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公开(公告)号：US07807701B2
公开(公告)日：2010-10-05
申请号：US11939359
申请日：2007-11-13
Applicant: Kimiya Maeda , Hironobu Nagamori , Hiroshi Nakamura , Hisashi Shinkai , Yasunori Suzuki , Daisuke Takahashi , Toshio Taniguchi
Inventor： Kimiya Maeda , Hironobu Nagamori , Hiroshi Nakamura , Hisashi Shinkai , Yasunori Suzuki , Daisuke Takahashi , Toshio Taniguchi
IPC: A61K31/41 , A61K31/42 , C07D257/04 , C07D263/30
CPC classification number: C07D213/74 , C07C229/46 , C07C255/58 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D231/38 , C07D239/42 , C07D249/14 , C07D257/06 , C07D261/14 , C07D263/48 , C07D271/07 , C07D271/10 , C07D275/02
Abstract: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 allyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7)(R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 allyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.
Abstract translation: 由式（1）表示的二苄胺化合物，其中R 1和R 2各自为任选被卤素原子等取代的C 1-6烯丙基; R 3，R 4和R 5各自为氢原子，卤素原子等，或者R 3和R 4可以与其键合的碳原子一起形成任选具有取代基的双环或杂环; A是-N（R 7）（R 8）等; 环B是芳基或杂环残基; R6是氢原子，卤素原子，硝基，C1-6烯丙基等; n为1〜3的整数，其前药及其药学上可接受的盐具有选择性且有效的CETP抑制活性，因此可作为高脂血症或动脉硬化等的治疗剂或预防剂使用。
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公开(公告)号：US07332514B2
公开(公告)日：2008-02-19
申请号：US10503185
申请日：2003-08-29
Applicant: Kimiya Maeda , Hironobu Nagamori , Hiroshi Nakamura , Hisashi Shinkai , Yasunori Suzuki , Daisuke Takahashi , Toshio Taniguchi
Inventor： Kimiya Maeda , Hironobu Nagamori , Hiroshi Nakamura , Hisashi Shinkai , Yasunori Suzuki , Daisuke Takahashi , Toshio Taniguchi
IPC: A61K31/42 , A61K31/41 , C07D263/30 , C07D257/04
CPC classification number: C07D213/74 , C07C229/46 , C07C255/58 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D231/38 , C07D239/42 , C07D249/14 , C07D257/06 , C07D261/14 , C07D263/48 , C07D271/07 , C07D271/10 , C07D275/02
Abstract: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 alkyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7) (R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 alkyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.
Abstract translation: 由式（1）表示的二苄胺化合物，其中R 1和R 2各自为任选被卤素取代的C 1-6烷基 原子等; R 3，R 4和R 5各自为氢原子，卤素原子等，或R 3， SUP>和R 4可以与其键合的碳原子一起形成任选具有取代基的杂环或杂环; A是-N（R 7）（R 8）等; 环B是芳基或杂环残基; R 6是氢原子，卤素原子，硝基，C 1-6烷基等; n为1〜3的整数，其前药及其药学上可接受的盐具有选择性且有效的CETP抑制活性，因此可作为高脂血症或动脉硬化等的治疗剂或预防剂使用。
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公开(公告)号：US08846746B2
公开(公告)日：2014-09-30
申请号：US13599665
申请日：2012-08-30
Applicant: Tomoya Miura , Yosuke Ogoshi , Kazuhito Ueyama , Dai Motoda , Toshihiko Iwayama , Koichi Suzawa , Hironobu Nagamori , Hiroshi Ueno , Akihiko Takahashi , Kazuyuki Sugimoto
Inventor： Tomoya Miura , Yosuke Ogoshi , Kazuhito Ueyama , Dai Motoda , Toshihiko Iwayama , Koichi Suzawa , Hironobu Nagamori , Hiroshi Ueno , Akihiko Takahashi , Kazuyuki Sugimoto
IPC: A01N43/56 , A61K31/415 , C07D405/14 , C07D403/14 , C07D403/12 , C07D409/12 , C07D401/12 , C07D413/12 , C07D405/12
CPC classification number: C07D403/12 , C07D401/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12
Abstract: 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.
