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21. 发明授权

US5496928A Endothelin antagonistic substance 失效
标题翻译：内皮素拮抗物质
公开(公告)号：US5496928A
公开(公告)日：1996-03-05
申请号：US230534
申请日：1994-04-20
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano , Masaru Nishikibe
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano , Masaru Nishikibe
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/087 , C07K5/103 , A61K38/06
CPC分类号： C07K5/1008 , C07K5/0202 , C07K5/0205 , C07K5/06034 , C07K5/06043 , C07K5/0808 , C07K5/0812 , A61K38/00
摘要： Peptides having the formula: ##STR1## inhibit the binding of endothelin and are useful in treating diseases associated with excess production or secretion of endothelin.
摘要翻译：具有下式的肽：（I）抑制内皮素的结合，并且可用于治疗与内皮素过量产生或分泌相关的疾病。

22. 发明授权

US5470833A Endothelin antagonistic peptide derivatives 失效
标题翻译：内皮素拮抗肽衍生物
公开(公告)号：US5470833A
公开(公告)日：1995-11-28
申请号：US213829
申请日：1994-03-14
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/103 , C07K5/00 , C07K5/08 , C07K5/10
CPC分类号： C07K5/06156 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/0808 , C07K5/1008 , A61K38/00
摘要： Peptides having the formula: ##STR1## inhibit the binding of endothelin to its receptor and are useful in treating diseases associated with excess production or secretion of endothelin.
摘要翻译：具有下式的肽：抑制内皮素与其受体的结合，并且可用于治疗与内皮素过量产生或分泌相关的疾病。

23. 发明授权

US4839353A Anti-ulcer substituted pyridine derivatives 失效
标题翻译：抗溃疡取代的吡啶衍生物
公开(公告)号：US4839353A
公开(公告)日：1989-06-13
申请号：US110369
申请日：1987-10-20
申请人： Masaaki Hosoi , Ryo Nishioka , Yoshio Hioki , Yoshiaki Iida , Hiroshi Takeshita , Kenji Niiyama , Yusuke Hidaka
发明人： Masaaki Hosoi , Ryo Nishioka , Yoshio Hioki , Yoshiaki Iida , Hiroshi Takeshita , Kenji Niiyama , Yusuke Hidaka
IPC分类号： C07D213/16 , C07D213/68 , C07D213/70 , C07D213/74 , C07D401/04
CPC分类号： C07D213/16 , C07D213/68 , C07D213/70 , C07D213/74 , C07D401/04
摘要： A substituted pyridine derivative represented by the general formula ##STR1## wherein R.sup.1 represents a phenyl or naphthyl group which may optionally be substituted by a substituent selected from the class consisting of a hydroxyl group, lower alkyl groups, lower alkoxy groups, cycloalkyl groups, lower alkoxycarbonyl groups, a phenyl group and halogen atoms; X represents an oxygen atom, a sulfur atom, a carbonyl group, or a group of the formula --CH(OH)-- or --N(R.sup.a)-- in which R.sup.a is a hydrogen atom or a lower alkyl group; Y represents a linear or branched lower alkylene group or a vinylene group which may optionally be substituted by a lower alkyl group, with the proviso that when X is an oxygen or sulfur atom, Y represents the lower alkylene group; R.sup.2 and R.sup.3 are identical or different and each represents a hydrogen atom or a lower alkyl group; R.sup.4 represents a hydrogen atom, a lower alkoxy group, a cycloalkyloxy group, a lower alkylthio group, a cycloalkylthio group, an aryloxy group, an aralkyloxy groups or a group of the formula ##STR2## in which R.sup.b and R.sup.c are identical or different and each represents a hydrogen atom or a lower alkyl group. or R.sup.b and R.sup.c, taken together, may form together with the adjacent nitrogen atom a 5- to 7-membered saturated heterocyclic ring which may optionally contain at least one additional hetero atom selected from the group consisting of oxygen, sulfur and nitrogen atoms and may optionally be substituted by a lower alkyl group; m and n are each 0 or 1, with the proviso that m and n are not 0 at the same time, or an acid addition salt thereof. This compound is useful as an antiulcer agent.
摘要翻译：由通式[IMAGE] [I]表示的取代的吡啶衍生物，其中R 1表示可任选被选自羟基，低级烷基，低级烷氧基，环烷基的取代基取代的苯基或萘基基团，低级烷氧基羰基，苯基和卤素原子; X表示氧原子，硫原子，羰基或式-CH（OH） - 或-N（Ra） - 的基团，其中Ra为氢原子或低级烷基; Y表示可以任选被低级烷基取代的直链或支链低级亚烷基或亚乙烯基，条件是当X是氧或硫原子时，Y代表低级亚烷基; R2和R3相同或不同，各自表示氢原子或低级烷基; R 4表示氢原子，低级烷氧基，环烷氧基，低级烷硫基，环烷硫基，芳氧基，芳烷氧基或式中的R 1和R c相同或不同的式各自表示氢原子或低级烷基。或Rb和Rc一起可以与相邻的氮原子一起形成5-7元饱和杂环，其可以任选地含有至少一个选自氧，硫和氮原子的另外的杂原子，并且可以任选被低级烷基取代; m和n各自为0或1，条件是m和n不同时为0，或其酸加成盐。该化合物可用作抗溃疡剂。

24. 发明授权

US4743609A Indole derivatives having gastric and antisecretory and cytoprotective properties, and pharmaceutical preparations containing same 失效
标题翻译：具有胃和抗分泌和细胞保护性质的吲哚衍生物和含有它们的药物制剂
公开(公告)号：US4743609A
公开(公告)日：1988-05-10
申请号：US827898
申请日：1986-02-10
申请人： Masaaki Hosoi , Fumio Nakano , Kenji Matsuyama , Hiroshi Takeshita , Kenji Niiyama , Susumu Nakagawa
发明人： Masaaki Hosoi , Fumio Nakano , Kenji Matsuyama , Hiroshi Takeshita , Kenji Niiyama , Susumu Nakagawa
IPC分类号： C07D401/12 , C07D401/14 , A61K31/405
CPC分类号： C07D401/12 , C07D401/14
摘要： This invention provides a class of new indole derivatives which are useful as medicinal compounds having a mild inhibitory effect on the gastric acid secretion as well as a remarkably cytoprotective effects on gastric muscosa, and which are represented by the general formula: ##STR1##
摘要翻译：本发明提供了一类新的吲哚衍生物，其可用作对胃酸分泌具有温和抑制作用的药物化合物以及对胃肌肉的显着的细胞保护作用，其通过以下通式表示：

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