19181-77-2

Usage

Uses

Used in Pharmaceutical Development:
8-Quinazolinecarboxylic acid, 3,4-dihydro-4-oxo-, is used as a key intermediate in the synthesis of various pharmaceutical compounds for its potential to exhibit biological activity. Its unique structure allows for the development of drugs targeting specific medical conditions.
Used in Medicinal Chemistry Research:
In the field of medicinal chemistry, 8-Quinazolinecarboxylic acid, 3,4-dihydro-4-oxo-, serves as a valuable research target for understanding its potential pharmacological properties and exploring its use in the creation of novel therapeutic agents.
Used in Drug Discovery:
8-Quinazolinecarboxylic acid, 3,4-dihydro-4-oxois utilized in drug discovery processes to identify new lead compounds with potential therapeutic effects. Its unique chemical structure may offer insights into the design of innovative drugs for treating a range of diseases.
Used in Biochemical Studies:
8-Quinazolinecarboxylic acid, 3,4-dihydro-4-oxo-, is employed in biochemical studies to investigate its interactions with biological systems, which can provide insights into its potential applications in medicine and help elucidate its mechanism of action.
Used in Chemical Synthesis:
8-Quinazolinecarboxylic acid, 3,4-dihydro-4-oxois used as a building block in the synthesis of more complex organic molecules, particularly those with potential applications in the pharmaceutical industry.
Used in Drug Design:
8-Quinazolinecarboxylic acid, 3,4-dihydro-4-oxo-, is used in drug design to create new molecular entities with improved pharmacokinetic and pharmacodynamic profiles, aiming to enhance the efficacy and safety of new medications.
Used in Targeted Drug Delivery Systems:
8-Quinazolinecarboxylic acid, 3,4-dihydro-4-oxomay be incorporated into targeted drug delivery systems to improve the bioavailability and therapeutic efficacy of drugs, particularly for challenging conditions that require precise targeting of specific biological pathways or tissues.
Used in Anticancer Research:
8-Quinazolinecarboxylic acid, 3,4-dihydro-4-oxo-, is used in anticancer research to explore its potential as an anticancer agent, given its structural features that may allow it to interact with specific cancer-related targets and pathways.

Upstream product

• 39622-79-2 2-aminoisophthalic acid 
• 77287-34-4 formamide 
• 1379546-43-6 4-oxo-4H-3,1-benzoxazine-8-carboxylic acid 
• 50-00-0 formaldehyd 
• 3473-63-0 formamidine acetic acid 

Downstream Products

• 1379545-91-1 4-[(S)-2-azetidin-1-yl-1-(3-fluorophenyl)-ethylamino]-quinazoline-8-carboxamide 
• 1240474-61-6 4-((S)-2-dimethylamino-1-phenyl-ethylamino)-quinazoline-8-carboxamide 
• 1240476-05-4 4-((S)-2-cyclopropylamino-1-phenyl-ethylamino)-quinazoline-8-carboxamide 
• 1240477-26-2 4-(3,4,5-trifluoro-benzylamino)-quinazoline-8-carboxamide 
• 1240476-18-9 4-(3,4-difluoro-benzylamino)-quinazoline-8-carboxamide 
• 1240472-53-0 4-(3,5-difluoro-benzylamino)-quinazoline-8-carboxamide 
• 1240473-65-7 4-(2,4-difluoro-benzylamino)-quinazoline-8-carboxamide 

Relevant academic research and scientific papers

QUINAZOLINE DERIVATIVES AS LPA RECEPTOR 2 INHIBITORS

The present invention relates to a compounds of general formula (I) inhibiting lysophosphatidic acid receptor 2 (LPA2), particularly the invention relates to compounds that are quinazoline derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful in the treatment of diseases or conditions associated with a dysregulation of LPA receptors, in particular fibrosis.

Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers

Herein, we report the discovery of a novel class of quinazoline carboxamides as dual p70S6k/Akt inhibitors for the treatment of tumors driven by alterations to the PI3K/Akt/mTOR (PAM) pathway. Through the screening of in-house proprietary kinase library, 4-benzylamino-quinazoline-8-carboxylic acid amide 1 stood out, with sub-micromolar p70S6k biochemical activity, as the starting point for a structurally enabled p70S6K/Akt dual inhibitor program that led to the discovery of M2698, a dual p70S6k/Akt inhibitor. M2698 is kinase selective, possesses favorable physical, chemical, and DMPK profiles, is orally available and well tolerated, and displayed tumor control in multiple in vivo studies of PAM pathway-driven tumors.

QUINAZOLINE CARBOXAMIDE AZETIDINES

The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer.

Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties

Recent clinical data provided proof-of-concept for selective B-Raf inhibitors in treatment of B-RafV600E mutant melanoma. Pyrazolopyridine-type B-Raf inhibitors previously described by the authors are potent and selective but exhibit low solubility requiring the use of amorphous dispersion-based formulation for achieving efficacious drug exposures. Through structure-based design, we discovered a new class of highly potent aminopyrimidine-based B-Raf inhibitors with improved solubility and pharmacokinetic profiles. The hinge binding moiety possesses a basic center imparting high solubility at gastric pH, addressing the dissolution limitation observed with our previous series. In our search for an optimal linker-hinge binding moiety system, amide-linked thieno[3,2-d]pyrimidine analogues 32 and 35 (G945), molecules with desirable physicochemical properties, emerged as lead compounds with strong efficacy in a B-RafV600E mutant mouse xenograft model. Synthesis, SAR, lead selection, and evaluation of key compounds in animal studies will be described.

RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF

Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

NOVEL AMINO AZAHETEROCYCLIC CARBOXAMIDES

The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

PROTEIN KINASE INHIBITORS AND METHODS FOR USING THEREOF

The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of AIk, AbI, Aurora- A, B-Raf, C- Raf, Bcr-Abl, BRK, BIk, Bmx, BTK, C-Kit, C-Raf, C-Src, EphB1, EphB2, EphB4, FGFR1, FGFR2, FGFR3, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRα, PDGFRβ, PKCα, p38, Src, SIK, Syk, Tie2 and TrkB kinases.