Category: 868551-99-9

On August 25, 2022, Lee, Hee Jin; Park, Jin Young; Lee, Hye Mi; Yang, Deok Mo; Nam, Eun Hye; Kim, Hak Do; Jung, Hui Jin; Choung, Won Ken published a patent.SDS of cas: 868551-99-9 The title of the patent was Preparation of pyrimidine-fused ring compounds with DNA-PK inhibition activity and use thereof. And the patent contained the following:

The invention relates to a pyrimidine-fused ring compounds of formula I, stereoisomers, pharmaceutically acceptable salts, or pharmaceutical compositions thereof that are useful for the prevention or treatment of cancer. The pyrimidine-fused ring compounds of the present invention exhibits excellent inhibitory activity against DNA-PK and thus can be advantageously used as a therapeutic agent for DNA-PK-related diseases. Compounds of formula I wherein the normalized bond is a single or double bond; n is 0-2; X1 is NR1 or CR2R3; X2 and X3 are independently -CR2R3-, -CR2-, -(C=O)-, or -(C=S)-; L1 is null or alkylene; Y is alkoxy, Q1, Q2, or (un)substituted (hetero)aryl; W1 is -CH2-, -NH-, -O-, or -S-; W2 is -CH- or -N-; a – d are independently 0-3; L2 is null or alkylene; Z is -Z1-L3-Z2; Z1 is (un)substituted (hetero)aryl or (un)substituted benzene-fused ring; L3 is alkylene, -(C=O)-, -(C=O)NH-, -NH-, etc.; Z2 is H, alkyl, hydroxyalkyl, alkoxyalkyl, etc.; R is H or alkyl; R1 – R3 are independently H or alkyl; are claimed. Example compound II was prepared by palladium-catalyzed cross-coupling reaction of 2-chloro-7-methyl-9-(tetrahydro-2H-pyran-4-yl)-7,9-dihydro-8H-purin-8-one with 2,5-dimethylbenzo[d]thiazol-6-amine in 11% yield. The invention compounds were evaluated for the DNA-pk inhibition activity (biol. data given). The experimental process involved the reaction of Methyl 5-amino-4-methylpicolinate(cas: 868551-99-9).SDS of cas: 868551-99-9

The Article related to pyrimidine fused ring preparation dnapk inhibition cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 868551-99-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 25, 2022, Lee, Hee Jin; Park, Jin Young; Lee, Hye Mi; Yang, Deok Mo; Nam, Eun Hye; Kim, Hak Do; Jung, Hui Jin; Choung, Won Ken published a patent.SDS of cas: 868551-99-9 The title of the patent was Preparation of pyrimidine-fused ring compounds with DNA-PK inhibition activity and use thereof. And the patent contained the following:

The invention relates to a pyrimidine-fused ring compounds of formula I, stereoisomers, pharmaceutically acceptable salts, or pharmaceutical compositions thereof that are useful for the prevention or treatment of cancer. The pyrimidine-fused ring compounds of the present invention exhibits excellent inhibitory activity against DNA-PK and thus can be advantageously used as a therapeutic agent for DNA-PK-related diseases. Compounds of formula I wherein the normalized bond is a single or double bond; n is 0-2; X1 is NR1 or CR2R3; X2 and X3 are independently -CR2R3-, -CR2-, -(C=O)-, or -(C=S)-; L1 is null or alkylene; Y is alkoxy, Q1, Q2, or (un)substituted (hetero)aryl; W1 is -CH2-, -NH-, -O-, or -S-; W2 is -CH- or -N-; a – d are independently 0-3; L2 is null or alkylene; Z is -Z1-L3-Z2; Z1 is (un)substituted (hetero)aryl or (un)substituted benzene-fused ring; L3 is alkylene, -(C=O)-, -(C=O)NH-, -NH-, etc.; Z2 is H, alkyl, hydroxyalkyl, alkoxyalkyl, etc.; R is H or alkyl; R1 – R3 are independently H or alkyl; are claimed. Example compound II was prepared by palladium-catalyzed cross-coupling reaction of 2-chloro-7-methyl-9-(tetrahydro-2H-pyran-4-yl)-7,9-dihydro-8H-purin-8-one with 2,5-dimethylbenzo[d]thiazol-6-amine in 11% yield. The invention compounds were evaluated for the DNA-pk inhibition activity (biol. data given). The experimental process involved the reaction of Methyl 5-amino-4-methylpicolinate(cas: 868551-99-9).SDS of cas: 868551-99-9

The Article related to pyrimidine fused ring preparation dnapk inhibition cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 868551-99-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On November 3, 2005, Dress, Klaus Ruprecht; Hu, Qiyue; Johnson, Ted William; Plewe, Michael Bruno; Tanis, Steven Paul; Wang, Hai; Yang, Anle; Yin, Chunfeng; Zhang, Junhu published a patent.Category: pyridine-derivatives The title of the patent was Preparation of N-hydroxy pyrrolopyrimidinecarboxamides as inhibitors of HIV integrase.. And the patent contained the following:

Title compounds [I; R1 = H, (substituted) alkyl, alkenyl, heteroalkyl; R2, R5 = H; R3 = (CR8R9)tNR10R11, (substituted) heteroalkyl; R4 = H, halo, alkyl, heteroalkyl, (substituted) alkenyl, alkynyl, OR12a, NR12aR12b; R6 = H, alkyl, heteroalkyl, (substituted) alkenyl; R8, R9 = H, alkyl; R10R11N = (substituted) cycloheteroalkyl; R12a, R12b, R12c = H, alkyl; t = 1-3], were prepared Thus, 1-(2,4-difluorobenzyl)-1H-pyrrolo[2,3-c]pyridine-5-carboxylic acid (preparation given) was stirred with O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate, Et3N, and NH2OH.HCl in DMF for 16 h to give 48% N-hydroxy-1-(2,4-difluorobenzyl)-1H-pyrrolo[2,3-c]pyridine-5-carboxamide. The latter showed an EC50 = 0.00795 μM in an HIV-1 cell protection assay. The experimental process involved the reaction of Methyl 5-amino-4-methylpicolinate(cas: 868551-99-9).Category: pyridine-derivatives

The Article related to pyrrolopyrimidinecarboxamide hydroxy preparation hiv integrase inhibitor, aids arc treatment hydroxamide pyrrolopyrimidine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On January 17, 2019, Ahmad, Nadia; Anderson, Corey; Arumugam, Vijayalaksmi; Asgian, Iuliana Luci; Camp, Joanne Louise; Fanning, Lev Tyler Dewey; Hadida Ruah, Sara Sabina; Hurley, Dennis; Schmidt, Yvonne; Shaw, David; Sheth, Urvi Jagdishbhai; Thomson, Stephen Andrew published a patent.Recommanded Product: Methyl 5-amino-4-methylpicolinate The title of the patent was Preparation of (hetero)aromatic carboxamides as modulators of sodium channels for the treatment of diseases. And the patent contained the following:

The invention relates to preparation of aryl heteroaryl carboxamides and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels. The example compound I was prepared by multistep synthesis (procedure given). Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain. The experimental process involved the reaction of Methyl 5-amino-4-methylpicolinate(cas: 868551-99-9).Recommanded Product: Methyl 5-amino-4-methylpicolinate

The Article related to aryl heteroaryl carboxamide preparation sodium channel modulator disease treatment, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Recommanded Product: Methyl 5-amino-4-methylpicolinate

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On June 5, 2014, Walsh, Shawn P.; Cato, Brian; Frie, Jessica L.; Kim, Dooseop; Pasternak, Alexander; Shi, Zhi-Cai published a patent.Recommanded Product: 868551-99-9 The title of the patent was Preparation of piperidine derivatives as inhibitors of the renal outer medullary potassium channel for treating cardiovascular diseases and edematous conditions. And the patent contained the following:

The present invention provides compounds of Formula I (wherein n = 0-1; the N-containing ring system is (un)substituted piperidinyl, etc.; R1 is -H, -OC1-3alkyl or -OH; R2 is -H or C1-3alkyl; R3 is -H, -F, -C1-3 alkyl or phenyl; or when n is 0, R2 and R3 are joined together to form a 4-6 member ring with the nitrogen and carbon to which each is attached; R4 and R5 are each independently -H or -C1-3-alkyl, or R4 and R5 are joined together with the carbon to which they are attached to form C3-6 cycloalkyl; Z1 is (un)substituted Ph, (un)substituted benzofuranyl, or (un)substituted benzopyranyl, and Z2 is a substituted N-containing heterocyclyl, (un)substituted Ph, etc.), and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention. Synthetic procedures for preparing I are exemplified. Example compound II was prepared by reacting intermediates 1-oxo-N-(piperidin-4-yl)-1,3-dihydroisobenzofuran-5-carboxamide hydrochloride and (4-methyl-1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetaldehyde. In the ROMK channel functional thallium flux assay, II had an IC50 of 0.01 μM. The experimental process involved the reaction of Methyl 5-amino-4-methylpicolinate(cas: 868551-99-9).Recommanded Product: 868551-99-9

The Article related to preparation piperidine derivative inhibitor renal medullary potassium channel, cardiovascular disease piperidine derivative inhibitor renal medullary potassium channel, edema treatment piperidine derivative inhibitor renal medullary potassium channel and other aspects.Recommanded Product: 868551-99-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On June 5, 2014, Walsh, Shawn P.; Cato, Brian; Frie, Jessica L.; Kim, Dooseop; Pasternak, Alexander; Shi, Zhi-Cai published a patent.Recommanded Product: 868551-99-9 The title of the patent was Preparation of piperidine derivatives as inhibitors of the renal outer medullary potassium channel for treating cardiovascular diseases and edematous conditions. And the patent contained the following:

The present invention provides compounds of Formula I (wherein n = 0-1; the N-containing ring system is (un)substituted piperidinyl, etc.; R1 is -H, -OC1-3alkyl or -OH; R2 is -H or C1-3alkyl; R3 is -H, -F, -C1-3 alkyl or phenyl; or when n is 0, R2 and R3 are joined together to form a 4-6 member ring with the nitrogen and carbon to which each is attached; R4 and R5 are each independently -H or -C1-3-alkyl, or R4 and R5 are joined together with the carbon to which they are attached to form C3-6 cycloalkyl; Z1 is (un)substituted Ph, (un)substituted benzofuranyl, or (un)substituted benzopyranyl, and Z2 is a substituted N-containing heterocyclyl, (un)substituted Ph, etc.), and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention. Synthetic procedures for preparing I are exemplified. Example compound II was prepared by reacting intermediates 1-oxo-N-(piperidin-4-yl)-1,3-dihydroisobenzofuran-5-carboxamide hydrochloride and (4-methyl-1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetaldehyde. In the ROMK channel functional thallium flux assay, II had an IC50 of 0.01 μM. The experimental process involved the reaction of Methyl 5-amino-4-methylpicolinate(cas: 868551-99-9).Recommanded Product: 868551-99-9

The Article related to preparation piperidine derivative inhibitor renal medullary potassium channel, cardiovascular disease piperidine derivative inhibitor renal medullary potassium channel, edema treatment piperidine derivative inhibitor renal medullary potassium channel and other aspects.Recommanded Product: 868551-99-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem