摘要:
New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
摘要:
##STR1## Compounds of formula (I), and salts and prodrugs thereof, wherein X is O,S,NR 4 or CH 2 ; R 1 represents H, certain optionally substituted C 1-6 alkyl, or C 3-7 cycloalkyl; R 2 represents phenyl having certain optional substituents; R 3 represents C 1-6 alkyl, halo or NR 6 R 7 ; m is 2,3 or 4; n is 1,2,3,4,5,6 7 or 8 when X is CH 2 or 2,3,4,5,6,7 or 8 when X is O, S or NR 4 ; and x is 0,1,2, or 3; are CCK and/or gastrin antagonists. They and compositions thereof are therefore useful in therapy.
摘要翻译:式(I)化合物及其盐和前体药物,其中X为O,S,NR4或CH2; R1表示H,某些任选取代的C 1-6烷基或C 3-7环烷基; R2表示具有某些任选取代基的苯基; R 3表示C 1-6烷基,卤代或NR 6 R 7; m是2,3或4; 当X为CH 2时,n为1,2,3,4,5,6,7或8,X为O,S或NR4时为2,3,4,5,6,7或8; x为0,1,2或3; 是CCK和/或胃泌素拮抗剂。 因此,它们及其组合物可用于治疗。
摘要:
New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
摘要:
New pyrazole derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
摘要:
The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
摘要:
Compounds of formula (I), or a salt or prodrug thereof, wherein Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; E represents a chemical bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1 to 6 carbon atoms, optionally substituted in any position by a hydroxy group; T represents nitrogen or CH; U represents nitrogen or C--R.sup.2 ; V represents oxygen, sulphur or N--R.sup.3 ; --F--G-- represents --CH2--N--, --CH2--CH-- or --CH.dbd.C--; R.sup.1 represents C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, any of which groups may be optionally substituted; and R.sup.2 and R.sup.3 independently represent hydrogen or C.sub.1-6 alkyl are selective agonists of 5-HT1D receptors, being potent agonists of the human 5-HT1Dalpha receptor subtype, while possessing at least a 10-fold selective affinity for the 5-HT1Dalpha receptor subtype, relative to the 5-HT1Dbeta subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
摘要:
New pyrazole derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
摘要:
The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the β2 adrenergic receptor.
摘要:
The present disclosure relates to 1, 2, 4 oxadiazole derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the S1P1 receptors.
摘要:
The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the β2 adrenergic receptor.