Alcohols-buliding-blocks

On November 23, 2017, Gao, Peng; Xiu, Wenhua; Wang, Shaobao; Liu, Lei; Bao, Rudi published a patent.Category: alcohols-buliding-blocks The title of the patent was FGFR4 inhibitor, preparation method and applications. And the patent contained the following:

The invention disclosed a kind of FGFR4 inhibitor, its preparation method and application. The claimed FGFR4 inhibitor is shown in structure I (X1 = -(CR3R4)m1-; X2 = -(CR5R6)m2-; X3 = -(CR7R8)m3-; Y = O or S; Z = NX4, O or S; X4 = H, C1-8 alkyl or haloalkyl, C3-8 cycloalkyl; R = H, halo, hydroxy, mercapto, cyano, etc.; R1 = H, halo, hydroxy, mercapto, cyano, nitro, C3-8 cycloalkyl, heterocyclo, etc.; R2 = halo, hydroxy, mercapto, cyano, nitro, etc.; R3,R4,R5,R6,R7,R8 = H, D, halo, C1-8 alkyl, C2-8 alkenyl, alkynyl, etc.). The claimed compound is prepared via multiple steps (procedure given). The prepared compound have a very-strong inhibition effect on the activity of FGFR4 kinase, has very-high selectivity, can be widely used in the preparation of drugs for treating cancers, specially liver cancer, stomach cancer, prostate cancer, skin cancer, ovarian cancer, lung cancer, breast cancer or colon cancer, and can be developed into a rnew-generation FGFR4 inhibitor drug. The experimental process involved the reaction of 1-[(Dibenzylamino)methyl]cyclopropanol(cas: 428855-17-8).Category: alcohols-buliding-blocks

The Article related to fgfr4 inhibitor preparation antitumor agent, 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.Category: alcohols-buliding-blocks

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On January 4, 2007, Ibrahim, Prahbha N.; Artis, Dean R.; Bremer, Ryan; Mamo, Shumeye; Nespi, Marika; Zhang, Chao; Zhang, Jiazhong; Zhu, Yong-Liang; Tsai, James; Hirth, Klaus-Peter; Bollag, Gideon; Spevak, Wayne; Cho, Hanna; Gillette, Samuel J.; Wu, Guoxiam; Zhu, Hongyao; Shi, Shenghua published a patent.Reference of (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Pyrrolo[2,3-b]pyridine derivatives as protein kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Compounds of formula I which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Compounds of formula I wherein Q is (un)substituted (hetero)aryl, and (un)substituted indole; A is O, S, (un)substituted methylene, NH and derivatives, CO, CS, SO and SO2; R4 – R6 are independently H, halo, (un)substituted lower alkyl, (un)substituted lower alkenyl, (un)substituted lower alkynyl, (un)substituted (hetero)cycloalkyl, (un)substituted (hetero)aryl, etc.; and their pharmaceutically acceptable salts, prodrugs, tautomer, and isomers thereof, are claimed. Example compound II was prepared by carboxylation of 2,4-difluoroaniline with benzyl chloroformate; the resulting benzyl 3-amino-2,6-difluorobenzoate underwent sulfonylation with propane-1-sulfonyl chloride to give benzyl 2,6-difluoro-3-(propylsulfonylamino)benzoate, which underwent hydrolysis to give the corresponding benzoic acid, which underwent chlorination and coupling with 5-bromo-7-azaindole to give compound II. All the invention compounds were evaluated for their protein kinase inhibitory activity. Several of the invention compounds exhibited good inhibitory activity against various protein kinases. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Reference of (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to pyrrolopyridine preparation 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.Reference of (6-(Trifluoromethyl)pyridin-3-yl)methanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On October 29, 2020, Siegel, Stephan; Siegel, Franziska; Schulze, Volker; Berger, Markus; Graham, Keith; Suelzle, Detlev; Boemer, Ulf; Korr, Daniel; Schroeder, Jens; Moenning, Ursula; Niehues, Michael; Meyerson, Matthew; Greulich, Heidi; Kaplan, Bethany published a patent.Synthetic Route of 1620510-51-1 The title of the patent was Preparation of 4H-pyrrolo[3,2-c]pyridin-4-one derivatives as EGFR inhibitors. And the patent contained the following:

Title compounds I [wherein X and Y independently = O or (un)substituted NH; R1 = Me, Et, or CF3, etc.; R2 = H, Me, or Et, etc.; R3 = H or F; R4 = H or Me; R5 = H, CF3, or C1-3 alkyl, etc.; A = (HCR6)n, n is 0 or 1; R6 = H, C1-3 alkyl, or C1-3 haloalkyl], and their pharmaceutically acceptable salts thereof, were prepared as EGFR inhibitors. Thus, the invention compound I (X = Y = O; R1 = OMe; R2 = Cl; R3 = H; R4 = H; R5 = H; A = absence) was prepared and gave a mutEGFR inhibition IC50 value of 1.59E-10 mol/L in D770_N771insSVD kinase assay. The experimental process involved the reaction of (R)-(4-Methylmorpholin-3-yl)methanol(cas: 1620510-51-1).Synthetic Route of 1620510-51-1

The Article related to pyrrolopyridinone antitumor preparation egfr 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.Synthetic Route of 1620510-51-1

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On August 4, 2022, Li, Ao; Chen, Yile; Cao, Guoqing published a patent.COA of Formula: C6H10O3 The title of the patent was Toxin molecule suitable for antibody-drug conjugate. And the patent contained the following:

The present invention provides a toxin mol. suitable for an antibody-drug conjugate. In particular, the present invention provides a compound represented by structure I (X = H, OH, NH2, NHR0; Y = (CR1R2)n; Z = bond, carbonyl, thiocarbonyl, sulfonyl, etc.; R0 = C1-8 alkyl, haloalkyl, alkoxy, etc.; R1,R2 = H, D, halo, alkyl, etc.; R3,R4 = halo, C1-8 alkyl, haloalkyl, etc.; n = 0-3 integers). The claimed compound is prepared via multiple steps (procedure given). The prepared compound can be used in the preparation of a pharmaceutical composition for treating diseases associated with tumor cell proliferation. The experimental process involved the reaction of 3-Cyclopropyl-2-hydroxypropanoic acid(cas: 1599840-16-0).COA of Formula: C6H10O3

The Article related to toxin mol preparation antibody drug conjugate antitumor agent, 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.COA of Formula: C6H10O3

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On January 4, 2007, Ibrahim, Prabha N.; Artis, Dean R.; Bremer, Ryan; Habets, Gaston; Mamo, Shumeye; Nespi, Marika; Zhang, Chao; Zhang, Jiazhong; Zhu, Yong-Liang; Zuckerman, Rebecca; West, Brian; Suzuki, Yoshihisa; Tsai, James; Hirth, Klaus-Peter; Bollag, Gideon; Spevak, Wayne; Cho, Hanna; Gillette, Samuel J.; Wu, Guoxian; Zhu, Hongyao; Shi, Shenghua published a patent.Formula: C7H6F3NO The title of the patent was Pyrrolo[2,3-b]pyridine derivatives as protein kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Compounds of formula I which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Compounds of formula I wherein Q is (un)substituted aryl, (un)substituted indole, (un)substituted heteroaryl, etc.; A is O, S, (un)substituted methylene, NH and derivatives, CO, CS, SO and SO2; R4 – R6 is H, halo, (un)substituted lower alkyl, (un)substituted lower alkenyl, (un)substituted alkynyl, (un)substituted (hetero)cycloalkyl, and (un)substituted (hetero)aryl; and their pharmaceutically acceptable salts, prodrugs, tautomers, and isomers thereof, are claimed. Example compound II was prepared by carboxylation of 2,4-difluoroaniline with benzyl chloroformate; the resulting benzyl 3-amino-2,6-difluorobenzoate underwent sulfonylation with propane-1-sulfonyl chloride to give benzyl 2,6-difluoro-3-(propylsulfonylamino)benzoate, which underwent hydrogenation to give the corresponding benzoic acid, which underwent chlorination, to give the corresponding acid chloride, which underwent reaction with 5-bromo-7-azaindole to give compound II. All the invention compounds were evaluated for their protein kinase inhibitory activity. Several of the tested compounds exhibited good protein kinase inhibitory activity against several kinases. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Formula: C7H6F3NO

The Article related to pyrrolopyridine preparation protein kinase inhibitory activity, 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.Formula: C7H6F3NO

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On July 3, 2008, Ibrahim, Prabha N.; Bremer, Ryan; Zhang, Chao; Zhang, Jiazhong; Hirth, Klaus-Peter; Wu, Guoxian; Zhu, Hongyao published a patent.Recommanded Product: 386704-04-7 The title of the patent was Pyrrolo[2,3-]pyridine compounds and methods for kinase modulation, preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Compounds of formula I, which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Compounds of formula I wherein A1 is O, CR40R41, CO and NH and derivatives; Z2 is N and CR56; Z6 is N and CR52; L3 is NH and derivatives, S, O, CONH and derivatives, NHCO and derivatives, etc.; R40, R41, R52 and R56 are independently H, F, lower (fluoro)alkyl, lower (fluoro)alkoxy, lower (fluoro)alkylthio, etc.; R61 is H, and lower (fluoro)alkyl; R100 and R101 are independently H, OH, NH2, CN, CO2H, NO2, SO2NH2, CONH2, etc.; R53 and R55 are independently H, halo, (un)substituted lower alkyl and (un)substituted lower alkoxy; n is 0, 1, 2 and 3; and their salts, prodrugs, tautomers, and isomers thereof, are claimed. Example compound II was prepared by addition of 7-azaindole to 4-(4-chlorobenzyloxy)-3-fluorobenzaldehyde; the resulting [4-(4-chlorobenzyloxy)-3-fluorophenyl]-(1H-pyrrolo[2,3-b]pyridin-3-yl)methanol underwent oxidation to give compound II. All the invention compounds were evaluated for their protein kinase modulatory activity (some data given). The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Recommanded Product: 386704-04-7

The Article related to pyrrolopyridine preparation protein kinase modulator treatment disease, 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.Recommanded Product: 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On July 3, 2008, Ibrahim, Prabha N.; Bremer, Ryan; Zhang, Chao; Zhang, Jiazhong; Hirth, Klaus-Peter; Wu, Guoxian; Zhu, Hongyao published a patent.Application of 386704-04-7 The title of the patent was Pyrrolo[2,3-b]pyridine compounds and methods for kinase modulation, preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Compounds of formula I, which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Compounds of formula I wherein n is 0, 1, 2 and 3; Z2 is N and CR12; Z6 is CR16; L4 is (CR10R11)p-X-(CR10R11)q; X is O, S, NH and derivatives, CO, CS, SO, SO2, CONH and derivatives, CSNH and derivatives, NHCO and derivatives, etc.; p and q are independently 0, 1 and 2, provides that at least one of p and 1 is 0; R4, R5, R6, R11, R15, R16 and R60 is H, halo, (un)substituted lower alkyl, (un)substituted lower alkenyl, (un)substituted lower alkynyl, (un)substituted (hetero)cycloalkyl, (un)substituted (hetero)aryl, etc.; R61 is H and lower (fluoro)alkyl; A is O, S, CH2, CHOH, CHNH2, CF2, CHF, NH and derivatives, CO, CS, SO, SO2, etc.; R10 and R11 and independently H, F and (un)substituted lower alkyl; R17 is H, halo, (un)substituted lower alkyl, OH and derivatives; and their salts, prodrugs, tautomers and isomers thereof, are claimed. Example compound II was prepared by benzylation of 4-hydroxy-3-methoxybenzaldehyde with 4-chlorobenzyl bromide; the resulting 4-(4-chlorobenzyloxy)-3-methoxybenzaldehyde underwent addition of 7-azaindole to give 3-((4-(4-chlorobenzyloxy)-3-methoxyphenyl)(methoxy)methyl)-1H-pyrrolo[2,3-b]pyridine, which underwent demethoxylation to give compound II. All the invention compounds were evaluated for their protein kinase modulatory activity (some data given). The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application of 386704-04-7

The Article related to pyrrolopyridine preparation protein kinase modulator treatment disease, 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.Application of 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On January 6, 2011, Guzzo, Peter R.; Surman, Matthew David; Henderson, Alan John; Jiang, May Xiaowu published a patent.Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Preparation of azinone-substituted azapolycycles as MCH-1 receptor antagonists and use in the treatment of diseases. And the patent contained the following:

Title compounds I [R1 = H, (un)substituted alkyl, alkenyl, alkynyl, etc; R2 and R4 independently = H, CONH2 and derivatives, (un)substituted alkyl, aryl, etc.; R2 and R3 or R3 and R4 taken together to form an (un)substituted 3- to 7-membered heterocycle; at least one of R2 and R3 or R3 and R4 taken together to form an (un)substituted 3- to 7-membered heterocycle; each R5 independently = H, halo, NH2 and derivatives, (un)substituted alkyl, aryl, etc.; R6 = H, halo, (un)substituted aryl, heteroaryl, etc.; A = (CH2)m; B = (un)substituted aryl, heteroaryl, cycloalkyl, etc.; D = (CH2)n; L = (CH2)pO, (CH2)p, CH=CH, or bond; X = CR12, C(R12)2, N, or NR12; Y = CR12, C, or N; Z = CH, C, or N; R12 = H, halo, NH2 and derivatives, (un)substituted alkyl, aryl, etc.; m and n = 0 or 1, wherein m + n = 1; p = 1 to 4; q = 0 to 3; dash bond represents an optional double bound], and their pharmaceutically acceptable salts, oxides, solvates, or prodrugs, are prepared and disclosed as MCH-1 receptor antagonists and useful in the treatment of obesity, anxiety, depression, non-alc. fatty liver disease, and psychiatric disorders. Thus, e.g., II·HCl was prepared by acylation of 2-(6-bromo-1-methyl-1H-indol-3-yl)ethanamine with 4-bromobutyryl chloride followed by intramol. cyclization, intramol. reductive N-alkylation, amination with 4-(benzyloxy)pyridin-2(1H)-one, and addition of hydrochloric acid. Select I were evaluated for their MCH-1 antagonistic activity, e.g., II·HCl demonstrated a Ki value of 14.9 nM. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to azinone azapolycycle preparation mch receptor antagonist treatment disease, 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.Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts