http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-115985-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_21fdee9b8f680c261663aa63946e1144 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K2300-00 |
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| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-497 |
| filingDate | 2019-08-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6ed27e67eacb5afce6ea32b8d79034eb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8abfae67be79dc2bb0f1fb2a8395479e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_43e1eae9b85bdd375f064cefce69b45c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2670c22d0a02ff5ce69896e12ee3c592 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e4432a293c80bcece52c42bf91ac67c2 |
| publicationDate | 2021-03-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-115985-A1 |
| titleOfInvention | PIRAZINE COMPOUNDS AND USES OF THEM |
| abstract | Pyrazine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). Also, pharmaceutical compositions comprising one or more of the compounds as active ingredients, and the use of the compounds in the treatment of diseases associated with the adenosine receptor (AR), for example cancer, such as NSCLC, RCC, prostate cancer and breast cancer. Claim 1: A compound characterized in that it is of formula (1), or a pharmaceutically acceptable salt thereof, where, X is selected from amino, halogen, hydroxyl, cyano, C₁₋₁₂ alkoxy, N- (C₁₋₁₂ alkyl) amino , N, N- (C₁₋₁₂ alkyl) ₂amino, C₁₋₁₂ alkanoylamino; Ring A is 3-12 membered saturated or unsaturated monocyclic or polycyclic heterocyclyl; Ring B is selected from 3-12 membered saturated or unsaturated carbocyclyl, or 3-12 membered saturated or unsaturated heterocyclyl; W is -C₁₋₁₂ alkylene- or -C (O) -, which may be independently monosubstituted or multisubstituted with hydroxyl, C₁₋₁₂ alkyl, C₁₋₁₂ alkoxy, or C₁₋₁₂ alkyl-OH; V is -NH-, -NH-C₁₋₁₂ alkylene-, -NH-C (O) -, or N-linked pyrrolidinyl, which may be independently monosubstituted or multisubstituted with hydroxyl, C₁₋₁₂ alkyl, C₁₋₁₂ alkoxy, N- (C₁₋₁₂alkyl) amino, N, N- (C₁₋₁₂alkyl) ₂amino or C₁₋₁₂alkyl-OH; Y is hydrogen, halogen, hydroxyl, cyano, amino, carbamoyl, urea, carbonyl, carbamate, sulfonyl, C₁₋₁₂ alkyl, C₁₋₁₂ alkoxy, C₁₋₁₂ alkanoyl, C₁₋₁₂ alkyl-OH, C₁₋₁₂ alkyl-cyano , C₁₋₁₂ haloalkyl, C₁₋₁₂ haloalkoxy, N- (C₁₋₁₂ alkyl) amino, N, N- (C₁₋₁₂ alkyl) ₂amino, N- (C₁₋₁₂ alkyl) carbamoyl, N, N- (C₁₋ ₁₂ alkyl) ₂carbamoyl, C₁₋₁₂ alkylsulfonyl, C₁₋₁₂ alkanoylamino, 3-12-membered saturated or unsaturated carbocyclyl, or 3-12-membered saturated or unsaturated heterocyclyl, which may be optionally independently monosubstituted or multisubstituted with R³; each R¹ is independently selected from halogen, hydroxyl, cyano, amino, carbamoyl, urea, carbamate, C₁₋₁₂ alkyl, C₁₋₁₂ haloalkyl, C₁₋₁₂ alkoxy, C₁₋₁₂ haloalkoxy, C₁₋₁₂ alkyl-OH, N - (C₁₋₁₂ alkyl) amino, N, N- (C₁₋₁₂ alkyl) ₂amino, N- (C₁₋₁₂ alkyl) carbamoyl, N, N- (C₁₋₁₂ alkyl) ₂carbamoyl, C₁₋₁₂ alkanoylamino, a carbocyclyl 3-10 membered saturated or unsaturated, or 3-10 membered saturated or unsaturated heterocyclyl, where each R¹ may further optionally be independently monosubstituted or multisubstituted with R⁴; each R² is independently selected from halogen, hydroxyl, cyano, amino, carbamoyl, urea, carbamate, C₁₋₁₂ alkyl, C₁₋₁₂ haloalkyl, C₁₋₁₂ alkoxy, C₁₋₁₂ haloalkoxy, C₁₋₁₂ alkyl-OH, N - (C₁₋₁₂ alkyl) amino, N, N- (C₁₋₁₂ alkyl) ₂amino, N- (C₁₋₁₂ alkyl) carbamoyl, N, N- (C₁₋₁₂ alkyl) ₂carbamoyl, C₁₋₁₂ alkanoylamino, a carbocyclyl 3-10 membered saturated or unsaturated, or 3-10 membered saturated or unsaturated heterocyclyl, where each R² may further optionally be independently monosubstituted or multisubstituted with R⁵; each R³ is independently selected from halogen, hydroxyl, cyano, amino, carbamoyl, urea, carbamate, sulfonyl, phosphate, phosphoryl, phosphinyl, C₁₋₁₂ alkyl, C₁₋₁₂ haloalkyl, C₁₋₁₂ alkoxy, C₁₋₁₂ haloalkoxy, C₁₋₁₂ alkyl-OH, N- (C₁₋₁₂ alkyl) amino, N, N- (C₁₋₁₂ alkyl) ₂amino, N- (C₃₋₁₂ cycloalkyl) amino, N- (C₁₋₁₂ alkyl) carbamoyl, N , N- (C₁₋₁₂ alkyl) ₂carbamoyl, (C₁₋₁₂ alkyl) sulfonyl, (C₁₋₁₂ alkyl) phosphinyl, (C₁₋₁₂ alkyl) ₂phosphinyl, (C₁₋₁₂ alkyl) phosphoryl, (C₁₋₁₂ alkyl) ₂phosphoryl , C₁₋₁₂ alkanoylamino, N- (C₁₋₁₂ alkyl-OH) amino, a 3-10 membered saturated or unsaturated carbocyclyl, or a 3-10 membered saturated or unsaturated heterocyclyl, where each R³ may furthermore be optionally monosubstituted or independently multisubstituted with R⁶; where each R⁴, R⁵, or R⁶ is independently selected from halogen, hydroxyl, cyano, amino, carbamoyl, sulfonyl, phosphinyl, urea, carbamate, C₁₋₁₂ alkyl, C₁₋₁₂ haloalkyl, C₁₋₁₂ alkoxy, C₁₋₁₂ haloalkoxy , C₁₋₁₂ alkyl-OH, N- (C₁₋₁₂ alkyl) amino, N, N- (C₁₋₁₂ alkyl) ₂amino, N- (C₁₋₁₂ alkyl) carbamoyl, N, N- (C₁₋₁₂ alkyl) ₂carbamoyl, (C₁₋₁₂ alkyl) sulfonyl, (C₁₋₁₂ alkyl) phosphinyl, (C₁₋₁₂ alkyl) ₂phosphinyl, C₁₋₁₂ alkanoylamino, C₁₋₁₂ alkylsulfonyl, C₁₋₁₂ haloalkoxy; m is 0, 1, 2, 3, or 4; n is 0, 1, 2, 3, or 4. |
| priorityDate | 2018-08-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 78.