替拉西秦 | 83275-56-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 中文名称: 替拉西秦
• 英文名称: 3-carbethoxyamino-5-dimethylaminoacetyl-10,11-dihydro-5H-dibenzazepine
• 英文别名: 3-Carbethoxyamino-5-dimethylaminoacetyl-iminodibenzyl；Bonnecor-Base；tiracizin；bonnecor；3-carbethoxyamino-5-dimethylaminoacetyl-10,11-dihydro-5H-dibenz[b,f]azepine；Tiracizine；ethyl N-[11-[2-(dimethylamino)acetyl]-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate
• CAS: 83275-56-3
• 化学式: C₂₁H₂₅N₃O₃
• mdl: MFCD00870638
• 分子量: 367.448
• InChiKey: KJAMZCVTJDTESW-UHFFFAOYSA-N

物化性质

• 熔点：
  127-128 °C(Solv: isopropanol (67-63-0))
• 沸点：
  525.3±50.0 °C(Predicted)
• 密度：
  1?+-.0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  61.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  替拉西秦 生成 10,11-二氢-5H-二苯[b,f]氮杂革-3-胺
  参考文献：
  名称：

  KOSILOVA, E. E.;BELOBORODOV, V. L.;RODIONOV, A. P.;LYSKOVTSEV, V. V.;ZALE+, MATER. MEZHDUNAR. NAUCH. SIMP. METOZHY KONTROLYA LEKARSTV. SREDSTV: COBPE+

  摘要：

  DOI：
• 作为产物：
  描述：

  10,11-二氢-5H-二苯[b,f]氮杂革-3-胺 在 sodium carbonate 作用下， 以 水 、 丙酮 、 甲苯 为溶剂， 反应 9.5h， 生成 替拉西秦
  参考文献：
  名称：

  Wunderlich; Stark; Carstens, Pharmazie, 1985, vol. 40, # 12, p. 827 - 830

  摘要：

  DOI：

文献信息

• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• Arrays of nucleic acid probes for analyzing biotransformation genes
  申请人：Cronin T. Maureen

  公开号：US20070054286A1

  公开（公告）日：2007-03-08

  The invention provides arrays of immobilized probes, and methods employing the arrays, for detecting mutations in the biotransformation genes, such as cytochromes P450. For example, one such array comprises four probe sets. A first probe set comprises a plurality of probes, each probe comprising a segment of at least three nucleotides exactly complementary to a subsequence of a reference sequence from a biotransformation gene, the segment including at least one interrogation position complementary to a corresponding nucleotide in the reference sequence. Second, third and fourth probe sets each comprise a corresponding probe for each probe in the first probe set. The probes in the second, third and fourth probe sets are identical to a sequence comprising the corresponding probe from the first probe set or a subsequence of at least three nucleotides thereof that includes the at least one interrogation position, except that the at least one interrogation position is occupied by a different nucleotide in each of the four corresponding probes from the four probe sets.

  本发明提供了固定探针的阵列和使用该阵列的方法，用于检测生物转化基因中的突变，例如细胞色素P450。例如，其中一个这样的阵列包括四个探针集。第一个探针集包括多个探针，每个探针包括至少三个核苷酸片段，完全互补于生物转化基因的参考序列的子序列，该片段包括至少一个与参考序列中对应核苷酸互补的询问位置。第二、第三和第四个探针集分别包括与第一个探针集中的每个探针相对应的探针。第二、第三和第四个探针集中的探针与包括来自第一个探针集的相应探针或至少包括该询问位置的三个核苷酸的子序列相同，不同的是四个相应探针中的每个探针中的至少一个询问位置由不同的核苷酸占据。
• CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS FOR PROLONGED EFFECT
  申请人：Hemmingsen Pernille Hoyrup

