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    • 146. 发明专利
    • ISOINDOLINE COMPOUNDS
    • GB1344663A
    • 1974-01-23
    • GB4991871
    • 1971-10-27
    • ERBA CARLO SPA
    • C07D209/44C07D209/46C07D27/50A61K27/00
    • 1344663 Isoindolinone derivatives CARLO ERBA SpA 27 Oct 1971 [5 Nov 1970 10 Nov 1970] 49918/71 Heading C2C The invention comprises compounds of formula wherein R is H or C 1-4 alkyl, R 1 is H, alkyl or (CH 2 ) n NR 2 R 3 , n is 1 or 2 and R 2 , R 3 are each H or C 1-4 alkyl, and their physiologically acceptable addition salts (where R 1 is H or aminoalkyl). In examples, these compounds are prepared (1) when R 1 is H, by hydrolysing (a) the corresponding esters or nitriles (II), or (b) the analogous iminoisoindolinecarboxylic acids or alkyl esters; (2) when R 1 is alkyl, by (a) esterifying the acids, (b) reducing the analogous phthalimide compounds, (c) reacting the corresponding alkyl p-aminophenylacetates with phthalide, thiophthalide or phthalaldehyde; (3) when R 1 is aminoalkyl, by reacting the corresponding acid chlorides with R 2 R 3 N(CH 2 ) n OH. Also prepared are the iminoisoindoline and phthalimide analogues of II. Therapeutic compositions having analgesic and anti-inflammatory activity comprise compounds of the above formula, and may be administered orally, parenterally, rectally or topically.
    • 150. 发明专利
    • ISOINDOLINE DERIVATIVES
    • GB1324936A
    • 1973-07-25
    • GB5781371
    • 1971-12-13
    • RHONE POULENC SA
    • C07D209/48C07D27/50A61K27/00C07D99/02
    • 1324936 Derivatives of 3-hydroxy-2-phenylisoindolinone RHONE-POULENC SA 13 Dec 1971 [14 Dec 1970] 57813/71 Heading C2C The invention comprises compounds of formula and their acid addition salts wherein X is halogen, C 1-4 alkyl or NO 2 , m is 0-4, Y is halogen, CN or NO 2 , or C 1-4 alkyl or alkoxy, and n is 0-5; R 1 is H or C 1-4 alkyl, and R 2 is C 1-4 alkyl or di-(C 1-4 alkyl)-amino-C 1-4 -alkyl, or NR 1 R 2 is a 5- or 6-membered monocyclic heterocyclic radical, possibly substituted by C 1-4 alkyl or hydroxyalkyl. These compounds may be prepared by reacting (a) a corresponding 3-hydroxy isoindolinone, in the form of its alkali metal salt, with ClCONR 1 R 2 , or (b) a corresponding phenyl/ 3-hydroxyindolinonyl carbonate with HNR 1 R 2 , the phenyl being optionally C 1-4 -alkyl-substituted. N-(3-cyanophenyl)phthalimide is also prepared. Therapeutic compositions having anticonvulsant and tranquillizing activity comprise compounds of the above formula, which may be administered orally, parenterally, rectally or topically.