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Therapeutic agent for pain

A cancer pain, pharmaceutical technology, applied in the field of pain treatment drugs or preventive drugs, can solve the problems of weak tumor shrinkage and deterioration during survival

Inactive Publication Date: 2011-04-20
ZERIA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

For example, gemcitabine hydrochloride, which is known to be used in the treatment of pancreatic cancer where pain is severe and pain management is a problem, has a relatively weak tumor shrinking effect in chemotherapy, but it shows an excellent pain relieving effect in pancreatic cancer patients (Non-Patent Document 15)
In addition, compared with gemcitabine hydrochloride alone, the combination of irinotecan and gemcitabine hydrochloride showed a strong tumor shrinkage effect on pancreatic cancer, but no difference was seen in the QOL evaluation including pain relief, and worsening during survival was reported. (Non-Patent Document 16)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] The B16-BL6 melanoma cell solution was subcutaneously transplanted into the plantar of the right foot of the mouse (2 × 10) using a syringe and an injection needle. 5 per mouse). After cancer transplantation, von Frey filament was used to stimulate the plantar of the transplanted side of the mouse, and the pain threshold (gram load of filament in response to tactile stimulation) was measured. A single dose of the calcium salt of Compound A (Compound A1) was administered on the 14th day after cancer transplantation, where the decrease in the pain threshold was considered to be significant and stable, and the change in the pain threshold was investigated. Compound (A1) was suspended in a 0.5% CMC-Na solution to prepare. show the result in figure 1 . In a cancer pain model, allodynia (allodynia) (ie, tactile stimuli that are not normally felt as pain), pain thresholds were significantly lowered, but a single oral dose of 100 mg / kg of compound ( A1) increased the pain t...

Embodiment 2

[0081] The B16-BL6 melanoma cell solution was subcutaneously transplanted into the plantar of the right foot of the mouse (2 × 10) using a syringe and an injection needle. 5 per mouse). After transplantation, von Frey filament was used to stimulate the plantar of the transplanted side of the mouse to measure the change in pain threshold (grams of filament load in response to tactile stimulation). The compound (A1) or the CCK2 receptor antagonist L-365260 was repeatedly orally administered at a dose of 100 mg / kg eight times a day from the seventh day after cancer transplantation, and changes in pain threshold were examined. show the result in figure 2 . Allodynia occurred on the 7th day after cancer transplantation, and the pain threshold decreased significantly on the 14th day after cancer transplantation, but oral administration of compound (A1) increased the pain threshold and improved allodynia. On the other hand, with L-365260, no improvement effect on allodynia was se...

Embodiment 3

[0083] The B16-BL6 melanoma cell solution was subcutaneously transplanted into the plantar of the right foot of the mouse (2 × 10) using a syringe and an injection needle. 5 per mouse). After transplantation, von Frey filament was used to stimulate the plantar of the transplanted side of the mouse to measure the change in pain threshold (grams of filament load in response to tactile stimulation). On the 14th day after cancer transplantation, 100 mg / kg of the calcium salt of Compound A (Compound A1) and 2.5 mg / kg of morphine hydrochloride were administered in combination. The result is as image 3 As shown, in the combined use group of Compound A1 and morphine, higher antiallodynic effects were confirmed than those of Compound A1 alone and morphine alone.

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Abstract

Disclosed is a therapeutic and / or prophylactic agent for cancer pain, which can be administered continuously for a long period between the early stage and the final stage of the cancer pain therapy in place of conventional non-opioid or opioid analgesic agents. The therapeutic and / or prophylactic agent for cancer pain comprises a 1,5-benzodiazepine derivative represented by general formula (1) [wherein R1 represents a C1-6 alkyl group; R2 represents a phenyl group or a cyclohexyl group; and Y represents a single bond or a C1-4 alkylene group] or a pharmaceutically acceptable salt thereof as an active ingredient.

Description

technical field [0001] The present invention relates to a pain therapeutic or preventive drug useful for pain, particularly cancer pain. Background technique [0002] The so-called pain refers to the result that the pain nerve ending plate perceives physical stimulation or chemical stimulation caused by pain substances, and the brain recognizes it as pain. This "pain" is one of the factors that reduces QOL the most. Pain is classified on the basis of its origin, and can be roughly divided into three categories: nociceptive pain, neurogenic pain, and psychogenic pain. The so-called nociceptive pain is pain felt by nociceptors, which occurs when tissue damage or a noxious stimulus with the possibility of injury is applied to a living body. In addition, the so-called neuropathic pain is caused by the primary damage of the nervous system or its function abnormality, or the pain caused by it, and is sometimes based on peripheral and central damage. In addition, the so-called p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D243/12A61K31/551A61K45/00A61P25/04
CPCC07D243/12A61K31/551A61P25/04A61P29/00A61P35/00A61K45/06
Inventor 吉长幸嗣滨野弘树堀井孝幸
Owner ZERIA PHARMA
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