Yeda Research and Develpment & Co. Ltd

Hugo Scheer

Avigdor Scherz

Yoram Salomon

Alexander Brandis

Ohad Mazor

Gerhard Hartwich

Nina Kammhuber

The invention provides anionic water-soluble tetracyclic and pentacyclic bacteriochlorophyll derivatives (Bchls) containing at least one, preferably two or three, negatively charged groups and/or acidic groups that are converted to negatively charged groups at the physiological pH, preferably Bchls having a group COO&#x3c;&#x2212;&#x3e;, COS&#x3c;&#x2212;&#x3e;, SO3&#x3c;&#x2212;&#x3e;, PO3&#x3c;2&#x2212;&#x3e;, COOH, COSH, SO3H, and/or PO3H2 bound through an ester or amide bond to one or more of the positions 17&#x3c;3&#x3e;, 13&#x3c;3&#x3e;, and 3&#x3c;2&#x3e; of the tetracyclic or pentacyclic Bchl molecule, for photodynamic therapy and diagnosis.

Water-soluble anionic bacteriochlorophyll derivatives and their uses

Novel C-13-COXR, C-17-COXRand C-13-COXR, C-17-COXRderivatives of chlorophyll and bacteriochlorophyll compounds are provided wherein X is O, S or N and Rand R, the same or different, may be an optionally substituted hydrocarbyl, amino acid, peptide, protein or saccharide radical. The compounds are for use in photodynamic therapy (PDT), for diagnosis of tumors, and for killing cells and infectious agents such as bacteria and virus, both in biological products and in living tissues.

Chlorophyll and bacteriochlorophyll esters, their preparation and pharmaceutical compositions comprising them

Palladium-substituted Bacteriochlorophyll derivatives are administered to a subject suspected of having a tumor and the patient is then irradiated and the fluorescence of the suspected area is measured. A high fluorescence indicates a tumor site. A preferred derivative is Pd-Bacteriopheophorbide a.

Method for tumor diagnosis comprising administering of palladium-substituted bacteriochlorophyll derivatives

Palladium-substituted Bacteriochlorophyll derivatives of formula (I), wherein A represents OH, OR , &mdash;O&mdash;(CH ) &mdash;Y, &mdash;S&mdash;(CH ) &mdash;Y, &mdash;NH&mdash;(CH ) &mdash;Y, &mdash;O&mdash;(CH ) &mdash;NH , &mdash;O&mdash;(CH ) &mdash;OH, &mdash;NH&mdash;(CH ) &mdash; N o, X&mdash;, &mdash;NH0(CH ) &mdash;NH&boxH;BOC or &mdash;N&mdash;(CH &mdash;CH&boxH;CH ) ; wherein R represents Na , K , (Ca ) , (Mg ) , Li , NH , NH &mdash;C(CH OH) NH &mdash;CH &mdash;(CHOH) &mdash;CH OH, NH (CH )&mdash;CH &mdash;(CHOH) &mdash;CH OH or N(C H ) ; R represents H, OH or COOR , wherein R is C -C alkyl or C -C cycloalkl; R represents H, OH or C -C alkyl or alkoxy; n is 1, 2, 3, 4, 5 or 6, Y is &mdash;NR&prime; R&prime; R&prime; , X-wherein R&prime; , R&prime; and R&prime; independently from each other represent &mdash;CH or &mdash;C H ; X is F, Cl, Br or 1, n&prime; is 1, 2, 3 or 4 and their oxidized forms, are useful in the field of photodynamic therapy (PDT).

Palladium-substituted bacteriochlorophyll derivatives and use thereof

The present invention relates to a new method of preparation of metalated bacteriochlorophyll derivatives for use in methods of in vivo photodynamic therapy (PDT) and diagnosis and in vitro photodynamic killing of viruses and microorganisms, and to some novel metal-substituted bacteriochlorophyll derivatives.

Growing community of inventors

Blonhofen, Germany

Hugo Scheer