Category: pyridine-derivatives

On March 20, 2014, Soll, Mark David; Le Hir de Fallois, Loic Patrick; Huber, Scot Kevin; Lee, Hyoung Ik; Wilkinson, Douglas Edward; Jacobs, Robert Toms published a patent.Formula: C6H3ClN2O3 The title of the patent was Preparation of arylazol-2-yl cyanoethylamino derivatives useful as pesticides. And the patent contained the following:

The invention relates to arylazol-2-yl-cyanoethylamino derivatives of formula I and their preparation, useful as pesticides, particularly for controlling endoparasitic or ectoparasitic pests on animals. Compounds of formula I, in which group P is N; Q is CR2 and N; V is CR8; W is CR9 and N; X is CR10 and N; Y is CR11 and N; R2, R8, R9, R10, and R11 are each independently H, amino, amido, CN, etc.; R3, R4, and R5 are each independently H, halo, alkyl, etc.; and CR4R5 taken together form cycloalkyl ring; n = 1 – 3; R6 and R7 are independently H, (alkoxy)alkyl, alkylcarbonyl, etc.; Z is direct bond, CO, CS, and S(O)p; p = 0 – 2; or salts thereof, are claimed. Example compound II was prepared by amidation of 2-amino-3-(5-chloro-2H-benzotriazol-2-yl)-2-methylpropionitrile with 4-trifluoromethoxybenzoyl chloride. Invention compounds were evaluated for their pesticidal activity. From the assay, it was determined that compound II exhibited >95% reduction in nematode infestation after 3 days. The experimental process involved the reaction of 5-Chloro-3-nitropicolinaldehyde(cas: 1086838-13-2).Formula: C6H3ClN2O3

The Article related to arylazole benzotriazole indazole pyrazolopyridine cyanoethylamine preparation pesticide, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Three Or More Hetero Atoms and other aspects.Formula: C6H3ClN2O3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 11, 2014, Van Gool, Michiel Luc Maria; Alonso-De Diego, Sergio-Alvar; Cid-Nunez, Jose Maria; Delgado-Gonzalez, Oscar; Decorte, Annelies Marie Antonius; Macdonald, Gregor James; Megens, Antonius Adrianus Hendrikus Petrus; Trabanco-Suarez, Andres Avelino; Garcia-Molina, Aranzazu; Andres-Gil, Jose Ignacio published a patent.Category: pyridine-derivatives The title of the patent was Preparation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mGluR2 receptors. And the patent contained the following:

Title compounds I [R1 = substituted Ph or 2-pyridinyl; R2 = substituted pyridinyl; R3 = H or alkyl; R4 = H, alkyl, mono- or polyhalo-alkyl, alkyl-O-alkyl or alkyl-OH], or a N-oxide, or a pharmaceutically acceptable salt or a solvate, are prepared as neg. allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (mGluR2). Thus, e.g., II was prepared by reaction of (7S)-methyl-3-(2-methylpyridin-4-yl)-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazin-4-one with 4-bromobenzotrifluoride. Compound II showed pIC50 value of 8.05 against hmGluR2 in GTPγS binding assay. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved, especially CNS disorders. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Category: pyridine-derivatives

The Article related to dihydropyrazolopyrazine preparation neg allosteric mglur2 receptors cns disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On May 14, 1991, Yamaji, Mitsuharu published a patent.Safety of 3-Methylpyridine-2,6-diamine The title of the patent was Preparation of 3-alkyl-2,6-diaminopyridines as developers for hair dyes. And the patent contained the following:

The diaminopyridines are prepared by treating 3-alkyl-2-aminopyridines with alkali metal amides in inert solvents and quenching the reaction mixtures with OH-containing compounds Thus, a solution of NaNH2 in Tetralin was treated dropwise with 2-amino-3-methylpyridine, then the mixture was quenched with H2O to give 62% 3-methyl-2,6-diaminopyridine. The experimental process involved the reaction of 3-Methylpyridine-2,6-diamine(cas: 51566-22-4).Safety of 3-Methylpyridine-2,6-diamine

