http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-118083-A1
Outgoing Links
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|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_57f93627efa04730df1522a17253f05a |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4365 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4725 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-113 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D495-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-541 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-113 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4725 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-54 |
| filingDate | 2020-02-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_48eb2a3aec7448463b46b870ad8e17b7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cf5a79fc87edb14a6cc2553ac8d720ec http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ad2e3015243b278a275d9c2efa51bbca http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c02db2d110e1312987a7c005afd311c7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9c6b120fa700425adecc6842911d8f3c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_609b2c2edc727d61aa7a58dcdbc6368d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d34db6550697ac06e8ead45c74735d02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5a9d0d7d5ab5b2e90a77b676b7a910d3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_420e5302d6a066338106fd4840893086 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_86b1ac370d0e471f20f9a99452494729 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2a15ddcf006c7c8d22c7c35c2f1e16ba http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_29fe0b30e5ca6091edfa4ca075b2e034 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_32d1b994b6b2bb261dbf577fc020d155 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f0c24a7db49f0eebaa831771da22946e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fa743a31e1e674622682c393b679e4ca http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6dd36b5ff97fcd098a3f14629e7b763a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_544d0278dcd0040fa297957bf02415e2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fee9f09e31f96f58a239d0d4faea1d38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_01a3a4d03fedf8e4adc82b931762ccd1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a5565a2af85dff6ee6d85ef1d2a0c9b1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d4c918ce4dee9f9ae8186b0e45853091 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_00a4a6563016ce6c31a470c4ef37c457 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bee7f163f285e5e8ceab1396828e5035 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f11f72adaf5d7ae497affc64601134ae http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8de8cef58055d07e990426c446d2aac1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f7b4c36b385f1cd596fb4730067b647b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dc1941148ad121d18e28fe4e56bf93e3 |
| publicationDate | 2021-09-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-118083-A1 |
| titleOfInvention | ENZYME INHIBITORS |
| abstract | The present provides compounds of formula (1) and (1a), compositions comprising said compounds; the use of said compounds in therapy; and methods of treating patients with said compounds; where A, B, n, R², R³, R⁴, R⁵ and R⁶ have the definition provided herein. Claim 1: A compound of formula (1) or (1a), where: n is 0, 1 or 2; A is (i) a 5-membered heteroaryl of formula (2), where W is S; Z is C or N; X and Y are C; R¹ is absent; R⁴ is absent or H; R² and R³ are independently selected from H, halo, alkyl, -SO₂NR¹³R¹⁴, - (CH₂) ₀₋₃heterocyclyl, - (CH₂) ₀₋₃NR¹² (CH₂) ₀₋₃ (heterocyclyl) and - (CH₂) ₀₋₃aryl; and wherein one of R² or R³ is not H; or where W is S; X, Y and Z are C; R¹ is absent; R³ is halo or alkyl; R⁴ is H, halo, or alkyl; and R² is selected from - (CH₂) ₀₋₃NR¹³R¹⁴, - (CH₂) ₀₋₃NR¹² (CH₂) ₀₋₃ (aryl), - (CH₂) ₀₋₃NR¹² (CH₂) ₀₋₃ (heterocyclyl), - (CH₂ ) ₀₋₃-O- (CH₂) ₀₋₃ (aryl), - (CH₂) ₀₋₃-O- (CH₂) ₀₋₃ (heterocyclyl), - (CH₂) ₀₋₃-O- (CH₂) ₀₋₃ (heteroaryl), - (CH₂) ₀₋₃-O- (CH₂) ₁₋₄NR¹³R¹⁴ and - (CH₂) ₀₋₃heterocyclyl; or where X, Y, and Z are independently N, C, or S; wherein at least one of X, Y, and Z is N or S; W is C; R³ and R⁴ are independently absent or independently selected from H, alkyl, and halo; R² is selected from H, halo, alkyl, and cycloalkyl; and R¹ is selected from - (CH₂) ₀₋₃NR¹² (CH₂) ₀₋₃ (heterocyclyl), - (CH₂) ₀₋₃NR¹²CO (CH₂) ₀₋₃ (heterocyclyl), - (CH₂) ₀₋₃-O- ( CH₂) ₀₋₃ (heterocyclyl) and - (CH₂) ₀₋₃heterocyclyl; or where Y and Z are N; W and X are C; R¹ and R² are selected from H, halo, alkyl, cycloalkyl, and - (CH₂) ₀₋₃aryl; R³ and R⁴ are independently absent or independently selected from - (CH₂) ₀₋₃heterocyclyl and - (CH₂) aryl; and wherein at least one of R³ or R⁴ is selected from - (CH₂) ₀₋₃heterocyclyl and - (CH₂) aryl; or where Y or Z are independently C, N, or S; wherein at least one of Y and Z is N or S; W and X are C; R¹ is H; R² is selected from H, alkyl, aryl, and halo; R⁴ is absent, or selected from H and alkyl; and R³ is (CH₂) ₀₋₃ (heterocyclyl); or where Y and X are independently C or N; wherein at least one of Y or X is N; W and Z are C; R¹ and R⁴ are independently selected from H, alkyl, and halo; and one of R² and R³ is absent and the other of R² and R³ is a residue of formula (4); m is 0, 1, 2, or 3; R⁹ is selected from H and alkyl; each R¹⁰ is independently selected from alkyl and halo; or A is (ii) a 9-membered heteroaromatic bicyclo of formula (3) wherein X and Y are independently selected from C, N, or S; wherein at least one of X and Y is N or S; wherein R¹ and R⁶ are independently absent or independently selected from H and - (CH₂) ₀₋₃heterocyclyl; wherein R² is selected from H, halo, - (CH₂) ₀₋₃NR¹² (CH₂) ₀₋₃ (heterocyclyl) and - (CH₂) ₀₋₃heterocyclyl; R³, R⁴, and R⁵ are independently selected from H, alkyl, and halo; and wherein at least one of R², R³, R⁴, R⁵ is not absent or H; or, formula (1a) where n is 0, 1 or 2; wherein Z and Y are independently selected from C and N; where R⁶ is selected from H and alkyl; wherein R⁴ and R⁵ are independently absent, or independently selected from H, alkyl, and halo; and wherein one of R² and R⁵ is - (CH₂) ₀₋₃NR¹² (CH₂) ₀₋₃ (heterocyclyl) and the other of R² and R⁵ is selected from H, alkyl, and halo; B is: (i) a fused 6.5 or 6.6 heteroaromatic bicyclic ring, containing N and optionally one or two additional heteroatoms independently selected from N, O and S; wherein the 6.5 or 6.6 fused heteroaromatic bicyclic ring may be optionally substituted with 1, 2, or 3 substituents selected from alkyl, alkoxy, OH, halo, CN, -COOR¹³, -CONR¹³R¹⁴, CF₃ and -NR¹³R¹⁴; wherein the 6.5 heteroaromatic bicyclic ring can be attached via the 6 or 5 membered ring; or (ii) phenyl substituted with - (CH₂) ₁₋₃NH₂ and two groups selected from methyl, ethyl and propyl; or (iii) pyridine substituted with NH₂ and two groups selected from methyl, ethyl and propyl; (iv) a fused 6.5 or 6.6 bicyclic ring containing N and containing an aromatic ring fused to a non-aromatic ring and optionally one or two additional heteroatoms independently selected from N, O and S; wherein the fused 6.5 or 6.6 bicyclic ring may be optionally substituted with 1, 2, or 3 substituents selected from alkyl, alkoxy, OH, halo, CN, -COOR¹³, -CONR¹³R¹⁴, CF₃ and -NR¹³R¹⁴; wherein the 6.5 bicyclic ring can be attached via the 6 or 5 membered ring; alkoxy is an O-linked linear hydrocarbon of 1 to 6 carbon atoms (C₁₋₆) or a branched O-linked hydrocarbon of 3 to 6 carbon atoms (C₃₋₆); alkoxy may be optionally substituted with 1 or 2 substituents independently selected from OH, CN, CF₃, -N (R¹²) ₂, and fluoro; alkyl is a linear saturated hydrocarbon having up to 10 C₁₋₁₀ carbon atoms or a branched saturated hydrocarbon of 3 to 10 C₃₋₁₀ carbon atoms; the alkyl may be optionally substituted with 1 or 2 substituents independently selected from C₁₋₆ alkoxy, OH, -NR¹³R¹⁴, -NHCOCH₃, -CO (heterocyclylᵇ), -COOR¹³, -CONR¹³R¹⁴, CN, CF₃, halo, oxo and heterocyclylᵇ; alkylᵇ is a linear saturated hydrocarbon having up to 10 carbon atoms (C₁₋₁₀) or a branched saturated hydrocarbon having between 3 and 10 carbon atoms (C₃₋₁₀); alkyl may be optionally substituted with 1 or 2 substituents independently selected from C₁₋₆ alkoxy, OH, -N (R¹²) ₂, -NHCOCH₃, CF₃, halo, oxo, cyclopropane, -O (arylᵇ), arylᵇ, and heterocyclylᵇ; alkylene is a divalent linear saturated hydrocarbon having 1 to 5 carbon atoms (C₁₋₅); Alkylene may be optionally substituted with 1 or 2 substituents independently selected from alkyl, C₁₋₆alkoxy, OH, CN, CF₃, and halo; aryl is phenyl, biphenyl, or naphthyl; aryl may be optionally substituted with 1, 2 or 3 substituents independently selected from alkyl, alkoxy, OH, -SO₂CH₃, halo, CN, - (CH₂) ₀₋₃-O-heteroarylᵇ, arylᵇ, -O -arylᵇ, - (CH₂ ) ₀₋₃-heterocyclylᵇ, - (CH₂) ₁₋₃-arylᵇ, - (CH₂) ₀₋₃-heteroarylᵇ, -COOR¹³, -CONR¹³R¹⁴, - (CH₂) ₀₋₃-NR¹³R¹⁴, OCF₃ and CF₃; or two adjacent ring carbon atoms in the aryl may optionally be linked by a heteroalkylene to form a non-aromatic ring containing 5, 6, or 7 ring members; or optionally wherein two adjacent aryl ring atoms are joined to form a 5- or 6-membered aromatic ring containing 1 or 2 heteroatoms selected from N, NR⁸, S, and O; arylᵇ is phenyl, biphenyl or naphthyl, which may be optionally substituted with 1, 2 or 3 substituents independently selected from methyl, ethyl, propyl, isopropyl, alkoxy, OH, -SO₂CH₃, N (R¹²) ₂, halo, CN and CF₃, or two adjacent carbon ring atoms on the aryl may optionally be linked by a heteroalkylene to form a non-aromatic ring containing 5, 6, or 7 ring members; cycloalkyl is a saturated monocyclic hydrocarbon ring of 3 to 6 carbon atoms (C₃₋₆); cycloalkyl may be optionally substituted with 1 or 2 substituents independently selected from alkylᵇ, C₁₋₆alkoxy, OH, CN, CF₃, and halogen; halo is F, Cl, Br, or I; heteroalkylene is a divalent linear saturated hydrocarbon having 2 to 5 carbon atoms (C₂₋₅), in which 1 or 2 of the 2 to 5 carbon atoms are replaced with NR⁸, S or O; heteroalkylene may be optionally substituted with 1 or 2 substituents independently selected from C₁₋₆alkoxy alkyl, OH, CN, CF₃, and halo; heteroaryl is a carbon-containing 5- or 6-membered aromatic ring containing 1, 2, 3, or 4 ring members selected from N, NR⁸, S, and O; heteroaryl may be optionally substituted with 1, 2 or 3 substituents independently selected from alkyl, alkoxy, arylᵇ, OH, OCF₃, halo, heterocyclylᵇ, CN and CF₃, heteroarylᵇ is a 5 or 6-membered carbon-containing aromatic ring containing one, two or three ring members selected from N, NR⁸, S, and O; heteroarylᵇ may be optionally substituted with 1, 2, or 3 substituents independently selected from methyl, ethyl, propyl, isopropyl, alkoxy, OH, OCF₃, halo, CN, and CF₃; heterocyclyl is a 4, 5, 6, or 7-membered non-aromatic carbon-containing ring containing one or two ring members selected from N, NR⁸, S, SO, SO₂, and O; the heterocyclyl may be optionally substituted with 1, 2, 3, or 4 substituents independently selected from alkylᵇ, alkoxy, OH, OCF₃, halo, oxo, CN, -NR¹³R¹⁴, -O (arylᵇ), -O (heteroarylᵇ) and CF₃; or optionally wherein two ring atoms in heterocyclyl are linked with an alkylene to form a non-aromatic ring containing 5, 6, or 7 ring members; or optionally wherein two adjacent ring atoms in heterocyclyl are linked to form a 5- or 6-membered aromatic ring containing 1 or 2 heteroatoms selected from N, NR⁸, S, and O; or optionally wherein a carbon ring atom in heterocyclyl is substituted with a heteroalkylene such that the carbon ring atom in heterocyclyl together with the heteroalkylene forms a heterocyclylᵇ which is spiro to heterocyclyl ring; heterocyclylᵇ is a 4, 5, 6 or 7-membered non-aromatic carbon-containing ring containing one or two ring members selected from N, NR¹², S, SO, SO₂, and O; heterocyclylᵇ may be optionally substituted with 1, 2, 3, or 4 substituents independently selected from methyl, ethyl, propyl, isopropyl, alkoxy, OH, OCF₃, halo, oxo, CN, and CF₃; R¹³ and R¹⁴ are independently selected from H, -SO₂CH₃, alkylᵇ, heteroarylᵇ, and cycloalkyl; or R¹³ and R¹⁴ together with the nitrogen atom to which they are attached form a 4-, 5-, 6- or 7-membered heterocyclyl ring containing carbon, optionally containing an additional heteroatom selected from N, NR⁸, S, SO, SO₂ and O , which may be saturated or unsaturated with 1 or 2 double bonds and which may be optionally mono or di-substituted with substituents independently selected from oxo, alkylᵇ, alkoxy, OH, halo, -SO₂CH₃ and CF₃, or R¹³ and R¹⁴ together with the nitrogen atom to which they are attached form a carbon-containing 5- or 6-membered heterocyclic ring, which fuses to an arylᵇ or a heteroarylᵇ; R⁸ is independently selected from H, -SO₂CH₃, alkylᵇ, - (CH₂) ₀₋₃arylᵇ, - (CH₂) ₀₋₃heteroarylᵇ, - (CH₂) ₀₋₃cycloalkyl and - (CH₂) ₀₋₃heterocyclylᵇ; or R⁸ is a 4, 5, 6, or 7-membered carbon-containing heterocyclic ring containing 1, 2, or 3 heteroatoms independently selected from N, NR¹², S, SO, SO₂, and O, which may be saturated or unsaturated with 1 or 2 double bonds and which may be optionally mono or disubstituted with substituents independently selected from oxo, alkylᵇ, alkoxy, OH, halo, -SO₂CH₃ and CF₃; R¹² is independently selected from H, -SO₂CH₃, -COCH₃, methyl, ethyl, propyl, isopropyl, and cycloalkyl; and tautomers, isomers, stereoisomers (including enantiomers, diastereoisomers, and racemic and non-racemic mixtures thereof), deuterated isotopes, and their pharmaceutically acceptable salts and / or solvates. |
| priorityDate | 2019-08-21-04:00^^<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: 84.