Category: amides-buliding-blocks

On February 22, 2017, Ma, Xiaodong; Yu, Haiqing; Song, Anran; Ge, Yang; Song, Zhendong; Huang, Shanshan; Wang, Changyuan; Liu, Kexin published a patent.SDS of cas: 16230-24-3 The title of the patent was Preparation of purine compounds as BTK tyrosine kinase inhibitors for treating large B cell lymphoma, follicular lymphoma or chronic lymphocytic leukemia. And the patent contained the following:

The invention relates to purine compounds, isomers or pharmaceutically acceptable salts or hydrates with formula of I, wherein R1 is one of H, methoxy, Me, chloro or fluoro; R2 is morpholine, 1-methylpiperazine, 1-ethylpiperazine, etc. The invention compounds can be used for treating diseases caused by BTK tyrosine kinase, especially disseminated anaplastic large B cell lymphoma, follicular lymphoma or chronic lymphocytic leukemia. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).SDS of cas: 16230-24-3

The Article related to purine preparation btk tyrosine kinase inhibitor lymphoma leukemia, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On September 28, 2018, Zhai, Xin; Zhou, Yuhong; Gong, Ping; Jing, Tongfei; Lei, Hongrui; Guo, Ming; Xing, Lingyun published a patent.Electric Literature of 16230-24-3 The title of the patent was Tetrahydropyrido[4,3-d]pyrimidine derivative useful in treatment of ATX and EGFR related diseases and its preparation. And the patent contained the following:

The invention relates to tetrahydropyrido[4,3-d]pyrimidine derivative of formula I useful in treatment of ATX and EGFR related diseases and its preparation Compounds I, wherein L is O(CH2)m, S(CH2)m, NH(CH2) m, etc.; m is 0-4; P is O, S, NH, etc; R1 is C6-10 aryl or 5-10-membered heteroaryl (containing 1-3 heteroatoms selected from N, O and S); R3 is C1-6 alkyl, C2-6 alkenyl, C3-6 alkenyl amino, C6-10 aryl, etc.; their optical stereoisomers, pharmaceutically acceptable salts, solvates, or prodrug, are claimed. The inventive compound shows high inhibitory activity on ATX and EGFR, and can be applied in the drugs for preventing and/or treating the diseases caused by abnormal expression of ATX and EGFR, especially the drugs for preventing and/or treating fibrosis and cancer. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Electric Literature of 16230-24-3

The Article related to tetrahydropyrido pyrimidine preparation treatment atx egfr disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On December 1, 2011, Yang, Shengyong; Wei, Yuquan published a patent.Recommanded Product: 16230-24-3 The title of the patent was (Arylamino)purine derivatives as EGFR and VEGFR inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:

(Arylamino)purine derivatives of formula I and their preparation methods are disclosed. The derivatives of formula I have inhibitory effects on non-small cell lung cancer with deletion mutation of exon 19 or L858R point mutation of exon 21 in epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR). Compounds of formula I wherein R1 is H, C0-4 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-8 alkyl, C1-8 alkyl-C3-7 cycloalkyl, 3- to 8-membered heterocycloalkyl, 3- to 8-membered heterocycloalkylamino and 6- to 8-membered (hetero)aryl; R2 is H, NH2, OH, F, Cl, Br, CF3, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylamino, 6- to 12-membered aryloxy and 6- to 12-membered arylamino; R3 is C3-7 cycloalkyl, C1-8 alkyl-C3-7 cycloalkyl and 6- to 80-membered (hetero)aryl; R4-R8 are independently H, F, Cl, Br, CF3, C1-8 alkoxy, C0-4 dioxaalkylene, (1-methyl-4-piperidinyl)aminocarbonyl, (1-methyl-4-piperazinyl)aminocarbonyl, etc.; are claimed. Example compound I (R1 = Pr-i, R2 = R5 = R6 = R7 = R8 = H, R3 = 4-bromphenyl and R4 = 4-methyl-1-piperazinyl) was prepared via cyclocondensation of 5-amino-4-(isopropylamino)-2-[4-(4-methylpiperazin-1-yl)phenyl]aminopyrimidine with 4-bromophenyl isothiocyanate. All the invention compounds were evaluated for their EGFR and VEGFR inhibitory activity. From the assay, it was determined that example compound I exhibited the IC50 values of 0.001 and 0.004 μM against RGFR-L858R and VEGFR2, resp. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Recommanded Product: 16230-24-3

The Article related to arylamino purine preparation egfr vegfr inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On June 19, 2014, Ahmed, Mahbub; Ashall-Kelly, Alexander; Gueritz, Louisa; McKenna, Jeffrey; McKenna, Joseph; Mutton, Simon; Parmar, Rakesh; Shepherd, Jon; Wright, Paul published a patent.Recommanded Product: 5455-98-1 The title of the patent was Azacycloalkanopyrrolopyrimidinedione derivatives as CFTR modulators and their preparation. And the patent contained the following:

