公开(公告)号：EP1202954B1

公开(公告)日：2003-10-01

申请号：EP00943698.1

申请日：2000-07-11

申请人： Leo Pharma A/S

发明人： OTTOSEN, Erik, Rytter ,  BJÖRKLING, Fredrik

IPC分类号： C07C225/22 ,  A61K31/136 ,  A61P17/10

CPC分类号： C07C225/22 ,  A61K31/136 ,  A61K31/166 ,  A61K31/325 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to compounds of formula (I) wherein R1 represents one or more, similar or different substituents; R2 represents hydrogen, hydroxy, halogen, alkyl, alkoxy, alkylthio, or cyano; R3 represents one or more, similar or different substituents; and R6 represents hydrogen or methyl; and salts thereof with pharmaceutically acceptable acids, hydrates, and solvates, and to the use of compounds of general formula (II) in which formula R1 and R2 independently represent one or more, similar or different substituents; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, phenyl, cyano, carboxy, or carbamoyl; R4, R5 and R6 represent independently hydrogen, trifluorormethyl, alkyl, carbamoyl, alkoxycarbonyl, or alkaloyl; X represents oxygen, N-OH, and N-O-alkyl, dialkoxy, cyclic dialkoxy, dialkylthio, or cyclic dialkylthio, and salts thereof with pharmaceutically acceptable, non-toxic acids. The compounds of the invention are useful in the human and veterinary practice.

公开(公告)号：EP1397355A1

公开(公告)日：2004-03-17

申请号：EP02771630.7

申请日：2002-05-24

申请人： LEO PHARMA A/S

发明人： BJÖRKLING, Fredrik

IPC分类号： C07D401/12 ,  A61K31/44 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D213/89 ,  A61K31/4439 ,  A61K45/06 ,  C07D401/12

摘要： Compounds according to formula (I) wherein R1 represents hydrogen, halogen or one or more straight or branched, saturated or unsaturated C1-6 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amico, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; X represents a straight or branched, saturated or unsaturated C1-12 hydrocarbon diradical, optionaly substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; Y represents a bond, O, C(O), S, S(O), S(O)2, C(O)O, NH, C(O)NH, OC(O) or NHC(O); Z represents an aromatic or non-aromatic heterocyclic radical with 5-12 ring atoms, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, aminoalkyl or straight or branched, saturated or unsaturated C1-4 hydrocarbon radical, optionally substituted with halogen, hydroxy,cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl or aminoalkyl; provided that R1 is not attached to the nitrogen-atom in the pyridyl ring, and pharmaceutically acceptable salts, solvates, hydrates, N-oxides and prodrugs thereof are disclosed. The compounds are useful in therapy.

摘要翻译： 其中R 1代表氢，卤素或任选被卤素，羟基，氰基，硝基，羧基，烷氧基，烷氧基羰基，烷基羰基，甲酰基，烷氧基羰基， ，氨基烷基，氨基羰基，烷基羰基氨基，磺基，氨基磺酰基，烷基磺酰基氨基，羟基磺酰氧基，二羟基膦酰基氧基或膦酰基; X代表被卤素，羟基，氰基，硝基，羧基，烷氧基，烷氧基羰基，烷基羰基，甲酰基，氨基，氨基烷基，氨基羰基，烷基羰基氨基，磺基，氨基磺酰基，烷基磺酰基氨基取代的直链或支链的饱和或不饱和C1-12烃二价基团 ，羟基磺酰氧基，二羟基膦酰氧基或膦酰基; Y表示键，O，C（O），S，S（O），S（O）2，C（O）O，NH，C（O）NH，OC（O）或NHC（O）。 Z代表任选被卤素，羟基，氰基，硝基，烷氧基，烷氧基羰基，烷基羰基，甲酰基，氨基烷基或直链或支链，饱和或不饱和的C 1-4烃基取代的具有5-12个环原子的芳族或非芳族杂环基 任选被卤素，羟基，氰基，硝基，烷氧基，烷氧基羰基，烷基羰基，甲酰基或氨基烷基取代; 条件是R1不与吡啶环中的氮原子连接，并公开了其药学上可接受的盐，溶剂合物，水合物，N-氧化物和前药。 这些化合物可用于治疗。

公开(公告)号：EP1397355B1

公开(公告)日：2009-09-09

申请号：EP02771630.7

申请日：2002-05-24

申请人： LEO PHARMA A/S

发明人： BJÖRKLING, Fredrik

IPC分类号： C07D401/12 ,  A61K31/44 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D213/89 ,  A61K31/4439 ,  A61K45/06 ,  C07D401/12

摘要： Compounds according to formula (I) wherein R1 represents hydrogen, halogen or one or more straight or branched, saturated or unsaturated C1-6 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amico, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; X represents a straight or branched, saturated or unsaturated C1-12 hydrocarbon diradical, optionaly substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; Y represents a bond, O, C(O), S, S(O), S(O)2, C(O)O, NH, C(O)NH, OC(O) or NHC(O); Z represents an aromatic or non-aromatic heterocyclic radical with 5-12 ring atoms, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, aminoalkyl or straight or branched, saturated or unsaturated C1-4 hydrocarbon radical, optionally substituted with halogen, hydroxy,cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl or aminoalkyl; provided that R1 is not attached to the nitrogen-atom in the pyridyl ring, and pharmaceutically acceptable salts, solvates, hydrates, N-oxides and prodrugs thereof are disclosed. The compounds are useful in therapy.