摘要:
The invention provides compounds that are modulators of neuropeptide Y (NPY) receptors, which can be selective inhibitors of NPY receptor Y2R. NPY receptor modulatory compounds are of the general formula Ar 2 -Y-Ar 1 -W-Ar 3 , wherein the variables are as defined herein. Compounds of the invention can be used for treatment of malconditions in patients wherein modulation of an NPY receptor is medically indicated, for example including drug or alcohol abuse, anxiety disorders, depression, stress-related disorders, neurological disorders, nerve degeneration, osteoporosis or bone loss, sleep/wake disorders, cardiovascular diseases, obesity, anorexia, inovulation, fertility disorders, angiogenesis, cell proliferation, learning and memory disorders, migraine and pain.
摘要:
Compounds are described that are prodrugs to active compounds that modulate a muscarinic receptor. In some cases, the compounds are prodrugs to. N-desmethylclozapine. The compounds may be used to treat neuropsychiatric disorders.
摘要:
Disclosed herein is a compound of Formula (I). Also disclosed herein is a method of modulating the activity of a cannabinoid receptor using a compound of Formula (I). Furthermore, disclosed herein is a method of treating a disease or condition that would be alleviated, improved or prevented by administration of a compound that modulates a cannabinoid receptor comprising identifying a subject in need thereof and administering to said subject a therapeutically effective amount of a compound of Formula (I). Also disclosed herein are pharmaceutical compositions comprising a compound of Formula (I).
摘要:
Die vorliegende Erfindung betrifft Verbindungen, Verfahren zur ihrer Herstellung, sie umfassende pharmazeutische Zusammensetzungen sowie ihre Verwendung bei der Behandlung und/oder Prophylaxe von Erkrankungen bei Menschen oder Tieren, insbesondere von Herz-Kreislauf-Erkrankungen, z. B. von Atherosklerose.
摘要:
The present invention relates to dibenzo-azepine derivatives and their use as alphaV integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors alphaVbeta3, alphaVbeta5, and/or alphaVbeta6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
摘要:
The present invention provides substituted dibenzoxazepine and dibenzothiazepine compounds of formula (I) which are useful as analgesic agents for the treatment of pain, and for prostaglandin-E2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of formula (I) in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of formula (I) to the animal, and a method for treating prostaglandin-E2 mediated diseases in an animal comprising administering a therapeutically-effective amount of a compound of formula (I) to the animal.
摘要:
The present invention provides substituted dibenzoxazepine compounds of formula (I) which are useful as analgesic agents for the treatment of pain, and as prostaglandin-E2 antagonists for the treatment of prostaglandin-E2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of formula (I) in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin-E2 mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of formula (I) to the animal.
摘要:
Compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein: X is CH2, O, S, or NR where R is C1-4 alkyl; R1 and R2 are independently selected from hydrogen, hydroxy, C1-4 alkyl, C1-4 alkoxy, halogen or CF3; R3 is C1-7 alkyl, C2-5 alkynyl, C3-7 cycloalkyl, C4-7 cycloalkenyl or C1-6 alkyl substituted by C2-7 alkenyl, C2-7alkynyl, C3-7 cycloalkyl, hydroxy, thiol, C1-6 alkoxy, C1-6 alkylthio, carboxy, C1-6 alkoxycarbonyl, C2-7 alkanoyl, amino optionally substituted by one or two C1-4 alkyl or by C4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C1-6 alkyl groups, or benzoyl or phenyl either being optionally ring-substituted by one or two C1-4 alkyl, C1-4 alkoxy, halogen or trifluoromethyl; and one of R4, R5 and R6 is C1-6 alkyl and the other two are independently hydrogen or C1-6 alkyl, having anti-depressant and/or anxiolytic activity, a process for their preparation and their use.
摘要翻译:式(I)化合物或其药学上可接受的盐,其中:X为CH 2,O,S或NR,其中R为C 1-4烷基; R 1和R 2独立地选自氢,羟基,C 1-4烷基,C 1-4烷氧基,卤素或CF 3; R3是C1-7烷基,C2-5炔基,C3-7环烷基,C4-7环烯基或被C2-7烯基取代的C1-6烷基,C2-7炔基,C3-7环烷基,羟基,硫醇,C1-6烷氧基 C 1-6烷硫基,羧基,C 1-6烷氧基羰基,C 2-7烷酰基,任选被一个或两个C 1-4烷基取代的氨基或任选地含有氧或氮原子的C 4-6二聚亚甲基,任选地被一个或多个N取代的氨基羰基 或两个C 1-6烷基,或任选被一个或两个C 1-4烷基,C 1-4烷氧基,卤素或三氟甲基环取代的苯甲酰基或苯基; R 4,R 5和R 6中的一个是C 1-6烷基,另外两个独立地是氢或具有抗抑郁和/或抗焦虑活性的C 1-6烷基,其制备方法和用途。