Tricyclic dicarbonyl derivatives
First Claim
1. A compound formula ##STR15## wherein R1 and R2 each independently is hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R3 R4 NS(O)2 -- and R3 and R4 are lower alkyl, andR2 can additionally be morpholino or thiomorpholino;
- a 5- or 6-membered heterocycle with 1-3N atoms, unsubstituted or substituted by lower alkyl, hydroxy, amino or the group --CH2 NHCH3 ;
a bicyclic heterocycle with 1-3N atoms;
or a group --NR5 R6 or --OR5 in which R5 and R6 can be the same or different and be hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl,as well as pharmaceutically usable salts of compounds of formulas Ia or Ib, excluding 2,3,5,6-tetrahydro- 1,2,4!-triazolo 1,5-c!quinazoline-2,5-dione.
2 Assignments
0 Petitions
Accused Products
Abstract
Compounds of general formula (Ia), (Ib) and (II), wherein R1 and R2 each independently signify hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R3 R4 NS(O)2 -- and R3 and R4 signify lower alkyl, and R2 can additionally signify morpholino or thiomorpholino, a 5- or 6-membered heterocycle with 1-3N atoms optionally substituted by lower alkyl, hydroxy, amino or the group --CH2 NHCH3, a bicyclic heterocycle with 1-3N atoms or a group --NR5 R6 or --OR5 in which R5 and R6 can be the same or different and signify hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl, and X in formula (II) signifies --CH═CH--, --CH═N--, --NH--, --CO-- or --O--, as well as pharmaceutically usable salts of compounds of general formula (Ia), (Ib) and (II). They can be used for the treatment or prevention of illnesses, especially for the treatment or prevention of ischemia, hypoglycaemia, hypoxia, cerebral vascular spasms, spasticity, trauma, hemorrhagia, infection (viral, bacterial, amoebic, prional), epileptic seizures, autoimmune diseases, withdrawal symptoms, Alzheimer'"'"'s disease, Parkinson'"'"'s disease, amyotrophic lateral sclerosis, Huntington'"'"'s disease, intoxications, olivoponto-cerebellar atrophy, spinal cord injuries, schizophrenia, depressions, anxiety states, dependence, pains,autism and mental retardation.
14 Citations
16 Claims
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1. A compound formula ##STR15## wherein R1 and R2 each independently is hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R3 R4 NS(O)2 -- and R3 and R4 are lower alkyl, and
R2 can additionally be morpholino or thiomorpholino; - a 5- or 6-membered heterocycle with 1-3N atoms, unsubstituted or substituted by lower alkyl, hydroxy, amino or the group --CH2 NHCH3 ;
a bicyclic heterocycle with 1-3N atoms;
or a group --NR5 R6 or --OR5 in which R5 and R6 can be the same or different and be hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl,as well as pharmaceutically usable salts of compounds of formulas Ia or Ib, excluding 2,3,5,6-tetrahydro- 1,2,4!-triazolo 1,5-c!quinazoline-2,5-dione. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13)
- a 5- or 6-membered heterocycle with 1-3N atoms, unsubstituted or substituted by lower alkyl, hydroxy, amino or the group --CH2 NHCH3 ;
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14. A pharmaceutical composition comprising an effective amount of a compound of ##STR16## wherein R1 and R2 each independently is hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R3 R4 NS(O)2 -- and R3 and R4 are lower alkyl, and
R2 can additionally be morpholino or thiomorpholino; - a 5- or 6-membered heterocycle with 1-3N atoms, unsubstituted or substituted by lower alkyl, hydroxy, amino or the group --CH2 NHCH3 ;
a bicyclic heterocycle with 1-3N atoms;
or a group --NR5 R6 or --OR5 in which R5 and R6 can be the same or different and be hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl,as well as pharmaceutically usable salts of compounds of formulas Ia or Ib, excluding 2,3,5,6-tetrahydro- 1,2,4!-triazolo 1,5-c!quinazoline-2,5-dione. - View Dependent Claims (15, 16)
- a 5- or 6-membered heterocycle with 1-3N atoms, unsubstituted or substituted by lower alkyl, hydroxy, amino or the group --CH2 NHCH3 ;
Specification
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- Resources
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Current AssigneeHoffmann-La Roche Incorporated (Roche Holding AG)
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Original AssigneeHoffmann-La Roche Incorporated (Roche Holding AG)
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InventorsGross, Laurence, Heitz Neidhart, Marie-Paule, Riemer, Claus, Godel, Thierry, Wyler, Rene, Buttelmann, Bernd
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Primary Examiner(s)Shah, Mukund J.
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Assistant Examiner(s)WONG, KING
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Application NumberUS08/737,240Time in Patent Office368 DaysField of Search544/251, 514/267US Class Current514/267CPC Class CodesA61P 17/00 Drugs for dermatological di...A61P 25/00 Drugs for disorders of the ...A61P 25/04 Centrally acting analgesics...A61P 25/18 Antipsychotics, i.e. neurol...A61P 25/20 Hypnotics; SedativesA61P 25/24 AntidepressantsA61P 25/26 Psychostimulants, e.g. nico...A61P 25/28 for treating neurodegenerat...A61P 3/08 for glucose homeostasis pan...A61P 39/02 AntidotesA61P 9/00 Drugs for disorders of the ...A61P 9/08 Vasodilators for multiple i...A61P 9/10 for treating ischaemic or a...C07D 471/04 Ortho-condensed systemsC07D 487/04 Ortho-condensed systems
