- TOLL LIKE RECEPTOR MODULATOR COMPOUNDS
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This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them.
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Paragraph 0463-0464
(2018/03/25)
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- GLUCOSE UPTAKE INHIBITORS
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Provided hererin are compounds that modulate glucose uptake activityand are useful for treating cancer, autoimmune diseases, inflammation, infectious diseases, and metabolic diseases. In certain embodiments, the compounds modulate glucose uptake activity by modulating cellular components, including, but not limited to those related to glycolysis and known transporters/co-transporters of glucose such as GLUT1 and other GLUT family members/alternative hexose transporters. In certain embodiments, the compounds have the structure of formula I: Formula (I) wherein the variables have the values disclosed herein.
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Paragraph 0687-0688
(2017/01/09)
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- TREATMENT OF INFECTIOUS DISEASES WITH GLUCOSE UPTAKE INHIBITORS
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Provided are methods of treating infectious diseases in mammals comprising administering a compound that inhibits glucose uptake. Particular infectious diseases that may be treated include malaria, leishmaniasis, African trypanosomiasis, tuberculosis, HIV, HCMV or herpes virus. In a first aspect, the invention features a method of treating infectious diseases in a mammal, comprising administering to a mammalian subject in need thereof a therapeutically effective amount of a compound or prodrug thereof, or pharmaceutically acceptable salt or ester of said compound or prodrug, wherein the compound is an inhibitor of glucose uptake.
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Paragraph 0337; 0338
(2017/01/09)
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- Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity
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Selective inhibitors of mammalian target of rapamycin (mTOR) kinase based upon saturated heterocycles fused to a pyrimidine core were designed and synthesized. Each series produced compounds with Ki 500-fold sel
- Koehler, Michael F. T.,Bergeron, Philippe,Blackwood, Elizabeth,Bowman, Krista K.,Chen, Yung-Hsiang,Deshmukh, Gauri,Ding, Xiao,Epler, Jennifer,Lau, Kevin,Lee, Leslie,Liu, Lichuan,Ly, Cuong,Malek, Shiva,Nonomiya, Jim,Oeh, Jason,Ortwine, Daniel F.,Sampath, Deepak,Sideris, Steve,Trinh, Lan,Truong, Tom,Wu, Jiansheng,Pei, Zhonghua,Lyssikatos, Joseph P.
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p. 10958 - 10971
(2013/02/25)
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- BICYCLIC PYRIMIDINE DERIVATIVES
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[wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m + n is 4 or less; R1 represents NR4R5 (wherein R4 and R5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); R2 represents the above Formula (II), Formula (IV) or the like; A represents a single bond, -C(=O)-, -SO2-, -OC(=O)- or the like; and R3 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or the like]ψBicyclic pyrimidine derivatives represented by the above Formula (I), or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof, or the like, are provided. These have anti-inflammatory activities or modulation activities on the functions of TARC and/or MDC and are useful for treating and/or preventing a disease which is related to T cells, such as an allergic disease, an autoimmune disease or transplant rejection.
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- PREVENTIVE AND/OR THERAPEUTIC DRUGS FOR ITCH
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The present invention provides an agent for prevention and/or treatment of itching comprising a substance capable of suppressing the function involved in signal transduction of GPR4 as an active ingredient. It also provides a nitrogen-containing tricyclic compound represented by the formula (I) or a quaternary ammonium salt thereof, or a pharmaceutically acceptable salt thereof; [wherein R1 represents substituted or unsubstituted lower alkyl, etc.; R2 represents hydrogen, substituted or unsubstituted lower alkyl, etc.; R3 and R4 are the same or different and each represents hydrogen, lower alkyl, etc.; n represents 0 or 1; X represents -(CH2)2-, etc.; and Y represents the formula (II); (wherein W represents CH or a nitrogen atom; Z1 and Z2 are the same or different and each represents hydrogen, substituted or unsubstituted lower alkyl, etc.; and Z3 represents hydrogen, substituted or unsubstituted lower alkyl, etc.)]
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- PREVENTIVE AND/OR THERAPEUTIC DRUGS FOR ASTHMA
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The present invention provides an agent for prevention and/or treatment of asthma comprising a substance capable of suppressing the function involved in signal transduction of GPR4 as an active ingredient. It also provides an agent for prevention and/or treatment of asthma which comprises a nitrogen-containing tricyclic compound represented by the formula (I) or a quaternary ammonium salt thereof, or a pharmaceutically acceptable salt thereof; [wherein R1 represents a substituted or unsubstituted lower alkyl, or the like; R2 represents hydrogen, a substituted or unsubstituted lower alkyl, or the like; R3 and R4 are the same or different and each represents hydrogen, lower alkyl, or the like; n represents 0 or 1; X represents -(CH2)2-, or the like; and Y represents the formula (II) (wherein W represents CH or a nitrogen atom; Z1 and Z2 are the same or different and each represents hydrogen, a substituted or unsubstituted lower alkyl, or the like; and Z3 represents hydrogen, a substituted or unsubstituted lower alkyl, or the like)] as an active ingredient.
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Page/Page column 61-62
(2010/02/11)
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