公开(公告)号：US09278944B2

公开(公告)日：2016-03-08

申请号：US14005512

申请日：2012-03-15

申请人： Toru Iijima ,  Hiroshi Sugama ,  Takayuki Kawaguchi ,  Jingkang Shen ,  Guangxin Xia ,  Jianshu Xie ,  Miki Hirai

发明人： Toru Iijima ,  Hiroshi Sugama ,  Takayuki Kawaguchi ,  Jingkang Shen ,  Guangxin Xia ,  Jianshu Xie ,  Miki Hirai

IPC分类号： C07D241/36 ,  C07D265/30 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D231/56

CPC分类号： C07D265/30 ,  C07D231/56 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

摘要： The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.

摘要翻译： 本发明提供式[I]的含氮饱和杂环化合物：其中R 1为环烷基等，R 22为任意取代的芳基等，R为低级烷基等，T为 羰基，Z为-O-等，R3〜R6相同或不同，为氢原子等; 或药学上可接受的盐，其可用作肾素抑制剂。

公开(公告)号：US08975252B2

公开(公告)日：2015-03-10

申请号：US12664637

申请日：2008-06-16

申请人： Hidenori Akatsuka ,  Hiroshi Sugama ,  Nobumasa Awai ,  Takayuki Kawaguchi ,  Yoichi Takahashi ,  Toru Iijima ,  Jingkang Shen ,  Guangxin Xia ,  Jianshu Xie

发明人： Hidenori Akatsuka ,  Hiroshi Sugama ,  Nobumasa Awai ,  Takayuki Kawaguchi ,  Yoichi Takahashi ,  Toru Iijima ,  Jingkang Shen ,  Guangxin Xia ,  Jianshu Xie

IPC分类号： A61K31/535 ,  C07D265/30 ,  C07D209/08 ,  C07D209/14 ,  C07D209/30 ,  C07D209/34 ,  C07D209/42 ,  C07D231/56 ,  C07D265/36 ,  C07D403/04 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

CPC分类号： C07D265/30 ,  C07D209/08 ,  C07D209/14 ,  C07D209/30 ,  C07D209/34 ,  C07D209/42 ,  C07D231/56 ,  C07D265/36 ,  C07D403/04 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： The present invention provides a morpholine derivative of the formula [I]; wherein R1 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, a cycloalkyl group or an alkyl group; R2 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, an optionally substituted alkylcarbonyl group, an optionally substituted arylcarbonyl group, an optionally substituted heterocyclo-substituted carbonyl group or a cycloalkylcarbonyl group; T is a methylene group or a carbonyl group; R3, R4, R5 and R6 are the same or different and a hydrogen atom, an optionally substituted carbamoyl group or an optionally substituted alkyl group; or pharmaceutically acceptable salts thereof. These compounds are useful as a renin inhibitor.

摘要翻译： 本发明提供式[I]的吗啉衍生物。 其中R1是取代的烷基，任选取代的芳基，任选取代的杂环基，环烷基或烷基; R 2是取代的烷基，任选取代的芳基，任选取代的杂环基，任选取代的烷基羰基，任选取代的芳基羰基，任选取代的杂环取代的羰基或环烷基羰基; T是亚甲基或羰基; R3，R4，R5和R6相同或不同，氢原子，任选取代的氨基甲酰基或任选取代的烷基; 或其药学上可接受的盐。 这些化合物可用作肾素抑制剂。

公开(公告)号：US20100240644A1

公开(公告)日：2010-09-23

申请号：US12664637

申请日：2008-06-16

申请人： Hidenori Akatsuka ,  Hiroshi Sugama ,  Nobumasa Awai ,  Takayuki Kawaguchi ,  Yoichi Takahashi ,  Toru Iijima ,  Jingkang Shen ,  Guangxin Xia ,  Jianshu Xie

发明人： Hidenori Akatsuka ,  Hiroshi Sugama ,  Nobumasa Awai ,  Takayuki Kawaguchi ,  Yoichi Takahashi ,  Toru Iijima ,  Jingkang Shen ,  Guangxin Xia ,  Jianshu Xie

IPC分类号： A61K31/538 ,  C07D265/30 ,  A61K31/5375 ,  C07D265/36 ,  C07D413/12 ,  A61K31/5377 ,  C07D409/12 ,  A61K31/5355 ,  A61P9/12

CPC分类号： C07D265/30 ,  C07D209/08 ,  C07D209/14 ,  C07D209/30 ,  C07D209/34 ,  C07D209/42 ,  C07D231/56 ,  C07D265/36 ,  C07D403/04 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： The present invention provides a morpholine derivative of the formula [I]; wherein R1 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, a cycloalkyl group or an alkyl group; R2 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, an optionally substituted alkylcarbonyl group, an optionally substituted arylcarbonyl group, an optionally substituted heterocyclo-substituted carbonyl group or a cycloalkylcarbonyl group; T is a methylene group or a carbonyl group; R3, R4, R5 and R6 are the same or different and a hydrogen atom, an optionally substituted carbamoyl group or an optionally substituted alkyl group; or pharmaceutically acceptable salts thereof. These compounds are useful as a renin inhibitor.

摘要翻译： 本发明提供式[I]的吗啉衍生物。 其中R1是取代的烷基，任选取代的芳基，任选取代的杂环基，环烷基或烷基; R 2是取代的烷基，任选取代的芳基，任选取代的杂环基，任选取代的烷基羰基，任选取代的芳基羰基，任选取代的杂环取代的羰基或环烷基羰基; T是亚甲基或羰基; R3，R4，R5和R6相同或不同，氢原子，任选取代的氨基甲酰基或任选取代的烷基; 或其药学上可接受的盐。 这些化合物可用作肾素抑制剂。

公开(公告)号：US20140011807A1

公开(公告)日：2014-01-09

申请号：US14005512

申请日：2012-03-15

申请人： Toru Iijima ,  Hiroshi Sugama ,  Takayuki Kawaguchi ,  Jingkang Shen ,  Guangxin Xia ,  Jianshu Xie

发明人： Toru Iijima ,  Hiroshi Sugama ,  Takayuki Kawaguchi ,  Jingkang Shen ,  Guangxin Xia ,  Jianshu Xie

IPC分类号： C07D265/30 ,  C07D403/12 ,  C07D231/56 ,  C07D413/14 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

CPC分类号： C07D265/30 ,  C07D231/56 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

摘要： The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.

摘要翻译： 本发明提供式[I]的含氮饱和杂环化合物：其中R 1为环烷基等，R 22为任意取代的芳基等，R为低级烷基等，T为 羰基，Z为-O-等，R3〜R6相同或不同，为氢原子等; 或药学上可接受的盐，其可用作肾素抑制剂。

公开(公告)号：US08188073B2

公开(公告)日：2012-05-29

申请号：US13167986

申请日：2011-06-24

申请人： Toru Iijima ,  Yasuo Yamamoto ,  Hidenori Akatsuka ,  Takayuki Kawaguchi

发明人： Toru Iijima ,  Yasuo Yamamoto ,  Hidenori Akatsuka ,  Takayuki Kawaguchi

IPC分类号： C07D279/16 ,  A61K31/5415

CPC分类号： C07D265/36 ,  C07D279/16 ,  C07D413/04

摘要： The present invention relates to a compound, useful as a mineralocorticoid receptor-modulating agent, of the following formula [I]: wherein Ring A is a benzene ring optionally having a substituent(s) other than R1 etc, R1 is a group of the formula: RaSO2NH— etc, Ra is an alkyl group etc, R2 and R3 are each a hydrogen atom, a phenyl group, an optionally substituted alkyl group etc, X is an oxygen atom etc, Y is a group of the formula: —C(═O)— etc, Ar is an optionally substituted aryl group or an optionally substituted heteroaryl group, Q is a single bond, an alkylene group etc, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及可用作以下式[I]的盐皮质激素受体调节剂的化合物：其中环A为任选具有除R1等以外的取代基的苯环，R1为 式：R a SO 2 NH-等，R a为烷基等，R 2和R 3各自为氢原子，苯基，任意取代的烷基等，X为氧原子等，Y为下式基团-C （= O） - 等，Ar为任选取代的芳基或任选取代的杂芳基，Q为单键，亚烷基等，或其药学上可接受的盐。

公开(公告)号：US20060094724A1

公开(公告)日：2006-05-04

申请号：US10540878

申请日：2004-01-08

申请人： Takayuki Kawaguchi ,  Hidenori Akatsuka ,  Toru Iijima ,  Tatsuya Watanabe ,  Jun Murakami ,  Takashi Mitsui

发明人： Takayuki Kawaguchi ,  Hidenori Akatsuka ,  Toru Iijima ,  Tatsuya Watanabe ,  Jun Murakami ,  Takashi Mitsui

IPC分类号： A61K31/498 ,  A61K31/4741 ,  C07D491/02

CPC分类号： C07D491/04 ,  C07D213/75

摘要： The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and, R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.

摘要翻译： 本发明提供式（I）的缩合呋喃化合物：其中环X为苯，吡啶等; Y是任选取代的氨基，任选取代的环烷基，任选取代的芳基，任选取代的饱和杂环基，任选取代的不饱和杂环基; A是单键，低级亚烷基，低级亚烯基，低级亚烯基或氧原子; R 3是氢等; 和R 4是氢等，或其药学上可接受的盐，其可用作药物，特别是作为活化凝血因子X抑制剂。

公开(公告)号：US08258131B2

公开(公告)日：2012-09-04

申请号：US12671479

申请日：2008-07-21

申请人： Yoichi Takahashi ,  Nobumasa Awai ,  Hidenori Akatsuka ,  Takayuki Kawaguchi ,  Toru Iijima

发明人： Yoichi Takahashi ,  Nobumasa Awai ,  Hidenori Akatsuka ,  Takayuki Kawaguchi ,  Toru Iijima

IPC分类号： C07D265/16 ,  A61K31/352 ,  A61K31/353

CPC分类号： C07D265/16 ,  C07D311/20 ,  C07D311/58 ,  C07D311/96 ,  C07D405/14 ,  C07D413/04

摘要： The present invention provides a novel fused bicyclic compound having an affinity to a receptor of mineral corticoid (MR), shown by the formula [I]: wherein the ring A is a benzene ring having a substituent R1, fused to an adjacent 6-membered heterocyclic ring and further optionally having a substituent(s) other than R1, R1 is an alkylsulfonylamino group etc., R2 and R3 are (a) the same of different and a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group, (b) combined each other to form an oxo group or (c) combined each other at its terminal together with the adjacent carbon atom to form a cycloalkyl group, X is a group of ═N—, ═C(R4)— or —CH(R4)—, R4 is (a) a hydrogen atom, (b) a cyano group, (c) a halogen atom, (d) an alkyl group, (e) an alkenyl group, (f) a cycloalkyl group (g) an alkanoyl group, (h) a carbamoyl group or (i) a cycloalkenyl group, Ar is an optionally substituted aromatic cyclic group and a dotted line means presence or absence of a double bond, or a pharmaceutically acceptable salt thereof, which is useful as an antihypertensive agent etc.

摘要翻译： 本发明提供了对式[I]所示的对矿物质类皮质激素（MR）的受体具有亲和性的新的稠合双环化合物：其中环A是具有取代基R 1的苯环，与相邻的6元 杂环，并且还可任选地具有除R1以外的取代基，R 1是烷基磺酰基氨基等，R 2和R 3是（a）不同的，和氢原子，烷基或取代或未取代的芳基， （b）彼此组合以形成氧代基团，或（c）在其末端与相邻的碳原子一起相互结合形成环烷基，X是一个= N - ， - C（R 4） - 或 - CH（R4） - ，R4是（a）氢原子，（b）氰基，（c）卤原子，（d）烷基，（e）烯基，（f）环烷基 g）烷酰基，（h）氨基甲酰基或（i）环烯基，Ar是任选取代的芳环基，虚线表示存在或不存在 双键或其药学上可接受的盐，其可用作抗高血压剂等。

公开(公告)号：US07605158B2

公开(公告)日：2009-10-20

申请号：US10571904

申请日：2004-09-24

申请人： Takayuki Kawaguchi ,  Hidenori Akatsuka ,  Masamichi Morimoto ,  Tatsuya Watanabe ,  Toru Iijima ,  Jun Murakami

发明人： Takayuki Kawaguchi ,  Hidenori Akatsuka ,  Masamichi Morimoto ,  Tatsuya Watanabe ,  Toru Iijima ,  Jun Murakami

IPC分类号： A61K31/5355 ,  A61K31/443 ,  C07D413/04 ,  C07D401/12 ,  C07D307/85

CPC分类号： C07D405/12 ,  C07D405/14

摘要： The present invention provides a carbamoyl-type benzofuran derivative of the formula [1]: wherein Ring Z is a group of the formula: etc.; A is a single bond, and the like; Y is a cycloalkanediyl group, etc.; R4 and R5 are the same or different and each is an optionally substituted lower alkyl group, etc.; R1 is a halogen atom, etc.; Ring B of the formula: is an optionally substituted benzene ring; and R3 is a hydrogen atom. etc., or a pharmaceutically acceptable salt thereof, which is useful as an FXa inhibitor.

摘要翻译： 本发明提供式[1]的氨基甲酰基型苯并呋喃衍生物：其中环Z是下式的基团：等等; A是单键等; Y是环烷二基等; R4和R5相同或不同，各自为任选取代的低级烷基等; R1是卤素原子等; 下式的环B是任选取代的苯环; R3为氢原子。 等等，或其药学上可接受的盐，其可用作FXa抑制剂。

公开(公告)号：US07737161B2

公开(公告)日：2010-06-15

申请号：US12320583

申请日：2009-01-29

申请人： Takayuki Kawaguchi ,  Hidenori Akatsuka ,  Toru Iijima ,  Tatsuya Watanabe ,  Jun Murakami ,  Takashi Mitsui

发明人： Takayuki Kawaguchi ,  Hidenori Akatsuka ,  Toru Iijima ,  Tatsuya Watanabe ,  Jun Murakami ,  Takashi Mitsui

IPC分类号： A61K31/444 ,  C07D491/048

CPC分类号： C07D491/04 ,  C07D213/75

摘要： The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and, R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.

摘要翻译： 本发明提供式（I）的缩合呋喃化合物：其中环X为苯，吡啶等; Y是任选取代的氨基，任选取代的环烷基，任选取代的芳基，任选取代的饱和杂环基，任选取代的不饱和杂环基; A是单键，低级亚烷基，低级亚烯基，低级亚烯基或氧原子; R3是氢等; 和R4为氢等，或其药学上可接受的盐，其可用作药物，特别是活性凝血因子X抑制剂。

公开(公告)号：US20090209511A1

公开(公告)日：2009-08-20

申请号：US12382787

申请日：2009-03-24

申请人： Takayuki Kawaguchi ,  Hidenori Akatsuka ,  Toru Iijima ,  Yasunori Tsuboi ,  Takashi Mitsui ,  Jun Murakami

发明人： Takayuki Kawaguchi ,  Hidenori Akatsuka ,  Toru Iijima ,  Yasunori Tsuboi ,  Takashi Mitsui ,  Jun Murakami

IPC分类号： A61K31/397 ,  A61K31/535 ,  A61K31/4439 ,  A61K31/421 ,  C07D413/14 ,  C07D405/12 ,  C07D263/00

CPC分类号： C07D413/14 ,  C07D307/85 ,  C07D405/12 ,  C07D405/14 ,  C07D417/14

摘要： The present invention provides a benzofuran derivative of the formula [1]: wherein x is a group of the formula: —N═ or —CH═; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R1 is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.

摘要翻译： 本发明提供式[1]的苯并呋喃衍生物：其中x是下式的基团：-N-或-CH-; Y是任选取代的氨基，任选取代的环烷基或任选取代的饱和杂环基; A是单键，在链的末端或其末端具有双键的碳链或氧原子; R1是氢原子或卤素原子; 环B是任选取代的苯环; 并且R 3是氢原子或其药学上可接受的盐，其可用作药物，特别是作为活化凝血因子X抑制剂。