23876-14-4Relevant academic research and scientific papers
HETEROCYCLIC INHIBITORS OF GLUTAMINASE
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Page/Page column 122, (2013/06/06)
The invention relates to the heterocyclic compounds of Formula (I) as defined further herein, and pharmaceutical preparations thereof. The invention further relates to methods of treating cancer, immunological or neurological diseases using the heterocyclic compounds of the invention.
PROCESS FOR THE PREPARATION OF INDOLONE DERIVATIVE
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Page/Page column 22, (2008/06/13)
A process for the preparation of 4-[2-(Di-n-propylamino) ethyl]-2,3-dihydro-1 H-indol-2-one of formula (I) and its pharmaceutically acceptable salts, solvates Formaula I involving new intermediates of compound of formula (A) and (B) wherein R represents (i) a halogen atom selected from fluorine, chlorine atom, bromine atom and iodine atom; (ii) lower alkanesulfonyloxy group selected from methanesulfonyloxy, ethanesulfonyloxy, isopropanesulfonyloxy, propanesulfonyloxy, butanesulfonyloxy, tert-butanesulfonyloxy, pentanesulfonyloxy, hexanesulfonyloxy; (iii) substituted or unsubstantiated arylsulfonyloxy group selected from phenylsulfonyloxy, 4-methylphenylsulfonyloxy, 2-methylphenylsulfonyloxy, 4- nitrophenylsulfonyloxy, 4- methoxyphenylsulfonyloxy, 3-chlorophenylsulfonyloxy; (iv) arylalkylsulfonyloxy group selected from benzylsulfonyloxy, 2- phenylethylsulfonyloxy, 4-phenylbutylsulfonyloxy, 4- methylbenzylsulfonyloxy, 2- methylbenzylsulfonyloxy, 4- nitrobenzylsulfonyloxy, 4-methoxybenzylsulfonyloxy, 3- chlorobenzylsulfonyloxy.
New indazole and indolone derivatives and their use pharmaceuticals
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Page/Page column 29, (2010/02/14)
The present invention provides for compounds of formula (I), which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.
2-IMIDAZOLINE, 2-OXAZOLINE, 2-THIAZOLINE, AND 4-IMIDAZOLE DERIVATIVES OF METHYLPHENYL, METHOXYPHENYL, AND AMINOPHENYL ALKYLSULFONAMIDES AND UREAS AND THEIR USE
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, (2008/06/13)
The present invention concerns novel compounds represented by the Formula: STR1 wherein: A is R 1 q (R 3 R 60 N). sub.m (Z)(NR 2) n ; m and q are each 0 or 1, with the proviso that when q is 1, m is 0 and when q is 0, m is 1; Z is C=O or SO 2 ; n is 1 with the proviso that, when Z is C=O, m is 1; X is--NH--,--CH 2--, or--OCH 2--; Y is 2-imidazoline, 2-oxazoline, 2-thiazoline, or 4-imidazole; R 1 is H, lower alkyl, or phenyl, with the proviso that, when R 1 is H, m is 1; R 2, R 3, R 60 are each independently H, lower alkyl, or phenyl; R 4, R 5, R. sup.6, and R 7 are each independently hydrogen, lower alkyl,--CF. sub.3, lower alkoxy, halogen, phenyl, lower alkeny, hydroxyl, lower alkylsulfonamido, or lower cycloalkyl, wherein R. sup.2 and R 7 optionally may be taken together to form alkylene or alkenylene of 2 to 3 atoms in an unsubstituted or optionally substituted 5-or 6-membered ring, wherein the optional substituents on the ring are halo, lower alkyl, or--CN, with the proviso that, when R 7 is hydroxyl or lower alkylsulfonamido, then X is not--NH--when Y is 2-imidazoline. The compounds include pharmaceutically acceptable salts of the above. In the above formula A may be, for example, (R 1 SO 2 NR 2--), (R. sup.3 R 60 NSO 2 NR 2--), or (R 3 R 60 NCONR 2--). The invention also includes the use of the above compounds, and compositions containing them, as alpha 1A/1L agonists in the treatment of various disease states such as urinary incontinence, nasal congestion, priapism, depression, anxiety, dementia, senility, Alzheimer's, deficiencies in attentiveness and cognition, and eating disorders such as obesity, bulimia, and anorexia.
