CN1041695A - 具有抗病毒和抗肿瘤作用的用于兽医和人类医学的药品及包括其使用的药物形式的制备方法 - Google Patents
具有抗病毒和抗肿瘤作用的用于兽医和人类医学的药品及包括其使用的药物形式的制备方法 Download PDFInfo
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Abstract
本文叙述了用于人类和兽医使用的药物的制备方法，该药物具有作为抗病毒和抗肿瘤化合物的治疗活性。
Description
本发明涉及一种具有抗病毒和抗肿瘤作用的用于兽医和人类医学的药品的制备方法。
按本发明的制剂是2，6-二氨基-3-苯基-偶氮-吡啶无机盐（参见式Ⅰ）。
该盐的碱基其本身作为纺织工业中的一种偶氮染料化合物是已知的，而有关它作为预防和治疗的化合物对家禽和哺乳动物感染作用的抗菌特性人们已进行了研究，但是仅仅是与氯霉素和土霉素一起研究的。而当前对这些化合物的其它作用仅仅是推测而已。现在本发明提出了该原有化合物的硼酸盐、碳酸盐、硫酸盐和盐酸盐等无机盐。
Guépin，Jason，Kruimel和Lorenzen在“Archiv für Hygiene和Bakteriologie（1961），nr.145，88页a.f.”中提出该碱基的盐酸盐对于病毒甚至对于同DNA和RNA有相似结构的病毒均具有化学治疗和预防作用。然而，文章中仅仅说明抗流行性感冒的结果。
Guépin进行了大量的实验，但未曾在这个方面公开其结果。
在Guépin去世之后，本申请人继续进行这些研究，他们用代谢物的微生物学和化学治疗研究扩大了该实验的范围。结果表明在身体中施用该药品后形成的碱的代谢物具有相当广的效用，尤其在温血动物中结果形成抗击病毒破坏的成功。从药理和分析结果证明准许该药对人类使用，将会产生同样良好的结果。体外实验后证实其与体内的结果相同。此外，用动物实验意外地表明其还显现了抗病毒引发的肉瘤的显著抗肿瘤作用，这从早期阶段的血原性转移可以了解。
在尿和粪便中测得的代谢物是由偶氮键还原裂解的产物，特别是在下列具有按式Ⅱ一般结构的N-杂环分子，如：胸苷，嘧啶和叠氮胸苷。在所述式中R1和R2分别表示糖，氨基和/或嘌呤基。
所述的N-杂环化合物被认为是抗不同病毒结构受体的活性成分。
所述化合物的另一些代谢物是N-乙酰氨基苯酚，对氨基苯酚和苯胺，推测它们有协同作用，但还未证明。
正如Ashwell在“Treuds of Biochemical Science”，（1977），nr.2，76页a.f.一文中叙述的那样，因线粒体细胞壁是重要的信息载体，并由于大部分危险的病毒化合物带有受体，而它们几乎只能通过体内形成的化合物即主要通过代谢得到的产物来抑制，所以曾想到若采用适当形式和浓度的2.6-二氨基-3-苯基-偶氮吡啶碱认为对于抑制人类和动物的病毒感染是极其重要的，同时，认为在对付HIV-Ⅱ-病毒，爱滋病的病源和抗病毒性肝炎（传染性和血清性肝炎）的斗争中实际应用对抗早期病毒肿瘤和其转移可能是有利的。
由于本发明的化合物仅有极为温和的肝脏毒性，因此它在人类的药物治疗中可以低浓度使用于轻度细菌性发炎，临床应用于病毒引发的肉瘤的病例已初见成效。最近这些病例已显示出其病症有了相当大的改善，该化合物必定有助于所述代谢物的作用或至少有助于上述三种基团的化合物之一的作用。
考虑到本发明化合物先前已知的抗菌作用，其还可以归为广谱药品，因此它可以规定为治疗极难诊断的疾病如目前在热带地区蔓延的疾病。
按本发明的具有抗菌的、抗病毒的抗肿瘤作用的用于曾医和人类治疗的药物制剂，其特征在于用于口服治疗时，2，6-二氨基-3-苯基偶氮-吡啶盐是以0.5-10.0%（重量/重要%）溶于水的浓度给药。
合适的盐是盐酸盐，硼酸盐和碳酸盐。
用于肌肉注射的是采用制备成一定浓度并灌装在50毫升安瓿中的2，6-二氨基-3-苯基-偶氮吡啶硼酸盐的有机溶剂或水溶液。
用于局部治疗是制备成5.0%（重量/重量%）的2，6-二氨基-3-苯基-偶氮吡啶盐的凡士林（石油凝胶）软膏。
该制剂对于哺乳动物和家禽是每天以每公斤重0.5-10mg之间给药。
治疗能连续进行2至6天无需中断。在诊查这种药物的效能时显示这种药物对患有由病毒引起疾病的或明显地将发生这种疾病的动物有显著的良好结果。还可以观察到，该制剂对于有肉瘤倾向的雄性Wistar白鼠给以预防的处理和治疗有良好结果。
牛和猪的病毒性脚和嘴的疾病以及鸡的Newcastle疾病到目前为止还认为是不能治愈的，但是现在应用按本发明的化合物是能治疗这些疾病的。
药用的本发明化合物的性质如下：
表Ⅰ：
形状：红色无味的结晶态粉末
熔点范围：235-239℃
溶解度：
乙醇： 3.5mg/ml
氯仿： 0.4mg/ml
乙醚： 0.2mg/ml
2-丙醇 2.1mg/ml
甲醇 2.7mg/ml
石油醚 0.1mg/ml
水 3.2mg/ml
本发明化合物的制备可以通过吩嗪与吡啶稠合或通过氯化苯基重氮物与α-α′-二氨基吡啶在水浴中回流冷却下偶合，再将得到的产物溶于硼酸、乙酸或稀盐酸。该化合物通过UV-光谱可以鉴定：取0.5mg化合物在100ml酸化乙醇中的溶液在210-450nm范围测得两个峰值238-240nm（ε＝2.2×104）及390-392nm（ε＝2.4×104）和三个显示较弱的峰220nm，272nm和296nm。
盐酸盐的分子式为C11H11N5·HCl
分子量为249.7
在Martindales Extra Pharmacopoeia（Pharmaclutical press，london），26，Ed.，1972，251页中曾报导除了超过剂量使用之外，该化合物不发生溶血性贫血，并应用于抗尿道和前列腺细菌性炎症。当以每天按每公斤高至20mg的剂量给患有细菌性感染的猫施用该化合物时不会发生贫血。
在Journal of the American Veterinary Medical Association，Vol.169（1976），no.3，327-331页中曾报导了该化合物在抗细菌感染期中的毒理学资料，但是它的抗病毒和抗肿瘤活性还未同时认可，因此尚未在此文中作公开报导。
下列表Ⅱ中仅重述了在动物治疗中抗病毒性疾病的结果：
表Ⅱ
疾病 治疗 治愈 恢复% 预防 有效%
A.猪
肺炎 2300 2270 99 1563 98
脚和嘴疾病 1000 958 96 124 100
猪疫病 355 345 98 50 100
猪痘泡 100 100 100 45 100
肠炎 974 974 100 4000 98
B.牛
脚和嘴疾病 3200 3072 96 40 96
C.狗
Carre狗病症 58 58 100 … …
家犬肝炎感染 17 17 100 … …
Kennels咳嗽 16 16 100 … …
鼻炎 10 10 100 … …
D.猫
猫疾病 140 127 92 … …
E.家禽
乌疫 205 200 100 50 100
Bleu冠毛病 200 200 100 … …
鸡痘孢 13 13 100 … …
肠炎 100 100 100
感冒 4800 4300 88 1200 100
C.R.D. 17000 16000 94 2470 100
疾病 治疗 治愈 恢复% 预防 有效%
新城病 20 20 100 … …
Marek病 673 665 99 … …
F.啮齿类动物（兔）
感冒 50 50 100 … …
C.马
流行性感冒 2 2 100 … …
Claims (6)
1、一种具有抗病毒和抗肿瘤作用的用于兽医和人类医学的药品的制备方法，其特征在于将无机盐形式的2，6-二氨基-3-苯基-偶氮吡啶溶于有机溶剂和水配制成0.5-10.0%(重量/重量)的浓度。
2、一种具有抗病毒和抗肿瘤作用的用于兽医和人类医学的药品的制备方法，其特征在于当2，6-二氨基-3-苯基-偶氮吡啶于肠胃外使用时，将其无机盐于有机溶剂和水中制成5.0%（重量/重量）的浓度装于无菌小瓶中。
3、一种具有抗病毒和抗肿瘤作用的用于兽医和人类医学的药品的制备方法，其特征在于当2，6-二氨基-3-苯基-偶氮吡啶于口服使用时，将其无机盐与乳糖、直链淀粉混合制成浓度为2.0-10.0%（重量/重量）的混合物再转制成片剂、胶囊和/或糖浆。
4、一种具有抗病毒和抗肿瘤作用的用于兽医和人类医学的药品的制备方法，其特征在于当2，6-二氨基-3-苯基-偶氮吡啶于局部使用时，将其无机盐与凡士林混合制成2.0-10.0%（重量/重量）浓度的软膏。
5、按权利要求1-5之任一项所述的方法，其特征在于作为无机硼酸盐、硫酸盐、碳酸盐和/或盐酸盐而进行制备的。
6、按权利要求1-4之任一项所述方法制备的药剂。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| NL8702446A NL8702446A (nl) | 1987-10-14 | 1987-10-14 | Werkwijze ter bereiding van een veterinair- en humaanmedisch preparaat met antivirale en antitumorale werking, alsmede het in farmaceutisch toepasbare vorm gebrachte preparaat. |
| NL8702446 | 1987-10-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1041695A true CN1041695A (zh) | 1990-05-02 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN88107207A Pending CN1041695A (zh) | 1987-10-14 | 1988-10-14 | 具有抗病毒和抗肿瘤作用的用于兽医和人类医学的药品及包括其使用的药物形式的制备方法 |
Country Status (15)
| Country | Link |
|---|---|
| EP (1) | EP0312132B1 (zh) |
| JP (1) | JPH01132525A (zh) |
| CN (1) | CN1041695A (zh) |
| AT (1) | ATE84418T1 (zh) |
| AU (1) | AU619767B2 (zh) |
| CA (1) | CA1338489C (zh) |
| DE (1) | DE3877499T2 (zh) |
| DK (1) | DK574588A (zh) |
| ES (1) | ES2042715T3 (zh) |
| GR (1) | GR3009556T3 (zh) |
| IE (1) | IE60506B1 (zh) |
| IL (1) | IL87867A (zh) |
| NL (1) | NL8702446A (zh) |
| NZ (1) | NZ226360A (zh) |
| ZA (1) | ZA887181B (zh) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6596777B1 (en) | 1997-05-29 | 2003-07-22 | Mcneil-Ppc, Inc. | Moisture containing compositions that are spreadable onto and adherable to biomembranes |
| RU2354384C1 (ru) * | 2007-12-28 | 2009-05-10 | Михаил Владимирович Кутушов | Применение органических красителей в качестве средства для лечения онкологических заболеваний |
-
1987
- 1987-10-14 NL NL8702446A patent/NL8702446A/nl not_active Application Discontinuation
-
1988
- 1988-08-24 AT AT88201797T patent/ATE84418T1/de not_active IP Right Cessation
- 1988-08-24 DE DE8888201797T patent/DE3877499T2/de not_active Expired - Fee Related
- 1988-08-24 ES ES88201797T patent/ES2042715T3/es not_active Expired - Lifetime
- 1988-08-24 EP EP19880201797 patent/EP0312132B1/en not_active Expired - Lifetime
- 1988-09-26 ZA ZA887181A patent/ZA887181B/xx unknown
- 1988-09-28 IL IL87867A patent/IL87867A/xx not_active IP Right Cessation
- 1988-09-28 NZ NZ226360A patent/NZ226360A/xx unknown
- 1988-09-30 CA CA000579070A patent/CA1338489C/en not_active Expired - Fee Related
- 1988-10-12 AU AU23663/88A patent/AU619767B2/en not_active Ceased
- 1988-10-14 JP JP63257448A patent/JPH01132525A/ja active Pending
- 1988-10-14 CN CN88107207A patent/CN1041695A/zh active Pending
- 1988-10-14 DK DK574588A patent/DK574588A/da not_active Application Discontinuation
- 1988-10-14 IE IE311688A patent/IE60506B1/en not_active IP Right Cessation
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1993
- 1993-03-29 GR GR930400677T patent/GR3009556T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2366388A (en) | 1989-06-01 |
| EP0312132A3 (en) | 1990-04-25 |
| DE3877499D1 (de) | 1993-02-25 |
| ZA887181B (en) | 1989-05-30 |
| EP0312132A2 (en) | 1989-04-19 |
| IE883116L (en) | 1989-04-14 |
| IE60506B1 (en) | 1994-07-27 |
| EP0312132B1 (en) | 1993-01-13 |
| IL87867A0 (en) | 1989-03-31 |
| DK574588D0 (da) | 1988-10-14 |
| NZ226360A (en) | 1990-08-28 |
| JPH01132525A (ja) | 1989-05-25 |
| NL8702446A (nl) | 1989-05-01 |
| ES2042715T3 (es) | 1993-12-16 |
| AU619767B2 (en) | 1992-02-06 |
| CA1338489C (en) | 1996-07-30 |
| GR3009556T3 (zh) | 1994-02-28 |
| DE3877499T2 (de) | 1993-06-03 |
| DK574588A (da) | 1989-04-15 |
| IL87867A (en) | 1992-11-15 |
| ATE84418T1 (de) | 1993-01-15 |
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