59514-86-2Relevant academic research and scientific papers
INHIBITORS OF LOW MOLECULAR WEIGHT PROTEIN TYROSINE PHOSPHATASE (LMPTP) AND USES THEREOF
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Paragraph 00305, (2018/11/26)
Protein tyrosine phosphatases (PTPs) are key regulators of metabolism and insulin signaling. As a negative regulator of insulin signaling, the low molecular weight protein tyrosine phosphatase (LMPTP) is a target for insulin resistance and related conditions. Described herein are compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and compositions, and methods of using these compounds and compositions.
Method for preparing 4-bromo-1,8-naphthyridine
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Paragraph 0020; 0021, (2017/10/11)
The invention discloses a method for preparing 4-bromo-1,8-naphthyridine. The method comprises the following steps: taking 2-aminopyridine as an initial raw material, and performing cyclization, bromination and reduction to obtain the 4-bromo-1,8-naphthyridine. The compound is an important intermediate compound for research and development of new drugs.
4-Aminoquinolone piperidine amides: Noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity
Naik, Maruti,Humnabadkar, Vaishali,Tantry, Subramanyam J.,Panda, Manoranjan,Narayan, Ashwini,Guptha, Supreeth,Panduga, Vijender,Manjrekar, Praveena,Jena, Lalit Kumar,Koushik, Krishna,Shanbhag, Gajanan,Jatheendranath, Sandesh,Manjunatha,Gorai, Gopinath,Bathula, Chandramohan,Rudrapatna, Suresh,Achar, Vijayashree,Sharma, Sreevalli,Ambady, Anisha,Hegde, Naina,Mahadevaswamy, Jyothi,Kaur, Parvinder,Sambandamurthy, Vasan K.,Awasthy, Disha,Narayan, Chandan,Ravishankar, Sudha,Madhavapeddi, Prashanti,Reddy, Jitendar,Prabhakar,Saralaya, Ramanatha,Chatterji, Monalisa,Whiteaker, James,McLaughlin, Bob,Chiarelli, Laurent R.,Riccardi, Giovanna,Pasca, Maria Rosalia,Binda, Claudia,Neres, Jo?o,Dhar, Neeraj,Signorino-Gelo, Fran?ois,McKinney, John D.,Ramachandran, Vasanthi,Shandil, Radha,Tommasi, Ruben,Iyer, Pravin S.,Narayanan, Shridhar,Hosagrahara, Vinayak,Kavanagh, Stefan,Dinesh, Neela,Ghorpade, Sandeep R.
, p. 5419 - 5434 (2014/07/08)
4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaffold starting from a whole cell screen, with potent cidality on Mycobacterium tuberculosis (Mtb). Evaluation of the minimum inhibitory concentrations, followed by whole genome sequencing of mutants raised against AQs, identified decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1) as the primary target responsible for the antitubercular activity. Mass spectrometry and enzyme kinetic studies indicated that AQs are noncovalent, reversible inhibitors of DprE1 with slow on rates and long residence times of ~100 min on the enzyme. In general, AQs have excellent leadlike properties and good in vitro secondary pharmacology profile. Although the scaffold started off as a single active compound with moderate potency from the whole cell screen, structure-activity relationship optimization of the scaffold led to compounds with potent DprE1 inhibition (IC50 10 nM) along with potent cellular activity (MIC = 60 nM) against Mtb.
2,4-DIARYL - SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER
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Paragraph 0271; 0276; 0277, (2013/05/08)
The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particu
2,4- DIARYL-SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER
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Page/Page column 74, (2012/01/14)
The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases playsa role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors
Microwave assisted synthesis of some 2, 4 dihydroxy 1, 8-naphthyridines and their derivatives devoid of solvent and catalyst
Maringanti, Thirumala Chary,Eppakayala, Laxminarayana,Sripelly, Shiva Shankar,Atmakuri, Narender
experimental part, p. 35 - 41 (2010/03/01)
Reaction of substituted 2-aminopyridines with diethylmalonates yields 2, 4- dihydroxy-l, 8-Naphthyridenes(l-18). The 6-chloro-2, 4-dihydroxy-l, 8- naphthyridene (5) when treated with different reagents varied substituted derivatives are produced. 6- chloro-2, 4-dihydroxy-l, 8-naphthyridene(5) when treated with sodium azide offered 2, 4-dihydroxy-1, 8-naphthyridene-6-thiones (19-21). 6-azido-1, 8-naphthyridine-2, 4- diols(22-24) were obtained by reacting 5 with sodiumazide. The 6-hydrazinyl-l, 8-naphthyridine-2, 4-diols (25-27) and 2, 4, 6-trihydroxy-l, 8-naphthyridenes (28-30) were produced by the reaction of 5 with hydrazine hydrate and acetic acid respectively.
Substituted pyridopyrimidinones, 1: Convenient PTC alkylation and halogenation of 2-hydroxy-4H-pyrido[1,2-a]pyrimidin-4-one
Abass, Mohamed,Mayas, Aisha S.
, p. 19 - 27 (2007/10/03)
Alkylation of 2-hydroxy-4H-pyrido[1,2-a]-pyrimidin-4-one (1) was investigated under solid-liquid phase transfer catalysis conditions (PTC), using tetrabutylammonium bromide and potassium carbonate. The reaction with alkyl halides led to the formation of various 2-alkoxy products, in fair yields. Reaction of compound 1 with epichlorohydrin and chloroacetonitrile, under the same PTC conditions, afforded novel O1,O3-disubstituted glycerol and oxazolopyridopyrimidone betaine derivatives, respectively. Some 3-halo-, 3,3-dihalo, and/or 2,3-dihalopyrido[1,2-a]pyrimidines were also prepared using different halogenating agents at different reaction conditions.
NAPHTHYRIDINE DERIVATIVE
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Page 9, (2008/06/13)
The present invention provides a novel naphthyridine derivative that is effective for relieving pain, less toxic, and also is effective for treating diabetic neuropathy, the derivative being represented by the general formula (1) : wherein R1,
