1220886-29-2Relevant academic research and scientific papers
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria
Skepper, Colin K.,Armstrong, Duncan,Balibar, Carl J.,Bauer, Daniel,Bellamacina, Cornelia,Benton, Bret M.,Bussiere, Dirksen,De Pascale, Gianfranco,De Vicente, Javier,Dean, Charles R.,Dhumale, Bhavesh,Fisher, L. Mark,Fuller, John,Fulsunder, Mangesh,Holder, Lauren M.,Hu, Cheng,Kantariya, Bhavin,Lapointe, Guillaume,Leeds, Jennifer A.,Li, Xiaolin,Lu, Peichao,Lvov, Anatoli,Ma, Sylvia,Madhavan, Shravanthi,Malekar, Swapnil,McKenney, David,Mergo, Wosenu,Metzger, Louis,Moser, Heinz E.,Mutnick, Daniel,Noeske, Jonas,Osborne, Colin,Patel, Ashish,Patel, Darshit,Patel, Tushar,Prajapati, Krunal,Prosen, Katherine R.,Reck, Folkert,Richie, Daryl L.,Rico, Alice,Sanderson, Mark R.,Satasia, Shailesh,Sawyer, William S.,Selvarajah, Jogitha,Shah, Nirav,Shanghavi, Kartik,Shu, Wei,Thompson, Katherine V.,Traebert, Martin,Vala, Anand,Vala, Lakhan,Veselkov, Dennis A.,Vo, Jason,Wang, Michael,Widya, Marcella,Williams, Sarah L.,Xu, Yongjin,Yue, Qin,Zang, Richard,Zhou, Bo,Rivkin, Alexey
, p. 7773 - 7816 (2020)
Since their discovery over 5 decades ago, quinolone antibiotics have found enormous success as broad spectrum agents that exert their activity through dual inhibition of bacterial DNA gyrase and topoisomerase IV. Increasing rates of resistance, driven lar
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria
Lapointe, Guillaume,Skepper, Colin K.,Holder, Lauren M.,Armstrong, Duncan,Bellamacina, Cornelia,Blais, Johanne,Bussiere, Dirksen,Bian, Jianwei,Cepura, Cody,Chan, Helen,Dean, Charles R.,De Pascale, Gianfranco,Dhumale, Bhavesh,Fisher, L. Mark,Fulsunder, Mangesh,Kantariya, Bhavin,Kim, Julie,King, Sean,Kossy, Lauren,Kulkarni, Upendra,Lakshman, Jay,Leeds, Jennifer A.,Ling, Xiaolan,Lvov, Anatoli,Ma, Sylvia,Malekar, Swapnil,McKenney, David,Mergo, Wosenu,Metzger, Louis,Mhaske, Keshav,Moser, Heinz E.,Mostafavi, Mina,Namballa, Sunil,Noeske, Jonas,Osborne, Colin,Patel, Ashish,Patel, Darshit,Patel, Tushar,Piechon, Philippe,Polyakov, Valery,Prajapati, Krunal,Prosen, Katherine R.,Reck, Folkert,Richie, Daryl L.,Sanderson, Mark R.,Satasia, Shailesh,Savani, Bhautik,Selvarajah, Jogitha,Sethuraman, Vijay,Shu, Wei,Tashiro, Kyuto,Thompson, Katherine V.,Vaarla, Krishniah,Vala, Lakhan,Veselkov, Dennis A.,Vo, Jason,Vora, Bhavesh,Wagner, Trixie,Wedel, Laura,Williams, Sarah L.,Yendluri, Satya,Yue, Qin,Yifru, Aregahegn,Zhang, Yong,Rivkin, Alexey
supporting information, p. 6329 - 6357 (2021/06/01)
Herein, we describe the discovery and optimization of a novel series that inhibits bacterial DNA gyrase and topoisomerase IV via binding to, and stabilization of, DNA cleavage complexes. Optimization of this series led to the identification of compound 25
QUINAZOLINONES AS PARP14 INHIBITORS
-
Paragraph 0242; 0751; 0752; 0753, (2019/07/10)
The present invention relates to quinazolinones and related compounds which are inhibitors of PARP14 and are useful, for example, in the treatment of cancer and inflammatory diseases.
QUINOLONE DERIVATIVES AS ANTIBACTERIALS
-
Page/Page column 102, (2016/04/20)
This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof, that inhibit bacterial gyrase. The compounds are useful as inhibitors of bacterial gyrase activity and bacterial infections, and have the structure of Formula (I) as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.
Condensed derivatives of imidazole useful as pharmaceuticals
-
Paragraph 0337, (2015/09/23)
The invention relates to the compounds (I) and their acids and bases salts: wherein: the dotted line indicates a double bond; X is N or C-R1 and Y is N or C-R2, X and Y not being simultaneously N; A is selected from the group consisting of phenyl, naphthyl and (5-11) membered monocyclic or bicyclic unsaturated cycle or heterocycle possibly substituted as defined in the application, and A can also comprise either a further (4-7) membered heterocycle, said heterocycle being a monocycle, fused, saturated or unsaturated, the polycyclic system then comprising up to 14 members and up to 5 heteroatoms selected from N, O and S; B is Hydrogen or a substituent as defined in the application, or B is a (4-10) membered mono or bicyclic saturated or unsaturated heterocycle containing 1-3 heteroatoms selected from N, O and S, and possibly substituted as defined in the application; B not being Hydrogen when X is N and Y is C-R2; R1 is Hydrogen or a substituent as defined in the application; B and R1 cannot be simultaneously Hydrogen; R2 is Hydrogen or Halogen; their preparation, their use in the antibacterial prevention and therapy, alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity, and pharmaceutical compositions and associations containing them.
1,4-DISUBSTITUTED PYRIDAZINE DERIVATIVES AND THEIR USE FOR TREATING SMN-DEFICIENCY-RELATED CONDITIONS
-
Page/Page column 42; 43, (2015/02/25)
The present invention provides a compound of formula IA or a pharmaceutically acceptable salt thereof; 5 (IA) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
TRICYCLIC SULFONAMIDE DERIVATIVES
-
Paragraph 1178; 1179, (2015/07/15)
The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of pain.
TRICYCLIC SULFONAMIDE DERIVATIVES
-
Page/Page column 139, (2015/07/16)
The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of pain.
SUBSTITUTED IMIDAZO[4,5-C]QUINOLINE DERIVATIVES AS BROMODOMAIN INHIBITORS
-
Page/Page column 20, (2014/09/03)
The present invention provides novel substituted imidazo[4,5-c]quinoline derivatives of formula (1), which may be therapeutically useful, more particularly as Bromodomain inhibitors; (1) in which Cyi, Cy2, R1, R2/sub
BICYCLIC AROMATIC CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
-
Paragraph 0485; 0486, (2014/07/23)
The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
