(R)-3-丙氧基吡咯烷 | 849924-75-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: (R)-3-丙氧基吡咯烷
• 英文名称: (R)-3-Propoxy-pyrrolidine
• 英文别名: (3R)-3-propoxypyrrolidine
• CAS: 849924-75-0
• 化学式: C₇H₁₅NO
• 分子量: 129.2
• InChiKey: JWNBCQQQLMTPLP-SSDOTTSWSA-N

物化性质

• 沸点：
  170.5±33.0 °C(Predicted)
• 密度：
  0.92±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  9
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] CYCLIC AMINE BASE-1 INHIBITORS HAVING A HETEROCYCLIC SUBSTITUENT<br/>[FR] INHIBITEURS D'AMINES CYCLIQUES BACE-1 RENFERMANT UN SUBSTITUANT HETEROCYCLIQUE
  申请人：SCHERING CORP

  公开号：WO2005014540A1

  公开（公告）日：2005-02-17

  Disclosed are novel compounds of the formula (I)or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is formula (I) X is -0-, -C(R14)2- or -N(R)-; Z is -C(R14)2- or -N(R)-; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, -CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, -OR35, -N(R24)(R25) or -SR35; R41 is alkyl, cycloalkyl, -S02(alkyl), -C(O)-alkyl, -C(O)-cycloalkyl or -alkyl-NH-C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula (I). Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.

  揭示了具有以下结构的新化合物（I）或其药学上可接受的盐或溶剂，其中R1为结构（I），X为-0-，-C(R14)2-或-N(R)-；Z为-C(R14)2-或-N(R)-；t为0、1、2或3；每个R和R2独立地为H、烷基、环烷基、环烷基烷基、芳基、杂环芳基、杂环烷基、芳基烷基、杂环芳基烷基、杂环烷基烷基、烯基或炔基；每个R14为H、烷基、烯基、炔基、卤素、-CN、卤代烷基、环烷基、环烷基烷基、芳基、杂环芳基、芳基烷基、杂环芳基烷基、杂环烷基烷基、-OR35、-N(R24)(R25)或-SR35；R41为烷基、环烷基、-S02(烷基)、-C(O)-烷基、-C(O)-环烷基或-烷基-NH-C(O)CH3；其余变量如规范中所定义。还揭示了包括化合物的药物组合物（I）的制剂以及使用化合物（I）治疗认知或神经退行性疾病的方法。还揭示了包括化合物（I）的药物组合物和治疗方法，其与治疗认知或神经退行性疾病有用的其他药剂结合使用。
• [EN] INHIBITORS OF FACTOR XA AND OTHER SERINE PROTEASES INVOLVED IN THE COAGULATION CASCADE<br/>[FR] INHIBITEURS DU FACTEUR XA ET AUTRES SERINE PROTEASES INTERVENANT DANS LA CASCADE DE LA COAGULATION
  申请人：WARNER LAMBERT CO

  公开号：WO2003045912A1

  公开（公告）日：2003-06-05

  The present invention provides compounds of Formula (I), wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula (I), processes for preparing compounds of Formula (I), and intermediates useful for preparing compounds of Formula (I).

  本发明提供了公式（I）的化合物，其中A、B、C、G和W1具有规范中定义的任何值，以及其药学上可接受的盐，用于治疗血栓性疾病。还公开了包含一个或多个公式（I）化合物的制药组合物，制备公式（I）化合物的方法以及用于制备公式（I）化合物的中间体。
• CYCLIC AMINE BACE-1 INHIBITORS HAVING A HETEROCYCLIC SUBSTITUENT
  申请人：Cumming Jared N.

  公开号：US20090312341A1

  公开（公告）日：2009-12-17

  Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is X is —O—, —C(R 14 ) 2 — or —N(R)—; Z is —C(R 14 ) 2 — or —N(R)—; t is 0, 1, 2 or 3; each R and R 2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R 14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR 35 , —N(R 24 ) (R 25 ) or —SR 35 ; R 41 is alkyl, cycloalkyl, —SO 2 (alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH 3 ; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I. Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.

  本发明涉及公式I的新化合物或其药学上可接受的盐或溶剂，其中R1为X为—O—，—C（R14）2—或—N（R）—；Z为—C（R14）2—或—N（R）—；t为0、1、2或3；每个R和R2独立地为H，烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，烯基或炔基；每个R14为H，烷基，烯基，炔基，卤素，—CN，卤代烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，—OR35，—N（R24）（R25）或—SR35；R41为烷基，环烷基，—SO2（烷基），—C（O）-烷基，—C（O）-环烷基或-烷基-NH-C（O）CH3；其余变量如规范中所定义。本发明还涉及包含公式I化合物的制药组合物以及使用公式I化合物治疗认知或神经退行性疾病的方法。本发明还涉及包含公式I化合物的制药组合物和治疗方法，其中该组合物与其他对治疗认知或神经退行性疾病有用的药物一起使用。
• VLA-4 INHIBITORY DRUG
  申请人：MACHINAGA Nobuo

  公开号：US20120157437A1

  公开（公告）日：2012-06-21

  This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH 2 ; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A 1 represents a nitrogen atom or C—R 3d wherein R 3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R 1 represents H or a C1-8 alkyl group; R 2 represents H, a halogen, a C1-8 alkoxy group, or an optionally-substituted benzyloxy group; and R 3a , R 3b and R 3c independently represent H, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group.

  本发明涉及一种VLA-4抑制药物，具有良好的口服吸收性，并在口服给药时表现出足够的抗炎作用，其中活性成分由公式（I）或其盐表示：Q代表一个含氮杂环基团，可以是单环或双环，该基团上的氮原子可选地被取代；Y代表氧原子或CH2；W代表一个可选取代的双环芳香族碳氢环基团或可选取代的双环芳香族杂环基团；A1代表一个氮原子或C-R3d，其中R3d代表氢原子、卤素原子、C1-8烷氧基或C1-8烷基；R1代表氢原子或C1-8烷基；R2代表氢原子、卤素原子、C1-8烷氧基或可选取代的苄氧基；以及R3a、R3b和R3c分别独立地代表氢原子、卤素原子、C1-8烷氧基或C1-8烷基。
• BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
  申请人：Christensen, IV Siegfried Benjamin

  公开号：US20120077794A1

  公开（公告）日：2012-03-29

  The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.

  本发明提供了一种新型的双吡啶基吡啶酮，其为黑色素浓集激素受体1（MCHR1）的拮抗剂，包含它们的制药组合物、制备它们的过程，并用于治疗肥胖症和糖尿病的治疗。