Phenyl-and aminophenyl-alkylsulfonamide and urea derivatives, their preparation and their use as alpha1A/1L adrenoceptor agonists
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, (2008/06/13)
The present invention concerns novel compounds represented by the Formula:*(formula 02)* wherein: A is R1q(R3R60N)m(Z)(NR2)n; m and q are each 0 or 1, with the proviso that when q is 1, m is 0 and when q is 0, m is 1; Z is C=O or SO 2; n is 1 with the proviso that, when Z is C=O, m is 1; X is -NH-, -CH2-, or -OCH2-; Y is 2-imidazoline, 2-oxazoline, 2-thiazoline, or 4-imidazole; R 1 is H, lower alkyl, or phenyl, with the proviso that, when R1 is H, m is 1; R2, R3, R60 are each independently H, lower alkyl, or phenyl; R4, R5, R6, and R7 are each independently hydrogen, lower alkyl, - CF 3, lower alkoxy, halogen, phenyl, lower alkeny, hydroxyl, lower alkylsulfonamido, or lower cycloalkyl, wherein R2 and R7 optionally may be taken together to form alkylene or alkenylene of 2 to 3 atoms in an unsubstituted or optionally substituted 5-or 6-membered ring, wherein the optional substituents on the ring are halo, lower alkyl, or -CN,with the proviso that, when R7 is hydroxyl or lower alkylsulfonamido, then X is not -NH- when Y is 2-imidazoline. The compounds include pharmaceutically acceptable salts of the above. In the above formula A may be, for example, (R1SO2NR2-), (R3R60NSO2NR2-), or (R3R60NCONR2-). The invention also includes the use of the above compounds, and compositions containing them, as alpha 1A/1L agonists in the treatment of various disease states such as urinary incontinence, nasal congestion, priapism, depression, anxiety, dementia, senility, Alzheimer's, deficiencies in attentiveness and cognition, and eating disorders such as obesity, bulimia, and anorexia.
Synthesis of 4-N,N-dialkylaminoethyl-2-indolones as potential dopamine agonists
Namil, A.,Benoit-Guyod, M.,Leclerc, G.
, p. 973 - 982 (2007/10/03)
A set of fourteen 4-ethyl>-2-indolone analogues of dopamine were synthesized in 15 steps and evaluated for their affinities towards the D2 receptor using sulpiride or spiperone as radioligands.Six analogues displayed D2 agonist activities comparable (Ki = 450 - 650 nM) to Ropinirole or SK and F 101468.The functionalized amino side chain introduced in the 4-position can be used to modulate the lipophlicity of the analogues without significantly affecting D2 activity. - Keywords: lactam; indolone; rigid dopamine analogue; D2 receptor binding
4--2(3H)-indolone: A Prejunctional Dopamine Receptor Agonist
Gallagher, Gregory,Lavanchy, Patricia G.,Wilson, James W.,Hieble, J. Paul,DeMarinis, Robert M.
, p. 1533 - 1536 (2007/10/02)
4--2(3H)-indolone (1c) (SK and F 101468) is a potent and selective prejunctional dopamine receptor agonist.It caused a dose-related inhibition of the constrictor response to electrical stimulation in the isolated perfused rabbit ear artery (EC50 = 100 nM), and this response was antagonized by (S)-sulpiride (KB = 7 nM).Compound 1c did not stimulate or block dopamine-sensitive adenylate cyclase and did not produce stimulation of the central nervous system in rats.It was prepared from (2-methyl-3-nitrophenyl)acetic acid in a multistep sequence based on the Reissert indole synthesis.
