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    • 72. 发明专利
    • RO63749A
    • 1979-01-15
    • RO7842074
    • 1974-04-15
    • BAYER AG
    • MOELLER EIKEMENG KARLWEHINGER EGBERTHORSTMANN HARALD
    • A61K31/415C07D231/18A61P7/02A61P7/10A61P9/12C07D231/20C07D231/24C07D231/52C07D401/06C07D231/12
    • 1429141 Pyrazolin-5-ones BAYER AG 16 April 1974 [17 April 1973 19 Dec 1973] 16507/74 Heading C2C The invention comprises compounds of formula (including tautomers thereof, especially when R is amino), wherein R is H, amino, alkyl, alkenyl, CF 3 or Ph; R 1 is H, alkyl, alkenyl or an optionally substituted aryl or aralkyl radical; R 2 is an alkyl group; and R 3 is a pyridyl radical or an aryl radical carrying 1 or 2 identical or different substituents, which are selected from halogen, CF 3 , alkyl, alkenyl, and alkoxy radicals, or carrying one mono- or di-alkylamino, CF 3 O, nitro, nitrile, carbamoyl, alkyl- or dialkylcarbamoyl, sulphamyl, or alkyl- or dialkylsulphamyl radical, or a group -B, -CO.B or -SO 2 .B (in which B is a saturated ring containing a nitrogen atom in the 1-position) or a -SO n alkyl group (in which n=0, 1 or 2), optionally together with 1 or 2 substituents selected from alkyl, alkenyl, alkoxy, halogen and CF 3 , or carrying none or 1 only of these substituents and a fused branched or unbranched, saturated or unsaturated 5-, 6- or 7- membered ring optionally containing 1 or 2 oxygen or sulphur atoms. In examples, these compounds are prepared by (a) reacting R 2 R 3 CHNHNH 2 with an appropriate ring-forming co-reactant, (2) replacing a compound in which R is halogen, by amino, (3) hydrolysing a compound in which R is (e.g.) NHCO 2 Et, or (4) introducing the R 2 R 3 CH group by N 1 -substitution. Therapeutic compositions having diuretic, saluretic, antihypertensive and antithrombotic activity comprise compounds of the above formula, and may be administered orally, parenterally, rectally, topically, or by spray.
    • 74. 发明专利
    • NO138530B
    • 1978-05-12
    • NO741365
    • 1974-04-16
    • BAYER AG
    • MOELLER EIKEMENG KARLWEHINGER EGBERTHORSTMANN HARALD
    • A61K31/415A61P7/02A61P7/10C07D231/18A61P9/12C07D231/20C07D231/24C07D231/52C07D401/06
    • 1429141 Pyrazolin-5-ones BAYER AG 16 April 1974 [17 April 1973 19 Dec 1973] 16507/74 Heading C2C The invention comprises compounds of formula (including tautomers thereof, especially when R is amino), wherein R is H, amino, alkyl, alkenyl, CF 3 or Ph; R 1 is H, alkyl, alkenyl or an optionally substituted aryl or aralkyl radical; R 2 is an alkyl group; and R 3 is a pyridyl radical or an aryl radical carrying 1 or 2 identical or different substituents, which are selected from halogen, CF 3 , alkyl, alkenyl, and alkoxy radicals, or carrying one mono- or di-alkylamino, CF 3 O, nitro, nitrile, carbamoyl, alkyl- or dialkylcarbamoyl, sulphamyl, or alkyl- or dialkylsulphamyl radical, or a group -B, -CO.B or -SO 2 .B (in which B is a saturated ring containing a nitrogen atom in the 1-position) or a -SO n alkyl group (in which n=0, 1 or 2), optionally together with 1 or 2 substituents selected from alkyl, alkenyl, alkoxy, halogen and CF 3 , or carrying none or 1 only of these substituents and a fused branched or unbranched, saturated or unsaturated 5-, 6- or 7- membered ring optionally containing 1 or 2 oxygen or sulphur atoms. In examples, these compounds are prepared by (a) reacting R 2 R 3 CHNHNH 2 with an appropriate ring-forming co-reactant, (2) replacing a compound in which R is halogen, by amino, (3) hydrolysing a compound in which R is (e.g.) NHCO 2 Et, or (4) introducing the R 2 R 3 CH group by N 1 -substitution. Therapeutic compositions having diuretic, saluretic, antihypertensive and antithrombotic activity comprise compounds of the above formula, and may be administered orally, parenterally, rectally, topically, or by spray.
    • 77. 发明专利
    • 3-AMINO-PYRAZOLONES-%5<. 3-AMINO-PYRAZOLONES-%5<.
    • AU5705173A
    • 1974-12-19
    • AU5705173
    • 1973-06-18
    • BAYER AG
    • HORSTMANN HARALDMENG KARLWEHINGER EGBERT
    • C07D231/44C07D231/52C07D49/16A61K27/00
    • 1391051 Aminopyrazolones BAYER AG 22 June 1973 [23 June 1972] 29785/73 Heading C2C The invention comprises compounds of the tautomeric formulae and their salts, wherein R is (a) a phenyl radical carrying one or two identical or different substituents selected from alkyl, phenyl, trifluoromethyl, trifluoromethoxy, nitro, nitrile, carbamoyl, sulphamoyl, alkylamino, fluorine, bromine and iodine radicals but cannot be a phenyl radical carrying trifluoromethyl only as one substituent, or (b) a phenyl radical carrying an annellated, branched or unbranched, saturated or unsaturated, five to seven-membered isocyclic or heterocyclic ring (the heterocyclic ring containing one or more oxygen and/or sulphur atoms); or (c) a phenyl radical carrying as substituent an SO n -alkyl group (n = 0, 1 or 2), an alkoxy group, or an -O-(CH 2 ) n -N(alkyl) 2 group (n = 2 or 3); or (d) a phenyl radical carrying two identical substituents selected from alkoxy and trifluoromethyl groups; or (e) a phenyl radical carrying two different substituents selected from alkyl, phenyl, halogen, alkoxy, trifluoromethyl, trifluoromethoxy, alkylamino, nitrile, carbamoyl, sulphamoyl, -SO n alkyl (n = 0, 1 or 2) and nitro radicals; or (f) a trichlorophenyl radical; or (g) a naphthyl radical carrying one or two identical or different substituents selected from halogen atoms and alkyl groups; or (h) an unsubstituted #-naphthyl, anthryl or phenanthryl radical. These compounds are prepared by reacting RCH 2 NHNH 2 with CNCH 2 COX or where X is OH, alkoxy, aralkoxy, NH 2 or alkylamino, and Y is alkoxy, aryloxy, aralkoxy, alkylmercapto, aralkylmercapto or NH 2 . Therapeutic compositions having diuretic, saluretic and antihypertensive activity comprise compounds of the above formulae, and may be administered orally, parenterally, rectally, topically or by means of a spray.