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1. 发明申请

US20100249146A1 HETEROARYLOXY QUINAZOLINE DERIVATIVE 有权
标题翻译：杂环喹啉衍生物
公开(公告)号：US20100249146A1
公开(公告)日：2010-09-30
申请号：US12742113
申请日：2008-11-10
申请人： Tomoharu Iino , Akio Ohno , Norikazu Otake , Takuya Suga , Masanori Asia
发明人： Tomoharu Iino , Akio Ohno , Norikazu Otake , Takuya Suga , Masanori Asia
IPC分类号： A61K31/517 , C07D401/14 , C07D403/14 , A61P3/10
CPC分类号： C07D401/14 , A61K31/517 , A61K38/28 , C07D403/14 , C07D417/14 , C07D513/04 , A61K2300/00
摘要： Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其具有葡糖激酶活化的作用，并且可用于治疗糖尿病，肥胖症等的药物领域（其中环A表示任选具有较低的烷基等;环B表示杂芳基; R表示低级烷基等; R 1表示下式的基团：（其中R 11和R 12各自独立地表示氢原子等; m表示整数 2〜6）等; R2表示低级烷基等; r表示0〜3的整数，k表示0〜4的整数）。

2. 发明授权

US08232284B2 Heteroaryloxy quinazoline derivative 有权
标题翻译：杂芳氧基喹唑啉衍生物
公开(公告)号：US08232284B2
公开(公告)日：2012-07-31
申请号：US12742113
申请日：2008-11-10
申请人： Tomoharu Iino , Akio Ohno , Norikazu Otake , Takuya Suga , Masanori Asai
发明人： Tomoharu Iino , Akio Ohno , Norikazu Otake , Takuya Suga , Masanori Asai
IPC分类号： A61K31/517
CPC分类号： C07D401/14 , A61K31/517 , A61K38/28 , C07D403/14 , C07D417/14 , C07D513/04 , A61K2300/00
摘要： Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其具有葡糖激酶活化的作用，并且可用于治疗糖尿病，肥胖症等的药物领域（其中环A表示任选具有较低的烷基等;环B表示杂芳基; R表示低级烷基等; R 1表示下式的基团：（其中R 11和R 12各自独立地表示氢原子等; m表示整数 2〜6）等; R2表示低级烷基等; r表示0〜3的整数，k表示0〜4的整数）。

3. 发明申请

US20100216758A1 Pyridone Compounds 审中-公开
标题翻译：吡啶酮化合物
公开(公告)号：US20100216758A1
公开(公告)日：2010-08-26
申请号：US11989876
申请日：2006-08-03
申请人： Makoto Ando , Etsuko Sekino , Yuji Haga , Norikazu Otake , Minoru Moriya
发明人： Makoto Ando , Etsuko Sekino , Yuji Haga , Norikazu Otake , Minoru Moriya
IPC分类号： A61K31/397 , C07D401/02 , A61K31/4439 , C07D213/04 , A61K31/44 , C07D401/14 , A61K31/444 , C07D239/36 , A61K31/513 , C07D213/89 , C07D403/14 , A61K31/55 , C07D211/94 , A61K31/4545 , C07D221/24 , A61P3/00 , A61P5/00 , A61P9/00 , A61P11/00 , A61P15/00 , A61P1/00 , A61P13/00 , A61P25/00 , A61P35/00
CPC分类号： C07D213/69 , C07D213/64 , C07D213/89 , C07D239/52 , C07D401/10 , C07D401/14 , C07D405/10 , C07D487/08
摘要： An active ingredient is a compound represented by the general formula [I]: [wherein R1 and R2 represent a lower alkyl group, a C3-6 cycloalkyl group or the like, X1 and X2 represent methine, an Ar—Y1—Y2—Y3-substituted methine or the like, however either of them is an Ar—Y1—Y2—Y3-substituted methine, X3 to X8 represent methine, —N— or the like, Y1 and Y3 represent a single bond, —O— or the like, Y2 represent a single bond, a lower alkylene group or the like, W represent —(O)—(CH2)n-(O)— or the like, n represents an integer of 1 to 4, L and Z2 represent a single bond or a methylene group, Z1 represents a single bond, a C1-4 alkylene group or the like, and Ar represents an aromatic carbocyclic group or the like]. The compound acts as a melanin-concentrating hormone receptor antagonist and useful as a therapeutic agent for obesity or the like.
摘要翻译：活性成分是由通式[I]表示的化合物：[其中R1和R2表示低级烷基，C3-6环烷基等，X1和X2表示次甲基，Ar-Y1-Y2-Y3 - 取代的次甲基等，但是它们都是Ar-Y1-Y2-Y3-取代的次甲基，X3至X8表示次甲基，-N-等，Y1和Y3表示单键，-O-或类似的，Y2表示单键，低级亚烷基等，W表示 - （O） - （CH2）n-（O） - 等，n表示1〜4的整数，L和Z2表示单键或亚甲基，Z1表示单键，C1-4亚烷基等，Ar表示芳香族碳环基等]。该化合物作为黑色素浓缩激素受体拮抗剂起作为肥胖症等的治疗剂的作用。

4. 发明申请

US20070129397A1 Ester derivatives 失效
标题翻译：酯衍生物
公开(公告)号：US20070129397A1
公开(公告)日：2007-06-07
申请号：US11648614
申请日：2007-01-03
申请人： Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
发明人： Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号： A61K31/46 , C07D451/00 , C07D211/34 , A61K31/445 , A61K31/40 , C07D207/04
CPC分类号： C07D207/08 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10
摘要： This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X−signifies an anion].
摘要翻译：本发明涉及具有选择性毒蕈碱M 3受体拮抗作用，副作用小，适用于吸入治疗的化合物，并且可用作通式（I）的呼吸系统疾病的治疗剂; [其中A表示由式（a 0 ）或（b 0>）表示的组; Ar表示任选取代的芳基或杂芳基; B 1和B 2表示脂族烃; R 1表示氟取代的环烷基; R 2，R 3和R 4表示低级烷基，单键或与B 1连接的亚烷基，或 R 2和R 3结合起来表示亚烷基; R 5和R 7表示氢，低级烷基或键合到B 2的单键或亚烷基; R 6表示氢，低级烷基或以-N（R 8）R 9表示的基团; 和X - 表示阴离子]。

5. 发明授权

US06251891B1 Carbapenem derivatives 失效
标题翻译：卡巴培南衍生物
公开(公告)号：US06251891B1
公开(公告)日：2001-06-26
申请号：US09294091
申请日：1999-04-19
申请人： Susumu Nakagawa , Norikazu Otake , Hideo Kiyonaga , Koji Yamada , Hideki Jona , Shigemitsu Okada , Masayuki Ogawa , Hideaki Imamura , Ryosuke Ushijima
发明人： Susumu Nakagawa , Norikazu Otake , Hideo Kiyonaga , Koji Yamada , Hideki Jona , Shigemitsu Okada , Masayuki Ogawa , Hideaki Imamura , Ryosuke Ushijima
IPC分类号： C07D47720
CPC分类号： C07D477/20
摘要： A compound represented by the general formula wherein R1 either represents a hydrogen atom or a lower alkyl group, R2 represents a hydrogen atom, an ester residue, an alkali metal or negative charge, and R3 and R4 are the same or different, and each represent a hydrogen atom or a hydrocarbonic group optionally containing hetero atom(s) selected from the group consisting of oxygen atom(s), sulfur atom(s) and nitrogen atom(s), or they are combined together with the nitrogen atom to which they bound to form a heterocyclic group, and the use thereof as an antibacterial agent.
摘要翻译：由通式化合物R1表示的化合物表示氢原子或低级烷基，R2表示氢原子，酯残基，碱金属或负电荷，R3和R4相同或不同，分别表示氢原子或任选含有选自氧原子，硫原子和氮原子的杂原子的烃基，或它们与它们所结合的氮原子结合在一起形成杂环基，其用作抗菌剂。

6. 发明授权

US5061794A Cephalosporin derivatives, and antibacterial agents 失效
标题翻译： CEPHALOSPORIN衍生物和抗菌剂
公开(公告)号：US5061794A
公开(公告)日：1991-10-29
申请号：US377086
申请日：1989-07-10
申请人： Susumu Nakagawa , Koji Yamada , Fumio Nakano , Norikazu Otake , Akira Asai , Satoru Kuroyanagi , Yoshiharu Tanaka , Moriaki Ishikawa , Ryosuke Ushijima , Ryuji Mitomo
发明人： Susumu Nakagawa , Koji Yamada , Fumio Nakano , Norikazu Otake , Akira Asai , Satoru Kuroyanagi , Yoshiharu Tanaka , Moriaki Ishikawa , Ryosuke Ushijima , Ryuji Mitomo
IPC分类号： C07D235/28 , C07D263/46 , C07D263/58 , C07D271/10 , C07D271/113 , C07D277/20 , C07D277/36 , C07D277/56 , C07D285/12 , C07D285/125 , C07D501/36
CPC分类号： C07D263/58 , C07D235/28 , C07D263/46 , C07D271/113 , C07D277/36 , C07D277/56 , C07D277/587 , C07D285/125
摘要： A compound having the formula: ##STR1## wherein R is a straight chain or branched chain lower alkyl, cyclic lower alkyl, lower alkenyl (except for 1-carboxy-1-vinyl), lower alkynyl, aralkyl, phenyl or 2-pyrrolidon-3-yl group which may be substituted, and Q is ##STR2## (wherein R.sup.1 is a hydrogen atom or an acetyl group, R.sup.2 is a hydrogen atom, a carboxyl group or a carboxymethyl group, Y is a sulfur atom or an oxygen atom, Z is a sulfur atom, an oxygen atom or an imino group which may be substituted by a lower alkyl group); or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.
摘要翻译：具有下式的化合物：其中R是直链或支链的低级烷基，环状低级烷基，低级烯基（1-羧基-1-乙烯基），低级炔基，芳烷基，苯基或2 可以被取代的吡咯烷酮-3-基，Q是氢原子或乙酰基，R2是氢原子，羧基或羧甲基， Y是硫原子或氧原子，Z是硫原子，氧原子或可被低级烷基取代的亚氨基）; 或其药学上可接受的盐，生理上可水解的酯或其溶剂合物。

7. 发明授权

US07875633B2 Phenylpyridone derivative 失效
标题翻译：苯基吡啶酮衍生物
公开(公告)号：US07875633B2
公开(公告)日：2011-01-25
申请号：US11990889
申请日：2006-08-23
申请人： Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
发明人： Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
IPC分类号： A61K31/444 , A61K31/4439 , A61K31/5377 , A61K31/4545 , A61P9/00 , A61P25/00 , A61P3/00 , C07D213/64 , C07D401/02 , C07D413/02 , C07D401/14
CPC分类号： C07D213/69 , C07D213/64 , C07D401/10 , C07D413/10
摘要： A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents —CH2—O—, —CH═CH— or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
摘要翻译：作为活性成分，含有式（I）所示的化合物：其中，R 1和R 2分别独立地表示氢原子，低级烷基等，或者与连接有L，Z 2和R 1的氮原子一起形成可以形成脂族氮杂环基，并且R 1和R 2与它们所连接的氮原子一起形成脂族氮杂环基; X表示次甲基或氮原子; Y表示-CH 2 -O-，-CH = CH-等; Z1表示单键，C1-4亚烷基等; Z2表示单键或C1-4亚烷基; L表示亚甲基，C3-8亚环烷基等; Ar表示芳族碳环基等。该化合物可用作中枢神经系统疾病，心血管疾病或代谢疾病的药物。

8. 发明授权

US07452908B2 Amide derivatives 失效
标题翻译：酰胺衍生物
公开(公告)号：US07452908B2
公开(公告)日：2008-11-18
申请号：US10838340
申请日：2004-05-05
申请人： Yufu Sagara , Minaho Uchiyama , Akira Naya , Toshifumi Kimura , Tomoshige Numazawa , Toru Fujikawa , Norikazu Otake , Kazuhito Noguchi
发明人： Yufu Sagara , Minaho Uchiyama , Akira Naya , Toshifumi Kimura , Tomoshige Numazawa , Toru Fujikawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号： A61K31/445 , C07D211/32
CPC分类号： C07D401/12 , C07D207/16 , C07D211/26 , C07D401/14 , C07D471/10 , C07D493/10
摘要： This invention relates to compounds which are represented by the general formula [I] [in which A stands for a group of the following formula [ao] or [b0] Ar1, Ar2 and Ar3 stand for optionally substituted phenyl; k stands for 0 or 1; m, n and s stand for 0, 1 or 2; R1 stands for hydrogen or optionally substituted lower alkyl; R2, R3, R4 and R5 either stand for hydrogen or optionally substituted lower alkyl, or R2 and R3, or R4 and R5 together stand for trimethylene and the like; R60 stands for hydrogen, alkyl, or the like; R61 and R71 either stand for alkyl and the like, or together stand for trimethylene and the like; X stands for carbonyl or methylene; Y stands for nitrogen or methine; and Q− stands for anion], and the like. The compounds of the invention exhibit selective antagonism to muscarinic M3 receptors, and therefore are useful as safe and effective agents showing little side effect, for treating diseases of the respiratory, urinary and digestive systems.
摘要翻译：本发明涉及由通式[I]表示的化合物[其中A代表下列通式[a]或[b] 0 Ar 1，Ar 2和Ar 3代表任选取代的苯基; k代表0或1; m，n和s代表0,1或2; R 1表示氢或任选取代的低级烷基; R 2，R 3，R 4和R 5均代表氢或任选取代的低级烷基，或 R 2和R 3，或R 4和R 5一起代表三亚甲基等; R 60代表氢，烷基等; R 61和R 71均代表烷基等，或一起代表三亚甲基等; X代表羰基或亚甲基; Y代表氮或次甲基; 和Q ^{代表阴离子]等。本发明的化合物对毒蕈碱M 3受体表现出选择性拮抗作用，因此可用作治疗呼吸，泌尿和消化系统疾病的副作用小的安全有效的药剂。}

9. 发明申请

US20060111380A1 Novel azole derivatives 失效
标题翻译：新型唑衍生物
公开(公告)号：US20060111380A1
公开(公告)日：2006-05-25
申请号：US10536360
申请日：2003-11-25
申请人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
发明人： Norikazu Otake , Yuji Haga , Makoto Jitsuoka , Akio Kanatani
IPC分类号： A61K31/4747 , C07D471/10
CPC分类号： C07D491/10
摘要： The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
摘要翻译：本发明涉及式（I）化合物：其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T，U，V和W独立为次甲基或氮，所述次甲基任选被取代基取代，T，U，V和W中的至少两个为所述次甲基; X是氮或次甲基。本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，神经系统疾病，基因疾病，代谢疾病，生殖器或生殖障碍，胃肠道疾病，呼吸系统疾病，炎症性疾病疾病或青光眼等。

10. 发明授权

US06809108B1 Amide derivatives 失效
标题翻译：酰胺衍生物
公开(公告)号：US06809108B1
公开(公告)日：2004-10-26
申请号：US10031716
申请日：2002-03-26
申请人： Yufu Sagara , Minaho Uchiyama , Akira Naya , Toshifumi Kimura , Tomoshige Numazawa , Toru Fujikawa , Norikazu Otake , Kazuhito Noguchi
发明人： Yufu Sagara , Minaho Uchiyama , Akira Naya , Toshifumi Kimura , Tomoshige Numazawa , Toru Fujikawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号： A61K31445
CPC分类号： C07D401/12 , C07D207/16 , C07D211/26 , C07D401/14 , C07D471/10 , C07D493/10
摘要： This invention relates to compounds which are represented by the general formula [I] [in which A stands for a group of the following formula [a0] or [b0] Ar1, Ar2 and Ar3 stand for optionally substituted phenyl; k stands for 0 or 1; m, n and a stand for 0, 1 or 2; R1 stands for hydrogen or optionally substituted lower alkyl; R2, R3, R4 and R5 either stand for hydrogen or optionally substituted lower alkyl, or R2 and R3, or R4 and R5 together stand for trimethylene and the like; R60 stands for hydrogen, alkyl, or the like; R61 and R71 either stand for alkyl and the like, or together stand for trimethylene and the like; X stands for carbonyl or methylene; Y stands for nitrogen or methine; and Q− stands for anion], and the like. The compounds of the invention exhibit selective antagonism to muscarinic M3 receptors, and therefore are useful as safe and effective agents showing little side effect, for treating diseases of the respiratory, urinary and digestive systems.
摘要翻译：本发明涉及由通式[I]表示的化合物[其中A代表下式[a0]或[b0] Ar 1的基团，Ar 2和Ar 3代表任选取代的苯基; k代表0或1; m，n和a代表0,1或2; R 1代表氢或任选取代的低级烷基; R 2，R 3，R 4和R 5分别代表氢或任选取代的低级烷基，或者R 2和R 3，或R 4和R 5，一起代表三亚甲基等; R 60代表氢，烷基等; R 61和R 71代表烷基等，或一起代表三亚甲基等; X代表羰基或亚甲基; Y代表氮或次甲基; 并且Q 1表示阴离子]等。本发明的化合物对毒蕈碱性M3受体表现出选择性拮抗作用，因此可用作治疗副作用小的安全有效药物，用于治疗呼吸道，尿和尿的疾病消化系统。

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