Month: October 2022

On May 29, 1991, Gueremy, Claude; Malleron, Jean Luc; Mignani, Serge published a patent.Recommanded Product: 4-Bromo-5-nitroisoquinoline The title of the patent was Preparation and formulation of 2-[4-(indolylmethyl)piperidinoethyl]naphthoisothiazole-1,1-dioxides and analogs as serotonin (5HP) reuptake inhibitors. And the patent contained the following:

R1(CH2)nQ [I; Q = Z3R3, Z4R4; R1 = anellated isothiazolo groups Q1-Q3, RSO2N(Z), etc.; R = 2-naphthyl; R3 = 1-indenyl, 1-indanyl, (CH2)mR2, etc.; R2 = indolyl, indanyl, indenyl, quinolyl, etc.; R4 = (CH2)mR2; Y = H, alkyl, alkoxy, Ph; Z = alkyl; Z1 = SO2, CO; Z2 = CH; Z2 may also = N when Z1 = SO2; Z3 = piperidine-1,4-diyl; Z4 = piperazine-1,4-diyl, 1,2,3,6-tetrahydropyridine-1,4-diyl; m = 1, 2; n = 2, 3] were prepared Thus, BrCH2CH2Cl was condensed with 1,8-naphthosultam and the product condensed with 4-[(5-fluoro-3-indolyl)methyl]piperidine to give, after N-methylation, title compound II. I had IC50 < 25 nM for binding of paroxetine (substrate not given). The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Recommanded Product: 4-Bromo-5-nitroisoquinoline

The Article related to naphthoisothiazole indolylmethylpiperidinoethyl serotonin reuptake inhibitor, indolylmethylpiperidinoethylnaphthoisothiazole preparation serotonin reuptake inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Recommanded Product: 4-Bromo-5-nitroisoquinoline

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 July 16, 2020, Marx, Matthew Arnold; Christensen, James Gail; Smith, Christopher Randolph; Fischer, John P.; Burns, Aaron Craig published a patent.Recommanded Product: 58142-46-4 The title of the patent was Preparation of pyrimidine derivatives as KRas G12C inhibitors for the treatment of KRas-mediated diseases. And the patent contained the following:

The invention relates to preparation of pyrimidines(I) that inhibit KRas G12C. Compounds I wherein X is a 4-12 membered saturated or partially saturated monocyclic, bridged, spirocyclic or fused bicyclic ring; Y is a bond, O, S, etc.; R2 is H, alkyl, alkoxy, etc.; L is bond, C(O), or C1-3 alkylene; R4 is H, aryl, cycloalkyl, etc.; etc., are claimed. The example compound II was prepared via multi-steps synthesis using 4,7-dichloropyrido[4,3-d]pyrimidine as starting material (procedure given). Compounds I are irreversible inhibitors of of KRas G12C (data given). Compounds I can be used in treatment of diseases that are KRas-mediated as well as caused by KRas G12C mutation. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Recommanded Product: 58142-46-4

The Article related to pyrimidine preparation kras g12c inhibitor disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On October 22, 2015, Wu, Frank published a patent.Synthetic Route of 74904-29-3 The title of the patent was Preparation of tyrosine kinase inhibitors. And the patent contained the following:

The present invention relates to tyrosine kinase inhibitors I [wherein Z1 and Z2 = independently N or (un)substituted CH; with the proviso that at least one of Z1 and Z2 is N; X = absence, O, S, (un)substituted CH or NH; Y = O, S, (un)substituted CH or NH; A = (un)substituted aryl, heteroaryl, heterocyclyl, or cycloalkyl; B and C = independently absence, (un)substituted ring or fused ring], pharmaceutically acceptable salts, esters, solvates and stereoisomers thereof. The compounds of the present invention can be used as tyrosine kinase inhibitors, or used to reduce or inhibit the activity of EGFR or mutants thereof (for example, EGFR mutants containing T790M mutation) in cells, or used to treat and/or prevent diseases (for example, cancer) related to overactivity of EGFR, especially drug-resistant diseases (for example, cancer) caused by mutation of EGFR (for example, T790M mutation of EGFR). For example, II was prepared in a multi-step synthesis, which showed inhibitory activity with IC50 of 5.7 nM against EGFR T790. The experimental process involved the reaction of 8-Methoxy-3,4-dihydroisoquinolin-1(2H)-one(cas: 74904-29-3).Synthetic Route of 74904-29-3

