Category: 1012882-90-4

On March 20, 2008, Flynn, Daniel L.; Kaufman, Michael D.; Patt, William C.; Petillo, Peter A. published a patent.Safety of Ethyl 5-chloro-2-iodobenzoate The title of the patent was Preparation of heterocyclic ureas as kinase inhibitors useful for the treatment of proliferative and inflammatory diseases. And the patent contained the following:

The present invention relates to novel kinase inhibitors and modulators of general formula I (wherein E1 is cyclopropyl, furyl, Ph, etc.; A is Ph, naphthyl, indanyl, etc.; Z6 is H, C1-C6alkyl, branched C3-C7alkyl, etc.; R3 and R16 are H, C1-C6 alkyl, branched C3-C7alkyl, etc.; R4 is H, C1-C6alkyl, hydroxyC1-C6alkyl, etc.; X2 is a direct bond or (un)branched C1-C6 alkyl; t is 1-3) useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration. Example compound II was prepared by reacting 2-amino-6-(3-amino-4-fluorophenyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (preparation given) and 3-tert-butyl-1-phenyl-1H-pyrazol-5-amine (preparation given). In general, the I tested exhibited >50 % inhibition activity at 0.2-2 渭M concentration in V600E B-Raf kinase and C-Raf kinase assays. In general, the I tested exhibited >50 % inhibition of proliferation at 1-10uM concentration against A375 cells. The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).Safety of Ethyl 5-chloro-2-iodobenzoate

The Article related to heterocyclic urea kinase inhibitor preparation proliferative inflammatory disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of Ethyl 5-chloro-2-iodobenzoate

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On December 3, 2020, Hopper, Allen Taylor; Mischke, Steven; La, Daniel published a patent.HPLC of Formula: 1012882-90-4 The title of the patent was Cyanopiperiddine compounds as CYP46A1 inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Described herein are cyanopiperidine compounds I that act as CYP46A1 inhibitors, compositions comprising these compounds, and methods of their use into treating neurodegenerative diseases and the like, or a pharmaceutically active salts thereof. Specifically, the invention relates to compounds of formula I wherein R1 is (un)substituted C6-10 aryl, (un)substituted C3-7 cycloalkyl, (un)substituted 3- to 7-membered heterocyclic ring, etc.; X is (CH2)0-2; Y is (CRaRb)0-4; Ra and Rb are independently H, halo, CN, OH, NO2, NH2 and derivatives, C1-6 alkyl, etc.; R7-R10 are independently H, C1-6 (halo)alkyl, C1-6 (halo)alkoxy, etc.; each of the R2 and R3 are independently halo, CN OH, NO2, NH2 and derivatives, C1-6 alkyl, C3-7 cycloalkyl, etc.; ring A is 5- to 6-membered N-containing heteroaryl; ring B is C6-10 aryl, 5- to 6-membered heteroaryl; and their pharmaceutically acceptable salts as CYP46A1 inhibitors in the treatment of diseases thereof, are claimed. Example compound II was prepared by using olefination, heterocyclization, and amidation as the key steps. All the invention compounds were evaluated for their CYP46A1 inhibitory activity. The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).HPLC of Formula: 1012882-90-4

The Article related to cyano piperiddine preparation cyp46a1 inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 1012882-90-4

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On September 6, 2012, Flynn, Daniel L.; Kaufman, Michael D. published a patent.HPLC of Formula: 1012882-90-4 The title of the patent was Preparation of heterocyclic urea derivatives as kinase inhibitors useful for the treatment of hyperproliferative and other diseases. And the patent contained the following:

Compounds of the present invention (I, wherein E1 is substituted phenyl; A is substituted pyrazolyl and imidazolyl; X2 is a direct bond, wherein E1 is directly linked to the NH group; X3 is -O-; Z6 is independently and individually selected from H, C1-6 alkyl, branched C3-7 alkyl, hydroxy, etc.; t = 1-3), alone and in combination with other active agents, find utility in the treatment of hyperproliferative diseases, mammalian cancers and especially human cancers including but not limited to for example malignant melanomas, myeloproliferative diseases, chronic myelogenous leukemia, acute lymphocytic leukemia, a disease caused by c-ABL kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof. More generally the invention relates to a method of treating mammalian disease with I wherein the disease etiol. or progression is at least partially mediated by the kinase activity of c-ABL kinase, BCR-ABL kinase, FLT-3 kinase, TIE-2 kinase, TRK-A kinase, TRK-B kinase, TRK-C kinase, VEGFR-2 kinases, c-MET kinase, PDGFR-alpha kinase, PDGFR-beta kinase, HER-1 kinase, HER-2 kinase, HER-3 kinase, HER-4 kinase, FGFR kinases, c-KIT kinase, RET kinase, c-FMS kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs of any of the foregoing. Synthetic procedures for preparing I are exemplified. Thus, e.g., II was prepared by coupling of 2,2,2-trichloroethyl 3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-ylcarbamate (preparation given) with 4-(4-amino-3-fluorophenoxy)-N-methylpicolinamide (preparation given). Assays were described for evaluating binding of I to various kinases, e.g., II demonstrated an IC50 value of 4 nM in the p-Abl kinase assay. The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).HPLC of Formula: 1012882-90-4

The Article related to preparation heterocyclic urea derivative kinase inhibitor treatment hyperproliferative disease, Aliphatic Compounds: Ureas, Carbamic Acids, Guanidines, and Their Sulfur-Containing Analogs and other aspects.HPLC of Formula: 1012882-90-4

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On March 14, 2013, Flynn, Daniel L.; Petillo, Peter A.; Kaufman, Michael D. published a patent.Recommanded Product: 1012882-90-4 The title of the patent was Preparation of heterocyclic urea derivatives as kinase inhibitors useful for the treatment of myeloproliferative diseases and other proliferative diseases. And the patent contained the following:

Compounds of the invention (I, wherein E1 is substituted phenyl; A is substituted pyrazolyl and imidazolyl; X2 is a direct bond, wherein E1 is directly linked to the NH group; X3 is -O-; Z6 is independently and individually selected from H, C1-6 alkyl, branched C3-7 alkyl, hydroxy, etc.; t = 1-3) find utility in the treatment of of cancer, secondary cancer growth arising from metastasis, hyperproliferative diseases, diseases characterized by hyper-vascularization, inflammation, osteoarthritis, respiratory diseases, stroke, systemic shock, immunol. diseases, autoimmune diseases, bone resorptive diseases, cardiovascular disease and diseases characterized by angiogenesis. The invention also provides a method of modulating a kinase activity of a wild-type kinase species, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs of any of the foregoing, by contacting said species with a compound I. Synthetic procedures for preparing I are exemplified. Thus, e.g., II was prepared by coupling of 2,2,2-trichloroethyl 3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-ylcarbamate (preparation given) with 4-(4-amino-3-fluorophenoxy)-N-methylpicolinamide (preparation given). Assays were described for evaluating binding of I to various kinases, e.g., II demonstrated an IC50 value of 4 nM in the p-Abl kinase assay. The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).Recommanded Product: 1012882-90-4

The Article related to preparation heterocyclic urea derivative kinase inhibitor treatment myeloproliferative disease, Aliphatic Compounds: Ureas, Carbamic Acids, Guanidines, and Their Sulfur-Containing Analogs and other aspects.Recommanded Product: 1012882-90-4

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On September 7, 2010, Flynn, Daniel L.; Petillo, Peter A.; Kaufman, Michael D. published a patent.Electric Literature of 1012882-90-4 The title of the patent was Preparation of urea derivatives as kinase inhibitors useful for the treatment of myeloproliferative diseases and other proliferative diseases. And the patent contained the following:

Title compounds I [E1 = (un)substituted Ph; A = (un)substituted imidazolyl or pyrazolyl; X2 = bond; X3 = O; each R3 independently = H, alkyl, carbocyclyl, etc.; each Z6 independently = H, alkyl, hydroxyalkyl, etc.; m = 1-3] are prepared and disclosed for treatment of myeloproliferative diseases and other proliferative diseases. Thus, e.g., II was prepared by coupling of 2,2,2-trichloroethyl 3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-ylcarbamate (preparation given) with 4-(4-amino-3-fluorophenoxy)-N-methylpicolinamide (preparation given). Select I were evaluated in Abl kinase and T315I Abl kinase assays (data given). The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).Electric Literature of 1012882-90-4

The Article related to urea derivative preparation myeloproliferative proliferative disease, Aliphatic Compounds: Ureas, Carbamic Acids, Guanidines, and Their Sulfur-Containing Analogs and other aspects.Electric Literature of 1012882-90-4

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On April 17, 2008, Petillo, Peter A.; Kaufman, Michael D.; Flynn, Daniel L. published a patent.COA of Formula: C9H8ClIO2 The title of the patent was Preparation of urea derivatives as kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases. And the patent contained the following:

Title compounds I [Q1 and Q2 independently = N or CZ6; E1 = cycloalkyl, pyrrolidinyl, piperidinyl, etc.; A = (un)substituted Ph, furyl, thienyl, etc.; X2 = alkyl or bond; X3 = CO, O, (un)substituted alkoxy, etc.; R3 independently = H, alkyl, carbocyclyl, and substituted phenyl; Z6 independently = H, alkyl, OH, hydroxyalkyl, etc.; m = 1-3] are prepared and disclosed for treatment of hyperproliferative diseases and mammalian cancers, especially human cancers. Thus, e.g., II was prepared by coupling of 2,2,2-trichloroethyl 3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-ylcarbamate (preparation given) with 4-(4-amino-3-fluorophenoxy)-N-methylpicolinamide (preparation given). Assays were described for evaluating binding of I to various kinases, e.g., II demonstrated an IC50 value of 4 nM in the p-Abl kinase assay. The invention also pertains to methods of modulating kinase activities, pharmaceutical compositions, and methods of treating individuals, incorporating or using the compounds The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).COA of Formula: C9H8ClIO2

The Article related to urea derivative preparation kinase inhibitor, Aliphatic Compounds: Ureas, Carbamic Acids, Guanidines, and Their Sulfur-Containing Analogs and other aspects.COA of Formula: C9H8ClIO2

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On January 31, 2022, Shen, Guodong; Lu, Qichao; Wang, Zeyou; Sun, Weiwei; Zhang, Yalin; Huang, Xianqiang; Sun, Manman; Wang, Zhiming published an article.Product Details of 1012882-90-4 The title of the article was Environmentally Friendly and Recyclable CuCl2 -Mediated C-S Bond Coupling Strategy Using DMEDA as Ligand, Base and Solvent. And the article contained the following:

An environment-friendly, recyclable and economic strategy was developed to synthesize diaryl chalcogenides by the CuCl2-catalyzed C-S bond-formation reaction via iodobenzenes and benzenethiols/1,2-diphenyldisulfanes using N,N’-dimethylethane-1,2-diamine (DMEDA) as ligand, base and solvent. For these reactions, especially the reactions of diiodobenzenes and aminobenzenethiols/disulfanediyldianilines, a range of substrates were compatible and gave the corresponding products in good to excellent yields. Both of the reagents in the catalytic system (CuCl2/DMEDA) were inexpensive, conveniently separable and recyclable for more than five cycles. The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).Product Details of 1012882-90-4

The Article related to iodobenzene thiophenol copper catalyst carbon sulfur bond formation, diphenylsulfane preparation green chem, diiodobenzene diphenyldisulfane copper catalyst carbon sulfur bond formation, bisphenylsulfanyl benzene preparation green chem and other aspects.Product Details of 1012882-90-4

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On January 31, 2022, Shen, Guodong; Lu, Qichao; Wang, Zeyou; Sun, Weiwei; Zhang, Yalin; Huang, Xianqiang; Sun, Manman; Wang, Zhiming published an article.Product Details of 1012882-90-4 The title of the article was Environmentally Friendly and Recyclable CuCl2 -Mediated C-S Bond Coupling Strategy Using DMEDA as Ligand, Base and Solvent. And the article contained the following:

An environment-friendly, recyclable and economic strategy was developed to synthesize diaryl chalcogenides by the CuCl2-catalyzed C-S bond-formation reaction via iodobenzenes and benzenethiols/1,2-diphenyldisulfanes using N,N’-dimethylethane-1,2-diamine (DMEDA) as ligand, base and solvent. For these reactions, especially the reactions of diiodobenzenes and aminobenzenethiols/disulfanediyldianilines, a range of substrates were compatible and gave the corresponding products in good to excellent yields. Both of the reagents in the catalytic system (CuCl2/DMEDA) were inexpensive, conveniently separable and recyclable for more than five cycles. The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).Product Details of 1012882-90-4

The Article related to iodobenzene thiophenol copper catalyst carbon sulfur bond formation, diphenylsulfane preparation green chem, diiodobenzene diphenyldisulfane copper catalyst carbon sulfur bond formation, bisphenylsulfanyl benzene preparation green chem and other aspects.Product Details of 1012882-90-4

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On August 2, 2018, Morales, Guilermo A.; Garlich, Joseph R.; Durden, Donald L. published a patent.Application In Synthesis of Ethyl 5-chloro-2-iodobenzoate The title of the patent was Preparation of thienopyranones and furanopyranones as kinase, bromodomain, and checkpoint inhibitors. And the patent contained the following:

The title compounds I-VI [M = (independently) S or O; R1 = H, halo, alkyl, etc.; R2 = VII, VIII (wherein X = C, N, P, P(O), SiRb; n = 0-2; Y = CR1, O, S, NRa, etc.; Z = O or S; R1 = H or independently at each instance any group defined in R1; Rb = H or independently at each instance any group defined in R1; and wherein R2 in III excludes morpholine; Cyc = (un)substituted aryl, heterocycle, carbocycle); R3 = R1; R4 = R1; Rc = a hydrolyzable linker group which is optionally substituted with a targeting agent; Ar = an aryl, heterocycle, or heteroaryl group unsubstituted beyond the attachment to thiophene (or furan) ring; and the R3 substituent is in the meta- or para-positions], useful for treating diseases including but not limited to, cancer, non-cancer proliferative disease, sepsis, autoimmune disease, viral infection, atherosclerosis, type 1 or 2 diabetes, obesity, inflammatory disease, or Myc-dependent disorder by modulating biol. processes by the inhibition of cell cycle checkpoint targets CDKs, and/or PI3 kinase, and/or bromodomain protein binding to substrates, were prepared E.g., a multi-step synthesis of IX, starting from 6-chloro-1-cyclopentyl-1,5,7-triaza-1H-indene-2-carboxylic acid and dimethylamine hydrochloride salt, was described. Representative compounds I were tested for their affinity toward CDK6, PI3K and BRD4 (data given). Pharmaceutical composition comprising compound I-VI was disclosed. The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).Application In Synthesis of Ethyl 5-chloro-2-iodobenzoate

The Article related to thienopyranone furanopyranone preparation kinase bromodomain checkpoint inhibitor antitumor antiviral, proliferative autoimmune disease sepsis treatment antiatherosclerotic thienopyranone furanopyranone preparation, antidiabetic antiobesity antiinflammatory thienopyranone furanopyranone preparation and other aspects.Application In Synthesis of Ethyl 5-chloro-2-iodobenzoate

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On December 31, 2020, Yuan, Zhenbo; Zeng, Yuye; Feng, Ziwen; Guan, Zhe; Lin, Aijun; Yao, Hequan published an article.Quality Control of Ethyl 5-chloro-2-iodobenzoate The title of the article was Constructing chiral bicyclo[3.2.1]octanes via palladium-catalyzed asymmetric tandem Heck/carbonylation desymmetrization of cyclopentenes. And the article contained the following:

A palladium-catalyzed asym. tandem Heck/carbonylation desymmetrization of cyclopentenes I (R = COMe, CO2Et; R1 = H, F, Cl, Me, OMe; X = I, Br) has been described. Alcs., (such as., n-propanol, isopropanol, cyclohexanol, etc.) phenols (such as., 4-methylphenol, biphenyl-4-ol, naphthol, etc.) and amines (such as., pyrrolidine, morpholine, benzylamine, etc.) are employed as versatile coupling reagents for the construction of multifunctional chiral bicyclo[3.2.1]octanes II (R2 = OMe, OEt, OPh, pyrrolidino, morpholino, thiomorpholino, etc.) with one all-carbon quaternary and two tertiary carbon stereogenic centers in high diastereo- and enantioselectivities. This study represents an important progress in both the asym. tandem Heck/carbonylation reactions and enantioselective difunctionalization of internal alkenes. The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).Quality Control of Ethyl 5-chloro-2-iodobenzoate

The Article related to bicyclooctane preparation diastereoselective enantioselective, cyclopentene alc heck carbonylation desymmetrization palladium catalyst, phenol cyclopentene heck carbonylation desymmetrization palladium catalyst, amine cyclopentene heck carbonylation desymmetrization palladium catalyst and other aspects.Quality Control of Ethyl 5-chloro-2-iodobenzoate

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com