- Spirocyclic oxetanes: Synthesis and properties
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(Chemical Presented) Wormholes through chemical space: Spirocyclic oxetanes are described as analogues of morpholine and also as topological siblings of their carbonyl counterparts. They are particularly promising in terms of both their physicochemical properties and the ease with which they can be grafted onto molecular structures. The data collected highlight oxetanes as both the hydrophilic sister of a gem-dimethyl unit and the carbonyl group's lipophilic brother.
- Wuitschik, Georg,Rogers-Evans, Mark,Buckl, Andreas,Bernasconi, Maurizio,Maerki, Moritz,Godel, Thierry,Fischer, Holger,Wagner, Bjoern,Parrilla, Isabelle,Schuler, Franz,Schneider, Josef,Alker, Andre,Schweizer, W. Bernd,Mueller, Klaus,Carreira, Erick M.
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- Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents
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The design, synthesis and antimicrobial evaluation of a novel series of azaspiro analogues of linezolid (1) have been described. Linezolid comprises of a morpholine ring which is known for its metabolism-related liabilities. Therefore, the key modificatio
- Gadekar, Pradip K.,Roychowdhury, Abhijit,Kharkar, Prashant S.,Khedkar, Vijay M.,Arkile, Manisha,Manek, Hardik,Sarkar, Dhiman,Sharma, Rajiv,Vijayakumar,Sarveswari
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- Synthesis and Properties of 2-Oxa-6-azaspiro[3.3]heptane Sulfonate Salts
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An improved synthesis of the bicyclic spiro compound 2-oxa-6-azaspiro[3.3]heptane is presented. While this compound is often isolated as an oxalate salt, its isolation as a sulfonic acid salt yields a more stable and more soluble product. With these improved properties access to a wider range of reaction conditions with the spirobicyclic 2-oxa-6-azaspiro[3.3]heptane has been enabled.
- Van Der Haas, Richard N. S.,Dekker, Jeroen A.,Hassfeld, Jorma,Hager, Anastasia,Fey, Peter,Rubenbauer, Philipp,Damen, Eric
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- The Development of a Manufacturing Route to an MCHr1 Antagonist
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Process development work to provide an efficient manufacturing route to a MCHr1 antagonist is presented herewith. Features of this development work include a scalable manufacturing route to the useful 6-oxa-2-azaspiro[3.3]heptane building block and the use of a (soluble) alternative to sodium triacetoxyborohydride.
- Golden, Michael,Legg, Danny,Milne, David,Arun Bharadwaj,Deepthi,Gopal, Madan,Dokka, Nagaraju,Nambiar, Sudhir,Ramachandra, Puranik,Santhosh,Sharma, Parhalad,Sridharan,Sulur, Manjunatha,Linderberg, Mats,Nilsson, Anders,Sohlberg, Roger,Kremers, John,Oliver, Samuel,Patra, Debasis
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- SUBSTITUTED PHENYLOXAZOLIDINONES FOR ANTIMICROBIAL THERAPY
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The present invention relates to novel oxazolidinones (Formula I): or a pharmaceutically acceptable salt having ring A characterized by N-containing monocyclic, bicyclic or spirocyclic substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.
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Page/Page column 138; 139
(2017/02/09)
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- Design, synthesis and biological evaluation of paclitaxel-mimics possessing only the oxetane D-ring and side chain structures
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Two spiro paclitaxel-mimics consisting only of an oxetane D-ring and a C-13 side chain were designed and synthesized on the basis of analysis of structure-activity relationships (SAR) of paclitaxel. In vitro microtubule-stabilizing and antiproliferative assays indicated a moderate weaker activity of the mimics than paclitaxel, but which still represented the first example of simplified paclitaxel analogues with significant anti-tumor biological activity.
- Chen, Xing-Xiu,Gao, Feng,Wang, Qi,Huang, Xing,Wang, Dan
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p. 111 - 115
(2014/01/06)
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- SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS
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Provided herein are novel substituted bicyclic aza-heterocycle sirtuin- modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin- modulating compound in combination with another therapeutic agent.
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- THIAZOLOPYRIMIDINE COMPOUNDS
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The present invention relates to the use of novel pyrrolopyrazine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
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- BICYCLIC PYRIDINES AND ANALOGS AS SIRTUIN MODULATORS
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Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
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- NITROGEN HETEROCYCLIC COMPOUNDS USEFUL AS PDE10 INHIBITORS
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Unsaturated nitrogen heterocyclic compounds of formula (I): (I), as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
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