73161-37-2

Usage

Uses

Used in Cancer Therapy:
N-(3-cyanopyridin-2-yl)-N-methylmethanesulfonamide is used as an anti-cancer agent for targeting hypoxic tumors. Its selective inhibition of carbonic anhydrase IX (CA IX) helps in reducing tumor progression and metastasis, making it a promising candidate for cancer treatment.
Used in Pharmaceutical Industry:
N-(3-cyanopyridin-2-yl)-N-methylmethanesulfonamide is used as a drug candidate for the development of novel therapeutic agents. Its potential applications extend beyond cancer therapy, as it has been investigated for the treatment of glaucoma, renal disease, and metabolic disorders, showcasing its versatility in addressing various medical conditions.
Used in Drug Delivery Systems:
To enhance the efficacy and bioavailability of N-(3-cyanopyridin-2-yl)-N-methylmethanesulfonamide, researchers are exploring the development of innovative drug delivery systems. These systems aim to improve the compound's pharmacokinetics, targeting, and therapeutic outcomes, further expanding its potential applications in the medical field.

Upstream product

• 1184-85-6 N-methylmethane sulphonamide 
• 3939-13-7 3-cyano-2-fluoropyridine 
• 24517-64-4 2-amino-3-pyridinecarbonitrile 
• 74-88-4 methyl iodide 
• 6602-54-6 2-chloro-3-pyridinecarbonitrile 

Downstream Products

• 73161-38-3 1-methyl-2,2-dioxo-1,2-dihydro-2λ⁶-pyrido[2,3-c][1,2]thiazin-4-ylamine 
• 939791-42-1 N-(3-(aminomethyl)pyridine-2-yl)-N-methylmethanesulfonamide 

Relevant academic research and scientific papers

Synthesis of carbo- and heterofused 5-amino-2H-1,2-thiazine 1,1-dioxides via the CSIC reaction strategy

Herein, we present a full account of our studies with respect to the synthesis of carbo- and heterofused β-enamino-δ-sultams annelated on face c (3,4-bond). This class of compounds was designed as isomeric counterpart of known pharmacological templates – fused δ-sultams annelated through a face e (5,6-bond) following the principles of bioisosteric replacement. The starting material for this synthesis is cyclic vicinal amino nitriles. In particular, several methods were developed for methanesulfonylation of 5- and 6-membered carbo- and heteroaromatic as well as sp3-enriched β-enamino nitriles depending on their chemical nature and reactivity. The obtained N-mono- or/and N,N-dimesylates were converted into the corresponding N-methylmethanesulfonamides, which were subjected to the CSIC (Carbanion-mediated Sulfonate (Sulfonamide) Intramolecular Cyclization) reaction protocols thus affording target carbo- and heterofused β-enamino-δ-sultams. Their synthetic utility was demonstrated by the reactions with carbo- and hetero electrophiles.

Design, Synthesis, and Evaluation of Highly Potent FAK-Targeting PROTACs

Focal adhesion kinase (FAK), a cytoplasmic protein tyrosine kinase, exerts kinase-dependent enzymatic functions and kinase-independent scaffolding functions, both of which are crucial in cancer development, early embryonic development, and reproduction. H

SUBSTITUTED PYRIMIDINES, PHARMACEUTICAL COMPOSITIONS AND THERAPEUTIC METHODS THEREOF

The invention provide novel pyrimidine derivatives and analogs having inhibitory activities towards certain tyrosine kinases, e.g., Bruton's tyrosine kinase (Btk) and/or Focal adhesion kinase (FAK), extracellular signal-regulated kinase (ERK), pharmaceutical compositions thereof, and methods of treatment, reduction or prevention of certain diseases or conditions mediated by such by tyrosine kinases, e.g., cancers, tumors, fibrosis, inflammatory diseases, autoimmune diseases, diabetes, or immunologically mediated diseases.

Compound for degrading FAK (Focal Adhesion Kinase) protein in targeting manner and application thereof

The invention provides a compound. The compound is a compound shown as a formula I or a stereoisomer, a geometric isomer, a tautomer, nitrogen oxide, hydrate, a solvate, a metabolic product, pharmaceutically acceptable salt or a prodrug thereof: X-Y-Z (formula I), wherein X represents a ligand of FAK protein, Z represents ligand of E3 ligase and Y represents a chain for connecting the X and the Z.

PYRAZOLOPYRIDINES AND PYRAZOLOPYRIMIDINES

A compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A and A′ are independently C or N, where C may be unsubstituted or substituted by halo or C1-C6 alkyl; R and R0 are independently selected from the group consisting of H, C1-C6 alkyl, hydroxy(C1-C6 alkyl), phenyl(C1-C6 alkyl), and —(CH2)n—W, where W is C3-C8 cycloalkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1-3 N, S and/or O atoms, —SO2—R′, —NHSO2—R′, —NR″SO2—R′ and SR′, where R′ and R″ are independently C1-C6 alkyl or C3-C8 cycloalkyl, etc.; wherein each of said alkyl, cycloalkyl, heterocyclic, phenyl, naphthyl or heteroaryl may be unsubstituted or substituted by phenyl, heteroaryl, etc.; or, R and R0 and the N atom to which they are bonded together form a monocyclic or bicyclic heterocyclic ring which may be unsubstituted or substituted by (a) halo, hydroxy, heteroaryl, C1-C6 alkyl, C1-C6 alkoxy, etc., or (b) —(CH2)n—W, where W is C3-C8 cycloalkyl, phenyl, etc.; R1 is H, halo or cyano; R2 and R2′ are independently H, C1-C6 alkyl, cyano, C1-C6 alkoxy, C1-C6 alkylthio, or C3-C8 cycloalkyl where alkyl, alkoxy, or cycloalkyl is optionally substituted by one or more fluorine atoms; X is a bond, —CO—, —CONH—, —SO2—, —SONH—, or —(CH2)m—; R3 is H, C1-C4 alkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1-3 N atoms, a 5-membered heteroaryl or heterocyclic, etc., or (c) 2 O or S atoms and 0-2 N atoms; wherein each of said phenyl, naphthyl, heteroaryl or heterocyclic is optionally substituted by alkyl, 1 substituent —Y—R4 and/or 1-4 substituents each independently selected from R5; with the proviso that when X is —CO— or —SO2—, R3 is not H; Y is a bond, —(CH2)m— or —O—; R4 is (a) H, C1-C6 alkyl, C3-C8 cycloalkyl, halo, oxo, —OR6, —NR7R8, —SR6, —SOR9, —SO2R9, —COR6, —OCOR6, —OCOR6, —NR6COR6, —CONR7R8, etc.; (b) phenyl or naphthyl, said phenyl and naphthyl being optionally substituted with 1-5 substituents selected from C1-C6 alkyl, C3-C8 cycloalkyl, halo, cyano, —OR6, —NR7R8, etc.; or (c) a 3 to 8-membered saturated or partially unsaturated monocyclic heteroaryl, etc.; R6 is H, C1-C6 alkyl or C3-C8 cycloalkyl, etc.; R7 and R8 are each independently H, C1-C6 alkyl or C3-C8 cycloalkyl or are taken together with the nitrogen atom to which they are attached to form a 4-, 5- or 6-membered saturated heterocyclic ring containing 1-2 nitrogen atoms or 1 nitrogen and 1 oxygen atom, said C1-C6 alkyl is optionally substituted by C3-C8 cycloalkyl, halo, etc., and said heterocyclic ring being optionally substituted by one or more C1-C6 alkyl or C3-C8 cycloalkyl groups; R9 is C1-C6 alkyl or C3-C8 cycloalkyl; and, m and n are independently 0, 1, 2 or 3. The invention also relates to pharmaceutically acceptable salts of these compounds and to pharmaceutically acceptable solvates thereof; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.

COMPOUNDS FOR REGULATING FAK AND/OR SRC PATHWAYS

The present application provides novel optionally substituted fused pyridine and pyrimidine bicyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating FAK and/or Src activity by administering a therapeutically effective amount of one or more of the compounds to a subject. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the FAK and/or Src pathway. Advantageously, these compounds perform as dual FAK and/or Src inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.

PYRROLOPYRIMIDINES AS FAK AND ALK INHIBITERS FOR TREATMENT OF CANCERS AND OTHER DISEASES

Disclosed are compounds which inhibit the activity of focal adhesion kinase (FAK) and anaplastic lymphoma kinase (ALK), compositions containing the compounds, and methods of treating diseases during which FAK and ALK are expressed. The diseases are, for example, cancers.

SULFONYL AMIDE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH

The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.

INHIBITORS OF FOCAL ADHESION KINASE

The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.