摘要:
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein A, B, C, D, Y, R1, R3, R4, R5, and R6 are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.
摘要:
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: A, B, C and D are N or CH; X is a bond or (un)substituted CH2; R1 is lower alkenyl or (un)substituted lower alkyl; R3 is lower alkyl; and R2, R4, R5, and R6 are variables defined herein; which compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatroy disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility or glaucoma, or for the increase of permeability of blood-brain barrier, pain, asthma, and rhinitis.
摘要翻译:公开了下式的化合物或其药学上可接受的无毒盐,其中:A,B,C和D是N或CH; X是一个或(un)取代的CH 2; R 1是低级烯基或(取代) 低级烷基; R3是低级烷基; 和R2,R4,R5和R6是本文定义的变量;这些化合物可用于诊断和治疗肾脏疾病,心力衰竭,高血压,梅尼埃病,阴道炎症和疼痛,外周循环障碍,更年期障碍,视网膜循环障碍, 心肌缺血,心肌梗死,心肌梗死后综合征,心绞痛,经皮腔内冠状动脉成形术后再狭窄,肝炎,肝硬化,胰腺炎,肠梗阻,糖尿病,糖尿病并发症,男性不育症或青光眼,或增加血脑屏障通透性 ,疼痛,哮喘和鼻炎。
摘要:
This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed.This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
摘要翻译:本发明涉及苯并咪唑,吡啶基咪唑和相关双环杂芳基化合物,所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A的苯并二氮杂部位的化合物, / SUB>受体。 本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗某些中枢神经系统(CNS)疾病中的用途。 公开了制备式I化合物的新方法。 本发明还涉及式I的苯并咪唑,吡啶基咪唑和相关的双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。 此外,本发明涉及使用这些化合物作为组织切片中GABA A A受体定位的探针。
摘要:
This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein X.sub.1, X.sub.2, X.sub.3 represent organic or inorganic substituents, n is 1, 2, or 3, R.sub.1 -R.sub.4 are hydrogen or organic substituents, and B is nitrogen, carbon, sulfur or oxygen, useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to human Neuropeptide Y1 receptors.
摘要:
Melanin concentrating hormone receptor ligands (especially substituted 2-(4-benzyl-piperazin-1-ylmethyl)-1H-benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
摘要:
Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
摘要:
This invention encompasses compounds of the formula where X1, X2, and X3, independently represent substituents of formula and the pharmaceutically acceptable salts thereof wherein the remaining variables are as defined herein and wherein said compounds are useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to human Neuropeptide Y1 receptors.
摘要:
This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein X.sub.1, X.sub.2, X.sub.3 represent organic or inorganic substituents, n is 1, 2, or 3, m is 2, 3, or 4, R.sub.1 -R.sub.4 are hydrogen or organic substituents, and B is nitrogen, carbon, sulfur or oxygen, useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to mammalian Neuropeptide Y1 receptors.
摘要:
Amido, amino and sulfonamide substituted benzylamine derivatives useful in treating eating disorders have the formula ##STR1## where X.sub.1, X.sub.2, and X.sub.3, independently represent substituents of formula ##STR2## D=H, lower straight or branched chain alkyl having 1-6 carbon atoms, a methylene unit incorporated into a ring connected with G as in the cases of pyrrolidine, pyrrolidone, piperidine, and piperidone;E=O or H.sub.2 ;O=0 or 1;G=straight or branched chain lower alkyl having 1-6 carbon atoms, aryl, aryl substituted with halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, heteroaryl--selected from the group consisting of 2-, 3-, or 4-pyridyl, 2-pyrazyl, 2-, or 3-thienyl, 2-pyrazinyl, 2-, 3-, or 4-quinolyl, 1-, 3-, or 4-isoquinolyl, 2-quinoxalyl, 3-, or 4-cinnolyl, said heteroaryl substituted with halogen, hydroxy, straight or branched chain lower alkyl having 1-6 carbon atoms, straight or branched chain lower alkoxy having 1-6 carbon atoms;and A, T and R.sub.1 -R.sub.4 are hydrogen or organic substituents.
摘要翻译:可用于治疗进食障碍的酰氨基,氨基和磺酰胺取代的苄基胺衍生物具有下式,其中X1,X2和X3独立地表示式D = H的取代基,具有1-6个碳原子的低级直链或支链烷基, 如吡咯烷,吡咯烷酮,哌啶和哌啶酮的情况下与G连接的环; E = O或H2; O = 0或1; G =具有1-6个碳原子的直链或支链低级烷基,芳基,被卤素取代的芳基,具有1-6个碳原子的直链或支链低级烷基,杂芳基 - 选自2-,3-或 4-吡啶基,2-吡嗪基,2-或3-噻吩基,2-吡嗪基,2-,3-或4-喹啉基,1-,3-或4-异喹啉基,2-喹喔啉基,3-或 所述杂芳基被卤素取代,羟基,具有1-6个碳原子的直链或支链低级烷基,具有1-6个碳原子的直链或支链低级烷氧基; 并且A,T和R 1 -R 4是氢或有机取代基。
摘要:
A digital signal processor implementation of three algorithms used to detect high impedance faults. The algorithms can be wavelet based, higher order statistics based and neural network based. The algorithms are modified to process one second of data instead of ten seconds of data and a double buffered acquisition is connected to the output of the algorithms.