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US4839155A
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US
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Iodotamoxifen derivatives and use for estrogen receptor-positive breast cancer detection and therapy
Assignee: BTG International Ltd
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Filing: 1987-09-09
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Granted: 1989-06-13
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Expires: 2007-09-09
Abstract
Abstract Iodotamoxifen derivatives which are compounds of formula (3) ##STR1## wherein X represents 3- or 4- iodo and R 1 and R 2 , which may be the same or different, represent C 1-3 alkyl, especially methyl or ethyl, groups or R 1 represents a hydrogen atom and R 2 a C 1-3 alkyl group or R 1 and R 2 together with the nitrogen atom to which they are attached represent a saturated heterocyclic group, especially a pyrrolidino, piperidino, 4-methylpiperidino or morpholino group, and their pharmaceutically acceptable acid addition salts are potent anti-estrogenic compounds useful for treatment of estrogen receptor-positive (hormone-dependent) breast cancers. Radioisotopic iodotamoxifen derivatives of formula (3) are useful in radiotherapy or gamma ray imaging of these cancers.
Inventors
- 👤 Raymond McCague
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 18:34
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/04; C07D295/08; C07D295/084; C07D295/088; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0404; A61K51/0406; A61K51/041; A61K51/044; A61K51/0446; A61P; A61P35/00
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
82 words
3- and 4-iodotamoxifen derivatives which are compounds of formula (3) ##STR8## wherein X represents a 3- or 4- iodo substituent and R 1 and R 2 , which may be the same or different, represent C 1-3 alkyl groups or R 1 represents a hydrogen atom and R 2 a C 1-3 alkyl group or R 1 and R 2 together with the nitrogen atom to which they are attached represent a saturated heterocyclic group and their pharmaceutically acceptable acid addition salts.
Claim 2
Dependent Claim
82 words
3- and 4-iodotamoxifen derivatives which are compounds of formula (3) ##STR8## wherein X represents a 3- or 4- iodo substituent and R 1 and R 2 , which may be the same or different, represent C 1-3 alkyl groups or R 1 represents a hydrogen atom and R 2 a C 1-3 alkyl group or R 1 and R 2 together with the nitrogen atom to which they are attached represent a saturated heterocyclic group and their pharmaceutically acceptable acid addition salts.
Claim 3
Dependent Claim
31 words
Iodotamoxifen derivatives according to claim 1 wherein R 1 and R 2 represent methyl groups or R 1 and R 2 together with the said nitrogen atom represent a pyrrolidino group.
Claim 4
Dependent Claim
14 words
Iodotamoxifen derivatives according to claim 2 wherein the iodo substituent is in the 4-position.
Claim 5
Dependent Claim
12 words
Iodotamoxifen derivatives according to claim 1, wherein the iodine atom is non-radioisotopic.
Claim 6
Dependent Claim
12 words
Iodotamoxifen derivatives acording to claim 2, wherein the iodine atom is non-radioisotopic.
Claim 7
Dependent Claim
12 words
Iodotamoxifen derivatives according to claim 3, wherein the iodine atom is non-radioisotopic.
Claim 8
Dependent Claim
21 words
A pharmaceutical composition comprising an iodotamoxifen derivative according to claim 1, in combination with a pharmaceutically effective diluent, carrier or excipient.
Claim 9
Dependent Claim
31 words
A method of treating an estrogen receptor-positive breast cancer in a human patient which comprises administering to the patient a therapeutically effective amount of a tamoxifen derivative according to claim 1.
Claim 10
Dependent Claim
31 words
A method of treating an estrogen receptor-positive breast cancer in a human patient which comprises administering to the patient a therapeutically effective amount of a tamoxifen derivative according to claim 4.
Claim 11
Dependent Claim
53 words
A method of detecting an estrogen receptor-positive breast cancer in a human ptient which comprises administering to the patient an effective amount of a tamoxifen derivative according to claim 1, wherein said iodine is a gammaray-emitting radioisotopic iodine atom and detecting the site at which the tamoxifen derivative binds to the estrogen receptor.
References Cited (Backward Citations)
US3288806A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-06-12 | 1992-12-12 | 1993-06-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-06-12 | 1996-12-12 | 1997-06-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-06-12 | 2000-12-12 | 2001-06-13 | $7700.00 | Window Closed / Lapsed |