The Article related to hair dye developer alkyldiaminopyridine, aminopyridine amination alkali amide, Dyes, Organic Pigments, Fluorescent Brighteners, and Photographic Sensitizers: Other Dyes and Pigments and other aspects.Safety of 3-Methylpyridine-2,6-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 1, 2020, Zhou, Xiaocong; He, Xinyi; Yan, Puzha; Li, Yuanqiang published a patent.Recommanded Product: 908267-63-0 The title of the patent was Trifluoromethylation of dimethyl substituted heterocyclic compounds. And the patent contained the following:

The invention relates to the trifluoromethylation of di-Me substituted heterocyclic compounds, and has the advantage of wide range of substrate selection. For example, 2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridine was prepared by trifluoromethylation of 2-isopropyridine and 5-(trifluoromethyl)-5H-dibenzo[b,d]thiophen-5-ium trifluoromethanesulfonate. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Recommanded Product: 908267-63-0

The Article related to trifluoromethylation preparation pyrimidine quinoxaline quinazoline pyrazine, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 13, 2009, Dorsey, Bruce D.; Milkiewicz, Karen L.; Pippin, Douglas A.; Theroff, Jay P.; Underiner, Ted; Weinberg, Linda; Zificsak, Craig A. published a patent.Name: 3-((6-Bromopyridin-2-yl)amino)propanoic acid The title of the patent was Preparation of pyridopyrazine derivatives as ALK and c-Met inhibitors. And the patent contained the following:

Title compounds I [ A = N or CH; X = -L2G1L3G2L4R7 or R8, wherein G1 and G2 independently = bond, (un)substituted (hetero)aryl or heterocycloalkyl; R7 = (un)substituted alkyl, alkenyl, alkynyl, (hetero)aryl or (hetero)cycloalkyl; R8 = H, halo, CN or CO2H; L1-4 independently = bond, alkyl-C(O)-alkyl, alkyl-C(O)O-alkyl, alkyl-O-alkyl, alkyl, alkenyl, alkynyl, etc.; R1 = (un)substituted (hetero)cycloalkyl or (hetero)aryl; R2 and R3 independently = H, OH or alkyl; R2 and R3 together may form a carbonyl group; R4, R5 and R6 independently = H or alkyl; R4 and R5 together may form a carbonyl group, or one of R4 and R5 forms a double bond with R6], and their pharmaceutically acceptable salts, are prepared and disclosed as Anaplastic Lymphoma Kinase (ALK) and c-Met inhibitors. Thus, e.g., II was prepared by acylation of 7-iodo-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine (preparation given) with benzoyl chloride followed by Suzuki coupling reaction with (4-ethoxycarbonylphenyl)boronic acid to generate intermediate 4-(1-benzyl-1,2,3,4-tetrahydropyrido[2,3-b]pyrazin-7-yl)benzoic acid Et ester followed by hydrolysis and amidation with (S)-(+)-1-[(2-pyrrolidinyl)methyl]pyrrolidine to provide II as trifluoroacetate salt. All exemplar compounds were tested for their ability to inhibit the kinase activity for ALK and c-Met. For instance, II exhibited IC50 values ranging from 0.1 to 1 μM for ALK and c-Met kinase inhibition, resp. As inhibitors of ALK and/or c-Met, I may be used to treat ALK- or c-Met-mediated disorders or conditions. The experimental process involved the reaction of 3-((6-Bromopyridin-2-yl)amino)propanoic acid(cas: 68638-67-5).Name: 3-((6-Bromopyridin-2-yl)amino)propanoic acid

The Article related to pyridopyrazine preparation anaplastic lymphoma kinase alk cmet inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Name: 3-((6-Bromopyridin-2-yl)amino)propanoic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On November 15, 2007, Dorsey, Bruce D.; Milkiewicz, Karen L.; Pippin, Douglas A.; Theroff, Jay P.; Underiner, Theodore L.; Weinberg, Linda; Zificsak, Craig A. published a patent.Formula: C8H9BrN2O2 The title of the patent was Preparation of pyridopyrazine derivatives as ALK and c-Met inhibitors. And the patent contained the following:

