882670-93-1Relevant articles and documents
Synthesis of novel N-aryl-4-[6-(2-fluoropyridin-3-yl)quinazolin-2-yl]-piperazine-1-carboxamide or -carbothioamide derivatives and their antimicrobial activity
Babu, D. Suresh,Srinivasulu, Doddaga,Kotakadi, Venkata S.
, p. 60 - 66 (2015)
A series of novel N-aryl-4-[6-(2-fluoropyridin-3-yl)quinazolin-2-yl]-piperazine-1-carboxamide or -carbothioamide derivatives was synthesized by cyclization of 5-bromo-2-fluorobenzaldehyde and guanidine carbonate in the presence of dimethylacetamide follow
INHIBITOR OF BRUTON'S TYROSINE KINASE
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, (2021/09/24)
Disclosed herein is a compound of Formula (I) with a Btk inhibitory activity, wherein all the variables are as defined herein. The compound can be used for the treatment of diseases such as autoimmune diseases, xenogeneic immune diseases, cancers or thromboembolic diseases. Also disclosed is a pharmaceutical composition comprising a compound of Formula (I). Futher provided is a compound capable of inhibiting the activity of Bruton's tyrosine kinase by covalent binding.
TREATMENT OF FIBROSIS WITH IRE1 SMALL MOLECULE INHIBITORS
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, (2020/11/30)
Provided herein are methods of using IRE1 small molecule inhibitors in combination therapies for treating fibrosis in a subject. The IRE1 small molecule inhibitors described herein may be used in combination therapies for treating fibrosis
COMBINATION THERAPIES WITH IRE1 SMALL MOLECULE INHIBITORS
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, (2020/12/01)
Provided herein are methods of using IRE1 small molecule inhibitors in combination therapies for treating cancer in a subject. The IRE1 small molecule inhibitors described herein may be used in combination therapies for treating solid and hematologic cancers.
IRE1 SMALL MOLECULE INHIBITORS
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, (2019/05/30)
Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
Inhibitor of Bruton tyrosine kinase
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Paragraph 0131-0133, (2019/02/19)
The invention discloses a compound of a formula (I) with Btk inhibiting activity, wherein all variables are as defined in the description. The compound can be used for treating autoimmune diseases, heteroimmune diseases, cancers or thrombembolia. The inve
IRE1 SMALL MOLECULE INHIBITORS
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, (2018/06/22)
Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a
IRE1 SMALL MOLECULE INHIBITORS
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, (2019/01/05)
Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
2-AMINOQUINAZOLINE DERIVATIVES
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Page/Page column 91, (2008/06/13)
2-Aminoquinazoline derivatives represented by the general formula (I) or pharmacologically acceptable salts thereof: (I) wherein R1 and R2 are each independently hydrogen, substituted or unsubstituted lower alkyl, or the like; X is a bond or CR7aR7b (wherein R7a and R7b are each independently hydrogen or the like); when X is a bond, R3 is substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group, while when X is CR7aR7b, R3 is substituted or unsubstituted lower alkoxy, substituted or unsubstituted aryl, or the like; R4 is hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or the like; and R5 is hydrogen, substituted or unsubstituted aryl, or the like.
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: Synthesis, SAR, and in vivo anti-inflammatory activity
DiMauro, Erin F.,Newcomb, John,Nunes, Joseph J.,Bemis, Jean E.,Boucher, Christina,Buchanan, John L.,Buckner, William H.,Cee, Victor J.,Chai, Lilly,Deak, Holly L.,Epstein, Linda F.,Faust, Ted,Gallant, Paul,Geuns-Meyer, Stephanie D.,Gore, Anu,Gu, Yan,Henkle, Brad,Hodous, Brian L.,Hsieh, Faye,Huang, Xin,Kim, Joseph L.,Lee, Josie H.,Martin, Matthew W.,Masse, Craig E.,McGowan, David C.,Metz, Daniela,Mohn, Deanna,Morgenstern, Kurt A.,Oliveira-Dos-Santos, Antonio,Patel, Vinod F.,Powers, David,Rose, Paul E.,Schneider, Stephen,Tomlinson, Susan A.,Tudor, Yan-Yan,Turci, Susan M.,Welcher, Andrew A.,White, Ryan D.,Zhao, Huilin,Zhu, Li,Zhu, Xiaotian
, p. 5671 - 5686 (2007/10/03)
The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and natural killer (NK) cells. Genetic evidence in both mice and humans demonstrates that Lck kinase activity is critical for signaling mediated by the T cell receptor (TCR), which leads to normal T cell development and activation. Selective inhibition of Lck is expected to offer a new therapy for the treatment of T-cell-mediated autoimmune and inflammatory disease. Screening of our kinase-preferred collection identified aminoquinazoline 1 as a potent, nonselective inhibitor of Lck and T cell proliferation. In this report, we describe the synthesis and structure-activity relationships of a series of novel aminoquinazolines possessing in vitro mechanism-based potency. Optimized, orally bioavailable compounds 32 and 47 exhibit anti-inflammatory activity (ED50 of 22 and 11 mg/kg, respectively) in the anti-CD3-induced production of interleukin-2 (IL-2) in mice.