摘要:
It provides LPA antagonists, as well as pharmaceutical compositions comprising the compounds disclosed herein. It also provides methods for treating LPA-associated diseases, disorders, and conditions.
摘要:
A chelate and associated security feature including a lanthanide metal and a ligand of formula (1), formula (2), or formula (3), where each of R1-R7 in formula (1) is independently selected from the group consisting of H, OH, NH2, Cl, F, OMe, OAr, OCF3, CF3, alkyl, aryl, phenyl, OPh, and heteroaromatic, where each of R1-R5 in formula (2) is independently selected from the group consisting of H, OH, NH2, Cl, F, OMe, OAr, OCF3, CF3, NMe2, ON, alkyl, aryl, phenyl, OPh, and heteroaromatic, and where Re in formula (2) is selected from the group consisting of H, ΝH2, Cl, F, OMe, OAr, OCF3, CF3, NMe2, CN, alkyl, aryl, phenyl, OPh, and heteroaromatic, and where each of R1-R5 in formula (3) is independently selected from the group consisting of H, OH, NH2, Cl, F, OMe, OAr, OCF3, CF3, alkyl, aryl, phenyl, OPh, and heteroaromatic.
摘要:
The invention relates to succinic acid addition salts or fumaric acid addition salts of piperazine derivatives of formula (I), as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and in particular as glycosidase inhibitors.
摘要:
The present invention relates to novel heterocyclic compounds of the general formula (I) their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers and polymorphs. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds and their use as the compounds of the invention belong to the family of NOD-like receptor family (NLR) protein NLRP3 modulators. The present invention thus relates to novel NLRP3 modulators as well as to the use of the novel inhibitor compounds in the treatment of diseases or conditions as well as treatment of disease states mediated by NLRP3 as well as treatment of diseases or conditions in which interleukin 1β activity and interleukin-18 (IL-18) is implicated.
摘要:
Provided herein are substituted imidazo[1,2-a]pyridines useful as inhibitors of BMP signaling. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention also provides medical uses of substituted imidazo [1,2-a] pyridines.
摘要:
Kinases can be engineered to utilize an ATP analog that is not readily utilized by wild-type kinases by introducing a mutation in the ATP-binding pocket. However, application of this method has been limited by the membrane impermeability of the ATP analog. Provided herein are methods for in situ visualization of substrates of an analog-sensitive kinase, the method comprising a mild fixation step. Also provided herein are kits comprising a fixative, an ATP analog, and an agent for detecting the substrates modified by the ATP analog.
摘要:
The present invention discloses novel conjugates of benzothiazole derivatives with cystine and glucosamine and their method of synthesis. Their method of synthesis is easy and eco-friendly, avoiding the use of hazardous materials or reactions, The compounds offer technical advantages of increased solubility, potency, selectivity and biological activity. The novel compounds show antibacterial, antifungal and anticancer activities. Formula, physico-chemical data and biological activity of the novel derivatives are as given in Tables 1 to 9.