- Chemo-enzymatic synthesis of novel β-hydroxy-β-methylbutryric acid (HMB)-medium chain triacylglycerol (MCT) complexes
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β-Hydroxy-β-methylbutyrate (HMB) is reported to have ergogenic benefits such as reducing muscle wasting, promoting exercise performance and skeletal muscle hypertrophy. When used as a dietary feed, it has been found to improve colostral milk fat and the growth of piglets. Medium chain triacylglycerols (MCT) are a good energy source as they can be subjected to β-oxidation in the liver without being stored as fats. When used as animal feed, HMB-MCT complexes are reported to stimulate growth and produce leaner meat product. A high yield two-steps chemo-enzymatic pathway for synthesis of HMB-MCT complexes has been developed. Ethyl HMB ester was first synthesized using a chemical catalyst. Following that, it was transesterified with MCT by using a biocatalyst. Approximately 85 wt% of HMB-MCT complexes can be achieved using this two-step synthetic pathway. The reaction mechanism and some of the reaction parameters were also briefly elucidated.
- Cheong, Ling-Zhi,Widzisz, Katarzyna,Wang, Yingyao,Jensen, Henrik Helligso,Theil, Peter Kappel,Guo, Zheng,Xu, Xuebing
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- Synthesis of 4-alkoxycarbonyl-butenolides by uncatalyzed one-pot cyclization of 1,3-bis(silyloxy)alk-1-enes with oxalyl chloride
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3-Hydroxy-4-alkoxycarbonyl-butenolides were prepared by one-pot cyclizations of 1,3-bis(silyloxy)alk-1-enes with oxalyl chloride.
- Dede, Rüdiger,Michaelis, Lars,Fuentes, Dilver,Yawer, Mirza Arfan,Hussain, Ibrar,Fischer, Christine,Langer, Peter
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- SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
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The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
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Paragraph 000618
(2019/06/05)
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- Substituted heteroaryl compounds and compositions and uses thereof (by machine translation)
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The invention discloses substituted heteroaryl compounds and compositions thereof and their use. The compounds of formula (I) compound or type shown in (I) a compound represented by stereo isomers, tautomers, nitrogen oxide, solvate, metabolite, pharmaceutically acceptable salt or its prodrug. The invention also provides a pharmaceutical composition, the compounds and pharmaceutical compositions can be regulated protein kinase, particularly Aurora kinase and JAK kinase activity, for the prevention, treatment, treatment and reduce protein kinase, in particular JAK kinase activity mediated diseases or disorders. (by machine translation)
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Paragraph 1692; 1703; 1704; 1705
(2019/06/07)
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- THIAZOLYL AND OXAZOLYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS
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Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
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Paragraph 00443
(2014/06/11)
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- N-(MONOCYCLIC ARYL),N'-PYRAZOLYL-UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS
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Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
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Paragraph 00627
(2014/06/11)
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- BICYCLIC HETEROARYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS
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Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
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Paragraph 00558
(2014/06/11)
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- N-BICYCLIC ARYL,N'-PYRAZOLYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS
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Compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
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Paragraph 00555
(2014/06/11)
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- N-(ARYLALKYL)-N'-PYRAZOLYL-UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS
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Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C, X, Ra, Rb, Rc, Rd and n are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
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Paragraph 00756
(2014/06/11)
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- BICYCLIC UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF PAIN
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Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
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Paragraph 00696
(2014/06/11)
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- Base-initiated Reformatsky Condensations in the Gas Phase
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The ester enolate anion CH2=C(OEt)O- reacts with acetaldehyde and with acetone in the gas phase to produce "stable" adducts that are amenable to study by collisional activation and tandem mass spectrometry (MS/MS).The activated adducts and deprotonated β-hydroxy ethyl ester reference ions both decompose by elimination of H2O, Et*, H2O followed by EtOH, and by a retro reaction to reform CH2=C(OEt)O-.The losses of H2O, Et*, and EtOH are assigned to be characteristic of a species of tetrahedral geometry.These losses are, however, attenuated for the ion-molecule adducts because, in addition to existing as tetrahedral complexes, they are also formed as ion-dipole and proton-bound species.
- Castle, Lyle W.,Hayes, Roger N.,Gross, Michael L.
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p. 267 - 271
(2007/10/02)
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- REFORMATSKY REACTION USING Zn/Ag COUPLE
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The Reformatsky reaction is easy to run in ethereal solvents in the presence of Zn/Ag couple.From methyl γ-bromocrotonate and krtones, remified esters are fromed in refluxing Et2O, linear ones in refluxing THF.
- Bortolussi, Michel,Seyden-Penne, Jacqueline
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p. 2355 - 2362
(2007/10/02)
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