CA2723185A1 - Inhibitors of protein kinases - Google Patents

Info

Publication number

CA2723185A1

CA2723185A1 CA2723185A CA2723185A CA2723185A1 CA 2723185 A1 CA2723185 A1 CA 2723185A1 CA 2723185 A CA2723185 A CA 2723185A CA 2723185 A CA2723185 A CA 2723185A CA 2723185 A1 CA2723185 A1 CA 2723185A1

Authority

CA

Canada

Prior art keywords

ylamino

pyrrolo

8alkylene

pyrimidin

compound

Prior art date

2008-04-22

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Abandoned

Links

• Espacenet
• Global Dossier
• CIPO
• Discuss

• 239000003112 inhibitor Substances 0.000 title abstract description 31
• 102000001253 Protein Kinase Human genes 0.000 title description 7
• 108060006633 protein kinase Proteins 0.000 title description 7
• 150000001875 compounds Chemical class 0.000 claims abstract description 373
• 102000042838 JAK family Human genes 0.000 claims abstract description 117
• 108091082332 JAK family Proteins 0.000 claims abstract description 117
• 238000000034 method Methods 0.000 claims abstract description 109
• 150000003839 salts Chemical class 0.000 claims abstract description 72
• 230000000694 effects Effects 0.000 claims abstract description 66
• 230000001404 mediated effect Effects 0.000 claims abstract description 64
• 208000007536 Thrombosis Diseases 0.000 claims abstract description 15
• 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims abstract description 14
• -1 amino, hydroxy Chemical group 0.000 claims description 197
• 125000000623 heterocyclic group Chemical group 0.000 claims description 150
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 114
• 125000000217 alkyl group Chemical group 0.000 claims description 104
• 125000003118 aryl group Chemical group 0.000 claims description 104
• 239000000203 mixture Substances 0.000 claims description 100
• 210000004027 cell Anatomy 0.000 claims description 98
• 125000001072 heteroaryl group Chemical group 0.000 claims description 94
• 125000001424 substituent group Chemical group 0.000 claims description 79
• 229910052739 hydrogen Inorganic materials 0.000 claims description 71
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 66
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 59
• 201000010099 disease Diseases 0.000 claims description 58
• 208000035475 disorder Diseases 0.000 claims description 55
• 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 52
• 125000005843 halogen group Chemical group 0.000 claims description 51
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 50
• 229910052757 nitrogen Inorganic materials 0.000 claims description 49
• 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims description 48
• 125000004093 cyano group Chemical group *C#N 0.000 claims description 44
• 125000004043 oxo group Chemical group O=* 0.000 claims description 42
• 229910052799 carbon Inorganic materials 0.000 claims description 39
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 37
• 208000023275 Autoimmune disease Diseases 0.000 claims description 34
• 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 31
• 210000003719 b-lymphocyte Anatomy 0.000 claims description 24
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 24
• 201000006417 multiple sclerosis Diseases 0.000 claims description 23
• 230000019491 signal transduction Effects 0.000 claims description 23
• 125000004076 pyridyl group Chemical group 0.000 claims description 22
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 21
• 206010020751 Hypersensitivity Diseases 0.000 claims description 19
• 125000005842 heteroatom Chemical group 0.000 claims description 19
• 230000002401 inhibitory effect Effects 0.000 claims description 19
• 238000011282 treatment Methods 0.000 claims description 19
• 206010052779 Transplant rejections Diseases 0.000 claims description 15
• 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 15
• 208000032839 leukemia Diseases 0.000 claims description 15
• 229910052736 halogen Inorganic materials 0.000 claims description 14
• IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 claims description 13
• 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 13
• 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 13
• 239000003937 drug carrier Substances 0.000 claims description 13
• 150000002367 halogens Chemical class 0.000 claims description 13
• 229910052717 sulfur Inorganic materials 0.000 claims description 13
• 208000002250 Hematologic Neoplasms Diseases 0.000 claims description 12
• 125000006598 aminocarbonylamino group Chemical group 0.000 claims description 12
• 208000037803 restenosis Diseases 0.000 claims description 12
• 206010039073 rheumatoid arthritis Diseases 0.000 claims description 12
• 208000006673 asthma Diseases 0.000 claims description 11
• 230000007815 allergy Effects 0.000 claims description 10
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 10
• 230000002062 proliferating effect Effects 0.000 claims description 10
• 208000007056 sickle cell anemia Diseases 0.000 claims description 10
• 208000027930 type IV hypersensitivity disease Diseases 0.000 claims description 10
• RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 9
• 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims description 9
• 125000003545 alkoxy group Chemical group 0.000 claims description 9
• 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 9
• 239000003085 diluting agent Substances 0.000 claims description 9
• 125000001841 imino group Chemical group [H]N=* 0.000 claims description 9
• 208000027866 inflammatory disease Diseases 0.000 claims description 9
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 9
• 125000003386 piperidinyl group Chemical group 0.000 claims description 9
• 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 8
• 206010025323 Lymphomas Diseases 0.000 claims description 8
• GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical group C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 8
• 206010053613 Type IV hypersensitivity reaction Diseases 0.000 claims description 8
• 229910052794 bromium Inorganic materials 0.000 claims description 8
• 208000010125 myocardial infarction Diseases 0.000 claims description 8
• 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 8
• NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 8
• 208000024172 Cardiovascular disease Diseases 0.000 claims description 7
• 206010062506 Heparin-induced thrombocytopenia Diseases 0.000 claims description 7
• 208000028622 Immune thrombocytopenia Diseases 0.000 claims description 7
• 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims description 7
• 125000005001 aminoaryl group Chemical group 0.000 claims description 7
• 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims description 7
• 208000026935 allergic disease Diseases 0.000 claims description 6
• 229910052801 chlorine Inorganic materials 0.000 claims description 6
• 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 6
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 6
• 229910052731 fluorine Inorganic materials 0.000 claims description 6
• 239000012528 membrane Substances 0.000 claims description 6
• ISPIWMLOLHWBJV-UHFFFAOYSA-N 1-[2-(4-piperazin-1-ylanilino)-7h-pyrrolo[2,3-d]pyrimidin-4-yl]piperidine-3-carboxamide Chemical compound C1C(C(=O)N)CCCN1C1=NC(NC=2C=CC(=CC=2)N2CCNCC2)=NC2=C1C=CN2 ISPIWMLOLHWBJV-UHFFFAOYSA-N 0.000 claims description 5
• VPQNMDJVVNHZTD-UHFFFAOYSA-N 2-[4-(4-acetylpiperazin-1-yl)anilino]-4-[4-(aminomethyl)piperidin-1-yl]-7h-pyrrolo[2,3-d]pyrimidine-5-carbonitrile Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(N2CCC(CN)CC2)=C(C(=CN2)C#N)C2=N1 VPQNMDJVVNHZTD-UHFFFAOYSA-N 0.000 claims description 5
• 208000004476 Acute Coronary Syndrome Diseases 0.000 claims description 5
• 206010002388 Angina unstable Diseases 0.000 claims description 5
• 201000001320 Atherosclerosis Diseases 0.000 claims description 5
• 201000004681 Psoriasis Diseases 0.000 claims description 5
• 208000021386 Sjogren Syndrome Diseases 0.000 claims description 5
