http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2771950-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_b0128b1ea25bace77f9ff5dc6b2210d7 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-05 |
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| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-416 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-401 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 |
| filingDate | 2015-02-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2020-07-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9b33f01e1dcd6b047713baa2d4150392 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_69586642ba4ec4da0ddb412ca56ae5af http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5a8ad2b919370673fbadc2266fbbfb6f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_91faed27476ef1302a3a5a3f4db588e4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1bf7924a81a6b92eba3c1ae1e9bf1e4e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d691a375ac80a8724f48b518f8489c78 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0c763860bc40fbc7bc371e00274465bc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_698c7c0e640c8661c0ace85354f4e2cb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2b3889931e8e47b5020f40f9d9e514fb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0069063e5d1ce54b9bc4d205df1345ba |
| publicationDate | 2020-07-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2771950-T3 |
| titleOfInvention | Aryl, heteroaryl and heterocyclic compounds for the treatment of complement-mediated disorders |
| abstract | A compound of Formula ** (See formula) ** and the pharmaceutically acceptable salts thereof, in which: R1, R1 ', R2, R2', R3 and R3 'are independently chosen from hydrogen, halogen, hydroxyl, nitro, cyano, amino, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C2-C6 alkynyl, C2-C6 alkanoyl, C1-C6 thioalkyl, hydroxy-C1-C6 alkyl, amino-C1 alkyl -C6, -C0-C4 alkylNR9R10, -C (O) OR9, -OC (O) R9, -NR9C (O) R10, -C (O) NR9R10, -OC (O) NR9R10, -NR9C (O) OR10 , C1-C2 haloalkyl and C1-C2 haloalkoxy, where R9 and R10 are independently selected at each occurrence from hydrogen, C1-C6 alkyl, (C3-C7 cycloalkyl) C0-C4 alkyl, -C0-C4 alkyl (C3-C7 cycloalkyl ) and -O-C0-C4 alkyl (C3-C7 cycloalkyl); or R1 and R2 can be taken together to form a 3-membered carbocyclic ring, or a 4- to 6-membered aryl or carbocyclic ring, or a 4- to 6-membered heteroaryl or heterocyclic ring containing 1 or 2 heteroatoms independently chosen from N , O or S; or R2 and R3 form a 3 to 6 membered aryl or carbocyclic ring or a 3 to 6 membered heteroaryl or heterocyclic ring; or R1 and R1 ', or R2 and R2', or R3 and R3 'form a 3- to 6-membered spiro carbocyclic ring; or R1 and R1 ', or R3 and R3' form a 3- to 6-membered spiro-heterocyclic ring containing 1 or 2 heteroatoms independently chosen from N, O, or S; or R2 and R2 'form a 3- to 6-membered spiro-heterocyclic ring, of which each ring is unsubstituted or substituted with 1 or more substituents independently chosen from halogen, hydroxyl, cyano, -COOH, C1-C4 alkyl, C2 alkenyl -C4, C2-C4 alkynyl, C1-C4 alkoxy, C2-C4 alkanoyl, hydroxy-C1-C4 alkyl, (mono- and di-C1-C4 alkylamino) C0-C4 alkyl, -C0-C4 alkyl (C3-cycloalkyl C7), -O-C0-C4 alkyl (C3-C7 cycloalkyl), C1-C2 haloalkyl and C1-C2 haloalkoxy; or R1 and R1 ', R2 and R2', or R3 and R3 'form a carbonyl group; or R1 and R2 or R2 and R3 form a carbon-carbon double bond; R5 and R6 are independently selected from -CHO, -C (O) NH2, -C (O) NH (CH3), C2-C6 alkanoyl, hydrogen, hydroxyl, halogen, cyano, nitro, -COOH, -SO2NH2, vinyl, C1-C6 alkyl, C2-C6 alkenyl, C1-C6 alkoxy, -C0-C4 alkyl (C3-C7 cycloalkyl), -C (O) C0-C4 alkyl (C3-C7 cycloalkyl), -P (O) (OR9 ) 2, -OC (O) R9, -C (O) OR9, -C (O) N (CH2CH2R9) (R10), -NR9C (O) R10, 5-6 membered phenyl or heteroaryl; and wherein each R5 and R6 other than hydrogen, hydroxyl, cyano, and -COOH is unsubstituted or optionally substituted; R8 and R8 'are independently selected from hydrogen, halogen, hydroxyl, C1-C6 alkyl, -C0-C4 alkyl (C3-C7 cycloalkyl), C1-C6 alkoxy and C0-C2 (C1-C4 alkylamino) alkyl; or R8 and R8 'are taken together to form an oxo group; or R8 and R8 'can be taken together with the carbon to which they are attached to form a 3-membered carbocyclic ring; X11 is N or CR11; X12 is N or CR12; X13 is N or CR13; X14 is N or CR14 and wherein no more than two of X11, X12, X13 and X14 are N; one of R12 and R13 is H and the other of R12 and R13 is R32, wherein at least one of R12 and R13 is present and is selected from R32; R32 is selected from aryl; saturated or unsaturated 5-6 membered heterocycle having 1, 2, or 3 heteroatoms independently chosen from N, O, and S, wherein the heterocycle is attached through a carbon atom in the heterocyclic ring to a carbon atom in the R12 or R13 position; and 5-6 membered heteroaryl having 1, 2 or 3 heteroatoms independently selected from N, O and S, wherein the aryl, heterocycle or heteroaryl ring may be optionally substituted; R11 and R14 are independently selected at each occurrence from hydrogen, halogen, hydroxyl, nitro, cyano, - O (PO) (OR9) 2, - (PO) (OR9) 2, C1-C6 alkyl, C2-C6 alkenyl, alkynyl C2-C6, C2-C6 alkanoyl, C1-C6 alkoxy, C1-C6 thioalkyl, -C0-C4 alkyl (mono- and di-C1-C6 alkylamino), -C0-C4 alkyl (C3-C7 cycloalkyl), -alkoxy C0-C4 (C3-C7 cycloalkyl), C1-C2 haloalkyl and C1-C2 haloalkoxy; R21 and R22 are independently selected at each occurrence from hydrogen, hydroxyl, cyano, amino, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, (C3-C7 cycloalkyl) C0-C4 alkyl, (phenyl) C0- alkyl C4, -C1-C4 alkyl (O) O-C1-C6 alkyl, -C1-C4OC alkyl (O) C1-C6 alkyl, -C1-C4C alkyl (O) O-C1-C6 alkyl, (heterocycloalkyl from 4 to 7-membered) C0-C4 alkyl having 1, 2, or 3 heteroatoms independently chosen from N, O, and S, and (5 or 6-membered aromatic or unsaturated heterocycle) C0-C4 alkyl having 1, 2, or 3 independently chosen heteroatoms between N, O and S, and each R21 and R22 may be optionally substituted; R23 is independently selected at each occurrence from C1-C6 alkyl, C1-C6 haloalkyl, (aryl) C0-C4 alkyl, (C3-C7 cycloalkyl) C0-C4 alkyl, (phenyl) C0-C4 alkyl, (4-4 heterocycloalkyl). 7-membered) C0-C4 alkyl having 1, 2, or 3 heteroatoms independently chosen from N, O, and S, and (5 or 6-membered aromatic or unsaturated heterocycle) C0-C4 alkyl having 1, 2, or 3 independently chosen heteroatoms between N, O and S, and each R23 may be optionally substituted; R24 and R25 are taken together with the nitrogen to which they are attached to form a 4- to 7-membered monocyclic heterocycloalkyl group or a 6 to 10-membered bicyclic heterocyclic group having fused, spiro, or attached rings, and each R24 and R25 may be optionally substituted; L is chosen from the formulas ** (See formula) ** or is a bond, where R17 is hydrogen, C1-C6 alkyl or -C0-C4 alkyl (C3-C7 cycloalkyl) and R18 and R18 'are independently chosen from hydrogen , halogen, hydroxymethyl and methyl; and m is 0, 1, 2, or 3; B is a monocyclic or bicyclic carbocyclic group; a monocyclic or bicyclic carbocyclic-oxy group; a monocyclic, bicyclic, or tricyclic heterocyclic group having 1, 2, 3, or 4 heteroatoms independently selected from N, O, and S, and from 4 to 7 ring atoms per ring; C2-C6 alkenyl; C2-C6 alkynyl; - (C0-C4 alkyl) (aryl); - (C0-C4 alkyl) (heteroaryl); or - (C0-C4 alkyl) (biphenyl) of which each B is unsubstituted or substituted with one or more substituents independently chosen from R33 and R34, and 0 or 1 substituents chosen from R35 and R36; R33 is independently selected from halogen, hydroxyl, -COOH, cyano, C1-C6 alkyl, C2-C6 alkanoyl, C1-C6 alkoxy, -C0-C4 alkylNR9R10, -SO2R9, C1-C2 haloalkyl, and C1-C2 haloalkoxy; R34 is independently selected from nitro, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 thioalkyl, -J-C3-C7 cycloalkyl, -B (OH) 2, -JC (O) NR9R23, -JOSO2OR21, -C ( O) (CH2) 1-4S (O) R21, -O (CH2) 1-4S (O) NR21R22, -JOP (O) (OR21) (OR22), - JP (O) (OR21) (OR22), -JOP (O) (OR21) R22, -JP (O) (OR21) R22, -JOP (O) R21R22, -JP (O) R21R22, -JSP (O) (OR21) (OR22), - JSP (O ) (OR21) (R22), -JSP (O) (R21) (R22), -JNR9P (O) (NHR21) (NHR22), -JNR9P (O) (OR21) (NHR22), - JNR9P (O) ( OR21) (OR22), -JC (S) R21, -JNR21SO2R22, -JNR9S (O) NR10R22, -JNR9SO2NR10R22, -JSO2NR9COR22, - JSO2NR9CONR21R22, -JNR21SO2R22, -JC22, -JC22 (NHR22) JC (NH2) NR9S (O) 2R22, -JOC (O) NR21R22, -JNR21C (O) OR22, -JNR21OC (O) R22, - (CH2) 1-4C (O) NR21R22, -JC (O) R24R25, -JNR9C (O) R21, -JC (O) R21, -JNR9C (O) NR10R22, -CCR21, - (CH2) 1-4OC (O) R21 and -JC (O) OR23; of which each R34 may be unsubstituted or substituted with one or more substituents independently chosen from halogen, hydroxyl, nitro, cyano, amino, oxo, -B (OH) 2, -Si (CH3) 3, -COOH, -CONH2 , -P (O) (OH) 2, C1-C6 alkyl, -C0-C4 alkyl (C3-C7 cycloalkyl), C1-C6 alkoxy, -C0-C2 alkyl (mono- and di-C1-C4 alkylamino), C1-C6 alkylester, C1-C4 alkylamino, hydroxyC1-C4 alkyl, C1-C2 haloalkyl, and C1-C2 haloalkoxy; R35 is independently selected from naphthyl, naphthyloxy, indanyl, (4- to 7-membered heterocycloalkyl) C0-C4 alkyl containing 1 or 2 heteroatoms selected from N, O, and S, and bicyclic heterocycle containing 1, 2, or 3 independently chosen heteroatoms between N, O and S, and containing from 4 to 7 ring atoms in each ring; of which each R35 is unsubstituted or substituted with one or more substituents independently chosen from halogen, hydroxyl, nitro, cyano, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkanoyl, C1-C6 alkoxy, (mono- and C1-C6 dialkylamino) C0-C4 alkyl, C1-C6 alkylester, -C0-C4 alkyl (C3-C7 cycloalkyl), -SO2R9, C1-C2 haloalkyl and C1-C2 haloalkoxy; and R36 is independently selected from tetrazolyl, (phenyl) C0-C2 alkyl, (phenyl) C1-C2 alkoxy, phenoxy, and 5- or 6-membered heteroaryl containing 1, 2, or 3 heteroatoms independently chosen from N, O, B, and S , of which each R36 is unsubstituted or substituted with one or more substituents independently chosen from halogen, hydroxyl, nitro, cyano, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkanoyl, C1-C6 alkoxy, (mono- and di-C1-C6 alkylamino) C0-C4 alkyl, C1-C6 alkylester, -C0-C4 alkyl (C3-C7 cycloalkyl), -SO2R9, -OSi (CH3) 2C (CH3) 3, -Si (CH3) 2C (CH3) 3, C1-C2 haloalkyl and C1-C2 haloalkoxy; and J is independently selected at each occurrence from a covalent bond, C1-C4 alkylene, -O-C1-C4 alkylene, C2-C4 alkenylene, and C2-C4 alkynylene; wherein, unless otherwise specified, any group that is optionally substituted may be independently substituted with one or more of the following: halogen; cyano; hydroxyl; nitro; azido; alkanoyl; carboxamide; alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, aryloxy such as phenoxy; alkylthio including those having one or more thioether linkages; alkylsulfimyl; alkylsulfonyl groups including those having one or more sulfonyl bonds; aminoalkyl groups including groups having one or more N atoms; aryl; arylalkyl having 1 to 3 separate or fused rings and 6 to about 14 or 18 ring carbon atoms; arylalkoxy having 1 to 3 separate or fused rings; or a saturated, unsaturated or aromatic heterocyclic group having 1 to 3 rings separated or fused with one or more N, O or S atoms; amino, -CHO, -COOH, -CONH2, C1-C6 alkylester, (mono- and di-C1-C6 alkylamino) C0-C2 alkyl, C1-C2 haloalkyl, hydroxy-C1-C6 alkyl, ester, carbamate, urea, sulfonamide, -C1-C6 alkyl (heterocycle), C1-C6 alkyl (heteroaryl), -C1-C6 alkyl (C3-C7 cycloalkyl), -O-C1-C6 alkyl (C3-C7 cycloalkyl), B (OH) 2, phosphate, phosphonate and C1-C2 haloalkoxy. |
| priorityDate | 2014-02-25-04:00^^<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: 939.