摘要:
A method and a device for providing automatic load alleviation to a high lift surface system, in particular to a landing flap system, of an aircraft when a blockage occurs, wherein in response to a control signal emitted by a control device at least one high lift surface, which is actuated by means of a local mechanical final control element, is brought to a predetermined position by a central drive unit that is connected by way of a rotary shaft arrangement to the local final control element by generating a torque transmitted by the central drive unit to the rotary shaft arrangement. If a signal is registered that indicates that there is a blockage within the high lift surface system, the torque transmitted by the central drive unit to the rotary shaft arrangement is automatically reduced to a predetermined low torque value, and the position of the high lift surface system is fixed.
摘要:
Novel phenyl-substituted 1,4-dihydropyridines, prepared by reacting halogenophenyl-aldehydes with &bgr;-ketoesters, if appropriate with isolation of the ylidene compounds and enamines. The substances can be employed as active compounds in medicaments, in particular in cerebrally active compositions.
摘要:
A process for the preparation of a 4-[3-carboxy-3-diazo-2-oxopropyl]azetidin-2-one of the formula ##STR1## comprising reacting a 4-acetoxy-2-azetininone of the formula ##STR2## with a compound of the formula ##STR3## in an inert solvent, in the presence of a base and of a silylating agent, in a one-pot process.Many of the products are new. The products are useful in the synthesis of carbapenem antibiotics.
摘要:
A new synthetic route to clausenamide having the formula ##STR1## has been found. It has been found that a compound of the formula ##STR2## can be oxidized to provide the stereochemically correctly configured product, clasuenamide. A number of new compounds useful in the total synthesis of clausenamide have also been found. These compounds have the general formula ##STR3## wherein R is ##STR4## and CH.sub.2 OH.
摘要:
A process for the preparation of a 7-acylamino-3-hydroxy-2-cephem-4-carboxylic acid, 7-acylamino-3-hydroxy-1-dethia-1-oxa-3-cephem-4-carboxylic acid or derivative thereof of the general formula ##STR1## in which R.sup.1 is hydrogen or optionally substituted alkyl, alkenyl, alkinyl, aralkyl, aryl, heteroaryl, heteroaralkyl, aryloxyalkyl, heteroaryloxyalkyl, alkoxyalkyl, arylthioalkyl, heteroarylthioalkyl, alkylthioalkyl, alkoxy, aryloxy, alkylthio or arylthio,R.sup.2 is hydrogen, a carboxy-protective group or a pharmaceutically useful ester radical, andX is sulphur or oxygen,which comprises:(a) reacting a compound of the formula ##STR2## with (i) a compound of the formula ##STR3## in which R.sup.2 and X have the abovementioned meaning and Y represents diazo (N.sub.2) or hydrogen (H.sub.2) in an inert solvent in the presence of a Lewis acid or proton acid catalyst, or(ii) a compound of the formulaHX--CH.sub.2 --C.tbd.C--COOR.sup.2 to form an intemediate compound having a triple bond, and hydrating the triple bond, the compounds thus obtained, for Y being hydrogen (H.sub.2)--(in case of Y=diazo (N.sub.2) directly the compounds of general formula (2) are obtained) thereby to produce a compound of the formula ##STR4## (b) reacting such compound with an azide in a solvent in the presence of a base to give a compound of the formula ##STR5## (c) converting said compound to the desired product by (i) irradiation in an inert solvent, or(ii) warming in the presence of a catalyst.The end products are, or can be converted to, known .beta.-lactam antibiotics.
摘要翻译:制备7-酰基氨基-3-羟基-2-头孢烯-4-羧酸,7-酰基氨基-3-羟基-1-脱硫-1-氧杂-3-头孢烯-4-羧酸或其衍生物的方法 烯基,炔基,芳烷基,芳基,杂芳基,杂芳烷基,芳氧基烷基,杂芳基氧基烷基,烷氧基烷基,芳硫基烷基,杂芳硫基烷基,烷硫基烷基,烷氧基,芳氧基,烷硫基或芳硫基,其中R 1为氢或任选取代的烷基, R2是氢,羧基保护基或药学上有用的酯基,X是硫或氧,其包括:(a)使式(IMAGE)的化合物与(i)下式化合物 其中R2和X具有上述含义,Y代表重氮(N 2)或氢(H 2)在惰性溶剂中,在路易斯酸或质子酸催化剂存在下,或(ii)式HX-CH2- C 3 C COR CO 2,以形成具有三键的中间体化合物,并且使三键水合,该共聚物 (H)在(Y =重氮(N 2)的情况下直接得到通式(2)的化合物),得到下式的化合物:(b)使此 在碱的存在下在溶剂中与叠氮化合物反应,得到下式的化合物:(c)通过(i)在惰性溶剂中照射将所述化合物转化为所需产物,或(ii)在 存在催化剂。 最终产品是或可以转化为已知的β-内酰胺抗生素。
摘要:
The present invention provides peptides and peptidomimetics corresponding to part or to the entirety of the region encompassed by residues 360-386 of human p53, said peptides and peptidomimetics characterized by the ability to activate DNA binding of wild-type p53 and of select tumor-derived p53 mutants. Pharmaceutical compositions of the compounds of the invention and methods of using these compositions therapeutically are also provided.
摘要:
The present invention provides peptides and peptidomimetics corresponding to part or to the entirety of the region encompassed by residues 360-386 of human p53, said peptides and peptidomimetics characterized by the ability to activate DNA binding of wild-type p53 and to select tumor-derived p53 mutants. Pharmaceutical compositions of the compounds of the invention and methods of using these compositions therapeutically are also provided.
摘要:
The invention relates to a packing system for unit loads which can be stacked in a plurality of adjacent piles or piles stacked on top of each other to form a substantially stable pile consisting of at least two stacked layers of unit loads. The invention is characterized in that spacers are provided between at least two successive stacked layers so that both stacked layers are vertically interspaced; at least one device is provided on top of and below the stack to protect at least partially the external contour of the unit loads located in the top and lower stack position; at least one fixing device encompassing the other periphery of the stack is included so that it encompasses the stack in such a way that the unit loads in a stack position are pressed against the unit loads in a directly and vertically adjacent stack position; and the fixing device extends over the protection device.
摘要:
4-Heterocyclyl-substituted dihydropyridines are prepared by reacting appropriate aldehydes with .beta.-keto esters and aminocrotonic acid esters, or by esterifying 4-hetero-cyclyl-substituted dihydropyridinecarboxylic acids. The 4-heterocyclyl-substituted dihydropyridines can be employed in medicaments, in particular for the treatment of disorders of the central nervous system.
摘要:
The invention provides pure enatiomers of 4,5-disubstituted .gamma.-butyrolactams of the general formula ##STR1## By means of the pure enantiomers of 4,5-disubstituted .gamma.-butyrolactams (I), according to the invention, it is now possible to synthesize (+)-(3R), (4S), (5S), (7R)-3-hydroxy-5-.alpha.-hydroxybenzyl-1-methyl-4-phenyl-pyrrolidin-2-one and derivatives in the form of pure enantiomers.