Category: 50743-01-6

On February 4, 2021, Tanaka, Yuta; Tanaka, Yuta; Kikuchi, Fumiaki; Yamamoto, Takeshi; Nakamura, Minoru; Takami, Kazuaki; Murakami, Masataka; Daini, Masaki; Wada, Yasufumi; Kakegawa, Keiko; Kasahara, Takahito; Ohashi, Tomohiro; Wang, Junsi; Ikeda, Zenichi; Puenner, Florian; Seto, Masaki; Mikami, Satoshi; Sasaki, Minoru published a patent.Related Products of 50743-01-6 The title of the patent was Heterocyclic compound for Gaucher disease. And the patent contained the following:

Provided is a compound which has a glucosylceramide synthase-inhibiting activity and is expected to be useful as a prophylactic or therapeutic agent for a lysosomal storage disease (e.g., Gaucher disease, Fabry disease, GM1-gangliosidosis, GM2 activation factor deficiency disease, Tay-Sachs disease, Sandhoff disease), a neurodegenerative disease (e.g., Parkinson’s disease, dementia with Lewy bodies, multiple system atrophy) and the like. The present invention relates to a compound represented by formula (I); or a salt thereof. The experimental process involved the reaction of 5-Bromo-1H-imidazole-4-carbaldehyde(cas: 50743-01-6).Related Products of 50743-01-6

The Article related to glucosylceramide synthase heterocyclic compound gaucher disease, Pharmaceuticals: Formulation and Compounding and other aspects.Related Products of 50743-01-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Stensio, Karl E.; Wahlberg, Kerstin; Wahren, Robert published an article in 1973, the title of the article was Synthesis of brominated imidazoles.COA of Formula: C4H3BrN2O And the article contains the following content:

Bromination of imidazole in HOAc containing NaOAc gives 2,4,5-tribromoimidazole (I) in a good yield. 4(5)-(2-Chloroethyl)imidazole, imidazole-4(5)-carboxaldehyde, and 4(5)-hydroxymethylimidazole were similarly brominated. Debromination of I with Na2SO3 or BuLi gives 4(5)-bromoimidazole. A simple synthesis of 4(5)-(2-bromoethyl)imidazole is described. The experimental process involved the reaction of 5-Bromo-1H-imidazole-4-carbaldehyde(cas: 50743-01-6).COA of Formula: C4H3BrN2O

The Article related to bromination imidazole, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.COA of Formula: C4H3BrN2O

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On January 25, 2021, Forrest, Michael D. published a patent.Related Products of 50743-01-6 The title of the patent was Therapeutic modifiers of the reverse mode of ATP synthase for treating diseases. And the patent contained the following:

Compounds that slow the ATP-hydrolyzing mode of ATP synthase are useful for treating various diseases and disorders including cancer, particularly cancers that utilize the Warburg effect. The experimental process involved the reaction of 5-Bromo-1H-imidazole-4-carbaldehyde(cas: 50743-01-6).Related Products of 50743-01-6

The Article related to atp synthase reverse mode modifier disease treatment, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Related Products of 50743-01-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On November 21, 2019, Yang, Wenjin; Chang, Kai-Wei; Liu, Suying; Tsai, Cheng-Han published a patent.Reference of 5-Bromo-1H-imidazole-4-carbaldehyde The title of the patent was Preparation of imidazolidines as matrix metalloproteinase (MMP) inhibitors useful in treatment of diseases. And the patent contained the following:

The invention relates to preparation of hydantoin-based compounds (I) useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Compounds I wherein ring B is (un)substituted aryl or heteroaryl; ring C is aryl or heteroaryl; ring D is aryl or heteroaryl; each X, Y, and Z each independently is O, CH2, NH, etc.; R1 is H or alkyl; R2 is H, halo, OH, etc.; R3 is H, halo, alkyl, etc.; R4 is H or alkyl; R5 is H; m is 1-4; n is 1-5, are claimed. The example compound II was prepared by a synthetic procedure from the intermediate compound(also prepared) (procedure given). Compounds I were evaluated for their biol. activities including selective MMP inhibiting activity (data given). Compounds I and related compositions are selective inhibitors of MMP-12 and can be used in treatment of diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis. The experimental process involved the reaction of 5-Bromo-1H-imidazole-4-carbaldehyde(cas: 50743-01-6).Reference of 5-Bromo-1H-imidazole-4-carbaldehyde

The Article related to imidazolidine preparation selective mmp inhibitor disease treatment, hydantoin preparation selective macrophage elastase mmp12 inhibitor disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Reference of 5-Bromo-1H-imidazole-4-carbaldehyde

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On February 14, 2008, McCormick, Kevin D.; Boyce, Christopher W.; Shih, Neng-Yang; Huang, Chia-Yu; Aslanian, Robert G.; Fevrier, Salem; Liang, Bo; Liu, Rong-Qiang; Liu, Ruiyan; Mangiaracina, Pietro; De Lera Ruiz, Manuel; Yu, Younong; Guise-Zawacki, Lisa; Zheng, Junying published a patent.SDS of cas: 50743-01-6 The title of the patent was Preparation of imidazolylmethylbenzoxazines and related compounds as α2c adrenoreceptor agonists.. And the patent contained the following:

Title compounds [I; A = (substituted) 5-membered heterocyclyl; X = O, S, SO, SO2, NR6; J1-J4 = N, NO, CR2; R2 = H, OH, halo, cyano, NO2, (substituted) alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, etc.; R3 = H, O, (substituted) alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, etc.; R4 = H, cyano, (substituted) alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, aryl, aryloxy, aralkyl, heteroaryl, heterocyclyl, etc.; R6 = H, (substituted) alkyl, alkoxy, alkenyl, alkenyloxy, cycloalkyl, aryl, aryloxy, aralkyl, heteroaryl, heterocyclyl, heterocyclylalkyl, etc.; m = 1-5; n = 1-3; p = 0-4; with provisos], were prepared Thus, 2,3-dihydro-1,4-benzoxazine was stirred with imidazole-4-carboxaldehyde, NaBH(OAc)3, and HOAc in dichloroethane at 60° overnight to give 50% title compound (II). II and other I showed α2c adrenoreceptor agonist activity at ≥30% Emax (GTPγS assay). The experimental process involved the reaction of 5-Bromo-1H-imidazole-4-carbaldehyde(cas: 50743-01-6).SDS of cas: 50743-01-6

The Article related to imidazolylmethylbenzoxazine preparation adrenoreceptor agonist, rhinitis nasal congestion pain diarrhea glaucoma treatment benzoxazine imidazolylmethyl, Heterocyclic Compounds (More Than One Hetero Atom): Oxazines (Including Morpholine) and other aspects.SDS of cas: 50743-01-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On March 1, 2007, McCormick, Kevin D.; Boyce, Christopher W.; Shih, Neng-Yang; Aslanian, Robert G.; Mangiaracina, Pietro; De Lera Ruiz, Manuel; Yu, Younong; Biju, Purakkattle J.; Huang, Chia-Yu; Liang, Bo; Liu, Ruiyan; Liu, Rong-Qiang; Guise-Zawacki, Lisa published a patent.Category: imidazoles-derivatives The title of the patent was Preparation of imidazolylmethylbenzoxazines and related compounds as α2c adrenoreceptor agonists.. And the patent contained the following:

Title compounds [I; A = (substituted) 5-membered heterocyclyl; X = O, S, SO, SO2, NR6; J1-J4 = N, NO, CR2; R2 = H, OH, halo, cyano, NO2, (substituted) alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, etc.; R3 = H, O, (substituted) alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, etc.; R4 = H, cyano, (substituted) alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, aryl, aryloxy, aralkyl, heteroaryl, heterocyclyl, etc.; R6 = H, (substituted) alkyl, alkoxy, alkenyl, alkenyloxy, cycloalkyl, aryl, aryloxy, aralkyl, heteroaryl, heterocyclyl, heterocyclylalkyl, etc.; m = 1-5; n = 1-3; p = 0-4; with provisos], were prepared Thus, 2,3-dihydro-1,4-benzoxazine was stirred with imidazole-4-carboxaldehyde, NaBH(OAc)3, and HOAc in dichloroethane at 60° overnight to give 50% title compound (II). II and other I showed α2c adrenoreceptor agonist activity at ≥30% Emax (GTPγS assay). The experimental process involved the reaction of 5-Bromo-1H-imidazole-4-carbaldehyde(cas: 50743-01-6).Category: imidazoles-derivatives

The Article related to imidazolylmethylbenzoxazine preparation adrenoreceptor agonist, rhinitis nasal congestion pain diarrhea glaucoma treatment benzoxazine imidazolylmethyl, Heterocyclic Compounds (More Than One Hetero Atom): Oxazines (Including Morpholine) and other aspects.Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On August 21, 2008, McCormick, Kevin D.; Boyce, Christopher W.; Shih, Neng-Yang; Aslanian, Robert G.; Fevrier, Salem; Mangiaracina, Pietro; De Lera Ruiz, Manuel; Yu, Younong; Zheng, Junying; Huang, Chia-Yu; Liang, Bo; Liu, Rong-Qiang; Liu, Ruiyan; Guise Zawacki, Lisa published a patent.Safety of 5-Bromo-1H-imidazole-4-carbaldehyde The title of the patent was 3,4-Dihydro-1,4-benzoxazine, 3,4-dihydro-1,4-benzothiazine and 1,2,3,4-tetrahydroquinoxaline derivatives as alpha2C adrenoreceptor agonists and their preparation. And the patent contained the following:

The invention relates to a class of benzomorpholine and benzothiomorpholine compounds of formula I useful as alpha2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the alpha2C adrenergic receptor agonists, such as allergic rhinitis, congestion, pain, diarrhea, glaucoma, congestive heart failure, cardiac ischemia, manic disorders, depression, anxiety and schizophrenia. Compounds of formula I wherein A is (un)substituted 5-membered heterocyclic ring; X is O, S, SO, SO2 and NH and derivatives; J1, J2, J3 and J4 are independently, N, NO and CR2, with the proviso that 0-3 of J1-J4 are N; R2 is H, OH, halo, CN, NO2, etc.; Y is (CH2)1-3; each R3 is H, halo, =O, alkyl, alkoxy, alkenyl, etc.; R4 is H, CN, halo, alkyl, alkoxy, alkenyl, etc.; n is 1-5; m is 0-4; and their pharmaceutically acceptable salts, esters, solvates and prodrugs thereof are claimed. Example compound II was prepared by reductive alkylation of 3,4-dihydro-2H-1,4-benzoxazine with imidazole-4-carboxaldehyde. All the invention compounds were evaluated for their 伪2C adrenoreceptor agonistic activity (some data given). The experimental process involved the reaction of 5-Bromo-1H-imidazole-4-carbaldehyde(cas: 50743-01-6).Safety of 5-Bromo-1H-imidazole-4-carbaldehyde

The Article related to benzoxazine benzothiazine quinoxaline preparation adrenoceptor agonist treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Safety of 5-Bromo-1H-imidazole-4-carbaldehyde

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On July 12, 2007, Hupe, Eike; Zagar, Cyrill; Witschel, Matthias; Kuehn, Toralf; Moberg, William Karl; Parra Rapado, Liliana; Stelzer, Frank; Vescovi, Andrea; Reinhard, Robert; Sievernich, Bernd; Grossmann, Klaus; Ehrhardt, Thomas published a patent.SDS of cas: 50743-01-6 The title of the patent was Preparation of piperazine-2,5-diones as herbicides. And the patent contained the following:

Title compounds [I; R1, R2 = cyano, alkyl, cycloalkyl, (cyclo)alkenyl, (cyclo)alkynyl, Ph, phenylalkyl, heterocyclyl, etc.; R3 = H, halo, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, cycloalkynyl, Ph, phenylalkyl, etc.; R4-R6 = H, OH, (substituted) alkyl, alkoxy; A1, A2 = (hetero)aryl; R9 = halo, cyano, NO2, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkadienyl, alkynyl, etc.; R10-R14 = H, halo, cyano, NO2, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkadienyl, alkynyl, etc.], were prepared Thus, methanesulfonic acid [(5-benzyl-1,4-dimethyl-3,6-dioxopiperazin-2-yl)-(2-nitrophenyl)methyl] ester (preparation given) was dropwise treated with DBU in THF at 0掳 followed by 4 h stirring at 0掳 to give 76% 3-benzyl-1,4-dimethyl-6-(2-nitrobenzylidene)piperazine-2,5-dione. I at 0.5-3 kg/ha were said to show very strong pre- and postemergent herbicidal activity. The experimental process involved the reaction of 5-Bromo-1H-imidazole-4-carbaldehyde(cas: 50743-01-6).SDS of cas: 50743-01-6

The Article related to piperazinedione preparation herbicide, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 50743-01-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On May 28, 2020, Panarese, Joseph; Davis, Dexter; Bartlett, Samuel; Chong, Katherine; Kenton, Nathaniel; Or, Yat Sun published a patent.Name: 5-Bromo-1H-imidazole-4-carbaldehyde The title of the patent was Functionalized heterocycles as antiviral agents and their preparation. And the patent contained the following:

The invention discloses compounds of formula I, or pharmaceutically acceptable salts, thereof which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. Compounds of formula I wherein Q1, Q2, Q3 and Q4 are independently H, halo, (un)substituted C1-6 alkyl, (un)substituted C1-6 alkoxy, etc.; Y1 is H, halo and (un)substituted C1-6 alkyl; Y2 is O, NH and derivatives, NOH and derivatives and NNH and derivatives; Y3 is CO2H and derivatives, CONHSO2H and derivatives, (un)substituted aryl; Y4 is H and (un)substituted methyl; Y2Y3 may be taken together to form 5- to 12-membered heterocyclic ring; Z1 is N and CR1; Z2 is N and CR2; Z3 is N and CR3; provided that at least one of Z1 – Z3 is N, and when Z3 is N, Z1 is CR1, Z2 is CR2, and R2 is not H; R1, R2 and R3 are independently H, halo, NO2, CN, (un)substituted C1-6 alkyl, etc.; and pharmaceutically acceptable salts, N-oxides, esters and prodrugs thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their antiviral activity. From the assay, it was determined that compound II exhibited an EC50 value of < 0.1渭M and a CC50 value of > 25渭M. The experimental process involved the reaction of 5-Bromo-1H-imidazole-4-carbaldehyde(cas: 50743-01-6).Name: 5-Bromo-1H-imidazole-4-carbaldehyde

The Article related to heterocycle preparation antiviral, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Name: 5-Bromo-1H-imidazole-4-carbaldehyde

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On April 8, 2021, Folmer, Rutger; Hekking, Koen F. W.; Calpe, Blaise; Mueller, Gerhard; Fabritius, Charles-Henry published a patent.SDS of cas: 50743-01-6 The title of the patent was Azaindole derivatives and related compounds as inhibitors of dual specificity tyrosine phosphorylation regulated kinase 1B and their preparation. And the patent contained the following:

The invention relates to compounds of formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, in particular for use in the treatment, amelioration or prevention of cancer, Alzheimer, Parkinson, Down syndrome, metabolic syndrome, diabetes and/or osteoarthritis. Compounds of formula I wherein X1 is N, CH and CF; X2 = N, CH and CR1; each R2 is independently H and R1; Y1 is S and O; Y2 is C, CN, CMe, CCl and CF; Y3 is N, CH and CR1; A is (un)substituted (mono/bi/tri)cyclic heterocyclyl; R1 is (un)substituted C1-6 alkyl, halo, CN, NO2, etc.; and pharmaceutically acceptable salts, solvates, cocrystals, tautomers, racemates, enantiomers, diastereomers and mixtures thereof, are claimed. Example compound II was prepared by cyclization of 2-chloro-1-(1H-pyrrolo[2,3-b]pyridin-3-yl)ethan-1-one with 1H-imidazole-4-carbothioamide. The invention compounds were evaluated for their DYRK1B inhibitory activity. From the assay it was determined that compound II exhibited IC50 value in the range of 10 nM to < 100 nM. The experimental process involved the reaction of 5-Bromo-1H-imidazole-4-carbaldehyde(cas: 50743-01-6).SDS of cas: 50743-01-6

The Article related to azaindole preparation dyrk1b 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.SDS of cas: 50743-01-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem