CN1081035C - Antimalarial compound naphtholquine - Google Patents

Antimalarial compound naphtholquine Download PDF

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Publication number
CN1081035C
CN1081035C CN97114291A CN97114291A CN1081035C CN 1081035 C CN1081035 C CN 1081035C CN 97114291 A CN97114291 A CN 97114291A CN 97114291 A CN97114291 A CN 97114291A CN 1081035 C CN1081035 C CN 1081035C
Authority
CN
China
Prior art keywords
medicine
naphtholquine
dihydroarteannuin
trimethoprim
phosphate
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CN97114291A
Other languages
Chinese (zh)
Other versions
CN1191113A (en
Inventor
李国桥
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Jianqiao Medicine Development Co., Ltd., Chongqing City
Original Assignee
Jianqiao Sci & Tech Dev Co Ltd Guangzhou City
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Jianqiao Sci & Tech Dev Co Ltd Guangzhou City filed Critical Jianqiao Sci & Tech Dev Co Ltd Guangzhou City
Priority to CN97114291A priority Critical patent/CN1081035C/en
Publication of CN1191113A publication Critical patent/CN1191113A/en
Priority to ZA9810472A priority patent/ZA9810472B/en
Priority to CO98067813A priority patent/CO4980890A1/en
Priority to PCT/CN1998/000274 priority patent/WO1999025351A1/en
Priority to AU12227/99A priority patent/AU1222799A/en
Priority to PE1998001114A priority patent/PE134499A1/en
Application granted granted Critical
Publication of CN1081035C publication Critical patent/CN1081035C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The present invention provides a novel compound naphtholquine medicine used for treating malaria, which is prepared from naphtholquine phosphate, dihydroartemisine and methoxypyrimidine. Clinical experiments show that the medicine has the characteristics of simple and ripe process, high stability, strong medicine effects, high speed for killing plasmodium, high cure rate, less side effect, high safety, simple and convenient medicine taking, etc., and has important significance for prevention and treating malaria.

Description

Antimalarial compound naphtholquine
The present invention relates to a kind of treatment and prevention of malaria new drug, particularly compound recipe naphthols quinoline new drug.
At present, the multiple drug resistance pernicious malaria whole world spreads, and Southeast Asia is particularly serious.The mefloquine (Wefloquine) and the compound recipe Fa Ximi (Fansiaef) thereof of very big hope expresses in World Health Organization (WHO), and also owing to its drug-fast rapid appearance, at first in Thailand, it is very poor to be in curative effect in Vietnam then, and the no small condition of toxicity.Arteannuin of having developed since China's the seventies and derivant artesunate thereof, Artemether, dihydroarteannuin etc. have high quick-acting advantage, just can reach high curative rate in 7 days but must take medicine, otherwise the recrudescence rate height are unfavorable for the control of the malaria source of infection.Therefore still not having better pernicious malaria curative at present can be for selecting for use.
Switzerland WORVATIS drugmaker is developing a technology-Coartem of buying to China again, (being made up of Artemether and benflumetol), might be better than existing antimalarial, but still need 3 days its course of treatment, and cost being higher.The Walarone that Britain Glaxo Wellcome company is developing is made up of naphthoquinone (Waphthoqinone) and cyclochloroguanidum, does not have active remedy in its prescription, 3 days courses of treatment, need take medicine every day 2 times.
Purpose of the present invention is intended to overcome the deficiencies in the prior art and provides that a kind of technology is simple ripe, to kill protozoon speed fast and toxicity is low, safety and stability, takes antimalarial compound naphtholquine simply and easily.
The object of the present invention is achieved like this:
A kind of compound recipe naphthols quinoline, it is characterized in that being made up of NAPHTHOQUINE PHOSPHATE (Waphthoqoine phosphate), dihydroarteannuin (Dihydroarteaisinin) or its similar medicine and trimethoprim (Trimethopria), the weight proportion scope of three medicines is:
NAPHTHOQUINE PHOSPHATE 5-8 part
Dihydroarteannuin or its similar medicine 1-2 part
Trimethoprim 2-3 part
Promptly the ratio of three medicine parts is 5-8: 1-2: 2-3
Dihydroarteannuin or its similar medicine are meant artesunate (Arteswnate), arteether (Arteether), Artemether (Arteaether) and arteannuin (Artemisinin), and artemisinin derivative.This type of medicine finally all is converted into dihydroarteannuin and brings into play it and kill the protozoacide effect in body.
Below by embodiment the present invention is described in further detail;
Prescription
Phosphoric acid Cai phenol quinoline (C 24H 28CLW 3O2H 3PO 4) 600g
Dihydroarteannuin (C 15H 24O 5) 100g
Trimethoprim (C 14H 10W 4O 3) 200g
Adjuvant (hydroxypropyl cellulose) is an amount of
Make 1000
Preparation process
Earlier raw and auxiliary material is detected,, cross 100 mesh sieves, then, accurately take by weighing raw material and adjuvant by recipe quantity with qualified raw material pulverize separately.NAPHTHOQUINE PHOSPHATE, trimethoprim, dihydroarteannuin and adjuvant hydroxypropyl cellulose (HPC) are mixed, and evenly tabletting is packed, and is finished product.
It is simple, ripe that medicine of the present invention shows that by clinical trial this compound medicine has technology, Good stability, drug action is strong, kills that malaria is former to go out the speed height, the cure rate height, toxic and side effect is few, The characteristics such as security is bigger, especially it takes medicine simple and conveniently, only needs to take medicine for 1-2 time, and is right Control in malaria disease is significant.

Claims (2)

1, a kind of compound recipe naphthols quinoline is characterized in that being made up of NAPHTHOQUINE PHOSPHATE, dihydroarteannuin or its similar medicine and trimethoprim, and the weight proportion scope of three medicines is:
NAPHTHOQUINE PHOSPHATE 5-8 part
Dihydroarteannuin or its similar medicine 1-2 part
Trimethoprim 2-3 part
Promptly the ratio of three medicine parts is 5-8: 1-2: 2-3.
2, compound recipe naphthols quinoline according to claim 1 is characterized in that the similar medicine of dihydroarteannuin is meant artesunate, arteether, Artemether and arteannuin, and artemisinin derivative.
CN97114291A 1997-11-18 1997-11-18 Antimalarial compound naphtholquine Expired - Fee Related CN1081035C (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
CN97114291A CN1081035C (en) 1997-11-18 1997-11-18 Antimalarial compound naphtholquine
ZA9810472A ZA9810472B (en) 1997-11-18 1998-11-16 An antimalarial composition
CO98067813A CO4980890A1 (en) 1997-11-18 1998-11-18 AN ANTIMALARIC COMPOSITION METHOD FOR TREATING MALARIA
PCT/CN1998/000274 WO1999025351A1 (en) 1997-11-18 1998-11-18 Antimalaria pharmaceutical compositions
AU12227/99A AU1222799A (en) 1997-11-18 1998-11-18 Antimalaria pharmaceutical compositions
PE1998001114A PE134499A1 (en) 1997-11-18 1998-12-01 COMPOSITION AGAINST MALARIA

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN97114291A CN1081035C (en) 1997-11-18 1997-11-18 Antimalarial compound naphtholquine

Publications (2)

Publication Number Publication Date
CN1191113A CN1191113A (en) 1998-08-26
CN1081035C true CN1081035C (en) 2002-03-20

Family

ID=5172855

Family Applications (1)

Application Number Title Priority Date Filing Date
CN97114291A Expired - Fee Related CN1081035C (en) 1997-11-18 1997-11-18 Antimalarial compound naphtholquine

Country Status (6)

Country Link
CN (1) CN1081035C (en)
AU (1) AU1222799A (en)
CO (1) CO4980890A1 (en)
PE (1) PE134499A1 (en)
WO (1) WO1999025351A1 (en)
ZA (1) ZA9810472B (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1135974C (en) * 2000-08-23 2004-01-28 重庆健桥医药开发有限公司 Antimalarial compound dihydroartemisinin
CN104666300B (en) * 2014-07-04 2017-01-18 昆药集团股份有限公司 Application of naphthoquine phosphate
CN111265527B (en) * 2020-03-05 2021-04-23 中国人民解放军军事科学院军事医学研究院 Application of naphthoquine and pharmaceutically acceptable salt thereof in preparation of anti-coronavirus medicines

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1041694A (en) * 1988-10-07 1990-05-02 赫彻斯特股份公司 The anti-malaria composition of quinidine, arteannuin and derivant thereof and Therapeutic Method

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2748333A1 (en) * 1977-10-28 1979-05-03 Hoechst Ag AGENT AGAINST MALARIA
US5219865A (en) * 1987-05-08 1993-06-15 Hoechst Aktiengesellschaft Pharmaceutical combination for the prophylaxis and therapy of malaria

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1041694A (en) * 1988-10-07 1990-05-02 赫彻斯特股份公司 The anti-malaria composition of quinidine, arteannuin and derivant thereof and Therapeutic Method

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
《中国医药工业杂志》，20(8) 1989.8.31 邓蓉仙，"我国近几年抗疟药研究新进展" *
《新编药物学》，第13版 1996.3.1 陈新谦，人民卫生出版社 *
《新编药物学》，第13版 1996.3.1 陈新谦，人民卫生出版社;《中国医药工业杂志》，20(8) 1989.8.31 邓蓉仙，"我国近几年抗疟药研究新进展" *

Also Published As

Publication number Publication date
WO1999025351A1 (en) 1999-05-27
AU1222799A (en) 1999-06-07
PE134499A1 (en) 2000-01-23
ZA9810472B (en) 1999-05-21
CO4980890A1 (en) 2000-11-27
CN1191113A (en) 1998-08-26

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Applicant after: Jianqiao Medicine Science & Technology Import & Export Co. Ltd.

Applicant before: Jianqiao Sci. & Tech. Dev. Co., Ltd., Guangzhou City

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Free format text: CORRECT: APPLICANT; FROM: JIANQIAO SCI. + TECH. DEV. CO., LTD., GUANGZHOU CITY TO: JIANQIAO MEDICALTECHNOLOGY IMPORT + EXPORT CO., LTD., GUANGZHOU CITY

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Address after: Yubei Jiangbei District Three Village of Chongqing City No. 30 red Ding International Garden Block A room 1908 zip code: 400020

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Address before: Guangdong Province, Guangzhou City Guanghua Road 11 No. 21 Xiangkang trade building room 804 zip code: 510400

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Termination date: 20131118