摘要:
In its many embodiments, the present invention provides a novel class of 5-membered, nitrogen-containing heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要:
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
摘要:
Disclosed is a method of treating a disease or condition (e.g., pain, diabetes or disorders of lipid metabolism) comprising administering an azetidine derivative of the formula I selected from the group consisting of the compounds defined by Tables 1, 2, 3a, 3b, 3c, 3d and 4a.
摘要:
The present invention relates to methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering a compound having the formula or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof, wherein: R1 and R2 are defined in Tables 1-6 herein, and R3 is -phenyl, -4-chlorophenyl, -2-pyridyl, or -3-pyridyl.
摘要:
The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).
摘要:
A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome and dyslipidemia.
摘要:
The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).
摘要:
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease. The novel compounds typically include a 15-20 member macrocycle and have the general structure of structural Formula 1: wherein Z′, L′, M′, R1, X and D are defined herein.
摘要:
The present invention relates to Azetidinone Derivatives, compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.
摘要:
Disclosed are compounds of the formula wherein Z1 is —CH2— or —C(O)—, R4 and R5 are carbon chains (and optionally, together can form a C2 bridge), u and v are independently an integer of 0-3 such that there sum is from 3 to 5, and R2 is heteroaryl, and R1 and R3 are as defined herein. Also disclosed are methods of treating pain, and methods of inhibiting the absorption of cholesterol using a compound of formula I.
摘要翻译:公开了下式的化合物其中Z 1是-CH 2 - 或-C(O) - ,R 4和R 4, 5是碳链(并且可选地,一起可以形成C 2 H 2桥),u和v独立地是0-3的整数,使得总和为3至5,并且 R 2是杂芳基,R 1和R 3如本文所定义。 还公开了治疗疼痛的方法,以及使用式I化合物抑制胆固醇吸收的方法。