80537-08-2

Upstream product

• 110-86-1 pyridine 
• 4341-76-8 Ethyl 2-butynoate 
• 6295-87-0 N-aminopyridin-1-ium iodide 
• 23326-27-4 Methyl 2-butynoate 
• 30843-10-8 2-methyl-pyrazolo[1,5-a]pyridine-3-carboxylic acid ethyl ester 

Downstream Products

• 80537-06-0 2-Methyl-pyrazolo[1,5-a]pyridine-3-carboxylic acid [2-(2-hydroxy-ethyl)-phenyl]-amide 
• 1610966-00-1 5-fluoro-N-(4-methoxyphenyl)-2-(2-methylpyrazolo[1,5-a]pyridin-3-yl)pyrimidine-4,6-diamine 
• 1542710-61-1 N-benzyl-2-{2-methylpyrazolo[1,5-a]pyridin-3-yl}-5,6,7,8-tetrahydroquinazolin-4-amine 

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.

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

SUBSTITUTED PYRIMIDINE BMI-1 INHIBITORS

Amine substituted pyrimidine compounds and forms thereof that inhibit the function and reduce the level of B -cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the

SUBSTITUTED TRIAZINE BMI-1 INHIBITORS

Amine substituted triazine compounds and forms thereof that inhibit the function and reduce the level of B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi- 1 function and reduce the level of Bmi- 1 to treat a cancer mediated by Bmi-1 are described herein.

SUBSTITUTED PYRIDINE AND PYRAZINE BMI-1 INHIBITORS

Amine substituted pyridine and pyrazine compounds and forms thereof that inhibit the function and reduce the level of B -cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.

Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)

The AAA-ATPase p97 plays vital roles in mechanisms of protein homeostasis, including ubiquitin-proteasome system (UPS) mediated protein degradation, endoplasmic reticulum-associated degradation (ERAD), and autophagy. Herein we describe our lead optimization efforts focused on in vitro potency, ADME, and pharmaceutical properties that led to the discovery of a potent, ATP-competitive, D2-selective, and orally bioavailable p97 inhibitor 71, CB-5083. Treatment of tumor cells with 71 leads to significant accumulation of markers associated with inhibition of UPS and ERAD functions, which induces irresolvable proteotoxic stress and cell death. In tumor bearing mice, oral administration of 71 causes rapid accumulation of markers of the unfolded protein response (UPR) and subsequently induces apoptosis leading to sustained antitumor activity in in vivo xenograft models of both solid and hematological tumors. 71 has been taken into phase 1 clinical trials in patients with multiple myeloma and solid tumors.

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.

SUBSTITUTED REVERSE PYRIMIDINE BMI-1 INHIBITORS

Amine substituted reverse pyrimidine compounds and forms thereof that inhibit the function and reduce the level of B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.

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.