119027-36-0Relevant academic research and scientific papers
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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Page/Page column 485, (2019/02/13)
In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured.The variables shown in Formula AA are as defined in the claims. The compounds of formula AA are NLRP3 activity modulators and, as such, can be used in the treatment of metabolic disorders (e.g. Type 2 diabetes, atherosclerosis, obesity or gout), a disease of the central nervous system (e.g. Alzheimer's disease, multiple sclerosis, Amyotrophic Lateral Sclerosis or Parkinson's disease), lung disease (e.g. asthma, COPD or pulmonary idiopathic fibrosis), liver disease (e.g. NASH syndrome, viral hepatitis or cirrhosis), pancreatic disease (e.g. acute pancreatitis or chronic pancreatitis), kidney disease (e.g. acute kidney injury or chronic kidney injury), intestinal disease (e.g. Crohn's disease or Ulcerative Colitis), skin disease (e.g. psoriasis), musculoskeletal disease (e.g. scleroderma), a vessel disorder (e.g. giant cell arteritis), a disorder of the bones (e.g. osteoarthritis, osteoporosis or osteopetrosis disorders), eye disease (e.g. glaucoma or macular degeneration), a disease caused by viral infection (e.g. HIV or AIDS), an autoimmune disease (e.g. Rheumatoid Arthritis, Systemic Lupus Erythematosus or Autoimmune Thyroiditis), cancer or aging.
COMPOUNDS AND THEIR METHODS OF USE
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Page/Page column 141, (2018/06/12)
The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Paragraph 00709, (2018/09/12)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
Pyridyl piperazines for the treatment of CNS disorders
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Page/Page column 15, (2010/02/15)
This invention is directed to compounds of Formula I and to pharmaceutical compositions comprising the compound of Formula I. where the dashed line represents an optional double bond; and where n is 1 or 2, and Ar1, Ar2, . . . and Z
PIPERAZINYLPHENALKYL LACTAM/AMINE LIGANDS FOR THE 5HT1B RECEPTOR
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Page/Page column 82, (2010/11/30)
The present invention relates to novel derivatives, that are compounds of Formula (I), wherein R1, R2, R3, R14, X, Y, n and m are defined herein, their pharmaceutically acceptable salts, pharmaceutical compositions and methods using said compounds in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, antagonists of 5-HT1B are useful.
11C-LABELED BENZYL-LACTAM COMPOUNDS AND THEIR USE AS IMAGING AGENTS
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Page/Page column 21-22, (2008/06/13)
The invention relates to ""C-labeled compounds, their preparation, compositions comprising an effective amount of a ""C-labeled compound, and the use of a ""C-labeled compound as a radiopharmaceutical for positron emission tomography.
NOVEL BENZYL(IDENE)-LACTAM DERIVATIVES
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Page/Page column 37-38, (2008/06/13)
The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula (I) wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13, X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.
Variable Electronic Properties of the CSNMe2 Group
Creary, Xavier,Aldridge, Timothy
, p. 4280 - 4285 (2007/10/02)
The ?I value for the CSNMe2 group has been determined and the value of 0.23 indicates that this group is inductively electron withdrawing.The effect of the p-CSNMe2 group on the solvolysis rate of cumyl chloride has also been determined and, relative to the p-H analogue, this group has a negligible effect on rate. p-CSNMe2 substitution slows the hydrolysis rate of substituted benzaldehyde dimethyl acetals. p-CSNMe2 substitution enhances the solvolysis rate of ArCH(OMs)PO(OEt)2.These variable rate effects on reactions involving cationic intermediates have been interpreted in terms of variable electronic properties of the CSNMe2 group.This group can be cation stabilizing, electroneutral, or cation destabilizing, depending on the charge demands of specific cations.This is a result of a conjugative interaction of CSNMe2 with a cationic center and resultant delocalization of positive charge onto sulfur.The importance of such conjugation is a function of the amount of transition-state charge developed on the carbon bearing the CSNMe2 group.The electronic effects of the amphielectronic p-CSNMe2 group are compared to the more conventional effects of CONMe2 and the m-CSNMe2 analogues.
