4108-90-1Relevant articles and documents
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH APJ RECEPTOR ACTIVITY
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Page/Page column 246; 248, (2020/05/15)
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize) the apelin receptor (also referred to herein as the APJ receptor; gene symbol APLNR). This disclosure also features compositions containing the same as well as other methods of using and making the same. The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which a decrease in APJ receptor activity (e.g., repressed or impaired APJ receptor signaling; e.g., repressed or impaired apelin-APJ receptor signaling) or downregulation of endogenous apelin contributes to the pathology and/or symptoms and/or progression of the disease, disorder, or condition. Non-limiting examples of such diseases, disorders, or conditions include: (i) cardiovascular disease; (ii) metabolic disorders; (iii) diseases, disorders, and conditions associated with vascular pathology; and (iv) organ failure; (v) diseases, disorders, and conditions associated with infections (e.g., microbial infections); and (vi) diseases, disorders, or conditions that are sequela or comorbid with any of the foregoing or any disclosed herein. More particular non-limiting examples of such diseases, disorders, or conditions include pulmonary hypertension (e.g., PAH); heart failure; type II diabetes; renal failure; sepsis; and systemic hypertension.
PYRAZOLE DERIVATIVES AND THEIR USE AS CANNABINOID RECEPTOR MEDIATORS
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Page/Page column 40, (2015/11/27)
The application relates to cannabinoid receptor mediators, or a pharmaceutically acceptable salt or ester thereof, useful in the treatment of e.g. obesity, diabetes or gout, having a structure of: wherein X and Y are each independently selected from optionally- substituted aryl, optionally-substituted heteroaryl, optionally- substituted cycloalkyl, optionally-substituted heterocycloalkyl, or optionally-substituted alkyl; ? Q is H, hydroxyl, or optionally-substituted alkoxy; ? R1, R2 , and R3 are each independently selected from H, optionally-substituted alkyl, optionally-substituted cycloalkyl, halogen, cyano, nitro, hydroxy, optionally-substituted alkoxy, amino, aminocarbonyl, optionally-substituted sulfonyl, optionally- substituted aryl, optionally-substituted heteroaryl, optionally- substituted carboxyl, acyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted phosphonyl, optionally-substituted phosphinyl, aralkyl, optionally-substituted thiol, or R2 and R3 together with Z form an optionally-substituted cycloalkyl ring or an optionally-substituted heterocycloalkyl ring; ? Z is B, N, -CH-, or P; ? D is -S(O) 2- or -C(O)-; and ? n is 0 to 5. The application also relates to compounds of Formula II wherein Ra is -C( =NH)R1; and Rb is a substituted sulfonyl or a substituted carbonyl.
ANTIBACTERIAL THIAZOLECARBOXYLIC ACIDS
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Page/Page column 109, (2015/01/09)
Compounds of general formula (I), wherein R1, R11, Y, R2, n and A are as defined herein are useful as inhibitors or metallo-β-lactamase (MBL) enzymes and can be used for reducing or removing antibiotic resistance in bacteria.
