http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-119311-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_dab7fd26f3cb605aab550ed208a2fe8c |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-573 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-57 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J67-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J63-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J1-00 |
| filingDate | 2020-06-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_60971a303a5cfcae8e19d96d55b51b24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_75c0fcfc4ebbe8611b4be27d11337eac http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a0da458ce59b5713c0eefe228568c00f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1aac8053822d4ada2e40813b8ab5ab80 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a27f885e03138a51bdea26e21efdda72 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e9248daad06afb26d32b46bbc337bb4a |
| publicationDate | 2021-12-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-119311-A1 |
| titleOfInvention | COMPOSITIONS AND METHODS FOR THE TREATMENT OF CNS DISORDERS |
| abstract | Claim 1: A compound of formula (1), (2) or (3), formula (1), or a pharmaceutically acceptable salt thereof; characterized in that: q is independently 0, 1, 2, or 3; r is independently 0, 1, or 2; s is independently 0, 1 or 2; t is independently 0, 1, 2 or 3; n is independently 1 or 2; u is independently 1 or 2; X is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -ORA¹ , -SRA¹, -N(RA¹)₂, -OC(=O)RA¹, -OC(=O)ORA¹, -OC(=O)SRA¹, -OC(=O)N(RA¹)₂, -SC( =O)RA², -SC(=O)ORA¹, -SC(=O)SRA¹, -SC(=O)N(RA¹)₂, -NHC(=O)RA¹, -NHC(=O)ORA¹, - NHC(=O)SRA¹, -NHC(=O)N(RA¹)₂, -OS(=O)₂RA², -OS(=O)₂ORA¹, -S-S(=O)₂RA², -S-S(=O)₂ORA¹ , -S(=O)RA², -SO₂RA², or -S(=O)₂ORA¹, where each instance of RA¹ is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted carbocyclyl or unsubstituted, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when bonded with an oxygen atom, an azure protecting group fre when bonded with a sulfur atom or a nitrogen protecting group when bonded with a nitrogen atom; and each instance of RA² is independently substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, R⁵ is hydrogen or methyl or when ⁻ ⁻ ⁻ ⁻ ⁻ is a double bond, R⁵ and one of R⁶ᵃ or R⁶ᵇ is absent; R¹⁹ is hydrogen or substituted or unsubstituted alkyl; R¹⁸ is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R³ is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; each of R⁶ᵃ and R⁶ᵇ is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl; or R⁶ᵃ and R⁶ᵇ come together to form an oxo (=O) group; and each of R²ᵃ, R²ᵇ, R⁴ᵃ, R⁴ᵇ, R¹¹ᵃ, R¹¹ᵇ, R¹⁶ᵃ or R¹⁶ᵇ is independently hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heterocyclyl, substituted alkynyl or unsubstituted, -ORD¹, -OC(=O)RD¹, -NH₂, -N(RD¹)₂, or -NRD¹C(=O)RD¹, where each instance of RD¹ is independently hydrogen, substituted or unsubstituted alkyl, substituted alkenyl or unsubstituted, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when bonded with an oxygen atom, a group nitrogen protecting when bonded with a nitrogen atom or two RD¹ groups bond to form a substituted or unsubstituted heterocyclic ring; or any one of R²ᵃ and R²ᵇ, or R⁴ᵃ and R⁴ᵇ, or R¹¹ᵃ and R¹¹ᵇ, or R¹⁶ᵃ and R¹⁶ᵇ join to form an oxo group (=O); provided that: q, s, r, u and t are not simultaneously 1; or formula (2), or a pharmaceutically acceptable salt thereof; where: ⁻ ⁻ ⁻ ⁻ ⁻ represents a single or double bond, provided that a double bond is present, then R⁵ and one of R⁶ᵃ or R⁶ᵇ is absent; R³ is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R⁵ is substituted or unsubstituted hydrogen or methyl, or when ⁻ ⁻ ⁻ ⁻ ⁻ is a double bond, R⁵ is absent; each of R⁶ᵃ and R⁶ᵇ is, independently, hydrogen, halogen, cyano, hydroxyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; or R⁶ᵃ and R⁶ᵇ come together to form an oxo (=O) group; each of R¹ᵃ, R¹ᵇ, R²ᵃ, R²ᵇ, R⁴ᵃ, R⁴ᵇ, R⁷ᵃ, R⁷ᵇ, R¹¹ᵃ, R¹¹ᵇ, R¹²ᵃ, R¹²ᵇ, R¹⁵ᵃ and R¹⁵ᵇ is independently unsubstituted or substituted hydrogen, halogen, alkyl, cyano, unsubstituted or unsubstituted hydrogen, halogen, alkyl, cyano substituted, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted alkynyl, -ORD¹, -OC(=O)RD¹, -NH₂, -N(RD¹)₂, or -NRD¹C(=O)RD¹, where each instance of RD¹ is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl, a protecting group of oxygen when bonded with an oxygen atom, a nitrogen protecting group when bonded with a nitrogen atom, or two RD¹ groups bond to form a substituted or unsubstituted heterocyclic ring; or any one of R¹ᵃ and R¹ᵇ, R²ᵃ and R²ᵇ, R⁴ᵃ and R⁴ᵇ, R¹¹ᵃ and R¹¹ᵇ, R¹²ᵃ and R¹²ᵇ, and R¹⁵ᵃ and R¹⁵ᵇ join to form an oxo (=O) group; each of R¹⁶ᵃ and R¹⁶ᵇ is independently hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted heteroaryl or unsubstituted, -ORA¹, -SRA¹, -N(RA¹)₂, -N(RA¹), -CN(RA¹)₂, -C(O)RA¹, -OC(=O)RA¹, -OC(=O )ORA¹, -OC(=O)SRA¹, -OC(=O)N(RA¹)₂, -SC(=O)RA², -SC(=O)ORA¹, -SC(=O)SRA¹, -SC( =O)N(RA¹)₂, -NHC(=O)RA¹, -NHC(=O)ORA¹, -NHC(=O)SRA¹, -NHC(=O)N(RA¹)₂, -OS(=O )₂RA², -OS(=O)₂ORA¹, -S-S(=O)₂RA², -S-S(=O)₂ORA¹, -S(=O)RA², -SO₂RA², or -S(=O)₂ORA¹, where each instance of RA¹ is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, a group ox guard nitrogen when bonded with an oxygen atom, a sulfur protecting group when bonded with a sulfur atom, a nitrogen protecting group when bonded with a nitrogen atom; SO₂RA², -C(O)RA², or two RA¹ groups join to form a substituted or unsubstituted heterocyclic or heteroaryl ring; and RA² is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R¹⁹ is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; R²⁸ is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -ORA¹, - N(RA¹)₂, -SRA¹, -C(=O)RA¹, -C(=O)ORA¹, -C(=O)SRA¹, -C(=O)N(RA¹)₂, -OC(=O )RA¹, -OC(=O)ORA¹, -OC(=O)N(RA¹)₂, -OC(=O)SRA¹, -OS(=O)₂RA¹, -OS(=O)₂ORA¹, -OS( =O)₂N(RA¹)₂, -N(RA¹)C(=O)RA¹, -N(RA¹)C(=NRA¹)RA¹, -N(RA¹)C(=O)ORA¹, -N(RA¹) C(=O)N(RA¹)₂, -N(RA¹)C(=NRA¹) N(RA¹)₂, -N(RA¹)S(=O)₂RA¹, -N(RA¹)S(=O)₂ORA¹ , -N(RA¹)S(=O)₂N(RA¹)₂, -SC(=O)RA¹, -SC(=O)ORA¹, -SC(=O)SRA¹, -SC(=O)N(RA¹ )₂, -S(=O)₂RA¹, -S(=O)₂ORA¹, or -S(=O)₂N(RA¹)₂, where each instance of RA¹ is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl, aryl substituted or unsubstituted, substituted or unsubstituted heteroaryl, an oxygen protecting group when bonded with oxygen, a nitrogen protecting group when bonded with nitrogen, a sulfur protecting group when bonded with sulfur, or two RA groups are taken¹ with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; n is 1, 2 or 3; and provided that the compound is not: a compound of the group of formulas (4); or formula (3), or a pharmaceutically acceptable salt thereof; where: ⁻ ⁻ ⁻ ⁻ ⁻ represents a single or double bond, whenever a double bond is present, then one of R⁶ᵃ or R⁶ᵇ is absent; R¹ is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -ORA¹, -N( RA¹)₂, -SRA¹, -C(=O)RA¹, -C(=O)ORA¹, -C(=O)SRA¹, -C(=O)N(RA¹)₂, -OC(=O)RA¹ , -OC(=O)ORA¹, -OC(=O)N(RA¹)₂, -OC(=O)SRA¹, -OS(=O)₂RA¹, -OS(=O)₂ORA¹, -OS(=O )₂N(RA¹)₂, -N(RA¹)C(=O)RA¹, -N(RA¹)C(=NRA¹)RA¹, -N(RA¹)C(=O)ORA¹, -N(RA¹)C( =O)N(RA¹)₂, -N(RA¹)C(=NRA¹)N(RA¹)₂, -N(RA¹)S(=O)₂RA¹, -N(RA¹)S(=O)₂ORA¹, - N(RA¹)S(=O)₂N(RA¹)₂, -SC(=O)RA¹, -SC(=O)ORA¹, -SC(=O)SRA¹, -SC(=O)N(RA¹)₂ , -S(=O)₂RA¹, -S(=O)₂ORA¹, or -S(=O)₂N(RA¹)₂, where each instance of RA¹ is independently selected from hydrogen, substituted or unsubstituted alkyl, alkenyl substituted or unsubstituted, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl, substituted aryl or unsubstituted, substituted or unsubstituted heteroaryl, an oxygen protecting group when bonded with oxygen, a nitrogen protecting group when bonded with nitrogen, a sulfur protecting group when bonded with sulfur, or two RA¹ groups are taken with atoms which intervene to form a substituted or unsubstituted heterocyclic ring; each of R²ᵃ, R²ᵇ, R⁴ᵃ, R⁴ᵇ, R⁷ᵃ, R⁷ᵇ, R¹¹ᵃ, R¹¹ᵇ, R¹²ᵃ, R¹²ᵇ or R¹⁷ᵇ is independently hydrogen, halogen, -CN, -NO₂, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, alkynyl or unsubstituted, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -ORA¹, -N(RA¹)₂, -SRA¹, -C(=O)RA¹, - C(=O)ORA¹, -C(=O)SRA¹, -C(=O)N(RA¹)₂, -OC(=O)RA¹, -OC(=O)ORA¹, -OC(=O)N (RA¹)₂, -OC(=O)SRA¹, -OS(=O)₂RA¹, -OS(=O)₂ORA¹, -OS(=O)₂N(RA¹)₂, -N(RA¹)C(=O )RA¹, -N(RA¹)C(=NRA¹)RA¹, -N(RA¹)C(=O)ORA¹, -N(RA¹)C(=O)N(RA¹)₂, -N(RA¹)C( =NRA¹) N(RA¹)₂, -N(RA¹)S(=O)₂RA¹, -N(RA¹)S(=O)₂ORA¹, -N(RA¹)S(=O)₂N(RA¹)₂, - SC(=O)RA¹, -SC(=O)ORA¹, -SC(=O)SRA¹, -SC(=O)N(RA¹)₂, -S(=O)₂RA¹, -S(=O)₂ORA¹ , or -S(=O)₂N(RA¹)₂, where each instance of RA¹ is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted alkynyl do or unsubstituted, substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when bonded with oxygen, a nitrogen protecting group when bonded with nitrogen , a sulfur protecting group when bonded with sulfur, or two RA¹ groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; R³ᵃ is hydrogen substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; R⁵ is hydrogen or methyl; when ⁻ ⁻ ⁻ ⁻ ⁻ is a double bond, R⁵ is absent; each of R⁶ᵃ and R⁶ᵇ is independently hydrogen, halogen, -CN, -NO₂, -OH, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl; or R⁶ᵃ and R⁶ᵇ bond to form an oxo (=O) group; each of R¹⁵ᵃ, R¹⁵ᵇ, R¹⁶ᵃ and R¹⁶ᵇ is independently hydrogen, halogen, -CN, -NO₂, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl substituted, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, -ORC³, -N(RC³)₂, -SRC³, -C(=O)RC³, -C(=O)ORC³, -C(=O)SRC³ , -C(=O)N(RC³)₂, -OC(=O)RC³, -OC(=O)ORC³, -OC(=O)N(RC³)₂, -OC(=O)SRC³, - OS(=O)₂RC³, -OS(=O)₂ORC³, -OS(=O)₂N(RC³)₂, -N(RC³)C(=O)RC³, -N(RC³)C(=NRC³)RC³ , -N(RC³)C(=O)ORC³, -N(RC³)C(=O)N(RC³)₂, -N(RC³)C(=NRC³)N(RC³)₂, -N(RC³) S(=O)₂RC³, -N(RC³)S(=O)₂ORC³, -N(RC³)S(=O)₂N(RC³)₂, -SC(=O)RC³, -SC(=O)ORC³ , -SC(=O)SRC³, -SC(=O)N(RC³)₂, -S(=O)₂RC³, -S(=O)₂ORC³, or -S(=O)₂N(RC³)₂, where each instance of RC³ is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted aryl or unsubstituted, substituted or unsubstituted heteroaryl, substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl, an oxygen protecting group when bonded with oxygen, a nitrogen protecting group when bonded with nitrogen, a sulfur protecting group when it bonds with sulfur, or two RC³ groups are taken with the intervening atoms to form a substituted or unsubstituted heterocyclic ring; R¹⁸ is substituted or unsubstituted alkyl; R¹⁹ is substituted or unsubstituted C₃₋₆ carbocyclyl or substituted or unsubstituted aryl; and n is 0, 1 or 2. |
| priorityDate | 2019-06-27-04:00^^<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: 38.