Category: 1820711-82-7

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 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 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

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 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 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

On October 1, 2019, Sun, Jiyun; Tang, Ruikun; Wang, Lu; Xu, Hao; Zhang, Xiaofei; Fan, Wei published a patent.Product Details of 1820711-82-7 The title of the patent was GluN2B subunit-targeted positron tracer for central nervous system and preparation thereof. And the patent contained the following:

The invention relates to GluN2B subunit-targeted positron tracer for central nervous system and preparation thereof, which has the advantages of stable structure, low metabolic rate, good electron tracing effect, mild reaction condition and high purity. In particular, the present invention relates to GluN2B subunit-targeted positron tracer for central nervous system with general formula I, wherein, R1 = Ph, benzene derivative, thienyl, thiophene derivatives GluN2B subunit-targeted positron tracer for central nervous system with general formulaIwas prepared by the following steps: methylation of the intermediate II with 11CH3I to obtain final product. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).Product Details of 1820711-82-7

The Article related to glun2b subunit targeted positron tracer preparation central nervous system, 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.Product Details of 1820711-82-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 31, 2021, Sun, Ji-yun; Kumata, Katsushi; Chen, Zhen; Zhang, Yi-ding; Chen, Jia-hui; Hatori, Akiko; Fu, Hua-long; Rong, Jian; Deng, Xiao-yun; Yamasaki, Tomoteru; Xie, Lin; Hu, Kuan; Fujinaga, Masayuki; Yu, Qing-zhen; Shao, Tuo; Collier, Thomas Lee; Josephson, Lee; Shao, Yi-han; Du, Yun-fei; Wang, Lu; Xu, Hao; Zhang, Ming-rong; Liang, Steven H. published an article.Electric Literature of 1820711-82-7 The title of the article was Synthesis and preliminary evaluation of novel 11C-labeled GluN2B-selective NMDA receptor negative allosteric modulators. And the article contained the following:

Abstract: N-methyl-D-aspartate receptors (NMDARs) play critical roles in the physiol. function of the mammalian central nervous system (CNS), including learning, memory, and synaptic plasticity, through modulating excitatory neurotransmission. Attributed to etiopathol. of various CNS disorders and neurodegenerative diseases, GluN2B is one of the most well-studied subtypes in preclin. and clin. studies on NMDARs. Herein, we report the synthesis and preclin. evaluation of two 11C-labeled GluN2B-selective neg. allosteric modulators (NAMs) containing N,N-dimethyl-2-(1H-pyrrolo[3,2-b]pyridin-1-yl)acetamides for positron emission tomog. (PET) imaging. Two PET ligands, namely [11C]31 and [11C]37 (also called N2B-1810 and N2B-1903, resp.) were labeled with [11C]CH3I in good radiochem. yields (decay-corrected 28% and 32% relative to starting [11C]CO2, resp.), high radiochem. purity (>99%) and high molar activity (>74 GBq/μmol). In particular, PET ligand [11C]31 demonstrated moderate specific binding to GluN2B subtype by in vitro autoradiog. studies. However, because in vivo PET imaging studies showed limited brain uptake of [11C]31 (up to 0.5 SUV), further medicinal chem. and ADME optimization are necessary for this chemotype attributed to low binding specificity and rapid metabolism in vivo. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).Electric Literature of 1820711-82-7

The Article related to glun2b receptor neg allosteric modulator pet imaging radiotracer brain, glun2b subunit, nmdars, carbon-11, ionotropic glutamate receptors (iglurs), positron emission tomography (pet) and other aspects.Electric Literature of 1820711-82-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem