2-Ethyl[1,3]thiazolo[4,5-c]pyridine | 98382-94-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-Ethyl[1,3]thiazolo[4,5-c]pyridine
• 英文别名: 2-ethyl-[1,3]thiazolo[4,5-c]pyridine
• CAS: 98382-94-6
• 化学式: C₈H₈N₂S
• 分子量: 164.231
• InChiKey: HNRWMEWACVOUQE-UHFFFAOYSA-N

物化性质

• 沸点：
  280.2±13.0 °C(Predicted)
• 密度：
  1.241±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  54
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-Ethyl[1,3]thiazolo[4,5-c]pyridine 、 7β-<2-(2-aminothiazol-4yl)-2-(Z)-methoximinoacetamide>-3-iodomethyl-2-<(trimethylsilyloxy)carbonyl>cephalosporin 在 甲醇 作用下， 生成 (6R,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-[(2-ethyl-[1,3]thiazolo[4,5-c]pyridin-5-ium-5-yl)methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
  参考文献：
  名称：

  Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins

  摘要：

  The preparation and biological evaluation of a series of 7 beta-[2-(2-aminothiazol-4-yl)-2(Z)-methoximinoacetamido]cep halosporins, substituted at the 3'-position with monocyclic or bicyclic nitrogen-containing heterocycles are described. The resulting family of parenteral compounds displays a broad spectrum of antibacterial activity. Some compounds exhibit a similar level of Gram-negative activity to that of the "third-generation" cephalosporins with increased staphylococcal activity. The in vitro and in vivo antimicrobial activity, structure-activity relationships, beta-lactamase stability, and in vitro and in vivo pharmacological evaluations are presented.

  DOI：

  10.1021/jm00170a011

文献信息

• ANTI-EGFR ANTIBODY DRUG CONJUGATES
  申请人：AbbVie Inc.

  公开号：US20190153107A1

  公开（公告）日：2019-05-23

  The invention relates to anti-Epidermal Growth Factor Receptor (EGFR) antibody drug conjugates (ADCs) which inhibit Bcl-xL, including compositions and methods of using said ADCs.

  这项发明涉及抑制Bcl-xL的抗表皮生长因子受体（EGFR）抗体药物结合物（ADCs），包括使用所述ADCs的组合物和方法。
• Improvements on or relating to 3-bicyclicpyridinium-methyl cephalosporins
  申请人：ELI LILLY AND COMPANY

  公开号：EP0138552A2

  公开（公告）日：1985-04-24

  Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetyiamino group and of the formula in which R is hydrogen, formyl, a-aminoadipoyl, protected a-aminoadipoyl, or an acyl group of the formula in which R' is a 5- or 6-membered heterocyclic ring of the for mulae R" is hydrogen, C1-C4 alkyl, a carboxy-substituted alkyl or carboxy-substituted cycloalkyl group of the formula: in which n is 0-3; a and b when taken separately are, independently, hydrogen or C1-C3 alkyl, and when taken together with the carbon to which they are bonded form a C3-C7 carbocyclic ring; R"' is hydrogen, C1-C4 alkoxy, amino, or OR°, in which R° is indanyl, phthalidyl, or an acyloxymethyl group of the formula -CH2-O-C(O)-R2 in wich R2 is C1-C4 alkyl or phenyl; or COOR° is a protected carboxy group; or R" is an N-substituted carbamoyl group of the formula in which R"" is C1-C4 alkyl, phenyl or C1-C3 alkyl substituted by phenyl; Y and m, independently, are integers equal to 0,1,2 or 3, provided that y plus m equals 3; R1 is hydrogen, C1-C4 alkyl, phenyl, thienyl, amino or C1-C4 alkanoylamino; X is O, S or N-R2, where R2 is hydrogen or C1-C4 alkyl; or a pharmaceutically-acceptable salt or biologically-cleavable ester thereof.

  在 7 位被 2-(5-或 6-元杂环)-2-氧亚氨基乙酰氨基取代的头孢菌素化合物，其式为 其中 R 是氢、甲酰基、a-氨基己二酰、受保护的 a-氨基己二酰或式中的酰基 式中，R'是一个 5 或 6 元杂环，其式为 R "是氢、C1-C4 烷基、式中的羧基取代的烷基或羧基取代的环烷基： 其中 n 为 0-3；a 和 b 分别为氢或 C1-C3 烷基，与所键合的碳一起形成 C3-C7 碳环；R"'是氢、C1-C4 烷氧基、氨基或 OR°，其中 R°是茚基、酞基或式 -CH2-O-C(O)-R2 的酰氧基甲基，其中 R2 是 C1-C4 烷基或苯基；或 COOR°是受保护的羧基；或 R "是 N-取代的氨基甲酰基，其式为 其中 R"" 是 C1-C4 烷基、苯基或被苯基取代的 C1-C3 烷基； Y 和 m 分别是等于 0、1、2 或 3 的整数，条件是 y 加 m 等于 3； R1 是氢、C1-C4 烷基、苯基、噻吩基、氨基或 C1-C4 烷酰氨基； X 是 O、S 或 N-R2，其中 R2 是氢或 C1-C4 烷基；或其药学上可接受的盐或生物可裂解酯。
• Compounds for the modulation of Myc activity
  申请人：Syros Pharmaceuticals, Inc.

  公开号：US11124527B2

  公开（公告）日：2021-09-21

  The present invention provides novel compounds of Formulas (I) and (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angio genesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.

  本发明提供了式(I)和(II)的新型化合物及其药学上可接受的盐、溶液剂、水合物、同系物、立体异构体、同位素标记的衍生物及其组合物。还提供了涉及这些化合物或组合物的方法和试剂盒，用于治疗或预防受试者的增殖性疾病，如癌症（如乳腺癌、前列腺癌、淋巴瘤、肺癌、胰腺癌、卵巢癌、神经母细胞瘤或结肠直肠癌）、良性肿瘤、血管生成、炎症性疾病、纤维化（如多囊肾）、自身炎症性疾病和自身免疫性疾病。
• BICYCLIC HETEROARYL SUBSTITUTED COMPOUNDS
  申请人：BISTOL-MYERS SQUIBB COMPANY

  公开号：US20190292176A1

  公开（公告）日：2019-09-26

  Disclosed are compounds of Formula (I) to (VIII): (I) (II) (III) (IV) (V) (VI) (VII) (VIII); or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a bicyclic heteroaryl group substituted with zero to 3 R 3a ; and R 1 , R 2 , R 3a , R 4 , and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.
• ANTI-CD98 ANTIBODIES AND ANTIBODY DRUG CONJUGATES
  申请人：AbbVie Inc.

  公开号：US20200121803A1

  公开（公告）日：2020-04-23

  The invention relates to anti-CD98 antibodies and antibody drug conjugates (ADCs), including compositions and methods of using said antibodies and ADCs.