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US4659567A
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Molecules with antibody combining sites that bind to hydrolytic transition states
Assignee: Scripps Research Institute
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Filing: 1984-09-07
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Granted: 1987-04-21
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Expires: 2004-09-07
Abstract
Abstract A phosphonamidate or phosphonate analog-ligand having a conformation that substantially corresponds to the conformation of a hydrolytic transition state of an amide or ester ligand is used to produce antibodies of predetermined specificity. The antibodies include an epitope that binds to and thereby stabilizes the tetrahedral carbon atom of the amide or ester hydrolysis transition state of the ligand to hydrolyze the ligand at a predetermined site.
Inventors
- 👤 Alfonso Tramontano
- 👤 Richard A. Lerner
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 09:27
CPC Classifications
C; C07; C07D; C07D405/00; C07D405/02; C07D405/12; C07D311/00; C07D311/02; C07D311/04; C07D311/06; C07D311/08; C07D311/16; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/40; C07F9/4003; C07F9/4056; C07F9/4071; C07F9/4084; C07F9/547; C07F9/553; C07F9/5537; C07F9/6558; C07F9/65586; C07K; C07K16/00; C07K16/44; G; G01; G01N; G01N33/00; G01N33/48; G01N33/50; G01N33/53; Y; Y10; Y10S; Y10S435/00; Y10S435/814
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
106 words
Antibodies that include an epitope that binds to and thereby stabilizes a tetrahedral carbon intermediate in the hydrolysis of an ester and that are raised in an animal host to a phosphonate of the formula ##STR16## wherein R 1 is ##STR17## R 4 is (i) a second bond between the oxygen and central phosphorous atom, (ii) hydrogen or (iii) C 1 -C 4 alkyl; said phosphonate having a conformation that substantially corresponds to the conformation of the tetrahedral carbon intermediate in the hydrolysis of an ester of the formula: ##STR18## wherein R 1 , R 2 , R 3 and R 4 are as defined above.
Claim 2
Dependent Claim
106 words
Antibodies that include an epitope that binds to and thereby stabilizes a tetrahedral carbon intermediate in the hydrolysis of an ester and that are raised in an animal host to a phosphonate of the formula ##STR16## wherein R 1 is ##STR17## R 4 is (i) a second bond between the oxygen and central phosphorous atom, (ii) hydrogen or (iii) C 1 -C 4 alkyl; said phosphonate having a conformation that substantially corresponds to the conformation of the tetrahedral carbon intermediate in the hydrolysis of an ester of the formula: ##STR18## wherein R 1 , R 2 , R 3 and R 4 are as defined above.
Claim 3
Dependent Claim
13 words
Antibodies raised in an animal host to a compound of the formula: ##STR19##
Claim 4
Dependent Claim
13 words
Antibodies raised in an animal host to a compound of the formula: ##STR19##
Claim 5
Dependent Claim
13 words
Antibodies raised in an animal host to a compound of the formula: ##STR20##
Claim 6
Dependent Claim
13 words
Antibodies raised in an animal host to a compound of the formula: ##STR20##
Claim 7
Dependent Claim
13 words
Antibodies raised in an animal host to a compound of the formula: ##STR21##
Claim 8
Dependent Claim
13 words
Antibodies raised in an animal host to a compound of the formula: ##STR21##
Claim 9
Dependent Claim
34 words
A compound of the formula: ##STR22## wherein R 1 is ##STR23## R 4 is (i) a second bond between the oxygen and central phosphorous atom, (ii) hydrogen or (iii) C 1 -C 4 alkyl.
Claim 10
Dependent Claim
34 words
A compound of the formula: ##STR22## wherein R 1 is ##STR23## R 4 is (i) a second bond between the oxygen and central phosphorous atom, (ii) hydrogen or (iii) C 1 -C 4 alkyl.
Claim 11
Dependent Claim
6 words
A compound of the formula: ##STR24##
Claim 12
Dependent Claim
6 words
A compound of the formula: ##STR24##
Claim 13
Dependent Claim
6 words
A compound of the formula: ##STR25##
Claim 14
Dependent Claim
6 words
A compound of the formula: ##STR25##
Claim 15
Dependent Claim
6 words
A compound of the formula: ##STR26##
Claim 16
Dependent Claim
6 words
A compound of the formula: ##STR26##
Claim 17
Dependent Claim
6 words
A compound of the formula: ##STR27##
Claim 18
Dependent Claim
6 words
A compound of the formula: ##STR27##
Claim 19
Dependent Claim
6 words
A compound of the formula: ##STR28##
Claim 20
Dependent Claim
6 words
A compound of the formula: ##STR28##
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) | 1990-04-20 | 1990-10-20 | 1991-04-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-04-20 | 1994-10-20 | 1995-04-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-04-20 | 1998-10-20 | 1999-04-21 | $7700.00 | Window Closed / Lapsed |