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1. 发明公开

EP0198605A1 Prophylaxis of pharmacotherapy of liver disorders 失效
标题翻译： Prohibaxe der Pharmakotherapie vonLeberentzündungen。
公开(公告)号：EP0198605A1
公开(公告)日：1986-10-22
申请号：EP86301960.0
申请日：1986-03-18
申请人： TEIJIN LIMITED
发明人： Yamamoto, Itaru , Koyama, Yasushi , Komoriya, Keiji , Hayami, Masaaki , Okazaki, Funeki
IPC分类号： C07D277/22 , A61K31/425
CPC分类号： C07D277/22
摘要： Methincyanine compounds having the following general formula (I) are effective for the prophylaxis or pharmacotherapy of liver disorders or hepatic diseases of warm-blooded animals.
wherein R l and R 2 may be the same or different and represent an unsubsituted or substituted alkyl group, R 3 , R 4 , R 5 , and R 6 independently represent a hydrogen atom or an alkyl group, and X ⊖ represents an anion.
摘要翻译：具有以下通式（I）的甲硫氨酸化合物对于预防或药物治疗温血动物的肝脏疾病或肝脏疾病是有效的。其中R 1和R 2可以相同或不同，表示未取代或取代的烷基，R 3，R 4，R 5和R 6独立地表示氢原子或烷基，X“（ - ）”表示阴离子。

2. 发明公开

EP0049902A3 Novel thiazolo(3,2-a)pyrimidines, derivatives thereof, processes for production thereof, and pharmaceutical use thereof 失效
标题翻译：新型三唑（3,2-A）吡啶类，其衍生物，其生产方法及其药物用途
公开(公告)号：EP0049902A3
公开(公告)日：1982-09-01
申请号：EP81108283
申请日：1981-10-13
申请人： TEIJIN LIMITED
发明人： Okamura, Noriaki , Toru, Takeshi , Oba, Takeo , Tanaka, Toshio , Watanabe, Kenzo , Bannai, Kiyoshi , Kurozumi, Seizi , Naruchi, Tatsuyuki , Komoriya, Keiji
IPC分类号： C07D513/04 , A61K31/505 , C07C101/20 , C07D277/00 , C07D239/00
CPC分类号： C07D513/04
摘要： A compound selected from thiazolo(3,2-a)pyrimidines or their enolate derivatives represented by the following general formula
wherein R 1 and R 2 are identical or different, and each represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 3 to 10 carbon atoms, a substituted or unsubstituted phenyl group, a substituted or unsubstituted cycloaliphatic group having 3 to 8 carbon atoms, a substituted or unsubstituted phenylalkyl group or a substituted or unsubstituted acyl group having 2 to 7 carbon atoms, provided that R and R 2 are not simultaneously hydrogen atoms or substituted or unsubstituted acyl groups having 2 to 7 carbon atoms; and R and R 2 , when taken together, may form, with the nitrogen atom to which they are bonded, a 5- or 6-membered ring which may further contain one or more hetero atoms; and acid addition salts of these compounds. The thiazolo(3,2-a)pyrimidines may be prepared by a process comprising (a) reacting a malonic acid derivative of the following general formula
wherein R' and R 2 are as defined with regard to formula (I), and R 4 and R 5 are identical or different and each represents an alkyl group having 1 to 6 carbon atoms, with 2-aminothiazoline under heat, if desired in the presence of an inert organic solvent, to induce cyclocondensation, or
(b) performing said condensation reaction in the presence of an alkali metal alkoxide, if desired in the presence of an inert organic solvent, and neutralizing the resulting enolate with an acid: and if desired, reacting the reaction product of (a) or (b) with an acid. The present invention provides also several processes for preparing enolate derivatives thereof. The thiazolo(3,2-a)pyrimidines, their enolate derivatives and acid addition compounds thereof are useful for regulating the immune function of a warm-blooded animal.
摘要翻译：选自噻唑并[3,2-a]嘧啶或其以下通式（I）表示的烯醇化物衍生物的化合物，其中R 1和R 2相同或不同，并且各自表示氢原子，具有1个碳原子数为3〜10的烯基，取代或未取代的苯基，取代或未取代的碳原子数为3〜8的脂环族基，取代或未取代的苯基烷基或取代或未取代的2位的酰基其中R 1和R 2不是同时为氢原子或具有2至7个碳原子的取代或未取代的酰基; 当R 1和R 2一起时可以与它们所键合的氮原子形成可以进一步含有一个或多个杂原子的5-或6-元环; 和这些化合物的酸加成盐。噻唑并[3,2-a]嘧啶可以通过以下方法制备，该方法包括：（a）使下列通式（II）的丙二酸衍生物（其中R 1和R 2如式（I）所定义），和R4和R5相同或不同，并且各自表示具有1至6个碳原子的烷基，如果需要，在惰性有机溶剂的存在下，加热下加入2-氨基噻唑啉，以诱导环化缩合，或（b）进行所述如果需要，在惰性有机溶剂的存在下，在碱金属醇盐的存在下进行缩合反应，并用酸中和所得的烯醇化物; 并且如果需要，使（a）或（b）的反应产物与酸反应。本发明还提供了几种制备其烯醇化物衍生物的方法。噻唑并[3,2-a]嘧啶，它们的烯醇化物衍生物及其酸加成化合物可用于调节温血动物的免疫功能。

3. 发明公开

EP0049902A2 Novel thiazolo(3,2-a)pyrimidines, derivatives thereof, processes for production thereof, and pharmaceutical use thereof 失效
标题翻译：噻唑（3,2-a）嘧啶，Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung。
公开(公告)号：EP0049902A2
公开(公告)日：1982-04-21
申请号：EP81108283.3
申请日：1981-10-13
申请人： TEIJIN LIMITED
发明人： Okamura, Noriaki , Toru, Takeshi , Oba, Takeo , Tanaka, Toshio , Watanabe, Kenzo , Bannai, Kiyoshi , Kurozumi, Seizi , Naruchi, Tatsuyuki , Komoriya, Keiji
IPC分类号： C07D513/04 , A61K31/505
CPC分类号： C07D513/04
摘要： A compound selected from thiazolo(3,2-a)pyrimidines or their enolate derivatives represented by the following general formula
wherein R 1 and R 2 are identical or different, and each represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 3 to 10 carbon atoms, a substituted or unsubstituted phenyl group, a substituted or unsubstituted cycloaliphatic group having 3 to 8 carbon atoms, a substituted or unsubstituted phenylalkyl group or a substituted or unsubstituted acyl group having 2 to 7 carbon atoms, provided that R and R 2 are not simultaneously hydrogen atoms or substituted or unsubstituted acyl groups having 2 to 7 carbon atoms; and R and R 2 , when taken together, may form, with the nitrogen atom to which they are bonded, a 5- or 6-membered ring which may further contain one or more hetero atoms; and acid addition salts of these compounds.
The thiazolo(3,2-a)pyrimidines may be prepared by a process comprising (a) reacting a malonic acid derivative of the following general formula

wherein R' and R 2 are as defined with regard to formula (I), and R 4 and R 5 are identical or different and each represents an alkyl group having 1 to 6 carbon atoms, with 2-aminothiazoline under heat, if desired in the presence of an inert organic solvent, to induce cyclocondensation, or

(b) performing said condensation reaction in the presence of an alkali metal alkoxide, if desired in the presence of an inert organic solvent, and neutralizing the resulting enolate with an acid: and if desired, reacting the reaction product of (a) or
(b) with an acid.

The present invention provides also several processes for preparing enolate derivatives thereof.
The thiazolo(3,2-a)pyrimidines, their enolate derivatives and acid addition compounds thereof are useful for regulating the immune function of a warm-blooded animal.
摘要翻译：选自噻唑并[3,2-a]嘧啶或其以下通式（I）表示的烯醇化物衍生物的化合物，其中R 1和R 2相同或不同，并且各自表示氢原子，具有1个碳原子数为3〜10的烯基，取代或未取代的苯基，取代或未取代的碳原子数为3〜8的脂环族基，取代或未取代的苯基烷基或取代或未取代的2位的酰基其中R 1和R 2不是同时为氢原子或具有2至7个碳原子的取代或未取代的酰基; 当R 1和R 2一起时可以与它们所键合的氮原子形成可以进一步含有一个或多个杂原子的5-或6-元环; 和这些化合物的酸加成盐。噻唑并[3,2-a]嘧啶可以通过以下方法制备，该方法包括：（a）使下列通式（II）的丙二酸衍生物（其中R 1和R 2如式（I）所定义），和R4和R5相同或不同，并且各自表示具有1至6个碳原子的烷基，如果需要，在惰性有机溶剂的存在下，加热下加入2-氨基噻唑啉，以诱导环化缩合，或（b）进行所述如果需要，在惰性有机溶剂的存在下，在碱金属醇盐的存在下进行缩合反应，并用酸中和所得的烯醇化物; 并且如果需要，使（a）或（b）的反应产物与酸反应。本发明还提供了几种制备其烯醇化物衍生物的方法。噻唑并[3,2-a]嘧啶，它们的烯醇化物衍生物及其酸加成化合物可用于调节温血动物的免疫功能。

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