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1. (WO1997019081) SYNTHETIC METAL-SUBSTITUTED BACTERIOCHLOROPHYLL DERIVATIVES AND USE THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/019081 International Application No.: PCT/IL1996/000161
Publication Date: 29.05.1997 International Filing Date: 24.11.1996
Chapter 2 Demand Filed: 17.06.1997
IPC:
A61K 41/00 (2006.01) ,C07D 487/22 (2006.01) ,C07D 491/22 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
41
Medicinal preparations obtained by treating materials with wave energy or particle radiation
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
22
in which the condensed system contains four or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
22
in which the condensed system contains four or more hetero rings
Applicants:
YEDA RESEARCH AND DEVELOPMENT CO. LTD. [IL/IL]; at the Weizmann Institute of Science P.O. Box 95 76100 Rehovot, IL (AllExceptUS)
SCHERZ, Avigdor [IL/IL]; IL (UsOnly)
SALOMON, Yoram [IL/IL]; IL (UsOnly)
SCHEER, Hugo [DE/DE]; DE (UsOnly)
HARTWICH, Gerhard [DE/DE]; DE (UsOnly)
BRANDIS, Alexander [IL/IL]; IL (UsOnly)
Inventors:
SCHERZ, Avigdor; IL
SALOMON, Yoram; IL
SCHEER, Hugo; DE
HARTWICH, Gerhard; DE
BRANDIS, Alexander; IL
Agent:
BEN-AMI, Paulina; Yeda Research and Development Co. Ltd. at the Weizmann Institute of Science P.O. Box 95 76100 Rehovot, IL
Priority Data:
11612624.11.1995IL
Title (EN) SYNTHETIC METAL-SUBSTITUTED BACTERIOCHLOROPHYLL DERIVATIVES AND USE THEREOF
(FR) DERIVES DE BACTERIOCHLOROPHYLLE SUBSTITUES PAR UN METAL SYNTHETIQUE ET LEUR UTILISATION
Abstract:
(EN) Metalated bacteriochlorophylls of the formula [M]-BChl, wherein M is a metal atom selected from divalent Pd, Co, Ni, Cu, Zn and Mn, trivalent Fe, Mn and Cr, and tetravalent Sn and Pt, and Bchl represents the residue of a demetalated natural or synthetic bacteriochlorophyll derivative, are prepared by transmetalation of the corresponding [Cd]-BChl derivatives carrying at position 173 a group COOR1, wherein R1 is a C1 - C25 hydrocarbyl residue, and further optional transesterification of the 173-COOR1 of the obtained [M]-BChl. The compounds are for use in photodynamic therapy and diagnosis and for killing cells and infectious agents, e.g. bacteria and viruses, both in biological products and in living tissue. Preferred compounds are those of formula (I') wherein R'1 is a residue selected from (i) optionally substituted hydrocarbyl; (ii) hydroxy-containing amino acid or peptide or a derivative thereof; and (iii) hydroxy-containing peptide or a cell-specific ligand, e.g. peptide or protein, linked to the COO-group via a spacer as defined in (i).
(FR) L'invention se rapporte à des bactériochlorophylles de la formule [M]-BChl ayant subi une métallation, formule dans laquelle M représente un atome de métal sélectionné parmi Pd, Co, Ni, Cu, Zn et Mn divalents, Fe, Mn et Cr trivalents, et Sn et Pt tétravalents, et Bchl représente le reste d'un dérivé de bactériochlorophylle natuel ou synthétique ayant subi une démétallation. Ces bactériochlorophylles sont préparés par transmétallation de dérivés correspondants de [Cd]-BChl supportant à la position 173 un groupe COOR1 dans lequel R1 représente un reste d'hydrocarbyle en C1 - C25, et ensuite par une transésterification éventuelle de 173-COOR1 de [M]-BChl obtenu. Ces composés sont destinés à être utilisés en thérapie photodynamique et en diagnostic et dans l'élimination de cellules et d'agents infectieux tels que des bactéries et des virus, à la fois dans des produits biologiques et dans des tissus vivants. Les composés préférés sont ceux de la formule (I') dans laquelle R'1 est un reste sélectionné parmi (i) hydrocarbyle éventuellement substitué; (ii) un acide aminé contenant hydroxy ou un peptide ou un dérivé de celui-ci; et (iii) un peptide contenant hydroxy ou un ligand spécifique des cellules tel qu'un peptide ou une proteine lié au groupe COO par un espaceur tel que défini dans (i).
Designated States: AM, AT, AU, BB, BG, BR, BY, CA, CH, CN, CZ, DE, DK, EE, ES, FI, GB, GE, HU, IL, IS, JP, KE, KG, KP, KR, KZ, LK, LR, LT, LU, LV, MD, MG, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, TJ, TM, TT, UA, UG, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
NO19982348NZ322179SG53725VN2640IL124502EP0863903
RU02193038VN2340US6333319JP2000500763CN1207741CA2237056
DE000069637149PT863903AU1996075857DK0863903