Cytopharm, Inc.

Emanuel Vogel

Alexander D Cross

Martin Muller

Thomas Benninghaus

Clemens Richert

Giulio Jori

Matthias Kocher

Martin Mueller

Otto Halpern

Afssaneh Rahbar

Norbert Jux

Peter A Koch

Wolfgang Hennig

Eduardo Rodriguez-Val

Stefan Boehm

Reiner Deponte

Coupling two moles of a 2-halopyrrole in the presence of an inert aromatic solvent and a catalytically effective amount of a substantially pure copper catalyst provides high yields of the corresponding bipyrrole.

High-yielding ullmann reaction for the preparation of bipyrroles

Novel 9-substituted porphycene compounds are useful in photodynamic therapy.

9-substituted porphycenes

Porphycene compounds having the formula ##STR1## wherein each R is --(CH.sub.2).sub.n --X, n=1-10, X is OR.sup.1 and R.sup.1 is alkyl, aralkyl or aryl are useful as photosensitizer compounds in photodynamic therapy.

9-Substituted porphycenes

A porphycene having the structure ##STR1## wherein each R.sup.1 is, independently, (a) --(CH.sub.2).sub.n --X, where n=1-4, X is OR.sup.2 and R.sup.2 is C.sub.1-6 alkyl, aralkyl or aryl; CN; OH; OSO.sub.2 R.sup.2 ; NH.sub.2 ; NHR.sup.2 ; NR.sub.2.sup.2 ; SH; SR.sup.2 ; S(O).sub.1-2 R.sup.2 ; COOH; CO.sub.2 R.sup.2 ; C(O)NH.sub.2 ; C(O)NHR.sup.2 ; C(O)NR.sub.2.sup.2 ; halogen; or CHO;

Porphycene compounds for photodynamic therapy

A porphycene having the structure ##STR1## wherein each R.sup.1 is, independently, (a) --(CH.sub.2).sub.n --X, where n= 1-4, X is OR.sup.2 and R.sup.2 is C.sub.1-6 alkyl, aralkyl or aryl; CN; OH; OSO.sub.2 R.sup.2 ; NH.sub.2 ; NHR.sup.2 ; NR.sup.2.sub.2 ; SH; SR.sup.2 ; S(O).sub.1-2 R.sup.2 ; COOH; CO.sub.2 R.sup.2 ; C(O)NH.sub.2 ; C(O)NHR.sup.2 ; C(O)NR.sup.2.sub.2 ; halogen; or CHO;

New porphycene compounds useful as photodynamic therapy agents. The porphycene compounds have an active group capable of binding to proteins and peptides and facilitating decomposition of the porphycenes following therapy.

Derivatives of porphycene for photodynamic therapy of cancer

Dihydro- and tetrahydro-acetylene-cumulene porphycene compounds having the structure shown below ##STR1## are useful as photogynamic therapy agents.

Acetylene-cumulene porphycene compounds for photodynamic therapy

The therapeutic compositions of this invention comprise one or more porphycene compounds incorporated within liposomes. The method of this invention for treating cancer comprises administering a therapeutically effective amount of a porphycene derivative to a patient, and exposing an affected body area of the patient to a therapeutically sufficient amount of light having a wavelength of from 600 to 950 nm.

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Cologne, Germany

Emanuel Vogel