cas 18740-39-1, 2,4-Dichlorothieno[2,3-d]pyrimidine

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Synthesis, Anti-Microbial Activity, and Docking Studies of Novel N-Pyridine Substituted 2-Chlorothieno[2,3-d]pyrimidine Derivatives
Abstract: A series of novel N-pyridine substituted 2-chloro-thieno[2,3-d]pyrimidin-4-amine derivatives has beensynthesized and characterized by 1H and13C NMR spectrometry. All the compounds have beendocked against acetyl-CoA carboxylase enzyme and also tested for their in vitro antimicrobial activity on Gram-positive(Micrococcus luteus, staphylococcusaureus) and Gram-negative bacteria (Salmonella typhi, klebsiella pneumoniae), and anti-fungalactivity on aspergillus niger and fusarium oxysporum. All synthesized compounds havedemonstrated moderate activity, and two products have exhibited goodantibacterial and antifungal activity.
Amperayani, Karteek rao,Parimi, Umadevi,Ummidi, Venkata Ravi Sankar,Vikram, Venugopalarao
p. 2483 - 2488
(2022/01/22)

Design, synthesis, and biological evaluation of novel thienopyrimidine derivatives as PI3Kα inhibitors
Three series of novel thienopyrimidine derivatives 9a-l, 15a-l, and 18a-h were designed and synthesized, and their IC50 values against four cancer cell lines HepG-2, A549, PC-3, and MCF-7 were evaluated. Most compounds show moderate cytotoxicity against the tested cancer cell lines. The most promising compound 9a showed moderate activity with IC50 values of 12.32 ± 0.96, 11.30 ± 1.19, 14.69 ± 1.32, and 9.80 ± 0.93 μM, respectively. The inhibitory activities of compounds 9a and 15a against PI3Kα and mTOR kinase were further evaluated. Compound 9a exhibited PI3Kα kinase inhibitory activity with IC50 of 9.47 ± 0.63 μM. In addition, docking studies of compounds 9a and 15a were also investigated.
Yu, Lide,Wang, Qinqin,Wang, Caolin,Zhang, Binliang,Yang, Zunhua,Fang, Yuanying,Zhu, Wufu,Zheng, Pengwu
(2019/10/02)

Pyrimidine derivatives, preparation method therefor and application of pyrimidine derivatives
The invention belongs to the field of drug synthesis and relates to novel pyrimidine derivatives, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, preparation methods of thenovel pyrimidine derivatives and the pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof and use of the novel pyrimidine derivatives and the pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof in preparation of therapeutic agents, particularly PAK inhibitors. The derivatives disclosed by the invention are represented by a general formula (I) or (II), wherein each substituent is as defined in claims.
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Paragraph 0150; 0151; 0155; 0156; 0159; 0160

(2018/03/26)

Heterocyclic-pyrimindine or pyrazine compound containing biarylamide structure and application thereof
The invention discloses a heterocyclic-pyrimindine or pyrazine compound containing a biarylamide structure. The heterocyclic-pyrimindine or pyrazine compound is as shown in a general formula I or II, wherein the general formula I and the general formula II are shown in the description. The heterocyclic-pyrimindine or pyrazine compound containing the biarylamide structure, and pharmaceutically acceptable salts, hydrates or solvates thereof are used as active components, and are mixed with a pharmaceutically acceptable carrier or excipient to prepare a composition; and the composition is prepared into clinically acceptable preparations. The compound provided by the invention can be used for treating and/or preventing proliferative diseases, and treating and/or preventing prostate cancer, lung cancer and cervical cancer.
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(2017/07/22)

Polyphenol compounds
PROBLEM TO BE SOLVED: To provide a polyphenol compound which has an inhibitory activity for poly(ADP-ribose)glycohydrase (PARG) and is useful as an anticancer agent or the like.SOLUTION: There is provided a polyphenol compound represented by the formula (I) or a pharmaceutically acceptable salt thereof (where, X represents a mono to tri-valent aromatic hydrocarbon group or aromatic heterocyclic group or the like; Y represents -N(R)-, -NHCO- or a bond; Rand Rrepresent a hydrogen atom, an alkyl group or the like; n represents 1, 2 or 3; and m represents an integer of 2 to 5.)
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Paragraph 0144-0145

(2017/08/04)

The structure containing [...] of thienopyrimidines preparation and application
The invention discloses a thienopyrimidine compound containing a chromone hydrazone structure, a geometrical isomer of the compound, pharmaceutically acceptable salts, hydrates, solvates or prodrugs of the compound, as well as application of the compound to preparation of medicines for treating and/or preventing hyperplastic diseases, application of the compound to preparation of medicines for treating and/or preventing cancers and application of the compound to preparation of medicines for treating and/or preventing lung cancers, liver cancers, gastric cancers, colon cancers and breast cancers.
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(2016/11/21)

Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors
Two series of thienopyrimidine derivatives (10a-k, 16a-j) bearing chromone moiety were designed and synthesized. All the compounds were evaluated for inhibitory activity against mTOR kinase at a concentration of 10uM. Four selected compounds were further evaluated for the IC50 values against mTOR kinase, PI3Kα kinase and two cancer cell lines. Some of the target compounds exhibited moderate to excellent mTOR/PI3Kα kinase inhibitory activity and cytotoxicity. The most promising compound 16i showed good inhibitory activity against mTOR/PI3Kα kinase and good antitumor potency for H460 and PC-3 cell lines with IC50 values of 0.16 ± 0.03 μM, 2.35 ± 0.19 μM, 1.20 ± 0.23 μM and 0.85 ± 0.04 μM, which were 8.6, >5, 7.9 and 19.1 times more active than compound I (1.37 ± 0.07 μM, >10 μM, 9.52 ± 0.29 μM, 16.27 ± 0.54 μM), respectively. Structure-activity relationships (SARs) and docking studies indicated that the chromone moiety is necessary for the potent antitumor activity and cytotoxicity of these compounds. Substitution of the chromone moiety at the 6-position has a significant impact to the inhibitory activity, in particular a carboxylic acid group, produced the best potency.
Zhu, Wufu,Chen, Chen,Sun, Chengyu,Xu, Shan,Wu, Chunjiang,Lei, Fei,Xia, Hui,Tu, Qidong,Zheng, Pengwu
p. 64 - 73
(2015/02/19)

ORGANIC COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME
The present invention relates to a novel compound and an organic electroluminescent device comprising the same. According to the present invention, the compound is used in an organic layer of the organic electroluminescent device, desirably a light emitting layer, thereby improving light emitting efficiency, driving voltage, life, etc of the organic electroluminescent device.COPYRIGHT KIPO 2015
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Paragraph 0100-0103

(2016/11/21)

Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)
The AAA-ATPase p97 plays vital roles in mechanisms of protein homeostasis, including ubiquitin-proteasome system (UPS) mediated protein degradation, endoplasmic reticulum-associated degradation (ERAD), and autophagy. Herein we describe our lead optimization efforts focused on in vitro potency, ADME, and pharmaceutical properties that led to the discovery of a potent, ATP-competitive, D2-selective, and orally bioavailable p97 inhibitor 71, CB-5083. Treatment of tumor cells with 71 leads to significant accumulation of markers associated with inhibition of UPS and ERAD functions, which induces irresolvable proteotoxic stress and cell death. In tumor bearing mice, oral administration of 71 causes rapid accumulation of markers of the unfolded protein response (UPR) and subsequently induces apoptosis leading to sustained antitumor activity in in vivo xenograft models of both solid and hematological tumors. 71 has been taken into phase 1 clinical trials in patients with multiple myeloma and solid tumors.
Zhou, Han-Jie,Wang, Jinhai,Yao, Bing,Wong, Steve,Djakovic, Stevan,Kumar, Brajesh,Rice, Julie,Valle, Eduardo,Soriano, Ferdie,Menon, Mary-Kamala,Madriaga, Antonett,Kiss Von Soly, Szerenke,Kumar, Abhinav,Parlati, Francesco,Yakes, F. Michael,Shawver, Laura,Le Moigne, Ronan,Anderson, Daniel J.,Rolfe, Mark,Wustrow, David
p. 9480 - 9497
(2016/01/12)

Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis
Recent clinical studies have demonstrated that dual orexin receptor antagonists (OX1R and OX2R antagonists or DORAs) represent a novel treatment option for insomnia patients. Previously we have disclosed several compounds in the diazepane amide DORA series with excellent potency and both preclinical and clinical sleep efficacy. Additional SAR studies in this series were enabled by the expansion of the acetonitrile-assisted, diphosgene-mediated 2,4-dichloropyrimidine synthesis to novel substrates providing an array of Western heterocycles. These heterocycles were utilized to synthesize analogs in short order with high levels of potency on orexin 1 and orexin 2 receptors as well as in vivo sleep efficacy in the rat.
Roecker, Anthony J.,Mercer, Swati P.,Harrell, C. Meacham,Garson, Susan L.,Fox, Steven V.,Gotter, Anthony L.,Prueksaritanont, Thomayant,Cabalu, Tamara D.,Cui, Donghui,Lemaire, Wei,Winrow, Christopher J.,Renger, John J.,Coleman, Paul J.
p. 2079 - 2085
(2014/05/06)

Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors
G9a is a histone lysine methyltransferase (HKMT) involved in epigenetic regulation via the installation of histone methylation marks. 6,7-Dimethoxyquinazoline analogues, such as BIX-01294, are established as potent, substrate competitive inhibitors of G9a. With an objective to identify novel chemotypes for substrate competitive inhibitors of G9a, we have designed and synthesised a range of heterocyclic scaffolds, and investigated their ability to inhibit G9a. These studies have led to improved understanding of the key pharmacophoric features of BIX-01294 and the identification of a new core quinoline inhibitory scaffold, which retains excellent potency and high selectivity. Molecular docking was carried out to explain the observed in vitro data. This journal is
Srimongkolpithak, Nitipol,Sundriyal, Sandeep,Li, Fengling,Vedadi, Masoud,Fuchter, Matthew J.
p. 1821 - 1828
(2015/01/08)

Identification of the fused bicyclic 4-amino-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors
2-Phenyl-4-piperidinyl-6,7-dihydrothieno[3,4-d]pyrimidine derivative (2) was found to be a new PDE4 inhibitor with moderate PDE4B activity (IC 50 = 150 nM). A number of derivatives with a variety of 4-amino substituents and fused bicyclic pyrim
Goto, Taiji,Shiina, Akiko,Yoshino, Toshiharu,Mizukami, Kiyoshi,Hirahara, Kazuki,Suzuki, Osamu,Sogawa, Yoshitaka,Takahashi, Tomoko,Mikkaichi, Tsuyoshi,Nakao, Naoki,Takahashi, Mizuki,Hasegawa, Masashi,Sasaki, Shigeki
supporting information
p. 3325 - 3328
(2013/06/27)

Rational design of phosphoinositide 3-kinase inhibitors that exhibit selectivity over the phosphoinositide 3-kinase isoform
Of the four class I phosphoinositide 3-kinase (PI3K) isoforms, PI3K has justly received the most attention for its potential in cancer therapy. Herein we report our successful approaches to achieve PI3K vs PI3K selectivity for two chemical series. In the thienopyrimidine series of inhibitors, we propose that select ligands achieve selectivity derived from a hydrogen bonding interaction with Arg770 of PI3K that is not attained with the corresponding Lys777 of PI3K. In the benzoxepin series of inhibitors, the selectivity observed can be rationalized by the difference in electrostatic potential between the two isoforms in a given region rather than any specific interaction.
Heffron, Timothy P.,Wei, Binqing,Olivero, Alan,Staben, Steven T.,Tsui, Vickie,Do, Steven,Dotson, Jennafer,Folkes, Adrian J.,Goldsmith, Paul,Goldsmith, Richard,Gunzner, Janet,Lesnick, John,Lewis, Cristina,Mathieu, Simon,Nonomiya, Jim,Shuttleworth, Stephen,Sutherlin, Daniel P.,Wan, Nan Chi,Wang, Shumei,Wiesmann, Christian,Zhu, Bing-Yan
p. 7815 - 7833
(2012/01/05)

The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes
New dipeptidyl peptidase IV inhibitors were designed based on Alogliptin using a scaffold-hopping strategy. All of the compounds constructed on a thienopyrimidine scaffold demonstrated good inhibition and selectivity for DPP-IV. Compound 10d exhibited subnanomolar (IC50 = 0.33 nM) DPP-IV inhibitory activity, good in vivo efficacy and an acceptable pharmacokinetic profile. A pharmacokinetic-driven optimization of 10d may lead to a new class of clinical candidate DPP-IV inhibitors.
Deng, Jifeng,Peng, Li,Zhang, Guicheng,Lan, Xiaobing,Li, Chufang,Chen, Fuxin,Zhou, Yayao,Lin, Zuoxian,Chen, Ling,Dai, Renke,Xu, Hongjiang,Yang, Ling,Zhang, Xiquan,Hu, Wenhui
experimental part
p. 71 - 76
(2011/02/25)

A convenient synthesis of new 3,7-diphenylthieno[3,2-e]bis[1,2,4] triazolo[4,3-a:4',3'-c]pyrimidine derivatives by oxidative cyclization Using alumina-supported calcium hypochlorite
New 3,7-diphenylthieno[3,2-e]bis[1,2,4]triazolo[4,3-a:4',3'-c]pyrimidine derivatives were easily synthesized at room temperature in good yield by the oxidative cyclization of thienopyrimidinyl hydrazones with alumina-supported calcium hypochlorite (Ca(OCl
Son, Hoon Young,Song, Yang-Heon
scheme or table
p. 2242 - 2246
(2010/11/05)

4-CYANOPHENYLAMINO-SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INHIBITORS
This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula (I) where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.
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Page/Page column 45

(2008/12/05)

THIENO [2,3-D] PYRIMIDINE COMPOUNDS AS INHIBITORS OF ADP-MEDIATED PLATELETS AGGREGATION
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I): wherein A1, A2, A3, A4, A5, A6, A7, A8, X4, X6, R2, R4, R5, and R6 are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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Page/Page column 92

(2008/06/13)

PYRAZOLE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSYNE KINASES
Compounds of formula (I): and their use in the inhibition of Trk activity are described.
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Page/Page column 108-109

(2008/06/13)