Category: 314021-93-7

On April 20, 2017, Aiguade Bosch, Jose; Connolly, Stephen; Eastwood, Paul Robert; Roberts, Richard Spurring; Sevilla Gomez, Sara; Caturla Javaloyes, Juan Francisco published a patent.Formula: C6H6N4O The title of the patent was Bicyclic heterocycle derivatives as TRPA1 antagonists and their preparation. And the patent contained the following:

The invention relates to bicyclic heterocyclic derivatives of I, to the process for preparing such compounds and to their use in the treatment of pruritus, pain, inflammatory dermatol. diseases, respiratory disorders, gastrointestinal inflammatory disorders, and urinary tract disorders susceptible to amelioration by TRPA1 channel inhibition or antagonism. A compound of formula I wherein G1 is C and N; G2, G3 and G5 are independently N, NRb, CRb and CRc; G4 is absent, N, NRb, CRb and CRc; G6, G7, and G8 are independently N and CRb; G9 and G10 are independently N and NRb; dashed bond is single bond and double bond; L is a bond, CH2, O, S, NRb; m is 0 and 1; Ra is halo, CN, C1-4 haloalkyl, etc; Rb is H and (un)branched C1-4 alkyl group; Rc is H, CN, (un)branched C1-4, etc; and pharmaceutically acceptable salts thereof are claimed. Compound II was prepared from the cross-coupling of 3-[(6-bromo-1H-imidazo[4,5-b]pyrazin-2-yl)methyl]-5-methylimidazo[5,1-f][1,2,4]triazin-4(3H)-one with (4-chlorophenyl)boronic acid. From the assay, it was determined that compound II exhibited an IC50 value in the range of 100 nM – 1000 nM. The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Formula: C6H6N4O

The Article related to bicyclic heterocycle preparation trpa1 antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Triazines and other aspects.Formula: C6H6N4O

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On June 25, 2009, Goldfarb, David Scott published a patent.Computed Properties of 314021-93-7 The title of the patent was Method using lifespan-altering compounds for altering the lifespan of eukaryotic organisms, and screening for such compounds. And the patent contained the following:

The invention discloses a method for altering the lifespan of a eukaryotic organism. The method comprises the steps of providing a lifespan-altering compound, and administering an effective amount of the compound to a eukaryotic organism, such that the lifespan of the organism is altered. In one embodiment, the compound is identified using the DeaD assay. The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Computed Properties of 314021-93-7

The Article related to lifespan alteration compound screening dead assay, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Computed Properties of 314021-93-7

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On October 15, 2015, Aguilar Izquierdo, Nuria; Buil Albero, Maria Antonia; Connolly, Stephen; Eastwood, Paul Robert; Roberts, Richard Spurring; Sevilla Gomez, Sara; Vidal Juan, Bernat published a patent.Product Details of 314021-93-7 The title of the patent was TRPA1 channel antagonists as therapeutic agents. And the patent contained the following:

The invention relates to compounds I, [G1= CH, N; G2= C(Ra), N; G3= C, N; G4= C, N; G5= C(Rb), N(Rc), N, O, S; G6= C(Rb), N(Rc), N, O, S; G7= C(Rb), N(Rc), N, O, S; Q= monocyclic or bicyclic C6-C14 aryl, monocyclic or bicyclic 5-14 membered heteroaryl ring, halogen, etc.; R1= H, halogen, C1-C4 alkyl, C1-C4 haloalkyl, C6-C14 aryl, CH2Ph; R2= H, halogen, C1-C4 alkyl, C1-C4 haloalkyl, C6-C14 aryl, CH2Ph; R3= H, F; R4= H, F; Ra= H, C1-C4 alkyl, halogen, C1-C4 alkoxy, etc., Rb= H, C1-C4 alkyl, halogen, C1-C4 alkoxy, etc., Rc= H, C1-C4 alkyl, C1-C4 haloalkyl, C3-C7 cycloalkyl], and the preparation and use for the treatment of a pathol. condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism. The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Product Details of 314021-93-7

The Article related to trpa1 channel antagonist preparation, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Product Details of 314021-93-7

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On February 1, 2007, Oslob, Johan D.; Yu, Chul Hyun published a patent.Reference of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol The title of the patent was Pyrazolopyrimidines useful as Aurora kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of Aurora kinase mediated diseases. And the patent contained the following:

The invention provides compounds having the formula I, which are useful as inhibitors of protein kinase (e.g., Aurora), and thus are useful, for example, for the treatment of Aurora mediated diseases. Compounds of formula I wherein dotted line is double bond as valency permits; R2 is H, halo, CN, NO2, (hetero)aliphatic, (hetero)alicyclic and (hetero)aromatic moiety; R4 is absent, H, (hetero)aliphatic, (hetero)alicyclic, and (hetero)aromatic moiety; if R4 is absent, X1 and X2 are independently NH and derivatives and CR1 proviso that only one of X1 and X2 are CR1; if R4 is present X1 and X2 are independently N and derivatives, and CR1, proviso that only one of X1 and X2 is CR1; R1 is H, halo, CN, No2, (hetero)aliphatic, etc.; L1 is 2-8 atom heteroaliph. linker; L2 is 1-6 atom heteroaliph. linker; Y is (hetero)alicyclic, and (hetero)aromatic moiety; Z is (hetero)alicyclic, (hetero)aliphatic, and (hetero)aromatic moiety; are claimed. Example compound II was prepared by amination of 4-chloro-5-methylpyrazolopyrimidine derivative with 2-[2-(3-trifluoromethylphenylurido)thiazol-2-yl]ethylamine. All the invention compounds were evaluated for their Aurora kinase inhibitory activity. The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Reference of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol

The Article related to pyrazolo pyrimidine preparation aurora kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On February 1, 2007, Oslob, Johan D.; Yu, Chul Hyun published a patent.Reference of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol The title of the patent was Pyrazolopyrimidines useful as Aurora kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of Aurora kinase mediated diseases. And the patent contained the following:

The invention provides compounds having the formula I, which are useful as inhibitors of protein kinase (e.g., Aurora), and thus are useful, for example, for the treatment of Aurora mediated diseases. Compounds of formula I wherein dotted line is double bond as valency permits; R2 is H, halo, CN, NO2, (hetero)aliphatic, (hetero)alicyclic and (hetero)aromatic moiety; R4 is absent, H, (hetero)aliphatic, (hetero)alicyclic, and (hetero)aromatic moiety; if R4 is absent, X1 and X2 are independently NH and derivatives and CR1 proviso that only one of X1 and X2 are CR1; if R4 is present X1 and X2 are independently N and derivatives, and CR1, proviso that only one of X1 and X2 is CR1; R1 is H, halo, CN, No2, (hetero)aliphatic, etc.; L1 is 2-8 atom heteroaliph. linker; L2 is 1-6 atom heteroaliph. linker; Y is (hetero)alicyclic, and (hetero)aromatic moiety; Z is (hetero)alicyclic, (hetero)aliphatic, and (hetero)aromatic moiety; are claimed. Example compound II was prepared by amination of 4-chloro-5-methylpyrazolopyrimidine derivative with 2-[2-(3-trifluoromethylphenylurido)thiazol-2-yl]ethylamine. All the invention compounds were evaluated for their Aurora kinase inhibitory activity. The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Reference of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol

The Article related to pyrazolo pyrimidine preparation aurora kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On July 1, 2021, Pinkerton, Anthony; Sergienko, Eduard; Kiyotsuka, Yohei; Kagechika, Katsuji; Kurosaki, Yasunobu; Arai, Yoshikazu; Nagamochi, Masatoshi; Ishibashi, Koutaro published a patent.Safety of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol The title of the patent was Preparation of bicyclic heteroaryls, especially thienopyrimidines, as ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) modulators. And the patent contained the following:

The invention is related to the preparation of bicyclic heteroaryl-based small mol. modulators of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), e.g., of formula I [B = aryl or a 5 or 6-membered heteroaryl; n = 0-3; X = (CH2)1-2; p = 0-3; Y1 = NR4, O; L1 = Y2L2, Y2L2L3; Y2 = a bond, CO; L2 = a bond, (un)substituted alk(en/yn)ylene, heteroalkylene, C2-C6 cycloalkylene; R1 = H, halo, CN, OH, etc.; R2 = H, COOH and derivatives, fluoroalkoxy, etc.; R3 = H, halo, SH and derivatives, NH2 and derivatives, etc.; R5 = independently at each occurrence H, NO2, CN, SO2NH2 and derivatives, etc.; R6 = independently at each occurrence halo, alk(en/yn)yl, etc.; ], their pharmaceutically acceptable salts and solvates , compositions containing them, and methods of using the compounds and compositions comprising the compounds for treating disorders associated with ENPP1, such as pseudogout. Thus, II was prepared by cyclization of Me 3-amino-4-methylthiophene-2-carboxylate with formamide, chlorination of 7-methylthieno[3,2-d]pyrimidin-4-ol with POCl3, amination of 4-chloro-7-methylthieno[3,2-d]pyrimidine with tert-Bu (piperidin-4-yl)carbamate, cleavage of tert-butoxycarbonyl group and benzylation of 1-(7-methylthieno[3,2-d]pyrimidin-4-yl)piperidin-4-amine with benzyl chloride. II inhibited ENPP1 in a TR-FRET assay (IC50 in the range of 0.1μM – 1.0μM). The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Safety of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol

The Article related to bicyclic heteroaryl preparation ectonucleotide pyrophosphatase phosphodiesterase 1 enpp1 inhibitor, thienopyrimidine pyrazolopyrimidine pyrazolopyridine thienopyridine preparation enpp1 inhibitor pseudogout antiarthritic, triazolopyrimidine isoxazolopyrimidine pyrazolopyridazine isothiazolopyrimidine preparation enpp1 inhibitor and other aspects.Safety of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On April 13, 2017, Aiguade Bosch, Jose; Connolly, Stephen; Eastwood, Paul Robert; Gomez Castillo, Elena; Moreno Mollo, Immaculada Montserrat; Roberts, Richard Spurring; Sevilla Gomez, Sara published a patent.Application of 314021-93-7 The title of the patent was Preparation of bicyclic fused pyrimidinone and triazinone derivatives as new TRPA1 antagonists. And the patent contained the following:

The present invention relates to compounds of Formula I [G1 = C or N atom; G2, G3, G4, G5 = each independently C(Ra), N(Rb), or N; G6 = N, G7 = C atom, G8 = N atom, G9 = O atom; Ra = H, linear or branched C1-4 alkyl, halogen atom, linear or branched C1-4 alkoxy, linear or branched C1-4 haloalkyl, linear or branched C1-4 haloalkoxy, oxo, C3-7 cycloalkyl, cyano, amino, mono – or di(C1-4 alkyl)amino, or hydroxy; Rb = H or linear or branched C1-4 alkyl; L = (un)substituted linear or branched C2-4 alkylene, C(Rb):C(Rb), C3-7 cycloalkylene, (CH2)2-3-O, (CH2)1-2-C(O), (CH2)1-2-S, (CH2)1-2-S(O), CONH, CF2O, or 4- to 6-membered N-containing heterocyclylene, wherein at least one nitrogen atom is linked the G7 group; Q = each (un)substituted monocyclic or bicyclic C6-14 aryl or monocyclic or bicyclic 5- to 14-membered heteroaryl containing at least one heteroatom selected from N, O and S; or when Q = Ph, L together with Q form a 5- to 7-membered N-containing heterocyclyl fused to the Ph group; n = 0-1; the solid/dashed line = single or a double bond], pharmaceutically acceptable salts, solvates, N-oxides, tautomers, stereoisomers, or isotopically-labeled derivatives thereof:. These compounds are used in the treatment of a pathol. condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism. The pathol. condition or disease is selected from acute and/or chronic pruritus, acute and/or chronic pain, inflammatory dermatol. diseases, respiratory disorders, gastrointestinal inflammatory disorders, and urinary tract disorders. Thus, a suspension of 0.040 g 5-methylquinazolin-4(3H)-one and 0.069 g potassium carbonate in 1.0 mL DMF was stirred at room temperature for 10 min, followed by adding a solution of 0.071 g 5-(chloromethyl)-3-[2-(4-chlorophenyl)ethyl]-1,2,4-oxadiazole in 0. 5 mL DMF, and the resulting mixture of was stirred for 3 h to give, after workup and flash chromatog., 72% 3-[[3-[2-(4-chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-5-methylquinazolin-4(3H)-one (II). II and 3-[[3-[2-(4-Chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-5-methylimidazo[5,1-f]-[1,2,4]triazin-4(3H)-one (III) inhibited the tetracycline-inducible human TRPA1 expression in CHO cells in a calcium flux assay with IC50 of 100-1,000 and <100 nM, resp. The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Application of 314021-93-7

The Article related to fused pyrimidinone preparation trpa1 antagonist, bicyclic fused triazinone preparation trpa1 antagonist, transient receptor potential cation channel trpa trpa1 antagonist, acute chronic pruritus treatment bicyclic heterocycle, chronic acute pain treatment bicyclic heterocycle and other aspects.Application of 314021-93-7

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics