1-methyl-DL-proline-methylamide | 99767-11-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 1-methyl-DL-proline-methylamide
• 英文别名: 1-Methyl-DL-prolin-methylamid；N,1-dimethylpyrrolidine-2-carboxamide
• CAS: 99767-11-0
• 化学式: C₇H₁₄N₂O
• mdl: MFCD01605580
• 分子量: 142.201
• InChiKey: XLFKIFVDLHBTIA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.857
• 拓扑面积：
  32.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-methyl-DL-proline-methylamide 在 盐酸 作用下， 生成 1-甲基吡咯烷-2-甲酸
  参考文献：
  名称：

  Pyrrolidinium Analogs of Choline and Betaine. Onium Compounds. XXI

  摘要：

  DOI：

  10.1021/ja01874a052
• 作为产物：
  描述：

  N-甲基1-甲基吡咯-2-羧酰胺 在 盐酸 、 乙醇 、 铂 作用下， 生成 1-methyl-DL-proline-methylamide
  参考文献：
  名称：

  Pyrrolidinium Analogs of Choline and Betaine. Onium Compounds. XXI

  摘要：

  DOI：

  10.1021/ja01874a052

文献信息

• [EN] 2-CYANOISOINDOLINE DERIVATIVES FOR TREATING CANCER<br/>[FR] DÉRIVÉS DE 2-CYANOISOINDOLINE POUR LE TRAITEMENT DU CANCER
  申请人：MISSION THERAPEUTICS LTD

  公开号：WO2017158388A1

  公开（公告）日：2017-09-21

  The invention relates to novel compounds of formula I which are inhibitors of deubiquitylating enzymes (DUBs) and/or desumoylating enzymes. In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 7 or ubiquitin specific peptidase 7 (USP7). The invention further relates to methods for the preparation of these compounds and to their use in the treatment of cancer.

  这项发明涉及公式I的新化合物，这些化合物是去泛素化酶（DUBs）和/或去泛素化酶的抑制剂。具体来说，该发明涉及抑制泛素C端水解酶7或泛素特异性肽酶7（USP7）。该发明还涉及这些化合物的制备方法以及它们在癌症治疗中的应用。
• [EN] CYCLOBUTENEDIONE DERIVATIVES<br/>[FR] DÉRIVÉS DE CYCLOBUTÈNE-DIONE
  申请人：PFIZER LTD

  公开号：WO2010131145A1

  公开（公告）日：2010-11-18

  The present invention relates to compounds of the formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly inflammatory conditions.

  本发明涉及以下式(I)的化合物：以及其药学上可接受的盐和所述化合物及盐的药学上可接受的溶剂化物，其中取代基在此处定义；含有这种化合物的组合物；以及这种化合物在治疗各种疾病，特别是炎症性疾病中的用途。
• [EN] POLYCYCLIC TLR7/8 ANTAGONISTS AND USE THEREOF IN THE TREATMENT OF IMMUNE DISORDERS<br/>[FR] ANTAGONISTES DE TLR7/8 POLYCYLIQUES ET LEUR UTILISATION DANS LE TRAITEMENT DE MALADIES IMMUNES
  申请人：MERCK PATENT GMBH

  公开号：WO2017106607A1

  公开（公告）日：2017-06-22

  The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as toll-like receptor 7/8 (TLR7/8) antagonists. In Formula (I), Ring A is aryl or heteroaryl; Ring B is aryl or heteroary; and X is C(R4)2, O, NR4, S, S(R4), or S(R4)2.

  本发明涉及式(I)的化合物及其药学上可接受的组合物，作为Toll样受体7/8（TLR7/8）拮抗剂。在式(I)中，环A是芳基或杂芳基；环B是芳基或杂芳基；X是C(R4)2、O、NR4、S、S(R4)或S(R4)2。
• BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
  申请人：SURLERAUX Nestor Ghislain Dominique Louis

  公开号：US20070135447A1

  公开（公告）日：2007-06-14

  The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R 1 and R 8 each are H, optionally substituted C 1-6 alkyl, C 2-6 alkenyl, C 3-7 cycloalkyl, aryl, Het 1 , Het 2 ; R 1 may also be a radical of formula (R 11a R 11b )NC(R 10a R 10b )CR 9 —; t is 0, 1 or 2; R 2 is H or C 1-6 alkyl; L is —C(═O)—, —O—C(═O)—, —NR 8 —C(═O)—, —O—C 1-6 alkanediyl-C(═O)—, —NR 8 —C 1-6 alkanediyl-C(═O)—, —S(═O) 2 —, —O—S(═O) 2 —, —NR 8 —S(═O) 2 ; R 3 is C 1-6 alkyl, aryl, C 3-7 cycloalkyl, C 3-7 cycloalkylC 1-4 alkyl, or arylC 1-4 alkyl; R 4 is H, C 1-4 alkylOC(═O), carboxyl, aminoC(═O), mono- or di(C 1-4 alkyl)aminoC(═O), C 3-7 cycloalkyl, C 2-6 alkenyl, C 2-6 alkynyl or optionally substituted C 1-6 alkyl; A is C 1-6 alkanediyl, —C(═O)—, —C(═S)—, —S(═O) 2 —, C 1-6 alkanediyl-C(═O)—, C 1-6 alkanediyl-C(═S)— or C 1-6 alkanediyl-S(═O) 2 —; R 5 is H, OH, C 1-6 alkyl, Het 1 C 1-6 alkyl, Het 2 C 1-6 alkyl, optionally substituted aminoC 1-6 alkyl; R 6 is C 1-6 alkylO, Het 1 , Het 1 O, Het 2 , Het 2 O, aryl, arylO, C 1-6 alkyloxycarbonylamino or amino; and in case -A- is other than C 1-6 alkanediyl then R 6 may also be C 1-6 alkyl, Het 1 C 1-4 alkyl, Het 1 OC 1-4 alkyl, Het 2 C 1-4 alkyl, Het 2 OC 1-4 alkyl, arylC 1-4 alkyl, arylOC 1-4 alkyl or aminoC 1-4 alkyl; whereby each of the amino groups in the definition of R 6 may optionally be substituted; -A-R 6 is hydroxyC 1-6 alkyl; R 5 and -A-R 6 taken together with the nitrogen atom to which they are attached may also form Het 1 or Het 2 It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

  本发明涉及具有以下式N-氧化物，盐，立体异构体，外消旋混合物，前药，酯和其代谢物，其中R1和R8各自为H，可选择性取代的C1-6烷基，C2-6烯基，C3-7环烷基，芳基，Het1，Het2; R1也可以是式（R11aR11b）NC（R10aR10b）CR9—的基团; t为0，1或2; R2为H或C1-6烷基; L为—C（═O）—，—O—C（═O）—，—NR8—C（═O）—，—O—C1-6烷二基-C（═O）—，—NR8—C1-6烷二基-C（═O）—，—S（═O）2—，—O—S（═O）2—，—NR8—S（═O）2; R3为C1-6烷基，芳基，C3-7环烷基，C3-7环烷基C1-4烷基，或芳基C1-4烷基; R4为H，C1-4烷基OC（═O），羧基，氨基C（═O），单烷基或双烷基氨基C（═O），C3-7环烷基，C2-6烯基，C2-6炔基或可选择性取代的C1-6烷基; A为C1-6烷二基，—C（═O）—，—C（═S）—，—S（═O）2—，C1-6烷二基-C（═O）—，C1-6烷二基-C（═S）—或C1-6烷二基-S（═O）2—; R5为H，OH，C1-6烷基，Het1C1-6烷基，Het2C1-6烷基，可选择性取代的氨基C1-6烷基; R6为C1-6烷基氧，Het1，Het1氧，Het2，Het2氧，芳基，芳基氧，C1-6烷氧羰基氨基或氨基; 如果-A-不是C1-6烷二基，则R6也可以是C1-6烷基，Het1C1-4烷基，Het1OC1-4烷基，Het2C1-4烷基，Het2OC1-4烷基，芳基C1-4烷基，芳基OC1-4烷基或氨基C1-4烷基; 其中定义R6中的每个氨基可选择性取代; -A-R6为羟基C1-6烷基; R5和-A-R6与它们所连接的氮原子一起还可以形成Het1或Het2。它进一步涉及它们作为广谱HIV蛋白酶抑制剂的用途，它们的制备过程以及包含它们的制药组合物和诊断试剂盒。它还涉及与另一种抗逆转录病毒药物的组合以及它们作为参考化合物或试剂在测定中的用途。
• SUBSTITUTED PYRIDINE SPLEEN TYROSINE KINASE (SYK) INHIBITORS
  申请人：Merck Sharp & Dohme Corp.

  公开号：US20150148327A1

  公开（公告）日：2015-05-28

  The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R cy , C y , and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

  本发明提供了以下公式（I）的某些取代吡啶或其药学上可接受的盐，其中R1，R2，R3，R4，Rcy，Cy和t如本文所定义。 本发明还提供了包含这种化合物的制药组合物，并且提供了使用这些化合物治疗由脾酪氨酸激酶（Syk）激酶介导的疾病或病症的方法。