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公开(公告)号:US06806275B2
公开(公告)日:2004-10-19
申请号:US10120408
申请日:2002-04-12
申请人: Masashi Nagamine , Makoto Gotoh , Masanori Yoshida , Atsuro Nakazato , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa
发明人: Masashi Nagamine , Makoto Gotoh , Masanori Yoshida , Atsuro Nakazato , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa
IPC分类号: A61K31505
CPC分类号: C07D401/14 , C07D409/14 , C07D417/14
摘要: The present invention provides an arylpiperidine derivative of the formula (I) or a pharmaceutically acceptable salt thereof, which has antipsychotic effect: wherein D is a carbon atom or a nitrogen atom, E is a CH group or a nitrogen atom, G is an oxygen atom, a sulfur atom, a nitrogen atom or an NH group, Y1 is a hydrogen atom or a halogen atom, n is an integer of 1 to 4, and R1 is a group represented by any of the formulas (i) to (iv) defined in the specification.
摘要翻译: 本发明提供具有抗精神病作用的式(I)的芳基哌啶衍生物或其药学上可接受的盐,其中D为碳原子或氮原子,E为CH基或氮原子,G为氧 原子,硫原子,氮原子或NH基,Y 1为氢原子或卤素原子,n为1〜4的整数,R 1为由式 (i)至(iv)。
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公开(公告)号:US20110065667A1
公开(公告)日:2011-03-17
申请号:US12951964
申请日:2010-11-22
申请人: Toshio NAKAMURA , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
发明人: Toshio NAKAMURA , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
IPC分类号: A61K31/695 , C07D231/10 , C07D413/12 , C07D281/06 , C07F7/10 , A61K31/415 , A61K31/5377 , A61K31/553 , A61P25/28 , A61P25/18 , A61P3/10 , A61P25/24 , A61P25/08 , A61P25/00
CPC分类号: C07D231/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/14
摘要: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.
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公开(公告)号:US20050119345A1
公开(公告)日:2005-06-02
申请号:US10500101
申请日:2002-12-26
申请人: Atsuro Nakazato , Shigeyuki Chaki , Kazunari Sakagami , Ryoko Dean , Hiroshi Ohta , Shiho Hirota , Akito Yasuhara
发明人: Atsuro Nakazato , Shigeyuki Chaki , Kazunari Sakagami , Ryoko Dean , Hiroshi Ohta , Shiho Hirota , Akito Yasuhara
IPC分类号: A61K45/00 , A61K31/00 , A61K31/196 , A61K31/198 , A61K31/381 , A61P25/18 , A61P43/00 , C07C229/50 , C07C237/04 , C07C237/26 , C07C255/54 , C07D333/16 , A61K31/195 , C07C229/32
CPC分类号: A61K31/381 , A61K31/00 , A61K31/196 , A61K31/198 , C07C229/50 , C07C237/04 , C07C237/26 , C07C255/54 , C07C2601/08 , C07C2602/18 , C07D333/16
摘要: An antidepressant comprising, as an active ingredient, a compound having an antagonistic effect on group II metabotropic glutamate receptors, as well as a 2-amino-3-alkoxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative of Formula [I]: [wherein R1 and R2, which may be the same or different, each represent a hydroxyl group, a C1-10 alkoxy group, etc.; R3 represents a C1-10 acyl group, a C1-6 alkoxy-C1-6 acyl group, etc.; and R4 and R5, which may be the same or different, each represent a hydrogen atom, a C1-10 alkyl group, etc.] or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译: 作为活性成分的抗抑郁药,其具有对II型代谢型谷氨酸受体具有拮抗作用的化合物,以及2-氨基-3-烷氧基-6-氟 - 双环[3.1.0]己烷-2,6-二 式[I]的二羧酸衍生物:其中R 1和R 2可以相同或不同,各自表示羟基,C 1〜 1-10个烷氧基等; R 3表示C 1-10烷基酰基,C 1-6烷氧基-C 1-6烷基, 酰基等; 和R 4和R 5可以相同或不同,各自表示氢原子,C 1-10烷基, 等]或其药学上可接受的盐或水合物。
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公开(公告)号:US06380384B1
公开(公告)日:2002-04-30
申请号:US09829203
申请日:2001-04-10
申请人: Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
发明人: Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
IPC分类号: C07D40106
CPC分类号: C07D401/06 , C07D215/54 , C07D241/44
摘要: A 1,2-dihydro-2-oxoquinoline derivative represented by the formula: wherein Ar is a pyridyl group or a group represented by the formula: (wherein X3 and X4 are the same or different, and are each a hydrogen atom, a halogen atom, a C1-5 alkyl group, a C1-5 alkoxy group, a hydroxyl group or a trifluoromethyl group), Y is a nitrogen atom, CH or C(OH), R1 and R2 are the same or different, and are each a hydrogen atom, a C1-10 alkyl group, a C3-15 alkoxyalkyl group or a C3-15 alkylaminoalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X1 and X2 are the same or different, and are each a hydrogen atom, a C1-5 alkyl group, a C1-5 alkoxy group or a halogen atom; or X1 and X2 taken together form an alkylenedioxy group, and n is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof.
摘要翻译: 由下式表示的1,2-二氢-2-氧代喹啉衍生物:其中Ar是吡啶基或由下式表示的基团:(其中X 3和X 4相同或不同,并且各自为氢原子,卤素 原子,C 1-5烷基,C 1-5烷氧基,羟基或三氟甲基),Y是氮原子,CH或C(OH),R 1和R 2相同或不同,各自相同或不同 氢原子,C 1-10烷基,C 3-15烷氧基烷基或C 3-15烷基氨基烷基,或者R 1和R 2与它们所连接的氮原子一起形成环状氨基,X 1和X 2是 相同或不同,并且各自为氢原子,C1-5烷基,C1-5烷氧基或卤素原子; 或者X1和X2一起形成亚烷基二氧基,n为1〜3的整数。 或其药学上可接受的盐。
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公开(公告)号:US06333358B1
公开(公告)日:2001-12-25
申请号:US09485006
申请日:2000-02-01
申请人: Atsuro Nakazato , Taketoshi Okubo , Toshio Nakamura , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Kenji Yamamoto , Koichiro Harada , Masanori Yoshida
发明人: Atsuro Nakazato , Taketoshi Okubo , Toshio Nakamura , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Kenji Yamamoto , Koichiro Harada , Masanori Yoshida
IPC分类号: A61K31135
CPC分类号: C07D213/40 , C07C233/25 , C07C233/33 , C07C233/54 , C07C235/38 , C07C235/78 , C07C237/30 , C07C247/10 , C07C275/32 , C07C311/27 , C07C311/29 , C07C311/46 , C07C323/20 , C07C323/41 , C07C323/60 , C07D213/643 , C07D213/65 , C07D213/68
摘要: An aryloxyaniline derivative represented by the formula: wherein Ar1 and Ar2 are each a substituted or unsubstituted phenyl group, pyridyl group or naphthyl group, R1 is a hydrogen atom, an alkyl group, etc., X1 is a hydrogen atom, an alkyl group, etc., y1 is a branched or unbranched alkylene group having 1 to 6 carbon atoms or a single bond; or a pharmaceutically acceptable salt thereof can provide medicines having a high affinity for MDR, and therefore, exhibiting a therapeutic or preventive effect on anxiety, related diseases thereto, depression, etc.
摘要翻译: 由下式表示的芳氧基苯胺衍生物:其中Ar1和Ar2各自为取代或未取代的苯基,吡啶基或萘基,R1为氢原子,烷基等,X1为氢原子,烷基, y1是具有1〜6个碳原子或单键的支链或非支链亚烷基; 或其药学上可接受的盐可以提供对MDR具有高亲和力的药物,因此对焦虑,其相关疾病,抑郁等具有治疗或预防作用。
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公开(公告)号:US06291467B1
公开(公告)日:2001-09-18
申请号:US09646309
申请日:2000-09-15
申请人: Atsuro Nakazato , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
发明人: Atsuro Nakazato , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
IPC分类号: C07D41706
CPC分类号: C07D231/12 , C07D401/06 , C07D417/06
摘要: An aromaheterocyclic derivative represented by the formula: wherein Z is a group represented by the following formula: wherein Ar1 is a phenyl group or a phenyl group substituted with a halogen atom or an alkyl group of 1 to 5 carbon atoms, R2 is an alkyl group of 1 to 5 carbon atoms, Y is a hydrogen atom, a mercapto group, an alkylthio group of 1 to 5 carbon atoms, an amino group or an amino group substituted with one or two alkyl groups having 1 to 5 carbon atoms, Ar2 is a phenyl group of one or two substituents selected from the group consisting of a halogen atom, an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms, a hydroxyl group and a trifluoromethyl group, or a phenyl group, B1-B2 is CH—CO or C═C(R1) (wherein R1 is a hydrogen atom or an alkyl group of 1 to 5 carbon atoms), and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof, which is a dopamine D4 receptor antagonist compound having an antipsychotic action without causing extrapyramidal diseases.
摘要翻译: 由下式表示的芳族杂环衍生物:其中Z为下式表示的基团:其中Ar1为苯基或被卤素原子或1〜5个碳原子的烷基取代的苯基,R2为烷基 1〜5个碳原子,Y为氢原子,巯基,1〜5个碳原子的烷硫基,氨基或被一个或两个碳原子数为1〜5的烷基取代的氨基,Ar2为 选自卤素原子,1〜5个碳原子的烷基,1〜5个碳原子的烷氧基,羟基和三氟甲基,或苯基中的一个或两个取代基的苯基 ,B1-B2为CH-CO或C = C(R1)(其中R1为氢原子或1〜5个碳原子的烷基),n为1〜4的整数,或其药学上可接受的盐 ,其是具有抗精神病作用而不引起外敷的多巴胺D4受体拮抗剂化合物 痉挛性疾病
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公开(公告)号:US08183387B2
公开(公告)日:2012-05-22
申请号:US12951964
申请日:2010-11-22
申请人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
发明人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
IPC分类号: C07D231/10
CPC分类号: C07D231/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/14
摘要: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.
摘要翻译: 本发明提供了用于痴呆,阿尔茨海默病,注意缺陷多动障碍,精神分裂症,进食障碍,肥胖症,糖尿病,高脂血症,睡眠障碍,发作性睡眠障碍,睡眠呼吸暂停综合征,昼夜节律紊乱,抑郁,过敏性鼻炎或 其他疾病 由式(1)表示的苯基吡唑衍生物或其药学上可接受的盐:其中可以相同或不同的R 1和R 2各自表示C 1 -C 6烷基或C 3 -C 8环烷基,或者R 1和R 2各自连接 与其相邻的氮原子一起形成4-至7-元饱和杂环(其中所述饱和杂环可被卤素或C 1 -C 6烷基取代),n表示0至2的整数,T表示氢 原子,卤素或C 1 -C 6烷基,R表示式(I):等)。
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公开(公告)号:US20100267687A1
公开(公告)日:2010-10-21
申请号:US12741754
申请日:2008-11-13
申请人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
发明人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
IPC分类号: A61K31/4155 , C07D403/12 , A61P25/28 , A61P25/18 , A61P25/08 , A61P3/04 , A61P3/10 , A61P3/06 , C07D413/14 , A61K31/5377 , C07D231/14 , C07D401/14 , A61K31/4439 , A61K31/422 , A61K31/454 , A61K31/553 , C07D403/14 , A61K31/496
CPC分类号: C07D231/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/14
摘要: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.
摘要翻译: 本发明提供了用于痴呆,阿尔茨海默病,注意缺陷多动障碍,精神分裂症,进食障碍,肥胖症,糖尿病,高脂血症,睡眠障碍,发作性睡眠障碍,睡眠呼吸暂停综合征,昼夜节律紊乱,抑郁,过敏性鼻炎或 其他疾病 由式(1)表示的苯基吡唑衍生物或其药学上可接受的盐:其中可以相同或不同的R 1和R 2各自表示C 1 -C 6烷基或C 3 -C 8环烷基,或者R 1和R 2各自连接 与其相邻的氮原子一起形成4-至7-元饱和杂环(其中所述饱和杂环可被卤素或C 1 -C 6烷基取代),n表示0至2的整数,T表示氢 原子,卤素或C 1 -C 6烷基,R表示式(I):等)。
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公开(公告)号:US07157594B2
公开(公告)日:2007-01-02
申请号:US10500101
申请日:2002-12-26
申请人: Atsuro Nakazato , Shigeyuki Chaki , Kazunari Sakagami , Ryoko Dean , Hiroshi Ohta , Shiho Hirota , Akito Yasuhara
发明人: Atsuro Nakazato , Shigeyuki Chaki , Kazunari Sakagami , Ryoko Dean , Hiroshi Ohta , Shiho Hirota , Akito Yasuhara
IPC分类号: C07C69/74 , C07C61/113
CPC分类号: A61K31/381 , A61K31/00 , A61K31/196 , A61K31/198 , C07C229/50 , C07C237/04 , C07C237/26 , C07C255/54 , C07C2601/08 , C07C2602/18 , C07D333/16
摘要: An antidepressant comprising, as an active ingredient, a compound having an antagonistic effect on group II metabotropic glutamate receptors, as well as a 2-amino-3-alkoxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative of Formula [I]: [wherein R1 and R2, which may be the same or different, each represent a hydroxyl group, a C1-10 alkoxy group, etc.; R3 represents a C1-10 acyl group, a C1-6 alkoxy-C1-6 acyl group, etc.; and R4 and R5, which may be the same or different, each represent a hydrogen atom, a C1-10 alkyl group, etc.] or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译: 一种抗抑郁药,其包含对II族代谢型谷氨酸受体具有拮抗作用的化合物以及2-氨基-3-烷氧基-6-氟 - 双环[3.1.0]己烷-2,6-二 式[I]的二羧酸衍生物:其中R 1和R 2可以相同或不同,各自表示羟基,C 1〜 1-10个烷氧基等; R 3表示C 1-10烷基酰基,C 1-6烷氧基-C 1-6烷基, 酰基等; 和R 4和R 5可以相同或不同,各自表示氢原子,C 1-10烷基, 等]或其药学上可接受的盐或水合物。
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公开(公告)号:US08193176B2
公开(公告)日:2012-06-05
申请号:US12951978
申请日:2010-11-22
申请人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
发明人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
IPC分类号: A61K31/5377 , A61K31/4155 , A61K31/397 , A61K31/553 , A61K31/496
CPC分类号: C07D231/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/14
摘要: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.
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