52023-68-4

Usage

Uses

5-Amino-2-(4-morpholinyl)pyridine is used as pharmaceutical intermediate.

InChI:InChI=1/C9H13N3O/c10-8-1-2-9(11-7-8)12-3-5-13-6-4-12/h1-2,7H,3-6,10H2/p+1

Upstream product

• 26820-62-2 4-(5-nitro-pyridin-2-yl)-morpholine 
• 110-91-8 morpholine 
• 13534-97-9 6-bromopyridine-3-amine 
• 40473-01-6 2-Bromo-5-chloro-pyridine 
• 59027-83-7 4-(5-chloro-pyridin-2-yl)-morpholine 
• 4548-45-2 2-chloro-5-nitropyridine 
• 456-24-6 2-Fluoro-5-nitropyridine 
• 4487-59-6 2-bromo-5-nitropyridine 

Downstream Products

• 940794-02-5 N-(6-morpholinopyridin-3-yl)-2-(6-phenylimidazo[2,1-b]thiazol-3-yl)acetamide 
• 1415835-26-5 2-[(6-morpholin-4-ylpyridin-3-yl)amino]-N’-(4-oxo-3-phenyl-1,3-thiazolidin-2-ylidene)acetohydrazide 
• 1415835-18-5 N'-(4-bromobenzylidene)-2-[6-(morpholin-4-yl)pyridin-3-ylamino]acetohydrazide 
• 1415835-21-0 5-{[(6-morpholin-4-ylpyridin-3-yl)amino]methyl}-3-[(4-phenylpiperazin-1-yl)methyl]-1,3,4-oxadiazole-2(3H)-thione 
• 1415835-22-1 2-{[(6-morpholin-4-ylpyridin-3-yl)amino]acetyl}-N-phenylhydrazinecarbothioamide 
• 1415835-23-2 N'-[5-(4-chlorophenyl)-3-phenyl-1,3-thiazol-2(3H)-ylidene]-2-{(6-morpholin-4-ylpyridin-3-yl)amino}acetohydrazide 
• 1445881-89-9 C₂₆H₂₇N₇O₃S 
• 1445883-86-2 C₁₈H₁₇N₅OS 
• 1445883-85-1 C₁₈H₁₅N₅O₃S 
• 1429297-30-2 C₂₄H₂₃Cl₂FN₄O₄ 

Relevant academic research and scientific papers

COMPOUNDS AND METHOD FOR TREATING CYTOKINE RELEASE SYNDROME

Disclosed herein are embodiments of a method for treating or preventing cytokine release syndrome (CRS). In certain embodiments, the method comprises administering a compound, or a salt, solvate, prodrug or pharmaceutical composition thereof, to a subject experiencing, or at risk of developing, CRS. The compound may be a kinase inhibitor, such as a JAK inhibitor and/or an IRAK inhibitor, and/or the compound may have a structure according to Formulas I, III, IV or VII. And the method may comprise administering the compound to a subject who is has received, is currently receiving, and/or will be receiving a cell therapy.

MALT1 INHIBITORS AND USES THEREOF

The invention provides compounds of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification which are potent inhibitors of the enzyme MALT1 and are useful in the treatment of autoimmune disorders and diseases and as an immunooncology approach to the treatment of cancer, especially bladder cancer, colon cancer, hepatocellular cancer and small cell or non-small cell lung cancer.

FUSED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF

The present disclosure relates to a class of fused pyrimidine compounds of Formula I, their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to a process of preparation of these fused pyrimidine compounds, and to pharmaceutical compositions containing them.

BENZIMIDAZOLE AND HYDROGENATED CARBAZOLE DERIVATIVES AS GPX4 INHIBITORS

This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.

C-TERMINAL SRC KINASE INHIBITORS

Provided herein are novel C-terminal Srk Kinase (CSK) inhibitors, e.g., having Formula G, I, II, or III. Also provided are methods of preparing the novel CSK inhibitors and method of using the novel CSK inhibitors for treating diseases or disorder such as cancer or for promoting immune response in a subject in need thereof. (G)

5-HETEROARYL SUBSTITUTED INDAZOLE-3-CARBOXAMIDES AND PREPARATION AND USE THEREOF

Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., tendinopathy, dermatitis, psoriasis, morphea, ichthyosis, Raynaud's syndrome, Darier's disease, scleroderma, cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.

NEW BENZAMIDE DERIVATIVES AS PPAR-GAMMA MODULATORS

The present invention relates to novel benzamides derivatives of formula (I) as modulators of PPAR-gamma receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to said compound for use in the treatment of pathological conditions, disorders or diseases that can improve by modulation of PPAR-gamma receptor, such as cancer; metabolic diseases, inflammatory diseases, respiratory disorders, autoimmune diseases, neurodegenerative diseases, cardiovascular diseases and renal diseases.

First-in-class DAPK1/CSF1R dual inhibitors: Discovery of 3,5-dimethoxy-N-(4-(4-methoxyphenoxy)-2-((6-morpholinopyridin-3-yl)amino)pyrimidin-5-yl)benzamide as a potential anti-tauopathies agent

Kinase irregularity has been correlated with several complex neurodegenerative tauopathies. Development of selective inhibitors of these kinases might afford promising anti-tauopathy therapies. While DAPK1 inhibitors halt the formation of tau aggregates and counteract neuronal death, CSF1R inhibitors could alleviate the tauopathies-associated neuroinflammation. Herein, we report the design, synthesis, biological evaluation, mechanistic study, and molecular docking study of novel CSF1R/DAPK1 dual inhibitors as multifunctional molecules inhibiting the formation of tau aggregates and neuroinflammation. Compound 3l, the most potent DAPK1 inhibitor in the in vitro kinase assay (IC50 = 1.25 μM) was the most effective tau aggregates formation inhibitor in the cellular assay (IC50 = 5.0 μM). Also, compound 3l elicited potent inhibition of CSF1R in the in vitro kinase assay (IC50 = 0.15 μM) and promising inhibition of nitric oxide production in LPS-induced BV-2 cells (55% inhibition at 10 μM concentration). Kinase profiling and hERG binding assay anticipated the absence of off-target toxicities while the PAMPA-BBB assay predicted potentially high BBB permeability. The mechanistic study and selectivity profile suggest compound 3l as a non-ATP-competitive DAPK1 inhibitor and an ATP-competitive CSF1R inhibitor while the in silico calculations illustrated binding of compound 3l to the substrate-binding site of DAPK1. Hence, compound 3l might act as a protein-protein interaction inhibitor by hindering DAPK1 kinase reaction through preventing the binding of DAPK1 substrates.

Streamlined Synthesis of Diaminopyridines by Pd-Catalyzed Ammonia Coupling with Deactivated Amino-Chloropyridines

An efficient and cost-effective two-step synthesis of diaminopyridines, fundamental building blocks of biologically active compounds, is reported. The advantages over previously reported routes include cost and wider availability of the bromo-chloropyridine starting materials and the straightforward accessibility to an extended array of diaminopyridine regioisomers. The key enabler of this synthetic strategy is the development of an unprecedented palladium-catalyzed coupling reaction of ammonia with chloropyridines deactivated by the presence of an alkylamino substituent. The coupling reaction was accomplished with very low catalyst loadings under remarkably mild reaction conditions, making the system particularly suitable for both academic and industrial applications. The utility of this methodology is exemplified by the application to the synthesis of highly relevant scaffolds, including the synthetic intermediates of the marketed drugs Ribociclib and Palbociclib.

METHODS OF USING INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/B-CATENIN SIGNALING PATHWAY INHIBITORS

This disclosure features the use of one or more indazole-3-carboxamide compounds or salts or analogs thereof, in the treatment of one or more diseases or conditions independently selected from the group consisting of a tendinopathy, dermatitis, psoriasis, morphea, ichthyosis, Raynaud's syndrome, and Darier's disease; and/or for promoting wound healing. The methods include administering to a subject (e.g., a subject in need thereof) a therapeutically effective amount of one or more indazole-3-carboxamide compounds or salts or analogs thereof as described anywhere herein.