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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。
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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.
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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。
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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.
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公开(公告)号:US4927958A
公开(公告)日:1990-05-22
申请号:US169570
申请日:1988-03-17
IPC分类号: C07C45/29 , C07C45/45 , C07C45/63 , C07C45/67 , C07C45/74 , C07C49/255 , C07C59/84 , C07C59/88 , C07C59/90 , C07C69/618 , C07C69/738 , C07D317/60
CPC分类号: C07D317/60 , C07C323/00 , C07C45/298 , C07C45/455 , C07C45/63 , C07C45/673 , C07C45/74 , C07C49/255 , C07C59/88 , C07C59/90
摘要: Styryl ketones of the formula ##STR1## wherein R.sup.8 and R.sup.9 are independently hydrogen or lower alkyl or together represent an additional carbon-carbon bond andR.sup.10 is a group of the formula ##STR2## as well as corresponding compounds of the formula ##STR3## wherein R.sup.10' is a group of formula (a), (b), (d) or (e) or a group of the formula--C(R.sup.18)(R.sup.19)OR.sup.20' ; (f') have mucosa-protective and/or gastric acid secretion-inhibiting properties, such that they can be used for the control or prevention of illnesses of the gastrointestinal tract, especially against gastric ulcers or duodenal ulcers.
摘要翻译: 式IMA的苯乙烯基酮其中R 8和R 9独立地是氢或低级烷基或一起代表额外的碳 - 碳键,并且R 10是下式的基团:以及相应的化合物 其中R 10'是式(a),(b),(d)或(e)的基团或式-C(R 18)(R 19)OR 20'的基团; (f')具有粘膜保护性和/或胃酸分泌抑制性质,使得它们可用于控制或预防胃肠道疾病,特别是胃溃疡或十二指肠溃疡。
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公开(公告)号:US4929741A
公开(公告)日:1990-05-29
申请号:US169643
申请日:1988-03-17
IPC分类号: C07C45/29 , C07C45/45 , C07C45/51 , C07C45/67 , C07C49/794 , C07C49/796 , C07C49/813 , C07C49/835 , C07C49/84 , C07C49/86 , C07C59/66 , C07C59/68 , C07C323/22 , C07D317/54 , C07D317/60 , C07F7/18
CPC分类号: C07F7/1852 , C07C323/22 , C07C45/298 , C07C45/45 , C07C45/515 , C07C45/673 , C07C49/794 , C07C49/796 , C07C49/813 , C07C49/835 , C07C49/84 , C07C49/86 , C07C59/66 , C07C59/68 , C07C67/313 , C07C67/343 , C07C69/732 , C07C69/734 , C07C69/738 , C07D317/54 , C07D317/60
摘要: Propiolophenone derivatives of the formula ##STR1## wherein R.sup.6 is hydrogen, lower alkyl or a group of the formula ##STR2## as well as corresponding hydroxy compounds of the formula ##STR3## wherein R.sup.6' is hydrogen, lower alkyl, a group of formula (a), (b), (c), (d) or (e) or a group of the formula--C(R.sup.14)(R.sup.15)OR.sup.16' (f'):exhibit mucosa-protective and/or gastric acid secretion-inhibiting properties, such that they can be used for the control or prevention of illnesses of the gastrointestinal tract, especially against gastric ulcers and/or duodenal ulcers.
摘要翻译: 式(I)其中R 6为氢,低级烷基或式COOR 7基团,(a)CONR 8 R 9,(b)C(R 10)O,(C)C(R 11)(OR 12)2, (d)C(OR 13)3(e)或C(R 14)(R 15)OR 16; (f)以及相应的式II的羟基化合物,其中R 6'是氢,低级烷基,式(a),(b),(c),(d)或(e) 式-C(R 14)(R 15)OR 16'(f')的基团表现出粘膜保护性和/或胃酸分泌抑制性质,使得它们可用于控制或预防胃肠道疾病 ,特别是针对胃溃疡和/或十二指肠溃疡。
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公开(公告)号:US4827004A
公开(公告)日:1989-05-02
申请号:US88315
申请日:1987-08-24
申请人: Albert Fischli , Max Schmid , Rudolf Schmid
发明人: Albert Fischli , Max Schmid , Rudolf Schmid
IPC分类号: A61K31/045 , A61K31/12 , A61K31/15 , A61K31/16 , A61K31/215 , A61K31/695 , A61P1/04 , C07C27/00 , C07C29/147 , C07C33/02 , C07C33/035 , C07C33/12 , C07C41/00 , C07C43/13 , C07C43/178 , C07C43/30 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/67 , C07C47/263 , C07C49/20 , C07C49/24 , C07C49/242 , C07C49/255 , C07C49/258 , C07C59/42 , C07C59/58 , C07C59/76 , C07C67/00 , C07C69/66 , C07C69/732 , C07C231/00 , C07C231/12 , C07C233/09 , C07C235/28 , C07C235/30 , C07C235/76 , C07C235/78 , C07C251/34 , C07C313/00 , C07C317/24 , C07C317/28 , C07C317/44 , C07C317/46 , C07C323/22 , C07C323/24 , C07C323/25 , C07C323/27 , C07C323/52 , C07C323/54 , C07C323/60 , C07C325/00 , C07C327/22 , C07D303/46 , C07D317/20 , C07D317/30 , C07F7/18 , C09F5/00
CPC分类号: C07F7/1852 , C07C323/00 , C07C323/24 , C07C33/02 , C07C33/035 , C07C33/12 , C07C43/178 , C07C43/315 , C07C45/298 , C07C45/673 , C07C47/263 , C07C49/24 , C07C49/242 , C07C49/255 , C07C49/258 , C07C59/42 , C07C59/76 , C07D317/20
摘要: Novel Isoprene Derivatives which have mucosa-protective and gastric acid secretion-inhibiting properties and are useful for combatting ulcers both by treating and as a prophylaxis against gastric and/or duodenal ulcers.
摘要翻译: 具有粘膜保护性和胃酸分泌抑制性质的新型异戊二烯衍生物,可用于通过治疗和预防胃和/或十二指肠溃疡来对抗溃疡。
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