(2S)-N-((2'S)-2'-amino-3',3-dimethylbutanoyl)pyrrolidine-2-carbonitrile | 171092-64-1

• 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: (2S)-N-((2'S)-2'-amino-3',3-dimethylbutanoyl)pyrrolidine-2-carbonitrile
• 英文别名: FE 999011；(2S)-1-([2'S]-2'-amino-3',3'-dimethyl-butanoyl)-pyrrolidine-2-carbonitrile；2-Pyrrolidinecarbonitrile, 1-((2S)-2-amino-3,3-dimethyl-1-oxobutyl)-, (2S)-；(2S)-1-[(2S)-2-amino-3,3-dimethylbutanoyl]pyrrolidine-2-carbonitrile
• CAS: 171092-64-1
• 化学式: C₁₁H₁₉N₃O
• 分子量: 209.291
• InChiKey: XGNBIYXILDDDQR-DTWKUNHWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  70.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  (2S)-1-(2-nitrophenyl)sulfonylpyrrolidine-2-carboxamide 在 吡啶 、 咪唑 、 盐酸 、 benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate 、 三乙胺 、 三氟乙酸 、 三氯氧磷 作用下， 以 1,4-二氧六环 、 乙醚 为溶剂， 生成 (2S)-N-((2'S)-2'-amino-3',3-dimethylbutanoyl)pyrrolidine-2-carbonitrile
  参考文献：
  名称：

  2-cyanopyrrolidides as potent, stable inhibitors of dipeptidyl peptidase IV

  摘要：

  A novel series of stable, potent inhibitors of dipeptidyl peptidase IV has been developed. A number of dipeptide analogues, incorporating a 2-cyanopyrrolidide, were found to have K-i values of less than 5 nM versus human DP-IV and half-lives of >48h in aqueous solution (pH 7.4). (C) 1996 Elsevier Science Ltd

  DOI：

  10.1016/0960-894x(96)00190-4

文献信息

• [EN] COMPOSITIONS AND DOSAGE FORMS FOR ENHANCED ABSORPTION OF METFORMIN<br/>[FR] COMPOSITIONS ET FORMES POSOLOGIQUES POUR UNE ABSORPTION AMELIOREE DE METFORMINE
  申请人：ALZA CORP

  公开号：WO2005041923A1

  公开（公告）日：2005-05-12

  A complex comprised of metformin and a transport moiety, such as a fatty acid, is described. The complex has an enhanced absorption in the gastrointestinal tract, particularly the lower gastrointestinal tract. The complex, and compositions and dosage forms prepared using the complex, provide for absorption by the body of the drug through a period of ten to twenty-four hours, thus enabling a once-daily dosage form for metformin.

  描述了由二甲双胍和传输基团（如脂肪酸）组成的复合物。该复合物在胃肠道中具有增强的吸收，特别是在下消化道。该复合物以及使用该复合物制备的组合物和剂型，使药物在十至二十四小时内通过身体吸收，从而实现二甲双胍的一日一次剂量形式。
• Inhibitors of glutaminyl cyclase
  申请人：——

  公开号：US20040224875A1

  公开（公告）日：2004-11-11

  The present invention relates to compounds that act as inhibitors of QC including those represented by the general formulae 1 to 9: 1 and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Corea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.

  本发明涉及一种作为QC抑制剂的化合物，包括由通式1至9表示的化合物及其组合物，用于治疗神经系统疾病，特别是阿尔茨海默病、唐氏综合症、帕金森病、亨廷顿舞蹈症、病理性精神病症、精神分裂症、食欲不振、睡眠-清醒状态、能量代谢的失调、自主神经功能障碍、激素平衡失调、体液调节失调、高血压、发热、睡眠失调、厌食症、焦虑相关障碍包括抑郁症、癫痫包括药物戒断和酗酒，神经退行性疾病包括认知功能障碍和痴呆症。
• Compositions and dosage forms for enhanced absorption of metformin
  申请人：Wong S.L. Patrick

  公开号：US20050158374A1

  公开（公告）日：2005-07-21

  A complex comprised of metformin and a transport moiety, such as a fatty acid, is described. The complex has an enhanced absorption in the gastrointestinal tract, particularly the lower gastrointestinal tract. The complex, and compositions and dosage forms prepared using the complex, provide for absorption by the body of the drug through a period of ten to twenty-four hours, thus enabling a once-daily dosage form for metformin.

  描述了由二甲双胍和转运基团（例如脂肪酸）组成的复合物。该复合物在胃肠道中，特别是在下消化道中，具有增强的吸收能力。使用该复合物制备的复合物、组合物和剂型，使药物在十至二十四小时内通过身体吸收，从而实现二甲双胍的一天一次剂量。
• Combination therapy for glycaemic control
  申请人：Demuth Hans-Ulrich

  公开号：US20060287251A1

  公开（公告）日：2006-12-21

  The present invention relates to method of treatment, in particular to a method for the treatment of diabetes mellitus, especially non-insulin dependent diabetes mellitus (NIDDM) or Type 2 diabetes and conditions associated with diabetes mellitus the predi,betic state and/or obesity and to compositions for use in s ch method.

  本发明涉及治疗方法，特别是一种用于治疗糖尿病的方法，尤其是非胰岛素依赖性糖尿病（NIDDM）或2型糖尿病以及与糖尿病相关的糖尿病前期状态和/或肥胖症的条件，以及用于该种方法的组合物。
• NOVEL DERIVATIVES OF ACYL CYANOPYRROLIDINES
  申请人：Akolkar Nakul Pramod

  公开号：US20120040897A1

  公开（公告）日：2012-02-16

  A compound of formula (I) or a tautomeric form, regioisomer, stereoisomer, solvate, N-oxide or pharmaceutically acceptable salts thereof; wherein ‘a’—is selected from the group consisting of substituted or unsubstituted heterocycloalkyl ring and substituted or unsubstituted carbohydrate moiety y is a member selected from —O—, —CO—, —S02-, aminoalkyl or formula (II) wherein, R w is hydrogen, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl; x is a member selected from -0-, —S—, —SO—, —S02-, CONR10, NR10CO and —NR d —, or x and y together represent a chemical bond; Z is selected from —CH—, —N—. t is an integer selected from O to 4; with the provisos that when ‘a’ is substituted or unsubstituted heterocycloalkyl ring then ‘t’ is not O and when y=—CO—, x is not NR d .

  化合物的公式（I）或其互变异构体，区域异构体，立体异构体，溶剂化物，N-氧化物或其药学上可接受的盐；其中，‘a’选择自取代或未取代的杂环烷基环或取代或未取代的碳水化合物基团，y为成员选择自—O—，—CO—，—S02-，氨基烷基或公式（II）其中，Rw为氢，取代或未取代的烷基，烯基，炔基，环烷基，芳基，杂环芳基；x为成员选择自-0-，—S—，—SO—，—S02-，CONR10，NR10CO和—NRd—，或x和y一起表示化学键；Z选择自—CH—，—N—。 t为整数，选择自0到4；条件是当‘a’为取代或未取代的杂环烷基环时，‘t’不为0，当y=—CO—时，x不为NRd。