- Synthetic method of 7-fluoro-5-hydroxy-2,3-dihydro-1hydrogen-indene-1-one
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The invention relates to a synthetic method of 7-fluoro-5-hydroxy-2,3-dihydro-1hydrogen-indene-1-one. The technical problem that there is no synthetic method suitable for industrialization at present is mainly solved. The synthetic method of the invention
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Paragraph 0007-0008
(2019/10/10)
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- Substituted Tetrahydroisoquinolines as Beta-secretase Inhibitors
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There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositi
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Page/Page column 19
(2008/12/06)
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- Potent pyrrolidine- and piperidine-based BACE-1 inhibitors
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Based on lead compound 1 identified from the patent literature, we developed novel patentable BACE-1 inhibitors by introducing a cyclic amine scaffold. Extensive SAR studies on both pyrrolidines and piperidines ultimately led to inhibitor 2f, one of the m
- Iserloh,Wu,Cumming,Pan,Wang,Stamford,Kennedy,Kuvelkar,Chen,Parker,Strickland,Voigt
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p. 414 - 417
(2008/04/03)
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- Efficient synthesis of halo indanones via chlorosulfonic acid mediated Friedel-Crafts cyclization of aryl propionic acids and their use in alkylation reactions
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Several halo indanones were synthesized from benzyl Meldrum's acid derivatives in two steps. Although several Lewis acids are effective for the Friedel-Crafts ring-closing reaction on more electron-rich arenes, in the case of the electron-deficient arenes this chemistry is not efficient. Here it is reported that chlorosulfonic acid (used as solvent) is an efficient reagent for cyclization of electron-withdrawing arenes. These molecules are potentially useful for subsequent alkylation reactions. The selective alkylation of 5,7-dibromo indanone is demonstrated using Pd-catalyzed Grignard coupling to provide monoalkylated indanone in good yield.
- Sharma, Anil K.,Subramani, Amutha V.,Gorman, Christopher B.
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p. 389 - 395
(2007/10/03)
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- Novel gamma-lactams as beta-secretase inhibitors
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There is provided a series of novel substituted gamma-lactams of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R4, R5 and R6 as defined herein, their ph
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Page/Page column 27
(2010/10/20)
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- NOVEL ISOPHTHALATES AS BETA-SECRETASE INHIBITORS
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There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
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Page/Page column 29
(2010/11/23)
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- CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT
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Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R is-C(O)-N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer’s disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, and N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
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Page/Page column 31-32
(2008/06/13)
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- CYCLIC AMINE BASE-1 INHIBITORS HAVING A HETEROCYCLIC SUBSTITUENT
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Disclosed are novel compounds of the formula (I)or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is formula (I) X is -0-, -C(R14)2- or -N(R)-; Z is -C(R14)2- or -N(R)-; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, -CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, -OR35, -N(R24)(R25)or -SR35; R41 is alkyl, cycloalkyl, -S02(alkyl), -C(O)-alkyl, -C(O)-cycloalkyl or -alkyl-NH-C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula (I). Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.
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Page/Page column 26-27
(2008/06/13)
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- BICYCLIC SUBSTITUTED INDOLE-DERIVATIVE STEROID HORMONE NUCLEAR RECEPTOR MODULATORS
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The present invention provides a compound of the formula: Formula (I); or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient, and methods for treating physiological disorders, particularly congestive heart disease, hypertension, and atherosclerosis, comprising administering to a patient in thereof an effective amount of a compound of Formula I. X-16125
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Page/Page column 52-53
(2010/02/14)
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- Epoxidation with Dioxiranes derived from 2-Fluoro-2-substituted-1-tetralones and -1-indanones
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Homochiral 2-fluoro-2-substituted-1-tetralones (10a, 10b, 13) and ethyl 2-fluoro-1-indanone-2-carboxylate (16) have been isolated.The dioxirane derivatives of these ketones have been prepared in situ, and have been shown to epoxidise alkenes but not enantioselectively.The dioxirane derivative of methyl 2,5,7-trifluoro-1-indanone-2-carboxylate (18) has been shown to be comparatively efficient in epoxidation.
- Brown, David S.,Marples, Brian A.,Smith, Paul,Walton, Lesley
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p. 3587 - 3606
(2007/10/02)
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- DOPAMINE-BETA-HYDROXYLASE INHIBITORS
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Potent DBH inhibitors having the formula can be used to inhibit DBH activity in mammals.
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- 4-Aralkyl-5-substituted-1,2,4-triazole-5-thiols
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Compounds of formula (I) and pharmaceutically acceptable salts thereof are described in which, n is 0 to 5; X1 to X5 are any accessible combination of hydrogen, halogen, C1 6alkyl, C1 6alkoxy, cyano, nitro, SONH2, SO2NH2, SO2CH3, SO2CH2F, SO2CHF2, SO2CF3, CF3, CHO, OH, CH2OH, CO2H, or CO2CpH2p+1wherein p is 1 to 4; R1 is phenyl substituted by X1 to X5, C1 4alkyl, C3 6cycloalkyl, or an arylC1 4alkyl group substituted by X1 to X5; R2 is hydrogen, C1 4alkyl or (CH2)m-CO2R3; m is 0 to 5; and R3 is H or C1 4alkyl. These compounds are dopamine-β-hydroxylase inhibitors. Pharmaceutical compositions are described as are methods of use. Processes for the preparation of these compounds are described.
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- Dopamine-β-hydroxylase inhibitors and use thereof
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The compounds of this invention are 1-phenylalkyl-2-mercaptotetrazole compounds which are dopamine-β-hydroxylase inhibitors.
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- Cannabis. Part 25. Synthesis of Cannabispirenone-B and its 5,7-Difluoro-analogue
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The naturally occuring cannabispirenone-B (1a) was synthesized by spiroannelation of the piperidine anamine of 5,7-dimethoxyindan-1-carbaldehyde to O-methylcannabispirenone (1b), followed by selective demethylation with lithium iodide in 2,4,6-collidine.I
- Novak, J.,Salemink, C. A.
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p. 2403 - 2406
(2007/10/02)
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