- A N - 2 - pyridine -5 - pyrimidine preparation of method (by machine translation)
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The invention belongs to the technical field of agricultural chemical intermediates, in particular to a N - 2 - pyridine - 5 - pyrimidine preparation of method. The preparation method is to cheap and easily obtained 3 - ethoxy - 2 - methyl acrolein as the starting material, with 25% ammonia reaction, to obtain 3 - amino - 2 - methyl acrolein; then with the formamide cyclized, to obtain 5 - methyl pyrimidine; in a carbon tetrachloride solution N - bromo succinimide bromide to obtain 5 - bromo methyl pyrimidine; then under the action of the triethylamine, with 2 - aminopyridine reaction to obtain N - 2 - pyridine - 5 - pyrimidine methylamine. The invention realized through designing a brand new N - 2 - pyridine - 5 pyrimidine methylamine preparation process route, in order to 3 - ethoxy - 2 - methyl acrolein as the starting material, through the ammoniation, cyclization, to obtain the bromide 5 - bromo methyl pyrimidine, then with 2 - aminopyridine reaction to obtain the target product; this invention adopts the cheap and easy to obtain 3 - ethoxy acrolein, in conventional process compared with the use of expensive 5 - pyrimidine formaldehyde, and greatly reduces the production cost. (by machine translation)
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Paragraph 0033; 0040; 0046
(2018/09/11)
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- A N - 2 - pyridyl -5 - pyrimidine preparation of method (by machine translation)
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The invention relates to a pesticide in the technical field, and discloses a N - 2 - pyridyl - 5 - pyrimidine preparation of method, comprises the following steps: the 3 - ethoxy - 2 - methyl acrolein with ammonia ammoniation reaction to produce 3 - amino - 2 - methacrolein, the quality of the ammonia concentration is 20 - 25%, the 3 - ethoxy - 2 - methyl acrolein and ammonia in a molar ratio of 1: 1.0 - 1.5: 1.0 - 6.0. The N - 2 - pyridyl - 5 - pyrimidine preparation of method, by 3 - ethoxy - 2 - methyl acrolein as the starting material, through the ammoniation, cyclizes and brominated to obtain 5 - bromo methyl pyrimidine, then with 2 - aminopyridine reaction to obtain the target product, this invention adopts the cheap and easy to obtain 3 - ethoxy acrolein, in conventional process compared with the use of expensive 5 - pyrimidine formaldehyde, and greatly reduces the production cost, at the same time the invention the preparation method has the advantage of high yield, low cost, high efficiency in the production of more, in low-cost cases can prepare more N - 2 - pyridyl - 5 - pyrimidine methylamine, high practicability. (by machine translation)
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Paragraph 0016; 0019; 0021; 0024; 0026; 0029
(2019/01/08)
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- BIARYL PYRAZOLES AS NRF2 REGULATORS
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The present invention relates to biaryl pyrazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
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Page/Page column 547
(2017/08/01)
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- SUBSTITUTED 3-PHENYLPROPYLAMINE DERIVATIVES FOR THE TREATMENT OF OPHTHALMIC DISEASES AND DISORDERS
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The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
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Paragraph 0495
(2014/09/29)
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- Novel HIV reverse transcriptase inhibitors
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The invention is related to compounds of Formula (I), (II), or (III): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
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Page/Page column 106
(2008/06/13)
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- Substituted bis-amide metalloprotease inhibitors
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This invention relates to substituted bis-amide pyrimidine compounds of Formula (I), which are useful for the treatment of metalloprotease mediated diseases, in particular MMP-13 related diseases.
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Page/Page column 60
(2010/11/27)
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- Compounds useful in therapy
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Compounds of formula (I), [image] or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6-alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6 alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
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Page/Page column 25
(2008/06/13)
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- Substituted triazolo-pyridazine derivatives as ligands for GABA receptors
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Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the α2 and/or α3 subunits.
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- PHARMACOLOGICALLY ACTIVE GUANIDINE COMPOUNDS
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The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-guanidines which are inhibitors of histamine activity.
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- PHARMACOLOGICALLY ACTIVE THIOUREA AND UREA COMPOUNDS
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The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
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