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51. 发明申请

US20060178375A1 Heteroaryloxy nitrogenous saturated heterocyclic derivative 有权
标题翻译：杂环氧基含氮饱和杂环衍生物
公开(公告)号：US20060178375A1
公开(公告)日：2006-08-10
申请号：US10561115
申请日：2004-06-24
申请人： Norikazu Ohtake , Akira Naya , Yuji Haga , Makoto Jitsuoka , Takuya Suga , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani
发明人： Norikazu Ohtake , Akira Naya , Yuji Haga , Makoto Jitsuoka , Takuya Suga , Ryo Yoshimoto , Shigeru Tokita , Akio Kanatani
IPC分类号： A61K31/506 , C07D413/14 , C07D403/14
CPC分类号： C07D401/12 , A61K31/4545 , A61K31/501 , A61K31/506 , C07D401/14 , C07D403/12 , C07D413/14 , C07D471/04
摘要： Compound of the formula: (I) [wherein each of X1, X2, and X3 independently represents N or CH, W represents the formula (II):(II) or the formula (III):(III) and Y represents a group of the formula (IV):(IV)], or a pharmacologically acceptable salt thereof. This compound exhibits histamine receptor H3 antagonist or inverse agonist activity and is useful of the treatment and/or prevention of obesity, diabetes, hormonal secretion abnormality, sleep, disorder, etc.
摘要翻译：式（I）的化合物[其中X 1，X 2和X 3各自独立地表示N或CH，W表示式（II）：（II）或式（III）：III），Y表示式（IV）：（IV）]的基团，或其药理学上可接受的盐。该化合物显示组胺受体H3拮抗剂或反向激动剂活性，并且可用于治疗和/或预防肥胖症，糖尿病，激素分泌异常，睡眠，障碍等。

52. 发明申请

US20050222161A1 Antagonists to melanin-concentrating hormone receptor comprising benzimidazole derivative as active ingredient 失效
标题翻译：黑色素浓缩激素受体的拮抗剂，其包含苯并咪唑衍生物作为活性成分
公开(公告)号：US20050222161A1
公开(公告)日：2005-10-06
申请号：US10522718
申请日：2003-07-29
申请人： Minoru Moriya , Akio Kanatani , Hisashi Iwaasa , Akane Ishihara , Takehiro Fukami
发明人： Minoru Moriya , Akio Kanatani , Hisashi Iwaasa , Akane Ishihara , Takehiro Fukami
IPC分类号： A61K31/4184 , A61K31/4196 , A61K31/4245 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P1/00 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , C07D235/30 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12
CPC分类号： C07D403/12 , A61K31/4184 , A61K31/4196 , A61K31/4245 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/55 , C07D235/30 , C07D401/04 , C07D401/12 , C07D403/04
摘要： This invention relates to a benzimidazole derivative of the general formula [I] [wherein B1, B2, and B3 represent hydrogen atom or lower alkyl; R1 and R2 are same or different and represent lower alkyl, etc.; R3 and R4 represent hydrogen atom, etc.; W represents a 3 to 8-membered aromatic or alphatic heterocycle, etc.; and Ar represents a substituted or unsubstituted aromatic heterocycle, etc.] This compound functions as an antagonist to melanin-concentrating hormone receptor and is useful as a drug for central diseases, circulatory diseases and metabolic diseases.
摘要翻译：本发明涉及通式[I]的苯并咪唑衍生物[其中B 1，B 2，B 3和B 3表示氢原子或低级烷基 R 1和R 2相同或不同，表示低级烷基等; R 3和R 4代表氢原子等; W表示3至8元芳族或脂肪杂环等; Ar表示取代或未取代的芳族杂环等。]该化合物作为黑色素浓缩激素受体的拮抗剂起作用，可用作中枢疾病，循环系统疾病和代谢性疾病的药物。