• 208000007814 Unstable Angina Diseases 0.000 claims description 5
• 125000006517 heterocyclyl carbonyl group Chemical group 0.000 claims description 5
• 201000004332 intermediate coronary syndrome Diseases 0.000 claims description 5
• 206010025135 lupus erythematosus Diseases 0.000 claims description 5
• 229910052760 oxygen Inorganic materials 0.000 claims description 5
• 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 5
• MFMUWALWYSDAIX-INIZCTEOSA-N (3s)-1-[2-(4-piperazin-1-ylanilino)-7h-pyrrolo[2,3-d]pyrimidin-4-yl]pyrrolidin-3-ol Chemical compound C1[C@@H](O)CCN1C1=NC(NC=2C=CC(=CC=2)N2CCNCC2)=NC2=C1C=CN2 MFMUWALWYSDAIX-INIZCTEOSA-N 0.000 claims description 4
• ITBJIOFDMUDQPI-UHFFFAOYSA-N 1-[2-[4-(4-acetylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]piperidine-3-carboxamide Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(F)C(N2CC(CCC2)C(N)=O)=N1 ITBJIOFDMUDQPI-UHFFFAOYSA-N 0.000 claims description 4
• BKSBYMLCXXKXNA-UHFFFAOYSA-N 1-[2-[4-(4-acetylpiperazin-1-yl)anilino]-7h-pyrrolo[2,3-d]pyrimidin-4-yl]piperidine-3-carboxamide Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(N2CC(CCC2)C(N)=O)=C(C=CN2)C2=N1 BKSBYMLCXXKXNA-UHFFFAOYSA-N 0.000 claims description 4
• QORZSWGMEPAGEF-UHFFFAOYSA-N 1-[2-[4-(4-acetylpiperazin-1-yl)anilino]-7h-pyrrolo[2,3-d]pyrimidin-4-yl]piperidine-4-carboxamide Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(N2CCC(CC2)C(N)=O)=C(C=CN2)C2=N1 QORZSWGMEPAGEF-UHFFFAOYSA-N 0.000 claims description 4
• KLNYWORCDSBKLN-UHFFFAOYSA-N 1-[4-[4-[(4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(N2CCCCC2)=C(C=CN2)C2=N1 KLNYWORCDSBKLN-UHFFFAOYSA-N 0.000 claims description 4
• XQNOAAQTRVPEJY-UHFFFAOYSA-N 1-[4-[4-[(4-pyrrolidin-1-yl-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(N2CCCC2)=C(C=CN2)C2=N1 XQNOAAQTRVPEJY-UHFFFAOYSA-N 0.000 claims description 4
• IMBSTVSBJXHUBW-SFHVURJKSA-N 1-[4-[4-[[4-[(3s)-3-hydroxypyrrolidin-1-yl]-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(N2C[C@@H](O)CC2)=C(C=CN2)C2=N1 IMBSTVSBJXHUBW-SFHVURJKSA-N 0.000 claims description 4
• UTOCZLMILKVPEA-UHFFFAOYSA-N 1-[4-[4-[[4-[2-(aminomethyl)piperidin-1-yl]-5-fluoropyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(F)C(N2C(CCCC2)CN)=N1 UTOCZLMILKVPEA-UHFFFAOYSA-N 0.000 claims description 4
• NSCXCHDGMQTJCY-UHFFFAOYSA-N 1-[4-[4-[[4-[4-(aminomethyl)piperidin-1-yl]-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(N2CCC(CN)CC2)=C(C=CN2)C2=N1 NSCXCHDGMQTJCY-UHFFFAOYSA-N 0.000 claims description 4
• IFHNDWIKIZOFSN-UHFFFAOYSA-N 1-[4-[4-[[6-[4-(aminomethyl)piperidin-1-yl]-7h-purin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(N2CCC(CN)CC2)=C(N=CN2)C2=N1 IFHNDWIKIZOFSN-UHFFFAOYSA-N 0.000 claims description 4
• QNDRJTWJOGGLGW-UHFFFAOYSA-N 1-[5-fluoro-2-(1h-indazol-6-ylamino)pyrimidin-4-yl]piperidine-3-carboxamide Chemical compound C1C(C(=O)N)CCCN1C1=NC(NC=2C=C3NN=CC3=CC=2)=NC=C1F QNDRJTWJOGGLGW-UHFFFAOYSA-N 0.000 claims description 4
• VMVVFAMYFKESAL-UHFFFAOYSA-N 2-[4-(4-acetylpiperazin-1-yl)anilino]-4-[4-(aminomethyl)piperidin-1-yl]pyrimidine-5-carboxamide Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(C(N)=O)C(N2CCC(CN)CC2)=N1 VMVVFAMYFKESAL-UHFFFAOYSA-N 0.000 claims description 4
• IOKYKLYLSOUELK-UHFFFAOYSA-N 2-n-(1h-indazol-6-yl)-4-n-methyl-5-pyridin-4-yl-7h-pyrrolo[2,3-d]pyrimidine-2,4-diamine Chemical compound C1=2C(NC)=NC(NC=3C=C4NN=CC4=CC=3)=NC=2NC=C1C1=CC=NC=C1 IOKYKLYLSOUELK-UHFFFAOYSA-N 0.000 claims description 4
• AIOJJUROCPYRGY-UHFFFAOYSA-N 4-[4-(aminomethyl)piperidin-1-yl]-n-(4-piperazin-1-ylphenyl)-7h-pyrrolo[2,3-d]pyrimidin-2-amine Chemical compound C1CC(CN)CCN1C1=NC(NC=2C=CC(=CC=2)N2CCNCC2)=NC2=C1C=CN2 AIOJJUROCPYRGY-UHFFFAOYSA-N 0.000 claims description 4
• WKIQOCLSDNSELN-UHFFFAOYSA-N 4-[[4-[4-(aminomethyl)piperidin-1-yl]-5-fluoropyrimidin-2-yl]amino]benzamide Chemical compound C1CC(CN)CCN1C1=NC(NC=2C=CC(=CC=2)C(N)=O)=NC=C1F WKIQOCLSDNSELN-UHFFFAOYSA-N 0.000 claims description 4
