阅读说明：本技术 溶血磷脂酸受体拮抗剂及其制备方法 (Lysophosphatidic acid receptor antagonists and process for their preparation ) 是由 娄军 陈永凯 彭微 张轶涵 郭晓丹 柳力 刘军华 钱丽娜 王朝东 于 2020-01-15 设计创作，主要内容包括：本发明属于药物化学技术领域,具体涉及一种溶血磷脂酸受体拮抗剂及其制备方法。申请人惊奇地发现,本发明的化合物具有高的LPAR1拮抗活性和选择性,且毒性低、代谢稳定性好,具有良好的药物开发前景,可以用于预防或治疗与LPAR1相关的疾病或病症。申请人还意外地发现,本发明部分化合物的IC-(50)值可以低至300nM以下,甚至50nM以下。并且,本发明的化合物都具有较好的安全性,其CC-(50)范围可高达200μM以上。此外,本发明的化合物在人、大鼠、小鼠中都具有较好的代谢稳定性,这样优异的抑制活性对于它们作为LPAR1抑制剂应用于上述疾病或病症而言是令人非常期待的。此外,本发明化合物的制备方法简单,反应条件温和,产品收率高,适于工业化生产。(The present invention belongs to the field of medicinal chemistry technologyIn particular to a lysophosphatidic acid receptor antagonist and a preparation method thereof. The applicant surprisingly found that the compounds of the present invention have high LPAR1 antagonistic activity and selectivity, low toxicity, good metabolic stability, good prospects for drug development, and can be used for preventing or treating diseases or disorders associated with LPAR 1. Applicants have also surprisingly found that the IC of some of the compounds of the present invention 50 Values can be as low as below 300nM, even below 50 nM. In addition, the compounds of the invention have better safety, and CC thereof 50 The range can be as high as more than 200 mu M. In addition, the compounds of the present invention have good metabolic stability in humans, rats, and mice, and such excellent inhibitory activity is highly desirable for their application as LPAR1 inhibitors in the above diseases or conditions. In addition, the preparation method of the compound is simple, mild in reaction conditions, high in product yield and suitable for industrial production.)