Category: 1092942-42-1

On January 16, 2014, Jana, Gourhari; Kurhade, Sanjay Pralhad; Jagdale, Arun Rangnath; Kukreja, Gagan; Sinha, Neelima; Palle, Venkata P.; Kamboj, Rajender Kumar published a patent.Application of 1092942-42-1 The title of the patent was Preparation of tetrahydroquinazolinone derivatives as PARP inhibitors for treating cancer. And the patent contained the following:

Disclosed are compounds of formula I, their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, (wherein M is C, CH, and N, and the dotted bond is either a single or double bond with provisos; R1 is H and (un)substituted alkyl; R2 and R3 together with the carbon atom(s) to which they are attached form a (un)substituted carbocycle; each R4 is halogen, cyano, (un)substituted alkyl, etc.; R5 and R6 are independently H, halogen, (un)substituted alkyl, etc., or R5 and R6 together constitute oxo or form part of an (un)substituted carbocycle; R7a, R8a, R7b R8b, R7c, R8c, R7d, and R8d are independently H, halogen, (un)substituted alkyl, etc., or any two form oxo or form part of an (un)substituted carbocycle or (un)substituted heterocycle, thereby making ring A either a spiro-bicycle or a fused-bicycle or a bridged-bicycle; Ar is (un)substituted aryl or (un)substituted heteroaryl; p = 0-3; and n = 1-4), pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PARP enzyme of a subject. I can also be used to sensitize a patient that has developed a resistance to other chemotherapeutics. Synthetic procedures for preparing I are exemplified. Example compound II, prepared from intermediates Et 6-oxospiro[2.5]octane-5-carboxylate and 4-(4-(4-chlorophenyl)piperazin-1-yl)butanimidamide, had a PARP 1 inhibition IC50 between 1 nM and 500 nM. The experimental process involved the reaction of 2-Bromo-N-methylthiazole-4-carboxamide(cas: 1092942-42-1).Application of 1092942-42-1

The Article related to tetrahydroquinazolinone derivative parp inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 1092942-42-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On December 18, 2008, Gaufreteau, Delphine; Nettekoven, Matthias; Plancher, Jean-Marc; Roche, Olivier; Schmitt, Sebastien; Takahashi, Tadakatsu published a patent.Application In Synthesis of 2-Bromo-N-methylthiazole-4-carboxamide The title of the patent was Preparation of cyclohexyl piperazinyl methanones as modulators of histamine H3 receptors.. And the patent contained the following:

Title compounds [I; R1 = alkyl, cycloalkyl; R2 = (substituted) heteroarylphenyl, heterocyclylphenyl, heteroaryl], were prepared Thus, cis-4-hydroxycyclohexanecarboxylic acid, 1-cyclobutylpiperazine dihydrochloride, TBTU, and diisopropylethylamine were stirred together for 8 h at room temperature in DMF to give 76% amide, which was stirred with 4-(1,2,4-triazol-1-yl)phenol, Ph3P, and di-tert-Bu azodicarboxylate in THF for 72 h to give 11% trans-(4-cyclobutylpiperazin-1-yl)-[4-[4-[1,2,4]triazol-1-ylphenoxy]cyclohexyl]methanone. The latter showed a Ki value of 6.5 nM in an H3 binding assay. The experimental process involved the reaction of 2-Bromo-N-methylthiazole-4-carboxamide(cas: 1092942-42-1).Application In Synthesis of 2-Bromo-N-methylthiazole-4-carboxamide

The Article related to cyclohexyl piperazinyl methanone preparation histamine h3 receptor modulator, obesity diabetes treatment cyclohexylcarbonylpiperazine preparation antihistamine, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application In Synthesis of 2-Bromo-N-methylthiazole-4-carboxamide

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On February 4, 2021, Anderson, David Randolph; Jacobsen, Eric Jon; Blinn, James Robert; Hockerman, Susan Landis; Mukherjee, Paramita; Changelian, Paul published a patent.Synthetic Route of 1092942-42-1 The title of the patent was Substituted sulfonamide pyrrolopyridines as JAK inhibitors and their preparation. And the patent contained the following:

The invention relates to sulfonamide pyrrolopyridine compounds of formula I and compositions useful in the treatment of JAK-mediated conditions. Methods of inhibition of JAK kinase activity in a human or animal subject are also provided. Exemplary indications treated by inhibition of JAK kinase activity include, but are not limited to, inflammatory bowel disease, Crohn’s disease, ulcerative colitis, irritable bowel syndrome, and Celiac disease. Compounds of formula I wherein R1 is CN, CO2C1-6 alkyl and (un)substituted 5- to 10-membered heteroaromatic ring; R2 and R3 are independently H, (un)substituted C1-4 alkyl and (un)substituted C0-2 alkyl-C3-6 cycloalkyl; R4 is (un)substituted C1-6 alkyl, (un)substituted C0-4 alkyl-C3-6 cycloalkyl, (un)substituted C2-5 alkyl-COC0-4 alkyl-C3-6 cycloalkyl, etc.; are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for the JAK inhibitory activity (data given). The experimental process involved the reaction of 2-Bromo-N-methylthiazole-4-carboxamide(cas: 1092942-42-1).Synthetic Route of 1092942-42-1

The Article related to pyrrolopyridine sulfonamide preparation jak inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Synthetic Route of 1092942-42-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On November 5, 2020, Jacobsen, Eric Jon; Anderson, David Randolph; Blinn, James Robert; Mukherjee, Paramita; Changelian, Paul; Xu, Canxin published a patent.Recommanded Product: 1092942-42-1 The title of the patent was Substituted pyrrolopyridines as JAK inhibitors and their preparation and their preparation. And the patent contained the following:

The invention relates to pyrrolopyridine compounds having the structures of formula I, and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of JAK kinase activity in a human or animal subject are also provided for the treatment diseases such as pruritus, alopecia, androgenetic alopecia, alopecia areata, vitiligo and psoriasis. Compounds of formula I wherein R1 is CN and (un)substituted heteroaryl; R2 is H, (un)substituted C1-4 alkyl, (un)substituted C3-6 cycloalkyl and (un)substituted C1-2 alkyl-C3-6 cycloalkyl; Q is absent, CH2 and CH2CH2; R3 is H, halo, (un)substituted C1-4 alkyl, (un)substituted C3-6 cycloalkyl, etc.; two R3 groups may be taken together to form a spirocyclic or bicyclic ring system; R4 is COR6, CH2R5, COC1-5 alkyl and COC3-6 cycloalkyl; R6 is C1-5 alkyl, C3-6 cycloalkyl, aryl, aryloxy, etc.; and derivatives thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their JAK inhibitory activity (data given). The experimental process involved the reaction of 2-Bromo-N-methylthiazole-4-carboxamide(cas: 1092942-42-1).Recommanded Product: 1092942-42-1

The Article related to pyrrolopyridine preparation jak inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Recommanded Product: 1092942-42-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica