24463-25-0Relevant academic research and scientific papers
DIHYDROQUINOXALINE BROMODOMAIN RECOGNITION PROTEIN INHIBITOR, PREPARATION METHOD AND USE THEREOF
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Paragraph 0152; 0153; 0157; 0248; 0249, (2020/02/14)
The present invention relates to dihydroquinoxaline bromodomain recognition protein inhibitor, preparation method and use thereof. The inhibitor of the present invention is compound represented by general formula (I), or stereoisomer, pharmaceutically acceptable salt, prodrug, solvate, hydrate and crystal form thereof. The definition of each substituent is as described in the description and claims. The compound represented by general formula (I) of the present invention may inhibit bromodomain recognition protein and may be used for preparing medicament which regulates the apparent state of cells and treats series of diseases and symptoms which are mediated by the bromodomain recognition protein.
TRIAZOLOPYRAZINE DERIVATIVES AND THEIR USE FOR TREATING NEUROLOGICAL AND PSYCHIATRIC DISORDERS
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Page/Page column 24; 25, (2013/03/26)
The present invention is directed to triazolopyrazine compounds of Formula (I). Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds as therapeutic agents treating neurological and psychiatric disorders.
Synthesis of substituted 1,3-dimethyl-1H-quinoxalin-2-ones from aniline derivatives
Li, Xun,Wang, Donghua,Wu, Jifeng,Xu, Wenfang
, p. 2741 - 2751 (2007/10/03)
Substituted 1,3-dimethyl-1H-quinoxalin-2-ones (7) have been synthesized through the procedures of acylation, nitration, reduction, intramolecular alkylation, oxidation, and N-methylation starting from 3,4-disubstituted aniline.
Novel approach to 3-methyl-1H-quinoxalin-2-ones
Li, Xun,Wang, Donghua,Wu, Jifeng,Xu, Wenfang
, p. 2553 - 2560 (2007/10/03)
A novel approach to the synthesis of 3-methyl-1H-quinoxalin-2-ones has been described. These compounds were regioselectively prepared by starting from substituted phenylamines and α-chloropropionyl chloride through the efficient procedures of acylation, nitration, reduction, intramolecular alkylation, and oxidation. Copyright Taylor & Francis, Inc.
Benzimidazolones and analogues
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, (2008/06/13)
The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5are independently selected from H or optionally substituted C1to C6alkyl, C2to C6alkenyl, C2to C6alknyl, C3to C8cycloalkyl, substituted C3to C8cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4and R5to from a 5 to 7 membered ring; R1is selected from H, OH, NH2, C1to C6alkyl, substituted C1to C6alkyl, C3to C6alkenyl, substituted C1to C6alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1to C3alkyl), —CO(aryl), —CO(C1to C3alkoxy), or —CO(C1to C3aminoalkyl) groups; R2is selected from H, halogen, CN, NO2, or optionally substituted C1to C6alkyl, C1to C6alkoxy, or C1to C6aminoalkyl groups; R3is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromatic ring containing 1 or 2 substituents; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt thereof. The invention also includes methods of contraception and methods of treating or preventing maladies associated with the progesterone receptor.
Combination therapies using benzimidazolones
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, (2008/06/13)
This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R6are independently selected from H or optionally substituted C1to C6alkyl, C2to C6alkenyl, C2to C6alkynyl, C3to C8cycloalkyl, substituted C3to C8cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4and R5to from a 5 to 7 membered ring; R1is selected from H, OH, NH2, C1to C6alkyl, substituted C1to C6alkyl, C3to C6alkenyl, substituted C1to C6alkenyl, alkynyl, substituted alkynyl, —COH, or optionally substituted —CO(C1to C3alkyl), —CO(aryl), —CO(C1to C3alkoxy), or —CO(C1to C3aminoalkyl) groups; R2is selected from H, halogen, CN, NO2, or optionally substituted C1to C6alkyl C1to C6alkoxy, or C1to C6aminoalkyl groups; R3is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromnatic ring containing 1 or 2 substituents; or a pharmaceutically acceptable salt thereof, in combination with a progestational agent, an estrogen, or both or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate. These combinations may also be used to in methods of contraception, to stimulate food intake or for minimization of side effects or cyclic menstrual bleeding.
