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Pharmaceutical compositions having immunosuppressant activity and methods therefor

Assignee: Smith Kline & French Laboratories Ltd
•
Filing: 1977-11-21
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Granted: 1980-05-27
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Expires: 1997-11-21
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Abstract

Abstract S-(Aminoalkyl)isothioureas which have immunosuppressant activity. Two specific compounds are 2-(3-dimethylaminopropylthio)-2-imidazoline and N,N'-dimethyl-S-(3-dimethylaminopropyl)isothiourea.

Inventors

  • 👤 Graham J. Durant
  • 👤 Charon R. Ganellin
  • 👤 Margaret R. Vickers

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-08 02:43
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/04; C07D295/08; C07D295/084; C07D295/088; C07C; C07C335/00; C07C335/30; C07C335/32; C07D233/00; C07D233/04; C07D233/28; C07D233/30; C07D233/42

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 92 words
An isothiourea derivative of the Formula: ##STR3## wherein n is 2, 3 or 4; R 1 and R 2 , which may be the same or different, are lower alkyl; and R 3 and R 4 , which may be the same or different, together form a --(CH 2 ) x -- group wherein x is 2, 3 or 4; provided that when n is 2, R 3 and R 4 must be such that together they form a (CH 2 ) 4 group; and the pharmaceutically acceptable acid addition salts thereof.
Claim 2
Dependent Claim 92 words
An isothiourea derivative of the Formula: ##STR3## wherein n is 2, 3 or 4; R 1 and R 2 , which may be the same or different, are lower alkyl; and R 3 and R 4 , which may be the same or different, together form a --(CH 2 ) x -- group wherein x is 2, 3 or 4; provided that when n is 2, R 3 and R 4 must be such that together they form a (CH 2 ) 4 group; and the pharmaceutically acceptable acid addition salts thereof.
Claim 3
Dependent Claim 12 words
An isothiourea according to claim 1 wherein n is 2 or 3.
Claim 4
Dependent Claim 39 words
An isothiourea according to claim 1 wherein n is 3; R 1 and R 2 are lower alkyl; and R 3 and R 4 together with the two nitrogen atoms and the carbon atom shown form an imidazoline ring.
Claim 5
Dependent Claim 27 words
An isothiourea according to claim 1 wherein R 3 and R 4 together with the two nitrogen atoms and the carbon atom shown form an imidazoline ring.
Claim 6
Independent Claim 85 words
A method of producing immunosuppressant activity by administering to an animal in need thereof an effective amount of an isothiourea of the formula: ##STR4## wherein n is 2, 3 or 4; R 1 and R 2 , which may be the same or different, are lower alkyl; and R 3 and R 4 , which may be the same or different, together form a --(CH 2 ) x -- group where x is 2, 3 or 4, or a pharmaceutically acceptable acid addition salt thereof.
Claim 7
Independent Claim 85 words
A method of producing immunosuppressant activity by administering to an animal in need thereof an effective amount of an isothiourea of the formula: ##STR4## wherein n is 2, 3 or 4; R 1 and R 2 , which may be the same or different, are lower alkyl; and R 3 and R 4 , which may be the same or different, together form a --(CH 2 ) x -- group where x is 2, 3 or 4, or a pharmaceutically acceptable acid addition salt thereof.
Claim 8
Independent Claim 86 words
A method of treating rheumatoid arthritis by administering to an animal in need thereof an effective amount of an isothiourea derivative of the formula: ##STR5## wherein n is 2, 3 or 4; R 1 and R 2 , which may be the same or different, are lower alkyl; and R 3 and R 4 , which may be the same or different, together form a --(CH 2 ) x -- group where x is 2, 3 or 4, or a pharmaceutically acceptable acid addition salt thereof.
Claim 9
Independent Claim 86 words
A method of treating rheumatoid arthritis by administering to an animal in need thereof an effective amount of an isothiourea derivative of the formula: ##STR5## wherein n is 2, 3 or 4; R 1 and R 2 , which may be the same or different, are lower alkyl; and R 3 and R 4 , which may be the same or different, together form a --(CH 2 ) x -- group where x is 2, 3 or 4, or a pharmaceutically acceptable acid addition salt thereof.
Claim 10
Independent Claim 85 words
A method of treating psoriasis by administering to an animal in need thereof a therapeutically effective amount of an isothiourea of the formula: ##STR6## wherein n is 2, 3 or 4; R 1 and R 2 , which may be the same or different, are lower alkyl; and R 3 and R 4 , which may be the same or different, together form a --(CH 2 ) x -- group where x is 2, 3 or 4, or a pharmaceutically acceptable acid addition salt thereof.
Claim 11
Independent Claim 85 words
A method of treating psoriasis by administering to an animal in need thereof a therapeutically effective amount of an isothiourea of the formula: ##STR6## wherein n is 2, 3 or 4; R 1 and R 2 , which may be the same or different, are lower alkyl; and R 3 and R 4 , which may be the same or different, together form a --(CH 2 ) x -- group where x is 2, 3 or 4, or a pharmaceutically acceptable acid addition salt thereof.
Claim 12
Independent Claim 84 words
A method of reducing inflammation by administering to an animal in need thereof a therapeutically effective amount of an isothiourea of the formula: ##STR7## wherein n is 2, 3 or 4; R 1 and R 2 , which may be the same or different, are lower alkyl; and R 3 and R 4 , which may be the same or different, together form a --(CH 2 ) x -- group where x is 2, 3 or 4, or a pharmaceutically acceptable acid salt thereof.
Claim 13
Independent Claim 84 words
A method of reducing inflammation by administering to an animal in need thereof a therapeutically effective amount of an isothiourea of the formula: ##STR7## wherein n is 2, 3 or 4; R 1 and R 2 , which may be the same or different, are lower alkyl; and R 3 and R 4 , which may be the same or different, together form a --(CH 2 ) x -- group where x is 2, 3 or 4, or a pharmaceutically acceptable acid salt thereof.
Claim 14
Dependent Claim 17 words
A method according to claim 8 wherein the isothiourea is 2-(2-dimethylaminoethylthio)-2-imidazoline or a pharmaceutically acceptable salt thereof.

References Cited (Backward Citations)

US2813102A Cited
US3334112A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1983-05-27 1983-11-26 1984-05-27 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1987-05-27 1987-11-26 1988-05-27 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1991-05-27 1991-11-26 1992-05-27 $7700.00 Window Closed / Lapsed

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