18791-99-6Relevant articles and documents
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines
Zhi, Lin,Tegley, Christopher M.,Pio, Barbara,West, Sarah J.,Marschke, Keith B.,Mais, Dale E.,Jones, Todd K.
, p. 415 - 418 (2000)
Synthesis and biological evaluation of 6-thiophene 1,2-dihydro or 1,2,3,4-tetrahydroquinoline derivatives resulted in a number of potent nonsteroidal antiprogestins. (C) 2000 Elsevier Science Ltd. All rights reserved.
2-AMINO-N-(AMINO-OXO-ARYL-LAMBDA6-SULFANYLIDENE)ACETAMIDE COMPOUNDS AND THEIR THERAPEUTIC USE
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Page/Page column 228, (2021/06/26)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(amino-oxo-aryl-λ6- sulfanylidene)acetamide compounds (referred to herein as ANASIA compounds) that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-tRNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.
Four and circular Anaplastic lymphoma kinase inhibitors
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Paragraph 0449; 0450; 0451, (2017/08/25)
The invention belongs to the technical field of medicines, and particularly relates to a four-ring anaplastic lymphoma kinase inhibitor as shown in a general formula (I), or stereisomers, or pharmaceutically acceptable salts, esters or solvates of the inhibitor, wherein A1, A2, A3, M, X, Y, Q, R4, R5, R6, R7 and n are defined in the specification. The invention also relates to a preparation method of these compounds, pharmaceutical preparations and pharmaceutical compositions containing these compounds, and application of the compound or the stereisomers, or the pharmaceutically acceptable salts, esters or solvates of the compound in preparation of medicines for treating and/or preventing ALK-mediated cancer related diseases.
QUINOLINE DERIVATIVES AND THEIR USE FOR TREATING ENDOPLASMIC RETICULUM STRESS-RELATED DISEASES AND DISORDERS
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Paragraph 0926; 0927, (2017/07/01)
Provided herein are quinolines, e.g., a compound of Formula I, pharmaceutical compositions thereof, and methods of their use for treating, preventing, or ameliorating one or more symptoms of an endoplasmic reticulum stress-caused disease. Also provided herein are methods of their use for reducing endoplasmic reticulum stress and modulating the activity of a sarcoplasmic/endoplasmic reticulum Ca2+ ATPase.
Alkali α-MnO2/Na: XMnO2 collaboratively catalyzed ammoxidation-Pinner tandem reaction of aldehydes
Jia, Xiuquan,Ma, Jiping,Wang, Min,Li, Xiaofang,Gao, Jin,Xu, Jie
, p. 7429 - 7436 (2016/10/21)
The tandem reaction is a growing field to yield important advances toward green and sustainable chemistry. Herein, we report a bifunctional manganese oxide catalyst with an interface binding redox phase (α-MnO2) and a basic phase (NaxMnO2). The molar ratio of NaOH/Mn plays a great role in the formation of α-MnO2/NaxMnO2. The sodium cation is essential for the formation of a basic NaxMnO2 phase while the potassium cation promotes the formation of a redox-active α-MnO2 phase. The interface structure of α-MnO2/NaxMnO2 geometrically favors the ammoxidation-Pinner tandem reaction to synthesize imidates in a 58-96% yield from aldehydes. Thus a phase collaborative effect is observed. In the ammoxidation process, the redox cycle of MnIV/MnIII is involved and the lattice oxygen in the α-MnO2 phase acts as an active oxygen species. The O-H in methanol is activated and dissociated on the basic sites of NaxMnO2 to the adsorbed methoxyl species to facilitate the Pinner synthesis. This approach bypasses the conventional synthesis of imidates, which suffer from harsh reaction conditions and the requirement for multiple steps.
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Structure-activity relationship of the aryl region
Probst, Gary D.,Bowers, Simeon,Sealy, Jennifer M.,Stupi, Brian,Dressen, Darren,Jagodzinska, Barbara M.,Aquino, Jose,Gailunas, Andrea,Truong, Anh P.,Tso, Luke,Xu, Ying-Zi,Hom, Roy K.,John, Varghese,Tung, Jay S.,Pleiss, Michael A.,Tucker, John A.,Konradi, Andrei W.,Sham, Hing L.,Jagodzinski, Jacek,Toth, Gergely,Brecht, Eric,Yao, Nanhua,Pan, Hu,Lin, May,Artis, Dean R.,Ruslim, Lany,Bova, Michael P.,Sinha, Sukanto,Yednock, Ted A.,Gauby, Shawn,Zmolek, Wes,Quinn, Kevin P.,Sauer, John-Michael
scheme or table, p. 6034 - 6039 (2010/11/04)
The structure-activity relationship of the prime region of hydroxyethylamine BACE inhibitors is described. Variation in the aryl linker region with 5- and 6-membered heterocycles provided compounds such as 33 with improved permeability and reduced P-gp liability compared to benzyl amine analog 1.
INDOLE SULFONAMIDE MODULATORS OF PROGESTERONE RECEPTORS
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Page/Page column 26, (2008/06/13)
Compounds of Formula (I), wherein n is 1 or 2, and R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein, their preparation, pharmaceutical compositions, and methods of use are disclosed.
Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3- thiophenecarboxamides
Bonafoux, Dominique,Bonar, Sheri,Christine, Lori,Clare, Michael,Donnelly, Ann,Guzova, Julia,Kishore, Nandini,Lennon, Patrick,Libby, Adam,Mathialagan, Sumathy,McGhee, William,Rouw, Sharon,Sommers, Cindy,Tollefson, Michael,Tripp, Catherine,Weier, Richard,Wolfson, Serge,Min, Yao
, p. 2870 - 2875 (2007/10/03)
A series of 21 novel 2-[(aminocarbonyl)amino]-5-acetylenyl-3- thiophenecarboxamides were synthesized and evaluated for the inhibition of IKK-2. In spite of their often modest activity on the enzyme, six selected analogs showed significant inhibition of th
THIENYL COMPOUNDS
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Page/Page column 19, (2008/06/13)
Compounds of formula I : and pharmaceutically-acceptable salts thereof, wherein Ar and R are as defined in the specification, compositions containing such compounds and the use of such compounds and compositions for use in therapy.
Selective cyclooxygenase-2 inhibitors: Heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents
Khanna,Yu,Huff,Weier,Xu,Koszyk,Collins,Cogburn,Isakson,Koboldt,Masferrer,Perkins,Seibert,Veenhuizen,Yuan,Yang,Zhang
, p. 3168 - 3185 (2007/10/03)
A series of heteroaryl modified 1,2-diarylimidazoles has been synthesized and found to be potent and highly selective (1000-9000-fold) inhibitors of the human COX-2.3-Pyridyl derived COX-2 selective inhibitor (25) exhibited excellent activity in acute (carrageenan induced paw edema, ED50 = 5.4 mg/kg) and chronic (adjuvant induced arthritis, ED50 = 0.25 mg/kg) models of inflammation. The relatively long half-life of 25 in rat and dog prompted investigation of the pyridyl and other heteroaromatic systems containing potential metabolic functionalities. A number of substituted pyridyl and thiazole containing compounds (e.g., 44, 46, 54, 76, and 78) demonstrated excellent oral activity in every efficacy model evaluated. Several orally active diarylimidazoles exhibited desirable pharmacokinetics profiles and showed no GI toxicity in the rat up to 100 mg/kg in both acute and chronic models. The paper describes facile and practical syntheses of the targeted diarylimidazoles. The structure-activity relationships and antiinflammatory properties of a series of diarylimidazoles are discussed.