Pentona | 42024-98-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: Pentona
• 英文别名: [(1R,3R,5R)-6,6,9-trimethyl-9-azabicyclo[3.3.1]nonan-3-yl] 2-hydroxy-2,2-dithiophen-2-ylacetate
• CAS: 42024-98-6
• 化学式: C₂₁H₂₇NO₃S₂
• 分子量: 405.6
• InChiKey: AMHPTVWBZSYFSS-BZUAXINKSA-N

物化性质

• 沸点：
  528.7±50.0 °C(Predicted)
• 密度：
  1.28±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  106
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• [EN] SUBSTITUTED HETEROCYCLIC COMPOUNDS AS ALLOSTERIC MODULATORS OF GROUP II METABOTROPIC GLUTAMATE RECEPTORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES SUBSTITUÉS UTILISÉS COMME MODULATEURS ALLOSTÉRIQUES DE RÉCEPTEURS MÉTABOTROPIQUES DU GLUTAMATE DU GROUPE II
  申请人：MAVALON THERAPEUTICS LTD

  公开号：WO2018206820A1

  公开（公告）日：2018-11-15

  The present invention provides novel heterocyclic compounds of the general formula (I), including novel compounds of formula (la), and pharmaceutical compositions containing them. Moreover, the compounds of formula (I) or (la) and the pharmaceutical compositions containing them are provided for use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. The compounds of formula (I) or (la) can act as modulators of nervous system receptors sensitive to glutamate, in particular as modulators of metabotropic glutamate receptors (mGluRs), which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. The present invention further provides compounds of formula (I) or (la) that are modulators of metabotropic glutamate receptors (mGluRs), particularly positive allosteric modulators of mG!uRs, and more specifically positive allosteric modulators of mGluR3.

  本发明提供了一般式(I)的新颖杂环化合物，包括一般式(la)的新化合物，以及含有它们的药物组合物。此外，提供了一般式(I)或(la)的化合物和含有它们的药物组合物，用于治疗和/或预防与改变谷氨酸能信号和/或功能相关的疾病，以及那些可能受到哺乳动物谷氨酸水平或信号改变影响的疾病。一般式(I)或(la)的化合物可以作为对谷氨酸敏感的神经系统受体的调节剂，特别是代谢型谷氨酸受体(mGluRs)的调节剂，这使它们特别适用于治疗和/或预防急性和慢性神经和/或精神障碍。本发明还提供了一般式(I)或(la)的化合物，它们是代谢型谷氨酸受体(mGluRs)的调节剂，特别是mGluRs的正向变构调节剂，更具体地说是mGluR3的正向变构调节剂。
• [EN] RUBIDIUM AND/OR ZINC COMPOUNDS FOR TREATING PARKINSON'S AND OTHER NEURODEGENERATIVE DISEASES<br/>[FR] COMPOSÉS DE RUBIDIUM ET/OU DE ZINC POUR LE TRAITEMENT DE LA MALADIE DE PARKINSON ET D'AUTRES MALADIES NEURODÉGÉNÉRATIVES
  申请人：VECTOR VITALE IP LLC

  公开号：WO2021071499A1

  公开（公告）日：2021-04-15

  Compositions that comprise salts, compounds and complexes of 64Zn-enriched zinc, such as 64Zn-enriched zinc aspartate, and further optionally include 85Rb-enriched rubidium salt compounds of general formula (1), below, wherein each of R1 through R14 is independently selected from H, OH, F, C1, Br, I, C1-C6 alkyl, C1-C6 alkoxy, and NO2, such as the compound of Formula 1 in which R3 is CH3 and all other R groups are H for use to treat a neurodegenerative disease (NDD), such as Parkinson's disease (PD). Methods that entail administering such compositions to treat an NDD, such as PD, optionally in combination with any other treatment for an NDD such as for PD.

  含有盐、化合物和富集64Zn的锌的化合物，例如富集64Zn的天冬酸锌，以及进一步可能包括通式（1）所示的富集85Rb的铷盐化合物，其中R1至R14中的每个均独立选择自H、OH、F、C1、Br、I、C1-C6烷基、C1-C6烷氧基和NO2，例如通式1中R3为CH3且所有其他R基为H的化合物，用于治疗神经退行性疾病（NDD），如帕金森病（PD）。方法包括向患有NDD的患者施用这种组合物以治疗NDD，如PD，可以选择与其他用于治疗NDD（如PD）的任何其他治疗方法结合使用。
• NOVEL COMPOUND AND MEDICAL USE THEREOF
  申请人：Kokubo Masaya

  公开号：US20130245074A1

  公开（公告）日：2013-09-19

  Provided is a levodopa prodrug that overcomes the problems attributed to the blood kinetics of levodopa such as large number of doses and the incidence of side effects due to frequent dosing. (2S)-2-Amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid, a salt thereof, or a solvate thereof is a levodopa prodrug, and provides a flat blood concentration-time profile of levodopa through oral administration, and therefore is useful as a preventive and/or therapeutic agent for Parkinson's disease and/or Parkinson's syndrome that overcomes the problems associated with pharmaceutical preparations of levodopa.

  提供了一种左多巴前药，它克服了左多巴的血液动力学问题，例如需要大量剂量和频繁给药导致的副作用。其化学名为(2S)-2-氨基-3-(3,4-双((2-(苯甲酰氧基)-2-甲基丙酰氧)苯基)丙酸，其盐或溶剂化合物是左多巴前药，通过口服给药提供了左多巴平稳的血药浓度时间曲线，因此可用作克服左多巴药物制剂相关问题的帕金森病和/或帕金森综合征的预防和/或治疗药物。
• Bicyclic compound
  申请人：Miyoshi Shiro

  公开号：US20060069098A1

  公开（公告）日：2006-03-30

  A novel compound represented by the following formula (1) or a salt thereof: wherein symbol “A” represents a saturated heterocyclic group, a 5-membered heteroaromatic group having two heteroatoms in the ring, a group represented by the formula A1 (R 2 , R 3 , and R 4 represent hydrogen atom, hydroxyl group, etc.), etc., B represents a group represented by the formula B1 (R 11 represents hydrogen atom, hydroxyl group, etc.), etc., R 1 represents an alkyl group, and symbol “n” represents an integer of 2 to 6, which has a parathyroid hormone depressing action and showing low toxicity, and a medicament containing the compound or salt thereof as an active ingredient.

  以下公式（1）所代表的一种新化合物或其盐：其中符号“A”代表饱和杂环基，一个含有两个杂原子的5元杂芳基，一个由公式A1（R2、R3和R4代表氢原子、羟基等）所代表的基团，等等，B代表由公式B1（R11代表氢原子、羟基等）所代表的基团，等等，R1代表烷基，符号“n”代表一个整数，范围为2至6，具有降钙素抑制作用和低毒性，并且含有该化合物或其盐作为活性成分的药物。
• [EN] COMBINATION THERAPY USING ENANTIOPURE, OXY-SUBSTITUTED, DEUTERIUM-ENRICHED 5-(BENZYL)-5-DEUTERO-THIAZOLIDINE-2, 4-DIONES FOR TREATMENT OF MEDICAL DISORDERS<br/>[FR] POLYTHÉRAPIE UTILISANT DES 5-(BENZYL)-5-DEUTÉRO-THIAZOLIDINE-2,4-DIONES OXY-SUBSTITUÉES ÉNANTIOPURES, ENRICHIES EN DEUTÉRIUM POUR LE TRAITEMENT DE TROUBLES MÉDICAUX
  申请人：DEUTERX LLC

  公开号：WO2016153948A1

  公开（公告）日：2016-09-29

  The invention provides combination therapy using enantiopure deuterium-enriched pioglitazone, pharmaceutical compositions, and methods of treating nonalcoholic steatohepatitis, diabetes, fibrotic disorders, and other disorders using the combination therapy.

  这项发明提供了使用对映纯的富氘吡格列酮的联合疗法，以及使用该联合疗法治疗非酒精性脂肪性肝炎、糖尿病、纤维化疾病和其他疾病的药物组合和治疗方法。