2-[4-[[2-乙基-4-甲基-6-(5,6,7,8-四氢咪唑并[1,2-a]吡啶-2-基)苯并咪唑-1-基]甲基]苯基]苯甲酸 | 144702-17-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 2-[4-[[2-乙基-4-甲基-6-(5,6,7,8-四氢咪唑并[1,2-a]吡啶-2-基)苯并咪唑-1-基]甲基]苯基]苯甲酸
• 英文名称: 4'-[(2-Ethyl-4-methyl-6-(5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl)-benzimidazol-1-yl)-methyl]-biphenyl-2-carboxylic acid
• 英文别名: 4'-[(2-ethyl-4-methyl-6-(5,6,7,8-tetrahydro-imidazo[1,2-a]-pyridin-2-yl)-benzimidazol-1-yl)-methyl]-2-carboxybiphenyl；Pomisartan；2-[4-[[2-ethyl-4-methyl-6-(5,6,7,8-tetrahydroimidazo[1,2-a]pyridin-2-yl)benzimidazol-1-yl]methyl]phenyl]benzoic acid
• CAS: 144702-17-0
• 化学式: C₃₁H₃₀N₄O₂
• 分子量: 490.605
• InChiKey: SOYCBUUKISWFER-UHFFFAOYSA-N

物化性质

• 沸点：
  779.5±60.0 °C(Predicted)
• 密度：
  1.27±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.9
• 重原子数：
  37
• 可旋转键数：
  6
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  72.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-[4-[[2-乙基-4-甲基-6-(5,6,7,8-四氢咪唑并[1,2-a]吡啶-2-基)苯并咪唑-1-基]甲基]苯基]苯甲酸 生成 4'-[(2-ethyl-4-methyl-6-(5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl)-benzimidazol-1-yl)-methyl]-2-sulpho-biphenyl
  参考文献：
  名称：

  Benzimidazoles and pharmaceutical compositions containing them

  摘要：

  抑制血管紧张素II的苯并咪唑类化合物，用于治疗高血压。示范性化合物包括：(a) 4'-[(2-正丙基-4-甲基-6-(1-甲基苯并咪唑-2-基)-苯并咪唑-1-基)-甲基]-2-(1,3-噻唑啉-2,4-二酮-5-甲基亚基)-联苯，(b) 4'-[(2-正丙基-4-甲基-6-(1-甲基苯并咪唑-2-基)-苯并咪唑-1-基)-甲基]-2-磺酸酯联苯，(c) 4'-[(2-乙基-4-甲基-6-(5,6,7,8-四氢咪唑[1,2-a]吡啶-2-基)-苯并咪唑-1-基)-甲基]-2-磺酸酯联苯，(d) 4'-[(2-正丙基-4-甲基-6-(1-甲基苯并咪唑-2-基)-苯并咪唑-1-基)-甲基]-2-三氟乙酰氨基联苯，(e) 4'-[(2-乙基-4-甲基-6-(5,6,7,8-四氢咪唑[1,2-a]吡啶-2-基)-苯并咪唑-1-基)-甲基]-2-三氟乙酰氨基联苯，(f) 4'-[(2-正丙基-4-甲基-6-(1-甲基苯并咪唑-2-基)-苯并咪唑-1-基)-甲基]-2-(4-甲氧基苄氨基甲酰氨基磺酰)-联苯，(g) 4'-[(2-正丙基-4-甲基-6-(1-甲基苯并咪唑-2-基)-苯并咪唑-1-基)-甲基]-2-(环己基氨基甲酰氨基磺酰)-联苯，(h) 4'-[(2-正丙基-4-甲基-6-(1-甲基苯并咪唑-2-基)-苯并咪唑-1-基)-甲基]-2-(苯甲酰氨基磺酰)-联苯，(i) 4'-[(2-乙基-4-甲基-6-(5,6,7,8-四氢咪唑[1,2-a]吡啶-2-基)-苯并咪唑-1-基)-甲基]-2-(苯甲酰氨基磺酰)-联苯，(j) 4'-[(2-正丁基-4-甲基-6-(丙磺酰胺-1-基)-苯并咪唑-1-基)-甲基]-2-(苯甲酰氨基磺酰)-联苯和(k) 4'-[(2-乙基-4-甲基-6-(5,6,7,8-四氢咪唑[1,2-a]吡啶-2-基)-苯并咪唑-1-基)-甲基]-2-(环己基氨基甲酰氨基磺酰)-联苯。

