Alkoxyl terminal group oligo-PEG modified aminopyrimidine derivative and antitumor application
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
An alkyl compound technology, applied in the field of pyrazolo[3,4-d]pyrimidine derivatives, can solve the problems of low bioavailability, high toxicity and side effects, and low specificity, so as to promote apoptosis, Promising effect of inhibiting cell proliferation and clinical medicinal use
Active Publication Date: 2017-08-29
WEST CHINA HOSPITAL SICHUAN UNIV
View PDF5 Cites 8 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
Problems solved by technology
Although there are a variety of drugs for the treatment of cancer on the market, they all have various defects, such as low bioavailability, low specificity, and large toxic and side effects.
These defects are often caused by the structural characteristics of the compound itself and its target, and it is difficult to overcome it in further research and development.
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
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0042] The preparation of embodiment 1 compound of the present invention
[0043]
[0044] Compound 1 (269mg, 1mmol) was dissolved in 1,4-dioxane / water (4:1) 150ml solution, and transferred to a 250ml round bottom flask, and then added (1.38g, 10mol) to the reaction solution Potassium carbonate, after stirring at room temperature for three minutes, add the catalyst bis-diphenylphosphinoferrocene palladium chloride (73.1 mg, 0.1 mol), heat the reaction mixture to 100 ° C, detect the reaction by TLC, after the reaction is completed , first, after the reaction solution is cooled, add 50ml of distilled water, then transfer to a separatory funnel, add 100ml of dichloromethane to extract 3 times, combine the organic phases, add anhydrous sodium sulfate, spin dry the organic solvent, and separate through a silica gel column Intermediate compound 2 (200 mg, 70%) was obtained, (dichloromethane:(dichloromethane:methanol)=100:2.5).
[0045] 1 H NMR (600MHz, DMSO-6d) δ9.83(s, 1H, HOA...
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
Login to view more
Abstract
The invention discloses a pyrazolo[3,4-d]pyrimidine derivative that is represented as the formula (I), which has significant growth inhibiting effect, apoptosis promoting effect and cell proliferation alleviating effect on tumor cells, can be used for preventing and/or treating tumor related diseases, and has wide application prospect.
Description
technical field [0001] The invention belongs to the field of compound drugs, in particular to pyrazolo[3,4-d]pyrimidine derivatives and applications thereof. Background technique [0002] Malignant tumors grow fast and show invasive growth, prone to hemorrhage, necrosis, ulcers, etc., and often have distant metastasis, resulting in body weight loss, weakness, anemia, loss of appetite, fever, and severe damage to organ functions, eventually causing The death of the patient poses a huge threat to the health and life of the crowd. [0003] Surgical treatment Radical resection is still the most basic and commonly used treatment for lung cancer, kidney cancer, liver cancer and other cancers. However, resection is usually traumatic, and it will cause damage to body tissues and loss of blood after surgery, so it is not suitable The elderly, those with poor physical fitness and those with heart, lung, liver and other important organ diseases are selected. Therefore, it is necessary...
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
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to view more 
Login to view more