摘要:
Heterobicyclic and heterocyclic intermediate compounds and their use in treating inflammation, hyperproliferative skin conditions such as psoriasis and allergy are disclosed.
摘要:
This invention relates to derivatives of 1,8-naphthyridines and 1,5,8-azanaphthyridines of the general formula wherein X is CH or N and the substitutents Y, Z, R 1 and R 2 are as defined herein. The compounds are useful for treating allergic reactions in mammals.
摘要:
Certain substituted 1,8-naphthyridines and 1,5,8-azanaphthyridines of formula I are disclosed which are useful for treating allergy or inflammation in mammals. A preferred use is the treatment of chronic obstructive lung disease in mammals. The compounds have the formula
wherein X is CH or N; R¹ represents alkenyl, alkynyl, cycloalkyl, cycloalkenyl, 2-, 3- or 4- pyridinyl, 2-, 4- or 5- pyrimidinyl, 2- or 3- thienyl, 2- or 3-furanyl, alkyl carbonyl, phenyl carbonyl or alkyl, each of which may be substituted with -COOH, hydroxy, halogen, alkoxy phenyl, 2-, 3-, or 4- pyridinyl, 2-, 4- or 5-pyrimidinyl, 2- or 3-thienyl, 2- or 3- furanyl, alkyl carbonyl, phenyl carbonyl, cycloalkyl, formyloxy, alkyl carbonyloxy, or phenyl carbonyloxy; R² represents hydrogen, hydroxyalkyl, dihydroxyalkyl, hydroxyalkoxyalkyl, a cation, alkenyl having, R a R b N(CH₂) n -(wherein R a and R b are hydrogen or alkyl and n is an integer from 2 to 6), alkynyl or a group of the general formula: where Z = 0 or 1; p is an integer of 0 to 5, R³ and R⁴ are each alkyl or R³ and R⁴ together form a cycloalkyl up to 6 carbon atoms, and M is H or where Y¹, Y² and Y³ represent hydrogen, hydroxy, halogen, alkyl, alkoxy, halogenated alkyl; and A is 2-, 3- or 4-biphenyl, 1- or 2-naphthylenyl, 4- or 5-indenyl, 4- or 5- indanyl, 2-, 3-, 4-, 5-, 6-, 7-or 8-quinolinyl, 1-, 3-, 4-, 5-, 6-, 7- or 8-isoquinolinyl, 2-, 3- or 4-pyridinyl, 2-, 4- or 5-pyrimidinyl, 2-pyrazinyl, 3- or 4-pyridazinyl, 3-, 5- or 6-(1,2,4-triazinyl), 2- or 3-furanyl, 2- or 3-thienyl, 2-, 3-, 4-, 5-, 6- or 7-benzofuranyl, 3- 4- or 5-pyrazolyl, 3- or 5-(1,2,4-triazolyl) each of which may be substituted with one or more of hydroxy, alkyl, halogen, nitro, alkoxy, trifluoromethyl or cyano.
摘要翻译:公开了可用于治疗哺乳动物过敏或炎症的某些取代的1,8-萘啶和1,5'-氮杂萘并吡啶。 优选的用途是治疗哺乳动物慢性阻塞性肺病。 化合物具有式CHEM,其中X是CH或N; R 1表示烯基,炔基,环烷基,环烯基,2-,3-或4-吡啶基,2-,4-或5-嘧啶基,2-或3-噻吩基,2-或3-呋喃基,烷基羰基, 苯基羰基或烷基,其各自可以被-COOH,羟基,卤素,烷氧基苯基,2-,3-或4-吡啶基,2-,4-或5-嘧啶基,2-或3-噻吩基, 2-或3-呋喃基,烷基羰基,苯基羰基,环烷基,甲酰氧基,烷基羰氧基或苯基羰基氧基; R 2表示氢,羟基烷基,二羟基烷基,羟基烷氧基烷基,阳离子,具有R aR b N(CH 2)n - (其中R a和R b是氢或烷基,n是2-6的整数)的烯基,炔基 或通式为:CHEM>其中Z = 0或1的基团; p为0至5的整数,R 3和R 4各自为烷基或R 3和R 4一起形成至多6个碳原子的环烷基,M为H或CHEM,其中 Y 1,Y 2和Y 3表示氢,羟基,卤素,烷基,烷氧基,卤代烷基; 和A是2-,3-或4-联苯基,1-或2-萘基,4-或5-茚基,4-或5-二氢茚基,2-,3-,4-,5-,6-,7 或8-喹啉基,1-,3-,4-,5-,6-,7-或8-异喹啉基,2-,3-或4-吡啶基,2-,4-或5-嘧啶基, 吡啶基,3-或4-哒嗪基,3-,5-或6-(1,2,4-三嗪基),2-或3-呋喃基,2-或3-噻吩基,2-,3-,4-, 5-,6-或7-苯并呋喃基,3- 4-或5-吡唑基,3-或5-(1,2,4-三唑基),其各自可以被一个或多个羟基,烷基,卤素, 硝基,烷氧基,三氟甲基或氰基。
摘要:
This invention relates to derivatives of 1,8-naphthyridines and 1,5,8-azanaphthyridines of the general formula wherein X is CH or N and the substitutents Y, Z, R 1 and R 2 are as defined herein. The compounds are useful for treating allergic reactions in mammals.