65873-73-6Relevant academic research and scientific papers
6 - Oxo -1, 6 - dihydropyridine derivative. Preparation method and application thereof in medicine
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Paragraph 0351-0354; 0358-0360, (2021/11/27)
The invention relates to 6 - oxo -1, 6 - dihydropyridine derivatives, a preparation method and an application thereof in medicine. , The present disclosure relates to I oxo 6 -1 dihydropyridine derivatives represented by the general formula (6 -), a prepa
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against mycobacterium tuberculosis
Hameed P, Shahul,Patil, Vikas,Solapure, Suresh,Sharma, Umender,Madhavapeddi, Prashanti,Raichurkar, Anandkumar,Chinnapattu, Murugan,Manjrekar, Praveena,Shanbhag, Gajanan,Puttur, Jayashree,Shinde, Vikas,Menasinakai, Sreenivasaiah,Rudrapatana, Suresh,Achar, Vijayashree,Awasthy, Disha,Nandishaiah, Radha,Humnabadkar, Vaishali,Ghosh, Anirban,Narayan, Chandan,Ramya,Kaur, Parvinder,Sharma, Sreevalli,Werngren, Jim,Hoffner, Sven,Panduga, Vijender,Kumar, C. N. Naveen,Reddy, Jitendar,Kumar Kn, Mahesh,Ganguly, Samit,Bharath, Sowmya,Bheemarao, Ugarkar,Mukherjee, Kakoli,Arora, Uma,Gaonkar, Sheshagiri,Coulson, Michelle,Waterson, David,Sambandamurthy, Vasan K.,De Sousa, Sunita M.
supporting information, p. 4889 - 4905 (2014/07/07)
DNA gyrase is a clinically validated target for developing drugs against Mycobacterium tuberculosis (Mtb). Despite the promise of fluoroquinolones (FQs) as anti-tuberculosis drugs, the prevalence of pre-existing resistance to FQs is likely to restrict their clinical value. We describe a novel class of N-linked aminopiperidinyl alkyl quinolones and naphthyridones that kills Mtb by inhibiting the DNA gyrase activity. The mechanism of inhibition of DNA gyrase was distinct from the fluoroquinolones, as shown by their ability to inhibit the growth of fluoroquinolone-resistant Mtb. Biochemical studies demonstrated this class to exert its action via single-strand cleavage rather than double-strand cleavage, as seen with fluoroquinolones. The compounds are highly bactericidal against extracellular as well as intracellular Mtb. Lead optimization resulted in the identification of potent compounds with improved oral bioavailability and reduced cardiac ion channel liability. Compounds from this series are efficacious in various murine models of tuberculosis.
HETEROARYL ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS
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Page/Page column 18, (2010/04/25)
Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
TRIAZOLOPYRIDINE COMPOUNDS USEFUL AS KINASE INHIBITORS
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Page/Page column 39-40, (2010/01/12)
A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I), and methods of treating conditions associated with the activity of
IMIDAZOPYRIDINE AND IMIDAZOPYRAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS
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Page/Page column 42; 49-50, (2010/01/12)
A compound of Formula (I) or Formula (II) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) or Formula (II), and methods of treating conditions
ANTHRANILIC ACID AMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE
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Page 42, (2008/06/13)
The present invention relates to new anthranilic acid amide derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof - alone or in combination with one or more
Heterocyclic derivatives for the treatment of diabetes and other diseases
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, (2008/06/13)
The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.
N-substituted heterocycles for the treatment of hypercholesteremia, dyslipidemia and other metabolic disorders; cancer, and other diseases
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, (2008/06/13)
The present invention relates to certain compounds of Formula (I) which can be useful in the treatment of diseases, such as, cancer, metabolic disorders, Type 2 Diabetes, dyslipidemia and/or hyperchloesterolemia:
Oxime derivatives for the treatment of dyslipidemia and hypercholesteremia
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, (2008/06/13)
The present invention relates to compounds of Formula (I) which may be useful in the treatment of diseases, such as, metabolic disorders, dyslipidemia and/or hyperchloesterolemia: 1
3,4-Dihydro-2-phenyl-2H-pyranopyridines. Novel Aza Analogs of Flavans
Bargar, T. M.,Wilson, T.,Daniel, J. K.
, p. 1583 - 1592 (2007/10/02)
Complementary approaches to the synthesis of the title compounds 1 are described.Metallation of 3,5-dibromo-2-methoxypyridine (5b) by bromine/lithium exchange gave selectively the 3-lithio intermediate 6 which was trapped with substituted cinnamaldehydes
