Category: 1251006-64-0

On January 9, 2020, Ji, Nan; Mainolfi, Nello; Weiss, Matthew published a patent.Synthetic Route of 1251006-64-0 The title of the patent was Preparation of novel bifunctional compounds as MerTK degraders and uses thereof. And the patent contained the following:

The present invention provides compounds I [TAMBM is an TAM receptor kinase binding moiety; L is a bivalent moiety that connects TAMBM to DIM; and DIM is a degradation inducing moiety selected from LBM, a lysine mimetic, and H] or pharmaceutically acceptable salts thereof, compositions thereof, and methods of using the same. E.g., a multi-step synthesis of trans-II, starting from Et 4-chloro-2-(methylsulfanyl)pyrimidine-5-carboxylate, was described. Exemplified compounds I were tested for MerTK degradation in vitro (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Synthetic Route of 1251006-64-0

The Article related to bifunctional compound preparation mertk degrader, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 1251006-64-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 25, 2020, Cheng, Zhanling; Khan, Nawaz; Kramer, Christian; Lerner, Christian; Pflieger, Philippe; Stoll, Theodor; Wang, Jianhua; Wang, Min; Wang, Yongguang; Yang, Song published a patent.Name: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Novel imidazopyrazine derivatives as antibacterial agents and their preparation. And the patent contained the following:

The invention provides imidazopyrazine derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases. Compounds of formula I wherein A is (mono/bi)cyclic C2-9 heterocycloalkyl ring; R1 is H, amino, sulfamoyl, OH, etc.; R2 is H, OH, carbamoyl, etc.; R3 is C1-6 alkyl, C1-6 haloalkyl C2-6 alkenyl, etc.; etc.; R4, R10 and R11 are independently H, halo, and C1-6 alkyl; R5, R6, R7, R8 and R9 are independently H, halo, amino, C1-6 alkoxycarbonyl-C1-6 alkoxy, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of 4-((3-(4-(difluoromethoxy)phenyl)imidazo[1,2-a]pyrazin-8-yl)amino)-2-methylbenzoic acid with Me piperidine-4-carboxylate; the resulting Me 1-(4-((3-(4-(difluoromethoxy)phenyl)imidazo[1,2-a]pyrazin-8-yl)amino)-2-methylbenzoyl)piperidine-4-carboxylate underwent hydrolysis to give compound II. The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 1.7μM. 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 imidazopyrazine antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Name: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On July 23, 2020, Looper, Ryan E.; Sebahar, Paul; Reddy, Hariprasada R. Kanna; Haussener, Travis J.; Testa, Charles A.; Tresco, Benlsaac C.; Grant, Seth; Napolitano, Carmela; Sabbatini, Fabio Maria published a patent.Formula: C13H24N2O2 The title of the patent was Preparation of cytosine derivatives as antimicrobial agents. And the patent contained the following:

The invention is directed to compounds I [Z = C(O), C(S), S(O), etc.; ring A = (un)substituted monocyclic heterocycloalkylene or bicyclic heterocycloalkylene; J = absent, (un)substituted alkylene, heterocycloalkylene, etc.; X1 and X2 = (independently) CH or N; Y = (un)substituted linear alkylene, alkenylene, or alkynylene; ring B = (un)substituted monocyclic cycloalkylene or monocyclic heterocycloalkylene; L = absent, or alkylene, wherein up to two methylene units may independently be replaced with O, NH, C(O), etc.; R1 = H, halo, haloalkyl, etc.; R11 = H or (un)substituted NH2; R2 and R3 = (independently) alkyl, halo, CN, etc.; m and n = (independently) 0-3] or pharmaceutically acceptable salts thereof, that are active as antibacterial agents. E.g., a 2-step synthesis of trans-II, starting from tert-Bu (1-(4-((1-(4-formylphenyl)-2-oxo-1,2-dihydropyrimidin-4-yl)carbamoyl)piperazin-1-yl)-2-methyl-1-oxopropan-2-yl)carbamate and N-Boc-trans-1,4-cyclohexanediamine, was described. Biol. activity of compounds I was determined (data given). The invention compounds I are active against gram-pos. and gram-neg. bacteria and can be used to treat infections caused by gram-pos. and gram-neg. bacteria. Also disclosed are processes and intermediates for making the compounds I. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Formula: C13H24N2O2

The Article related to cytosine aminopyrimidinone derivative preparation antibacterial antimicrobial, gram pos neg bacteria infection cytosine aminopyrimidinone derivative preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C13H24N2O2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 25, 2020, Blanc, Jean-Baptiste; Cheng, Zhanling; Han, Xingchun; Khan, Nawaz; Kramer, Christian; Kuehne, Holger; Lerner, Christian; Nettekoven, Matthias; Pflieger, Philippe; Puellmann, Bernd; Schmitt, Sebastien; Stoll, Theodor; Wang, Jianhua; Wang, Yongguang; Yang, Song published a patent.Recommanded Product: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Novel imidazopyrazine derivatives as antibacterials and their preparation. And the patent contained the following:

The invention provides imidazopyrazine derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases. Compounds of formula I wherein R1 is (un)substituted C1-6 alkyl; R11 is H, halo and C1-6 alkyl; R1R11 can be taken together to form β-, γ-, δ- and ε-lactam; R2 is H, C1-6 alkyl, C1-6 haloalkyl, C1-6 cyanoalkyl, etc.; R3 is H, halo, C1-6 alkyl, NO2, CN, etc.; R4 and R10 are independently H, halo and (un)substituted C1-6 alkyl; R5, R6, R7, R8 and R9 are independently H, halo, amino, C1-6 alkoxycarbonyl-C1-6 alkoxy, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of 4-amino-2-methylbenzoic acid with dimethylamine hydrochloride; the resulting 4-amino-N,N,2-trimethylbenzamide underwent arylation with 8-chloro-3-(2,3-difluoro-4-methoxyphenyl)imidazo[1,2-a]pyrazine to give compound II. The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 0.12μM. 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 imidazopyrazine antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Recommanded Product: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 25, 2020, Blanc, Jean-Baptiste; Khan, Nawaz; Kramer, Christian; Lerner, Christian; Pflieger, Philippe; Stoll, Theodor; Yang, Song published a patent.Electric Literature of 1251006-64-0 The title of the patent was Novel imidazopyrazine derivatives as antibacterials and their preparation. And the patent contained the following:

The invention provides imidazopyrazine derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases. Compounds of formula I wherein A is C2-9 heterocycloalkyl, C3-12 cycloalkyl, C6-14 aryl and C1-13 heteroaryl; R1 is H, C1-6 alkyl, C1-6 haloalkyl, etc.; R2 is H, OH, carboxyl, amino, etc.; R3, R4 and R5 are independently H and OH; R6 is H, halo, C1-6 alkyl, NO2, CN, etc.; R7 and R13 are independently H, halo and C1-6 alkyl; R8, R9, R10, R11 and R12 are independently H, halo, amino, C1-6 alkoxycarbonyl-C1-6 alkoxy, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of 4-((3-(2,3-difluoro-4-methoxyphenyl)imidazo[1,2-a]pyrazin-8-yl)amino)-2-ethylbenzoic acid with tert-Bu cis-N-(3-aminocyclobutyl)carbamate; the resulting 4-((3-(2,3-difluoro-4-methoxyphenyl)imidazo[1,2-a]pyrazin-8-yl)amino)-2-ethylbenzoic acid underwent hydrolysis to give compound II. The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 0.084μM. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Electric Literature of 1251006-64-0

The Article related to imidazopyrazine preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Electric Literature of 1251006-64-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 25, 2020, Cheng, Zhanling; Khan, Nawaz; Kramer, Christian; Lerner, Christian; Nettekoven, Matthias; Pflieger, Philippe; Puellmann, Bernd; Schmitt, Sebastien; Stoll, Theodor; Wang, Jianhua; Yang, Song published a patent.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Novel imidazopyrazine derivatives as antibacterials and their preparation. And the patent contained the following:

The invention provides imidazopyrazine derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases. Compounds of formula I wherein R1 is R12-C1-6 alkyl-X-C1-6 alkyl; R2 is H, C1-6 alkyl, C1-6 haloalkyl, C1-6 cyanoalkyl, etc.; R3 is H, halo, C1-6 alkyl, NO2, CN, etc.; R4 and R10 are independently H, halo and C1-6 alkyl; R5, R6, R7, R8 and R9 are independently H, halo, amino, C1-6 alkoxycarbonyl-C1-6 alkoxy, etc.; R11 is H, halo and C1-6 alkyl; R12 is H, vinyl, C2-6 alkynyl, OH, etc.; X is O, NH, S, SO, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II•TFA was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 0.12μM. 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 imidazopyrazine preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 25, 2020, Cheng, Zhanling; Khan, Nawaz; Kramer, Christian; Lerner, Christian; Pflieger, Philippe; Stoll, Theodor; Wang, Jianhua; Wang, Yongguang; Yang, Song published a patent.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Novel imidazopyrazine derivatives as antibacterials and their preparation. And the patent contained the following:

The invention provides imidazopyrazine derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases. Compounds of formula I wherein ring A is (mono/bi)cyclic C2-9 heterocycloalkyl; R1 is H, amino, C1-6 alkyl-NH, OH, etc.; R2 is H, OH, carbamoyl, etc.; R3 is H, halo, NO2 and CN; R4, R10 and R11 are independently H, halo and C1-6 alkyl; R5, R6, R7, R8 and R9 are independently H, halo, amino, C1-6 alkoxycarbonyl-C1-6 alkoxy, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of 2-chloro-4-((3-(2,3-difluoro-4-methoxyphenyl)imidazo[l,2-a]pyrazin-8-yl)amino)benzoic acid with 1-tert-Bu 2-Me piperazine-1,2-dicarboxylate; the resulting 1-tert-Bu 2-Me 4-[2-chloro-4-[[3-(2,3-difluoro-4-methoxy-phenyl)imidazo[1,2-a]pyrazin-8-yl]amino]benzoyl]piperazine-1,2-dicarboxylate underwent Boc-deprotection to give Me 4-[2-chloro-4-[[3-(2,3-difluoro-4-methoxy-phenyl)imidazo[1,2-a]pyrazin-8-yl]amino]benzoyl]piperazine-2-carboxylate, which underwent hydrolysis to give compound II. The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 1.9μM. 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 imidazopyrazine preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 2, 2021, Wang, Qiuwen; Guo, Yunhang; Wang, Zhiwei published a patent.Category: piperidines The title of the patent was Synthesis of pyridazine Tyk-2 inhibitors for treating inflammatory or autoimmune diseases. And the patent contained the following:

The synthesis of pyridazine heterocyclic Tyk-2 inhibitors I, wherein R1 can be H, or optionally substituted C1-6-alkyl or C3-6cycloalkyl groups; R2 can be a -C(O)- group with an (un)substituted 4-10 membered heterocyclic ring system; R3 is a fused bicyclic heterocyclic ring system with independently substituted H, halo, cyano or alkyl groups are prepared as pharmaceutically acceptable salts for treating inflammatory or autoimmune diseases. Of note, II was prepared and tested in biochem. and cellular assays with nM inhibition and high selectivity. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Category: piperidines

The Article related to pyridazine tyk2 inhibitor preparation antiinflammatory autoimmune disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On October 14, 2021, Netherton, Matthew; Brucelle, Francois published a patent.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Preparation of substituted hydroxyphenylpyridazinamines for treating BAF complex-related disorders. And the patent contained the following:

The present disclosure features compounds I [X1 = O or NR2; each X2 = (independently) halo; k = 0-4; m = 0-4; R1 = halo or (un)substituted alkyl; R2 = H or (un)substituted alkyl; L1 = (un)substituted alkylene; L = L2(L3)n; n = 0-3; L2 = (un)substituted alkylene, heteroalkylene, or heterocyclylene; each L3 = (independently) O, (un)substituted heteroalkylene, carbocyclylene, etc.; and D = a degradation moiety] or pharmaceutically acceptable salts thereof, useful for the treatment of BAF complex-related disorders. E.g., a multi-step synthesis of II, starting from 4-bromo-6-chloropyridazin-3-amine and Et 2-(piperazin-1-yl)acetate, was described. Exemplified compounds I were evaluated for their ability to degrade a HiBit-BRM or HiBit-BRG1 fusion protein in a cell-based degradation assay (data given). Pharmaceutical composition comprising compound I was 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 hydroxyphenylpyridazinamine preparation baf complex related disorder, brm brg1 fusion protein degradation hydroxyphenylpyridazinamine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Safety 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.HPLC of Formula: 1251006-64-0 The title of the patent was Preparation of 4-cyanobenzyl carbamimidoylcarbamate derivatives as AOC3 inhibitors. And the patent contained the following:

The invention relates to new benzonitrile derivatives I [R1 = H or halo; R2 = H or halo;R3 = H or halo (with the proviso that not more than one of R1-R3 is halo); A = II-IV, etc. (R4 = pyrrolidinyl, piperidinyl, piperazinyl; a CH2 group of the pyrrolidinyl, oxazolidinyl, piperidinyl or piperazinyl group of R4 is optionally replaced with a C(O) group)] or a pharmaceutically acceptable salt thereof, to their medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them. Over ninety compounds I were prepared E.g., a multi-step synthesis of compound V, starting from 4-bromo-2,5-difluoro-benzonitrile and 4-(piperazinyl)benzonitrile, was described. Exemplified compounds I were tested in the AOC3 assay (IC50 values 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 cyanobenzyl carbamimidoylcarbamate aoc3 inhibitor, 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