- ION CHANNEL INHIBITOR COMPOUNDS FOR CANCER TREATMENT
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The present invention concerns a compound of following general formula (I): where: either R is an R1 group and R′ is an -A1-Cy1 group, or R is an -A1-Cy1 group and R′ is an R1 group, R1 particularly being H or (C1-C6)alkyl group;A1 being an —NH— radical or —NH—CH2— radical;Cy1 particularly being a phenyl group,A is a fused (hetero)aromatic ring having 5 to 7 atoms, for use for treating cancer.
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Paragraph 0261; 0262; 0263; 0264; 0265
(2021/01/25)
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- MODULATORS OF HSD17B13 AND METHODS OF USE THEREOF
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The disclosure relates to compounds and pharmaceutical compositions capable of modulating the hydroxysteroid 17-beta dehydrogenase (HSD17B) family member proteins including inhibiting the HSD17B member proteins, e.g. HSD17B13. The disclosure further relates to methods of treating liver diseases, disorders, or conditions with the compounds and pharmaceutical compositions disclosed herein, in which the HSD17B family member protein plays a role.
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Paragraph 0403; 0432
(2021/01/23)
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- Preparation method of chiral compound
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The invention discloses a preparation method of a chiral compound S-5-methoxy-1-tetrahydronaphthalene amine. A particular method of the preparation method of the chiral compound S-5-methoxy-1-tetrahydronaphthalene amine comprises the following steps of using 5-methoxy-1-tetralone as a raw material, making the 5-methoxy-1-tetralone react with hydroxylamine to generate oxime, then carrying out catalytic hydrogenation reduction on the oxime through a catalyst to obtain 5-methoxy-1-tetrahydronaphthalene amine, and then carrying out a dynamic kinetic resolution reaction catalyzed by a biological enzyme on the amine, so that the S-5-methoxy-1-tetrahydronaphthalene amine can be obtained. The preparation method of the chiral compound S-5-methoxy-1-tetrahydronaphthalene amine has the characteristics that the operation is simple, a product is high in yield, a resolved product is high in optical purity, and the like, and has extremely high guide value and application value in the preparation process of the S-5-methoxy-1-tetrahydronaphthalene amine.
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Paragraph 00070011
(2017/07/01)
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- Preparation of optical homochiral amine
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The invention discloses a preparation method of an optical homochiral amine R-5-methoxy-1-naphthalenamine. The method concretely comprises the following steps: carrying out reducing ammonification on a raw material 5-methoxy-1-tetralone to obtain rac-5-methoxy-1-tetralone, and carrying out enzyme-catalyzed dynamic kinetic resolution on the above racemic amine to obtain R-5-methoxy-1-naphthalenamine. The method has the characteristics of simplicity in operation, easily available raw materials, and realization of good yield and high optical purity of the above product.
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Paragraph 0006
(2017/03/08)
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- PYRIMIDINEDIONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE
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The present invention provides compounds of Formula (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
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Paragraph 00206
(2013/10/22)
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- Analogues of σ receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4- tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with added polar functionality and reduced lipophilicity for potential use as positron emission tomography radiotracers
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1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl] piperazine 1 (PB28) represents an excellent lead candidate for therapeutic and/or diagnostic applications in oncology. However, because its utility is limited by its relatively high de
- Abate, Carmen,Niso, Mauro,Lacivita, Enza,Mosier, Philip D.,Toscano, Annamaria,Perrone, Roberto
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scheme or table
p. 1022 - 1032
(2011/04/26)
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- 10A-AZALIDE COMPOUND HAVING 4-MEMBERED RING STRUCTURE
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A 10a-azalide compound having a 4-membered ring structure crosslinked at the 10a- and 12-positions, which is represented by the formula (I), and is effective on even Haemophilus influenzae, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci).
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Page/Page column 56
(2011/04/14)
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- SUBSTITUTED FLUOROETHYL UREAS AS ALPHA 2 ADRENERGIC AGENTS
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Therapeutic compounds, and methods, compositions, and medicaments related thereto are disclosed herein.
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Page/Page column 34
(2008/12/04)
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- Novel flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof
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The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers,—savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.
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Page/Page column 97
(2008/06/13)
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- Substituted aryl 1,4-pyrazine derivatives
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Substituted aryl 1,4-pyrazine derivatives and their use in treating anxiety disorders, depression and stress related disorders are disclosed.
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- 1-Aryl-4-[(1-tetralinyl)alkyl]piperazines: Alkylamido and alkylamino derivatives. Synthesis, 5-HT(1A) receptor affinity, and selectivity
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The synthesis and binding profile on 5-HT(1A), 5-HT2, D-1, D-2, α1, and α2receptors of the N-4 long-chain arylpiperazines 22-40 are reported, where an amino or amido function is inserted into the intermediate chain linked
- Perrone, Roberto,Berardi, Francesco,Leopoldo, Marcello,Tortorella, Vincenzo,Fornaretto, Maria Gioia,Caccia, Carla,McArthur, Robert A.
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p. 3195 - 3202
(2007/10/03)
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