- ANTI-BACTERIAL HETEROCYCLIC COMPOUNDS AND THEIR SYNTHESIS
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The compounds of Formula I and Formula (B) are described herein along with their stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms, and pharmaceutically active
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Paragraph 000170; 000178
(2019/06/17)
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- Macrocyclic derivative of pyrazole[3,4-d]pyrimidin-3-one and pharmaceutical composition and application thereof
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The present invention relates to a macrocyclic derivative of pyrazole[3,4-d]pyrimidin-3-one as shown in the formula (I) and/or a pharmaceutically acceptable salt thereof, and a composition of a compound of the formula (I) and/or a pharmaceutically acceptable salt thereof, a preparation method thereof, application thereof as a Wee1 inhibitor and application thereof as a sensitizer for cancer chemotherapy or radiotherapy. The macrocyclic derivative of pyrazole[3,4-d]pyrimidin-3-one can effectively inhibit Wee1 and related signaling pathways, and has good cancer treatment and/or relieving effect.The formula is shown in the description.
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Paragraph 0332; 0362; 0363; 0364
(2018/10/19)
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- HETEROCYCLIC COMPOUNDS USEFUL AS ANTI-BACTERIAL AGENTS AND METHOD FOR PRODUCTION
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The present disclosure relates to compounds of Formula I, its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms thereof and pharmaceutical compositions containing them as the active ingredient which can be used as medicaments. The aforementioned substances can also be used in the manufacture of medicaments for treatment, prevention or suppression of diseases, and conditions mediated by microbes. The present disclosure also relates to the synthesis.and characterization of aforementioned substances.
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Paragraph 000133
(2017/12/15)
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- BRIDGED COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Novel bridged compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
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Page/Page column 0075; 0077
(2016/08/23)
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- Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents
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Bacterial resistance is eroding the clinical utility of existing antibiotics necessitating the discovery of new agents. Bacterial type II topoisomerase is a clinically validated, highly effective, and proven drug target. This target is amenable to inhibit
- Singh, Sheo B.,Kaelin, David E.,Wu, Jin,Miesel, Lynn,Tan, Christopher M.,Meinke, Peter T.,Olsen, David,Lagrutta, Armando,Bradley, Prudence,Lu, Jun,Patel, Sangita,Rickert, Keith W.,Smith, Robert F.,Soisson, Stephen,Wei, Changqing,Fukuda, Hideyuki,Kishii, Ryuta,Takei, Masaya,Fukuda, Yasumichi
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supporting information
p. 609 - 614
(2014/06/09)
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- Short and efficient synthesis of oxazinone-and thiazinone-containing bicyclic heteroaromatic aldehydes
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Short and efficient route for the synthesis of oxazinone-and thiazinone-containing bicyclic heteroaromatic aldehydes, which involves the key step of palladium-catalyzed reductive carbonylation, is described. Overall routes for the synthesis of these aldehydes are short, versatile, and scalable with good yields of the product. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications for the following free supplemental resource(s): Full experimental and spectral details.]
- Hameed P., Shahul,Shanbhag, Gajanan,Shinde, Vikas,Chinnapattu, Murugan,Manjrekar, Praveena,Puttur, Jayashree,Patil, Vikas,Ugarkar, Bheemarao
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supporting information
p. 3315 - 3321
(2013/10/01)
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- BRIDGED BICYCLIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
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Page/Page column 79
(2013/03/26)
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- RING-FUSED MORPHOLINE DERIVATIVE HAVING PI3K-INHIBITING ACTIVITY
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The present invention provides compounds or a pharmaceutically acceptable salt thereof which inhibit the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and are therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused morpholine compound shown in the present specification, or a pharmaceutically acceptable salt thereof.
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Page/Page column 35
(2011/07/30)
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- The design of efficient and selective routes to pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes
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This Letter describes the synthesis of challenging pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes. The six different routes described are high yielding, contain no major purification issues and have been used to give gram quantities of each aldehyde.
- Brooks, Gerald,Dabbs, Steven,Davies, David T.,Hennessy, Alan J.,Jones, Graham E.,Markwell, Roger E.,Miles, Timothy J.,Owston, Nathan A.,Pearson, Neil D.,Peng, Tony W.
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scheme or table
p. 5035 - 5037
(2011/01/04)
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- Antibacterial Agents
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Naphthalene, quinoline, quinoaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 10-11; 12
(2008/12/07)
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- ANTIBACTERIAL AGENTS
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Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 35
(2010/11/25)
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- ANTIBACTERIAL AGENTS
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2H-chromen-2-one derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 30
(2008/06/13)
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- ANTIBACTERIAL AGENTS
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Naphthyridine and related derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 22
(2008/06/13)
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- ANTIBACTERIAL AGENTS
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Naphthyridine and related derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 23
(2008/06/13)
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- ANTIBACTERIAL AGENTS
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Naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 25
(2008/06/13)
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- ANTIBACTERIAL AGENTS
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Naphthyridine and quinoline derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 22
(2008/06/13)
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- ANTIBACTERIAL AGENTS
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Naphthyridine and related derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 23
(2008/06/13)
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- ANTIBACTERIAL AGENTS
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Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 93; 97; 100-101
(2010/02/15)
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- ANTIBACTERIAL AGENTS
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Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 44-45
(2010/10/19)
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- ANTIBACTERIAL AGENTS
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Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 24-25
(2010/10/20)
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- ANTIBACTERIAL AGENTS
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Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 23
(2010/10/20)
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- ANTIBACTERIAL AGENTS
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Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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Page/Page column 34; 37
(2010/10/20)
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- Bicyclic pyrazole compounds as antibacterial agents
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Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.
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Page/Page column 25
(2010/11/24)
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- COMPOUNDS
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Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
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Page/Page column 40
(2008/06/13)
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- ANTIBACTERIAL COMPOUNDS
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Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man
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- AMINOCYCLOHEXENE QUINOLINES AND THEIR AZAISOSTERIC ANALOGUES WITH ANTIBACTERIAL ACTIVITY
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Cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
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Page/Page column 33
(2010/02/06)
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- NITROGEN-CONTAINING BICYCLIC HETEROCYCLES FOR USE AS ANTIBACTERIALS
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Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives hereof useful in methods of treatment of bacterial infections in mammals, particularly man.
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Page/Page column 100
(2010/02/07)
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