CN103588666A - Compound with high optical purity - Google Patents
Compound with high optical purity Download PDFInfo
- Publication number
- CN103588666A CN103588666A CN201310534476.9A CN201310534476A CN103588666A CN 103588666 A CN103588666 A CN 103588666A CN 201310534476 A CN201310534476 A CN 201310534476A CN 103588666 A CN103588666 A CN 103588666A
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- Prior art keywords
- pain
- compound
- cancer
- optical purity
- high optical
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- WUYGAPDBAIUWLJ-NZHRPXBSSA-N CC/C=C\CC(/C=C/C=C\C=C\C=C\CC[C@@H](/C(/O)=C\CCC(NCC)=O)O)O Chemical compound CC/C=C\CC(/C=C/C=C\C=C\C=C\CC[C@@H](/C(/O)=C\CCC(NCC)=O)O)O WUYGAPDBAIUWLJ-NZHRPXBSSA-N 0.000 description 1
- LKFAAGBKHANSKU-MXEZQCJESA-N CC/C=C\CC/C=C/C=C\C=C\C=C\CC[C@H](/C(/O)=C\CCC(NCC)=O)O Chemical compound CC/C=C\CC/C=C/C=C\C=C\C=C\CC[C@H](/C(/O)=C\CCC(NCC)=O)O LKFAAGBKHANSKU-MXEZQCJESA-N 0.000 description 1
Abstract
Belonging to the technical field of medicines, the invention in particular relates to application of a compound with high optical purity in preparation of cancer pain drugs. The invention also relates to pharmaceutical compositions containing the compound.
Description
Technical field
The invention belongs to biomedicine field, be specifically related to 7S, 8R, 175-trihydroxy--4Z, 9E, 11E, 13Z, 15E, the application of 19Z-bis-dodecahexaenes-N-buserelin in preparation control cancer pain medicine.
Background technology
Pain is one of modal Tumor-assaciated symptom, and the definition of pain is " sensation and the emotional experience that are associated with actual or potential tissue injury or similar lesions ".Cancer pain refers to the pain due to cancer, cancer related pathologies and anticancer therapy.Cancer pain is often chronic pain.Pain is cancer patients's common sympton, the cancer patients of approximately 1/4 new diagnosis, 1/3 cancer patients who is receiving treatment and 3/4 patient with advanced cancer merge pain, cancer pain patient may survive several months or several years, if can not get appropriate pain management, patient is by the torment bearing the pain for a long time, and greatly affect their activity, sleep, mood and whole quality of life, pain caused by cancer is patient's personality integrity totteringly, arrange their self consciousness, causing lasting angor in the depth of one's heart.The misery that canurous ache patients is experienced in spirit, social mentality, mode of life, anxiety often surpass the pain that disease itself causes.
The World Health Organization (WHO) organizes palliative treatment expert, cancer pain expert to formulate the global guide of alleviating cancer pain nineteen eighty-two, i.e. famous three step analgesia therapies, although pass by for more than 20 years, the fundamental principle of three ladders is still widely accepted.WHO has determined the international benchmark of the pain therapy centered by opium kind analgesics, becomes the main flow of cancer pain treatment according to the therapeutics of this benchmark.Mild pain: the first ladder of first-selected three ladders be take the NSAID (non-steroidal anti-inflammatory drug) (Nonsteroidal Antiinflammatory Drugs, NSAIDs) that acetylsalicylic acid is representative; Moderate pain: first-selected weak opioid drug (take Cocaine as representative), and can share non-steroidal anti-inflammatory drugs; Severe pain: first-selected strong opioid drug (take morphine as representative), and can share non-steroidal anti-inflammatory drugs simultaneously.But easily there is the side effects such as gastrointestinal damage or renal impairment in known nonopioid analgesic NSAIDs.Also know opium kind analgesics morphine as representational side effect have constipation, feel sick, vomiting etc., also have owing to ending suddenly administration or reducing dosage and bring Withrawal symptom.In addition, in cancer pain, also comprise neuropathic pain, because it is the pain that peripheral nerve or nervus centralis come to harm and occur, so opiates effect is limited.In addition, when morphine chronic administration, the anti-opioid such as cholecystokinin or neuropeptide tyrosine strengthens, and causes the analgesic effect of morphine to decline, and forms analgesia resistance.So need to develop the anodyne of few side effects, replace existing non-opium and opium kind analgesics.
Summary of the invention
The object of the invention is, in order to make up the deficiency of product on market, provides a kind of compound that is high-optical-purity, and described compound is as follows: 7S, 8R, 17S-trihydroxy--4Z, 9E, 11E, 13Z, 15E, 19Z-bis-dodecahexaenes-N-buserelin, its structural formula is as follows:
Further, 7S, 8R, 17S-trihydroxy--4Z, 9E, 11E, 13Z, 15E, the application of 19Z-bis-dodecahexaenes-N-buserelin in preparation control cancer pain medicine.
The compound that is high-optical-purity of the present invention can be made pharmaceutically acceptable arbitrary formulation with one or more pharmaceutical excipients.
Embodiment
Embodiment 1. is alleviated the evaluation of cancer pain drug effect
Animal modeling: after Animal Anesthesia, left side hind leg cropping, 75% ethanol disinfection femur and shin bone place skin, a skin incision that is about 0.5～1.0cm is cut along rectus femoris muscle tendon direction by knee joint place, the careful kneecap that exposes, first with disposable sterilized 1mL syringe needle, at kneecap, along the puncture of femur long axis direction, punch, then change 10 μ L syringes and enter marrow cavity of femur, slowly inject the Lewis murine lung cancer cell solution of 10 μ L (containing 3 * 10
5individual cell) to femur.After injection, with bone wax seal, live pin hole, clean wound, skin closure.Sham operated rats animal left side kneecap injects isopyknic physiological saline, and all the other operate same model group, and blank group is not carried out any processing.
Evaluation index: measure the thermal stimulus threshold of pain with hot plate method in mice, first that hot plate temperature is constant in (50 ± 1) ℃, then mouse is placed on hot plate, when occurring licking metapedes, needed time value (s) is the threshold of pain of this animal, every mouse is surveyed 3 times, interval 5min, gets 3 averages as the thermal stimulus threshold of pain of this animal (screening Basic Pain Threshold the animal of 10～30s for experiment).
Medication and result: modeling starts administration on the 8th day, is used in conjunction 7d.Modeling the 14th day, the treatment group thermal stimulus threshold of pain obviously extends, and relatively has significant difference (P<0.05), in Table 1 with model group.
Table 1. pain caused by cancer is respectively organized the variation of the mouse different time points thermal stimulus threshold of pain
With model group with time point comparison
Δp<0.05
Conclusion: table 1 data fully show that this compound has the effect of good control cancer pain, are compound 7S, 8R, 17S-trihydroxy--4Z, 9E, 11E, 13Z, 15E, the application of 19Z-bis-dodecahexaenes-N-buserelin in preparation control cancer pain medicine provides solid foundation.
Claims (3)
1. a compound that is high-optical-purity:
7S, 8R, 17S-trihydroxy--4Z, 9E, 11E, 13Z, 15E, 19Z-bis-dodecahexaenes-N-buserelin, its structural formula is as follows:
2. a kind of compound that is high-optical-purity according to claim 1, is characterized in that: the application in preparation control cancer pain medicine.
3. a kind of compound that is high-optical-purity described in claim 1～2, is characterized in that: can make pharmaceutically acceptable arbitrary formulation with one or more pharmaceutical excipients.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310534476.9A CN103588666A (en) | 2013-10-26 | 2013-10-26 | Compound with high optical purity |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310534476.9A CN103588666A (en) | 2013-10-26 | 2013-10-26 | Compound with high optical purity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103588666A true CN103588666A (en) | 2014-02-19 |
Family
ID=50079023
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310534476.9A Pending CN103588666A (en) | 2013-10-26 | 2013-10-26 | Compound with high optical purity |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103588666A (en) |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006044381A2 (en) * | 2004-10-13 | 2006-04-27 | University Of Connecticut | Cannabinergic lipid ligands |
| US20120245229A1 (en) * | 2009-09-15 | 2012-09-27 | Ru-Rong Ji | Method for treating neuropathic pain |
| CN102725261A (en) * | 2009-11-25 | 2012-10-10 | 赛托麦蒂克斯有限公司 | Arachidonic acid analogs and methods for analgesic treatment using same |
| CN103193647A (en) * | 2013-04-01 | 2013-07-10 | 史克勇 | Cancer pain treatment medicine with high optical purity |
| CN103193646A (en) * | 2013-04-01 | 2013-07-10 | 史克勇 | Medicine for treating pain |
-
2013
- 2013-10-26 CN CN201310534476.9A patent/CN103588666A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006044381A2 (en) * | 2004-10-13 | 2006-04-27 | University Of Connecticut | Cannabinergic lipid ligands |
| US20120245229A1 (en) * | 2009-09-15 | 2012-09-27 | Ru-Rong Ji | Method for treating neuropathic pain |
| CN102725261A (en) * | 2009-11-25 | 2012-10-10 | 赛托麦蒂克斯有限公司 | Arachidonic acid analogs and methods for analgesic treatment using same |
| CN103193647A (en) * | 2013-04-01 | 2013-07-10 | 史克勇 | Cancer pain treatment medicine with high optical purity |
| CN103193646A (en) * | 2013-04-01 | 2013-07-10 | 史克勇 | Medicine for treating pain |
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| C06 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C05 | Deemed withdrawal (patent law before 1993) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20140219 |