Tag: 100-200

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

On April 5, 2017, Zhang, Yinsheng; Gao, Yong; Wang, Qinglin; Wang, Zhao published a patent.Application of 16230-24-3 The title of the patent was Preparation of deuterated diphenylamino pyrimidine compounds for treating cancer. And the patent contained the following:

The title compound I [wherein R1-R7 and R10-R26 = independently H or D; with the proviso that at least one of them is D; R8 = trifluoromethyl; R9 = H; with exclusions] or pharmaceutically acceptable salts thereof were prepared for treating EGFR related disease, such as cancer. For example, II was prepared in a multi-step synthesis. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to preparation deuteration diphenylaminopyrimidine treatment proliferation human, 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 7, 2016, Chen, Wei; Yan, Shunqi; Loury, David J.; Frye, Leah Lynn; Greenwood, Jeremy Robert; Shelley, Mee Yoo; Wang, Longcheng published a patent.Application In Synthesis of N-(3-Aminophenyl)acrylamide The title of the patent was 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. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds 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. 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 purine preparation bruton tyrosine kinase inhibitor autoimmune disease 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

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 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 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