US4904697A
Expired / Lapsed
US
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Controlling the growth of certain tumor tissue with chalcone derivatives
Assignee: Aventis Pharmaceuticals Inc
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Filing: 1987-04-09
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Granted: 1990-02-27
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Expires: 2007-04-09
Abstract
Abstract Certain chalcone derivatives are reported to inhibit the polymerization of tubulin to form microtubules and are therefore antimitotic agents which can be used to control the growth of tumor tissue and can be used as antigout agents.
Inventors
- 👤 Sai P. Sunkara
- 👤 Michael L. Edwards
- 👤 David M. Stemerick
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 16:20
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/12; A61K31/16; A61K31/165; A61K31/13; A61K31/135
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
79 words
A method of inhibiting the polymerization of tubulin to form microtubules which comprises administering to a patient in need thereof an effective amount of a chalcone derivative of the structure ##STR4## wherein Ar is a 2,5-dimethoxyphenyl, 2,3,4-trimethoxyphenyl, or 3,4,5-trimethoxyphenyl substituent; R 1 is a hydrogen, (C 1 -C 4 )alkyl, chloro, or bromo substituent; and R 2 is a --N(R) 2 or NHCOR wherein R is a (C 1 -C 4 )alkyl substituent or a pharmaceutically acceptable salt thereof.
Claim 2
Independent Claim
79 words
A method of inhibiting the polymerization of tubulin to form microtubules which comprises administering to a patient in need thereof an effective amount of a chalcone derivative of the structure ##STR4## wherein Ar is a 2,5-dimethoxyphenyl, 2,3,4-trimethoxyphenyl, or 3,4,5-trimethoxyphenyl substituent; R 1 is a hydrogen, (C 1 -C 4 )alkyl, chloro, or bromo substituent; and R 2 is a --N(R) 2 or NHCOR wherein R is a (C 1 -C 4 )alkyl substituent or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
16 words
A method of claim 1 wherein R 1 is a (C 1 -C 4 ) substituent.
Claim 4
Dependent Claim
12 words
A method of claim 1 wherein R 1 is a methyl substituent.
Claim 5
Dependent Claim
16 words
A method of claim 1, 2, or 3 wherein R 2 is a --N(R) 2 .
Claim 6
Dependent Claim
11 words
A method of claim 4 wherein R is a methyl substituent.
Claim 7
Dependent Claim
12 words
A method according to claim 5 wherein Ar is a 2,5-dimethoxyphenyl substituent.
Claim 8
Dependent Claim
24 words
A method of claim 1 wherein R 1 is a methyl substituent, R 2 is a dimethylamino substituent, and Ar is a 2,5-dimethoxyphenyl substituent.
Claim 9
Independent Claim
87 words
A method for controlling the growth of tumor tissues sensitive to treatment with the chalcone derivative as defined below which comprises administering to a patient in need thereof an effective amount of a chalcone derivative of the structure ##STR5## wherein Ar is a 2,5-dimethoxyphenyl, 2,3,4-trimethoxyphenyl, or 3,4,5-trimethoxyphenyl substituent; R 1 is a hydrogen, (C 1 -C 4 )alkyl, chloro, or bromo substituent; and R 2 is a --N(R) 2 or NHCOR wherein R is a (C 1 -C 4 )alkyl substituent or a pharmaceutically acceptable salt thereof.
Claim 10
Independent Claim
87 words
A method for controlling the growth of tumor tissues sensitive to treatment with the chalcone derivative as defined below which comprises administering to a patient in need thereof an effective amount of a chalcone derivative of the structure ##STR5## wherein Ar is a 2,5-dimethoxyphenyl, 2,3,4-trimethoxyphenyl, or 3,4,5-trimethoxyphenyl substituent; R 1 is a hydrogen, (C 1 -C 4 )alkyl, chloro, or bromo substituent; and R 2 is a --N(R) 2 or NHCOR wherein R is a (C 1 -C 4 )alkyl substituent or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim
16 words
A method of claim 8 wherein R 1 is a (C 1 -C 4 ) substituent.
Claim 12
Dependent Claim
12 words
A method of claim 8 wherein R 1 is a methyl substituent.
Claim 13
Dependent Claim
16 words
A method of claim 8, 9, or 10 wherein R 2 is a --N(R) 2 .
Claim 14
Dependent Claim
11 words
A method of claim 11 wherein R is a methyl substituent.
Claim 15
Dependent Claim
12 words
A method according to claim 12 wherein Ar is a 2,5-dimethoxyphenyl substituent.
Claim 16
Dependent Claim
24 words
A method of claim 8 wherein R 1 is a methyl substituent, R 2 is a dimethylamino substituent, and Ar is a 2,5-dimethoxyphenyl substituent.
Claim 17
Dependent Claim
22 words
A method according to claim 8 wherein said tumor tissue is selected from the group consisting of melanoma, lymphoma, leukemia, and sarcoma.
Claim 18
Dependent Claim
29 words
A method according to claim 8 wherein said tumor is a hematologic tumor selected from the group consisting of acute lymphoblastic leukemia, acute myelocytic leukemia and chronic myelocytic leukemia.
Claim 19
Dependent Claim
23 words
A method according to claim 8 wherein said tumor is a lymphoma selected from the group consisting of Hodgkin's disease and malignant lymphoma.
Claim 20
Dependent Claim
11 words
A method according to claim 16 wherein said compound is α-methyl-4-dimethylamino-2',5'-dimethoxychalcone.
Claim 21
Dependent Claim
11 words
A method according to claim 17 wherein said compound is α-methyl-4-dimethylamino-2',5'-dimethoxychalcone.
Claim 22
Dependent Claim
11 words
A method according to claim 1 wherein said compound is α-methyl-4-dimethylamino-2',5'-dimethoxychalcone.
Claim 23
Dependent Claim
11 words
A method according to claim 8 wherein said compound is α-methyl-4-dimethylamino-2',5'-dimethoxychalcone.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-02-26 | 1993-08-28 | 1994-02-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-02-26 | 1997-08-28 | 1998-02-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-02-26 | 2001-08-28 | 2002-02-27 | $7700.00 | Window Closed / Lapsed |