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标题翻译：有机化合物的组合

公开(公告)号：WO2006029349A1

公开(公告)日：2006-03-16

申请号：PCT/US2005/032224

申请日：2005-09-08

申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , MAHER, William , MERCURI, Michele , NEVATIA, Meenakshi , CHEN, Hong , WANG, Pei-Ran

发明人： MAHER, William , MERCURI, Michele , NEVATIA, Meenakshi , CHEN, Hong , WANG, Pei-Ran

IPC分类号： A61P25/30 , A61P9/00 , A61P3/06 , A61P3/10 , A61K31/00 , A61K31/522 , A61K31/422 , A61P3/04

CPC分类号： A61K31/00 , A61K31/422 , A61K31/522 , A61K2300/00

摘要： The present invention relates to a pharmaceutical composition, comprising a PPAR agonist, or pharmaceutically acceptable salts thereof, alone or in combination with at least one active ingredient selected from the group consisting of (i) HDL increasing compounds; (ii) anti-diabetics; (iii) an anti-hypertensive agent; (iv) cholesterol absorption modulator; (v) apo-A1 analogs and mimetics; (vi) renin inhibitors; (vii) thrombin inhibitors; (viii) aldosterone inhibitors; (ix) GLP-1 agonists; (x) glucagon receptor antagonists; (xi) cannabinoid receptor 1 antagonists; (xii) anti-obesity agents; and (xiii) inhibitors of platelet aggregation or, in each case, a pharmaceutically acceptable salt thereof; and optionally a pharmaceutically acceptable carrier. The pharmaceutical composition may be employed for the treatment of addictions (for example, nicotine and cocaine), dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, stroke, intermittent claudication, restenosis after PCTA, hypertension, obesity including reduction in CV risk in obese patients, inflammation, arthritis, cancer including breast, colon and prostate cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, IBDs (irritable bowel disease), Crohn's disease, hypofibrinolysis, hypercoaguable state, metabolic/cardiometabolic syndrome, elevated CRP, appearance of microalbuminuria, reduction of proteinuria, renal failure (DM, non-DM), NASH (non alcoholic steato hepatitis) non-alcoholic fatty liver, CV events in patients with high CRP, vascular dementia, psoriasis, ischaemia reperfusion injury, asthma, COPD, eosinophilia, RA, airway hyperresponsiveness (AHR), inflammatory digestive diseases (e.g. ulcerative colitis) diseases of anitgen-induced inflammatory responses. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions such as impaired glucose tolerance, hyperglycemia, insulin resistance, type-1 and type-2 diabetes and Syndrome X. Also contemplated is the administration of the combinations of the present invention for the improvement of cardiac metabolism and cardioprotection in heart transplant patients, to facilitate smoking cessation or reduction and to prevent or treat conditions associated with smoking.

摘要翻译：本发明涉及一种药物组合物，其包含PPAR激动剂或其药学上可接受的盐，其单独或与至少一种选自（i）HDL增加的化合物的活性成分组合; （ii）抗糖尿病患者; （iii）抗高血压药; （iv）胆固醇吸收调节剂; （v）apo-A1类似物和模拟物; （vi）肾素抑制剂; （vii）凝血酶抑制剂; （viii）醛固酮抑制剂; （ix）GLP-1激动剂; （x）胰高血糖素受体拮抗剂; （xi）大麻素受体1拮抗剂; （十二）抗肥胖剂; 和（xiii）血小板聚集抑制剂，或在每种情况下为其药学上可接受的盐; 和任选的药学上可接受的载体。药物组合物可用于治疗成瘾（例如尼古丁和可卡因），血脂异常，高脂血症，高胆固醇血症，动脉粥样硬化，高甘油三酯血症，心力衰竭，心肌梗塞，血管疾病，心血管疾病，中风，间歇性跛行，PCTA后再狭窄高血压，肥胖，包括肥胖患者的CV风险降低，炎症，关节炎，包括乳腺，结肠和前列腺癌在内的癌症，阿尔茨海默病，皮肤病，呼吸系统疾病，眼科疾病，IBDs（肠易激惹），克罗恩病，低纤维蛋白溶解，高可溶性状态，代谢/心脏代谢综合征，CRP升高，微量白蛋白尿出现，蛋白尿减少，肾功能衰竭（DM，非DM），NASH（非酒精性脂肪性肝炎）非酒精性脂肪肝，高CRP患者的CV事件，血管性痴呆，牛皮癣，局部缺血再灌注损伤，哮喘，COPD，嗜酸性粒细胞增多，RA，气道高反应性（AHR），炎性消化疾病（例如，溃疡性结肠炎）anitgen诱导的炎症反应的疾病。本发明的化合物特别可用于哺乳动物，作为用于治疗和预防葡萄糖耐量降低，高血糖症，胰岛素抵抗，1型和2型糖尿病和X综合征等症状的降血糖药。用于改善心脏移植患者心脏代谢和心脏保护的本发明的组合，以促进戒烟或减少并预防或治疗与吸烟有关的病症。

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