  公开号：

  US05565469A1

文献信息

• [EN] METHOD FOR THE METAL-FREE PREPARATION OF A BIARYL BY A PHOTOSPLICING REACTION AND THEIR USES<br/>[FR] PROCÉDÉ DE PRÉPARATION SANS MÉTAL D'UN BIARYLE PAR RÉACTION DE PHOTOCOLLAGE ET UTILISATIONS ASSOCIÉES
  申请人：LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST HKI

  公开号：WO2019101679A1

  公开（公告）日：2019-05-31

  The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar-Ar' by photochemically reacting a precursor compound of formula (II): Ar-L-Ar' to form a biaryl compound of general formula: Ar-L-Ar' (II) → Ar-Ar' (I) wherein Ar and Ar', independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5–20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group –X–Y–Z– as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.

  本发明涉及一种通过光切割反应无金属制备联芳烃化合物的方法，以及其在化学化合物制备中的用途，特别是在制药和农药领域中的活性成分的制备中的用途。具体而言，它涉及一种通过光化学反应化学前体化合物（II）：Ar-L-Ar'与形成一般式的联芳烃化合物（II）→Ar-Ar'（I）反应，从而实现联芳烃化合物（I）的区域控制制备的方法，其中Ar和Ar'分别表示未取代或取代的C6-C20芳基或由碳、氮、氧和硫选择的5-20个环原子的杂芳基，L表示如本文所定义的一个组-X-Y-Z-。这些联芳烃化合物通常适用于有机化学合成的广泛领域中的中间体或关键构建块，以及它们各自的用途。它们在活性成分合成领域中的用途是本发明的一个方面，它们在制备药用活性成分中的用途尤为理想。
• Nitric oxide enhancing diuretic compounds, compositions and methods of use
  申请人：Garvey S. David

  公开号：US20060189603A1

  公开（公告）日：2006-08-24

  The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia. The nitric oxide enhancing diuretic compounds comprise at least one nitric oxide enhancing group linked to the diuretic compound through one or more sites such as carbon, oxygen and/or nitrogen via a bond or moiety that cannot be hydrolyzed.

  该发明描述了包含至少一种增强一氧化氮利尿化合物或其药用盐的新型组合物和试剂盒，以及可选地，至少一种增强一氧化氮化合物和/或至少一种治疗剂的试剂盒。该发明还提供了以下方法：(a)治疗由过多水分和/或电解贮留引起的症状；(b)治疗心血管疾病；(c)治疗肾血管疾病；(d)治疗糖尿病；(e)治疗由氧化应激引起的疾病；(f)治疗内皮功能障碍；(g)治疗由内皮功能障碍引起的疾病；(h)治疗肝硬化；(j)治疗子痫前期；(k)治疗骨质疏松症；(l)治疗肾病；(m)治疗外周血管疾病；(n)治疗门静脉高压；(o)治疗中枢神经系统疾病；(p)治疗代谢综合征；(q)治疗性功能障碍；以及(r)高脂血症。增强一氧化氮利尿化合物包括至少一种增强一氧化氮基团，通过碳、氧和/或氮等一个或多个位点与利尿化合物连接，连接通过不能水解的键或基团。
• [EN] NEW COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS
  申请人：VICORE PHARMA AB

  公开号：WO2021053344A1

  公开（公告）日：2021-03-25

  There is provided herein a compound of formula I, wherein R1, R2, R3 Y1, Y2, Y3, Y4, R4, R5 and R6 are as defined herein, which compounds are useful in the treatment of autoimmune and/or fibrotic diseases, including interstitial lung diseases, such as idiopathic pulmonary fibrosis and sarcoidosis.

  本文提供了一种化合物，其化学式为I，其中R1、R2、R3、Y1、Y2、Y3、Y4、R4、R5和R6如本文所定义，这些化合物在治疗自身免疫和/或纤维化疾病方面具有用途，包括间质肺病，如特发性肺纤维化和结节病。
• [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。