- Synthesis method of ropinirole hydrochloride intermediate of 2-methyl-3-nitrophenylacetic acid
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The invention discloses a synthesis method of a ropinirole hydrochloride intermediate of 2-methyl-3-nitrophenylacetic acid. 6-halogenated-2-methyl nitrobenzene and halogenated ethyl acetate react under the catalyst effect to obtain 2-methyl-3-nitrophenyla
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Paragraph 0037-0042
(2019/06/11)
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- PROCESS FOR THE PREPARATION OF INDOLONE DERIVATIVE
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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.
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Page/Page column 22; 23
(2008/06/13)
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- New indazole and indolone derivatives and their use pharmaceuticals
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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.
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Page/Page column 29
(2010/02/14)
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- ESTER COMPOUND AND MEDICINAL USE THEREOF
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A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1") (wherein ???R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; ???X is -COO- or -CON(R10)-; ???R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; ???R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; ???R8 and R9 are each independently hydrogen atom, C1-C6 alkyl, -CON(R18)(R19) or -COO(R20), etc.; ???ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; ???Alk1 and Alk2 are each independently alkanediyl, etc.; ???l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.
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- 4--2(3H)-indolone: A Prejunctional Dopamine Receptor Agonist
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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.
- Gallagher, Gregory,Lavanchy, Patricia G.,Wilson, James W.,Hieble, J. Paul,DeMarinis, Robert M.
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p. 1533 - 1536
(2007/10/02)
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