  公开号：US20100239667A1

  公开（公告）日：2010-09-23

  Layered pharmaceutical composition suitable for oral use in the treatment of diseases where absorption takes place over a large part of the gastrointestinal tract. The composition comprising A) a solid inner layer comprising i) an active substance, and ii) one or more disintegrants/exploding agents, one of more effervescent agents or a mixture thereof. the solid inner layer being sandwiched between two outer layers B1) and B2), each outer layer comprising iii) a substantially water soluble and/or crystalline polymer or a mixture of substantially water soluble and/or crystalline polymers, the polymer being a polyglycol in the form of one of a) a homopolymer having a MW of at least about 100,000 daltons, and b) a copolymer having a MW of at least about 2,000 daltons, or a mixture thereof, and iv) an active substance, which is the same as in said solid inner layer A), and layer A being different from layer B, the layered composition being coated with a coating C) that has at least one opening exposing at least one surface of said outer layer, the coating being substantially insoluble in and impermeable to fluids and comprising a polymer, and the composition having a cylindrical form optionally with one or more tapered ends, wherein the ratio between the surface area of one end surface of the cylinder and the length of the cylinder is in a range of from 0.02 to 45 mm.

  分层制药组合物，适用于口服治疗吸收发生在胃肠道大部分的疾病。该组合物包括A) 一个固体内层，其中包括i) 一种活性物质，和ii) 一种或多种分散剂/爆炸剂，一种或多种泡腾剂或其混合物。该固体内层被夹在两个外层B1)和B2)之间，每个外层包括iii) 一种或多种水溶性和/或结晶聚合物，或者水溶性和/或结晶聚合物的混合物，聚合物为聚乙二醇，形式为a) 分子量至少为约100,000道尔顿的同聚物，和b) 分子量至少为约2,000道尔顿的共聚物，或其混合物，和iv) 一种活性物质，其与所述固体内层A)中的活性物质相同，且层A与层B不同，该分层组合物被涂覆有一种涂层C)，该涂层具有至少一个开口，暴露出至少一个外层的表面，该涂层在液体中具有相当的不溶性和不透性，包括一种聚合物，该组合物具有圆柱形状，可选地具有一个或多个锥形端部，其中圆柱体的一个端面的表面积与圆柱体的长度之比在0.02至45毫米的范围内。
• Novel kinase inhibitors
  申请人：Thormann Michael

  公开号：US20120329785A1

  公开（公告）日：2012-12-27

  The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases.

  本发明涉及式（I）的新型化合物，这些化合物能够抑制一个或多个激酶，特别是SYK（脾酪氨酸激酶）、LRRK2（富含亮氨酸重复的激酶2）和/或MYLK（肌球蛋白轻链激酶）或其突变体。这些化合物可用于治疗各种疾病。
• Arrays of Nucleic Acid Probes for Analyzing Biotransformation Genes
  申请人：Cronin Maureen T.

  公开号：US20130150248A1

  公开（公告）日：2013-06-13

  The invention provides arrays of immobilized probes, and methods employing the arrays, for detecting mutations in the biotransformation genes, such as cytochromes P450. For example, one such array comprises four probe sets. A first probe set comprises a plurality of probes, each probe comprising a segment of at least three nucleotides exactly complementary to a subsequence of a reference sequence from a biotransformation gene, the segment including at least one interrogation position complementary to a corresponding nucleotide in the reference sequence. Second, third and fourth probe sets each comprise a corresponding probe for each probe in the first probe set. The probes in the second, third and fourth probe sets are identical to a sequence comprising the corresponding probe from the first probe set or a subsequence of at least three nucleotides thereof that includes the at least one interrogation position, except that the at least one interrogation position is occupied by a different nucleotide in each of the four corresponding probes from the four probe sets.

  本发明提供了一种固定探针阵列及其应用方法，用于检测生物转化基因中的突变，例如细胞色素P450。例如，其中一种阵列包括四个探针集合。第一探针集合包括多个探针，每个探针包括至少三个核苷酸片段，与生物转化基因的参考序列的一个子序列完全互补，该片段包括至少一个与参考序列中相应核苷酸互补的询问位置。第二、第三和第四探针集合分别包括与第一探针集合中的每个探针相应的探针。第二、第三和第四探针集合中的探针与第一探针集合中相应探针的序列相同，或包括至少三个核苷酸的子序列，其中包括至少一个询问位置，但是四个探针集合中的四个相应探针中的至少一个询问位置被不同的核苷酸占据。