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1. 发明授权

US4636569A Pharmaceutical compositions containing compounds with a flavanone skeleton, process for the preparation of the said compound and novel compounds obtained 失效
标题翻译：含有具有黄酮酮骨架的化合物的药物组合物，所述化合物的制备方法和获得的新化合物
公开(公告)号：US4636569A
公开(公告)日：1987-01-13
申请号：US587684
申请日：1984-03-06
申请人： Ezio Bombardelli , Bruno Gabetta , Maria J. Magistretti
发明人： Ezio Bombardelli , Bruno Gabetta , Maria J. Magistretti
IPC分类号： A61K31/35 , A61K31/352 , A61P1/16 , A61P3/06 , A61P11/10 , C07D311/32 , C07D311/04
CPC分类号： C07D311/32
摘要： Compounds with a flavanone skeleton having the formula I ##STR1## in which R.sub.1 and R.sub.2, which may be the same or different, represent hydrogen, hydroxyl, methoxyl, thiomethyl, amino or substituted amino, are endowed with expectorant, mucolytic, mucopoietic, choleretic and hypolipaemia-producing activity.
摘要翻译：具有式I的黄酮酮骨架的化合物（I）其中可以相同或不同的R 1和R 2表示氢，羟基，甲氧基，硫代甲基，氨基或取代的氨基，赋予祛痰剂，粘液溶解，造血，胆汁淤血和降血脂产生活性。

2. 发明授权

US4925871A Therapeutic use of proanthocyanidine A2 for treatment of vascular system 失效
标题翻译：原花青素A2治疗血管系统的治疗用途
公开(公告)号：US4925871A
公开(公告)日：1990-05-15
申请号：US356896
申请日：1989-05-25
申请人： Bruno Gabetta , Maria J. Magistretti
发明人： Bruno Gabetta , Maria J. Magistretti
IPC分类号： A61K31/35 , A61P1/04 , A61P3/06 , A61P9/14 , A61P43/00 , C07D493/18
CPC分类号： C07D493/18 , A61K31/35 , A61K36/77 , A61K9/4858 , A61K2236/00 , A61K9/0014 , A61K9/0019 , A61K9/0056 , Y10S514/926 , Y10S514/927
摘要： There is described a process for preparing proanthocyanidine A2 by extraction from cortex or fruits of Aesculus hippocastanum and related species and its activity for stimulating healing processes, e.g. healing wounds and injuries of various origins, gastric and duodenal ulcers for modifying conditions of impaired capillary permeability and resistance and for obtaining an anti-lipid peroxidation effect.There are also described pharmaceutical formulations suitable for use by topical and systemic routes.

3. 发明授权

US4925870A Therapeutic use of proanthocyanidine A2 as a cytoprotective agent 失效
标题翻译：原花青素A2作为细胞保护剂的治疗用途
公开(公告)号：US4925870A
公开(公告)日：1990-05-15
申请号：US356895
申请日：1989-05-25
申请人： Bruno Gabetta , Maria J. Magistretti , Philippe Dostert
发明人： Bruno Gabetta , Maria J. Magistretti , Philippe Dostert
IPC分类号： A61K31/35 , A61P1/04 , A61P3/06 , A61P9/14 , A61P43/00 , C07D493/18
CPC分类号： C07D493/18 , A61K31/35 , A61K36/77 , A61K9/4858 , A61K2236/00 , A61K9/0014 , A61K9/0019 , A61K9/0056 , Y10S514/926 , Y10S514/927
摘要： There is described a process for preparing proanthocyanidine A2 by extraction from cortex or fruits of Aesculus hippocastanum and related species and its activity for stimulating healing processes, e.g. healing wounds and injuries of various origins, gastric and duodenal ulcers for modifying conditions of impaired capillary permeability and resistance and for obtaining an anti-lipid peroxidation effect.There are also described pharmaceutical formulations suitable for use by topical and systemic routes.

4. 发明授权

US4863956A Process for obtaining proanthocyanidine A2, pharmaceutical compositions and their therapeutic use 失效
标题翻译：获得原花青素A2，药物组合物及其治疗用途的方法
公开(公告)号：US4863956A
公开(公告)日：1989-09-05
申请号：US886790
申请日：1986-07-18
申请人： Bruno Gabetta , Maria J. Magistretti , Philippe Dostert
发明人： Bruno Gabetta , Maria J. Magistretti , Philippe Dostert
IPC分类号： A61K31/35 , A61P1/04 , A61P3/06 , A61P9/14 , A61P43/00 , C07D493/18
CPC分类号： C07D493/18 , A61K31/35 , A61K36/77 , A61K9/4858 , A61K2236/00 , A61K9/0014 , A61K9/0019 , A61K9/0056 , Y10S514/926 , Y10S514/927
摘要： There is described a process for preparing proanthocyanidine A2 by extraction from cortex or fruits of Aesculus hippocastanum and related species and its activity for stimulating healing processes, e.g. healing wounds and injuries of various origins, gastric and duodenal ulcers for modifying conditions of impaired capillary permeability and resistance and for obtaining an anti-lipid peroxidation effect.There are also described pharmaceutical formulations suitable for use by topical and systemic routes.
摘要翻译：描述了通过从眉毛和相关物种的皮质或果实中提取原花青素A2的方法及其刺激愈合过程的活性，例如，治愈各种原因的伤口和伤口，胃和十二指肠溃疡，用于修饰毛细血管通透性和抗性受损的病症，并获得抗脂质过氧化作用。还描述了适用于局部和全身途径的药物制剂。

