| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2017093299 |
| Title |
1,3,4-Thiadiazole Compounds and Their Use In Treating Cancer. |
| Abstract |
A compound of Formula (I) or a pharmaceutically acceptable salt thereof, where: Q can be 1,2,4-triazin-3-yl, pyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R1 can be hydrogen, methoxy, trifluoromethoxy, oxetan-3-yl, 3-fluoroazetidin-1-yl, 3-methoxyazetidin-1-yl, or 3,3- difluoroazetidin-1-yl; R2 can be hydrogen or fluoro; R3 can be hydrogen or methoxy; and R4 can be methoxy, ethoxy, or methoxymethyl; provided that when R1 is hydrogen, methoxy or trifluoromethoxy, then R3 is not hydrogen, and/or R4 is methoxymethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1. |
| Applicant(s) |
Astrazeneca Ab Cancer Research Technology Limited |
| Representative Drug(s) |
D02IVA |
Drug Info
|
IC50 = 64.9 nM |
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[1] |
|
2
|
D07KON
|
Drug Info
|
IC50 = 190 nM
|
[1] |
| Patent ID |
WO2017089587 |
| Title |
Bis-Pyridazine Compounds and Their Use In Treating Cancer. |
| Abstract |
A compound of Formula (I) or a pharmaceutically acceptable salt thereof, where R1 can be hydro, methoxy, difluoromethoxy or trifluoromethoxy; R2 can be hydro, methoxy, trifluoromethoxy or trifluoromethyl; and R3 can be hydro or methoxy. The compound of formula (I) can inhibit glutaminase, e.g., GLS1. |
| Applicant(s) |
Astrazeneca Ab Cancer Research Technology Limited |
| Representative Drug(s) |
D02IVA |
Drug Info
|
IC50 = 64.9 nM |
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[1] |
|
2
|
D07KON
|
Drug Info
|
IC50 = 190 nM
|
[1] |
| Patent ID |
WO2016090350 |
| Title |
Inhibitors of Kidney-Type Glutaminase, Gls-1. |
| Abstract |
The present invention relates generally to glutaminase inhibitors of Formula I, Formula II, or Formula III, as well as pharmaceutical compounds containing them and methods of their use. |
| Applicant(s) |
Cornell University |
| Representative Drug(s) |
D01RUI |
Drug Info
|
IC50 = 5500 nM; Kd = 2700 nM |
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[1] |
|
2
|
D0YE0P
|
Drug Info
|
IC50 = 25000 nM; Kd = 54000 nM
|
[1] |
| Patent ID |
WO2017084598 |
| Title |
Selenium-Containing Inhibitors That Bind To The Allosteric Site of Glutaminase and/or Inhibit Glutamate Dehydrogenase and Their Applications. |
| Abstract |
Disclosed is a class of selenium-containing inhibitors that bind to the allosteric site of glutaminase, and/or inhibit glutamate dehydrogenase, which has a long carbon chain or similar derivative structure linked with N atom of benzoisoselenazole-3-ketone. |
| Applicant(s) |
Hangzhou Gamma Biotech Co., Ltd |
| Representative Drug(s) |
D05CXZ |
Drug Info
|
N.A. |
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[1] |
|
2
|
D07IQM
|
Drug Info
|
N.A.
|
[1] |
| Patent ID |
WO2018039442 |
| Title |
Treatment of Cancer with Inhibitors of Glutaminase. |
| Abstract |
The invention relates to method of treating a disease or disorder (e.g., such as cancer) in a subject, comprising administering to the subject heterocyclic compounds and pharmaceutical preparations described herein, if the subject is determined to possess at least one G allele at single nucleotide polymorphism (SNP) rs6983267. |
| Applicant(s) |
Calithera Biosciences, Inc |
| Representative Drug(s) |
D05TBZ |
Drug Info
|
IC50 = 5 nM |
[1] |
| Patent ID |
WO2017112831 |
| Title |
Salt forms and Polymorphs of (R)-1-(4-(6-(2-(4-(3,3-Difluorocyclobutoxy)-6-Methylpyridin-2-Yl) Acetamido) Pyridazin-3-Yl)-2-Fluorobutyl)-N-Methyl-1H-1,2,3-Triazole-4-Carboxamide. |
| Abstract |
Disclosed herein is the compound (R)-l-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6- methylpyridin-2-yl)acetamido) pyridazin-3-yl)-2-fluorobutyl)-N-methyl-lH-l,2,3-triazole-4- carboxamide, and salt forms and polymorphs thereof demonstrating improved exposure after oral dosing. Methods of inhibition GLSl activity in a human or animal subject are also provided. |
| Applicant(s) |
Board of Regents, the University of Texas System |
| Representative Drug(s) |
D0KP4J |
Drug Info
|
IC50 < 100 nM |
[1] |
| Patent ID |
WO2016054388 |
| Title |
Glutaminase Inhibitors. |
| Abstract |
A compound, or a pharmaceutically acceptable salt thereof, having a structure of: Formula A wherein A is a ring; Y1 and Y2 are each independently N or C with the proper valency; X1 and X2 are each independently -NH-, -0-, -CH2-0-, -NH-CH2-, or -N(CH3)-CH2-, provided that when at least one of X1 and X2 is -CH2-0-, -NH-CH2-, or -N(CH3)-CH2- then the - CH2- is directly connected to A; a and b are each independently 0 or 1; c and d are each independently 0 or 1; Z1 and Z2 are each independently a heterocyclic; and R1 and R2 are each independently optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, amino, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl; provided that if Y1 and Y2 are each C, then a is 1 and b is 1; provided that if Y1 and Y2 are each N, then a is 0 and b is 0; provided that if Y1 is N and Y2 is C, then a=0 and b=l; provided that if Y1 is C and Y2 is N, then a=l and b=0; provided that if c=0 and d=0, then R1 and R2 are both amino; provided that if c is 1 and d is 1, then both R1 and R2 are not amino; provided that if c is 0 and d is 1, then R1 is amino and R2 is optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl; and provided that if c is 1 and d is 0, then R2 is amino and R1 is optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl. |
| Applicant(s) |
University of Pittsburgh - of the Commonwealth System of Higher Education Cornell University |
| Representative Drug(s) |
D0KN6L |
Drug Info
|
IC50 = 29 nM |
[1] |
| Patent ID |
WO2007128588 |
| Title |
Glutadon. |
| Abstract |
The present invention relates to a pharmaceutical combination product for cancer therapy. The combination product comprises the two active ingredients glutaminase and 6-diazo-5-oxo-L-norleucine (DON). The invention further relates to the use of such a combination product for the treatment of cancers. |
| Applicant(s) |
MEDICAL ENZYMES AG [DE] |
| United States Patent and Trademark Office (USPTO) |
| Patent ID |
US20170291895 |
| Title |
Gls1 Inhibitors for Treating Disease. |
| Representative Drug(s) |
D00KII |
Drug Info
|
IC50 < 100 nM |
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[1] |
|
2
|
D0P0ES
|
Drug Info
|
IC50 < 100 nM
|
[1] |
| Patent ID |
US6451828 |
| Title |
Selective Inhibition of Glutaminase By Bis-Thiadiazoles. |
| Representative Drug(s) |
D0G4YI |
Drug Info
|
IC50 = 180 nM |
[1] |
| Intellectual Property Office of Australia (IP Australia) |
| Patent ID |
AU2018202954 |
| Title |
Compounds and Methods of Use. |
