Month: November 2022

On June 18, 2015, Deligny, Michaeel Louis Robert; Heer, Jag Paul; Jackson, Victoria Elizabeth; Kroeplien, Boris; Lecomte, Fabien Claude; Porter, John Robert published a patent.Reference of 3-Bromo-2-fluoro-6-methoxybenzaldehyde The title of the patent was Imidazopyridine derivatives as modulators of TNF activity and their preparation. And the patent contained the following:

A series of substituted 3H-imidazo[4,5-b]pyridine derivatives of formula I, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurol. and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncol. disorders. Compounds of formula I wherein E is a bond, SO2 and NH and derivatives; Q is a bond, O, S, SO, SO2, etc.; Y is (un)substituted C3-7 cycloalkyl, (un)substituted aryl, (un)substituted C3-7 heterocycloalkyl, and (un)substituted heteroaryl; Z is H, halo, CF3, C1-6 alkyl, etc.; R1, R2 and R3 are independently H, halo, CN, NO2, OH, CF3, etc.; R5 is (un)substituted C1-5 alkyl; and N-oxides, pharmaceutically acceptable salts, solvates, glucuronide derivatives, and co-crystals thereof, are claimed. Example compound II was prepared by cyclocondensation of 6-chloro-N2-[(2,5-dichlorophenyl)methyl]pyridine-2,3-diamine with 2-(4-carbamoylphenoxy)acetic acid. The invention compounds were evaluated for their TNFα modulatory activity (some data given). The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methoxybenzaldehyde(cas: 1160653-94-0).Reference of 3-Bromo-2-fluoro-6-methoxybenzaldehyde

The Article related to imidazopyridine preparation tnfalpha modulator, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Reference of 3-Bromo-2-fluoro-6-methoxybenzaldehyde

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On November 30, 2021, Zhang, Weidong; Sun, Qingyan; Zhao, Menghao; Chen, Haomin; Guo, Jingwen; Zhang, Panpan published a patent.Name: 1-Bromo-3-isocyanato-2-methyl-benzene The title of the patent was Preparation of cyclopentene compounds as STAT3 inhibitor for prevention and/or treatment of cell proliferative diseases. And the patent contained the following:

The present invention relates to the preparation of cyclopentene compounds as STAT3 inhibitor for prevention and/or treatment of cell proliferative diseases. In particular, the cyclopentene compound I (wherein, ring A = C6-C10 aryl group or 5-6 membered heteroaryl group and the heteroatom in the 5-6 membered heteroaryl group = one or more of N, O, S and the number of heteroatoms = 1-4; n = 0,1,2,3 or 4; R2 = independently C1-C6 alkyl group, C1-C6 alkyl group -O-, C1-C6 alkyl group -C(=O)-N(R2a)- etc.; R2a and R2b = independently H or C1-C4 alkyl group; L1 = -C(=O)-, -N(R11)-C(=O)-N(R10)-, -C(=O)-N(R12)-, -N(R13)-C(=O)- etc., where R10, R11, R12, R13, R14, R15, R16, R17, R18, R19 and R20 = independently H or C1-C4 alkyl group). Further, (R1 = H, C1-C6 alkyl substituted with one or more substituents Ra, C3-C10 cycloalkyl group, C3-C10 cycloalkyl substituted by one or more substituents Rb, C6-C10 aryl group, C3-C10 aryl substituted by one or more substituents Rc, 5-10 membered heterocycloalkyl etc., and the heteroatom = N, O, S etc., and the number of heteroatoms = 1-3; Ra, Rb, Rc, Rd, Re = independently (R1a R1b) N-C(=O)-, C1-C6 alkyl -O-, C1-C6 alkyl -C(=O)-N(R1c)- or O=). Further, (R1a, R1b and R1c = independently H or C1-C4 alkyl group; alternatively, R2 is connected to C or N in R1-L1 to form a 4-7 membered heterocycloalkyl group together with the atoms connected to ring A; the heteroatoms in the 4-7 membered heterocycloalkyl group = one or more of N, O, S, S(=O) and S(=O)2, and the number of heteroatoms = 1-3; the 4-7 membered heterocycloalkyl group is optionally substituted by the substituents: C1-C4 alkyl group or =O; a carbon atom with * represents a chiral carbon atom, which is in the S configuration, R configuration, or a mixture) or its pharmaceutically acceptable salt was prepared The inventive cyclopentene compounds has selectivity for STAT3 in preliminary activity study, and at the same time, shows a strong inhibitory activity against tumor cell proliferation with a significant killing effect on human cancer cells, especially human breast cancer cell line MDA-MB-231, human prostate cancer cell line PC-3 and human prostate cancer cell line DU-145, therefore it can be used as a series of novel STAT3 inhibitors in the preparation of corresponding novel antitumor drugs for diseases with a good market prospect. The experimental process involved the reaction of 1-Bromo-3-isocyanato-2-methyl-benzene(cas: 1261475-16-4).Name: 1-Bromo-3-isocyanato-2-methyl-benzene

The Article related to cyclopentene compound stat3 inhibitor antitumor agent, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Name: 1-Bromo-3-isocyanato-2-methyl-benzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 30, 2021, Yang, Yi; Chen, Xianjun; Xie, Xin; Su, Ni published a patent.Related Products of 185345-46-4 The title of the patent was New method for detecting and quantifying RNA. And the patent contained the following:

Provided in the present invention are an aptamer nucleic acid mol., a compound containing the aptamer and a fluorophore small mol., a method for detecting RNA, DNA, or another target mol. inside or outside of a cell by using the aptamer nucleic acid mol., and a kit containing the aptamer. The aptamer of the present invention can specifically bind to a fluorophore small mol. and significantly improves the fluorescence intensity under light excitation at suitable wavelength. The experimental process involved the reaction of 3-Bromo-5-fluoro-4-hydroxybenzaldehyde(cas: 185345-46-4).Related Products of 185345-46-4

The Article related to aptamer nucleic acid mol preparation detection rna dan, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Related Products of 185345-46-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 24, 2021, Yang, Yi; Chen, Xianjun; Xie, Xin; Su, Ni published a patent.Related Products of 185345-46-4 The title of the patent was New method for detecting and quantifying RNA. And the patent contained the following:

The invention relates to a nucleic acid mol., including a complex of an aptamer and a fluorophore small mol. The nucleic acid mol. is used for detecting intracellular or extracellular RNA, DNA or other target mols. The invention also provides a test kit including the aptamer. The aptamer of the invention can specifically bind a fluorophore small mol. and significantly increase its fluorescence intensity upon excitation with light of the appropriate wavelength. The experimental process involved the reaction of 3-Bromo-5-fluoro-4-hydroxybenzaldehyde(cas: 185345-46-4).Related Products of 185345-46-4

The Article related to aptamer nucleic acid mol preparation detection rna dan, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Related Products of 185345-46-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On June 4, 2020, Guillemont, Jerome Emile Georges; Lancois, David Francis Alain; Chao, Sovy; Angibaud, Patrick Rene; Mercey, Guillaume Jean Maurice; Raboisson, Pierre Jean-Marie Bernard; Michaut, Antoine Benjamin; Rigaux, Peter published a patent.Name: 3-Bromo-2-fluoro-6-methoxybenzaldehyde The title of the patent was Further heteroaromatic compounds having activity against RSV and their preparation. And the patent contained the following:

The invention concerns compounds of formula I having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment or prevention of respiratory syncytial virus infection. Compounds of formula I wherein A is substituted 1,2,3,4-tetrahydroisoquinolinyl, substituted azepanyl, amino, etc.; R5 is substituted Ph, substituted pyridinyl, substituted benzopyranyl, etc.; R15 is H and C1-4 alkyl; X1, X2 and X3 are independently N and CR; R is H and C1-4 alkyl; with provisions; and stereochem. isomeric forms thereof, are claimed. Example compound II was prepared by carboxylation of 4-(8-cyclopropyl-6-[(1R)-1-methyl-1,2,3,4-tetrahydroisoquinoline-2-carbonyl]imidazo[1,2-a]pyridin-2-yl)-3-fluorobenzoic acid. The invention compounds were evaluated for their antiviral activity. From the assay, it was determined that compound II exhibited EC50 value of 0.510μM and a CC50 value of 60.4μM. The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methoxybenzaldehyde(cas: 1160653-94-0).Name: 3-Bromo-2-fluoro-6-methoxybenzaldehyde

The Article related to heteroaromatic preparation treatment rsv infection antiviral, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Name: 3-Bromo-2-fluoro-6-methoxybenzaldehyde

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On April 15, 2020, Sandfort, Frederik; Knecht, Tobias; Pinkert, Tobias; Daniliuc, Constantin G.; Glorius, Frank published an article.Name: 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Site-Selective Thiolation of (Multi)halogenated Heteroarenes. And the article contained the following:

A general and simple strategy for the site-selective thiolation of various pharmaceutically relevant electron-rich heteroarenes with thiols is reported. This mild and reliable photocatalytic protocol enables C-S coupling at the most electron-rich position of the (multi)halogenated substrates, complementing established methodologies. Exptl. and computational studies suggest a radical chain mechanism with the key step being a homolytic aromatic substitution of the heteroaryl halide by an electrophilic thiyl radical, highlighting an underdeveloped reactivity mode. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Name: 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to heteroarene thiol site selective thiolation photochem iridium, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Name: 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On October 15, 2021, there was a patent about enzymes.Reference of 3-Bromo-5-fluoro-4-hydroxybenzaldehyde The title of the patent was Fluorescent dye, preparation method therefor and use thereof. And the patent contained the following:

A fluorescent dye I [wherein Ar = (un)substituted arylene or heteroarylene; Y = O or S; R1 = H or alkyl; R2 = halo, OH, or CN], a preparation method therefor and use thereof. For example, II was prepared in a multi-step synthesis. The fluorescent dye has the advantages of sensitivity and specificity to viscosity response, low background fluorescence and the like, and can also be used as a fluorescence activation lighting-type probe for fluorescence labeling, quantification or detection of proteins, enzymes or nucleic acids. The experimental process involved the reaction of 3-Bromo-5-fluoro-4-hydroxybenzaldehyde(cas: 185345-46-4).Reference of 3-Bromo-5-fluoro-4-hydroxybenzaldehyde

The Article related to fluorescent dye preparation fluorescence probe proteins enzyme nucleic acid, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Reference of 3-Bromo-5-fluoro-4-hydroxybenzaldehyde

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 30, 2021, Zhang, Dasheng published a patent.HPLC of Formula: 185345-46-4 The title of the patent was Fluorescent dye, preparation method therefor and use thereof. And the patent contained the following:

A fluorescent dye I [wherein Ar = (un)substituted arylene or heteroarylene; Y = O or S; R1 = H or alkyl; R2 = halo, OH, or CN], a preparation method therefor and use thereof. For example, II was prepared in a multi-step synthesis. The fluorescent dye has the advantages of sensitivity and specificity to viscosity response, low background fluorescence and the like, and can also be used as a fluorescence activation lighting-type probe for fluorescence labeling, quantification or detection of proteins, enzymes or nucleic acids. The experimental process involved the reaction of 3-Bromo-5-fluoro-4-hydroxybenzaldehyde(cas: 185345-46-4).HPLC of Formula: 185345-46-4

The Article related to fluorescent dye preparation fluorescence probe proteins enzyme nucleic acid, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.HPLC of Formula: 185345-46-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 10, 2020, Yamada, Yousuke; Takashima, Hajime; Walmsley, David Lee; Ushiyama, Fumihito; Matsuda, Yohei; Kanazawa, Harumi; Yamaguchi-Sasaki, Toru; Tanaka-Yamamoto, Nozomi; Yamagishi, Junya; Kurimoto-Tsuruta, Risa; Ogata, Yuya; Ohtake, Norikazu; Angove, Hayley; Baker, Lisa; Harris, Richard; Macias, Alba; Robertson, Alan; Surgenor, Allan; Watanabe, Hayato; Nakano, Koichiro; Mima, Masashi; Iwamoto, Kunihiko; Okada, Atsushi; Takata, Iichiro; Hitaka, Kosuke; Tanaka, Akihiro; Fujita, Kiyoko; Sugiyama, Hiroyuki; Hubbard, Roderick E. published an article.Formula: C13H11Br The title of the article was Fragment-Based Discovery of Novel Non-Hydroxamate LpxC Inhibitors with Antibacterial Activity. And the article contained the following:

UDP-3-O-acyl-N-acetylglucosamine deacetylase (LpxC) is a zinc metalloenzyme that catalyzes the first committed step in the biosynthesis of Lipid A, an essential component of the cell envelope of Gram-neg. bacteria. The most advanced, disclosed LpxC inhibitors showing antibacterial activity coordinate zinc through a hydroxamate moiety with concerns about binding to other metalloenzymes. Here, we describe the discovery, optimization, and efficacy of two series of compounds derived from fragments with differing modes of zinc chelation. A series was evolved from a fragment where a glycine moiety complexes zinc, which achieved low nanomolar potency in an enzyme functional assay but poor antibacterial activity on cell cultures. A second series was based on a fragment that chelated zinc through an imidazole moiety. Structure-guided design led to a 2-(1S-hydroxyethyl)-imidazole derivative exhibiting low nanomolar inhibition of LpxC and a min. inhibitory concentration (MIC) of 4μg/mL against Pseudomonas aeruginosa, which is little affected by the presence of albumin. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Formula: C13H11Br

The Article related to non hydroxamate palpxc inhibitor fragment discovery synthesis antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Formula: C13H11Br

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On October 1, 2020, Komandla, Mallareddy; Miura, Joanne; Wang, Haixia; Wang, Xiaolun; Lawson, John David; Tyhonas, John published a patent.COA of Formula: C9H9BrO3 The title of the patent was 2-oxo-2,3-dihydro-1H-imidazo[4,5-B]pyridin-6-yl)-4-methylbenzamide derivatives and related heterocycles as RIPK2 inhibitors for the treatment of autoimmune and other diseases. And the patent contained the following:

The invention relates to preparation of dihydroimidazopyridine benzamides(I) and related heterocycles, and pharmaceutically acceptable salts thereof, as RIPK2 inhibitors. Compounds I wherein α is a single bond; β is a double bond; R2 is oxo; R3 is C1-6 alkyl; R4, R5, R6, R7 and R8 each independently is H, halo, C1-4 alkyl, etc.; R9 is C1-6 alkyl, C3-8 haloalkyl, C2-8 heteroalkyl, etc.; etc., are claimed. The example compound II was prepared from the intermediates(also prepared), (procedure given). Compounds I were evaluated for their biol. activities (data given). Compounds I are receptor-interacting protein kinase 2 (RIPK2) inhibitors and can be useful for treating e.g. type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer and non-malignant proliferative disorders, such as e.g. allergic rhinitis, asthma, atopic dermatitis, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, lupus nephritis, psoriasis, immune thrombocytopenic purpura, inflammatory bowel disease, chronic obstructive pulmonary disease, Sjogren’s syndrome, ankylosing spondylitis, Behcet’s disease, graft vs. host disease, pemphigus vulgaris, idiopathic plasmacytic lymphadenopathy, atherosclerosis, myocardial infarction and thrombosis. The experimental process involved the reaction of 5-Bromo-2-methoxy-4-methylbenzoic acid(cas: 90326-61-7).COA of Formula: C9H9BrO3

The Article related to dihydroimidazopyridine benzamide preparation ripk2 inhibitor autoimmune disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.COA of Formula: C9H9BrO3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary