Patent EP0220686A2 successfully refreshed from Google Patents.
EP0220686A2
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Porphyrin derivatives, and their production and use
Assignee: Photochemical Co Ltd
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Filing: 1986-10-23
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Granted: —
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Expires: 2006-10-23
Abstract
Abstract A porphyrin compound of the formula: wherein R 1 and R 2 are each -CH=CH 2 , -CH 2 CH 3 , -CH(O-lower alkanoyl)CH 3 , -CH(OR)CH 3 or -CH(O-lower alkylene-OR)CH 3 ; R 3 is -H, -COOH, -COO-lower alkyl, -COO-lower alkylene-OR or -COO-lower alkylene -OOC-Z; R 4 is -H, -lower alkyl or -lower alkylene-OR; R is -H, -lower alkyl or a residue of a polyfunctional carboxyl compound exluding a hydrogen atom therefrom; Z is a residue of the compound of the formula (I) excluding R 3 therefrom; A is -CH 2 - or-CO-; and the dotted line from the gamma-position indicates no bonding or a single direct bond; and the dotted line between the 7- and 8-positions indicates the presence of a single bond or a double bond; and its complexes with a metal(s) in the porphine skeleton and/or at the residue of the polyfunctional carboxyl compound, at least one of R 1 , R 2 , R 3 and R 4 being a group containing R which represents the residue of the polyfunctional carboxyl compound and R 1 being capable of representing 1-iodoethyl in addition to said meanings when R 3 is -COO-lower alkylene-OOC-Z, which shows a high accumulation in the locus of cancer with quick excretion from normal tissues.
Inventors
- 👤 Isao Sakata
- 👤 Susumu Nakajima
- 👤 Koichi Koshimizu
- 👤 Natsuki Samejima
- 👤 Kazumi Inohara
- 👤 Hiroyuki Takata
- 👤 Hirohiko Yamauchi
- 👤 Nobuo Ueda
- 👤 Masaaki Hazue
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 09:01
CPC Classifications
C; C07; C07D; C07D403/00; C07D403/14; C07D487/00; C07D487/22
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
198 words
A porphyrin compound of the formula: wherein R 1 and R 2 are each -CH = CH 2 , -CH 2 CH 3 , -CH(O-lower alkanoyl)CH 3 , -CH(OR)CH 3 or -CH(O-lower alkylene-OR)CH 3 ; R 3 is -H, -COOH, -COO-lower alkyl, -COO-lower alkylene-OR or -COO-lower alkylene-OOC-Z; R 4 is -H, -lower alkyl or -lower alkylene-OR; R is -H, -lower alkyl or a residue of a polyfunctional carboxyl compound excluding a hydrogen atom therefrom; Z is a residue of the compound of the formula (I) excluding R 3 therefrom; A is -CH 2 - or -CO-; and the dotted line from the gamma-position indicates no bonding or a single direct bond; and the dotted line between the 7- and 8-positions indicates the presence of a single bond or a double bond; and its complexes with a metal(s) in the porphine skeleton and/or at the residue of the polyfunctional carboxyl compound, at least one of R 1 , R 2 , R 3 and R 4 being a group containing R which represents the residue of the polyfunctional carboxyl compound and R 1 being capable of representing 1-iodoethyl in addition to said meanings when R 3 is -COO-lower alkylene-OOC-Z.
Claim 2
Dependent Claim
198 words
A porphyrin compound of the formula: wherein R 1 and R 2 are each -CH = CH 2 , -CH 2 CH 3 , -CH(O-lower alkanoyl)CH 3 , -CH(OR)CH 3 or -CH(O-lower alkylene-OR)CH 3 ; R 3 is -H, -COOH, -COO-lower alkyl, -COO-lower alkylene-OR or -COO-lower alkylene-OOC-Z; R 4 is -H, -lower alkyl or -lower alkylene-OR; R is -H, -lower alkyl or a residue of a polyfunctional carboxyl compound excluding a hydrogen atom therefrom; Z is a residue of the compound of the formula (I) excluding R 3 therefrom; A is -CH 2 - or -CO-; and the dotted line from the gamma-position indicates no bonding or a single direct bond; and the dotted line between the 7- and 8-positions indicates the presence of a single bond or a double bond; and its complexes with a metal(s) in the porphine skeleton and/or at the residue of the polyfunctional carboxyl compound, at least one of R 1 , R 2 , R 3 and R 4 being a group containing R which represents the residue of the polyfunctional carboxyl compound and R 1 being capable of representing 1-iodoethyl in addition to said meanings when R 3 is -COO-lower alkylene-OOC-Z.
Claim 3
Dependent Claim
38 words
The porphyrin compound according to claim 1, wherein A is -CH 2 -, the dotted line from the gamma-position indicates no bonding and the dotted line between the 7- and 8-positions indicates the presence of a double bond.
Claim 4
Dependent Claim
38 words
The porphyrin compound according to claim 1, wherein A is -CO-, the dotted line from the gamma-position indicates a single direct bond and the dotted line between the 7- and 8-positions indicates the presence of a single bond.
Claim 5
Dependent Claim
26 words
The porphyrin compound according to claim 1, wherein R is a residue of a polyfunctional carboxyl compound, which is a carboxylic acid having a chelate-forming group.
Claim 6
Dependent Claim
18 words
The porphyrin compound according to claim 1, wherein the carboxylic acid having a chelate-forming group is diethylenetriaminepentaacetic acid.
Claim 7
Dependent Claim
23 words
The porphyrin compound according to claim 1, wherein R is a residue of of a polyfunctional carboxyl compound, which is an amino acid.
Claim 8
Dependent Claim
13 words
The porphyrin compound according to claim 6, wherein the amino acid is glycine.
Claim 9
Dependent Claim
14 words
The porphyrin compound according to claim 6, wherein the amino acid is glutamic acid.
Claim 10
Dependent Claim
19 words
The complex of the porphyrin compound according to claim 1, wherein the metal is present in the porphine skeleton.
Claim 11
Dependent Claim
23 words
The complex of the porphyrin compound according to claim 1, wherein the metal is present at the residue of the polyfunctional carboxyl compound.
Claim 12
Dependent Claim
28 words
The complex of the porphyrin compound according to claim 1, wherein the metals are present in the porphine skeleton and at the residue of the polyfunctional carboxyl compound.
Claim 13
Dependent Claim
31 words
The complex of the porphyrin compound according to claim 1, wherein the metals are chosen from Si, Mn, Fe, Co, Ni, Zn, Ga, In, Sn, Sm, Eu, Gd, Tc and Tl.
Claim 14
Dependent Claim
17 words
The complex of the porphyrin compound according to claim 1, wherein at least one metal is radioactive.
Claim 15
Dependent Claim
22 words
A radioactive diagnostic composition comprising the complex of the porphyrin compound according to claim 1, wherein at least one metal is radioactive.
Claim 16
Dependent Claim
256 words
A process for preparing a porphyrin compound of the formula: wherein R 1 and R 2 are each -CH=CH 2 , -CH 2 CH 3 , -CH(O-lower alkanoyl)CH 3 , -CH(OR)CH 3 or -CH(O-lower alkylene-OR)CH 3 ; R 3 is -H, -COOH, -COO-lower alkyl, -COO-lower alkylene-OR or -COO-lower alkylene-OOC-Z; R 4 is -H, -lower alkyl or -lower alkylene-OR; R is -H, -lower alkyl or a residue of a polyfunctional carboxyl compound excluding a hydrogen atom therefrom; Z is a residue of the compound of the formula (I) excluding R 3 therefrom; A is -CH 2 - or -CO-; and the dotted line from the gamma-position indicates no bonding or a single direct bond; and the dotted line between the 7- and 8-positions indicates the presence of a single bond or a double bond; and its complexes with a metal(s) in the porphine skeleton and/or at the residue of the polyfunctional carboxyl compound, at least one of R 1 , R 2 , R 3 and R 4 being a group containing R which represents the residue of the polyfunctional carboxyl compound and R 1 being capable of representing 1-iodoethyl in addition to said meanings when R 3 is -COO-lower alkylene-OOC-Z, which comprises reacting a hydroxyl or carboxyl compound which corresponds to the formula (I) but R is -H, or its reactive derivative, or the metax complex thereof, with a polyfunctional carboxyl compound of the formula: R-H wherein R is as defined above, or its reactive derivative, optionally followed by complexing and/or chelating with a metal atom(s).
Claim 17
Dependent Claim
256 words
A process for preparing a porphyrin compound of the formula: wherein R 1 and R 2 are each -CH=CH 2 , -CH 2 CH 3 , -CH(O-lower alkanoyl)CH 3 , -CH(OR)CH 3 or -CH(O-lower alkylene-OR)CH 3 ; R 3 is -H, -COOH, -COO-lower alkyl, -COO-lower alkylene-OR or -COO-lower alkylene-OOC-Z; R 4 is -H, -lower alkyl or -lower alkylene-OR; R is -H, -lower alkyl or a residue of a polyfunctional carboxyl compound excluding a hydrogen atom therefrom; Z is a residue of the compound of the formula (I) excluding R 3 therefrom; A is -CH 2 - or -CO-; and the dotted line from the gamma-position indicates no bonding or a single direct bond; and the dotted line between the 7- and 8-positions indicates the presence of a single bond or a double bond; and its complexes with a metal(s) in the porphine skeleton and/or at the residue of the polyfunctional carboxyl compound, at least one of R 1 , R 2 , R 3 and R 4 being a group containing R which represents the residue of the polyfunctional carboxyl compound and R 1 being capable of representing 1-iodoethyl in addition to said meanings when R 3 is -COO-lower alkylene-OOC-Z, which comprises reacting a hydroxyl or carboxyl compound which corresponds to the formula (I) but R is -H, or its reactive derivative, or the metax complex thereof, with a polyfunctional carboxyl compound of the formula: R-H wherein R is as defined above, or its reactive derivative, optionally followed by complexing and/or chelating with a metal atom(s).
Claim 18
Dependent Claim
19 words
The process according to claim 15, wherein the polyfunctional carboxyl compound is a carboxylic acid having a chelate-forming group.
Claim 19
Dependent Claim
17 words
The process according to claim 16, wherein the carboxylic acid having a chete-forming group is diethylenetriaminepentaacetic acid.
Claim 20
Dependent Claim
15 words
The process according to claim 15, wherein the polyfunctional carboxyl compound is an amino acid.
Claim 21
Dependent Claim
12 words
The process according to claim 18, wherein the amino acid is glycine.
Claim 22
Dependent Claim
13 words
The process according to claim 18, wherein the amino acid is glutamic acid.
Claim 23
Dependent Claim
16 words
The process according to claim 15, wherein the reaction is carried out in an inert solvent.
Claim 24
Dependent Claim
21 words
The process according to claim 15, wherein the reaction is carried out in the presence of a reaction-promoting or condensing agent.
References Cited (Backward Citations)
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