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1. 发明授权

US4554280A Pyridyl methyl thio or sulfinyl indeno(5,6-d)imidazoles 失效
标题翻译：吡啶基甲基硫代或亚磺酰基茚并（5,6-d）咪唑
公开(公告)号：US4554280A
公开(公告)日：1985-11-19
申请号：US560698
申请日：1983-12-12
申请人： Anna Krasso , Henri Ramuz
发明人： Anna Krasso , Henri Ramuz
IPC分类号： C07D401/12 , A61K31/415 , A61K31/44 , A61K31/4427 , A61P1/04 , C07C37/20 , C07C45/00 , C07C45/68 , C07C205/06 , C07D209/08 , C07D231/10 , C07D235/02 , C07D235/28 , C07D317/46 , C07D319/08 , C07D401/14 , C07D487/04 , C07D491/04 , C07D491/056
CPC分类号： C07D235/02 , C07C205/06 , C07C205/45 , C07C37/50 , C07C45/00 , C07C45/68 , C07D209/08 , C07D231/10 , C07D317/46 , C07D319/08 , C07D487/04 , C07D491/04 , C07C2102/08 , Y10S514/926 , Y10S514/927
摘要： Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 or 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.
摘要翻译：其中R 1为任选被低级烷基或低级烷氧基取代的2-吡啶基，n为0或1的整数，R 2为氢或低级烷基，R 3和R 4独立地为氢或低级烷基，A是下式的基团：其中m是整数2或3，R5，R6，R7和R8独立地是氢或低级烷基，R9是氢，R10 如果A为式-CH = CH-CH = CH-或 - （CH 2）4 - 的基团，则R 3和R 4中的至少一个为低级烷基，，及其药学上可接受的酸加成盐。式I的化合物抑制胃酸分泌并防止胃溃疡的形成。

2. 发明授权

US4950677A Benzimidazole derivative compounds and method of making 失效
标题翻译：苯并咪唑衍生物及其制备方法
公开(公告)号：US4950677A
公开(公告)日：1990-08-21
申请号：US222593
申请日：1988-07-21
申请人： Albert Fischli , Anna Krasso , Andre Szente
发明人： Albert Fischli , Anna Krasso , Andre Szente
IPC分类号： C07D401/04 , C07D471/04 , C07D487/04 , C07D491/044 , C07D495/04
CPC分类号： C07D401/04
摘要： A compound of the formula ##STR1## wherein R.sup.1 -R.sup.19 are as described in the specification. The present invention is concerned with benzimidazole derivatives, particularly benzimidazole-2-yl pyridinium compounds of formula I which are pharmaceutically useful in treating or preventing gastric and duodenal ulcers. The invention includes the compounds I, pharmaceutical compositions containing such compounds and the use of such compounds in therapeutic treatment or prevention of gastric and duodenal ulcers.
摘要翻译：其中R1-R19如说明书中所述的式（Ⅰ）化合物。本发明涉及可用于治疗或预防胃和十二指肠溃疡的苯并咪唑衍生物，特别是式I的苯并咪唑-2-基吡啶鎓化合物。本发明包括化合物I，含有这些化合物的药物组合物以及这些化合物在治疗性或预防胃和十二指肠溃疡中的用途。

