84388-68-1Relevant articles and documents
ARYLMETHYLENE HETEROCYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
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Paragraph 0205-0206, (2021/04/17)
A compound of Formula I ( I ), or a pharmaceutically acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
ARYL HETEROCYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
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Paragraph 0328-0329, (2021/04/17)
A compound of Formula (I), or a pharmaceutically-acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
ARYLMETHYLENE AROMATIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
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Paragraph 0232-0233, (2021/04/17)
A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles
Guo, Bin,Guo, Shimeng,Huang, Jing,Li, Jingya,Li, Jia,Chen, Qian,Zhou, Xianli,Xie, Xin,Yang, Yushe
, p. 5780 - 5791 (2018/11/06)
GPR40 has become a new potential therapeutic target for the treatment of diabetes due to its role in mediating the enhancement of glucose-stimulated insulin secretion in pancreatic β cells with a low risk of hypoglycemia. As an effort to extend the chemical space and identify structurally distinct GPR40 agonists with improved liver safety, a novel series of fused-ring phenyl propanoic acid analogues were designed. Comprehensive structure-activity relationship studies around novel scaffolds were conducted and led to several analogues exhibited potent GPR40 agonistic activities and high selectivity against other fatty acid receptors. Further evaluation of pharmacokinetic (PK) profiles and in vivo efficacy identified compound 40a with excellent PK properties and significant glucose-lowering efficacy during an oral glucose tolerance test. In addition, compound 40a displayed lower hepatobiliary transporter inhibition and favorable druggability. All results indicate that compound 40a is a promising candidate for further development.
Pd-Catalyzed Ortho C-H Hydroxylation of Benzaldehydes Using a Transient Directing Group
Chen, Xiao-Yang,Ozturk, Seyma,Sorensen, Erik J.
supporting information, p. 6280 - 6283 (2017/12/08)
The direct Pd-catalyzed ortho C-H hydroxylation of benzaldehydes was achieved using 4-chloroanthranilic acid as the transient directing group, 1-fluoro-2,4,6-trimethylpyridnium triflate as the bystanding oxidant, and p-toluenesulfonic acid as the putative oxygen nucleophile. The unusual C-H chlorination and polyfluoroalkoxylation reactions signaled the importance of external nucleophiles to the outcome of Pd(IV) reductive eliminations.
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models
Cheng, Jianjun,Giguere, Patrick M.,Schmerberg, Claire M.,Pogorelov, Vladimir M.,Rodriguiz, Ramona M.,Huang, Xi-Ping,Zhu, Hu,McCorvy, John D.,Wetsel, William C.,Roth, Bryan L.,Kozikowski, Alan P.
supporting information, p. 578 - 591 (2016/02/05)
A series of novel compounds with two halogen substituents have been designed and synthesized to further optimize the 2-phenylcyclopropylmethylamine scaffold in the quest for drug-like 5-HT2C agonists. Compound (+)-22a was identified as a potent
CYCLOPROPYLMETHANAMINES AS SELECTIVE 5-HT(2C) RECEPTOR AGONISTS
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Paragraph 0273-0275, (2016/08/23)
Disclosed are 2-phenyl-cyclopropylmethanamines which are selective 5-HT(2C) receptor agonists and are used in the treatments of diseases and conditions wherein modulation of 5-HT(2C) receptors provides a benefit, such as obesity and psychiatric disorders.
BORONIC ACID BEARING LIPHAGANE COMPOUNDS AS INHIBITORS OF P13K- a AND/OR B
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Paragraph 0114; 0123, (2015/02/25)
Compounds with unique liphagane meroterpenoid scaffold having boronic acid functionality in the skeleton are described (formula 1) together with pharmacological potential of these compounds as anticancer agents. A method of preparation and inhibiting the activity of phosphoinositide-3-kinase (PI3K-alpha and beta) has been presented. In particular, the invention describes a method of inhibiting PI3K isoforms, wherein the compounds are novel structures based on liphagane scaffold with unique boronic acid functionality. The methods and uses thereof are described herein this invention.
BORONIC ACID BEARING LIPHAGANE COMPOUNDS AS INHIBITORS OF PI3K-alpha AND/OR beta
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Page/Page column 19; 30, (2013/10/08)
Compounds with unique liphagane meroterpenoid scaffold having boronic acid functionality in the skeleton are described [formula 1] together with pharmacological potential of these compounds as anticancer agents. A method of preparation and inhibiting the activity of phosphoinositide-3-kinase (PI3K-alpha and beta) has been presented. In particular, the invention describes a method of inhibiting PI3K isoforms, wherein the compounds are novel structures based on liphagane scaffold with unique boronic acid functionality. The methods and uses thereof are described herein this invention. The claimed Markush formula is: [Formular 1], Y can be O, NH, NR, S; Representative compounds are: [Compounds A, B, C, D]
WATER-SOLUBLE SHPS AS NOVEL ALKYLATING AGENTS
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Page 9, (2010/02/09)
The present invention relates to compounds according to the structure (I): Where R is —CH3 or —CH2CH2Cl; R′ is C1-C7 alkyl or —CH2CH2Cl; R2 or R4 is OPOsub