Unlock instant, AI-driven research and patent intelligence for your innovation.

Substituted tricyclic heterocyclic compounds and uses thereof

A technology for compounds and uses, applied in the field of tricyclic heterocyclic compounds, for the treatment of conditions caused by cancer and neurodegenerative diseases, capable of addressing problems such as hyperphosphorylation

Active Publication Date: 2021-10-29
SUZHOU YABAO PHARMA R&D CO LTD +1
View PDF7 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Overexpression of the PD pathogenic mutant protein LRRK2R1441G has been reported to lead to Parkinsonian symptoms and Tau hyperphosphorylation in a transgenic mouse model [42]

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Substituted tricyclic heterocyclic compounds and uses thereof
  • Substituted tricyclic heterocyclic compounds and uses thereof
  • Substituted tricyclic heterocyclic compounds and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0368]

[0369] step 1

[0370] Synthesis of 4-chloro-3-iodine-1H-pyrazole [4,3-C] pyridine (intermediate 1):

[0371]

[0372] At room temperature, iodine (19 g, 76 mmol) was added to 4-chloro-1H-pyrazole [4,3-C] pyridine (5.8 g, 38 mmol, synthesized according to WO 201010633 A1 and WO 2012038743 A1) and KOH (8g, 142 mmol) The mixture in 1,4-dioxane (100 mL). The reaction mixture was stirred at 75 ° C for 4 hours, then cooled to room temperature. Tissue solution Na 2 S 2 O 3 (Aqueous solution) diluted, filtered the resulting precipitate and dried to give a yellow solid (4.1 g). The filtrate was allowed to stand for 3 days, and the resulting precipitate was filtered to produce an additional 3.55 g of a product. The yield (7.65 g, 72%). 1 H NMR (400MHz, CDCL 3 ΔPPM7.65 (D, J = 6.0 Hz, 1H), 8.13 (D, J = 6.0 Hz, 1H), 14.22 (S, 1H) .M / Z (ESI) + : 280 [M + H] +

[0373] Step 2

[0374] Synthesis 1- (4-methoxybenzyl) -4-chloro-3-iodine-1H-pyrazole [4,3-C] pyridine (intermediate 2...

Embodiment 2-14

[0402] Example 2-14 is prepared from the first embodiment by using a suitable amine in step 3.

[0403]

[0404]

[0405]

Embodiment 15

[0407] In step 4, methyl methacrylate was used for methyl methacrylate, and Example 15 was prepared in Example 14.

[0408]

[0409]

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
Login to View More

Abstract

The substituted tricyclic heterocyclic compound of general formula I or its stereoisomer, tautomer, N-oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt, ester or Prodrugs, pharmaceutical compositions comprising the above structures and their uses. Substituted tricyclic heterocyclic compounds and pharmaceutical compositions comprising the compounds disclosed herein are useful for treating conditions caused by at least one of cancer and neurodegenerative diseases. In addition, such compounds and pharmaceutical compositions comprising the compounds disclosed herein are also useful in the prophylaxis or treatment of conditions arising from, associated with, or accompanying any abnormal kinase activity.

Description

[0001] Cross-reference related application [0002] The present application claims the priority and equity of the application number submitted to the National Intellectual Property Office on June 15, 2016, and the entire contents are incorporated herein by reference. Technical field [0003] The present invention is belonging to the field of pharmaceutical technology, and more particularly to compounds, including the use thereof and the use of the condition caused by cancer and neurodegenerative diseases. In particular, this paper provides a three-ring heterocyclic compound capable of suppressing a kinase, in particular LRRK, more particularly substituted with LRRK2. Background technique [0004] Parkinson Disease (PD) is the second common neurodegenerative disease, affecting 1-2% of the elderly people [1]. All genome association analysis (GWAS) has 28 associated genetic risk variations in 24 sites of non-family PD [2]. Among them, mutations in LRRK2 (Park8) were found to be in ge...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07D491/14C07D267/04C07D487/04C07D243/06C07D498/04C07D519/00A61P35/00A61P25/00A61K31/437A61K31/4162
CPCA61P25/00A61P35/00C07D471/14C07D471/22A61K31/55
Inventor 夏岩爱德华·贾尔斯·麦卡弗宋阳徐元元朱琳褚纯隽吴玲刘淼贾斯丁·史蒂文·布莱恩斯
Owner SUZHOU YABAO PHARMA R&D CO LTD