• CJZAKNKOVZAWIW-UHFFFAOYSA-N 6-[[4-[4-(aminomethyl)piperidin-1-yl]-5-fluoropyrimidin-2-yl]amino]-3,4-dihydro-1h-quinolin-2-one Chemical compound C1CC(CN)CCN1C1=NC(NC=2C=C3CCC(=O)NC3=CC=2)=NC=C1F CJZAKNKOVZAWIW-UHFFFAOYSA-N 0.000 claims description 4
• KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims description 4
• 108010016797 Sickle Hemoglobin Proteins 0.000 claims description 4
• 208000002903 Thalassemia Diseases 0.000 claims description 4
• 208000035868 Vascular inflammations Diseases 0.000 claims description 4
• 208000007475 hemolytic anemia Diseases 0.000 claims description 4
• XZZALAYXCNVFOZ-UHFFFAOYSA-N methyl n-[4-[[4-(cyclobutylamino)-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]-n-methylcarbamate Chemical compound C1=CC(N(C)C(=O)OC)=CC=C1NC1=NC(NC2CCC2)=C(C=CN2)C2=N1 XZZALAYXCNVFOZ-UHFFFAOYSA-N 0.000 claims description 4
• RTPBRAGXGHSNGI-UHFFFAOYSA-N n-(4-piperazin-1-ylphenyl)-4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidin-2-amine Chemical compound C1CCCCN1C1=NC(NC=2C=CC(=CC=2)N2CCNCC2)=NC2=C1C=CN2 RTPBRAGXGHSNGI-UHFFFAOYSA-N 0.000 claims description 4
• LGSSRXTZRZRCGP-UHFFFAOYSA-N n-(4-piperazin-1-ylphenyl)-4-pyrrolidin-1-yl-7h-pyrrolo[2,3-d]pyrimidin-2-amine Chemical compound C1CCCN1C1=NC(NC=2C=CC(=CC=2)N2CCNCC2)=NC2=C1C=CN2 LGSSRXTZRZRCGP-UHFFFAOYSA-N 0.000 claims description 4
• HQXXUQWPFMATCL-UHFFFAOYSA-N n-[4-[2-(aminomethyl)piperidin-1-yl]-5-fluoropyrimidin-2-yl]-1h-indazol-6-amine Chemical compound NCC1CCCCN1C1=NC(NC=2C=C3NN=CC3=CC=2)=NC=C1F HQXXUQWPFMATCL-UHFFFAOYSA-N 0.000 claims description 4
• LUQJBQPCCBQITJ-UHFFFAOYSA-N n-[4-[4-(aminomethyl)piperidin-1-yl]-5-fluoropyrimidin-2-yl]-1h-indazol-6-amine Chemical compound C1CC(CN)CCN1C1=NC(NC=2C=C3NN=CC3=CC=2)=NC=C1F LUQJBQPCCBQITJ-UHFFFAOYSA-N 0.000 claims description 4
• SMQOSQSCUMJLTB-UHFFFAOYSA-N n-[4-[[4-[4-(aminomethyl)piperidin-1-yl]-5-fluoropyrimidin-2-yl]amino]phenyl]-n-methylacetamide Chemical compound C1=CC(N(C(C)=O)C)=CC=C1NC1=NC=C(F)C(N2CCC(CN)CC2)=N1 SMQOSQSCUMJLTB-UHFFFAOYSA-N 0.000 claims description 4
• 125000004193 piperazinyl group Chemical group 0.000 claims description 4
• IKMBLWLVMKDJOW-UHFFFAOYSA-N tert-butyl n-[[1-[2-(4-carbamoylanilino)-5-fluoropyrimidin-4-yl]piperidin-4-yl]methyl]carbamate Chemical compound C1CC(CNC(=O)OC(C)(C)C)CCN1C1=NC(NC=2C=CC(=CC=2)C(N)=O)=NC=C1F IKMBLWLVMKDJOW-UHFFFAOYSA-N 0.000 claims description 4
• RJPFULDFMSGSPC-UHFFFAOYSA-N tert-butyl n-[[1-[2-[4-[acetyl(methyl)amino]anilino]-5-fluoropyrimidin-4-yl]piperidin-4-yl]methyl]carbamate Chemical compound C1=CC(N(C(C)=O)C)=CC=C1NC1=NC=C(F)C(N2CCC(CNC(=O)OC(C)(C)C)CC2)=N1 RJPFULDFMSGSPC-UHFFFAOYSA-N 0.000 claims description 4
• TWGVBXWKYXJGIH-UHFFFAOYSA-N tert-butyl n-[[1-[5-fluoro-2-(1h-indazol-6-ylamino)pyrimidin-4-yl]piperidin-2-yl]methyl]carbamate Chemical compound CC(C)(C)OC(=O)NCC1CCCCN1C1=NC(NC=2C=C3NN=CC3=CC=2)=NC=C1F TWGVBXWKYXJGIH-UHFFFAOYSA-N 0.000 claims description 4
• DSBLPCYZGDBXSG-UHFFFAOYSA-N 1-[2-(4-piperazin-1-ylanilino)-7h-pyrrolo[2,3-d]pyrimidin-4-yl]piperidine-4-carboxamide Chemical compound C1CC(C(=O)N)CCN1C1=NC(NC=2C=CC(=CC=2)N2CCNCC2)=NC2=C1C=CN2 DSBLPCYZGDBXSG-UHFFFAOYSA-N 0.000 claims description 3
• AMHCKXVMDFGYGX-UHFFFAOYSA-N 1-[4-[4-[[4-[4-(aminomethyl)piperidin-1-yl]-5-fluoropyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(F)C(N2CCC(CN)CC2)=N1 AMHCKXVMDFGYGX-UHFFFAOYSA-N 0.000 claims description 3
• FPDOGAOCLXKEHW-UHFFFAOYSA-O 2-[3-(4-aminophenyl)imidazol-1-ium-1-yl]-4-(cyclopropylamino)pyrimidine-5-carboxamide Chemical compound NC(=O)C1=CN=C([N+]2=CN(C=C2)C=2C=CC(N)=CC=2)N=C1NC1CC1 FPDOGAOCLXKEHW-UHFFFAOYSA-O 0.000 claims description 3
• LDBJYWUOPXAMJZ-UHFFFAOYSA-O 2-[4-(4-aminophenyl)pyridin-1-ium-1-yl]-4-(cyclopropylamino)pyrimidine-5-carboxamide Chemical compound NC(=O)C1=CN=C([N+]=2C=CC(=CC=2)C=2C=CC(N)=CC=2)N=C1NC1CC1 LDBJYWUOPXAMJZ-UHFFFAOYSA-O 0.000 claims description 3
• YLMFCAFPWOCZSU-UHFFFAOYSA-N 2-n-(1h-indazol-6-yl)-4-n-methyl-5-pyridin-3-yl-7h-pyrrolo[2,3-d]pyrimidine-2,4-diamine Chemical compound C1=2C(NC)=NC(NC=3C=C4NN=CC4=CC=3)=NC=2NC=C1C1=CC=CN=C1 YLMFCAFPWOCZSU-UHFFFAOYSA-N 0.000 claims description 3
• WSHBDAVXQWKPGV-UHFFFAOYSA-N 4-[4-(aminomethyl)piperidin-1-yl]-5-fluoro-n-(3,4,5-trimethoxyphenyl)pyrimidin-2-amine Chemical compound COC1=C(OC)C(OC)=CC(NC=2N=C(C(F)=CN=2)N2CCC(CN)CC2)=C1 WSHBDAVXQWKPGV-UHFFFAOYSA-N 0.000 claims description 3
• HWSABLWOHJZHQB-UHFFFAOYSA-N 4-[[4-[4-(aminomethyl)piperidin-1-yl]-5-fluoropyrimidin-2-yl]amino]benzenesulfonamide Chemical compound C1CC(CN)CCN1C1=NC(NC=2C=CC(=CC=2)S(N)(=O)=O)=NC=C1F HWSABLWOHJZHQB-UHFFFAOYSA-N 0.000 claims description 3
• 208000014767 Myeloproliferative disease Diseases 0.000 claims description 3
• 125000005100 aryl amino carbonyl group Chemical group 0.000 claims description 3
• 208000020832 chronic kidney disease Diseases 0.000 claims description 3
• 208000028208 end stage renal disease Diseases 0.000 claims description 3
• 201000000523 end stage renal failure Diseases 0.000 claims description 3
• 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 3
• 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 3
• DTZXUJSOKGXUCS-CYBMUJFWSA-N (2r)-2-[[2-(4-piperazin-1-ylanilino)-7h-pyrrolo[2,3-d]pyrimidin-4-yl]amino]propan-1-ol Chemical compound N=1C=2NC=CC=2C(N[C@@H](CO)C)=NC=1NC(C=C1)=CC=C1N1CCNCC1 DTZXUJSOKGXUCS-CYBMUJFWSA-N 0.000 claims description 2
• KJACBIQVKKDJCK-KRWDZBQOSA-N (2s)-1-[4-[[4-[2-(2-aminoethoxy)ethylamino]-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]pyrrolidine-2-carboxamide Chemical compound N=1C=2NC=CC=2C(NCCOCCN)=NC=1NC(C=C1)=CC=C1N1CCC[C@H]1C(N)=O KJACBIQVKKDJCK-KRWDZBQOSA-N 0.000 claims description 2
• DTZXUJSOKGXUCS-ZDUSSCGKSA-N (2s)-2-[[2-(4-piperazin-1-ylanilino)-7h-pyrrolo[2,3-d]pyrimidin-4-yl]amino]propan-1-ol Chemical compound N=1C=2NC=CC=2C(N[C@H](CO)C)=NC=1NC(C=C1)=CC=C1N1CCNCC1 DTZXUJSOKGXUCS-ZDUSSCGKSA-N 0.000 claims description 2
• 125000006636 (C3-C8) cycloalkylcarbonyl group Chemical group 0.000 claims description 2
• FQUYSHZXSKYCSY-UHFFFAOYSA-N 1,4-diazepane Chemical group C1CNCCNC1 FQUYSHZXSKYCSY-UHFFFAOYSA-N 0.000 claims description 2
• SJPPNZACXQFMNM-UHFFFAOYSA-N 1-[2-[4-(4-acetylpiperazin-1-yl)anilino]-7h-purin-6-yl]piperidine-3-carboxamide Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(N2CC(CCC2)C(N)=O)=C(N=CN2)C2=N1 SJPPNZACXQFMNM-UHFFFAOYSA-N 0.000 claims description 2
• QKXBGQYQXGMLCG-UHFFFAOYSA-N 1-[2-[4-(4-acetylpiperazin-1-yl)anilino]-7h-purin-6-yl]piperidine-3-carboxylic acid Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(N2CC(CCC2)C(O)=O)=C(N=CN2)C2=N1 QKXBGQYQXGMLCG-UHFFFAOYSA-N 0.000 claims description 2
• XNQDTXPMUWEHIU-UHFFFAOYSA-N 1-[4-(cyclopropylamino)-2-(1h-indazol-6-ylamino)-7h-pyrrolo[2,3-d]pyrimidin-5-yl]ethanone Chemical compound C=12C(C(=O)C)=CNC2=NC(NC=2C=C3NN=CC3=CC=2)=NC=1NC1CC1 XNQDTXPMUWEHIU-UHFFFAOYSA-N 0.000 claims description 2
• YPPGEPDDWNRUCU-UHFFFAOYSA-N 1-[4-[4-[(5-fluoro-4-piperazin-1-ylpyrimidin-2-yl)amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(F)C(N2CCNCC2)=N1 YPPGEPDDWNRUCU-UHFFFAOYSA-N 0.000 claims description 2
• UTBMAXNCUMKDHF-UHFFFAOYSA-N 1-[4-[4-[[4-(2-methoxyethylamino)-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound N=1C=2NC=CC=2C(NCCOC)=NC=1NC(C=C1)=CC=C1N1CCN(C(C)=O)CC1 UTBMAXNCUMKDHF-UHFFFAOYSA-N 0.000 claims description 2
• PRVQGVFQRVRVNF-UHFFFAOYSA-N 1-[4-[4-[[4-(4-aminopiperidin-1-yl)-5-fluoropyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(F)C(N2CCC(N)CC2)=N1 PRVQGVFQRVRVNF-UHFFFAOYSA-N 0.000 claims description 2
• ZNOASPNIGDFOQH-UHFFFAOYSA-N 1-[4-[4-[[4-(cyclopropylamino)-5-pyridin-4-yl-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(NC2CC2)=C(C(=CN2)C=3C=CN=CC=3)C2=N1 ZNOASPNIGDFOQH-UHFFFAOYSA-N 0.000 claims description 2
• PSFSHWDADXKQTD-UHFFFAOYSA-N 1-[4-[4-[[4-(methylamino)-5-pyridin-4-yl-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound N=1C=2NC=C(C=3C=CN=CC=3)C=2C(NC)=NC=1NC(C=C1)=CC=C1N1CCN(C(C)=O)CC1 PSFSHWDADXKQTD-UHFFFAOYSA-N 0.000 claims description 2
• XJTYNCJATWFGOR-UHFFFAOYSA-N 1-[4-[4-[[4-(piperidin-4-ylmethylamino)-5-pyridin-4-yl-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(NCC2CCNCC2)=C(C(=CN2)C=3C=CN=CC=3)C2=N1 XJTYNCJATWFGOR-UHFFFAOYSA-N 0.000 claims description 2
• MFSDUZLYAOQMHU-KRWDZBQOSA-N 1-[4-[4-[[4-[(3s)-3-aminopiperidin-1-yl]-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(N2C[C@@H](N)CCC2)=C(C=CN2)C2=N1 MFSDUZLYAOQMHU-KRWDZBQOSA-N 0.000 claims description 2
• PFQZSZKQBYZRGW-UHFFFAOYSA-N 1-[4-[4-[[4-[(4-aminocyclohexyl)amino]-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(NC2CCC(N)CC2)=C(C=CN2)C2=N1 PFQZSZKQBYZRGW-UHFFFAOYSA-N 0.000 claims description 2
• AXPRUMVDNQHMHM-UHFFFAOYSA-N 1-[4-[4-[[4-[4-(aminomethyl)piperidin-1-yl]-5-chloropyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(Cl)C(N2CCC(CN)CC2)=N1 AXPRUMVDNQHMHM-UHFFFAOYSA-N 0.000 claims description 2
• WVGLLIMUMJTKGE-CQSZACIVSA-N 1-[4-[4-[[4-[[(2r)-1-hydroxypropan-2-yl]amino]-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound N=1C=2NC=CC=2C(N[C@@H](CO)C)=NC=1NC(C=C1)=CC=C1N1CCN(C(C)=O)CC1 WVGLLIMUMJTKGE-CQSZACIVSA-N 0.000 claims description 2
• KCWJGNYVKTXHCU-UHFFFAOYSA-N 1-[4-[4-[[5-fluoro-4-[4-(hydroxymethyl)piperidin-1-yl]pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(F)C(N2CCC(CO)CC2)=N1 KCWJGNYVKTXHCU-UHFFFAOYSA-N 0.000 claims description 2
• JTHRAEIOHKMUAR-UHFFFAOYSA-N 1-[4-[[4-(cyclobutylamino)-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]piperidin-4-ol Chemical compound C1CC(O)CCN1C(C=C1)=CC=C1NC1=NC(NC2CCC2)=C(C=CN2)C2=N1 JTHRAEIOHKMUAR-UHFFFAOYSA-N 0.000 claims description 2
• DHKNMIIKOXMEOH-UHFFFAOYSA-N 1-[4-[[4-(cyclobutylamino)-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]sulfonylpiperidin-4-ol Chemical compound C1CC(O)CCN1S(=O)(=O)C(C=C1)=CC=C1NC1=NC(NC2CCC2)=C(C=CN2)C2=N1 DHKNMIIKOXMEOH-UHFFFAOYSA-N 0.000 claims description 2
• BCARHLFFBREYNY-UHFFFAOYSA-N 2-(6-amino-7-chloroindazol-1-yl)-4-(cyclopropylamino)pyrimidine-5-carboxamide Chemical compound NC(=O)C1=CN=C(N2C3=C(Cl)C(N)=CC=C3C=N2)N=C1NC1CC1 BCARHLFFBREYNY-UHFFFAOYSA-N 0.000 claims description 2
• ZBEZUCCTWJQKCZ-UHFFFAOYSA-N 2-[1-[2-[(2-oxo-3,4-dihydro-1h-quinolin-6-yl)amino]-7h-pyrrolo[2,3-d]pyrimidin-4-yl]piperidin-4-yl]acetamide Chemical compound C1CC(CC(=O)N)CCN1C1=NC(NC=2C=C3CCC(=O)NC3=CC=2)=NC2=C1C=CN2 ZBEZUCCTWJQKCZ-UHFFFAOYSA-N 0.000 claims description 2
• WIQRWQXZZNVZFL-UHFFFAOYSA-N 2-[1-[2-[(2-oxo-3,4-dihydro-1h-quinolin-6-yl)amino]-7h-pyrrolo[2,3-d]pyrimidin-4-yl]piperidin-4-yl]acetic acid Chemical compound C1CC(CC(=O)O)CCN1C1=NC(NC=2C=C3CCC(=O)NC3=CC=2)=NC2=C1C=CN2 WIQRWQXZZNVZFL-UHFFFAOYSA-N 0.000 claims description 2
• OUNCMUFBHHDXDZ-UHFFFAOYSA-N 2-[1-[2-[4-(4-acetylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]piperidin-4-yl]acetamide Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(F)C(N2CCC(CC(N)=O)CC2)=N1 OUNCMUFBHHDXDZ-UHFFFAOYSA-N 0.000 claims description 2
• RUXYFSXSLVMGLX-UHFFFAOYSA-N 2-[2-(1h-indazol-6-yl)hydrazinyl]-n-(1h-pyrazol-5-yl)-7h-pyrrolo[2,3-d]pyrimidin-4-amine Chemical compound C=1C=C2C=NNC2=CC=1NNC(N=C1NC=CC1=1)=NC=1NC1=CC=NN1 RUXYFSXSLVMGLX-UHFFFAOYSA-N 0.000 claims description 2
• DAXRFYNBHYORGQ-UHFFFAOYSA-N 2-[2-(1h-indazol-6-yl)hydrazinyl]-n-(2-methoxyethyl)-7h-pyrrolo[2,3-d]pyrimidin-4-amine Chemical compound C1=C2C=NNC2=CC(NNC=2N=C(C=3C=CNC=3N=2)NCCOC)=C1 DAXRFYNBHYORGQ-UHFFFAOYSA-N 0.000 claims description 2
• INHNRAOOPAMPNA-UHFFFAOYSA-N 2-[4-(4-acetylpiperazin-1-yl)anilino]-4-(cyclopropylamino)-7h-pyrrolo[2,3-d]pyrimidine-5-carbonitrile Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(NC2CC2)=C(C(=CN2)C#N)C2=N1 INHNRAOOPAMPNA-UHFFFAOYSA-N 0.000 claims description 2
• YZAMAONAYMDYCQ-UHFFFAOYSA-N 2-[4-(4-acetylpiperazin-1-yl)anilino]-4-(piperidin-4-ylmethylamino)-7h-pyrrolo[2,3-d]pyrimidine-5-carbonitrile Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(NCC2CCNCC2)=C(C(=CN2)C#N)C2=N1 YZAMAONAYMDYCQ-UHFFFAOYSA-N 0.000 claims description 2
• BJDUWZPFQALELV-UHFFFAOYSA-N 2-[4-(4-acetylpiperazin-1-yl)anilino]-4-[2-(2-hydroxyethyl)piperidin-1-yl]pyrimidine-5-carboxamide Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(C(N)=O)C(N2C(CCCC2)CCO)=N1 BJDUWZPFQALELV-UHFFFAOYSA-N 0.000 claims description 2
• JZHKSVWZKLSVCP-UHFFFAOYSA-N 2-[4-(4-acetylpiperazin-1-yl)anilino]-4-[4-(2-hydroxyethyl)-1,4-diazepan-1-yl]pyrimidine-5-carboxamide Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(C(N)=O)C(N2CCN(CCO)CCC2)=N1 JZHKSVWZKLSVCP-UHFFFAOYSA-N 0.000 claims description 2
• HUQPDXIUYNLBPK-UHFFFAOYSA-N 2-[4-(4-acetylpiperazin-1-yl)anilino]-4-[4-[(carbamoylamino)methyl]piperidin-1-yl]pyrimidine-5-carboxamide Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(C(N)=O)C(N2CCC(CNC(N)=O)CC2)=N1 HUQPDXIUYNLBPK-UHFFFAOYSA-N 0.000 claims description 2
• LBRXDVLOQBLRLS-UHFFFAOYSA-N 2-[6-[[4-(cyclobutylamino)-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-2-oxo-3,4-dihydroquinolin-1-yl]-n-[2-(dimethylamino)ethyl]acetamide Chemical compound C=1C=C2N(CC(=O)NCCN(C)C)C(=O)CCC2=CC=1NC(N=C1NC=CC1=1)=NC=1NC1CCC1 LBRXDVLOQBLRLS-UHFFFAOYSA-N 0.000 claims description 2
• DNXQUONSOHUEFK-UHFFFAOYSA-N 2-[6-[[4-(cyclobutylamino)-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-2-oxo-3,4-dihydroquinolin-1-yl]acetic acid Chemical compound C=1C=C2N(CC(=O)O)C(=O)CCC2=CC=1NC(N=C1NC=CC1=1)=NC=1NC1CCC1 DNXQUONSOHUEFK-UHFFFAOYSA-N 0.000 claims description 2
• MFSCCROVLRTUIZ-UHFFFAOYSA-N 2-[[2-(1h-indazol-6-ylamino)-7h-pyrrolo[2,3-d]pyrimidin-4-yl]amino]acetamide Chemical compound C1=C2C=NNC2=CC(NC=2N=C(C=3C=CNC=3N=2)NCC(=O)N)=C1 MFSCCROVLRTUIZ-UHFFFAOYSA-N 0.000 claims description 2
• IJXFJCXEFCZUHQ-UHFFFAOYSA-N 2-[[2-[2-(1h-indazol-6-yl)hydrazinyl]-7h-pyrrolo[2,3-d]pyrimidin-4-yl]amino]ethanol Chemical compound C1=C2C=NNC2=CC(NNC=2N=C(C=3C=CNC=3N=2)NCCO)=C1 IJXFJCXEFCZUHQ-UHFFFAOYSA-N 0.000 claims description 2
• MWRMPCHAICBCFB-UHFFFAOYSA-N 2-[[4-[[4-(cyclobutylamino)-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]sulfonyl-methylamino]acetic acid Chemical compound C1=CC(S(=O)(=O)N(CC(O)=O)C)=CC=C1NC1=NC(NC2CCC2)=C(C=CN2)C2=N1 MWRMPCHAICBCFB-UHFFFAOYSA-N 0.000 claims description 2
• BCBKSVRFPODRJE-UHFFFAOYSA-N 2-[[4-[[4-(cyclobutylamino)-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]sulfonylamino]acetamide Chemical compound C1=CC(S(=O)(=O)NCC(=O)N)=CC=C1NC1=NC(NC2CCC2)=C(C=CN2)C2=N1 BCBKSVRFPODRJE-UHFFFAOYSA-N 0.000 claims description 2
• LYUSDPQLOXYNQI-UHFFFAOYSA-N 2-n-(1h-indazol-6-yl)-4-n-(3-morpholin-4-ylpropyl)-7h-pyrrolo[2,3-d]pyrimidine-2,4-diamine Chemical compound N=1C(NC=2C=C3NN=CC3=CC=2)=NC=2NC=CC=2C=1NCCCN1CCOCC1 LYUSDPQLOXYNQI-UHFFFAOYSA-N 0.000 claims description 2
• ZILHMIGQJBOTJU-UHFFFAOYSA-N 2-n-(1h-indazol-6-yl)-4-n-piperidin-4-yl-7h-pyrrolo[2,3-d]pyrimidine-2,4-diamine Chemical compound C1CNCCC1NC1=NC(NC=2C=C3NN=CC3=CC=2)=NC2=C1C=CN2 ZILHMIGQJBOTJU-UHFFFAOYSA-N 0.000 claims description 2
• XHIDLBPGINEBMS-UHFFFAOYSA-N 2-n-(1h-indazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidine-2,4-diamine Chemical compound C1=C2C=NNC2=CC(NC=2N=C(C=3C=CNC=3N=2)N)=C1 XHIDLBPGINEBMS-UHFFFAOYSA-N 0.000 claims description 2
• KHILDJMDZDCFIM-UHFFFAOYSA-N 3-[4-[2-[4-(4-acetylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]piperazin-1-yl]-3-oxopropanenitrile Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(F)C(N2CCN(CC2)C(=O)CC#N)=N1 KHILDJMDZDCFIM-UHFFFAOYSA-N 0.000 claims description 2
• SWSXBKTUJLNCGY-UHFFFAOYSA-N 3-[[2-(4-piperazin-1-ylanilino)-7h-pyrrolo[2,3-d]pyrimidin-4-yl]amino]benzamide Chemical compound NC(=O)C1=CC=CC(NC=2C=3C=CNC=3N=C(NC=3C=CC(=CC=3)N3CCNCC3)N=2)=C1 SWSXBKTUJLNCGY-UHFFFAOYSA-N 0.000 claims description 2
• RELRBBLHABEMQR-UHFFFAOYSA-N 3-[[2-(4-piperazin-1-ylanilino)-7h-pyrrolo[2,3-d]pyrimidin-4-yl]amino]benzenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CC(NC=2C=3C=CNC=3N=C(NC=3C=CC(=CC=3)N3CCNCC3)N=2)=C1 RELRBBLHABEMQR-UHFFFAOYSA-N 0.000 claims description 2
• XRPNJXNZMNEFBT-UHFFFAOYSA-N 3-[[2-[4-(4-acetylpiperazin-1-yl)anilino]-7h-pyrrolo[2,3-d]pyrimidin-4-yl]amino]benzamide Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC(NC=2C=C(C=CC=2)C(N)=O)=C(C=CN2)C2=N1 XRPNJXNZMNEFBT-UHFFFAOYSA-N 0.000 claims description 2
• IZFWMBQWJLCGRI-UHFFFAOYSA-N 4-(benzylamino)-2-[(1-methyl-2-oxo-3,4-dihydroquinolin-6-yl)amino]-7h-pyrrolo[2,3-d]pyrimidine-5-carbonitrile Chemical compound C=1C=C2N(C)C(=O)CCC2=CC=1NC(N=C1NC=C(C1=1)C#N)=NC=1NCC1=CC=CC=C1 IZFWMBQWJLCGRI-UHFFFAOYSA-N 0.000 claims description 2
• MQBFQWRJAMUKER-UHFFFAOYSA-N 4-(cyclobutylamino)-2-(1h-indazol-6-ylamino)-6,7-dihydropyrrolo[2,3-d]pyrimidin-5-one Chemical compound C=12C(=O)CNC2=NC(NC=2C=C3NN=CC3=CC=2)=NC=1NC1CCC1 MQBFQWRJAMUKER-UHFFFAOYSA-N 0.000 claims description 2
• FKBFTAHPPHQKHW-UHFFFAOYSA-N 4-(cyclopropylamino)-2-(1h-indazol-6-ylamino)-7h-pyrrolo[2,3-d]pyrimidine-5-carbonitrile Chemical compound C=12C(C#N)=CNC2=NC(NC=2C=C3NN=CC3=CC=2)=NC=1NC1CC1 FKBFTAHPPHQKHW-UHFFFAOYSA-N 0.000 claims description 2
• DWLXOZFJWNKMTA-UHFFFAOYSA-N 4-(cyclopropylamino)-2-[(2-oxo-3,4-dihydro-1h-quinolin-6-yl)amino]-7h-pyrrolo[2,3-d]pyrimidine-5-carbonitrile Chemical compound C=1C=C2NC(=O)CCC2=CC=1NC(N=C1NC=C(C1=1)C#N)=NC=1NC1CC1 DWLXOZFJWNKMTA-UHFFFAOYSA-N 0.000 claims description 2
• LQUFEFDXJHVJER-UHFFFAOYSA-N 4-(cyclopropylamino)-2-[(2-oxo-3,4-dihydro-1h-quinolin-6-yl)amino]-7h-pyrrolo[2,3-d]pyrimidine-5-carboxamide Chemical compound C=12C(C(=O)N)=CNC2=NC(NC=2C=C3CCC(=O)NC3=CC=2)=NC=1NC1CC1 LQUFEFDXJHVJER-UHFFFAOYSA-N 0.000 claims description 2
• BYAABDGMFIJTGO-ZDUSSCGKSA-N 4-[(2s)-2-(aminomethyl)pyrrolidin-1-yl]-n-(1h-indazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-amine Chemical compound NC[C@@H]1CCCN1C1=NC(NC=2C=C3NN=CC3=CC=2)=NC2=C1C=CN2 BYAABDGMFIJTGO-ZDUSSCGKSA-N 0.000 claims description 2
• LOZSNQHTJGMXGM-LBPRGKRZSA-N 4-[(3s)-3-aminopiperidin-1-yl]-n-(1h-indazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-amine Chemical compound C1[C@@H](N)CCCN1C1=NC(NC=2C=C3NN=CC3=CC=2)=NC2=C1C=CN2 LOZSNQHTJGMXGM-LBPRGKRZSA-N 0.000 claims description 2
• VHWAWQGJURZMQB-UHFFFAOYSA-N 4-[(4-amino-5-pyridin-4-yl-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino]benzoic acid Chemical compound N=1C=2NC=C(C=3C=CN=CC=3)C=2C(N)=NC=1NC1=CC=C(C(O)=O)C=C1 VHWAWQGJURZMQB-UHFFFAOYSA-N 0.000 claims description 2
• WICMQZFDKXYPCK-UHFFFAOYSA-N 4-[2-[4-(4-acetylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]piperazine-1-carboxamide Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1NC1=NC=C(F)C(N2CCN(CC2)C(N)=O)=N1 WICMQZFDKXYPCK-UHFFFAOYSA-N 0.000 claims description 2
• NQYHQKSIEQVZFT-UHFFFAOYSA-N 4-[[4-(cyclopropylamino)-5-pyridin-4-yl-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]benzamide Chemical compound C1=CC(C(=O)N)=CC=C1NC1=NC(NC2CC2)=C(C(=CN2)C=3C=CN=CC=3)C2=N1 NQYHQKSIEQVZFT-UHFFFAOYSA-N 0.000 claims description 2
• FJZSYCRTFSDIJP-UHFFFAOYSA-N 4-[[4-[4-(aminomethyl)piperidin-1-yl]-5-fluoropyrimidin-2-yl]amino]benzoic acid Chemical compound C1CC(CN)CCN1C1=NC(NC=2C=CC(=CC=2)C(O)=O)=NC=C1F FJZSYCRTFSDIJP-UHFFFAOYSA-N 0.000 claims description 2
• VLFNWZFPKCQGCX-UHFFFAOYSA-N 4-[[4-[4-[(dimethylamino)methyl]piperidin-1-yl]-5-fluoropyrimidin-2-yl]amino]benzamide Chemical compound C1CC(CN(C)C)CCN1C1=NC(NC=2C=CC(=CC=2)C(N)=O)=NC=C1F VLFNWZFPKCQGCX-UHFFFAOYSA-N 0.000 claims description 2
• CFUQUMNDXZYNSK-UHFFFAOYSA-N 4-[[4-[[1-(2-cyanoacetyl)piperidin-3-yl]amino]-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]benzamide Chemical compound C1=CC(C(=O)N)=CC=C1NC1=NC(NC2CN(CCC2)C(=O)CC#N)=C(C=CN2)C2=N1 CFUQUMNDXZYNSK-UHFFFAOYSA-N 0.000 claims description 2
• SBDWLPPYBIFYSR-UHFFFAOYSA-N 4-[[4-[[1-(2-cyanoacetyl)piperidin-4-yl]amino]-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]benzamide Chemical compound C1=CC(C(=O)N)=CC=C1NC1=NC(NC2CCN(CC2)C(=O)CC#N)=C(C=CN2)C2=N1 SBDWLPPYBIFYSR-UHFFFAOYSA-N 0.000 claims description 2
• BEUOVQXMNPBPSS-UHFFFAOYSA-N 4-[[5-cyano-4-(cyclopropylamino)-7h-pyrrolo[2,3-d]pyrimidin-2-yl]amino]benzamide Chemical compound C1=CC(C(=O)N)=CC=C1NC1=NC(NC2CC2)=C(C(=CN2)C#N)C2=N1 BEUOVQXMNPBPSS-UHFFFAOYSA-N 0.000 claims description 2
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