Tag: 100-200

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 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 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

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