The Article related to preparation tyrosine kinase inhibitor treatment cancer egfr human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 74904-29-3

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On October 22, 2020, Marx, Matthew Arnold; Christensen, James Gail; Smith, Christopher Ronald; Fischer, John P.; Burns, Aaron Craig published a patent.Recommanded Product: 4-Bromo-5-nitroisoquinoline The title of the patent was Preparation of pyridopyrimidine derivatives as KRas G12C inhibitors for the treatment of KRas-mediated diseases. And the patent contained the following:

The invention relates to preparation of pyridopyrimidines, e.g., I, that inhibit KRas G12C. Thus, I was prepared via intermediate II. Pyridopyrimidines of the invention are irreversible inhibitors of KRas G12C (data given) and can be used in treatment of diseases that are KRas-mediated as well as caused by KRas G12C mutation. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Recommanded Product: 4-Bromo-5-nitroisoquinoline

The Article related to pyridopyrimidine preparation kras g12c inhibitor disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 4-Bromo-5-nitroisoquinoline

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On October 31, 2017, Moon, Seong Yun; Kim, Seul Gi; Lee, Seon Hui; Choi, Yeon Hui; Park, Chi Hyeon published a patent.Application of 58142-46-4 The title of the patent was Preparation of condensed polycyclic compounds for organic electric device. And the patent contained the following:

Disclosed are compounds I [X = N-L1-R1, S, O, etc.; n, m = 0 or 1 such as m+n≥1 (when n or m is 0, then A or B, at each occurrence, represents a single bond); A, B = independently single bond, N-L2-R2, S, etc.; Z1-Z12 = independently CR3 or N with a proviso that at least one of Z1-Z12 is N; R1-R3 = independently H, aryl, fluorenyl, etc.; L1, L2 = single bond, arylene, fluorenylene, etc.] and electronic device thereby. For example, red electroluminescent device comprising II (phosphorescent host material) showed improvements in luminous efficiency, lifespan and driving voltage compared to device using CBP. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Application of 58142-46-4

The Article related to condensed polycycle preparation organic elec device material, Optical, Electron, and Mass Spectroscopy and Other Related Properties: Luminescence and other aspects.Application of 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On April 23, 2019, Shen, Jianhua; Leng, Ying; Chen, Tingting; Wang, Kai; Ning, Mengmeng published a patent.SDS of cas: 74904-29-3 The title of the patent was Preparation of amide compounds as GPR40 agonists. And the patent contained the following:

The title amide compound is shown in formula I, wherein, A is 5-7-membered heteroaryl or 6-10-membered aryl; M is O, S or N-alkyl; R1 is H or halogen; R2 is hydroxypropyl, cyclopropyl or propynyl; R3 is H, alkyl, alkoxy or halogen; R4 and R5 are independently selected from H, indanyl, alkyl, 5-7-membered heterocyclic group, etc. The inventive amide compound is capable of regulating GPR40 activity, and can be applied in treating GPR40 activity-related diseases, such as diabetes and metabolic syndrome. The experimental process involved the reaction of 8-Methoxy-3,4-dihydroisoquinolin-1(2H)-one(cas: 74904-29-3).SDS of cas: 74904-29-3

The Article related to amide preparation gpr40 agonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.SDS of cas: 74904-29-3

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On June 23, 2021, Fang, Yuying; Chen, Xiucai; Tan, Qingyun; Zhou, Huihao; Xu, Jun; Gu, Qiong published an article.Name: 8-Methoxy-3,4-dihydroisoquinolin-1(2H)-one The title of the article was Inhibiting Ferroptosis through Disrupting the NCOA4-FTH1 Interaction: A New Mechanism of Action. And the article contained the following:

Ferroptosis is an iron-dependent form of oxidative cell death, and the inhibition of ferroptosis is a promising strategy with which to prevent and treat neurol. diseases. Herein we report a new ferroptosis inhibitor 9a(I) with a novel mechanism of action. It is demonstrated that nuclear receptor coactivator 4 (NCOA4), a cargo receptor for ferritinophagy, is the target of 9a. Compound 9a blocks ferroptosis by reducing the amount of bioavailable intracellular ferrous iron through disrupting the NCOA4-FTH1 protein-protein interaction. Further studies indicate that 9a directly binds to recombinant protein NCOA4383-522 and effectively blocks the NCOA4383-522-FTH1 interaction. In a rat model of ischemic stroke, 9a significantly ameliorates the ischemic-refusion injury. With the first ligand 9a, this work reveals that NCOA4 is a promising drug target. Addnl., 9a is the first NCOA4-FTH1 interaction inhibitor. This work paves a new road to the development of ferroptosis inhibitors against neurol. diseases. The experimental process involved the reaction of 8-Methoxy-3,4-dihydroisoquinolin-1(2H)-one(cas: 74904-29-3).Name: 8-Methoxy-3,4-dihydroisoquinolin-1(2H)-one

The Article related to neurol diseases ferroptosis inhibitor ncoa4 fth1 ppi iron ferritin, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Name: 8-Methoxy-3,4-dihydroisoquinolin-1(2H)-one

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On July 14, 2005, Fernandes, Prabhavathi B.; Mailman, Richard Bernard; Nichols, David Earl; Postlethwait, Robert Neil published a patent.Computed Properties of 58142-46-4 The title of the patent was Preparation of dopamine D1 receptor agonists and co-administration with D2 receptor antagonists for treatment of neurological and psychiatric disorders. And the patent contained the following:

Methods for treating a patient having neurol., psychotic, and psychiatric disorders are described comprising the steps of administering to the patient an effective amount of a partial and/or full dopamine D1 receptor agonist, and administering to the patient an effective amount of a dopamine D2 receptor antagonist. Pharmaceutical compositions comprising a dopamine D1 receptor agonist and a dopamine D2 receptor antagonist are also described. The D1 dopamine receptor agonist and the D2 dopamine receptor antagonist can be administered to the patient in the same or in a different composition or compositions The agonist is a compound selected from the group consisting of hexahydrobenzophenanthridines, hexahydrothienophenanthridines, phenylbenzodiazepines, chromenoisoquinolines, naphthoisoquinolines, and their analogs, derivatives and pharmaceutically acceptable salts; the synthesis of such compounds is disclosed. The dopamine D2 receptor antagonist is specifically claimed to be an antipsychotic agent. The pharmaceutical composition further comprise one or more cholinergic agents, cholinergic agonists, acetylcholine mimetics, acetylcholine esterase inhibitors, or combinations thereof. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Computed Properties of 58142-46-4

The Article related to dopamine receptor ligand neurol psychiatric disorder treatment, phenanthridine phenylbenzodiazepine isoquinoline analog preparation neurol disorder treatment, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Computed Properties of 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On June 11, 2021, Gu, Qiong; Xu, Jun; Fang, Yuying published a patent.Electric Literature of 74904-29-3 The title of the patent was Preparation of benzimidazole compounds for ferroptosis inhibitors. And the patent contained the following:

The present invention relates to preparation of (aryl)benzimidazole compounds for ferroptosis inhibitors. In particular, I and II [wherein, R1 is 4-methylpiperazin-1-yl, 4-methyl-1-piperidyl, 1-piperidyl, morpholino; R2 is morpholino, 1,3-benzodioxol-5-yl, 4-pyrimidin-2-ylpiperazin-1-yl, etc.; R is halogen, Me, alkoxy, alkynyloxy or hydroxy; X is C or N] were prepared The benzimidazole compound provided by the invention has better ferroptosis inhibiting activity by introducing a lipophilic group at the R1 position and introducing a specific group at the R2 position, the compound can be used as a lead compound for preventing and treating nervous system diseases such as stroke. The experimental process involved the reaction of 8-Methoxy-3,4-dihydroisoquinolin-1(2H)-one(cas: 74904-29-3).Electric Literature of 74904-29-3

The Article related to benzimidazole compound preparation ferroptosis inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Electric Literature of 74904-29-3

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem