US 12,213,957 B2
Use of aminoacetonitrile compounds for the treatment of infection and disease
Roger Aston, Claremont (AU); and Richard Mollard, Claremont (AU)
Assigned to PITNEY PHARMACEUTICALS PTY LIMITED, Claremont (AU)
Appl. No. 17/924,537
Filed by PITNEY PHARMACEUTICALS PTY LIMITED, Claremont (AU)
PCT Filed May 11, 2021, PCT No. PCT/AU2021/050435
§ 371(c)(1), (2) Date Nov. 10, 2022,
PCT Pub. No. WO2021/226662, PCT Pub. Date Nov. 18, 2021.
Claims priority of application No. 2020901514 (AU), filed on May 11, 2020; and application No. 2020901776 (AU), filed on May 29, 2020.
Prior Publication US 2023/0181516 A1, Jun. 15, 2023
Int. Cl. A61K 31/277 (2006.01); A61P 31/14 (2006.01); A61P 35/00 (2006.01)
CPC A61K 31/277 (2013.01) [A61P 31/14 (2018.01); A61P 35/00 (2018.01)] 12 Claims
 
1. A method for the treatment of cancer, or one or more mTOR pathway related diseases, the method comprising administering to a patient in need thereof an amount of a compound of formula (I):

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt or solvate thereof, sufficient to achieve a plasma concentration of said compound and/or a metabolite thereof of about 0.005 μM, about 0.01 μM, about 0.05 μM, about 0.1 μM, about 0.2 μM, about 0.3 μM, about 0.4 μM, about 0.5 μM, about 0.6 μM, about 0.7 UM, about 0.8 μM, or about 0.9 μM,
wherein
R1, R2 and R3 and R5 are each independently selected from H, alkyl, halogen, —CF3 or —CN;
R4 and R6 are each independently selected from H, alkyl, halogen, alkoxy, —CF3, —OCF3, —SO2CF3, —SOCF3 or —SCF3;
X is heteroatom, N(alkyl) or NH; and
n is 1 to 20;
and
wherein the cancer is selected from bladder cancer, kidney cancer, liver cancer, lung cancer, esophageal cancer, gall bladder cancer, pancreatic cancer, stomach cancer, thyroid cancer, B-cell lymphoma, T-cell lymphoma, Hodgkins lymphoma, non-Hodgkins lymphoma, hairy cell lymphoma, mantle cell lymphoma, myeloma, Burkett's lymphoma, myelodysplastic syndrome, rhabdomyosarcoma, astrocytoma, neuroblastoma, schwannoma, seminoma, teratocarcinoma, osteosarcoma, or Kaposi's sarcoma, and
wherein the mTOR pathway related disease is selected from Alzheimer's disease, Huntington's disease, motor neurone disease/amyotrophic lateral sclerosis, Parkinson's disease, age-related diseases, diseases related to transplant rejection, chronic inflammatory diseases, diseases related to glycogen storage, systemic lupus, diseases related to inflammation and immune activation, anaemia, leucopenia, thrombocytopenia, diseases related to stent coatings, renal insufficiency, obesity, diabetes/insulin resistance, diseases related to non-alcoholic fatty liver, polycystic kidney, fibrosis, or vial infection.