- HETEROCYCLIC COMPOUNDS FOR MODULATING NR2F6
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The present disclosure relates to compounds capable of modulating the activity of NR2F6. The compounds of the disclosure may be used in methods for the prevention and/or the treatment of diseases and disorders associated with modulating NR2F6 activity.
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Paragraph 00516-00518
(2021/09/04)
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- THERAPEUTIC COMPOUNDS AND METHODS TO TREAT INFECTION
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Disclosed herein are compounds of formula I: or a salt thereof and compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof, alone or in combination with a bacterial efflux pump inhibitor.
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Paragraph 0472-0473
(2019/02/13)
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- Ruthenium-catalyzed chemo-and enantioselective hydrogenation of isoquinoline carbocycles
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A chemoselective hydrogenation of isoquinoline carbocycles was achieved by using the catalyst prepared from Ru(methallyl)2(cod) and trans-chelate chiral ligand PhTRAP. The unique chemoselectivity achieved in this hydrogenation could be ascribed to the trans-chelation of the chiral ligand. The procedure for preparing the catalyst strongly affects the reproducibility of the carbocycle hydrogenation. Various 5-, 6-, 7-, and 8-substituted isoquinolines were selectively hydrogenated at their carbocycles to afford 5,6,7,8-tetrahydroisoquinolines as major products in high yields with moderate or good enantioselectivities. Some mechanistic studies suggested that the stereogenic center was created during the initial addition of H2 to the aromatic ring in the hydrogenation of 5-substituted isoquinolines. In other words, the stereochemical control was accompanied by the dearomatization.
- Jin, Yushu,Makida, Yusuke,Uchida, Tatsuya,Kuwano, Ryoichi
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p. 3829 - 3839
(2018/04/14)
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- Discovery of novel 2,5-dioxoimidazolidine-based P2X7 receptor antagonists as constrained analogues of KN62
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Novel 2,5-dioxoimidazolidine-based conformationally constrained analogues of KN62 (1) were developed as P2X7 receptor (P2X7R) antagonists using a rigidification strategy of the tyrosine backbone of 1. SAR analysis of the 2,5-dioxoimidazolidine scaffold indicated that piperidine substitution at the N3 position and no substitution at N1 position were preferable. Further optimization of the substituents at the piperidine nitrogen and the spacer around the skeleton resulted in several superior antagonists to 1, including 1-adamantanecarbonyl analogue 21i (IC50 = 23 nM in ethidium uptake assay; IC50 = 14 nM in IL-1β ELISA assay) and (3-CF3-4-Cl)benzoyl analogue (-)-21w (54 nM in ethidium uptake assay; 9 nM in IL-1β ELISA assay), which was more potent than the corresponding (+) isomer. Compound 21w displayed potent inhibitory activity in an ex vivo model of LTP-induced pain signaling in the spinal cord and significant anti-inflammatory activity in in vivo models of carrageenan-induced paw edema and type II collagen-induced joint arthritis.
- Park, Jin-Hee,Lee, Ga-Eun,Lee, So-Deok,Hien, Tran Thi,Kim, Sujin,Yang, Jin Won,Cho, Joong-Heui,Ko, Hyojin,Lim, Sung-Chul,Kim, Yoon-Gyoon,Kang, Keon-Wook,Kim, Yong-Chul
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supporting information
p. 2114 - 2134
(2015/03/30)
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- SUBSTITUTED 6,7-DIALKOXY-3-ISOQUINOLINOL DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASE 10 (PDE10A)
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The invention relates to compounds of the formula wherein R′, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
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Page/Page column 37
(2012/09/05)
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- SUBSTITUTED PYRIDINONES
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Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
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Page/Page column 293
(2008/06/13)
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- THROMBIN INHIBITORS
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Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group consisting of: or a pharmaceutically acceptable salt thereof, wherein T is selected from the group consisting of D, E, F, G, H, I, and J are independently N or CY 1, provided that the number of such variables D, E, F, G, H, I, and J representing N is 0, 1, or 2; K, L, M and Q are independently NH or CY1Y2, provided that the number of such variables D, E, F, K, L, M, and Q representing N is 0, 1, or 2; Y1 and Y2 are independently selected from the group consisting of hydrogen, C1-4 alkyl, halogen, anino, or hydroxy; A is
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- 1-Phenyl isoquinoline-5-acetic acid compounds and analgesic compositions thereof
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Novel isoquinoline derivatives of the general formula STR1 wherein R represents a lower alkyl group, a lower cycloalkyl group, or a group of the formula STR2 in which R2 represents a hydrogen atom, a halogen atom, a methyl group, a trifluoromethyl group, a methoxy group, a methylamino group or a dimethylami no group; R1 represents a hydrogen atom or a lower alkyl group; and Y represents a carboxyl group, a cyano group, a carbamoyl group, a lower alkoxycarbonyl group or a lower alkylaminocarbonyl group; or a salt thereof; a process for the production thereof. The above compound is useful as an anti-inflammatory and analgesic agent.
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