摘要:
In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
摘要:
The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.
摘要:
Provided is the use of or compositions or formulations comprising Burkholderia species, filtrate, supernatant, extract, pesticidally active compound or metabolite derived therefrom as an insecticide, particularly against infestation of Corn Rootworm larvae, and/or as crop yield enhancer.
摘要:
The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth. Specifically, the invention provides azole derivatives represented by general formula (I), or pharmaceutically acceptable salts thereof that have an antagonistic action against the arginine-vasopressin (AVP) V1b receptor:
摘要:
Compounds are disclosed that are effective in inhibition of fatty acid amide hydrolase, an enzyme responsible for catabolism of endogenous cannabinoids such as anandamide. The compounds are useful as analgesic compounds and as sleep-inducing compounds, that can be orally administered, and that can have a relatively long duration of effect. Methods of preparation of the compounds are also provided. The compounds are conformationally constrained analogs of heterocyclylketones such as oxazolylketones.
摘要:
Disclosed is a novel triazinone compound with an inhibitory activity on a T-type voltage-dependent calcium channel, and is specifically useful for prevention or treatment of pain, chronic kidney disease and atrial fibrillation. A novel triazinone compound of Formula (I), wherein each substituent in the formula is defined in detail in the description, R4 means a hydrogen atom, or a C1-6 alkoxy group, etc., L1 and L2 each independently mean a single bond, or NR2, etc., L3 means a C1-6 alkylene group, etc., A means a C6-14 aryl group or a 5 to 10-membered heteroaryl group which may be substituted, B means a C3-11 cycloalkylene group, etc., D means a C6-14 aryl amino group or a 5 to 10-membered heteroaryl group which may be substituted, etc., a tautomer of the compound, a pharmaceutically acceptable salt of the compound, or a solvate of the compound, the tautomer, or the pharmaceutically acceptable salt.
摘要:
This disclosure provides compounds having the structure: wherein L3, R7, Rd and p are defined herein, which are modulators of MAGL and/or ABHD6. Further provided is the use of these compounds as medicinal agents, processes for their preparation, and pharmaceutical compositions that include the disclosed compounds. The disclosure also provides a method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
摘要:
Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP(1-42), PTH(1-34), Glucagon(1-29), GLP-2(1-33), GLP-1(7-36), GLP-1(9-36), oxyntomodulin and exendin variants.
摘要:
This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.