3. 发明授权

US4766133A (Bezimidazol-2-yl)-pyridinium compounds 失效
公开(公告)号：US4766133A
公开(公告)日：1988-08-23
申请号：US893856
申请日：1986-08-06
申请人： Albert Fischli , Anna Krasso , Andre Szente
发明人： Albert Fischli , Anna Krasso , Andre Szente
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D417/14 , C07D473/38 , C07D491/04 , A61K31/44
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D417/14 , C07D473/38 , C07D491/04
摘要： (Benzimidazol-2-yl)-pyridinium compounds of the formula ##STR1## wherein A is --SR.sup.9, --SO.sub.3.sup.- or --S--SO.sub.3.sup.- ; R.sup.1 and R.sup.3 each is hydrogen or (C.sub.1 -C.sub.7)-alkyl; R.sup.2 is hydrogen, (C.sub.1 -C.sub.7)-alkyl, (C.sub.1 -C.sub.7)-alkoxy or a negatively charged oxygen atom; R.sup.4 is hydrogen or a negative charge; R.sup.5, R.sup.6, R.sup.7 and R.sup.8 each is hydrogen, (C.sub.1 -C.sub.7)-alkyl, aryl, halogen, cyano, nitro, formyl, (C.sub.2 -C.sub.7)-alkanoyl, arylcarbonyl, carboxy, carboxy-(C.sub.1 -C.sub.7)-alkyl, (C.sub.1 -C.sub.7)-alkoxycarbonyl, aryloxycarbonyl, aryl-(C.sub.1 -C.sub.7)-alkoxycarbonyl, (C.sub.1 -C.sub.7)-alkoxycarbonyl-(C.sub.1 -C.sub.7)-alkyl, carbamoyl, mono- or di-(C.sub.1 -C.sub.7)-alkylcarbamoyl, pyrrolidinocarbonyl, piperidinocarbonyl, carbamoyl-(C.sub.1 -C.sub.7)-alkyl, mono- or di-(C.sub.1 -C.sub.7)-alkylcarbamoyl-(C.sub.1 -C.sub.7)-alkyl, pyrrolidinocarbonyl-(C.sub.1 -C.sub.7)-alkyl, piperdinocarbonyl-(C.sub.1 -C.sub.7)-alkyl, hydroxy, (C.sub.1 -C.sub.7)-alkoxy, (C.sub.2 -C.sub.7)-alkanoloxy, aryloxy, arylcarbonyloxy, (C.sub.1 -C.sub.7)-alkoxycarbonyloxy, aryl-(C.sub.1 -C.sub.7)-alkoxycarbonyloxy, aryloxycarbonyloxy, carbamoyloxy, mono- or di-(C.sub.1 -C.sub.7)-alkylcarbamoyloxy, pyrrolidinocarbonyloxy, piperidinocarbonyloxy, hydroxy-(C.sub.1 -C.sub.7)-alkyl, trifluoromethyl, di-(C.sub.1 -C.sub.7)-alkoxymethyl or (C.sub.2 -C.sub.3)-alkylenedioxymethyl or two of these substituents which are adjacent jointly and together with the carbon atoms to which they are attached are a 5-, 6- or 7-membered ring; and R.sup.9 is (C.sub.1 -C.sub.20)-alkyl, (C.sub.3 -C.sub.7)-cycloalkyl, (C.sub.3 -C.sub.7)-alkenylalkyl, (C.sub.3 -C.sub.7)-alkynylalkyl, substituted (C.sub.3 -C.sub.7)- alkenyl-alkyl, aryl, aryl-(C.sub.1 -C.sub.7)-alkyl, hydroxy- (C.sub.2 -C.sub.7)-alkyl, (C.sub.1 -C.sub.7)-alkoxy- (C.sub.2 -C.sub.7)-alkyl, (C.sub.1 -C.sub.7)-alkoxycarbonyl- (C.sub.1 -C.sub.7)-alkyl, carboxy-(C.sub.1 -C.sub.7)-alkyl, di-(C.sub.1 -C.sub.7)-alkoxycarbonyl-(C.sub.2 -C.sub.7)-alkyl, dicarboxy-(C.sub.2 -C.sub.7)-alkyl, carboxy-(C.sub.1 -C.sub.7)-alkylcarbamoyl-(C.sub.1 -C.sub.7)-alkyl, optionally N-substituted amino-(C.sub.2 -C.sub.7)-alkyl, optionally N-substituted amino-carboxy-(C.sub.2 -C.sub.7)-alkyl, optionally N-substituted amino-(C.sub.1 -C.sub.7)-alkoxycarbonyl-(C.sub.2 -C.sub.7)-alkyl, heteroaryl, heteroaryl-(C.sub.1 -C.sub.7)-alkyl or a residue derived from a cysteine-containing oligopeptide by elimination of the SH group;provided that when there is a net single positive charge there is an external anion, or a pharmaceutically acceptable acid addition salt thereof.

4. 发明授权

US4599347A Tetrahydro-naphth (2.3-d) imidazole derivatives 失效
标题翻译：四氢 - 萘（2.3-d）咪唑衍生物
公开(公告)号：US4599347A
公开(公告)日：1986-07-08
申请号：US560699
申请日：1983-12-12
申请人： Anna Krasso , Henri Ramuz
发明人： Anna Krasso , Henri Ramuz
IPC分类号： C07D401/12 , A61K31/415 , A61K31/44 , A61K31/4427 , A61P1/04 , C07C37/20 , C07C45/00 , C07C45/68 , C07C205/06 , C07D209/08 , C07D231/10 , C07D235/02 , C07D235/28 , C07D317/46 , C07D319/08 , C07D401/14 , C07D487/04 , C07D491/04 , C07D491/056
CPC分类号： C07D235/02 , C07C205/06 , C07C205/45 , C07C37/50 , C07C45/00 , C07C45/68 , C07D209/08 , C07D231/10 , C07D317/46 , C07D319/08 , C07D487/04 , C07D491/04 , C07C2102/08 , Y10S514/926 , Y10S514/927
摘要： Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 to 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.
摘要翻译：其中R 1为任选被低级烷基或低级烷氧基取代的2-吡啶基，n为0至1的整数，R 2为氢或低级烷基，R 3和R 4独立地为氢或低级烷基，A是下式的基团：其中m是整数2或3，R5，R6，R7和R8独立地是氢或低级烷基，R9是氢，R10 如果A为式-CH = CH-CH = CH-或 - （CH 2）4 - 的基团，则R 3和R 4中的至少一个为低级烷基，，及其药学上可接受的酸加成盐。式I的化合物抑制胃酸分泌并防止胃溃疡的形成。

