Patent US32655A successfully refreshed from Google Patents.
Patent US489642A successfully refreshed from Google Patents.
Patent US4853221A successfully refreshed from Google Patents.
US4853221A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Method for treating non-small cell lung cancer, head and neck cancers and breast cancer
Assignee: Warner Lambert Co LLC
•
Filing: 1987-10-23
•
Granted: 1989-08-01
•
Expires: 2007-10-23
Abstract
Abstract 5-Methyl-6-[[(3,4,5-trimethoxyphenyl)amino]-methyl]-2,4-quinazolinediamine (trimetrexate) has been shown to possess clinical activity against non-small cell lung cancer, head and neck squamous cancers, and breast cancer. The compound also demonstrates therapeutic synergy with several known antineoplastic agents. Methods of treating non-small cell lung cancer, head and neck cancers, and breast cancer by administering trimetrexate alone or in combination with other neoplastic agents is disclosed.
Inventors
- 👤 Edward F. Elslager
- 👤 Wilbur R. Leopold, III
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 17:31
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505
Claims Analysis
Total Claims: 27
Claim 1
Independent Claim
111 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]-methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of a compound selected from the group consisting of (a) (8S,10S)-10-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-8-glycoloyl-7,8,9,10-tetrahydro-6,8,11-trihydroxy-1-methoxy-5,12-naphthacenedione or a pharmaceutically acceptable salt thereof; (b) 5-fluoro-2,4(1H,3H)-pyrimidinedione or a pharmaceutically acceptable salt thereof; (c) 2-amino-1,7-dihydro-6H-purine-6-thione or a pharmaceutically acceptable salt thereof; (d) 22-oxo-vincaleukoblastine or a pharmaceutically acceptable salt thereof; (e) 2-bis[(2-chloroethyl)amino]tetrahydro-2H-1,3,2- oxazaphosphorine, 2-oxide, or a pharmaceutically acceptable salt thereof; (f) N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-L-glutamic acid, or a pharmaceutically acceptable salt thereof; or (g) cis-diamminedichloroplatinum (II).
Claim 2
Independent Claim
111 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]-methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of a compound selected from the group consisting of (a) (8S,10S)-10-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-8-glycoloyl-7,8,9,10-tetrahydro-6,8,11-trihydroxy-1-methoxy-5,12-naphthacenedione or a pharmaceutically acceptable salt thereof; (b) 5-fluoro-2,4(1H,3H)-pyrimidinedione or a pharmaceutically acceptable salt thereof; (c) 2-amino-1,7-dihydro-6H-purine-6-thione or a pharmaceutically acceptable salt thereof; (d) 22-oxo-vincaleukoblastine or a pharmaceutically acceptable salt thereof; (e) 2-bis[(2-chloroethyl)amino]tetrahydro-2H-1,3,2- oxazaphosphorine, 2-oxide, or a pharmaceutically acceptable salt thereof; (f) N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-L-glutamic acid, or a pharmaceutically acceptable salt thereof; or (g) cis-diamminedichloroplatinum (II).
Claim 3
Dependent Claim
14 words
The method of claim 1 wherein said pharmaceutically acceptale salt is the D-glucuronate salt.
Claim 4
Dependent Claim
14 words
The method of claim 1 wherein said pharmaceutically acceptable salt is the 2-hydroxyethanesulfonate salt.
Claim 5
Independent Claim
32 words
A method of treating non-small cell lung cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5 trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof.
Claim 6
Independent Claim
32 words
A method of treating non-small cell lung cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5 trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
33 words
The method as defined in claim 4 wherein said 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof is administered at a dose of between about 5.6 mg/m 2 and about 38.18 mg/m 2 .
Claim 8
Independent Claim
31 words
A method of treating head and neck cancers in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof.
Claim 9
Independent Claim
31 words
A method of treating head and neck cancers in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim
33 words
The method as defined in claim 6 wherein said 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof is administered at a dose of between about 8 mg/m 2 and about 20 mg/m 2 .
Claim 11
Independent Claim
29 words
A method of treating breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof.
Claim 12
Independent Claim
29 words
A method of treating breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof.
Claim 13
Dependent Claim
33 words
The method as defined in claim 8 wherein said 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof is administered at a dose of between about 8 mg/m 2 and about 20 mg/m 2 .
Claim 14
Independent Claim
55 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of (8S,10S)-10-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-8-glycoloyl-7,8,9,10-tetrahydro-6,8,11-trihydroxy-1-methoxy-5,12-naphthacenedione or a pharmaceutically acceptable salt thereof.
Claim 15
Independent Claim
55 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of (8S,10S)-10-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-8-glycoloyl-7,8,9,10-tetrahydro-6,8,11-trihydroxy-1-methoxy-5,12-naphthacenedione or a pharmaceutically acceptable salt thereof.
Claim 16
Independent Claim
55 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of 5-fluoro-2,4(1H,3H)-pyrimidinedione or a pharmaceutically acceptable salt thereof.
Claim 17
Independent Claim
55 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of 5-fluoro-2,4(1H,3H)-pyrimidinedione or a pharmaceutically acceptable salt thereof.
Claim 18
Independent Claim
55 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of 2-amino-1,7-dihydro-6H-purine-6-thione or a pharmaceutically acceptable salt thereof.
Claim 19
Independent Claim
55 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of 2-amino-1,7-dihydro-6H-purine-6-thione or a pharmaceutically acceptable salt thereof.
Claim 20
Independent Claim
55 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of 22-oxo-vincaleukoblastine or a pharmaceutically acceptable salt thereof.
Claim 21
Independent Claim
55 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of 22-oxo-vincaleukoblastine or a pharmaceutically acceptable salt thereof.
Claim 22
Independent Claim
56 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of 2-bis[(2-chloroethyl)amino]tetrahydro-2H-1,3,2-oxazaphosphorine, 2-oxide, or a pharmaceutically acceptable salt thereof.
Claim 23
Independent Claim
56 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of 2-bis[(2-chloroethyl)amino]tetrahydro-2H-1,3,2-oxazaphosphorine, 2-oxide, or a pharmaceutically acceptable salt thereof.
Claim 24
Independent Claim
56 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-L-glutamic acid, or a pharmaceutically acceptable salt thereof.
Claim 25
Independent Claim
56 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-L-glutamic acid, or a pharmaceutically acceptable salt thereof.
Claim 26
Independent Claim
50 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of cis-diamminedichloroplatinum (II).
Claim 27
Independent Claim
50 words
A method of treating non-small cell lung cancer, head and neck cancers, or breast cancer in a mammal in need thereof comprising administering to said mammal an antineoplastically effective amount of 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine or a pharmaceutically acceptable salt thereof alone or in combination with an antineoplastically effective amount of cis-diamminedichloroplatinum (II).
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) | 1992-07-31 | 1993-01-30 | 1993-08-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-07-31 | 1997-01-30 | 1997-08-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-07-31 | 2001-01-30 | 2001-08-01 | $7700.00 | Window Closed / Lapsed |