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US5438050A Expired / Lapsed US ⏱️ 0.0 years remaining

Indolocarbazole derivatives, processes for their preparation and compositions containing them

Assignee: Goedecke GmbH
•
Filing: 1994-01-21
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Granted: 1995-08-01
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Expires: 2014-01-21
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Abstract

Abstract New indolocarbazoles of formula: ##STR1## or a pharmaceutically acceptable salt thereof, processes for their preparation, compositions containing, and methods for using the composition for the inhibition of protein kinases, such as protein kinase C, for the prevention and/or treatment of heart and blood vessel diseases such as thromboses, arterioscleroses, hypertension, or for inflammatory processes, allergies, cancers, viral diseases, and certain degenerative damages of the central nervous system are disclosed.

Inventors

  • 👤 Jurgen Kleinschroth
  • 👤 Johannes Hartenstein
  • 👤 Hubert Barth
  • 👤 Christoph Schachtele
  • 👤 Claus Rudolph
  • 👤 Gunter Weinheimer
  • 👤 Hartmut Osswald

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-04 11:00
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/12; C07D487/14

Claims Analysis

Total Claims: 17
Claim 1
Independent Claim 140 words
A compound of the formula ##STR11## or a pharmaceutically acceptable salt thereof wherein R 1 and R 2 taken together are alkylene of from 2-4 carbon atoms unsubstituted or substituted by hydroxyl, alkoxy of 1-4 carbon atoms or amino which is unsubstituted or is mono- or di-substituted by benzyl or by alkyl of from 1-4 carbon atoms; X and Y are each hydrogen or one is hydrogen and the other is hydroxyl or alkoxy of from 1-4 carbon atoms; R 3 , R 4 , R 5 , R 6 , and R 10 are each independently hydrogen, bromine, chlorine, methyl, ethyl, hydroxyl methoxy, 2-aminoethoxy, 3-aminopropoxy, 1-amino-2-propoxy, 2-dimethylaminoethoxy, 3-dimethylamino-1-propoxy, 3-dimethylamino-2-propoxy, or 2-diethylaminoethoxy; R 6 and R 7 are hydrogen with the proviso that at least one and as many as four of R 3 to R 4 are not hydrogen.
Claim 2
Dependent Claim 140 words
A compound of the formula ##STR11## or a pharmaceutically acceptable salt thereof wherein R 1 and R 2 taken together are alkylene of from 2-4 carbon atoms unsubstituted or substituted by hydroxyl, alkoxy of 1-4 carbon atoms or amino which is unsubstituted or is mono- or di-substituted by benzyl or by alkyl of from 1-4 carbon atoms; X and Y are each hydrogen or one is hydrogen and the other is hydroxyl or alkoxy of from 1-4 carbon atoms; R 3 , R 4 , R 5 , R 6 , and R 10 are each independently hydrogen, bromine, chlorine, methyl, ethyl, hydroxyl methoxy, 2-aminoethoxy, 3-aminopropoxy, 1-amino-2-propoxy, 2-dimethylaminoethoxy, 3-dimethylamino-1-propoxy, 3-dimethylamino-2-propoxy, or 2-diethylaminoethoxy; R 6 and R 7 are hydrogen with the proviso that at least one and as many as four of R 3 to R 4 are not hydrogen.
Claim 3
Dependent Claim 8 words
A compound described as 12, 13-butano-6,7,12,13-tetrahydro-5-oxo-5H-indolo [2,3-a]pyrrolo [3,4-c]carbazole.
Claim 4
Dependent Claim 8 words
A compound described as 12, 13-butano-6,7,12,13-tetrahydro-5-oxo-5H-indolo [2,3-a]pyrrolo [3,4-c]carbazole.
Claim 5
Dependent Claim 143 words
The compound of the formula ##STR12## or a pharmaceutically acceptable salt thereof wherein R 1 and R 2 taken together are alkylene of from 2-4 carbon atoms unsubstituted or substituted by hydroxyl, alkoxy of 1-4 carbon atoms or amino which is unsubstituted or is mono- or di-substituted by benzyl or by alkyl of from 1-4 carbon atoms; X and Y are each hydrogen or one is hydrogen and the other is hydroxyl or alkoxy of from 1-4 carbon atoms; R 3 , R 4 , R 5 , R 6 , R 9 and R 10 are each independently hydrogen, bromine, chlorine, alkyl of from 1-4 carbon atoms or alkoxy of from 1-4 carbon atoms; R 6 and R 7 are hydrogen with the proviso that at least one and as many as four of R 3 to R 10 are not hydrogen.
Claim 6
Dependent Claim 143 words
The compound of the formula ##STR12## or a pharmaceutically acceptable salt thereof wherein R 1 and R 2 taken together are alkylene of from 2-4 carbon atoms unsubstituted or substituted by hydroxyl, alkoxy of 1-4 carbon atoms or amino which is unsubstituted or is mono- or di-substituted by benzyl or by alkyl of from 1-4 carbon atoms; X and Y are each hydrogen or one is hydrogen and the other is hydroxyl or alkoxy of from 1-4 carbon atoms; R 3 , R 4 , R 5 , R 6 , R 9 and R 10 are each independently hydrogen, bromine, chlorine, alkyl of from 1-4 carbon atoms or alkoxy of from 1-4 carbon atoms; R 6 and R 7 are hydrogen with the proviso that at least one and as many as four of R 3 to R 10 are not hydrogen.
Claim 7
Dependent Claim 26 words
A pharmaceutical composition for treating blood vessel diseases comprising an effective amount of a compound according to claim 1 in admixture with a pharmaceutically acceptable carrier.
Claim 8
Dependent Claim 27 words
A method for treating diseases of blood vessels which comprises treating a host suffering therefrom with a pharmaceutical composition according to claim 1 in unit dosage form.
Claim 9
Dependent Claim 17 words
A compound according to claim 1 wherein R 5 or R 8 is methoxy, methyl, or chloro.
Claim 10
Dependent Claim 17 words
A compound according to claim 1 wherein R 4 or R 9 is methoxy, methyl, or chloro.
Claim 11
Dependent Claim 20 words
A compound according to claim 1 wherein R 5 and R 8 are both methoxy, hydroxyl, methyl, bromo, or chloro.
Claim 12
Dependent Claim 19 words
A compound according to claim 1 wherein R 4 and R 9 are both methoxy, methyl, bromo, or chloro.
Claim 13
Dependent Claim 24 words
A compound according to claim 1 wherein R 4 and R 5 or R 8 and R 9 are the same and are methoxy.
Claim 14
Dependent Claim 35 words
A compound according to claim 1 wherein R 4 , R 5 , R 8 , and R 9 are methoxy and R 3 , R 6 , R 7 and R 10 are hydrogen.
Claim 15
Dependent Claim 22 words
A pharmaceutical composition comprising an effective amount of a compound as defined in claim 1 in combination with a pharmaceutically acceptable carrier.
Claim 16
Dependent Claim 32 words
A method for treating and/or preventing heart and blood vessel diseases which comprises administering to a mammal in need of such treatment a composition according to claim 12 in unit dosage form.
Claim 17
Dependent Claim 26 words
A compound according to claim 1 wherein R 1 and R 2 when taken together form a butylene or a propylene radical unsubstituted or hydroxy substituted.

References Cited (Backward Citations)

US4785085A Cited
US4808613A Cited
US4923986A Cited

USPTO Annuity & Maintenance Windows

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3.5 Years (Year 4) 1998-07-31 1999-01-30 1999-08-01 $2000.00 Window Closed / Lapsed
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