WO1989002741A2 - Inhibiteurs de la transcriptase inverse de l'hiv servant au traitement du sida - Google Patents

Inhibiteurs de la transcriptase inverse de l'hiv servant au traitement du sida

Info

Publication number
WO1989002741A2
WO1989002741A2 PCT/US1988/003114 US8803114W WO8902741A2 WO 1989002741 A2 WO1989002741 A2 WO 1989002741A2 US 8803114 W US8803114 W US 8803114W WO 8902741 A2 WO8902741 A2 WO 8902741A2
Authority
WO
WIPO (PCT)
Prior art keywords
composition according
compound
group
salts
immunodeficiency virus
Prior art date
Application number
PCT/US1988/003114
Other languages
English (en)
Other versions
WO1989002741A1 (fr
Inventor
Fritz Reusser
William Gary Tarpley
Irene W. Althaus
Original Assignee
The Upjohn Company
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by The Upjohn Company filed Critical The Upjohn Company
Publication of WO1989002741A2 publication Critical patent/WO1989002741A2/fr
Publication of WO1989002741A1 publication Critical patent/WO1989002741A1/fr

Links

Definitions

  • This invention is a novel treatment of patients infected with a human immunodeficiency virus.
  • AZT zidovudine
  • This invention is a method for treating a human infected with one or more than one strain of a human immunodeficiency virus which comprises administering an effective amount of a compound selected from the group consisting of lomofungin, paulomycin A, mycorhodin, antibiotic 357b, phenolphthalein diacetate, phenolphthalexon, thymophthalexon, U-64161, U-46768, U-18230, U-21052A, U-23278D, U-45483, U-57057, U-62455, U-12978E, U-42529, U-23034, diazaquinomycin A, maduramycin, and chelocardin or salts thereof, to the infected human.
  • a compound selected from the group consisting of lomofungin, paulomycin A, mycorhodin, antibiotic 357b, phenolphthalein diacetate, phenolphthalexon, thymophthalexon, U-64161, U-46768, U-18230, U-210
  • human immunodeficiency virus means human immunodeficiency virus type I, human immunodeficiency virus type II, or strains, apparent to one skilled in the art, which belong to the same viral family and which create similar physiological effects in humans as human immunodeficiency virus types I or II.
  • dosage forms include oral formulations, such as tablets or capsules, or parenteral formulations, such as sterile solutions.
  • an effective amount is from about 1 to 100 mg per kg per day.
  • a typical unit dose for a 70 kg human would be from about 200 mg to 1000 mg taken one to four times per day.
  • Either solid or fluid dosage forms can be prepared for oral administration.
  • Solid compositions are prepared by mixing the compounds used to practice the method claimed in this invention with conventional ingredients such as talc, magnesium stearate, dicalcium phosphate, magnesium aluminum silicate, calcium sulfate, starch, lactose, acacia, methyl cellulose, or functionally similar pharmaceutical diluents and carriers.
  • Capsules are prepared by mixing the compounds used to practice the method claimed in this invention with an inert pharmaceutical diluent and placing the mixture into an appropriately sized hard gelatin capsule.
  • Soft gelatin capsules are prepared by machine encapsulation of a slurry of the compounds used to practice the method claimed in this invenition with an acceptable inert oil such as vegetable oil or light liquid petrolatum.
  • Syrups are prepared by dissolving the compounds used to practice the method claimed in this invention in an aqueous vehicle and adding sugar, aromatic flavoring agents and preservatives.
  • Elixirs are prepared using a hydroalcoholic vehicle such as ethanol, suitable sweeteners such as sugar or saccharin and an aromatic flavoring agent.
  • Suspensions are prepared with an aqueous vehicle and a suspending agent such as acacia, tragacanth, or methyl cellulose.
  • parenteral solutions are prepared by dissolving the compounds used to practice the method claimed in this invention in water and filter sterilizing the solution before placing in a suitable sealable vial or ampule.
  • Parenteral suspensions are prepared in substantially the same way except a sterile suspension vehicle is used and the compounds used to practice the method claimed in this invention are sterilized with ethylene oxide or suitable gas before it is suspended in the vehicle.
  • Patients to be treated would be those individuals: 1) infected with one or more than one strain of a human immunodeficiency virus as determined by the presence of either measurable viral antibody or antigen in the serum and 2) having either a symptomatic AIDS defining infection such as i) disseminated histoplasmosis, ii) isoporiasis, iii) bronchial and pulmonary candidiasis including pneumocystis pneumonia iv) non-Hodgkin's lymphoma or v) Kaposi's sarcoma and being less than sixty years old; or having an absolute CD4 lymphocyte count of less than 200/mm 3 in the peripheral blood.
  • Treatment would consist of maintaining an inhibitory level of the compounds of this invention in the patient at all times and would continue until the occurrence of a second symptomatic AIDS defining infection indicates alternate therapy is needed.
  • One thousand two-piece hard gelatin capsules for oral use, each capsule containing 50 mg of phenolphthalein diacetate, are prepared from the following:
  • Phenolphthalein diacetate 50 gm Lactose 100 gm
  • Example 2 Tablets One thousand tablets, each containing 50 mg of phenolphthalein diacetate, are prepared from the following:
  • a sterile aqueous solution for parenteral intravenous injection containing 150 mg of phenolphthalein diacetate in one liter of solution is prepared from the following:
  • the phenolphthalein diacetate sodium salt is sterilized, added to the sterile water, filled into sterile containers and sealed.
  • Diazaquinomycin A which is rather insoluble in DMF or water, was tested as a suspension.

Abstract

Les composés décrits, qui sont sélectionnés dans un groupe composé de lomofungine, paulomycine A, mycorhodine, antibiotique 357b, diacétate de phénolphthaléine, phénolphthalexon, thymophthalexon, U-64161, U-46768, U-18230, U-21052A, U-23278D, U-45483, U-57057, U-62455, U-12978E, U-42529, U-23034, diazoquinomycine A, maduramycine et chélocardine ou de sels de ces composés peuvent être utilisés pour traiter des patients humains infectés avec une ou plusieurs souches d'un virus d'immunodéficience humain (HIV).
PCT/US1988/003114 1987-09-28 1988-09-16 Inhibiteurs de la transcriptase inverse de l'hiv servant au traitement du sida WO1989002741A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US107,123 1979-12-26
US10170687A 1987-09-28 1987-09-28
US101,706 1987-09-28
US10712387A 1987-10-09 1987-10-09

Publications (2)

Publication Number Publication Date
WO1989002741A2 true WO1989002741A2 (fr) 1989-04-06
WO1989002741A1 WO1989002741A1 (fr) 1989-04-06

Family

ID=26798544

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1988/003114 WO1989002741A1 (fr) 1987-09-28 1988-09-16 Inhibiteurs de la transcriptase inverse de l'hiv servant au traitement du sida

Country Status (2)

Country Link
AU (1) AU2527488A (fr)
WO (1) WO1989002741A1 (fr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6800658B2 (en) * 1997-11-20 2004-10-05 Children's Medical Center Corporation Substituted diphenyl indanone, indane and indole compounds and analogues thereof useful for the treatment of prevention of diseases characterized by abnormal cell proliferation
US8754054B2 (en) 2010-07-09 2014-06-17 Albany Molecular Research, Inc. Antibacterial compounds, methods of making them, and uses thereof

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3359165A (en) * 1966-11-02 1967-12-19 Upjohn Co Antibiotic lomondomycin and method of production

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