- Microwave-assisted sequential one-pot synthesis of 8-substituted pyrazolo[1,5-a][1,3,5]triazines
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This paper reports a convenient sequential one-pot approach for the synthesis of an array of 14 pyrazolo[1,5-a][1,3,5]triazines, substituted in C8 by halogen (Br), various functions (CN and CO2Et)2 and alkyl or (het)aryl groups. This study conf
- Besson, Thierry,Elie, Jonathan,Fruit, Corinne
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- Adenosine receptor antagonists
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The invention provides a compound shown as a formula (I) and a pharmaceutical composition thereof. The compounds of formula (I) of the present invention are useful as adenosine receptor inhibitors, especially A2A and/or A2B inhibitors, for example, the product can be used for prevention or treatment of diseases associated with A2A and/or A2B activity or expression.
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Paragraph 0125-0126; 0129
(2020/12/15)
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- Chemical Validation of DegS As a Target for the Development of Antibiotics with a Novel Mode of Action
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Despite the availability of hundreds of antibiotic drugs, infectious diseases continue to remain one of the most notorious health issues. In addition, the disparity between the spread of multidrug-resistant pathogens and the development of novel classes of antibiotics exemplify an important unmet medical need that can only be addressed by identifying novel targets. Herein we demonstrate, by the development of the first in vivo active DegS inhibitors based on a pyrazolo[1,5-a]-1,3,5-triazine scaffold, that the serine protease DegS and the cell envelope stress-response pathway σE represent a target for generating antibiotics with a novel mode of action. Moreover, DegS inhibition is synergistic with well-established membrane-perturbing antibiotics, thereby opening promising avenues for rational antibiotic drug design.
- Bongard, Jens,Schmitz, Anna Laura,Wolf, Alex,Zischinsky, Gunther,Pieren, Michel,Schellhorn, Birgit,Bravo-Rodriguez, Kenny,Schillinger, Jasmin,Koch, Uwe,Nussbaumer, Peter,Klebl, Bert,Steinmann, J?rg,Buer, Jan,Sanchez-Garcia, Elsa,Ehrmann, Michael,Kaiser, Markus
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p. 1074 - 1078
(2019/05/07)
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- Pyrazolopyrimidines and related heterocycles as CK2 inhibitors
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The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and have the following general formula:
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Page/Page column 285; 286
(2016/05/02)
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- PYRAZOLO[1,5-A][1,3,5]TRIAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AS CDK INHIBITORS
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The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L1, L2, R1,R2, R3, R4, R6, m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.
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Page/Page column 41
(2016/09/26)
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- FUSED BICYCLIC HETEROAROMATIC DERIVATIVES AS KINASE INHIBITORS
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A series of fused bicyclic heteroaromatic derivatives of formula (I), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, inc
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- Pyrazolopyrimidin CK2 and related heterocyclic compound as an inhibitor
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The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and have the following general formula:
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Paragraph 0552
(2016/10/08)
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- COMPOUNDS WITH ANTIBACTERIAL ACTIVITY AGAINST CLOSTRIDIUM
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The present invention is related to novel compounds of formula (I) having antibacterial activity against Clostridium bacteria, in particular Clostridium perfringens, pharmaceutical compositions comprising these compounds, and chemical processes for prepar
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- COMPOUNDS WITH ANTIBACTERIAL ACTIVITY AGAINST CLOSTRIDIUM
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The present invention is related to novel compounds of formula (I) having antibacterial activity against Clostridium bacteria, in particular Clostridium perfringens, pharmaceutical compositions comprising these compounds, and chemical processes for prepar
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- Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF1) receptor antagonists
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To identify structurally novel CRF1 receptor antagonists, a series of bicyclic core antagonists, pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a] pyrimidines, imidazo[1,2-a]pyrimidines and pyrazolo[1,5-a][1,3,5]triazines were designed, synthesized and evaluated as CRF1 receptor antagonists. Compounds 2-27 showed binding affinity (IC50 = 4.2-418 nM) and antagonist activity (EC50 = 4.0-889 nM). Compound 5 was found to show oral efficacy in an Elevated Plus Maze test in rats. Further chemical modification of them led us to discovery of the tricyclic core antagonists pyrazolo[1,5-a]pyrrolo[3,2-e] pyrimidines. The discovery process of these compounds is presented, as is the study of the structure-activity relationship.
- Saito, Tetsuji,Obitsu, Tetsuo,Minamoto, Chiaki,Sugiura, Tsuneyuki,Matsumura, Naoya,Ueno, Sonoko,Kishi, Akihiro,Katsumata, Seishi,Nakai, Hisao,Toda, Masaaki
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p. 5955 - 5966
(2011/11/04)
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- COMPOUNDS THAT MODULATE EGFR ACTIVITY AND METHODS FOR TREATING OR PREVENTING CONDITIONS THEREWITH
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Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.
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- PHARMACEUTICALLY USEFUL HETEROCYCLE-SUBSTITUTED LACTAMS
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The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, infections, and certain immunological disorders.
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Page/Page column 147
(2011/04/18)
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- COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS
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The invention relates to triazine and pyrimidine derivatives having Formula (1) or (2), and methods for using such compounds. For example, the compounds of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-IR), and/or insulin receptor (InsR) or a combination thereof.
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- Fused heterocyclic compounds useful as kinase modulators
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Compounds having the formula (1), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are usefuil as kinase modulators, including MK2 modulation, wherein one of E and F is a nitrogen atom and the other of E and F is a carbon atom, Z is N or CR3, and R1, R2, R3, X and Y are as defined herein.
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Page/Page column 50
(2010/11/26)
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- PYRAZOLO (1,5A) 1,3,5-TRIAZINES
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Pyrazolo[1,5a]1,3,5-triazines are disclosed which are useful as inhibitors of phosphodiesterase enzymes or intermediate in the production process. Such triazines are of general structure: wherein R1, R2 and R3 are as defined hereinafter, or heterocyclic derivatives thereof. Also disclosed are substituted pyrazole derivatives which are used to prepare the pyrazolo[1,5a]1,3,5-triazines of this invention
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