EP0233701A2
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Porphyrin derivatives
Assignee: Hamari Chemicals Ltd
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Filing: 1987-01-16
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Granted: —
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Expires: 2007-01-16
Abstract
Abstract Novel porphyrin derivatives of the general formula: wherein R 1 each independently denotes a hydrogen, a C 1 -C 4 alkyl group or an ethenyl group, and R 2 each independently denotes COZ(C m H 2m )Q, COZCH(C m H 2m Q) 2 , -CH 2 -Q [wherein ' Z is 0, S or NH, m is an interger of 1 to 23, and 0 is a di-(C 1 -C 4 alkyl)amino group or tri-(C 1 -C 4 alkyl)ammonium halide group] or (wherein X is a halogen); or R 1 each independently denotes -C 2 H 4 -Q (wherein Q is the same as defined above). -C 2 H 4 - (wherein X is the same as defined above), and R 2 each independently denotes a carboxyl group or a C 1 -C 4 alkoxycarbonyl group, exhibit affinity and photosensitizing activity for cancer cells and can be employed for diagnosing and treating cancer under irradiation of laser light.
Inventors
- 👤 Yozo Fukuda
- 👤 Takuzo Otani
- 👤 Haruo Yamada
- 👤 Michikazu Sawada
- 👤 Katsuo Aizawa
- 👤 Mari Uchimoto
- 👤 Michito Karasawa
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 19:36
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/22
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
126 words
A porphyrin derivative of the general formula (I): wherein R1 each independently denotes a hydrogen, a C 1 -C 4 alkyl group or an ethenyl group, and R 2 each independently denotes COZ(C m H 2m )Q, COZCH(C m H 2m Q) 2 , -CH 2 -Q [wherein Z is O, S or NH, m is an integer of 1 to 23, and Q is a di-(C 1 -C 4 alkyl)amino group or tri-(C 1 -C 4 alkyl)ammonium halide group] or (wherein X is a halogen); or R 1 each independently denotes -C 2 H 4 -Q (wherein Q is as defined above), (wherein X is as defined above), and R 2 each independently denotes a carboxyl group or a C 1 -C 4 alkoxycarbonyl group.
Claim 2
Dependent Claim
126 words
A porphyrin derivative of the general formula (I): wherein R1 each independently denotes a hydrogen, a C 1 -C 4 alkyl group or an ethenyl group, and R 2 each independently denotes COZ(C m H 2m )Q, COZCH(C m H 2m Q) 2 , -CH 2 -Q [wherein Z is O, S or NH, m is an integer of 1 to 23, and Q is a di-(C 1 -C 4 alkyl)amino group or tri-(C 1 -C 4 alkyl)ammonium halide group] or (wherein X is a halogen); or R 1 each independently denotes -C 2 H 4 -Q (wherein Q is as defined above), (wherein X is as defined above), and R 2 each independently denotes a carboxyl group or a C 1 -C 4 alkoxycarbonyl group.
Claim 3
Dependent Claim
68 words
A porphyrin derivative as claimed in claim 1, which is represented by the formula III; wherein each R 1 ' is a hydrogen, a C 1 -C 4 alkyl group or an ethenyl group, and each R 3 is O(C m H 2m )Q, OCH(CH 2 Q) 2 , S(C m H 2m )Q or NH(C m H 2m )Q (wherein m and Q are as defined above).
Claim 4
Dependent Claim
42 words
A porphyrin derivative as claimed in claim 1, which is represented by the formula IV: wherein each R 1 ' is as defined above, and each R 4 is a tri(C 1 -C 4 alkyl) ammonium halide group or pyridinium halide group.
Claim 5
Dependent Claim
50 words
A porphyrin derivative as claimed in claim 1, which is represented by the formula VI: (wherein each R 5 is a tri-(C 1 -C 4 alkyl)ammonium halide group, pyridinium halide group or quinolinium halide group, and each R 6 is a hydrogen or a C 1 -C 4 alkyl group).
Claim 6
Independent Claim
162 words
A method for producing a porphyrin derivative of the formula IIIA; (wherein each R 1 1 denotes a hydrogen , a C 1 -C 4 alkyl group or an ethenyl group and each R 2 1 denotes O(C m H 2m )Q', OCH-(CH 2 Q') 2 , S(C m H 2m )Q' or NH(C m H 2m )Q' [wherein m is an integer of 1 to 23, and Q' is a di-(C 1 -C 4 alkyl)amino group]) which comprises subjecting a compound of the formula II A ; (wherein each X denotes a halogen, and each R 1 ' is as defined above) to a condensation reaction with a compound of the formula, HO(C m H 2m )N(R) 2 , HOCH(CH 2 N(R) 2 ) 2 , HS(C m H 2m )N(R) 2 or H 2 N ( C m H 2m ) N (R) 2 (wherein R is a C 1 -C 4 alkyl group and m is as defined above).
Claim 7
Independent Claim
162 words
A method for producing a porphyrin derivative of the formula IIIA; (wherein each R 1 1 denotes a hydrogen , a C 1 -C 4 alkyl group or an ethenyl group and each R 2 1 denotes O(C m H 2m )Q', OCH-(CH 2 Q') 2 , S(C m H 2m )Q' or NH(C m H 2m )Q' [wherein m is an integer of 1 to 23, and Q' is a di-(C 1 -C 4 alkyl)amino group]) which comprises subjecting a compound of the formula II A ; (wherein each X denotes a halogen, and each R 1 ' is as defined above) to a condensation reaction with a compound of the formula, HO(C m H 2m )N(R) 2 , HOCH(CH 2 N(R) 2 ) 2 , HS(C m H 2m )N(R) 2 or H 2 N ( C m H 2m ) N (R) 2 (wherein R is a C 1 -C 4 alkyl group and m is as defined above).
Claim 8
Independent Claim
99 words
A method for producing a porphyrin derivative of the formula IIIB; (wherein each R 1 ' is as defined above and R 2 " is O(C m H 2m )N + (R) 3 ·X - , OCH(CH 2 N + (R) 3 ) 2 ·2X - , S(C m H 2m )N + (R) 3 · X or NH(C m N 2m )N + (R) 3 ·X - , which comprises reacting a porphyrin derivative of the formula IIIA; (wherein R 1 ' and R 2 ' are as defined above) with a C 1 -C 4 alkyl halide.
Claim 9
Independent Claim
99 words
A method for producing a porphyrin derivative of the formula IIIB; (wherein each R 1 ' is as defined above and R 2 " is O(C m H 2m )N + (R) 3 ·X - , OCH(CH 2 N + (R) 3 ) 2 ·2X - , S(C m H 2m )N + (R) 3 · X or NH(C m N 2m )N + (R) 3 ·X - , which comprises reacting a porphyrin derivative of the formula IIIA; (wherein R 1 ' and R 2 ' are as defined above) with a C 1 -C 4 alkyl halide.
Claim 10
Independent Claim
51 words
A method for producing a porphyrin derivative of the formula IV; (wherein R 1 ' and R 4 are the same as defined above) which comprises reacting a porphyrin derivative of the formula VA; (wherein R 1 ' and X are as defined above) with a tri-(C 1 -C 4 alkyl)amine.
Claim 11
Independent Claim
51 words
A method for producing a porphyrin derivative of the formula IV; (wherein R 1 ' and R 4 are the same as defined above) which comprises reacting a porphyrin derivative of the formula VA; (wherein R 1 ' and X are as defined above) with a tri-(C 1 -C 4 alkyl)amine.
Claim 12
Independent Claim
47 words
A method for producing a porphyrin derivative of the formula VI; (wherein R 5 and R 6 are as defined above) which comprises reacting a porphyrin derivative of the formula VII; (wherein X and R 6 are as defined above) with a tri-(C 1 -C 4 alkyl)amine.
Claim 13
Independent Claim
47 words
A method for producing a porphyrin derivative of the formula VI; (wherein R 5 and R 6 are as defined above) which comprises reacting a porphyrin derivative of the formula VII; (wherein X and R 6 are as defined above) with a tri-(C 1 -C 4 alkyl)amine.
Claim 14
Dependent Claim
28 words
A pharmaceutical composition comprising a compound as claimed in any one of Claims 1 to 4 in admixture or otherwise associated with a pharmacologically acceptable diluent or carrier.
Claim 15
Dependent Claim
21 words
A compound as claimed in any one of Claims 1 to 4 for use in the diagnosis or treatment of cancer.
Claim 16
Dependent Claim
30 words
The use of a compound as claimed in any one of Claims 1 to 4 in the manufacture of a composition for use in the diagnosis or treatment of cancer.
References Cited (Backward Citations)
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