Category: 1251006-64-0

On April 30, 2020, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Crews, Craig M.; Jaime-Figueroa, Saul; Dong, Hanqing; Qian, Yimin; Zimmermann, Kurt published a patent.HPLC of Formula: 1251006-64-0 The title of the patent was Bifunctional heterocycles, their use in targeted degradation of rapidly accelerated fibrosarcoma polypeptides and their preparation. And the patent contained the following:

The present disclosure relates bifunctional compounds of formula ULM-L-PTM, their use in modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein) and treatment of diseases that result from aggregation or accumulation of the target protein. and their preparation Compounds of formula ULM-L-PTM, wherein ULM is a small mol. E3 ubiquitin ligase binding moiety; PTM is a small mol. comprising a RAF protein targeting moiety; L is a bond or chem. linking moiety connecting ULM and PTM; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorph and prodrug thereof, are claimed. Compound I was prepared using a multistep procedure (procedure given). The present disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein (data given). The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).HPLC of Formula: 1251006-64-0

The Article related to bifunctional heterocycle preparation raf modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.HPLC of Formula: 1251006-64-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 30, 2021, Araujo, Erika; Sparks, Steven M.; Berlin, Michael; Zhang, Wei; Wang, Jing published a patent.Reference of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Indazole based compounds and associated methods of use. And the patent contained the following:

Bifunctional compounds (e.g., I), which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Reference of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to indazole hetero bifunctional leucine rich repeat kinase inhibitor preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 8, 2017, Himmelsbach, Frank; Blum, Andreas; Peters, Stefan published a patent.Recommanded Product: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Preparation of pyridinylmethyl carbamimidoylcarbamate derivatives as AOC3 inhibitors. And the patent contained the following:

The invention relates to new heteroaryl derivatives I [X1 = N and CH; X2 = N and CF (with the proviso that at least one of X1 and X2 is N); A = II-IV (R4 = (un)substituted azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, etc.)] or a pharmaceutically acceptable salt thereof, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them. Over one-hundred compounds I were prepared General procedures for preparation of compounds I were provided. For example, compound I was prepared, starting from (2,3-difluoro-4-pyridyl)methanol and 3-phenylazetidine. Exemplified compounds I were tested for their pharmacol. activity in the AOC3 assay (IC50 values were given). The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Recommanded Product: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to pyridinylmethyl carbamimidoylcarbamate preparation aoc3 vascular adhesion protein 1 inhibitor, heteroaryl carbamimidoylcarbamate preparation aoc3 vascular adhesion protein 1 inhibitor and other aspects.Recommanded Product: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On April 25, 2013, Connolly, Peter J.; Bian, Haiyan; Li, Xun; Liu, Li; Macielag, Mark J.; McDonnell, Mark E. published a patent.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Preparation of piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors. And the patent contained the following:

The title compounds I [Y and Z = (un)substituted aryl, heteroaryl, 1,3-dihydro-3H-benzimidazol-2-on-yl, etc.; R = H or OH], useful for treating various diseases, syndromes, conditions and disorders, including pain, were prepared E.g., a multi-step synthesis of II, starting from tert-Bu 3-iodoazetidine-1-carboxylate, was described. Exemplified compounds I were tested in the MGL activity assay (data given). Pharmaceutical composition comprising compound I is disclosed. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to piperidinylazetidine diamide amide preparation monoacylglycerol lipase inhibitor analgesic, inflammatory pain treatment piperidinylazetidine amide preparation monoacylglycerol lipase inhibitor and other aspects.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On May 7, 2020, Hehn, Joerg P.; Blum, Andreas; Hucke, Oliver; Peters, Stefan published a patent.Name: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Preparation of pyridine-3-sulfonamide derivatives as amine oxidase copper containing 3 (AOC3) inhibitors and pharmaceutical compositions and uses thereof. And the patent contained the following:

