US4675338A
Expired / Lapsed
US
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Tetrapyrrole therapeutic agents
Assignee: PORPHYRIN PRODUCTS Inc
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Filing: 1984-07-18
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Granted: 1987-06-23
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Expires: 2004-07-18
Abstract
Abstract The present invention relates to compounds having the following formula: ##STR1## or the corresponding di- or tetrahydrotetrapyrroles wherein ##STR2## provided that when R 1 , R 2 , R 3 , R 4 , R 7 and R 8 represent two substituents or are divalent and attached to the same carbon, the respective pyrrole ring to which attached is a dihydropyrrole; R is lower alkyl or benzyl; R 6 and R 9 , taken together are ##STR3## with the proviso that at least one of R 1 -R 9 includes a free carboxyl group; and salts thereof. These compounds are useful in the photodiagnosis and phototherapy of tumors.
Inventors
- 👤 Jerry C. Bommer
- 👤 Bruce F. Burnham
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 13:26
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/44; A; A61; A61K; A61K41/00; A61K41/0057; A61K41/0071; A61K49/00; A61K49/001; A61K49/0013; A61K49/0017; A61K49/0019; A61K49/0021; A61K49/0036; A61K49/005; A61K49/0052; A61P; A61P35/00; C07K; C07K14/00; C07K14/795; C07K5/00; C07K5/04; C07K5/06; C07K5/06104; C07K5/06113; C07K5/08; C07K5/0819; C07K5/10; C07K5/1021; A61K38/00
Claims Analysis
Total Claims: 44
Claim 1
Independent Claim
144 words
A fluorescent mono-, di, tri- or tetramide of an amino acid containing two carboxy groups and a carboxy containing tetrapyrrole compound of the formula: ##STR57## or the corresponding di- or tetrahydrotetrapyrroles, said amide linkage being formed between the amino group of the amino acid and a carboxy-containing substituent attached to the tetrapyrrole; wherein ##STR58## provided that when R 1 , R 2 , R 3 , R 4 , R 7 and R 8 represent two substituents or are divalent and attached to the same carbon, the respective pyrrole ring to which attached is a dihydropyrrole; R is lower alkyl or benzyl; or R 6 and R 9 , taken together are ##STR59## with the proviso that at least one of R 1 -R 9 includes a free carboxyl group; and salts thereof; with the further proviso that said compound is not mesoporphyrin-bis-L-glutamic acid.
Claim 2
Dependent Claim
144 words
A fluorescent mono-, di, tri- or tetramide of an amino acid containing two carboxy groups and a carboxy containing tetrapyrrole compound of the formula: ##STR57## or the corresponding di- or tetrahydrotetrapyrroles, said amide linkage being formed between the amino group of the amino acid and a carboxy-containing substituent attached to the tetrapyrrole; wherein ##STR58## provided that when R 1 , R 2 , R 3 , R 4 , R 7 and R 8 represent two substituents or are divalent and attached to the same carbon, the respective pyrrole ring to which attached is a dihydropyrrole; R is lower alkyl or benzyl; or R 6 and R 9 , taken together are ##STR59## with the proviso that at least one of R 1 -R 9 includes a free carboxyl group; and salts thereof; with the further proviso that said compound is not mesoporphyrin-bis-L-glutamic acid.
Claim 3
Dependent Claim
14 words
The mono- or polyamide according to claim 1 wherein the tetrapyrrole is a porphyrin.
Claim 4
Dependent Claim
14 words
The mono- or polyamide according to claim 1 wherein the tetrapyrrole is a chlorin.
Claim 5
Dependent Claim
14 words
The mono- or polyamide according to claim 1 wherein the tetrapyrrole is a bacteriochlorin.
Claim 6
Dependent Claim
15 words
The amide according to claim 1 wherein the amino acid is an alpha aminodicarboxylic acid.
Claim 7
Dependent Claim
13 words
The amide according to claim 1 wherein the amino acid is aspartic acid.
Claim 8
Dependent Claim
13 words
The amide according to claim 1 wherein the amino acid is glutamic acid.
Claim 9
Dependent Claim
11 words
The compound according to claim 1 which is monoaspartyl trans-mesochlorin IX.
Claim 10
Dependent Claim
11 words
The compound according to claim 1 which is diaspartyl trans-mesochlorin IX.
Claim 11
Dependent Claim
11 words
The compound according to claim 1 which is monoglutamyl trans-mesochlorin IX.
Claim 12
Dependent Claim
11 words
The compound according to claim 1 which is diglutamyl trans-mesochlorin IX.
Claim 13
Dependent Claim
13 words
The compound according to claim 1 which is monoaspartyl chlorin e 6 .
Claim 14
Dependent Claim
13 words
The compound according to claim 1 which is. triaspartyl chlorin e 6 .
Claim 15
Dependent Claim
13 words
The compound according to claim 1 which is monoglutamyl chlorin e 6 .
Claim 16
Dependent Claim
11 words
The compound according to claim 1 which is diglutamyl protoporphyrin IX.
Claim 17
Dependent Claim
13 words
The compound according to claim 1 which is monoaspartyl mesochlorin e 6 .
Claim 18
Dependent Claim
11 words
The compound according to claim 1 which is monoglutamyl protoporphyrin IX.
Claim 19
Dependent Claim
11 words
The compound according to claim 1 which is monoaspartyl mesoporphyrin IX.
Claim 20
Dependent Claim
11 words
The compound according to claim 1 which is diaspartyl mesoporphyrin IX.
Claim 21
Dependent Claim
11 words
The compound according to claim 1 which is diglutamyl mesoporphyrin IX.
Claim 22
Dependent Claim
11 words
The compound according to claim 1 which is diaspartyl protoporphyrin IX.
Claim 23
Dependent Claim
12 words
The compound according to claim 1 which is monoaspartylbacteriochlorin e 4 .
Claim 24
Dependent Claim
11 words
The compound according to claim 1 which is diaspartyl deuteroporphyrin IX.
Claim 25
Dependent Claim
11 words
The compound according to claim 1 which is monoaspartyl deuteroporphyrin IX.
Claim 26
Dependent Claim
12 words
The compound according to claim 1 which is monoglutamylbacterioisochlorin e 4 .
Claim 27
Dependent Claim
11 words
The compound according to claim 1 which is diglutamyl deuteroporphyrin IX.
Claim 28
Dependent Claim
13 words
The compound according to claim 1 which is mono- or diaspartyl photoprotoporphyrin IX.
Claim 29
Dependent Claim
13 words
The compound according to claim 1 which is mono- or diglutamyl photoprotoporphyin IX.
Claim 30
Dependent Claim
15 words
The compound according to claim 1 which is mono-, di-, tri- or tetraglutamyl coporphyrin III.
Claim 31
Dependent Claim
13 words
The compound according to claim 1 which is mono- or diaspartyl hematoporphyrin IX.
Claim 32
Dependent Claim
13 words
The compound according to claim 1 which is mono- or diglutamyl hematoporphyrin IX.
Claim 33
Dependent Claim
15 words
The compound according to claim 1 which is mono- or diglutamyl chlorin e 4 .
Claim 34
Dependent Claim
15 words
The compound according to claim 1 which is mono- or diglutamyl mesochlorin e 4 .
Claim 35
Dependent Claim
15 words
The compound according to claim 1 which is mono- or diaspartyl chlorin e 4 .
Claim 36
Dependent Claim
11 words
The compound according to claim 1 which is monoglutamyl deuteroporphyrin IX.
Claim 37
Dependent Claim
149 words
A pharmaceutical composition comprising an effective therapeutic amount of a fluorescent mono-, di-, tri- or tetramide of an amino acid containing two carboxy groups and a carboxy containing tetrapyrrole compound of the formula: ##STR60## or the corresponding di- or tetrahydrotetrapyrroles, said amide linkage being formed between the amino group of the amino acid and a carboxy-containing substituent attached to the tetrapyrrole; wherein ##STR61## provided that when R 1 , R 2 , R 3 , R 4 , R 7 and R 8 represent two substituents or are divalent and attached to the same carbon, the respective pyrrole ring to which attached is a dihydropyrrole; R is lower alkyl or benzyl; or R 6 and R 9 taken together are ##STR62## with the proviso that at least one of R 1 -R 9 includes a free carboxyl group; and pharmaceutically acceptable salts thereof, and a pharmaceutically acceptable carrier therefor.
Claim 38
Dependent Claim
149 words
A pharmaceutical composition comprising an effective therapeutic amount of a fluorescent mono-, di-, tri- or tetramide of an amino acid containing two carboxy groups and a carboxy containing tetrapyrrole compound of the formula: ##STR60## or the corresponding di- or tetrahydrotetrapyrroles, said amide linkage being formed between the amino group of the amino acid and a carboxy-containing substituent attached to the tetrapyrrole; wherein ##STR61## provided that when R 1 , R 2 , R 3 , R 4 , R 7 and R 8 represent two substituents or are divalent and attached to the same carbon, the respective pyrrole ring to which attached is a dihydropyrrole; R is lower alkyl or benzyl; or R 6 and R 9 taken together are ##STR62## with the proviso that at least one of R 1 -R 9 includes a free carboxyl group; and pharmaceutically acceptable salts thereof, and a pharmaceutically acceptable carrier therefor.
Claim 39
Dependent Claim
15 words
The composition according to claim 36 wherein the amino acid is an alpha aminodicarboxylic acid.
Claim 40
Dependent Claim
12 words
The composition according to claim 37 wherein the tetrapyrrole is a chlorin.
Claim 41
Dependent Claim
12 words
The composition according to claim 37 wherein the tetrapyrrole is a bacteriochlorin.
Claim 42
Dependent Claim
12 words
The composition according to claim 37 wherein the tetrapyrrole is a porphyrin.
Claim 43
Dependent Claim
13 words
The composition according to claim 37 wherein the amino acid is aspartic acid.
Claim 44
Dependent Claim
13 words
The composition according to claim 37 wherein the amino acid is glutamic acid.
References Cited (Backward Citations)
US4393071A
Cited
WO1984001382A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-06-22 | 1990-12-22 | 1991-06-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-06-22 | 1994-12-22 | 1995-06-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-06-22 | 1998-12-22 | 1999-06-23 | $7700.00 | Window Closed / Lapsed |