Category: 175357-98-9

On June 30, 2005, Freyne, Eddy Jean Edgard; Willems, Marc; Storck, Pierre Henri; Poncelet, Virginie Sophie; Van Emelen, Kristof; Buijnsters, Peter Jacobus Johannes Antonius; Embrechts, Werner Constant Johan; Perera, Timothy Pietro Suren published a patent.Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine The title of the patent was Pyrido- and pyrimidopyrimidine derivatives as antiproliferative agents. And the patent contained the following:

The present invention concerns pyrido- and pyrimidopyrimidine macrolide derivatives One example compound prepared was I. Reactions are given for preparation of a number of intermediates and other derivatives similar to I. Pharmacol. data include in vitro inhibition of EGF receptors and serum starved proliferation assay on ovarian carcinoma SKOV3 cells. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

The Article related to pyridopyrimidine pyrimidopyrimidine derivative preparation antiproliferative agent, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On November 23, 2017, Fischer, John P.; Fell, Jay Bradford; Blake, James F.; Hinklin, Ronald Jay; Mejia, Macedonio J.; Hicken, Erik James; Chicarelli, Mark Joseph; Gaudino, John J.; Vigers, Guy P.A.; Burgess, Laurence E.; Marx, Matthew Arnold; Christensen, James Gail; Lee, Matthew Randolf; Savechenkov, Pavel; Zecca, Henry J. published a patent.Related Products of 175357-98-9 The title of the patent was Preparation of substituted pyridopyrimidines as KRas G12C inhibitors for treating cancer. And the patent contained the following:

The title compounds I [X = (un)substituted 4-12 membered saturated or partially saturated monocyclic, bridged or spirocyclic ring; Y = a bond, O, S or NR5; R1 = C(O)C(Ra)( or =)C(Rb)p or SO2C(Ra)( or =)C(Rb)p; R2 = H, alkyl, hydroxyalkyl, etc.; R3 = (independently) alkyl, oxo, haloalkyl; L = a bond, C(O), alkylene; R4 = H, cycloalkyl, heterocyclyl, etc.; R5 = (independently) H, alkyl; m = 0-2; Ra = absent, H, alkyl; each Rb = (independently) H, alkyl, alkylaminylalkyl, dialkylaminylalkyl or heterocyclylalkyl; p = 0 or 2] or a pharmaceutically acceptable salts thereof that inhibit KRas G12C, were prepared E.g., a multi-step synthesis of II, starting from tert-Bu 4-chloro-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxylate and benzyl 1-piperazinecarboxylate, was described. Exemplified compounds I were tested for inhibition of KRas G12C activity (data given). In particular, the present invention relates to compounds I that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds I and methods of use therefor. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Related Products of 175357-98-9

The Article related to pyridopyrimidine preparation kras g12c inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 175357-98-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On October 14, 1999, Matsuno, Kenji; Nomoto, Yuji; Ichimura, Michio; Ide, Shin-ichi; Oda, Shoji published a patent.COA of Formula: C7H3ClFN3 The title of the patent was Preparation of nitrogenous heterocyclic compounds for inhibiting phosphorylation of PDGF receptors. And the patent contained the following:

Nitrogenous heterocyclic compounds [I; W = 1,4-piperazinediyl, etc.; U = NR1R2 (wherein R1 = H, (un)substituted alkyl, etc.; R2 = H, etc.), OR4 or SR5 (wherein R4, R5 = (un)substituted alkyl, alicyclic alkyl, heterocyclic, etc.); V = O, S, NR6, or CR7R8 (wherein R6 = R1, cyano, OH, NO2, etc.; R7, R8 = H, cyano, NO2, etc.); at least one of X, Y, and Z = N and the remainder are the same or different and each represents N or CRA (wherein RA = R1, halo, cyano, NO2, etc.); and D1, D2, D3, and D4 each independently = N, O, S, CRB (wherein RB = RA), etc. or any adjacent two of D1-D4 in combination = N, O, S, etc.] or pharmacol. acceptable salts thereof, effective in inhibiting phosphorylation of PDGF receptors and in treating cell proliferation diseases such as arteriosclerosis, vascular reocclusion, cancers, glomerulosclerosis, etc., are prepared CF3CO2H was added to a solution of tert-Bu 4-[(4-phenoxyphenyl)carbamoyl]-1-piperazinecarboxylate in CH2Cl2 with stirring under cooling, the concentrate was dissolved in DMF containing Et3N and the solution was treated with 6-chloropurine under Ar at room temperature to give 71% N-(4-phenoxyphenyl)-4-(6-purinyl)-1-piperazinecarboxamide, which showed IC50 of 0.29 μM against phosphorylation of PDGF receptor. Four addnl. I showed 66-95% inhibition. Tablet, powder and syrup formulations were given. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).COA of Formula: C7H3ClFN3

The Article related to phosphorylation inhibitor pdgf piperazinylquinazoline piperazinylpurine heterocyclylpiperazine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.COA of Formula: C7H3ClFN3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 16, 2010, Smaill, Jeffrey Bruce; Patterson, Adam Vorn; Denny, William Alexander; Wilson, William Robert; Lu, Guo-Liang; Anderson, Robert Forbes; Lee, Ho Huat; Ashoorzaden, Amir published a patent.Electric Literature of 175357-98-9 The title of the patent was Preparation of novel prodrug compounds containing a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger and their use as anti-proliferative agents. And the patent contained the following:

The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a pos. charge. Title compounds I [where X = neg. charged counterion; R1 = group of the formula -(CH2)nTr, wherein Tr = an aromatic nitroheterocycle or aromatic nitrocarbocycle and -(CH2)nTr acts as a reductively-activated fragmenting trigger, and n = 0-6; R2, R3, and R4 independently = aliphatic or aromatic groups of a tertiary amine kinase inhibitor, (R2)(R3)(R4)N; or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor; or one of R2, R3, and R4 may be absent and two of R2, R3, and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor] are claimed. For example, compound II was prepared via alkylation of (2E)-N-[4-(3-bromoanilino)-6-quinazolinyl]-4-(dimethylamino)-2-butenamide with 2-nitrobenzyl bromide. Select I were assayed for their ability to inhibit erbB1 tyrosine kinase and compound II was found to possess an IC50 value of 0.20 nM. The compounds of the invention are useful in treating proliferative diseases such as cancer. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Electric Literature of 175357-98-9

The Article related to alkylammonium bromide derivative preparation kinase inhibitor antiproliferative agent, alkyl ammonium trifluoroacetate derivative preparation kinase inhibitor treatment cancer and other aspects.Electric Literature of 175357-98-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 17, 2005, Edwards, Paul John; Gibson, Karl Richard; Mantell, Simon John; Maw, Graham Nigel; Poinsard, Cedric published a patent.COA of Formula: C7H3ClFN3 The title of the patent was Preparation of azaquinazoline derivatives for treating pain. And the patent contained the following:

The title 6-amino-7-azaquinazolines I [X = a bond, alkylene; R1 = (un)substituted cycloalkyl, cycloalkyl fused to (hetero)cycloalkyl, heterocycloalkyl; R2 = OR4, NR4R5; R4 = alkyl, cycloalkyl, etc.; R5 = H, alkyl, cycloalkyl; or NR4R5 = aziridinyl, azetidinyl, piperidinyl, etc.], useful in the treatment of pain, were prepared and formulated. Thus, reacting cycloheptyl-(6-fluoropyrido[3,4-d]pyrimidin-4-yl)amine (preparation given) with piperidin-4-ol afforded I [X = a bond; R1 = cycloheptyl; R2 = 4-hydroxypiperidin-1-yl]. The exemplified compounds I were tested in mGluR1 assay and were found to have an IC50 of 10 μM or less. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).COA of Formula: C7H3ClFN3

The Article related to azaquinazoline preparation analgesic glutamate receptor metabotropic mglur1 antagonist, azaquinazolinamine preparation analgesic glutamate receptor metabotropic mglur1 antagonist and other aspects.COA of Formula: C7H3ClFN3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On October 29, 2020, Heymach, John; Robichaux, Jacqulyne; Nilsson, Monique; Jones, Philip; Cross, Jason; Theroff, Jay published a patent.Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine The title of the patent was Preparation of pyridopyrimidines as inhibitors of tyrosine kinase for the treatment or prevention of diseases. And the patent contained the following:

The invention relates to preparation of pyridopyrimidines(I) as inhibitors of tyrosine kinase which may be useful as inhibitors of HER2 or EGFR for the treatment or prevention of diseases, including cancer. Compounds I wherein A1 is C(R1)or N; A2 is C(R2)or N; A3 is C(R3)or N; Ar1 is aryl or heteroaryl; R1 is halo, CN, OR6, etc.; R2 is H, alkyl, alkoxy; R3 is H or alkyl; R6 is alkyl, H, C(=O)alkyl, are claimed. The example compound II was prepared via 10-step synthetic procedure using 6-fluoropyridin-3-amine as starting material (procedure given). Compounds I were evaluated for their biol. activity (data given). Compounds I can be used in treatment or prevention of HER2- and EGFR-mediated diseases. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

The Article related to enamide pyridopyrimidine preparation tyrosine kinase inhibitor cancer treatment prophylaxis, pyridopyrimidine preparation mutation her2 egfr inhibitor disease treatment prophylaxis and other aspects.Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On June 11, 2007, Harbottle, Gareth W.; Feeder, Neil; Gibson, Karl R.; Glossop, Mel; Maw, Graham N.; Million, William A.; Morel, Florence F.; Osborne, Simon; Poinsard, Cedric published an article.Application In Synthesis of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine The title of the article was Microwave-assisted synthesis of mGluR1 ligands: carbon, nitrogen, and oxygen linked derivatives of pyrido[3,4-d]pyrimidin-4-ylamines. And the article contained the following:

