- Application of 1,1-ADEQUATE, HMBC, and Density Functional Theory to Determine Regioselectivity in the Halogenation of Pyridine N-Oxides
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The 1,1-ADEQUATE spectrum clearly shows specific two-bond proton to carbon correlations to unequivocally distinguish the major and minor regioisomers of ortho-halogenated pyridines and to aid in assignment of the corresponding proton and carbon chemical shifts. M06-2X/6-31+G(d,p) free energies of the regioisomeric intermediates arising from deprotonation correctly predict the experimentally observed preference and thus can be used to tune the substituent pattern to yield a desired regiochemical outcome.
- Hwang, Tsang-Lin,Bartberger, Michael D.,Chen, Ying
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p. 1956 - 1959
(2016/06/01)
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- Highly Regioselective Halogenation of Pyridine N -Oxide: Practical Access to 2-Halo-Substituted Pyridines
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A highly efficient and regioselective halogenation reaction of unsymmetrical pyridine N-oxide under mild conditions is described. The methodology provides a practical access to various 2-halo-substituted pyridines, which are pharmaceutically important intermediates.
- Chen, Ying,Huang, Jinkun,Hwang, Tsang-Lin,Chen, Maosheng J.,Tedrow, Jason S.,Farrell, Robert P.,Bio, Matthew M.,Cui, Sheng
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supporting information
p. 2948 - 2951
(2015/06/30)
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- NOVEL ALKYNE COMPOUNDS WITH AN MCH-ANTAGONISTIC ACTION AND MEDICAMENTS COMPRISING SAID COMPOUNDS
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The invention relates to individual alkyne compounds with an antagonistic action against the MCH-receptor. Said compounds are suitable for producing medicaments for the treatment of metabolic disorders and/or eating disorders, in particular adiposity and diabetes.
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Page/Page column 58-59
(2008/06/13)
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- NOVEL ALKYNE COMPOUNDS EXHIBITING AN MCH ANTAGONISTIC EFFECT AND DRUGS CONTAINING SAID COMPOUNDS
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The invention relates to an alkyne compound of general formula (I) in which A, B, W, X, Y, Z, R and R groups and residuals have the meanings given in claim 1. Drugs containing at least one type of inventive alkyne are also disclosed. The inventive drugs exhibiting an MCH-receptor antagonistic activity are suitable for treating metabolic disturbances and/or eating disorders, in particular adiposity, bulimia, anorexia, hyperphagia and diabetes.
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Page/Page column 66-67
(2008/06/13)
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- NOVEL ALKYNE COMPOUNDS WITH AN MCH-ANTAGONISTIC ACTION AND MEDICAMENTS CONTAINING SAID COMPOUNDS
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The invention relates to alkyne compounds of general formula (I), in which the groups and radicals A, B, W, X, Y, Z, R1 and R2 are defined as cited in claim 1. The invention also relates to medicaments containing at least one inventive alkyne. As a result of the antagonistic action against the MCH-receptor, the inventive medicaments are suitable for treating metabolic disorders and/or eating disorders, in particular adiposity and diabetes.
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Page/Page column 98
(2010/02/14)
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- NOVEL ALKYNE COMPOUNDS HAVING AN MCH-ANTAGONISTIC EFFECT, AND MEDICAMENTS CONTAINING SAID COMPOUNDS
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The invention relates to alkyne compounds of general formula (I), wherein the groups and radicals A, B, W, X, Y, Z, R1, and R2 have the meanings indicated in claim 1. The invention further relates to medicaments containing at least one inventive alkyne. The disclosed medicaments are suitable for the treatment of metabolic disorders and/or eating disorders, particularly adiposity and diabetes, as a result of the MCH receptor antagonistic activity thereof.
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Page/Page column 103
(2010/02/14)
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- Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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The present invention relates to alkyne compounds of general formula I wherein the groups and radicals A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one alkyne according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.
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Page/Page column 45
(2010/02/14)
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- Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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Alkyne compounds of formula I wherein A, B, W, X, Y, Z, R1, and R2 have the meanings given herein, which have MCH-receptor antagonistic activity and are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.
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Page/Page column 39
(2010/02/14)
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- Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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Alkyne compounds having MCH-receptor antagonistic activity, which are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.
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Page/Page column 25
(2008/06/13)
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- Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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Alkyne compounds of formula I wherein A, B, W, X, Y, Z, R1, and R2 have the meanings given herein, which have MCH-receptor antagonistic activity and are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.
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Page/Page column 25
(2010/02/14)
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- 3-fluoropyridines, process for their preparation, and their use in liquid-crystal mixtures
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A 3-fluoropyridine of the formula (I) STR1 in which the symbols have the following meanings: R1 and R2, independently of one another, are, for example, H or straight-chain or branched alkyl, A1, A2, A3 and A4 are identical or different and are, for example, 1,4-phenylene, pyrazine-2,5-diyl or trans-1,4-cyclohexylene, M1, M2, M3 and M4 are identical or different and are, for example, --O-- or --CO--O--, R3, R4, R6 and R7, independently of one another are, for example, H or straight-chain or branched alkyl, M5 is for example, --O--CO-- or a single bond, k, l, m, n, o, p, q and r are zero or one, with the proviso that the sum k+m+p+r is less than 4 and greater than zero, can advantageously be employed as a component in ferroelectric liquid-crystal mixtures.
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