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公开(公告)号:US20080070928A1
公开(公告)日:2008-03-20
申请号:US10582564
申请日:2004-12-28
申请人: Katsumasa Nonoshita , Makoto Ishikawa , Hiroshi Nakashima , Daisuke Tsukahara , Yoshio Ogino , Fumiko Sakai , Yoshikazu Nagae , Keisuke Arakawa , Teruyuki Nishimura , Jun-Ichi Eiki
发明人: Katsumasa Nonoshita , Makoto Ishikawa , Hiroshi Nakashima , Daisuke Tsukahara , Yoshio Ogino , Fumiko Sakai , Yoshikazu Nagae , Keisuke Arakawa , Teruyuki Nishimura , Jun-Ichi Eiki
IPC分类号: A61K31/497 , A61K31/4184 , A61K31/422 , A61K31/4245 , A61K31/427 , A61P3/04 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/02 , C07D413/02 , C07D403/02 , A61P3/10 , A61K31/506 , A61K31/433 , A61K31/4439 , A61K31/444
CPC分类号: C07D401/14 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/14 , C07D417/04
摘要: A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided.A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II): (in the formula, X represents a carbon atom or a nitrogen atom); R1 represents an aryl, etc.; R2 represents a hydroxy, etc.; R3 represents a —C1-6 alkyl, etc.; R4 represents a —C1-6 alkyl, etc.; X5 represents —O—, etc.; a indicates an integer of 1, 2 or 3; q indicates an integer of from 0 to 2; m indicates an integer of from 0 to 2].
摘要翻译: 提供葡糖激酶活化剂; 提供了糖尿病的补救措施和/或预防,糖尿病的补救和/或预防,如视网膜病变,肾病,神经症,缺血性心脏病,动脉硬化,以及进一步的补救措施和/或预防肥胖症。 一种葡糖激酶活化剂,其特征在于含有通式(I-0)的2-杂芳基取代的苯并咪唑衍生物或其药学上可接受的盐:[式中X表示碳原子或氮原子; X 1,X 2,X 3和X 4各自独立地表示碳原子或氮原子; 环A表示式(II)的5-或6-元含氮芳族杂环:(式中,X表示碳原子或氮原子); R 1表示芳基等; R 2表示羟基等; R 3表示-C 1-6烷基等; R 4表示-C 1-6烷基等; X 5表示-O-等; a表示1,2或3的整数; q表示0〜2的整数, m表示0〜2的整数]。
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公开(公告)号:US07728025B2
公开(公告)日:2010-06-01
申请号:US10582564
申请日:2004-12-28
申请人: Katsumasa Nonoshita , Makoto Ishikawa , Hiroshi Nakashima , Daisuke Tsukahara , Yoshio Ogino , Fumiko Sakai , Yoshikazu Nagae , Keisuke Arakawa , Teruyuki Nishimura
发明人: Katsumasa Nonoshita , Makoto Ishikawa , Hiroshi Nakashima , Daisuke Tsukahara , Yoshio Ogino , Fumiko Sakai , Yoshikazu Nagae , Keisuke Arakawa , Teruyuki Nishimura
IPC分类号: A01N43/50
CPC分类号: C07D401/14 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/14 , C07D417/04
摘要: A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided.A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II): (in the formula, X represents a carbon atom or a nitrogen atom); R1 represents an aryl, etc.; R2 represents a hydroxy, etc.; R3 represents a —C1-6 alkyl, etc.; R4 represents a —C1-6 alkyl, etc.; X5 represents —O—, etc.; a indicates an integer of 1, 2 or 3; q indicates an integer of from 0 to 2; m indicates an integer of from 0 to 2].
摘要翻译: 提供葡糖激酶活化剂; 提供了糖尿病的补救措施和/或预防,糖尿病的补救和/或预防,如视网膜病变,肾病,神经症,缺血性心脏病,动脉硬化,以及进一步的补救措施和/或预防肥胖症。 一种葡糖激酶活化剂,其特征在于含有通式(I-0)的2-杂芳基取代的苯并咪唑衍生物或其药学上可接受的盐:[式中X表示碳原子或氮原子; X1,X2,X3和X4各自独立地表示碳原子或氮原子; 环A表示式(II)的5-或6-元含氮芳族杂环:(式中,X表示碳原子或氮原子); R1表示芳基等。 R2代表羟基等; R3代表-C 1-6烷基等; R4代表-C 1-6烷基等; X5表示-O-等。 a表示1,2或3的整数; q表示0〜2的整数, m表示0〜2的整数]。
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公开(公告)号:US20060205750A1
公开(公告)日:2006-09-14
申请号:US11431274
申请日:2006-05-10
申请人: Norikazu Otake , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
发明人: Norikazu Otake , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
IPC分类号: A61K31/4747 , A61K31/4184 , C07D487/10
CPC分类号: C07D473/30 , C07D405/04 , C07D471/04 , C07D471/10 , C07D473/00 , C07D491/04
摘要: The present invention relates to a compound of the formula (I): (wherein A, B, C and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is —N(SO2R4)—, —N(COR5)— or —CO—; Y is —C(R6)(R7)—, —O— or —N(R8)—, provided that the compound (I) when E is nitrogen, n is 0, X is —CO—, and Y is —O— is excluded) and the like, which are useful as an agent for the treatment of various diseases related to NPY, for example cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorder, inflammatory diseases or glaucoma, and the like, also for example, atherosclerosis, hypogonadism, hyperandrogenism, polycystic ovary syndrome (Pickwickian syndrome), hirsutism, gastro-intestinal motility disorder, obesity-related gastro-esophageal reflux, obesity hypoventilation, sleep apnea, inflammation, systemic inflammation of the vasculature, osteoarthritis, insulin resistance, bronchoconstriction, alcohol preference, metabolic syndrome, Alzheimer's disease, cardiac hypertrophy, left ventricular hypertrophy, hypertriglyceridemia, low HDL cholesterol, cardiovascular disorders such as coronary heart disease (CHD), cerebrovascular disease, stroke, peripheral vascular disease, sudden death, gallbladder diseases, cancer (breast, endometrial, colon), breathlessness, hyperuricemia, impaired fertility, low back pain, or increased anesthetic risk, and the like.
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公开(公告)号:US20100048600A1
公开(公告)日:2010-02-25
申请号:US12605503
申请日:2009-10-26
申请人: NORIKAZU OTAKE , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
发明人: NORIKAZU OTAKE , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
IPC分类号: A61K31/438 , C07D401/04 , C07D401/14 , A61P3/10
CPC分类号: C07D473/30 , C07D405/04 , C07D471/04 , C07D471/10 , C07D473/00 , C07D491/04
摘要: The present invention relates to a compound of the formula (I): (wherein A, B, C and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is —N(SO2R4)—, —N(COR5)— or —CO—; Y is —C(R6)(R7)—, —O— or —N(R8)—, provided that the compound (I) when E is nitrogen, n is 0, X is —CO—, and Y is —O— is excluded) and the like, which are useful as an agent for the treatment of various diseases related to NPY, for example cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorder, inflammatory diseases or glaucoma, and the like, also for example, atherosclerosis, hypogonadism, hyperandrogenism, polycystic ovary syndrome (Pickwickian syndrome), hirsutism, gastro-intestinal motility disorder, obesity-related gastro-esophageal reflux, obesity hypoventilation, sleep apnea, inflammation, systemic inflammation of the vasculature, osteoarthritis, insulin resistance, bronchoconstriction, alcohol preference, metabolic syndrome, Alzheimer's disease, cardiac hypertrophy, left ventricular hypertrophy, hypertriglyceridemia, low HDL cholesterol, cardiovascular disorders such as coronary heart disease (CHD), cerebrovascular disease, stroke, peripheral vascular disease, sudden death, gallbladder diseases, cancer (breast, endometrial, colon), breathlessness, hyperuricemia, impaired fertility, low back pain, or increased anesthetic risk, and the like.
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公开(公告)号:US07803807B2
公开(公告)日:2010-09-28
申请号:US12605503
申请日:2009-10-26
申请人: Norikazu Otake , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
发明人: Norikazu Otake , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
IPC分类号: A61K31/438 , C07D401/14 , A61P3/10
CPC分类号: C07D473/30 , C07D405/04 , C07D471/04 , C07D471/10 , C07D473/00 , C07D491/04
摘要: The present invention relates to compounds of Formula (I) wherein A, B and C are independently methine, said methine being optionally substituted; D is nitrogen; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted and least two of T, U, V and W are said methine groups; X is —N(SO2R4)—, N(COR5)— or —CO—; Y is C(R6)(R7)—, —O— or —N(R8) and a pharmaceutically acceptable salt, ester or N-oxide derivative thereof.
摘要翻译: 本发明涉及式(I)的化合物,其中A,B和C独立地为次甲基,所述次甲基任选被取代; D是氮; T,U,V和W独立地是次甲基或氮,所述次甲基任选被取代,T,U,V和W中的至少两个是所述次甲基; X是-N(SO 2 R 4) - ,N(COR 5) - 或-CO-; Y是C(R6)(R7) - , - O-或-N(R8)及其药学上可接受的盐,酯或N-氧化物衍生物。
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公开(公告)号:US07687514B2
公开(公告)日:2010-03-30
申请号:US11431274
申请日:2006-05-10
申请人: Norikazu Otake , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
发明人: Norikazu Otake , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
IPC分类号: A61K31/4747 , C07D221/20
CPC分类号: C07D473/30 , C07D405/04 , C07D471/04 , C07D471/10 , C07D473/00 , C07D491/04
摘要: The present invention relates to a compound of the formula (I): (wherein A, B, C and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is —N(SO2R4)—, —N(COR5)— or —CO—; Y is —C(R6)(R7)—, —O— or —N(R8)—, provided that the compound (I) when E is nitrogen, n is 0, X is —CO—, and Y is —O— is excluded) and the like, which are useful as an agent for the treatment of various diseases related to NPY.
