Isoleucyl-thiazolidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: Isoleucyl-thiazolidine
• 英文别名: (2S,3S)-2-amino-3-methyl-1-(1,3-thiazolidin-2-yl)pentan-1-one
• 化学式: C₉H₁₈N₂OS
• 分子量: 202.32
• InChiKey: ARNUPLMOASAEAN-ASLNEKEESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  80.4
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels
  申请人：——

  公开号：US20030176357A1

  公开（公告）日：2003-09-18

  The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for lowering blood pressure levels.

  本发明提供了本发明的DPIV抑制剂的新用途，以及其相应的药用可接受的酸盐形式，用于降低血压水平。
• Novel compounds and therapeutic uses thereof
  申请人：TORRENT PHARMACEUTICALS LTD.

  公开号：US20040106802A1

  公开（公告）日：2004-06-03

  The invention discloses a novel series of compound represented by general formula (I), 1 its derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, pharmaceutically acceptable salts, solvates wherein X, n, k, z, R1, R2, R3, R4, R5 and R6 are as defined in the specification that are useful in (i) normalizing elevated blood glucose levels in diabetes, (ii) treating disorders related to glucose intolerance and (iii) for scavenging free radicals of mammals. The invention also discloses pharmaceutically acceptable composition comprising these compounds, method for preparation of the compounds as defined above and method of treating mamnnals including human beings by administering an effective amount of said compounds to a subject in need thereof. The invention further discloses use of these compounds in the manufacture of a medicament useful for treatment of different disease conditions as stated above.

  该发明揭示了一种由通式(I)表示的新型化合物系列，其衍生物、类似物、互变异构体、立体异构体、多型体、药用可接受盐、溶剂合物，其中X、n、k、z、R1、R2、R3、R4、R5和R6如规范中定义的那样，在(i)正常化糖尿病患者的升高血糖水平，(ii)治疗与葡萄糖不耐受有关的疾病，以及(iii)清除哺乳动物体内自由基方面具有用处。该发明还揭示了包括这些化合物的药用可接受组合物，所述化合物的制备方法如上所述，并通过向需要的受试者施用有效量的该化合物来治疗包括人类在内的哺乳动物的方法。该发明进一步揭示了这些化合物在制造用于治疗上述不同疾病状况的药物中的应用。
• Novel compounds that inhibit dipeptidyl peptidase (DPP-IV) and neprilysin (NEP) and/or angiotensin converting enzyme (ACE)
  申请人：Pierau Sabine

  公开号：US20060046978A1

  公开（公告）日：2006-03-02

  This invention relates to novel compounds, compositions containing the compounds, that inhibit dipeptidyl peptidase (especially DPP-IV) and neprilysin (NEP, neutral endopeptidase) as well as dipeptidyl peptidase (especially DPP-IV) and angiotensin converting enzyme (ACE) and/or dipeptidyl Peptidase (especially DPP-IV) and vasopeptidases (especially ACE and NEP). These compounds and pharmaceutical compositions thereof are useful for the treatment as well as the prevention of type 2 diabetes mellitus.

  该发明涉及新型化合物，含有这些化合物的组合物，这些化合物抑制二肽基肽酶（特别是DPP-IV）和神经肽酶（NEP，中性内肽酶）以及二肽基肽酶（特别是DPP-IV）和血管紧张素转化酶（ACE）和/或二肽基肽酶（特别是DPP-IV）和血管肽酶（特别是ACE和NEP）。这些化合物及其药物组合物对于治疗和预防2型糖尿病是有用的。
• [EN] AZOLIDINECARBONITRILES AND THEIR USE AS DPP-IV INHIBITORS<br/>[FR] AZOLIDINECARBONITRILES ET LEUR APPLICATION COMME INHIBITEURS DE DPP-IV
  申请人：SANKARANARAYANAN ALANGUDI

  公开号：WO2005033106A1

  公开（公告）日：2005-04-14

  The invention discloses a novel heterocyclic compounds that falls within f the ambit of general formula (I), its stereoisomers, pharmaceutically acceptable salts or solvates wherein X, n,k,z, R1, R2, R3, R4, R5 and R6 are as defined in the specification that are useful in (i) normalizing elevated blood pglucose levels in diabetes, (ii) treating disorders related to glucose intolerance and (iii) for scavenging free radicals of mammals. The invention also discloses pharmaceutically acceptable composition comprising these compounds, method for preparation of the compounds as defined bove and method of treating mammals including human beings by administering an effective amount of said compounds to a subject in need thereof. The invention further discloses use of these compounds in the manufacture of a medicament useful for treatment of different disease conditions as stated above.

  本发明公开了一种新型杂环化合物，属于一般式(I)的范围内，其立体异构体、药学上可接受的盐或溶剂，其中X、n、k、z、R1、R2、R3、R4、R5和R6如规范中所定义，可用于(i)正常化糖尿病患者的高血糖水平，(ii)治疗与葡萄糖不耐受有关的疾病和(iii)清除哺乳动物的自由基。本发明还公开了包含这些化合物的药学上可接受的组合物，制备上述化合物的方法以及通过向需要此类化合物的受试者投与有效量的化合物来治疗哺乳动物包括人类的方法。本发明还公开了这些化合物在制造用于治疗上述不同疾病状态的药物中的使用。
• New effectors of dipeptidyl peptidase IV for topical use
  申请人：——

  公开号：US20020165164A1

  公开（公告）日：2002-11-07

  The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula 1 wherein A is an amino acid having at least one functional group in the side chain; B is a chemical compound covalently bound to a functional group of the side chain of A, chosen from the group consisting of (a) oligopeptides having a chain length of up to 20 amino acids, (b) homopolymers of glycine consisting of up to 6 glycine monomers, and (c) polyethylene glycols having molar masses of up to 20 000 g/mol; and C is a group amide-bonded to A chosen from the group consisting of thiazolidine, pyrrolidine, cyanopyrrolidine, hydroxyproline, dehydroproline or piperidine. The invention further relates to the use of said compounds for targeted intervention in local immunological processes (chemotaxis, inflammatory processes, autoimmune diseases), as well as effective and targeted treatment of pathophysiological and physiological processes related thereto (psoriasis, periodontitis, arthritis, allergies, inflammation), inter alia.

  本发明涉及一种影响二肽基肽酶活性的局部化合物，其通式为1，其中： A是具有至少一个侧链功能基团的氨基酸； B是与A的侧链功能基团共价结合的化合物，所述化合物选择自以下组中的一种：(a)链长高达20个氨基酸的寡肽；(b)由高达6个甘氨酸单体组成的甘氨酸同聚物；以及(c)摩尔质量高达20,000克/摩尔的聚乙二醇； C是与A酰胺键结合的基团，所述基团选择自以下组中的一种：噻唑烷、吡咯烷、氰基吡咯烷、羟脯氨酸、去氢脯氨酸或哌啶。 本发明还涉及使用上述化合物进行靶向干预局部免疫过程（趋化作用、炎症过程、自身免疫疾病），以及有效和有针对性地治疗与之相关的病理生理过程（牛皮癣、牙周炎、关节炎、过敏、炎症）等。