公开(公告)号：EP1138674A4

公开(公告)日：2002-08-21

申请号：EP99972205

申请日：1999-11-11

申请人： FUJISAWA PHARMACEUTICAL CO ,  DAICEL CHEM

发明人： MURAI YOSHIYUKI ,  YAMASAKI NORITSUGU ,  IMOTO TAKAFUMI ,  NISHIKAWA MASAHIRO ,  DOHTSU KUNIHIKO

IPC分类号： A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61P3/10 ,  A61P15/00 ,  C07D209/08 ,  C07D209/10 ,  C07D235/08

CPC分类号： A61K31/415 ,  A61K31/404 ,  C07D209/08 ,  C07D209/10 ,  C07D235/08

摘要： 3-(2,4-Dichlorobenzyl)-2-methyl-N-(pentylsulfonyl)-3H-benzimidazole-5-carboxamide having a hypoglycemic activity or a PDE5 inhibitory effect occurs as three crystalline forms which are distinguishable from each other based on the powdery X-ray diffraction data. The most stable crystalline form thereof is useful as a bulk powder for drugs. Other crystalline forms comprise larger crystals, which can be very easily isolated by filtration and efficiently purified by crystallization, are useful in purifying 3-(2,4-dichlorobenzyl)-2-methyl-N-(pentylsulfonyl)-3H-benzimidazole-5-carboxamide.

公开(公告)号：EP0882718A4

公开(公告)日：1999-08-04

申请号：EP96943331

申请日：1996-12-27

申请人： FUJISAWA PHARMACEUTICAL CO

发明人： YAMASAKI NORITSUGU ,  IMOTO TAKAFUMI ,  MURAI YOSHIYUKI ,  HIRAMURA TAKAHIRO ,  OKU TERUO ,  SAWADA KOUZOU

IPC分类号： A61K31/4184 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61P1/00 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P15/10 ,  A61P17/00 ,  A61P27/06 ,  A61P27/16 ,  A61P43/00 ,  C07D209/08 ,  C07D235/08 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D235/10 ,  C07D235/22 ,  C07D235/24 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30

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.

公开(公告)号：EP0748801A4

公开(公告)日：1997-04-16

申请号：EP95910724

申请日：1995-03-02

申请人： DAICEL CHEM

发明人： MURAI YOSHIYUKI ,  NISHIKAWA MASAHIRO ,  UEDA YOICHIRO ,  ONOMURA OSAMU ,  TAKASE ICHIRO

IPC分类号： C07C213/00 ,  C07C213/10 ,  C07C215/28 ,  C07C269/06 ,  C07C273/18 ,  C07D261/04

CPC分类号： C07C269/06 ,  C07C213/00 ,  C07C213/10 ,  C07C273/1854 ,  C07D261/04 ,  C07C215/08 ,  C07C215/28

摘要： An intermediate useful for synthesizing a 2,5-diamino-1,6-diphenyl-3-hydroxyhexane derivative serving as an intermediate for preparing medicines such as retrovirus protease inhibitors including human immunodeficiency virus (HIV) protease inhibitors; and a process for producing the above derivative from the above intermediate. Specifically, the invention provides a 2-isoxazoline derivative represented by general formula [1] and a process for producing the 2,5-diamino-1,6-diphenyl-3-hydroxyhexane derivative represented by general formula [6] by reducing the above derivative [1]; wherein Ph represents phenyl; and R?1 and R2¿ represent each independently hydrogen, acyl, alkyloxycarbonyl, arylalkyloxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylalkylaminocarbonyl, arylaminocarbonyl, alkyl, arylalkyl, aryl, alkylsulfonyl, arylalkylsulfonyl or arylsulfonyl, or R?1 and R2¿ are combined together to represent divalent acyl.