CAS: 571170-77-9; (R)-2-(4-(4-Chlorobenzyl)-7-Fluoro-5-(Methylsulfonyl)-1,2,3,4-Tetrahydrocyclopenta[b]Indol-3-yl)Acetic Acid

该化合物是选择性的 prostaglandin D2(PGD2) 受体敌体, 主要是与针线菌结合使用, 以减轻冲洗的副作用. 它通过阻塞 DP1 受体, 使 PGD2 产生血管血管变异和皮肤冲洗. 这个机制可以改善病人对针线癌疗法的耐受力, 特别是在对流性贫血的治疗中. Laropiprant 显示高受体特性和最低目标外活动, 有助于其有利的安全配置 . 它的药用植物基因学支持每天一次的剂量, 增强合规性. 化合物通常被配制成一种固定剂量的组合, 与延长释放的针线菌素, 优化治疗效果, 同时减少不良效果. Laropiprant的定向行动使得它在控制脂肪紊乱方面成为有价值的辅助剂 .

结构式图片

欧盟法规

C&L通报

上下游产品

(E)-2-(4-(4-Chlorobenzyl)-7-Fluoro-5-(Methylsulfonyl)-1,2-Dihydrocyclopenta[b]Indol-3(4H)-Ylidene)Acetic Acid 866215-99-8
(E)-2-(4-(4-氯苄基)-7-氟-5-(甲基磺酰基)-1,2-二氢环戊并[b]吲哚-3(4H)-基)乙酸 2-[4-[(4-Chlorophenyl)Methyl]-7-Fluoro-5-Methylsulfonyl-1,2-Dihydrocyclopenta[b]Indol-3-Ylidene]Acetic Acid 866215-99-8
[(3R)-5-Bromo-4-(4-Chlorobenzyl)-7-Fluoro-1,2,3,4-Tetrahydrocyclopenta[b]Indol-3-Yl]Acetic Acid 393509-05-2
[4-(4-Chlorobenzyl)-7-Fluoro-5-Bromo-1,2,3,4-Tetrahydrocyclopenta[b]Indol-3-Yl]Acetic Acid 393509-04-1
2-(5-溴-7-氟-1,2,3,4-四氢环戊并b吲哚-3-基)乙酸 (5-Bromo-7-Fluoro-1,2,3,4-Tetrahydrocyclopenta[b]Indol-3-yl)Acetic Acid 393509-23-4
7-氟-5-溴-1,2,3,4-四氢乙酯 Ethyl (7-Fluoro-1,2,3,4-Tetrahydrocyclopenta[b]Indol-3-yl)Acetate 393509-21-2
2-(7-氟-1,2,3,4-四氢环戊并b吲哚-3-基)乙酸 2-(7-Fluoro-1,2,3,4-Tetrahydrocyclopenta[b]Indol-3-yl)Acetic Acid 393509-22-3
(2As,9Bs,9Cs)-6-Bromo-8-Fluoro-2A,3,9B,9C-Tetrahydro-4H-Benzo[b]Cyclopenta[gh]Pyrrolizin-4-One 828932-44-1

合成工艺路线路线简述

    Methyl 2-[(3R)-4-(4-Chlorobenzyl)-7-Fluoro-5-(Methylsulfonyl)-1,2,3,4-Tetrahydrocyclopenta[b]Indol-3-Yl]Acetate置于sodium Hydroxide体系中,用 N,N-二甲基乙酰胺 作为反应溶剂,化学反应 2.0H,以604 Mg的收率获得产物拉罗皮兰
    参考文献:前列腺素d 2受体拮抗剂的不对称合成
    标题:前列腺素d 2受体拮抗剂的不对称合成
    摘要:开发了一种不对称合成物,用于生产前列腺素d 2受体拮抗剂,用于治疗变应性鼻炎.使用不对称烯丙基烷基化化学方法设定立体异构中心,并通过pd催化的n-环化/ Heck方法构建结构的核心.合成依赖于后期的二氢吲哚氧化,不会使产物外消旋.
    DOI:10.1021/jo048305+

    海关参考信息

    专利信息


    专利号:US-9750749-B2
    优先权日:2010-05-03
    标题 :Methods of treating thyroid eye disease
    发明人:PHIPPS RICHARD P; GUO NAXIN; FELDON STEVEN
    权利人:PHIPPS RICHARD P; GUO NAXIN; FELDON STEVEN; UNIV ROCHESTER
    摘要:The present invention relates to a methods and compositions for the treatment of and management of symptoms for thyroid eye disease. The methods include administering to a patient having thyroid eye disease an agent that interferes with hyaluronan synthesis in an amount that is effective to inhibit hyaluronan synthesis in a retro-ocular space. The pharmaceutical compositions that includes a carrier suitable for ophthalmic delivery and an agent that interferes with hyaluronan synthesis. Combination therapies are also disclosed.

    专利号:US-7612106-B2
    优先权日:2004-12-23
    标题 :Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof
    发明人:BOATMAN P DOUGLAS; SCHRADER THOMAS O; SEMPLE GRAEME; SKINNER PHILIP J; JUNG JAE-KYU
    权利人:ARENA PHARM INC
    摘要:The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. n nAlso provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.

