التفاصيل البيبلوغرافية
| العنوان: |
METHOD FOR TREATING TUBERCULOSIS |
| Document Number: |
20120225113 |
| تاريخ النشر: |
September 6, 2012 |
| Appl. No: |
13/041047 |
| Application Filed: |
March 04, 2011 |
| مستخلص: |
Disclosed is a method for treating a symptom of M. tuberculosis infection in a subject, comprising administering the patient with an effective amount of (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)zetidin-2-one (EZETIMIBE). In the preferred embodiments, EZETIMIBE is capable of significantly inhibiting the survival and proliferation of Mycobacterium tuberculosis in the monocytes. The anti-tuberculous effect of EZETIMIBE is partly through stimulating CD13 leading to monocytes activation and thus bacterial killing of Mycobacterium tuberculosis, and partly through depleting the intracellular nutrition necessary for the survival of Mycobacterium tuberculosis. It is also proved that EZETIMIBE is capable of directly killing Mycobacterium tuberculosis outside cells. |
| Inventors: |
Lu, Yen-Ta (Taipei City, TW); Tsai, I-Fang (Taipei City, TW) |
| Assignees: |
MACKAY MEMORIAL HOSPITAL (Taipei City, TW) |
| Claim: |
1. A method for treating a symptom of Mycobacterium tuberculosis infection in a subject, comprising administering the subject an therapeutically effective amount of a compound of structural formula I or the pharmaceutically acceptable salt thereof, wherein [chemical expression included] R1 is selected from the group consisting of chloro, fluoro, —C≡C—C1-6alkyl-NR2R3, —(CH2)XCH═CH—C1-6alkyl-NR2R3, —C1-8alkyl-NR2R3, —C≡C—C1-4alkyl-CH—(CH2-NR2R3)2, —(CH2)XCH═CH—C1-4alkyl-CH—(CH2—NR2R3)2, —C1-6alkyl-CH—(CH2—NR2R3)2, —C≡C—C1-6alkyl-R3a, —(CH2)XCH═CH—C1-6alkyl-R3a, —C1-8alkyl-R3a, —C≡C—C1-6alkyl, —(CH2)XCH═CH—C1-6alkyl, —C1-8alkyl, —C2-15alkynyl mono- or poly-substituted with —OH and optionally substituted with R6, —C2-15alkenyl mono- or poly-substituted with —OH and optionally substituted with R6, and —C1-15alkyl mono- or poly-substituted with —OH and optionally substituted with R6, and x is an integer selected from 0, 1 and 2; R2 is independently selected at each occurrence from the group consisting of —H and —C1-3alkyl; R3 is independently selected at each occurrence from the group consisting of —H, —C1-3alkyl, —C(O)—C1-3alkyl, —C(O)—NR2R2, —SO2—C1-3alkyl and —SO2-phenyl; R3a is selected from the group consisting of —C(O)—NR2R2, —SO2—C1-3alkyl, and —SO2— phenyl; R4 is selected from the group consisting of —H, —OH, —C2-15alkynyl mono- or poly-substituted with —OH and optionally substituted with R6, —C2-15alkenyl mono- or poly-substituted with —OH and optionally substituted with R6, —C1-15alkyl mono- or poly-substituted with —OH and optionally substituted with R6; R5 is selected from the group consisting of —H and —OH; and R6 is a sugar residue optionally substituted with —COOH, —COOC1-3alkyl and —C1-3alkyl-OH. |
| Claim: |
2. The method as claimed in claim 1, wherein the subject is a mammal. |
| Claim: |
3. The method as claimed in claim 2, wherein the mammal is a human. |
| Claim: |
4. The method as claimed in claim 1, wherein the compound or the pharmaceutically acceptable salt thereof is administered orally, parentally, or topically. |
| Claim: |
5. The method as claimed in claim 1, wherein the compound is (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)zetidin-2-one. |
| Claim: |
6. A method for preventing a symptom of Mycobacterium tuberculosis infection in a subject, comprising administering the subject a prophylactically effective amount of the compound as claimed in claim 1 or the pharmaceutically acceptable salt thereof. |
| Claim: |
7. The method as claimed in claim 6, wherein the subject is a mammal. |
| Claim: |
8. The method as claimed in claim 7, wherein the mammal is a human. |
| Claim: |
9. The method as claimed in claim 6, wherein the compound or the pharmaceutically acceptable salt thereof is administered orally, parentally, or topically. |
| Claim: |
10. The method as claimed in claim 6, wherein the compound is (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)zetidin-2-one. |
| Claim: |
11. A pharmaceutical composition for treating or preventing a symptom of Mycobacterium tuberculosis infection in a subject, comprising the compound as claimed in claim 1 and a pharmaceutically acceptable carrier, diluent or excipient. |
| Claim: |
12. The pharmaceutical composition as claimed in claim 11, wherein the pharmaceutical composition is in the form of a tablet, a capsule, a powder, a granule, a solution, an emulsion, a gel, a transdermal patch, an aerosol, a microcapsule, or a liposome. |
| Claim: |
13. The pharmaceutical composition as claimed in claim 11, wherein the subject is a mammal. |
| Claim: |
14. The pharmaceutical composition as claimed in claim 13, wherein the mammal is a human. |
| Claim: |
15. The pharmaceutical composition as claimed in claim 11, wherein the compound is (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)zetidin-2-one. |
| Current U.S. Class: |
424/450 |
| Current International Class: |
61; 61; 61 |
| رقم الانضمام: |
edspap.20120225113 |
| قاعدة البيانات: |
USPTO Patent Applications |