Water soluble bis-dioxopiperazine derivatives
AssigneeZenyaku Kogyo Kabushiki Kaisha
InventorsMuneaki Takase, Toshiharu Narita, Toshihiko Komatsu
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Abstract
A pharmaceutically-acceptable acid addition salt of a bis-dioxopiperazine derivative of the formula (I): ##STR1## which derivative exhibits anti-tumor potency and is water-soluble, wherein R.sup.1 is a C.sub.1-6 alkyl group, R.sup.2 represents a hydrogen atom or: ##STR2## R.sup.3 represents a hydrogen atom, a C.sub.1-6 alkyl group or (CH.sub.2).sub.n A, wherein A respresents carboxyl, benzyloxycarbonyl, mercapto, amino, benzyloxycarbonylamino or: ##STR3## and n is an integer of 1, 2, 3 or 4, and R.sup.4 represents a hydrogen atom or is coupled with R.sup.3 into a 5-membered ring, which may contain one sulfur atom as an additional ring heteroatom.
Claims16
A pharmaceutically acceptable acid addition salt of a bis-dioxopiperazine derivative represented by the formula (I):
- ##STR13## wherein R.sup.1 represents a C.sub.1-6 alkyl group, R.sup.2 represents a hydrogen atom or:
- ##STR14## and R.sup.3 is coupled with R.sup.4 into a 5-membered saturated ring, which either contains no additional ring heteroatoms or contains one sulfur atom as an additional ring heteroatom.
A synthetic intermediate of a bis-dioxopiperazine derivative, represented by the formula (II):
- ##STR16## wherein R.sup.1 represents a C.sub.1-8 alkyl group, R.sup.5 represents a hydrogen atom or:
- ##STR17## R.sup.6 is coupled with R.sup.7 into a 5-membered saturated ring, which may contain one sulfur atom as an additional ring heteroatom, and
- R.sup.8 represents a protecting group for the amino group.
Dependencies are inferred from the claim text.