Abstract translation: 本发明提供具有SGLT1抑制活性的以下通式[Ib]的吡唑化合物或其药学上可接受的盐，包含其的药物组合物及其药物用途：其中每个符号与描述中定义的相同 。
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公开(公告)号：US20100240634A1
公开(公告)日：2010-09-23
申请号：US12576605
申请日：2009-10-09
Applicant: Takahisa Motomura , Hironobu Nagamori , Koichi Suzawa , Hirotsugu Ito , Toru Morita , Satoru Kobayashi , Hisashi Shinkai
Inventor： Takahisa Motomura , Hironobu Nagamori , Koichi Suzawa , Hirotsugu Ito , Toru Morita , Satoru Kobayashi , Hisashi Shinkai
IPC: A61K31/397 , C07C35/38 , A61K31/045 , C07D231/12 , A61K31/415 , C07D401/12 , A61K31/435 , A61P3/10 , A61P9/10 , A61P9/04 , A61P9/12 , A61P35/00
CPC classification number: C07D205/04 , A61K31/045 , A61K31/05 , A61K31/085 , A61K31/10 , A61K31/121 , A61K31/136 , A61K31/166 , A61K31/167 , A61K31/192 , A61K31/235 , A61K31/277 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4196 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/4523 , A61K31/5375 , C07C35/52 , C07C39/42 , C07C43/23 , C07C43/253 , C07C49/83 , C07C59/56 , C07C59/72 , C07C65/17 , C07C69/712 , C07C69/732 , C07C69/76 , C07C215/44 , C07C215/70 , C07C217/20 , C07C233/18 , C07C233/25 , C07C235/42 , C07C235/66 , C07C255/12 , C07C255/53 , C07C259/10 , C07C271/16 , C07C271/30 , C07C311/04 , C07C317/22 , C07C2603/18 , C07D207/04 , C07D211/06 , C07D213/30 , C07D213/56 , C07D231/12 , C07D239/26 , C07D249/08 , C07D257/04 , C07D263/32 , C07D271/06 , C07D271/10 , C07D275/02 , C07D295/08 , C07D295/18 , C07D295/192 , C07D333/22 , C07D401/06 , C07D401/12 , C07D403/12 , C07F7/081
Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.
Abstract translation: 本发明提供了用于预防或治疗糖尿病，糖尿病并发症，胰岛素抵抗综合征，代谢综合征，高血糖症，血脂异常，动脉粥样硬化，心力衰竭，心肌病，心肌缺血，脑缺血，脑中风，肺动脉高压，高乳酸血症，线粒体 疾病，线粒体性脑病或癌症，即PDHK抑制剂等。 由下式[I]表示的化合物或其药学上可接受的盐或其溶剂化物：其中每个符号如说明书中所定义。
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公开(公告)号：US20080146620A1
公开(公告)日：2008-06-19
申请号：US11939359
申请日：2007-11-13
Applicant: Kimiya Maeda , Hironobu Nagamori , Hiroshi Nakamura , Hisashi Shinkai , Yasunori Suzuki , Daisuke Takahashi , Toshio Taniguchi
Inventor： Kimiya Maeda , Hironobu Nagamori , Hiroshi Nakamura , Hisashi Shinkai , Yasunori Suzuki , Daisuke Takahashi , Toshio Taniguchi
IPC: A61K31/4406 , C07C211/27 , A61K31/136 , C07D257/06 , A61K31/41 , A61P3/06 , A61P3/04 , A61P3/10 , A61P9/10 , A61K31/4184 , C07D277/38 , A61K31/426 , C07D211/56
CPC classification number: C07D213/74 , C07C229/46 , C07C255/58 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D231/38 , C07D239/42 , C07D249/14 , C07D257/06 , C07D261/14 , C07D263/48 , C07D271/07 , C07D271/10 , C07D275/02
Abstract: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 allyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7)(R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 allyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.
Abstract translation: 由式（1）表示的二苄胺化合物，其中R 1和R 2各自为任选被卤素取代的C 1-6 - 烯丙基 原子等; R 3，R 4和R 5各自为氢原子，卤素原子等，或R 3， SUP>和R 4可以与其键合的碳原子一起形成任选具有取代基的杂环或杂环; A是-N（R 7）（R 8）等; 环B是芳基或杂环残基; R 6是氢原子，卤素原子，硝基，C 1-6烯丙基等; n为1〜3的整数，其前药及其药学上可接受的盐具有选择性且有效的CETP抑制活性，因此可作为高脂血症或动脉硬化等的治疗剂或预防剂使用。
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公开(公告)号：US20130085132A1
公开(公告)日：2013-04-04
申请号：US13599665
申请日：2012-08-30
Applicant: Tomoya MIURA , Yosuke OGOSHI , Kazuhito UEYAMA , Dai MOTODA , Toshihiko IWAYAMA , Koichi SUZAWA , Hironobu NAGAMORI , Hiroshi UENO , Akihiko TAKAHASHI , Kazuyuki SUGIMOTO
Inventor： Tomoya MIURA , Yosuke OGOSHI , Kazuhito UEYAMA , Dai MOTODA , Toshihiko IWAYAMA , Koichi SUZAWA , Hironobu NAGAMORI , Hiroshi UENO , Akihiko TAKAHASHI , Kazuyuki SUGIMOTO
IPC: C07D403/12 , C07D405/12 , C07D403/14 , C07D413/12 , C07D409/12 , C07D401/12 , C07D405/14
CPC classification number: C07D403/12 , C07D401/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12
Abstract: 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.
