公开(公告)号：WO2009025820A3

公开(公告)日：2009-05-22

申请号：PCT/US2008009909

申请日：2008-08-20

Applicant: STC UNM ,  TIMMINS GRAHAM ,  MASTER SHARON ,  DERETIC VOJO P

Inventor： TIMMINS GRAHAM ,  MASTER SHARON ,  DERETIC VOJO P

IPC: A61K31/4409 ,  A61K31/44 ,  A61P31/00 ,  A61P43/00 ,  C07D213/127 ,  C07D213/16

CPC classification number: C07D213/81 ,  A61K9/0019 ,  A61K9/0073 ,  A61K31/44 ,  A61K31/4409 ,  C07D213/83 ,  C07D213/86

Abstract: The present invention relates to the use of isotopically labeled derivatives of isoniazid, ethionamide and related compounds as effective therapy for the treatment of mycobacterial diseases, including Mycobacterium tuberculosis.

Abstract translation: 本发明涉及异烟肼，乙硫异烟胺和相关化合物的同位素标记衍生物作为治疗包括结核分枝杆菌的分枝杆菌疾病的有效疗法的用途。

公开(公告)号：CA3055311A1

公开(公告)日：2018-08-16

申请号：CA3055311

申请日：2018-02-02

Applicant: STC UNM

Inventor： TIMMINS GRAHAM ,  DERETIC VOJO P

IPC: C07B59/00 ,  A61K31/136 ,  A61K51/04 ,  A61P11/00 ,  A61P31/04 ,  C07C213/08 ,  C07C215/68

Abstract: The present invention is directed to 13C and/or 2H isotope enhanced ambroxol ("isotope enhanced ambroxol") and its use in the treatment of autophagy infections, especially mycobacterial and other infections, disease states and/or conditions of the lung, such as tuberculosis, especially including drug resistant and multiple drag resistant tuberculosis. Pharmaceutical compositions comprising isotope enhanced amhroxol, alone or in combination with an additional bioactive agent, especially rifamycin antibiotics, including an additional autophagy modulator (an agent which is active to promote or inhibit autophagy), thus being useful against, an autophagy mediated disease state and/or condition), especially an antophagy mediated disease state and/or condition which occurs in the lungs, for example, a Mycobacterium infection. Chronic Obstructive Pulmonary Disease (COPD), asthma, pulmonary fibrosis, cystic fibrosis, Sjogren's disease and lung cancer (small cell and non-small cell lung cancer, among other disease states and/or conditions, especially of the lung. Methods of treating autophagy disease states and/or conditions, especially including autophagy disease states or conditions which occur principally in the lungs of a patient represent a further embodiment of the present invention. An additional embodiment includes methods of synthesizing compounds according to the present invention as otherwise disclosed herein.