152533-46-5Relevant academic research and scientific papers
Enantioselective approach to 7-azabicyclo[2.21lheptane ring systems using D-(-)quinic acid as the chiral educt: Application to the formal synthesis of (+)-epibatidine
Albertini, Enrichetta,Barco, Achille,Benetti, Simonetta,De Risi, Carmela,Pollini, Gian P.,Zanirato, Vinicio
, p. 681 - 684 (1997)
By utilizing, D-(-)-quinic acid as the chiral starting material the optically pure 7-[(1,1-dimethylethoxy)carbonyl]-7-azabicyclo[ 2.2.1]heptan-2-one 2, an advanced intermediate already taken to (+)-epibatidine 1, a non-opioid analgesic isolated from Ecuadorian poison frogs, was synthetized through a facile, regioselective intramolecular nucleophilic ring opening of a cyclic sulfate moiety.
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793
Préville, Cathy,Bonaventure, Pascal,Koudriakova, Tatiana,Lord, Brian,Nepomuceno, Diane,Rizzolio, Michele,Mani, Neelakandha,Coe, Kevin J.,Ndifor, Anthony,Dugovic, Christine,Dvorak, Curt A.,Coate, Heather,Pippel, Daniel J.,Fitzgerald, Anne,Allison, Brett,Lovenberg, Timothy W.,Carruthers, Nicholas I.,Shireman, Brock T.
supporting information, p. 2002 - 2009 (2020/05/18)
The orexin system consists of two neuropeptides (orexin-A and orexin-B) that exert their mode of action on two receptors (orexin-1 and orexin-2). While the role of the orexin-2 receptor is established as an important modulator of sleep wake states, the role of the orexin-1 receptor is believed to play a role in addiction, panic, or anxiety. In this manuscript, we describe the optimization of a nonselective substituted azabicyclo[2.2.1]heptane dual orexin receptor antagonist (DORA) into orally bioavailable, brain penetrating, selective orexin-1 receptor (OX1R) antagonists. This resulted in the discovery of our first candidate for clinical development, JNJ-54717793.
PROTEASOME ACTIVITY ENHANCING COMPOUNDS
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Page/Page column 160; 163; 198-199, (2020/01/24)
The present invention is directed towards compounds having the Formula (lb) or the Formulae (III) and pharmaceutically acceptable salts, solvates and clathrates thereof, compositions thereof, as well as towards the use of said compounds in methods for the treatment of a condition associated with a dysfunction in proteostasis.
SUBSTITUTED 7-AZABICYCLES AND THEIR USE AS OREXIN RECEPTOR MODULATORS
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Paragraph 0392; 0393, (2016/03/13)
The present invention is directed to compounds of Formula I: wherein ring A is phenyl, naphihalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyi, tlisazolyl, isoxazolvl, pyrazolyl, imidazothiazolyi, benzimidazolyl, or indazolyi; R1 is H, alky], aikoxy, hydroxyalkylene, OH, halo, phenyl, triazolyl, oxazolyl, isoxazofyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazmyl, piperazinyl, pyrazolyl, oxadiazolvl, pyrrolidinyl, thiophenyi, morpholinyl, or dialkyiamino; R2 is H, alkyl, aikoxy, hydroxyalkylene, or halo; Z is NH, N-alkyl, or O; R5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazmyl, qumazolinyi, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, aikoxy, or halo; and n is 0 or 1, Methods of making the compounds of Formula 1 are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
Substituted Imidazopyridines as HDM2 Inhibitors
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, (2014/07/08)
The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
PURINE INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA
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Page/Page column 90, (2014/06/11)
The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflamation, asthma, COPD and cancer.
Tetraaza-cyclopenta[a]indenyl derivatives
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Paragraph 0110-0111, (2015/01/18)
The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator.
TETRAAZA-CYCLOPENTA[A]INDENYL DERIVATIVES
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, (2015/01/09)
The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator.
7-AZONIABICYCLO [2.2.1] HEPTANE DERIVATIVES, METHODS OF PRODUCTION, AND PHARMACEUTICAL USES THEREOF
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, (2011/08/21)
Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided.
BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 201; 202, (2009/05/30)
The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
