公开(公告)号：US07521430B2

公开(公告)日：2009-04-21

申请号：US10566585

申请日：2004-07-30

申请人： Sumihiro Nomura ,  Toshiaki Sakamoto ,  Kiichiro Ueta

发明人： Sumihiro Nomura ,  Toshiaki Sakamoto ,  Kiichiro Ueta

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H5/06 ,  C07H19/00

CPC分类号： C07H15/203 ,  C07H5/04 ,  C07H17/02

摘要： A compound of the formula: wherein Ring A and Ring B are (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, wherein —NR— group and —CH2— group are both on the same ring of the unsaturated fused heterobicyclic ring, and Ring B is an optionally substituted monocyclic unsaturated heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; and R is a hydrogen atom, a lower alkyl group, a lower alkanoyl group or a lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, or a prodrug thereof.

摘要翻译： 下式的化合物：其中环A和环B是（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选地 取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环，或（3）环A是 任选取代的不饱和稠合杂双环，其中-NR-基和-CH2-基都在不饱和稠合杂双环的相同环上，环B是任选取代的单环不饱和杂环，任选取代的不饱和稠合杂双环 ，或任选取代的苯环; 或其前体药物，R为氢原子，低级烷基，低级烷酰基或低级烷氧基羰基，或其药学上可接受的盐。

公开(公告)号：US20070060545A1

公开(公告)日：2007-03-15

申请号：US10566585

申请日：2004-07-30

申请人： Sumihiro Nomura ,  Toshiaki Sakamoto ,  Kiichiro Ueta

发明人： Sumihiro Nomura ,  Toshiaki Sakamoto ,  Kiichiro Ueta

IPC分类号： A61K31/7008 ,  C07H5/04

CPC分类号： C07H15/203 ,  C07H5/04 ,  C07H17/02

摘要： A compound of the formula: wherein Ring A and Ring B are (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, wherein —NR— group and —CH2— group are both on the same ring of the unsaturated fused heterobicyclic ring, and Ring B is an optionally substituted monocyclic unsaturated heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; and R is a hydrogen atom, a lower alkyl group, a lower alkanoyl group or a lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, or a prodrug thereof.

摘要翻译： 下式的化合物：其中环A和环B是（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的不饱和单环杂环 取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环，或（3）环A是 任选取代的不饱和稠合杂双环，其中-NR-基团和-CH 2 - 基团都在不饱和稠合杂双环环的相同环上，环B是任选取代的单环不饱和杂环 ，任选取代的不饱和稠合杂双环，或任选取代的苯环; 或其前体药物，R为氢原子，低级烷基，低级烷酰基或低级烷氧基羰基，或其药学上可接受的盐。

公开(公告)号：US20120058941A1

公开(公告)日：2012-03-08

申请号：US13174814

申请日：2011-07-01

申请人： Sumihiro NOMURA ,  Eiji Kawanishi ,  Kiichiro Ueta

发明人： Sumihiro NOMURA ,  Eiji Kawanishi ,  Kiichiro Ueta

IPC分类号： A61K31/7034 ,  A61K38/28 ,  A61K38/26 ,  A61P3/10 ,  A61P27/02 ,  A61P25/02 ,  A61P13/12 ,  A61P17/02 ,  A61P5/48 ,  A61P7/00 ,  A61P3/06 ,  A61P3/04 ,  A61P3/00 ,  A61P9/10 ,  A61P9/12 ,  A61P7/02 ,  A61K31/7056

CPC分类号： C07H19/048 ,  A61K45/06 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07H19/06

摘要： A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.

摘要翻译： 下式的化合物：其中环A和环B是：（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环，或 任选取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环或任选取代的不饱和稠环杂双环，或（3）环A是任选取代的不饱和稠合杂双环 环和环B独立地是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环; X是碳原子或氮原子; Y为 - （CH 2）n - （n为1或2）; 或其药学上可接受的盐，或其前药。

公开(公告)号：US07943788B2

公开(公告)日：2011-05-17

申请号：US11045446

申请日：2005-01-31

申请人： Sumihiro Nomura ,  Eiji Kawanishi ,  Kiichiro Ueta

发明人： Sumihiro Nomura ,  Eiji Kawanishi ,  Kiichiro Ueta

IPC分类号： C07D409/00 ,  A01N43/04 ,  C07D277/04 ,  C07D277/08 ,  C07D487/00 ,  C07D257/04 ,  C07D257/10 ,  C07D403/00

CPC分类号： C07H19/048 ,  A61K45/06 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07H19/06

摘要： A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); a pharmaceutically acceptable salt thereof, or a prodrug thereof.

摘要翻译： 下式的化合物：其中环A和环B是：（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环，或 任选取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环或任选取代的不饱和稠环杂双环，或（3）环A是任选取代的不饱和稠合杂双环 环和环B独立地是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环; X是碳原子或氮原子; Y为 - （CH 2）n - （n为1或2）; 其药学上可接受的盐或其前药。

公开(公告)号：US20050233988A1

公开(公告)日：2005-10-20

申请号：US11045446

申请日：2005-01-31

申请人： Sumihiro Nomura ,  Eiji Kawanishi ,  Kiichiro Ueta

发明人： Sumihiro Nomura ,  Eiji Kawanishi ,  Kiichiro Ueta

IPC分类号： A61K31/7072 ,  C07H19/048 ,  C07H19/06

CPC分类号： C07H19/048 ,  A61K45/06 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07H19/06

摘要： A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); a pharmaceutically acceptable salt thereof, or a prodrug thereof.

摘要翻译： 下式的化合物：其中环A和环B是：（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环，或 任选取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环或任选取代的不饱和稠环杂双环，或（3）环A是任选取代的不饱和稠合杂双环 环和环B独立地是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环; X是碳原子或氮原子; Y是 - （CH 2）n - （n是1或2）; 其药学上可接受的盐或其前药。

公开(公告)号：US20110105424A1

公开(公告)日：2011-05-05

申请号：US13005757

申请日：2011-01-13

申请人： Sumihiro NOMURA ,  Eiji Kawanishi ,  Kiichiro Ueta

发明人： Sumihiro NOMURA ,  Eiji Kawanishi ,  Kiichiro Ueta

IPC分类号： A61K31/70 ,  C07H19/00 ,  A61P3/10 ,  A61P17/02 ,  A61P7/00 ,  A61P9/00 ,  A61P3/04

CPC分类号： C07H19/048 ,  A61K45/06 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07H19/06

摘要： A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.

摘要翻译： 下式的化合物：其中环A和环B是：（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环，或 任选取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环或任选取代的不饱和稠环杂双环，或（3）环A是任选取代的不饱和稠合杂双环 环和环B独立地是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环; X是碳原子或氮原子; Y为 - （CH 2）n - （n为1或2）; 或其药学上可接受的盐，或其前药。

公开(公告)号：US08785403B2

公开(公告)日：2014-07-22

申请号：US13494602

申请日：2012-06-12

申请人： Sumihiro Nomura ,  Eiji Kawanishi ,  Kiichiro Ueta

发明人： Sumihiro Nomura ,  Eiji Kawanishi ,  Kiichiro Ueta

IPC分类号： C07H5/02 ,  A01N43/04 ,  A61K31/70

CPC分类号： C07H19/056 ,  A61K31/7042 ,  A61K31/7056 ,  A61K38/24 ,  A61K38/28 ,  A61K45/06 ,  C07H7/04 ,  C07H7/06 ,  C07H19/04 ,  C07H19/044 ,  C07H19/048 ,  A61K2300/00

摘要： A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.

摘要翻译： 下式的化合物：其中环A和环B是：（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环，或 任选取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环或任选取代的不饱和稠环杂双环，或（3）环A是任选取代的不饱和稠合杂双环 环和环B独立地是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环; X是碳原子或氮原子; Y为 - （CH 2）n - （n为1或2）; 或其药学上可接受的盐，或其前药。

公开(公告)号：US08222219B2

公开(公告)日：2012-07-17

申请号：US13174814

申请日：2011-07-01

申请人： Sumihiro Nomura ,  Eiji Kawanishi ,  Kiichiro Ueta

发明人： Sumihiro Nomura ,  Eiji Kawanishi ,  Kiichiro Ueta

IPC分类号： A01N43/04 ,  A61K31/70

CPC分类号： C07H19/048 ,  A61K45/06 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07H19/06

摘要： A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.

公开(公告)号：US08202984B2

公开(公告)日：2012-06-19

申请号：US13005757

申请日：2011-01-13

申请人： Sumihiro Nomura ,  Eiji Kawanishi ,  Kiichiro Ueta

发明人： Sumihiro Nomura ,  Eiji Kawanishi ,  Kiichiro Ueta

IPC分类号： C07H19/00 ,  C07H19/22 ,  C07H19/048 ,  C07H19/056 ,  A01N43/04 ,  A61K31/70 ,  C07H19/06

CPC分类号： C07H19/048 ,  A61K45/06 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07H19/06

摘要： A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.

摘要翻译： 下式的化合物：其中环A和环B是：（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环，或 任选取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环或任选取代的不饱和稠环杂双环，或（3）环A是任选取代的不饱和稠合杂双环 环和环B独立地是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环; X是碳原子或氮原子; Y为 - （CH 2）n - （n为1或2）; 或其药学上可接受的盐，或其前药。

公开(公告)号：US08853385B2

公开(公告)日：2014-10-07

申请号：US12863429

申请日：2009-01-16

申请人： Kiichiro Ueta ,  Kenji Arakawa ,  Yasuaki Matsushita

发明人： Kiichiro Ueta ,  Kenji Arakawa ,  Yasuaki Matsushita

IPC分类号： C07H7/04

CPC分类号： A61K31/706 ,  A61K31/40 ,  A61K31/401 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/7004 ,  A61K31/7008 ,  A61K31/7034 ,  A61K31/7056 ,  A61K45/06 ,  C07H7/04 ,  A61K2300/00

摘要： The present invention relates to combination therapy comprising a DPP4 inhibitor and an SGLT inhibitor. The combination of the present invention leads to increase plasma GLP-1 level and the combination is useful for prevention or treatment of conditions such as diabetes and diseases related to diabetes.

摘要翻译： 本发明涉及包含DPP4抑制剂和SGLT抑制剂的组合疗法。 本发明的组合导致血浆GLP-1水平升高，并且该组合可用于预防或治疗诸如糖尿病和与糖尿病相关的疾病的病症。