Tag: 100-200

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 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

Kendall, Jackie D.; O’Connor, Patrick D.; Marshall, Andrew J.; Frederick, Raphael; Marshall, Elaine S.; Lill, Claire L.; Lee, Woo-Jeong; Kolekar, Sharada; Chao, Mindy; Malik, Alisha; Yu, Shuqiao; Chaussade, Claire; Buchanan, Christina; Rewcastle, Gordon W.; Baguley, Bruce C.; Flanagan, Jack U.; Jamieson, Stephen M. F.; Denny, William A.; Shepherd, Peter R. published an article in 2012, the title of the article was Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors.Recommanded Product: 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid And the article contains the following content:

A novel series of pyrazolo[1,5-a]pyridines were prepared as PI3 kinase inhibitors, and their selectivity for the p110α isoform over the other Class Ia PI3 kinases was demonstrated. The SAR around the pyrazolo[1,5-a]pyridine ring system was investigated, and N’-[(5-cyanopyrazolo[1,5-a]pyridin-3-yl)methylene]-N,2-dimethyl-5-nitrobenzenesulfonic acid hydrazide was shown to be a particularly potent example (p110α IC50 0.9 nM). This compound inhibits cell proliferation and phosphorylation of Akt/PKB, a downstream marker of PI3 kinase activity, and showed in vivo activity in an HCT-116 human xenograft model. The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).Recommanded Product: 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid

The Article related to pyrazolopyrazinylmethylene benzenesulfonylhydrazine preparation pi3 kinase inhibitor anticancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Recommanded Product: 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid

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

On November 26, 2020, Bandiera, Tiziano; Bertozzi, Fabio; Di Fruscia, Paolo; Sorana, Federico; Berti, Francesco; Rodriguez Gimeno, Alejandra; Caci, Emanuela; Ferrera, Loretta; Pedemonte, Nicoletta; Vicente Galietta, Luis Juan published a patent.Synthetic Route of 1186608-73-0 The title of the patent was Preparation of pyrazolopyridines and related heterocycles and compositions containing them for the treatment of cystic fibrosis. And the patent contained the following:

The invention relates to preparation of pyrazolopyridines and related heterocycles of formula (I) or pharmaceutically acceptable salts or solvates thereof: It further discloses a pharmaceutical composition comprising the compounds I and their uses, in particular to modulate CFTR protein or ABC protein activities. Compounds I wherein R1 is H; Z is CO or SO2; X1-X4 each independently is CRVII and N, with the proviso that the number of nitrogen atoms in the ring is comprised from O to 2; R2 is H, OH, NO, etc.; A1-A4 each independently is O, SO2, CO, etc.; B represents an unsubstituted or a substituted aromatic or heteroaromatic ring; n and m are each independently selected from the group consisting of O, 1, 2; etc., are claimed. The example compound II was prepared using 3-hydrazinobenzoic acid as starting material (procedure given). Compounds I were evaluated for their biol. activity (data given). Compounds I and pharmaceutical composition comprising them, are modulators of CFTR protein or ABC protein activities, and can be used in treatment of cystic fibrosis and other diseases. The experimental process involved the reaction of 3-Methyl-1H-pyrazolo[3,4-b]pyridin-5-amine(cas: 1186608-73-0).Synthetic Route of 1186608-73-0

The Article related to pyrazolopyridine preparation cftr modulator abc protein cystic fibrosis treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Synthetic Route of 1186608-73-0

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

On September 11, 2009, Ahrendt, Kateri A.; Buckmelter, Alexandre J.; De Meese, Jason; Grina, Jonas; Hansen, Joshua D.; Laird, Ellen R.; Lunghofer, Paul; Moreno, David; Newhouse, Brad; Ren, Li; Seo, Jeongbeob; Tian, Hongqi; Wenglowsky, Steven Mark; Feng, Bainian; Gunzner, Janet; Malesky, Kim; Mathieu, Simon; Rudolph, Joachim; Wen, Zhaoyang; Young, Wendy B. published a patent.Reference of 3-Methyl-1H-pyrazolo[3,4-b]pyridin-5-amine The title of the patent was N-Pyrazolo[3,4-b]pyridinyl benzamide derivatives as Raf inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Compounds of formula I are useful for inhibition of Raf kinases. Methods of using compounds of formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo prevention or treatment of Raf-mediated disorders in mammalian cells, or associated pathol. conditions are disclosed. Compounds of formula I wherein R1 and R2 are independently H, halo, CN, C1-3 alkyl and C1-3 alkoxy; R3 is H, halo and C1-3 alkyl; R4 is C3-5 cycloalkyl, C1-6 alkyl, C2-6 alkenyl, etc.; R5 is H, halo, CN, NH2 and derivatives, etc.; and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cyclization of 1H-pyrazol-5-amine with 2-bromomalonaldehyde; the resulting 5-bromo-1H-pyrazolo[3,4-b]pyridine underwent alkylation with 2-(trimethylsilyl)ethoxymethyl chloride to give 5-bromo-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-pyrazolo[3,4-b]pyridine, which underwent cross-coupling with tert-Bu carbamate to give tert-Bu 1-((2-(trimethylsilyl)ethoxy)methyl)-1H-pyrazolo[3,4-b]pyridin-5-ylcarbamate, which underwent hydrolysis to give 1H-pyrazolo[3,4-b]pyridin-5-amine, which underwent amidation with 2.6-difluoro-3-(propylsulfonamido)benzoic acid to give compound II. All the invention compounds were evaluated for their Raf inhibitory activity. From the assay, it was determined that compound II along with the other example compound exhibited IC50 values of less than 1 μM. The experimental process involved the reaction of 3-Methyl-1H-pyrazolo[3,4-b]pyridin-5-amine(cas: 1186608-73-0).Reference of 3-Methyl-1H-pyrazolo[3,4-b]pyridin-5-amine

The Article related to pyrazolopyridinyl benzamide preparation raf inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Reference of 3-Methyl-1H-pyrazolo[3,4-b]pyridin-5-amine

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 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 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

Seela, Frank; Menkhoff, Sabine published an article in 1986, the title of the article was 2′-Deoxyribofuranosides of 6-oxoallopurinol and of related 4,6-disubstituted pyrazolo[3,4-d]pyrimidines.Computed Properties of 98138-75-1 And the article contains the following content:

Deoxypentofuranosylpyrazolopyrimidine I (R = OMe) was aminated to I (R = NH2) and demethylated to pyrimidinones II and III. I (R = OMe) was prepared by phase-transfer glycosidation of methoxylated or chlorinated pyrimidine base. The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).Computed Properties of 98138-75-1

The Article related to pentofuranosylpyrazolopyrimidinedione, pyrazolopyrimidine deoxypentofuranosyl glycosidation, methoxypyrazolopyrimidinylpentofuranose preparation hydrolysis, Carbohydrates: Nucleosides and Nucleotides, Cobalamins, Riboflavin and other aspects.Computed Properties of 98138-75-1

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