摘要:
The present invention relates to a compound of the formula: W-X-Q-Y-CH(R1)-O-N=C(R2)-A-COM, or a pharmaceutically acceptable salt thereof wherein W is optionally substituted aryl or heteroaryl; X is a valence bond, or methylene, divalent alkylene, alkenylene, alkynylene or alkyloxy; Q is a valence bond, or -O-, -S-, > NR4 or > NCOR5; Y is optionally substituted phenyl, biphenyl, naphthyl, tetrahydronaphthyl, indolyl, pyridyl, or benzo[b]thienyl, thienyl, thiazolyl, or thiazolylphenyl; R1 is alkyl, cycloalkyl, alkoxyalkyl, aryl or arylalkyl, heteroaryl or heteroarylalkyl; R2 is hydrogen, alkyl or hydroxyalkyl; A is a valence bond or is selected from alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, pyridylene, thienylene and furylene; and M is a pharmaceutically acceptable, metabolically cleavable group, -OR?6, -NR6R7¿, -NH-tetrazoyl, -NH-2-, 3-, or 4-pyridyl, and -NH-2-, 4-, or 5-thiazolyl which inhibit leukotriene biosynthesis and are useful in the treatment of inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method for inhibiting lipoxygenase activity and leukotriene biosynthesis.
摘要:
Compounds of formula (I), are novel P2X3 and P2X2/P2X3 antagonists which are useful in treating pain, urinary incontinence and bladder overactivity.
摘要:
Compounds of formula (I), are novel P2X3 and P2X2/P2X3 antagonists which are useful in treating pain, urinary incontinence and bladder overactivity.
摘要:
The present invention describes pyridazinone compounds of formula (I) which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important 'housekeeping' enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectively of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).
摘要:
L'invention concerne des composés ayant la formule (I) dans laquelle p et q sont égaux à zéro ou un, mais sont différents l'un de l'autre, M est un cation pharmaceutiquement acceptable ou un groupe clivable par le métabolisme, B est une liaison de valence ou un groupe alkylène linéaire ou ramifié, R est alkyle, cycloalkyle ou -NR1R2, où R1 et R2 sont hydrogène, alkyle, cycloalkyle ou alcanoyle, et A est aryle, furyle, benzo[b]furyle, thiényle ou benzo[b]thiényle carbocyclique substitué ou non; ces composés sont de puissants inhibiteurs des enzymes de lipoxygénase et par conséquent ils inhibent la biosynthèse des leukotriènes. Les composés de cette invention sont utiles pour traiter ou pour améliorer les états pathologiques allergiques et inflammatoires.
摘要:
The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), wherein L1, R1, R2, R3, R4, R5, R6, R7 and Rc are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
摘要:
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
摘要:
Compounds having formula (I), wherein W is the same at each occurrence and is selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R?1 and R2¿ are independently selected from hydrogen, alkyl, haloalkyl, alkoxy, halogen; R3 is a valence bond or is selected from hydrogen and alkyl; X is a valence bond or is selected from alkylene, alkenylen, and alkynylene; and Z is selected from (a) COM, (b) CH=N-O-A-COM, (c) CH¿2?-O-N=A-COM wherein A is selected from alkylene and cycloalkylene, and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) -OR?6¿, (c) -NR7R8, (d) -NR6SO2R9, (e) -NH-Tetrazolyl, and (f) glycinyl inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method of inhibiting leukotriene biosynthesis.
摘要:
L'invention concerne des composés utiles pour inhiber la biosynthèse de leucotrienes, de la structure (I), dans laquelle M représente hydrogène, un cation pharmaceutiquement acceptable ou un groupe clivable de manière métabolique, R4 représente alkyle, cycloalkyle ou -NR5R6, où R5 et R6 représentent hydrogène, alkyle, cycloalkyle ou alcanoyle, dans laquelle A représente une liaison de valence ou un groupe alkylène divalent droit ou ramifié comprenant un à douze atomes de carbone, R2 et R3 sont choisis indépendamment entre hydrogène, alkyle droit ou ramifié comprenant un à douze atomes de carbone, halogène ou trifluoroalkyle, et R1 est choisi entre phénoxy, phénylthio, 2-, 3- ou 4-pyridiloxy, 1, ou 2-naphtyloxy, ou 2, 4, 5 ou 8-quinolyloxy, tous facultativement substitués par alkyle, haloalkyle, alcoxy, hydrogène ou halogène.
摘要:
L'invention concerne des composés d'urée N-hydroxy de phényle, naphtyle et thiényle à substitution, formant une classe d'inhibiteurs puissants de lipoxygénase 5 et 12, utiles dans le traitement d'états inflammatoires dans lesquels des leucotriènes ainsi que d'autres produits présentant une activité enzymatique de lipoxygénase sont impliqués.