Alkyl and aralkyl-substituted pyrrolocarbazole derivatives that

Details Alkyl and aralkyl-substituted pyrrolocarbazole derivatives that Alkyl and aralkyl-substituted pyrrolocarbazole derivatives that

1996-11-08

1998-03-17

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

5142328, 514338, 514410, 544142, 546 41, 5462767, 548423, A61K 3141, A61K 3144, C07D48704

Patent

active

057287090

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 PCT/JP96/00557 filed Mar. 7, 1996.
1. Technical Field
The present invention relates to novel pyrrolocarbazole derivatives and pharmaceutically acceptable salts thereof useful as a therapeutic agent for thrombocytopenia.
2. Background Art
A decrease of platelets in number due to various hematopoietic disorders causes serious symptoms including a bleeding tendency. At present, platelet transfusion is considered to be effective against a decrease in platelets. However, a sufficient amount of platelets is not always supplied. Other than platelet transfusion, interleukin (IL) 6, IL-11, c-Mpl ligand and indolocarbazole derivatives are known to stimulate platelet production (Blood, 75, 1602 (1990); Blood, 81, 901 (1993); Nature, 369, 533 (1994); and WO94/06799).
Pyrrolocarbazole derivatives are known to have inhibiting activity against protein kinase C and antitumor activity (JP,2-142791,A and JP,4-178387,A).
However, it is unknown any type of pyrrolocarbazole derivatives stimulate platelet production.


DISCLOSURE OF THE INVENTION

The present invention relates to pyrrolocarbazole derivatives represented by Formula (I) and pharmaceutically acceptable salts thereof: ##STR2## wherein R.sup.1 is lower alkyl or aralkyl; R.sup.2 is hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, or substituted or unsubstituted aralkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different, and are hydrogen, halogen, nitro, substituted or unsubstituted lower alkanoyl, NR.sup.9 R.sup.10 {wherein R.sup.9 and R.sup.10 may be the same or different, and are hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, aroyl, lower alkoxycarbonyl, aralkyloxycarbonyl or an amine acid residue in which a hydroxyl group in a carboxylic acid is removed (an amine group of the amine acid may be protected by a protective group)} or OR.sup.11 (wherein R.sup.11 is hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, aroyl, or substituted or unsubstituted aralkyl, or heteroaralkyl); R.sup.8 is hydrogen or is combined with R.sup.3 to form --CONR.sup.12 -- (wherein R.sup.12 is hydrogen or substituted or unsubstituted lower alkyl); and when R.sup.1 is benzyl, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are not simultaneously hydrogen.
Hereinafter, compounds represented by Formula (I) are referred to as Compound (I). The same shall apply to compounds represented by other formulae.
In the definitions of the groups in Compound (I), the lower alkyl means a straight-chain or branched alkyl group having 1 to 6 carbon atoms such as methyl, ethyl, propyl, isopropyl, butyl, iso-butyl, sec-butyl, tert-butyl, pentyl, neopentyl and hexyl. The substituted lower alkyl has 1 to 3 substituents, which may be the same or different, and, for example, are hydroxyl, halogen, lower alkanoyl, lower alkoxy, carboxy, lower alkoxycarbonyl, p-toluenesulfonyloxy, NR.sup.13 R.sup.14 {wherein R.sup.13 and R.sup.14 may be the or different, and are hydrogen, lower alkyl, cycloalkyl, or aralkyloxycarbonyl, or R.sup.13 and R.sup.14 are combined together to form a heterocyclic group containing N therein (the heterocyclic group may contain an oxgen atom, a sulfur atom, or another nitrogen atom)}, CONR.sup.15 R.sup.16 {wherein R.sup.15 and R.sup.16 may be the same or different, and are hydrogen or lower alkyl, or R.sup.15 and R.sup.16 are combined together to form a heterocyclic group having N therein (the heterocyclic group may contain an oxygen atom, sulfur atom or another nitrogen atom)}, NR.sup.17 R.sup.18 R.sup.19 Hal {wherein R.sup.17 and R.sup.18 may be the same or different, and are hydrogen or lower alkyl, or R.sup.17 and R.sup.18 are combined together to form a heterocyclic group having N therein (the heterocyclic group may contain an oxygen atom, a sulfur atom, or another nitrogen atom); R.sup.19 is lower alkyl; and Hal is a chlorine, bromine, or iodine atom}, trimethylsilylethoxy, or the like. The alkyl moiety of t

REFERENCES:
patent: 4912107 (1990-03-01), Kleinschroth et al.
patent: 5166204 (1992-11-01), Nagai et al.
Bio. & Medicinal Chem. Letters, vol. 5, No. 11 (1995) 1167-69.

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