NPS R-568 hydrochloride

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: NPS R-568 hydrochloride
• 英文别名: R-568；N-(3-[2-chlorophenyl]propyl)-(R)-α-methyl-3-methoxybenzylamine hydrochloride；(R)-N-(3-methoxy-α-phenylethyl)-3-(2'-chlorophenyl)-1-propylamine hydrochloride；Tecalcet hydrochloride；3-(2-chlorophenyl)-N-[(1R)-1-(3-methoxyphenyl)ethyl]propan-1-amine;hydron;chloride
• 化学式: C₁₈H₂₂ClNO*ClH
• 分子量: 340.293
• InChiKey: YJXUXANREVNZLH-PFEQFJNWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.05
• 重原子数：
  22
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  21.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  3-(2-氯苯基)-1-丙胺 在 盐酸 、 (R)-3,3'-bis[4-methyl-3,5-dinitrophenyl]-1,1'-binaphthyl-2,2'-disulfonimide 、 2,6-二甲基-1,4-二氢吡啶-3,5-二甲酸二叔丁酯 作用下， 以 1,4-二氧六环 、 乙醚 、 均三甲苯 为溶剂， 反应 172.0h， 生成 NPS R-568 hydrochloride
  参考文献：
  名称：

  二磺酰亚胺催化的N-烷基亚胺的不对称还原

  摘要：

  在Boc 2 O存在的情况下，已开发出一种以Hantzsch酯为氢源的手性二磺酰亚胺（DSI）催化N烷基亚胺的不对称还原。该反应可提供具有出色收率和对映选择性的Boc保护的N-烷基胺。该方法可耐受多种烷基胺，从而说明了酮与各种胺的一般还原性交叉偶联的潜力，并已用于药物（S）-利伐斯的明，NPS R-568盐酸盐的合成，以及（R）-芬迪林。

  DOI：

  10.1002/anie.201504052

文献信息

• PYRIDO [4,3-d] PYRIMIDIN-4 (3H) -ONE DERIVATIVES AS CALCIUM RECEPTOR ANTAGONISTS
  申请人：Didiuk T. Mary

  公开号：US20080085887A1

  公开（公告）日：2008-04-10

  The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula I wherein the variables R 1 , R 2 , R 3 , R 4 and R 5 are as described herein. Also provided are pharmaceutical compositions comprising the compounds of formula I as well as methods of treatment employing compounds of formula I to treat a disease or disorder characterized by abnormal bone or mineral homeostasis such as hypoparathyroidism, osteoporosis, osteopenia, periodontal disease, Paget's disease, bone fracture, osteoarthritis, rheumatoid arthritis, and humoral hypercalcemia of malignancy.

  本发明涉及新型的吡啶[4,3-d]嘧啶-4(3H)-酮衍生物及其药用可接受的盐，其结构公式为I，其中变量R1、R2、R3、R4和R5如本文所述。还提供了包含公式I化合物的药物组合物，以及使用公式I化合物治疗由异常骨骼或矿物质稳态特征性疾病或失调的方法，例如低甲状旁腺功能症、骨质疏松症、骨量减少、牙周病、佩吉特病、骨折、骨关节炎、类风湿性关节炎和恶性体液性高钙血症。
• [EN] 1,1-(Dimethyl-Ethylamino)-2-Hydroxy-Propoxy]-Ethyl}-3-Methyl-Biphenyl-4- Carboxylic Acid Derivatives As Calcium Receptor Antagonists<br/>[FR] DÉRIVÉS DE L'ACIDE 1,1-(DIMÉTHYL-ÉTHYLAMINO)-2-HYDROXY-PROPOXY]-ÉTHYL}-3-MÉTHYL-BIPHÉNYL-4-CARBOXYLIQUE UTILES EN TANT QU'ANTAGONISTES DES RÉCEPTEURS DU CALCIUM
  申请人：PFIZER

  公开号：WO2010103429A1

  公开（公告）日：2010-09-16

  The present invention is directed to novel 1,1 -(dimethyl-ethylamino)-2- hydroxy-propoxy]-ethyl}-3-methyl-biphenyl-4-carboxylic acid derivatives and pharmaceutically acceptable salts thereof of structural formula I wherein the variable R1 is as described herein. Also provided are pharmaceutical compositions comprising the compounds of formula I as well as methods of treatment employing compounds of formula I to treat a disease or disorder characterized by abnormal bone or mineral homeostasis such as hypoparathyroidism, osteoporosis, osteopenia, periodontal disease, Paget's disease, bone fracture, osteoarthritis, rheumatoid arthritis, and humoral hypercalcemia of malignancy.

  本发明涉及新颖的1,1-(二甲基乙基氨基)-2-羟基-丙氧基]-乙基}-3-甲基联苯基-4-羧酸衍生物及其结构式I中的药用盐，其中变量R1如本文所述。还提供了包含结构式I化合物的药物组合物，以及利用结构式I化合物治疗由异常骨骼或矿物质稳态特征的疾病或紊乱的方法，如甲状旁腺功能减退症、骨质疏松症、骨质疏松症、牙周病、帕吉特病、骨折、骨关节炎、类风湿性关节炎和恶性高钙血症。
• [EN] POLYMERIC HYPERBRANCHED CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS POLYMÉRIQUES HYPERBRANCHÉS
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024048A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble carrier-linked prodrugs of formula (I),wherein POL is a polymeric moiety,each Hyp is independently a hyperbranched moiety,each moiety SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, m is 0 or 1, each n is independently an integer from 2 to 200 and each x is independently 0 or 1. It further relates to pharmaceutical compositions comprising said water- soluble carrier-linked prodrugs and methods of treatment.

  本发明涉及水溶性载体连接的前药，其化学式为（I），其中POL是聚合物基团，每个Hyp是独立的超支化基团，每个基团SP是独立的间隔基团，每个L是独立的可逆前药连接基团，m为0或1，每个n是独立的整数，范围从2到200，每个x是独立的0或1。此外，还涉及包含所述水溶性载体连接的前药的药物组合物和治疗方法。
• [EN] HIGH-LOADING WATER-SOLUBLE CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS HYDROSOLUBLES DE FORTE CHARGE
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024047A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein B, A and Hyp form the carrier, B is a branching core, each A is independently a poly(ethylene glycol)-based polymeric chain, each Hyp is independently a branched moiety, each SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, each D is independendly a biologically active moiety, each x is independently 0 or 1, each m is independently an integer of from 2 to 64, n is an integer from 3 to 32; or the pharmaceutically acceptable salt thereof. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs, their use asmedicament or diagnostic, and methods of treatment.

  本发明涉及水溶性载体连接的前药，其化学式为(I)，其中B、A和Hyp形成载体，B是一个分支核心，每个A独立地是一条聚乙二醇基聚合链，每个Hyp独立地是一个分支基团，每个SP独立地是一个间隔基团，每个L独立地是一个可逆前药连接基团，每个D独立地是一个生物活性基团，每个x独立地为0或1，每个m独立地是从2到64的整数，n是从3到32的整数；或其药学上可接受的盐。进一步涉及包括所述水溶性载体连接的前药的药物组合物，其用作药物或诊断，以及治疗方法。
• [EN] RELEASABLE CONJUGATES<br/>[FR] CONJUGUÉS LIBÉRABLES
  申请人：QUIAPEG PHARMACEUTICALS AB

  公开号：WO2018163131A1

  公开（公告）日：2018-09-13

  The present application provides compounds of Formula (B), or pharmaceutically acceptable salts thereof, wherein D is a residue of a biologically active drug, which underdo hydrolysis under physiological conditions to release the biologically active drug and which are useful in the treatment of disorders that could be beneficially treated with the drug.

  本申请提供了化合物的公式（B），或其药用盐，其中D是生物活性药物的残留物，在生理条件下经过水解释放出生物活性药物，并且对可能受益于该药物治疗的疾病具有用处。