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公开(公告)号：EP1132087A4
公开(公告)日：2002-06-26
申请号：EP99972100
申请日：1999-11-10
IPC分类号： A61K31/404 , A61K31/415 , A61K31/4184 , A61P3/10 , A61P15/00 , C07D209/08 , C07D209/10 , C07D235/08 , A61K31/40
CPC分类号： A61K31/415 , A61K31/404 , C07D209/08 , C07D209/10 , C07D235/08
摘要： Remedies for polycystic ovary syndrome which contain as the active ingredient compounds represented by general formula (1) or (2) or pharmaceutically acceptable salts thereof, wherein each symbol is as defined in the description.
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公开(公告)号：EP1142880A4
公开(公告)日：2002-02-27
申请号：EP99961320
申请日：1999-12-22
发明人： YAMASAKI NORITSUGU , IMOTO TAKAFUMI , HIRAMURA TAKAHIRO , KAWAUCHI MIHO , OKU TERUO , KAYAKIRI HIROSHI , SAWADA HITOSHI , ABE YOSHITO , HAMASHIMA HITOSHI , ISHIBASHI NAOKI , SETOI HIROYUKI
IPC分类号： A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P15/10 , A61P27/06 , C07D235/08 , C07D235/12 , C07D405/10 , C07D405/12 , C07D409/10 , C07D409/12 , C07D409/14 , A61K31/4184 , A61K31/5377
CPC分类号： C07D405/10 , C07D235/08 , C07D235/12 , C07D405/12 , C07D409/10 , C07D409/12 , C07D409/14
摘要： Novel benzimidazole derivatives represented by general formula (I) or salts thereof, which have hypoglycemic and PDE5-inhibiting effects and are therefore useful as drugs; in formula (I) R1 is lower alkyl which may be substituted with lower alkyloxy; R2 is hydrogen, halogeno, C1-C8 alkyl, aryl, or the like; R3 is lower alkyl, lower alkenyl, aryl, lower alkylaryl, aryl-substituted lower alkenyl, halothienyl, lower alkylamino or aryl lower alkylamino; A is a benzene ring, a naphthalene ring, or a pyridine ring; and X is halogeno.
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公开(公告)号：EP0995742A4
公开(公告)日：2004-08-25
申请号：EP98929715
申请日：1998-06-24
发明人： KAYAKIRI HIROSHI , ABE YOSHITO , HAMASHIMA HITOSHI , SAWADA HITOSHI , MIZUTANI TSUYOSHI , YAMASAKI NORITSUGU , ONOMURA OSAMU , NISHIKAWA MASAHIRO , HIRAMURA TAKAHIRO , OKU TERUO , IMOTO TAKAFUMI
IPC分类号： G06Q50/10 , A61K20060101 , A61K31/381 , A63B69/36 , C07D20060101 , C07D215/48 , C07D231/56 , C07D239/96 , C07D241/52 , C07D249/18 , C07D307/79 , C07D333/54 , C07D333/56 , C07D333/62 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07F20060101 , A61K31/34 , A61K31/38 , A61K31/415 , A61K31/437 , A61K31/47 , A61K31/495 , A61K31/505 , C07D235/26
CPC分类号： C07D241/52 , C07D215/48 , C07D231/56 , C07D239/96 , C07D249/18 , C07D307/79 , C07D333/54 , C07D333/62 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Sulfonamide compounds represented by the general formula (I) R1-SO2NHCO-A-X-R2, salts thereof, and medicinal compositions containing the same. In said formula, R1 represents alkyl, alkenyl, alkynyl, etc.; A represents an optionally substituted polyheterocyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenz-imidazolyl and 2,3-dihydrobenzoxazinyl; X represents alkylene, oxygen, oxygenated lower alkylene, etc.; and R2 represents optionally substituted aryl, substituted biphenylyl, etc. These compounds are useful in treating diseases curable based on the hypoglycemic effect, and diseases curable based on the cGMP-PDE inhibitory, leiolytic, bronchodilating, vasodilating, smooth muscle cell inhibitory, and antiallergic effects.
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公开(公告)号：EP1020452A4
公开(公告)日：2003-04-02
申请号：EP98929723
申请日：1998-06-26
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： 可用作药物的通式（I）的新的苯并咪唑衍生物或其盐，其中R 1为烷基等; R2是可被取代的含芳环的低级烷基; R3是烷基等; 并且-X-是通式（V）的基团等。
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公开(公告)号：EP1136492A4
公开(公告)日：2002-03-27
申请号：EP99973290
申请日：1999-12-01
发明人： KAYAKIRI HIROSHI , ABE YOSHITO , HAMASHIMA HITOSHI , SAWADA HITOSHI , ISHIBASHI NAOKI , SETOI HIROYUKI , OKU TERUO , YAMASAKI NORITSUGU , IMOTO TAKAFUMI , HIRAMURA TAKAHIRO
IPC分类号： A61P43/00 , C07D471/04 , A61K31/437 , A61P3/06 , A61P3/10 , A61P9/08 , A61P11/08 , A61P37/08
CPC分类号： C07D471/04
摘要： Sulfonamide compounds represented by general formula (I), or salts thereof; and drug compositions containing the same (wherein each symbol is as defined in the description). These compounds serve as preventive or therapeutic agents efficacious against diseases which can be cured through decrease in blood sugar level and those which can be cured through inhibition of cGMP-PDE, relaxation of smooth muscle, bronchodilation, vasodilation, inhibition of smooth muscle fiber, or inhibition of allergy.
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6.发明公开CRYSTALLINE FORMS OF 3-(2,4-DICHLOROBENZYL)-2-METHYL-N-(PENTYLSULFONYL)-3H-BENZIMIDAZOLE-5-CARBOXAMIDE 审中-公开3-（2,4-二氯苄基）-2-甲基-N-（戊基磺酰基）-3H-苯并咪唑-5-甲酰胺结晶形式
公开(公告)号：EP1138674A4
公开(公告)日：2002-08-21
申请号：EP99972205
申请日：1999-11-11
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.
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公开(公告)号：EP1070705A4
公开(公告)日：2002-04-17
申请号：EP99912110
申请日：1999-04-05
发明人： YAMASAKI NORITSUGU , IMOTO TAKAFUMI , OKU TERUO , KAYAKIRI HIROSHI , ONOMURA OSAMU , HIRAMURA TAKAHIRO
IPC分类号： C07D209/10 , C07D209/12 , C07D405/10 , C07D409/10 , C07D409/12 , A61K31/404
CPC分类号： C07D405/10 , C07D209/10 , C07D209/12 , C07D409/10 , C07D409/12
摘要： Novel indole derivatives represented by formula (I) or salts thereof, wherein R1 is aryl-substituted lower alkyl in which the aryl may be substituted by at least one member selected among halogen atoms, aryls, heterocyclic groups, aryl-substituted lower alkyls, aryl-substituted lower alkenyls, lower haloalkyls, (lower cycloalkyl)-substituted lower alkyloxys, (lower cycloalkyloxy)-substituted lower alkyls, aryl-substituted lower alkynyls, aryloxy-substituted lower alkyls, aryl-substituted lower alkyloxys, lower alkylthios, lower alkyloxys, and alkenyls; and R2 is a lower alkyl, lower alkenyl, aryl, or heterocyclic group optionally substituted by halogeno, lower alkyl, lower alkenyl, or aryl. These compounds have a hypoglycemic activity and a PDE5 inhibitory activity and are useful as a drug.
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公开(公告)号：EP1142879A4
公开(公告)日：2002-02-06
申请号：EP99959929
申请日：1999-12-20
发明人： KAYAKIRI HIROSHI , ABE YOSHITO , HAMASHIMA HITOSHI , SAWADA HITOSHI , ISHIBASHI NAOKI , SETOI HIROYUKI , OKU TERUO , YAMASAKI NORITSUGU , IMOTO TAKAFUMI , HIRAMURA TAKAHIRO
IPC分类号： A61K31/4174 , A61K31/4178 , A61P3/10 , A61P43/00 , C07D233/54 , C07D233/64 , C07D233/68 , C07D233/90 , C07D233/94 , C07D401/06 , C07D405/10 , C07D409/10 , C07D409/12
CPC分类号： C07D233/64 , C07D233/90 , C07D233/94 , C07D405/10 , C07D409/10 , C07D409/12
摘要： Imidazole compounds represented by general formula (I) and salts thereof and medicinal compositions containing the same. These compounds are useful in treating diseases which can be treated based on the hypoglycemic effect thereof, and diseases which can be treated based on the cGMP-PDE inhibitory effect, smooth muscular relaxant effect, bronchodilating effect, vasodilating effect, smooth muscle cell regulatory effect and allergy-inhibitory effects thereof, wherein each symbol is as defined in the description.
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公开(公告)号：EP1000932A4
公开(公告)日：2000-08-09
申请号：EP98929724
申请日：1998-06-26
发明人： YAMASAKI NORITSUGU , IMOTO TAKAFUMI , HIRAMURA TAKAHIRO , ONOMURA OSAMU , NISHIKAWA MASAHIRO , KAYAKIRI HIROSHI , ABE YOSHITO , HAMASHIMA HITOSHI , SAWADA HITOSHI
IPC分类号： C07C311/51 , C07D213/78 , C07D213/81 , C07D233/54 , C07D233/56 , C07D233/64 , C07D233/68 , C07D409/06 , A61K31/18 , A61K31/415 , A61K31/44 , C07D213/56 , C07D409/12
CPC分类号： C07D213/78 , C07C311/51 , C07D213/81 , C07D233/64 , C07D233/68 , C07D409/06
摘要： Novel aromatic ring derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof. Because of having hypoglycemic and PDE 5 inhibitory activities, these compounds and salts thereof are useful as remedies for impaired glucose tolerance, diabetes, complication of diabetes, insulin-resistant syndrome, polycystic ovary syndrome, hyperlipidemia, atherosclerosis, cardio-vascular diseases, hyperglycemia, hypertension, angina pectoris, pulmonary hypertension, congestive heart failure, glomerular diseases, tubular interstitial diseases, renal insufficiency, atherosclerosis, angiostenosis, peripheral vascular diseases, cerebral stroke, chronic reversible obstructive diseases, autoimmune diseases, allergic rhinitis, urticaria, glaucoma, diseases characterized by disordered intestinal motion, sexual impotence, nephritis, cachexia, pancreatitis, post-PTCA reconstriction, etc. In said formula (I), Nu represents a 5- or 6-membered aromatic ring; ch1 and ch2 represent each a cross-linking group; and A represents an aromatic ring.
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公开(公告)号：EP0882718A4
公开(公告)日：1999-08-04
申请号：EP96943331
申请日：1996-12-27
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.
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