Category: 16230-24-3

On August 28, 2014, Chen, Wei; Yan, Shunqi; Loury, David J.; Frye, Leah Lynn; Greenwood, Jeremy Robert; Shelley, Mee Yoo; Wang, Longcheng published a patent.Product Details of 16230-24-3 The title of the patent was Preparation of purine compounds as inhibitors of Bruton’s tyrosine kinase. And the patent contained the following:

Disclosed herein are compounds that form covalent bonds with Bruton’s tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk and reversible inhibitors of Btk. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. Title compound I [R1 = (un)substituted heteroalkyl, (C=O)-alkyl, CHO, etc.; R2 = H, halo, CN, NO2, etc.; R3 independently = halo, CN, NO2, OH, etc.; m = 0-2], and their pharmaceutically acceptable solvates, salts, or prodrugs, are prepared Thus, e.g., II was prepared in a multi-step synthesis starting from 2,4-dichloro-5-nitropyrimidine with tert-Bu (3-aminophenyl)carbamate. Compounds of invention were tested Btk in vitro inhibitory activity, e.g., II showed IC50 value of < 100 nM against Btk. The invention compounds are useful for treating autoimmune diseases and cancer. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Product Details of 16230-24-3

The Article related to purine preparation bruton tyrosine kinase inhibitor autoimmune disease cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Product Details of 16230-24-3

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

On December 3, 2021, Wu, Xiaoyun; Li, Qinlan; Guo, Qian; Wan, Shanhe; Li, Zhonghuang; Zhang, Jiajie published a patent.Formula: C9H10N2O The title of the patent was Preparation of dioxopiperidinyl-isoindolyl-alkylamidophenylamino-pyrimidinylaminophenyl piperazinyl-oxopentanamide derivative and application thereof. And the patent contained the following:

The present invention relates to the preparation of dioxopiperidinyl-isoindolyl-alkylamidophenylamino-pyrimidinylaminophenyl piperazinyl-oxopentanamide derivative and application thereof. In particular, the dioxopiperidinyl-isoindolyl-alkylamidophenylamino-pyrimidinylaminophenyl piperazinyl-oxopentanamide derivative I (wherein, L contains at least one of an alkyl group, a carbonyl group, an ether bond or an amine group) were prepared The inventive compound can be used as an EFGR inhibitor, has strong inhibitory activity against the cell line H1975 with high expression of EGFRL858R/T790M, and can effectively inhibit the growth of lung cancer cells, which can be used for preparing drugs for treating, preventing, delaying, assisting in treating or treating diseases related to EGFR activity and drugs for treating tumor diseases. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Formula: C9H10N2O

The Article related to dioxopiperidinyl isoindolyl alkylamidophenylamino piperazinyl oxopentaneamide preparation efgr inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C9H10N2O

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

On March 5, 2020, Krainc, Dimitri; Silverman, Richard B.; Zheng, Jianbin published a patent.SDS of cas: 16230-24-3 The title of the patent was Preparation of pyrrolopyrimidine compounds and uses thereof for modulating glucocerebrosidase activity. And the patent contained the following:

The invention relates to preparation of new small mols. having a pyrrolopyrimidine (I) core structure and the uses thereof for modulating glucocerebrosidase activity. Compounds I wherein m is o-6; R1 is aryl, heteroaryl, etc.; R2 is C1-6 alkyl or pyridinyl, are claimed. The example compound II was prepared via 3-step synthesis (procedure given). Also disclosed are pharmaceutical compositions comprising the small mols. which may be administered in methods of treating diseases or disorders associated with glucocerebrosidase activity, including neurol. diseases and disorders such as Gaucher’s disease and Parkinson’s disease. Compounds I may be utilized to generate activated glucocerebrosidase. The activated glucocerebrosidase can be administered in enzyme replacement therapy and/or utilized in screening assays for new small mols. that bind to the activated glucocerebrosidase and/or modulate the activity of the activated glucocerebrosidase. 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 pyrrolopyrimidine preparation glucocerebrosidase modulator neurodegenerative metabolic disease treatment, 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 April 13, 2016, Yao, Li published a patent.Quality Control of N-(3-Aminophenyl)acrylamide The title of the patent was Preparation of pyrimidine derivatives as EGFR and ALK kinase inhibitors for treatment of cancer. And the patent contained the following:

The present invention discloses compounds represented by formula I [wherein R1 and R2 are selected from H, halogen, cyano, etc.; R3 is selected from H, halogen, substituted or unsubstituted C1-C6 alkyl and C3-C8 cycloalkyl; R are independently selected from H, halo, CN, OH, NH2, etc.; X and Y are independently selected from CH, C-halo, C-CN, N, etc. with the proviso that at least one of X and Y is N; and so on] or their pharmaceutically acceptable salts, enantiomers, diastereomers, tautomers, solvates, polymorphs or prodrugs, and preparation method and pharmaceutical application thereof. For example, compound II was prepared in a multi-step synthesis. The compounds of the present invention have good kinase inhibitory activity, particularly on EGFR and ALK kinases and mutants thereof, and have good prospect in medicine for the treatment of cancer. (assay data given). 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 preparation pyrimidine derivative human egfr alk kinase inhibitors, treatment cancer antitumor, 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 May 21, 2019, Li, Jiarui; Xu, Ruyi; Cao, Qinyuan published a patent.HPLC of Formula: 16230-24-3 The title of the patent was Anti-tumor compound, and its preparation method and application in preparing drug for treating myelocytic leukemia. And the patent contained the following:

The invention relates to N-(3-((5-chloro-2-((4-((4-hydroxypiperidin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide I (named as BY4009) and its pharmaceutically acceptable salts (sulfate, pyrosulfate, etc.). Compound I was prepared starting from 1-(bromomethyl)-4-nitrobenzene, 4-hydroxypiperidine, and 3-nitroaniline by using benzylation, reduction, amidation and amination as the key steps. A pharmaceutical composition comprises the anti-tumor compound or its pharmaceutically acceptable salt, and pharmaceutically acceptable carrier. The pharmaceutical composition has application in preparing drug for treating tumor (myelocytic leukemia) by inhibiting BTK Tyrosine kinase phosphorylation. The anti-tumor compound has new mechanism of action, and is more effective. 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 piperidinyl pyrimidinyl phenyl acrylamide preparation btk treatment myelocytic leukemia, 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 25, 2019, Sun, Xiuli; Chi, Fuyun; Shu, Xiaohong; Ma, Xiaodong; Sun, Fangfang; Mo, Guangquan; Shangguan, Xinghe; Cai, Wei; Wang, Yao; Jiang, Feng; Wang, Yi; Sun, Guozhen published a patent.Electric Literature of 16230-24-3 The title of the patent was Pyrimidothiazole heterocyclic compound, composition, and used for treating lymphocytic leukemia. And the patent contained the following:

A pyrimidothiazole heterocyclic compound I and II having capability of treating tumor diseases by inhibiting JAK3 tyrosine kinase, Burkitt’s lymphoma, follicular lymphoma or chronic lymphocytic leukemia, and diffusing large B-cell lymphoma is provided. In compounds I and II, X is selected from the group consisting of NH or oxygen, and R1 is hydrogen, chlorine, Me, and fluorine or methoxy group;. For instance, the invention compound I (X = O; R1 = H) was prepared via substitution of 2,4-dichloro-thieno[3,2-d]pyrimidine with N-(3-hydroxyphenyl)-2-propenamide followed by substitution with 4-[3-(4-morpholinyl)propoxy]-benzenamine. 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 pyrimidothiazole heterocyclic antitumor leukemia lymphoma jak inhibitor preparation, 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 31, 2017, Ma, Xiaodong; Zhao, Dan; Wang, Luhong; Qu, Menghua; Huang, Shanshan; Wang, Changyuan; Shu, Xiaohong; Liu, Kexin published a patent.Computed Properties of 16230-24-3 The title of the patent was Sulfoamido pyrimidine compound as Bruton tyrosine kinase inhibitor and its preparation. And the patent contained the following:

The invention relates to sulfoamido pyrimidine compound of formula I as Bruton tyrosine kinase inhibitor and its preparation Compounds I, wherein R1 is Cl, F, nitro or trifluoromethyl; R2 is H, Me, methoxy or Cl; X is NH or O; R3 is Me, methoxy, or F; their pharmaceutically acceptable salts, are claimed. The inventive compound can inhibit Bruton tyrosine kinase, so as to treat tumors, especially Burkitts lymphoma, disseminated 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).Computed Properties of 16230-24-3

The Article related to sulfoamido pyrimidine preparation bruton tyrosine kinase inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 16230-24-3

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

On March 8, 2016, Xu, Yong published a patent.Synthetic Route of 16230-24-3 The title of the patent was Synthesis of N-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide. And the patent contained the following:

A method for preparing BTK inhibitor CC-292 of formula I, comprising: (1) reacting 4-(2-methoxyethoxy)aniline with cyanamide to obtain a compound of formula II; (2) reacting compound of formula II with di-Et 2-fluoromalonate to obtain a compound of formula III; (3)reacting III with trifluoromethanesulfonic anhydride to obtain a compound of formula IV; and (4) reacting IV with a compound of formula V to obtain I. Compound I can be used in therapy. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Synthetic Route of 16230-24-3

The Article related to diarylamino fluoropyrimidine derivative preparation btk inhibitor disease therapy, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 16230-24-3

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

On April 7, 2020, Choi, Hwan Geun; Ko, Eun Hwa; Kim, So Yeong; Kang, Seok Yong; Ryu, Hui Yun; Kim, Su Heon published a patent.Recommanded Product: 16230-24-3 The title of the patent was Preparation of pyrido[2,3-d]pyrimidine derivatives, and pharmaceutical compositions comprising them as active ingredients for preventing or treating cancer. And the patent contained the following:

The present invention relates to pyrido[2,3-d]pyrimidine derivatives I [double-dotted line = single bond or double bond; R1 = H, linear or branched alkyl, aryl, etc.; R2 = H, or linear or branched alkoxy; R3 = H or -NH-C(=O)-CH=CH2; n = 0 or 1; A1 = -C(R4)=, -N= or -N(R5)-; R4 = H, halogen or (un)substituted heterocycloalkyl; R5 = H, or linear or branched alkoxyalkyl; A2 = -C(R6)= or -N=; R6 = -NRaRb or -(C=O)NRcRd; Ra, Rb, Rc and Rd = independently H, (un)substituted linear or branched alkyl, etc.], a method for preparing them, and pharmaceutical compositions comprising them as active ingredients for preventing or treating cancer. For example, compound II (preparation given) was subjected to reaction with N1,N1,N2-trimethylethane-1,2-diamine followed by reduction of the nitro group and coupling with acryloyl chloride to provide compound III. The invention compounds exhibit inhibitory activity against various kinases, and in particular, exhibit high inhibitory ability against EGFR (epidermal growth factor receptor) wild type or mutants, and thus they can be usefully used in the treatment of diseases associated with the activity of various kinases, particularly cancers expressing EGFR wild type or EGFR mutation. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Recommanded Product: 16230-24-3

The Article related to pyridopyrimidine derivative preparation kinase egfr inhibitor cancer treatment, 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 April 17, 2020, Xiao, Cheng; Li, Si; Ma, Xiaodong; Chen, Lixue; Zheng, Xu; Wang, Changyuan published a patent.Application In Synthesis of N-(3-Aminophenyl)acrylamide The title of the patent was Azole-substituted pyrimidine derivative, its pharmaceutical composition, and its application in treatment of tumor. And the patent contained the following:

The invention relates to azole-substituted pyrimidine derivative of formula I as Bruton’s tyrosine kinase inhibitor useful in treatment of leukemia and its preparation Compounds I, wherein R1 and R2 are independently H, C1-6 alkyl or C3-8 cycloalkyl; R3 is halo; their stereoisomers, geometry isomers, tautomers, N-oxides, metabolite, hydrates, solvates, pharmaceutical salts, or prodrug, are claimed. Therefore, the inventive compound can be applied in the treatment of tumors, especially chronic lymphocytic leukemia, acute lymphocytic leukemia, chronic myeloid leukemia and acute myeloid leukemia. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application In Synthesis of N-(3-Aminophenyl)acrylamide

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

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