2-Acetamidoacetamide;2,2,2-trichloroethane-1,1-diol | 17427-14-4

• 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
• 英文名称: 2-Acetamidoacetamide;2,2,2-trichloroethane-1,1-diol
• 英文别名: 2-acetamidoacetamide;2,2,2-trichloroethane-1,1-diol
• CAS: 17427-14-4
• 化学式: C6H11Cl3N2O4
• 分子量: 281.5
• InChiKey: IYWCBBFJDGWEAZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.72
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  113
• 氢给体数：
  4
• 氢受体数：
  4

文献信息

• [EN] TRIAZOLOBENZAZEPINES AS VASOPRESSIN V1A RECEPTOR ANTAGONISTS<br/>[FR] TRIAZOLOBENZAZÉPINES UTILISÉES EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE LA VASOPRESSINE V1A
  申请人：RICHTER GEDEON NYRT

  公开号：WO2019116324A1

  公开（公告）日：2019-06-20

  The present invention relates to 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine derivatives of general formula (I) and/or salts thereof and/or geometric isomers thereof and/or stereoisomers thereof and/or enantiomers thereof and/or racemates thereof and/or diastereomers thereof and/or biologically active metabolites thereof and/or prodrugs thereof and/or solvates thereof and/or hydrates thereof and/or polymorphs thereof which are centrally and/or peripherally acting V1a receptor modulators, particularly V1a receptor antagonists. Additional subject of the present invention is the process for the preparation of the compounds and the intermediates of the preparation process as well. The invention also relates to the pharmaceutical compositions containing the compounds or together with one or more other active substances, as well as to the use in the treatment and/or prophylaxis of a disease or condition associated with V1a receptor function.

  本发明涉及一般式(I)的5,6-二氢-4H-[1,2,4]三唑并[4,3-a][1]苯并蒽啉衍生物和/或其盐和/或其几何异构体和/或其立体异构体和/或其对映异构体和/或其消旋体和/或其非对映异构体和/或其生物活性代谢物和/或其前药和/或其溶剂化合物和/或其水合物和/或其多晶形式，这些化合物是中枢和/或外周作用的V1a受体调节剂，特别是V1a受体拮抗剂。本发明的另一个主题是制备这些化合物的过程以及制备过程的中间体。该发明还涉及含有这些化合物或与一个或多个其他活性物质一起的药物组合物，以及在治疗和/或预防与V1a受体功能相关的疾病或症状中的用途。
• [EN] TRICYCLIC COMPOUNDS AS VASOPRESSIN V1A RECEPTOR ANTAGONISTS<br/>[FR] COMPOSÉS TRICYCLIQUES UTILISÉS EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE LA VASOPRESSINE V1A
  申请人：RICHTER GEDEON NYRT

  公开号：WO2019116325A1

  公开（公告）日：2019-06-20

  The present invention relates to 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine derivatives of general formula (I) and/or salts thereof and/or geometric isomers thereof and/or stereoisomers thereof and/or enantiomers thereof and/or racemates thereof and/or diastereomers thereof and/or biologically active metabolites thereof and/or prodrugs thereof and/or solvates thereof and/or hydrates thereof and/or polymorphs thereof which are centrally and/or peripherally acting V1a receptor modulators, particularly V1a receptor antagonists. Additional subject of the present invention is the process for the preparation of the compounds and the intermediates of the preparation process as well. The invention also relates to the pharmaceutical compositions containing the compounds or together with one or more other active substances, as well as to the use in the treatment and/or prophylaxis of a disease or condition associated with V1a receptor function.

  本发明涉及通式（I）的5,6-二氢-4H-[1,2,4]三唑[4,3-a][1]苯并蒽啉衍生物和/或其盐和/或其几何异构体和/或其立体异构体和/或其对映异构体和/或其消旋体和/或其二对映异构体和/或其生物活性代谢物和/或其前药和/或其溶剂化合物和/或其水合物和/或其多晶型，这些化合物是中枢和/或外周作用V1a受体调节剂，特别是V1a受体拮抗剂。本发明的另一个主题是化合物的制备方法以及制备过程的中间体。该发明还涉及含有这些化合物或与一个或多个其他活性物质一起的药物组合物，以及在治疗和/或预防与V1a受体功能相关的疾病或症状中的使用。
• 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。
• Controlled release formulation with continuous efficacy
  申请人：Egalet Ltd.

  公开号：EP2700400A1

  公开（公告）日：2014-02-26

  The present invention relates to pharmaceutical compositions, which provide controlled release of a drug. The compositions are suitable for continuous administration as they remain effective throughout the treatment regimen. The present invention also relates to the use of the compositions for preparation of a medicament for continuous treatment of an individual.

  本发明涉及可控制药物释放的药物组合物。这些组合物适合连续给药，因为它们在整个治疗过程中都能保持有效。本发明还涉及使用这些组合物制备用于对个人进行连续治疗的药物。
• Pharmaceutical compositions resistant to abuse
  申请人：Egalet Ltd.

  公开号：US10105321B2

  公开（公告）日：2018-10-23

  The present invention provides immediate release pharmaceutical compositions for oral administration that are resistant to abuse.

  本发明提供了抗滥用的口服速释药物组合物。