US4197296A
Expired / Lapsed
US
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Androstanes
Assignee: Glaxo Group Ltd
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Filing: 1978-09-26
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Granted: 1980-04-08
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Expires: 1998-09-26
Abstract
Abstract Steroids of the androstane series are described which possess a 3α-hydroxy group, a 5α- or 5β- hydrogen atom, a 10- methyl group, an 11α- substituted amino group. The 17-position may be unsubstituted or substituted by a methyl or ethyl group in the β-configuration or by an oxo group, or there may be a 16β, 17β-epoxide group. A 2β-alkoxy group may optionally be present. The compounds, particularly their salts, have anaesthetic activity.
Inventors
- 👤 Gordon H. Phillipps
- 👤 George B. Ewan
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 22:03
CPC Classifications
C; C07; C07J; C07J41/00; C07J41/0005; C07J41/0016; C07J1/00; C07J1/0003; C07J1/0011; C07J13/00; C07J13/007; C07J21/00; C07J21/005; C07J21/008; C07J41/0011; C07J41/0033; C07J41/005; C07J71/00; C07J71/0005; C07J71/001
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
113 words
A compound of the formula ##STR2## wherein: one of R 1 and R 2 is a methyl group, the other group being a C 1-4 alkyl group, or R 1 and R 2 are both ethyl groups; R 3 is a hydrogen atom or a C 1-4 alkoxy group; and R 4 is a hydrogen atom or a methyl or ethyl group and R 5 and R 6 are hydrogen atoms; or R 4 and R 6 together represent an epoxide grouping and R 5 is a hydrogen atom; or R 4 and R 5 together represent an oxo group and R 6 is a hydrogen atom; and the acid addition salts thereof.
Claim 2
Dependent Claim
113 words
A compound of the formula ##STR2## wherein: one of R 1 and R 2 is a methyl group, the other group being a C 1-4 alkyl group, or R 1 and R 2 are both ethyl groups; R 3 is a hydrogen atom or a C 1-4 alkoxy group; and R 4 is a hydrogen atom or a methyl or ethyl group and R 5 and R 6 are hydrogen atoms; or R 4 and R 6 together represent an epoxide grouping and R 5 is a hydrogen atom; or R 4 and R 5 together represent an oxo group and R 6 is a hydrogen atom; and the acid addition salts thereof.
Claim 3
Dependent Claim
12 words
A compound as claimed in claim 1 which possesses a 5α-hydrogen atom.
Claim 4
Dependent Claim
14 words
A compound as claimed in claim 2 wherein R 3 is an alkoxy group.
Claim 5
Dependent Claim
14 words
A compound as claimed in claim 3 wherein R 3 is an ethoxy group.
Claim 6
Dependent Claim
17 words
A compound as claimed in claim 1 wherein R 1 and R 2 are both methyl groups.
Claim 7
Dependent Claim
32 words
A compound as claimed in claim 1 wherein R 4 and R 5 together represent an oxo group and R 3 is an alkoxy group, and wherein a 5α-hydrogen atom is present.
Claim 8
Dependent Claim
23 words
A compound as claimed in claim 1, said compound being: 11α-N,N-dimethylamino-2β-ethoxy-17β-methyl-5α-androstan-3α-ol; 11α-N,N-dimethylamino-2β-ethoxy-5α-androstan-3α-ol; 11α-N,N-dimethylamino-16β,17β-epoxy-2β-ethoxy-5α-androstan-3α-ol; or 11α-N,N-dimethylamino-17β-methyl-5α-androstan-3α-ol; or a physiologically acceptable acid addition salt thereof.
Claim 9
Dependent Claim
19 words
A compound as claimed in claim 1, said compound being 11α-N,N-dimethylamino-2β-ethoxy-3α-hydroxy-5α-androstan-17-one or a physiologically acceptable acid addition salt thereof.
Claim 10
Dependent Claim
16 words
A compound as claimed in claim 1 in the form of its hydrochloride or citrate salt.
Claim 11
Dependent Claim
19 words
A pharmaceutical composition consisting essentially of a compound as claimed in claim 1 and a pharmaceutical carrier or excipient.
Claim 12
Dependent Claim
17 words
A composition as claimed in claim 10 wherein said compound is formulated in a parenterally acceptable vehicle.
Claim 13
Dependent Claim
23 words
A composition as claimed in claim 11 which is an aqueous solution of a physiologically acceptable acid addition salt of the active compound.
Claim 14
Dependent Claim
26 words
A method of inducing anaesthesia in man or animals which comprises administering to the subject an effective amount of a compound as claimed in claim 1.
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) | 1983-04-08 | 1983-10-08 | 1984-04-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-04-08 | 1987-10-08 | 1988-04-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-04-08 | 1991-10-08 | 1992-04-08 | $7700.00 | Window Closed / Lapsed |