- GLP-1R AGONISTS AND USES THEREOF
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Provided are compounds of Formula (I) and pharmaceutical compositions thereof, for use in, e.g. treating type 2 diabetes mellitus, pre-diabetes, obesity, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and cardiovascular disease.
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Page/Page column 64; 77
(2020/06/10)
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- Preparation method for 4-chloro-2-fluoro-phenylpropionic acid
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The invention relates to the technical field of chemical synthesis, in particular to a preparation method for 4-chloro-2-fluoro-phenylpropionic acid. The preparation method is characterized in that cheap and easily-available 4-chloro-2-fluorotoluene is ta
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Paragraph 0047; 0048
(2017/07/07)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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- HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
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Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metab
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Page/Page column 130
(2010/12/29)
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- Method for preparing substituted benzyl bromides
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PCT No. PCT/EP98/04485 Sec. 371 Date Jan. 11, 2000 Sec. 102(e) Date Jan. 11, 2000 PCT Filed Jul. 20, 1998 PCT Pub. No. WO99/06339 PCT Pub. Date Feb. 11, 1999Substituted benzyl bromides of the formula I where at least one substituent R1-5 is an electron-at
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- Enantioselective syntheses of no-carrier-added (n.c.a.) (S)-4-chloro-2-[18F] fluorophenylalanine and (S) - (α-methyl) -4-chloro-2-[18F]fluorophenylalanine
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(S)-4-Chloro-2-fluorophenylalanine and (S)-(α-methyl)-4-chloro-2-fluorophenylalanine were synthesized and labeled with no carrier added (n.c.a.) fluorine-18 through a radiochemical synthesis relying on the highly enantioselective reaction between 4-chloro-2-[18F]fluorobenzyl iodide and the lithium enolate of (2S)-1-(tert-butyloxycarbonyl)-2-(tert-butyl)-3-methyl-1,3-imidazolidine-4-one for (S)-4-chloro-2-[18F]fluorophenylalanine and (2S,5S)-1-(tert-butyloxycarbonyl)-2-(tert-butyl)-3,5-dimethyl-1,3-imidazolidine-4-one for (S) - (α-methyl)-4-chloro-2-[18F] fluorophenylalanine. Quantities of about 20-25 mCi were obtained at the end of synthesis, ready for injection after hydrolysis and high performance liquid chromatography (HPLC) purification, with a radiochemical yield of 17%-20% corrected to the end of bombardment after a total synthesis time of 90-105 min from [18F]fluoride. The enantiomeric excesses were shown to be 97% or more for both molecules without chiral separation and the radiochemical and chemical purities were 98% or better.
- Al-Darwich,Plenevaux,Lemaire,Fiore,Christiaens,Comar,Luxen
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p. 117 - 124
(2007/10/03)
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- The Synthesis and Liquid-Crystal Transition Temperatures of Some Fluoro-Substituted Benzonitriles
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Various laterally fluoro-substituted benzonitriles have been prepared containing a trans-4-(n-alkyl)cyclohexane ring linked to the 4-position of the benzonitriles either through a methyleneoxy (-CH2O-) or an ethylene (-CH2CH2-) bridge.The bridging group links the benzonitrile and cyclohexane rings either directly or through an additional 1,4-bonded cyclohexane or benzene ring.The synthesis and liquid-crystal transition temperatures of these new compounds are described.In several cases the nematic-isotropic transition temperatures of F-substituted benzonitriles are found to be higher than those of the non-laterally substituted analogues.
- Kelly, Stephen M.,Schad, Hanspeter
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p. 1444 - 1452
(2007/10/02)
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