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71. 发明授权

US07119107B2 Pyridone derivatives 失效
标题翻译：吡啶酮衍生物
公开(公告)号：US07119107B2
公开(公告)日：2006-10-10
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： A61K31/4439 , C07D401/14
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 R5 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 5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，癫痫症，痴呆症，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，生殖器或生殖障碍如不孕，早产，性功能障碍等。，胃肠道疾病，呼吸系统疾病，炎性疾病或青光眼等。

72. 发明申请

US20060135559A1 Novel imidazoline compounds 失效
标题翻译：新型咪唑啉化合物
公开(公告)号：US20060135559A1
公开(公告)日：2006-06-22
申请号：US11348459
申请日：2006-02-07
申请人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
发明人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
IPC分类号： A61K31/4709 , A61K31/4439 , A61K31/4178 , C07D409/02 , C07D403/02
CPC分类号： C07D401/04 , C07D233/26 , C07D401/14 , C07D403/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds represented by the general formula (I): wherein Ar1 and Ar2 are each aryl or heteroaryl; R1 is lower cycloalkyl, —Ar3, or a group of the general formula (a), (b) or (c): and R2 and R3are each hydrogen, lower cycloalkyl, lower alkenyl, or optionally substituted lower alkyl (with the proviso that when R2 and R3 are simultaneously hydrogen, Ar1, Ar2 and R1 do not simultaneously represent unsubstituted phenyl). The compounds are useful as treating agents for various NPY-related diseases, for example, circulatory diseases including hypertension, kidney diseases, cardiac diseases, vasospasm and arteriosclerosis; central nervous system diseases including hyperphagia, depression, anxiety, convulsion, epilepsy, dementia, pain, alcohol dependence, and withdrawal symptoms due to abstinence from drugs; metabolic diseases including obesity, diabetes, hormonal disorders, hypercholesterolemia, and hyperlipidemia; sexual dysfunction and reproductive function disorders; digestive diseases including enterokinetic disorders; respiratory diseases; inflammation; or glaucoma.
摘要翻译：由通式（I）表示的化合物：其中Ar 1和Ar 2各自为芳基或杂芳基; R 1是低级环烷基，-Ar 3或通式（a），（b）或（c）的基团：R 2， R 3和R 3各自为氢，低级环烷基，低级烯基或任选取代的低级烷基（条件是当R 2和R 3' / SUP>同时为氢，Ar 1，Ar 2和R 1不同时表示未取代的苯基）。这些化合物可用作各种NPY相关疾病的治疗剂，例如包括高血压，肾脏疾病，心脏病，血管痉挛和动脉硬化的循环系统疾病; 中枢神经系统疾病，包括食欲过多，抑郁，焦虑，惊厥，癫痫，痴呆，疼痛，酒精依赖以及戒毒症状; 代谢疾病包括肥胖，糖尿病，激素失调，高胆固醇血症和高脂血症; 性功能障碍和生殖功能障碍; 消化疾病包括肠动力障碍; 呼吸疾病; 炎; 或青光眼。

73. 发明授权

US07064142B2 Imidazonline compounds 失效
标题翻译：咪唑啉化合物
公开(公告)号：US07064142B2
公开(公告)日：2006-06-20
申请号：US10204267
申请日：2001-02-22
申请人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
发明人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
IPC分类号： A61K31/415 , C07D233/26
CPC分类号： C07D401/04 , C07D233/26 , C07D401/14 , C07D403/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds represented by the general formula (I): wherein Ar1 and Ar2 are each aryl or heteroaryl; R1 is lower cycloalkyl, —Ar3, or a group of the general formula (a), (b) or (c): and R2 and R3 are each hydrogen, lower cycloalkyl, lower alkenyl, or optionally substituted lower alkyl (with the proviso that when R2 and R3 are simultaneously hydrogen, Ar1, Ar2 and R1 do not simultaneously represent unsubstituted phenyl). The compounds are useful as treating agents for various NPY-related diseases, for example, circulatory diseases including hypertension, kidney diseases, cardiac diseases, vasospasm and arteriosclerosis; central nervous system diseases including hyperphagia, depression, anxiety, convulsion, epilepsy, dementia, pain, alcohol dependence, and withdrawal symptoms due to abstinence from drugs; metabolic diseases including obesity, diabetes, hormonal disorders, hypercholesterolemia, and hyperlipidemia; sexual dysfunction and reproductive function disorders; digestive diseases including enterokinetic disorders; respiratory diseases; inflammation; or glaucoma.
摘要翻译：由通式（I）表示的化合物：其中Ar 1和Ar 2各自为芳基或杂芳基; R 1是低级环烷基，-Ar 3或通式（a），（b）或（c）的基团：R 2， R 3和R 3各自为氢，低级环烷基，低级烯基或任选取代的低级烷基（条件是当R 2和R 3' / SUP>同时为氢，Ar 1，Ar 2和R 1不同时表示未取代的苯基）。这些化合物可用作各种NPY相关疾病的治疗剂，例如包括高血压，肾脏疾病，心脏病，血管痉挛和动脉硬化的循环系统疾病; 中枢神经系统疾病，包括食欲过多，抑郁，焦虑，惊厥，癫痫，痴呆，疼痛，酒精依赖以及戒毒症状; 代谢疾病包括肥胖，糖尿病，激素失调，高胆固醇血症和高脂血症; 性功能障碍和生殖功能障碍; 消化疾病包括肠动力障碍; 呼吸疾病; 炎; 或青光眼。

74. 发明申请

US20060106046A1 Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient 失效
标题翻译：黑色素浓缩激素受体拮抗剂含有哌啶衍生物作为活性成分
公开(公告)号：US20060106046A1
公开(公告)日：2006-05-18
申请号：US10544261
申请日：2004-02-09
申请人： Minoru Moriya , Toshihiro Sakamoto , Makoto Ishikawa , Akio Kanatani , Takehiro Fukami
发明人： Minoru Moriya , Toshihiro Sakamoto , Makoto Ishikawa , Akio Kanatani , Takehiro Fukami
IPC分类号： A61K31/4747 , A61K31/4545 , C07D471/10 , C07D401/02
CPC分类号： C07D401/04 , A61K31/438 , A61K31/4439 , A61K31/445 , C07D211/26 , C07D491/10
摘要： The invention provides melanin-concentrating hormone receptor antagonists containing as the active ingredient piperidine derivatives represented by the general formula [I]: [wherein R1 is hydrogen, hydroxyl, lower alkyl, or the like; R2, R3a, R3b, R4a, R4b, R5a, R5b and R6 each stands for hydrogen, halogen, or the like; W1 and W2 each independently stands for —O—, —CH2—, or the like; Y1, Y2, Y3 and Y4 stand for —CH—, —CF—, —N—, or the like; Z stands for lower alkyl, an aliphatic heterocyclic group, or the like; Ar is a mono- or bi-cyclic aliphatic heterocycle or an aromatic heterocycle; and n is an integer of 1 to 8]. The compounds act as antagonist against melanin-concentrating hormone receptor and are useful as drugs for central diseases, circulatory diseases, or metabolic diseases.
摘要翻译：本发明提供了含有作为活性成分的通式[I]表示的哌啶衍生物的黑色素浓缩激素受体拮抗剂：其中R 1是氢，羟基，低级烷基等; R 2，R 3，R 3b，R 4a，R 4b，R 4b， R 5a，R 5b和R 6各自代表氢，卤素等; W 1和W 2各自独立地代表-O-，-CH 2 - 等; Y 1，Y 2，Y 3和Y 4代表-CH - ， - CF - ， - N-等; Z代表低级烷基，脂族杂环基等; Ar是单环或双环脂族杂环或芳族杂环; n为1〜8的整数]。该化合物作为拮抗黑素浓缩激素受体的拮抗剂，可用作中枢疾病，循环系统疾病或代谢疾病的药物。

75. 发明授权

US06495559B2 NPY Y5 receptor antagonists 失效
标题翻译： NPY Y5受体拮抗剂
公开(公告)号：US06495559B2
公开(公告)日：2002-12-17
申请号：US09896940
申请日：2001-06-29
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： C07D22120
CPC分类号： C07D221/20 , C07D471/10
摘要： Compounds of general structural formula I such as that shown in structural formula II are selective NPY Y5 receptor antagonists, useful in the treatment of obesity and the complications associated therewith.
摘要翻译：一般结构式I的化合物如结构式II所示的化合物是选择性NPY Y5受体拮抗剂，可用于治疗肥胖症及其相关并发症。

76. 发明授权

US06258837B1 Neuropeptide Y receptor antagonist 失效
标题翻译：神经肽Y受体拮抗剂
公开(公告)号：US06258837B1
公开(公告)日：2001-07-10
申请号：US09403031
申请日：1999-12-08
申请人： Takehiro Fukami , Takahiro Fukuroda , Akio Kanatani , Masaki Ihara , Takayoshi Okabe
发明人： Takehiro Fukami , Takahiro Fukuroda , Akio Kanatani , Masaki Ihara , Takayoshi Okabe
IPC分类号： A01N4316
CPC分类号： C07D311/82 , A61K31/352
摘要： The present invention relates to a neuropeptide Y receptor antagonist comprising a compound represented by the formula [I]: as an active ingredient.
摘要翻译：本发明涉及包含由式[I]表示的化合物作为活性成分的神经肽Y受体拮抗剂。

77. 发明授权

US06191160B1 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：US06191160B1
公开(公告)日：2001-02-20
申请号：US09436120
申请日：1999-11-08
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： A61K31495
CPC分类号： C07D221/20 , C07D471/10
摘要： Compounds of the general structural formula I are selective NPY Y5 receptor antagonists. The compounds and compositions of the present invention are useful in the treatment of obesity and complications associated therewith.
摘要翻译：化合物的一般结构式Iare选择性NPY Y5受体拮抗剂。本发明的化合物和组合物可用于治疗与其相关的肥胖症和并发症。

78. 发明授权

US06180653B2 Aminopyrazole derivatives 失效
标题翻译：氨基吡唑衍生物
公开(公告)号：US06180653B2
公开(公告)日：2001-01-30
申请号：US09319912
申请日：1999-07-28
申请人： Takehiro Fukami , Takahiro Fukuroda , Akio Kanatani , Masaki Ihara
发明人： Takehiro Fukami , Takahiro Fukuroda , Akio Kanatani , Masaki Ihara
IPC分类号： C07D40104
CPC分类号： C07D231/38 , C07D231/40 , C07D401/04
摘要： The present invention relates to a compound represented by the general formula [I]: wherein Ar1 represents an aryl or heteroaryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl, lower alkenyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower alkylamino, lower dialkylamino, acyl and aryl groups; Ar2 represents an aryl or heteroaryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl, lower alkenyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower alkylamino, lower dialkylamino and aryl groups; n is zero, 1 or 2; and R1 and R2 may be the same or different and each represents a hydrogen atom or a lower alkyl group, or its salt, a method for its preparation as well as an agent for the treatment of bulimia, obesity or diabetes comprising it as an active ingredient.
摘要翻译：本发明涉及由通式[I]表示的化合物：其中Ar 1表示可以具有选自卤素原子和低级烷基，低级链烯基，低级卤代烷基，低级烷氧基，低级烷硫基，低级烷基氨基，低级二烷基氨基，酰基和芳基; Ar2表示可以具有选自卤素原子和低级烷基，低级烯基，低级卤代烷基，低级烷氧基，低级烷硫基，低级烷基氨基，低级二烷基氨基和芳基的取代基的芳基或杂芳基; n为零，1或2; 并且R 1和R 2可以相同或不同，并且各自表示氢原子或低级烷基，或其盐，其制备方法以及用于治疗贪食，肥胖症或糖尿病的药物，其包含其作为活性物质成分。

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