摘要:
Disclosed are 2-substituted adenosine derivatives of the formula ##STR1## in which R represents a substituted amino grouping of the formula ##STR2## as defined herein; pharmaceutically acceptable ester derivatives thereof in which free hydroxy groups are esterified in the form of a pharmaceutically acceptable prodrug ester; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for their preparation; and their use in mammals as therapeutically effective adenosine-2 (A-2) agonists.
摘要:
Disclosed are the compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl or aryl-lower alkyl; R.sub.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -alkenyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, or optionally lower alkyl substituted (C.sub.3 -C.sub.7 -cycloalkyl, bicycloheptyl, bicycloheptenyl, adamantyl, tetrahydropyranyl or tetrahydrothiopyranyl)-lower alkyl, or diaryl-lower alkyl; R.sub.2 represents hydrogen or lower alkyl; R.sub.3 represents hydroxymethyl or --CONHR.sub.4 in which R.sub.4 represents hydrogen, lower alkyl, aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or hydroxy-lower alkyl; pharmaceutically acceptable ester derivatives thereof in which one or more of the hydroxy groups are esterified in form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; methods of preparation; pharmaceutical compositions; and their use as adenosine-2 agonists in mammals.
摘要:
Compounds of the formula ##STR1## wherein each R is hydrogen or one R is hydrogen and the other is lower alkyl, R.sub.1 is hydrogen, lower alkyl, aryl, aralkyl or lower carboalkoxy, R.sub.2 is hydrogen or lower alkyl, and the ring A is unsubstituted or substituted by lower alkyl, lower alkoxy, halo or trifluoromethyl, and pharmaceutically acceptable salts thereof, their preparation, pharmaceutical compositions and the uses thereof, such as .alpha..sub.2 -adrenergic blocking agents, e.g. antidepressants, cognition enhancers and appetite suppressants, and as intraocular pressure reducing agents are disclosed.
摘要:
[1,2,4]triazolo[1,5-c]quinazoline compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted phenyl, pyridyl, furyl thienyl, dihydro or tetrahydro furanyl or thienyl, pyranyl, or 0-ribofuranosyl; R.sub.2 is hydrogen or lower alkyl; X is oxygen or NR.sub.3, R.sub.3 is as defined in the claims, and ring A is unsubstituted or substituted as set forth in the claims. The compounds wherein X is N--R.sub.3 are especially useful as adenosine antagonists and for the treatment of asthma. The compounds wherein X is oxygen are useful as benzodiazepine antagonists and as intermediates in the synthesis of the compounds wherein X is N--R.sub.3.
摘要:
Automatic and simultaneous retraction of a pair of stabilizer legs for a backhoe loader machine 10 is beneficial for the operator when operation of the backhoe loader is complete. Instead of retracting the stabilizer legs by manually holding a pair of control switches continuously in a control position, the operator may simply push an auto-up switch with a single, “one-touch” contact. Once the auto-up switch has been activated by the “one-touch” contact, a timer relay is enabled. The timer relay acts independently of the auto-up switch to control the simultaneously retraction of the stabilizer legs without any further contact to the auto-up switch. When the timer relay is enabled, it sends a signal to activate the control switches for a preselected time. The activation of the control switches actuates a pair of solenoid valves which control the movement of the stabilizer legs from any one of a plurality of extended positions to a fully retracted position within the preselected time.
摘要:
A re-enterable seal (25) for sealing an elongate object (16) passing through a barrier (24) between two environments (53, 54) includes an invertible enclosing member (30) containing a sealant (40). The sealant (40) is adhered to the inside surface (31) of the enclosing member (30). During insertion of the elongate member (16), the enclosing member (30) is inverted inside-out, with the sealant remaining on the inside surface (31) (now positioned outside the enclosing member). The elongate member (16) is then pulled back, causing the enclosing member (30) to re-invert, and bringing the sealant (40) into sealing compression against the elongate member (16).
摘要:
New 1-(azacyclic aralkoxyphenyl)-2- or 3-(diphenylalkylamino)-alkanes, e.g those of the formula: ##STR1## R = 5- or 6-membered, mono- or bicyclic, nitrogen-containing aromatic radicalM,n,p= 1-4; r = 1 or 2;R.sub.1 = h or OHor therapeutically acceptable salts thereof are hypotensive and cardioactive agents.
摘要:
A method and apparatus for minimizing the loader frame stress induced by the twisting action which results from unequal travel in the actuators. The method includes the use of electro-hydraulics in conjunction with feedback from actuators displacement sensors. Each actuator is controlled by an individual control valve. The amount of extension of each actuator's piston is monitored. Control signals are sent to the control valves which control fluid flow to each actuator to maintain the actuators' piston extensions at the same amount.
摘要:
Modules integral with the body of the assembly include one for drop wire connections, one for subscriber wire connections, one for an electronics interface, and one for a network interface device. Protective sealant material within the assembly protects contacts from corrosion and other deterioration, and from shorting. Sealant plungers and a chamber containing a compressed gas impose compressive forces upon the sealant material. Shunt plugs associated with two of the modules permit signal transmission across the modules at desired times, and when removed eliminate the possibility of a subscriber being shocked or transmitting a spark when accessing subscriber components of the assembly. The main body and the modules of the assembly preferably are integrally connected and form a unitary sealed assembly.