摘要翻译: 本发明涉及式(I)化合物:其中A,B,C和D独立地为氮或任选取代的次甲基; E为氮,次甲基或羟基取代的次甲基; n为0或1; T,U ,V和W独立地为氮或任选取代的次甲基; X为-N(SO2R4) - , - N(COR5) - 或-CO-; Y为-C(R6)(R7) - , - O-或-N (R8) - ,条件是当E为氮时的化合物(I),n为0,X为-CO-,Y为-O-时除外)等,其可用作治疗 与NPY相关的各种疾病。
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公开(公告)号:US07105526B2
公开(公告)日:2006-09-12
申请号:US10463390
申请日:2003-06-18
申请人: Norikazu Otake , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
发明人: Norikazu Otake , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
IPC分类号: A61K31/52 , C07D239/70
CPC分类号: C07D473/30 , C07D405/04 , C07D471/04 , C07D471/10 , C07D473/00 , C07D491/04
摘要: The present invention relates to novel benzimidazole derivatives which are useful as neuropeptide Y receptor antagonists.
摘要翻译: 本发明涉及可用作神经肽Y受体拮抗剂的新型苯并咪唑衍生物。
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公开(公告)号:US20130149525A1
公开(公告)日:2013-06-13
申请号:US13637184
申请日:2011-03-10
申请人: Yoshikazu Nagae , Junya Satou , Shiro Imai
发明人: Yoshikazu Nagae , Junya Satou , Shiro Imai
IPC分类号: C09D125/08
CPC分类号: C09D125/08 , C08L9/06 , C09J7/243 , C09J7/29 , C09J7/387 , C09J2201/162 , C09J2423/006 , C09J2423/106 , C09J2427/006 , C09J2453/00 , Y10T428/25 , Y10T428/2848 , Y10T428/2878 , C08L2666/06
摘要: A surface protection film has moderate adhesive properties for bonding to adherend bodies with a rough surface, a rear surface with good slipping properties, and blocking resistance and good unwinding properties. The surface protection film has a laminated structure formed at least of an adhesive layer and a back layer, wherein the adhesive layer is formed mainly of a styrene-based elastomer while the back layer is formed mainly of a propylene-based resin containing 0.5 wt % to 10 wt % of a fluorine-containing compound having a polyfluorohydrocarbon group and a polyoxy ethylene group.
摘要翻译: 表面保护膜具有适度的粘合性能,用于粘合具有粗糙表面的被粘物体,具有良好滑动性能的后表面,以及耐粘连性和良好的退绕性能。 表面保护膜具有至少形成有粘合剂层和背层的叠层结构,其中粘合剂层主要由苯乙烯基弹性体形成,而背层主要由含有0.5重量%的丙烯类树脂形成, 至10重量%的具有多氟烃基和聚氧乙烯基的含氟化合物。
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公开(公告)号:US20130011614A1
公开(公告)日:2013-01-10
申请号:US13637518
申请日:2011-03-10
申请人: Yoshikazu Nagae , Junya Satou , Miyuki Tokumaru , Shiro Imai
发明人: Yoshikazu Nagae , Junya Satou , Miyuki Tokumaru , Shiro Imai
CPC分类号: B32B27/08 , B32B27/20 , B32B27/302 , B32B27/308 , B32B27/32 , B32B2250/03 , B32B2270/00 , B32B2272/00 , B32B2274/00 , B32B2307/538 , B32B2307/72 , B32B2307/746 , B32B2307/748 , B32B2457/20 , Y10T428/24355 , Y10T428/24372
摘要: A surface protection film has moderate adhesive properties for adherend bodies with a rough surface, has a rear surface with good slipping properties, and blocking resistance and good unwinding properties (decreased unwinding tension to enable easy, high-speed sticking of the film to an adherend without causing creases or flaws). The surface protection film has a three-layered composite structure including an adhesive layer, an interlayer, and a back layer, wherein the adhesive layer is formed of 35 to 90 wt % of a linear low density polyethylene, 5 to 50 wt % of a styrene-based elastomer, and 15 wt % or less of a tackifier, the interlayer formed mainly of a propylene-based resin, and the back layer formed mainly of the same propylene-based resin as that constituting the interlayer and/or a different propylene-based resin therefrom, and also wherein the back layer has a surface roughness of 3 μm or more in terms of ten-point average roughness (Rz).
摘要翻译: 表面保护膜对于具有粗糙表面的被粘物体具有适度的粘合性能,具有良好的滑动性能的后表面,并且具有抗粘连性和良好的退绕性能(降低退绕张力以使膜容易地高速粘贴到被粘物上 而不会引起折痕或缺陷)。 表面保护膜具有包括粘合剂层,中间层和背层的三层复合结构,其中粘合剂层由线形低密度聚乙烯的35至90重量%,和5-50重量%的 苯乙烯系弹性体和15重量%以下的增粘剂,主要由丙烯系树脂形成的中间层和主要由与构成中间层的丙烯系树脂相同的丙烯类树脂和/或不同的丙烯 的树脂,并且其中背层以十点平均粗糙度(Rz)表示的表面粗糙度为3μm以上。
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