Provided are novel treprostinil salts as well as methods for making treprostinil salts.

Provided are a compound represented by the following General Formula (A1-1), a method for producing the same, and the use of the compound:

##STR00001##

wherein R.sup.5 and R.sup.6 represent a hydrogen atom or an alkyl group, L.sup.1 and L.sup.2 represent an alkylene group having 1 to 6 carbon atoms, Sp.sup.a and Sp.sup.b represent a single bond or a divalent linking group, R.sup.11 and R.sup.21 represent a substituent, and v1 and w1 are an integer of 0 to 4. Further provided that a structure represented by (R.sup.11).sub.v1-benzen ring/cyclopentadiene skeleton/naphthalene ring-(R.sup.21).sub.w1 is not line-symmetrical, where “/” represents that two rings described on left and right sides of the structure are fused.

Provided are a compound represented by the following General Formula (A1-1), a method for producing the same, and the use of the compound:

##STR00001##

wherein R.sup.5 and R.sup.6 represent a hydrogen atom or an alkyl group, L.sup.1 and L.sup.2 represent an alkylene group having 1 to 6 carbon atoms, Sp.sup.a and Sp.sup.b represent a single bond or a divalent linking group, R.sup.11 and R.sup.21 represent a substituent, and v1 and w1 are an integer of 0 to 4. Further provided that a structure represented by (R.sup.11).sub.v1-benzen ring/cyclopentadiene skeleton/naphthalene ring-(R.sup.21).sub.w1 is not line-symmetrical, where “/” represents that two rings described on left and right sides of the structure are fused.

The present invention relates to compounds of formula (I): including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of, for example, cancer.

The present invention relates to compounds of formula (I): including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of, for example, cancer.

This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.

This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.

This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.

Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates. ##STR00001##

Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates. ##STR00001##