27330-34-3

Usage

Uses

Used in Pharmaceutical Industry:
3-Amino-5-chloropyridine-2-carboxamide is used as a building block for the synthesis of various drug molecules, contributing to the development of new medications for the treatment of diseases and conditions.
Used in Cancer Treatment:
3-AMINO-5-CHLOROPYRIDINE-2-CARBOXAMIDE is used as a potential therapeutic agent for the treatment of various types of cancer, due to its ability to inhibit the activity of certain enzymes and its potential to be incorporated into drug molecules with anticancer properties.
Used in Inflammatory Disorders:
3-Amino-5-chloropyridine-2-carboxamide is used as a potential treatment for inflammatory disorders, as it may have properties that help reduce inflammation and alleviate symptoms associated with these conditions.
Used in Agricultural Chemicals:
3-AMINO-5-CHLOROPYRIDINE-2-CARBOXAMIDE is used in the development of agricultural chemicals, where it may contribute to the creation of products that enhance crop protection and yield.
Used in Biological Research:
3-Amino-5-chloropyridine-2-carboxamide is used as a tool for biological research, particularly in the study of enzyme inhibition and the development of new therapeutic approaches for various diseases and conditions.

Upstream product

• 181123-11-5 5-chloro-2-cyano-3-nitropyridine 
• 1336-21-6 ammonium hydroxide 
• 408538-29-4 3-amino-5-chloropicolinonitrile 
• 21427-61-2 5-chloro-3-nitropyridin-2-ol 
• 75806-86-9 2-bromo-5-chloro-3-nitropyridine 
• 1072-98-6 5-chloro-2-pyridylamine 
• 856834-36-1 5-chloro-3-nitro-pyridine-2-carboxylic acid amide 
• 5409-39-2 2-amino-5-chloro-3-nitropyridine 

Downstream Products

• 27330-35-4 ethyl 3-amino-5-chloropicolinate 
• 212378-47-7 ethyl 3-phenylacetylamido-5-chloropicolinate 
• 372951-25-2 ethyl 3-(m-methyl)phenylacetylamido-5-chloropicolinate 
• 372951-22-9 ethyl 3-(p-chloro)phenylacetylamido-5-chloropicolinate 
• 372951-24-1 ethyl 3-(o-chloro)phenylacetylamido-5-chloropicolinate 
• 372951-23-0 ethyl 3-(m-chloro)phenylacetylamido-5-chloropicolinate 
• 181123-12-6 ethyl 3-(m-methoxy)phenylacetylamido-5-chloropicolinate 
• 372951-26-3 5-chloro-3-[2-(3-nitro-phenyl)-acetylamino]-pyridine-2-carboxylic acid ethyl ester 
• 181122-94-1 ACEA 762 
• 181123-13-7 ethyl 3-(m-phenoxyphenyl)acetylamido-5-chloropicolinate 
• 53636-68-3 3-amino-5-chloropyridine-2-carboxylic acid 
• 1624603-36-6 4-((3-((4S,6S)-2-amino-4-(fluoromethyl)-6-(trifluoromethyl)-5,6-dihydro-4H-1,3-oxazin-4-yl)-4-fluorophenyl)amino)pyrido[3,2-d]pyrimidine-7-carbonitrile 
• 1624605-29-3 (4S,6S)-4-(5-((7-chloropyrido[3,2-d]pyrimidin-4-yl)amino)-2-fluoro-3-methylphenyl)-4-(fluoromethyl)-6-(trifluoromethyl)-5,6-dihydro-4H-1,3-oxazin-2-amine 
• 1624603-26-4 (4S,6S)-4-(2-fluoro-5-((7-methoxypyrido[3,2-d]pyrimidin-4-yl)amino)phenyl)-4-(fluoromethyl)-6-(trifluoromethyl)-5,6-dihydro-4H-1,3-oxazin-2-amine 

Relevant academic research and scientific papers

Discovery of novel dual extracellular regulated protein kinases (Erk) and phosphoinositide 3-kinase (pi3k) inhibitors as a promising strategy for cancer therapy

Concomitant inhibition of MAPK and PI3K signaling pathways has been recognized as a promising strategy for cancer therapy, which effectively overcomes the drug resistance of MAPK signaling pathway-related inhibitors. Herein, we report the scaffold-hopping generation of a series of 1H-pyrazolo[3,4-d]pyrimidine dual ERK/PI3K inhibitors. Compound 32d was the most promising candidate, with potent inhibitory activities against both ERK2 and PI3Kα which displays superior anti-proliferative profiles against HCT116 and HEC1B cancer cells. Meanwhile, compound 32d possessed acceptable pharmacokinetic profiles and showed more efficacious anti-tumor activity than GDDC-0980 and the corresponding drug combination (BVD-523 + GDDC-0980) in HCT-116 xenograft model, with a tumor growth inhibitory rate of 51% without causing observable toxic effects. All the results indicated that 32d was a highly effective anticancer compound and provided a promising basis for further optimization towards dual ERK/PI3K inhibitors.

Dual-Stage Picolinic Acid-Derived Inhibitors of Toxoplasma gondii

Toxoplasma gondii causes a prevalent human infection for which only the acute stage has an FDA-approved therapy. To find inhibitors of both the acute stage parasites and the persistent cyst stage that causes a chronic infection, we repurposed a compound library containing known inhibitors of parasitic hexokinase, the first step in the glycolysis pathway, along with a larger collection of new structural derivatives. The focused screen of 22 compounds showed a 77% hit rate (>50% multistage inhibition) and revealed a series of aminobenzamide-linked picolinic acids with submicromolar potency against both T. gondii parasite forms. Picolinic acid 23, designed from an antiparasitic benzamidobenzoic acid class with challenging ADME properties, showed 60-fold-enhanced solubility, a moderate LogD7.4, and a 30% improvement in microsomal stability. Furthermore, isotopically labeled glucose tracing revealed that picolinic acid 23 does not function by hexokinase inhibition. Thus, we report a new probe scaffold to interrogate dual-stage inhibition of T. gondii.

IDENTIFICATION AND USE OF ERK5 INHIBITORS

The present invention covers heterocyclic compounds of general formula (I) in which T, U, Y, Z, R1 and R3 are as defined herein, 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 for the treatment or prophylaxis of diseases, in particular of cancer disorders, as a sole agent or in combination with other active ingredients.

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.

BRIDGED BICYCLIC AMINO THIAZINE DIOXIDE COMPOUNDS AS INHIBITORS OF BETA-SECRETASE AND METHODS OF USE THEREOF

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, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.

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.

PERFLUORINATED 5,6-DIHYDRO-4H-1,3-OXAZIN-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, each of R1 and R2, R3 and R7 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 Formulas II and III, and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.

FUSED MULTI-CYCLIC SULFONE COMPOUNDS AS INHIBITORS OF BETA-SECRETASE AND METHODS OF USE THEREOF

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 A5, A6, A8, R1, R2, R3, R7, X, Y, n and o 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, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.

PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE

PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE ABSTRACT OF THE DISCLOSURE 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: {INSERT STRUCTURE HERE} I wherein variables A4, A5, A6, A8, 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 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 Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

FUSED HETEROARYL PYRIDYL AND PHENYL BENZENESUFLONAMIDES AS CCR2 MODULATORS FOR THE TREAMENT OF INFLAMMATION

Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2- mediated diseases and as controls in assays for the identification of CCR2 antagonists. A compound of the formula (I) or a salt thereof: where: R1 and R2 are each independently hydrogen, halogen, C1-8alkyl, -CN. or C1-8 haloalkyl, provided that at least one of R11or R2 is other than hydrogen; each R3 is independently hydrogen; R4 is hydrogen; R5 is halogen or C1-8 alkyl; R6 is hydrogen; X1 is CR7, N or NO; X2 and X4 are N or NO; X3 is CR7; X6 and X7 are each independently selected from CR7, N, and NO; each R7 is independently selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C2-8 alkyl, substituted or unsubstituted C2-8 alkeπyl, substituted or unsubstituted C2-8 alkynyl, -CN. =O, -NO2, -OR6, -OC(O)R8, -CO2R8, -C(O)R8, -C(O)NR0R8, -OC(O)NR9R8, -NR10C(O)R8, -NR10C(O)NR9R8, -NR9R8, -NR10CO2R8, -SR8, -S(O)R8, -S(O)2R8, -S(O)2NR9R8, -NR10S(O)2R8, substituted or unsubstituted C6-10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl and substituted or unsubstituted 3- to 10-membered heterocyclyl;