    专利号:CN-117645564-A
    优先权日:2022-12-02
    标 题 :A kind of fluoroalkyl substituted indole derivative and its synthesis method and application

    专利号:CN-115925611-A
    优先权日:2022-12-02
    标题 :A kind of fluoroalkyl substituted indole derivative and its synthesis method
    台州市科瑞生物技术有限公司
    ⚠️ 未注册 · 未认证企业
    ⚠️ 该商家尚未完成注册及企业认证,请用户仔细辨别,谨慎交易。
    数据来源于公开网络搜索,平台未作核实,请自行辨别。
    🏢敬请 企业认领
    🏬开设公司展台
    📢获取免费会员权益
    🎖️点亮专属注册企业标签
    📇展现公司完整信息 样本查看立即注册认领 →
    网址: http://www.pharm-intermediates.com
    企业联系电话:0576-88813233👤
    📞台州市科瑞生物技术有限公司 ⚠️参考联系方式
    联系人:金崇光
    电话:0576-88813233
    手机:13396860566
    传真:0576-88813233
    邮箱:sales@pharm-intermediates.com
    通信地址: 台州市开发大道东段288号
    邮编: 318000
    🆔 联系时候可告知是从"百琢研"平台获取的信息.
    ⚠️ 声明: 该企业未认证、未认领,请自行辨别信息的真实性和可靠性。咨询或交易时请注意风险评估与信息核实,百琢研不参与任何交易。企业认领注册入口→

    地址:台州市开发大道东段288号
    ⚠️ 未注册 · 未认证企业
    注册入口 备注: 📌 数据来源说明:本展台内容基于各搜索引擎等公开数据整理,仅作展示用途。请用户自行辨别
    ✉️ 若企业需抹除展台内容或有异议, 请通过页面底部联系方式告知我们,我们会尽快处理。
    潍坊鲁泽新材料有限公司
    ⚠️ 未注册 · 未认证企业
    ⚠️ 该商家尚未完成注册及企业认证,请用户仔细辨别,谨慎交易。
    数据来源于公开网络搜索,平台未作核实,请自行辨别。
    🏢敬请 企业认领
    🏬开设公司展台
    📢获取免费会员权益
    🎖️点亮专属注册企业标签
    📇展现公司完整信息 样本查看立即注册认领 →
    网址: http://www.ruzenm.cn
    电话:0536-19577738444👤
    📞 潍坊鲁泽新材料有限公司⚠️参考联系方式

    电话: 0536-19577738444
    邮件:matthew@ruzenm.com
    网址: http://www.ruzenm.cn
    地址:山东省寿光市软件园精细化工产业中心
    🆔 联系时候可告知是从"百琢研"平台获取的信息.
    ⚠️ 声明: 该企业未认证、未认领,请自行辨别信息的真实性和可靠性。咨询或交易时请注意风险评估与信息核实,百琢研不参与任何交易。企业认领注册入口→

    山东省寿光市软件园精细化工产业中心
    ⚠️ 未注册 · 未认证企业
    注册入口 备注: 数据来源说明:本展台内容基于各搜索引擎等公开数据整理,仅作展示用途。请用户自行辨别. 若企业需抹除展台内容或有异议, 请通过页面底部联系方式告知我们,我们会尽快处理。
    第 1 / 1 页
    现货

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: El Khoury P, Waldmann E, Huby T, Gall J, Couvert P, Lacorte JM, Chapman J, Frisdal E, Lesnik P, Parhofer KG, Le Goff W, Guerin M. Extended-Release Niacin/Laropiprant Improves Overall Efficacy of Postprandial Reverse Cholesterol Transport. Arterioscler Thromb Vasc Biol. 2016 Feb;36(2):285-94. doi: 10.1161/ATVBAHA.115.306834. Epub 2015 Dec 17. doi: 10.2217/pgs.15.79. Epub 2015 Jul 31. doi: 10.1016/j.jacl.2015.02.006. Epub 2015 Mar 2. doi: 10.1155/2015/154014. Epub 2015 Apr 29.
    6: Bays HE, Brinton EA, Triscari J, Chen E, Maccubbin D, MacLean AA, Gibson KL, Ruck RA, Johnson-Levonas AO, O'Neill EA, Mitchel YB. Extended-release niacin/laropiprant significantly improves lipid levels in type 2 diabetes mellitus irrespective of baseline glycemic control. Vasc Health Risk Manag. 2015 Feb 24;11:165-72. doi: 10.2147/VHRM.S70907. eCollection 2015.
    7: Bloomfield HE. ACP Journal Club: adding niacin plus laropiprant to statins did not reduce vascular events and increased serious adverse events. Ann Intern Med. 2014 Nov 18;161(10):JC8. doi: 10.7326/0003-4819-161-10-201411180-02008. doi: 10.1002/jcph.383. Epub 2014 Sep 4. doi: 10.5114/aoms.2014.43738. Epub 2014 Jun 27.

    合成参考文献


    参考文献:10.4061/2011/830434
    摘要:Kei A, Elisaf M, Moutzouri E, Tsiara S, Liberopoulos E. Add-on-Statin Extended Release Nicotinic Acid/Laropiprant but Not the Switch to High-Dose Rosuvastatin Lowers Blood Pressure: An Open-Label Randomized Study. International Journal of Hypertension. 2011;2011():1–6. doi: 10.4061/2011/830434.
    参考文献:10.1007/s10354-011-0908-4
    摘要:Föger B. Lipid lowering therapy in type 2 diabetes. Wien Med Wochenschr. 2011 Jun;161(11-12):289–96. doi: 10.1007/s10354-011-0908-4.
    参考文献:10.2147/dmso.s11244
    摘要:Arca M, Pigna G. Treating statin-intolerant patients. Diabetes Metab Syndr Obes. 2011;4():155–66.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知