Tag: 200-300

On May 7, 2020, Lee, Matthew Randolph; Varano, Anthony Joseph, Jr. published a patent.Product Details of 58142-46-4 The title of the patent was Sulfonylisoquinolinone derivatives as ROCK kinase inhibitors and their preparation. And the patent contained the following:

The invention relates to compounds of formulas I and II that inhibit ROCK activity. The invention relates to compounds of formulas I and II, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the invention. Compounds of formulas I and II wherein ring X is partially saturated aza-containing heteroaryl; Y is CH and 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; and 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. The invention compounds were evaluated for their ROCK kinase inhibitory activity. From the assay, it was determined that compound III exhibited IC50 value in the range of 1,000 nM to ≤ 10,000 nM. 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 sulfonylisoquinolinone preparation rock kinase inhibitor, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Product Details of 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On May 14, 2021, Lee, Matthew Randolph; Varano, Anthony Joseph; Bobinski, Thomas P. published a patent.Safety of 4-Bromo-5-nitroisoquinoline The title of the patent was Sulfonylisoquinolinone derivatives as ROCK kinase inhibitors and their preparation. And the patent contained the following:

The present invention relates to compounds that inhibit ROCK activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the present invention. Example compound I 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 I. The invention compounds were evaluated for their ROCK kinase inhibitory activity. From the assay, it was determined that compound I exhibited IC50 value in the range of 1,000 nM to ≤ 10,000 nM. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Safety of 4-Bromo-5-nitroisoquinoline

The Article related to sulfonylisoquinolinone preparation rock kinase inhibitor, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Safety of 4-Bromo-5-nitroisoquinoline

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On August 20, 2020, Lee, Matthew Randolph; Varano Jr., Anthony Joseph; Bobinski, Thomas P. published a patent.SDS of cas: 58142-46-4 The title of the patent was Sulfonylisoquinolinone derivatives as ROCK kinase inhibitors and their preparation. And the patent contained the following:

The present invention relates to compounds that inhibit ROCK activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the present invention. Example compound I 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 I. The invention compounds were evaluated for their ROCK kinase inhibitory activity. From the assay, it was determined that compound I exhibited IC50 value in the range of 1,000 nM to ≤ 10,000 nM. 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 sulfonylisoquinolinone preparation rock kinase inhibitor, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.SDS of cas: 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On June 6, 2013, Aebi, Johannes; Amrein, Kurt; Chen, Wenming; Hornsperger, Benoit; Kuhn, Bernd; Liu, Yongfu; Maerki, Hans P.; Mayweg, Alexander V.; Mohr, Peter; Tan, Xuefei; Wang, Zhanguo; Zhou, Mingwei published a patent.Application of 58142-46-4 The title of the patent was New bicyclic dihydroisoquinolin-1-one derivatives as aldosterone synthase inhibitors and their preparation. And the patent contained the following:

The invention provides compounds having formula I, compositions including the compounds and methods of using the compounds as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome. Compounds of formula I wherein E is absent and CR3R4; A1 is CR8 and N; A2 is CR9 and N; A3 is CR10 and N; A4 is CR11 and N; A5 is CR6 and N; R1, R2, R3 and R4 are independently H, alkyl, cycloalkyl, haloalkyl, etc.; R2R4 can be taken together to form a double bond, then R5 is H; R1R2, R3R4 or R1R3 can be taken together to form substituted cycloalkyl and heterocycloalkyl; R5, R6, R7 and R8 are independently halo, CN, alkoxy, hydroxyalkoxy, etc.; R9 is H, halo, OH, CN, alkyl, etc.; R10 is (un)substituted alkoxy and substituted alkyl; R11 is H; and with proviso; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by N-arylation of 6-chloro-3,4-dihydroisoquinolin-1(2H)-one with 3-bromopyridine. The invention compounds were evaluated for their aldosterone synthase inhibitory activity. From the assay, it was determined that compound II exhibited EC50 values of 0.0860 μM and 4.6072 μM towards CYP11B2 and CYP11B1, resp. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Application of 58142-46-4

The Article related to dihydroisoquinolinone preparation aldosterone synthase inhibitor, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application of 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On October 31, 1978, Hamada, Yoshiki; Sugiura, Michiharu; Hirota, Minoru published an article.Related Products of 58142-46-4 The title of the article was Studies on nitrogen-containing heterocyclic compounds. XXXIII. Syntheses of 3-alkoxyisoquinolines and 7-,8-substituted-1,6-naphthyridines from isoquinoline and 1,6-naphthyridine. And the article contained the following:

1,3-Dialkoxy-4-bromo-2-cyano-1,2,3,4-tetrahydroisoquinolines are obtained quant. by the addition of BrCN to isoquinoline dissolved in the corresponding alc., followed by application of Br and saturated sodium carbonate solution These products are a mixture of stereoisomers with the H atoms in 3- and 4-positions in cis (main) and trans configuration. Dehydrobromination of the cis-type compounds with KCN easily gives 3-alkoxyisoquinolines. Hydrolysis with HCl affords 4-bromoisoquinoline from cis-type compounds and 4-chloroisoqinoline from trans-type compounds 4-Bromo-5-nitroisoquinoline was obtained from 5-nitroisoquinoline by the application of the above reaction but 3-methoxy-5-nitroisoquinoline could not be obtained. Application of this reaction to 1,6-naphthyridine easily gave 8-bromo-1,6-naphthyridine and 7-methoxy-1,6-naphthyridine. 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 alkoxy, naphthyridine methoxy, cyanoisoquinoline alkoxy, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Related Products of 58142-46-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

On January 29, 2004, Yamada, Rintaro; Seto, Minoru published a patent.Safety of 4-Bromo-5-nitroisoquinoline The title of the patent was Preparation of 5-substituted isoquinoline derivatives as myosin regulatory light-chain phosphorylation inhibitors. And the patent contained the following:

The title compounds I [wherein R1 = H, halo, OH, NH2, or alkoxy; R2 = H, halo, alkenyl, alkynyl, alkoxy,alkylthio, alkyl-SO, alkylsulfonyl, CN, (un)substituted alkyl, amino, etc.; R3 = (un)substituted OH, SO2NH2, or NH2] or salts thereof are prepared as myosin regulatory light-chain phosphorylation inhibitors. For example, N-(tert-butoxycarbonyl)-1,3-propanediamine was reacted with isoquinoline-5-sulfonyl chloride in CH2Cl2 in the presence of NEt3 to give the sulfonamide. The sulfonamide was reacted with 3-phenyl-1-propanol in THF in the presence of 1,1′-azobis(N,N-dimethylformamide) and Bu3P, followed by hydrolysis to provide II•xHCl. II showed inhibitory activity with IC50 of 0.8 μM against human myosin regulatory light-chain phosphorylation. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Safety of 4-Bromo-5-nitroisoquinoline

The Article related to isoquinoline myosin regulatory light chain phosphorylation inhibitor preparation human, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Safety of 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 June 7, 2022, Tang, Feng; Li, Zhen; Zhang, Guobao; Zhou, Feng; Chen, Ping; Ren, Jinsheng published a patent.Product Details of 58142-46-4 The title of the patent was Preparation of (piperazinyl)tetrahydropyridopyrimidine derivatives and application for treating KRAS G12C mutant tumors. And the patent contained the following:

The present invention relates to the preparation of (piperazinyl)tetrahydropyridopyrimidine derivatives and uses thereof. In particular, (piperazinyl)tetrahydropyridopyrimidine derivatives I (R is -C(R6)=CH(R7), furanyl, -CH(F)(Cl), etc.; Q is selected from C=O or S(=O)2; R1 is selected from heterocyclyl or NR4R5; R2 is selected from aryl or heteroaryl; R3 is selected from hydrogen or NC-CH2; R4 and R5 are independently selected from hydrogen, alkyl, aryl or heteroaryl, alkylacyl, C1-4 alkyloxyacyl, or R4 and R5 together with the nitrogen atom to which they are attached form a heterocyclyl; R6 is selected from hydrogen or fluorine; R7 is selected from hydrogen, halogen, C1-4 alkyl or C1-4 alkoxy, described C1-4 alkyl or C1-4 alkoxy is optionally by =O, halogen, C1-4 alkoxy, etc.; n is selected from 0, 1, 2; m is selected from 1, 2, 3) were prepared The inventive compounds or a pharmaceutically acceptable salts, pharmaceutical compositions are used in preparation of medicaments for preventing and/or treating KRAS G12C mutant tumors. 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 piperazinyl tetrahydropyridopyrimidine preparation antitumor agent, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Product Details of 58142-46-4

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 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