5975-12-2

Usage

Uses

Used in Pharmaceutical Industry:
2,4-Dichloro-3-nitropyridine is used as a reactant in the discovery and synthesis of Imigliptin, a novel selective dipeptidyl peptidase IV (DPP-4) inhibitor. Imigliptin is an important drug used in the treatment of type 2 diabetes, as it helps regulate blood sugar levels by inhibiting the DPP-4 enzyme, which is responsible for the rapid degradation of insulinotropic hormones.
The application of 2,4-Dichloro-3-nitropyridine in the pharmaceutical industry is primarily due to its ability to serve as a key intermediate in the development of new drugs, specifically those targeting type 2 diabetes. Its unique chemical structure allows for further modification and functionalization, making it a valuable component in the synthesis of therapeutic agents.

InChI:InChI=1/C5H2Cl2N2O2/c6-3-1-2-8-5(7)4(3)9(10)11/h1-2H

Upstream product

• 89282-12-2 2,4-dihydroxy-3-nitropyridine 
• 6975-44-6 4,6-dihydroxynicotinic acid ethyl ester 
• 685542-71-6 MB₂₁₈₃₃ 
• 6317-97-1 ethyl 2,4-dihydroxy-3-nitropyridine-5-carboxylate 
• 89282-12-2 4-hydroxy-3-nitro-2(1H)-pyridone 
• 165547-79-5 2-hydroxy-3-nitro-4-chloropyridine 
• 5466-62-6 4,6-dihydroxy-nicotinic acid 
• 626-03-9 3-deazauracil 

Downstream Products

• 173772-63-9 2,4-dichloropyridin-3-ylamine 
• 24501-21-1 2,4-diamino-3-nitropyridine 
• 600553-60-4 2-chloro-3-nitro-4-[2-(1-triphenylmethyl-4-piperidyl)ethyl]aminopyridine 
• 629655-23-8 2-chloro-3-nitro-4-hydroxypyridine 
• 881844-09-3 2-chloro-N-(4-methoxybenzyl)-3-nitropyridin-4-amine 
• 600553-76-2 4-chloro-1-[2-(1-triphenylmethyl-4-piperidyl)ethyl]-1H-imidazo[4,5-c]pyridine 
• 600553-70-6 3-amino-2-chloro-4-[2-(1-triphenylmethyl-4-piperidyl)ethyl]aminopyridine 
• 87871-09-8 erythro-9-(2-hydroxy-3-nonyl)-3-deazaadenine 
• 52559-11-2 2,3,4-pyridinetriamine 
• 2789-25-5 2-chloro-3-nitropyridin-4-amine 
• 871836-48-5 N-benzyl-4-chloro-3-nitropyridin-2-amine 
• 60186-14-3 2,4-difluoro-3-nitropyridine 
• 1047619-53-3 2,4-dibenzylamino-3-nitro-pyridine 
• 165547-79-5 2-hydroxy-3-nitro-4-chloropyridine 

Relevant academic research and scientific papers

IMIDAZOPYRIDINE DERIVATIVE COMPOUNDS AND USE OF SAME

One aspect of the present invention provides a compound selected from among a compound of chemical formula 1 having lysine-specific demethylase-1 (LSD1) inhibitory activity, and a tautomer, a stereoisomer, and a solvate thereof, and pharmaceutically accep

Substituted benzimidazoles as modulators of Ras signaling

Benzimidazole compounds that increase the rate of SOS-mediated nucleotide exchange on Ras by binding to a functionally relevant, chemically tractable pocket on the SOS protein, as part of the Ras:SOS:Ras complex.

1-SUBSTITUTED 1,2,3,4-TETRAHYDRO-1,7-NAPHTHYRIDIN-8-AMINE DERIVATIVES AND THEIR USE AS EP4 RECEPTOR ANTAGONISTS

The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof has an EP4 receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of EP4 receptor associated diseases (e.g., rheumatoid arthritis, aortic aneurysm (e.g. abdominal aortic aneurysm, thoracic aortic aneurysm, thoracoabdominal aortic aneurysm etc.), endometriosis, ankylosing spondylitis, inflammatory breast cancer etc.) and the like.

