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1. 发明授权

US06649624B2 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06649624B2
公开(公告)日：2003-11-18
申请号：US10226225
申请日：2002-08-23
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： A61K31438
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： A method for treating a central nervous system disorder, which involves administering to a patient in need a therapeutically effective amount of a compound of formula (I): wherein Ar1 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, nitro, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, cyclo(lower) alkyl, lower alkenyl, lower alkoxy, halo(lower) alkoxy, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylene optionally substituted with oxo, and a group represented by the formula —Q—Ar2; Ar2 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, cyano, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, hydroxy, lower alkoxy, halo(lower) alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl: n represents 0 or 1; Q represents a single bond or carbonyl; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine; Y represents an imino which may be substituted with lower alkyl, or oxygen; or a salt or ester thereof
摘要翻译：一种治疗中枢神经系统疾病的方法，其涉及向需要的患者施用治疗有效量的式（I）化合物：其中Ar 1表示可被取代的芳基或杂芳基，所选择的取代基卤代低级烷基，羟基（低级）烷基，环（低级）烷基，低级烯基，低级烷氧基，卤代（低级）烷氧基，低级烷硫基，羧基，低级烷酰基，低级烷氧基羰基，任选被氧代取代的低级亚烷基和由式-Q-Ar 2表示的基团; Ar 2表示可被取代的芳基或杂芳基，该取代基选自卤素，氰基，低级烷基，卤代（低级）烷基，羟基（低级）烷基，羟基，低级烷氧基，卤代（低级）烷氧基，低级烷基氨基，二低级烷基氨基，低级烷酰基和芳基：n表示0或1; Q表示单键或羰基; T，U，V和W各自独立地表示反应可以具有选自卤素，低级烷基，羟基和低级烷氧基的取代基的氮原子或次甲基，其中至少两个表示所述次甲基; X表示次甲基; Y表示亚氨基，被低级烷基或氧取代; 或其盐或酯

2. 发明授权

US06388077B1 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06388077B1
公开(公告)日：2002-05-14
申请号：US09983598
申请日：2001-10-25
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： C07D491107
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： Compounds of the general formula VI-1 and processes for their preparation: wherein t, u, v and w each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and optionally protected hydroxy; and wherein at least two of which represent the methine group. These compounds serve as intermediates for novel spiro compounds which exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.
摘要翻译：通式VI-1的化合物及其制备方法：其中t，u，v和w各自独立地表示氮原子或次甲基，其可以具有选自卤素，低级烷基，低级烷氧基和任选保护的羟基; 并且其中至少两个表示次甲基。这些化合物用作新的螺旋化合物的中间体，其表现出神经肽Y受体（NPY）拮抗活性，并且可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，中枢神经系统疾病，代谢疾病等。

3. 发明授权

US06335345B1 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06335345B1
公开(公告)日：2002-01-01
申请号：US09928431
申请日：2001-08-14
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： A61K31506
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： Spiro compounds of the general formula (I): wherein Ar1 represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents methine; Y represents an optionally substituted imino or oxygen atom. These novel spiro compounds exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.
摘要翻译：通式（I）的螺环化合物：其中Ar1表示任选取代的芳基或杂芳基; n表示0或1; T，U，V和W各自表示氮原子或任选取代的次甲基，其中至少两个其表示次甲基; X表示次甲基; Y表示任选取代的亚氨基或氧原子。这些新型螺环化合物表现出神经肽Y受体（NPY）拮抗活性，可用作治疗与NPY有关的各种疾病的药剂，例如心血管疾病，中枢神经系统疾病，全身性疾病等。

4. 发明授权

US06326375B1 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06326375B1
公开(公告)日：2001-12-04
申请号：US09640784
申请日：2000-08-18
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： A61K31438
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： Spiro compounds of the general formula (I): wherein Ar1 represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents nitrogen; Y represents an optionally substituted imino or oxygen atom, which exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.
摘要翻译：通式（I）的螺环化合物：其中Ar1表示任选取代的芳基或杂芳基; n表示0或1; T，U，V和W各自表示氮原子或任选取代的次甲基，其中至少两个代表所述次甲基; X表示氮; Y表示任选取代的亚氨基或氧原子，其表现出神经肽Y受体（NPY）拮抗活性，可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，中枢神经系统疾病，全身性疾病等。

5. 发明授权

US07304072B2 Spiro compounds 失效
标题翻译：螺环化合物
公开(公告)号：US07304072B2
公开(公告)日：2007-12-04
申请号：US10922869
申请日：2004-08-23
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh , Masato Chiba
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh , Masato Chiba
IPC分类号： A61K31/4355 , C07D491/048
CPC分类号： C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10
摘要： Compounds represented by the general formula (I) wherein Ar1 represents an aryl or heteroaryl which may be substituted; n represents 0 or 1; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen; and a salt, ester or N-oxide derivative thereof. The compounds exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases, sexual and reproductive dysfunctions, gastro-intestinal disorders, respiratory disorders, inflammation or glaucoma, and the like.
摘要翻译：由通式（I）表示的化合物

6. 发明授权

US06803372B2 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06803372B2
公开(公告)日：2004-10-12
申请号：US10092549
申请日：2002-03-08
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： A61K31506
CPC分类号： C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10
摘要： Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.
摘要翻译：通式（I）的化合物：其中Ar 1表示任选取代的芳基或杂芳基; n表示0或1; T，U，V和W各自独立地表示氮原子或任选取代的次甲基，其中至少两个代表所述次甲基; X表示次甲基或羟基取代的次甲基; Y表示任选取代的亚氨基或氧原子。这些新颖的螺环化合物可用作神经肽Y受体拮抗剂和用作治疗各种心血管疾病，中枢神经系统疾病，代谢疾病等的药剂。

7. 发明授权

US06723847B2 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06723847B2
公开(公告)日：2004-04-20
申请号：US10453737
申请日：2003-06-04
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： C07D40514
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： The present invention is directed to novel spiro compounds useful as neuropeptide Y receptor antagonists.
摘要翻译：本发明涉及可用作神经肽Y受体拮抗剂的新型螺环化合物。

8. 发明申请

US20050032820A1 Novel spiro compounds 失效
公开(公告)号：US20050032820A1
公开(公告)日：2005-02-10
申请号：US10922869
申请日：2004-08-23
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh , Masato Chiba
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh , Masato Chiba
IPC分类号： C07D491/107 , A61K31/438 , A61P1/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/06 , A61P29/00 , A61P43/00 , C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10 , C07D519/00 , C07D487/14 , A61K31/4747 , A61K31/519
CPC分类号： C07D213/61 , C07D307/94 , C07D405/12 , C07D471/10 , C07D491/10
摘要： A Compound represented by the general formula (I): wherein AR1 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of hydroxy, halogen, nitro, lower alkyl, halo(lower)alkyl, hydroxy(lower)alkyl, cyclo(lower)alkyl, lower alkenyl, lower alkoxy, halo(lower)alkoxy, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylene optionally substituted with oxo, and a group represented by the formula —Q—Ar2; Ar2represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, cyano, lower alkyl, halo(lower)alkyl, hydroxy(lower)alkyl, hydroxy, lower alkoxy, halo(lower)alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl; n represents 0 or 1; Q represents a single bond or carbonyl; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen; and a salt, ester or N-oxide derivative thereof exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis and the like, central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal and the like, metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia and the like, sexual and reproductive dysfunction, gastro-intestinal disorder, respiratory disorder, inflammation or glaucoma, and the like.

9. 发明授权

US06462053B1 Spiro compounds 失效
标题翻译：螺环化合物
公开(公告)号：US06462053B1
公开(公告)日：2002-10-08
申请号：US10101221
申请日：2002-03-20
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： A61K34355
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： A method for treating a cardiovascular disorder, which involves administering to a patient in need a therapeutically effective amount of a compound of formula (I): wherein Ar1 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, nitro, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, cyclo(lower) alkyl, lower alkenyl, lower alkoxy, halo(lower) alkoxy, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylene optionally substituted with oxo, and a group represented by the formula —Q—Ar2; Ar2 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, cyano, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, hydroxy, lower alkoxy, halo(lower) alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl: n represents 0 or 1; Q represents a single bond or carbonyl; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine; Y represents an imino which may be substituted with lower alkyl, or oxygen; or a salt or ester thereof.
摘要翻译：一种治疗心血管疾病的方法，其涉及向需要的患者施用治疗有效量的式（I）化合物：其中Ar1表示可被取代的芳基或杂芳基，所述取代基选自卤素，硝基，低级烷基，卤代（低级）烷基，羟基（低级）烷基，环（低级）烷基，低级烯基，低级烷氧基，卤代（低级）烷氧基，低级烷硫基，羧基，低级烷酰基，低级烷氧基羰基，任选被氧代取代的基团和由式-Q-Ar 2表示的基团; Ar 2表示可被取代的芳基或杂芳基，所述取代基选自卤素，氰基，低级烷基，卤代（低级）烷基，羟基（低级）烷基，羟基，低级烷氧基，卤代（低级）烷氧基，低级烷基氨基，二低级烷基氨基，低级烷酰基和芳基：n表示0或1; Q表示单键或羰基; T，U， W各自独立地表示硝基可以具有选自卤素，低级烷基，羟基和低级烷氧基的取代基的次甲基，其中至少两个表示所述次甲基; X表示次甲基; Y表示可以被取代的亚氨基与低级烷基或氧; 或其盐或酯。

10. 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。

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