1151512-25-2

Upstream product

• 70201-42-2 3,5-dibromopyridine-4-carboxaldehyde 
• 2365-48-2 Methyl thioglycolate 
• 625-92-3 3,5-dibromopyridine 
• 1809004-78-1 ethyl 4-bromothieno[2,3-c]pyridine-2-carboxylate 
• 145325-40-2 4-bromo-thieno<2,3-c>pyridine-2-carboxylic acid methyl ester 

Downstream Products

• 1296224-08-2 4-bromothieno[2,3-c]pyridine 

Relevant academic research and scientific papers

Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors

Bicyclic heteroaromatic motifs with hydrogen bond donor–acceptor hinge binder motifs are frequently used as ATP-mimetic kinase inhibitors. Althought the thieno[2,3-c]pyridine scaffold also meets these criteria its use was limited so far by the availability of synthetic building blocks. Inspired by two X-ray structures of kinase bound thieno[2,3-c]pyridines we prepared a diverse collection of simple thieno[2,3-c]pyridine derivatives that could serve as starting points for future drug discovery programs. In our search for inhibitors of the GRK2 kinase we also identified a hit compound bearing the thieno[2,3-c]pyridine moiety. Following a structure-driven optimization process a collection of potent and highly ligand efficient inhibitors were prepared and characterized, which could form the basis of a future drug discovery program. Graphical abstract: [Figure not available: see fulltext.]

Five-membered heterocyclic oxo carboxylic acid compound and medical application thereof

The invention relates to a five-membered heterocyclic oxo carboxylic acid compound and a medical application thereof. Specifically, the invention relates to a compound, a pharmaceutical salt, a prodrug, a hydrate, a solvate or a crystal form as shown in a formula (I), and also relates to a preparation method of the compound, a pharmaceutical composition containing the compound and an application of the pharmaceutical composition as a secretion regulator of interferon type I, especially as an STING agonist in preparation of medicines for preventing and/or treating I-type interferon related diseases.

AMPK INHIBITORS

The 5'-AMP-activated protein kinase AMPK functions as a master switch to maintain cellular and whole-body energy homeostasis and abnormal activity profiles of AMPK may cause pathological disorders. The present invention relates to a series of compounds (I

PYRAZOLE DERIVATIVES AS MALT1 INHIBITORS

Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, R6, R5, G1, and G2 are defined herein.

CONDENSED RING DERIVATIVE, AND PREPARATION METHOD, INTERMEDIATE, PHARMACEUTICAL COMPOSITION AND USE THEREOF

Disclosed are a condensed ring derivative, and a preparation method, an intermediate, a pharmaceutical composition and a use thereof. The condensed ring derivative of the present invention has a significant inhibitive effect on URAT1, which can effectively alleviate or treat hyperuricemia and other related diseases.

2-METHYL-QUINAZOLINES

The present invention describes 2-methyl-quinazoline compounds of general formula (I), methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions. The 2-methyl substituted quinazoline compounds of general formula(I) effectively and selectively inhibit the Ras-Sos interaction without significantly targeting the EGFR receptor. They are therefore useful for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, such as cancer as a sole agent or in combination with other active ingredients.

HETEROCYCLIC COMPOUNDS, PROCESS FOR PREPARATION OF THE SAME AND USE THEREOF

The present invention provides a heterocyclic compound represented by the formula (I), its stereoisomers, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and their use in preparing a medicament for the prevention and/or treatment of central nervous system disease.

1,2,4-TRIAZINE-6-CARBOXAMIDE DERIVATIVE

The present invention provides a compound represented by the following general formula (I) or a salt thereof which has a Syk inhibitory effect (in the formula R1 represents a hydrogen atom or an optionally Ra-substituted C1-C6 alkyl group; A represents a hydrogen atom, an optionally Ra-substituted C1-C8 alkyl group, an optionally Ra-substituted C2-C6 alkenyl group, an optionally Ra-substituted C2-C6 alkynyl group, an optionally Rb-substituted C3-C10 cycloalkyl group, an optionally Rb-substituted C6-C14 aromatic hydrocarbon group, an optionally Rb-substituted 4- to 10-membered unsaturated heterocyclic group, or an optionally Rb-substituted 4-to 10-membered saturated heterocyclic group, or optionally forms a 4- to 10-membered unsaturated heterocyclic ring or a 4- to 10-membered saturated heterocyclic ring together with R1 and the nitrogen atom bonded thereto; R2 represents a hydrogen atom or an optionally Ra-substituted C1-C6 alkyl group; and B represents an optionally Rc-substituted unsaturated heterocyclic group).