Dl-3-(4-联苯)丙氨酸盐酸盐 | 63024-23-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: Dl-3-(4-联苯)丙氨酸盐酸盐
• 英文名称: 2-amino-3-biphenyl-4-ylpropionic acid hydrochloride
• 英文别名: 4-phenylphenylalanine-hydrochloride；3-(4-Biphenyl)-DL-alanin-Hydrochlorid；2-amino-3-(4-phenylphenyl)propanoic acid;hydron;chloride
• CAS: 63024-23-7
• 化学式: C₁₅H₁₅NO₂*ClH
• mdl: MFCD07700218
• 分子量: 277.751
• InChiKey: ZUZSOLFZHJQIAX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.46
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.133
• 拓扑面积：
  63.3
• 氢给体数：
  3
• 氢受体数：
  3

安全信息

• 海关编码：
  2922499990

反应信息

• 作为反应物：
  描述：

  Dl-3-(4-联苯)丙氨酸盐酸盐 在 盐酸 、 五氯化磷 、 三乙胺 、 乙酰氯 作用下， 以 乙酸乙酯 为溶剂， 反应 9.0h， 生成 3-biphenyl-4-yl-2-{2-[(1H-indole-2-carbonyl)amino]benzoylamino}propionic acid ethyl ester
  参考文献：
  名称：

  Anthranilic acid based CCK1 receptor antagonists: preliminary investigation on their second “touch point”

  摘要：

  In this phase of structure-affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series Of Unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one order of magnitude greater than the lead and, as a general rule, it points out how the hypothesized receptorial pocket which accommodates the Phe residue allows much more structural modification than that interacting with the N-terminal group. Hence, the modification of the C-terminal pharmacophoric group of our lead VL-0395 can not only enhance the affinity of anthranific acid derivatives but can modulate the selectivity for one CCK receptor subtype or afford mixed antagonists. (c) 2005 Elsevier SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2005.01.002
• 作为产物：
  描述：

  联苯-4-甲醇 在 盐酸 、 氢溴酸 、 sodium ethanolate 作用下， 以 1,4-二氧六环 、 乙醇 、 水 为溶剂， 反应 5.5h， 生成 Dl-3-(4-联苯)丙氨酸盐酸盐
  参考文献：
  名称：

  Anthranilic acid based CCK1 receptor antagonists: preliminary investigation on their second “touch point”

  摘要：

  In this phase of structure-affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series Of Unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one order of magnitude greater than the lead and, as a general rule, it points out how the hypothesized receptorial pocket which accommodates the Phe residue allows much more structural modification than that interacting with the N-terminal group. Hence, the modification of the C-terminal pharmacophoric group of our lead VL-0395 can not only enhance the affinity of anthranific acid derivatives but can modulate the selectivity for one CCK receptor subtype or afford mixed antagonists. (c) 2005 Elsevier SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2005.01.002

文献信息

• SUBSTITUTED CARBAMOYLCYCLOALKYL ACETIC ACID DERIVATIVES AS NEP
  申请人：KARKI Rajeshri Ganesh

  公开号：US20120122764A1

  公开（公告）日：2012-05-17

  The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.

  本发明提供了一种具有化学式I的化合物； 或其药学上可接受的盐，其中R 1 ，R 2 ，R 3 ，R 4 ，R 5 ，B，X，m和n在此处被定义。该发明还涉及制造该发明化合物的方法及其治疗用途。本发明进一步提供了该发明化合物的药物组合物，以及具有药理活性剂和该发明化合物的组合。
• Sulfonamide derivative as a matrix metalloproteinase inhibitor
  申请人：——

  公开号：US20020169314A1

  公开（公告）日：2002-11-14

  The present invention provides a novel sulfonamide derivative of general formula (I) useful as an inhibitor of matrix metalloproteinase (MMP), its isomers, pharmaceutically acceptable salts thereof and a process for preparing the same. Since the sulfonamide derivatives of the present invention selectively inhibit MMP activity in vitro, the MMP inhibitors comprising the sulfonamide derivatives as an effective ingredient can be practically applied for the prevention and treatment of all sorts of diseases caused by overexpression and overactivation of MMP. 1

  本发明提供了一种新型磺胺衍生物的一般式(I)，其作为基质金属蛋白酶（MMP）抑制剂，其异构体，药用盐及其制备方法。由于本发明的磺胺衍生物在体外选择性地抑制MMP活性，包含磺胺衍生物作为有效成分的MMP抑制剂可以实际应用于预防和治疗由MMP过度表达和过活化引起的各种疾病。
• Topographic probes of angiotensin and receptor: potent angiotensin II agonist containing diphenylalanine and long-acting antagonists containing biphenylalanine and 2-indan amino acid in position 8
  作者：Kun Hwa Hsieh、Thomas R. LaHann、Robert C. Speth

  DOI：10.1021/jm00124a028

  日期：1989.4

  A series of phenylalanine-mimicking amino acids with increasing conformational restraint were prepared and incorporated into angiotensin II, in order to develop topographic probes of angiotensin useful for probing receptor boundaries by molecular graphics analysis and for conformational analysis of the ligand by NMR. In binding studies, all analogues displayed high affinity for rat uterus (Ki of 0

  制备了一系列具有增加的构象约束力的模拟苯丙氨酸的氨基酸，并将其掺入血管紧张素II中，以开发血管紧张素的拓扑探针，可用于通过分子图形分析探测受体边界和通过NMR进行配体的构象分析。在结合研究中，所有类似物均对大鼠子宫（Ki为0.74-6.08 nM）和脑（0.46-1.82 nM）受体表现出高亲和力。在平滑肌（大鼠子宫）收缩试验中，含二苯丙氨酸的[Sar1，Dip8] AII和[Sar1，D-Dip8] AII是有效的激动剂，分别具有[Asn1] AII 284％和48％的活性。相反，含联苯丙氨酸的[Sar1，Bip8] AII，[Sar1，D-Bip8] AII和含2-茚满氨基酸的[Sar1,2-Ind8] AII是有效的抑制剂，大约9、2和1 。比标准拮抗剂[Sar1，Leu8] AII有效4倍。在大鼠子宫试验中，它们各自的pA10值分别为8.87、8.70和8.82。相比之下，[Sar1，Leu8]
• ORALLY AVAILABLE VIRIDIOFUNGIN DERIVATIVE POSSESSING ANTI-HCV ACTIVITY
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：US20150210666A1

  公开（公告）日：2015-07-30

  An object of the present invention is to provide a compound that is useful as an orally available anti-HCV agent. The present invention relates to a compound represented by formula (1) or a pharmaceutically acceptable salt thereof. This compound has an anti-HCV activity and is useful as a medicine.

  本发明的目的是提供一种可口服的抗丙型肝炎病毒药物化合物。本发明涉及一种由式（1）所表示的化合物或其药学上可接受的盐。该化合物具有抗丙型肝炎病毒的活性，是一种有用的药物。
• Phosphono/biaryl substituted dipeptide derivatives
  申请人：CIBA-GEIGY AG

  公开号：EP0511940A2

  公开（公告）日：1992-11-04

  Novel N-phosphonomethyl-biaryl substituted dipeptide derivatives of formula I wherein R and R' represent independently hydrogen, carbocyclic aryl, 6-tetrahydronaphthyl, 5-indanyl, acyloxymethyl or acyloxymethyl monosubstituted on methyl carbon by C1-C2o-alkyl, by C5-C7-cycloalkyl, by aryl or by aryl-lower alkyl ; A represents a direct bond, lower alkylene, phenylene or cyclohexylene ; m represents 1 or zero, provided that m represents 1 when A is a direct bond ; R1 represents phenyl, phenyl substituted by one to three substituents selected from lower alkyl, hydroxy, lower alkoxy, lower alkanoyloxy, halogen, cyano, trifluoromethyl, lower alkanoylamino or lower alkoxycarbonyl, naphthyl, naphthyl substituted by lower alkyl, lower alkoxy or halogen, thienyl, thienyl substituted by lower alkyl, furanyl, furanyl substituted by lower alkyl, pyridyl, pyridyl substituted by lower alkyl, halogen or cyano, pyrrolyl or N-lower alkylpyrrolyl ; R2 represents hydrogen, hydroxy, lower alkyl, aryl-lower alkyl, C5-C7-cycloalkyl-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, lower alkylthio-lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkylthio-lower alkyl or aryl-lower alkoxy-lower alkyl ; COR3 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester or amide ; and pharmaceutically acceptable salts thereof are useful as neutral endopeptidase (NEP) inhibitors. Suitable methods for their be manufacture are described.

  式 I 的新颖 N-膦酰甲基-叔丁基取代二肽衍生物 其中 R 和 R'独立地代表氢、碳环芳基、6-四氢萘基、5-茚基、酰氧基甲基或在甲基碳上被 C1-C2o- 烷基、C5-C7-环烷基、芳基或芳基-低级烷基单取代的酰氧基甲基；A 代表直接键、低级亚烷基、亚苯基或环己基；m 代表 1 或 0，但当 A 为直接键时，m 代表 1；R1 代表苯基、被选自低级烷基、羟基、低级烷氧基、低级烷酰氧基、卤素、氰基、 三氟甲基、低级烷酰胺基或低级烷氧基羰基的一至三个取代基取代的苯基、萘基被低级烷基、低级烷氧基或卤素取代的萘基，噻吩基，被低级烷基取代的噻吩基，呋喃基，被低级烷基取代的呋喃基，吡啶基，被低级烷基、卤素或氰基取代的吡啶基，吡咯基或 N-低级烷基吡咯基；R2代表氢、羟基、低级烷基、芳基-低级烷基、C5-C7-环烷基-低级烷基、氨基-低级烷基、羟基-低级烷基、低级烷硫基-低级烷基、低级烷氧基-低级烷基、芳基-低级烷硫基-低级烷基或芳基-低级烷氧基-低级烷基；COR3代表羧基或以药学上可接受的酯或酰胺形式衍生的羧基；其药学上可接受的盐可用作中性内肽酶（NEP）抑制剂。本文介绍了制造它们的适当方法。