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Therapeutic or preventive agent for nausea/vomiting

一种预防剂、治疗剂的技术，应用在预防恶心和呕吐的治疗剂或预防剂领域，能够解决抗恶心和呕吐的治疗和预防作用没有揭示、很差效果等问题

Inactive Publication Date: 2006-12-06
TORAY IND INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the following problems have recently been discovered: 5-HT 3 Antagonists have poor effect on delayed emesis that occurs 2 or more days after administration of anticancer drugs
However, the therapeutic and preventive effects of the indomorphinan (indolomorphinan) derivatives, quinolinomorphinan (quinolinomorphinan) derivatives and 7-benzylidene morphinan derivatives of the present invention against nausea and vomiting are not revealed in these reports

Method used

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  • Therapeutic or preventive agent for nausea/vomiting
  • Therapeutic or preventive agent for nausea/vomiting
  • Therapeutic or preventive agent for nausea/vomiting

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Inhibitory effect of NTI on morphine-induced nausea and vomiting:

[0086] Experiment with male ferrets. The frequency of nausea and vomiting was observed from the time of morphine administration to 1 hour after administration.

[0087] Morphine (0.1-3 mg / kg) was injected subcutaneously to male ferrets. Lower doses can significantly induce nausea and vomiting. To investigate the inhibitory effect of NT1 on morphine-induced nausea and vomiting. NT1 (5 mg) was injected subcutaneously 30 minutes before morphine administration (0.6 mg / kg). The inhibitory effect of NT1 on morphine-induced nausea and vomiting is shown in Figures 1 and 2.

Embodiment 2

[0089] Inhibitory effects of test compounds on morphine-induced nausea and vomiting:

[0090] Experiment with male hounds. The frequency of nausea and vomiting was observed 10 minutes after morphine administration.

[0091]Morphine (0.5 mg / kg) was injected intravenously in the forelegs of male retrievers. Nausea and vomiting were evident within 5 minutes of injection. Fifteen minutes after the morphine injection, the test compound was injected intravenously into the front leg. See Table 1 for the doses of the test compounds to inhibit nausea and vomiting induced by morphine.

[0092] The antiemetic effect of table 1 test compound

[0093] Test compound dose (mg / kg)

[0094] Compound 2 (comparative example 2) 1.0

[0095] Compound 3 (comparative example 3) 1.0

[0096] Compound 4 (comparative example 4) 3.0

[0097] Compound 5 (comparative example 5) 1.0

[0098] Compound 6 (comparative example 6) 3.0

[0099] Compound 7 (comparative example 7) 1.0

[0100...

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PUM

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Abstract

A therapeutic or preventive agent for nausea / vomiting which contains as an active ingredient either a morphinane derivative represented by the general formula (I): (I) (wherein R<1> represents cyclopropylmethyl, etc.; R<2> and R<3> each represents hydroxy, methoxy, etc.; R<4> and R<5> are bonded to each other to form -O-, etc.; R<6> represents hydrogen, etc.; and Q represents (II) which has been optionally substituted, etc., provided that X represents NH, NMe, etc.) or a pharmacologically acceptable acid addition salt thereof. The compound or salt is useful in a medicine widely applicable to vomiting caused by drugs having emetic activity, especially in a therapeutic or preventive agent for nausea / vomiting induced by agonists represented by morphine.

Description

technical field [0001] The present invention relates to therapeutic or preventive agents for preventing nausea and vomiting. Specifically, the present invention relates to a therapeutic or preventive agent for preventing nausea and vomiting caused by mu-opioid agonists represented by morphine. Background technique [0002] Nausea and vomiting caused by taking emetic drugs such as opioid analgesics and anticancer drugs is one of the most distressing side effects experienced by patients. In particular, morphine, an analgesic commonly used by cancer patients, is known to frequently cause side effects of nausea and vomiting. Due to morphine, D 2 Antagonists such as domperidone and haloperidol or antiemetic drugs including 5-HT 3 Antagonists are used to prevent nausea and vomiting, but the antiemetic effects of these drugs are unclear. In particular, in the initial stage of morphine administration, the administered dose is often insufficient to relieve pain due to nausea and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D491/18C07D491/22C07D491/08A61K45/00A61K31/485A61P1/08A61P25/00
CPCA61K31/485C07D491/18A61P1/08A61P25/00A61P43/00C07D491/08
Inventor 河合孝治斋藤显宜铃木知比古长谷部光铃木勉
Owner TORAY IND INC
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