53. 发明申请

US20050154025A1 Novel pyridone derivatives 失效
标题翻译：新型吡啶酮衍生物
公开(公告)号：US20050154025A1
公开(公告)日：2005-07-14
申请号：US10505476
申请日：2003-03-14
申请人： Nagaaki Sato , Tsuyoshi Nagase , Keita Nagai , Makoto Ando , Akio Kanatani
发明人： Nagaaki Sato , Tsuyoshi Nagase , Keita Nagai , Makoto Ando , Akio Kanatani
IPC分类号： A61K31/444 , A61P1/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/06 , A61P29/00 , A61P43/00 , C07D401/14 , C07D41/14
CPC分类号： C07D401/14 , A61K31/444
摘要： A compound of the formula (I): wherein R1 is hydrogen, halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy, lower alkoxy or aralkyloxy; R2 and R3 are each independently hydrogen, halogen or halo-lower alkyl; and R4 and R are each independently hydrogen or halogen, is useful as a pharmaceutical composition 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, etc., 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, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
摘要翻译：式（I）的化合物：其中R 1是氢，卤素，氰基，低级烷基，卤代低级烷基，羟基，低级烷氧基或芳烷氧基; R 2和R 3各自独立地为氢，卤素或卤代低级烷基; R 4和R 4各自独立地为氢或卤素，可用作治疗与NPY相关的各种疾病的药物组合物，例如心血管疾病如心绞痛，急性或充血性心力衰竭，心肌梗死，高血压，肾病，电解质异常，血管痉挛等，神经系统疾病如贪食症，抑郁症，焦虑症，癫痫，癫痫，痴呆，疼痛，酒精中毒，药物戒断，昼夜节律紊乱，精神分裂症，记忆障碍，睡眠障碍，认知障碍等，代谢疾病如肥胖，糖尿病，激素异常，痛风，脂肪肝等，生殖器官或生殖障碍如不育症，早产，性功能障碍等，胃肠道疾病，呼吸系统疾病，炎症性疾病或青光眼等。

54. 发明授权

US06869966B2 N-substituted-2-oxodihydropyridine derivatives 失效
标题翻译： N-取代-2-氧代二氢吡啶衍生物
公开(公告)号：US06869966B2
公开(公告)日：2005-03-22
申请号：US10641017
申请日：2003-08-15
申请人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
发明人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
IPC分类号： A61P3/04 , C07D213/80 , C07D401/04 , C07D401/14 , C07D401/02 , A61K31/44 , C07D213/02
CPC分类号： C07D213/80 , C07D401/04 , C07D401/14
摘要： A compound of the formula (I): (wherein Ar1 and Ar2 are independently aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of cyano, halogen, nitro, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl, lower alkenyl, lower alkylamino, di-lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, arylsulfonylamino, hydroxy, lower alkoxy, halo-lower alkoxy, aryloxy, heteroaryloxy, lower alkylthio, carboxyl, formyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, lower alkylsulfonyl, arylsulfonyl, aryl and heteroaryl; R1 and R2 are independently lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl or lower alkoxy, any of which is optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl;R3, R4 and R5 are independently hydrogen, cyano, halogen or hydroxy, or lower alkyl, lower alkoxy or lower alkylthio, the last three groups being optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl), or a salt or ester thereof is useful as a neuropeptide Y receptor antagonist agent and is also useful as an agent for the treatment of bulimia, obesity or diabetes.
摘要翻译：式（I）的化合物（其中Ar 1和Ar 2独立地是芳基或杂芳基，其中任何一个任选被选自氰基，卤素，硝基，低级烷基，卤代低级烷基，羟基 - 低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基，低级烯基，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，低级烷基磺酰基氨基，芳基磺酰基氨基，羟基，低级烷氧基，低级烷氧基，芳氧基，杂芳氧基，低级烷硫基，羧基，甲酰基，低级烷酰基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，二低级烷基氨基甲酰基，低级烷基磺酰基，芳基磺酰基，芳基和杂芳基; R 1和R 2独立地为低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基或低级烷氧基，其中任何一个任选被选自卤素，低级烷基氨基，二低级烷基氨基，低级烷酰氨基，羟基，低级烷氧基，甲酰基，低级烷基氧羰基，低级烷基氨基甲酰基和二低级烷基氨基甲酰基; R 3，R 4和R 5独立地是氢，氰基，卤素或羟基，或低级烷基，低级烷氧基或低级烷硫基，最后三个基团是任选的被选自卤素，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，羟基，低级烷氧基，甲酰基，低级烷氧基羰基，低级烷基氨基甲酰基和二低级烷基氨基甲酰基的取代基取代）或其盐或酯是有用的作为神经肽Y受体拮抗剂，也可用作治疗贪食症，肥胖症或糖尿病的药剂。

55. 发明申请

US20050032820A1 Novel spiro compounds 失效
公开(公告)号：US20050032820A1
公开(公告)日：2005-02-10
申请号：US10922869
申请日：2004-08-23
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh , Masato Chiba
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh , Masato Chiba
IPC分类号： C07D491/107 , A61K31/438 , A61P1/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/06 , A61P29/00 , A61P43/00 , C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10 , C07D519/00 , C07D487/14 , A61K31/4747 , A61K31/519
CPC分类号： C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10
摘要： A Compound represented by the general formula (I): wherein AR1 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of hydroxy, halogen, nitro, lower alkyl, halo(lower)alkyl, hydroxy(lower)alkyl, cyclo(lower)alkyl, lower alkenyl, lower alkoxy, halo(lower)alkoxy, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylene optionally substituted with oxo, and a group represented by the formula —Q—Ar2; Ar2represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, cyano, lower alkyl, halo(lower)alkyl, hydroxy(lower)alkyl, hydroxy, lower alkoxy, halo(lower)alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; n represents 0 or 1; Q represents a single bond or carbonyl; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen; and a salt, ester or N-oxide derivative thereof exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis and the like, central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal and the like, metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia and the like, sexual and reproductive dysfunction, gastro-intestinal disorder, respiratory disorder, inflammation or glaucoma, and the like.

56. 发明授权

US06638942B1 Spiro-indolines as Y5 receptor antagonists 失效
标题翻译：螺吲哚啉作为Y5受体拮抗剂
公开(公告)号：US06638942B1
公开(公告)日：2003-10-28
申请号：US10228250
申请日：2002-08-26
申请人： Ying-Duo Gao , Douglas J. MacNeil , Lihu Yang , Nancy R. Morin , Takehiro Fukami , Akio Kanatani , Takahiro Fukuroda , Yasuyuki Ishii , Masaki Ihara
发明人： Ying-Duo Gao , Douglas J. MacNeil , Lihu Yang , Nancy R. Morin , Takehiro Fukami , Akio Kanatani , Takahiro Fukuroda , Yasuyuki Ishii , Masaki Ihara
IPC分类号： C07D47110
CPC分类号： C07D221/20 , C07D471/10
摘要： Compounds of general structural formula I are selective NPY Y5 receptor antagonists, useful in the treatment of obesity and the complications associated therewith.
摘要翻译：通用结构式的化合物Iare选择性NPY Y5受体拮抗剂，可用于治疗肥胖及其相关并发症。

57. 发明授权

US06462053B1 Spiro compounds 失效
标题翻译：螺环化合物
公开(公告)号：US06462053B1
公开(公告)日：2002-10-08
申请号：US10101221
申请日：2002-03-20
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： A61K34355
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： A method for treating a cardiovascular disorder, which involves administering to a patient in need a therapeutically effective amount of a compound of formula (I): wherein Ar1 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, nitro, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, cyclo(lower) alkyl, lower alkenyl, lower alkoxy, halo(lower) alkoxy, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylene optionally substituted with oxo, and a group represented by the formula —Q—Ar2; Ar2 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, cyano, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, hydroxy, lower alkoxy, halo(lower) alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl: n represents 0 or 1; Q represents a single bond or carbonyl; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine; Y represents an imino which may be substituted with lower alkyl, or oxygen; or a salt or ester thereof.
摘要翻译：一种治疗心血管疾病的方法，其涉及向需要的患者施用治疗有效量的式（I）化合物：其中Ar1表示可被取代的芳基或杂芳基，所述取代基选自卤素，硝基，低级烷基，卤代（低级）烷基，羟基（低级）烷基，环（低级）烷基，低级烯基，低级烷氧基，卤代（低级）烷氧基，低级烷硫基，羧基，低级烷酰基，低级烷氧基羰基，任选被氧代取代的基团和由式-Q-Ar 2表示的基团; Ar 2表示可被取代的芳基或杂芳基，所述取代基选自卤素，氰基，低级烷基，卤代（低级）烷基，羟基（低级）烷基，羟基，低级烷氧基，卤代（低级）烷氧基，低级烷基氨基，二低级烷基氨基，低级烷酰基和芳基：n表示0或1; Q表示单键或羰基; T，U， W各自独立地表示硝基可以具有选自卤素，低级烷基，羟基和低级烷氧基的取代基的次甲基，其中至少两个表示所述次甲基; X表示次甲基; Y表示可以被取代的亚氨基与低级烷基或氧; 或其盐或酯。

58. 发明授权

US6011039A Aminopyridine derivatives 失效
标题翻译：氨基吡啶衍生物
公开(公告)号：US6011039A
公开(公告)日：2000-01-04
申请号：US142162
申请日：1998-10-13
申请人： Takehiro Fukami , Toshiaki Mase , Yoshimi Tsuchiya , Akio Kanatani , Takahiro Fukuroda
发明人： Takehiro Fukami , Toshiaki Mase , Yoshimi Tsuchiya , Akio Kanatani , Takahiro Fukuroda
IPC分类号： C07D213/74 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14 , A61K31/44
CPC分类号： C07D417/06 , C07D213/74 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/12 , C07D417/14
摘要： A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for hyperphagia, obesity or diabetes, which comprises such a compound or salt as an active ingredient: ##STR1## wherein Ar.sup.1, Ar.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and W are as defined.
摘要翻译： PCT No.PCT / JP97 / 00890 Sec。 371日期：1998年10月13日 102（e）日期1998年10月13日PCT 1997年3月19日PCT公布。公开号WO97 / 34873 日期1997年9月25日由式（I）表示的化合物或其药学上可接受的盐，以及包含这样的作为活性成分的化合物或盐的食欲过盛，肥胖或糖尿病的药物组合物，其中Ar1，Ar2，R1 ，R2，R3，R4和W如上所定义。

59. 发明授权

US07960394B2 Quinazoline derivative 失效
标题翻译：喹唑啉衍生物
公开(公告)号：US07960394B2
公开(公告)日：2011-06-14
申请号：US11628087
申请日：2005-05-30
申请人： Takashi Mizutani , Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
发明人： Takashi Mizutani , Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
IPC分类号： A01N43/00 , C07D239/70
CPC分类号： C07D239/91 , C07D401/12 , C07D403/04 , C07D471/04
摘要： This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R1 represents a lower alkyl group et al; R2 and R3 are same and different and represents hydrogen atm et al; R4 represents the substituent of the formula (II) et al; X1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
摘要翻译：本发明提供式（I）的化合物或其药学上可接受的盐，其中R 1表示低级烷基等; R2和R3相同且不同，代表氢原子; R4表示式（II）等的取代基; X1表示NH，O或S; Y表示N或C; Ar是通过从其中除去两个氢原子而衍生自芳基等的二价取代基; 环A表示5-或6-元杂芳基; 该化合物具有组胺H3受体拮抗作用或组胺H3受体反向激动作用，可用于预防或治疗代谢系统疾病，循环系统疾病或神经系统疾病。

60. 发明授权

US07803807B2 Benzimidazole derivatives 失效
标题翻译：苯并咪唑衍生物
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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