Tag: 200-300

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

On September 3, 1998, Thorsett, Eugene D.; Porter, Warren J.; Nissen, Jeffrey S.; Latimer, Lee H.; Audia, James E.; Droste, James J. published a patent.COA of Formula: C10H18N2O3 The title of the patent was Preparation of heterocyclic compounds and their use for inhibiting β-amyloid peptide release. And the patent contained the following:

Disclosed are modified heterocyclic di- and tripeptide analogs which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer’s disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer’s disease both prophylactically and therapeutically with such pharmaceutical compositions Title compounds, e.g. I, were prepared in a multistep synthesis and inhibited β-amyloid peptide production by at least 30% as compared to control. The experimental process involved the reaction of (S)-tert-Butyl (2-oxopiperidin-4-yl)carbamate(cas: 1055049-80-3).COA of Formula: C10H18N2O3

The Article related to heterocyclic peptide preparation inhibitor amyloid release, alzheimer treatment heterocyclic compound preparation, amyloid peptide release inhibitor heterocyclic compound and other aspects.COA of Formula: C10H18N2O3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 14, 2003, Thorsett, Eugene D.; Porter, Warren J.; Nissen, Jeffrey S.; Latimer, Lee H.; Audia, James E.; Droste, James published a patent.Product Details of 1055049-80-3 The title of the patent was Preparation of heterocyclic compounds and their use for inhibiting β-amyloid peptide release. And the patent contained the following:

Disclosed are modified heterocyclic di- and tripeptide analogs which inhibit β-amyloid peptide release and/or its synthesis and, accordingly, have utility in treating Alzheimer’s disease. Compounds of formula R1NHCHR2(CONHCHR6)pCONHCHR5C(:NR4)R4 [R1 = H or acyl; R2, R5, R6 = (un)substituted alk(en)(yn)yl, cycloalkyl, (hetero)aryl, heterocyclyl; p = 0 or 1; R3and R4 combine to form a heterocyclic ring, which may be substituted] are claimed. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer’s disease both prophylactically and therapeutically with such pharmaceutical compositions Title compounds, e.g. I, were prepared in a multistep synthesis and inhibited β-amyloid peptide production by at least 30% as compared to control. The experimental process involved the reaction of (S)-tert-Butyl (2-oxopiperidin-4-yl)carbamate(cas: 1055049-80-3).Product Details of 1055049-80-3

The Article related to heterocyclic peptide preparation inhibitor amyloid release, alzheimer treatment heterocyclic compound preparation, amyloid peptide release inhibitor heterocyclic compound and other aspects.Product Details of 1055049-80-3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 30, 2013, Razavi, Seyyede Faeze; Khoobi, Mehdi; Nadri, Hamid; Sakhteman, Amirhossein; Moradi, Alireza; Emami, Saeed; Foroumadi, Alireza; Shafiee, Abbas published an article.HPLC of Formula: 39512-49-7 The title of the article was Synthesis and evaluation of 4-substituted coumarins as novel acetylcholinesterase inhibitors. And the article contained the following:

A series of 4-hydroxycoumarin derivatives were designed and synthesized as new acetylcholinesterase (AChE) inhibitors which could be considered for Alzheimer’s disease therapeutics. Among the 19 coumarin-derived compounds tested toward Electrophorus electricus acetylcholinesterase (eelAChE) and horse serum butyrylcholinesterase (eqBChE), N-(1-benzylpiperidin-4-yl)acetamide derivative I displayed highest AChE inhibitory activity (IC50 = 1.2 μM) and good selectivity (37 times). The docking study of the most potent compound I, indicated that Phe330 is responsible for ligand recognition and trafficking by forming π-cation interaction with benzylpiperidine moiety. Furthermore, the formation of an addnl. π-π interaction between coumarin moiety and Trp279 of peripheral anionic site could stabilize the ligand in the active site resulting in more potent inhibition of the enzyme. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).HPLC of Formula: 39512-49-7

The Article related to coumarin preparation acetylcholinesterase inhibitor, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) and other aspects.HPLC of Formula: 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 2, 2016, Zhang, Wen; Wang, Fei; McCann, Scott D.; Wang, Dinghai; Chen, Pinhong; Stahl, Shannon S.; Liu, Guosheng published an article.Electric Literature of 39512-49-7 The title of the article was Enantioselective cyanation of benzylic C-H bonds via copper-catalyzed radical relay. And the article contained the following:

Direct methods for stereoselective functionalization of sp3-hybridized carbon-hydrogen [C(sp3)-H] bonds in complex organic mols. could facilitate much more efficient preparation of therapeutics and agrochems. Here, we report a copper-catalyzed radical relay pathway for enantioselective conversion of benzylic C-H bonds into benzylic nitriles. Hydrogen-atom abstraction affords an achiral benzylic radical that undergoes asym. C(sp3)-CN bond formation upon reaction with a chiral copper catalyst. The reactions proceed efficiently at room temperature with the benzylic substrate as limiting reagent, exhibit broad substrate scope with high enantioselectivity (typically 90 to 99% enantiomeric excess), and afford products that are key precursors to important bioactive mols. Mechanistic studies provide evidence for diffusible organic radicals and highlight the difference between these reactions and C-H oxidations mediated by enzymes and other catalysts that operate via radical rebound pathways. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Electric Literature of 39512-49-7

