http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-114994-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_73ce6b87cca6304176233ef349b24575 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07H21-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7016 |
| filingDate | 2018-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c1ed60ce1d5df5d4767926c981f32bbe http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_404e4351b583a10b9b0830fac0e400d8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_48e70e60512abeba07a80ee1efc3ea78 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0f6e31f386a754b6c43dfe3e37513c46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1694a901b42c0a8d04796527c8332dee |
| publicationDate | 2020-11-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-114994-A1 |
| titleOfInvention | 2'2 'CYCLIC DINUCLEOTIDES WITH PHOSPHONATE BINDING THAT ACTIVATE THE ADAPTER PROTEIN STING |
| abstract | Provided herein are 2'2 'cyclic phosphonate dinucleotides of formula (1), their pharmaceutically acceptable salts, hydrates or solvates, a pharmaceutical composition containing them, and combinations of said substances and other drugs or pharmaceuticals. The disclosure also relates to the use of said compounds for the treatment or prevention of diseases or conditions modifiable by modulation of the STING protein, such as cancer or viral, allergic and inflammatory diseases. Furthermore, dinucleotides can be used as adjuvants in vaccines. Claim 1: A compound of formula (1), or a pharmaceutically acceptable salt thereof, characterized in that L¹ is -C (R⁶R⁷) -O- and L² is -C (R¹³R¹⁴) -O-, L¹ is -C (R⁶R⁷ ) -O- and L² is -OC (R¹³R¹⁴) -, L¹ is -OC (R⁶R⁷) - and L² is -C (R¹³R¹⁴) -O-, L¹ is -C (R⁶R⁷) -K¹-C (R⁶R⁷) - and L² is -C (R¹³R¹⁴) -K¹-C (R¹³R¹⁴) -, L¹ is -C (R⁶R⁷) -K¹-C (R⁶R⁷) - and L² is -OC (R¹³R¹⁴) -, L¹ is -OC (R⁶R⁷) - and L² is -C (R¹³R¹⁴) -K¹-C (R¹³R¹⁴) -, L¹ is -CH (OR¹⁵) - and L² is -CH (OR¹⁵) -, L¹ is -CH (OR¹⁵) - and L² is -OC (R¹³R¹⁴) -, or L¹ is -OC (R⁶R⁷) - and L² is -CH (OR¹⁵) -; Y¹ and Y² are each independently -O-, -S-, or -CH₂-; X¹ and X³ are each independently OH, SH, OR¹⁵, SR¹⁵, or N (R¹⁵) ₂; X² and X⁴ are each independently O or S; R¹, R⁵, R⁸, and R¹² are each independently H, CN, N₃, F, Cl, Br, I, COOR¹⁵, CON (R¹⁵) ₂, C₁₋₆-alkyl, C₂₋₆-alkenyl, C₂₋₆-alkynyl , OR¹⁵, SR¹⁵, or N (R¹⁵) ₂; R², R³, R⁴, R⁹, R¹⁰ and R¹¹ are each independently H, OH, F, Cl, Br, I, CN, N₃, alkyl-C alqu alkenyl-C₂₋₆, alkynyl-C₂₋₆, OR¹⁵, SR¹⁵, or N (R¹⁵) ₂; R⁶, R⁷, R¹³ and R¹⁴ are each independently H, CN, N₃, F, CI, Br, I, COOR¹⁵, CON (R¹⁵) ₂, OR¹⁵, SR¹⁵, N (R¹⁵) ₂, C₁₋₆-alkyl, alkenyl -C₂₋₆, C₂₋₆-alkynyl, C₃₋₇-cycloalkyl, C₂₋₁₀-heterocycloalkyl, C₆₋₁₀-aryl, or C₂₋₁₀-heteroaryl; each R¹⁵ is independently H, -C (= Z) R¹⁶, -C (= Z) OR¹⁶, -C (= Z) SR¹⁶, -C (= Z) N (R¹⁶) ₂, C₁₋₆-alkyl, alkenyl- C₂₋₆, C₂₋₆-alkynyl, C ciclo-cycloalkyl, Cc-heterocycloalkyl, C₆₋₁₀-aryl, or C₂₋₁₀-heteroaryl; each R¹⁶ is independently H, C₁₋₆-alkyl, C₂₋₆-alkenyl, C₂₋₆-alkynyl, C₃₋₇-cycloalkyl, C₂₋₁₀-heterocycloalkyl, C₆₋₁₀-aryl, or C₂₋₁₀-heteroaryl; each Z is independently O, S, or NR¹⁵; K¹ is -O-, -S-, -S (O) -, -S (O) ₂-, -NH-, or -NR¹⁵-; Base¹ and Base² are each independently: a compound selected from the group of formulas (2) characterized in that A, A¹, A², A³ and A⁴ are each independently H, OH, SH, F, CI, Br, I, NH₂, OR¹⁵ , SR¹⁵, NHR¹⁵, N (R¹⁵) ₂, or R¹⁶; and characterized in that C₁₋₆-alkyl, C₂₋₆-alkenyl, C₂₋₆-alkynyl, C₂₋₁₀-heterocycloalkyl, C₆₋₁₀-aryl, or C₂₋₁₀-heteroaryl independently in each case is optionally substituted with 1, 2, or 3 -OH; -SH; -NH₂; = O; = NH; = S; halogen; -N₃; C₆₋₁₀-aryl optionally substituted with 1, 2, or 3 -OH, -CN, -O (C = O) ORB, -O (C = O) RB, or -COORB; unsubstituted C₁₋₆-alkyl; unsubstituted C₁₋₆-alkoxy; unsubstituted C₁₋₆-alkylthio; unsubstituted C₁₋₆-alkylamino; unsubstituted dialkylamino-C;; -CN; -O (C = O) ORB; -O (C = O) RB; or -COORB; characterized in that RB is H or unsubstituted C₁₋₆-alkyl. |
| priorityDate | 2017-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
| Predicate | Subject |
|---|---|
| isDiscussedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419559215 http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID6326969 |
Total number of triples: 21.