http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-116717-A1
Outgoing Links
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|---|---|
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| filingDate | 2019-10-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
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| publicationDate | 2021-06-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-116717-A1 |
| titleOfInvention | A-1 ANTITRYPSIN MODULATORS |
| abstract | Compounds, compositions and methods of use and preparation thereof, which may be useful for the treatment of α-1 antitrypsin deficiency (AATD). A compound of formula (1), a tautomer thereof, a pharmaceutically acceptable salt of any of the foregoing, or a deuterated derivative of any of the foregoing; characterized in that: (i) R⁰ is selected from (a) linear, branched and cyclic C₁₋₈ alkyl groups, wherein the alkyl group is optionally substituted with 1-4 RA; and (b) 5- to 10-membered aromatic rings optionally substituted with 1-4 RA, where each RA is independently chosen from halogens, cyano, hydroxy, thiol, sulfuric acid, sulfonamide, sulfinamide, amino, amide, aromatic rings of 5 to 10 members, and linear, branched, and cyclic C₁₋₆ groups, wherein the linear, branched, and cyclic C₁₋₆ groups are selected from alkyl, alkoxy, thioalkyl, alkylsulfoxide, alkylsulfonyl, alkylsulfonamide, alkylsulfinamide, aminoalkyl, and alkylamide, and wherein the 5 to 10 membered aromatic rings and the linear, branched and cyclic C₁₋₆ groups are optionally substituted with 1-4 substituents selected from halogens and methoxy; (ii) R¹ is selected from (a) linear, branched, and cyclic C₁₋₈ alkyl groups, wherein the alkyl group is optionally substituted with 1-4 substituents selected from halogens, carboxylic acid, cyano, and linear C₁₋₆ groups, branched and cyclic, where the linear, branched and cyclic C₁₋₆ groups are chosen from alkyl and alkoxy groups, and where the linear, branched and cyclic C₁₋₆ groups are optionally substituted with 1-4 halogens, (b) groups linear, branched and cyclic C₁₋₈ alkoxy optionally substituted with 1-4 substituents selected from halogens, cyano, and linear, branched and cyclic C₁₋₆ alkyl groups that are optionally substituted with 1-4 halogens; (c) C₁₋₈ heterocycles, and (d) linear, branched and cyclic C₂₋₆ alkenyl groups; (iii) R² is selected from: hydrogen, cyano, halogens, alkylamide groups, linear, branched and cyclic C₁₋₈ alkyl groups optionally substituted with an oxo group, a linear, branched and cyclic C₁₋₈ alkoxy group, a heteroaryl group of 5 or 6 membered, a cyano group, an amino group, an aminoalkyl group, an alkylamide group, an alkylsulfonyl group, an alkylsulfonamide group, an alkylsulfoxide group, a group of formula (2) or of formula (3) where RB is selected from amino groups, linear, branched and cyclic C₁₋₈ alkyl groups, and O-RC groups, wherein RC is selected from linear, branched and cyclic C₁₋₈ alkyl groups substituted with an aryl group, a NC group (O) -RB where RB is selected from amino groups, linear, branched and cyclic C₁₋₈ alkyl groups, and O-RC, where RC is selected from linear, branched and cyclic C₁₋₈ alkyl groups substituted with an aryl group, a group of formula (4) wherein Ring A is chosen from 4-8 membered rings that optionally comprise one or two heteroatoms in addition to Ring A nitrogen, and / or a carboxylic acid group esterified with a uronic acid, linear, branched and cyclic C₂₋₆ alkenyl groups, linear, branched and cyclic C₂₋₆ alkynyl groups, A groups -CO₂R⁴ where A is optionally present and if present is selected from linear, branched and cyclic C₁₋₈ alkyl and alkoxy groups, linear, branched and cyclic C₂₋₆ alkenyl groups, C₃₋₈ cycloalkyl groups linked to C₁₋ alkyl groups Linear or branched ₈, linear or branched C₁₋₈ alkyl groups linked to C₃₋₈ cycloalkyl groups, C₃₋₈ cycloalkyl groups linked to C₃₋₈ cycloalkyl groups, linear, branched and cyclic C₁₋₈ alkyl groups linked to C₃₋ cycloalkyl groups ₈ bonded to linear, branched and cyclic C₁₋₈ alkyl groups, where up to 3 carbon atoms of A are optionally substituted with 1-4 halogens or 1-3 linear, branched or cyclic C₁₋₄ groups, where linear, branched, or cyclic C₁₋₄ groups are chosen from alkyl and alkoxy groups, and wherein linear, branched, or cyclic C₁₋₄ groups are optionally substituted with 1-4 halogens, and where R⁴ is selected from hydrogen, groups C₁₋₈ linear, branched, and cyclic alkyl, and C₂₋₆ linear, branched, and cyclic alkenyl groups, AC (O) NH₂ groups where A is optionally present and if present is selected from linear C₁₋₈ alkyl and alkoxy groups, branched and cyclic, linear, branched and cyclic C₂₋₆ alkenyl groups, C₃₋₈ cycloalkyl groups linked to linear or branched C₁₋₈ alkyl groups, linear or branched C₁₋₈ alkyl groups linked to C₃₋₈ cycloalkyl groups, C₃ cycloalkyl groups ₋₈ linked to C₃₋₈ cycloalkyl groups, linear, branched and cyclic C₁₋₈ alkyl groups linked to C₃₋₈ cycloalkyl groups linked to linear, branched and cyclic C₁₋₈ alkyl groups, where up to 3 carbon atoms of A are optionally substituted with 1-4 halogens or 1-3 linear, branched or cyclic C₁₋₄ groups, where the linear, branched or cyclic C₁₋₄ groups are chosen from alkyl and alkoxy groups, and where the linear C₁₋₄ groups, Branched or cyclic are optionally substituted with 1-4 halogens, and where R⁴ is selected from hydrogen, linear, branched, and cyclic C₁₋₈ alkyl groups, and linear, branched, and cyclic C₂₋₆ alkenyl groups, C (O) NR⁶R⁷ in where R⁶ and R⁷ are independently chosen from hydrogen, linear, branched and cyclic C₁₋₈ alkyl groups, linear, branched and cyclic C₂₋₆ alkenyl groups, 4- to 8-membered heterocycles optionally substituted by one or more substituents chosen from cyano, halogens C₁₋₈ linear, branched and cyclic alkyl groups, and C₂₋₆ linear, branched and cyclic alkenyl groups, or R⁶ and R⁷ together with the nitrogen to which they are attached form a 4-8 membered ring optionally comprising one or two heteroatoms in addition to d the nitrogen to which they are attached, and the ring is optionally substituted with a substituent selected from halogens, cyano, hydroxy, and linear, branched, and cyclic C₁₋₆ alkyl groups, SO₂R⁵ groups where R⁵ is selected from linear C₁₋₈ alkyl groups , branched and cyclic, and linear, branched and cyclic C₂₋₆ alkenyl groups, and groups of formula (4) wherein Ring A is a 4-8 membered ring optionally comprising one or two heteroatoms in addition to the nitrogen of Ring A ; (iv) X¹ and X² are independently chosen from hydrogen, halogens, cyano, hydroxy, linear, branched and cyclic C₁₋₆ groups where the linear, branched and cyclic C₁₋₆ groups are chosen from alkyl, alkoxy, thioalkyl and aminoalkyl groups , and wherein the linear, branched and cyclic C₁₋₆ groups are optionally substituted by 1-4 halogens; (v) each ⁻ ⁻ ⁻ ⁻ ⁻ represents a single or double bond, provided that no more than one ⁻ ⁻ ⁻ ⁻ ⁻ is a double bond; (vi) each R³ is independently chosen from hydrogen, halogens, cyano, linear, branched, and cyclic C₁₋₆ alkyl groups, and linear, branched, and cyclic C₁₋₆ alkoxy groups, wherein the linear, branched, and cyclic alkyl and alkoxy groups are optionally substituted with 1-4 halogens; (vii) n is an integer chosen from 0, 1, 2, and 3; and (viii) Z¹, Z², and Z³ are independently chosen from carbon, nitrogen, sulfur, and oxygen, where when Z¹, Z², and / or Z³ are carbon or nitrogen, the valencies of carbon and nitrogen are completed with hydrogen atoms. C₁₋₈ linear, branched and cyclic alkyls, or cyano. |
| priorityDate | 2018-10-05-04:00^^<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: 81.