- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH APJ RECEPTOR ACTIVITY
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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.
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Page/Page column 246; 248
(2020/05/15)
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- 1-(CYCLOALKYL-CARBONYL)PROLINE DERIVATIVE
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A compound represented by formula (1) (in the formula: ring-D represents a three- to eight-membered hydrocarbon ring; Ra represents an optionally substituted amino C1-6 alkyl group or the like; Rb1 and Rb2 each independently represent a hydrogen atom, a halogen atom, or the like; Rc represents an optionally substituted C6-10 aryl group or the like; Rd represents a hydrogen atom or the like; and ring-Q represents a (hetero)aryl group or the like which may be substituted with a carboxyl group or the like) or a pharmaceutically acceptable salt thereof exhibits an excellent FXIa inhibitory activity, and is useful as a therapeutic agent against thrombosis or the like.
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Paragraph 0657; 1442; 1443
(2015/06/03)
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- PYRAZOLE DERIVATIVES AND THEIR USE AS CANNABINOID RECEPTOR MEDIATORS
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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.
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Page/Page column 40
(2015/11/27)
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- SUBSTITUTED PYRAZOLO[1,5-A] PYRIDINE AS TROPOMYOSIN RECEPTOR KINASE (TRK) INHIBITORS
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The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
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Paragraph 0599; 0600
(2015/01/06)
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- ANTIBACTERIAL THIAZOLECARBOXYLIC ACIDS
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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.
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Page/Page column 109
(2015/01/09)
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- SUBSTITUTED PYRAZOLO[1,5-A] PYRIDINE AS TROPOMYOSIN RECEPTOR KINASE (TRK) INHIBITORS
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The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors., method of making and pharmaceutical compositions comprising such compounds.
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Page/Page column 66
(2013/07/05)
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- Kinetic and mechanistic studies on sulfamate esters: Models of enzyme inhibitors
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Many compounds containing a sulfamate moiety, such as NH2SO 2O - are now known to be medicinally important. However, very little is known about their mechanisms of reaction even under non-biological conditions. In this work the vario
- McCaw, Cheryl J. A.,Spillane, William J.
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p. 512 - 517
(2007/10/03)
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- PYRIMIDYL SULPHONE AMIDE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS
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A compound of formula (I), pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof for the treatment of asthma, allergic rhinitis, COPD, inflammatory bowel disease, irritable bowel syndrome, osteoarthritis, osteoporosis, rheumatoid
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- Carbonic anhydrase inhibitors: Inhibition of cytosolic isozymes I and II with sulfamide derivatives
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A novel class of effective CAIs has been identified, starting from a very weak carbonic anhydrase inhibitor (CAI), sulfamide, whose X-ray crystal structure in the adduct with hCA II has recently been reported. A series of N,N-disubstituted- and N-substitu
- Casini, Angela,Winum, Jean-Yves,Montero, Jean-Louis,Scozzafava, Andrea,Supuran, Claudiu T.
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p. 837 - 840
(2007/10/03)
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