التفاصيل البيبلوغرافية
| العنوان: |
LACTONE FORMULATIONS AND METHOD OF USE |
| Document Number: |
20110092588 |
| تاريخ النشر: |
April 21, 2011 |
| Appl. No: |
12/968508 |
| Application Filed: |
December 15, 2010 |
| مستخلص: |
Compounds of Formulae Ia and Ic having a lactone structure and an methylene group at the alpha-position of the lactone structure and methods for using and making the compounds have been disclosed. The lactone compounds can be reacted with an neucleaphilic agent to open the lactone ring to a compound of Formula Ib. The lactone of Formula Ia and its functional derivatives have been isolated from Securidaca virgata. These compounds are referred to as LMSV-6 or Securolide™. The purified compounds have demonstrated activity in assays for anti-bacterial and anti-fungal activities, and for treating proliferation disorders such as cancer. Based on the in vitro assays, the lactones are useful for treating proliferation disorders including, for example, breast cancer, colon cancer, rectal cancer, stomach cancer, pancreatic cancer, lung cancer, liver cancer, ovarian cancer, esophageal cancer, and leukemia. They are also effective for treatment of bacterial and fungal infections, including treatment of peptic ulcer disease; gingivitis and periodontitis. The lactone and its derivatives has the following chemical structure: [chemical expression included] wherein R1-R9 and Y1-Y3 taken independently are preferably a hydrogen atom, a halogen atom, a hydroxyl group, or any other organic groups or groupings which optionally include a heteroatom such as oxygen, sulfur, or nitrogen groupings in linear, branched, or cyclic structural formats; Z and X are independently and preferably a heteroatom such as oxygen, sulfur, or nitrogen groupings in linear, branched, or cyclic structural formats; and Z′ may a hydrogen atom, a halogen atom, a hydroxyl group, or any other organic groups or groupings which optionally include a heteroatom such as oxygen, sulfur, or nitrogen groupings in linear, branched, or cyclic structural formats. |
| Inventors: |
Terrero, David (Ensanche Quisquella, DO) |
| Claim: |
1.-31. (canceled) |
| Claim: |
32. A method of treating an infection or a disease or disorder caused by an infection in a patient, the method comprising administering a pharmaceutical composition comprising an effective amount of a compound of Formula Ia [chemical expression included] wherein R1-R7 taken independently or R3-R6 taken together are a hydrogen atom or a group or grouping selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, halo, hydroxyl, alkoxy, substituted alkoxy, phenoxy, substituted phenoxy, aroxy, substituted aroxy, alkylthio, substituted alkylthio, phenylthio, substituted phenylthio, arylthio, substituted arylthio, cyano, isocyano, substituted isocyano, carbonyl, substituted carbonyl, carboxyl, substituted carboxyl, amino, substituted amino, amido, substituted amido, sulfonyl, substituted sulfonyl, sulfonic acid, phosphoryl, substituted phosphoryl, phosphonyl, substituted phosphonyl, polyaryl, substituted polyaryl, C1-C20 cyclic, substituted C1-C20 cyclic, heterocyclic, substituted heterocyclic, aminoacid, peptide, and polypeptide groups; Z is a heteroatom selected from the group consisting of oxygen, sulfur, and nitrogen groupings in linear, branched, or cyclic structural formats; and X is a heteroatom selected from the group consisting of oxygen, sulfur, and nitrogen groupings in linear, branched, or cyclic structural formats, or a pharmaceutically acceptable salt thereof; and a pharmaceutical carrier for enteral, parenteral, or topical administration. |
| Claim: |
33. The method of claim 43 wherein the infection is bacterial. |
| Claim: |
34. The method of claim 43 wherein the infection is fungal. |
| Claim: |
35. The method of claim 43, wherein the infection is viral. |
| Claim: |
36. The method of claim 43, wherein the bacteria is selected from the group consisting of Escherichia coli, Klebsiela pneumoniae, Pseudomona aeroginosa, and Staphylococus aureus. |
| Claim: |
37. The method of claim 43, wherein the disease or disorder is selected from the group consisting of peptic ulcer disease, gastritis, dyspepsia, periodontal disease, and gingivitis. |
| Claim: |
38. The method of claim 44, wherein the fungal infection is caused by a fungus selected from the group consisting of Saccharomyces cerevisiae, Candida albicans, Candida glabrata, Candida krusei, Candida tropicalis, Candida pseudotropicalis, Candida parapsilosis, Aspergillus fumigatus, Aspergillus flavus, Aspergillus niger, Cryptococcus neoformans, Microsporum canis, Trichophyton rubrun, Trichophyton mentagrophyte. |
| Claim: |
39. The method of claim 44, wherein the disease or disorder caused by the fungal infection is selected from the group consisting of candidosis, cryptococcosis, and aspergillosis. |
| Claim: |
40. The method of claim 49, wherein candidosis is selected from the group consisting of digestive candidosis, urinary candidosis, vaginal candidosis, and cutaneous candidosis. |
| Claim: |
41. The method of claim 49, wherein the cryptococcosis is selected from the group consisting of neuromeningeal cryptococcosis, pulmonary cryptococcosis, and cutaneous cryptococcosis. |
| Claim: |
42. The method of claim 49, wherein the aspergillosis is selected from the group consisting of bronchopulmonary aspergillosis, pulmonary aspergillosis, and invasive aspergillosis of the immunodepressive system. |
| Claim: |
43. The method of claim 43 wherein the carrier for oral administration is selected from the group consisting of a mouthwash, lozenge, tablet, capsule, solution, suspension, granule, and lollipop. |
| Claim: |
44. The method of claim 53, wherein the effective amount comprises a dose from about 0.1 to about 50 mg/kg/day. |
| Claim: |
45. The method of claim 54, wherein the dose is administered as a single daily dose or a divided daily dose. |
| Claim: |
46. The method of claim 43 wherein the carrier for topical administration is selected from the group consisting of a suppository, ointment, cream, gel, paste, colloidion, glycerogelatin, liniment, lotion, paste, plaster, powder, tape, patch, aerosol, solution, and tincture. |
| Claim: |
47. The method of claim 43 wherein the composition is suitable for administration by injection. |
| Claim: |
48. The method of claim 55, wherein the effective amount comprises a dose from about 0.1 to about 100 mg/kg/day. |
| Claim: |
49. The method of claim 56, wherein the dose is administered as a single daily dose or a divided daily dose. |
| Claim: |
50. The method of claim 43 wherein the lactone is defined by the structure: [chemical expression included] wherein R1-R6 are hydrogen atoms; Z is an oxygen; and X is an oxygen. |
| Claim: |
51. The method of claim 58 wherein X is oxygen. |
| Claim: |
52. The method of claim 58 wherein R5 is an exocyclic methylene. |
| Claim: |
53. The method of claim 43, wherein the effective amount is from 1 to 5 mg/kg/day. |
| Claim: |
54. The method of claim 43, wherein the pharmaceutical composition further comprises one or more additional active agents. |
| Current U.S. Class: |
514/473 |
| Current International Class: |
61; 61; 61; 61 |
| رقم الانضمام: |
edspap.20110092588 |
| قاعدة البيانات: |
USPTO Patent Applications |
