摘要:
The invention relates to 4-substituted quinoline compounds of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 and X5 is C—R′1, to C—R′5 respectively, or alternatively at most one represents N, Y represents CHR, CO, CROH, CRNH2, CRF or CF2, R being a hydrogen or alkyl, m is 1, 2 or 3 and n is 0, 1 or 2, Z is CH2 or Z is O, S, SO, SO2 and, in this case, n is equal to 2, R2 is —CO2R, —CH2CO2R, —CH2—CH2CO2R, —CH2OH or —CH2—CH2OH, wherein R is as defined above, R3 represents phenyl, heteroaryl or alk-Ro3, where alk is alkyl and Ro3 represents various groups, where appropriate containing oxygen, sulfur or amine, in their enantiomeric or diastereoisomeric forms or their mixtures, and/or where appropriate in the syn or anti form or their mixtures, and their salts.
摘要翻译:本发明涉及以下通式的4-取代喹啉化合物:其作为抗微生物剂是有活性的,其中:X 1,X 2,X 3, >,X 4和X 5分别为C-R'1,C-R'5, 或者至多一个表示N,Y表示CHR,CO,CROH,CRNH 2,CRF或CF 2,R为氢或烷基,m为1,2 或3,n为0,1或2,Z为CH 2或Z为O,S,SO,SO 2,在这种情况下,n等于 2,R 2是-CO 2 R,-CH 2 CO 2 R,-CH 2, 2个-CH 2 CO 2 R 2,-CH 2 OH或-CH 2 -CH(CH 2) R 2 OH,其中R如上所定义,R 3表示苯基,杂芳基或烷基-SO 3 - , - 其中烷基是烷基,R 3 O 3表示各种基团,其中适当地含有它们的对映体或非对映异构形式或其混合物中的氧,硫或胺, d /或适当时以合成或反式形式或其混合物及其盐。
摘要:
Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. ##STR1## In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula --(CH.sub.2).sub.m --X.sub.1 --(CH.sub.2).sub.n --Z in which X.sub.1 =single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH.sub.2 radicals to be substituted; Z represents carboxyl, COOR.sub.6 (R.sub.6 =alkyl), CON(R.sub.7)(R.sub.8) (R.sub.7 =hydrogen or alkyl and R.sub.8 =hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR.sub.9).sub.2 (R.sub.9 =hydrogen or alkyl), an --NH--CO--T (T=hydrogen or optionally substituted alkyl) radical, or else--a ##STR2## radical, R.sub.1 and R.sub.2 =hydrogen or halogen or alkyl, alkyloxy, which is optionally substituted, alkylthio, alkyloxycarbonyl or else R.sub.1 and R.sub.2, at the ortho position with respect to one another, form an optionally substituted heterocycle containing 1 or 2 heteroatoms, R.sub.3 and R.sub.4 =hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio. carboxyl or alkyloxycarbonyl, R.sub.5 =hydrogen, alkyl, alkylthio, X=O or S or --NH--, --CO--, methylene, vinyldiyl, alkene-1,1-diyl or cycloalkane-1,1-diyl, and Y=O or S, in the racemic form, as well as the optical isomers (diastereomers and enantiomers) and the salts of the product of formula (I). The compounds of formula (I) are farnesyl transferase inhibitors which exhibit notable antitumor and antileukemic properties.
摘要翻译:式(I)的新产品,其制备方法,含有它们的药物组合物及其在制备药物中的用途。 在式(I)中,以下取代基是优选的:Ar表示取代或稠合的苯基或多环或杂环芳族基,R表示通式 - (CH 2)m -X1(CH 2)n Z 其中X1 =单键,O,S; m = 0,1, n = 0,1,2; CH2基可以被取代; Z代表羧基,COOR6(R6 =烷基),CON(R7)(R8)(R7 =氢或烷基,R8 =氢,羟基,芳基磺酰基,杂环基,任选取代的氨基,任选取代的烷氧基或任选取代的烷基),PO OR 9)2(R 9 =氢或烷基),-NH-CO-T(T =氢或任选取代的烷基)基团,或者 - 基团,R 1和R 2 =氢或卤素或烷基,烷氧基, 取代的烷硫基,烷氧基羰基,或者R1和R2相对于彼此的邻位,形成含有1或2个杂原子的任选取代的杂环,R 3和R 4 =氢或卤素或烷基,烯基,烷氧基,烷硫基。 羧基或烷氧基羰基,R5 =氢,烷基,烷硫基,X = O或S或-NH-,-CO-,亚甲基,乙烯基二烯基,烯-1,1-二基或环烷烃-1,1-二基,Y = O 或S,外消旋形式,以及光学异构体(非对映体和对映体)和式(I)的产物的盐。 式(I)化合物是具有显着的抗肿瘤和抗白血病性质的法呢基转移酶抑制剂。
摘要:
Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. ##STR1## In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula --(CH.sub.2).sub.m --X.sub.1 --(CH.sub.2).sub.n --Z in which X.sub.1 =single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH.sub.2 radicals to be substituted; Z represents carboxyl, COOR.sub.6 (R.sub.6 =alkyl), CON(R.sub.7)(R.sub.8) (R.sub.7 =hydrogen or alkyl and R.sub.8 =hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR.sub.9).sub.2 (R.sub.9 =hydrogen or alkyl), an --NH--CO--T (T=hydrogen or optionally substituted alkyl) radical, or elsea ##STR2## radical, R.sub.1 and R.sub.2 =hydrogen or halogen or alkyl, alkyloxy which is optionally substituted, alkylthio, alkyloxycarbonyl or else R.sub.1 and R.sub.2, at the ortho position with respect to one another, form an optionally substituted heterocycle containing 1 or 2 heteroatoms, R.sub.3 and R.sub.4 =hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio, carboxyl or alkyloxycarbonyl, R.sub.5 =hydrogen, alkyl, alkylthio, X=O or S or --NH--, --CO--, methylene, vinyldiyl, alkene-1,1-diyl or cycloalkane-1,1-diyl, and Y=O or S, in the racemic form, as well as the optical isomers (diastereomers and enantiomers) and the salts of the product of formula (I). The compounds of formula (I) are farnesyl transferase inhibitors which exhibit notable antitumor and antileukemic properties.
摘要:
Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula —(CH2)m—X1—(CH2)n—Z in which X1=single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH2 radicals to be substituted; Z represents carboxyl, COOR6 (R6=alkyl), CON(R7)(R8) (R7=hydrogen or alkyl and R8=hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR9)2 (R9=hydrogen or alkyl), an —NH—CO—T (T=hydrogen or optionally substituted alkyl) radical, or else—a radical, R1 and R2=hydrogen or halogen or alkyl, alkyloxy, which is optionally substituted, alkylthio, alkyloxycarbonyl or else R1 and R2, at the ortho position with respect to one another, form an optionally substituted heterocycle containing 1 or 2 heteroatoms, R3 and R4=hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio, carboxyl or alkyloxycarbonyl, R5=hydrogen, alkyl, alkylthio, X=O or S or —NH—, —CO—, methylene, vinyldiyl, alkene-1,1-diyl or cycloalkane-1,1-diyl, and Y=O or S, in the racemic form, as well as the optical isomers (diastereomers and enantiomers) and the salts of the product of formula (I). The compounds of formula (I) are farnesyl transferase inhibitors which exhibit notable antitumor and antileukemic properties.
摘要:
The present invention discloses and claims compounds of formula I and their pharmaceutically acceptable salts, and methods of using said compounds of formula I, either alone or in combination with other medicaments, as antiarrhythmic medicaments with a cardioprotective component for prophylaxis or treatment of infarction, for the treatment of angina pectoris, and as inhibitors of pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure. Pharmaceutical compositions comprising compounds of formula I or compounds of formula I in combination with one or more other medicaments and processes for the preparation of compounds of formula I are also disclosed and claimed.
摘要:
The present invention discloses and claims compounds of formula I and their pharmaceutically acceptable salts, and methods of using said compounds of formula I, either alone or in combination with other medicaments, as antiarrhythmic medicaments with a cardioprotective component for prophylaxis or treatment of infarction, for the treatment of angina pectoris, and as inhibitors of pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure. Pharmaceutical compositions comprising compounds of formula I or compounds of formula I in combination with one or more other medicaments and processes for the preparation of compounds of formula I are also disclosed and claimed.
摘要:
Image surveillance and reporting technology, in which an event that is indicative of potential physical activity within an area corresponding to a location of a camera unit is detected. In response to detection of the event, the camera unit is controlled to capture one or more images of the area corresponding to the location of the camera unit. The one or more images captured by the camera unit are analyzed to determine whether the one or more images include image data that is indicative of relevant physical activity within the area corresponding to the location of the camera unit. The one or more images are handled based on the determination of whether the one or more images include image data that is indicative of relevant physical activity within the area corresponding to the location of the camera unit.
摘要:
Techniques are described for moving asset location tracking and monitoring system technology. A system monitors for events related to a monitoring system that monitors a fixed property and the system detects an event related to the monitoring system based on the monitoring. The system performs an operation that leverages geographic location tracking of at least one mobile asset associated with the fixed property based on the detected event.
摘要:
Techniques are described for handling an event where a control panel or an alarm signaling device is tampered with or destroyed by a disablement tactic, e.g., a “crash and smash intrusion.”
摘要:
Techniques are described for establishing a two-way voice communication session with an alarm system. The alarm system may establish a two-way voice communication session with an operator associated with a monitoring service that provides monitoring services for alarm events detected by the alarm system. The alarm system also may establish a two-way voice communication session with a notification recipient that is interested in receiving notifications associated with events detected by the alarm system.