5. 发明授权

US5196449A Methods and pharmaceutical compositions for the treatment of ophthalmic diseases 失效
标题翻译：用于治疗眼底疾病的方法和药物组合物
公开(公告)号：US5196449A
公开(公告)日：1993-03-23
申请号：US557558
申请日：1990-06-24
申请人： Maria J. Magistretti , Marisa Conti , Giorgio Pifferi
发明人： Maria J. Magistretti , Marisa Conti , Giorgio Pifferi
IPC分类号： C07D311/62 , A61K31/00 , A61K31/35 , A61K31/352 , A61K31/353 , A61P9/00 , A61P9/14 , A61P27/00 , A61P27/02
CPC分类号： A61K31/35 , Y10S514/912
摘要： The anthocyanidins pelargonidin and delphidin, have been found to possess novel and unexpected activity in the ophthalmic field, specifically that they are active in reducing the permeability of ciliary body vessels. According to one aspect of the present invention there is provided a method of reducing the hyperpermeability of the ciliary body ocular vessels in a subject which comprises administering to the subject an effective dose of pelargonidin or delphidin. The invention further provides the use of pelargonidin or delphidin in the manufacture of pharmaceutical compositions for carrying out the method of treatment referred to above.

6. 发明授权

US4275071A Imidazole derivatives 失效
标题翻译：咪唑衍生物
公开(公告)号：US4275071A
公开(公告)日：1981-06-23
申请号：US56290
申请日：1979-07-10
申请人： Dante Nardi , Alberto Tajano , Maria J. Magistretti
发明人： Dante Nardi , Alberto Tajano , Maria J. Magistretti
IPC分类号： C07D233/54 , A61K31/415 , A61K31/4164 , A61P25/08 , C07C45/46 , C07C49/80 , C07C49/813 , C07D233/58 , C07D233/60 , C07D521/00
CPC分类号： E04F11/1851 , C07C45/46 , C07C49/80 , C07C49/813 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Imidazole derivatives of the formula I and pharmaceutically acceptable acid addition salts thereof are provided: ##STR1## In the formula, R.sub.4 1- or 2-naphthyl, optionally substituted with Cl, Br, or I; 1,2,3,4-tetrahydro-6-naphthyl; 3-duryl, optionally 6-substituted by Cl, Br, I, NO.sub.2, CH.sub.3 or benzyl; mesityl, phenyl 2-, 3- or 4-substituted by OH, NH.sub.2, NO.sub.2, CH.sub.3 CONH, phenyl, phenoxy, cyclohexyl, phenylthio, benzylthio, C.sub.1 -C.sub.6 alkyl or C.sub.1 C.sub.6 alkylthio; 4-bibenzylyl; 3,4-dihydroxyphenyl,n=0, 1 or 2 and(a) R=H, alkyl having 1 to 6 carbon atoms or phenyl R.sub.1 =H, alkyl having 1 to 6 carbon atoms or phenyl one of R.sub.2 and R.sub.3 =H the other of R.sub.2 and R.sub.3 =H, OH, benzoyloxy, C.sub.2 -C.sub.7 alkanoyloxy, N-(C.sub.1 -C.sub.6 alkyl)-carbamoyloxy, N,N-[di-(C.sub.1 C.sub.6)alkyl]-carbamoyloxy, but if R.sub.2 =R.sub.3 =H then R=R.sub.1 =H, or(b) R=H, C.sub.1 -C.sub.6 alkyl, phenyl R.sub.1 =H, C.sub.1 -C.sub.6 alkyl, phenyl R.sub.2 +R.sub.3 =O, or ##STR2## The compounds of formula I are anti-convulsivants.
摘要翻译：提供了式I的咪唑衍生物及其药学上可接受的酸加成盐：式中，任选被Cl，Br或I取代的R 4 1-或2-萘基; 1,2,3,4-四氢-6-萘基; 任选地被Cl，Br，I，NO 2，CH 3或苄基取代的3-硬脂基; 甲基苯基，2-，3-或4-被OH，NH2，NO2，CH3CONH，苯基，苯氧基，环己基，苯硫基，苄硫基，C1-C6烷基或C1C6烷硫基取代的苯基; 4-联苯基; 3,4-二羟基苯基，n = 0,1或2和（a）R = H，具有1至6个碳原子的烷基或苯基R 1 = H，具有1至6个碳原子的烷基或苯基，R 2和R 3 = H R2和R3中的另一个为H，OH，苯甲酰氧基，C2-C7烷酰氧基，N-（C1-C6烷基） - 氨基甲酰氧基，N，N- [二（C1C6）烷基] - 氨基甲酰氧基，但如果R2 = R3 = 然后R = R 1 = H，或（b）R = H，C 1 -C 6烷基，苯基R 1 = H，C 1 -C 6烷基，苯基R 2 + R 3 = O或（c）是抗惊厥药。

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