- BICYCLIC COMPOUNDS
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Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
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Paragraph 00232
(2020/06/01)
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- Alternative and straightforward synthesis of dopaminergic 5-methoxy-1,2,3,4-tetrahydronaphthalen-2-amine
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5-Methoxy-1,2,3,4-tetrahydronaphthalen-2-amine was synthesized from 2-naphthoic acid in six steps with an overall yield of 27%. Following the reaction sequence, bromination, esterification, substitution with NaOMe in the presence of CuI, the Birch reducti
- Oeztaskin, Necla,Goeksu, Sueleyman,Hasan Secen
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experimental part
p. 2017 - 2024
(2011/06/24)
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- Modulation on C- and N-terminal moieties of a series of potent and selective linear tachykinin NK2 receptor antagonists
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Herein we describe the synthesis of a series of new potent tachykinin NK2 receptor antagonists by the modulation of the Cand N-terminal moieties of ibodutant (MEN 15596, 1). The Nterminal benzo[b]thiophene ring was replaced by different substituted naphthalenes and benzofurans, while further modifications were evaluated at the C-terminal tetrahydropyran moiety. Most compounds demonstrated a high affinity for the human NK2 receptor and high in vitro antagonist potency, indicating that a wide range of substituents at both termini can be incorporated in the molecule without detrimental effects on the interactions with the NK2 receptor. Selected compounds were tested in vivo confirming their activity as NK2 antagonists. In particular, after both iv and id administration to guinea pig, compound 61b was able to antagonize NK2-induced colonic contractions with a potency and duration-of-action fully comparable to the reference compound 1 (MEN 15596, ibodutant).
- Gensini, Martina,Altamura, Maria,Dimoulas, Tula,Fedi, Valentina,Giannotti, Danilo,Giuliani, Sandro,Guidi, Antonio,Harmat, Nicholas J. S.,Meini, Stefania,Nannicini, Rossano,Pasqui, Franco,Tramontana, Manuela,Triolo, Antonio,Maggi, Carlo Alberto
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scheme or table
p. 65 - 78
(2010/11/16)
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- Melanin concentrating hormone antagonists
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The present invention relates to compounds capable of serving as moderators of human and mammalian appetite and as such provide a means for reducing body mass and controlling obesity.
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Page/Page column 9
(2010/11/30)
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- Indole derivatives for the treatment of depression and anxiety
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The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.
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Page/Page column 15
(2010/02/05)
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- Design and Syntheses of 1,6-Naphthalene Derivatives as Selective HCMV Protease Inhibitors
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Through high throughput screening of various libraries, substituted styryl naphthalene 6 was identified as an HCMV protease inhibitor. Optimization of various regions of the lead molecule using parallel synthesis resulted in 1,6-substituted naphthalenes 1
- Gopalsamy, Ariamala,Lim, Kitae,Ellingboe, John W.,Mitsner, Boris,Nikitenko, Antonia,Upeslacis, Janis,Mansour, Tarek S.,Olson, Matthew W.,Bebernitz, Geraldine A.,Grinberg, Diane,Feld, Boris,Moy, Franklin J.,O'Connell, John
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p. 1893 - 1899
(2007/10/03)
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- Piperidines derivatives and their use as serotonin receptor antagonists
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The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.
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- SYNTHESIS AND POLYMERIZATION OF SOME ETHYNYL TRIFLUOROMETHYL NAPHTHALENES
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Some bromonaphthoic acids were fluorinated with SF4 to bromo(trifluoromethyl)naphthalenes.Although a reaction of Grignard reagent of one of the bromides with Cl2C=CF2 gave low yield of a (dichlorofluorovinyl)(trifluoromethyl)naphthalene, lithio derivatives gave the desired ethynyl(trifluoromethyl)naphthalenes in improved yields after subsequent eliminations of the vinylic halogens with n-butyllithium.Polymerization of the acetylenes was carried out with photo-activated W(CO)6 catalyst to yield high-molecular-weight polymers.
- Okano, T.,Ito, K.,Kodaira, K.,Hosokawa, K.,Nishida, M.,et al.
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p. 139 - 152
(2007/10/02)
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- 1-Arylmethyl-2-imidazolidinones
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A series of 1-arylmethyl-2-imidazolidinones are useful as antidepressant agents.
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