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：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：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。

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：US20080161326A1

公开(公告)日：2008-07-03

申请号：US10589693

申请日：2005-02-15

申请人： Norikazu Otake ,  Yoshio Ogino ,  Akio Kanatani

发明人： Norikazu Otake ,  Yoshio Ogino ,  Akio Kanatani

IPC分类号： A61K31/52 ,  C07D235/04 ,  A61K31/4184 ,  A61P3/04 ,  A61P3/10 ,  C07D473/00

CPC分类号： C07D471/04 ,  C07D235/14 ,  C07D473/00 ,  C07D487/04

摘要： The present invention relates to compounds of the general formula (I): wherein A, B, C and D each independently are a methine group or a nitrogen atom, said methine group optionally having a substituent(s) with at least one of them meaning the methine group; E means a group represented by the following formulae (E1): R1 means a lower alkyl group or an aryl group optionally having a substituent(s) or means a lower alkylene group linked to arbitrary, linkable position(s) of E, and others. The compounds of the present invention are useful as an agent for the treatment of a variety of diseases related to NPY.

摘要翻译： 本发明涉及通式（I）的化合物：其中A，B，C和D各自独立地为次甲基或氮原子，所述次甲基任选具有取代基，其中至少一个为含义 次甲基; E表示由下式（E1）表示的基团：R 1表示低级烷基或任选具有取代基的芳基，或指与任意可连接位置连接的低级亚烷基 （E）等。 本发明的化合物可用作治疗与NPY有关的各种疾病的药剂。

公开(公告)号：US20060205750A1

公开(公告)日：2006-09-14

申请号：US11431274

申请日：2006-05-10

申请人： Norikazu Otake ,  Minoru Moriya ,  Yoshio Ogino ,  Kenji Matsuda ,  Yoshikazu Nagae ,  Akio Kanatani ,  Takehiro Fukami

发明人： Norikazu Otake ,  Minoru Moriya ,  Yoshio Ogino ,  Kenji Matsuda ,  Yoshikazu Nagae ,  Akio Kanatani ,  Takehiro Fukami

IPC分类号： A61K31/4747 ,  A61K31/4184 ,  C07D487/10

CPC分类号： C07D473/30 ,  C07D405/04 ,  C07D471/04 ,  C07D471/10 ,  C07D473/00 ,  C07D491/04

摘要： The present invention relates to a compound of the formula (I): (wherein A, B, C and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is —N(SO2R4)—, —N(COR5)— or —CO—; Y is —C(R6)(R7)—, —O— or —N(R8)—, provided that the compound (I) when E is nitrogen, n is 0, X is —CO—, and Y is —O— is excluded) and the like, which are useful as an agent for the treatment of various diseases related to NPY, for example cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorder, inflammatory diseases or glaucoma, and the like, also for example, atherosclerosis, hypogonadism, hyperandrogenism, polycystic ovary syndrome (Pickwickian syndrome), hirsutism, gastro-intestinal motility disorder, obesity-related gastro-esophageal reflux, obesity hypoventilation, sleep apnea, inflammation, systemic inflammation of the vasculature, osteoarthritis, insulin resistance, bronchoconstriction, alcohol preference, metabolic syndrome, Alzheimer's disease, cardiac hypertrophy, left ventricular hypertrophy, hypertriglyceridemia, low HDL cholesterol, cardiovascular disorders such as coronary heart disease (CHD), cerebrovascular disease, stroke, peripheral vascular disease, sudden death, gallbladder diseases, cancer (breast, endometrial, colon), breathlessness, hyperuricemia, impaired fertility, low back pain, or increased anesthetic risk, and the like.