909186-02-3

Basic information

• Product Name: 3-broMopyrido[2,3-d]pyridazin-8(7h)-one
• Synonyms: 3-broMopyrido[2,3-d]pyridazin-8(7h)-one
• CAS NO: 909186-02-3
• Molecular Formula: C7H4BrN3O
• Molecular Weight: 226.03016
• Mol File: 909186-02-3.mol

Chemical Properties

• Appearance: /
• Density: 2.01±0.1 g/cm3(Predicted)
• Storage Temp.: Inert atmosphere,Room Temperature
• PKA: 10.19±0.20(Predicted)
• CAS DataBase Reference: 3-broMopyrido[2,3-d]pyridazin-8(7h)-one(CAS DataBase Reference)
• NIST Chemistry Reference: 3-broMopyrido[2,3-d]pyridazin-8(7h)-one(909186-02-3)
• EPA Substance Registry System: 3-broMopyrido[2,3-d]pyridazin-8(7h)-one(909186-02-3)

Safety Data

• Hazardous Substances Data: 909186-02-3(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
3-Bromopyrido[2,3-d]pyridazin-8(7H)-one is used as a key intermediate in the synthesis of Naphthyridine compounds, which are known to act as inhibitors of Hematopoietic progenitor kinase 1 (HPK1). The inhibition of HPK1 has been identified as a promising strategy for the treatment of various types of cancer, making 3-broMopyrido[2,3-d]pyridazin-8(7h)-one an important building block in the development of novel anticancer drugs.

Upstream product

• 886365-43-1 5-bromo-3-methylpyridine-2-carboxylic acid 
• 213771-32-5 5-bromo-3-methylpyridine-2-carboxylic acid methyl ester 

Downstream Products

• 794592-14-6 3-bromo-8-chloropyrido[2,3-d]pyridazine 
• 1600511-18-9 N-(3-((3R)-5-amino-3,6,6-trimethyl-1,1-dioxido-3,6-dihydro-2H-1,4-thiazin-3-yl)-4-fluorophenyl)-3-bromopyrido[2,3-d]pyridazin-8-amine 
• 1600508-22-2 (R)-8-((3-(5-amino-3,6,6-trimethyl-1,1-dioxido-3,6-dihydro-2H-1,4-thiazin-3-yl)-4-fluorophenyl)amino)pyrido[2,3-d]pyridazine-3-carbonitrile 

Relevant articles and documents

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor

Structure-based optimization of a set of aryl urea RAF inhibitors has led to the identification of Type II pan-RAF inhibitor GNE-9815 (7), which features a unique pyrido[2,3-d]pyridazin-8(7H)-one hinge-binding motif. With minimal polar hinge contacts, the pyridopyridazinone hinge binder moiety affords exquisite kinase selectivity in a lipophilic efficient manner. The improved physicochemical properties of GNE-9815 provided a path for oral dosing without enabling formulations. In vivo evaluation of GNE-9815 in combination with the MEK inhibitor cobimetinib demonstrated synergistic MAPK pathway modulation in an HCT116 xenograft mouse model. To the best of our knowledge, GNE-9815 is among the most highly kinase-selective RAF inhibitors reported to date.

NAPHTHYRIDINES AS INHIBITORS OF HPK1

Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

CYCLOPROPYL FUSED THIAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE

The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I): wherein variables A4, A5, A6, A8, and each of Ra, Rb, R1, R2, R3 and R7 of Formula (I), independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and 15 deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimers Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas (II) and (III), and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

AMINO-DIHYDROTHIAZINE AND AMINO-DIOXIDO DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE

The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.

Phthalazine, aza- and diaza-phthalazine compounds and methods of use

The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.