- MACROCYCLIC AZOLOPYRIDINE DERIVATIVES AS EED AND PRC2 MODULATORS
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The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula (I), or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X1, X2, X3, A1, A2, Y, R1, R2, R3, and R4 are as described herein.
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Paragraph 1214
(2020/10/09)
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- Synthesis of N,N-Dioxopyridazines
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Despite many efforts, one of the smallest heterocycles containing two nitrogen atoms, pyridazine, could not be converted to its N,N-dioxide (see, however, Nakadate et al. Chem. Pharm. Bull. 1970, 18, 1211-1218). HOF·CH3CN, made easily from diluted fluorine, was able to accomplish this task in a fast reaction with good yields.
- Rozen, Shlomo,Shaffer, Avshalom
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supporting information
p. 4707 - 4709
(2017/09/23)
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- 3-OXO-TETRAHYDRO-FURO[3,2-B]PYRROL-4(5H)-YL) DERIVATIVES II
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The invention relates to amidic oxotetrahydro-2H-furo[3.2-b]pyrrol-4(5H)-yl) derivatives as dual CatS/K inhibitors exhibiting a pronounced CatK-inhibition, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 34; 40
(2015/12/11)
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- 3-OXO-TETRAHYDRO-FURO[3,2-B]PYRROL-4(5H)-YL) DERIVATIVES I
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The invention relates to amidic oxotetrahydro-2H-furo[3.2-b]pyrrol-4(5H)-yl) derivatives as dual CatS/K inhibitors, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 60; 70; 71
(2015/11/16)
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- Thiazole-4-carboxyamide derivatives
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The present invention is concerned with novel thiazole 4-carboxyamide derivatives of the general formula (I) and with methods for the preparation thereof, which compounds are useful as metabotropic glutamate receptor antagonists: wherein R1 to R4 are as defined in the specification.
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Page/Page column 54-55
(2008/06/13)
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- Heteroaryl-substituted imidazole derivatives
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The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3 and R4 are described hereinbelow. These compounds can be used in the treatment or prevention of mGluR5 receptor me
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Page/Page column 13
(2008/06/13)
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- The Mechanisms of the Conversion of Thiophosphoryl Compounds into their Phosphoryl Analogues by Photochemically Excited 3-Methylpyridazine 2-Oxide and by 2-Methyl-3-p-nitrophenyloxaziridine; a Comparison
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Reactions of tri-p-substituted triarylphosphine sulphides with 3-methylpyridazine 2-oxide, under photolysis, and with 2-methyl-3-p-nitrophenyloxaziridine both give the corresponding phosphine oxides.A detailed study and comparison of the two reactions shows that they are mechanistically quite distinct and that it is unlikely that the active oxygenating species generated by photolysis of the N-oxide, which attacks the phosphine sulphides, is an oxaziridine.The evidence presented suggests that this species may in fact be 'oxene'.
- Rowley, Alan G.,Steedman, John R. F.
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p. 1113 - 1120
(2007/10/02)
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