Claims
- 1. A method for the manufacture of a topical pharmaceutically active antimicrobial composition which comprises admixing a sterol conjugate compound of the formula ##STR15## wherein each R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is individually selected from the group consisting of H, OH and OSO.sub.3 H; and wherein Y is NH(CH.sub.2).sub.3 NH(CH.sub.2).sub.4 NH(CH.sub.2).sub.3 NH.sub.2, NHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, or NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 together with a pharmaceutically acceptable carrier for topical administration, said conjugate compound being in a sufficient concentration as to provide an antimicrobial dose of from 1 .mu.g to 100 mg of said conjugate compound.
- 2. A method according to claim 1 wherein the resulting antimicrobial composition is a gel, ointment, solution, or salve.
- 3. A method for bringing about an antimicrobial effect in a mammal which comprises administering to said mammal by topical means an antimicrobial composition which comprises an active agent consisting of a sterol conjugate compound of the formula ##STR16## wherein each R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is individually selected from the group consisting of H, OH and OSO.sub.3 H; and wherein Y is NH(CH.sub.2).sub.3 NH(CH.sub.2).sub.4 NH(CH.sub.2).sub.3 NH.sub.2, NHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, or NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 in admixture with a pharmaceutically acceptable carrier suitable for topical administration, said agent being present in a sufficient amount to bring about the antimicrobial effect.
- 4. A method to bring about an antimicrobial effect in a mammal which comprises administering to said mammal by topical means an antimicrobial composition which comprises a pharmaceutically-active sterol conjugate compound of a formula selected from the group consisting of (A) ##STR17## wherein R.sub.1 is from the group H or SO.sub.3 H, and wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 ; (B) ##STR18## wherein R.sub.1 is from the group H or SO.sub.3 H, and wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 ; (C) ##STR19## wherein R.sub.1 is from the group H or SO.sub.3 H, and wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 ; (D) ##STR20## wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 ; (E) ##STR21## wherein R.sub.1 is from the group H or SO.sub.3 H, and wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 ; (F) ##STR22## wherein R.sub.1 is from the group H or SO.sub.3 H, and wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 ; and (G) ##STR23## wherein R.sub.1 is from the group H or SO.sub.3 H, and wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2.
- 5. A method for the manufacture of a topical pharmaceutically-active antimicrobial composition which comprises admixing a sterol conjugate compound of a formula selected from the group consisting of (A) ##STR24## wherein R.sub.1 is from the group H or SO.sub.3 H, and wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 ; (B) ##STR25## wherein R.sub.1 is from the group H or SO.sub.3 H, and wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 ; (C) ##STR26## wherein R.sub.1 is from the group H or SO.sub.3 H, and wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 ; (D) ##STR27## wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 ; (E) ##STR28## wherein R.sub.1 is from the group H or SO.sub.3 H, and wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 ; (F) ##STR29## wherein R.sub.1 is from the group H or SO.sub.3 H, and wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 ; and (G) ##STR30## wherein R.sub.1 is from the group H or SO.sub.3 H, and wherein R.sub.2 is from the group CO-spermine, CONHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, and CONHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2 with a pharmaceutically acceptable carrier for topical administration, said conjugate being in a sufficient concentration as to provide an antimicrobial dose of from 1 .mu.g to 100 mg of said conjugate compound.
Parent Case Info
This is a continuation of application Ser. No. 08/711,161, filed Sep. 9, 1996, now abandoned, which is a continuation-in-part of application Ser. No. 08/452,846, filed May 30, 1995, now U.S. Pat. No. 5,583,239.
Government Interests
Partial financial support in the making of the invention described herein was provided by the National Institutes of Health. In view of providing financial support to the making of the invention described herein, the United States government has certain statutory interests in the invention under 35 USC 200 et seq.
US Referenced Citations (3)
Non-Patent Literature Citations (1)
Entry |
International Publication No. WO 95/29186; Compositions and methods for cell transformation; based upon International Patent Application No. PCT/US95/04806; Inventors: Kahne and Kahne; Applicant: The Trustees of Princeton University; Nov. 2, 1995. |
Continuations (1)
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711161 |
Sep 1996 |
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Continuation in Parts (1)
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452846 |
May 1995 |
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