321352-52-7Relevant articles and documents
INHIBITORS OF MTOR-MEDIATED INDUCTION OF AUTOPHAGY
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Paragraph 088, (2021/04/30)
The invention provides amides that inhibit apoptosis or induce autophagy through mTOR-mediated induction of autophagy, or inhibit a related disease such as cerebral ischemia/reperfusion or neurodegenerative diseases, including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
DIARYL ETHER DERIVATIVES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS
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Page/Page column 77, (2011/05/05)
The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
Structure based evolution of a novel series of positive modulators of the AMPA receptor
Jamieson, Craig,MacLean, John K.F.,Brown, Christopher I.,Campbell, Robert A.,Gillen, Kevin J.,Gillespie, Jonathan,Kazemier, Bert,Kiczun, Michael,Lamont, Yvonne,Lyons, Amanda J.,Moir, Elizabeth M.,Morrow, John A.,Pantling, John,Rankovic, Zoran,Smith, Lynn
scheme or table, p. 805 - 811 (2011/02/27)
Starting from compound 1, we utilized biostructural data to successfully evolve an existing series into a new chemotype with a promising overall profile, exemplified by 19.
INDANE DERIVATIVES
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Page/Page column 19, (2010/11/03)
The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer' s disease.
Discovery of N -[(2 s)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1 H -inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator
Ward, Simon E.,Harries, Mark,Aldegheri, Laura,Andreotti, Daniele,Ballantine, Stuart,Bax, Benjamin D.,Harris, Andrew J.,Harker, Andy J.,Lund, Jesper,Melarange, Rosemary,Mingardi, Anna,Mookherjee, Claudette,Mosley, Julie,Neve, Marta,Oliosi, Beatrice,Profeta, Roberto,Smith, Kathrine J.,Smith, Paul W.,Spada, Simone,Thewlis, Kevin M.,Yusaf, Shahnaz P.
scheme or table, p. 5801 - 5812 (2010/11/05)
A series of AMPA receptor positive allosteric modulators has been optimized from poorly penetrant leads to identify molecules with excellent preclinical pharmacokinetics and CNS penetration. These discoveries led to 17i, a potent, efficacious CNS penetrant molecule with an excellent pharmacokinetic profile across preclinical species, which is well tolerated and is also orally bioavailable in humans.
INDANE DERIVATIVES AS AMPA RECEPTOR MODULATORS
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Page/Page column 20, (2009/12/28)
The present invention relates to a heterocyclic derivative according to formula (I); wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceut
SUBSTITUTED INDAN-2-YL, TETRAHYDRONAPHTHALEN-2-YL, OR DIHYDR0-2H-CHR0MEN-3-YL ARYLSULFONAMIDES AND METHODS OF THEIR USE
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Page/Page column 41-42, (2008/12/05)
Compounds of formula (I) and pharmaceutically acceptable salts thereof, which are modulators of secreted frizzled related protein- 1, are disclosed. The compounds, and compositions containing the compounds, can be used to treat various diseases and disord
6-AMINO(AZA)INDANE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECPTOR
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Page/Page column 92-93, (2008/06/13)
The present invention relates to 6-amino(aza)indane compound of the formula (I) Wherein Ar is phenyl or an aromatic 5-or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry I or 2 radicals Rb; X is N or CH; E is CR6R7 or NR 3; R1 is C 1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2, 3 or 4; R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3; R3 is H or C,-C4-alkyl; and the physiologically tolerated acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof and to a method for treating a medical disorder susceptible to treatment with a dopamine D3 receptor ligand, said method comprising administering an effective amount of at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof.
COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE
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Page/Page column 30, (2008/06/13)
Compounds which potentiate glutamate receptor and uses thereof in medicine Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C 1-6alkyl, haloC1-6 alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R 2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C 1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4 alkylamino or diC1-4alkylamino; each R4, which may be the same or different, is C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4 alkoxy, cyano, nitro, amino, monoC1-4 alkylamino or diC1-4alkylamino; p is 0, 1 or 2; n is 1 or 2; R5 and R6, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C 1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consisting of C1-6alkyl, C1-6alkoxy, acetyl, halogen, haloC1-6alkyl, cyano, nitro, amino, monoC1-4alkylamino and diC1-4alkylamino. Methods of preparation of the compounds, and uses thereof in medicine, for example treatment of schizophrenia, are also disclosed.
Carboxamides useful as inhinitors of microsomal triglyceride transfer protein and of apolipoprotein b secretion
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, (2008/06/13)
Compounds of formula (1) wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, heteroaryl or (aryl or heteroaryl)-lower alkoxy; R2, R3, R4 and R5 are independently hydrogen, lower alkyl, lower alkoxy, halo, trifluoromethyl or cyano; R6 is (i) or (ii) m is 1, 2 or 3; R7 is hydrogen, lower alkyl (aryl or heteroaryl)-lower alkyl, lower alkoxy, (aryl or heteroaryl)-lower alkoxy, hydroxy, oxo, lower alkylenedioxy or lower alkanoyloxy; W is O, S or NR8; R8 is —CORa, (iii), —COORd, —SO2Re, hydrogen, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Ra, Rd and Re, are independently optionally substituted lower alkyl, cycloalkyl, adamantyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Rb and Rc are independently hydrogen, cycloalkyl, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl) lower alkyl; or Rb and Rc together represent lower alkylene; and pharmaceutically acceptable salts thereof; and enantiomers thereof; which are useful as inhibitors of microsomal triglyceride transfer protein (MTP) and of apolipoprotein B (apoB) secretion.
