摘要:
The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.The advantage of the process of the present invention is that it makes the desired compounds of the Formula I available in a simple manner, with high yields and in a short reaction time.
摘要:
The invention relates to new oxidiazole-alkyl-purine-derivatives of the Formula I ##STR1## and pharmaceutically acceptable salts thereof wherein A stands for C.sub.1-4 alkylene andR.sup.1 represents C.sub.1-6 alkyl, hydroxyalkyl, halogenoalkyl, carboxyalkyl, C.sub.5-6 cycloalkyl or aminoalkyl of the Formula --(CH.sub.2).sub.n --NR.sup.2 R.sup.3 in which group n is an integer 1-3; R.sup.2 and R.sup.3 each stand for hydrogen or C.sub.1-4 alkyl or together with the adjacent nitrogen atom they are attached to form a 5- or 6-membered nitrogen containing heterocyclic ring which may optionally comprise a further nitrogen atom or an oxygen atom as heteroatom; orR.sup.1 stands for phenyl, hydroxyphenyl, carboxyphenyl, benzyl or dimethoxybenzylThe compounds of the Formula I can be prepared by methods known per se and can be used in therapy as antitussive agents.
摘要翻译:本发明涉及式I的新型氧化噻唑烷基嘌呤衍生物及其药学上可接受的盐,其中A代表C1-4亚烷基,R1代表C1-6烷基,羟基烷基,卤代烷基,羧基烷基,C5-6环烷基 或其中基团n为整数1-3的式 - (CH 2)n -NR 2 R 3的氨基烷基; R 2和R 3各自代表氢或C 1-4烷基或与它们相连的相邻氮原子一起形成5-或6-元含氮杂环,其可以任选地包含另外的氮原子或氧原子作为杂原子; 或R 1代表苯基,羟基苯基,羧基苯基,苄基或二甲氧基苄基。式I化合物可以通过本身已知的方法制备,并且可用于作为止咳剂的治疗。
摘要:
Compounds of the formula ##STR1## are disclosed wherein R.sup.1 stands for hydrogen, C.sub.1-4 straight or branched alkyl or pharmacologically acceptable cation,R.sup.2 stands for hydrogen, C.sub.1-4 alkanoyl, benzoyl, or benzoyl substituted by C.sub.1-4 alkyl or halogen, and R.sup.2 can further represent tetrahydropyranyl, trialkylsilyl or alkoxyalkyl,A stands for ethylene, cis or trans-vinylene or --C.dbd.C--,n may represent 2, 3 or 4. The compounds are highly effective in the inhibition of thrombocyte aggregation while at the same time exert only a very small hypotensive effect.
摘要:
A voltage transformer for a fully insulated high-voltage installation containing several conductors includes a plurality of electrodes corresponding to respective ones of the conductors. The electrodes are disposed outside of the arrangement of the conductors in such a manner that each one of the electrodes is disposed directly adjacent a corresponding one of the conductors. Each of the electrodes and the conductor directly adjacent thereto conjointly define a high-voltage capacitor. A plurality of low-voltage capacitors are disposed outside of the region occupied by the electrodes and are connected to corresponding ones of the high-voltage capacitors so as to conjointly define therewith respective capacitive voltage dividers.
摘要:
A measuring transformer arrangement with a capacitor bushing and devices for measuring voltage and current associated with the capacitor bushing is suitable for use in a high-voltage installation with metal encapsulation carrying several high-voltage conductors. The capacitor bushing provided for each high-voltage conductor is arranged in a bulkhead partition of the metal encapsulation and carries a current measuring device which includes at the periphery of the bushing at least one current transformer core with a secondary winding system mounted thereon.
摘要:
A spliced fiber tow (40) having a uniform density along its entire length is provided. The spliced fiber tow is manufactured by rarefying the ends (22, 32) of the two fiber tow segments to be joined, aligning the rarefied regions (26, 36) and then applying pressurized gas to entangle the filaments in the rarefied regions. An apparatus (50) for forming the spliced fiber tow includes a pair of rarefying blades (86, 92) and an entanglement element (58).
摘要:
A linear guide with a guide carriage longitudinally movably arranged on a guide rail, which is preferably U-shaped and a braking device effectively arranged between the guide rail and the guide carriage. An actuator for actuating the braking device is provided and the actuator has an electro-active polymer effectively arranged in the longitudinal axis of the linear guide which engages around the guide rail for actuating the braking device.
摘要:
A lighter-than-air aircraft is propelled via a bending-rotating tail whip. Two actuating areas located on opposite sides in a rear area of a lifting gas body are shortened by activated actuators. A vertical plane of symmetry of the lifting gas body and thus, the lifting gas body itself, are pivoted in an area of bending zones about angles a and β. An activated state exists when the actuator performs work for propelling the aircraft. Propulsion can be provided by deformation of the lifting gas body. Changes in direction can also be effected by asymmetrical sequences of movements.
摘要:
The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen: or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.
摘要:
A method of using a compound of the Formula (V) ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, wherein R.sup.1 and R.sup.2 are each C.sub.1 to C.sub.6 aliphatic acyloxy, unsubstituted or substituted by halogen, or are each C.sub.7 to C.sub.11 aromatic acyloxy,for preventing amination of the 6-position when a compound of the Formula (I) ##STR2## or a pharmaceutically acceptable salt thereof is to be formed, which comprises the steps of:(a) aminating the compound of the Formula (V) or a pharmaceutically acceptable salt thereof with piperazine in an inert organic solvent to yield a compound of the Formula (VII) ##STR3## or a pharmaceutically acceptable salt thereof, and (b) hydrolyzing the compound of the Formula (VII) or a pharmaceutically acceptable salt thereof, after or without isolation, to obtain the compound of the Formula (I), and if desired, converting the compound of the Formula (I) into a pharmaceutically acceptable salt thereof, or setting free the compound of the Formula (I) from its pharmaceutically acceptable salt.