- Asymmetric Synthesis of N-Substituted γ-Amino Esters and γ-Lactams Containing α,γ-Stereogenic Centers via a Stereoselective Enzymatic Cascade
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γ-Amino esters and γ-lactams containing α,γ-stereogenic centers are widely used as chiral intermediates in various bioactive compounds, while their efficient synthesis remains a challenge. Herein, an enzymatic cascade reaction involving an ene reductase (
- Li, Ming,Cui, Yunfeng,Xu, Zefei,Chen, Xi,Feng, Jinhui,Wang, Min,Yao, Peiyuan,Wu, Qiaqing,Zhu, Dunming
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p. 372 - 379
(2021/10/25)
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- MACROCYCLIC SULFONYLUREA DERIVATIVES USEFUL AS NLRP3 INHIBITORS
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The present invention relates to macrocyclic compounds, such as macrocyclic sulfonyl ureas. The present invention further relates to associated salts, solvates, prodrugs and pharmaceutical compositions and to the use of such compounds in the treatment and
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Page/Page column 147
(2021/02/26)
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- Biocatalytic synthesis of chiral cyclic γ-oxoesters by sequential C-H hydroxylation, alcohol oxidation and alkene reduction
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A three-step biocatalytic procedure is described for the conversion of methyl and ethyl cyclopentene- and cyclohexenecarboxylates into both the enantiomers of the corresponding chiral 3-oxoesters, which are useful building blocks for the synthesis of active pharmaceutical ingredients. The allylic hydroxylation of the starting cycloalkenecarboxylates is carried out by using R. oryzae resting cells entrapped in alginate beads, in acetate buffer solution at 25 °C. The oxidation of the intermediate allylic alcohols to unsaturated ketones, performed by the laccase/TEMPO system, and the ene-reductase mediated hydrogenation of the alkene bond were carried out in the same reaction vessel in a sequential mode at 30 °C. Being entirely biocatalytic, our multistep procedure provides considerable advantages in terms of selectivity and environmental impact over reported chemical methods.
- Brenna, Elisabetta,Crotti, Michele,Gatti, Francesco G.,Monti, Daniela,Parmeggiani, Fabio,Pugliese, Andrea,Tentori, Francesca
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p. 5122 - 5130
(2017/11/09)
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- COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING NEURODEGENERATIVE DISORDERS
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Compounds, pharmaceutical compositions, methods and kits are described for treating or preventing neurodegenerative diseases such as Alzheimer's disease.
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Page/Page column 77
(2017/03/08)
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- Glutaminase inhibitors as well as compositions and applications thereof
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The invention provides a series of heterocyclic compounds expressed in a formula I. The compound comprises glutaminase inhibition activity, and can be used for treating diseases and symptoms related to dysfunction of glutaminase or raising activity of glutaminase.
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Paragraph 0408; 0409; 0410; 0411
(2018/01/09)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
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Paragraph 0217
(2016/10/06)
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- Bifunctional Ligand-Assisted Catalytic Ketone α-Alkenylation with Internal Alkynes: Controlled Synthesis of Enones and Mechanistic Studies
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Here, we describe a detailed study of the rhodium(I)-catalyzed, bifunctional ligand-assisted ketone α-C-H alkenylation using internal alkynes. Through controlling the reaction conditions, conjugated enamines, α,β- or β,γ-unsaturated ketones, can be selectively accessed. Both aromatic and aliphatic alkynes can be employed as coupling partners. The reaction conditions also tolerate a broad range of functional groups, including carboxylic esters, malonates, secondary amides, thioethers, and free alcohols. In addition, excellent E-selectivity was observed for the tetra-substituted alkene when forming the α,β-unsaturated ketone products. The mechanism of this transformation was explored through control experiments, kinetic monitoring, synthesizing the rhodium-hydride intermediates and their reactions with alkynes, deuterium-labeling experiments, and identification of the resting states of the catalyst.
- Mo, Fanyang,Lim, Hee Nam,Dong, Guangbin
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p. 15518 - 15527
(2015/12/26)
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- Isothiazole derivatives as GPR120 agonists for the treatment of type II diabetes
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Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and Q are defined herein.
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Page/Page column 75
(2015/07/07)
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- ISOTHIAZOLE DERIVATIVES AS GPR120 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and Q are defined herein.
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Page/Page column 89
(2015/11/02)
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- GPR120 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, G, and Q are defined herein; and wherein R11, R21, R41, RB1 and G1, are defined herein.
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Paragraph 0809; 0810
(2014/09/30)
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- ANTIBACTERIAL AGENTS
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Antibacterial compounds of formula (I) are provided, as well as stereoisomers and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
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Page/Page column 165-166
(2013/12/03)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
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Page/Page column 96
(2013/03/26)
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- BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE
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The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular
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Page/Page column 59
(2010/10/03)
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- Combined effects on selectivity in Fe-catalyzed methylene oxidation
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Methylene C-H bonds are among the most difficult chemical bonds to selectively functionalize because of their abundance in organic structures and inertness to most chemical reagents. Their selective oxidations in biosynthetic pathways underscore the power of such reactions for streamlining the synthesis of molecules with complex oxygenation patterns. We report that an iron catalyst can achieve methylene C-H bond oxidations in diverse natural-product settings with predictable and high chemo-, site-, and even diastereoselectivities. Electronic, steric, and stereoelectronic factors, which individually promote selectivity with this catalyst, are demonstrated to be powerful control elements when operating in combination in complex molecules. This small-molecule catalyst displays site selectivities complementary to those attained through enzymatic catalysis.
- Chen, Mark S.,White, M. Christina
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scheme or table
p. 533 - 571
(2010/10/05)
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- TETRAHYDROPYRANYL CYCLOPENTYL TETRAHYDROISOQUINOLINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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The present invention is directed to compounds of the formula I: I(wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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Page/Page column 50
(2010/02/07)
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- Cyclopentyl modulators of chemokine receptor activity
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The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6 and X are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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- Indium metal as a reducing agent. Selective reduction of the carbon-carbon double bond in highly activated conjugated alkenes
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(Equation presented) Indium metal in aqueous ethanolic ammonium chloride reduces the C=C bond in highly activated conjugated alkenes such as α,α-dicyano olefins, β-arylenones, and enone esters.
- Ranu, Brindaban C.,Dutta, Jyotirmoy,Guchhait, Sankar K.
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p. 2603 - 2605
(2007/10/03)
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- Process for preparing xanthine derivatives, in particular 1,3-dipropyl-8-(3-oxocyclopentyl)-xanthine
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This invention relates to a process for preparing xanthine derivatives of formula I: STR1 characterized in that a uracil derivative of formula A or B STR2 is dissolved in a suitable organic-aqueous solvent and cyclized in the presence of LiOH.
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- Regioselectivity in Photochemical Chlorocarbonylation of Carbonyl Compounds
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Photochemical chlorocarbonylation of a series of cyclic and acyclic carbonyl compounds shows remarkable regioselectivity and gives β- or γ-substituted products in reasonable yields.Irradiation of cyclopentanone in oxalyl chloride followed by esterification with methanol gave methyl 3-oxocyclopentanecarboxylate (4).Similarly, photochemical chlorocarbonylation of cyclobutanone yielded methyl 3-oxocyclobutanecarboxylate (6).Application of the chlorpcarbonylation reaction to 3-pentanone gave methyl 4-oxohexanoate (8) and dimethyl 4-oxopimelate (9).When a mixture of 3-methylbutanoic acid and oxalyl chloride was irradiated, dimethyl 3-methylglutarate (11) was obtained after methanolysis.A kinetically-controlled mechanism for the photochemical process was deduced.
- Bashir-Hashemi, A.,Hardee, J. R.
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p. 2132 - 2134
(2007/10/02)
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- 3-(indian-5-yloxy (or thio)) cyclopentanecarboxylic acid analogues
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The present invention relates to novel compounds of the general formula: STR1 wherein X represent an oxygen atom or a sulfur atom and R represents a hydrogen atom or an alkyl group of 1-4 carbon atoms, and non-toxic salts thereof when R represents a hydro
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- Antibacterial agents, and 4-thio azetidinone intermediates
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This invention relates to 2-substituted and 2,6-disubstituted penem compounds of the formula STR1 wherein Y is hydrogen, halo or certain organic substituents and X represents certain organic substituents. Also included in the invention are pharmaceutically acceptable salts of the above compounds and derivatives of the above compounds in which the carboxyl group at the 3-position is protected as by an easily removable ester protecting group. The compounds of the present invention are potent antibacterial agents or are of use as intermediates in the preparation of such agents.
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