摘要:
A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, or solvate thereof, wherein, R.sup.o represents an aryl group, optionally substituted; X represents O or S; R.sup.1 and R.sup.1a each independently represents hydrogen or an alkyl group; R.sup.2 represents OCH.sub.2 CO.sub.2 H, or an ester or amide thereof, or R.sup.2 represents a moiety of formula (b): ##STR2## wherein R.sup.4 represent hydrogen, alkyl, hydroxyalkyl, arylalkyl, aralkyloxyalkyl or cycloalkyl and R.sup.5 represent hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, arylalkoxyalkyloxy, cycloalkyloxy, hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, arylalkyloxyalkyl or R.sup.5 together with OR.sup.4 represents O(CH.sub.2).sub.n O wherein n is 2, 3 or 4; and R.sup.3 represents hydrogen, halogen, alkyl or alkoxy or R.sup.3 together with R.sup.2 represents a moiety of formula (c): ##STR3## or an ester or amide thereof; a pharmaceutical composition containing such a compound, a process of preparing such a compound and the use of such a compound in medicine.
摘要翻译:式(I)的化合物:其中,R 1表示任选被取代的芳基;(I)化合物或其药学上可接受的盐或其溶剂合物, X表示O或S; R 1和R 1a各自独立地表示氢或烷基; R 2表示OCH 2 CO 2 H或其酯或酰胺,或R 2表示式(b)的部分:其中R 4表示氢,烷基,羟烷基,芳烷基,芳烷氧基烷基或环烷基,R 5表示羟基,烷氧基,芳基烷氧基 ,羟烷基氧基,烷氧基烷氧基,芳基烷氧基烷氧基,环烷氧基,氢,烷基,取代烷基,环烷基,芳基,芳基烷基,芳基烷氧基烷基或R5与OR4一起表示O(CH2)nO,其中n为2,3或4; 并且R 3表示氢,卤素,烷基或烷氧基,或者R 3与R 2一起表示式(c)的部分:(c)或其酯或酰胺; 含有这种化合物的药物组合物,制备这种化合物的方法以及这种化合物在医药中的用途。
摘要:
A compound of the formula (I), or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein, X represents a moiety of formula (a), in which A.sup.1 represents --CH.dbd.CH.dbd., NH, S or O; A.sup.2 represents an oxo or a thioxo group; A.sup.3 represents H or an alkylcarbonyl group; and A.sup.4 represents hydroxy or NR.sup.s R.sup.t wherein R.sup.s and R.sup.t each independently represents H or alkyl; R.sup.0 and R.sup.1 each independently represents hydrogen or an alkyl group; R.sup.2 represents OCH.sub.2 CO.sub.2 H, or an ester or amide thereof, or R.sup.2 represents a moiety of formula (b), wherein R.sup.4 and R.sup.5 each independently represent hydrogen, alkyl, hydroxyalkyl, cycloalkyl or R.sup.4 together with R.sup.5 represents (CH.sub.2).sub.n wherein n is 2, 3 or 4; and R.sup.3 represents hydrogen, halogen, alkyl or alkoxy or R.sup.3 together with R.sup.2 represents a moiety of formula (c) or an ester or amide thereof, wherein R represents hydrogen, alkyl, hydroxymethyl or a moiety of formula (CH.sub.2).sub.n CO.sub.2 H, wherein n is zero or an integer 1, 2 or 3, or an ester or amide thereof; a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of such a compound and composition in medicine.
摘要:
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl, or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description.The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis or osteoarthritis or neurodegenerative disorders.
摘要:
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.
摘要:
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: A is C1-6alkyl, C3-6cycloalkyl, —CH2—R6, —CHMe-R7, —CMe2-R7, or optionally substituted aryl; wherein, when A is optionally substituted aryl, said aryl group is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of halogen, C1-6alkyl, —CF3, C1-4alkoxy, C1fluoroalkoxy, cyano, NR8R9, and pyridyl wherein the pyridyl is optionally substituted by one methyl; R1 is chlorine, fluorine, —CF3, cyano or C1-6alkyl; R2, R3 and R5 independently are hydrogen, fluorine, chlorine, —CF3, cyano or C1-6alkyl, such that at least one of R2, R3 and R5 is other than hydrogen; R4 is hydrogen. These compounds and salts are thought to be P2X7 receptor antagonists. The invention also provides for the treatment of pain, inflammation, rheumatoid arthritis, osteoarthritis, or a neurodegenerative disease.
摘要:
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH2 CO, S or NH, or the moiety X—R1 is hydrogen; Y1 and Y2 independently represent CH or N; Ar is a mono- or fused bicyclic aromatic or heteroaromatic group which may be optionally substituted; one of X1 and X2 is selected from O, S or NR11 and the other is CH, wherein R11 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl.
摘要翻译:化合物及其作为药物的用途,特别是用作治疗神经创伤性疾病,癌症,慢性神经变性,疼痛,偏头痛和心脏肥大的Raf激酶抑制剂。 其中X是O,CH 2 CO,S或NH,或者X-R 1部分是氢; Y 1和Y 2独立地表示CH或N; Ar是可以任选取代的单或二稠合双环芳族或杂芳族基团; X 1和X 2之一选自O,S或NR 11,另一个是CH,其中R 11, / SUP>是氢,C 1-6烷基,芳基或芳基C 1-6烷基。
摘要:
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.
摘要:
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis or osteoarthritis or neurodegenerative disorders.
摘要:
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.
摘要:
The present invention relates to novel benzazepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.