Dihydropteridin-one derivatives or pharmaceutically acceptable salts thereof, preparation method thereof and pharmaceutical composition for use in preventing or treating PI3 kinase related diseases

The present invention relates to dihydropteridin-one derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same as an effective component for preventing or treating PI3 kinase-related diseases. According to the present invention, the dihydropteridin-one derivatives have excellent selective inhibitory effects on PI3 kinase, and thus may be beneficially used in preventing or treating PI3 kinase-related diseases such as the following: cancers including blood cancer, ovarian cancer, cervical cancer, breast cancer, large intestine cancer, liver cancer, stomach cancer, pancreatic cancer, colon cancer, periotoneal cancer, skin cancer, bladder cancer, prostate cancer, lung cancer, osteosarcoma, fibrous tumor, and brain tumor; autoimmune diseases including rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, type 1 diabetes, hyperthyroidism, myasthenia gravis, Crohnandprime;s disease, ankylosing spondylitis, psoriasis, pernicious anemia, and Sjogrenandprime;s syndrome; and respiratory diseases including chronic obstructive pulmonary disease (COPD), rhinitis, asthma, chronic bronchitis, chronic pulmonary inflammatory diseases, silicosis, pulmonary sarcoidosis, pleuritis, alveolitis, vasculitis, emphysema, pneumonia, and bronchiectasis.COPYRIGHT KIPO 2017

Scaffold morphing leading to evolution of 2,4-diaminoquinolines and aminopyrazolopyrimidines as inhibitors of the ATP synthesis pathway

The success of bedaquiline as an anti-tubercular agent for the treatment of multidrug-resistant tuberculosis has validated the ATP synthesis pathway and in particular ATP synthase as an attractive target. However, limitations associated with its use in the clinic and the drug-drug interactions with rifampicin have prompted research efforts towards identifying alternative ATP synthesis inhibitors with differentiated mechanisms of action. A biochemical assay was employed to screen AstraZeneca's corporate compound collection to identify the inhibitors of mycobacterial ATP synthesis. The high-throughput screening resulted in the identification of 2,4-diaminoquinazolines as inhibitors of the ATP synthesis pathway. A structure-activity relationship for the quinazolines was established and the knowledge was utilized to morph the quinazoline core into quinoline and pyrazolopyrimidine to expand the scope of chemical diversity. The morphed scaffolds exhibited a 10-fold improvement in enzyme potency and over 100-fold improvement in selectivity against inhibition of mammalian mitochondrial ATP synthesis. These novel compounds were bactericidal and demonstrated growth retardation of Mycobacterium tuberculosis in the acute mouse model of tuberculosis infection.

ANTI-FIBROTIC PYRIDINONES

This application relates to polycyclic compounds with a pyridinone or pyridinone derivative core including, substituted pyridinones, 5,6- and 6,6- bicyclic heterocycles and substituted pyridine-thiones. This application also discloses methods of preparing these polycyclic compounds, pharmaceutical compositions and medicaments comprising said compounds and methods to treat, prevent or diagnose diseases, disorders or conditions associated with fibrosis.

ANTI-FIBROTIC PYRIDINONES

Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.

Process Development and Multikilogram-Scale Synthesis of a TRPV1 Antagonist

The process development and multikilogram preparation of a TRPV1 antagonist, 1, is described. Pyrido[2,3-b]pyrazine 1 was prepared in a convergent manner by the coupling of two key fragments, glyoxal 2 and diamine 3. Glyoxal 2 was synthesized in six chemical steps in 20% overall yield, the key step being a challenging Grignard reaction to install the glyoxalate moiety. Diamine 3 was also prepared in six chemical steps in 46% overall yield, exploiting a regioselective nucleophilic aromatic substitution to obtain the key nitrodiamine intermediate 19.

Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin- 3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists

Pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones were evaluated as corticotropin-releasing factor-1 receptor antagonists. The synthesis, SAR studies and pharmacokinetic evaluation of these analogs are described herein.

INHIBITORS OF IAP

The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I), and G, X1, X2, R1, R2, R3, R4/sub