4-piperidone monochloride monohydrate

• 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: 4-piperidone monochloride monohydrate
• 英文别名: 1-Chloropiperidin-4-one;hydrate
• 化学式: C₅H₈ClNO*H₂O
• 分子量: 151.593
• InChiKey: XLCIMRTWHZGVMM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.02
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-piperidone monochloride monohydrate 在 palladium-carbon catalyst ammonium chloride 、 三乙胺 作用下， 以 四氢呋喃 、 甲醇 、 氯仿 、 水 为溶剂， 生成 N-Boc-4-哌啶乙醇
  参考文献：
  名称：

  N-acyl cyclic amine derivatives

  摘要：

  该发明涉及由通式[I]表示的化合物 ##STR1## [其中Ar表示芳基或杂环基，可能具有从卤原子、较低烷基基团和较低烷氧基团中选择的取代基; R.sup.1表示可用氟原子取代的C.sub.3-C.sub.6环烷基基团; R.sup.2和R.sup.4表示氢原子，表示为--(A.sup.1).sub.m--NH--B或类似基团; R.sup.3和R.sup.5表示氢原子，可用较低烷基基团取代的C.sub.1-C.sub.6脂肪烃基团或类似基团; n表示0或1; X表示氧原子或硫原子]。根据该发明的化合物，由于它们不仅具有对M.sub.3胆碱能受体具有强效选择性拮抗活性，而且表现出优异的口服活性、持久作用和药代动力学特性，因此在对抗呼吸、泌尿和消化系统疾病时非常有用，且副作用很小，是安全有效的药物。

  公开号：

  US06140333A1

文献信息

• [EN] METHOD OF MAKING IMIDAZOAZEPINONE COMPOUNDS<br/>[FR] PROCÉDÉ DE FABRICATION DE COMPOSÉS IMIDAZOAZÉPINONES
  申请人：EISAI E & D MAN CO LTD

  公开号：WO2009070305A1

  公开（公告）日：2009-06-04

  A method of making a compound of Formula I: is carried out by (a) providing a compound of Formula (II) or (III): wherein ring A is C3-14 aryl or C3-14 heteroaryl such as phenyl or furanyl, and then (b) combining the compound of Formula (II) or (III) with an acid to produce a compound of Formula I.

  通过以下步骤制备化合物I的方法：(a)提供化合物II或III：其中环A为C3-14芳基或C3-14杂芳基，如苯基或呋喃基；然后(b)将化合物II或III与酸结合以产生化合物I。
• LIQUID CRYSTALLINE COMPOUND HAVING PIPERIDINE RING, LIQUID CRYSTAL COMPOSITION AND LIQUID CRYSTAL DISPLAY ELEMENT
  申请人：CHISSO CORPORATION

  公开号：EP1072593A1

  公开（公告）日：2001-01-31

  The present invention relates to a novel liquid crystalline compound represented by Formula (1): wherein R represents an alkyl group having 1 to 10 carbon atoms or a fluoroalkyl group having 1 to 10 carbon atoms, and R' represents an alkyl group having 1 to 10 carbon atoms, a fluoroalkyl group having 1 to 10 carbon atoms, a fluorine atom, a chlorine atom, a bromine atom or a cyano group, in which any methylene groups which are not adjacent to each other in these alkyl groups and any methylene groups and/or fluoromethylene groups which are not adjacent to each other in the fluoroalkyl groups may be substituted with oxygen atoms, sulfur atoms or -CH=CH-; the rings A1, A2, A3 and A4 each independently represent 1,4-cyclohexylene, 1,4-phenylene in which 1 to 2 hydrogen atoms may be substituted with fluorine atoms, dioxane-2,5-diyl, pyrimidine-2,5-diyl, pyridine-2,5-diyl, piperidine-1,4-diyl or 1-sila-1,4-cyclohexylene; B1, B2, B3, B4 and B5 each independently represent a single bond, -CH2CH2-, -CH=CH-, -OCH2-, -CH2O-, -(CH2)4-, -OCO- or -COO-; l, m, n and p each independently represent 0 or 1; and Z represents one group selected from the following moieties (I) to (V): provided that when Z is the moiety (II), l + m + n + p > 0, and the rings A1, A2, A3 and A4 each independently represent 1,4-phenylene in which 1 to 2 hydrogen atoms are substituted with fluorine atoms, pyrimidine-2,5-diyl, pyridine-2,5-diyl, piperidine-1,4-diyl or 1-sila-1,4-cyclohexylene; and that when Z is the moiety (III) and l = m = n = p = 0, R is an alkyl group, and R' is not a fluorine atom or a cyano group when B5 is a single bond. The present invention further relates to a liquid crystal composition comprising the above compound and a liquid crystal display element comprising the above composition. The liquid crystalline compound of the present invention has a particularly large dielectric anisotropy and refractive anisotropy and a low viscosity and is excellent in a low temperature compatibility.

  本发明涉及一种新颖的液晶化合物，其表示为式（1）所示：其中R代表具有1至10个碳原子的烷基基团或具有1至10个碳原子的氟烷基基团，R'代表具有1至10个碳原子的烷基基团、具有1至10个碳原子的氟烷基基团、氟原子、氯原子、溴原子或氰基，在这些烷基基团中不相邻的任何亚甲基基团和不相邻的亚甲基和/或氟亚甲基基团可以用氧原子、硫原子或-CH=CH-取代；环A1、A2、A3和A4分别独立地表示1,4-环己亚甲基、1,4-苯基，其中1至2个氢原子可以用氟原子取代，二氧杂环戊二亚基、嘧啶-2,5-二亚基、吡啶-2,5-二亚基、哌啶-1,4-二亚基或1-硅-1,4-环己亚甲基；B1、B2、B3、B4和B5分别独立地表示单键、-CH2CH2-、-CH=CH-、-OCH2-、-CH2O-、-(CH2)4-、-OCO-或-COO-；l、m、n和p各自独立地表示0或1；Z表示从以下基团（I）到（V）中选择的一个基团：但是当Z为基团（II）时，l + m + n + p > 0，环A1、A2、A3和A4分别独立地表示1,4-苯基，其中1至2个氢原子被氟原子取代，嘧啶-2,5-二亚基、吡啶-2,5-二亚基、哌啶-1,4-二亚基或1-硅-1,4-环己亚甲基；当Z为基团（III）且l = m = n = p = 0时，R为烷基基团，当B5为单键时，R'不是氟原子或氰基。本发明还涉及包括上述化合物的液晶组合物和包括上述组合物的液晶显示元件。本发明的液晶化合物具有特别大的介电各向异性和折射各向异性，低粘度，并且在低温兼容性方面表现出色。
• [EN] AMINOPYRIMIDINES AS SORBITOL DEHYDROGENASE INHIBITORS<br/>[FR] AMINOPYRIMIDINES COMME INHIBITEURS DE SORBITOL DESHYDROGENASE
  申请人：PFIZER PROD INC

  公开号：WO2000059510A1

  公开（公告）日：2000-10-12

  This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula (I), wherein R?1, R2 and R3¿ are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefor at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula (I) of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula (I) of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula (I) and to processes for preparing those intermediates.

  本发明涉及式（I）的山梨醇脱氢酶抑制剂，其中R1、R2和R3在说明书中定义。本发明还涉及含有这些化合物的药物组合物，以及通过将这些化合物用于患有糖尿病并因此有患上这些并发症风险的哺乳动物进行治疗或预防糖尿病并发症，特别是糖尿病神经病变、糖尿病肾病、糖尿病微血管病、糖尿病大血管病和糖尿病心肌病的方法。本发明还涉及一种包含本发明式（I）化合物和醛还原酶抑制剂的药物组合物以及用于治疗或预防糖尿病并发症的方法。本发明还涉及一种包含本发明式（I）化合物和NHE-1抑制剂的药物组合物以及用于治疗心肌病和其他心脏相关问题的方法。本发明还涉及用于合成式（I）化合物的某些中间体以及制备这些中间体的方法。
• Sorbitol dehydrogenase inhibitors
  申请人：——

  公开号：US20040077671A1

  公开（公告）日：2004-04-22

  This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, 1 wherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula I and to processes for preparing those intermediates.

  本发明涉及公式I的山梨醇脱氢酶抑制剂，其中R1、R2和R3如规范中所定义。本发明还涉及含有这些化合物的制药组合物以及通过向患有糖尿病且因此有发展这些并发症风险的哺乳动物投与这些化合物来治疗或预防糖尿病并发症，特别是糖尿病神经病、糖尿病肾病、糖尿病微血管病、糖尿病大血管病和糖尿病心肌病的方法。本发明还涉及一种公式I化合物与醛糖还原酶抑制剂的组合物制药组合物以及用于治疗或预防糖尿病并发症的方法。本发明还涉及一种公式I化合物与NHE-1抑制剂的组合物制药组合物以及用于治疗心肌病和其他心脏相关问题的方法。本发明还涉及用于合成公式I化合物的某些中间体以及制备这些中间体的方法。
• Salts of zopolrestat
  申请人：——

  公开号：US20010056095A1

  公开（公告）日：2001-12-27

  This invention relates to [4-oxo-(5-trifluoromethyl-benzothiazol-2-ylmethyl)-3,4-dihydro-phthalazin-1-yl]-acetic acid ethanolamine salt, pharmaceutical compositions thereof and methods of treating diabetic complications in mammals comprising administering to said mammals said salt and said compositions. This invention is also directed to combinations of said diethylamine salt with NHE-1 inhibitors, selective serotonin retuptake inhibitors (SSRIs), glycogen phosphorylase inhibitors (GPIs), sorbitol dehydrogenase inhibitors (SDIs) and antihypertensive agents. Said combinations are useful in treating diabetic complications in mammals.

  本发明涉及[4-氧代-(5-三氟甲基苯并噻唑-2-基甲基)-3,4-二氢-邻苯二氮平-1-基]-乙酸乙醇胺盐，以及其制药组合物和治疗哺乳动物糖尿病并发症的方法，包括向该哺乳动物施用该盐和该组合物。本发明还涉及将该二乙酰胺盐与NHE-1抑制剂、选择性5-羟色胺再摄取抑制剂（SSRIs）、糖原磷酸化酶抑制剂（GPIs）、山梨醇脱氢酶抑制剂（SDIs）和降压药物组合的方法。该组合物在治疗哺乳动物糖尿病并发症方面具有用途。