32399-13-6Relevant academic research and scientific papers
HYDROPYRAZINO[1,2-D][1,4]DIAZEPINE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
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Page/Page column 20, (2021/05/07)
The present invention relates to compounds of formula (I), wherein R1 to R3 and n are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.
1,8-NAPHTHYRIDIN-2-ONE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
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Page/Page column 19; 20, (2021/06/04)
The present invention relates to compounds of formula (I), wherein R1 to R3, m and n are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
HEXAHYDRO-1H-PYRAZINO[1,2-A]PYRAZINE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
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Page/Page column 55, (2020/10/21)
The present invention relates to compounds of formula (I), wherein R1 to R3, n and A are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.
A preparation method of the midbody shakang zuo
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Paragraph 0033-0038, (2018/05/16)
The invention relates to a preparation method of an isavuconazole intermediate. The isavuconazole intermediate is 2-methylamino-3-pyridylcarbinol. The method comprises the following steps: (1) reacting 2-chloronicotinic acid with methylamine dissolved in a methylamine solution to generate 2-methylamino-3-pyridylformic acid, wherein the methylamine solution is formed by dissolving methylamine in water, methanol or a water-methanol mixture; and (2) reducing the 2-methylamino-3-pyridylformic acid in a solvent in the presence of a reducer sodium borohydride/iodine, sodium borohydride/Lewis acid or red aluminum to obtain the 2-methylamino-3-pyridylcarbinol. The method has the advantages of low cost, high product yield and purity, and mild and controllable conditions, and is suitable for industrial scale-up production.
Design and synthesis of niflumic acid-based N-acylhydrazone derivatives as novel anti-inflammatory and analgesic agents
Kheradmand, Amin,Navidpour, Latifeh,Shafaroodi, Hamed,Saeedi-Motahar, Ghazaleh,Shafiee, Abbas
, p. 2411 - 2420 (2013/07/26)
A new series of niflumic acid-based N-acylhydrazone derivatives 5a-p were synthesized and evaluated for their anti-inflammatory and analgesic activities. Most of the compounds have shown anti-inflammatory activity with a moderate-to-excellent activity range (20-80 % reduction in inflammation). Among them, 3-chlorophenyl 5d and 3-pyridyl derivatives 5o exhibited the most potent anti-inflammatory activity relative to niflumic acid as the reference drug (77, 76, and 70 % reduction in inflammation at 1-h postdrug administration, respectively). Also, molecular simplification of niflumic acid through replacing the N-aryl group with N-methyl group produced compounds 6a-f with anti-inflammatory activity in a quite similar manner to those of their parent derivatives. In this subgroup, 4-pyridyl derivative 6f showed the most potent anti-inflammatory activity relative to niflumic acid (80 % reduction in inflammation at 1-h postdrug administration). The compounds with highest anti-inflammatory activity were subjected to analgesic assays and showed moderate-to-excellent analgesic activities. The compound 5j, 4-methoxy derivative, exhibited the highest analgesic activity relative to niflumic acid (97 and 68 % activity, respectively).
RING-FUSED 2-PYRIDONE DERIVATIVES AND HERBICIDES
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Page/Page column 69, (2011/12/12)
Provided are 2-pyridone derivatives which have excellent herbicidal activity and exhibit high safety to useful crops and so on; salts thereof; and herbicides containing same. In more detail, 2-pyridone derivatives represented by general formula [I] or agrochemically acceptable salts thereof, and herbicides containing these compounds are provided. In general formula [I], X1 is an oxygen atom or a sulfur atom; X2, X3, and X4 are to each CH or N(O)m; m is an integer of 0 or 1; R1 is a hydrogen atom, a C1-12 alkyl group, or the like; R2 is a halogen atom, a cyano group, or the like; n is an integer of 0 to 4; R3 is a hydroxyl group, a halogen atom, or the like; A1 is C(R11R12); A2 is C(R13R14) or C═O; A3 is C(R15R16); and R11, R12, R13, R14, R15, and R16 are each independently a hydrogen atom or a C1-6 alkyl group.
Microwave-assisted synthesis of 2-aminonicotinic acids by reacting 2-chloronicotinic acid with amines
Quevedo, Camilo E.,Bavetsias, Vassilios,McDonald, Edward
experimental part, p. 2481 - 2483 (2009/08/17)
2-(Methylamino)nicotinic acid was readily prepared in high yield by reacting 2-chloronicotinic acid with 40% aq MeNH2 under microwave irradiation either at 120 °C for 2 h or at 140 °C for 1.5 h. Subsequently, we found that a range of 2-aminonicotinic acids could be obtained under microwave heating. The optimal reaction conditions involved the use of 3 equiv of amine, water as the solvent and heating at 200 °C for 2 h in the presence of diisopropylethylamine (3 equiv).
OXYTOCIN INHIBITORS
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Page 95-96, (2010/02/06)
This invention relates to compounds of formula (I).
Substituted 1,3-Dihydro-2H-pyrrolopyridin-2-ones as Potential Antiinflammatory Agents
Ting, Pauline C.,Kaminski, James J.,Sherlock, Margaret H.,Tom, Wing C.,Lee, Joe F.,et al.
, p. 2697 - 2706 (2007/10/02)
A series of analogues based on the 1,3-dihydro-2H-pyrrolopyridin-2-one ring system have been synthesized and shown to possess oral antiinflammatory activity in both the reverse passive Arthus reaction (RPAR) pleural cavity assay in rats and in the adjuvant-induced arthritic rat model (AAR).Several members of this series additionally exhibit an inhibitory effect on the in vivo production of prostaglandin- and leukotriene-derived products or arachidonic acid metabolism although these compounds exhibit no significant inhibitory activity against the cyclooxygenase and 5-lipoxygenase enzymes in vitro.Structure-activity relationships in this series are discussed.
Imination of N-Methylazinium Salts by Liquid Ammonia/Potassium Permanganate
Wozniak, M.,Buurman, D.J.,Plas, H.C. van der
, p. 765 - 769 (2007/10/02)
Treatment of 1-methylquinolinium-, 1,4-dimethylquinolinium- and 1-methyl-1,X-naphthyridinium iodides (X=5,8) with liquid ammonia/potassium permanganate leads to introduction of the imino group at C-2 forming the 1,2-dihydro-2-imino-1-methylquinolines and 1,2-dihydro-2-imino-1-methyl-1,X-naphthyridines (X=5,8) respectively. 1,2-Dimethylquinolinium iodide, when subjected to treatment with liquid ammonia/potassium permanganate undergoes an oxo-demethylation reaction, yielding 1-methylquinol-2-one.The nmr-measurements of solutions of the above-mentioned salts in liquid ammonia clearly show the formation of ?-adduct, strongly suggesting that these ?-adducts are intermediates in the imination reactions.
