Category: 87674-15-5

On February 17, 2005, Vanotti, Ermes; D’Alessio, Roberto; Tibolla, Marcellino; Varasi, Mario; Montagnoli, Alessia; Santocanale, Corrado; Martina, Katia; Menichincheri, Maria published a patent.COA of Formula: C7H8FNO The title of the patent was Preparation of pyridylpyrrole derivatives active as kinase inhibitors. And the patent contained the following:

Pyridylpyrrole derivatives of formula I [R1 = H, amino, etc.; R2, R’2 = H, halo, etc.; further detail on R1 and R’2 is given; R3, R’3, R4, R’4 = H, alkyl, etc.; R5 = H, halo, etc.] and pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. Thus, 2-(2-cyclopentylaminopyridin-4-yl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one was prepared from 2-(2-chloropyridin-4-yl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one and cyclopentylamine. Compounds of this invention in vitro showed IC50 values of 2 nM to 20 nM against Cdc7 kinase. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).COA of Formula: C7H8FNO

The Article related to pyridylpyrrole derivative preparation kinase inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.COA of Formula: C7H8FNO

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On January 11, 2017, Duan, Wenhu; Geng, Meiyu; Yan, Wei; Ding, Jian; Ai, Jing; Zhao, Bin; Fan, Jun; Peng, Xia; Chen, Yi published a patent.Electric Literature of 87674-15-5 The title of the patent was Preparation of 3-(heteroaryl)indazole derivatives useful as FGFR1 inhibitor for the treatment of cancer. And the patent contained the following:

The invention relates to 3-(heteroaryl)indazole derivatives of formula I, method for their preparation and their use as FGFR1 inhibitor for the treatment of cancer. Compounds of formula I, wherein R1, R2, R3 are independently H and halo; R9 is (un)substituted 5- to 7-membered heteroaryl; R8 and R10 are independently H, halo, C1-3alkyl and C1-3alkoxy; R4, R5, R6 and R7 are independently H, halo, (un)substituted C1-8alkyl, etc.; M is CH2, CH, N, O and S; W is O and NH; dotted bond is single or double bond and can not be same, are claimed. Example compound II was prepared via a multistep procedure (procedure given). All the invention compounds were evaluated for their FGFR1 inhibitory activity. From the assay, it was determined that example compound II exhibited IC50 value of < 10 nM towards FGFR1. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).Electric Literature of 87674-15-5

The Article related to heteroarylindazole preparation fgfr1 inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Electric Literature of 87674-15-5

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On January 19, 2017, Duan, Wenhu; Geng, Meiyu; Yan, Wei; Ding, Jian; Ai, Jing; Zhao, Bin; Fan, Jun; Peng, Xia; Chen, Yi published a patent.Formula: C7H8FNO The title of the patent was Preparation of 3-(heteroaryl)indazole derivatives useful as FGFR1 inhibitor for the treatment of cancer. And the patent contained the following:

The invention relates to 3-(heteroaryl)indazole derivatives of formula I, method for their preparation and their use as FGFR1 inhibitor for the treatment of cancer. Compounds of formula I, wherein R1, R2, R3 are independently H and halo; R9 is (un)substituted 5- to 7-membered heteroaryl; R8 and R10 are independently H, halo, C1-3alkyl and C1-3alkoxy; R4, R5, R6 and R7 are independently H, halo, (un)substituted C1-8alkyl, etc.; M is CH2, CH, N, O and S; W is O and NH; dotted bond is single or double bond and can not be same, are claimed. Example compound II was prepared via a multistep procedure (procedure given). All the invention compounds were evaluated for their FGFR1 inhibitory activity. From the assay, it was determined that example compound II exhibited IC50 value of < 10 nM towards FGFR1. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).Formula: C7H8FNO

The Article related to heteroarylindazole preparation fgfr1 inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Formula: C7H8FNO

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On August 30, 2007, Vanotti, Ermes; Martina, Katia; Menichincheri, Maria; D’Alessio, Roberto published a patent.Quality Control of 1-(3-Fluoropyridin-4-yl)ethanol The title of the patent was Preparation of pyrrolopyrrolones as kinase inhibitors for treating cancer and other diseases. And the patent contained the following:

Compounds represented by formula I (wherein A is pyridin-4-yl, 3-fluoropyridin-4-yl, and 2-aminopyrimidin-4-yl; R1 is H, halo, and (C1-C6)alkyl; R2 is H, (C1-C6)alkyl, (C2-C6)alkenyl, etc.; R3 and R4 are H, (C1-C6)alkyl, (C3-C6)cycloalkyl, etc., or taken together form a (C3-C6)cycloalkyl), compositions thereof, and methods of use thereof. I are useful, in therapy, as agents against a host of diseases caused by and/or associated to a disregulated protein kinase activity and more particularly, Cdk2 and Cdc7 activity. I have protein kinase inhibiting activity and more particularly, Cdk2 and Cdc7 inhibiting activity; no biol. data is given in the patent. Example compound II was synthesized by cyclization of DL-2-(1-Amino-2-benzyloxyethyl)-5-(2-aminopyrimidin-4-yl)-1H-pyrrole-3-carboxylic acid. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).Quality Control of 1-(3-Fluoropyridin-4-yl)ethanol

The Article related to pyrrolopyrrolone preparation kinase inhibitor cancer other disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Quality Control of 1-(3-Fluoropyridin-4-yl)ethanol

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On June 21, 2007, Vanotti, Ermes; Menichincheri, Maria; Orsini, Paolo; Scolaro, Alessandra; Varasi, Mario published a patent.Electric Literature of 87674-15-5 The title of the patent was Preparation of N-substituted pyrrolopyridinones active as kinase inhibitors. And the patent contained the following:

The title compounds I [A = pyridin-4-yl, 3-fluoropyridin-4-yl, 2-aminopyrimidin-4-yl; R1 = H, halo, alkyl; R2 = alkyl, cycloalkyl, aryl, etc.; R3-R6 = H, alkyl, aryl, etc.], useful as Cdk2 or Cdc7 antagonists, were prepared Thus, reacting tert-Bu 2-(2-aminopyrimidin-4-yl)-4-oxo-1,4,6,7-tetrahydropyrrolo[3,2-c]pyridine-5-carboxylate with 1-bromo-2-fluoroethane followed by deprotection afforded 2-(2-aminopyrimidin-4-yl)-1-(2-fluoroethyl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one. Pharmaceutical composition comprising the compound I is disclosed. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).Electric Literature of 87674-15-5

The Article related to pyrrolopyridinone preparation cdk2 cdc7 protein kinase inhibitor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Electric Literature of 87674-15-5

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On June 21, 2007, Vanotti, Ermes; Forte, Barbara; Martina, Katia; Menichincheri, Maria; Cirla, Alessandra; Orsini, Paolo published a patent.HPLC of Formula: 87674-15-5 The title of the patent was Preparation of heteroarylpyrrolopyridinones active as kinase inhibitors. And the patent contained the following:

The title compounds I [A = pyridin-4-yl, 3-fluoropyridin-4-yl, 2-aminopyrimidin-4-yl; R1 = H, halo, alkyl; R2 = H, alkyl, cycloalkyl, etc.; R3-R6 = H, haloalkyl, polyfluorinated alkyl, etc.; and their pharmaceutically acceptable salts] that are effective in antagonizing activity toward Cdk2 or Cdc7, were prepared Over twenty compounds I were prepared Thus, reacting tert-Bu DL-6-(3-aminopropyl)-4-oxo-2-(pyridin-4-yl)-1,4,6,7-tetrahydropyrrolo[3,2-c]pyridine-5-carboxylate with 2-methylpropionaldehyde in the presence of sodium cyanoborohydride followed by deprotection afforded DL-6-(3-isobutylaminopropyl)-2-(pyridin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one as dihydrochloride. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).HPLC of Formula: 87674-15-5

The Article related to heteroarylpyrrolopyridinone preparation cdk2 cdc7 protein kinase inhibitor, heteroaryl pyrrolopyridinone preparation cdk2 cdc7 protein kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.HPLC of Formula: 87674-15-5

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On April 3, 2008, Johansson, Rolf; Karlstroem, Sofia; Kers, Annika; Nordvall, Gunnar; Rein, Tobias; Slivo, Can published a patent.Synthetic Route of 87674-15-5 The title of the patent was Preparation of [(pyridinyl)ethyl]thio[(hydroxymethyl)alkyl]amino[1,3]thiazolo[4,5-d]pyrimidinone derivatives for use as therapeutic agents. And the patent contained the following:

Title compounds I [R1 = Me or CF3; R2 = halo, CN, or alkyl; R3 and R4 independently = H or Me; n = 0 to 2], and their pharmaceutically acceptable salts, are prepared and disclosed as therapeutic agents. Thus, e.g., II was prepared by oxidation of (2R)-2-[[5-[[(1S)-1-(5-chloropyridin-2-yl)ethyl]thio]-2-methoxy[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol (preparation given). Select I were evaluated in recombinant human fractalkine hCX3CR1 binding assay, e.g., II demonstrated a Ki value of 5.8 (nM). Title compounds I are disclosed as therapeutic agents of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).Synthetic Route of 87674-15-5

The Article related to pyrimidinone pyridinylethylthio hydroxymethylalkylamino thiazolo derivative preparation nervous system disease, pyridinylethylthio hydroxymethylalkylamino thiazolopyrimidinone derivative preparation atherosclerosis multiple sclerosis asthma and other aspects.Synthetic Route of 87674-15-5

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On May 20, 2021, Bestvater, Brian P.; Du, Zhimin; Farand, Julie; Notte, Gregory; Tang, Doris T.; Venkataramani, Chandrasekar; Wang, Peiyuan; Yang, Kin S.; Zagorska, Anna; Phillips, Barton W. published a patent.COA of Formula: C7H8FNO The title of the patent was Preparation of triazole carbamate pyridyl sulfonamides as LPA receptor antagonists and uses thereof. And the patent contained the following:

The present disclosure relates generally to compounds I [R1 = (un)substituted alkyl, cycloalkyl, 6-10 membered aryl, etc.; R2 = H, (un)substituted alkyl, cycloalkyl; R3 = H, halo, (un)substituted alkyl, etc.; R4 = D, halo, (un)substituted alkyl, etc.; n = 0-2; R5 = (un)substituted alkyl, cycloalkyl, 3-6 membered heterocyclyl having 1-2 heteroatoms independently selected from N, O, and S; X = NH or O; Y = H or (un)substituted alkyl; Z = (un)substituted alkyl, alkoxy, cycloalkyl, etc.; or Y and Z together with the carbon to which they are attached form (un)substituted cycloalkyl, aryl, 3-12 membered heterocyclyl having 1-4 heteroatoms independently selected from N, O, and S, or 5-12 membered heteroaryl having 1-4 heteroatoms independently selected from N, O, and S] or pharmaceutically acceptable salts thereof, that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. E.g., a multi-step synthesis of (R)-II, starting from 2H-1,2,3-triazole, was described. Exemplified compounds I were tested for their in vitro LPAR1 activity (data given). The disclosure further relates to the use of the compounds I for the treatment of diseases and/or conditions through binding of LPAR1, including fibrosis and liver diseases such as non-alc. steatohepatitis (NASH). Pharmaceutical compositions comprising compound I, alone or in combination with other therapeutic agents, were disclosed. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).COA of Formula: C7H8FNO

The Article related to triazole carbamate pyridyl sulfonamide preparation lpa lpar1 receptor antagonist, lysophosphatidic acid receptor lpar1 antagonist triazole carbamate pyridyl sulfonamide, fibrosis liver disease treatment triazole carbamate pyridyl sulfonamide preparation, nonalcoholic steatohepatitis nash treatment triazole carbamate pyridyl sulfonamide preparation and other aspects.COA of Formula: C7H8FNO

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