Category: 1014631-89-0

On April 10, 2008, Elzein, Elfatih; Kalla, Rao V.; Li, Xiaofen; Perry, Thao; Gimbel, Art; Zeng, Dewan; Lustig, David; Leung, Kwan; Zablocki, Jeff published an article.COA of Formula: C9H7N3O2 The title of the article was Discovery of a Novel A2B Adenosine Receptor Antagonist as a Clinical Candidate for Chronic Inflammatory Airway Diseases. And the article contained the following:

Recently, the authors have reported a series of new 1,3-sym. (R1 = R3) substituted xanthines which have high affinity and selectivity for the human adenosine A2B receptors (hA2B-AdoR). Unfortunately, this class of compounds had poor pharmacokinetic properties. This prompted us to investigate the effect of differential alkyl substitution at the N-1 and N-3 positions (N1-R ≠ N3-R) on A2B-AdoR affinity and selectivity; the authors had the dual objectives of enhancing affinity and selectivity for the A2B-AdoR, as well as improving oral bioavailability. This effort has led to the discovery of compound (I), that displayed high affinity and selectivity for the hA2B-AdoR (Ki = 22 nM). In addition, compound I showed high functional potency in inhibiting the accumulation of cAMP induced by 5′-N-ethylcarboxamidoadenosine in HEK-A2B-AdoR and NIH3T3 cells with KB values of 6 and 2 nM, resp. In a single ascending-dose phase I clin. study, compound I had no serious adverse events and was well tolerated. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).COA of Formula: C9H7N3O2

The Article related to adenosine receptor antagonist preparation antiinflammatory inflammatory airway disease pharmacokinetics, Pharmacology: Structure-Activity and other aspects.COA of Formula: C9H7N3O2

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

On April 21, 2011, Bretschneider, Thomas; Fuesslein, Martin; Koehler, Adeline; Muehlthau, Friedrich August; Franken, Eva-Maria; Voerst, Arnd published a patent.Computed Properties of 1014631-89-0 The title of the patent was Synthesis of 1-(pyrid-3-yl)-pyrazoles and 1-(pyramid-5-yl)-pyrazoles and use as insecticide and/or acaricide.. And the patent contained the following:

The invention relates to the use of partially known heterocyclic compounds for combating animal pests, including arthropods and in particular insects, and further relates to novel heterocyclic compounds and to methods for synthesis thereof. Also disclosed are the rates of effectiveness of selected compounds, relating to the invention, in killing particular insect and acarid pests on sample crops. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Computed Properties of 1014631-89-0

The Article related to pyridyl pyramidyl pyrazole insecticide acaricide crop protection, Agrochemical Bioregulators: Invertebrate and other aspects.Computed Properties of 1014631-89-0

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

On April 21, 2011, Bretschneider, Thomas; Voerste, Arnd; Fuesslein, Martin; Koehler, Adeline; Goergens, Ulrich published a patent.Reference of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Amides and thioamides as pesticides and their preparation. And the patent contained the following:

The invention relates to amides and thioamides of formula I, to a method for the production thereof, and to the use thereof for combating pests. Compounds of formula I wherein G is N, CH, C-halo, C-NO2, C-CN, etc.; R1 is H, alkyl, haloalkyl, cycloalkyl, halo, etc.; X is O and S; R2 is H, alkyl, haloalkyl, alkoxy, etc.; R3 is H, alkyl, haloalkyl, cyanoalkyl, alkenyl, etc.; and their salts and N-oxides thereof, are claimed. Example compound II was prepared by N-arylation of pyrazole-4-carbonitrile with 3-bromopyridine; the resulting 1-(pyridin-3-yl)-1H-pyrazole-4-carbonitrile underwent hydrolysis to give the corresponding carboxylic acid, which underwent chlorination to give the corresponding carboxylic acid chloride hydrochloride, which underwent amidation with ethylamine to give compound II. All the invention compounds were evaluated for their pesticidal activity (some data given). The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Reference of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid

The Article related to amide thioamide preparation pesticide, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Reference of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid

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

On March 31, 2022, Lanier, Marion; Boehm, Marcus; Huang, Liming; Martinborough, Esther; Sainz, Marcos; Selfridge, Brandon; Yeager, Adam published a patent.Computed Properties of 1014631-89-0 The title of the patent was Preparation of modulators of MAS-related G-protein receptor X2 and related products and methods. And the patent contained the following:

Methods are provided for modulating MRGPR X2 generally, or for treating a MRGPR X2 or a MRGPR X2 ortholog dependent condition, more specifically, by contacting the MRGPR X2 or the MRGPR X2 ortholog by administering to a subject in need thereof, resp., an effective amount of a compound of formula I and pharmaceutically acceptable salts, isomers, hydrates, solvates and isotopes thereof. Compounds of formula I, wherein R1 is cycloalkyl, aryl, heterocyclyl;, R2, R3, R4, R5, R6 are independently H, aryl, cycloalkyl, heteroaryl, heterocyclyl, etc.; each Rx is independently H, aryl, CN, etc.; W is N and CR7 and Z is N and CR8; R7 and R8 are independently H, aryl, cycloalkyl, heteroaryl, etc.; and pharmaceutically acceptable salts, isomers, hydrates, solvates and isotopes thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their MRGPR X2 modulatory activity (some data given). The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Computed Properties of 1014631-89-0

The Article related to quinoline preparation mrgpr2 x2 modulator, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Computed Properties of 1014631-89-0

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

On April 28, 2022, Lanier, Marion; Boehm, Marcus; Huang, Liming; Martinborough, Esther; Sainz, Marcos; Selfridge, Brandon; Yeager, Adam published a patent.Application of 1014631-89-0 The title of the patent was Modulators of mas-related g-protein receptor x2 and related products and their use. And the patent contained the following:

Methods are provided for modulating MRGPRX2 or a MRGPRX2 ortholog generally, or for treating a MRGPRX2 or a MRGPRX2 ortholog dependent condition more specifically, by contacting the MRGPRX2 or the MRGPRX2 ortholog by administering to a subject in need thereof, resp., an effective amount of a compound having structure I: or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein W, Z, R1, R2, R3, R4, R5, R6 and Rx are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Application of 1014631-89-0

The Article related to mrgppx2 modulator preparation treatment disease, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application of 1014631-89-0

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

On March 10, 2016, Bergman, Ylva Elisabet; Foitzik, Richard Charles; Morrow, Benjamin Joseph; Camerino, Michelle Ang; Walker, Scott Raymond; Lagiakos, H. Rachel; Feutrill, John; Stevenson, Graeme Irvine; Stupple, Paul Anthony published a patent.SDS of cas: 1014631-89-0 The title of the patent was Preparation of tetrahydroisoquinoline derivatives as PRMT5 inhibitors. And the patent contained the following:

The invention relates to tetrahydroisoquinoline derivatives of formula I as PRMT5-inhibitors; their preparation and use in the treatment of cancer and hemoglobinopathy. Compounds of formula I, wherein n = 1 and 2; p is 0 and 1; R1 is halo and Me; R2a and R2b are independently F, H, Me and CH2OH; R2c and R2n are independently F, H, Me and CH2OH; R3a and R3b are independently H and Me; R4 is H and Me; R5 is H and Me; R6a and R6b are independently H and Me; A is (un)substituted Ph, (un)substituted naphthyl; and (un)substituted C5-12 heteroaryl, are claimed. Example compound II was prepared by amidation of 2-fluoro-4-(morpholine-4-carbonyl)benzoic acid with tert-Bu (S)-3-((R)-2-amino-1-hydroxyethyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate followed by BOC-deprotection. The invention compounds were evaluated for their PRMT5 inhibitory activity. From the assay, it was determined that example II exhibited IC50 value of 0.383 μM. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).SDS of cas: 1014631-89-0

The Article related to tetrahydroisoquinoline preparation prmt5 inhibitor treatment cancer hemoglobinopathy, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.SDS of cas: 1014631-89-0

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

On March 10, 2016, Bergman, Ylva Elisabet; Lessene, Romina; Ganame, Danny; Foitzik, Richard Charles; Morrow, Benjamin Joseph; Camerino, Michelle Ang; Walker, Scott Raymond; Lagiakos, H. Rachel; Feutrill, John; Stupple, Paul Anthony published a patent.Application of 1014631-89-0 The title of the patent was Preparation of aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5 inhibitors. And the patent contained the following:

The invention relates to compounds of formula I, II and III as PRMT5-inhibitors; their preparation and use in the treatment of cancer and hemoglobinopathy. Compounds of formula I, II and III wherein n = 1 and 2; R is H and Me; R1 is halo and Me; R2a and R2b are independently F, H, Me and CH2OH; R2c and R2n are independently F, H, Me and CH2OH; R3a and R3b are independently H and Me; R4a is OH, NH2, CONH2 and CH2OH; R4b is H and Me; R5 is H and Me; A is (un)substituted Ph, (un)substituted naphthyl; and (un)substituted C5-12 heteroaryl, are claimed. Example compound IV was prepared by acylation of 1-amino-3-((2,3-dihydro-1H-inden-2-yl)amino)propan-2-ol with 4-chlorobenzoic acid. The invention compounds were evaluated for their PRMT5 inhibitory activity. From the assay, it was determined that example IV exhibited IC50 value of 0.792 μM. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Application of 1014631-89-0

The Article related to aminoindane aminotetrahydronaphthalene aminobenzocyclobutane preparation prmt5 inhibitor treatment cancer hemoglobinopathy, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application of 1014631-89-0

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

On October 20, 2011, Bretschneider, Thomas; Koehler, Adeline; Fischer, Reiner; Fuesslein, Martin; Jescke, Peter; Kluth, Joachim; Muehlthau, Friedrich August; Voerste, Arnd; Malsam, Olga; Goergens, Ulrich; Sato, Yoshitaka published a patent.Recommanded Product: 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Preparation of novel heterocyclic compounds as pest control agents. And the patent contained the following:

The invention relates to amides and thioamides of formula I, to a method for the producing same, and to the use thereof for treating animal pests. Compounds of formula I wherein A1 and A2 are independently H, halo, CN, NO2, alkyl, cycloalkyl and alkoxy; G1 is N and CA1; G2 is substituted thiazolyl, thiadiazolyl, and pyrazolyl; are claimed. Example compound II was prepared by reduction of 3-(4-methyl-5-nitrothiazol)pyridine; the resulting 4-methyl-2-(pyridin-3-yl)thiazol-5-amine underwent acylation with 3,3,3-trifluoropropanoyl chloride to give compound II. All the invention compounds were evaluated for their pesticidal activity (data given). The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Recommanded Product: 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid

The Article related to heterocycle preparation pesticide, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Recommanded Product: 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid

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

On March 10, 2016, Bergman, Ylva Elisabet; Foitzik, Richard Charles; Morrow, Benjamin Joseph; Camerino, Michelle Ang; Walker, Scott Raymond; Lagiakos, H. Rachel; Feutrill, John; Stevenson, Graeme Irvine; Stupple, Paul Anthony published a patent.SDS of cas: 1014631-89-0 The title of the patent was Preparation of tetrahydroisoquinoline derivatives as PRMT5 inhibitors. And the patent contained the following:

The invention relates to tetrahydroisoquinoline derivatives of formula I as PRMT5-inhibitors; their preparation and use in the treatment of cancer and hemoglobinopathy. Compounds of formula I, wherein n = 1 and 2; p is 0 and 1; R1 is halo and Me; R2a and R2b are independently F, H, Me and CH2OH; R2c and R2n are independently F, H, Me and CH2OH; R3a and R3b are independently H and Me; R4 is H and Me; R5 is H and Me; R6a and R6b are independently H and Me; A is (un)substituted Ph, (un)substituted naphthyl; and (un)substituted C5-12 heteroaryl, are claimed. Example compound II was prepared by amidation of 2-fluoro-4-(morpholine-4-carbonyl)benzoic acid with tert-Bu (S)-3-((R)-2-amino-1-hydroxyethyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate followed by BOC-deprotection. The invention compounds were evaluated for their PRMT5 inhibitory activity. From the assay, it was determined that example II exhibited IC50 value of 0.383 μM. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).SDS of cas: 1014631-89-0

The Article related to tetrahydroisoquinoline preparation prmt5 inhibitor treatment cancer hemoglobinopathy, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.SDS of cas: 1014631-89-0

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

On March 10, 2016, Bergman, Ylva Elisabet; Lessene, Romina; Ganame, Danny; Foitzik, Richard Charles; Morrow, Benjamin Joseph; Camerino, Michelle Ang; Walker, Scott Raymond; Lagiakos, H. Rachel; Feutrill, John; Stupple, Paul Anthony published a patent.Application of 1014631-89-0 The title of the patent was Preparation of aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5 inhibitors. And the patent contained the following:

The invention relates to compounds of formula I, II and III as PRMT5-inhibitors; their preparation and use in the treatment of cancer and hemoglobinopathy. Compounds of formula I, II and III wherein n = 1 and 2; R is H and Me; R1 is halo and Me; R2a and R2b are independently F, H, Me and CH2OH; R2c and R2n are independently F, H, Me and CH2OH; R3a and R3b are independently H and Me; R4a is OH, NH2, CONH2 and CH2OH; R4b is H and Me; R5 is H and Me; A is (un)substituted Ph, (un)substituted naphthyl; and (un)substituted C5-12 heteroaryl, are claimed. Example compound IV was prepared by acylation of 1-amino-3-((2,3-dihydro-1H-inden-2-yl)amino)propan-2-ol with 4-chlorobenzoic acid. The invention compounds were evaluated for their PRMT5 inhibitory activity. From the assay, it was determined that example IV exhibited IC50 value of 0.792 μM. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Application of 1014631-89-0

The Article related to aminoindane aminotetrahydronaphthalene aminobenzocyclobutane preparation prmt5 inhibitor treatment cancer hemoglobinopathy, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application of 1014631-89-0

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