Category: 362703-57-9

On May 15, 2006, Gilmore, John L.; King, Bryan W.; Harris, Cathy; Maduskuie, Thomas; Mercer, Stephen E.; Liu, Rui-Qin; Covington, Maryanne B.; Qian, Mingxin; Ribadeneria, Maria D.; Vaddi, Krishna; Trzaskos, James M.; Newton, Robert C.; Decicco, Carl P.; Duan, James J.-W. published an article.Safety of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate The title of the article was Synthesis and structure-activity relationship of a novel, achiral series of TNF-α converting enzyme inhibitors. And the article contained the following:

A novel series of achiral TNF-α converting enzyme (TACE) inhibitors has been discovered. These compounds exhibited activities from 0.35 to 11 nM in a porcine TACE assay and inhibited TNF-α production in an LPS-stimulated whole blood assay with an IC50 value of 23 nM for the most potent one. They also have excellent selectivities over related metalloproteases including aggrecanases. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Safety of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate

The Article related to metalloprotease preparation sar tnf tumor necrosis factor inhibitor, Pharmacology: Structure-Activity and other aspects.Safety of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On May 15, 2006, Gilmore, John L.; King, Bryan W.; Harris, Cathy; Maduskuie, Thomas; Mercer, Stephen E.; Liu, Rui-Qin; Covington, Maryanne B.; Qian, Mingxin; Ribadeneria, Maria D.; Vaddi, Krishna; Trzaskos, James M.; Newton, Robert C.; Decicco, Carl P.; Duan, James J.-W. published an article.Safety of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate The title of the article was Synthesis and structure-activity relationship of a novel, achiral series of TNF-α converting enzyme inhibitors. And the article contained the following:

A novel series of achiral TNF-α converting enzyme (TACE) inhibitors has been discovered. These compounds exhibited activities from 0.35 to 11 nM in a porcine TACE assay and inhibited TNF-α production in an LPS-stimulated whole blood assay with an IC50 value of 23 nM for the most potent one. They also have excellent selectivities over related metalloproteases including aggrecanases. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Safety of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate

The Article related to metalloprotease preparation sar tnf tumor necrosis factor inhibitor, Pharmacology: Structure-Activity and other aspects.Safety of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 12, 2014, Frei, Beat; Gobbi, Luca; Grether, Uwe; Kimbara, Atsushi; Nettekoven, Matthias; Roever, Stephan; Rogers-Evans, Mark; Schulz-Gasch, Tanja published a patent.Safety of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate The title of the patent was Preparation of novel pyridine derivatives as cannabinoid receptor 2 agonists. And the patent contained the following:

The title compounds I [R1 = halo, cycloalkylalkoxy, alkylsulfonyl, etc.; R2 = halo, cycloalkyl, haloalkyl, etc.; R3 = (alkyl)(oxo)pyrrolidinyl or C(R4R5)C(R6R7)C(O)R8; R4, R5 = H, alkyl, Ph, etc.; or R4 and R5 together with the carbon atom to which they are attached form cycloalkyl, oxetanyl, thiethanyl, etc.; R6, R7 = H, alkyl; or one of R4 and R5 and one of R6 and R7, together with the carbon atoms to which they are attached, form cycloalkyl, and the other ones are both hydrogen at the same time; R8 = NH2, alkoxy, alkylamino, OH], useful as CB2 receptor agonists were prepared and formulated. E.g., a multi-step synthesis of the amide II, starting from Me 5-bromo-pyridine-2-carboxylate, was described. The exemplified compounds I showed an excellent affinity for the CB2 receptor with affinities below 10 μM (specific data given). The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Safety of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate

The Article related to pyridine amide preparation cannabinoid receptor 2 cb2 agonist, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Safety of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 10, 2015, Takayama, Tetsuo; Shibata, Tsuyoshi; Shiozawa, Fumiyasu; Kawabe, Kenichi; Shimizu, Yuki; Hamada, Makoto; Hiradate, Akira; Takahashi, Masato; Ushiyama, Fumihito; Oi, Takahiro; Shirasaki, Yoshihisa; Matsuda, Daisuke; Koizumi, Chie; Kato, Sota published a patent.Synthetic Route of 362703-57-9 The title of the patent was Pharmaceutical compositions containing N-[[1-[[6-(4-chlorophenoxy)-3-pyridinyl]methyl]-4-hydroxy-2-oxo-1,2,5,6-tetrahydro-3-pyridinyl]carbonyl]glycine as prolyl hydroxylase 2 (PHD2) inhibitor. And the patent contained the following:

Oral solid pharmaceutical compositions contain N-[[1-[[6-(4-chlorophenoxy)-3-pyridinyl]methyl]-4-hydroxy-2-oxo-1,2,5,6-tetrahydro-3-pyridinyl]carbonyl]glycine or its pharmaceutically acceptable salt as active ingredient. The compound inhibits PHD2, thus useful for prevention and treatment of anemia. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Synthetic Route of 362703-57-9

The Article related to tetrahydropyridinylcarbonylglycine preparation antianemic prolyl hydroxylase inhibitor oral solid, Pharmacology: Effects Of Cardiovascular, Hematologic, and Renal Drugs and other aspects.Synthetic Route of 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On November 24, 2021, Dorsheimer, Julia R.; Ashley, Melissa A.; Rovis, Tomislav published an article.Synthetic Route of 362703-57-9 The title of the article was Dual Nickel/Photoredox-Catalyzed Deaminative Cross-Coupling of Sterically Hindered Primary Amines. And the article contained the following:

Authors report a method to activate α-3° amines for deaminative arylation via condensation with an electron-rich aldehyde and merge this reactivity with nickel metallaphotoredox to generate benzylic quaternary centers, a common motif in pharmaceuticals and natural products. The reaction is accelerated by added ammonium salts. Evidence is provided in support of two roles for the additive – inhibition of nickel black formation and acceleration of the overall reaction rate. Authors demonstrate a robust scope of amine and haloarene coupling partners and show an expedited synthesis of ALK2 inhibitors. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Synthetic Route of 362703-57-9

The Article related to primary amine deaminative cross coupling nickel photoredox, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: General and other aspects.Synthetic Route of 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 10, 2015, Takayama, Tetsuo; Shibata, Tsuyoshi; Shiozawa, Fumiyasu; Kawabe, Kenichi; Shimizu, Yuki; Hamada, Makoto; Hiradate, Akira; Takahashi, Masato; Ushiyama, Fumihito; Oi, Takahiro; Shirasaki, Yoshihisa; Matsuda, Daisuke; Koizumi, Chie; Kato, Sota published a patent.Synthetic Route of 362703-57-9 The title of the patent was Pharmaceutical compositions containing N-[[1-[[6-(4-chlorophenoxy)-3-pyridinyl]methyl]-4-hydroxy-2-oxo-1,2,5,6-tetrahydro-3-pyridinyl]carbonyl]glycine as prolyl hydroxylase 2 (PHD2) inhibitor. And the patent contained the following:

Oral solid pharmaceutical compositions contain N-[[1-[[6-(4-chlorophenoxy)-3-pyridinyl]methyl]-4-hydroxy-2-oxo-1,2,5,6-tetrahydro-3-pyridinyl]carbonyl]glycine or its pharmaceutically acceptable salt as active ingredient. The compound inhibits PHD2, thus useful for prevention and treatment of anemia. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Synthetic Route of 362703-57-9

The Article related to tetrahydropyridinylcarbonylglycine preparation antianemic prolyl hydroxylase inhibitor oral solid, Pharmacology: Effects Of Cardiovascular, Hematologic, and Renal Drugs and other aspects.Synthetic Route of 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On November 24, 2021, Dorsheimer, Julia R.; Ashley, Melissa A.; Rovis, Tomislav published an article.Synthetic Route of 362703-57-9 The title of the article was Dual Nickel/Photoredox-Catalyzed Deaminative Cross-Coupling of Sterically Hindered Primary Amines. And the article contained the following:

Authors report a method to activate α-3° amines for deaminative arylation via condensation with an electron-rich aldehyde and merge this reactivity with nickel metallaphotoredox to generate benzylic quaternary centers, a common motif in pharmaceuticals and natural products. The reaction is accelerated by added ammonium salts. Evidence is provided in support of two roles for the additive – inhibition of nickel black formation and acceleration of the overall reaction rate. Authors demonstrate a robust scope of amine and haloarene coupling partners and show an expedited synthesis of ALK2 inhibitors. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Synthetic Route of 362703-57-9

The Article related to primary amine deaminative cross coupling nickel photoredox, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: General and other aspects.Synthetic Route of 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On April 23, 2020, Blake, James F.; Boys, Mark Laurence; Chicarelli, Mark Joseph; Cook, Adam; Elsayed, Mohamed S. A.; Fell, Jay B.; Fischer, John P.; Hinklin, Ronald Jay; McNulty, Oren T.; Mejia, Macedonio J.; Rodriguez, Martha E.; Wong, Christina E. published a patent.HPLC of Formula: 362703-57-9 The title of the patent was Preparation of pyridopyrazines and related derivatives as SHP2 protein tyrosine phosphatase inhibitors. And the patent contained the following:

The invention is related to the preparation of compounds I [X1-3independently = CH, N; L1 = a bond, S, CH2, O, NH; R1 = (un)substituted Ph, heteroaryl, bicyclic hetero/aryl, bicyclic heterocyclyl; R2 = ; R48 = H, Me, 4-amino-4-methylpiperidin-1-yl, 1,7-diazaspiro[3.5]nonan-7-yl, 4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl, etc.] , their stereoisomers, tautomers and pharmaceutically acceptable salts, that inhibit SHP2 protein tyrosine phosphatase and are useful for treating hyperproliferative and neoplastic diseases. Methods of using compounds I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathol. conditions are disclosed. Thus, reaction of 6-chloropyrido[2,3-b]pyrazin-2-yl trifluoromethanesulfonate (preparation given) with tert-Bu (4-methylpiperidin-4-yl)carbamate, treatment of tert-Bu [1-(6-chloropyrido[2,3-b]pyrazin-2-yl)-4-methylpiperidin-4-yl]carbamate with 2-amino-3-chloropyridine-4-thiol (preparation given) and cleavage of the tert-butoxycarbonyl group gave II. Certain exemplary compounds were assayed for their SHP2 inhibition activity in an enzymic assay; II showed an iC50 of 33 nM. A cell- based assay was used to determine the effect of SHP2 inhibitors on downstream signaling by assaying ERK1/2 phosphorylation. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).HPLC of Formula: 362703-57-9

The Article related to pyridopyrazine preparation shp2 protein tyrosine phosphatase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.HPLC of Formula: 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 14, 2017, Mainolfi, Nello; Moyer, Mikel P. published a patent.Electric Literature of 362703-57-9 The title of the patent was Indole-2-carboxamides as 3-phosphoglycerate dehydrogenase inhibitors and their preparation. And the patent contained the following:

The invention provides compoundsof formula I, compositions thereof, and methods of using the same. Compounds of formula I wherein R1 and R6 are independently H, C1-4 alkyl; R2 and R3 are independently halo, CN, (un)substituted C1-6 aliphatic, etc.; R4 is H, halo, CN, etc.; R8 os H, CO2H and derivs and (un)substituted C1-6 aliphatic group; R9 is H, halo and (un)substituted C1-4 alkyl; A is (un)saturated 3- to 8-membered carbocyclyl, (un)substituted 7- to 12-membered bicyclic carbocyclyl, (un)saturated 4- to 8-membered heterocyclyl, etc.; L1 is a bond and (un)branched C1-6 bivalent hydrocarbon chain wherein 1 to 5 methylene units may be replaced with O, CO, CO2, etc.; n is 0, 1, 2, 3, 4 and 5; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their PHGDH inhibitory activity (data given). The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Electric Literature of 362703-57-9

The Article related to indole carboxamide 3phosphoglycerate dehydrogenase inhibitor, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Electric Literature of 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On February 6, 2014, Takayama, Tetsuo; Shibata, Tsuyoshi; Shiozawa, Fumiyasu; Kawabe, Kenichi; Shimizu, Yuki; Hamada, Makoto; Hiratate, Akira; Takahashi, Masato; Ushiyama, Fumihito; Oi, Takahiro; Shirasaki, Yoshihisa; Matsuda, Daisuke; Koizumi, Chie; Kato, Sota published a patent.HPLC of Formula: 362703-57-9 The title of the patent was Preparation of partially saturated nitrogen-containing heterocyclic compounds, and PHD2 inhibitors, EPO formation promoters, and antianemic agents containing the heterocyclic compounds. And the patent contained the following:

Provided is a compound which is represented by general formula (I) and has an excellent PHD2-inhibiting activity or a pharmaceutically acceptable salt thereof. (In the general formula (I), W, Y, R2, R3, R4 and Y4 are as defined in the description.). Thus, N-[[4-hydroxy-2-oxo-1-[[4′-(trifluoromethyl)biphenyl-4-yl]methyl]-9-oxa-1-azaspiro[5.5]undeca-3-en-3-yl]carbonyl]glycine (preparation given) at 1 μM inhibited 78% human PHD2 activity in NM_022051-expressing insect HighFive cells. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).HPLC of Formula: 362703-57-9

The Article related to preparation heterocycle phd2 inhibitor epo formation promoter antianemic, oxaazaspiroundecaenylcarbonylglycine preparation phd2 inhibitor epo formation promoter antianemic and other aspects.HPLC of Formula: 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem