公开(公告)号：US08754113B2

公开(公告)日：2014-06-17

申请号：US13516441

申请日：2010-12-14

Applicant: Koji Masuda ,  Shiro Kida ,  Naoki Yoshikawa ,  Manabu Katou ,  Terukazu Kato ,  Mado Nakajima ,  Eiichi Kojima ,  Mitsuhiro Yonehara

Inventor： Koji Masuda ,  Shiro Kida ,  Naoki Yoshikawa ,  Manabu Katou ,  Terukazu Kato ,  Mado Nakajima ,  Eiichi Kojima ,  Mitsuhiro Yonehara

IPC: A61K31/428 ,  A61K31/423 ,  A61K31/4245 ,  C07D413/06 ,  C07D417/06

CPC classification number: A61K31/423 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14 ,  C07D513/04

Abstract: A compound represented by the formula: or its pharmaceutically acceptable salt. Ring A is aromatic carbocycle or aromatic heterocycle, Z is —O— or —S—, R1 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2 and R3 are each independently hydrogen, halogen, hydroxy or the like, R4 is a group represented by the formula: —(CR6R7)n—R8, R6 and R7 are each independently hydrogen, halogen, hydroxy or the like, n is an integer of 0 to 3, R8 is carboxy, cyano, substituted or unsubstituted alkyl or the like, Rx is halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, and m is an integer of 0 to 3.

Abstract translation: 由下式表示的化合物或其药学上可接受的盐。 环A是芳族碳环或芳族杂环，Z是-O-或-S-，R1是氢，卤素，羟基，氰基，硝基，羧基，取代或未取代的烷基，取代或未取代的烯基等，R2和R3是 各自独立地为氢，卤素，羟基等，R4为下式表示的基团： - （CR6R7）n-R8，R6和R7各自独立地为氢，卤素，羟基等，n为0〜 3，R8为羧基，氰基，取代或未取代的烷基等，Rx为卤素，羟基，氰基，硝基，羧基，取代或未取代的烷基，取代或未取代的烯基等，m为0〜3的整数 。

公开(公告)号：US20120253040A1

公开(公告)日：2012-10-04

申请号：US13516441

申请日：2010-12-14

Applicant: Koji Masuda ,  Shiro Kida ,  Naoki Yoshikawa ,  Manabu Katou ,  Terukazu Kato ,  Mado Nakajima ,  Eiichi Kojima ,  Mitsuhiro Yonehara

Inventor： Koji Masuda ,  Shiro Kida ,  Naoki Yoshikawa ,  Manabu Katou ,  Terukazu Kato ,  Mado Nakajima ,  Eiichi Kojima ,  Mitsuhiro Yonehara

IPC: C07D271/10 ,  C07D413/10 ,  C07D241/36 ,  C07D513/04 ,  C07D417/12 ,  C07D215/14 ,  C07D285/135

CPC classification number: A61K31/423 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14 ,  C07D513/04

Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is aromatic carbocycle or aromatic heterocycle, Z is —NR5—, —O— or —S—, R5 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl or the like, R1 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2 and R3 are each independently hydrogen, halogen, hydroxy or the like, R4 is a group represented by the formula: —(CR6R7)n-R8, wherein R6 and R7 are each independently hydrogen, halogen, hydroxy or the like, n is an integer of 0 to 3, R8 is carboxy, cyano, substituted or unsubstituted alkyl or the like, Rx is halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, m is an integer of 0 to 3.

Abstract translation: 公开了可用作内皮脂肪酶抑制剂的化合物。 由下式表示的化合物：其药学上可接受的盐或其溶剂化物，其中环A是芳族碳环或芳族杂环，Z是-NR5-，-O-或-S-，R5是氢，取代或未取代的烷基， 取代或未取代的烯基，取代或未取代的炔基，取代或未取代的芳基等，R 1是氢，卤素，羟基，氰基，硝基，羧基，取代或未取代的烷基，取代或未取代的烯基等， 独立地是氢，卤素，羟基等，R 4是由下式表示的基团： - （CR 6 R 7）n -R 8，其中R 6和R 7各自独立地为氢，卤素，羟基等，n为0〜 3，R8为羧基，氰基，取代或未取代的烷基等，Rx为卤素，羟基，氰基，硝基，羧基，取代或未取代的烷基，取代或未取代的烯基等，m为0〜3的整数。

公开(公告)号：US20150246938A1

公开(公告)日：2015-09-03

申请号：US14343992

申请日：2012-09-07

Applicant: Akira Matsumura ,  Naotake Kobayashi ,  Yuji Nishiura ,  Sachie Tagashira ,  Shiro Kida ,  Kana Kurahashi ,  Mitsuhiro Yonehara

Inventor： Akira Matsumura ,  Naotake Kobayashi ,  Yuji Nishiura ,  Sachie Tagashira ,  Shiro Kida ,  Kana Kurahashi ,  Mitsuhiro Yonehara

IPC: C07F7/18 ,  C07D213/643 ,  C07D401/12 ,  C07D417/04 ,  C07D213/40 ,  C07D401/06 ,  C07D239/34 ,  C07D237/14 ,  C07D277/34 ,  C07D213/69

CPC classification number: C07F7/1804 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/4858 ,  C07C217/62 ,  C07C233/18 ,  C07C271/16 ,  C07C271/22 ,  C07C275/64 ,  C07D213/40 ,  C07D213/643 ,  C07D213/65 ,  C07D213/69 ,  C07D213/73 ,  C07D213/80 ,  C07D213/81 ,  C07D213/84 ,  C07D231/12 ,  C07D231/18 ,  C07D231/20 ,  C07D233/70 ,  C07D237/14 ,  C07D239/34 ,  C07D261/12 ,  C07D277/34 ,  C07D285/06 ,  C07D309/10 ,  C07D309/12 ,  C07D319/06 ,  C07D333/20 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07F7/0812

Abstract: The object of the present invention is to provide novel compounds having ACC2 inhibiting activity. In addition, the object of the present invention is to provide a pharmaceutical composition comprising the compound.A compound of formula (I′): wherein R1 is substituted or unsubstituted aryl etc., R2 is each independently hydrogen, substituted or unsubstituted alkyl etc., R3 is each independently hydrogen, substituted or unsubstituted alkyl etc., n is an integer from 0 to 3, R12 is hydrogen, substituted or unsubstituted alkyl etc., Ring A is aromatic carbocycle or aromatic heterocycle, R9 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl etc., m is an integer from 0 to 4, R4 and R5 is each independently hydrogen, substituted or unsubstituted alkyl etc., R6 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl etc., R13 is hydrogen, substituted or unsubstituted alkyl etc., X5 is bond etc., R7 is hydrogen or substituted or unsubstituted alkyl, R8 is substituted or unsubstituted alkylcarbonyl, substituted or unsubstituted alkenylcarbonyl etc.

Abstract translation: 本发明的目的是提供具有ACC2抑制活性的新化合物。 此外，本发明的目的是提供一种包含该化合物的药物组合物。 式（I'）的化合物：其中R 1为取代或未取代的芳基等，R 2各自独立地为氢，取代或未取代的烷基等，R 3各自独立地为氢，取代或未取代的烷基等，n为 0〜3，R 12为氢，取代或未取代的烷基等，环A为芳香族碳环或芳香族杂环，R9为取代或未取代的烷基，取代或未取代的链烯基等，m为0〜4的整数，R4和R5 各自独立地为氢，取代或未取代的烷基等，R 6为取代或未取代的烷基，取代或未取代的烯基等，R 13为氢，取代或未取代的烷基等，X 5为键等，R 7为氢或取代或未取代的 烷基，R8是取代或未取代的烷基羰基，取代或未取代的烯基羰基等