N-(N-formyl-N-methyl)aminopiperidine | 86755-90-0

• 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: N-(N-formyl-N-methyl)aminopiperidine
• 英文别名: N-methyl-N-piperidin-1-ylformamide
• CAS: 86755-90-0
• 化学式: C₇H₁₄N₂O
• 分子量: 142.201
• InChiKey: IPOVGCYDEWFVQU-UHFFFAOYSA-N

物化性质

• 沸点：
  203.9±23.0 °C(Predicted)
• 密度：
  1.04±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  23.6
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(N-formyl-N-methyl)aminopiperidine 、 lithium phenylacetylide 以 四氢呋喃 为溶剂， 以92%的产率得到苯丙炔醛
  参考文献：
  名称：

  The role of chelation in the formylation of grignard reagents with N-formyl amines.

  摘要：

  DOI：

  10.1016/s0040-4039(00)86387-x

文献信息

• [EN] FUSED THIAZOLE AND THIOPHENE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] DÉRIVÉS THIAZOLE ET THIOPHÈNE FUSIONNÉS COMME INHIBITEURS DE KINASE
  申请人：UCB PHARMA SA

  公开号：WO2009071895A1

  公开（公告）日：2009-06-11

  A series of fused bicyclic thiazole and thiophene derivatives which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, and in the 4-position by hydroxy, oxo or an amine moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. (I)

  一系列在2位被一个可选择取代的吗啡啉-4-基团取代，并在4位被羟基、酮基或胺基团取代的融合双环噻唑和噻吩衍生物，作为选择性PI3激酶酶抑制剂，在医学上具有益处，例如在治疗炎症、自身免疫、心血管、神经退行性、代谢、肿瘤、疼痛或眼科疾病方面。（I）
• [EN] TRICYCLIC KINASE INHIBITORS<br/>[FR] INHIBITEURS TRICYCLIQUES DE KINASE
  申请人：UCB PHARMA SA

  公开号：WO2009071890A1

  公开（公告）日：2009-06-11

  A series of fused tricyclic thiazole and thiophene derivatives which are substituted in the 2-position of the thiazole or thiophene ring by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

  一系列融合的三环噻唑和噻吩衍生物，其在噻唑或噻吩环的2位被一个可选择取代的吗啡啉-4-基团取代，是选择性PI3激酶酶抑制剂，在医学上具有益处，例如在治疗炎症性、自身免疫性、心血管、神经退行性、代谢性、肿瘤学、疼痛性或眼科疾病方面。
• [EN] AMINOPYRIMIDINE DERIVATIVES AS JNK INHIBITORS<br/>[FR] DERIVES D'AMINOPYRIMIDINE EN TANT QU'INHIBITEURS DE LA JNK
  申请人：CELLTECH R&D LTD

  公开号：WO2006038001A1

  公开（公告）日：2006-04-13

  A compound of formula (I) or a pharmaceutically acceptable salt, solvate or N-­oxide thereof: wherein A represents a pyrrole, pyrazole, imidazole or triazole ring; B represents a benzene, pyridine or pyrimidine ring; M represents the residue of an azetidine, pyrrolidine or piperidine ring; E represents a covalent bond or an optionally substituted straight or branched alkylene chain containing from 1 to 4 carbon atoms; Z represents hydrogen, -CORa, -C02Rb, -CONKc Rd, -CONRcORb, -COCO2Rb, - COCONRcRd, -COCH2NRcRd, -COCH2NRcCONKcRd, COCH2NRcCO2Rb, -NRcCORa, - NRcCO2Rb, -NRcCONRcRd, -S02Re, -SO2NRcRd or -SO2NRcC02Rb; or Z represents an optionally substituted phenyl, heteroaryl or C3-7 heterocycloalkyl group; R1 and R2 independently represent hydrogen, halogen, cyano, nitro, C1-6 alkyl, trifluoromethyl, hydroxy, C1-6 alkoxy, difluoromethoxy, trifluoromethoxy, C1-6 alkylsulphonyl, amino, C1-6 alkylamino, di(C1-6)alkylamino, aminocarbonyl or C2-6 alkoxycarbonyl; R3 represents hydrogen, C1-6 alkyl, -CH2CONRcRd or -SO2Re; R4 represents hydrogen, C1-6 alkoxy, oxo, -CO2Rb or -CONKcRd. The compounds of the present invention are potent inhibitors of JNK.

  式（I）的化合物或其药学上可接受的盐、溶剂或N-氧化物：其中A代表吡咯、吡唑、咪唑或三唑环；B代表苯、吡啶或嘧啶环；M代表氮杂环丙烷、吡咯丙烷或哌啶环的残基；E代表共价键或含有1至4个碳原子的可选取代的直链或支链烷基链；Z代表氢、-CORa、-C02Rb、-CONKcRd、-CONRcORb、-COCO2Rb、-COCONRcRd、-COCH2NRcRd、-COCH2NRcCONKcRd、COCH2NRcCO2Rb、-NRcCORa、-NRcCO2Rb、-NRcCONRcRd、-S02Re、-SO2NRcRd或-SO2NRcC02Rb；或Z代表可选取代的苯基、杂环芳基或C3-7杂环烷基基团；R1和R2独立地代表氢、卤素、氰基、硝基、C1-6烷基、三氟甲基、羟基、C1-6烷氧基、二氟甲氧基、三氟甲氧基、C1-6烷基磺酰基、氨基、C1-6烷基氨基、二(C1-6)烷基氨基、氨基甲酰基或C2-6烷氧羰基；R3代表氢、C1-6烷基、-CH2CONRcRd或-SO2Re；R4代表氢、C1-6烷氧基、氧代、-CO2Rb或-CONKcRd。本发明的化合物是JNK的有效抑制剂。
• [EN] PYRROLOTHIAZOLES AS PI3-KINASE INHIBITORS<br/>[FR] PYRROLOTHIAZOLES COMME INHIBITEURS DE LA PI3 KINASE
  申请人：UCB PHARMA SA

  公开号：WO2009071888A1

  公开（公告）日：2009-06-11

  A series of 4,5-dihydro-6H-pyrrolo[3,4-d][1,3]thiazol-6-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

  一系列在2-位置被一个可选择取代的吗啡啶-4-基团取代的4,5-二氢-6H-吡咯并[3,4-d][1,3]噻唑-6-酮衍生物及其类似物，是选择性PI3激酶酶抑制剂，在医学上具有益处，例如在治疗炎症、自身免疫、心血管、神经退行性、代谢、肿瘤、疼痛或眼科疾病方面。
• New (hetero)aryl compounds with MCH antagonistic activity and medicaments comprising these compounds
  申请人：Roth Juergen Gerald

  公开号：US20070111981A1

  公开（公告）日：2007-05-17

  The present invention relates to (hetero)aryl compounds of general formula I wherein the groups and radicals A, B, Q, W, X, Y, Z, R 1 , R 2 , R 4a , R 4b , R 5a , R 5b , have the meanings given in claim 1 . Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

  本发明涉及一般式I的（杂）芳基化合物，其中A、B、Q、W、X、Y、Z、R1、R2、R4a、R4b、R5a和R5b基团和基团具有权利要求1中给出的含义。此外，本发明涉及至少含有本发明中的一种化合物的制药组合物。由于其MCH受体拮抗活性，根据本发明的制药组合物适用于治疗代谢紊乱和/或进食障碍，尤其是肥胖症、贪食症、厌食症、暴食症和糖尿病。