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公开(公告)号：US08343994B2
公开(公告)日：2013-01-01
申请号：US12576605
申请日：2009-10-09
Applicant: Takahisa Motomura , Hironobu Nagamori , Koichi Suzawa , Hirotsugu Ito , Toru Morita , Satoru Kobayashi , Hisashi Shinkai
Inventor： Takahisa Motomura , Hironobu Nagamori , Koichi Suzawa , Hirotsugu Ito , Toru Morita , Satoru Kobayashi , Hisashi Shinkai
IPC: A61K31/44 , C07D221/16
CPC classification number: C07D205/04 , A61K31/045 , A61K31/05 , A61K31/085 , A61K31/10 , A61K31/121 , A61K31/136 , A61K31/166 , A61K31/167 , A61K31/192 , A61K31/235 , A61K31/277 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4196 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/4523 , A61K31/5375 , C07C35/52 , C07C39/42 , C07C43/23 , C07C43/253 , C07C49/83 , C07C59/56 , C07C59/72 , C07C65/17 , C07C69/712 , C07C69/732 , C07C69/76 , C07C215/44 , C07C215/70 , C07C217/20 , C07C233/18 , C07C233/25 , C07C235/42 , C07C235/66 , C07C255/12 , C07C255/53 , C07C259/10 , C07C271/16 , C07C271/30 , C07C311/04 , C07C317/22 , C07C2603/18 , C07D207/04 , C07D211/06 , C07D213/30 , C07D213/56 , C07D231/12 , C07D239/26 , C07D249/08 , C07D257/04 , C07D263/32 , C07D271/06 , C07D271/10 , C07D275/02 , C07D295/08 , C07D295/18 , C07D295/192 , C07D333/22 , C07D401/06 , C07D401/12 , C07D403/12 , C07F7/081
Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.
Abstract translation: 本发明提供了用于预防或治疗糖尿病，糖尿病并发症，胰岛素抵抗综合征，代谢综合征，高血糖症，血脂异常，动脉粥样硬化，心力衰竭，心肌病，心肌缺血，脑缺血，脑中风，肺动脉高压，高乳酸血症，线粒体 疾病，线粒体性脑病或癌症，即PDHK抑制剂等。 由下式[I]表示的化合物或其药学上可接受的盐或其溶剂化物：其中每个符号如说明书中所定义。
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公开(公告)号：US20050059810A1
公开(公告)日：2005-03-17
申请号：US10503185
申请日：2003-08-29
Applicant: Kimiya Maeda , Hironobu Nagamori , Hiroshi Nakamura , Hisashi Shinkai , Yasunori Suzuki , Daisuke Takahashi , Toshio Taniguchi
Inventor： Kimiya Maeda , Hironobu Nagamori , Hiroshi Nakamura , Hisashi Shinkai , Yasunori Suzuki , Daisuke Takahashi , Toshio Taniguchi
IPC: A61P3/04 , A61P3/06 , A61P9/10 , A61P43/00 , C07C229/46 , C07C255/58 , C07D213/74 , C07D231/38 , C07D239/42 , C07D249/14 , C07D257/06 , C07D261/14 , C07D263/48 , C07D271/06 , C07D271/07 , C07D271/10 , C07D275/02 , C07D277/42 , C07F5/00 , C07C211/30 , C07C255/50
CPC classification number: C07D213/74 , C07C229/46 , C07C255/58 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D231/38 , C07D239/42 , C07D249/14 , C07D257/06 , C07D261/14 , C07D263/48 , C07D271/07 , C07D271/10 , C07D275/02
Abstract: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 alkyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7) (R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 alkyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.
Abstract translation: 由式（1）表示的二苄胺化合物，其中R 1和R 2各自为任选被卤素原子等取代的C 1-6烷基; R 3，R 4和R 5各自为氢原子，卤素原子等，或者R 3和R 4可以与其键合的碳原子一起形成稠环或 任选具有取代基的杂环; A是-N（R 7）（R 8）等; 环B是芳基或杂环残基; R 6是氢原子，卤原子，硝基，C 1-6烷基等; n为1〜3的整数，其前药及其药学上可接受的盐具有选择性且有效的CETP抑制活性，因此可作为高脂血症或动脉硬化等的治疗剂或预防剂使用。
