EP0025599A1
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Benzopyran compounds, useful as chemotherapeutic agents
Assignee: Wellcome Foundation Ltd
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Filing: 1980-09-12
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Granted: —
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Expires: 2000-09-12
Abstract
Abstract Known and novel compounds of formula (I) wherein R 4 is hydrogen or lower alkyl, R 3 is hydrogen or lower alkyl and R 5 is a substituent, or R 3 and R 5 together form a group -CH 2 - or -CH 2 -CH 2 -, and R 1 and R 2 each represent four substituents or one or both R 1 and R 2 represents a methylenedioxy group and two substituents are active against viruses, especially rhinoviruses. Methods for producing the compounds are described, as are pharmaceutical formulations and methods for administering the compounds to cure or prevent rhinoviral infections.
Inventors
- 👤 John Frederick Batchelor
- 👤 Harold Francis Hodson
- 👤 Jeremy Gilbert Vinter
- 👤 John William Talbot Selway
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-31 20:51
CPC Classifications
C; C07; C07D; C07D311/00; C07D311/02; C07D311/94; A; A61; A61P; A61P31/00; A61P31/12; C07C; C07C45/00; C07C45/61; C07C45/67; C07C45/68; C07C45/72; C07C45/74; C07C49/00; C07C49/76; C07C49/82; C07C49/835; C07D311/04; C07D311/22; C07D311/26; C07D311/34; C07D311/58; C07D311/60; C07D311/78
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
158 words
A compound of formula (I), as a medicament, characterised in that R 4 is a hydrogen atom or a lower alkyl group and R 3 is a hydrogen atom or a lower alkyl group and R 5 is a substituent or R 3 and R 5 together form a group -CH 2 - or -CH 2 -CH 2 - and R 1 and R 2 each represent four substituents or one or both R and R 2 represents a methylenedioxy group and two substituents, each of the aforementioned substituents, R 1 , R 2 , and R 5 being independently selected from hydrogen and halogen atoms, ( lower ) alkyl, hydroxy( lower )alkyl, carboxy ( lower )alkyl, ( lower )alkoxy, amino, ( lower )alkylamino, di( lower ) alkylamino, acylamino, nitro, cyano, trifluoromethyl, carboxyl and hydroxyl groups; provided that at least one of R 3 and R 4 is other than hydrogen; and where appropriate salts or esters thereof.
Claim 2
Dependent Claim
158 words
A compound of formula (I), as a medicament, characterised in that R 4 is a hydrogen atom or a lower alkyl group and R 3 is a hydrogen atom or a lower alkyl group and R 5 is a substituent or R 3 and R 5 together form a group -CH 2 - or -CH 2 -CH 2 - and R 1 and R 2 each represent four substituents or one or both R and R 2 represents a methylenedioxy group and two substituents, each of the aforementioned substituents, R 1 , R 2 , and R 5 being independently selected from hydrogen and halogen atoms, ( lower ) alkyl, hydroxy( lower )alkyl, carboxy ( lower )alkyl, ( lower )alkoxy, amino, ( lower )alkylamino, di( lower ) alkylamino, acylamino, nitro, cyano, trifluoromethyl, carboxyl and hydroxyl groups; provided that at least one of R 3 and R 4 is other than hydrogen; and where appropriate salts or esters thereof.
Claim 3
Dependent Claim
36 words
A compound as claimed in claim 1 characterised in that R and R 2 each represent four substituents independently selected from hydrogen and halogen atoms, amino, hydroxyl, methyl, ethyl, methoxy, ethoxy, hydroxymethyl, trifluoromethyl and cyano groups.
Claim 4
Dependent Claim
37 words
A compound as claimed in either claim 1 or claim 2 characterised in that at least two of the substituents represented by R 1 and at least two of the substituents represented by R are hydrogen atoms.
Claim 5
Dependent Claim
53 words
A compound as claimed in claim 3 characterised in that substituents other than hydrogen atoms represented by R in the compound of formula ( I ) are located at the 6 and/or 7 positions and substituents other than hydrogen atoms represented by R 2 are located at the 3', 4', and/or 5' positions.