The Article related to enantioselective cyanation benzylic carbon copper catalyzed radical relay, Physical Organic Chemistry: Stereochemistry and Stereochemical Relationships, Including Conformational Inversions and Rotational Isomerization and other aspects.Electric Literature of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On October 29, 2020, Scully, Stephen S.; Laplaca, Derek; Pelly, Rachel; Parmar, Rubina Giare; Maetani, Micah published a patent.Application of 357935-97-8 The title of the patent was Preparation of ionizable amine lipids and lipid nanoparticles. And the patent contained the following:

Ionizable amine lipids of formula I [X1 = O, (substituted) NH, bond; X2 = alkylene; X3 = CO, bond; R1 = H, Me; R2, R3 = alkyl; R2X2N = heterocyclyl; R2R3N = heterocyclyl; Y1 = alkylene; Y2 = CH2CH=CH, CO-OCH2CH=CH, CO-O; n = 0-3; R4 = alkyl; Z1 = alkylene, bond; Z2 = CO-O, absent; R5, R6 = alkyl, alkoxy; W = methylene, bond; R7 = H, Me] are prepared which are useful for the delivery of biol. active agents, for example delivering biol. active agents to cells to prepare engineered cells. The ionizable amine lipids disclosed herein are useful as ionizable lipids in the formulation of lipid nanoparticle-based compositions Thus, II was prepared, and had editing efficiency of 23.74% at 0.1 mg/kg, 58.48% at 0.3 mg/kg and 73.6% at 1 mg/kg in mice liver. The experimental process involved the reaction of 1-Ethylpiperidin-4-amine dihydrochloride(cas: 357935-97-8).Application of 357935-97-8

The Article related to lipid nanoparticle ionizable amine lipid preparation, Biomolecules and Their Synthetic Analogs: Prostaglandins and Other Arachidonic Acid Cascade Substances, Thromboxanes, Fatty Acids and other aspects.Application of 357935-97-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On October 18, 2019, Lin, Zhiyang; Lan, Yun; Wang, Chuan published an article.Formula: C11H14ClNO The title of the article was Reductive Allylic Defluorinative Cross-Coupling Enabled by Ni/Ti Cooperative Catalysis. And the article contained the following:

Tertiary alkyl chlorides, secondary alkyl chlorides and bromides, and primary alkyl bromides underwent chemoselective defluorinative cross-coupling reactions with α-trifluoromethyl aryl alkenes in the presence of (indenyl)TiCl3, NiBr2, and 3,4,7,8-tetramethyl-1,10-phenanthroline to yield α-substituted aryl difluoroalkenes such as 4-MeOC6H4C(:CF2)CH2R (R = t-Bu, cyclohexyl, n-octyl). Unfunctionalized and ester-functionalized alkyl halides underwent cross-coupling under the reaction conditions, while a variety of functionalized aryl alkenes underwent cross-coupling. Using this method, gem-difluoroalkene analogs of azaperone, haloperidol, and benperidol were prepared The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Formula: C11H14ClNO

The Article related to alkyl aryl difluoroalkene chemoselective preparation, nickel titanium catalyst reductive defluorinative coupling trifluoromethylalkene chloroalkane bromoalkane, tertiary secondary chloroalkane reductive defluorinative coupling trifluoromethyl aryl alkene, secondary primary bromoalkane reductive defluorinative coupling trifluoromethyl aryl alkene and other aspects.Formula: C11H14ClNO

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

On May 31, 2017, Dalwadi, Dhwanil A.; Kim, Seongcheol; Schetz, John A. published an article.Name: 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Activation of the sigma-1 receptor by haloperidol metabolites facilitates brain-derived neurotrophic factor secretion from human astroglia. And the article contained the following:

Glial cells play a critical role in neuronal support which includes the production and release of the neurotrophin brain-derived neurotrophic factor (BDNF). Activation of the sigma-1 receptor (S1R) has been shown to attenuate inflammatory stress-mediated brain injuries, and there is emerging evidence that this may involve a BDNF-dependent mechanism. In this report we studied S1R-mediated BDNF release from human astrocytic glial cells. Astrocytes express the S1R, which mediates BDNF release when stimulated with the prototypical S1R agonists 4-PPBP and (+)-SKF10047. This effect could be antagonized by a selective concentration of the S1R antagonist BD1063. Haloperidol is known to have high affinity interactions with the S1R, yet it was unable to facilitate BDNF release. Remarkably, however, two metabolites of haloperidol, haloperidol I and haloperidol II (reduced haloperidol), were discovered to facilitate BDNF secretion and this effect was antagonized by BD1063. Neither 4-PPBP, nor either of the haloperidol metabolites affected the level of BDNF mRNA as assessed by qPCR. These results demonstrate for the first time that haloperidol metabolites I and II facilitate the secretion of BDNF from astrocytes by acting as functionally selective S1R agonists. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Name: 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to human astroglia haloperidol metabolite brain neurotrophic factor sigma receptor, (+)-skf10047, 4-ppbp, astrocytes, bd1063, bdnf, haloperidol (pubchem cid: 3559), haloperidol metabolite i, haloperidol metabolite iii, in situ elisa, ne-100, neurotrophin, pf-04418948, pge2, reduced haloperidol, sigma receptor and other aspects.Name: 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem