http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-118934-A1
Outgoing Links
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| filingDate | 2020-05-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dda8e764e56c4714baa8d732a2bad19c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bf6a87143948e19a9066ba8e570ea0e2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bf54431c3db8a6bc96bc56402ed170d3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7d0de5b63faddad86284a4614fb1c305 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d09c05f81332212a7cc6d6bdf7a7b9eb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_696bf9915d3d703a6a0499e98ccc541f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8dcc69f4df858ac4512abfd47603fdcb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0b92c05b3ae134c1933c290f8088567d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_187d7d6f9a6b0bf26adfc8e279bf602c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_95c5f4e2aae8f61e05c367f33c5c7e70 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e7308b1342f3e194d35a3e8686528642 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2f5e8c7a7919c1bc32b06df14e443848 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5caa9a5bf51920dae020c5b9e8e3466f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_82b9b8ff200200a41ff6a92492dc60dc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3e52400a656f1d976f468fc3f49cef75 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_056e2cfd5a2a4c09b01a75d9532f1bd7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_61f0f42d5f9916cc96f5d055fc3fd412 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7ecc1c9a7ab60657bf51e1d3ae35d9be http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c57318a7170ff1b5c53448088bada85d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5bb6997d1e068ff4834938890bed286c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_58b0fafde2b2ef8cd44dd4a1ea9f2e48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9d5c10609695f0d222fca266f4b6b699 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_458d4d3bcbbacbac10406a01089d714e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4a13e8556683b7d890b0b7cf61decd52 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ed6a4cbb9d64f94e75fd62fcd699ca90 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3166642e507537f0c17215333289eeac http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3549e40bee39c239ec1837905ad208da http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e5dd517f10b99bdc073cb0acb50d988a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_43f6a306801a26ea97dc85b7797b3213 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dadf400c731a3d4d8d9ead09ff4fff4f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0d2bf27ade66031d8b04468384c1d127 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_80eabeea4aabce3636660fd4f513a6d4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_801ac3b503b2c1cb46f0d8c99208e665 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_35de0bb0604dbc2d410f51abc90fe24a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_50ffb4e888ae0dd8d60eb3e37bab7ff8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f8db5ccdf7e64dfd47e118a58c1abeb9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_938652d9791f0a17dc7c427efa956f68 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_29295951d3b590f09dcc67be938bd752 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7c95e01937114cf17c6489b4295187ae http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_51e590913c29d8e6d70fccf80db6d143 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9a295f537a1333f307c50c9d34c679b1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e75910fdbb0914ddae5e29fef84622fd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c16ae7d5fdf4dba1f7283b4e175b7da8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e6209247d7025cc35791e13bfce81abe |
| publicationDate | 2021-11-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-118934-A1 |
| titleOfInvention | α-1 ANTITRYPSIN MODULATORS |
| abstract | The disclosure provides compounds useful for treating a-1 antitrypsin deficiency (AATD), according to formula (1), tautomers thereof, pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable salts of the tautomers, deuterated derivatives of the compounds , deuterated derivatives of tautomers, and deuterated derivatives of salts, solid forms of those compounds, and processes for preparing those compounds. A compound of formula (1), a tautomer thereof, a pharmaceutically acceptable salt of any of the foregoing, and/or a deuterated derivative of any of the foregoing; wherein: (i) R⁰ is selected from (a) straight, branched and cyclic C₁₋₈ alkyl groups, wherein the alkyl group is optionally substituted with 1-4 RA; and (b) 5 to 14 membered aromatic rings optionally substituted with 1-4 RA; wherein each RA is independently selected from halogen, cyano, hydroxy, thiol, sulfonic acid, sulfonamide, sulfinamide, amino, amide, carboxylic acid, 5 to 10 membered aromatic rings, and straight, branched, and cyclic C₁₋₆ groups , wherein the amide nitrogen atom in the amide of RA is optionally substituted with a heterocyclyl group which is optionally further substituted with oxo, wherein the straight, branched and cyclic C₁₋₆ groups are selected from alkyl, alkoxy , thioalkyl, alkylsulfoxide, alkylsulfonyl, alkylsulfonamide, alkylsulfinamide, aminoalkyl and alkylamide, wherein the 5 to 10 membered aromatic rings and linear, branched and cyclic C₁₋₆ groups are optionally substituted with 1-4 substituents selected from halogen, C₁ groups linear, branched, and cyclic ₋₆, and methoxy, and wherein an RA group is optionally bonded to an RB group in an R² group; (ii) R¹ is selected from (a) hydrogen, (b) straight, branched and cyclic C₁₋₈ alkyl groups, wherein the alkyl group is optionally substituted with 1-4 substituents independently selected from halogen, cyano, cyanoalkyl, hydroxy, alkylsulfonyl, and linear, branched, and cyclic C₁₋₆ groups, wherein the linear, branched, and cyclic C₁₋₆ groups are independently selected from alkyl and alkoxy groups, and wherein the linear, branched, and cyclic are optionally substituted with 1-4 substituents independently selected from halogen, hydroxy, and straight, branched, and cyclic C₁₋₆ alkoxy groups, (c) straight, branched, and cyclic C₁₋₈ alkoxy or cyclic thioalkyl groups optionally substituted with 1 - 4 substituents independently selected from halogen, cyano, cyanoalkyl; sulfone, sulfonamide, hydroxy, and straight, branched and cyclic C₁₋₆ alkyl groups, which are optionally substituted with 1-4 halogen or alkoxy groups; (d) straight, branched and cyclic C₁₋₆ alkylsulfonyl groups, optionally substituted with straight or branched C₁₋₆ alkyl groups; (e) aminosulfonyl groups, optionally substituted with 1 or 2 substituents independently selected from straight, branched and cyclic C₁₋₆ alkyl groups; (f) straight, branched and cyclic C₁₋₆ alkylsulfonylamino groups; and (g) phosphine oxide groups, optionally substituted with 1 or 2 substituents independently selected from straight, branched and cyclic C₁₋₆ alkyl groups; (h) straight, branched and cyclic C₁₋₆ trialkylsilyl groups; (i) C₁₋₆ alkylamide; (iii) R² is selected from 5 and 6 membered heterocyclic rings (optionally substituted with oxo and/or straight and branched C₁₋₆ alkyl groups) and 5 to 6 membered aromatic rings comprising 0-4 heteroatoms selected from O, N , and S, wherein the 5-membered aromatic ring is optionally substituted with 1-4 RB groups and the 6-membered aromatic ring is optionally substituted with 1-5 RB groups, wherein the RB groups are independently selected from: amides, optionally substituted with 1-3 groups selected from C₁₋₆ straight, branched and cyclic alkyl groups (optionally substituted with heteroaryl), 4 to 6 membered heterocyclyl (optionally substituted with oxo, C₁₋₆ straight, branched and cyclic alkyl groups , hydroxyalkyl, amide, alkylsulfonyl, and acetamide); or wherein the amide nitrogen atom forms part of a 3 to 8 membered heterocyclyl ring (optionally substituted with alkylsulfonyl or a straight, branched and cyclic C₁₋₆ alkyl group), imidazolidine-2,4-dione, heterocyclyls, optionally substituted with one or more groups independently selected from oxo, acyl, and a straight, branched, and cyclic C₁₋₆ alkyl group (which is optionally further substituted with 1-3 groups independently selected from oxo, hydroxy, and acyl), phosphorous acid optionally esterified with a C₁₋₆ linear, branched or cyclic group, dialkyl(C₁₋₆)phosphine oxides, alkyl(C₁₋₆)phosphinic acids optionally esterified with a C₁₋₆ alkyl group linear, branched or cyclic, halogens, cyano, hydroxy, carboxylic acids optionally esterified with a uronic acid or a linear, branched or cyclic C₁₋₆ alkyl group, oxo, dihydroxylboryl, 5- and 6-membered aromatic rings comprising 0-4 sele heteroatoms independently substituted with O, N, and S, optionally substituted with 1 or 2 substituents independently selected from straight, branched and cyclic C₁₋₆ alkyl groups which are optionally substituted with 1-4 substituents independently selected from hydroxy, carboxylic acids, pyrrolidin-2-one, straight, branched, and cyclic C₁₋₆ alkyl groups, and straight, branched, and cyclic C₁₋₆ alkylsulfonyl groups, and straight, branched, and cyclic C₁₋₆ alkoxy groups, sulfonic acid, alkylsulfonamide, C₁₋₆ straight, branched and cyclic alkylsulfonyl, aminosulfonyl groups, optionally substituted with 1 or 2 substituents independently selected from C₁₋₆ straight, branched and cyclic alkyl groups, C₁₋₆ straight, branched and cyclic alkyl groups which are optionally substituted with 1-4 substituents independently selected from halogen, hydroxy, carboxylic acid, straight, branched and C₁₋₆ alkoxy groups cyclic, heterocyclyl optionally substituted with oxo, and amide, straight, branched and cyclic C₁₋₆ alkoxy groups which are optionally substituted with 1-4 substituents independently selected from halogen, hydroxy, carboxylic acid, straight, branched C₁₋₆ alkyl groups and cyclic, and straight, branched and cyclic C₁₋₆ alkoxy groups, and tetrazolyl groups which are optionally substituted with substituents selected from halogen, hydroxy, carboxylic acid, straight, branched and cyclic C₁₋₆ alkyl groups, and C₁₋₆ alkoxy groups linear, branched, and cyclic, wherein 2 adjacent hydrogens on the 5- or 6-membered aromatic ring may be replaced by bonds to a second 5- or 6-membered aromatic ring comprising 0-4 heteroatoms independently selected from O, N, and S to form a bicyclic R² group which is optionally substituted with 1-6 RB groups; (iv) X¹ and X² are independently selected from hydrogen, halogens, cyano, hydroxy, straight, branched and cyclic C₁₋₆ groups, wherein straight, branched and cyclic C₁₋₆ groups are independently selected from alkyl, alkoxy, thioalkyl and aminoalkyl, and wherein the C₁₋₆ straight, branched and cyclic groups are optionally substituted with 1-4 independently selected halogens; (v) each of W¹ and W² is independently selected from C and N; (vi) each ⁻ ⁻ ⁻ ⁻ ⁻ represents a single or double bond, provided that not more than one ⁻ ⁻ ⁻ ⁻ ⁻ is a double bond; (vii) each R³ is independently selected from hydrogen, halogens, cyano, linear branched and cyclic C₁₋₆ alkyl groups, and linear branched and cyclic C₁₋₆ alkoxy groups, wherein linear branched and cyclic C₁₋₆ alkyl groups and the cyclic, branched, linear C₁₋₆ alkoxy groups are optionally substituted with 1-4 substituents independently selected from halogen, hydroxy and carboxylic acid groups; (viii) n is an integer selected from 0, 1, 2 and 3; and (ix) Z¹, Z², and Z³ are independently selected from carbon, nitrogen, sulfur, and oxygen, wherein, when Z¹, Z², and/or Z³ are carbon or nitrogen, the valencies of carbon and nitrogen are completed with hydrogen atoms, halogen, straight, branched and cyclic C₁₋₆ alkyl groups, and straight, branched and cyclic C₁₋₆ alkoxy groups, wherein straight, branched and cyclic C₁₋₆ alkyl groups and straight C₁₋₆ alkoxy groups , branched and cyclic are optionally substituted with 1-4 substituents selected from halogen, hydroxy and carboxylic acid groups. |
| priorityDate | 2019-05-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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