Category: 97483-79-9

On July 2, 2015, Wang, Yansong; Hausch, Felix published a patent.HPLC of Formula: 97483-79-9 The title of the patent was Bicyclic aza-amides for treatment of psychiatric disorders. And the patent contained the following:

The present invention relates to compounds of formula (I) having a bicyclic aza-amides scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said bicyclic aza-amides compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions. The experimental process involved the reaction of Ethyl 6-cyanopicolinate(cas: 97483-79-9).HPLC of Formula: 97483-79-9

The Article related to bicyclic aza amide preparation fkbp inhibitor psychiatric neurol disease, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 97483-79-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On January 29, 2014, Wang, Yansong; Hausch, Felix published a patent.Electric Literature of 97483-79-9 The title of the patent was Preparation of bicyclic aza-amides for treatment of psychiatric disorders. And the patent contained the following:

The invention relates to bicyclic aza-amides of formula I as inhibitors of FK506 binding proteins (FKBP) useful in the prophylaxis and/or treatment of psychiatric, neurodegenerative diseases. Compounds of formula I wherein X is CH2, CH2CH2, CH(CH=CH2), etc.; R1 is H, Me, Et, etc.; R2 is substituted Ph, substituted cyclohexyl, substituted pyridyl, etc. and enantiomers, stereoisomeric forms, mixtures of enantiomers, anomers, deoxyforms, diastereomers, mixtures of diastereomers, prodrugs, tautomers, hydrates, solvates and racemates of the above mentioned compounds, are claimed. Example compound II was prepared by alkylation of benzyl 2-oxo-3,9-diazabicyclo[3.3.1]nonane-9-carboxylate with 4-(2-bromoethoxy)-1,2-dimethoxybenzene; the resulting benzyl 3-(2-(3,4-dimethoxyphenoxy)ethyl)-2-oxo-3,9-diazabicyclo[3.3.1]nonane-9-carboxylate underwent Cbz-deprotection followed by sulfonylation with 3,5-dichlorobenzene sulfonyl chloride. From the assay, it was determined that example II exhibited IC50 value of 12.2±3.7 μM, 8.8±1.1 μM and 0.14±0.01 μM towards FKBP52, FKBP51 and FKBP12, resp. The experimental process involved the reaction of Ethyl 6-cyanopicolinate(cas: 97483-79-9).Electric Literature of 97483-79-9

The Article related to bicyclic aza amide preparation fkbp inhibitor psychiatric neurol disease, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Electric Literature of 97483-79-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On January 30, 2014, Wang, Yansong; Hausch, Felix published a patent.Reference of Ethyl 6-cyanopicolinate The title of the patent was Preparation of bicyclic aza-amides for treatment of psychiatric disorders. And the patent contained the following:

The invention relates to bicyclic aza-amides of formula I as inhibitors of FK506 binding proteins (FKBP) useful in the prophylaxis and/or treatment of psychiatric, neurodegenerative diseases. Compounds of formula I wherein X is CH2, CH2CH2, CH(CH=CH2), etc.; R1 is H, Me, Et, etc.; R2 is substituted Ph, substituted cyclohexyl, substituted pyridyl, etc. and enantiomers, stereoisomeric forms, mixtures of enantiomers, anomers, deoxyforms, diastereomers, mixtures of diastereomers, prodrugs, tautomers, hydrates, solvates and racemates of the above mentioned compounds, are claimed. Example compound II was prepared by alkylation of benzyl 2-oxo-3,9-diazabicyclo[3.3.1]nonane-9-carboxylate with 4-(2-bromoethoxy)-1,2-dimethoxybenzene; the resulting benzyl 3-(2-(3,4-dimethoxyphenoxy)ethyl)-2-oxo-3,9-diazabicyclo[3.3.1]nonane-9-carboxylate underwent Cbz-deprotection followed by sulfonylation with 3,5-dichlorobenzene sulfonyl chloride. The invention compounds were evaluated for their FKBP binding affinity in which II inhibited FKBP51 and FKBP52 with an IC50 of 1.3±0.13 μM and 2.5±0.38 μM, resp. From the assay, it was determined that example II exhibited IC50 value of 12.2±3.7 μM, 8.8±1.1 μM and 0.14±0.01 μM towards FKBP52, FKBP51 and FKBP12, resp. The experimental process involved the reaction of Ethyl 6-cyanopicolinate(cas: 97483-79-9).Reference of Ethyl 6-cyanopicolinate

The Article related to bicyclic aza amide preparation fkbp inhibitor psychiatric neurol disease, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Reference of Ethyl 6-cyanopicolinate

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On February 28, 1985, Sakamoto, Takao; Kaneda, Sohichi; Nishimura, Sumiko; Yamanaka, Hiroshi published an article.Computed Properties of 97483-79-9 The title of the article was Site-selectivity in the cyanation of 3-substituted pyridine 1-oxides with trimethylsilanecarbonitrile. And the article contained the following:

Treatment of pyridine 1-oxides I (R = Br, Cl, F, OMe, NMe2, Me, Et, Ph, CONEt2, CO2Et, cyano) with Me3SiCN gave 2- and 6-cyanopyridines II and III. The II – III ratio was strongly influenced by R, with II being the only product when R = F, OMe, NMe2. Nitropyridine 1-oxides underwent deoxygenation but not cyanation with Me3SiCN. The experimental process involved the reaction of Ethyl 6-cyanopicolinate(cas: 97483-79-9).Computed Properties of 97483-79-9

The Article related to pyridine oxide trimethylsilyl cyanide cyanation, cyanopyridine, deoxygenation pyridine oxide trimethylsilyl cyanide, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Computed Properties of 97483-79-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 20, 2018, Fahrni, Christoph J.; McCallum, Adam M.; Morgan, Michael Thomas published a patent.Quality Control of Ethyl 6-cyanopicolinate The title of the patent was Preparation of substituted phenylthiazole compounds as zinc-selective fluorescent probes for emission-ratiometric imaging. And the patent contained the following:

The title compounds I [Z = II; X1-X4 = (independently) N and CH; Y1 = NR4, S, and O; Y2 = NR5, S, and O; R = Ar, OR4, N((CH2)qAr)2; R1-R4 = (independently) H, halo, alkyl, etc.; R5 = Cn-alkyl optionally substituted with OR4 or Ar; Ar = (independently) aryl and heteroaryl; n = 1-3; q = 1-3; and wherein any one of the aforementioned can be substituted or unsubstituted], useful for detecting zinc in a biol. sample (two-photo excitation microscopy (TPEM) or conventional fluorescence microscopy), were prepared E.g., a multi-step synthesis of III, starting from Et 6-bromopicolinate, was described. The latter was tested for Zn(II)-binding affinity and its analyte selectivity (data given). To evaluate the Zn(II)-dependent ratiometric response of III within the chem. complexity of a live cell, the authors performed a perfusion experiment with NIH 3T3 mouse fibroblasts as model system (data given). The experimental process involved the reaction of Ethyl 6-cyanopicolinate(cas: 97483-79-9).Quality Control of Ethyl 6-cyanopicolinate

The Article related to phenylthiazole preparation zinc selective fluorescent probe emission ratiometric imaging, two photo excitation microscopy tpem phenylthiazole preparation zinc probe, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Quality Control of Ethyl 6-cyanopicolinate

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On May 23, 2013, Wang, Yansong; Kirschner, Alexander; Fabian, Anne-Katrin; Gopalakrishnan, Ranganath; Kress, Christoph; Hoogeland, Bastiaan; Koch, Uwe; Kozany, Christian; Bracher, Andreas; Hausch, Felix published an article.Formula: C9H8N2O2 The title of the article was Increasing the Efficiency of Ligands for FK506-Binding Protein 51 by Conformational Control. And the article contained the following:

The design of efficient ligands remains a key challenge in drug discovery. In the quest for lead-like ligands for the FK506-binding protein 51 (FKBP51), we designed two new classes of bicyclic sulfonamides to probe the contribution of conformational energy in these ligands. The [4.3.1] scaffold had consistently higher affinity compared to the [3.3.1] or monocyclic scaffolds, which could be attributed to better preorganization of two key recognition motifs. Surprisingly, the binding of the rigid [4.3.1] scaffold was enthalpy-driven and entropically disfavored compared to the flexible analogs. Cocrystal structures at at. resolution revealed that the sulfonamide nitrogen in the bicyclic scaffolds can accept an unusual hydrogen bond from Tyr113 that mimics the putative FKBP transition state. This resulted in the first lead-like, functionally active ligand for FKBP51. Our work exemplifies how atom-efficient ligands can be achieved by careful conformational control even in very open and thus difficult binding sites such as FKBP51. The experimental process involved the reaction of Ethyl 6-cyanopicolinate(cas: 97483-79-9).Formula: C9H8N2O2

The Article related to conformational control ligand fk506 binding protein 51, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.Formula: C9H8N2O2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 20, 2018, Fahrni, Christoph J.; McCallum, Adam M.; Morgan, Michael Thomas published a patent.Quality Control of Ethyl 6-cyanopicolinate The title of the patent was Preparation of substituted phenylthiazole compounds as zinc-selective fluorescent probes for emission-ratiometric imaging. And the patent contained the following:

The title compounds I [Z = II; X1-X4 = (independently) N and CH; Y1 = NR4, S, and O; Y2 = NR5, S, and O; R = Ar, OR4, N((CH2)qAr)2; R1-R4 = (independently) H, halo, alkyl, etc.; R5 = Cn-alkyl optionally substituted with OR4 or Ar; Ar = (independently) aryl and heteroaryl; n = 1-3; q = 1-3; and wherein any one of the aforementioned can be substituted or unsubstituted], useful for detecting zinc in a biol. sample (two-photo excitation microscopy (TPEM) or conventional fluorescence microscopy), were prepared E.g., a multi-step synthesis of III, starting from Et 6-bromopicolinate, was described. The latter was tested for Zn(II)-binding affinity and its analyte selectivity (data given). To evaluate the Zn(II)-dependent ratiometric response of III within the chem. complexity of a live cell, the authors performed a perfusion experiment with NIH 3T3 mouse fibroblasts as model system (data given). The experimental process involved the reaction of Ethyl 6-cyanopicolinate(cas: 97483-79-9).Quality Control of Ethyl 6-cyanopicolinate

The Article related to phenylthiazole preparation zinc selective fluorescent probe emission ratiometric imaging, two photo excitation microscopy tpem phenylthiazole preparation zinc probe, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Quality Control of Ethyl 6-cyanopicolinate

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On May 23, 2013, Wang, Yansong; Kirschner, Alexander; Fabian, Anne-Katrin; Gopalakrishnan, Ranganath; Kress, Christoph; Hoogeland, Bastiaan; Koch, Uwe; Kozany, Christian; Bracher, Andreas; Hausch, Felix published an article.Formula: C9H8N2O2 The title of the article was Increasing the Efficiency of Ligands for FK506-Binding Protein 51 by Conformational Control. And the article contained the following:

The design of efficient ligands remains a key challenge in drug discovery. In the quest for lead-like ligands for the FK506-binding protein 51 (FKBP51), we designed two new classes of bicyclic sulfonamides to probe the contribution of conformational energy in these ligands. The [4.3.1] scaffold had consistently higher affinity compared to the [3.3.1] or monocyclic scaffolds, which could be attributed to better preorganization of two key recognition motifs. Surprisingly, the binding of the rigid [4.3.1] scaffold was enthalpy-driven and entropically disfavored compared to the flexible analogs. Cocrystal structures at at. resolution revealed that the sulfonamide nitrogen in the bicyclic scaffolds can accept an unusual hydrogen bond from Tyr113 that mimics the putative FKBP transition state. This resulted in the first lead-like, functionally active ligand for FKBP51. Our work exemplifies how atom-efficient ligands can be achieved by careful conformational control even in very open and thus difficult binding sites such as FKBP51. The experimental process involved the reaction of Ethyl 6-cyanopicolinate(cas: 97483-79-9).Formula: C9H8N2O2

The Article related to conformational control ligand fk506 binding protein 51, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.Formula: C9H8N2O2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 1, 1987, Heinisch, Gottfried; Loetsch, Gerhard published an article.Synthetic Route of 97483-79-9 The title of the article was Homolytic alkoxycarbonylation reactions in two-phase systems. 3. Introduction of a single carboxylic acid ester function into cyano- or (alkoxycarbonyl)-substituted N-heteroaromatics. And the article contained the following:

Radical alkoxycarbonylation of pyridines I (R = cyano, CO2Et, R1-R3 = H; R = R2 = R3 = H, R1 = cyano, CO2Et; R = R1 = R3 = H, R2 = cyano, CO2Et) with MeCOCO2Me or MeCOCO2Et in H2O-CH2Cl2 containing H2O2-FeSO4 gave mainly monosubstitution products. Thus, I (R = cyano, R1-R3 = H) was treated with MeCOCO2Et to give 34% I (R = cyano, R1 = R3 = H, R2 = CO2Et) and 13% I (R = cyano, R1 = R2 = H, R3 = CO2Et). Similarly, I (R = R2 = R3 = H, R1 = CO2Et) reacted with MeCOCO2Me to give 29% I (R = CO2Me, R1 = CO2Et, R2 = R3 = H), 36% I (R = R3 = H, R1 = CO2Et, R2 = CO2Me), and 20% I (R = R2 = H, R1 = CO2Et, R3 = CO2Me). Only the mixed ester I (R = CO2Me, R1 = R3 = H, R2 = CO2Et) was obtained (in 81% yield) by treating I (R = R1 = R3 = H, R2 = CO2Et) with MeCOCO2Me. The experimental process involved the reaction of Ethyl 6-cyanopicolinate(cas: 97483-79-9).Synthetic Route of 97483-79-9

The Article related to pyridine alkoxycarbonyl cyano, cyanopyridinecarboxylate, pyridazinedicarboxylate, homolytic alkoxycarbonylation cyanopyridine pyruvate, radical alkoxycarbonylation pyridinecarboxylate pyruvate and other aspects.Synthetic Route of 97483-79-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 13, 2003, Kajino, Masahiro; Kawada, Akira; Nakayama, Yutaka; Kimura, Haruhide published a patent.Quality Control of Ethyl 6-cyanopicolinate The title of the patent was Preparation of 2-heterocyclyl-1,3-benzothiazinone derivatives as inhibitors of apoptosis or cytoprotective agents. And the patent contained the following:

Compounds represented by the following general formula (I) or salts thereof (wherein R1 represents hydrogen, halogeno, hydroxy, nitro, optionally halogenated alkyl, optionally substituted alkoxy, acyl or optionally substituted amino; R2 represents pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each optionally substituted; and n is 1 or 2), which and have a high safety and favorable effects of inhibiting cell death and binding to macrophage migration inhibitory factor (MIF), are prepared Also disclosed are apoptosis inhibitors, cytoprotective agents, or myocardial cell death inhibitors, or preventives/remedies for diseases caused by apoptosis or MIF which contain the compounds of the general formula (I), in particular for the prevention and/or treatment of circulatory diseases, bone or joint diseases, infectious diseases, inflammatory bowel diseases, or kidney. They are also useful for the prevention and/or treatment of heart diseases, heart failure syndromes, neurodegenerative diseases, brain vascular diseases, central nerve infections, traumatic diseases, demyelinating diseases, liver diseases, myelodysplastic syndrome, AIDS, cancer, etc. Thus, a mixture of 0.67 g thiosalicylic acid Me ester, 2-cyano-6-propylthiopyridine, and 0.84 mL Et3N in 50 mL toluene was refluxed for 48 h to give 37% 2-(6-propylthio-2-pyridyl)-4H-1,3-benzothiazin-4-one which was oxidized by m-chloroperbenzoic acid in EtOAc at room temperature for 18 h to give 2-(6-propylsulfinyl-2-pyridyl)-4H-1,3-benzothiazin-4-one (II). II was further oxidized by m-chloroperbenzoic acid in EtOAc at room temperature for 18 h to give 41% 2-(6-propylsulfonyl-2-pyridyl)-4H-1,3-benzothiazin-4-one (III). II and III showed the minium effective concentration of 0.019 and 0.010 μM, resp., for inhibiting apoptosis of new born rat’s first generation myocardial cells. A tablet and a capsule formulation containing 2-(6-methylsulfonyl-2-pyridyl)-4H-1,3-benzothiezin-4-one were described. The experimental process involved the reaction of Ethyl 6-cyanopicolinate(cas: 97483-79-9).Quality Control of Ethyl 6-cyanopicolinate

The Article related to heterocyclylbenzothiazinone preparation apoptosis inhibitor cytoprotective agent, myocardial cell death inhibitor heterocyclylbenzothiazinone preparation, circulatory disease prevention treatment heterocyclylbenzothiazinone preparation, bone joint disease prevention treatment heterocyclylbenzothiazinone preparation and other aspects.Quality Control of Ethyl 6-cyanopicolinate

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem