Tag: 400-500

On February 5, 2015, Koizumi, Noriko; Okumura, Naoki; Kinoshita, Shigeru published a patent.Recommanded Product: 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one The title of the patent was Drug for prevention or treatment of diseases associated with abnormalities in extracellular matrix (ECM) of corneal endothelium. And the patent contained the following:

The drug, especially for diseases associated with Fuchs’ corneal endothelial dystrophy. contains a TGF-β signal inhibitor. Also claimed are the TGF-β signal inhibitor for the drug, and the treatment/prevention method by administration of the TGF-β inhibitor. Such diseases include photophobia, blurred vision, vision disorders, eye pain, tearing, hyperemia, pain, bullous keratopathy, eye discomfort, contrast reduction, glare, edema of the corneal stroma, bullous keratopathy and corneal opacity. The TGF β-signal inhibitor may be 4-[4-(1,3-benzodioxole-5-yl)-5-(2-pyridinyl)-1H-imidazole-2-yl]benzamide. The experimental process involved the reaction of 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one(cas: 1009104-85-1).Recommanded Product: 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one

The Article related to tgf signal inhibitor corneal endothelial ecm disease fuchs dystrophy, Pharmaceuticals: Formulation and Compounding and other aspects.Recommanded Product: 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On February 28, 2021, Aseem, Sayed Obaidullah; Jalan-Sakrikar, Nidhi; Chi, Cheng; Navarro-Corcuera, Amaia; De Assuncao, Thiago M.; Hamdan, Feda H.; Chowdhury, Shiraj; Banales, Jesus M.; Johnsen, Steven A.; Shah, Vijay H.; Huebert, Robert C. published an article.Computed Properties of 1009104-85-1 The title of the article was Epigenomic Evaluation of Cholangiocyte Transforming Growth Factor-β Signaling Identifies a Selective Role for Histone 3 Lysine 9 Acetylation in Biliary Fibrosis. And the article contained the following:

Transforming growth factor β (TGFβ) upregulates cholangiocyte-derived signals that activate myofibroblasts and promote fibrosis. Assay for Transposase-Accessible Chromatin using sequencing (ATAC-seq) was used to investigate changes in chromatin accessibility. TGFβ stimulation caused widespread changes in histone 3 lysine 27 acetylation (H3K27ac), and was associated with global TGFβ-mediated transcription. In contrast, H3K9ac was gained in a smaller group of chromatin sites and was associated with fibrosis pathways. These pathways included overexpression of hepatic stellate cell (HSC) activators such as fibronectin 1 (FN1) and SERPINE1. The promoters of these genes showed H3K9ac enrichment following TGFβ. Of the acetyltransferases responsible for H3K9ac, cholangiocytes predominantly express Lysine Acetyltransferases 2A (KAT2A). Small interfering RNA knockdown of KAT2A or H3K9ac inhibition prevented the TGFβ-mediated increase in FN1 and SERPINE1. SMAD3 ChIP-seq and ATAC-seq suggested that TGFβ-mediated H3K9ac occurs through SMAD signaling, which was confirmed using colocalization and genetic knockdown studies. Pharmacol. inhibition or cholangiocyte-selective deletion of Kat2a was protective in mouse models of biliary fibrosis. Cholangiocyte expression of HSC-activating signals occurs through SMAD-dependent, KAT2A-mediated, H3K9ac, and can be targeted to prevent biliary fibrosis. The experimental process involved the reaction of 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one(cas: 1009104-85-1).Computed Properties of 1009104-85-1

The Article related to biliary fibrosis cholangiocyte transforming growth factor histone h3 acetylation, epigenetics, fn, pai1, Mammalian Pathological Biochemistry: Digestive Tract Diseases and other aspects.Computed Properties of 1009104-85-1

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On August 2, 2012, Heller, Stefan; Ronaghi, Mohammad; Oshima, Kazuo published a patent.Application In Synthesis of 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one The title of the patent was Methods for generating inner ear cells in vitro from pluripotent stem cells. And the patent contained the following:

Methods, compositions and kits are provided for generating inner ear cells in vitro. These methods find use a number of applications, such as in preparing inner ear cells for in vitro screening for agents that are toxic to inner ear cells, for in vitro screening for agents that prevent against, mitigate, or reverse the toxic effects of such agents, and for in vitro screening for agents that promote otoregeneration. The experimental process involved the reaction of 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one(cas: 1009104-85-1).Application In Synthesis of 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one

The Article related to inner ear cell pluripotent stem in vitro, Fermentation and Bioindustrial Chemistry: Animal Cell Culture and other aspects.Application In Synthesis of 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On September 1, 2020, Yu, Xiyong; Lan, Huiyao; Hu, Wenhui; Yang, Zhongjin; Wu, Nannan published a patent.Recommanded Product: 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one The title of the patent was Azaindoles and their application as antitumor drugs. And the patent contained the following:

The invention provides azaindoles and its application, which can effectively inhibit the phosphorylation of SMAD3, and has good antitumor activity in the tumor model induced by LCC in rats. The invention provides azaindole or its pharmaceutically acceptable salt or stereoisomer or prodrug mol. as shown in formula I, wherein D is selected from C and N; and R2 does not exist when D is N; A and B are independently selected from N and CR3; R1 is selected from H, C1-C6 alkyl, C6-C10 aryl, C3-C8 cycloalkyl, halogen, CN; R2 selected from: H, C1-C6 alkyl; each R3 is independently selected from H, C1-C6 alkyl, halogen, CN; R4 is selected from carbonyl compounds; R5, R5a, R5b = H, halogen, CN, C1-C6 alkyl, C3-C8 cycloalkyl. For example, compound II was prepared in a multi-step synthesis. The title compound can be used as a pharmaceutical composition for the prevention and/or treatment of cancer. The experimental process involved the reaction of 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one(cas: 1009104-85-1).Recommanded Product: 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one

The Article related to azaindole anticancer agent elimination reaction amidation substitution, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On April 30, 2021, Wang, Dao-Cai; Yan, Ting-Ting; Chen, Bin; Liu, Feng; Liu, Xiao-Peng; Xie, Yong-Mei published an article.Name: 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one The title of the article was SIS3, a good candidate for the reverse of type 2 diabetes mellitus in mice. And the article contained the following:

TGF-β signaling plays an extremely important role in the occurrence and development of type 2 diabetes mellitus (T2DM), and the blockade of TGF-b/Smad3 pathway protests against the high-fat diet-induced obesity and diabetes. As a specific small mol. inhibitor of Smad3 protein, the biol. activities of compound SIS3 were evaluated by high-fat diet-induced T2DM model mice. In vivo results indicated that SIS3 can not only significantly reduce the body weight, fat mass, and fasting blood glucose in high-fat diet-induced T2DM model mice, but also improve insulin sensitivity and oral glucose tolerance of high-fat diet-induced T2DM model mice after the injection of SIS3 with 5 mg/kg for 45 days. The experimental process involved the reaction of 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one(cas: 1009104-85-1).Name: 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one

The Article related to compound sis diabetes mellitus mouse, sis3, smad3 inhibitor, treatment, type 2 diabetes mellitus, Pharmacology: Effects Of Agents For Treating Metabolic and Endocrine Disorders and other aspects.Name: 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On February 28, 2008, Lautens, Mark; Yuen, Josephine; Fang, Yuanqing published a patent.Application of 1009104-85-1 The title of the patent was Process for preparation of pyrrole derivatives. And the patent contained the following:

The present invention pertains to processes for the chem. synthesis of pyrrole derivatives, particularly azaindole and thienopyrrole compounds that are substituted at the 2-position of the azaindole or thienopyrrole ring. For example, to a mixture of 3-(2,2-dibromoethenyl)-N-methyl-2-pyridinamine (preparation given), phenylboronic acid, and K3PO4•H2O under argon was added a solution of Pd(OAc)2 and S-Phos in toluene. The reaction was heated to 100 °C for 2 h., then cooled to room temperature, worked-up with saturated NaHCO3 solution, extracted with Et2O, dried over Na2SO4, and concentrated in vacuo. The crude material was purified using chromatog. eluting with 25 % EtOAc/hexane to yield the product, 1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridine, as a white solid in 84% yield. 1-Methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridine obtained above can be used for the preparation of com. important azaindole compounds as pharmaceutical agents. The experimental process involved the reaction of 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one(cas: 1009104-85-1).Application of 1009104-85-1

The Article related to preparation pyrrolopyridine thienopyrrole azaindole, 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 1009104-85-1

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem