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1. 发明申请

WO9900373A8 BENZIMIDAZOLE DERIVATIVES 审中-公开
标题翻译：苯并咪唑衍生物
公开(公告)号：WO9900373A8
公开(公告)日：2000-07-20
申请号：PCT/JP9802885
申请日：1998-06-26
申请人： FUJISAWA PHARMACEUTICAL CO , YAMASAKI NORITSUGU , IMOTO TAKAFUMI , OKU TERUO , KATAYAMA AKIRA , KAYAKIRI HIROSHI , ONOMURA OSAMU , HIRAMURA TAKAHIRO , NISHIKAWA MASAHIRO , SAWADA HITOSHI
发明人： YAMASAKI NORITSUGU , IMOTO TAKAFUMI , OKU TERUO , KATAYAMA AKIRA , KAYAKIRI HIROSHI , ONOMURA OSAMU , HIRAMURA TAKAHIRO , NISHIKAWA MASAHIRO , SAWADA HITOSHI
IPC分类号： A61K31/4184 , A61K31/4725 , A61P3/10 , C07D235/08 , C07D401/06 , C07D405/10 , C07D409/10 , C07D409/12 , A61K31/415 , A61K31/47 , C07D235/26 , C07D235/28
CPC分类号： C07D401/06 , C07D235/08 , C07D405/10 , C07D409/10 , C07D409/12
摘要： New benzimidazole derivatives of general formula (I) or salts thereof, useful as medicines, wherein R1 is alkyl or the like; R2 is aromatic ring-containing lower alkyl which may be substituted; R3 is alkyl or the like; and -X- is a group of general formula (V) or the like.
摘要翻译：用作药物的通式（I）的新的苯并咪唑衍生物或其盐，其中R 1是烷基等; R2是可被取代的含芳环的低级烷基; R3是烷基等; 和-X-是通式（V）等的基团。

2. 发明申请

WO1998015530A1 INDOLE DERIVATIVES 审中-公开
标题翻译： INDOLE DORIVATIVES
公开(公告)号：WO1998015530A1
公开(公告)日：1998-04-16
申请号：PCT/JP1997003592
申请日：1997-10-07
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , YAMASAKI, Noritsugu , IMOTO, Takafumi , MURAI, Yoshiyuki , HIRAMURA, Takahiro , ONOMURA, Osamu , NISHIKAWA, Masahiro , OKU, Teruo , SAWADA, Kouzou , KAYAKIRI, Hiroshi
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D209/08
CPC分类号： C07D401/06 , C07D209/08 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/10 , C07D417/12 , C07D417/14
摘要： Novel indole derivatives represented by general formula (V) or pharmaceutically acceptable salts thereof. Because of having hypoglycemic or PDE5-inhibitory activities, these compouds or salts thereof are useful as remedies for impaired glucose tolerance, diabetes, complication of diabetes, insulin resistant syndrome, hyperlipidemia, atherosclerosis, cardiovascular diseases, hyper glycemia, hypertension; diseases characterized by angina pectoris, high blood pressure, pulmonary hypertension, congestive heart failure, glomerular diseases, tubular interstitial diseases, renal insufficiency, atherosclerosis, angiostenosis, peripheral vascular diseases, cerebral stroke, chronic reversible obstructive diseases, allergic rhinitis, urticaria, glaucoma or intestinal motility disorders; sexual impotence, complication of diabetes, osteoporosis, nephritis, cancerous cachexia or post-PTCA reconstriction, wherein R13 to R15 represent each: 1) hydrogen, 2) lower alkyl, lower alkylthio or lower alkoxy-substituted lower alkyl, or 3) lower alkyl, hydroxy, hydroxylated lower alkyl, lower alkyloxy, etc. bonded to or substituted by aryl or a heterocycle; provided that R13 to R15 do not represent hydrogen at the same time; R16 represents: 1) hydrogen, or 2) lower alkyl; and R17 represents optionally esterified carboxy.
摘要翻译：由通式（V）表示的新型吲哚衍生物或其药学上可接受的盐。由于具有低血糖或PDE5抑制活性，这些化合物或其盐可用作葡萄糖耐量降低，糖尿病，糖尿病并发症，胰岛素抵抗综合征，高脂血症，动脉粥样硬化，心血管疾病，高血糖症，高血压症的补救措施; 特征为心绞痛，高血压，肺动脉高压，充血性心力衰竭，肾小球疾病，肾小管间质疾病，肾功能不全，动脉粥样硬化，血管狭窄症，外周血管疾病，脑中风，慢性可逆性阻塞性疾病，过敏性鼻炎，荨麻疹，青光眼或肠蠕动障碍; 性功能障碍，糖尿病并发症，骨质疏松症，肾炎，癌性恶病质或PTCA后重建，其中R13至R15各自表示：1）氢，2）低级烷基，低级烷硫基或低级烷氧基取代的低级烷基，或3）低级烷基，羟基，羟基化的低级烷基，低级烷氧基等，与芳基或杂环结合或取代; 条件是R13至R15不同时代表氢; R16表示：1）氢，或2）低级烷基; R 17代表任意酯化的羧基。

3. 发明申请

WO1997024334A1 BENZIMIDAZOLE DERIVATIVES 审中-公开
标题翻译：苯并咪唑衍生物
公开(公告)号：WO1997024334A1
公开(公告)日：1997-07-10
申请号：PCT/JP1996003858
申请日：1996-12-27
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , YAMASAKI, Noritsugu , IMOTO, Takafumi , MURAI, Yoshiyuki , HIRAMURA, Takahiro , OKU, Teruo , SAWADA, Kouzou
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D235/08
CPC分类号： C07D401/06 , C07D209/08 , C07D235/08 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/10 , C07D417/12 , C07D417/14
摘要： Novel benzimidazole derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof wherein R3 represents carboxy, esterified carboxy, carboxamide, amino, amido or sulfonyl. Because of having hypoglycemic or PDE5 inhibitory effects, these compounds or salts thereof are useful as remedies for impaired glucose tolerance, diabetes, complications of diabetes, insulin resistant syndrome, hyperlipidemia, atherosclerosis, cardiovascular diseases, hyperglycemia, hypertension, angina pectoris, pulmonary hypertension, congestive heart failure, glomerular diseases, tubular interstitial diseases, renal failure, angiostenosis, peripheral vascular disease, apoplexy, chronic reversible obstructive diseases, allergic rhinitis, urticaria, glaucoma, diseases characterized by abnormality in intestinal motility, sexual impotence, nephritis, cancerous cachexia, or post-PCTA reconstriction.
摘要翻译：由通式（I）表示的新型苯并咪唑衍生物或其药学上可接受的盐，其中R 3表示羧基，酯化羧基，羧酰胺，氨基，酰氨基或磺酰基。由于具有低血糖或PDE5抑制作用，这些化合物或其盐可用作葡萄糖耐量减低，糖尿病，糖尿病并发症，胰岛素抵抗综合征，高脂血症，动脉粥样硬化，心血管疾病，高血糖症，高血压，心绞痛，肺动脉高压，充血性心力衰竭，肾小球疾病，管状间质性疾病，肾衰竭，血管狭窄症，外周血管疾病，中风，慢性可逆性阻塞性疾病，过敏性鼻炎，荨麻疹，青光眼，肠蠕动异常特征性疾病，性阳ence，肾炎，癌性恶病质，或后PCTA重新约束。

4. 发明申请

WO1988008427A1 NUCLEOSIDE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：核苷衍生物及其制备方法
公开(公告)号：WO1988008427A1
公开(公告)日：1988-11-03
申请号：PCT/JP1988000393
申请日：1988-04-22
申请人： RIKAGAKU KENKYUSHO , KUZUHARA, Hiroyoshi , KAMANA, Masajiro , YAMASAKI, Noritsugu , NISHIKAWA, Masahiro
发明人： RIKAGAKU KENKYUSHO
IPC分类号： C07H19/052
CPC分类号： C07D473/00 , C07D405/04 , C07H19/06 , C07H19/16 , Y02P20/55
摘要： Dideoxynucleoside derivatives effective as antiviral agents, intermediates for their synthesis, and process for their synthesis are disclosed. The process is characterized in that a mesyl, tosyl or trifluoromethanesulfonyl group is introduced selectively into the 3'-position of a ribose unit of various nucleoside whose base and 2'- and 5'-positions of the ribose unit are protected, and the product is treated with a base and a reducing agent to give an intermediate useful for synthesizing the dinucleoside derivatives. This process enables preparation of various novel intermediates and dideoxynucleoside derivatives. Another process of synthesizing intermediates useful for synthesizing dideoxynucleoside derivatives is also disclosed, which comprises reacting a nucleoside derivative whose base and 2'- and 5'-positions of the ribose unit are protected by pivaloyl groups and 3'-position is protected by a mesyl, tosyl or trifluoromethanesulfonyl group with an alkaline compound to thereby selectively eliminate pivaloyl groups of the base.

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