The syntheses of 6-fluoropyrido[3,4-d]pyrimidin-4-ylamine derivatives is reported herein. Methods for generating C-, N-, and O-linked analogs by subsequent nucleophilic aromatic substitution of fluoride with alcs. or amines under microwave irradiation are described. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Application In Synthesis of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

The Article related to pyridopyrimidinylamine mglur1 ligand preparation, fluoropyridopyrimidinylamine amine nucleophilic aromatic substitution, alc fluoropyridopyrimidinylamine nucleophilic aromatic substitution and other aspects.Application In Synthesis of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 16, 2010, Smaill, Jeffrey Bruce; Patterson, Adam Vorn; Denny, William Alexander; Wilson, William Robert; Lu, Guo-Liang; Anderson, Robert Forbes; Lee, Ho Huat; Ashoorzaden, Amir published a patent.Electric Literature of 175357-98-9 The title of the patent was Preparation of novel prodrug compounds containing a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger and their use as anti-proliferative agents. And the patent contained the following:

The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a pos. charge. Title compounds I [where X = neg. charged counterion; R1 = group of the formula -(CH2)nTr, wherein Tr = an aromatic nitroheterocycle or aromatic nitrocarbocycle and -(CH2)nTr acts as a reductively-activated fragmenting trigger, and n = 0-6; R2, R3, and R4 independently = aliphatic or aromatic groups of a tertiary amine kinase inhibitor, (R2)(R3)(R4)N; or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor; or one of R2, R3, and R4 may be absent and two of R2, R3, and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor] are claimed. For example, compound II was prepared via alkylation of (2E)-N-[4-(3-bromoanilino)-6-quinazolinyl]-4-(dimethylamino)-2-butenamide with 2-nitrobenzyl bromide. Select I were assayed for their ability to inhibit erbB1 tyrosine kinase and compound II was found to possess an IC50 value of 0.20 nM. The compounds of the invention are useful in treating proliferative diseases such as cancer. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Electric Literature of 175357-98-9

The Article related to alkylammonium bromide derivative preparation kinase inhibitor antiproliferative agent, alkyl ammonium trifluoroacetate derivative preparation kinase inhibitor treatment cancer and other aspects.Electric Literature of 175357-98-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 17, 2005, Edwards, Paul John; Gibson, Karl Richard; Mantell, Simon John; Maw, Graham Nigel; Poinsard, Cedric published a patent.COA of Formula: C7H3ClFN3 The title of the patent was Preparation of azaquinazoline derivatives for treating pain. And the patent contained the following:

The title 6-amino-7-azaquinazolines I [X = a bond, alkylene; R1 = (un)substituted cycloalkyl, cycloalkyl fused to (hetero)cycloalkyl, heterocycloalkyl; R2 = OR4, NR4R5; R4 = alkyl, cycloalkyl, etc.; R5 = H, alkyl, cycloalkyl; or NR4R5 = aziridinyl, azetidinyl, piperidinyl, etc.], useful in the treatment of pain, were prepared and formulated. Thus, reacting cycloheptyl-(6-fluoropyrido[3,4-d]pyrimidin-4-yl)amine (preparation given) with piperidin-4-ol afforded I [X = a bond; R1 = cycloheptyl; R2 = 4-hydroxypiperidin-1-yl]. The exemplified compounds I were tested in mGluR1 assay and were found to have an IC50 of 10 μM or less. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).COA of Formula: C7H3ClFN3

The Article related to azaquinazoline preparation analgesic glutamate receptor metabotropic mglur1 antagonist, azaquinazolinamine preparation analgesic glutamate receptor metabotropic mglur1 antagonist and other aspects.COA of Formula: C7H3ClFN3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On October 29, 2020, Heymach, John; Robichaux, Jacqulyne; Nilsson, Monique; Jones, Philip; Cross, Jason; Theroff, Jay published a patent.Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine The title of the patent was Preparation of pyridopyrimidines as inhibitors of tyrosine kinase for the treatment or prevention of diseases. And the patent contained the following:

The invention relates to preparation of pyridopyrimidines(I) as inhibitors of tyrosine kinase which may be useful as inhibitors of HER2 or EGFR for the treatment or prevention of diseases, including cancer. Compounds I wherein A1 is C(R1)or N; A2 is C(R2)or N; A3 is C(R3)or N; Ar1 is aryl or heteroaryl; R1 is halo, CN, OR6, etc.; R2 is H, alkyl, alkoxy; R3 is H or alkyl; R6 is alkyl, H, C(=O)alkyl, are claimed. The example compound II was prepared via 10-step synthetic procedure using 6-fluoropyridin-3-amine as starting material (procedure given). Compounds I were evaluated for their biol. activity (data given). Compounds I can be used in treatment or prevention of HER2- and EGFR-mediated diseases. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

The Article related to enamide pyridopyrimidine preparation tyrosine kinase inhibitor cancer treatment prophylaxis, pyridopyrimidine preparation mutation her2 egfr inhibitor disease treatment prophylaxis and other aspects.Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia