摘要:
Novel basic ether of general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen or C.sub.1-4 alkoxy, or together they represent a 3,4-methylenedioxy group,R stands for C.sub.1-8 alkyl,R.sup.3 represents hydrogen, C.sub.1-4 alkyl or hydroxy,A is a valency bond or methylene group,R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-12 alkyl or C.sub.1-12 alkenyl, orR.sup.4 and R.sup.5 form together with the adjacent nitrogen atom 1-pyrrolidinyl, 1-piperidinyl, morpholino or 1-piperazinyl groups, stereo and optically active isomers and their possible mixtures, acid-addition salts and quaternary ammonium derivatives thereof. The basic ethers have antiulceric and anxiolytic activities.
摘要:
The invention relates to novel, pharmaceutically active trisubstituted cycloalkane derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same. The invention also encompasses the use of the said cycloalkane derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The compounds according to the invention are characterized by the general formula (I), ##STR1## wherein R represents hydrogen, C.sub.1-4 alkyl or hydroxyl,R.sup.1 stands for C.sub.1-12 alkyl,R.sup.2 and R.sup.3 each represents hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 4- to 7-membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter may carry a phenyl, benzyl or C.sub.1-4 alkyl substituent,R.sup.4 and R.sup.5 each stands for hydrogen, halogen or C.sub.1-4 alkoxy, or together represent a 3,4-methylenedioxy group,n is an integer from 2 to 5,A represents a valency bond or a --CH.sub.2 -- group.The compounds exert a valuable antiulcer effect, so they can be used to advantage in the therapy.
摘要:
The invention relates to novel, pharmaceutically active benz[e]indene derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, further to the use of the said benz[e]indene derivatives in the treatment of certain diseases and in the preparation of pharmaceutical compositions suitable for the treatment of said diseases.The new benz[e]indene derivatives according to the invention correspond to the general formula ##STR1## wherein A represents a group of the formula alk-NR.sup.1 R.sup.2, wherein alk represents a C.sub.2-7 alkylene group optionally carrying a hydroxy substituent,R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, mono(C.sub.1-7)alkylamino(C.sub.1-7)alkyl, di(C.sub.1-7)alkylamino(C.sub.1-7)alkyl or C.sub.3-7 cycloalkyl; orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a 4 to 7 membered ring, optionally comprising an oxygen atom or a further nitrogen atom, which latter may carry a phenyl, benzyl, pyridyl, pyrimidinyl or C.sub.1-3 alkyl substituent which substituents may, in turn, bear a hydroxy or methoxy group or a halogen atom or a halophenyl group; orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a phthalimido group; orA represents pyrimidino, 2,3-epoxypropyl or a group of the formula --C(O)NHR.sup.3, whereinR.sup.3 stands for C.sub.1-7 alkyl, C.sub.2-7 alkenyl or C.sub.3-8 cycloalkyl; andR denotes hydrogen or C.sub.1-7 alkyl,stereoisomers and optically active isomers and the possible mixtures thereof, further acid addition salts and quaternary ammonium derivatives of these compounds.
摘要:
The invention refers to pharmaceutical compositions for the prevention and/or treatment of gastrointestinal diseases connected with infections caused by Helicobacter pylori and a method for the treatment of such diseases.The pharmaceutical composition of the invention comprises as active ingredient a cyclic ketone derivative of the formula I ##STR1## wherein and R.sup.1 mean independently hydrogen or halo;R.sup.0 stands for hydrogen or a C.sub.1-4 alkoxy group;R.sup.2 and R.sup.3 independently represent hydrogen; a straight or branched chain C.sub.1-8 alkyl optionally substituted by a dimethylamino group; a C.sub.2-6 alkenyl or a C.sub.3-7 cycloalkyl group; orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 6-membered heterocyclic group containing an additional nitrogen atom that may bear a phenyl group optionally substituted by a C.sub.1-4 alkoxy group;or its stereoisomer or optical isomer or a possible mixture thereof, or a pharmaceutically acceptable acid addition salt or quaternary ammonium salt thereof in admixture with carrier(s) commonly used in pharmaceutical compositions.
摘要:
This invention relates to new 1-�2-(substituted vinyl)!-5H-2,3-benzodiazepine derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said benzodiazepine derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases. The compounds according to the invention correspond to the general formula (I), ##STR1## wherein the variables are herein below defined, and the compounds possess central nervous activities.
摘要:
Process for the preparation of 8 -[4 -[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8-aza-spiro[4.5]decane-7,9-dione (buspiron) of the Formula I ##STR1## and the hydrochlorides thereof having high purity by continuously adding a solution of 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]-but-2 -inyl]-8-aza-spiro[4.5]decane-7,9-dione of the formula II ##STR2## formed with an inert organic solvent having a concentration of at least 40% by weight to a suspension of a hydrogenation catalyst in an inert organic solvent and optionally converting the 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8-aza-spiro[4.5]decane-7,9-dione thus obtained into the hydrochloride thereof.
摘要:
The invention relates to new 2,3-benzodiazepine derivatives of general Formula (I), (wherein R1 stands for methyl, formyl, carboxy, cyano, —CH═NOH, —CH═NNHCONH2 or —NR5R6, wherein R5 and R6 independently from each other represent hydrogen or lower alkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R2 is nitro or amino; R3 stands for hydrogen, lower alkanoyl or CO—NR7R8, wherein R7 and R8 independently from each other stand for hydrogen, lower alkoxy, lower alkyl or lower cycloalkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R4 is hydrogen or lower alkyl; the dotted lines have the following meaning: if R3 and R4 are not present, the bond between positions C8 and C9 is a single bond and the bond between positions C8 and N7 is a double bond; if R3 and R4 are present, the bonds between positions C8 and C9 and between position C8 and N7 are single bonds; and if R3 is present and R4 is missing, the bond between positions C8 and C9 is a double bond and the bond between positions C8 and N7 is a single bond) and salts thereof. The invention compounds have neuroprotective effect.
摘要:
An interface for a small form factor electronic device by enabling explicit measurement of extension or retraction of a retractable cord by monitoring the amount of string that passes by sensors, as the string exits the enclosure of the device. Input to such small form factor devices may be provided by sensors that measure the length of a string or wire that has been pulled out of an enclosure, in addition to an angle or direction (e.g., in 1-, 2- or 3-dimensions) at which the string was pulled out. Additionally, the rate of acceleration for the pulling and retracting motion may also be used as additional forms of input. In a further embodiment, a string interface is provided for a small form factor device that communicates information in the form of a pixel display provided integral with the string in response to string manipulation.
摘要:
A pyrimidine derivative of the formulae (Ia), (Ib) and (Ic), ##STR1## wherein R stands for an alkyl group group with 1 to 6 carbon atoms or an aryl group optionally substituted by halogen atom; andX stands for chlorine or bromine atom or an arylsulfonyloxy group optionally substituted by 1 to 3 lower alkyl groups.The subject pyrimidine derivatives are intermediates for preparing 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine.
摘要:
An information handling system, comprising an information handling device containing memory for information specific to a particular role or function to be performed by a user of the device, having a display for displaying a portion of the information and functional portions for manipulating the information; and apparatus for coupling to the device, the apparatus being associated with a user of the device and containing information concerning identity and preferences of the user of the device. The apparatus acts a dock for receiving the device. A method comprising loading information from the apparatus to which the device is coupled so as to customize operation of the device. Information can include at least one of preferences, settings, authorization rights, security codes and programs preferred by a user of the apparatus. Role of the device may change in response to communications hardware for receiving signals indicative of location of the device, which changes roles based on the signals.