Unlock instant, AI-driven research and patent intelligence for your innovation.
Fused ring gamma-amino acid derivatives and their preparation methods and applications in medicine
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
A compound and composition technology, applied in the field of fused ring γ-amino acid derivatives, can solve the problems of patients with abuse, low safety, and dependence
Active Publication Date: 2020-12-15
SICHUAN HAISCO PHARMA CO LTD
View PDF10 Cites 0 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
[0003]
However, for gabapentin, the proportion of improving the pain of patients with diabetic peripheral neuropathy is about 60% (Acta Neurol. Scand. 101:359-371, 2000), for pregabalin, although its tolerance is better than gabapentin , but its safety is lower, and it has the possibility of abuse or making patients dependent (Am J Health SystPharm.2007; 64(14):1475-1482)
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.
[0095] Lithium aluminum tetrahydride (3.8g, 100mmol) was added to dry methyl tert-butyl ether (300mL), and cyclohexene-1-carbonitrile (1A) (6g, 56mmol) in methyl tert-butyl ether was added dropwise (300mL) solution, add reflux reaction for 1 hour, after cooling, add 1 equivalent of water, 1 equivalent of sodiumhydroxideaqueous solution (15%), stir for 30 minutes, filter out the solid, filter cake with water (100mL) and methyl Wash with tert-butyl ether (100mL), separate the organic phase from the filtrate,...
[0142] The first step: cyclopent-1-en-1-ylmethylamine (2B)
[0143] cyclopent-1-en-1-ylmethanamine
[0144]
[0145] Lithiumaluminum hydride (7.4g, 200mmol) was dissolved in methyl tert-butyl ether (400mL), and cyclopent-1-ene-1-carbonitrile (2A) (10g, 110mmol) was dissolved in methyl tert-butyl dropwise Base ether (400 mL) solution was heated to reflux for 1 hour after dropping. Cool to room temperature, add dropwise water (7.4mL), sodiumhydroxideaqueous solution (15% (w%), 7.4mL) and water (15mL) successively under ice-water bath, filter with suction, dry with anhydroussodiumsulfate, filter, the filtrate reduces conce...
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 relates to a fused cyclic gamma-amino acid derivative, a preparation method of the fused cyclic gamma-amino acid derivative, and an application of the fused cyclic gamma-amino acid derivative to pharmaceuticals, and particularly relates to the fused cyclic gamma-amino acid derivative shown as in the formula (I), or a stereisomer, a solvate, a metabolite, a prodrug, a pharmaceutically acceptable salt or co-crystal of the fused cyclic gamma-amino acid derivative, a pharmaceutical composition comprising the fused cyclic gamma-amino acid derivative, and the application of the compound or composition to the field of analgesia, wherein the definitions of various substituent groups in the formula (I) and the definitions in the description are the same.
Description
technical field [0001] The present invention relates to a fused ring γ-amino acid derivative represented by general formula (I), or its stereoisomer, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal, and its drug Composition and use in the field of analgesia. Background technique [0002] Voltage-gated calcium channels are composed of α1 subunits and accessory proteins α2δ, β, and γ subunits. α2δ protein can regulate the density and voltage-dependent dynamics of calcium channels (Felix et al(199 7) J.Neuroscience 17:6884-6891; Klugbauer et al(1999) J.Neuroscience 19:684-691; Hobom et al. al (2000) Eur. J. Neuroscience 12:1217-1226; and Qin et al (2002) Mol. Pharmacol. 62:485-496). Compounds that exhibit high affinity binding to the voltage-dependent calcium channel subunit α2δ have been shown to be effective in the treatment of pain, such as pregabalin and gabapentin. In mammals, there are four subtypes of α2δ protein, each of which is encoded ...
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