Tag: 200-300

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 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 January 10, 1990, Comte, Marie Therese; Gueremy, Claude; Malleron, Jean Luc; Mignani, Serge; Peyronel, Jean Francois; Truchon, Alain published a patent.Recommanded Product: 58142-46-4 The title of the patent was Preparation and formulation of (aza)naphthalenesultam derivatives as serotoninergic antagonists. And the patent contained the following:

Title compounds I [R1 = 4-(hetero)aryl-substituted 1,2,3,6-tetrahydro-1-pyridyl, 1-piperazinyl, or piperidino; R2, R3 = H, halo, R4 = H; or R2 = R4 = H, R3 = halo, AcNH; or R2 = R3 = H, R4 = halo, all with X = CH; or R2 = R3 = R4 = H, X = N; Z = (un)substituted alkylene; various provisos] were prepared as serotonergic 5-HT2 receptor antagonists (no data). Thus, N-alkylation of 1,8-naphthosultam by Br(CH2)3Cl using NaH in DMF gave the N-(3-chloropropyl) derivative, which reacted with 1-(4-fluorophenyl)piperazine in PhMe containing Et3N to give (piperazinylpropyl)naphthoisothiazole derivative II. Three formulations and 61 syntheses are given. The IC50 of I for displacement of [3H]-ketanserin from 5-HT receptors are said to be generally <25 nM. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Recommanded Product: 58142-46-4

The Article related to naphthalenesultam preparation serotoninergic antagonist, naphthoisothiazole preparation 5ht antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Recommanded Product: 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On September 2, 2005, Yamada, Rintaro; Seto, Minoru published a patent.Related Products of 58142-46-4 The title of the patent was Preparation of isoquinoline derivatives as inhibitors of myosins light chain phosphorylation. And the patent contained the following:

The title compounds I [wherein R1 = H, halo, OH, NH2, or alkoxy; R2 = H, halo, alkyl, etc.; R3 = (un)substituted OH, NH2, or SO2NH2] or salts thereof are prepared as inhibitors of myosins light chain phosphorylation for the treatment of glaucoma, chronic obstructive pulmonary disease, asthma, etc. For example, the compound II•xHCl was prepared II•xHCl inhibited human myosins light chain phosphorylation with IC50 of 0.8 μM. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Related Products of 58142-46-4

The Article related to isoquinoline preparation inhibitor myosin regulatory light chain phosphorylation obstruction, human treatment glaucoma chronic obstructive pulmonary disease asthma, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Related Products of 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On May 14, 2020, Lee, Matthew Randolph; Varano, Anthony Joseph published a patent.Reference of 4-Bromo-5-nitroisoquinoline The title of the patent was Sulfonylisoquinoline derivatives as Rock kinase inhibitors and their preparation. And the patent contained the following:

The invention relates to compounds of formula I as Rho-associated protein kinases (ROCK) inhibitors useful for treatment of cerebral cavernous malformation syndrome and cardiovascular diseases. Compounds of formulas I and II wherein ring X is partially saturated aza-containing heteroaryl; Y is CH or N; m is 0, 1, 2 and 3; each R1 is independently CN, OH, hydroxyalkyl, halo, etc.; R2 is H and halo; R3 is H, halo and C1-3 alkyl; with provisions; and pharmaceutically acceptable salts thereof, are claimed. Example compound III was prepared by sulfonylation of 1-chloroisoquinoline with chlorosulfonic acid; the resulting 1-chloroisoquinoline-5-sulfonyl chloride underwent hydrolysis to give 1-hydroxyisoquinoline-5-sulfonic acid, which underwent chlorination to give the corresponding sulfonyl chloride, which underwent amidation with 4-methylisoindoline to give compound III. Exemplified I were evaluated for selective ROCK kinase inhibitory activity from which III demonstrated IC50 values in the range of >1000 nM and ≤10,000 nM for both ROCK1 and ROCK2 compared to IC50 values of >10,000 for PKACA, AKT1, and PKG, resp. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Reference of 4-Bromo-5-nitroisoquinoline

The Article related to sulfonylisoquinoline derivative preparation rock kinase inhibitor cavernous malformation syndrome, selective rock1 rock2 inhibitor cardiovascular disease, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Reference of 4-Bromo-5-nitroisoquinoline

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On July 31, 1992, Werra, W.; Heber, D. published an article.Product Details of 58142-46-4 The title of the article was 1H and 13C NMR studies of substituted isoquinolinium derivatives in different solvents. And the article contained the following:

1H and 13C NMR data for 1-cyano-, 4-cyano-, 4-bromo- and 4-bromo-5-nitro-substituted isoquinolines, isoquinoline N-oxides and N-methoxy and N-Et salts in different solvents are reported. The substituent chem. shifts are discussed with regard to the reactivity of the N-methoxy compounds in the presence of nucleophilic reagents. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Product Details of 58142-46-4

The Article related to nmr isoquinolinium compound solvent effect, Physical Organic Chemistry: Resonance Spectra (Electron Spin, Nuclear Magnetic and Fourier Transform Nuclear Magnetic, Quadrupole, etc.) and other aspects.Product Details of 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On December 16, 2004, Yamada, Rintaro; Seto, Minoru published a patent.HPLC of Formula: 58142-46-4 The title of the patent was Preparation of diazaphenalene compounds as myosin-control light chains phosphorylation inhibitors. And the patent contained the following:

