Day: November 4, 2022

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 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 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 March 20, 2008, Glatthar, Ralf; Johns, Donald; Umbricht, Daniel published a patent.Application of 85614-89-7 The title of the patent was Preparation of pyridine derivatives as modulators of metabotropic glutamate receptors. And the patent contained the following:

Title compounds represented by the formula I [wherein R1 – (un)substituted alkyl or benzyl; R2 = H, alkyl or (un)substituted benzyl; or R1R2N = (un)substituted heterocyclyl; R3 = halo, alkoxy, alkyl(amino) or dialkylamino; R4 = OH, halogen, alkyl or alkoxy; Q = CH, CR4 or N; V = CH, CR4 or N; W = CH, CR4 or N; X = CH or N; Y = CH, CR3 or N; Z = CH2, NH or O; provided that Q, V and W are not N at the same time; and in free base or acid addition salt form] were prepared as metabotropic glutamate receptors (mGluR) antagonist, especially mGluR5 antagonist,. For example, reaction of 6-chloro-N,N-diethylnicotinamide with 4-chloroaniline gave II in 56% yield. I were tested for inhibition of the glutamate induced elevation of intracellular Ca2+-concentration at a concentration of 10 μM, and I were also in clin. testing. Thus, I and their pharmaceutical compositions are useful as mGluR modulator for the treatment, prevention or delay of progression of cognitive dysfunction. The experimental process involved the reaction of Ethyl 5-methyl-6-oxo-1,6-dihydropyridine-3-carboxylate(cas: 85614-89-7).Application of 85614-89-7

The Article related to pyridine derivative preparation metabotropic glutamate receptor modulator, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Application of 85614-89-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On November 26, 1976, there was a patent about herbicides.Category: pyridine-derivatives The title of the patent was Herbicidal quaternary bipyridylium salts. And the patent contained the following:

The salts I (R, R1 = alkyl, alkenyl, alkynyl, substituted alkyl; X, X1 = Cl, Br, iodo, 4-MeC6H4SO3) (104 compounds) were prepared by quaternization. Thus 4,4′-bipyridine was treated with EtI and 4-(4-pyridyl)pyridinium ethiodide treated with CH2:CMeCH2I to give I (R = Et, R1 = CH2CMe:CH2, X = X1 = iodo). At 1 kg/ha I (R = Et, R1 = CH2CMe:CH2, X = X1 = iodo) post emergence gave ∼80% control of Avena fatua. The experimental process involved the reaction of 1,1′-Dipropyl-[4,4′-bipyridine]-1,1′-diium bromide(cas: 52243-87-5).Category: pyridine-derivatives

The Article related to bipyridinium salt, quaternary bipyridinium salt, herbicide bipyridinium salt, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Van der Does, L.; Den Hertog, H. J. published an article in 1972, the title of the article was Didehydrohetarenes. XXV. Amination of alkyl substituted halopyridines with potassium amide in liquid ammonia.Quality Control of 6-(tert-Butyl)pyridin-3-amine And the article contains the following content:

The action of KNH2 in liquid NH3 on Me substituted 3- and 4-bromo(or chloro)pyridines, of 5-bromo-2-tert-butylpyridine and of 3-bromo(or chloro) and 4-bromo(or chloro)-2,6-dimethylpyridine was studied. The results of the reactions indicate the occurrence of derivatives of 3,4-didehydropyridine as intermediates. An interpretation is given of the influence of the substituent and the hetero atom on the course of the aminations. The experimental process involved the reaction of 6-(tert-Butyl)pyridin-3-amine(cas: 39919-70-5).Quality Control of 6-(tert-Butyl)pyridin-3-amine

The Article related to hetarene didehydro, amination alkylhalopyridine, pyridine alkylhalo amination, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Quality Control of 6-(tert-Butyl)pyridin-3-amine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 21, 2018, Wang, Xiaoqin; Zhao, Chuping; He, Minghua; Zhong, Zhiqian; Chen, Jiahe; Wang, Yanchun; Wang, Maoqin published a patent.Formula: C10H10N4 The title of the patent was Preparation of 3,3′-disubstituted bipyridine derivative as anti-Alzheimer’s disease drug. And the patent contained the following:

This invention provides 3,3′-disubstituted dipyridine derivatives I and II [wherein R = H, OH, halo, etc.; R1 = O(CH2)mCH3 or OH; m and n = independently 0-3; R2 = alkyl, one or more Me or Et substituted amino, etc.]. The title compounds can be used in preparing drugs for prevention and/or treatment of Alzheimer’s disease, vascular dementia or myasthenia gravis disease. The invention has the advantages of low biotoxicity, good safety, and broad application space in preparing anti-Alzheimer’s disease drugs. The experimental process involved the reaction of [2,2′-Bipyridine]-3,3′-diamine(cas: 75449-26-2).Formula: C10H10N4

The Article related to bipyridine treatment alzheimer disease vascular dementia myasthenia gravis human, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Formula: C10H10N4

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 31, 2015, Lebedeva, O. V.; Chesnokova, A. N.; Badlueva, T. V.; Sipkina, E. I.; Rzhechitskii, A. E.; Pozhidaev, Yu. N. published an article.Reference of Pyridine-3-sulfonic acid The title of the article was Hybrid ion-exchange membranes based on heteroaromatic sulfonic acid derivatives. And the article contained the following:

Membranes exhibiting proton conductivity have been prepared by sol-gel synthesis using tetraethoxysilane and heteroaromatic sulfonic acid derivatives (2-phenyl-5-benzimidazolesulfonic acid and 3-pyridinesulfonic acid) in the presence of phosphoric acid and polyvinyl butyral. The membranes are gels composed of a polyvinyl butyral polymer matrix with uniformly distributed particles of silica containing mols. of heteroaromatic sulfonic acid derivatives mech. incorporated in its network structure. The membranes synthesized from 2-phenyl-5-benzimidazolesulfonic acid or 3-pyridinesulfonic acid exhibit a conductivity of 0.1X10-2 or 0.55X10-2 S/cm at 353 K, an ion-exchange capacity of 2.70 or 1.84 mequiv/g, and a proton-transfer activation energy of 24.93 or 21.73 kJ/mol, resp.; at a relative water content of 50%, the tensile strength is 4 or 6 MPa and the elastic modulus is 128 or 191 MPa, resp. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Reference of Pyridine-3-sulfonic acid

The Article related to tetraethoxysilane heteroaromatic sulfonic acid derivative membrane mech elec property, Plastics Fabrication and Uses: Plastic Product Uses and other aspects.Reference of Pyridine-3-sulfonic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On January 31, 1974, Fleckenstein, Erwin; Heinrich, Ernst; Mohr, Reinhard published a patent.HPLC of Formula: 51566-22-4 The title of the patent was Pyridine derivatives. And the patent contained the following:

Pyridine derivatives I (R and R1 = amino, alkoxy, alkylthio, CN, Cl) (642 compounds) were prepared by substitution reactions on I (R = R1 = Cl). The experimental process involved the reaction of 3-Methylpyridine-2,6-diamine(cas: 51566-22-4).HPLC of Formula: 51566-22-4

The Article related to pyridine dichloro substitution, substitution dichloropyridine, dye intermediate poridine, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 51566-22-4

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 16, 2008, Beaton, Graham; Chen, Mi; Coon, Timothy Richard; Ewing, Todd; Jiang, Wanlong; Lowe, Richard; Moree, Willy; Smith, Nicole; Wade, Warren; Zhao, Liren; Zhu, Yun-Fei; Rowbottom, Martin; Ashweek, Neil published a patent.Synthetic Route of 156267-13-9 The title of the patent was Preparation of benzenecarboxamide derivatives as Gonadotropin-releasing hormone receptor antagonists. And the patent contained the following:

Title compounds represented by the formula I [wherein A = pyridyl, Ph, quinolinyl, etc.; R1a = H, halo, alkyl, etc.; R1b, R1c = independently H, halo, OH, etc.; R1d = F, Cl, Me, CF3 or cyano; R2 = alkyl-(R5)p; R2a = (un)substituted Ph, (hetero)aryl or alkyl; R5 = independently H, OH, amino, etc.; p = 1-3; and stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof] were prepared as Gonadotropin-releasing hormone receptor (GnRH) antagonists. For example, II was provided in a multi-step synthesis starting from 3-bromo-4-chlorobenzoic acid. I were tested in one or more of the peptide competitive human receptor binding assays and showed Ki values of 1 μM or less. Thus, I and their pharmaceutical compositions are useful for the treatment of a variety of sex-hormone related conditions in both men and women. The experimental process involved the reaction of N,3-Dimethylpyridin-2-amine(cas: 156267-13-9).Synthetic Route of 156267-13-9

The Article related to benzenecarboxamide pyridinyl preparation gonadotropin releasing hormone receptor antagonist, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Synthetic Route of 156267-13-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem