Procyte Corporation

Light Sciences Oncology Inc.

Health Research, Inc.

Purdue Pharmaceutical Products L.p.

Alexander J Pallenberg

Leon Xu

Leonard M Patt

Ronald E Trachy

Ravindra Kumar Pandey

Thomas J Dougherty

An improved two stage reaction process for production of mono-L-aspartyl chlorin e. In a first stage, the activation reaction between chlorin eand a carbodiimide produces a previously unknown anhydride in an activation reaction product (Formula I). This reaction product is purified to remove a significant proportion of the precursors of di-L-aspartyl chlorin e. The purified activation reaction product contains a higher concentration of the previously unknown anhydride. This purified reaction product is used in a second stage: a coupling reaction of the purified activation reaction product with aspartate. The coupling reaction produces a coupling reaction product that has significantly reduced di-L-aspartyl chlorin e6 concentration. This reduced di-L-aspartyl chlorin e6 concentration facilitates purification of mono-L-aspartyl chlorin e6 from the coupling reaction mixture. 

Compositions and methods of making a photoactive agent

A composition of matter of an anhydride of formula 1 below and an improved two stage reaction process for production of mono-L-aspartyl chlorin e, utilizing the anhydride: 

An improved two stage reaction process for production of mono-L-aspartyl chlorin e. In a first stage, the activation reaction between chlorin eand a carbodiimide produces a previously unknown anhydride in an activation reaction product. This reaction product is purified to remove a significant proportion of the precursors of di-L-aspartyl chlorin e. The purified activation reaction product contains a higher concentration of the previously unknown anhydride. This purified reaction product is used in a second stage: a coupling reaction of the purified activation reaction product with aspartate. The coupling reaction produces a coupling reaction product that has significantly reduced di-L-aspartyl chlorin e6 concentration. This reduced di-L-aspartyl chlorin e6 concentration facilitates purification of mono-L-aspartyl chlorin e6 from the coupling reaction mixture.

A process for the preparation of pyropheophorbide a and its derivatives, including 3-devinyl-3-(1'-hexyloxy)ethyl-pyropheophorbide-a, otherwise known as HPPH, is provided. The process involves treating chlorin e, in the form of its trimethyl ester, with a base, followed by heating to give pyropheophorbide a, which is converted to HPPH by treatment with acid, followed by hexyl alcohol under basic conditions.

Efficient synthesis of pyropheophorbide a and its derivatives

Peptide-copper complexes are disclosed which stimulate the growth of hair on warm-blooded animals. In one aspect of this invention, the peptide-copper complexes are dipeptides or tripeptides chelated to copper at a molar ratio ranging from about 1:1 to 3:1, with the second position of the peptide from the amino terminus being histidine, arginine or a derivative thereof. The peptide-copper complexes may be formulated for administration by, for example, topical application or injection. Any affliction associate with hair loss, including hair loss associated with both androgenetic and secondary alopecia, may be treated with the peptide-copper complexes of this invention.

Stimulation of hair growth by peptide copper complexes

Zinc(II) complexes and methods relating thereto are disclosed. The zinc(II) complexes comprise a zinc(II) ion complexed by a multi-dentate ligand. Methods of this invention include the use of the zinc(II) complexes as anti-viral agents and/or as anti-inflammatory agents. Methods of this invention also include inhibition of viral infection, as well as inhibiting transmission of sexually transmitted diseases. Exemplary zinc(II) complexes include zinc(II):neocuproine (2:1) and zinc(II):bathocuproine disulfonic acid (2:1).

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Duvall, WA, United States of America

Alexander J Pallenberg