Category: 215610-30-3

On December 7, 2017, Eriksen, Birgitte Langer; Gustafsson, Magnus; Hougaard, Charlotte; Jacobsen, Thomas Amos; Jefson, Martin R.; Klein, Jessica; Larsen, Janus Schreiber; Lowe, John A., III; McCall, John M.; Strooebaek, Dorte; Von Schoubye, Nadia Lyboel; Keaney, Gregg F. published a patent.Safety of 5-Methoxy-1H-pyrazole The title of the patent was Preparation of cycloalkylamino nitrogen heterocycles as potassium channel modulators for the treatment and prevention of disorders. And the patent contained the following:

The invention relates to preparation of cycloalkylamino nitrogen heterocycles of formula I wherein all the variables are as defined in the disclosure, and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions which can be affected by potassium channel modulation. Also provided are pharmaceutical compositions comprising the compounds I pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with potassium channels. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Safety of 5-Methoxy-1H-pyrazole

The Article related to cycloalkylamino nitrogen heterocycle potassium channel modulator disease treatment prophylaxis, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of 5-Methoxy-1H-pyrazole

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

On August 11, 2016, Moussy, Alain; Benjahad, Abdellah; Pez, Didier; Sandrinelli, Franck; Martin, Jason; Picoul, Willy; Chevenier, Emmanuel published a patent.Computed Properties of 215610-30-3 The title of the patent was Preparation of phenylamino-oxazole or phenylamino-thiazole compounds with antitumor activity. And the patent contained the following:

The invention relates to compounds of formula I and pharmaceutical compositions thereof, useful to destroy, inhibit, or prevent the growth or spread of cells, especially malignant cells, into surrounding tissues implicated in a variety of human and animal diseases. I [wherein A = an optionally substituted heterocyclyl; B = aryl or heteroaryl; X = N, C-R6; R1, R2, R4, R5, and R6 independently = H, CN, CF3, etc.; R3 = H] or a pharmaceutically acceptable salt thereof, which are claimed and exemplified. Reaction of N-(5-methoxy-2-methylphenyl)acetamide with 5-[6-(1H-pyrazol-1-yl)pyridin-3-yl]-2-chlorooxazole provided example compound II in 68% yield. Candidate compounds of I were evaluated for antitumor activity in solid and hematol. tumor cells using CellTiter-Blue cell-based survival proliferation assay (data given). The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Computed Properties of 215610-30-3

The Article related to phenylaminothiazole phenylaminooxazle antitumor malignancy, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Computed Properties of 215610-30-3

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

On December 6, 2007, Blom, Petra; Defert, Olivier; Kaletta, Titus; Leysen, Dirk Casimir Maria published a patent.Name: 5-Methoxy-1H-pyrazole The title of the patent was Preparation of thiazole and pyridinyl carboxamides and related heterocyclic analogs that interact with ion channels. And the patent contained the following:

Title compounds I [X = substituted thiazole, pyridine, oxopiperidine, etc.; R1 = H, halo, OH, NO2, alkyl, etc.; L1 = alkylene, cycloalkylene, pyrrolidinlenealkylene, etc.; m = 0-4], and their pharmaceutically acceptable salts, are prepared and disclosed as being capable of interacting with ion channels, in particular ion channels from the kv family. Thus, e.g., II was prepared by coupling of the corresponding 4-bromothiazole derivative (preparation given) with Ph boronic acid. Inhibition assays of the kv4.3 ion channel are described, e.g., II provided above 50% inhibition. The invention also relates to methods for preparing said compounds, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in methods for treatment of the human and animal body. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Name: 5-Methoxy-1H-pyrazole

The Article related to thiazole carboxamide derivative preparation ion channel modulator kv, pyridine carboxamide derivative preparation ion channel modulator kv, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Name: 5-Methoxy-1H-pyrazole

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

On April 1, 2022, Huang, Liye; Li, Hua; Liu, Huabin; Wang, Zhiyuan; Li, Tao; Ouyang, Feiyan; Zhang, Xinmiao published a patent.Quality Control of 5-Methoxy-1H-pyrazole The title of the patent was Preparation of N-(3-(2-((1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-1H-indol-7-yl)pyrrolidine-2-carboxamide derivatives as Jak1 kinase inhibitors. And the patent contained the following:

The invention discloses the preparation of N-(3-(2-((1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-1H-indol-7-yl)pyrrolidine-2-carboxamide derivatives with general formula I as Jak1 kinase inhibitors wherein R1=H, halogen, substituted or unsubstituted C1-C6 linear or branched alkyl, substituted or unsubstituted C3-C6 cycloalkyl or ORa; R2=H, substituted or unsubstituted C1-C6 straight or branched chain alkyl, substituted or unsubstituted C3-C10 cycloalkyl, substituted or unsubstituted C2-C10 heterocycloalkyl; R3=H, halogen, cyano radical, unsubstituted or halogenated C1-C6 straight or branched chain alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl; R4=SO2Ra2, CORa2, COORa2, substituted or unsubstituted C3-C10 cycloalkyl, substituted or unsubstituted C2-C10 heterocycloalkyl; R5=F, cyano, C1-C6 straight or branched chain alkyl, C3-C6 cycloalkyl or ORa5; Ra, Ra2, Ra5=H, substituted or unsubstituted C1-C10 straight or branched chain alkyl, substituted or unsubstituted C2-C10 alkenyl, substituted or unsubstituted C2-C10 alkynyl, substituted or unsubstituted C3 -C10 cycloalkyl, substituted or unsubstituted C2-C10 heterocycloalkyl; R6=D, halogen, cyano, hydroxyl, unsubstituted or halogenated C1-C6 straight or branched chain alkyl, C2-C6 alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, C2-C6heterocycloalkyl, ORa6, SRa6, NRb6Rc6, CORa6, CONRb6Rc6, COORd6, SO2Ra6, SO2NRb6Rc6, NRb6CORa6, NRd6CONRb6Rc6, NRb6SO2Ra6, NRd6SO2NRb6Rc6 or SORa. For example, (S)-N-(3-(5-fluoro-2-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-1H-indol-7-yl)-1-(methylsulfonyl)pyrrolidine-2-carboxamide was prepared from Me 3-methoxy-1H-pyrazole-4-carboxylate by hydrolysis, nitration, reduction, substitution reaction, amidation and so on. The title compounds have good inhibitory activity against Jak1 kinase and can be used to prepare drugs for the treatment of inflammation, autoimmune diseases or cancer. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Quality Control of 5-Methoxy-1H-pyrazole

The Article related to amidation preparation pyrimidine treatment human inflammation autoimmune disease cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 5-Methoxy-1H-pyrazole

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

On December 7, 2017, Eriksen, Birgitte Langer; Gustafsson, Magnus; Hougaard, Charlotte; Jacobsen, Thomas Amos; Jefson, Martin R.; Klein, Jessica; Larsen, Janus Schreiber; Lowe, John A., III; McCall, John M.; Strooebaek, Dorte; Von Schoubye, Nadia Lyboel; Keaney, Gregg F. published a patent.Safety of 5-Methoxy-1H-pyrazole The title of the patent was Preparation of cycloalkylamino nitrogen heterocycles as potassium channel modulators for the treatment and prevention of disorders. And the patent contained the following:

The invention relates to preparation of cycloalkylamino nitrogen heterocycles of formula I wherein all the variables are as defined in the disclosure, and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions which can be affected by potassium channel modulation. Also provided are pharmaceutical compositions comprising the compounds I pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with potassium channels. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Safety of 5-Methoxy-1H-pyrazole

The Article related to cycloalkylamino nitrogen heterocycle potassium channel modulator disease treatment prophylaxis, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of 5-Methoxy-1H-pyrazole

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

On November 11, 2021, Tang, Xinxing; Horan, Joshua Courtney; Mente, Scot Richard; Pelish, Henry Efrem; Shair, Matthew D.; Tangpeerachaikul, Anupong published a patent.Formula: C4H6N2O The title of the patent was Preparation of heteroaromatic macrocyclic ether chemotherapeutic agents for treatment of cancer. And the patent contained the following:

Disclosed are heterocyclic heteroaromatic macrocyclic ether compounds of formula I useful alone or in combination addnl. tyrosine kinase inhibitors for the treatment or prevention of cancer. Compounds of formula I [wherein Q = CH or N; Z = CR5 or N; X = 5-membered heteroarylene, comprising 1 to 3 heteroatoms selected from N, O, and S, wherein the 5-membered heteroarylene is substituted with 0, 1, or 2 occurrences of R2, with proviso; Y = 5- to 6-membered heteroarylene, comprising 1 to 3 heteroatoms selected from N, O, and S, wherein the heteroarylene is substituted with 0, 1, or 2 occurrences of R3; R1 = H, Me, and hydroxymethyl; each R2 and R3 independently = H, CN, halo, C1-4alkoxy, etc.; R4 and R5 independently = H or F] and pharmaceutically acceptable salts and pharmaceutical compositions thereof, are claimed and exemplified. Example compound II was prepared from a multistep synthesis (preparation given). Exemplified I were evaluated for inhibition of mutant and wild-type ROS1 and ALK kinases from which II demonstrated apparent inhibitory constants of <50 nM for each kinase. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Formula: C4H6N2O

The Article related to heteroaromatic macrocyclic ether preparation cancer ros1 alk kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.Formula: C4H6N2O

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

On September 6, 2019, Tang, Haifeng; Boyce, Sarah; Hanson, Michael; Nie, Zhe published a patent.Name: 5-Methoxy-1H-pyrazole The title of the patent was Compounds and compositions for treating conditions associated with APJ receptor activity. And the patent contained the following:

The invention relates to substituted triazoles of formula I and pharmaceutically acceptable salts thereof (wherein R1 is (Y1)0-1Y2; Y1 is (un)substituted C1-6 alkylene; Y2 is (un)substituted C3-10 cycloalkyl, (un)substituted C6-10 aryl, (un)substituted heteroaryl, etc.; R2 is (un)substituted C6-10 aryl, (un)substituted heteroaryl; R3 is (Y3)0-1Y4; Y3 is (un)substituted C1-6 alkylene; Y4 is (un)substituted C3-6 cycloalkyl, (un)substituted C6-10 aryl, (un)substituted 5- to 10-membered heteroaryl; R4 is H and C1-3 alkyl;) as apelin receptor modulators; their preparation and use in the treatment of pulmonary arterial hypertension. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their APJ modulatory activities. From the assay, it was determined that compound II exhibited EC50 value of less than 1 nM. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Name: 5-Methoxy-1H-pyrazole

The Article related to triazole preparation apj receptor modulator treatment pulmonary arterial hypertension, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Name: 5-Methoxy-1H-pyrazole

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

On January 17, 2019, Hoffman, Thomas James; Stierli, Daniel; Pitterna, Thomas; Rajan, Ramya published a patent.Application of 215610-30-3 The title of the patent was Preparation of oxadiazole derivatives as microbicides. And the patent contained the following:

Compounds of the formula I useful as pesticides, especially as fungicides. Compounds of formula I wherein Z is substituted pyrazolyl; R1, R2, R3 and R4 are independently H and F, provided that 0 – 2 of R1 – R4 are F; R5 and R6 are independently H and Me; and salts and N-oxides thereof, are claimed. Example compound II was prepared by amidation of 1-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]pyrazole-4-carboxylic acid with N-cyclopropylethylamine. The invention compounds were evaluated for their fungicidal activity (data given). The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Application of 215610-30-3

The Article related to oxadiazole preparation fungicide microbicide, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Application of 215610-30-3

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

On November 11, 2021, Horan, Joshua Courtney; Mente, Scot Richard; Pelish, Henry Efrem; Shair, Matthew D.; Tang, Xinxing; Tangpeerachaikul, Anupong published a patent.Related Products of 215610-30-3 The title of the patent was Preparation of heteroaromatic macrocyclic ether chemotherapeutic agents for treatment of cancer. And the patent contained the following:

Disclosed are heterocyclic heteroaromatic macrocyclic ether compounds of formula I useful alone or in combination addnl. tyrosine kinase inhibitors for the treatment or prevention of cancer. Compounds of formula I [wherein Q = CH or N; Z = CR5 or N; X = 5-membered heteroarylene, comprising 1 to 3 heteroatoms selected from N, O, and S, wherein the 5-membered heteroarylene is substituted with 0, 1, or 2 occurrences of R2, with proviso; Y = 5- to 6-membered heteroarylene, comprising 1 to 3 heteroatoms selected from N, O, and S, wherein the heteroarylene is substituted with 0, 1, or 2 occurrences of R3; R1 = H, Me, and hydroxymethyl; each R2 and R3 independently = H, CN, halo, C1-4alkoxy, etc.; R4 and R5 independently = H or F] and pharmaceutically acceptable salts and pharmaceutical compositions thereof, are claimed and exemplified. Example compound II was prepared from a multistep synthesis (preparation given). Exemplified I were evaluated for inhibition of mutant and wild-type ROS1 and ALK kinases from which II demonstrated apparent inhibitory constants of <50 nM for each kinase. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Related Products of 215610-30-3

The Article related to heteroaromatic macrocyclic ether preparation cancer ros1 alk kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.Related Products of 215610-30-3

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

On February 18, 2021, Abela, Alexander Russell; Anderson, Corey Don; Bookser, Brett C.; Busch, Brett B.; Clemens, Jeremy J.; Cleveland, Thomas; Coon, Timothy Richard; Frieman, Bryan; Ghirmai, Senait G.; Gulevich, Anton V.; Hadida Ruah, Sara Sabina; Ishihara, Yoshihiro; Khatuya, Haripada; McCartney, Jason; Miller, Mark Thomas; Paraselli, Prasuna; Pierre, Fabrice; Termin, Andreas; Swift, Sara E.; Uy, Johnny; Vogel, Carl V.; Zhou, Jinglan; Grootenhuis, Peter published a patent.SDS of cas: 215610-30-3 The title of the patent was Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator and preparation. And the patent contained the following:

This disclosure provides compounds of formula I as modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR), pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical compositions, and processes for making such modulators. Compound I, wherein ring A is a Ph, indole, 5-membered hetereoaryl ring, etc.; ring B is Ph, pyridinyl and pyrimidinyl ring; X is O, NH and N(C1-6 alkyl); each R1 is independently C1-6 alkyl, C1-6 alkoxyl,C1-6 haloalkyl; m is 0, 1, 2, 3 and 4; each R2 is independently halo, cyano, (un)substituted C1-6 alkyl; n is 0, 1 and 2; R0 is H, halo, cyano, etc.; each R3 is (un)substituted C1-6 alkyl and two R3 are joined to form C3-6 cycloaklyl ring; Z is a divalent linker (L)r wherein r is 1, 2, 3, 4, 5 and 6; each L is independently C(R8)(R9), O, NRb, etc.; each R8 and R9 is independently H, halo, C1-6 haloalkyl, etc.; and tautomers, deuterated derivatives and pharmaceutically acceptable salts thereof, are claimed. Compound II was prepared using a multi-step procedure (procedure given). Compound II was tested for CFTR modulatory activity giving an EC50 of <1μM. Compounds of the invention were tested for their CFTR modulatory activity (data given). The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).SDS of cas: 215610-30-3

The Article related to macrocycle preparation cftr modulator cystic fibrosis, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.SDS of cas: 215610-30-3

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