[(1S,2S)-2-[[2,2-dimethylpropyl(nonyl)carbamoyl]amino]cyclohexyl] 3-[(2,2,5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propanoate

• 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: [(1S,2S)-2-[[2,2-dimethylpropyl(nonyl)carbamoyl]amino]cyclohexyl] 3-[(2,2,5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propanoate
• 化学式: C₃₃H₆₁N₃O₆
• 分子量: 595.9
• InChiKey: NWLFOBZKYXKBOF-QIELNMHASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.2
• 重原子数：
  42
• 可旋转键数：
  17
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.91
• 拓扑面积：
  106
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Absorption-enhancing composition for pantothenic acid derivative
  申请人：FUJIREBIO INC.

  公开号：EP0998927A1

  公开（公告）日：2000-05-10

  A composition showing an improved bioavailability rate of pantothenic acid derivatives represented by the following general formula and improved storage stability and being applicable as drugs over an enlarged range: wherein R1 and R2 are the same or different and each represents a hydrogen atom or a hydroxyl-protective group; R3 represents a saturated or unsaturated, linear, branched or cyclic C5-25 monovalent aliphatic hydrocarbon group optionally substituted by an aromatic group, or an amino group represented by the formula -N(R4)R5 (wherein R4 represents a saturated or unsaturated, linear, branched or cyclic C5-25 monovalent aliphatic hydrocarbon group; and R5 represents a hydrogen atom or a saturated or unsaturated, linear, branched or cyclic monovalent aliphatic hydrocarbon group optionally substituted by an aromatic group); A represents a saturated or unsaturated, linear, branched or cyclic C2-16 divalent aliphatic hydrocarbon group, divalent aromatic hydrocarbon group or divalent heteroaryl group optionally substituted by an aromatic group; one of X and Y represents an amino group represented by the formula -N(R6)- while the other represents -O-, -S- or an amino group represented by the formula -N(R7)- (wherein R6 and R7 represent each a hydrogen atom or a lower alkyl group); and n is an integer of from 1 to 4. The pantothenic acid derivative represented by the above general formula (I) is dissolved in a neutral or alcoholic ester and a nonionic surfactant is added thereto to give the absorption-enhancing composition.

  一种通式如下的泛酸衍生物组合物，其生物利用率有所提高，贮存稳定性有所改善，可在更大范围内作为药物使用： 其中 R1 和 R2 相同或不同，各自代表氢原子或羟基保护基团； R3 代表饱和或不饱和、线性、支链或环状 C5-25 单价脂肪族烃基，可选择被芳香族基团取代，或由式 -N(R4)R5 所代表的氨基（其中 R4 代表饱和或不饱和、线性、支链或环状 C5-25 单价脂肪族烃基；R5 代表氢原子或饱和或不饱和、线性、支链或环状单价脂肪族烃基，可选择被芳香族基团取代）； A 代表饱和或不饱和、线性、支链或环状 C2-16 二价脂肪族烃基、二价芳香族烃基或任选被芳香族基团取代的二价杂芳基； X 和 Y 中的一个代表由式-N(R6)-表示的氨基，而另一个代表-O-、-S-或由式-N(R7)-表示的氨基（其中 R6 和 R7 分别代表氢原子或低级烷基）；以及 将上述通式（I）所代表的泛酸衍生物溶解在中性酯或醇酯中，再加入非离子表面活性剂，即可得到增强吸收的组合物。
• NOVEL ANILIDE COMPOUNDS AND DRUGS CONTAINING THE SAME
  申请人：Kowa Co., Ltd.

  公开号：EP1020451A1

  公开（公告）日：2000-07-19

  The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same. The invention relates to a compound represented by the following general formula:    represents a divalent residue of benzene with a substituent(s), heterocycle-condensed benzene which may or may not have a substituent, pyridine which may or may not have a substituent, cyclohexane or naphthalene or Ar represents an aryl group which may or may not have a substituent; X represents -NH-, oxygen atom or sulfur atom; Y represents -NR4-, oxygen atom, sulfur atom, sulfoxide or sulfone; Z represents single bond or -NR5-; R4 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; R5 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; and n represents an integer of 0 to 15. The inventive compounds are useful in the form of pharmaceutical composition, specifically as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitor.

  本发明涉及一种新型苯胺化合物和含有该化合物的药物组合物。本发明涉及由以下通式代表的化合物： 代表带有取代基的苯、可能带有也可能不带取代基的杂环缩合苯、可能带有也可能不带取代基的吡啶、环己烷或萘的二价残基 或 Ar 代表芳基，可以有取代基，也可以没有取代基； X 代表-NH-、氧原子或硫原子； Y 代表-NR4-、氧原子、硫原子、亚砜或砜； Z 代表单键或-NR5-； R4 代表氢原子、低级烷基、芳基或硅烷化低级烷基，可带有或不带有取代基； R5 代表氢原子、低级烷基、芳基或硅烷化低级烷基，可以有或没有取代基；以及 n 代表 0 至 15 的整数。 本发明化合物以药物组合物的形式使用，特别是作为酰基辅酶 A 胆固醇酰基转移酶（ACAT）抑制剂。
• MEDICINAL COMPOSITIONS CONTAINING ANGIOTENSIN II RECEPTOR ANTAGONIST
  申请人：Sankyo Company, Limited

  公开号：EP1421953A1

  公开（公告）日：2004-05-26

  The present invention relates to a pharmaceutical composition for administering simultaneously, separately or sequentially an angiotensin II receptor antagonist and an ACAT inhibitor.

  本发明涉及一种药物组合物，用于同时、分别或依次给药血管紧张素 II 受体拮抗剂和 ACAT 抑制剂。
• MEDICINAL COMPOSITION FOR TREATING ARTERIOSCLEROSIS
  申请人：Sankyo Company, Limited

  公开号：EP1555032A1

  公开（公告）日：2005-07-20

  [Constitution] A medicinal composition characterized in that an ADP receptor antagonist and an ACAT inhibitor are administered either simultaneously or separately at a defined interval. [Advantage] A medicinal composition, wherein an ADP receptor antagonist and an ACAT inhibitor are administered either simultaneously or separately at a defined interval, is useful as a preventive or a remedy (in particular, a remedy) for arteriosclerosis or diseases derived from arteriosclerosis such as ischemic heart disease, ischemic brain disease and peripheral circulation failure in warm-blooded animals (in particular, humans).

  [章程]一种药物组合物，其特征在于，ADP 受体拮抗剂和 ACAT 抑制剂以规定的间隔同时或分别给药。 [优点]一种药物组合物，其中 ADP 受体拮抗剂和 ACAT 抑制剂以规定的间隔同时或分别给药，可用于预防或治疗（特别是）动脉硬化或动脉硬化引起的疾病，如温血动物（特别是人类）的缺血性心脏病、缺血性脑病和外周循环衰竭。
• Thyromimetics for the treatment of fatty liver diseases
  申请人：Cable Edward E.

  公开号：US10130643B2

  公开（公告）日：2018-11-20

  The present invention is directed toward the use of thyromimetic compounds that are thyroid receptor ligands, pharmaceutically acceptable salts thereof, and to prodrugs of these compounds for preventing, treating, or ameliorating fatty liver diseases such as steatosis, non-alcoholic fatty liver disease, and non-alcoholic steatohepatitis.

  本发明的目的是利用作为甲状腺受体配体的拟甲状腺化合物、其药学上可接受的盐以及这些化合物的原药来预防、治疗或改善脂肪肝疾病，如脂肪变性、非酒精性脂肪肝和非酒精性脂肪性肝炎。