3-(3'-6'-dihydro-2'-H-[2,4']bipyridinyl-1'-yl)-propylamine | 179482-69-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-(3'-6'-dihydro-2'-H-[2,4']bipyridinyl-1'-yl)-propylamine
• 英文别名: 3-(3',6'-Dihydro-[2,4'-bipyridin]-1'(2'H)-yl)propan-1-amine；3-(4-pyridin-2-yl-3,6-dihydro-2H-pyridin-1-yl)propan-1-amine
• CAS: 179482-69-0
• 化学式: C₁₃H₁₉N₃
• 分子量: 217.314
• InChiKey: VRGZFSZAAYVZFS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  16
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  42.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-(3'-6'-dihydro-2'-H-[2,4']bipyridinyl-1'-yl)-propylamine 在 palladium dihydroxide 氢气 作用下， 以 甲醇 为溶剂， 以95%的产率得到3-[4-(pyridin-2-yl)-piperidine-1-yl]propylamine
  参考文献：
  名称：

  Efficient synthesis of the optically active dihydropyrimidinone of a potent α_1A- selective adrenoceptor antagonist

  摘要：

  描述了一种有效的α_1A-选择性肾上腺素受体拮抗剂的汇聚合成。合成的显著特点包括对混合二氢嘧啶酮的酶分离和在2,4'-二吡啶基的合成中使用钯偶联反应。关键词：二氢嘧啶酮，酶分离，钯偶联。

  DOI：

  10.1139/v02-079
• 作为产物：
  描述：

  2,4'-二吡啶 在 sodium tetrahydroborate 作用下， 以 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 10.0h， 生成 3-(3'-6'-dihydro-2'-H-[2,4']bipyridinyl-1'-yl)-propylamine
  参考文献：
  名称：

  Alpha 1A adrenergic receptor antagonists

  摘要：

  这项发明涉及某些新颖化合物及其衍生物，它们的合成以及它们作为α1a肾上腺素受体拮抗剂的用途。这些化合物的一个应用是用于治疗良性前列腺增生。这些化合物在其能够放松富含α1a受体亚型的平滑肌组织方面具有选择性，同时不会引起低血压。这样的组织之一是围绕尿道内膜的组织。因此，这些化合物的一个用途是通过减少尿液流动的阻碍，为患有良性前列腺增生的男性提供急性缓解。这些化合物的另一个用途是与人类5α-还原酶抑制剂化合物结合，从而实现对良性前列腺增生影响的急性和慢性缓解。

  公开号：

  US06339090B1

文献信息

• Dihydropyrimidines and uses thereof
  申请人：Merck and Co., Inc

  公开号：US20010041707A1

  公开（公告）日：2001-11-15

  This invention is directed to dihydropyrimidines which are selective antagonists for human &agr; 1a receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the &agr; 1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

  本发明涉及选择性拮抗人类α1A受体的二氢嘧啶类化合物。本发明还涉及使用这些化合物来放松下尿道组织、治疗良性前列腺增生以及治疗任何需要拮抗α1A受体的疾病。本发明还提供了一种药物组合物，包括上述定义的化合物的治疗有效量和药用载体。
• Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof
  申请人：——

  公开号：US20030069261A1

  公开（公告）日：2003-04-10

  This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of modifying feeding behavior of a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. This invention further provides a method of treating a feeding disorder in a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. In an embodiment of the invention, the feeding disorder is bulimia, bulimia nervosa or obesity.

  本发明涉及一种选择性拮抗黑色素浓缩激素-1（MCH1）受体的化合物。该发明提供了一种药物组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明提供了一种通过组合本发明化合物的治疗有效量和药学上可接受的载体制备药物组合物的方法。本发明还提供了一种制备药物组合物的方法，包括将本发明化合物的治疗有效量和药学上可接受的载体组合。本发明还提供了一种改变受试者进食行为的方法，包括向受试者投药一种有效减少受试者进食的本发明化合物。本发明还提供了一种治疗受试者进食障碍的方法，包括向受试者投药一种有效减少受试者进食的本发明化合物。在本发明的实施例中，进食障碍是贪食症、神经性贪食症或肥胖症。
• DNA encoding a human melanin concentrating hormone receptor (MCH1) and uses thereof
  申请人：——

  公开号：US20030077701A1

  公开（公告）日：2003-04-24

  This invention provides an isolated nucleic acid encoding a human MCH1 receptor, a purified human MCH1 receptor, vectors comprising isolated nucleic acid encoding a human MCH1 receptor, cells comprising such vectors, antibodies directed to a human MCH1 receptor, nucleic acid probes useful for detecting nucleic acid encoding human MCH1 receptors, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding human MCH1 receptors, transgenic, nonhuman animals which express DNA encoding a normal or mutant human MCH1 receptor, methods of isolating a human MCH1 receptor, methods of treating an abnormality that is linked to the activity of a human MCH1 receptor, as well as methods of determining binding of compounds to mammalian MCH1 receptors. This invention provides a method of modifying the feeding behavior of a subject which comprises administering to the subject an amount of an MCH1 antagonist effective to decrease the body mass of the subject and/or decrease the consumption of food by the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of an MCH1 antagonist effective to treat the subject's depression and/or anxiety.

  本发明提供了编码人MCH1受体的分离核酸、纯化的人MCH1受体、包含编码人MCH1受体的分离核酸的载体、包含这种载体的细胞、针对人MCH1受体的抗体、用于检测编码人MCH1受体的核酸探针、互补于编码人MCH1受体独特序列的反义寡核苷酸、表达正常或突变人MCH1受体DNA的转基因非人类动物、分离人MCH1受体的方法、治疗与人MCH1受体活性相关的异常的方法，以及确定化合物与哺乳动物MCH1受体结合的方法。本发明提供了一种修改受试者进食行为的方法，该方法包括向受试者施用足以减少受试者体重和/或减少受试者食物摄入量的MCH1拮抗剂。本发明还提供了一种治疗患有抑郁和/或焦虑的受试者的方法，该方法包括向受试者施用足以治疗受试者抑郁和/或焦虑的MCH1拮抗剂。
• Dihydropyridinones and pyrrolinones useful as alpha 1A adrenoceptor antagonists
  申请人：Merck & Co., Inc.

  公开号：US06235759B1

  公开（公告）日：2001-05-22

  Novel dihydropyridinone and pyrrolinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

  本发明涉及新型二氢吡啶酮和吡咯酮化合物及其药学上可接受的盐。还描述了这些化合物的合成以及它们作为α1a肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是用于治疗良性前列腺增生症。这些化合物具有选择性，在不引起低血压的同时，能够松弛富含α1a受体亚型的平滑肌组织。这样的组织包括围绕尿道内膜的组织。因此，这些化合物的一个应用是通过允许更少受阻的尿液流动，为患有良性前列腺增生症的男性提供急性缓解。这些化合物的另一个应用是与人类5α-还原酶抑制剂化合物结合，以实现良性前列腺增生症的急性和慢性缓解。
• 5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US06268369B1

  公开（公告）日：2001-07-31

  This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

  本发明涉及以下式的二氢嘧啶化合物，这些化合物是人类α1C受体的选择性拮抗剂。本发明还涉及使用这些化合物降低眼压、抑制胆固醇合成、放松下尿路组织、治疗良性前列腺增生、阳痿、心律失常以及治疗任何需要α1C受体拮抗剂的疾病。本发明还提供一种制药组合物，包括上述定义的化合物的治疗有效量和药学上可接受的载体。