The invention provides a compound of formula I or a pharmaceutically acceptable salt thereof;a nd its therapeutic uses. The invention further provides a combination of pharmacol. active agents and a pharmaceutical composition Compounds of formula I wherein A is (CHR4)n; R1 is (un)substituted Ph, (un)substituted C4-7 cycloalkenyl and (un)substituted 5- to 6- membered heteroaryl; R2 is (un)substituted C1-6 alkyl, (un)substituted C3-7 cycloalkyl, (un)substituted C4-7 cycloalkenyl, etc.; R3 is Me and Et; when X is S, then Z is CHR4a and n is 1; when X is CHR4b, then Z is NR5 and N is 1 and 2; when Z is CHR4b, then Z is CHR4a and n is 0, 1 and 2; when X is C=CH2, CF2 and C(CH3)2, then Z is CHR4a and n is 0 and 1; R4 is H, C1-4 alkyl,C1-4 haloalkyl, Ph, etc.; R4a is H, C1-4 alkyl, C1-4 hydroxyalkyl, etc.; R4b is H and Me; R5 is H and C1-4 alkyl, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cyclization of 6-(2-mercaptoethyl)-1,3-dimethyl-5-phenyl-1,6-dihydropyrrolo[3,4-d]pyrimidine-2,4-dione with 5-methylfuran-2-carboxaldehyde. The invention compounds were evaluated for their CFTR modulatory activity (some data given). The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Recommanded Product: 5455-98-1

The Article related to azacycloalkanopyrrolopyrimidinedione preparation cftr modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 5455-98-1

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On March 16, 2016, Lu, Xianping; Yu, Jindi; Yang, Qianjiao; Li, Zhibin; Pan, Desi; Shan, Song; Zhu, Jiangfei; Wang, Xianghui; Liu, Xiangheng; Ning, Zhiqiang published a patent.Safety of N-(3-Aminophenyl)acrylamide The title of the patent was Preparation of pyrimidine derivatives and their application as the inhibitor of JAK. And the patent contained the following:

The invention is related to the preparation of pyrimidine derivatives I and their application as the inhibitor of JAK. The invention compounds I, wherein X is halogen; R1 is H, cyano, halogen, etc.; R2 is H or halo; R3 is C1-6 alkyl or substituted alkyl; n is integer of 1-7; p is integer of 1-3; A is C6-10 aryl or C5-10 heteroaryl; and their pharmaceutically acceptable salts are claimed. Compound I was prepared by multi-step procedure (procedure given). The pyrimidine derivatives I or pharmaceutically acceptable salts have JAK kinase inhibitory activity, especially have selectivity and high inhibitory activity on JAK3 kinase, and can be used for preparing JAK3 kinase inhibitors as well as medicines for prevention or treatment of diseases related to JAK3 kinase activity abnormity, so as to prevent or treat diseases related to JAK3 kinase activity abnormity. From assay, it was determined that I exhibited the IC50 value of 0.65-1.22 uM against JAK1. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Safety of N-(3-Aminophenyl)acrylamide

The Article related to preparation pyrimidine derivative application inhibitor jak, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of N-(3-Aminophenyl)acrylamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On July 31, 2020, Haggam, Reda A.; Soylem, Essam. A.; Assy, Mohamed. G.; Arastiedy, Marium. F. published an article.Category: amides-buliding-blocks The title of the article was Synthesis and antimicrobial evaluation of new series of quinazolin-5-one derivatives. And the article contained the following:

A new series of quinazolinone derivatives, e.g., I, were synthesized starting with anthranilic acid and cinnamoylisothiocyanate in high yields 55-99%. The study of the biol. activity of all the novel compounds is reported. The minimal inhibitory concentration of some quinazolin-5-one derivatives, e.g., I, showed potential activity against both Gram (+ve) and Gram (-ve) microorganisms more than the reference cefotaxime. In addition, some derivatives of quinazolin-5-one, e.g., I, can be considered as antifungal agents comparing with the standard drug nystatin. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Category: amides-buliding-blocks

The Article related to quinazolinone preparation antibacterial antifungal activity, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On July 27, 2018, Zhang, Yinsheng; Ren, Jing; Gao, Yong; Zhao, Damin; Zhou, Yu; Wang, Qinglin published a patent.Reference of N-(3-Aminophenyl)acrylamide The title of the patent was Bruton’s tyrosine kinase (BTK) inhibitor for preparing drugs for preventing or treating BTK-mediated diseases. And the patent contained the following:

The inhibitor has the structural formula I, wherein R1 includes hydrogen, halogen, etc.; R2 includes hydrogen, hydroxyl, etc., L includes imino, oxygen, etc.. The inhibitor includes N-(3-((2-((1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide, N-(3-((2-((2-hydroxy-2,3-dihydrobenzo[d][1,2]oxaborol-6-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide, etc., or its pharmaceutically acceptable salts. A pharmaceutical composition comprises the inhibitor and its pharmaceutically acceptable salts, and is used in preparing drugs for preventing or treating BTK-mediated diseases. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Reference of N-(3-Aminophenyl)acrylamide

The Article related to acrylamide preparation bruton tyrosine kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of N-(3-Aminophenyl)acrylamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On April 13, 2016, Lu, Xianping; Yu, Jindi; Yang, Qianjiao; Li, Zhibin; Pan, Desi; Shan, Song; Zhu, Jiangfei; Wang, Xianghui; Liu, Xiangheng; Ning, Zhiqiang published a patent.HPLC of Formula: 16230-24-3 The title of the patent was Preparation of pyrimidine derivatives as JAK inhibitors. And the patent contained the following:

The title pyrimidine derivatives shown in formula I [wherein, R1 is H, halogen, etc.; R2 is H, hydroxy, carboxyl, etc.; R3 is selected from H, halogen, cyano, etc.; R4 is H, C1-6 alkyl, etc.; X is NH or O] or pharmaceutically acceptable salts thereof were prepared as JAK inhibitors, and especially showed selective high inhibitory activity on JAK3. For example, compound II was prepared in a multi-step synthesis. The title pyrimidine derivatives can be used in preparing the drugs for preventing and treating the diseases related to JAK3 activity abnormality, e.g., autoimmune diseases, inflammation, cancer, proliferative diseases, bone resorption disease, organ transplant rejection, rheumatoid arthritis, Crohn’s disease, systemic lupus erythematosus, multiple sclerosis, type I diabetes, psoriasis, allergic diseases, asthma, chronic obstructive pulmonary disease, leukemia or lymphoma. (assay data given). The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).HPLC of Formula: 16230-24-3

The Article related to preparation pyrimidine derivative human jak inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On August 13, 2015, Zhang, Dawei published a patent.Application of 16230-24-3 The title of the patent was Substituted pyrimidines useful as EGFR-T790M kinase inhibitors and their preparation. And the patent contained the following:

The invention is directed to pyrimidines of formula I, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases and/or mutants mediated diseases and conditions. Compounds of formula I wherein R1 is H, C1-6 alkoxy, F, Cl and CF3; R2 is C1-6 alkyl and acyl; with provisions; and pharmaceutically acceptable salts, solvates, prodrugs, stereoisomers, tautomers and metabolites thereof, are claimed. Example compound II was prepared by amination of 2,4-dichloro-5-(trifluoromethyl)pyrimidine with 1-(4-(4-aminophenyl)piperazin-1-yl)ethanone; the resulting 1-[4-[4-[[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone underwent amination with N-(3-aminophenyl) prop-2-enamide to give compound II. The invention compounds were evaluated for their EGFR-T790M kinase inhibitory activity. From the assay, it was determined that compound II exhibited Kd value of 0.54 nM. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to pyrimidine preparation egfr t790m kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On September 1, 2016, Tao, Chunlin; Polat, Tulay; Weingarten, Paul; Nallan, Laxman; Arp, Forrest; Wang, Qinwei; Ho, David published a patent.COA of Formula: C9H10N2O The title of the patent was Preparation of pyrimidine derivatives as kinase inhibitors and their therapeutic applications. And the patent contained the following:

The invention provides kinase inhibitors of formula I comprising substituted pyrimidine derivatives and pharmaceutically-acceptable formulations thereof, novel methods for making I as well as the use of I for treatment of proliferative disorders such as cancer. I [wherein W is selected from F, Cl, Br, I, CN, C1-C4 alkyl, C1-C6 alkoxy, etc.; Ar represents (un)substituted heteroaryl or (un)substituted aryl; R5 and R6 are independently selected from H, F, Cl, Br, CN, C1-C4 alkyl, C1-C6 alkoxy; R7, R8, and R9 are independently selected from H, C1-C4 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C10 (hetero)aryl, etc.] or pharmaceutically acceptable salts thereof, are claimed and exemplified. Reaction of 4-((3S,5R)-3,5-dimethylpiperazin-1-yl)aniline with 4-chloro-6-((4,7-difluoro-2-methyl-1H-indol-5-yl)oxy)pyrimidine-5-carbonitrile provided (3S,5R)-II in 95% yield. II was evaluated for inhibitory activity against a panel of fibroblast growth factor receptor (FGFR) kinases demonstrating IC50 values of 11.4 nM, 17.6 nM, 32.6 nM, and 92.1 nM for FGFR1, FGFR2, FGFR3, and FGFR4, resp. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).COA of Formula: C9H10N2O

The Article related to pyrimidine derivative preparation kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C9H10N2O

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics