http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2852123-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f2534bb9f13460c6429c25acf8df25d0 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F7-0812 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-541 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-551 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-553 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 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/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-541 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-551 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-553 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 |
| filingDate | 2017-11-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2021-09-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ca4d4a12b0228de1f35366076548929f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a0ca5a12e29ec72265e1e310b6f82de2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b3557c50bd54f9e75c6c586be0ca5136 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1e013b678d951223f798bd3ac968ebf2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f7c7fc469a20d01091b2750014ecc9ff http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dd098d38d26d6bb78fdbe813393d10ff http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_18e573b35155382a8029ab6322d994ee http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c805118fa1df0a41d263fe6207e2ed99 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b6bc7d35f62d2775882c72a9bd318b2a |
| publicationDate | 2021-09-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2852123-T3 |
| titleOfInvention | Derivatives of ((pyridin-2-yl) -amino) pyrido [3,4-d] pyrimidine and ((pyridazin-3-yl) -amino) pyrido [3,4-d] pyrimidine as CDK4 / 6 inhibitors for try p. ex. rheumatoid arthritis, arteriosclerosis, pulmonary fibrosis, stroke, or cancer |
| abstract | A compound represented by formula (I): **(See formula)** wherein in the formula, R1 represents C3-12 cycloalkyl, C4-12 cycloalkenyl, 4-12 membered heterocyclyl, C6-10 aryl, or 5 to 10 membered heteroaryl, wherein each heteroatom-containing group represented by R1 contains from one to four heteroatoms independently selected from oxygen, sulfur and nitrogen atoms, R1 is optionally substituted with one to six substituents selected from the group consisting of one halogen atom, =O, -OH, -CN, -COOH, -COOR6, -R7, C3-6 cycloalkyl substituted with zero to two -OH groups, zero to two fluorine atoms, zero substituted C1-8 acyl to two -OH groups, zero to two C1-8 alkoxy groups, and zero to six fluorine atoms, and C1-8 alkoxy substituted with zero to two -OH groups, zero to two C1-8 alkoxy groups, and zero to six fluorine atoms; R6 and R7 each independently represent C1-6 alkyl substituted with zero to two -OH groups, zero to two C1-8 alkoxy groups, and zero to six fluorine atoms; R2 represents C1-8 alkyl, C3-8 cycloalkyl, 4-6 membered heterocyclyl, C1-8 acyl, -COOR8, or -CONR9R10, where each C1-8 alkyl represented by R2 is independently substituted with zero to a group -OH, zero to two C1-8 alkoxy groups substituted with zero to one -OH group, zero to one C1-4 alkoxy group, and zero to three fluorine atoms and zero to five fluorine atoms; each C3-8 cycloalkyl represented by R2 is independently substituted with zero to an -OH group, zero to two C1-8 alkoxy groups substituted with zero to an -OH group, zero to a C1-4 alkoxy group, and zero to three fluorine atoms, zero to one hydroxymethyl group, and zero to five fluorine atoms; provided that R2 is not an unsubstituted C1-8 alkyl or an unsubstituted C3-8 cycloalkyl or trifluoromethyl group; each of R8, R9 and R10 independently represents a hydrogen atom or C1-8 alkyl; each 4-6 membered heterocyclyl represented by R2 is optionally substituted with one to four substituents selected from the group consisting of fluorine atom, -OH group, C1-4 alkyl groups and C1-4 alkoxy groups; each of C1-8 acyl group, -COOR8 and -CONR9R10 represented by R2 is optionally independently substituted with one to four substituents selected from the group consisting of fluorine atom, -OH group and C1-4 alkoxy groups; R9 and R10 of -CONR9R10 represented by R2 are optionally linked via a single bond or -O- to form a ring including the nitrogen atom attached to R9 and R10; each heterocyclyl group represented by R2 contains one oxygen atom as a heteroatom in the case of a 4- or 5-membered ring, and one to two oxygen atoms as a heteroatom in the case of a 6-membered ring; R3 represents a hydrogen atom, C1-8 alkyl or a halogen atom; X represents CR11 or a nitrogen atom; R11 represents a hydrogen atom, C1-6 alkyl, or C3-6 cycloalkyl; R4 is represented by -A1-A2-A3; A1 represents a single bond or C1-8 alkylene; one to two sp3 carbon atoms at any position of A1 are optionally replaced independently with one or two structures selected from the group consisting of -O-, -NR14-, -C(=O)-, -C(=O )-O-, -O-C(=O)-, -O-C(=O)-O-, -C(=O)-NR15-, -O-C(=O)-NR16-, -NR17-C(=O )-, -NR18-C(=O)-O-, -NR19-C(=O)-NR20-, -S(=O)p-, -S(=O)2- NR21-, -NR22- S(=O)2-, and -NR23-S(=O)2-NR24-, provided that no structure selected from -O-O-, -O-NR14-, -NR14-O-, -O-CH2-O -, -O-CH2-NR14-, and -NR14-CH2-O- is formed in the case of substitution of two sp3 carbon atoms; A2 represents a single bond, C1-7 alkylene, C3-12 cycloalkylene, C3-12 cycloalkylidene, 4-12 membered heterocyclylene, 4-12 membered heterocyclylidene, C6-10 arylene or 5-10 membered heteroarylene; A3 represents a halogen, -CN, -NO2, -R25, -OR26, -NR27R28, -C(=O)R29, -C(=O)-OR30, -O-C(=O)R31, -OC(=O )-NR32R33, -C(=O)-NR34R35, -NR36-C(=O)R37, -NR38-C(=O)-OR39, -S(=O)2-R40, -S(=O) 2-NR41R42, or -NR43-S(=O)2R44; provided that A3 represents -R25 if the terminal of A1 on the side of A2 is a structure selected from the group consisting of -O-, -NR14-, -C(=O)-, -C(=O)-O- , -O-C(=O)-, -O-C(=O)-O-, -C(=O)-NR15-, -OC(=O)-NR16-, -NR17-C(=O)-, - NR18-C(=O)-O-, -NR19-C(=O)-NR20-, -S(=O)p-, -S(=O)2-NR21-, -NR22-S(=O )2-, and -NR23-S(=O)2-NR24- and A2 is a single bond; each of R14, R32, R34, R36, R38, R41 and R43 independently represents a hydrogen atom, C1-8 alkyl, C1-8 acyl, C1-8 alkylsulfonyl, 4- to 12-membered heterocyclyl, C3-12 cycloalkyl, aryl C6-10, 5-10 membered heteroaryl, (4-12 membered heterocyclyl)-C1-3 alkyl, (C3-12 cycloalkyl)-C1-3 alkyl, (C6-10 aryl)-C1-3 alkyl or ( 5- to 10-membered heteroaryl)-C1-3alkyl; each of R15 to R31, R33, R35, R37, R39, R40, R42 and R44 independently represents a hydrogen atom, C1-8 alkyl, 4-12 membered heterocyclyl, C3-12 cycloalkyl, C6-10 aryl, heteroaryl 5 to 10 membered, (4 to 12 membered heterocyclyl)-C1-3 alkyl, (C3-12 cycloalkyl)-C1-3 alkyl, (C6-10 aryl)-C1-3 alkyl or (5 to 10 heteroaryl members)- C1-3 alkyl; A1, A2, A3 and R14 to R44 contained in A1 and A3 are each optionally substituted independently with one to four substituents selected from the group consisting of -OH, =O, -COOH, -SO3H, -PO3H2, -CN, -NO2, a halogen, C1-8 alkyl substituted with zero to two -OH groups, zero to two -OR45 groups, and zero to six fluorine atoms, C3-12 cycloalkyl substituted with zero to two -OH groups, zero to two -OR46 groups, and zero to six fluorine atoms, C1-8 alkoxy substituted with zero to two -OH groups, zero to two -OR47 groups, and zero to six fluorine atoms, and 4 to 12-membered heterocyclyl substituted with zero to two -OH groups, zero to two -OR49 groups, and zero to six fluorine atoms; R14 to R44 are optionally attached at A1, at A3, between A1 and A2, between A1 and A3, or between A2 and A3 via a single bond, -O-, -NR50-, or -S(=O)p - to form a ring; R11 is optionally linked to A1, A2, or A3 through a single bond, -O-, -NR51-, or -S(=O)p- to form a ring; R45 to R47 and R49 to R51 each represent a hydrogen atom, or C1-4 alkyl substituted with zero to one -OH group and zero to six fluorine atoms; p represents an integer from zero to two; and each of heterocyclyl, heteroaryl, (heterocyclyl)-alkyl and (heteroaryl)-alkyl represented by A1 and A3 and heterocyclylene, heterocyclylidene and heteroarylene represented by A2 contains from one to four heteroatoms independently selected from oxygen, sulfur and nitrogen, or a pharmaceutically acceptable salt thereof. |
| priorityDate | 2016-11-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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