Title compounds I [ A = N or CH; X = -L2G1L3G2L4R7 or R8, wherein G1 and G2 independently = bond, (un)substituted (hetero)aryl or heterocycloalkyl; R7 = (un)substituted alkyl, alkenyl, alkynyl, (hetero)aryl or (hetero)cycloalkyl; R8 = H, halo, CN or CO2H; L1-4 independently = bond, alkyl-C(O)-alkyl, alkyl-C(O)O-alkyl, alkyl-O-alkyl, alkyl, alkenyl, alkynyl, etc.; R1 = (un)substituted (hetero)cycloalkyl or (hetero)aryl; R2 and R3 independently = H, OH or alkyl; R2 and R3 together may form a carbonyl group; R4, R5 and R6 independently = H or alkyl; R4 and R5 together may form a carbonyl group, or one of R4 and R5 forms a double bond with R6], and their pharmaceutically acceptable salts, are prepared and disclosed as Anaplastic Lymphoma Kinase (ALK) and c-Met inhibitors. Thus, e.g., II was prepared by acylation of 7-iodo-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine (preparation given) with benzoyl chloride followed by Suzuki coupling reaction with (4-ethoxycarbonylphenyl)boronic acid to generate intermediate 4-(1-benzyl-1,2,3,4-tetrahydropyrido[2,3-b]pyrazin-7-yl)benzoic acid Et ester followed by hydrolysis and amidation with (S)-(+)-1-[(2-pyrrolidinyl)methyl]pyrrolidine to provide II as trifluoroacetate salt. All exemplar compounds were tested for their ability to inhibit the kinase activity for ALK and c-Met. For instance, II exhibited IC50 values ranging from 0.1 to 1 μM for ALK and c-Met kinase inhibition, resp. As inhibitors of ALK and/or c-Met, I may be used to treat ALK- or c-Met-mediated disorders or conditions. The experimental process involved the reaction of 3-((6-Bromopyridin-2-yl)amino)propanoic acid(cas: 68638-67-5).Formula: C8H9BrN2O2

The Article related to pyridopyrazine preparation anaplastic lymphoma kinase alk cmet inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Formula: C8H9BrN2O2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 6, 2014, Xiao, Dengming; Xu, Xinhe; Liu, Xijie; Hu, Yuandong; Yu, Honghao; Liu, Zhihua; Peng, Yong; Sun, Yinghui; Luo, Hong; Kong, Fansheng; Han, Yongxin; Sun, Jian published a patent.Formula: C6H5Br2NO The title of the patent was Preparation of substituted 2-aminopyridine derivatives as protein kinase inhibitors. And the patent contained the following:

The present invention discloses substituted 2-aminopyridine derivatives I [wherein R4 = independently H, halo, alkyl, (un)substituted NH2, etc.; A2 = substituted Ph, pyridyl, or pyrimidinyl; A5 = substituted heterocyclyl] or pharmaceutically acceptable salts thereof as inhibitors of protein kinase, specifically anaplastic lymphoma kinase (ALK), for treating non-small-cell lung cancer, anaplastic large cell lymphoma, inflammatory myofibroma, nasopharyngeal carcinoma, breast cancer, colorectal cancer, diffuse large B cell lymphoma, systemic histiocytosis, and neuroblastoma. For example, II was prepared in a multi-step synthesis, which showed inhibitory activity with IC50 of 9.8 nM against ALK. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Formula: C6H5Br2NO

The Article related to preparation aminopyridine alk inhibitor treatment cancer human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Formula: C6H5Br2NO

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 7, 2014, Xiao, Dengming; Xu, Xinhe; Liu, Xijie; Hu, Yuandong; Yu, Honghao; Liu, Zhihua; Peng, Yong; Sun, Yinghui; Luo, Hong; Kong, Fansheng; Han, Yongxin; Sun, Jian published a patent.Application of 25813-24-5 The title of the patent was Preparation of substituted 2-aminopyridine derivatives as protein kinase inhibitors. And the patent contained the following:

The present invention discloses substituted 2-aminopyridine derivatives I [wherein A1 = H, substituted aryl, aryloxymethyl, etc.; A2 = substituted Ph, pyridyl, pyrimidinyl, or pyrazolyl; A3 = H, arylamino, substituted heteroaryl, etc.; A5 = substituted heterocyclyl; with the proviso that at least one of A1 or A3 is H] or pharmaceutically acceptable salts thereof as inhibitors of protein kinase, specifically anaplastic lymphoma kinase (ALK), for treating non-small-cell lung cancer, anaplastic large cell lymphoma, inflammatory myofibroma, nasopharyngeal carcinoma, breast cancer, colorectal cancer, diffuse large B cell lymphoma, systemic histiocytosis, and neuroblastoma. For example, II was prepared in a multi-step synthesis, which showed inhibitory activity with IC50 of 9.8 nM against ALK. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Application of 25813-24-5

The Article related to preparation aminopyridine alk inhibitor treatment cancer human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 25813-24-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 6, 2014, Xiao, Dengming; Xu, Xinhe; Liu, Xijie; Hu, Yuandong; Yu, Honghao; Liu, Zhihua; Peng, Yong; Sun, Yinghui; Luo, Hong; Kong, Fansheng; Han, Yongxin; Sun, Jian published a patent.Safety of 3,5-Dibromo-4-methoxypyridine The title of the patent was Preparation of substituted 2-aminopyridine derivatives as protein kinase inhibitors. And the patent contained the following:

The present invention discloses substituted 2-aminopyridine derivatives I [wherein A1 = H, substituted aryl, aryloxymethyl, etc.; A2 = substituted Ph, pyridyl, pyrimidinyl, or pyrazolyl; A3 = H, arylamino, substituted heteroaryl, etc.; A5 = substituted heterocyclyl; with the proviso that at least one of A1 or A3 is H] or pharmaceutically acceptable salts thereof as inhibitors of protein kinase, specifically anaplastic lymphoma kinase (ALK), for treating non-small-cell lung cancer, anaplastic large cell lymphoma, inflammatory myofibroma, nasopharyngeal carcinoma, breast cancer, colorectal cancer, diffuse large B cell lymphoma, systemic histiocytosis, and neuroblastoma. For example, II was prepared in a multi-step synthesis, which showed inhibitory activity with IC50 of 9.8 nM against ALK. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Safety of 3,5-Dibromo-4-methoxypyridine

The Article related to preparation aminopyridine alk inhibitor treatment cancer human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Safety of 3,5-Dibromo-4-methoxypyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On May 22, 2014, Chatterjee, Arnab Kumar; Nagle, Advait Suresh; Paraselli, Prasuna; Leong, Seh Yong; Roland, Jason Thomas; Mishra, Pranab Kumar; Yeung, Bryan K. S.; Zou, Bin published a patent.Formula: C7H10N2 The title of the patent was Preparation of imidazopyrazines for treating parasitic diseases. And the patent contained the following:

The invention is related to the preparation of title compounds I [n = 0-2; p = 0-3; A = aryl, heteroaryl, and fused bycyclyl comprising a heterocycloalkyl fused to a phenyl; B = the imidazo[1,2-a]pyrazine fused ring depicted in I; D = Ph, heteroaryl, cycloalkyl, heterocycloalkyl, fused bicyclyl comprising a heterocycloalkyl fused to a phenyl; L = *CO, alkylene, *NR2CO, *CH2NR2, etc.; * represents the point of attachment of L to ring B; R2 = H, alkyl, R0-alkylene ; R0 = alkoxyamino, heteroaryl, alkylamino, etc.; R1 = independently at each occurrence halo, CN, NH2 and derivatives; R15, R16 = independently H, alkyl, haloalkyl; R17 = independently at each occurrence halo, OH and derivatives, SO2NH2 and derivatives, etc.], or a pharmaceutical acceptable salt, tautomer or stereoisomer, useful for treating, preventing, inhibiting, ameliorating, or eradicating the pathol. and/or symptomol. of a disease, such as malaria, caused by a Plasmodium parasite. Thus, a multi-step synthesis starting from chloroacetaldehyde and 5-amino-2-pyrazinecarboxylic acid Et ester was given for II. I were tested for their capacity to inhibit proliferation of parasitemia in 3D7 Plasmodium falciparum infected red blood cells and had EC50 of 10 μM or less. I showed delay of the proliferation of P. yoelii in liver cells in a P. yoelii sporozoite invasion assay (EC50 for II = 14 nM). The experimental process involved the reaction of N,3-Dimethylpyridin-2-amine(cas: 156267-13-9).Formula: C7H10N2

The Article related to imidazopyrazine preparation antimalarial plasmodium falciparum, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Formula: C7H10N2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem