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公开(公告)号：EP1679309A4
公开(公告)日：2007-03-28
申请号：EP04793164
申请日：2004-10-22
IPC分类号： A61K31/505 , A61K31/506 , A61K31/517 , A61P25/00 , C07D239/42 , C07D409/12
CPC分类号： C07D409/12 , A61K31/505 , A61K31/506 , A61K31/517 , C07D239/42
摘要： A compound of the general formula: (I) (wherein the ring A represents a substituted or unsubstituted cyclic group; Q a substituted or unsubstituted alkyl or a substituted or unsubstituted cyclic group; the ring D a substituted or unsubstituted cyclic group; W a bond or a spacer with a principal chain of 1 to 4 atoms; and Y a spacer with a principal chain of 1 to 4 atoms), or its salt, N-oxide or solvate, or a prodrug thereof. The compound of the general formula (I), or its salt, N-oxide or solvate, or a prodrug thereof has affinity with MBR, thereby being useful as a preventive and/or curative drug for diseases caused by stress.
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2.发明公开NITROGEN-CONTAINING 5-MEMBERED CYCLIC COMPOUNDS AND DRUGS CONTAINING THESE COMPOUNDS AS THE ACTIVE INGREDIENT 审中-公开，五元，环状化合物并将此作为活性成分的药物含含氮
公开(公告)号：EP1254901A4
公开(公告)日：2003-03-05
申请号：EP01946857
申请日：2001-01-25
发明人： OHMOTO KAZUYUKI , ITAGAKI IORI
IPC分类号： A61K31/41 , A61K31/4245 , A61K31/4439 , A61K31/454 , A61K31/5377 , C07D257/04 , C07D257/06 , C07D271/06 , C07D271/07 , C07D401/04 , C07D401/06 , C07D403/12 , C07D413/04 , C07D413/06 , A61P9/00 , A61P11/00 , A61P29/00 , A61P33/00 , A61P37/00 , C07D271/113
CPC分类号： C07D257/04 , A61K31/41 , A61K31/4245 , A61K31/4439 , A61K31/454 , A61K31/5377 , C07D257/06 , C07D271/07 , C07D401/04 , C07D401/06 , C07D403/12 , C07D413/04 , C07D413/06
摘要： Nitrogen-containing 5-membered cyclic compounds represented by the general formula (I) and nontoxic salts thereof, wherein each symbol is as defined in the description. Because of having a cysteine protease inhibitory activity, the compounds of the general formula (I) are useful as preventives and/or remedies for inflammatory diseases, diseases caused by apoptosis, diseases caused by immune response error, autoimmune diseases, diseases caused by the degradation of biological constituent proteins, shock, circulatory error, blood coagulation error, malignant tumor, acquired immunological deficiency syndrome (AIDS), AIDS related complex (ARC), parasitogenic diseases, neurodegenerative diseases, lung disorder, bone resorption diseases, hyper endocrine diseases, etc.
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公开(公告)号：EP1162199A4
公开(公告)日：2002-06-05
申请号：EP00907995
申请日：2000-03-10
IPC分类号： C07D271/10 , C07D413/12 , C07K5/078 , C07K5/097 , C07K5/062
CPC分类号： C07D271/10 , C07D413/12 , C07K5/06139 , C07K5/0821 , Y02P20/55
摘要： Oxadiazole derivatives represented by general formula (I) (wherein R1 represents hydrogen or an amino-protecting group; and R?2, R3, and R4¿ each independently represents alkyl, cycloalkyl, optionally substituted phenyl, or 3,4-methylenedioxyphenyl, provided that R?3 and R4¿ may in combination represent C¿2-6? alkylene); and a process for producing an oxadiazole derivative represented by general formula (II) (wherein all symbols have the same meanings as the above) from any of the derivatives represented by general formula (I). By the process, a compound represented by general formula (II) can be produced in high yield through a smaller number of steps.
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公开(公告)号：EP1886693A4
公开(公告)日：2010-03-03
申请号：EP06756919
申请日：2006-06-02
IPC分类号： A61K45/00 , A61K31/426 , A61K31/427 , A61K47/40 , A61P9/00 , A61P19/08 , A61P25/00 , A61P43/00 , C07D277/20 , C07D277/56 , C07D417/12
CPC分类号： A61K31/426 , A61K9/0019 , A61K31/427 , A61K45/06 , A61K47/6951 , B82Y5/00 , C07D277/20 , C07D277/56 , C07D417/12
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5.发明公开DIKETOHYDRAZINE DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS AS THE ACTIVE INGREDIENT 有权DIZETHYDRAZINDERIVATVERBINDUNGEN UND ARZNEIMITTEL，DIE DIE VERBINDUNGEN ALS WIRKSTOFF ENTHALTEN
公开(公告)号：EP1498411A4
公开(公告)日：2005-11-30
申请号：EP03723188
申请日：2003-04-24
发明人： HATAYAMA AKIRA , TSURUTA HIROSHI , OCHI YASUO , IMAWAKA HARUO , OHMOTO KAZUYUKI
IPC分类号： C07C243/24 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/4152 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/429 , C07C243/34 , C07C251/76 , C07C251/84 , C07C251/86 , C07D207/22 , C07D207/50 , C07D209/46 , C07D209/48 , C07D211/28 , C07D211/72 , C07D211/86 , C07D211/98 , C07D213/70 , C07D213/76 , C07D213/77 , C07D213/78 , C07D233/38 , C07D233/52 , C07D233/80 , C07D239/10 , C07D239/18 , C07D239/36 , C07D241/08 , C07D241/18 , C07D263/26 , C07D263/28 , C07D265/08 , C07D265/10 , C07D265/32 , C07D265/33 , C07D275/02 , C07D275/03 , C07D275/06 , C07D277/18 , C07D277/36 , C07D277/50 , C07D277/54 , C07D277/60 , C07D277/82 , C07D279/02 , C07D279/06 , C07D279/12 , C07D285/10 , C07D285/16 , C07D309/04 , C07D309/28 , C07D335/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D513/10 , C07F9/59 , C07F9/6558 , C07D207/408 , C07D211/26 , C07D213/53 , C07D231/08 , C07D233/32 , C07D307/52 , C07D309/06 , C07D413/12 , C07D487/04
CPC分类号： C07D209/48 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/4152 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/429 , C07C243/34 , C07C251/76 , C07C251/84 , C07C251/86 , C07C2601/08 , C07C2601/14 , C07D207/22 , C07D207/50 , C07D209/46 , C07D211/28 , C07D211/72 , C07D211/86 , C07D211/98 , C07D213/70 , C07D213/76 , C07D213/77 , C07D213/78 , C07D233/38 , C07D233/52 , C07D233/80 , C07D239/10 , C07D239/18 , C07D239/36 , C07D241/08 , C07D241/18 , C07D263/26 , C07D263/28 , C07D265/08 , C07D265/10 , C07D265/33 , C07D275/02 , C07D275/03 , C07D275/06 , C07D277/18 , C07D277/36 , C07D277/50 , C07D277/54 , C07D277/60 , C07D277/82 , C07D279/02 , C07D279/06 , C07D279/12 , C07D285/10 , C07D285/16 , C07D309/04 , C07D309/28 , C07D335/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D513/10 , C07F9/591 , C07F9/65583
摘要： The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
摘要翻译： 本发明涉及式（I）的二酮肼衍生物及其药学上可接受的盐（式中的符号具有与说明书中所述相同的含义）。 式（I）化合物对半胱氨酸蛋白酶具有抑制活性，可用于治疗炎性疾病，免疫疾病，缺血性疾病，呼吸系统疾病，循环系统疾病，血液病，神经元疾病 ，肝或胆道疾病，骨关节疾病，代谢疾病等。该化合物对弹性蛋白酶具有抑制活性，也可用于治疗慢性阻塞性肺疾病（慢性阻塞性肺疾病）。
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6.发明公开NOVEL CRYSTALS OF 1,3,4-OXADIAZOLE DERIVATIVE, PROCESS FOR PRODUCING THE CRYSTALS AND MEDICINES CONTAINING THE SAME AS THE ACTIVE INGREDIENT 审中-公开1,3,4-恶二唑衍生物新晶体，用于晶体的生产并将此作为活性物质的含药
公开(公告)号：EP1318150A4
公开(公告)日：2004-04-14
申请号：EP01963508
申请日：2001-09-07
发明人： KOJIMA TSUTOMU , OHMOTO KAZUYUKI
IPC分类号： A61P1/02 , A61P9/02 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/00 , A61P25/28 , A61P27/02 , A61P29/02 , A61P35/00 , A61P37/06 , A61P43/00 , C07D413/12
CPC分类号： C07D413/12
摘要： Form 2 crystals of 2-[5-amino-6-oxo-2-phenyl-1,6-dihydro-1-pyrimidyl]-N-[1-(2-[5-t-butyl-1,3,4-oxadiazolyl]carbonyl)-2-R,S)-methylpropyl]acetamide (I); a process for producing the crystals; and medicines containing the same as the active ingredient.
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7.发明公开BENZENE-FUSED HETEROCYCLE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 审中-公开苯并杂环衍生物并将此作为有效成分含药物
公开(公告)号：EP1254898A4
公开(公告)日：2003-03-12
申请号：EP01946856
申请日：2001-01-25
发明人： OHMOTO KAZUYUKI , ITAGAKI IORI
IPC分类号： A61K38/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P3/14 , A61P7/04 , A61P7/06 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/08 , A61P19/02 , A61P19/10 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/28 , A61P27/10 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D223/16 , C07D243/12 , C07D243/14 , C07D267/02 , C07D267/14 , C07D281/02 , C07D281/10 , C07D285/36 , C07D401/12 , C07D403/12 , C07D409/12 , C07D491/048 , C07D491/056 , C07K5/06 , C07K5/065 , C07K5/068 , C07K5/078 , A61K31/55 , A61K31/5513 , A61K31/553 , A61K31/554 , A61P9/00 , A61P33/00 , A61P37/00
CPC分类号： C07D223/16 , A61K38/00 , C04B35/632 , C07D243/12 , C07D243/14 , C07D267/02 , C07D267/14 , C07D281/02 , C07D281/10 , C07D285/36 , C07D401/12 , C07D403/12 , C07D409/12 , C07K5/06052 , C07K5/06078 , C07K5/06086 , C07K5/06139 , C07K5/06191
摘要： Benzene-fused heterocycle derivatives of the general formula (I); and nontoxic salts thereof (wherein each symbol is as defined in the description). The compounds of the general formula (I) exhibit inhibitory activities against cysteine proteases and are useful as preventive and/or therapeutic drugs for immunopathy (such as autoimmune diseases and infectious diseases), inflammatory diseases (such as inflammatory diseases of intestine, multiple encephalosclerosis, and arthritis), nerve degeneration diseases (such as Alzheimer's disease and muscular dystrophy), bone resorptive diseases (such as osteoporosis), respiratory diseases, diabetes, shock, and so on.
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8.发明公开COMPOUND HAVING DETRUSOR MUSCLE-CONTRACTING ACTIVITY AND URETHRAL SPHINCTER MUSCLE-RELAXING ACTIVITY 有权的活动而FOR收缩疏散和肌肉与活动松弛HARNRÖHRENSCHLIESSMUSKELS的
公开(公告)号：EP2441760A4
公开(公告)日：2012-12-05
申请号：EP10786192
申请日：2010-06-09
IPC分类号： C07D277/20 , A61K31/426 , A61K45/00 , A61P13/02 , A61P13/10 , A61P43/00 , C07D277/56
CPC分类号： C07D277/56 , A61K31/426 , A61K45/06 , A61K47/6951 , B82Y5/00 , C07D277/20 , C07D277/36 , C08B37/00
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公开(公告)号：EP1707208A4
公开(公告)日：2010-03-17
申请号：EP04819909
申请日：2004-12-02
IPC分类号： A61K31/5575 , A61K31/427 , A61K31/429 , A61K31/559 , C07C405/00 , C07D277/56
CPC分类号： A61K31/5575 , A61K31/427 , A61K31/429 , A61K31/559 , C07C405/00 , C07D277/56
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公开(公告)号：EP1829874A4
公开(公告)日：2010-01-06
申请号：EP05820106
申请日：2005-12-21
IPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61P1/00 , A61P1/04 , A61P1/12
CPC分类号： C07D471/14 , A61K31/4375 , A61K31/438 , A61K45/06 , C07D471/04 , C07D471/10
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