Category: 175357-98-9

On January 4, 2017, Saji, Hideo; Kimura, Hiroyuki; Matsuda, Hirokazu; Nakanishi, Shuichi published a patent.Related Products of 175357-98-9 The title of the patent was Preparation of pyridopyrimidine derivatives as nuclear medicine diagnostic imaging agents. And the patent contained the following:

Provided is a radioactive labeled compound that can detect a secondary mutation of an epidermal growth factor receptor and which is a compound represented by formula I or a pharmaceutically acceptable salt thereof. Compounds of formula I, wherein L1 is an alkanediyl group having 1 to 5 carbon atoms or an alkenediyl carbonyl group having 3 to 8 carbon atoms; R1 is a radioactive halogen atom, or 5- to 7-membered monocyclic nitrogen-containing heterocycloalkyl that may have one substituent, R2 is a 6- to 8-membered aryl group or nitrogen-containing heteroaryl group with one substituent; R1 or R2 contains a radioactive halogen atom or a radioactive carbon atom (11C), and Y is NH or O; are claimed. Example compound II was prepared by a multistep procedure (preparation given). The invention compounds were evaluated for their tyrosine kinase inhibiting activity (some data given). 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 derivative nuclear medicine imaging agent tyrosine kinase inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Related Products of 175357-98-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On August 5, 2021, Heymach, John; Robichaux, Jacqulyne published a patent.Safety of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine The title of the patent was Use of quinazoline-based tyrosine kinase inhibitors for the treatment of cancers with NRG1 fusions. And the patent contained the following:

Provided herein are methods of selecting cancer patients for treatment with quinazoline-based tyrosine kinase inhibitors, either alone or in combination with anti-HER2/HER3 antibodies, as well as methods of treating cancer patients so selected. Cancer patients are selected for treatment if their cancer has an NRG1 fusion. Selected patients are then treated with quinazoline-based tyrosine kinase inhibitors alone or in combination with anti-HER2/HER3 antibodies. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Safety of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

The Article related to tyrosine kinase inhibitor quinazoline her antibody nrg1 fusion cancer, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Safety of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 4, 2017, Saji, Hideo; Kimura, Hiroyuki; Matsuda, Hirokazu; Nakanishi, Shuichi published a patent.Related Products of 175357-98-9 The title of the patent was Preparation of pyridopyrimidine derivatives as nuclear medicine diagnostic imaging agents. And the patent contained the following:

Provided is a radioactive labeled compound that can detect a secondary mutation of an epidermal growth factor receptor and which is a compound represented by formula I or a pharmaceutically acceptable salt thereof. Compounds of formula I, wherein L1 is an alkanediyl group having 1 to 5 carbon atoms or an alkenediyl carbonyl group having 3 to 8 carbon atoms; R1 is a radioactive halogen atom, or 5- to 7-membered monocyclic nitrogen-containing heterocycloalkyl that may have one substituent, R2 is a 6- to 8-membered aryl group or nitrogen-containing heteroaryl group with one substituent; R1 or R2 contains a radioactive halogen atom or a radioactive carbon atom (11C), and Y is NH or O; are claimed. Example compound II was prepared by a multistep procedure (preparation given). The invention compounds were evaluated for their tyrosine kinase inhibiting activity (some data given). 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 derivative nuclear medicine imaging agent tyrosine kinase inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Related Products of 175357-98-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On August 5, 2021, Heymach, John; Robichaux, Jacqulyne published a patent.Safety of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine The title of the patent was Use of quinazoline-based tyrosine kinase inhibitors for the treatment of cancers with NRG1 fusions. And the patent contained the following:

Provided herein are methods of selecting cancer patients for treatment with quinazoline-based tyrosine kinase inhibitors, either alone or in combination with anti-HER2/HER3 antibodies, as well as methods of treating cancer patients so selected. Cancer patients are selected for treatment if their cancer has an NRG1 fusion. Selected patients are then treated with quinazoline-based tyrosine kinase inhibitors alone or in combination with anti-HER2/HER3 antibodies. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Safety of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

The Article related to tyrosine kinase inhibitor quinazoline her antibody nrg1 fusion cancer, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Safety of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On July 24, 1997, Showalter, Howard Daniel Hollis; Winter, Roy Thomas; Rewcastle, Gordon William; Denny, William Alexander published a patent.Application of 175357-98-9 The title of the patent was Improved process for preparing 4,6-disubstituted pyrido[3,4-d]pyrimidines. And the patent contained the following:

The title compounds [I; R = aryl, alkyl, arylalkyl; R1, R2 = H, alkyl, hydroxyalkyl, etc.; R1R2 = 5-6 membered ring] were prepared Thus, reaction of 5-amino-2-fluoropyridine with di-tert-Bu dicarbonate followed by treatment of the resulting 5-[N-(tert-butoxycarbonyl)amino]-2-fluoropyridine with CO2, deprotection of 5-[N-(tert-butoxycarbonyl)amino]-2-fluoropyridine-4-carboxylic acid with CF3CO2H, reaction of 5-amino-2-fluoropyridine-4-carboxylic acid with formamidine acetate, treatment of 6-fluoropyrido[3,4-d]pyrimidin-4(3H)-one with SOCl2, reaction of 4-chloro-6-fluoropyrido[3,4-d]pyrimidine with 3-bromoaniline, and reaction of 4-[(3-bromophenyl)amino]-6-fluoropyrido[3,4-d]pyrimidine with MeNH2 afforded I [R = 3-BrC6H4; R1 = H; R2 = Me]. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Application of 175357-98-9

The Article related to pyridopyrimidine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 175357-98-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 16, 2019, Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Cook, Adam; Fell, Jay Bradford; Fischer, John P.; Marx, Matthew Arnold; Mejia, Macedonio J.; Savechenkov, Pavel; Vigers, Guy P.A.; Smith, Christopher Ronald; Rodriguez, Martha E. published a patent.Electric Literature of 175357-98-9 The title of the patent was 5,6,7,8-Tetrahydropyrido[3,4-d]pyrimidine derivatives as KRas G12C inhibitors and their preparation. And the patent contained the following:

The invention relates to compounds of formula I that inhibit KRas G12C. The invention relates to compounds of formula I that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor. Compounds of formula I wherein L is a bond, CO and C1-3 alkylene; ring X is a 4- to 12-membered (mono/spiro)cyclic or bridged ring; Y is a bond, O, S and NH and derivatives; R1 is (un)substituted alkenoyl, (un)substituted alkynoyl, (un)substituted ethenylsulfonyl, etc.; R2 is H, alkyl, hydroxyalkyl, aryl, etc.; R3 is C1-3 alkyl, oxo, haloalkyl, etc.; R4 is H, cycloalkyl, aryl, etc.; n is 0, 1 and 2; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their KRas G12C inhibitory activity. From the assay, it was determined that compound II exhibited > 25 % inhibition at 5 μM concentration 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 pyridopyrimidine preparation kras g12c inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 175357-98-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 15, 2018, Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Fell, Jay Bradford; Fischer, John P.; Gaudino, John J.; Hicken, Erik James; Hinklin, Ronald Jay; Lee, Matthew Randolf; Marx, Matthew Arnold; Mejia, Macedonio J.; Rodriguez, Martha E.; Savechenkov, Pavel; Tang, Tony P.; Vigers, Guy P.A.; Zecca, Henry J. published a patent.Category: pyrimidines The title of the patent was Preparation of substituted pyrido[3,4-d]pyrimidine compounds as KRas G12C inhibitors. And the patent contained the following:

The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to 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(R)(= or )C(R’)p, or SO2C(R)(= or )C(R’)p; R2 = H, alkyl, hydroxyalkyl, etc.; Z = alkylene; R3 = (independently) alkyl, oxo, or haloalkyl; L = a bond, C(O), or alkylene; R4 = H, cycloalkyl, heterocyclyl, etc.; R5 = (independently) H or alkyl; R = absent, H, or alkyl; R’ = (independently) H, alkyl, alkylaminylalkyl, etc.; p = 0-1; m = 0-2] that irreversibly inhibit the activity of KRas G12C, to pharmaceutical compositions comprising the compounds and methods of use therefor. Over 400 compounds I were prepared E.g., a multi-step synthesis of (2S)-II, starting from (S)-tert-Bu 2-(hydroxymethyl)pyrrolidine-1-carboxylate, was described. Exemplified compounds I were tested in the KRas G12C modification assay, and for inhibition of KRas G12C-dependent cell growth (data given). The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Category: pyrimidines

The Article related to pyridopyrimidine preparation kras g12c inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On October 23, 1997, Bridges, Alexander James; Denny, William Alexander; Dobrusin, Ellen Myra; Doherty, Annette Marian; Fry, David W.; Mcnamara, Dennis Joseph; Showalter, Howard Daniel Hollis; Smaill, Jeffrey B.; Zhou, Hairong published a patent.Reference of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine The title of the patent was Preparation of N-quinazolinylacrylamides and analogs as tyrosine kinase inhibitors. And the patent contained the following:

Title compounds [I; R = (CHR6)pR9; R1R2 = CH:CR7CR8:CH, CH:CR7CR8:N, CH:CR7N:CH, etc.; R6 = H or alkyl; 1 of R7,R8 = Z1Z2R10 and the other = OR4, SR4, NHR3; R3,R4 = (un)substituted alkyl, heterocyclylalkyl, etc.; R9 = (un)substituted Ph; R10 = CR11:CHR5, CCR5, CR11:C:CHR5; R5 = H, halo, alkyl, Ph, etc.; R11 = H, halo, alkyl; Z1 = bond, O, (alkyl)imino, CH2, etc.; Z2 = CO, SO, P(O)(OH), etc.; p = 0 or 1] were prepared Thus, I (R = C6H4Br-3, R1R2 = CH:NCR8:CH, R8 = F) was condensed with 3-morpholinoprpanamine and the product acylated by CH2:CHCOCl to give title compound II. Data for biol. activity of I were given. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Reference of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

The Article related to quinazolinylacrylamide preparation tyrosine kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On October 16, 2002, Bhattacharya, Samit Kumar; Kath, John Charles; Morris, Joel published a patent.Category: pyrimidines The title of the patent was Preparation of substituted bicyclo[]-4-amino-pyridopyrimidine derivatives as kinase inhibitors. And the patent contained the following:

Title compounds I [R1-2 = H, alkyl; R3 = (CR1R2)mR4; m = 0-6 or NR1R3 = (CR1R2)n-indol(in)yl; n = 0-2; X = N and Y is CR9 or X = CR9 and Y = N; R9 = fused-ring bicyclic, bridged bicyclic or spirobicylic group] were prepared For instance, 4-chloro-6-fluoropyrido[3,4-d]pyrimidine (preparation given) was reacted with [3-methyl-4-(pyridin-3-yloxy)phenyl]amine (t-BuOH/ClCH2CH2Cl, reflux, 1 h) and the product coupled to (3-azabicyclo[3.1.0]hex-6-yl)carbamic acid tert-Bu ester (EtOH, sealed tube, 105°, 24 h) and finally deprotected to give II. Selected compounds of the invention had IC50 in the range of 1 nM to 1 pM for erbB-2 receptor kinase. I are used for the treatment of hyperproliferative disorders. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Category: pyrimidines

The Article related to bicyclic amino pyridopyrimidine erbb2 kinase inhibitor preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 28, 2019, Chen, Chen published a patent.Computed Properties of 175357-98-9 The title of the patent was Preparation of cyclic iminopyrimidine derivatives as B-Raf V600E kinase inhibitors. And the patent contained the following:

The invention relates to cyclic iminopyrimidine compounds and their bicyclic derivatives of formula I and their preparation, useful in treating proliferation disorders such as cancer or tumors or for diseases or disorders related to the dysregulation of kinase such as, but not limited to B-Raf V600E kinase. Compounds of formula I are claimed, in which X1, X2, X3, Y1, Y2, and Y3 are each independently N and (un)substituted CH; Z1 is O, S, and (un)substituted NH and CH2; Z2 is bond and NH and derivatives; m = 0-3, n = 1-3; R1-R3 are each independently H, halo, CN, NO2, (un)substituted C1-6 alkyl, etc.; R4 is H and C1-6 alkyl; or pharmaceutically acceptable salts, solvates, or isotopic derivatives thereof. Example compound II was prepared via a multistep process (procedure given). Invention compounds were evaluated for their B-Raf V600E kinase inhibitory activity. From the assay, it was determined that II exhibited growth inhibition of 50% (GI50) at <100 nM. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Computed Properties of 175357-98-9

The Article related to cyclic iminopyrimidine dihydroimidazoquinazoline preparation kinase inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 175357-98-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia