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1. 发明申请

US20100184771A1 Bicyclic Heterocyclic Compound 审中-公开
标题翻译：双环杂环化合物
公开(公告)号：US20100184771A1
公开(公告)日：2010-07-22
申请号：US12097685
申请日：2006-12-14
申请人： Hisao Nakai , Tetsuji Saito , Yoshifumi Kagamiishi
发明人： Hisao Nakai , Tetsuji Saito , Yoshifumi Kagamiishi
IPC分类号： A61K31/5025 , C07D487/04 , A61P25/00 , A61P1/00 , A61P25/22 , A61P25/18 , A61P25/24
CPC分类号： C07D487/04 , A61K45/06
摘要： A compound represented by the formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof: wherein X1 represents N and X2 represents C, or X1 represents C and X2 represents N; Y1 represents CR4 or N; Y2 represents CH or N; wherein both Y1 and Y2 do not represent N at the same time; R1 represents (1) C3-10 branched alkyl which may be substituted or (2) —(CH2)m—NR5R6; R2, R3, and R4 each independently represent H, C1-4 alkyl, a halo-substituted C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, or the like; R5 and R6 each independently represent C1-6 alkyl which may be substituted, or R5 represents H, and R6 represents C3-6 branched alkyl which may be substituted; and Ar represents an aromatic ring which may be substituted, is useful as a pharmacologically active ingredient having a CRF antagonistic activity in preventing and/or treating neuropsychiatric diseases, diseases of peripheral organs or the like.
摘要翻译：由式（I）表示的化合物，其盐，其N-氧化物，其溶剂合物或其前药：其中X1表示N，X2表示C，或X1表示C，X2表示N; Y1表示CR4或N; Y2表示CH或N; 其中Y1和Y2同时不表示N; R1表示（1）可被取代的C3-10支链烷基或（2） - （CH2）m-NR5R6; R2，R3和R4各自独立地表示H，C1-4烷基，卤素取代的C1-4烷基，C2-4烯基，C2-4炔基等; R5和R6各自独立地表示可以被取代的C1-6烷基，或R5表示H，R6表示可以被取代的C3-6支链烷基; Ar表示可以被取代的芳香环，可用作在预防和/或治疗神经精神疾病，外周器官等疾病中具有CRF拮抗作用的药理活性成分。

2. 发明申请

US20090281120A1 BICYCLIC HETEROCYCLIC COMPOUND 审中-公开
标题翻译：双相杂环化合物
公开(公告)号：US20090281120A1
公开(公告)日：2009-11-12
申请号：US12097024
申请日：2006-12-11
申请人： Hisao Nakai , Tetsuji Saito , Yoshifumi Kagamiishi
发明人： Hisao Nakai , Tetsuji Saito , Yoshifumi Kagamiishi
IPC分类号： A61K31/519 , A61K31/437 , A61K31/415 , C07D487/04 , C07D471/04 , C07D235/02
CPC分类号： C07D471/04 , A61K45/06
摘要： A compound represented by the formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof: wherein X, Y, and W each independently represent a carbon atom or a nitrogen atom;Z represents CH or a nitrogen atom;R1 represents (1) C3-10 branched alkyl which may be substituted or (2) —(CH2)m—NR4R5; R2 and R3 each independently represent (1) a hydrogen atom, (2) C1-4 alkyl which may be substituted with a halogen atom, hydroxy which may be protected, amino which may be protected, or carboxyl which may be protected, (3) C2-4 alkenyl, (4) C2-4 alkynyl, (5) nitrile, (6) COOR6, (7) CONR7R8, (8) COR101, (9) S(O)nR102, or (10) a halogen atom, in which R6 represents a hydrogen atom or C1-4 alkyl, R7 and R8 each independently represent a hydrogen atom or C1-4 alkyl, R101 represents a hydrogen atom or C1-4 alkyl, R102 represents C1-4 alkyl, n represents 1 or 2; andAr represents an aromatic ring which may be substituted, is useful as a pharmacologically active ingredient having a CRF antagonist action in preventing and/or treating neuropsychiatric diseases, diseases of peripheral organs or the like.
摘要翻译：由式（I）表示的化合物，其盐，其N-氧化物，其溶剂化物或其前药：其中X，Y和W各自独立地表示碳原子或氮原子; Z表示CH或氮原子; R1表示（1）可以被取代的C3-10支链烷基或（2） - （CH2）m-NR4R5; R2和R3各自独立地表示（1）氢原子，（2）可以被卤素原子取代的C1-4烷基，可被保护的羟基，可被保护的氨基或可被保护的羧基，（3 ）C2-4烯基，（4）C2-4炔基，（5）腈，（6）COOR6，（7）CONR7R8，（8）COR101，（9）S（O）nR102或（10）卤素原子其中R 6表示氢原子或C 1-4烷基，R 7和R 8各自独立地表示氢原子或C 1-4烷基，R 101表示氢原子或C 1-4烷基，R 102表示C 1-4烷基，n表示1 或2; Ar表示可被取代的芳环，可用作具有CRF拮抗作用的药理活性成分，用于预防和/或治疗神经精神疾病，外周器官等疾病。

3. 发明申请

US20060122392A1 Tri-heterocyclic compounds and a pharmaceutical comprising them as an active ingredient 失效
标题翻译：三杂环化合物和包含它们作为活性成分的药物
公开(公告)号：US20060122392A1
公开(公告)日：2006-06-08
申请号：US11219736
申请日：2005-09-07
申请人： Hisao Nakai , Yoshifumi Kagamiishi
发明人： Hisao Nakai , Yoshifumi Kagamiishi
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04 , C07D487/14 , C07D491/14 , C07D495/14
摘要： Tri-heterocyclic compound of formula (I) wherein each of W, X and Y is carbon or nitrogen; each of U and Z is CR2, NR13, nitrogen, oxygen, sulfur etc.; A ring is carbocyclic ring, heterocyclic ring; R1 is alkyl, alkenyl, alkynyl, NR4R5, OR6 etc.; R3 is carbocyclic ring, heterocyclic ring; and a pharmaceutically acceptable salt thereof, a process for the preparation thereof, a pharmaceutical comprising them as an active ingredient. A compound of formula (I) is useful, in order to possess corticotropin releasing factor receptor antagonistic activity, for the prevention and/or treatment of depression, anxiety, eating disorder, posttraumatic stress disorder, peptic ulcer, irritable bowl syndrome, Alzheimer's disease, drug addiction or alcohol dependence syndrome etc.
摘要翻译：式（I）的三杂环化合物其中W，X和Y各自为碳或氮; U和Z各自为CR 2，NR 13，氮，氧，硫等; 环是碳环，杂环; R 1是烷基，烯基，炔基，NR 4 R 5或OR 6等; R 3是碳环，杂环; 及其药学上可接受的盐，其制备方法，包含它们作为活性成分的药物。为了预防和/或治疗抑郁症，焦虑症，进食障碍，创伤后应激障碍，消化性溃疡，易怒性碗综合症，阿尔茨海默氏病，阿尔茨海默氏症等，可以使用式（I）化合物，以便具有促肾上腺皮质激素释放因子受体拮抗作用，药物成瘾或酒精依赖综合征等

4. 发明授权

US07034153B2 Tricyclic and heterocyclic derivative compounds and drugs containing these compounds as the active ingredient 失效
标题翻译：三环和杂环衍生物化合物和含有这些化合物作为活性成分的药物
公开(公告)号：US07034153B2
公开(公告)日：2006-04-25
申请号：US10250328
申请日：2001-12-27
申请人： Hisao Nakai , Yoshifumi Kagamiishi
发明人： Hisao Nakai , Yoshifumi Kagamiishi
IPC分类号： C07D239/00
CPC分类号： C07D471/04 , C07D487/04 , C07D487/14 , C07D491/14 , C07D495/14
摘要： Tri-heterocyclic compound of formula (I) wherein each of W, X and Y is carbon or nitrogen; each of U and Z is CR2, NR13, nitrogen, oxygen, sulfur etc.; A ring is carbocyclic ring, heterocyclic ring; R1 is alkyl, alkenyl, alkynyl, NR4R5, OR6 etc.; R3 is carbocyclic ring, heterocyclic ring; and a pharmaceutically acceptable salt thereof, a process for the preparation thereof, a pharmaceutical comprising them as an active ingredient. A compound of formula (I) is useful, in order to possess corticotropin releasing factor receptor antagonistic activity, for the prevention and/or treatment of depression, anxiety, eating disorder, posttraumatic stress disorder, peptic ulcer, irritable bowl syndrome, Alzheimer's disease, drug addiction or alcohol dependence syndrome etc.
摘要翻译：式（I）的三杂环化合物，其中W，X和Y各自为碳或氮; U和Z各自为CR 2，NR 13，氮，氧，硫等; 环是碳环，杂环; R 1是烷基，烯基，炔基，NR 4 R 5或OR 6等; R 3是碳环，杂环; 及其药学上可接受的盐，其制备方法，包含它们作为活性成分的药物。为了预防和/或治疗抑郁症，焦虑症，进食障碍，创伤后应激障碍，消化性溃疡，易怒性碗综合症，阿尔茨海默氏病，阿尔茨海默氏症等，可以使用式（I）化合物，以便具有促肾上腺皮质激素释放因子受体拮抗作用，药物成瘾或酒精依赖综合征等

5. 发明授权

US07807688B2 Tri-heterocyclic compounds and a pharmaceutical comprising them as an active ingredient 失效
标题翻译：三杂环化合物和包含它们作为活性成分的药物
公开(公告)号：US07807688B2
公开(公告)日：2010-10-05
申请号：US12202984
申请日：2008-09-02
申请人： Hisao Nakai , Yoshifumi Kagamiishi
发明人： Hisao Nakai , Yoshifumi Kagamiishi
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D471/04 , C07D487/04 , C07D487/14 , C07D491/14 , C07D495/14
摘要： Tri-heterocyclic compound of formula (I) wherein each of W, X and Y is carbon or nitrogen; each of U and Z is CR2, NR13, nitrogen, oxygen, sulfur etc.; A ring is carbocyclic ring, heterocyclic ring; R1 is alkyl, alkenyl, alkynyl, NR4R5, OR6 etc.; R3 is carbocyclic ring, heterocyclic ring; and a pharmaceutically acceptable salt thereof, a process for the preparation thereof, a pharmaceutical comprising them as an active ingredient. A compound of formula (I) is useful, in order to possess corticotropin releasing factor receptor antagonistic activity, for the prevention and/or treatment of depression, anxiety, eating disorder, posttraumatic stress disorder, peptic ulcer, irritable bowl syndrome, Alzheimer's disease, drug addiction or alcohol dependence syndrome etc.
摘要翻译：式（I）的三杂环化合物其中W，X和Y各自为碳或氮; U和Z分别为CR2，NR13，氮，氧，硫等; 环是碳环，杂环; R1是烷基，烯基，炔基，NR4R5，OR6等; R3是碳环，杂环; 及其药学上可接受的盐，其制备方法，包含它们作为活性成分的药物。为了预防和/或治疗抑郁症，焦虑症，进食障碍，创伤后应激障碍，消化性溃疡，易怒性碗综合症，阿尔茨海默氏病，阿尔茨海默氏症等，可以使用式（I）化合物，以便具有促肾上腺皮质激素释放因子受体拮抗作用，药物成瘾或酒精依赖综合征等

6. 发明授权

US07459459B2 Tri-heterocyclic compounds and a pharmaceutical comprising them as an active ingredient 失效
标题翻译：三杂环化合物和包含它们作为活性成分的药物
公开(公告)号：US07459459B2
公开(公告)日：2008-12-02
申请号：US11219736
申请日：2005-09-07
申请人： Hisao Nakai , Yoshifumi Kagamiishi
发明人： Hisao Nakai , Yoshifumi Kagamiishi
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D239/70 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D471/04 , C07D487/04 , C07D487/14 , C07D491/14 , C07D495/14
摘要： Tri-heterocyclic compound of formula (I) wherein each of W, X and Y is carbon or nitrogen; each of U and Z is CR2, NR13, nitrogen, oxygen, sulfur etc.; A ring is carbocyclic ring, heterocyclic ring; R1 is alkyl, alkenyl, alkynyl, NR4R5, OR6 etc.; R3 is carbocyclic ring, heterocyclic ring; and a pharmaceutically acceptable salt thereof, a process for the preparation thereof, a pharmaceutical comprising them as an active ingredient. A compound of formula (I) is useful, in order to possess corticotropin releasing factor receptor antagonistic activity, for the prevention and/or treatment of depression, anxiety, eating disorder, posttraumatic stress disorder, peptic ulcer, irritable bowl syndrome, Alzheimer's disease, drug addiction or alcohol dependence syndrome etc.
摘要翻译：式（I）的三杂环化合物其中W，X和Y各自为碳或氮; U和Z分别为CR2，NR13，氮，氧，硫等; 环是碳环，杂环; R1是烷基，烯基，炔基，NR4R5，OR6等; R3是碳环，杂环; 及其药学上可接受的盐，其制备方法，包含它们作为活性成分的药物。为了预防和/或治疗抑郁症，焦虑症，进食障碍，创伤后应激障碍，消化性溃疡，易怒性碗综合症，阿尔茨海默氏病，阿尔茨海默氏症等，可以使用式（I）化合物，以便具有促肾上腺皮质激素释放因子受体拮抗作用，药物成瘾或酒精依赖综合征等

7. 发明申请

US20100137318A1 BICYCLIC HETEROCYCLIC COMPOUND 有权
标题翻译：双相杂环化合物
公开(公告)号：US20100137318A1
公开(公告)日：2010-06-03
申请号：US12597302
申请日：2008-04-25
申请人： Tetsuji Saito , Tetsuo Obitsu , Yoshifumi Kagamiishi
发明人： Tetsuji Saito , Tetsuo Obitsu , Yoshifumi Kagamiishi
IPC分类号： A61K31/53 , C07D487/04 , A61P25/22 , A61P25/18 , A61P1/00
CPC分类号： C07D487/04 , A61K31/53 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： A compound of a formula (I): wherein R1 represents a C3-10 branched alkyl group which may be substituted; R2 represents a hydrogen atom or a C1-4 alkyl group which may be substituted; R3 represents a C1-4 alkyl group which may be substituted or a halogen atom; R4 represents a C1-4 alkyl group which may be substituted; and ring 1 represents a cyclic group which has planarity and may have a substituent group, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a medicinal component having CRF antagonistic activity for the prevention and/or treatment of a neuropsychiatric disease, a peripheral organ disease and the like.
摘要翻译：式（I）的化合物：其中R1表示可被取代的C3-10支链烷基; R2表示氢原子或可被取代的C1-4烷基; R 3表示可以被取代的C 1-4烷基或卤素原子; R 4表示可以被取代的C 1-4烷基; 环1表示具有平面性并且可以具有取代基的环状基团，其盐，其N-氧化物或其溶剂合物或其前药可用作具有CRF拮抗活性的药物成分，用于预防和/ /或治疗神经精神疾病，外周器官疾病等。

8. 发明授权

US08420810B2 Bicyclic heterocyclic compound 有权
标题翻译：双环杂环化合物
公开(公告)号：US08420810B2
公开(公告)日：2013-04-16
申请号：US12597302
申请日：2008-04-25
申请人： Tetsuji Saito , Tetsuo Obitsu , Yoshifumi Kagamiishi
发明人： Tetsuji Saito , Tetsuo Obitsu , Yoshifumi Kagamiishi
IPC分类号： C07D487/04 , A61K31/53 , A61P3/04 , A61P15/12 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/30 , A61P25/32
CPC分类号： C07D487/04 , A61K31/53 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： A compound of a formula (I): wherein R1 represents a C3-10 branched alkyl group which may be substituted; R2 represents a hydrogen atom or a C1-4 alkyl group which may be substituted; R3 represents a C1-4 alkyl group which may be substituted or a halogen atom; R4 represents a C1-4 alkyl group which may be substituted; and ring 1 represents a cyclic group which has planarity and may have a substituent group, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a medicinal component having CRF antagonistic activity for the prevention and/or treatment of a neuropsychiatric disease, a peripheral organ disease and the like.
摘要翻译：式（I）的化合物：其中R1表示可被取代的C3-10支链烷基; R2表示氢原子或可被取代的C1-4烷基; R 3表示可以被取代的C 1-4烷基或卤素原子; R 4表示可以被取代的C 1-4烷基; 环1表示具有平面性并且可以具有取代基的环状基团，其盐，其N-氧化物或其溶剂合物或其前药可用作具有CRF拮抗活性的药物成分，用于预防和/ /或治疗神经精神疾病，外周器官疾病等。

9. 发明授权

US09517221B2 (2R)-2-propyloctanoic acid for functional brain disease 有权
标题翻译：（2R）-2-丙酸辛酸用于功能性脑病
公开(公告)号：US09517221B2
公开(公告)日：2016-12-13
申请号：US12282298
申请日：2007-03-08
申请人： Rika Shinagawa , Yoshifumi Kagamiishi , Taiji Shimoda
发明人： Rika Shinagawa , Yoshifumi Kagamiishi , Taiji Shimoda
IPC分类号： A61K31/20 , A61K45/06
CPC分类号： A61K31/20 , A61K45/06
摘要： [Problem to be solved]Provision of an agent for preventing or treating a functional brain disease and/or inhibiting symptom development of the same.[Means for solving the problems]An agent for preventing or treating a functional brain disease and/or inhibiting symptom development of the same, which comprises (2R)-2-propyloctanoic acid or a salt thereof.The agent for preventing or treating a functional brain disease and/or inhibiting symptom development of the same, which comprises (2R)-2-propyloctanoic acid or a salt thereof, can be safely administered to patients of, for example, functional brain diseases such as depression, menopausal mood disorder, perimenopausal mood disorder, panic disorder, irritable bowel syndrome, social anxiety disorder, post-traumatic stress disorder or the like, and also can show excellent effects.
摘要翻译：包括（2R）-2-丙基辛酸或其盐在内的预防或治疗功能性脑病和/或抑制其症状发展的药剂可以安全地施用于例如功能性脑疾病如作为抑郁症，绝经情绪障碍，围绝经期情绪障碍，恐慌症，肠易激综合征，社交焦虑症，创伤后应激障碍等，并且也可以显示出优异的效果。

10. 发明申请

US20080114012A1 Tricyclic Compound And Use Thereof 有权
标题翻译：三环化合物及其用途
公开(公告)号：US20080114012A1
公开(公告)日：2008-05-15
申请号：US11722623
申请日：2005-12-21
申请人： Kazuyuki Ohmoto , Masashi Kato , Yoshifumi Kagamiishi , Junichiro Manako
发明人： Kazuyuki Ohmoto , Masashi Kato , Yoshifumi Kagamiishi , Junichiro Manako
IPC分类号： A61K31/4747 , A61K31/4745 , C07D471/14
CPC分类号： C07D471/14 , A61K31/4375 , A61K31/438 , A61K45/06 , C07D471/04 , C07D471/10
摘要： The present invention relates to the compound represented by formula (I): (wherein, all the symbols has the same meanings as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof.Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.
摘要翻译：本发明涉及由式（I）表示的化合物：其中所有符号与说明书的含义相同），其盐，其溶剂合物或其前药。由于本发明的化合物具有抗应激作用，因此可用于由应激引起的疾病的预防和/或治疗剂，特别是由应激引起的消化系统疾病，优于口服吸收。

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