5. 发明授权

US4248880A Treatment of gastric ulcers with naphthimidazole derivatives 失效
标题翻译：用萘并噻唑衍生物治疗胃溃疡
公开(公告)号：US4248880A
公开(公告)日：1981-02-03
申请号：US54210
申请日：1979-07-02
申请人： Anna Krasso , Ernst-Peter Krebs
发明人： Anna Krasso , Ernst-Peter Krebs
IPC分类号： C07D417/12 , C07D213/26 , C07D213/30 , C07D235/02 , C07D235/28 , C07D401/12 , C07D403/12 , A61K31/425 , A61K31/415
CPC分类号： C07D213/30 , C07D213/26 , C07D235/02 , Y10S514/925
摘要： Imidazole derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, X and n are as hereinafter set forth,and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of gastric ulcers.
摘要翻译：描述了其中R 1，R 2，R 3，R 4，R 5，X和n如下文所述的式（I）所示的咪唑衍生物及其药学上可接受的酸加成盐。式I化合物可用于治疗胃溃疡。

6. 发明授权

US5959113A Imidazol derivatives 失效
标题翻译：咪唑衍生物作为蛋白激酶抑制剂，特别是egf-r酪氨酸激酶
公开(公告)号：US5959113A
公开(公告)日：1999-09-28
申请号：US860750
申请日：1997-06-12
申请人： Charles Stanford Harmon , Markus Kamber , Anna Krasso , Wolfgang Pirson , Pierre-Charles Wyss
发明人： Charles Stanford Harmon , Markus Kamber , Anna Krasso , Wolfgang Pirson , Pierre-Charles Wyss
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/495 , A61K31/535 , A61P9/10 , A61P35/00 , A61P43/00 , C07D233/64 , C07D401/04 , C07D413/14 , A61K31/47 , C07D403/04
CPC分类号： C07D401/04
摘要： This invention relates to novel imidazole derivatives of formula a ##STR1## and pharmaceutically acceptable salts of these compounds, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5, R.sup.7 and R.sup.8 are as disclosed herein. These compounds are protein kinase inhibitors useful in the treatment of atherosclerosis, psoriasis, alopecia, and tumors.
摘要翻译： PCT No.PCT / EP95 / 04741 Sec。 371日期：1997年6月12日 102（e）日期1997年6月12日PCT 1995年12月1日PCT PCT。公开号WO96 / 18626 日本1996年6月20日本发明涉及式（a）的新型咪唑衍生物和这些化合物的药学上可接受的盐，其中R 1，R 2，R 3，R 5，R 7和R 8如本文所公开。这些化合物是可用于治疗动脉粥样硬化，牛皮癣，脱发和肿瘤的蛋白激酶抑制剂。

7. 发明授权

US4634710A Tricyclic imidazole derivatives 失效
标题翻译：三环咪唑衍生物
公开(公告)号：US4634710A
公开(公告)日：1987-01-06
申请号：US720775
申请日：1985-04-08
申请人： Albert Fischli , Anna Krasso , Henri Ramuz , Andre Szente
发明人： Albert Fischli , Anna Krasso , Henri Ramuz , Andre Szente
IPC分类号： A61K31/4184 , A61K31/44 , A61K31/4427 , A61P1/04 , C07D213/06 , C07D213/127 , C07D213/26 , C07D213/68 , C07D213/89 , C07D317/00 , C07D401/12 , C07D491/04 , C07D491/056 , A61K31/415
CPC分类号： C07D213/06 , C07D213/26 , C07D213/68 , C07D213/89 , C07D401/12 , C07D491/04
摘要： Tricyclic imidazole derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.3 is lower alkyl and the other is hydrogen or lower alkyl, R.sup.2 is lower alkyl, n is the number 0 or 1, A is ##STR2## R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each is lower alkyl and R.sup.8 is hydrogen or lower alkyl, and their acid addition salts are described. These compounds are useful as agents for control or prevention of ulcers and of increased gastric acid secretion.
摘要翻译：式I的三环咪唑衍生物其中R 1和R 3之一是低级烷基，另一个是氢或低级烷基，R 2是低级烷基，n是数字0或1，A是R 4，R 5， R6和R7各自为低级烷基，R8为氢或低级烷基，并描述其酸加成盐。这些化合物可用作控制或预防溃疡和增加胃酸分泌的药剂。

8. 发明授权

US4981861A Tricyclic imidazole derivatives 失效
标题翻译：三环咪唑衍生物
公开(公告)号：US4981861A
公开(公告)日：1991-01-01
申请号：US463879
申请日：1990-01-05
申请人： Albert Fischli , Anna Krasso , Henri Ramuz , Andre Szente
发明人： Albert Fischli , Anna Krasso , Henri Ramuz , Andre Szente
IPC分类号： A61K31/4184 , A61K31/44 , A61K31/4427 , A61P1/04 , C07D213/06 , C07D213/127 , C07D213/26 , C07D213/68 , C07D213/89 , C07D317/00 , C07D401/12 , C07D491/04 , C07D491/056
CPC分类号： C07D213/06 , C07D213/26 , C07D213/68 , C07D213/89 , C07D401/12 , C07D491/04
摘要： Tricyclic imidazole derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.3 is lower alkyl and the other is hydrogen or lower alkyl, R.sup.2 is lower alkyl, n is the number 0 or 1, A is ##STR2## R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each is lower alkyl land R.sup.8 is hydrogen nor lower alkyl,and their acid addition salts are described. These compounds are useful as agents for control or prevention of ulcers and of increaased gastric acid secretion.

9. 发明授权

US4435406A Imidazole derivatives 失效
标题翻译：咪唑衍生物
公开(公告)号：US4435406A
公开(公告)日：1984-03-06
申请号：US290032
申请日：1981-08-05
申请人： Anna Krasso , Henri Ramuz
发明人： Anna Krasso , Henri Ramuz
IPC分类号： C07D401/12 , A61K31/415 , A61K31/44 , A61K31/4427 , A61P1/04 , C07C37/20 , C07C45/00 , C07C45/68 , C07C205/06 , C07D209/08 , C07D231/10 , C07D235/02 , C07D235/28 , C07D317/46 , C07D319/08 , C07D401/14 , C07D487/04 , C07D491/04 , C07D491/056 , C07D491/14
CPC分类号： C07D235/02 , C07C205/06 , C07C205/45 , C07C37/50 , C07C45/00 , C07C45/68 , C07D209/08 , C07D231/10 , C07D317/46 , C07D319/08 , C07D487/04 , C07D491/04 , C07C2102/08 , Y10S514/926 , Y10S514/927
摘要： Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 or 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.
摘要翻译：其中R 1为任选被低级烷基或低级烷氧基取代的2-吡啶基，n为0或1的整数，R 2为氢或低级烷基，R 3和R 4独立地为氢或低级烷基，A是下式的基团：其中m是整数2或3，R5，R6，R7和R8独立地是氢或低级烷基，R9是氢，R10 如果A为式-CH = CH-CH = CH-或 - （CH 2）4 - 的基团，则R 3和R 4中的至少一个为低级烷基，，及其药学上可接受的酸加成盐。式I的化合物抑制胃酸分泌并防止胃溃疡的形成。

10. 发明授权

US4182766A Naphth[2,3-d]imidazoles 失效
标题翻译：萘[2,3-d]咪唑
公开(公告)号：US4182766A
公开(公告)日：1980-01-08
申请号：US941343
申请日：1978-09-11
申请人： Anna Krasso , Ernst-Peter Krebs
发明人： Anna Krasso , Ernst-Peter Krebs
IPC分类号： C07D417/12 , C07D213/26 , C07D213/30 , C07D235/02 , C07D235/28 , C07D401/12 , C07D403/12 , A61K31/44
CPC分类号： C07D213/30 , C07D213/26 , C07D235/02 , Y10S514/925
摘要： Imidazole derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 R.sub.4, R.sub.5, X and n are as hereinafter set forth,and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of gastric ulcers.
摘要翻译：其中R 1，R 2，R 3 + L，R 4，R 5，X和n如下文所述的式Ⅰ的咪唑衍生物及其药学上可接受的酸加成盐被描述。式I化合物可用于治疗胃溃疡。

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