Tag: 200-300

On February 5, 2004, Kwan, Tricia Ann; Lagreca, Susan Deborah; Lippa, Blaise Scott; Morris, Joel; Wessel, Matthew David published a patent.Formula: C8H10BrN The title of the patent was Preparation of isothiazole derivatives as anticancer agents. And the patent contained the following:

The title compounds I [X = O or S; R1 = (substituted)heterocyclic aromatic ring; R2 = H, (cyclo)alkyl, alkenyl, alkynyl, etc.] were prepared Compounds I are useful as as anticancer agents (no data). Thus, reaction of 3-methanesulfonyl-5-(pyridin-4-ylamino)-isothiazole-4-carboxylic acid amide (preparation given) with (4-chlorophenyl)-methanethiol yielded compound II. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Formula: C8H10BrN

The Article related to isothiazole derivative preparation anticancer, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Formula: C8H10BrN

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On September 30, 2021, Zhou, Enxing; Liu, Yuan; Wang, Hanping; Wang, Jing; Shao, Ning; Wu, Guanglong published a patent.Recommanded Product: 908267-63-0 The title of the patent was Preparation of heteroaryl compounds as casein kinase inhibitors. And the patent contained the following:

The title compounds with general formula I [wherein R1 = halogen; n = 0-2, X = independently C or N; R2 = absent or O; R3 = absent or CN; A = absent, a 4- to 7- membered (un)substituted cycloalkyl, heterocycloalkyl, a 5- to 6- membered (un)substituted heteroaryl, etc.; ring B = a 4- to 7-membered (un)substituted cycloalkyl, heterocycloalkyl, or a 5- to 6-membered (un)substituted heteroaryl, wherein up to 2 carbon atoms are replaced with a heteroatom selected from =N- or -O-] or pharmaceutically acceptable salts thereof were prepared novel casein kinase inhibitors. For example, compound II was prepared in a multi-step synthesis. Corresponding pharmaceutical compositions were also disclosed for the treatment of mood disorder, depression, bipolar disorder, solid tumor, blood cancer, lymphoma, breast cancer, melanoma, leukemia, liver cancer, and brain cancer. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Recommanded Product: 908267-63-0

The Article related to preparation heteroaryl pyrazolopyrazine pyrimidine imidazopyrazine furopyridine, human casein kinase inhibitor treatment mood disorder cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 12, 1996, Kelly, T. Ross; Lang, Fengrui published an article.Safety of Methyl 6-bromo-5-methoxypicolinate The title of the article was Total Synthesis of Dimethyl Sulfomycinamate. And the article contained the following:

Di-Me sulfomycinamate, a methanolysis product from the natural antibiotic sulfomycin I, is synthesized in 11 steps. The chem. of various pyridine, thiazole, and oxazole heterocycles and their coupling reactions under palladium catalysis are examined The key transformations in the synthesis are the selective palladium-catalyzed coupling reactions on a doubly-activated pyridine and the condensation reaction between bromo ketone and amide to form the oxazole moiety. The first preparation of oxazole triflates is described, as is some of their chem. properties. The experimental process involved the reaction of Methyl 6-bromo-5-methoxypicolinate(cas: 170235-18-4).Safety of Methyl 6-bromo-5-methoxypicolinate

The Article related to sulfomycinamate preparation, oxazole triflate preparation coupling reaction, pyridyl triflate preparation coupling thiazole, Biomolecules and Their Synthetic Analogs: Other Bacterial and Fungal Metabolites and other aspects.Safety of Methyl 6-bromo-5-methoxypicolinate

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On May 11, 2018, Crowley, Brendan M.; Bell, Ian M.; Harvey, Andrew John; Campbell, Brian T.; Greshock, Thomas J.; Rada, Vanessa L. published a patent.Product Details of 908267-63-0 The title of the patent was Preparation of substituted 6-membered aryl or heteroaryl allosteric modulators of nicotinic acetylcholine receptors. And the patent contained the following:

The present disclosure relates to compounds of formula I that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer’s disease, Parkinson’s disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation. Compounds of formula I wherein X is SONH2 and derivatives, OSONH2 and derivatives, SO2H and SO2-C1-4 alkyl; Y is from 1 to 4 substituents and each are independently H, (un)substituted C1-4 alkyl, halo and OH; A is substituted 6-membered aryl and heteroaryl; R3 and R4 are independently H, halo and (un)substituted C1-4 alkyl; R3R4 can be taken together to form (un)substituted cyclopropyl, (un)substituted cyclobutyl, (un)substituted cyclopentyl and (un)substituted cyclohexyl; R5 and R6 are independently H and C1-4 alkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cyclization of (1R,3R)-2,2-dimethyl-3-(4-sulfamoylphenyl)cyclopropanecarboximidamide with 3-(dimethylamino)-1-[5-(trifluoromethyl)pyridin-3-yl]prop-2-en-1-one. The invention compounds were evaluated for their α7 nAChR modulatory activity (some data given). The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Product Details of 908267-63-0

The Article related to heteroaryl phenylcyclopropane preparation nicotinic acetylcholine receptor modulator allosteric modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Product Details of 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On September 11, 2014, Wang, Shaomeng; Ran, Xu; Zhao, Yujun; Yang, Chao-Yie; Liu, Liu; Bai, Longchuan; McEachern, Donna; Stuckey, Jeanne; Meagher, Jennifer Lynn; Sun, Duxin; Li, Xiaoqin; Zhou, Bing; Karatas, Hacer; Luo, Ruijuan; Chinnaiyan, Arul; Asangani, Irfan A. published a patent.Quality Control of 4-Bromo-2-isopropylpyridine The title of the patent was Preparation of pyridoindole, pyridazinoindole and pyrimidinoindole compounds as BET bromodomain inhibitors. And the patent contained the following:

The title compounds I [X = NRa, O or S; Y1, Y3 = CH or N; Y2 = CH, CRa (wherein Ra = H, alkyl, benzyl), or absent; Z = H, II (wherein B = (un)substituted aryl, heteroaryl, heterocycloalkyl, etc.; Rb = alkyl, halo, aryl, etc.; n = 0-3), G(L)C(Rc)3 (G = N, O, or S; L = absent, H, C(Rd)3; Rc, Rd = H, alkyl, (un)substituted aryl, etc.), halo, OH, or absent; A = (un)substituted 5-membered heterocyclyl; R1 = H, halo, OH, etc.] that are inhibitors of BET bromodomains useful in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, were prepared E.g., a multi-step synthesis of III, starting from 4-hydroxypyridin-2(1H)-one, was described. The ability of exemplified compounds I to bind to BET bromodomain proteins was evaluated (data given for representative compounds I). Pharmaceutical compositions comprising compound I, alone or in combination with second therapeutic agent, surgery and radiation, were disclosed. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Quality Control of 4-Bromo-2-isopropylpyridine

The Article related to pyridoindole pyridazinoindole pyrimidinoindole preparation bet bromodomain inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 4-Bromo-2-isopropylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 2, 2021, Bartolozzi, Alessandra; Proudfoot, John Robert; Briggs, Timothy; Mancuso, John; Bos, Maxence; Guo, Tianlin; Ly, Vu Linh; Blois, Anna; Lanter, Bernard; Taylor, Steven John; Buckbinder, Leonard published a patent.Synthetic Route of 1820711-82-7 The title of the patent was Synthesis of fused azole heterocycles as AHR antagonists treating cancers. And the patent contained the following:

The synthesis of fused azole heterocycles, I, wherein the dashed bonds can be independently single or double bonds; X can selectively be N, S,CH, or NH depending on bond arrangements; Y can independently be N or CH as it relates to the fused azole; ring A and B are chosen from optionally substituted aryl, heteraryl, cycloalkyl or heterocycloalky moieties; and L is chosen from a bond and -NT-C(O)-, wherein T can be H or Me are presented as pharmaceutically acceptable salts for treating or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling. Of note, II was synthesized and demonstrated an HEPG2 Luc IC50 of less than 100 nM; an aqueous solubility of less than 0.1μM at pH 7/4; and a human hepatocyte clearance of between 20 and 50 mL/min/Kg. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).Synthetic Route of 1820711-82-7

The Article related to fused azole heterocycle ahr antagonist anticancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 1820711-82-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On June 5, 2014, Scobie, Martin; Helleday, Thomas; Koolmeister, Tobias; Jacques, Sylvain; Desroses, Matthieu; Jacques-Cordonnier, Marie-Caroline published a patent.SDS of cas: 199522-66-2 The title of the patent was Preparation of pyrimidine-2,4-diamine derivatives for treatment of cancer. And the patent contained the following:

A compound of formula I, or a pharmaceutically acceptable salt thereof, is useful in the treatment of cancer or other diseases that may benefit from inhibition of MTH1. Compounds of formula I wherein R1 is (un)substituted heteroaryl and (un)substituted aryl; R2 is H, halo, CN, (un)substituted C1-12 alkyl, etc.; R3 is (un)substituted C1-12 alkyl and (un)substituted heterocycloalkyl; R2R3 can be taken together to form 5- to 8-membered nonaromatic ring; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of 4-chloro-6-phenylpyrimidin-2-amine with cyclohexanamine. The invention compounds were evaluated for their MTH1 inhibitory activity (data given). The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).SDS of cas: 199522-66-2

The Article related to pyrimidinediamine preparation treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 199522-66-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On April 7, 2022, Borjesson, Ulf; Perry, Matthew William Dampier; Grebner, Christoph; Michaelides, Iacovos Neal; Hayhow, Thomas George Christopher; Kettle, Jason Grant; Collie, Gavin William; Storer, Robert Ian; Bagal, Sharanjeet Kaur; Fallan, Charlene published a patent.SDS of cas: 1820711-82-7 The title of the patent was Synthesis of heterocyclic substituted pyrimidine anticancer agents. And the patent contained the following:

The synthesis of heterocyclic substituted pyrimidine anticancer agents I, wherein A is a protein binder unit; Z can be a bicyclic heterocyclic ring system with multiple heteroaroms N, O, S; Y can be a pyrimidine dione moiety; R can be a substituent on any available C or N such that alkyl, alkenyl, alkynyl or related groups with optional halo, nitrile, amino or similar groups; L, as a linker, can be an (un)saturated framework comprising C and H atoms and at least one heteroatom; and n can be an integer between 0-3 are prepared as pharmaceutically acceptable salts. Of note, II demonstrated a Cereblon HTRF IC50 binding of 2.1μM and can be employed in the treatment of cancers in humans or animals such that solid tumors, BRD4-sensitive tumors. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).SDS of cas: 1820711-82-7

The Article related to heterocyclic pyrimidine anticancer preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 1820711-82-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 10, 2015, Scobie, Martin; Wallner, Olov; Koolmeister, Tobias; Vallin, Karl Sven Axel; Henriksson, Carl Martin; Homan, Evert; Helleday, Thomas; Jacques, Sylvain; Desroses, Matthieu; Jacques-Cordonnier, Marie-Caroline; Fiskesund, Roland Julius Yu published a patent.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine The title of the patent was Diaminopyrimidines as MTH1 inhibitors for treatment of inflammatory and autoimmune conditions and their preparation. And the patent contained the following:

A compound of formula I, or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions. Compounds of formula I wherein R2 is (un)substituted Ph, substituted 6-membered heteroaryl, 5- to 10-membered (mono/bi)cyclic heteroaryl, etc.; R2 is H, halo, CN, (un)substituted C1-3 alkyl, etc.; R3 is X-L-J, (un)substituted C1-12 alkyl and (un)substituted heterocycloalkyl; X is (un)substituted C1-6 alkylene, and (un)substituted C0-2 alkyl-heterocycloalkylene-C0-2 alkyl; L is single bond, O, S, O-C1-6 alkylene, etc.; J is (un)substituted 6- to 10-membered aryl and (un)substituted 5- to 11-membered (mono/bi)cyclic heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of 4-chloro-6-phenylpyrimidin-2-amine with cyclohexanamine. The invention compounds were evaluated for their MTH1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of less than 200 nM. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

The Article related to diaminopyrimidine preparation mth1 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 30, 2018, Bartolome-Nebreda, Jose Manuel; Trabanco-Suarez, Andres Avelino; Alcazar-Vaca, Manuel Jesus published a patent.Related Products of 1820711-82-7 The title of the patent was [1,2,4]Triazolo[1,5-a]pyrimidinyl derivatives substituted with piperidine, morpholine or piperazine as OGA inhibitors and their preparation. And the patent contained the following:

The invention relates to compounds of formula I as O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising compounds of formula I, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer’s disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathol., in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations. Compounds of formula I wherein X1 and X3 are independently CRxa, N and NH and derivatives; X2 is CH; X4 is C and N; X5, X6, X7 and X8 are independently C, CRxb and N; with the proviso that at least one of X1 and X3 is N and NH and derivatives; Rxa and Rxb are independently H, halo, CN, (un)substituted C1-4 alkyl, etc.; La is a bond, CHR1, O and NR1; Ra is CHR1, O, NR1, (un)substituted piperidinyl, (un)substituted morpholinyl, etc.; R1 is H and (un)substituted C1-4 alkyl; dashed bonds are single and double bonds; and tautomers and stereoisomeric forms thereof, are claimed. Example compound II was prepared by N-sulfonylation of 7-((3R)-piperidin-3-yl)-[1,2,4]triazolo[1,5-a]pyrimidine with 2-acetylaminothiazole-5-sulfonyl chloride. The invention compounds were evaluated for their OGA inhibitory activity. From the assay, it was determined that compound II exhibited pIC50 value of 6.06 and Emax of 94.20 %. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).Related Products of 1820711-82-7

The Article related to triazolopyrimidine preparation oga inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 1820711-82-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem