公开(公告)号：US20140072576A1

公开(公告)日：2014-03-13

申请号：US14075538

申请日：2013-11-08

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Masaya KOKUBO ,  Motoyuki TANAKA ,  Hiroshi OCHIAI ,  Yoshikazu TAKAOKA ,  Shiro SHIBAYAMA

IPC: A61K31/695 ,  C07D233/64 ,  A61K45/06 ,  C07D471/10 ,  A61K31/435 ,  A61K31/5377 ,  C07F7/18 ,  A61K31/4178

CPC classification number: A61K31/695 ,  A61K31/4178 ,  A61K31/435 ,  A61K31/5377 ,  A61K45/06 ,  C07D233/64 ,  C07D471/10 ,  C07F7/1804

Abstract: The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.

Abstract translation: 本发明涉及由式（I）表示的化合物：其中所有符号如本文所定义，其盐，其溶剂化物或其前药。 本发明的化合物对CXCR4具有拮抗作用，因此可用作CXCR4介导的疾病的预防和/或治疗剂，例如炎性和免疫疾病（例如类风湿性关节炎，关节炎，视网膜病变，肺纤维化 ，移植器官的排斥等），过敏性疾病，感染（例如，人类免疫缺陷病毒感染，获得性免疫缺陷综合征等），精神神经病，脑疾病，心血管疾病，代谢疾病和癌性疾病（例如， 癌症，癌症转移等）或再生治疗剂。

公开(公告)号：US20130085275A1

公开(公告)日：2013-04-04

申请号：US13682784

申请日：2012-11-21

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Yoshikazu TAKAOKA ,  Shiro SHIBAYAMA ,  Rena NISHIZAWA

IPC: C07D413/12 ,  C07D401/06 ,  C07D401/14 ,  C07D401/12 ,  C07D211/58

CPC classification number: C07D413/12 ,  A61K31/00 ,  C07D211/58 ,  C07D231/12 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14

Abstract: A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof: (wherein each symbol is as defined in the description.) The compounds represented by formula (I) has the antagonistic activity against CCR5, so they are useful in preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, inflammatory bowel disease such as ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation (rejection of graft of solid organ, rejection of graft of pancreatic islet cells in therapy for diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, infection with RSV, etc.), allergic diseases (atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), cardiovascular diseases (arteriosclerosis, ischemic reperfusion injury, etc.), acute respiratory distress syndrome, shock accompanying bacterial infection, diabetes, cancer metastasis and so on.

Abstract translation: 由式（I）表示的化合物，其盐，其N-氧化物，其溶剂合物或其前药：（其中各符号如说明书中所定义）。式（I）表示的化合物具有拮抗作用 因此它们可用于预防和/或治疗CCR5相关疾病，例如各种炎性疾病（哮喘，肾炎，肾病，肝炎，关节炎，类风湿关节炎，鼻炎，结膜炎，炎性肠病如溃疡性结肠炎） 等等），免疫疾病（自身免疫性疾病，器官移植排斥反应（实体器官移植排斥反应，胰岛细胞移植对糖尿病的治疗排斥反应，移植物抗宿主病等），免疫抑制，牛皮癣， 多发性硬化症等），感染性疾病（人类免疫缺陷病毒感染，获得性免疫缺陷综合征，RSV感染等），过敏性疾病（特应性皮炎，荨麻疹，过敏性 急性呼吸窘迫综合征，伴随细菌感染的休克，糖尿病，癌症转移等），心血管疾病（动脉硬化，缺血再灌注损伤等）。