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1. 发明授权

US06852732B2 Tetrahydropyridino or piperidino heterocylic derivatives 失效
标题翻译：四氢吡啶基或哌啶子杂环衍生物
公开(公告)号：US06852732B2
公开(公告)日：2005-02-08
申请号：US10311277
申请日：2001-07-04
申请人： Atsuro Nakazato , Toshihito Kumagai , Taketoshi Okubo , Kazuya Kameo
发明人： Atsuro Nakazato , Toshihito Kumagai , Taketoshi Okubo , Kazuya Kameo
IPC分类号： A61K31/4365 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/4709 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/5377 , A61P1/00 , A61P1/14 , A61P7/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P17/14 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P37/02 , A61P43/00 , C07D401/04 , C07D401/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , A01N43/42
CPC分类号： C07D401/04 , C07D401/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： A tetrahydropyridino or piperidino heterocyclic derivative represented by the formula [I]: A-Het [I] has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.
摘要翻译：由式[I]表示的四氢吡啶基或哌啶子基杂环衍生物对CRF受体具有高亲和力，并且对于被认为涉及CRF的疾病有效。

2. 发明申请

US20050009874A1 Tetrahydropyridin or piperidino heterocyclic derivatives 失效
标题翻译：四氢吡啶或哌啶子基杂环衍生物
公开(公告)号：US20050009874A1
公开(公告)日：2005-01-13
申请号：US10912185
申请日：2004-08-06
申请人： Atsuro Nakazato , Toshihito Kumagai , Taketoshi Okubo , Kazuya Kameo
发明人： Atsuro Nakazato , Toshihito Kumagai , Taketoshi Okubo , Kazuya Kameo
IPC分类号： A61K31/4365 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/4709 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/5377 , A61P1/00 , A61P1/14 , A61P7/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P17/14 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P37/02 , A61P43/00 , C07D401/04 , C07D401/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61K31/454 , C07
CPC分类号： C07D401/04 , C07D401/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： A tetrahydropyridino or piperidino heterocyclic derivative represented by the formula [I]: A-Het [I]has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.
摘要翻译：由式[I]表示的四氢吡啶基或哌啶子基杂环衍生物：A-Het [I]对CRF受体具有高亲和力，并且对于CRF被认为涉及的疾病有效。

3. 发明授权

US06329525B1 1,2-Dihydro-2-oxoquinoline derivatives 失效
标题翻译： 1,2-二氢-2-氧代喹啉衍生物
公开(公告)号：US06329525B1
公开(公告)日：2001-12-11
申请号：US09555568
申请日：2000-06-01
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： C07D215227
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，各自为氢原子，C1-5烷基，C1-5烷氧基或卤素原子，或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。

4. 发明授权

US06281355B1 Nitrogen-containing tetracyclic compounds 失效
标题翻译：含氮四环化合物
公开(公告)号：US06281355B1
公开(公告)日：2001-08-28
申请号：US09555570
申请日：2000-06-01
申请人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Kuniaki Kondoh , Masanori Yoshida
发明人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Kuniaki Kondoh , Masanori Yoshida
IPC分类号： A61K31403
CPC分类号： C07D471/04 , C07D495/04
摘要： A nitrogen-containing tetracyclic compound represented by the formula: wherein Y1—Y2—Y3 is N—C═N or a group represented by the formula: C═C—NR3 (wherein R3 is a hydrogen atom, a C1-5 alkyl group or a nitrogen-containing C2-10 alkyl group), Y4 is S, SO, SO2, CH2 or a group represented by the formula: NR4 (wherein R4 is a C1-5 alkanoyl group or a C1-5 alkyl group), 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, and n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.
摘要翻译：一种由下式表示的含氮四环化合物：其中Y1-Y2-Y3为NC = N或由下式表示的基团：C = C-NR3（其中R3为氢原子，C1-5烷基或含氮的C2-10烷基），Y4是S，SO，SO2，CH2或由下式表示的基团：NR4（其中R4是C1-5烷酰基或C1-5烷基），R1和R2 各自为氢原子，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，X1和X2相同或不同，分别为氢原子，C1-5烷基，C1-5烷氧基或卤素原子，n为0,1或2; 或其药学上可接受的盐。

5. 发明授权

US06187781B1 4-Tetrahydropyridylpyrimidine derivatives 失效
标题翻译： 4-四氢吡啶基嘧啶衍生物
公开(公告)号：US06187781B1
公开(公告)日：2001-02-13
申请号：US09381462
申请日：1999-09-21
申请人： Atsuro Nakazato , Toshihito Kumagai , Taketoshi Okubo , Izumi Aibe , Hideo Tanaka , Shigeyuki Chaki , Shigeru Okuyama , Kazuyuki Tomisawa
发明人： Atsuro Nakazato , Toshihito Kumagai , Taketoshi Okubo , Izumi Aibe , Hideo Tanaka , Shigeyuki Chaki , Shigeru Okuyama , Kazuyuki Tomisawa
IPC分类号： C07D40144
CPC分类号： C07D401/04 , C07D405/14 , C07D409/14
摘要： A 4-tetrahydropyridylpyrimidine compound represented by formula (I): wherein Ar represents a phenyl group substituted with 1 to 3 substituents selected from a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, and a trifluoromethyl group, a phenyl group, a thienyl group or a furanyl group; R1 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or 2 alkyl groups having 1 to 5 carbon atoms; R2 represents an alkyl group having 1 to 5 carbon atoms, a cycloalkylalkyl group having 4 to 7 carbon atoms, an alkenyl group having 2 to 5 carbon atoms or an alkynyl group having 2 to 5 carbon atoms; and X1, X2, and X3, which may be the same or different, each represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, an alkylthio group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or 2 alkyl groups having 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof. The 4-Tetrahydropyridylpyrimidine compound finds utility in the treatment of diseases in which CRF is implicated.
摘要翻译：由式（I）表示的4-四氢吡啶基嘧啶化合物：其中Ar表示被1至3个选自卤素原子，具有1至5个碳原子的烷基，具有1至5个碳原子的烷氧基的取代基取代的苯基，和三氟甲基，苯基，噻吩基或呋喃基; R1表示氢原子，碳原子数1〜5的烷基，氨基或被1〜2个碳原子数1〜2的烷基取代的氨基。 R2表示碳原子数1〜5的烷基，碳原子数4〜7的环烷基烷基，碳原子数2〜5的烯基或碳原子数2〜5的炔基。 X 1，X 2和X 3可以相同或不同，分别表示氢原子，卤素原子，碳原子数1〜5的烷基，碳原子数1〜5的烷氧基，烷硫基， 1至5个碳原子的氨基或被1或2个具有1至5个碳原子的烷基取代的氨基，或其药学上可接受的盐。 4-四氢吡啶基嘧啶化合物可用于治疗涉及CRF的疾病。

6. 发明授权

US06600038B1 Carbamoyl tetrahydropyridine derivatives 失效
标题翻译：氨基甲酰四氢吡啶衍生物
公开(公告)号：US06600038B1
公开(公告)日：2003-07-29
申请号：US09914534
申请日：2001-08-30
申请人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Kazuyuki Tomisawa
发明人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Kazuyuki Tomisawa
IPC分类号： C07D47334
CPC分类号： A61K31/519 , C07D473/00 , C07D487/04
摘要： Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1-Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7)N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.
摘要翻译：由下式表示的氨基甲酰基四氢吡啶衍生物：[式中，R 1和R 2相同或不同，各自表示氢原子，C 1 -C 5烷基等; Y1-Y2表示（R4）C = C（R5），（R6）C = N，N = N，（R7）N-CO或N = C（R8） X1，X2和X3相同或不同，各自表示氢原子，卤素原子等; R3，R4，R5和R6相同或不同，各自表示氢原子或烷基; R7表示氢原子，C1-C5烷基等; 并且R8表示氢原子或氨基甲酰基]或其药学上可接受的盐，并且提供其制备的中间体。上述衍生物对于被认为涉及CRF的疾病是有效的。

7. 发明授权

US06380384B1 1,2-dihydro-2-oxoquinoline derivatives 失效
标题翻译： 1,2-二氢-2-氧代喹啉衍生物
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。

8. 发明授权

US06894168B2 Carbamoyl tetrahydropyridine derivatives 失效
标题翻译：氨基甲酰四氢吡啶衍生物
公开(公告)号：US06894168B2
公开(公告)日：2005-05-17
申请号：US10347288
申请日：2003-01-21
申请人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Kazuyuki Tomisawa
发明人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Kazuyuki Tomisawa
IPC分类号： A61K31/519 , A61P1/00 , A61P7/10 , A61P9/10 , A61P9/12 , A61P17/02 , A61P25/08 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P37/02 , A61P43/00 , C07D473/00 , C07D487/04 , C07D211/78
CPC分类号： A61K31/519 , C07D473/00 , C07D487/04
摘要： Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1—Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7) N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.
摘要翻译：由下式表示的氨基甲酰基四氢吡啶衍生物：[式中，R 1，R 2和R 2'相同或不同，各自表示氢原子，C 1 C 5 -C 15烷基等; Y 1 - （CH 2）2（R 4 S）（R 5），（R 6） CN，NN，（R 7）N-CO或NC（R 8）; X 1，X 2和X 3相同或不同，各自表示氢原子，卤素原子等; R 3，R 4，R 5和R 6相同或不同，并且各自表示氢原子或烷基; R 7表示氢原子，C 1 -C 5烷基等; 和R 8表示氢原子或氨基甲酰基]或其药学上可接受的盐，以及其制备中间体。上述衍生物对于被认为涉及CRF的疾病是有效的。

9. 发明申请

US20110137031A1 PYRROLOPYRIMIDINE AND PYRROLOTRIAZINE DERIVATIVES 失效
标题翻译：吡咯并嘧啶和吡咯烷酮衍生物
公开(公告)号：US20110137031A1
公开(公告)日：2011-06-09
申请号：US10584946
申请日：2005-01-06
申请人： Atsuro Nakazato , Taketoshi Okubo , Dai Nozawa , Tomoko Tamita , Ludo E.J. Kennis
发明人： Atsuro Nakazato , Taketoshi Okubo , Dai Nozawa , Tomoko Tamita , Ludo E.J. Kennis
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, dermatitides, schizophrenia, pain, etc. A pyrrolopyrimidine or pyrrolotriazine derivative substituted with a carbamoyl group represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.
摘要翻译：本发明的目的是提供一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默氏病，帕金森病，亨廷顿氏舞蹈病，进食疾病，高血压，胃疾病，药物依赖，癫痫，脑梗塞，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，特异性，肠易激综合征，睡眠障碍，皮肤病，精神分裂症，疼痛等。由下式[I]表示的氨基甲酰基取代的吡咯并嘧啶或吡咯并三嗪衍生物：对CRF受体具有高亲和力，并且对于认为涉及CRF的疾病是有效的。

10. 发明申请

US20080287397A1 Pyrrolopyrimidine Derivatives Substituted with Cyclic Amino Group 失效
标题翻译：用环状氨基取代的吡咯并嘧啶衍生物
公开(公告)号：US20080287397A1
公开(公告)日：2008-11-20
申请号：US12106873
申请日：2008-04-21
申请人： Atsuro NAKAZATO , Taketoshi Okubo , Dai Nozawa , Mikako Yamaguchi , Tomoko Tamita , Ludo E.J. Kennis , Marcel F.L. De Bruyn , Jean-Pierre A.M. Bongartz , Frans M.A. Van Den Keybus , Yves E.M. Van Roosbroeck , Marcel G.M. Luyckx , Robert J.M. Hendrickx
发明人： Atsuro NAKAZATO , Taketoshi Okubo , Dai Nozawa , Mikako Yamaguchi , Tomoko Tamita , Ludo E.J. Kennis , Marcel F.L. De Bruyn , Jean-Pierre A.M. Bongartz , Frans M.A. Van Den Keybus , Yves E.M. Van Roosbroeck , Marcel G.M. Luyckx , Robert J.M. Hendrickx
IPC分类号： A61K31/661 , C07D487/04 , A61P25/00 , A61P17/00 , A61P1/00 , A61P29/00 , A61K31/519
CPC分类号： C07D471/04 , C07D487/04 , C07F9/6561
摘要： An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.
摘要翻译：本发明的目的是提供一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默氏病，帕金森病，亨廷顿氏舞蹈病，进食疾病，高血压，胃疾病，药物依赖，癫痫，脑梗塞，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，脱发，肠易激综合征，睡眠障碍，癫痫，皮肤病，精神分裂症等。可以用由以下式[I]表示的环氨基取代的吡咯并嘧啶或吡咯并吡啶衍生物来解决问题，其具有对CRF受体的高亲和力，并且对于CRF被认为涉及的疾病是有效的。

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