(公告)日：2007-01-25
申请号：US11487029
申请日：2006-07-14
申请人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
发明人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
IPC分类号： A61K31/4747 , C07D471/14
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。

7. 发明授权

US08093389B2 Substituted spirochromanone derivatives 有权
标题翻译：取代的螺二氢茚酮衍生物
公开(公告)号：US08093389B2
公开(公告)日：2012-01-10
申请号：US12007000
申请日：2008-01-08
申请人： Tomoharu Iino , Hideki Jona , Jun Shibata , Tadashi Shimamura , Takeru Yamakawa , Lihu Yang
发明人： Tomoharu Iino , Hideki Jona , Jun Shibata , Tadashi Shimamura , Takeru Yamakawa , Lihu Yang
IPC分类号： C07D413/06 , C07D405/04 , A61K31/438
CPC分类号： C07D519/00 , C07D491/10
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 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.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar1表示由选自吲哚，1H-吲唑，2H-吲唑，1H-噻吩并[2,3-c]所示的芳环形成的基团，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-C 1 -C 6烷氧基，环-C 3 -C 6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，环-C3-C6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烯基或-Q1-N（Ra）-Q2-Rb的基团; 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C 1 -C 6烷基或环-C 3 -C 6烷基取代的氨基甲酰基，或者 -N（R f）R f; 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。

8. 发明申请

US20080171761A1 Substituted spirochromanone derivatives 有权
公开(公告)号：US20080171761A1
公开(公告)日：2008-07-17
申请号：US12007000
申请日：2008-01-08
申请人： Tomoharu Iino , Hideki Jona , Jun Shibata , Tadashi Shimamura , Takeru Yamakawa , Lihu Yang
发明人： Tomoharu Iino , Hideki Jona , Jun Shibata , Tadashi Shimamura , Takeru Yamakawa , Lihu Yang
IPC分类号： C07D491/107 , 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 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.

9. 发明申请

US20110319396A1 BENZODIAZEPIN-2-ON DERIVATIVES 审中-公开
标题翻译：苯并咪唑-2-酮衍生物
公开(公告)号：US20110319396A1
公开(公告)日：2011-12-29
申请号：US13142005
申请日：2010-01-19
申请人： Masanori Asai , Tasuku Haketa , Seiichi Inamura , Makoto Ishikawa , Hideki Jona , Hiroshi Kawamoto , Hideki Kurihara , Jun Shibata , Tadashi Shimamura , Takuya Suga , Hitomi Watanabe
发明人： Masanori Asai , Tasuku Haketa , Seiichi Inamura , Makoto Ishikawa , Hideki Jona , Hiroshi Kawamoto , Hideki Kurihara , Jun Shibata , Tadashi Shimamura , Takuya Suga , Hitomi Watanabe
IPC分类号： A61K31/5513 , C07D401/12 , C07D417/12 , A61P3/04 , C07D409/12 , A61P3/06 , A61P3/10 , C07D243/14 , C07D403/12
CPC分类号： C07D243/12 , A61K31/551 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
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.
摘要翻译：本发明涉及由式（I）表示的化合物：其中R1表示氢原子等; R2代表低级烷基等; R3和R4表示低级烷基等; R5表示苯基等; R6表示氢原子等; m为0〜2的整数; p是1至4的整数; 和q为1〜5的整数，或其药学上可接受的盐和包含该化合物的DGAT 1抑制剂。

10. 发明申请

US20110065739A1 NOVEL ISOXAZOLE DRIVATIVE 审中-公开
标题翻译：新的异丙唑驱动剂
公开(公告)号：US20110065739A1
公开(公告)日：2011-03-17
申请号：US12992387
申请日：2009-05-28
申请人： Makoto Ishikawa , Tasuku Haketa , Chisato Nakama , Teruyuki Nishimura , Jun Shibata , Tadashi Shimamura , Takeru Yamakawa
发明人： Makoto Ishikawa , Tasuku Haketa , Chisato Nakama , Teruyuki Nishimura , Jun Shibata , Tadashi Shimamura , Takeru Yamakawa
IPC分类号： A61K31/506 , C07D261/12 , A61K31/42 , A61P3/10 , A61P3/04 , A61P3/06 , C07D413/04 , A61K31/4439
CPC分类号： C07D261/12 , C07D413/04 , C07D413/12
摘要： Disclosed is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, which has an agonistic activity on GPR120 and is therefore useful for the treatment of diabetes, obesity or hyperlipemia. [In formula (I), the A represents a phenyl group which may be substituted by a lower alkoxy group or the like; the 13 represents a bivalent group produced by removing two hydrogen atoms from a benzene ring which may be substituted by a halogen atom or the like; X represents a lower alkylene group having 2 to 4 carbon atoms in its main chain or the like, wherein a carbon atom constituting the main chain may be substituted by an oxygen atom or the like; and Y represents a hydrogen atom or the like.]
摘要翻译：公开了由式（I）表示的化合物或其药学上可接受的盐，其对GPR120具有激动作用，因此可用于治疗糖尿病，肥胖症或高脂血症。 [式（I）中，A表示可被低级烷氧基等取代的苯基， 13表示通过从可被卤素原子等取代的苯环除去2个氢原子而生成的二价基团; X表示其主链等中具有2〜4个碳原子的低级亚烷基，其中构成主链的碳原子可以被氧原子等取代; Y表示氢原子等。]

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