Claim 6
Dependent Claim
131 words
A compound of formula ( IA ) as a medicament wherein R is a hydrogen atom or a lower alkyl group and R 3 is a hydrogen atom or a lower alkyl group and R is a substituent selected from the group defined below, or R and R 5 together form a group -CH 2 - or -CH 2 -CH 2 - and R 1A and R 2A are the same or different and are selected from hydrogen or halogen atoms, ( lower )alkyl, hydroxy ( lower )alkyl, carboxy ( lower )alkyl, ( lower )alkoxy, amino, ( lower )alkylamino, di( lower )alkylamino, acylamino, nitro, cyano, trifluoromethyl, carboxyl and hydroxyl groups; provided that at least one of R 3 and R is other than hydrogen; and where appropriate salts or esters thereof.
Claim 7
Dependent Claim
131 words
A compound of formula ( IA ) as a medicament wherein R is a hydrogen atom or a lower alkyl group and R 3 is a hydrogen atom or a lower alkyl group and R is a substituent selected from the group defined below, or R and R 5 together form a group -CH 2 - or -CH 2 -CH 2 - and R 1A and R 2A are the same or different and are selected from hydrogen or halogen atoms, ( lower )alkyl, hydroxy ( lower )alkyl, carboxy ( lower )alkyl, ( lower )alkoxy, amino, ( lower )alkylamino, di( lower )alkylamino, acylamino, nitro, cyano, trifluoromethyl, carboxyl and hydroxyl groups; provided that at least one of R 3 and R is other than hydrogen; and where appropriate salts or esters thereof.
Claim 8
Dependent Claim
52 words
A compound as claimed in claim 5 characterised in that R is a hydrogen atom, R 3 is a methyl group or a hydrogen atom and R 5 is a hydrogen atom, or R and R 5 together form a group -CH 2 - or -CH 2 - CH 2 - .
Claim 9
Dependent Claim
35 words
Trans-3-methylflavan, trans-4',6-dichloro-3-methylflavan, cis-4b,10,10a,11-tetrahydrobenz(b)indeno(2,1-e)pyran, cis-8-chloro 4b, 10, 10a, 11-tetrahydrobenz(b)indeno(2,1-e)pyran, cis-2-chloro 4b, 10, 10a, 11-tetrahydrobenz(b)indeno(2,1-e)pyran, cis-2,8-dichloro 4b, 10, 10a, 11-tetrahydrobenz(b)indeno(2,1-e)pyran, cis-5, 6, 6a, 12a-tetrahydro-7H-benzo(e)xanthene, cis-3-chloro 5, 6, 6a, 12a-tetrahydro-7H-benzo(c)xanthene, and cis-9-chloro 5, 6, 6a, 12a-tetrahydro-7H-benzo(c)xanthene, as medicaments.
Claim 10
Dependent Claim
35 words
Trans-3-methylflavan, trans-4',6-dichloro-3-methylflavan, cis-4b,10,10a,11-tetrahydrobenz(b)indeno(2,1-e)pyran, cis-8-chloro 4b, 10, 10a, 11-tetrahydrobenz(b)indeno(2,1-e)pyran, cis-2-chloro 4b, 10, 10a, 11-tetrahydrobenz(b)indeno(2,1-e)pyran, cis-2,8-dichloro 4b, 10, 10a, 11-tetrahydrobenz(b)indeno(2,1-e)pyran, cis-5, 6, 6a, 12a-tetrahydro-7H-benzo(e)xanthene, cis-3-chloro 5, 6, 6a, 12a-tetrahydro-7H-benzo(c)xanthene, and cis-9-chloro 5, 6, 6a, 12a-tetrahydro-7H-benzo(c)xanthene, as medicaments.
Claim 11
Dependent Claim
101 words
A compound of formula ( IA ) characterised in that R 4 is a hydrogen atom or a lower alkyl group and R 3 is a hydrogen atom or a lower alkyl group and R 5 is hydrogen or R 3 and R 5 together form a group -CH 2 - or -CH 2 -CH 2 - and R 1A and R 2A are the same or different and are selected from halogen atom, cyano, nitro and trifluoromethyl groups; provided that at least one of R 3 and R 4 is other than hydrogen; and where appropriate salts or esters thereof.
Claim 12
Dependent Claim
101 words
A compound of formula ( IA ) characterised in that R 4 is a hydrogen atom or a lower alkyl group and R 3 is a hydrogen atom or a lower alkyl group and R 5 is hydrogen or R 3 and R 5 together form a group -CH 2 - or -CH 2 -CH 2 - and R 1A and R 2A are the same or different and are selected from halogen atom, cyano, nitro and trifluoromethyl groups; provided that at least one of R 3 and R 4 is other than hydrogen; and where appropriate salts or esters thereof.
References Cited (Backward Citations)
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