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1. 发明授权

US06670360B2 Optically active pyrrolopyridazine derivatives 失效
标题翻译：光学活性吡咯并哒嗪衍生物
公开(公告)号：US06670360B2
公开(公告)日：2003-12-30
申请号：US10021214
申请日：2001-12-12
申请人： Masahiko Hagihara , Nobuhiko Shibakawa , Keiji Matsunobu , Hiroshi Fujiwara , Keiichi Ito
发明人： Masahiko Hagihara , Nobuhiko Shibakawa , Keiji Matsunobu , Hiroshi Fujiwara , Keiichi Ito
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： An optically active pyrrolopyridazine compound of the formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is alkyl; R2 and R3 are each independently alkyl; R4 is optionally substituted aryl; and A is imino, oxygen or sulfur. The pyrrolopyridazine compound or pharmaceutically acceptable salts thereof of the present invention exhibit excellent gastric acid secretory inhibition activity and gastric mucous membrane protection activity, as well as excellent antibacterial activity against Helicobacter pylori. They are useful medicines and are particularly useful for treating or preventing ulcerative diseases.
摘要翻译：式（I）的光学活性吡咯并哒嗪化合物或其药学上可接受的盐：其中R 1是烷基; R 2和R 3各自独立地为烷基; R 4是任选取代的芳基; A是亚氨基，氧或硫。本发明的吡咯并哒嗪化合物或其药学上可接受的盐显示出优异的胃酸分泌抑制活性和胃粘膜保护活性，以及对幽门螺杆菌的优良抗菌活性。它们是有用的药物，特别适用于治疗或预防溃疡性疾病。

2. 发明授权

US06063782A Pyrrolopyridazine derivatives 失效
标题翻译：吡咯并哒嗪衍生物
公开(公告)号：US06063782A
公开(公告)日：2000-05-16
申请号：US676375
申请日：1996-07-17
申请人： Tomio Kimura , Nobuhiko Shibakawa , Hiroshi Fujiwara , Etsuro Itoh , Keiji Matsunobu , Keiichi Tabata , Hiroshi Yasuda , Yoshimi Fujihara, deceased
发明人： Tomio Kimura , Nobuhiko Shibakawa , Hiroshi Fujiwara , Etsuro Itoh , Keiji Matsunobu , Keiichi Tabata , Hiroshi Yasuda , Yoshimi Fujihara, deceased
IPC分类号： E04F13/08 , A61K31/5025 , A61P1/04 , C07D487/04 , E04F13/073 , E04F13/26 , E04F19/02
CPC分类号： C07D487/04
摘要： Pyrrolopyridazine derivatives having the general formula. ##STR1## In the above formula, R.sup.1 represents a C.sub.2 -C.sub.6 alkenyl-group, a halogeno-C.sub.2 -C.sub.6 -alkenyl group, a C.sub.6 -C.sub.10 aryl-C.sub.2 -C.sub.6 -alkenyl group, a C.sub.2 -C.sub.6 alkynyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a C.sub.3 -C.sub.7 cycloalkyl-C.sub.1 -C.sub.6 -alkyl group, a C.sub.5 -C.sub.7 cycloalkenyl-C.sub.1 -C.sub.6 -alkyl group or a halogeno-C.sub.1 -C.sub.6 -alkyl group; R.sup.2 and R.sup.3 are the same or different and each represents a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.6 -C.sub.10 aryl group; R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.5 represents a C.sub.6 -C.sub.10 aryl group or a 5-10 membered heteroaryl group comtaining heteroatom(s) selected from nitrogen, oxygen and sulfur;
摘要翻译：具有通式的吡咯并哒嗪衍生物。在上式中，R 1表示C 2 -C 6链烯基，卤代-C 2 -C 6 - 烯基，C 6 -C 10芳基-C 2 -C 6 - 烯基，C 2 -C 6炔基，C 3 -C 7环烷基 C 3 -C 7环烷基-C 1 -C 6烷基，C 5 -C 7环烯基-C 1 -C 6烷基或卤代-C 1 -C 6烷基; R2和R3相同或不同，各自表示氢原子，C1-C6烷基或C6-C10芳基; R4表示氢原子或C1-C6烷基; R5表示C6-C10芳基或含有选自氮，氧和硫的杂原子的5-10元杂芳基;

3. 发明授权

US06734181B2 Pyrrolopyridazine compounds 失效
标题翻译：吡咯并哒嗪化合物
公开(公告)号：US06734181B2
公开(公告)日：2004-05-11
申请号：US10215246
申请日：2002-08-08
申请人： Haruo Iwabuchi , Masahiko Hagihara , Nobuhiko Shibakawa , Keiji Matsunobu , Hiroshi Fujiwara
发明人： Haruo Iwabuchi , Masahiko Hagihara , Nobuhiko Shibakawa , Keiji Matsunobu , Hiroshi Fujiwara
IPC分类号： A61K315025
CPC分类号： C07D487/04 , A61K31/5025
摘要： A pyrrolopyridazine compound having the formula (I) or a pharmaceutically acceptable salt thereof: wherein, R1 is a C2-C6 alkenyl group, a halogeno C2-C6 alkenyl group, a C3-C7 cycloalkyl group which may be optionally substituted or a C3-C7 cycloalkyl- C1-C6 alkyl group which may be optionally substituted. R2 is a C1-C6 alkyl group. R3 is a hydroxymethyl group, a C2-C6 aliphatic acyloxymethyl group, a C6-C10 arylcarbonyloxymethyl group which may be optionally substituted, a C1-C6 alkoxycarbonyloxymethyl group, a formyl group, a carboxyl group, a C1-C6 alkoxycarbonyl group or a C6-C10 aryloxycarbonyl group which may be optionally substituted. R4 is a C6-C10 aryl group which may be optionally substituted. A is an imino group, an oxygen atom or a sulfur atom. These compounds exhibit excellent gastric acid secretory inhibition activity and gastric mucous membrane protection activity etc. They are useful for prevention or treatment of ulcerative diseases and for Helicobacter pylori infections.
摘要翻译：具有式（I）的吡咯并哒嗪化合物或其药学上可接受的盐：其中R 1为C 2 -C 6烯基，卤代C 2 -C 6烯基，可任意取代的C 3 -C 7环烷基或可以任意取代的C 3 -C 7环烷基-C 1 -C 6烷基。 R 2是C 1 -C 6烷基。 R 3是羟甲基，C 2 -C 6脂族酰氧基甲基，可以任意取代的C 6 -C 10芳基羰基氧基甲基，C 1 -C 6烷氧基羰基氧基甲基，甲酰基，羧基，C 1 -C 6烷氧基羰基或可任意取代的C 6 -C 10芳氧基羰基。 R 4是可以任选取代的C 6 -C 10芳基。 A是亚氨基，氧原子或硫原子。这些化合物表现出优异的胃酸分泌抑制活性和胃粘膜保护活性等，它们可用于预防或治疗溃疡性疾病和幽门螺杆菌感染。

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