- CYCLIC BRIDGEHEAD ETHER DGAT1 INHIBITORS
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The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.
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Paragraph 0402;0403; 0404
(2013/11/06)
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- FLUOROPHENYL BICYCLIC HETEROARYL COMPOUNDS
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The present invention provides a compound of formula (I); a method for manufacturing the compounds of the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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Page/Page column 50
(2012/09/22)
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- HYDROXY SUBSTITUTED ISOQUINOLINONE DERIVATIVES
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The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
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Page/Page column 158-159
(2013/02/28)
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- ETHER DERIVATIVES OF BICYCLIC HETEROARYLS
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The invention relates to compounds of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; such compounds as a medicament; such compounds for the treatment of a proliferative disease
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Page/Page column 60
(2011/04/18)
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- Design and synthesis of cell potent BACE-1 inhibitors: Structure-activity relationship of P1′ substituents
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Using structure-guided design, hydroxyethylamine BACE-1 inhibitors were optimized to nanomolar Aβ cellular inhibition with selectivity against cathepsin-D. X-ray crystallography illuminated the S1′ residues critical to this effort, which culminated in compounds 56 and 57 that exhibited potency and selectivity but poor permeability and high P-gp efflux.
- Sealy, Jennifer M.,Truong, Anh P.,Tso, Luke,Probst, Gary D.,Aquino, Jose,Hom, Roy K.,Jagodzinska, Barbara M.,Dressen, Darren,Wone, David W.G.,Brogley, Louis,John, Varghese,Tung, Jay S.,Pleiss, Michael A.,Tucker, John A.,Konradi, Andrei W.,Dappen, Michael S.,Toth, Gergely,Pan, Hu,Ruslim, Lany,Miller, Jim,Bova, Michael P.,Sinha, Sukanto,Quinn, Kevin P.,Sauer, John-Michael
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scheme or table
p. 6386 - 6391
(2010/06/11)
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- OXIME DERIVATIVE SUBSTITUTED HYDROXYETHYLAMINE ASPARTYL PROTEASE INHIBITORS
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The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a colletion of diseases, disorders, and conditions associated with abnormal deposition of A-beta protei
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Page/Page column 100
(2008/06/13)
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- OXIME DERIVATIVE HYDROXYETHYLAMINE ASPARTYL-PROTEASE INHIBITORS
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The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
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Page/Page column 105
(2010/02/15)
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- SUBSTITUTED HYDROXYETHYLAMINE ASPARTYL PROTEASE INHIBITORS
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The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
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Page/Page column 283-284
(2008/06/13)
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- SUBSTITUTED UREA AND CARBAMATE, PHENACYL-2-HYDROXY-3-DIAMINOALKANE, AND BENZAMIDE-2-HYDROXY-3-DIAMINOALKANE ASPARTYL-PROTEASE INHIBITORS
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The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in treating at least one disease, disorder, and condition associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and condition associated with abnormal deposition of A-beta protein.
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Page/Page column 368
(2010/02/14)
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- SUBSTITUTED HYDROXYETHYLAMINE ASPARTYL PROTEASE INHIBITORS
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The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
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Page/Page column 138-139
(2010/02/14)
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- [3,3] Sigmatropic rearrangement of some fluorinated 1,5-hexadienes
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Fluorine atoms incorporated into 1,5-hexadiene molecule should influence the kinetic as well as the thermodynamic parameters of [3,3] sigmatropic rearrangement (Cope rearrangement). Within few decades is has been documented that this transformation proceeds in a concerted manner, rather than stepwise with some radical intermediates involved. Few new terminally fluorinated 1,5-hexadienes (compounds 3, 5A, 7, 9 and 5B) have been synthesized. The activation parameters of rearrangement have been determined and compared with those known for hydrocarbon analogues. While systems developing chair-like transition states (compounds 3 and 5) showed close similarity with hydrocarbon analogues (compound 1), those developing boat-like transition states (compounds 7, 9 and 5B) may proceed through radical stepwise mechanism. Computational studies of the transition states were carried out, showing that only ab initio methods (MP2 and especially DFT) can give approximate correlation with experimental data, whereas in the case of hydrocarbon analogues even simple semiempirical methods (AM1) were reliable enough to reproduce experimental results.
- Dolbier Jr., William R.,Palmer, Keith W.,Tian, Feng,Fiedorow, Piotr,Zaganiaczyk, Andrzej,Koroniak, Henryk
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p. 1517 - 1532
(2007/10/03)
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- A useful α, α' - Annulation reaction of enamines
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The reactions of a series of enamines generated from a range of cyclic ketones with chloromethyl and iodomethyl vinyl ketone have been studied. The principal products are bridged ring diketones. The four carbon bridge, bearing a 2-oxobutyl function, spans
- Frontier, Alison J.,Danishefsky, Samuel J.,Koppel, Gary A.,Meng, Dongfang
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p. 12721 - 12736
(2007/10/03)
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