Antienit, 5,6-Dihydro-6-(2-thienyl)-imidazo<2,1-b>thiazol | 5719-88-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并噻唑类
• 英文名称: Antienit, 5,6-Dihydro-6-(2-thienyl)-imidazo<2,1-b>thiazol
• 英文别名: 6-thiophen-2-yl-5,6-dihydro-imidazo[2,1-b]thiazole；Antienite；6-thiophen-2-yl-5,6-dihydroimidazo[2,1-b][1,3]thiazole
• CAS: 5719-88-0
• 化学式: C₉H₈N₂S₂
• 分子量: 208.308
• InChiKey: RFOLEEQBNNSICL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  69.1
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  Antienit, 5,6-Dihydro-6-(2-thienyl)-imidazo<2,1-b>thiazol 在 盐酸 作用下， 以 乙醚 、 丙酮 为溶剂， 生成 6-thiophen-2-yl-5,6-dihydro-imidazo[2,1-b]thiazole hydrochloride
  参考文献：
  名称：

  Synthesis and evaluation of thiophenyl derivatives as inhibitors of alkaline phosphatase

  摘要：

  Pathological calcifications induced by deposition of basic phosphate crystals or hydroxyapatite (HA) on soft tissues are a large family of diseases comprising of ankylosing spondylitis (AS), end-stage osteoarthritis (OA) and vascular calcification. High activity of tissue non-specific alkaline phosphatase (TNAP) is a hallmark of pathological calcifications induced by HA deposition. The use of TNAP inhibitor is a possible therapeutic option to address calcific diseases produced by HA deposition on soft tissues. We report the synthesis of a series of thiopheno-imidazo[2,1-b] thiazole derivatives which were evaluated as potential inhibitors of TNAP displaying a large range of IC50 at pH 10.4 (from 42 +/- 13 mu M to more than 800 mu M). (C) 2011 Published by Elsevier Ltd.

  DOI：

  10.1016/j.bmcl.2011.02.089
• 作为产物：
  描述：

  2-Imino-3-(2-thenoylmethyl)thiazoline 在 sodium tetrahydroborate 、 氯化亚砜 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 反应 2.5h， 生成 Antienit, 5,6-Dihydro-6-(2-thienyl)-imidazo<2,1-b>thiazol
  参考文献：
  名称：

  Synthesis and evaluation of thiophenyl derivatives as inhibitors of alkaline phosphatase

  摘要：

  Pathological calcifications induced by deposition of basic phosphate crystals or hydroxyapatite (HA) on soft tissues are a large family of diseases comprising of ankylosing spondylitis (AS), end-stage osteoarthritis (OA) and vascular calcification. High activity of tissue non-specific alkaline phosphatase (TNAP) is a hallmark of pathological calcifications induced by HA deposition. The use of TNAP inhibitor is a possible therapeutic option to address calcific diseases produced by HA deposition on soft tissues. We report the synthesis of a series of thiopheno-imidazo[2,1-b] thiazole derivatives which were evaluated as potential inhibitors of TNAP displaying a large range of IC50 at pH 10.4 (from 42 +/- 13 mu M to more than 800 mu M). (C) 2011 Published by Elsevier Ltd.

  DOI：

  10.1016/j.bmcl.2011.02.089

文献信息

• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Intraruminal drug delivery device
  申请人：COOPERS ANIMAL HEALTH LIMITED

  公开号：EP0333311A1

  公开（公告）日：1989-09-20

  An intraruminal device for administering an active agent in the rumen of an animal, comprises a metal weight (8) which gives the device sufficient density to be retained in the rumen which is made from compacted unsintered metal. The metal weight may be cylindrical and constructed of one (8, 20, 37 or 44) or several (31,32) pieces of compacted unsintered metal, of a tubular or annular (21,69) nature or incorporated as a discrete mass (66) within a drug matrix (67). When the weight is in an exposed position of the device (e.g. Fig.4), it is preferably enclosed with a material (38) that prevents damage to the weight from rough handling.

  一种用于在动物瘤胃中施用活性剂的瘤胃内装置，包括一个金属重块（8），它使装置具有足够的密度，可保留在瘤胃中，金属重块由压实的未烧结金属制成。金属砝码可以是圆柱形的，由一块（8、20、37 或 44）或几块（31、32）压实的未烧结金属组成，具有管状或环状（21、69）的性质，或作为一个离散的块状物（66）包含在药物基质（67）中。当砝码处于设备的外露位置时（如图 4），最好用材料（38）将其封闭，以防止砝码因粗暴操作而损坏。
• Dispensing devices
  申请人：COOPERS ANIMAL HEALTH LIMITED

  公开号：EP0398663A1

  公开（公告）日：1990-11-22

  An intraruminal device for administering an active agent into the rumen of an animal, comprising a chamber (3) enclosing the active material between a closure (2) and propulsion means (a piston) (8), one of the closure and propulsion means has one or more apertures for expulsion of the active material. The active material is conveniently expelled from the device by means of a piston biased against it by the tension of the spring. The tension spring may be constructed of materials that are environmentally preferred to metal springs and in addition hold the device together.

  一种将活性剂注入动物瘤胃的瘤胃内装置，包括一个腔室（3），将活性物质封闭在封闭装置（2）和推进装置（活塞）（8）之间，其中一个封闭装置和推进装置有一个或多个孔，用于排出活性物质。通过活塞在弹簧拉力的作用下将活性材料排出装置，非常方便。拉力弹簧可由比金属弹簧更环保的材料制成，此外还可将装置固定在一起。
• 8-ARM POLYETHYLENE GLYCOL DERIVATIVE, MANUFACTURING METHOD AND MODIFIED BIO-RELATED SUBSTANCE THEREBY
  申请人：Xiamen Sinopeg Biotech Co., Ltd.

  公开号：EP3315531A1

  公开（公告）日：2018-05-02

  Disclosed are an 8-arm polyethylene glycol (PEG) derivative (formula 1), manufacturing method and modified bio-related substance thereby, wherein a tetravalent group U and four trivalent groups Ec form a highly symmetric octavalent central structure CORE0 together, Lc connects the octavalent center to eight PEG arms having polydiversity or monodiversity and having n1-n8 as the degrees of polymerization thereof. The terminal of one PEG chain is connected to at least one functional group F (k ≥ 1), and said PEG chain and F can be directly connected (g = 0) or connected with a divalent linking group L0 connected with a terminal branched group G (g = 1) therebetween. The latter provides more reacting sites to combine more pharmaceutical molecules, thereby increasing the drug loading capacity. The near-center symmetric structure of the derivative allows more precise control over the molecular weight during large-scale production, thereby facilitating acquisition of a product having a narrower molecular weight distribution. A bio-related substance modified thereby has a more uniform and controllable performance.

  本发明公开了一种 8 臂聚乙二醇（PEG）衍生物（式 1）、其制造方法和改性生物相关物质，其中一个四价基团 U 和四个三价基团 Ec 共同形成一个高度对称的八价中心结构 CORE0，Lc 将八价中心连接到八个 PEG 臂上，这些 PEG 臂具有多元性或单元性，其聚合度为 n1-n8。一条 PEG 链的末端与至少一个官能团 F（k ≥ 1）相连，所述 PEG 链和 F 可以直接相连（g = 0），也可以通过二价连接基 L0 与中间的末端支化基 G（g = 1）相连。后者提供了更多的反应位点，可以结合更多的药物分子，从而提高药物负载能力。衍生物的近中心对称结构可以在大规模生产过程中更精确地控制分子量，从而有利于获得分子量分布更窄的产品。由此改性的生物相关物质具有更均匀、更可控的性能。
• Eight-arm polyethylene glycol derivative, production method therefor, and modified bio-related substance thereof
  申请人：XIAMEN SINOPEG BIOTECH CO., LTD.

  公开号：US10434182B2

  公开（公告）日：2019-10-08

  Disclosed are an eight-arm polyethylene glycol (PEG) derivative (formula I), production method therefor and modified bio-related substance thereby. Wherein, one tetravalent group U together with four trivalent groups Ec form a highly symmetrical octavalent group CORE0; Lc connects the octavalent group to eight PEG chains having polydispersity or monodispersity and having n1 to n8 as the degree of polymerization thereof; the terminal of one PEG chain is connected to at least one functional group F (k≥1); said PEG chain and F therebetween can be directly connected (g=0) or be indirectly connected via a linking group L0 to a terminal end-branching group G (g=1); the latter provides more reactive sites for binding more drug molecules and increases the drug loading. The eight-arm polyethylene glycol derivative has a centrosymmetric or approximately centrosymmetric structure, and leads to more precise control of the molecular weight in large-scale production and much narrower distribution of molecular weight for products. The modified bio-related substance thereby has a more uniform and controllable performance.

  本发明公开了一种八臂聚乙二醇（PEG）衍生物（式 I）、其生产方法及其改性生物相关物质。其中，一个四价基团 U 与四个三价基团 Ec 形成一个高度对称的八价基团 CORE0；Lc 将八价基团连接到八条具有多分散性或单分散性且聚合度为 n1 至 n8 的 PEG 链上；一条 PEG 链的末端与至少一个官能团 F 连接（k≥1）；所述 PEG 链和 F 之间可以直接连接（g=0），也可以通过连接基团 L0 与末端支化基团 G 间接连接（g=1）；后者提供了更多的反应位点，可以结合更多的药物分子，增加药物负载量。八臂聚乙二醇衍生物具有中心对称或近似中心对称结构，因此在大规模生产中可以更精确地控制分子量，产品的分子量分布也更窄。因此，改性生物相关物质的性能更均匀、更可控。