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    ISOTOPE ENHANCED AMBROXOL FOR LONG LASTING AUTOPHAGY INDUCTION
    1.
    发明申请
    ISOTOPE ENHANCED AMBROXOL FOR LONG LASTING AUTOPHAGY INDUCTION 审中-公开

    公开(公告)号：US20190269806A1

    公开(公告)日：2019-09-05

    申请号：US16412017

    申请日：2019-05-14

    Applicant: STC.UNM

    Inventor： Graham Timmins ,  Vojo P. Deretic

    IPC: A61K51/04 ,  A61K35/00 ,  A61P11/00 ,  A61P31/06 ,  A61K31/136

    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 ambroxol, 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 autophagy 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.

    IRGM AND PRECISION AUTOPHAGY CONTROLS FOR ANTIMICROBIAL AND INFLAMMATORY DISEASE STATES AND METHODS OF DETECTION OF AUTOPHAGY
    5.
    发明申请
    IRGM AND PRECISION AUTOPHAGY CONTROLS FOR ANTIMICROBIAL AND INFLAMMATORY DISEASE STATES AND METHODS OF DETECTION OF AUTOPHAGY 审中-公开

    公开(公告)号：US20180236024A1

    公开(公告)日：2018-08-23

    申请号：US15553786

    申请日：2016-02-25

    Applicant: STC.UNM

    Inventor： Vojo P. Deretic ,  Tomonori Kimura

    IPC: A61K38/05 ,  A61K45/06 ,  A61K38/17 ,  A61K31/713 ,  A61P1/00 ,  A61P29/00

    CPC classification number: A61K38/05 ,  A61K31/713 ,  A61K38/17 ,  A61K45/06 ,  A61P1/00 ,  A61P29/00 ,  A61K2300/00

    Abstract: The present invention relates to the discovery that IRGM, encoded by a uniquely human gene which confers risk for inflammatory diseases, affects autoophagy through a hitherto unknown mechanism. The present invention shows that IRGM controls autophagy and that IRGM modulators, in particular, double-stranded RNA, including poly I:C, poly-UG (polyUGUGU) and polyl-CLC and muramyldipeptide and related analogs of same, including N-acetyl muramyl-L-alanyl-D-isoglutamine (DMP) and numerous other compounds as identified herein, which may be used alone, in combination, or in combination with alternative autophagy modulators and additional bioactive agents to provide effective therapies for a number of diseases, including cancer, bacterial infections and inflammatory diseases, especially including tuberculosis infections and Crohn's disease, among others. The present invention is also directed to compositions and methods for treating inflammatory or autophagy-related diseases including diseases which cause excessive inflammation in patients.

    TREATMENT OF AUTOPHAGY-RELATED DISORDERS
    6.
    发明申请
    TREATMENT OF AUTOPHAGY-RELATED DISORDERS 审中-公开
    治疗自身免疫性疾病

    公开(公告)号：US20160136123A1

    公开(公告)日：2016-05-19

    申请号：US14898062

    申请日：2014-05-29

    Applicant: Vojo P. DERETIC ,  Michale MANDELL ,  STC.UNM

    Inventor： Vojo P. Deretic ,  Michael Mandell

    IPC: A61K31/201 ,  C12Q1/61 ,  C12Q1/44 ,  A61K45/06 ,  A61K38/53

    CPC classification number: A61K31/201 ,  A61K38/53 ,  A61K45/06 ,  C12N9/93 ,  C12Q1/44 ,  C12Q1/61 ,  C12Y603/02 ,  G01N2333/92 ,  G01N2405/00 ,  G01N2405/02 ,  G01N2500/20 ,  G01N2800/7028

    Abstract: The present invention relates to the use of neutral lipids, including triglycerides, diglycerides and monoglycerides which may be used to increase neutral lipids (lipid stores and/or lipid droplets) and neutral lipid stores in order to regulate (in particular, induce) autophagy and treat and/or prevent autophagy related disease states and/or conditions. In one embodiment, the invention relates to the use of neutral lipids and/or TRIM proteins which may be used to regulate (in particular, induce) autophagy, target autophagic substrates and treat and/or prevent autophagic disease states and/or conditions.

    Abstract translation: 本发明涉及使用中性脂质，包括甘油三酸酯，甘油二酯和甘油单酯，其可用于增加中性脂质（脂质储存和/或脂质液滴）和中性脂质储存物，以调节（特别是诱导）自噬和 治疗和/或预防自噬相关疾病状态和/或病症。 在一个实施方案中，本发明涉及可用于调节（特别是诱导）自噬，靶自噬底物并治疗和/或预防自噬性疾病状态和/或病症的中性脂质和/或TRIM蛋白的用途。

    ISOTOPE ENHANCED AMBROXOL FOR LONG LASTING AUTOPHAGY INDUCTION
    8.
    发明申请
    ISOTOPE ENHANCED AMBROXOL FOR LONG LASTING AUTOPHAGY INDUCTION 审中-公开

    公开(公告)号：US20200237687A1

    公开(公告)日：2020-07-30

    申请号：US16778220

    申请日：2020-01-31

    Applicant: STC.UNM

    Inventor： Graham Timmins ,  Vojo P. Deretic

    IPC: A61K31/137 ,  A61K45/06 ,  A61K35/00 ,  A61K51/04 ,  A61K9/00 ,  C07C213/08 ,  A61K31/136 ,  A61P31/04 ,  A61P11/00 ,  C07C215/68 ,  A61K31/395 ,  C07C215/42 ,  C07B59/00 ,  A61P31/06 ,  A61K45/00

    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 ambroxol, 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.

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