摘要:
Disclosed herein are 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivative of formula I, or pharmaceutically acceptable salts or solvates thereof wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives according to the present invention and their use in therapy.
摘要:
Substituted pyridines, pyrimidines, pyrazines, pyridinones, pyrimidinones, pyrazinones and phenylacetamides useful in treating depression, stress and other disorders are disclosed. The compounds are of the formualae: Other embodiments are also disclosed.
摘要:
The present invention relates to 2-(4-oxo4H-quinazolin-3-yl)acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.
摘要:
Disclosed herein are quinazolinone derivatives of formula I, or pharmaceutically acceptable salts or solvates thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising quinazolinone or isoquinolinone according to the present invention and its use in therapy.
摘要:
Disclosed herein are 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivative of formula I, or pharmaceutically acceptable salts or solvates thereof wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives according to the present invention and their use in therapy.
摘要:
The invention provides for compounds having the structure according to the formula I wherein: X is a carbon or nitrogen atom; Ar is phenyl or heteroaromatic ring; R1 is hydrogen, halogen, CN or (1C-4C)alkyl; R2 is hydrogen, halogen or optionally fluorinated (1C-3C)alkoxy; R3 and R5 are independently hydrogen, optionally halogenated (1C-4C)alkyl, optionally halogenated (1C-4C)alkoxy, optionally halogenated aryl(1C-4C)alkoxy, optionally halogenated (1C-4C)alkenyl or hydroxylmethyl; R4 is hydrogen, halogen, optionally halogenated (1C-4C)alkoxy or optionally halogenated aryl(1C-4C)alkoxy; R6 is hydrogen, benzyl, optionally substituted with one or more halogens or (1C-4C)alkyl, or R6 is optionally halogenated (1C-4C)alkyl; each R7 independently is hydrogen, halogen, optionally halogenated (1C-4C)alkyl or optionally halogenated (1C-4C)alkoxy and pharmaceutically suitable acid addition salts thereof for use as glucocorticoid receptor modulators, in particular for treatment of central nervous system disorders.
摘要翻译:本发明提供具有式I结构的化合物,其中:X是碳原子或氮原子; Ar是苯基或杂芳环; R 1是氢,卤素,CN或(1C-4C)烷基; R 2是氢,卤素或任选氟化的(1C-3C)烷氧基; 卤代(1C-4C)烷氧基,任选卤代(1C-4C)烷氧基,任意卤代的芳基(1C-4C)烷氧基 ,任选卤代(1C-4C)烯基或羟甲基; R 4是氢,卤素,任选卤代的(1C-4C)烷氧基或任选的卤代芳基(1C-4C)烷氧基; R 6是氢,任选被一个或多个卤素或(1C-4C)烷基取代的苄基,或任选被卤代(C 1 -C 4)烷基取代; 每个R 7独立地是氢,卤素,任选卤代(1C-4C)烷基或任选卤代(1C-4C)烷氧基及其药学上合适的酸加成盐,用作糖皮质激素受体调节剂,特别是 治疗中枢神经系统疾病。
摘要:
The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulas:
摘要:
Disclosed herein are quinazolinone or isoquinolinone derivatives of formula I, or pharmaceutically acceptable salts or solvates thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising quinazolinone or isoquinolinone according to the present invention and its use in therapy.
摘要:
A genus of dihydropyridine chemical modulators of synaptojanin is disclosed. These modulators are selective inhibitors of synaptojanin 1 and may be used to treat cognitive impairment or traumatic brain injury, including promoting regeneration in cases of traumatic brain injury, or for treating neurodegenerative disorders.
摘要:
This disclosure relates generally to compounds and compositions comprising one or more diphenylethylene, diphenylethylyne, and azobenzene analogs. These compounds are useful for treating diseases associated with NF-kB and p53 activity, such as cancer and inflammatory disease.