Category: 16230-24-3

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

On April 6, 2016, Fu, Kaiyong; Li, Hua; Zhang, Changjiang published a patent.Category: amides-buliding-blocks The title of the patent was Process for preparation of tyrosine kinase inhibitor Rociletinib. And the patent contained the following:

The invention relates to a method for preparing tyrosine kinase inhibitor Rociletinib, namely N-[3-[[2-[[4-(4-acetyl-1-piperazinyl)-2-p-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-acrylamide, with a total yield of 60-65%. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks

The Article related to preparation tyrosine kinase inhibitor rociletinib, 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 March 9, 2016, Li, Yao; Wei, Yonggang; Zhang, Guobiao; Chen, Lei; Zhang, Xiaobo; Qiu, Guanpeng; Xu, Bo published a patent.HPLC of Formula: 16230-24-3 The title of the patent was Pyrimidine derivative, its preparation method and pharmaceutical application. And the patent contained the following:

The invention disclosed a kind of pyrimidine derivative, its preparation method and pharmaceutical application. The claimed pyrimidine derivative i shown in structure I (M1,M2 = (un)substituted Michael receptor groups; ring D = 6-10 member heterocycle, ring E,A = C6-10 ring, or 4-10 member heterocycle, etc.; ring B,C = (un)substituted 4-7 heterocycle, or not exist; W1,W2 = Nh, O or S; W3,W4 = NH, O, S or not exist). The claimed compound is prepared via multiple steps (procedure given). The obtained compound, its stereoisomer, hydrate, metabolite, solvate, pharmaceutically acceptable salt, eutectic, or prodrug, can be used as EGFR inhibitor for treating or prevention hyperproliferative diseases such as brain tumors, non-small cell lung cancer, squamous cell cancer, bladder cancer, pancreatic cancer, colon cancer, breast cancer, ovarian cancer, cervical cancer, endometrial cancer, colorectal cancer, renal cancer, esophageal adenocarcinoma, esophageal squamous cell carcinoma, solid tumors, Non-Hodgkin’s lymphoma, liver cancer, lung cancer, skin cancer, thyroid cancer, head and neck cancer, prostate cancer, glioma and nasopharyngeal carcinoma. 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 pyrimidine derivative preparation egfr 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 January 4, 2018, Kim, In Woo; Han, Mi Ryeong; Yoo, Jakyung; Oh, Yun Ju; Kim, Ji Duck; Kim, Nam Youn; Jun, Sun Ah; Lee, Jun Hee; Park, Joon Seok published a patent.Electric Literature of 16230-24-3 The title of the patent was Pyrazolopyrimidine derivatives as kinase inhibitor and their preparation. And the patent contained the following:

The invention relates to a pyrazolopyrimidine derivative of formula I, or a pharmaceutically acceptable salt thereof. The compound according to the invention can be usefully used for the prevention or treatment of diseases which are associated with kinase inhibitory actions. Compounds of formula I wherein R1 is (un)substituted C6-10 aryl and (un)substituted C2-10 heteroaryl; R2 is H, C1-4 alkyl and halo; R3 is (un)substituted C1-4 alkyl, (un)substituted C2-6 alkenyl and (un)substituted C2-6 alkynyl; X1 is CR4 and N; R4 is H, C1-4 alkyl and halo; X2 is CR5 and N; R5 is H, C1-4 alkyl, C1-4 alkoxy, halo, etc.; X3 is NH and derivatives, O and S; X4 is CH and N; X5 is a bond and NH; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amination of 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine with tert-Bu (R)-3-aminopiperidin-1-carboxylate followed by Boc-deprotection; the resulting (R)-2-chloro-N-(piperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride underwent N-acylation with acryloyl chloride followed by amination with 4-(4-methylpiperazin-1-yl)aniline to give compound II. The invention compounds were evaluated for their kinase inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of 3.73 nM and 10.7 nM towards JAK3 and BTK, resp. 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 pyrazolopyrimidine preparation kinase inhibitor, 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 May 11, 2018, Zhang, Xiaoqing; Song, Zhichun; Bao, Jinyuan published a patent.Application of 16230-24-3 The title of the patent was Preparation of pyrimidine derivatives useful as IDO inhibitors. And the patent contained the following:

The invention relates to pyrimidine derivatives of formula I, and their pharmaceutically acceptable salts, isomers, racemates, diastereoisomers and pharmaceutical composition thereof, method for their preparation and their use for the treatment of diseases related to indoleamine 2,3-dioxygenase (IDO), specifically in the treatment of tumors, Alzheimer’s disease, depression, cataract, etc. Compounds of formula I, wherein R2 is halo, H, (un)substituted Ph, 4-pyrazolyl, etc.; R is (un)substituted C5-12aryl, C1-6alkyl, NH2, 1-substituted-4-pyrazolyl, etc.; W is 4-fluoroanilino, C1-6alkoxy, cyclopentylamino, 4- to 8-membered heterocycle containing at least one N, and their pharmaceutically acceptable salts, are claimed. Example compound II was prepared via a multistep procedure (procedure given). All the invention compounds were evaluated for their IDO inhibitory activity. From the assay, it was determined that example compound II exhibited 46 % and 26 % inhibition towards IDO1 at 10 μM and 1 μM resp. Pharmacokinetic behaviors of the invented compounds in rats are studied, and the results show that the compound of the present invention has a significant pharmacokinetic absorption effect and a good clin. application prospect. 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 derivative preparation ido 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 January 15, 2015, Hu, Shaojing; Liu, Xiangyong; Bai, Jinlong; Long, Wei published a patent.COA of Formula: C9H10N2O The title of the patent was Preparation of pyrimidines as protein tyrosine kinase modulators. And the patent contained the following:

Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative,and methods of treatment for diseases associated with protein kinase enzymic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed. Compounds I [X = absent, O, S, or NR16; R16 = H or alkyl; Y = halogen, OH, NH2, CN, N3, NO2, or (un)substituted alkyl; Z = O, S, NR20, or CR20R21; and each R20 or R21 independently = H, halogen, (un)substituted alkyl, or alkoxy; R1 = hydroxy, alkyl, haloalkyl, aryl, arylalkyl, etc.; R2 = H, F, or alkyl; or R3 = H, halogen, or a 5 or 6 member heterocyclic ring; R4 = H, alkoxy, alkenyloxy, cycloalkyloxy, halogen, etc.; R5 = H, F, alkyl, haloalkyl, alkoxy, etc.; R6 = H, halo, CN, NO2, cycloalkyl, etc.; R7 = H, halo, alkyl, alkoxy, alkenyloxy, etc.], and their pharmaceutically acceptable salts, are prepared and disclosed. Thus, e.g., II was prepared by. Compound II showed IC50 value of 27.9 nM in ALK assay, 44.3 nM in EGFR (ErB1) L858R assay and 4.08 nM in EGFR (ErbB1) T790M L858R assay. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).COA of Formula: C9H10N2O

The Article related to pyrimidine preparation protein tyrosine kinase, 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

On April 19, 2017, Ma, Xiaodong; Song, Anran; Wang, Luhong; Liu, He; Zhang, Baojing; Wang, Changyuan; Meng, Qiang; Shu, Xiaohong; Zhen, Yuhong; Liu, Kexin published a patent.Category: amides-buliding-blocks The title of the patent was Preparation of distyryl pyrimidine derivatives as antitumor agents. And the patent contained the following:

Title compounds I [wherein X = NH or O; R1 = Cl, F, CF3, or NO2; R2 = H, Me, OMe, or CN; R3 = (R4)n, n is 1 to 4, R4 is H, Me, OMe, OH, F, Cl, or Br], and their pharmaceutically acceptable salts thereof, were prepared as EGFR inhibitors useful as antitumor agents. Thus, the invention compound II was prepared and gave an EGFR inhibition IC50 value of 51.34nmmol. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks

The Article related to distyryl pyrimidine antitumor egfr preparation, 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 May 22, 2020, Ma, Xiaodong; Wang, Changyuan; Sun, Xiuli; Chen, Lixue; Zheng, Xu; Liu, Kexin; Xu, Jiawen; Li, Yanxia; Ai, Min; Chi, Fuyun published a patent.Recommanded Product: N-(3-Aminophenyl)acrylamide The title of the patent was Thiazolopyrimidine heterocyclic compound, composition and use thereof in treatment of lymphocytic leukemia. And the patent contained the following:

The present invention provides a thiazolopyrimidine heterocyclic compound, a composition and use thereof in preparation of drugs for treatment of lymphocytic leukemia. The thiazolopyrimidine heterocyclic compound is specifically a compound as represented in general formula I and II, wherein X is NH or O; R1 is H, Cl, Me, F, or OMe. The present invention further provides a use of the compound as represented in general formula I and II or pharmaceutically acceptable salts thereof or of a pharmaceutical composition containing same in treatment of tumor diseases by means of inhibiting JAK3 tyrosine kinase, in particular in preparation of drugs for treatment of Burkitt’s lymphoma, diffuse 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).Recommanded Product: N-(3-Aminophenyl)acrylamide

The Article related to thiazolopyrimidine heterocyclic preparation antitumor jak lymphoma leukemia, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: N-(3-Aminophenyl)acrylamide

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

On October 22, 2019, Xiang, Hua; Teng, Yu; Zou, Yumei; Lin, Xin; Wang, Xuening; Shen, Hongtao; Cheng, Yu; Ha, Si; Tong, Chao; Wang, Han published a patent.Quality Control of N-(3-Aminophenyl)acrylamide The title of the patent was Preparation of benzopyrimidine compounds useful as Btk or PI3K kinase inhibitors for the treatment of cancer. And the patent contained the following:

The invention relates to benzopyrimidine compounds of formula I and II, method for their preparation and their use as Btk or PI3K kinase inhibitors for the treatment of cancer. Compounds of formula I and II, wherein ring A is (hetero)aryl; R2 is H, C1-3alkyl, C1-3alkoxy, halo, etc.l R3 is H and Me; X is C, O and N; R3 is R4CONH; R4 is C1-4alkyl, C2-4alkeny and C2-4alkynyl; A is (CH2)2-4, and their pharmaceutically acceptable salts, are claimed. Example compound III was prepared via a multistep procedure (procedure given). The above compounds can be used for preparing Btk or PI3K kinase inhibitors to treat or prevent diseases related to protein kinase activity, including tumors, such as leukemias and lymphomas. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Quality Control of N-(3-Aminophenyl)acrylamide

The Article related to benzopyrimidine preparation btk pi3k kinase inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of N-(3-Aminophenyl)acrylamide

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

On April 19, 2017, Ma, Xiaodong; Ge, Yang; Zhang, Jianbin; Liu, He; Huang, Shanshan; Li, Zhen; Wang, Changyuan; Liu, Zhihao; Peng, Jinyong; Liu, Kexin published a patent.Electric Literature of 16230-24-3 The title of the patent was Diphenylamine pyrimidine compounds as BTK and/or JAK3 inhibitors and their preparation. And the patent contained the following:

The invention relates to diphenylamine pyrimidine compounds of formula I as BTK and/or JAK3 inhibitors and their preparation Compounds I, wherein X is H, Cl, F, NO2, or CF3; Y is O or NH; L is COCH2 or CH2CO; R1 is H, Me, OMe, or Cl; R2 is diethylamino, dibutylamino, etc.; their pharmaceutically acceptable salts, are claimed. The invention compounds can be used for treating tumor disease by suppressing Bruton’s tyrosyl protein kinase BTK and/or Janus tyrosine kinase JAK3, especially for the treatment of Burkitt’s lymphoma, diffuse large B cell lymphoid tumor, follicular lymphoma or chronic lymphocytic leukemia. 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 diphenylamine pyrimidine preparation btk jak3 inhibitor treatment cancer, 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