Category: 1036991-35-1

On February 1, 2021, Yang, Bowen; Wu, Qian; Huan, Xiajuan; Wang, Yingqing; Sun, Yin; Yang, Yueyue; Liu, Tongchao; Wang, Xin; Chen, Lin; Xiong, Bing; Zhao, Dongmei; Miao, Zehong; Chen, Danqi published an article.Category: nitriles-buliding-blocks The title of the article was Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors. And the article contained the following:

In an inhouse screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC50 values lower than 1 nM. Some compounds showed concentration-dependent characteristics of IL-2 inhibition. These results provided new applications of TNIK inhibitors and new prospects of TNIK as a drug target. The experimental process involved the reaction of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile(cas: 1036991-35-1).Category: nitriles-buliding-blocks

The Article related to pyrrolopyridine drug discovery synthesis potent tnik inhibitor, 1h-pyrrolo[2,3-b]pyridine, il-2 secretion inhibitory, tnik inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Category: nitriles-buliding-blocks

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On December 30, 2021, Vu, Binh; Dominique, Romyr; Li, Hongju; Fahr, Bruce; Chen, Yi published a patent.COA of Formula: C13H17BN2O2 The title of the patent was Methods and aromatic compounds for restoring mutant p53 function and their preparation. And the patent contained the following:

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The disclosure describes compounds of formula I and methods that restore DNA binding affinity of p53 mutants. The compounds of the disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds of formula I can be used to reduce the progression of cancers that contain a p53 mutation. Compounds of formula I wherein X1 is CR7 and N; X2 is CR2 and N; R1 and R2 are independently alkyl, NR8R9, CONR8R9, NHCOR9, etc.; Q is NHCH2C(:CH2)CONH2, NHCOCH:CH2, NHCH2C(:CH2)CN, etc.; R5 is H, halo, (un)substituted aryl, (un)substituted heteroaryl, etc.; R6 is (un)substituted (mono/bi)cyclic aryl and (un)substituted (mono/bi)cyclic heteroaryl; R7, R8 and R9 are independently (un)substituted alkyl, (un)substituted alkenyl, (un)substituted cycloalkyl, etc.; and with provisions; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their DNA binding affinity of mutant p53 protein. The experimental process involved the reaction of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile(cas: 1036991-35-1).COA of Formula: C13H17BN2O2

The Article related to aromatic compound preparation restore mutant p53 function, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C13H17BN2O2

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On August 5, 2021, Lamotte, Yann; Dodic, Nerina; Tap, Aurelien; Denis, Alexis; Brusq, Jean-Marie; Daoubi Khamlichi, Mourad; Benderitter, Pascal Andre Rene published a patent.Application In Synthesis of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile The title of the patent was Preparation of macrocyclic RIP2-kinase inhibitors. And the patent contained the following:

The invention relates to macrocyclic compounds of formula I and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of RIP2-kinase, and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of RIP2-kinase associated diseases. Moreover, the invention provides methods of using said compounds, for instance as a medicine or diagnostic agent. Compounds of formula I, wherein R1 is halo, alkynyl, CN, etc.; R2 and R10 are independently H and halo; R3, R3′, R4, R4′, R7 and R8 are independently H and C1-6 alkyl; R5 is OH, halo, CN, etc.; R6 is H, halo, C1-6 alkyl, etc.; R9 is H, C1-6 alkyl, COC1-6alkyl, etc.; and stereoisomers, tautomers, racemates, salts, hydrates, N-oxide forms, and solvates thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their RIP-2 kinase inhibitory activities (some data given). The experimental process involved the reaction of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile(cas: 1036991-35-1).Application In Synthesis of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile

The Article related to macrocycle rip2 kinase inhibitor preparation diagnostic treatment, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.Application In Synthesis of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On December 27, 2018, Du-Cuny, Lei; Xiao, Qitao; Xun, Guoliang; Zheng, Qiangang published a patent.Product Details of 1036991-35-1 The title of the patent was Preparation of substituted 5-cyanoindole compounds for the treatment of lysine (K)-specific demethylase 1A mediated diseases. And the patent contained the following:

A compound of formula I, or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for the treatment of lysine (K)-specific demethylase 1A (LSD1) – mediated diseases or disorders. Compounds of formula I wherein R1 is substituted C1-6 alkyl, substituted C3-6 cycloalkyl, substituted 7- to 11-membered spirocyclyl, etc.; R2 is H, halo, C1-4 alkyl, C1-4 haloalkyl, etc.; R3 is (un)substituted aminophenyl, (un)substituted aminopyridinyl, (un)substituted indolinyl, etc.; R4 is H, halo and C1-4 alkyl; R5 is H, halo, C1-4 alkyl, C1-4 haloalkyl, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their LSD1 modulatory activity. From the assay, it was determined that compound II exhibited IC50 value of 0.010 μM. The experimental process involved the reaction of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile(cas: 1036991-35-1).Product Details of 1036991-35-1

The Article related to cyanoindole preparation lsd1 modulator, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Product Details of 1036991-35-1

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On August 11, 2022, Zhai, Wenqiang; Zhang, Zhimin; Pan, Hao; Wang, Zhe; Guo, Liubin; Zhang, Yuren; Liu, Dongzhou published a patent.Category: nitriles-buliding-blocks The title of the patent was Pyrrolopyridazine compound, and preparation method therefor and use thereof. And the patent contained the following:

The present invention relates to a pyrrolopyridazine compound as represented by a formula I [wherein X = C or N; R1 = H, halo, alkyl, alkenyl, etc.; Y = H, halo, OH, NH2, etc.; R3 = H, halo, alkyl, alkenyl, etc.; L2 = a single bond, CO, alkylene, etc.; Cy2 = cycloalkylene, heterocyclylene, O, etc.; R6 = independently halo, OH, NH2, CN, etc.; L3 = a single bond, O, or alkylene; Cy3 = cycloalkyl, heterocyclyl, aryl, or heteroaryl; R8 = independently H, halo, alkyl, etc.; m = 0-4; p = 0-3; with provisos] or a pharmaceutically acceptable salt thereof, and also relates to a pharmaceutical preparation, a pharmaceutical composition and the use thereof, wherein the compound can be used for the preparation of drugs for treating or preventing related diseases mediated by HPK1. For example, II was prepared in a multi-step synthesis. The experimental process involved the reaction of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile(cas: 1036991-35-1).Category: nitriles-buliding-blocks

The Article related to pyrrolopyridazine hpk1 treatment cancer human, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Category: nitriles-buliding-blocks

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On June 11, 2020, Vacca, Joseph P.; Wager, Travis T. published a patent.Application In Synthesis of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile The title of the patent was Preparation of substituted sulfonamido benzamides for the treatment of various diseases. And the patent contained the following:

The invention relates to preparation of substituted sulfonamido benzamides(I) for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmol. diseases, and viral infections. Compounds I wherein ring A is aryl or heteroaryl; R1 is H, C1-6 alkyl or C1-6 haloalkyl; R2 is C1-6 alkyl or C1-6 alkenyl, C1-6 heteroalkyl, etc.; R3-R5 each independently is H, halo, C1-6 alkyl; R6 is (un)substituted C1-6 alkyl; R7 is C1-6 alkyl, etc., are clamed. The example compound II was prepared using f 5-amino-2-chloro-benzoic acid as starting material (procedure given). Compounds I were evaluated for their biol. activity (data given). Compounds I can be used in treatment of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmol. diseases, and viral infections. The experimental process involved the reaction of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile(cas: 1036991-35-1).Application In Synthesis of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile

The Article related to sulfonamido benzamide preparation neuroprotectant antitumor antiviral ophthalmol musculoskeletal drug, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Application In Synthesis of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On July 3, 2008, Berdini, Valerio; Besong, Gilbert Ebai; Callaghan, Owen; Carr, Maria Grazia; Congreve, Miles Stuart; Gill, Adrian Liam; Griffiths-Jones, Charlotte Mary; Madin, Andrew; Murray, Christopher William; Nijjar, Rajdeep Kaur; O’Brien, Michael Alistair; Pike, Andrew; Saxty, Gordon; Taylor, Richard David; Vickerstaffe, Emma published a patent.Product Details of 1036991-35-1 The title of the patent was Preparation of bicyclic heterocyclic compounds as FGFR inhibitors. And the patent contained the following:

The title compounds I [X1, X2, X3 = C or N, such that at least one of X1-X3 = N; X4 = CR3 or N; X5 = CR5, N or C(O); provided that no more than 3 of X1-X5 = N; R1 = NHCONR4R5, NHCO2R4, NHCSOR4, etc.; R3 = halo, H, alkyl, etc.; R3 = H, halo, alkyl, etc.; R4, R5 = H, alkyl, cycloalkyl, etc.; A = (un)substituted (non)aromatic carbocyclic or heterocyclic group; with the provisos], useful in the treatment of diseases, e.g. cancer, were prepared E.g., a 2-step synthesis of II, starting from 6-chloro-3-iodoimidazo[1,2-a]pyridine with 3-acetylaminophenylboronic acid, was given. Exemplified compounds I were tested in in vitro FGFR3 and PDGFR kinase assays. Many compounds I showed IC50 of <10 渭M or provided at least 50% inhibition of the FGFR3 activity at a concentrate of 10 渭M. Preferred I showed IC50 of <1 渭M or provided at least 50% inhibition of the FGFR3 activity at a concentrate of 1 渭M. Pharmaceutical composition comprising the compound I is disclosed. The experimental process involved the reaction of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile(cas: 1036991-35-1).Product Details of 1036991-35-1

The Article related to bicyclic heterocyclic imidazopyridine preparation fibroblast growth factor receptor inhibitor, fgfr3 inhibitor antitumor bicyclic heterocyclic imidazopyridine preparation and other aspects.Product Details of 1036991-35-1

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On June 11, 2020, Vacca, Joseph P.; Wager, Travis T. published a patent.Application In Synthesis of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile The title of the patent was Preparation of substituted sulfonamido benzamides for the treatment of various diseases. And the patent contained the following:

The invention relates to preparation of substituted sulfonamido benzamides(I) for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmol. diseases, and viral infections. Compounds I wherein ring A is aryl or heteroaryl; R1 is H, C1-6 alkyl or C1-6 haloalkyl; R2 is C1-6 alkyl or C1-6 alkenyl, C1-6 heteroalkyl, etc.; R3-R5 each independently is H, halo, C1-6 alkyl; R6 is (un)substituted C1-6 alkyl; R7 is C1-6 alkyl, etc., are clamed. The example compound II was prepared using f 5-amino-2-chloro-benzoic acid as starting material (procedure given). Compounds I were evaluated for their biol. activity (data given). Compounds I can be used in treatment of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmol. diseases, and viral infections. The experimental process involved the reaction of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile(cas: 1036991-35-1).Application In Synthesis of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile

The Article related to sulfonamido benzamide preparation neuroprotectant antitumor antiviral ophthalmol musculoskeletal drug, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Application In Synthesis of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts