摘要:
An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.
摘要:
The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine-II3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I), as well as methods or using them to treat obesity and other histamine II3 receptor-related diseases.
摘要:
The invention provides N-cyclic sulfonamido compounds for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula I, wherein R4, R5, R6, R7, and R8, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula I.
摘要:
This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, —(CR32)1-4X(CO)Y; each R3A is independently H or alkyl; X is —O—, —NH, or —N-alkyl; and Y is —NR6R7, or —N(R3)(CH2)2-6NR6R7. Also disclosed is a method of treating Alzheimer's Disease.
摘要翻译:本发明公开了下式的新型γ分泌酶抑制剂:其中:R 1是取代的芳基或取代的杂芳基; R 2是R 1基团,烷基,-X(CO)Y, - (CR 3)2 1-4X(CO)Y; 每个R 3A独立地是H或烷基; X是-O-,-NH或-N-烷基; 并且Y是-NR 6 R 7或-N(R 3)(CH 2)2-6 NR 6 R 7。 还公开了治疗阿尔茨海默病的方法。
摘要:
A compound of the formula: 1 wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) nullSnull, nullSOnull or nullSO2null, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc., (iv) nullCOnullOnull or (v) null(CH2)p-X1-, null(CH2)p-X1-(CH2)q-, null(CH2)r-CO-X1-, nullSO2nullNR8- or null(CH2)r-SO2nullNR8- wherein X1 is O or NR8, R8 is H, a hydrocarbon group which may be substituted or an acyl, p is 0 to 5, q is 1 to 5, pnullq is 1 to 5, and r is 1 to 4; Y is a divalent C1-6 aliphatic hydrocarbon group optionally containing O or S, which may be substituted; R1 and R2 each is H or a lower alkyl which may be substituted, or R1 and R2 form a N-containing heterocyclic ring which may be substituted; Ring A is a benzene ring which may be further substituted; and Ring B is a 4- to 8-membered ring which may be further substituted, or a salt thereof has the effect of inhibiting amyloid-null protein production and/or secretion and is useful as a pharmaceutical composition for preventing and/or treating the neurodegenerative disease, etc.
摘要:
Compounds of formula (I): ##STR1## (in which R.sup.1 is alkoxy, R is alkyl, haloalkyl, alkylamino, cycloalkyl or optionally substituted phenyl, X is chlorine or fluorine and Y is selected from certain specific heterocycles) have excellent antibacterial activity. They may be prepared by introducing the group represented by Y into the corresponding compound in which Y is replaced by a halogen atom.
摘要:
Novel 1-R-1,4-dihydro-4-oxo-6-fluoro-7-(Z.dbd.N--)-quinolinecarboxylic acids and esters thereof, where R is amino, lower-alkylamino, 2-propenylamino or di-lower-alkylamino, R" is hydrogen or lower-alkyl, and Z.dbd.N is a heterocyclic group, useful as antibacterial agents, are prepared by reacting the corresponding 7-chloroquinoline derivatives with the appropriate heterocyclic compound, Z.dbd.NH. A preferred group of compounds are those where Z.dbd.N is 1-piperazinyl or 4-lower-alkyl-1-piperazinyl.