Category: 1340372-11-3

On November 18, 2021, Vu, Binh; Dominique, Romyr; Li, Hongju; Fahr, Bruce; Good, Andrew published a patent.Recommanded Product: 1340372-11-3 The title of the patent was Preparation of heteroaryl-substituted indole derivatives for restoring mutant p53 function. And the patent contained the following:

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The disclosure provided compounds of formula I capable of binding to mutant p53 and restoring the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. Compounds of formula I [wherein X1 to X4 independently = N, O, S, (un)substituted C, etc.; X5 = CH, N, or (un)substituted NH; wherein at least one of X1 to X4 is a carbon atom connected to Q1; A = (un)substituted ring; Q1 = C=O, C=S, alkylene, etc.; m = 1, 2, 3, or 4; Y = N, O, or absent; R1 = alkyl, halo, (hetero)aryl, etc.; R2 = alkyl, alkenyl, aryl, etc.; R3 and R4 independently = alkyl, aryl, heteroaryl, etc.; R3 and R4 together with the nitrogen atom to which R3 and R4 are bound form a ring] and pharmaceutically acceptable salts thereof, are claimed and exemplified. Example compound II was prepared a multistep procedure (preparation given). Exemplified I were evaluated for DNA binding activity using recombinant His-tag Y220C p53 DBD protein and TR-FRET anal. with some invention candidates demonstrating SC150 results in the range of 0μM to less than 2μM. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation. The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Recommanded Product: 1340372-11-3

The Article related to heteroaryl indole preparation mutant p53 restoration cancer progression, dna binding oncogene p53 stabilization heteroaryl indole, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 1340372-11-3

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

On September 10, 2020, Cregg, James Joseph; Buckl, Andreas; Aay, Naing; Tambo-Ong, Arlyn A.; Koltun, Elena S.; Gill, Adrian Liam; Thompson, Severin; Gliedt, Micah J. published a patent.Reference of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Preparation of bicyclic heterocyclyl compounds as SOS1 modulators. And the patent contained the following:

The present disclosure is directed to the title compounds I [Q1 = CH or N; Q4 = CH, C, or N; each Q2 = (independently) CR1 or N (wherein one Q2 = N and the other Q2 = CR1); each Q3 and Q5 = (independently) (un)substituted CH2, NH, CO, O, S, or SO2; wherein at least one of Q1-Q5 = N, (un)substituted NH, O, or SO2; m = 0-3; n = 0-3; wherein when m = 0, then n is not 0; R1 = H, alkyl, halo, etc.; L2 = a bond, C(O), C(O)O, etc.; R2 = H, alkyl, cycloalkyl, etc.; R3 and R4 = (independently) H or alkyl optionally substituted with halo or OH; wherein at least one of R3 and R4 = H or wherein R3 and R4 together with the atom to which they are attached combine to form a 3-6 membered cycloalkyl; A = (un)substituted 6-membered aryl or 5-6 membered heteroaryl; with the proviso] or pharmaceutically acceptable salts, solvates, isomers, prodrugs, or tautomers thereof, that are modulators of SOS1 and their use in the treatment of disease. E.g., a multi-step synthesis of (1R)-II, starting from 2,4-dichloro-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidine and morpholine-4-carbonyl chloride, was described. Exemplified compounds I were evaluated for their activity as SOS1 modulators (data given for representative compounds I). Also disclosed are pharmaceutical compositions comprising compounds I. The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Reference of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

The Article related to bicyclic heterocyclyl compound pyrrolopyrimidinamine cyclopentapyrimidinamine pyrimidoazepinamine preparation sos1 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

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

On November 18, 2021, Vu, Binh; Dominique, Romyr; Li, Hongju; Fahr, Bruce; Good, Andrew published a patent.Recommanded Product: 1340372-11-3 The title of the patent was Preparation of heteroaryl-substituted indole derivatives for restoring mutant p53 function. And the patent contained the following:

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The disclosure provided compounds of formula I capable of binding to mutant p53 and restoring the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. Compounds of formula I [wherein X1 to X4 independently = N, O, S, (un)substituted C, etc.; X5 = CH, N, or (un)substituted NH; wherein at least one of X1 to X4 is a carbon atom connected to Q1; A = (un)substituted ring; Q1 = C=O, C=S, alkylene, etc.; m = 1, 2, 3, or 4; Y = N, O, or absent; R1 = alkyl, halo, (hetero)aryl, etc.; R2 = alkyl, alkenyl, aryl, etc.; R3 and R4 independently = alkyl, aryl, heteroaryl, etc.; R3 and R4 together with the nitrogen atom to which R3 and R4 are bound form a ring] and pharmaceutically acceptable salts thereof, are claimed and exemplified. Example compound II was prepared a multistep procedure (preparation given). Exemplified I were evaluated for DNA binding activity using recombinant His-tag Y220C p53 DBD protein and TR-FRET anal. with some invention candidates demonstrating SC150 results in the range of 0μM to less than 2μM. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation. The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Recommanded Product: 1340372-11-3

The Article related to heteroaryl indole preparation mutant p53 restoration cancer progression, dna binding oncogene p53 stabilization heteroaryl indole, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 1340372-11-3

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

On September 10, 2020, Cregg, James Joseph; Buckl, Andreas; Aay, Naing; Tambo-Ong, Arlyn A.; Koltun, Elena S.; Gill, Adrian Liam; Thompson, Severin; Gliedt, Micah J. published a patent.Reference of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Preparation of bicyclic heterocyclyl compounds as SOS1 modulators. And the patent contained the following:

The present disclosure is directed to the title compounds I [Q1 = CH or N; Q4 = CH, C, or N; each Q2 = (independently) CR1 or N (wherein one Q2 = N and the other Q2 = CR1); each Q3 and Q5 = (independently) (un)substituted CH2, NH, CO, O, S, or SO2; wherein at least one of Q1-Q5 = N, (un)substituted NH, O, or SO2; m = 0-3; n = 0-3; wherein when m = 0, then n is not 0; R1 = H, alkyl, halo, etc.; L2 = a bond, C(O), C(O)O, etc.; R2 = H, alkyl, cycloalkyl, etc.; R3 and R4 = (independently) H or alkyl optionally substituted with halo or OH; wherein at least one of R3 and R4 = H or wherein R3 and R4 together with the atom to which they are attached combine to form a 3-6 membered cycloalkyl; A = (un)substituted 6-membered aryl or 5-6 membered heteroaryl; with the proviso] or pharmaceutically acceptable salts, solvates, isomers, prodrugs, or tautomers thereof, that are modulators of SOS1 and their use in the treatment of disease. E.g., a multi-step synthesis of (1R)-II, starting from 2,4-dichloro-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidine and morpholine-4-carbonyl chloride, was described. Exemplified compounds I were evaluated for their activity as SOS1 modulators (data given for representative compounds I). Also disclosed are pharmaceutical compositions comprising compounds I. The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Reference of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

The Article related to bicyclic heterocyclyl compound pyrrolopyrimidinamine cyclopentapyrimidinamine pyrimidoazepinamine preparation sos1 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

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

On April 3, 2014, Eskildsen, Joergen published a patent.Recommanded Product: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Preparation of indolylalkylamide derivatives for use as positive allosteric modulators of nicotinic acetylcholine receptor. And the patent contained the following:

Title compounds I [R1, R2, R4, and R5 independently = H, F, CN, (un)substituted alkyl, alkenyl, or alkynyl; R3 = H, CN, (un)substituted alkyl, alkenyl, or alkynyl; R6 = H or Me; Q = substituted isoxazolyl, isothiazolyl, or pyrazolyl], and their pharmaceutically acceptable salts, are prepared and disclosed as pos. allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor. Thus, e.g., II was prepared by a multistep procedure (preparation given). I were evaluated in α7 NNR receptor PAM flux activity assays, e.g., II demonstrated an EC50 value of 2200 nM. The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Recommanded Product: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

The Article related to indolylalkylamide preparation pos allosteric modulators nicotinic acetylcholine receptor, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

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

On January 16, 2020, Brace, Gareth Neil; Brookings, Daniel Christopher; Foulkes, Gregory; Lecomte, Fabien Claude published a patent.Name: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Spirocyclic indane analogs as IL-17 modulators and their preparation. And the patent contained the following:

A series of substituted spirocyclic indane derivatives of formula I, and analogs thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders. Compounds of formula I wherein ring A is C3-9 cycloalkyl, C3-7 heterocycloalkyl and C4-9 heterobicycloalkyl; B is CR2 and N; D is CR3 and N; E is CR4 and N; XY is OCY1Y2, NHSO2 and derivatives, CO2, etc.; R1 is (un)substituted C1-6 alkyl, (un)substituted C3-9 cycloalkyl, (un)substituted aryl, (un)substituted heteroaryl, etc.; R2, R3 and R4 H, halo, CN, C1-6 alkyl, etc.; Y1 is H, halo, CN, CF3, etc.; Y2 is H, halo and C1-6 alkyl; and N-oxides as pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of lithium 2-cyclooctyl-2-(3-methylisoxazole-4-carboxamido)acetate with spiro[indene-1,4′-oxane]-5-amine. The invention compounds were evaluated for their IL-17 modulatory activity (some data given). The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Name: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

The Article related to spirocyclic indane preparation il17 modulator, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Name: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

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

On March 29, 2012, Bartolozzi, Alessandra; Bosanac, Todd; Chen, Zhidong; De Lombaert, Stephane; Huber, John D.; Liu, Weimin; Lo, Ho Yin; Loke, Pui Leng; Riether, Doris; Tye, Heather; Wu, Lifen; Zindell, Renee M. published a patent.Quality Control of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Preparation of oxadiazole inhibitors of leukotriene production. And the patent contained the following:

The title compounds I [R1, R2 = H, alkyl, carboxyxlice (with the proviso that both R1 and R2 are not hydrogen); R3 = (un)substituted 5-11 membered heteroaryl ring containing 1-3 heteroatoms selected from N, O and S; R4 = H, halo, alkyl, nitrile; R5 = (un)substituted alkyl, C3-10 carbocycle, 5-11 membered heterocycle, etc.], useful in treating a leukotriene-mediated disorders, were prepared Thus, reacting compound II (preparation given) with the pyrimidine derivative III afforded the title compound IV. Biol. testing showed that compounds I are effective inhibitors of 5-lipoxygenase activating protein (FLAP) and thus inhibit leukotriene production (IC50 values were given). The invention also relates to pharmaceutical compositions comprising compounds I, methods of I in the treatment of various diseases and disorders, processes for preparing I and intermediates useful in these processes. The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Quality Control of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

The Article related to oxadiazole preparation leukotriene production ltb4 inhibitor, lipoxygenase activating protein flap inhibitor oxadiazole preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Quality Control of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

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