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1. 发明申请

WO0009505A9 NAPHTHYRIDINE DERIVATIVES 审中-公开
标题翻译：萘啶衍生物
公开(公告)号：WO0009505A9
公开(公告)日：2001-03-01
申请号：PCT/JP9904257
申请日：1999-08-05
申请人： SUMITOMO PHARMA , MURAOKA MASAMI , BAN HITOSHI , OHASHI NAOHITO
发明人： MURAOKA MASAMI , BAN HITOSHI , OHASHI NAOHITO
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： Compounds represented by general formula (1), prodrugs thereof or pharmaceutically acceptable salts of the same which are useful as remedies for hyperlipemia and arteriosclerosis because of having an acyl-CoA:cholesterol acyltransferase (ACAT) inhibitory effect, wherein the ring A represents an optionally substituted pyridine ring; Y represents optionally substituted alkyl, etc.; R represents hydrogen, optionally substituted alkyl, etc.; R represents hydrogen or lower alkyl; R represents lower alkyl; and Z represents: 1) -D -Q (wherein D represents a bond, divalent C1-8 hydrocarbyl, etc.; and Q represents hydroxy, carboxy, etc.; or 2) -D -M-E-W (wherein D represents a bond, a divalent C1-8 hydrocarbyl, etc.; M represents oxygen, sulfur, etc.; E represents a bond, divalent C1-8 hydrocarbyl, etc.; and W represents hydroxy, carboxy, etc.
摘要翻译：由通式（1）表示的化合物，其前体药物或其药学上可接受的盐，由于具有酰基辅酶A：胆固醇酰基转移酶（ACAT）抑制作用，可用作高脂血症和动脉硬化的治疗剂，其中环A代表任选地取代的吡啶环; Y表示任选取代的烷基等; R 1表示氢，任选取代的烷基等; R 2表示氢或低级烷基; R 3表示低级烷基; Z表示：1）-D 1 -Q（其中D 1表示键，二价C 1-8烃基等; Q表示羟基，羧基等;或2）-D 2 -MEW（其中D 2表示键，二价C 1-8烃基等; M表示氧，硫等; E表示键，二价C 1-8烃基等; W表示羟基，羧基等

2. 发明申请

WO9907352A3 METHOD FOR PROMOTING EXPRESSION OF LDL RECEPTOR GENE 审中-公开
标题翻译：促进低密度脂蛋白受体基因表达的方法
公开(公告)号：WO9907352A3
公开(公告)日：1999-05-14
申请号：PCT/JP9803595
申请日：1998-08-12
申请人： SUMITOMO PHARMA , TULARIK INC , UENO YOSHIHIDE , MORISHITA KOJI , MURAOKA MASAMI , OHASHI NAOHITO , SHAN BEI
发明人： UENO YOSHIHIDE , MORISHITA KOJI , MURAOKA MASAMI , OHASHI NAOHITO , SHAN BEI
IPC分类号： C07D253/06 , A61K31/53 , A61P3/06 , A61P43/00 , C07D253/07 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14
CPC分类号： C07D253/07 , A61K31/53 , C07D401/04
摘要： Method of promoting expression of LDL receptor gene and an agent therefor, which comprises as an active ingredient a 1,2,4-triazin-5-one derivative of formula (I), wherein R is unsubstituted or substituted phenyl, unsubstituted or substituted heterocycle; R is unsubstituted or substituted phenyl, unsubstituted or substituted naphthyl, unsubstituted or substituted aralkyl, unsubstituted or substituted 5- to 6-membered aromatic heteromonocycle, unsubstituted or substituted C1-C6alkyl, or unsubstituted or substituted C2-C6alkenyl, or pharmaceutically acceptable salt thereof, said active compound (I) increasing the LDL receptor amount by promoting expression of LDL receptor gene (amount of mRNA), by which showing activity of reducing cholesterol level in the blood, and therefore being useful in the prophylaxis or treatment of hyperlipidemia.
摘要翻译：促进LDL受体基因表达的方法及其制剂，其包含作为活性成分的式（I）的1,2,4-三嗪-5-酮衍生物，其中R 1为未取代或取代的苯基，未取代的或取代的杂环; R 2是未取代或取代的苯基，未取代或取代的萘基，未取代或取代的芳烷基，未取代或取代的5至6元芳族杂单环，未取代或取代的C 1 -C 6烷基，或未取代或取代的C 2 -C 6烯基或药学上可接受的其盐，所述活性化合物（I）通过促进LDL受体基因的表达（mRNA的量）增加LDL受体量，通过其显示降低血液中胆固醇水平的活性，因此可用于预防或治疗高脂血症。

3. 发明申请

WO1997030978A1 SULFONYLUREIDOPYRAZOLE DERIVATIVES 审中-公开
标题翻译：硫代吡唑衍生物
公开(公告)号：WO1997030978A1
公开(公告)日：1997-08-28
申请号：PCT/JP1997000532
申请日：1997-02-25
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED , MATSUSHITA, Kayo , HASEGAWA, Hirohiko , KURIBAYASHI, Yoshikazu , OHASHI, Naohito
发明人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
IPC分类号： C07D231/40
CPC分类号： C07D521/00 , C07D231/40 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D417/04
摘要： Sulfonylureidopyrazole derivatives represented by general formula (1) or (2). Because of having inhibitory effects on endothelin converter enzyme, these compounds are useful in the prevention and treatment of various circulatory diseases, bronchial contraction, nervous disorders, hyposecretion, vascular lesions, various ulcers, etc.
摘要翻译：由通式（1）或（2）表示的磺酰脲基吡唑衍生物。由于对内皮素转化酶具有抑制作用，这些化合物可用于预防和治疗各种循环系统疾病，支气管收缩，神经障碍，分泌不良，血管病变，各种溃疡等。

4. 发明申请

WO1996038445A1 NOVEL NAPHTHYRIDINE DERIVATIVES 审中-公开
标题翻译：新型萘啶衍生物
公开(公告)号：WO1996038445A1
公开(公告)日：1996-12-05
申请号：PCT/JP1996001429
申请日：1996-05-28
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED , MURAOKA, Masami , IORIYA, Katsuhisa , OHASHI, Naohito
发明人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Naphthyridine derivatives represented by general formula (1) and acid-addition salts thereof, having the activity of inhibiting acyl CoA: cholesterol acyltransferases, and useful for preventing and treating hyperlipemia, arteriosclerosis and related diseases. In said formula, ring A represents an optionally substituted pyridine ring; X represents -NR -CO-; R represents hydrogen, alkyl, substituted alkyl, etc.; Z represents a bond, -NH-, C1-C2 alkylene, or -CH=CH-; Y represents alkyl, substituted alkyl, aryl, substituted aryl, etc.; and B represents alkyl, substituted alkyl, aryl, substituted aryl, etc.
摘要翻译：具有抑制酰基CoA：胆固醇酰基转移酶活性的通式（1）表示的萘啶衍生物及其酸加成盐，可用于预防和治疗高脂血症，动脉硬化及相关疾病。在所述式中，环A表示任选取代的吡啶环; X代表-NR 2 -CO-; R 2表示氢，烷基，取代的烷基等; Z表示键，-NH-，C 1 -C 2亚烷基或-CH = CH-; Y表示烷基，取代的烷基，芳基，取代的芳基等; B代表烷基，取代烷基，芳基，取代芳基等

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