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1. 发明授权

US07482358B2 Imidazoline compounds 失效
标题翻译：咪唑啉化合物
公开(公告)号：US07482358B2
公开(公告)日：2009-01-27
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： A61K31/435 , C07D401/00
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Ar1和Ar2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R2和R3同时为氢时，Ar1，Ar2和R1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。

2. 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。

3. 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。

4. 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。

5. 发明授权

US08044070B2 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：US08044070B2
公开(公告)日：2011-10-25
申请号：US12540534
申请日：2009-08-13
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： A61K31/445 , C07D211/00
CPC分类号： C07D401/12 , A61K31/4545 , A61K31/501 , A61K31/506 , C07D401/14 , C07D403/12 , C07D413/14 , C07D471/04
摘要： Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: wherein X1, X2 and X3 each independently represent N or CH; W represents the following formula (II): or the following formula (III): Y represents a group of a formula (IV): The compounds have a histamine-H3 receptor antagonistic or inverse-agonistic activity and are useful for remedy and/or prevention of obesity, diabetes, hormone secretion disorders, sleep disorders, etc.
摘要翻译：提供式（I）化合物及其药学上可接受的盐：其中X1，X2和X3各自独立地表示N或CH; W表示下式（II）：或下式（III）：Y表示式（IV）的基团：所述化合物具有组胺H3受体拮抗或反向激动活性，可用于治疗和/或预防肥胖，糖尿病，激素分泌障碍，睡眠障碍等

6. 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。

7. 发明申请

US20120149703A1 AZA-SUBSTITUTED SPIRO DERIVATIVES 审中-公开
标题翻译： AZA替代的SPIRO衍生物
公开(公告)号：US20120149703A1
公开(公告)日：2012-06-14
申请号：US13396887
申请日：2012-02-15
申请人： Makoto Jitsuoka , Nagaaki Sato , Daisuke Tsukahara
发明人： Makoto Jitsuoka , Nagaaki Sato , Daisuke Tsukahara
IPC分类号： A61K31/5377 , A61K31/439 , C07D491/107 , A61P3/06 , A61P9/00 , A61P3/00 , A61P9/10 , A61P9/12 , A61P25/20 , A61P25/00 , A61P25/24 , A61P25/18 , A61P25/28 , A61P25/16 , A61P25/08 , A61P25/30 , A61P25/32 , A61P3/10 , A61P3/04 , A61K31/506
CPC分类号： C07D491/10
摘要： A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: [wherein X, Y, Z and W each independently represent a methine group or a nitrogen atom, provided that a case where all of X, Y, Z and W are methine group; A represents —O— or the like, B represents —C(O)— or the like, D represent —(CH2)m2-, —O— or the like, and m2 represents 0 or 1; Q represents a methine group or a nitrogen atom; and R represents a group represented by the following formula (II-1) (wherein R6, R7 and R8 independently represent a lower alkyl group or the like].
摘要翻译：提供下式（I）的化合物或其药学上可接受的盐：[其中X，Y，Z和W各自独立地表示次甲基或氮原子，条件是X，Y，Z全部为 W是次甲基; A表示-O-等，B表示-C（O） - 等，D表示 - （CH2）m2-，-O-等，m2表示0或1; Q表示次甲基或氮原子; 并且R表示由下式（II-1）表示的基团（其中R 6，R 7和R 8独立地表示低级烷基等）。

8. 发明申请

US20110009622A1 LONG-CHAIN FATTY ACYL ELONGASE INHIBITOR COMPRISING ARYLSULFONYL DERIVATIVE AS ACTIVE INGREDIENT 有权
标题翻译：包含ARYLSULFONYL衍生物作为活性成分的长链脂肪ACYL ELONGASE抑制剂
公开(公告)号：US20110009622A1
公开(公告)日：2011-01-13
申请号：US12933444
申请日：2009-04-17
申请人： Makoto Jitsuoka , Tsuyoshi Nagase , Nagaaki Sato , Daisuke Tsukahara
发明人： Makoto Jitsuoka , Tsuyoshi Nagase , Nagaaki Sato , Daisuke Tsukahara
IPC分类号： C07D223/06 , C07D413/12 , C07D265/30 , C07D239/38 , C07D487/08 , C07D241/18 , C07D221/22 , C07D498/04 , C07D471/04 , C07D413/04 , C07D401/04 , C07D401/12 , C07D211/96 , C07D211/54 , C07D213/56 , C07D249/12 , C07D235/14 , C07D403/12 , C07D231/18 , C07D207/48 , C07C311/16 , C07C237/20 , C07D413/14
CPC分类号： C07D211/96 , C07C311/16 , C07C311/19 , C07C311/20 , C07C317/44 , C07C2601/02 , C07C2601/14 , C07D207/48 , C07D213/70 , C07D213/75 , C07D231/40 , C07D231/52 , C07D239/38 , C07D249/12 , C07D265/28 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/04 , C07D453/06 , C07D471/04 , C07D471/06 , C07D471/08 , C07D487/04 , C07D487/08 , C07D491/04 , C07D491/08
摘要： [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides.[Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].
摘要翻译： [问题]提供可用作循环系统疾病，神经系统疾病，代谢紊乱，繁殖系统疾病，消化系统疾病，肿瘤，感染性疾病等的预防药物或补救剂的化合物或作为除草剂。 [解决方案]长链脂肪酰基延伸酶抑制剂，其包含作为其活性成分的式（I）的化合物或其药物活性盐：[其中W表示氢原子，C 1-6烷基等等 X表示芳基，杂芳基等; n表示0或1; Z表示氢原子，C1-6烷基等; A1，A2，A3和A4各自独立地表示CH或N]。

9. 发明申请

US20090258871A1 Aza-Substituted Spiro Derivatives 有权
标题翻译：氮杂取代的螺衍生物
公开(公告)号：US20090258871A1
公开(公告)日：2009-10-15
申请号：US12084817
申请日：2006-11-10
申请人： Makoto Jitsuoka , Nagaaki Sato , Daisuke Tsukahara
发明人： Makoto Jitsuoka , Nagaaki Sato , Daisuke Tsukahara
IPC分类号： A61K31/5377 , C07D221/20 , A61K31/438 , C07D295/00 , C07D239/24 , A61K31/506 , A61P3/00 , A61P25/00
CPC分类号： C07D491/10
摘要： A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: [wherein X, Y, Z and W each independently represent a methine group or a nitrogen atom, provided that a case where all of X, Y, Z and W are methine group; A represents —O— or the like, B represents —C(O)— or the like, D represent —(CH2)m2-, —O— or the like, and m2 represents 0 or 1; Q represents a methine group or a nitrogen atom; and R represents a group represented by the following formula (II-1) (wherein R6, R7 and R8 independently represent a lower alkyl group or the like].
摘要翻译：提供下式（I）的化合物或其药学上可接受的盐：[其中X，Y，Z和W各自独立地表示次甲基或氮原子，条件是X，Y，Z全部为 W是次甲基; A表示-O-等，B表示-C（O） - 等，D表示 - （CH2）m2-，-O-等，m2表示0或1; Q表示次甲基或氮原子; 并且R表示由下式（II-1）表示的基团（其中R 6，R 7和R 8独立地表示低级烷基等）。

10. 发明申请

US20100210637A1 HETEROARYLOXY NITROGENOUS SATURATED HETEROCYCLIC DERIVATIVE 有权
标题翻译：杂环氧化氮饱和杂环衍生物
公开(公告)号：US20100210637A1
公开(公告)日：2010-08-19
申请号：US12540534
申请日：2009-08-13
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： A61K31/5377 , C07D403/12 , A61K31/506 , A61P3/10 , A61P3/04 , A61P1/16 , A61P3/06 , A61P9/10 , C07D401/12 , A61K31/4545 , C07D413/14 , A61K31/501
CPC分类号： C07D401/12 , A61K31/4545 , A61K31/501 , A61K31/506 , C07D401/14 , C07D403/12 , C07D413/14 , C07D471/04
摘要： Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: wherein X1, X2 and X3 each independently represent N or CH; W represents the following formula (II): or the following formula (III): Y represents a group of a formula (IV): The compounds have a histamine-H3 receptor antagonistic or inverse-agonistic activity and are useful for remedy and/or prevention of obesity, diabetes, hormone secretion disorders, sleep disorders, etc.
摘要翻译：提供式（I）化合物及其药学上可接受的盐：其中X1，X2和X3各自独立地表示N或CH; W表示下式（II）：或下式（III）：Y表示式（IV）的基团：所述化合物具有组胺H3受体拮抗或反向激动活性，可用于治疗和/或预防肥胖，糖尿病，激素分泌障碍，睡眠障碍等

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