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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。
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公开(公告)号:US07504432B2
公开(公告)日:2009-03-17
申请号:US11648614
申请日:2007-01-03
申请人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
发明人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号: A01N43/36 , C07D207/00
CPC分类号: C07D207/08 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10
摘要: This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X− signifies an anion].
摘要翻译: 本发明涉及具有选择性毒蕈碱M3受体拮抗作用,副作用小,适用于吸入治疗的化合物,并且可用作通式(I)的呼吸系统疾病的治疗剂; [其中A表示由式(a0)或(b0)表示的组; Ar表示任选取代的芳基或杂芳基; B1和B2表示脂族烃; R1表示氟取代的环烷基; R2,R3和R4表示低级烷基,单键或与B1键合的亚烷基,或者R2和R3相连,表示亚烷基; R5和R7表示氢,低级烷基或键合到B2的单键或亚烷基; R6表示氢,低级烷基或表示为-N(R8)R9的基团; 和X-表示阴离子]。
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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。
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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。
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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。
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公开(公告)号:US07164024B2
公开(公告)日:2007-01-16
申请号:US10475447
申请日:2002-04-19
申请人: Takeru Yamakawa , Yoshio Ogino , Yufu Sagara , Kenji Matsuda , Akira Naya , Toshifumi Kimura , Norikazu Otake
发明人: Takeru Yamakawa , Yoshio Ogino , Yufu Sagara , Kenji Matsuda , Akira Naya , Toshifumi Kimura , Norikazu Otake
IPC分类号: A61K31/44
CPC分类号: C07D401/14 , C07D409/14
摘要: This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I] [in which R1 and R2 stand for, e.g., hydrogen atoms; R3a, R3b, R4, R5 stand for, e.g., hydrogen atoms and alkyl groups; R6 stands for e.g., aryl or heteroaryl groups; A ring stands for 5- to 8-membered aliphatic heterocyclic ring containing one nitrogen atom; and Z stands for carbonyl group or sulfonyl group]. The benzimidazolone derivatives of the invention exhibit antagonism to muscarinic acetylcholine receptors, and are useful as treating agent and/or prophylactic of Parkinson's disease, drug-induced parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary dyskinesia, achalasia, pain, itch, cholinergic urticaria, irritable bowel syndrome, vomiting, nausea, dizziness, Meniere's disease, motion sickness and urinary disturbance.
摘要翻译: 本发明涉及由通式[I] [其中R 1,R 2和R 2]的化合物代表的例如氢原子的苯并咪唑酮衍生物; R 3a,R 3b,R 4,R 5表示例如氢原子和烷基; R 6表示例如芳基或杂芳基; 环代表含有一个氮原子的5-至8-元脂族杂环; Z代表羰基或磺酰基]。 本发明的苯并咪唑酮衍生物对毒蕈碱性乙酰胆碱受体表现出拮抗作用,可用作帕金森病,药物诱发的帕金森综合征,肌张力障碍,运动不良,胰腺炎,胆石,胆囊炎,胆汁运动障碍,贲门失弛缓症,疼痛,瘙痒的治疗剂和/或预防 ,胆碱能性荨麻疹,肠易激综合征,呕吐,恶心,眩晕,梅尼埃病,运动病和尿紊乱。
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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.
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公开(公告)号:US4814328A
公开(公告)日:1989-03-21
申请号:US911780
申请日:1986-09-26
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D217/02 , C07D501/46
CPC分类号: C07D217/02 , Y02P20/55
摘要: The compound having the formula: ##STR1## wherein R is a straight chain, branched chain or cyclic lower alkyl, a lower alkenyl or a lower alkynyl group which may be substituted by a carboxyl group, and R.sup.1 is hydrogen atom or an acetyl group; or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.
摘要翻译: 具有下式的化合物:其中R是可被羧基取代的直链,支链或环状低级烷基,低级链烯基或低级炔基,R 1是氢原子 或乙酰基; 或其药学上可接受的盐,生理上可水解的酯或其溶剂合物。
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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。
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公开(公告)号:US20070129397A1
公开(公告)日:2007-06-07
申请号:US11648614
申请日:2007-01-03
申请人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
发明人: Yoshio Ogino , Hideki Kurihara , Kenji Matsuda , Tomoshige Numazawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号: A61K31/46 , C07D451/00 , C07D211/34 , A61K31/445 , A61K31/40 , C07D207/04
CPC分类号: C07D207/08 , C07C219/10 , C07C219/14 , C07D205/04 , C07D207/12 , C07D209/52 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D239/06 , C07D451/02 , C07D451/06 , C07D471/08 , C07D471/10 , C07D487/10
摘要: This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X−signifies an anion].
摘要翻译: 本发明涉及具有选择性毒蕈碱M 3受体拮抗作用,副作用小,适用于吸入治疗的化合物,并且可用作通式(I)的呼吸系统疾病的治疗剂; [其中A表示由式(a
0 SUB>)或(b 0>)表示的组; Ar表示任选取代的芳基或杂芳基; B 1和B 2表示脂族烃; R 1表示氟取代的环烷基; R 2,R 3和R 4表示低级烷基,单键或与B 1连接的亚烷基,或 R 2和R 3结合起来表示亚烷基; R 5和R 7表示氢,低级烷基或键合到B 2的单键或亚烷基; R 6表示氢,低级烷基或以-N(R 8)R 9表示的基团; 和X - 表示阴离子]。
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