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1. 发明授权

US08609699B2 Oxotetrahydrofuran-2-yl-benzimidazole derivative 有权
标题翻译：氧四氢呋喃-2-基 - 苯并咪唑衍生物
公开(公告)号：US08609699B2
公开(公告)日：2013-12-17
申请号：US13059307
申请日：2009-08-03
申请人： Tomoharu Iino , Masanori Asai , Akio Ohno , Seiichi Inamura , Makoto Ishikawa , Norikazu Ohtake
发明人： Tomoharu Iino , Masanori Asai , Akio Ohno , Seiichi Inamura , Makoto Ishikawa , Norikazu Ohtake
IPC分类号： A61K31/4439 , C07D401/14
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

US20110144162A1 OXOTETRAHYDROFURAN-2-YL-BENZIMIDAZOLE DERIVATIVE 有权
标题翻译：氧自由基2-YL-苯并咪唑衍生物
公开(公告)号：US20110144162A1
公开(公告)日：2011-06-16
申请号：US13059307
申请日：2009-08-03
申请人： Tomoharu Iino , Masanori Asai , Akio Ohno , Seiichi Inamura , Makoto Ishikawa , Norikazu Ohtake
发明人： Tomoharu Iino , Masanori Asai , Akio Ohno , Seiichi Inamura , Makoto Ishikawa , Norikazu Ohtake
IPC分类号： A61K31/444 , C07D401/14 , A61K31/4439 , A61P3/10
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。

3. 发明授权

US08232284B2 Heteroaryloxy quinazoline derivative 有权
标题翻译：杂芳氧基喹唑啉衍生物
公开(公告)号：US08232284B2
公开(公告)日：2012-07-31
申请号：US12742113
申请日：2008-11-10
申请人： Tomoharu Iino , Akio Ohno , Norikazu Otake , Takuya Suga , Masanori Asai
发明人： Tomoharu Iino , Akio Ohno , Norikazu Otake , Takuya Suga , Masanori Asai
IPC分类号： A61K31/517
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.; 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).
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其具有葡糖激酶活化的作用，并且可用于治疗糖尿病，肥胖症等的药物领域（其中环A表示任选具有较低的烷基等;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; R2表示低级烷基等; r表示0〜3的整数，k表示0〜4的整数）。

4. 发明申请

US20100249146A1 HETEROARYLOXY QUINAZOLINE DERIVATIVE 有权
标题翻译：杂环喹啉衍生物
公开(公告)号：US20100249146A1
公开(公告)日：2010-09-30
申请号：US12742113
申请日：2008-11-10
申请人： Tomoharu Iino , Akio Ohno , Norikazu Otake , Takuya Suga , Masanori Asia
发明人： Tomoharu Iino , Akio Ohno , Norikazu Otake , Takuya Suga , Masanori Asia
IPC分类号： A61K31/517 , C07D401/14 , C07D403/14 , A61P3/10
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.; 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).
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其具有葡糖激酶活化的作用，并且可用于治疗糖尿病，肥胖症等的药物领域（其中环A表示任选具有较低的烷基等;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; R2表示低级烷基等; r表示0〜3的整数，k表示0〜4的整数）。

5. 发明授权

US07432287B2 Heteroarylcarbamoylbenzene derivative 有权
标题翻译：杂芳基氨基甲酰基苯衍生物
公开(公告)号：US07432287B2
公开(公告)日：2008-10-07
申请号：US10546962
申请日：2004-02-26
申请人： Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K31/4439 , A61K31/4155 , C07D401/10 , C07D231/40
CPC分类号： C07D213/75 , C07D231/40 , C07D237/20 , C07D239/42 , C07D241/20 , C07D249/04 , C07D261/14 , C07D271/07 , C07D275/03 , C07D277/18 , C07D277/46 , C07D277/60 , C07D277/82 , C07D285/08 , C07D285/10 , C07D285/135 , C07D401/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D513/04
摘要： Compounds represented by formula (I): as well as their pharmaceutically acceptable salts are disclosed. The compounds are useful as glucokinase activating agents for the treatment of diabetes and related conditions. Compositions and methods of treatment are also included.
摘要翻译：公开了由式（I）表示的化合物及其药学上可接受的盐。该化合物可用作糖尿病治疗和相关病症的葡糖激酶活化剂。还包括组合物和治疗方法。

6. 发明申请

US20090018056A1 Heteroarylcarbamoylbenzene derivatives 有权
标题翻译：杂芳基氨基甲酰基苯衍生物
公开(公告)号：US20090018056A1
公开(公告)日：2009-01-15
申请号：US12231856
申请日：2008-09-05
申请人： Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K38/28 , C07D277/28 , C07D241/10 , C07D239/28 , C07D261/14 , A61K31/426 , A61K31/495 , A61K31/433 , A61K31/4439 , A61P3/10 , A61K31/501 , A61K31/4365 , A61K31/42 , A61K31/4965 , C07D285/08 , C07D471/04 , C07D401/10 , C07D403/10
CPC分类号： C07D213/75 , C07D231/40 , C07D237/20 , C07D239/42 , C07D241/20 , C07D249/04 , C07D261/14 , C07D271/07 , C07D275/03 , C07D277/18 , C07D277/46 , C07D277/60 , C07D277/82 , C07D285/08 , C07D285/10 , C07D285/135 , C07D401/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D513/04
摘要： Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): [wherein X1 represents oxygen, etc., X2 represents oxygen, etc., R1 represents a group on Ring A such as alkylsulfonyl, etc., R2 represents C3-7 cyclic alkyl optionally substituted with a halogen, etc., R3 represents a substituent on Ring B such as lower alkyl, etc., formula (II): [Chemical Formula 1] represents 6- to 10-membered aryl, etc., and formula (III): [Formula 1] represents monocyclic or bicyclic heteroaryl optionally having on Ring B a substituent represented by R3 above, wherein the carbon atom of Ring B which is bonded to the nitrogen atom of the amide group of formula (I) forms a C═N bond with the nitrogen atom of the ring], as well as their pharmaceutically acceptable salts.
摘要翻译：具有葡糖激酶活化作用的化合物，可用作由下式（I）表示的糖尿病治疗：[其中X1表示氧等，X2表示氧等，R1表示环A上的基团，例如烷基磺酰基等等，R 2表示任选被卤素取代的C 3-7环烷基等，R 3表示环B上的取代基，例如低级烷基等，式（II）：[化学式1]表示6-至10 （III）表示：[式1]表示在环B上任选具有由上述R 3表示的取代基的单环或双环杂芳基，其中键合到氮原子上的环B的碳原子式（I）的酰胺基与环的氮原子形成CN键，以及它们的药学上可接受的盐。

7. 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。

8. 发明授权

US07253188B2 Aminobenzamide derivative 失效
标题翻译：氨基苯甲酰胺衍生物
公开(公告)号：US07253188B2
公开(公告)日：2007-08-07
申请号：US10952471
申请日：2004-09-27
申请人： Teruyuki Nishimura , Tomoharu Iino , Yasufumi Nagata , Jun-ichi Eiki
发明人： Teruyuki Nishimura , Tomoharu Iino , Yasufumi Nagata , Jun-ichi Eiki
IPC分类号： C07D401/12 , C07D401/14 , A61K31/4427 , A61K31/506 , A61K31/5377 , A61P3/04 , A61P3/10 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , A61K31/47 , A61K31/497 , A61K31/501
CPC分类号： C07D401/12 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/506 , C07D277/46 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/04
摘要： This invention relates to a novel compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is —S(O)p-A, —S—(O)q-B or —O-D, wherein p and q, which are the same or different, each represent an integer from 0 to 2, A is a straight chain C1-C10 alkyl group which may be substituted by R10, and B and D each independently represent R12 which may be substituted by R10; R2 is a hydrogen atom, a halogen atom, or a straight chain or branched C1-C6 alkyl group which may be substituted by R10; X1 and X2 each independently represent N or CH, but cannot both be N; the formula (II): shows a monocyclic or bicyclic heteroaryl group which has a nitrogen atom adjacent to the carbon atom bonded to the amide group, and the heteroaryl group may be substituted by R10; R10 is R11, or a hydrocarbon group which may be substituted by R11; R11 is, for example, a hydrogen atom or amino; and R12 is, for example, phenyl, thiazolyl, pyridyl or methylene dioxyphenyl. The compound according to this invention has a glucokinase activation effect, and for example, is useful in the treatment and prevention of diabetes mellitus, and in the prevention of its complications such as diabetic nephropathy, diabetic retinopathy, diabetic neuropathy and diabetic arteriosclerosis.
摘要翻译：本发明涉及由式（I）表示的新化合物或其药学上可接受的盐，其中R 1是-S（O）p A，-S-（O）qB或-OD 其中相同或不同的p和q各自表示0至2的整数，A是可以被R 10取代的直链C 1 -C 10烷基，B和 D各自独立地表示可被R 10取代的R 12， R 2是氢原子，卤素原子或可被R 10取代的直链或支链C 1 -C 6烷基; X 1和X 2各自独立地表示N或CH，但不能都是N; 式（II）表示具有与结合到酰胺基上的碳原子相邻的氮原子的单环或双环杂芳基，杂芳基可以被R 10取代; R 10是R 11，或可被R 11取代的烃基; R 11是例如氢原子或氨基; R 12是例如苯基，噻唑基，吡啶基或亚甲基二氧苯基。根据本发明的化合物具有葡糖激酶活化作用，例如可用于治疗和预防糖尿病，并且可用于预防其并发症如糖尿病性肾病，糖尿病性视网膜病，糖尿病性神经病和糖尿病性动脉硬化。

9. 发明授权

US06608098B1 Isoindole derivatives 失效
标题翻译：异吲哚衍生物
公开(公告)号：US06608098B1
公开(公告)日：2003-08-19
申请号：US10069376
申请日：2002-02-25
申请人： Toshio Nagase , Tomoharu Iino , Yoshiyuki Sato , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Toshio Nagase , Tomoharu Iino , Yoshiyuki Sato , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K31403
CPC分类号： C07D498/04
摘要： This invention relates to compounds represented by the general formula [I] wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及由通式[I]表示的化合物，其中R表示叠氮基等，R 1和R 2相同或不同，表示氢原子等，R 3和R 4相同或不同，表示氢原子等，X1表示氧原子等，X2表示氧原子等，Y表示氧原子等，Z表示缩合芳基等，或其药学上可接受的盐，其制备方法和糖尿病治疗剂，用于糖尿病慢性并发症的预防剂或抗肥胖药物，含有作为有效成分的化合物或其药学上可接受的盐。

10. 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。

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