847805-31-6Relevant articles and documents
MDM2 DEGRADERS AND USES THEREOF
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Paragraph 00988; 00989-00990, (2021/09/26)
The present invention relates to compounds and methods useful for the modulation of mouse double minute 2 homolog ("MDM2") protein via ubiquitination and/or degradation by compounds according to the present invention.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 00962; 004168-004170, (2020/06/19)
The present invention provides compounds, compositions thereof, and methods of using the same.
DIHYDROPYRIMIDINE COMPOUND AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0214; 0215, (2019/07/18)
The present invention relates to a dihydropyrimidine compound having an antiviral activity, a pharmaceutical composition comprising same, a preparation method therefor and the uses thereof in the prevention or treatment of viral diseases including, but no
PYRIDINONE DICARBOXAMIDE FOR USE AS BROMODOMAIN INHIBITORS
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Page/Page column 90, (2017/04/11)
The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
BENZO[B]FURANS AS BROMODOMAIN INHIBITORS
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Page/Page column 75; 76, (2017/11/06)
The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
CXCR4 Receptor Antagonists
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Paragraph 0370; 0371, (2013/11/06)
Disclosed are compounds that are antagonists of the CXCR4 receptor.
Design and synthesis of reboxetine analogs morpholine derivatives as selective norepinephrine reuptake inhibitors
Xu, Wenjian,Gray, David L.,Glase, Shelly A.,Barta, Nancy S.
scheme or table, p. 5550 - 5553 (2009/05/30)
As part of a discovery effort aimed at identifying novel norepinephrine reuptake inhibitors (NRIs), a number of substituted morpholines were designed and synthesized. The target compounds contain vicinal stereogenic centers, and the program was greatly facilitated by the adoption of efficient synthetic routes which allowed for the late stage incorporation of structural and physicochemical diversity into the targets. Structure-activity relationships were developed by optimizing individual ring components of the structure for NRI potency and for selectivity against other monoamine reuptake transporters. Several novel morpholine derivatives with a potent and selective NRI profile are described.
Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER
Tamagnan, Gilles D.,Brenner, Eric,Alagille, David,Staley, Julie K.,Haile, Colin,Koren, Andrei,Early, Michelle,Baldwin, Ronald M.,Tarazi, Frank I.,Baldessarini, Ross J.,Jarkas, Nachwa,Goodman, Mark M.,Seibyl, John P.
, p. 533 - 537 (2007/10/03)
A series of reboxetine analogs was synthesized and evaluated for in vitro binding as racemic mixtures. The best candidate (INER) was synthesized as the optically pure (S,S) enantiomer, labeled with iodine-123 and its in vivo binding determined by SPECT im
NOREPINEPHRINE TRANSPORTER RADIOTRACERS AND METHODS OF SYNTHESES THEREOF
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Page/Page column 52; 53, (2008/06/13)
The present invention provides compounds and radiotracers thereof for locating, diagnosing, identifying, evaluating, detecting or quantitating NET by in vivo imaging. The invention also provides methods for locating, diagnosing, identifying, evaluating, detecting or quantitating NET, using radiotracers of high-affinity or labeled compounds of the invention, which exhibit low toxicity, can cross the blood-brain barrier and, preferably, distinguish among normal and abnormal brains. For example, a radiotracer of the invention can be administered to a patient in an amount suitable for in vivo imaging thereof. Preferably, radiotracers of the invention can also be used to locate, diagnosis, identify, evaluate, detect and quantitate NET in such diseases, disorders, conditions or maladies as, without limitation, depression, anxiety, ADHD and drug dependency.
Asymmetric synthesis of (+)-(S,S)-reboxetine via a new (S)-2- (hydroxymethyl)morpholine preparation
Brenner, Eric,Baldwin, Ronald M.,Tamagnan, Gilles
, p. 937 - 939 (2007/10/03)
(Chemical Equation Presented) (S,S)-Reboxetine was synthesized stereospecifically in 30% overall yield and 99% ee in eight steps. Key steps were selective oxidation of an N-protected hydroxymethylmorpholine and aryl-chromium-mediated aromatic nucleophilic substitution.