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A kind of polypeptide derivative and its use in the field of medicine

A technology of derivatives and polypeptides, which is applied in polypeptide derivatives and its pharmaceutical and pharmaceutical fields to achieve good analgesic activity and less side effects

Active Publication Date: 2022-05-13
CHENGDU SINTANOVO BIOTECHNOLOGV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, once the κ opioid receptor (KOR) agonist with less side effects is approved for marketing, it will definitely become a highly competitive analgesic and anti-inflammatory product, which will have a great impact on the existing market

Method used

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  • A kind of polypeptide derivative and its use in the field of medicine
  • A kind of polypeptide derivative and its use in the field of medicine
  • A kind of polypeptide derivative and its use in the field of medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] Such as figure 2 Shown, TM1 can be prepared by the following process steps:

[0077] Step 1: Synthesis of intermediate SM3

[0078] Swell 2-CTC Resin (the degree of substitution is 0.993mmol / g, 2g) with DCM (20mL) at room temperature, the swelling time is 15min, the solvent is removed, SM2 (1.120g, 2.4mmol) and DIEA (0.516g, 4.0 mmol) in DCM (15mL) was added to the swollen resin and reacted for 2h at room temperature; then methanol (2mL) and DIEA (1mL) were added and the reaction was continued for 0.5h; the solvent was drained and washed three times with DCM (30mL) , and finally washed three times with DMF (30mL), and directly put the resin to the next step for reaction.

[0079] Step 2: Synthesis of intermediate SM4

[0080] Add piperidine / DMF (V / V=1 / 4, 20mL) to the product obtained in step 1, react at room temperature for 10min, drain, add piperidine / DMF again (V / V=1 / 4, 20mL ), drained after reacting 10mim at room temperature, and washed 5 times with DMF (30mL), ...

Embodiment 2

[0102] like image 3 Shown, TM2 can be made through the following process steps:

[0103] Step 1: Synthesis of intermediate SM11-2

[0104] At room temperature, acetic acid (72mg, 0.6mmol), SM9 (300mg, 0.3mmol) and SM10-2 (46mg, 0.3mmol) were dissolved in 1,2-dichloroethane (5mL) for 30min at room temperature, and then Sodium triacetoxyborohydride (126 mg, 0.6 mmol) was added to react at room temperature for 4 h; quenched with 30 mL of water, extracted 3 times with DCM (30 mL), dried the organic phase and spin-dried to obtain the crude product, which was purified by preparative HPLC to obtain Intermediate SM11-2 (211 mg).

[0105] ESI-MS(m / z):1136.6(M+H+)

[0106] Step 2: Synthesis of intermediate SM12-2

[0107] At room temperature, SM11-2 (190 mg, 0.18 mmol) was added to 10 mL of methanol solution of methylamine, stirred and reacted for 1 h at room temperature, and the reaction solution was directly spin-dried, and the obtained crude product was purified by preparative H...

Embodiment 3

[0114] like Figure 4 Shown, TM3 can be prepared by the following process steps:

[0115] Step 1: Synthesis of intermediate SM11-3

[0116] At room temperature, acetic acid (72mg, 0.6mmol), SM9 (300mg, 0.3mmol) and SM10-3 (45mg, 0.3mmol) were dissolved in 1,2-dichloroethane (5mL) for 30min at room temperature, and then Sodium triacetoxyborohydride (126 mg, 0.6 mmol) was added to react at room temperature for 4 h; quenched with 30 mL of water, extracted 3 times with DCM (30 mL), dried the organic phase and spin-dried to obtain the crude product, which was purified by preparative HPLC to obtain Intermediate SM11-3 (205 mg).

[0117] ESI-MS(m / z):1136.6(M+H+)

[0118] Step 2: Synthesis of intermediate SM12-3

[0119] At room temperature, SM11-3 (190 mg, 0.18 mmol) was added to 10 mL of methanol solution of methylamine, stirred and reacted at room temperature for 1 h, and the reaction solution was directly spin-dried to obtain the crude product, which was purified by preparativ...

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Abstract

The invention discloses a polypeptide derivative and its use in the field of medicine, which belongs to the field of medicine, and specifically relates to a polypeptide derivative containing a boronic acid group and a preparation method thereof, and discloses its use in the prevention and treatment of Use in medicine for various diseases caused by kappa opioid receptors.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a polypeptide derivative and its application in the field of medicine. Background technique [0002] Analgesics mainly act on the central or peripheral nervous system, selectively inhibit and relieve various pains, and relieve pain caused by fear, tension and anxiety pain. In terms of product types, the current global pain relief market is dominated by opioids and non-steroidal anti-inflammatory drugs (NSAIDS), accounting for more than 52% of the total market revenue in 2015. According to a report by Transparency Market Research (TMR), the global pain relief market will reach $88.2534 billion by the end of 2025. [0003] Traditional μ opioid receptor agonists (such as morphine and its derivatives) are the main drugs for clinically relieving severe pain, and are the most powerful analgesics used in the world. The most effective drug for posterior pain and moderate to severe pain caused b...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K5/107C07K7/02A61K38/07A61K38/08A61P25/02A61P25/04
CPCC07K5/1016C07K7/02A61P25/02A61P25/04A61K38/00
Inventor 付晓平李元波高剑袁瑜张佳丽
Owner CHENGDU SINTANOVO BIOTECHNOLOGV CO LTD
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