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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 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。

8. 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。

9. 发明授权

US06500958B2 Carboxylic acid derivatives and process for producing the same 失效
标题翻译：羧酸衍生物及其制备方法
公开(公告)号：US06500958B2
公开(公告)日：2002-12-31
申请号：US10176528
申请日：2002-06-24
申请人： Atsuro Nakazato , Toshihito Kumagai , Kazunari Sakagami , Kazuyuki Tomisawa
发明人： Atsuro Nakazato , Toshihito Kumagai , Kazunari Sakagami , Kazuyuki Tomisawa
IPC分类号： C07D23500
CPC分类号： C07D235/02 , C07C62/26 , C07C65/40 , C07C69/757 , C07C2602/18 , C07D339/06 , C07D495/10
摘要： The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.0]hexane-6-carboxylic acid derivatives represented by the formula as follows: [wherein, R1 represents a hydrogen atom, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, an aryl C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, a C1-C6 alkylthio C1-C6 alkyl group, a C1-C6 mercaptoalkyl group, a tetrahydrofuranyl group, or a tetrahydropyranyl group; R2 and R3 are identical or different, and each represents a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, or an aryl C1-C6 alkyl group, or alternatively, R2 and R3 together represent —(CH2)n— (wherein n represents 2 or 3); and Y1 and Y2 are identical or different, and each represents a sulfur atom, an oxygen atom, or a nitrogen atom].
摘要翻译：本发明涉及可用于高效合成2-氨基-4-氧代双环[3.1.0]己烷-2,6-二羧酸的化合物。根据本发明的化合物包含2-氧代双环[3.1.0] 由下式表示的己烷-6-羧酸衍生物：[其中，R1表示氢原子，C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基基团，芳基C1-C6烷基，C1-C6烷氧基C1-C6烷基，C1-C6羟基烷基，C1-C6烷硫基C1-C6烷基，C1-C6巯基烷基，四氢呋喃基，或四氢吡喃基; R2和R3相同或不同，各自表示C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基或芳基C1-C6烷基，或或者，R2和R3一起表示 - （CH 2）n - （其中n表示2或3）; Y 1和Y 2相同或不同，各自表示硫原子，氧原子或氮原子]。

10. 发明授权

US06479674B1 Carboxylic acid derivatives and process for producing same 失效
标题翻译：羧酸衍生物及其制备方法
公开(公告)号：US06479674B1
公开(公告)日：2002-11-12
申请号：US09937212
申请日：2001-09-24
申请人： Atsuro Nakazato , Toshihito Kumagai , Kazunari Sakagami , Kazuyuki Tomisawa
发明人： Atsuro Nakazato , Toshihito Kumagai , Kazunari Sakagami , Kazuyuki Tomisawa
IPC分类号： C07D31500
CPC分类号： C07D235/02 , C07C62/26 , C07C65/40 , C07C69/757 , C07C2602/18 , C07D339/06 , C07D495/10
摘要： The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.0]hexane-6-carboxylic acid derivatives represented by the formula as follows: [wherein, R1 represents a hydrogen atom, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, an aryl C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, a C1-C6 alkylthio C1-C6 alkyl group, a C1-C6 mercaptoalkyl group, a tetrahydrofuranyl group, or a tetrahydropyranyl group; R2 and R3 are identical or different, and each represents a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, or an aryl C1-C6 alkyl group, or alternatively, R2 and R3 together represent —(CH2)n— (wherein n represents 2 or 3); and Y1 and Y2 are identical or different, and each represents a sulfur atom, an oxygen atom, or a nitrogen atom].
摘要翻译：本发明涉及可用于高效合成2-氨基-4-氧代双环[3.1.0]己烷-2,6-二羧酸的化合物。根据本发明的化合物包含2-氧代双环[3.1.0] 由下式表示的己烷-6-羧酸衍生物：[其中，R1表示氢原子，C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基基团，芳基C1-C6烷基，C1-C6烷氧基C1-C6烷基，C1-C6羟基烷基，C1-C6烷硫基C1-C6烷基，C1-C6巯基烷基，四氢呋喃基，或四氢吡喃基; R2和R3相同或不同，各自表示C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基或芳基C1-C6烷基，或或者，R2和R3一起表示 - （CH 2）n - （其中n表示2或3）; Y 1和Y 2相同或不同，各自表示硫原子，氧原子或氮原子]。

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