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method for the preparation of new gesub honor pyridine derivatives applicable as medicines with antihistamine, allergic and bronchodilatore force.
method for the preparation of new gesub honor pyridine derivatives applicable as medicines with antihistamine, allergic and bronchodilatore force.
Novel compounds useful as antihistamine agents, antiallergy agents, and bronchodilators are represented by the following formula WHEREIN R1 represents cyclohexyl, phenyl, or substituted phenyl wherein the substituent on the substituted phenyl is selected from halogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, or a lower alkoxy group of from 1 to 4 carbon atoms; R2 represents hydrogen or hydroxy; R3 represents hydrogen; or R2 and R3 taken together form a second bond between the carbon atoms bearing R2 and R3; n is an integer of from 1 to 3; Z represents thienyl, naphthyl, phenyl, or substituted phenyl wherein the substituent on the substituted phenyl may be attached at the ortho, meta or para position of the phenyl ring and is selected from halogen, a straight or branched alkyl group of from 1 to 6 carbon atoms, an alkoxy group of from 1 to 6 carbon atoms, a cycloalkyl group of from 3 to 6 carbon atoms, di(lower)alkylamino, or a saturated monocyclic heterocyclic group such as pyrrolidino, piperidino, morpholino, or N-(lower)alkylpiperazino with the proviso that when R1 is phenyl, Z is naphthyl or phenyl substituted with a straight or branched alkyl group of 5 or 6 carbon atoms, a lower alkoxy group of 5 or 6 carbon atoms, or a cycloalkyl group of from 3 to 6 carbon atoms. Pharmaceutically acceptable acid addition salts and individual optical isomers of compounds of the above formula are also included as a part of this invention.
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机译:用作抗组胺药,抗过敏药和支气管扩张药的新型化合物由下式表示:其中R1代表环己基,苯基或取代的苯基,其中取代的苯基上的取代基选自卤素,直链或支链的低级烷基,范围为1 -4个碳原子,或1-4个碳原子的低级烷氧基; R 2代表氢或羟基; R3代表氢; R 2和R 3一起在带有R 2和R 3的碳原子之间形成第二键; n为1至3的整数; Z表示噻吩基,萘基,苯基或取代的苯基,其中取代的苯基上的取代基可以连接在苯环的邻,间或对位,并且选自卤素,1至6的直链或支链烷基碳原子,具有1至6个碳原子的烷氧基,具有3至6个碳原子的环烷基,二(低级)烷基氨基或饱和单环杂环基,例如吡咯烷基,哌啶子基,吗啉代或N-(低级) )烷基哌嗪子基,条件是当R1为苯基时,Z为萘基或被5或6个碳原子的直链或支链烷基,5或6个碳原子的低级烷氧基或3至3的环烷基取代的萘基或苯基6个碳原子。上式化合物的药学上可接受的酸加成盐和各个旋光异构体也包括在本发明中。
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