The invention relates to new pyridinyl sulfonamide derivatives of the formula I [ring A = azetidin-1-yl, pyrrolidin-1-yl, 3-azabicyclo[3.1.0]hexan-3-yl, or piperidin-4-yl; R1 = H, F, Ci, Br, cyano, OH, or each (un)substituted C1-4-alkyl, C1-4-alkyloxy, (CH2)m-CO2H, (CH2)m-C(O)O-(C1-4-alkyl), (CH2)m-C(O)-heterocyclyl, (CH2)m-C(O)NH2, (CH2)m-C(O)NH-(C1-4-alkyl), (CH2)m-C(O)-N-(C1-4-alkyl)2, C(O)-NH-C3-6-cycloalkyl, C(O)-NH-heterocyclyl, (CH2)m-NH-C(O)(C1-3-alkyl), N-(C1-3-alkyl)-C(O)-(C1-4-alkyl), N-(C1-3-alkyl)-C(O)NH2, NH-C(O)NH-(C1-4-alkyl), heterocyclyl, or Ph; wherein multiple R1 may be identical or different, if n = 2; n = 1 or 2; m = 0, 1, or 2] or salts thereof. The compounds I or salts thereof are selective inhibitors of AOC3 (amine oxidase, copper containing 3; vascular adhesion protein 1) and are useful for the treatment of cancer, NASH (non-alc. steatohepatitis), pulmonary fibrosis, retinopathy, nephropathy, or stroke. Thus, 326 mg trans-3-[(6-chloropyridin-3-yl)sulfonyl]-3-azabicyclo[3.1.0]hexane-6-carboxylic acid methylamide and 216 mg tert-Bu N-[2-(fluoromethylidene)-3-hydroxypropyl]carbamate were dissolved in 1 mL THF and 1 mL DMSO, cooled to 0°, treated with 0.53 mL 2 M sodium tert-butoxide/THF solution, and to give stirred at 0° for 5 min and at room temperature for 35 min to give trans-3-[6-[[2-[[(tert-butoxycarbonyl)amino]methyl]-3-fluoroallyl]oxy]pyridine-3-sulfonyl]-3-azabicyclo[3.1.0]hexane-6-carboxylic acid methylamide trifluoroacetate. The latter precursor (410 mg) was dissolved in 15 mL CH2Cl2, treated with 266μL CF3CO2H, and stirred at room temperature for 2.5 h to give 38% trans-3-[6-[((E)-2-aminomethyl-3-fluoroallyl)oxy]pyridine-3-sulfonyl]-3-azabicyclo[3.1.0]hexane-6-carboxylic acid methylamide trifluoroacetate (II). II showed IC50 of 12, 162, 43,370 nM against AOC3, AOC2, and AOC1, resp. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Name: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to pyridinesulfonamide preparation aoc3 inhibitor, amine oxidase copper containing 3 aoc3 inhibitor, vascular adhesion protein 1 inhibitor, azetidinylsulfonylpyridine pyrrolidinylsulfonylpyridine preparation aoc3 inhibitor, azabicyclohexanylsulfonylpyridine piperidinylsulfonylpyridine preparation aoc3 inhibitor and other aspects.Name: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On May 7, 2020, Hehn, Joerg P.; Blum, Andreas; Hucke, Oliver; Peters, Stefan published a patent.Recommanded Product: 1251006-64-0 The title of the patent was Preparation of pyridine-3-sulfonamide derivatives as amine oxidase copper containing 3 (AOC3) inhibitors and pharmaceutical compositions and uses thereof. And the patent contained the following:

The invention relates to new pyridinyl sulfonamide derivatives of the formula I [ring A = azetidin-1-yl, pyrrolidin-1-yl, 3-azabicyclo[3.1.0]hexan-3-yl, or piperidin-4-yl; R1 = H, F, Ci, Br, cyano, OH, or each (un)substituted C1-4-alkyl, C1-4-alkyloxy, (CH2)m-CO2H, (CH2)m-C(O)O-(C1-4-alkyl), (CH2)m-C(O)-heterocyclyl, (CH2)m-C(O)NH2, (CH2)m-C(O)NH-(C1-4-alkyl), (CH2)m-C(O)-N-(C1-4-alkyl)2, C(O)-NH-C3-6-cycloalkyl, C(O)-NH-heterocyclyl, (CH2)m-NH-C(O)(C1-3-alkyl), N-(C1-3-alkyl)-C(O)-(C1-4-alkyl), N-(C1-3-alkyl)-C(O)NH2, NH-C(O)NH-(C1-4-alkyl), heterocyclyl, or Ph; wherein multiple R1 may be identical or different, if n = 2; n = 1 or 2; m = 0, 1, or 2] or salts thereof. The compounds I or salts thereof are selective inhibitors of AOC3 (amine oxidase, copper containing 3; vascular adhesion protein 1) and are useful for the treatment of cancer, NASH (non-alc. steatohepatitis), pulmonary fibrosis, retinopathy, nephropathy, or stroke. Thus, a solution of 0.19 mmol 1-[1-(6-chloropyridine-3-sulfonyl)piperidin-4-yl]-3-methylimidazolidin-2-one in NMP and Et3N was cooled in an ice bath, treated with a solution of 0.19 mmol tert-butyl-N-[2-(fluoromethylidene)-3-hydroxypropyl]carbamate in 0.5 mL THF and 390μL 2 M sodium tert-butoxide/THF, and stirred at room temperature for 2 h to give 1-[1-[6-((Z)-2-(tert-butoxycarbonylamino)methyl-3-fluoroallyloxy)pyridine-3-sulfonyl]piperidin-4-yl]-3-methylimidazolidin-2-one (isolated as trifluoroacetate salt) which was stirred with CF3CO2H in CH2Cl2 at room temperature for 2 h to give 1-[1-[6-((Z)-2-aminomethyl-3-fluoroallyloxy)pyridine-3-sulfonyl]piperidin-4-yl]-3-methylimidazolidin-2-one trifluoroacetate (II). II showed IC50 of 7, 120, 15,265 nM, and >50.0μM against AOC3, AOC2, AOC1, and monoamine oxidase-A (MAO-A), resp. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Recommanded Product: 1251006-64-0

The Article related to pyridinesulfonamide preparation aoc3 inhibitor, amine oxidase copper containing 3 aoc3 inhibitor, vascular adhesion protein 1 inhibitor, azetidinylsulfonylpyridine pyrrolidinylsulfonylpyridine preparation aoc3 inhibitor, azabicyclohexanylsulfonylpyridine piperidinylsulfonylpyridine preparation aoc3 inhibitor and other aspects.Recommanded Product: 1251006-64-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem