Category: 1227595-34-7

On June 10, 2021, Bartolome-Nebreda, Jose Manuel; Trabanco-Suarez, Andres Avelino; De Lucas Olivares, Ana Isabel published a patent.Related Products of 1227595-34-7 The title of the patent was Synthesis of heterocyclic Oga inhibitors treating tauopathies, in particular Alzheimer’s and Parkinson’s diseases. And the patent contained the following:

The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors I, tautomers, or stereoisomers such that Ra can be a six- or five-membered heteroaryl ring system or nine, ten membered bicyclic heterocyclic ring; L is selected from O, OCH2, or CH2O; R1a-b an R2a-b are independently H, Me or (un)substituted C1-3 alkyl; R is H or methyl; Rb can be a bicyclic heteroaryl ring systems are prepared as pharmaceutically acceptable salts and solvates. Of note, II was prepared for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer’s disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathol., in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations; or alpha synucleinopathies, in particular Parkinson’s disease, dementia due to Parkinson’s (or neurocognitive disorder due to Parkinson’s disease), dementia with Lewy bodies, multiple system atrophy, or alpha synucleinopathy caused by Gaucher’s disease. The experimental process involved the reaction of 4-(Chloromethyl)-2-methoxy-6-methylpyridine(cas: 1227595-34-7).Related Products of 1227595-34-7

The Article related to heterocyclic oga inhibitor preparation alzheimers parkinson tauopathy, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Related Products of 1227595-34-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On June 10, 2021, Bartolome-Nebreda, Jose Manuel; Trabanco-Suarez, Andres Avelino; De Lucas Olivares, Ana Isabel published a patent.Related Products of 1227595-34-7 The title of the patent was Synthesis of heterocyclic Oga inhibitors treating tauopathies, in particular Alzheimer’s and Parkinson’s diseases. And the patent contained the following:

The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors I, tautomers, or stereoisomers such that Ra can be a six- or five-membered heteroaryl ring system or nine, ten membered bicyclic heterocyclic ring; L is selected from O, OCH2, or CH2O; R1a-b an R2a-b are independently H, Me or (un)substituted C1-3 alkyl; R is H or methyl; Rb can be a bicyclic heteroaryl ring systems are prepared as pharmaceutically acceptable salts and solvates. Of note, II was prepared for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer’s disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathol., in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations; or alpha synucleinopathies, in particular Parkinson’s disease, dementia due to Parkinson’s (or neurocognitive disorder due to Parkinson’s disease), dementia with Lewy bodies, multiple system atrophy, or alpha synucleinopathy caused by Gaucher’s disease. The experimental process involved the reaction of 4-(Chloromethyl)-2-methoxy-6-methylpyridine(cas: 1227595-34-7).Related Products of 1227595-34-7

The Article related to heterocyclic oga inhibitor preparation alzheimers parkinson tauopathy, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Related Products of 1227595-34-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On November 9, 2000, Dow, Robert Lee; Liu, Kevin Kun-Chin; Morgan, Bradley Paul; Swick, Andrew Gordon published a patent.Reference of 4-(Chloromethyl)-2-methoxy-6-methylpyridine The title of the patent was Preparation of nonracemic octahydrophenanthrene and other tricyclic derivatives as selective modulators of glucocorticoid receptors. And the patent contained the following:

Title compounds [e.g., I; D = CR7, CR7R16, N, NR7, O’ E = C, CR6, N; F = CR4, CR4R5, O; R = XR1; R1 = H, alkyl, acylalkyl, arylalkyl, etc.; R2 = H, halo, alkyl, alkoxy, etc.; R3 = H, alkyl, arylalkyl, etc.; 1 of R2,R3 = null when adjacent dashed line = bond; R4,R5 = H, cyano, alkyl, alkoxy, etc.; R4R5 = O; R6 = H, cyano, alkyl, alkoxy, OH, etc.; R7,R16 = H, halo, cyano, alkyl, etc.; R7R16 = O; R8R9 = atoms to complete a substituted heteroaromatic ring; R14,R15 = H, halo, alkyl, alkoxy, etc.; R14R15 = O when adjacent dashed lines = null; X = bond, CH2, CH(OH), CO; Z = (un)substituted CH2, -CH2CH2, -CH2CO, CO, etc.; dashed lines = optional bonds] were prepared as glucocorticoid receptor modulators (no data). E.g., 6-methoxy-2-tetralone was alkylated by formation of the pyrrolidine enamine and alkylation with benzyl bromide; the benzylated ketone then undergoes asym. Michael addition with Me vinyl ketone in the presence of (S)-(-)-α-methylbenzylamine followed by cyclocondensation with sodium methoxide to give a nonracemic methoxytetrahydrophenanthrenone derivative E.g., demethylation of the methoxytetrahydrophenanthrenone with boron trichloride, reduction of the enone with lithium and ammonia, addition of 1-lithiopropyne to the ketone, formation of the aryl triflate with triflic anhydride and carbonylation with carbon monoxide in the presence in the presence of palladium acetate and bis(diphenylphosphino)propanol gives an hydroxyoctahydrophenanthrenecarboxylic acid derivative which is coupled with 4-(aminomethyl)pyridine in the presence of trimethylaluminum to give the octahydrophenanthrenecarboxamide II as one of the title compounds The experimental process involved the reaction of 4-(Chloromethyl)-2-methoxy-6-methylpyridine(cas: 1227595-34-7).Reference of 4-(Chloromethyl)-2-methoxy-6-methylpyridine

The Article related to nonsteroidal glucocorticoid receptor selective agonist antagonist preparation, treatment obesity diabetes inflammation nonsteroidal glucocorticoid receptor modulator, glucocorticoid receptor modulator preparation and other aspects.Reference of 4-(Chloromethyl)-2-methoxy-6-methylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On November 9, 2000, Dow, Robert Lee; Liu, Kevin Kun-Chin; Morgan, Bradley Paul; Swick, Andrew Gordon published a patent.Reference of 4-(Chloromethyl)-2-methoxy-6-methylpyridine The title of the patent was Preparation of nonracemic octahydrophenanthrene and other tricyclic derivatives as selective modulators of glucocorticoid receptors. And the patent contained the following:

Title compounds [e.g., I; D = CR7, CR7R16, N, NR7, O’ E = C, CR6, N; F = CR4, CR4R5, O; R = XR1; R1 = H, alkyl, acylalkyl, arylalkyl, etc.; R2 = H, halo, alkyl, alkoxy, etc.; R3 = H, alkyl, arylalkyl, etc.; 1 of R2,R3 = null when adjacent dashed line = bond; R4,R5 = H, cyano, alkyl, alkoxy, etc.; R4R5 = O; R6 = H, cyano, alkyl, alkoxy, OH, etc.; R7,R16 = H, halo, cyano, alkyl, etc.; R7R16 = O; R8R9 = atoms to complete a substituted heteroaromatic ring; R14,R15 = H, halo, alkyl, alkoxy, etc.; R14R15 = O when adjacent dashed lines = null; X = bond, CH2, CH(OH), CO; Z = (un)substituted CH2, -CH2CH2, -CH2CO, CO, etc.; dashed lines = optional bonds] were prepared as glucocorticoid receptor modulators (no data). E.g., 6-methoxy-2-tetralone was alkylated by formation of the pyrrolidine enamine and alkylation with benzyl bromide; the benzylated ketone then undergoes asym. Michael addition with Me vinyl ketone in the presence of (S)-(-)-α-methylbenzylamine followed by cyclocondensation with sodium methoxide to give a nonracemic methoxytetrahydrophenanthrenone derivative E.g., demethylation of the methoxytetrahydrophenanthrenone with boron trichloride, reduction of the enone with lithium and ammonia, addition of 1-lithiopropyne to the ketone, formation of the aryl triflate with triflic anhydride and carbonylation with carbon monoxide in the presence in the presence of palladium acetate and bis(diphenylphosphino)propanol gives an hydroxyoctahydrophenanthrenecarboxylic acid derivative which is coupled with 4-(aminomethyl)pyridine in the presence of trimethylaluminum to give the octahydrophenanthrenecarboxamide II as one of the title compounds The experimental process involved the reaction of 4-(Chloromethyl)-2-methoxy-6-methylpyridine(cas: 1227595-34-7).Reference of 4-(Chloromethyl)-2-methoxy-6-methylpyridine

The Article related to nonsteroidal glucocorticoid receptor selective agonist antagonist preparation, treatment obesity diabetes inflammation nonsteroidal glucocorticoid receptor modulator, glucocorticoid receptor modulator preparation and other aspects.Reference of 4-(Chloromethyl)-2-methoxy-6-methylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem