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:
Disclosed are compounds of the formula ##STR1## wherein R.sub.1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R.sub.3 and R.sub.4 are organic or inorganic substituents which may together form ring structures; m is zero, one or two; and R.sub.5 and R.sub.6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要:
Disclosed are compounds of the formula: ##STR1## wherein R.sub.1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y optionally substituted nitrogen or carbon atoms; R.sub.3 and R.sub.4 are organic or inorganic substitutents which may together form ring structures; m is zero, one or two; and R.sub.5 and R.sub.6 are are organic or inorganic substituents;and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要:
A tethered surveillance balloon having a relatively low lift-to-weight ratio (e.g., 1.1) and an aerodynamic device to help maintain the surveillance balloon elevation when subject to high velocity wind conditions at an altitude which is a high percentage of the altitude the surveillance balloon would assume if there was zero wind velocity and all other conditions were the same (e.g. temperature, air density). The surveillance balloon also includes a sensing device such as a TV detector for detecting objects and relaying information to a ground station and with possibly a target designation device, if so desired. The balloon is formed of a material which is virtually, if not entirely, radar and visibly transparent.
摘要:
This invention relates to compositions, methods of production and uses of non-combustible nuclear radiation shields, with particular emphasis on those containing a high concentration of hydrogen atoms, especially effective for moderating neutron energy by elastic scatter, dispersed as a discontinuous phase in a continuous phase of a fire resistant matrix.
摘要:
The present invention is directed to a method and a system for fault detection analysis in a power device which is operatively associated with a differential protection unit. The power device has one input side and one output side through which an input current and an output current flows into and out from it, respectively. Signals representative of the input and output currents are processed in order to verify if an occurring fault is external to the power device. Under a condition of an external fault, the differential protection unit is disabled for a determined interval of time.
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 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.