30843-10-8

Upstream product

• 4341-76-8 Ethyl 2-butynoate 
• 6295-87-0 N-aminopyridin-1-ium iodide 
• 141-97-9 ethyl acetoacetate 
• 110-86-1 pyridine 

Downstream Products

• 80537-08-2 2-methylpyrazolo<1,5-a>pyridine-3-carboxylic acid 
• 1542710-61-1 N-benzyl-2-{2-methylpyrazolo[1,5-a]pyridin-3-yl}-5,6,7,8-tetrahydroquinazolin-4-amine 
• 80537-06-0 2-Methyl-pyrazolo[1,5-a]pyridine-3-carboxylic acid [2-(2-hydroxy-ethyl)-phenyl]-amide 
• 1312891-94-3 (E)-3-[4-({isopropyl-[2-(2-methylpyrazolo[1,5-a]pyridin-3-yl)ethyl]amino}methyl)phenyl]acrylic acid methyl ester 
• 1312891-54-5 (E)-N-hydroxy-3-(4-{[2-(2-methylpyrazolo[1,5-a]pyridin-3-yl)ethylamino]methyl}phenyl)acrylamide 
• 1312891-91-0 (E)-3-(4-{[2-(2-methylpyrazolo[1,5-a]pyridin-3-yl)ethylamino]methyl}phenyl)acrylic acid methyl ester 

Relevant academic research and scientific papers

ANTIBACTERIAL COMPOUNDS

The present invention relates to the following compounds, wherein the integers are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of tuberculosis.

Pyrazolo[1, 5-a]pyridine compound and use thereof

The invention discloses a pyrazolo[1, 5-a]pyridine compound with the structure characteristic shown in the formula (I) or its pharmaceutically acceptable salt, stereoisomer or prodrug molecule and a use thereof. The compound has good in-vitro anti-tubercle bacillus activity, has the minimal inhibitory concentration (MIC) less than 0.1 micrograms per milliliter and partial MIC of 0.01 micrograms per milliliter and has strong inhibition effects on a clinically sorted multi-drug-resistant tuberculosis (MDR-TB) strain. In an in-vivo experiment, at a dosage of 20mg/kg/d, the pyrazolo[1, 5-a]pyridine compound can effectively eliminate H37Ra infection in a mouse and is a novel anti-tuberculosis compound.

9H-PYRIMIDO[4,5-B]INDOLES AND RELATED ANALOGS AS BET BROMODOMAIN INHIBITORS

The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.

Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents

A series of pyrazolo[1,5-a]pyridine-3-carboxamide derivatives were designed and synthesized as new anti-Mycobacterium tuberculosis (Mtb) agents. The compounds exhibit promising in vitro potency with nanomolar MIC values against the drug susceptive H37Rv s

Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors

Histone deacetylase (HDAC) inhibitors have shown promise in treating various forms of cancer. However, many HDAC inhibitors from diverse structural classes have been associated with QT prolongation in humans. Inhibition of the human ether a-go-go related gene (hERG) channel has been associated with QT prolongation and fatal arrhythmias. To determine if the observed cardiac effects of HDAC inhibitors in humans is due to hERG blockade, a highly potent HDAC inhibitor devoid of hERG activity was required. Starting with dacinostat (LAQ824), a highly potent HDAC inhibitor, we explored the SAR to determine the pharmacophores required for HDAC and hERG inhibition. We disclose here the results of these efforts where a high degree of pharmacophore homology between these two targets was discovered. This similarity prevented traditional strategies for mitigating hERG binding/modulation from being successful and novel approaches for reducing hERG inhibition were required. Using a hERG homology model, two compounds, 11r and 25i, were discovered to be highly efficacious with weak affinity for the hERG and other ion channels.

HETEROARYLS AND THEIR USE AS PI3K INHIBITORS

This invention provides compounds of formula (IA) or (IB): wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

Pyrazolo[1,5-a]pyridine-3-carboxylic acid derivatives and their pharmaceutical use

Described herein are pyrazolo[1,5-a]pyridine-3-carboxylic acid derivatives represented by the following formula (I): STR1 wherein R 1 and R 2 individually mean a hydrogen atom or a lower alkyl group, R 3 denotes an azabicyclo group containing a tertiary nitrogen atom, and Y stands for --O-- or --NH--, or salts thereof. Their preparation process and serotonin receptor antagonists containing them as active ingredients are also described.

1,3-Dipolar Addition of Pyridine N-Imine to Acetylenes and the Use of C-13 NMR in Several Structural Assignments

Addition of pyridine-N-imine to a variety of acetylenic mono- (Scheme I) and di- (Scheme II) carboxylic ester dipolarophiles was carried out.Several of the 3-azapyrrocoline esters obtained were further converted into acids, amides and hydrazides as shown in Schemes I and II.