公开(公告)号：US08097610B2

公开(公告)日：2012-01-17

申请号：US11990977

申请日：2006-08-24

申请人： Akiko Itai ,  Susumu Muto ,  Ryuko Tokuyama ,  Hiroshi Fukasawa ,  Takafumi Ohara ,  Terukazu Kato

发明人： Akiko Itai ,  Susumu Muto ,  Ryuko Tokuyama ,  Hiroshi Fukasawa ,  Takafumi Ohara ,  Terukazu Kato

IPC分类号： A61K31/55 ,  A61K31/5377 ,  A61K31/4535 ,  C07D401/04 ,  C07D413/14 ,  C07D417/04

CPC分类号： C07D211/22 ,  C07D211/58 ,  C07D241/04 ,  C07D241/44 ,  C07D277/82 ,  C07D401/04 ,  C07D403/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12

摘要： A compound of the formula (I): or a pharmaceutically acceptable salt thereof.

摘要翻译： 式（I）的化合物或其药学上可接受的盐。

公开(公告)号：US20110294813A1

公开(公告)日：2011-12-01

申请号：US13173819

申请日：2011-06-30

申请人： Akiko Itai ,  Susumu Muto ,  Ryuko Tokuyama ,  Hiroshi Fukasawa ,  Takeshi Yanase

发明人： Akiko Itai ,  Susumu Muto ,  Ryuko Tokuyama ,  Hiroshi Fukasawa ,  Takeshi Yanase

IPC分类号： A61K31/4439 ,  C07D263/24 ,  A61P3/10 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/496 ,  C07D413/12 ,  A61K31/421

CPC分类号： C07D263/20 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D413/12

摘要： Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(═O)— or —NR3S(═O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.

摘要翻译： 公开了可用作11-羟基类固醇脱氢酶1型抑制剂的化合物。 由下式表示的化合物：其药学上可接受的盐或其溶剂化物，其中R 1是任选取代的环烷基，任选取代的环烷基烷基，任选取代的杂环或任选取代的杂环烷基，X是-O-，-NR 3 - ， - NR 3 C（= O） - 或-NR 3 S（= O）2 - ，R 2是任选取代的芳基，任选取代的芳基烷基，任选取代的杂芳基或任选取代的杂芳基烷基，R 3是氢或任选取代的烷基。

公开(公告)号：US20080255069A1

公开(公告)日：2008-10-16

申请号：US12065099

申请日：2006-09-07

申请人： Koichi Shudo ,  Hiroyuki Kagechika ,  Hiroshi Fukasawa ,  Tetsuro Matsuishi ,  Naoko Katsumura ,  Miwako Ishido

发明人： Koichi Shudo ,  Hiroyuki Kagechika ,  Hiroshi Fukasawa ,  Tetsuro Matsuishi ,  Naoko Katsumura ,  Miwako Ishido

IPC分类号： A61K31/695 ,  A61K31/27

CPC分类号： A61K31/192

摘要： A medicament for preventive and/or therapeutic treatment of a bowel diseases such as inflammatory bowel diseases including Crohn's disease, which comprises as an active ingredient a retinoid such as, for example, 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid.

摘要翻译： 一种用于预防和/或治疗诸如包括克罗恩病在内的肠疾病的肠疾病的药物，其包含类视黄醇作为活性成分，例如4 - [（5,6,7,8-四氢 - 5,5,8,8-四甲基-2-萘基）氨基甲酰基]苯甲酸。

公开(公告)号：US20100324134A1

公开(公告)日：2010-12-23

申请号：US12872171

申请日：2010-08-31

申请人： Koichi SHUDO ,  Hiroyuki KAGECHIKA ,  Hiroshi FUKASAWA ,  Tetsuro MATSUISHI ,  Naoko KATSUMURA ,  Miwako ISHIDO

发明人： Koichi SHUDO ,  Hiroyuki KAGECHIKA ,  Hiroshi FUKASAWA ,  Tetsuro MATSUISHI ,  Naoko KATSUMURA ,  Miwako ISHIDO

IPC分类号： A61K31/27 ,  A61P1/00

CPC分类号： A61K31/192

摘要： A medicament for preventive and/or therapeutic treatment of a bowel diseases such as inflammatory bowel diseases including Crohn's disease, which comprises as an active ingredient a retinoid such as, for example, 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid.

公开(公告)号：US20100234363A1

公开(公告)日：2010-09-16

申请号：US12679159

申请日：2008-09-17

申请人： Akiko Itai ,  Susumu Muto ,  Ryuko Tokuyama ,  Hiroshi Fukasawa ,  Takeshi Yanase

发明人： Akiko Itai ,  Susumu Muto ,  Ryuko Tokuyama ,  Hiroshi Fukasawa ,  Takeshi Yanase

IPC分类号： A61K31/5415 ,  C07D279/08 ,  A61P3/10 ,  C07D265/24 ,  A61K31/536

CPC分类号： C07D279/06 ,  C07D265/24 ,  C07D279/08 ,  C07D417/04 ,  C07D417/12

摘要： Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein X is O or S, a broken line and a wavy line represent the presence or the absence of a bond, (i) when a broken line represents the presence of a bond, a wavy line represents the absence of a bond, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, (ii) when a broken line represents the absence of a bond, a wavy line represents the presence of a bond, R1 and R4 are each independently hydrogen, halogen or the like, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, and R5 and R6 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like.

摘要翻译： 公开了可用作11-羟基类固醇脱氢酶1型抑制剂的化合物。 由下式表示的化合物：其药学上可接受的盐或其溶剂合物，其中X为O或S，虚线和波浪线表示存在或不存在键，（i）当虚线表示 键的存在，波浪线表示不存在键，R2和R3各自独立地为氢，卤素，氰基，羟基，羧基，任选取代的烷基，任选取代的烯基，任选取代的炔基等，（ii）当 虚线表示不存在键，波浪线表示键的存在，R 1和R 4各自独立地为氢，卤素等，R 2和R 3各自独立地为氢，卤素，氰基，羟基，羧基，任选地 取代的烷基，任选取代的烯基，任选取代的炔基等，R 5和R 6各自独立地为氢，任选取代的烷基，任选取代的烯基，任选取代的炔基等。

公开(公告)号：US20100113448A1

公开(公告)日：2010-05-06

申请号：US12594093

申请日：2008-03-27

申请人： Akiko Itai ,  Susumu Muto ,  Ryuko Tokuyama ,  Hiroshi Fukasawa ,  Takeshi Yanase

发明人： Akiko Itai ,  Susumu Muto ,  Ryuko Tokuyama ,  Hiroshi Fukasawa ,  Takeshi Yanase

IPC分类号： A61K31/421 ,  C07D413/12 ,  C07D263/24 ,  A61P3/10 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/496

CPC分类号： C07D263/20 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D413/12

摘要： Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(═O)— or —NR3S(═O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.

摘要翻译： 公开了可用作11-羟基类固醇脱氢酶1型抑制剂的化合物。 由下式表示的化合物：其药学上可接受的盐或其溶剂合物，其中R 1是任选取代的环烷基，任选取代的环烷基烷基，任选取代的杂环或任选取代的杂环烷基，X是-O-，-NR 3 - ， - NR 3 C（= O） - 或-NR 3 S（= O）2 - ，R 2是任选取代的芳基，任选取代的芳基烷基，任选取代的杂芳基或任选取代的杂芳基烷基，R 3是氢或任选取代的烷基。

公开(公告)号：US08168677B2

公开(公告)日：2012-05-01

申请号：US12559268

申请日：2009-09-14

申请人： Koichi Shudo ,  Hiroyuki Kagechika ,  Hiroshi Fukasawa ,  Tetsuro Matsuishi ,  Naoko Katsumura ,  Miwako Ishido

发明人： Koichi Shudo ,  Hiroyuki Kagechika ,  Hiroshi Fukasawa ,  Tetsuro Matsuishi ,  Naoko Katsumura ,  Miwako Ishido

IPC分类号： A61K31/192 ,  A61K31/554 ,  A61K31/5513 ,  A61K31/695

CPC分类号： A61K31/192

摘要： Method for therapeutic treatment of inflammatory bowel disease, including Crohn's disease, comprising administering to a patient in need thereof a therapeutically effective amount of a composition comprising a retinoid as an active ingredient to treat the inflammatory bowel disease, the retinoid being selected from the group consisting of 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl) carbamoyl]benzoic acid, 4-[(3,5-bis-trimethylsilylphenyl)carboxamido]benzoic acid, 4-[2,3-(2,5-dimethyl-2,5-hexano)dibenzo[b,f][1,4]thiazepin-11-yl]benzoic acid, and 4-(5H-7,8,9,10-tetrahydro-5,7,7,10,10-pentamethylbenzo[e]naphtho[2,3-b][1,4]diazepin-13-yl)benzoic acid.

摘要翻译： 包括克罗恩病在内的治疗性治疗炎症性肠病的方法，包括向有需要的患者施用治疗有效量的包含类视黄醇作为活性成分以治疗炎性肠病的组合物，所述类视色素选自 的4 - [（5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基）氨基甲酰基]苯甲酸，4 - [（3,5-双三甲基甲硅烷基苯基）甲酰氨基]苯甲酸 ，4- [2,3-（2,5-二甲基-2,5-己烷）二苯并[b，f] [1,4]硫杂吖庚因-11-基]苯甲酸和4-（5H- ，9,10-四氢-5,7,7,10,10-五甲基苯并[e]萘并[2,3-b] [1,4]二氮杂-13-基）苯甲酸。

公开(公告)号：US08071647B2

公开(公告)日：2011-12-06

申请号：US12872171

申请日：2010-08-31

申请人： Koichi Shudo ,  Hiroyuki Kagechika ,  Hiroshi Fukasawa ,  Tetsuro Matsuishi ,  Naoko Katsumura ,  Miwako Ishido

发明人： Koichi Shudo ,  Hiroyuki Kagechika ,  Hiroshi Fukasawa ,  Tetsuro Matsuishi ,  Naoko Katsumura ,  Miwako Ishido

IPC分类号： A61K31/196

CPC分类号： A61K31/192

摘要： Method for suppressing adhesion of the intestines or therapeutic treatment of adhesion of the intestines comprising administering to a patient in need thereof a therapeutically effective amount of 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid. There is also provided a medicament for suppressing adhesion of the intestines and/or therapeutic treatment of bowel diseases such as inflammatory bowel diseases, including Crohn's disease, which comprises as an active ingredient a retinoid such as, for example, 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid.

摘要翻译： 用于抑制肠粘连的方法或肠道粘连的治疗处理方法，包括向有需要的患者施用治疗有效量的4 - [（5,6,7,8-四氢-5,5,8,8-四氢 - 四甲基-2-萘基）氨基甲酰基]苯甲酸。 还提供了一种用于抑制肠粘连和/或诸如包括克罗恩病在内的肠疾病的肠道疾病的治疗性治疗的药物，其包含类视黄醇作为活性成分，例如4 - [（5， 6,7,8-四氢-5,5,8,8-四甲基-2-萘基）氨基甲酰基]苯甲酸。

公开(公告)号：US20090286974A1

公开(公告)日：2009-11-19

申请号：US11990977

申请日：2006-08-24

申请人： Akiko Itai ,  Susumu Muto ,  RYuko Tokuyama ,  Hiroshi Fukasawa ,  Takafumi Ohara ,  Terukazu Kato

发明人： Akiko Itai ,  Susumu Muto ,  RYuko Tokuyama ,  Hiroshi Fukasawa ,  Takafumi Ohara ,  Terukazu Kato

IPC分类号： C07D417/04 ,  C07D403/04

CPC分类号： C07D211/22 ,  C07D211/58 ,  C07D241/04 ,  C07D241/44 ,  C07D277/82 ,  C07D401/04 ,  C07D403/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12

摘要： A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein Ring Q is optionally substituted monocyclic aryl, optionally substituted monocyclic heteroaryl, optionally substituted fused aryl or optionally substituted fused heteroaryl, Y1 is a bond or —NR6— or the like, Ring A is optionally substituted nonaromatic heterocyclediyl, a group of the formula: -Y2Z1- is a group of the formula: R7 are each independently hydrogen, optionally substituted lower alkyl or the like, R8 and R9 are each independently hydrogen or optionally substituted lower alkyl, n is an integer between 1 and 3, Z1 is a bond, —O—, —S— or —NR9—, Ring B is optionally substituted aromatic carbocyclediyl or optionally substituted aromatic heterocyclediyl, Y3 is a bond, optionally substituted lower alkylene optionally intervened by —O—, optionally substituted lower alkenylene or the like, and Z2 is COOR3 or the like.

摘要翻译： 式（I）的化合物：其药学上可接受的盐或溶剂化物，其中环Q是任选取代的单环芳基，任选取代的单环杂芳基，任选取代的稠合芳基或任选取代的稠合杂芳基，Y1是键或-NR 6 - 或 环A是任选取代的非芳族杂环二基，下式基团：-Y 2 Z 1 - 是下式​​的基团：R 7各自独立地为氢，任选取代的低级烷基等，R 8和R 9各自独立地为氢或任选地 取代的低级烷基，n是1和3之间的整数，Z 1是键，-O-，-S-或-NR 9 - ，环B是任选取代的芳族碳环二基或任选取代的芳族杂环二基，Y 3是一个键， 任选地被-O-，任选取代的低级亚烯基等所介导的低级亚烷基，Z 2是COOR 3等。

公开(公告)号：US07998992B2

公开(公告)日：2011-08-16

申请号：US12594093

申请日：2008-03-27

申请人： Akiko Itai ,  Susumu Muto ,  Ryuko Tokuyama ,  Hiroshi Fukasawa ,  Takeshi Yanase

发明人： Akiko Itai ,  Susumu Muto ,  Ryuko Tokuyama ,  Hiroshi Fukasawa ,  Takeshi Yanase

IPC分类号： A01N43/76 ,  A01N43/36 ,  A61K31/42 ,  A61K31/535 ,  A61K31/40 ,  C07D263/00

CPC分类号： C07D263/20 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D413/12

摘要： Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(═O)— or —NR3S(═O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.

摘要翻译： 公开了可用作11-羟基类固醇脱氢酶1型抑制剂的化合物。 由下式表示的化合物：其药学上可接受的盐或其溶剂化物，其中R 1是任选取代的环烷基，任选取代的环烷基烷基，任选取代的杂环或任选取代的杂环烷基，X是-O-，-NR 3 - ， - NR 3 C（= O） - 或-NR 3 S（= O）2 - ，R 2是任选取代的芳基，任选取代的芳基烷基，任选取代的杂芳基或任选取代的杂芳基烷基，R 3是氢或任选取代的烷基。