Heterocycle-substituted benzimidazole derivative
    11.
    发明授权
    Heterocycle-substituted benzimidazole derivative 有权
    杂环取代的苯并咪唑衍生物

    公开(公告)号:US07994331B2

    公开(公告)日:2011-08-09

    申请号:US11988592

    申请日:2006-07-12

    IPC分类号: C07D413/14 A61K31/44

    摘要: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein X1 to X4 independently represent a carbon atom or the like; the ring A represents a 5- to 6-membered heteroaryl having 1 to 4 heteroatoms independently selected from the group consisting of a nitrogen atom, a sulfur atom and an oxygen atom; X5 represents an oxygen atom or the like; X represents a carbon atom or the like; Het represents a 5- or 6-membered aliphatic heterocycle; R1 represents an aryl or the like; R2 represents a formyl group or the like; and R3 represents a —C1-6 alkyl or the like. The compound or salt has a glucokinase activation effect and is useful as a therapeutic agent for diabetes.

    摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐:(I)其中X 1至X 4独立地表示碳原子等; 环A表示具有1至4个独立地选自氮原子,硫原子和氧原子的杂原子的5-至6-元杂芳基; X 5表示氧原子等; X表示碳原子等; Het代表5-或6-元脂族杂环; R1表示芳基等; R2表示甲酰基等; 并且R 3表示-C 1-6烷基等。 化合物或盐具有葡糖激酶活化作用,可用作糖尿病的治疗剂。

    2-heteroaryl-substituted benzimidazole derivative
    12.
    发明授权
    2-heteroaryl-substituted benzimidazole derivative 有权
    2-杂芳基取代的苯并咪唑衍生物

    公开(公告)号:US07728025B2

    公开(公告)日:2010-06-01

    申请号:US10582564

    申请日:2004-12-28

    IPC分类号: A01N43/50

    摘要: A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided.A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II): (in the formula, X represents a carbon atom or a nitrogen atom); R1 represents an aryl, etc.; R2 represents a hydroxy, etc.; R3 represents a —C1-6 alkyl, etc.; R4 represents a —C1-6 alkyl, etc.; X5 represents —O—, etc.; a indicates an integer of 1, 2 or 3; q indicates an integer of from 0 to 2; m indicates an integer of from 0 to 2].

    摘要翻译: 提供葡糖激酶活化剂; 提供了糖尿病的补救措施和/或预防,糖尿病的补救和/或预防,如视网膜病变,肾病,神经症,缺血性心脏病,动脉硬化,以及进一步的补救措施和/或预防肥胖症。 一种葡糖激酶活化剂,其特征在于含有通式(I-0)的2-杂芳基取代的苯并咪唑衍生物或其药学上可接受的盐:[式中X表示碳原子或氮原子; X1,X2,X3和X4各自独立地表示碳原子或氮原子; 环A表示式(II)的5-或6-元含氮芳族杂环:(式中,X表示碳原子或氮原子); R1表示芳基等。 R2代表羟基等; R3代表-C 1-6烷基等; R4代表-C 1-6烷基等; X5表示-O-等。 a表示1,2或3的整数; q表示0〜2的整数, m表示0〜2的整数]。

    Heterocycle-substituted benzimidazole derivative
    13.
    发明申请
    Heterocycle-substituted benzimidazole derivative 有权
    杂环取代的苯并咪唑衍生物

    公开(公告)号:US20100087360A1

    公开(公告)日:2010-04-08

    申请号:US11988592

    申请日:2006-07-12

    摘要: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein X1 to X4 independently represent a carbon atom or the like; the ring A represents a 5- to 6-membered heteroaryl having 1 to 4 heteroatoms independently selected from the group consisting of a nitrogen atom, a sulfur atom and an oxygen atom; X5 represents an oxygen atom or the like; X represents a carbon atom or the like; Het represents a 5- or 6-membered aliphatic heterocycle; R1 represents an aryl or the like; R2 represents a formyl group or the like; and R3 represents a —C1-6 alkyl or the like. The compound or salt has a glucokinase activation effect and is useful as a therapeutic agent for diabetes.

    摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐:(I)其中X 1至X 4独立地表示碳原子等; 环A表示具有1至4个独立地选自氮原子,硫原子和氧原子的杂原子的5-至6-元杂芳基; X 5表示氧原子等; X表示碳原子等; Het代表5-或6-元脂族杂环; R1表示芳基等; R2表示甲酰基等; 并且R 3表示-C 1-6烷基等。 化合物或盐具有葡糖激酶活化作用,可用作糖尿病的治疗剂。

    Novel Sulfone Amide Amide Derivatives
    15.
    发明申请
    Novel Sulfone Amide Amide Derivatives 失效
    新型磺酰胺酰胺衍生物

    公开(公告)号:US20080161326A1

    公开(公告)日:2008-07-03

    申请号:US10589693

    申请日:2005-02-15

    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。

    Benzimidazolone derivatives
    16.
    发明授权
    Benzimidazolone derivatives 失效
    苯并咪唑酮衍生物

    公开(公告)号:US07164024B2

    公开(公告)日:2007-01-16

    申请号:US10475447

    申请日:2002-04-19

    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。

    Novel benzimidazole derivatives
    17.
    发明申请

    公开(公告)号:US20060205750A1

    公开(公告)日:2006-09-14

    申请号:US11431274

    申请日:2006-05-10

    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.

    Aryloxy-Substituted Benzimidazole Derivatives
    18.
    发明申请
    Aryloxy-Substituted Benzimidazole Derivatives 有权
    芳氧基取代的苯并咪唑衍生物

    公开(公告)号:US20080125429A1

    公开(公告)日:2008-05-29

    申请号:US11666555

    申请日:2005-11-01

    摘要: A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided.The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group β; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of X1 to X4 are carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.

    摘要翻译: 提供葡糖激酶活化剂; 提供糖尿病的治疗和/或预防,或治疗和/或预防糖尿病如视网膜病,肾病,神经症,缺血性心脏病,动脉硬化,以及进一步的治疗和/或预防肥胖症。 本发明涉及式(I)的化合物:其中R 1和R 2代表氢等; R 3表示氢原子,卤素原子等; R 4各自独立地表示氢原子,低级烷基等; Q表示碳原子,氮原子或硫原子(硫原子可以被氧代基单取代或二取代)。 R 5和R 6各自表示氢原子,低级烷基等; X 1,X 2,X 3和X 4各自独立地表示碳原子或氮原子; Z表示氧原子,硫原子或氮原子; Ar表示任选被选自取代基组β的基团单取代至三取代的芳基或杂芳基; 环A表示5-或6-元含氮杂芳基; m表示1〜6的整数, n表示0〜3的整数, p表示0〜2的整数(条件是X 1〜X 4中的至少2个为碳原子); q表示0或1]或其药学上可接受的盐,其具有葡糖激酶活化的作用,并且可用作糖尿病的治疗。