Title compounds I [R1 = H, chloro, OH; X1···X2 represents CH(R2)-CH(R3), etc.; R2, R3 = H, alkyl; A1, A11, A2, A21 = H, alkyl; Y = CH(A3), etc.; A3 = H, alkyl; Z = OH, etc.] were prepared For example, cyclization of compound II using potassium tert-butoxide followed by deprotection of tert-butoxycarbonyl group with HCl afforded compound III hydrochloride. In myosin regulatory light chains phosphorylation inhibition assays, the IC50 value of compound III·HCl was ≤10 μM. Compounds I are claimed to be useful for the treatment of glaucoma, bronchial asthma, etc. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).HPLC of Formula: 58142-46-4

The Article related to diazaphenalene preparation myosin regulatory light chain phosphorylation inhibitor, antiglaucoma diazaphenalene preparation myosin regulatory light chain phosphorylation inhibition, antiasthmatic diazaphenalene preparation myosin regulatory light chain phosphorylation inhibition and other aspects.HPLC of Formula: 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Ray Choudhury, Abhijnan; Mukherjee, Santanu published an article in 2016, the title of the article was Enantioselective dearomatization of isoquinolines by anion-binding catalysis en route to cyclic α-aminophosphonates.Name: 4-Bromo-5-nitroisoquinoline And the article contains the following content:

An enantioselective dearomatization of isoquinolines has been developed using chiral anion-binding catalysis. This transformation, catalyzed by a simple and easy to prepare tert-leucine-based thiourea derivative, makes use of silyl phosphite as a nucleophile and generates cyclic α-aminophosphonates. This is the first time asym. anion-binding catalysis has been applied to the synthesis of α-aminophosphonates. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Name: 4-Bromo-5-nitroisoquinoline

The Article related to enantioselective dearomatization isoquinoline anion binding catalysis, cyclic alpha aminophosphonate preparation crystal mol structure, tert leucine based thiourea catalyzed silyl phosphite reaction isoquinoline and other aspects.Name: 4-Bromo-5-nitroisoquinoline

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On January 6, 1976, Serban, Alexander published a patent.Category: isoquinoline The title of the patent was 3-Chloro-5-acetamidoisoquinoline as a herbicide. And the patent contained the following:

Isoquinolines I (R = H, halo, NO2, NH2, AcNH, CN; R1 = H, Me, Bu, NO2, NH2, halo, CN, Me) and I.HR2 [R2 = Cl, CF3CO2, Br, iodide, C6Cl5O, 2,4-(O2N)2C6H3O, substituted phenoxy, ClCF2CO2, 2,4-(O2N)2C6H3CO2] (∼110 compounds), which possessed herbicidal, insecticidal, acaricidal, and fungicidal activity, were prepared Isoquinolines were nitrated by H2SO4-KNO3 to give nitro derivatives of I which were reduced to the amino derivatives; Sandmeyer or Schiemann reaction of aminoisoquinolines yielded halo derivatives of I. The title compound was a selective herbicide at 0.25-10 lb/acre against ipomoea, mustard, and sunflower in areas cultivated in wheat, peas, yegrass, or oats. I.HR2 (R = H, 5-Cl, 5-Br, 5-NO2; R1 = H, 1-Me; R2 = Cl, substituted phenoxy) controlled cabbage moth at 0.2% weight/vol and I.HR2 (R = H, 5-NO2; R1 = H, 3-Me; R2 = iodide, CF3CO2) at 1% weight/volume possessed ∼100% effective acaricidal activity against cattle tick nymphs and engorged adults. 4-Bromo-5-nitroisoquinoline possessed fungicidal activity against wheat powdery mildew at 0.008% weight/volume The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Category: isoquinoline

The Article related to isoquinoline nitro insecticide, haloisoquinoline herbicide, nitroalkylisoquinoline acaricide, bromonitroisoquinoline fungicide, chloroacetamidoisoquinoline herbicide, acetamidochloroisoquinoline herbicide and other aspects.Category: isoquinoline

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On July 25, 2002, Nichols, David Earl; Mailman, Richard Bernard; Huang, Xuemei published a patent.SDS of cas: 58142-46-4 The title of the patent was Method using D1 dopamine receptor agonists for treatment of dopamine-related dysfunction. And the patent contained the following:

The invention relates to the treatment of dopamine-related dysfunction using full D1 dopamine receptor agonists in an intermittent dosing protocol with a short, but essential, “”off-period””. The D1 agonist concentration is reduced during the “”off-period”” to obtain a plasma concentration of agonist that suboptimally activates D1 dopamine receptors for a period of time to prevent induction of tolerance. Specifically, the method comprises administering to a patient a full D1 agonist with a half-life of up to about 6 h periodically at a dose resulting in a first plasma concentration of agonist capable of activating D1 dopamine receptors to produce a therapeutic effect. The dose is reduced at least once every 24 h to obtain a second lower plasma concentration of agonist which results in suboptimal activation of D1 dopamine receptors for a period of time sufficient to prevent induction of tolerance. The dopamine D1 agonist is e.g. dinoxyline (preparation described). The methodol. of the invention may be used to treat e.g. Parkinson’s disease. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).SDS of cas: 58142-46-4

The Article related to dopamine related disease treatment d1 agonist tolerance prevention, dinoxyline preparation d1 agonist dopamine disease treatment, parkinson disease dopamine d1 agonist tolerance prevention and other aspects.SDS of cas: 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem