公开(公告)号：US07875633B2

公开(公告)日：2011-01-25

申请号：US11990889

申请日：2006-08-23

申请人： Akira Naya ,  Toshihiro Sakamoto ,  Yuji Haga ,  Norikazu Otake

发明人： Akira Naya ,  Toshihiro Sakamoto ,  Yuji Haga ,  Norikazu Otake

IPC分类号： A61K31/444 ,  A61K31/4439 ,  A61K31/5377 ,  A61K31/4545 ,  A61P9/00 ,  A61P25/00 ,  A61P3/00 ,  C07D213/64 ,  C07D401/02 ,  C07D413/02 ,  C07D401/14

CPC分类号： C07D213/69 ,  C07D213/64 ,  C07D401/10 ,  C07D413/10

摘要： A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents —CH2—O—, —CH═CH— or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.

摘要翻译： 作为活性成分，含有式（I）所示的化合物：其中，R 1和R 2分别独立地表示氢原子，低级烷基等，或者与连接有L，Z 2和R 1的氮原子一起形成 可以形成脂族氮杂环基，并且R 1和R 2与它们所连接的氮原子一起形成脂族氮杂环基; X表示次甲基或氮原子; Y表示-CH 2 -O-，-CH = CH-等; Z1表示单键，C1-4亚烷基等; Z2表示单键或C1-4亚烷基; L表示亚甲基，C3-8亚环烷基等; Ar表示芳族碳环基等。 该化合物可用作中枢神经系统疾病，心血管疾病或代谢疾病的药物。

公开(公告)号：US20090137587A1

公开(公告)日：2009-05-28

申请号：US11990889

申请日：2006-08-23

申请人： Akira Naya ,  Toshihiro Sakamoto ,  Yuji Haga ,  Norikazu Otake

发明人： Akira Naya ,  Toshihiro Sakamoto ,  Yuji Haga ,  Norikazu Otake

IPC分类号： A61K31/444 ,  C07D213/64 ,  C07D401/02 ,  C07D413/02 ,  A61K31/4439 ,  A61P9/00 ,  A61P25/00 ,  A61P3/00 ,  C07D401/14 ,  A61K31/5377 ,  A61K31/4545

CPC分类号： C07D213/69 ,  C07D213/64 ,  C07D401/10 ,  C07D413/10

摘要： A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents —CH2—O—, —CH═CH— or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.

摘要翻译： 作为活性成分，含有式（I）所示的化合物：其中，R 1和R 2分别独立地表示氢原子，低级烷基等，或者与连接有L，Z 2和R 1的氮原子一起形成 可以形成脂族氮杂环基，并且R 1和R 2与它们所连接的氮原子一起形成脂族氮杂环基; X表示次甲基或氮原子; Y表示-CH 2 -O - ， - CH-CH-等; Z1表示单键，C1-4亚烷基等; Z2表示单键或C1-4亚烷基; L表示亚甲基，C3-8亚环烷基等; Ar表示芳族碳环基等。 该化合物可用作中枢神经系统疾病，心血管疾病或代谢疾病的药物。

公开(公告)号：US07732456B2

公开(公告)日：2010-06-08

申请号：US10591373

申请日：2005-03-04

申请人： Norikazu Otake ,  Yuji Haga ,  Akira Naya ,  Sayaka Mizutani ,  Akio Kanatani

发明人： Norikazu Otake ,  Yuji Haga ,  Akira Naya ,  Sayaka Mizutani ,  Akio Kanatani

IPC分类号： A61K31/444 ,  C07D401/02

CPC分类号： C07D213/69 ,  C07D237/16 ,  C07D239/52 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D451/02 ,  C07D471/04

摘要： The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R1 and R2 may be same or different and stands for H, etc., or R1 and R2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X1-X3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X4-X7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y1 and Y3 may be same or different and stand for single bond, —O—, —NR—, —S—, etc; Y2 stands for lower lkylene, etc.; R stands for H, etc., L stands for methylene; Z1 and Z2 may be same or different and stand for single bond or lower alkylene; or R1, L and Z2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R1 binds; and Ar stands for aromatic carbocyclic group, etc.].

摘要翻译： 本发明提供由通式（I）表示的吡啶酮衍生物[在该式中，R 1和R 2可以相同或不同，代表H等，或者R 1和R 2可以与脂族含氮杂环基一起形成 他们绑定的N X1-X3可以相同或不同，代替次甲基或N，但不是全部同时代表氮; X4-X7可以相同或不同，代表次甲基或N，条件是它们中的三个或更多不同时代表N; Y1和Y3可以相同或不同，代表单键，-O-，-NR-，-S-等; Y2代表低级亚烷基等; R代表H等，L代表亚甲基; Z 1和Z 2可以相同或不同，代表单键或低级亚烷基; 或R1，L和Z2可以与R1结合的N形成脂族含氮杂环基; 和Ar代表芳族碳环基团等]。

公开(公告)号：US20070208046A1

公开(公告)日：2007-09-06

申请号：US10591373

申请日：2005-03-04

申请人： Norikazu Otake ,  Yuji Haga ,  Akira Naya ,  Sayaka Mizutani ,  Akio Kanatani

发明人： Norikazu Otake ,  Yuji Haga ,  Akira Naya ,  Sayaka Mizutani ,  Akio Kanatani

IPC分类号： A61K31/513 ,  A61K31/444 ,  A61K31/4412 ,  C07D403/02 ,  C07D401/02

CPC分类号： C07D213/69 ,  C07D237/16 ,  C07D239/52 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D451/02 ,  C07D471/04

摘要： The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R1 and R2 may be same or different and stands for H, etc., or R1 and R2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X1-X3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X4-X7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y1 and Y3 may be same or different and stand for single bond, —O—, —NR—, —S—, etc; Y2 stands for lower alkylene, etc.; R stands for H, etc., L stands for methylene; Z1 and Z2 may be same or different and stand for single bond or lower alkylene; or R1, L and Z2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R1 binds; and Ar stands for aromatic carbocyclic group, etc.].

摘要翻译： 本发明提供由通式（I）表示的吡啶酮衍生物[在式中，R 1和R 2可以相同或不同，代表H等， 或R 1和R 2可以与它们所键合的N一起形成脂族含氮杂环基; X 1 -X 3可以相同或不同，代表次甲基或N，但并不全部同时代表氮; X 4 -X 7可以相同或不同，代表次甲基或N，条件是它们中的三个或更多个不同时代表N; Y 1和Y 3可以相同或不同，代表单键，-O-，-NR-，-S-等; Y 2代表低级亚烷基等; R代表H等，L代表亚甲基; Z 1和Z 2可以相同或不同，代表单键或低级亚烷基; 或R 1，L和Z 2可以与R 1结合的N形成脂族含氮杂环基; 和Ar代表芳族碳环基团等]。

公开(公告)号：US20100216758A1

公开(公告)日：2010-08-26

申请号：US11989876

申请日：2006-08-03

申请人： Makoto Ando ,  Etsuko Sekino ,  Yuji Haga ,  Norikazu Otake ,  Minoru Moriya

发明人： Makoto Ando ,  Etsuko Sekino ,  Yuji Haga ,  Norikazu Otake ,  Minoru Moriya

IPC分类号： A61K31/397 ,  C07D401/02 ,  A61K31/4439 ,  C07D213/04 ,  A61K31/44 ,  C07D401/14 ,  A61K31/444 ,  C07D239/36 ,  A61K31/513 ,  C07D213/89 ,  C07D403/14 ,  A61K31/55 ,  C07D211/94 ,  A61K31/4545 ,  C07D221/24 ,  A61P3/00 ,  A61P5/00 ,  A61P9/00 ,  A61P11/00 ,  A61P15/00 ,  A61P1/00 ,  A61P13/00 ,  A61P25/00 ,  A61P35/00

CPC分类号： C07D213/69 ,  C07D213/64 ,  C07D213/89 ,  C07D239/52 ,  C07D401/10 ,  C07D401/14 ,  C07D405/10 ,  C07D487/08

摘要： An active ingredient is a compound represented by the general formula [I]: [wherein R1 and R2 represent a lower alkyl group, a C3-6 cycloalkyl group or the like, X1 and X2 represent methine, an Ar—Y1—Y2—Y3-substituted methine or the like, however either of them is an Ar—Y1—Y2—Y3-substituted methine, X3 to X8 represent methine, —N— or the like, Y1 and Y3 represent a single bond, —O— or the like, Y2 represent a single bond, a lower alkylene group or the like, W represent —(O)—(CH2)n-(O)— or the like, n represents an integer of 1 to 4, L and Z2 represent a single bond or a methylene group, Z1 represents a single bond, a C1-4 alkylene group or the like, and Ar represents an aromatic carbocyclic group or the like]. The compound acts as a melanin-concentrating hormone receptor antagonist and useful as a therapeutic agent for obesity or the like.

摘要翻译： 活性成分是由通式[I]表示的化合物：[其中R1和R2表示低级烷基，C3-6环烷基等，X1和X2表示次甲基，Ar-Y1-Y2-Y3 - 取代的次甲基等，但是它们都是Ar-Y1-Y2-Y3-取代的次甲基，X3至X8表示次甲基，-N-等，Y1和Y3表示单键，-O-或 类似的，Y2表示单键，低级亚烷基等，W表示 - （O） - （CH2）n-（O） - 等，n表示1〜4的整数，L和Z2表示 单键或亚甲基，Z1表示单键，C1-4亚烷基等，Ar表示芳香族碳环基等]。 该化合物作为黑色素浓缩激素受体拮抗剂起作为肥胖症等的治疗剂的作用。

公开(公告)号：US20060111380A1

公开(公告)日：2006-05-25

申请号：US10536360

申请日：2003-11-25

申请人： Norikazu Otake ,  Yuji Haga ,  Makoto Jitsuoka ,  Akio Kanatani

发明人： Norikazu Otake ,  Yuji Haga ,  Makoto Jitsuoka ,  Akio Kanatani

IPC分类号： A61K31/4747 ,  C07D471/10

CPC分类号： C07D491/10

摘要： The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.

摘要翻译： 本发明涉及式（I）化合物：其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T，U，V和W独立为次甲基或氮，所述次甲基任选被取代基取代，T，U，V和W中的至少两个为所述次甲基; X是氮或次甲基。 本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，神经系统疾病，基因疾病，代谢疾病，生殖器或生殖障碍，胃肠道疾病，呼吸系统疾病，炎症性疾病 疾病或青光眼等。

公开(公告)号：US20090264426A1

公开(公告)日：2009-10-22

申请号：US11991334

申请日：2006-09-05

申请人： Shunji Sakuraba ,  Minoru Kameda ,  Hiroyuki Kishino ,  Yuji Haga ,  Norikazu Otake ,  Minoru Moriya

发明人： Shunji Sakuraba ,  Minoru Kameda ,  Hiroyuki Kishino ,  Yuji Haga ,  Norikazu Otake ,  Minoru Moriya

IPC分类号： A61K31/5377 ,  C07D401/10 ,  C07D413/14 ,  A61K31/47 ,  A61P9/10

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D405/04 ,  C07D471/04

摘要： Disclosed is a compound represented by the formula (I): Wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like; X1, X2 and X3 independently represent a methine group or a nitrogen atom; Y1 and Y3 independently represent a single bond, —O— or the like; Y2 represents a lower alkylene group or the like; W1 to W4 independently represent a single bond, a methylene group or the like; L represents a single bond, a methylene group or the like; Z1 and Z2 independently represent a single bond, a C1-4 alkylene group or the like; Ar1 represents an aromatic carbocyclic ring or the like; and Ar2 represents a bicyclic aromatic carbocyclic ring or the like. The compound is useful as a pharmaceutical for a central disease, a cardiovascular disease or a metabolic disease.

摘要翻译： 公开了由式（I）表示的化合物：其中R1和R2独立地表示氢原子，低级烷基等; X1，X2和X3独立地表示次甲基或氮原子; Y1和Y3独立地表示单键，-O-等; Y2表示低级亚烷基等; W1至W4独立地表示单键，亚甲基等; L表示单键，亚甲基等; Z 1和Z 2独立地表示单键，C 1-4亚烷基等; Ar 1表示芳香族碳环等， Ar 2表示双环芳香族碳环等。 该化合物可用作中枢性疾病，心血管疾病或代谢性疾病的药物。

公开(公告)号：US07589096B2

公开(公告)日：2009-09-15

申请号：US12071808

申请日：2008-02-26

申请人： Norikazu Otake ,  Yuji Haga ,  Makoto Jitsuoka ,  Akio Kanatani

发明人： Norikazu Otake ,  Yuji Haga ,  Makoto Jitsuoka ,  Akio Kanatani

IPC分类号： A61K31/438 ,  A61K31/506 ,  A61K31/4545 ,  C07D233/96 ,  C07D401/14 ,  C07D401/02

CPC分类号： C07D491/10

摘要： The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, wherein a methine may be optionally substituted by a substituent, and at least two of T, U, V and W are methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.

摘要翻译： 本发明涉及式（I）化合物：其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T，U，V和W独立地是次甲基或氮，其中次甲基可以任选地被取代基取代，并且T，U，V和W中的至少两个是次甲基; X是氮或次甲基。 本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，神经系统疾病，基因疾病，代谢疾病，生殖器或生殖障碍，胃肠道疾病，呼吸障碍 ，炎症性疾病或青光眼等。

公开(公告)号：US20080188507A1

公开(公告)日：2008-08-07

申请号：US12071808

申请日：2008-02-26

申请人： Norikazu Otake ,  Yuji Haga ,  Makoto Jitsuoka ,  Akio Kanatani

发明人： Norikazu Otake ,  Yuji Haga ,  Makoto Jitsuoka ,  Akio Kanatani

IPC分类号： A61K31/4747 ,  C07D491/14

CPC分类号： C07D491/10

摘要： The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine.The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.

摘要翻译： 本发明涉及式（I）化合物：其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T，U，V和W独立为次甲基或氮，所述次甲基任选被取代基取代，T，U，V和W中的至少两个为所述次甲基; X是氮或次甲基。 本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，神经系统疾病，基因疾病，代谢疾病，生殖器或生殖障碍，胃肠道疾病，呼吸障碍 ，炎症性疾病或青光眼等。

公开(公告)号：US07365079B2

公开(公告)日：2008-04-29

申请号：US10536360

申请日：2003-11-25

申请人： Norikazu Otake ,  Yuji Haga ,  Makoto Jitsuoka ,  Akio Kanatani

发明人： Norikazu Otake ,  Yuji Haga ,  Makoto Jitsuoka ,  Akio Kanatani

IPC分类号： A61K31/4355 ,  C07D471/04

CPC分类号： C07D491/10

摘要： The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.

摘要翻译： 本发明涉及式（I）化合物：其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T，U，V和W独立为次甲基或氮，所述次甲基任选被取代基取代，T，U，V和W中的至少两个为所述次甲基; X是氮或次甲基。 本发明的化合物可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，神经系统疾病，基因疾病，代谢疾病，生殖器或生殖障碍，胃肠道疾病，呼吸系统疾病，炎症性疾病 疾病或青光眼等。