US4439356A
Expired / Lapsed
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Unsymmetrical fluorescein derivatives
Assignee: Siemens Healthcare Diagnostics GmbH Germany
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Filing: 1981-03-03
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Granted: 1984-03-27
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Expires: 2001-03-03
Abstract
Abstract Unsymmetrically substituted 6-hydroxy-3H-xanthen-3-ones for use as fluorescers or quenchers, particularly conjugated to provide reagents in competitive protein binding assays. Substituents are aliphatic groups bonded to an annular carbon atom through carbon or oxygen.
Inventors
- 👤 Pyare Khanna
- 👤 Warren Colvin
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 01:19
CPC Classifications
C; C07; C07D; C07D311/00; C07D311/02; C07D311/78; C07D311/80; C07D311/82; Y; Y10; Y10S; Y10S435/00; Y10S435/961
Claims Analysis
Total Claims: 29
Claim 1
Independent Claim
205 words
A compound of the formula ##STR6## wherein: one of the γs will be of the formula --(O).sub.ε ρ and the other is δ; wherein ε is 0 or 1 and ρ is an aliphatic group of from about 1 to 12 carbon atoms and 0-1 carboxyl groups; the δ's are the same or different and are hydrogen or halogen of atomic number 17 to 80; L is a bond or divalent organic radical of up to 20 carbon atoms; α may be taken together with Ψ to define an active group capable of forming a stable covalent bond with carbon, nitrogen or oxygen or is an organic compound, and is at other than the ortho position when L is benzene and Ψ and α are taken together to define carboxy; Ψ, when not taken together with α is a linking group to α; v is 1 when Ψ is taken together with α and is otherwise on the average at least 1 and not more than the molecular weight of α divided by 500. with the proviso that when ε is 0, one of the δ's may be an aliphatic group of from about 1 to 12 carbon atoms asymmetrically substituted in relation to ρ.
Claim 2
Dependent Claim
205 words
A compound of the formula ##STR6## wherein: one of the γs will be of the formula --(O).sub.ε ρ and the other is δ; wherein ε is 0 or 1 and ρ is an aliphatic group of from about 1 to 12 carbon atoms and 0-1 carboxyl groups; the δ's are the same or different and are hydrogen or halogen of atomic number 17 to 80; L is a bond or divalent organic radical of up to 20 carbon atoms; α may be taken together with Ψ to define an active group capable of forming a stable covalent bond with carbon, nitrogen or oxygen or is an organic compound, and is at other than the ortho position when L is benzene and Ψ and α are taken together to define carboxy; Ψ, when not taken together with α is a linking group to α; v is 1 when Ψ is taken together with α and is otherwise on the average at least 1 and not more than the molecular weight of α divided by 500. with the proviso that when ε is 0, one of the δ's may be an aliphatic group of from about 1 to 12 carbon atoms asymmetrically substituted in relation to ρ.
Claim 3
Dependent Claim
10 words
A compound according to claim 1 conjugated to a support.
Claim 4
Dependent Claim
144 words
A compound of the formula ##STR7## wherein: one of the Gs is of the formula --(O) e R and is otherwise D, where e is 0 or 1 and R is an aliphatic group of from 1 to 6 carbon atoms having from 0 to 1 carboxy groups; Z is carboxy or sulphonoxy; D is hydrogen or halogen of atom number 17 to 80; W is a bond or divalent organic radical having up to 10 carbon atoms; Y may be taken together with A to form an active functionality capable of forming a covalent bond with carbon, nitrogen or oxygen when not taken together with A, Y is a linking functionality; A when not taken together with Y is a ligand or receptor of at least about 125 daltons; X is halo of atomic number 9 to 80; m is 1 to 3;
Claim 5
Dependent Claim
144 words
A compound of the formula ##STR7## wherein: one of the Gs is of the formula --(O) e R and is otherwise D, where e is 0 or 1 and R is an aliphatic group of from 1 to 6 carbon atoms having from 0 to 1 carboxy groups; Z is carboxy or sulphonoxy; D is hydrogen or halogen of atom number 17 to 80; W is a bond or divalent organic radical having up to 10 carbon atoms; Y may be taken together with A to form an active functionality capable of forming a covalent bond with carbon, nitrogen or oxygen when not taken together with A, Y is a linking functionality; A when not taken together with Y is a ligand or receptor of at least about 125 daltons; X is halo of atomic number 9 to 80; m is 1 to 3;
Claim 6
Dependent Claim
71 words
p is 0 to 3, with the sum of m and p being not greater than 4; n will be 1 when Y and A are taken together or otherwise be on the average 1 to the molecular weight of A divided by 500, with the proviso that when W is a bond and Y and A are taken together to define carboxy, Y is at other than the ortho position.
Claim 7
Dependent Claim
71 words
p is 0 to 3, with the sum of m and p being not greater than 4; n will be 1 when Y and A are taken together or otherwise be on the average 1 to the molecular weight of A divided by 500, with the proviso that when W is a bond and Y and A are taken together to define carboxy, Y is at other than the ortho position.
Claim 8
Dependent Claim
10 words
A compound according to claim 3, wherein e is 0.
Claim 9
Dependent Claim
10 words
A compound according to claim 3, wherein e is 1.
Claim 10
Dependent Claim
242 words
A compound of the formula ##STR8## wherein: one of G' or G" is --(O) e' R' and is otherwise D', wherein e' is 0 or 1 and R' is alkyl of from 1 to 3 carbon atoms; D' is hydrogen or halogen of atomic number 17 to 80; Y' may be taken together with A' to define a non-oxo-carbonyl group and is otherwise a non-oxo-carbonyl group forming an amide group with an amino group of A'; A' when not taken together with Y', is a ligand or receptor of at least about 125 daltons; W' is a bond or aliphatic linking group of from 1 to 12 atoms other than hydrogen, which are carbon, nitrogen, oxygen or sulfur, there being from 0 to 8 carbon atoms and 0 to 8 heteroatoms, wherein nitrogen is present as amino or amido; and oxygen and sulfur are present as oxy, oxo or the sulfur analogs thereof; Z' is carboxy; X' is halo of atomic number 9 to 80; n' is 1 when Y' and A' are taken together and is otherwise on the average at least 1 to the molecular weight of A' divided by about 1,000; m' is 0 to 2; p' is 0 to 3, the sum of m' and p' being not greater than 4, with the proviso that, when W' is a bond and Y' and A' are taken together to define carboxy, Y' is at other than the ortho position.
Claim 11
Dependent Claim
242 words
A compound of the formula ##STR8## wherein: one of G' or G" is --(O) e' R' and is otherwise D', wherein e' is 0 or 1 and R' is alkyl of from 1 to 3 carbon atoms; D' is hydrogen or halogen of atomic number 17 to 80; Y' may be taken together with A' to define a non-oxo-carbonyl group and is otherwise a non-oxo-carbonyl group forming an amide group with an amino group of A'; A' when not taken together with Y', is a ligand or receptor of at least about 125 daltons; W' is a bond or aliphatic linking group of from 1 to 12 atoms other than hydrogen, which are carbon, nitrogen, oxygen or sulfur, there being from 0 to 8 carbon atoms and 0 to 8 heteroatoms, wherein nitrogen is present as amino or amido; and oxygen and sulfur are present as oxy, oxo or the sulfur analogs thereof; Z' is carboxy; X' is halo of atomic number 9 to 80; n' is 1 when Y' and A' are taken together and is otherwise on the average at least 1 to the molecular weight of A' divided by about 1,000; m' is 0 to 2; p' is 0 to 3, the sum of m' and p' being not greater than 4, with the proviso that, when W' is a bond and Y' and A' are taken together to define carboxy, Y' is at other than the ortho position.
Claim 12
Dependent Claim
13 words
A compound according to claim 6, wherein A' is taken together with Y'.
Claim 13
Dependent Claim
12 words
A compound according to claims 6 or 7, wherein R' is methyl.
Claim 14
Dependent Claim
19 words
A compound according to claims 6 or 7, wherein at least one of the D's and X's are chloro.
Claim 15
Dependent Claim
11 words
A compound according to claim 6, wherein A' is a ligand.
Claim 16
Dependent Claim
11 words
A compound according to claim 6, wherein A' is a receptor.
Claim 17
Dependent Claim
56 words
A compound of the formula ##STR9## wherein: D' is hydrogen or chloro; e' is 0 or 1; the sum of m' and p' is 0 to 4, wherein m' is 0 to 2; A' is hydroxyl or a ligand or receptor of at least about 125 daltons; and --COA' is at other than the ortho position.
Claim 18
Dependent Claim
56 words
A compound of the formula ##STR9## wherein: D' is hydrogen or chloro; e' is 0 or 1; the sum of m' and p' is 0 to 4, wherein m' is 0 to 2; A' is hydroxyl or a ligand or receptor of at least about 125 daltons; and --COA' is at other than the ortho position.
Claim 19
Dependent Claim
10 words
A compound according to claim 12, wherein e' is 0.
Claim 20
Dependent Claim
10 words
A compound according to claim 12, wherein e' is 1.
Claim 21
Dependent Claim
12 words
A compound according to claims 13 and 14, wherein A' is hydroxyl.
Claim 22
Dependent Claim
13 words
A compound according to claims 13 and 14, wherein A' is a ligand.
Claim 23
Dependent Claim
69 words
A compound of the formula ##STR10## wherein: e' is 0 or 1; m' is 0 to 2; p' is 0 to 3, the sum of m' and p' being not greater than 4; D' is hydrogen or chloro; and A' is hydroxyl or a ligand or receptor of at least about 125 daltons; with the proviso that, when A' is hydroxyl, --COA' is at other than the ortho position.
Claim 24
Dependent Claim
69 words
A compound of the formula ##STR10## wherein: e' is 0 or 1; m' is 0 to 2; p' is 0 to 3, the sum of m' and p' being not greater than 4; D' is hydrogen or chloro; and A' is hydroxyl or a ligand or receptor of at least about 125 daltons; with the proviso that, when A' is hydroxyl, --COA' is at other than the ortho position.
Claim 25
Dependent Claim
10 words
A compound according to claim 17, wherein e' is 0.
Claim 26
Dependent Claim
10 words
A compound according to claim 17, wherein e' is 1.
Claim 27
Dependent Claim
12 words
A compound according to claims 17 and 18, wherein A' is hydroxyl.
Claim 28
Dependent Claim
12 words
A compound according to claims 13 or 17, bound to a support.
Claim 29
Dependent Claim
13 words
A compound according to claims 18 or 19, wherein A' is a ligand.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-03-27 | 1987-09-26 | 1988-03-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-03-27 | 1991-09-26 | 1992-03-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-03-27 | 1995-09-26 | 1996-03-27 | $7700.00 | Window Closed / Lapsed |