CA2700988A1 - Inhibiteurs de la rho kinase - Google Patents

Inhibiteurs de la rho kinase Download PDF

Info

Publication number: CA2700988A1
Authority: CA; Canada
Prior art keywords: alkyl; independently selected; hydroxy; halo; amino
Prior art date: 2006-09-27
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

Application number

CA2700988A

Other languages

English (en)

Inventor

Alessandra Bartolozzi

Stewart Campbell

Bridget Cole

James Ellis

Hope Foudoulakis

Brian Kirk

Siya Ram

Paul Sweetnam

Martin Hauer-Jensen

Marjan Boerma

Junru Wang

Qiang Fu

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Surface Logix Inc

Original Assignee

Individual

Priority date (The priority date 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 date listed.)

2006-09-27

Filing date

2007-09-27

Publication date

2008-05-08

2007-09-27 Application filed by Individual filed Critical Individual

2008-05-08 Publication of CA2700988A1 publication Critical patent/CA2700988A1/fr

Status Abandoned legal-status Critical Current

Links

239000003590 rho kinase inhibitor Substances 0.000 title 1
150000001875 compounds Chemical class 0.000 claims abstract 28
238000000034 method Methods 0.000 claims abstract 17
239000003112 inhibitor Substances 0.000 claims abstract 9
101000669921 Homo sapiens Rho-associated protein kinase 2 Proteins 0.000 claims abstract 5
102100039314 Rho-associated protein kinase 2 Human genes 0.000 claims abstract 5
229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims abstract 3
-1 hydroxy, amino Chemical group 0.000 claims 310
125000005843 halogen group Chemical group 0.000 claims 176
125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 150
125000004093 cyano group Chemical group *C#N 0.000 claims 150
125000001424 substituent group Chemical group 0.000 claims 150
125000005010 perfluoroalkyl group Chemical group 0.000 claims 143
125000005842 heteroatom Chemical group 0.000 claims 126
125000000623 heterocyclic group Chemical group 0.000 claims 125
125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 120
125000003342 alkenyl group Chemical group 0.000 claims 116
125000000753 cycloalkyl group Chemical group 0.000 claims 112
125000003118 aryl group Chemical group 0.000 claims 110
125000001072 heteroaryl group Chemical group 0.000 claims 94
125000003710 aryl alkyl group Chemical group 0.000 claims 83
125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 64
125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 53
125000000217 alkyl group Chemical group 0.000 claims 53
125000004043 oxo group Chemical group O=* 0.000 claims 53
125000004650 C1-C8 alkynyl group Chemical group 0.000 claims 32
125000003545 alkoxy group Chemical group 0.000 claims 26
125000002887 hydroxy group Chemical group [H]O* 0.000 claims 26
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 26
125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 20
150000003839 salts Chemical class 0.000 claims 20
229910052760 oxygen Inorganic materials 0.000 claims 15
125000004432 carbon atom Chemical group C* 0.000 claims 13
102100029077 3-hydroxy-3-methylglutaryl-coenzyme A reductase Human genes 0.000 claims 7
101710158485 3-hydroxy-3-methylglutaryl-coenzyme A reductase Proteins 0.000 claims 7
229940123934 Reductase inhibitor Drugs 0.000 claims 7
239000011435 rock Substances 0.000 claims 7
241000124008 Mammalia Species 0.000 claims 2
ZGGHKIMDNBDHJB-NRFPMOEYSA-M (3R,5S)-fluvastatin sodium Chemical compound [Na+].C12=CC=CC=C2N(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC([O-])=O)=C1C1=CC=C(F)C=C1 ZGGHKIMDNBDHJB-NRFPMOEYSA-M 0.000 claims 1
XOJFMGDJHFFTHY-UHFFFAOYSA-N 1-[2-(dimethylamino)ethyl]-3-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenyl]urea Chemical compound CN(C)CCNC(=O)NC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 XOJFMGDJHFFTHY-UHFFFAOYSA-N 0.000 claims 1
AIMAJNUGNPTGKD-UHFFFAOYSA-N 2-(3-fluoro-4-phenylphenyl)-n-(1h-indazol-5-yl)-7-methoxy-6-(2-pyrrolidin-1-ylethoxy)quinazolin-4-amine Chemical compound COC1=CC2=NC(C=3C=C(F)C(=CC=3)C=3C=CC=CC=3)=NC(NC=3C=C4C=NNC4=CC=3)=C2C=C1OCCN1CCCC1 AIMAJNUGNPTGKD-UHFFFAOYSA-N 0.000 claims 1
OWCSOONUBWZLEZ-UHFFFAOYSA-N 2-(3-fluoro-4-phenylphenyl)-n-(1h-indazol-5-yl)-7-methoxy-6-[2-(4-methylpiperazin-1-yl)ethoxy]quinazolin-4-amine Chemical compound COC1=CC2=NC(C=3C=C(F)C(=CC=3)C=3C=CC=CC=3)=NC(NC=3C=C4C=NNC4=CC=3)=C2C=C1OCCN1CCN(C)CC1 OWCSOONUBWZLEZ-UHFFFAOYSA-N 0.000 claims 1
YYVHDXMDAODPKY-UHFFFAOYSA-N 2-[2-[4-(1h-indazol-5-ylamino)-7-methoxy-2-(3-phenylphenyl)quinazolin-6-yl]oxyethyl-methylamino]-n,n-dimethylacetamide Chemical compound N=1C(NC=2C=C3C=NNC3=CC=2)=C2C=C(OCCN(C)CC(=O)N(C)C)C(OC)=CC2=NC=1C(C=1)=CC=CC=1C1=CC=CC=C1 YYVHDXMDAODPKY-UHFFFAOYSA-N 0.000 claims 1
OBUCKVXMPAONRB-UHFFFAOYSA-N 2-[3-[4-(1h-indazol-5-ylamino)-7-methoxy-6-(2-methoxyethoxy)quinazolin-2-yl]phenoxy]-n-propan-2-ylacetamide Chemical compound N1=C2C=C(OC)C(OCCOC)=CC2=C(NC=2C=C3C=NNC3=CC=2)N=C1C1=CC=CC(OCC(=O)NC(C)C)=C1 OBUCKVXMPAONRB-UHFFFAOYSA-N 0.000 claims 1
XPJNQJBUMWQHSU-UHFFFAOYSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-1-(4-methylpiperazin-1-yl)ethanone Chemical compound C1CN(C)CCN1C(=O)COC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 XPJNQJBUMWQHSU-UHFFFAOYSA-N 0.000 claims 1
KHAMJMLSXLNIBO-UHFFFAOYSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-1-morpholin-4-ylethanone Chemical compound C=1C=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=CC=1OCC(=O)N1CCOCC1 KHAMJMLSXLNIBO-UHFFFAOYSA-N 0.000 claims 1
HLHIWDZGVXGOLI-UHFFFAOYSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-1-piperidin-1-ylethanone Chemical compound C=1C=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=CC=1OCC(=O)N1CCCCC1 HLHIWDZGVXGOLI-UHFFFAOYSA-N 0.000 claims 1
DRAIYBWXGHOGHP-UHFFFAOYSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-n-(2,2,2-trifluoroethyl)acetamide Chemical compound FC(F)(F)CNC(=O)COC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 DRAIYBWXGHOGHP-UHFFFAOYSA-N 0.000 claims 1
WBNSLYAHQGEHEX-UHFFFAOYSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-n-(2-methoxyethyl)acetamide Chemical compound COCCNC(=O)COC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 WBNSLYAHQGEHEX-UHFFFAOYSA-N 0.000 claims 1
DDMFMKLSTFGJME-UHFFFAOYSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-n-(2-methylpropyl)acetamide Chemical compound CC(C)CNC(=O)COC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 DDMFMKLSTFGJME-UHFFFAOYSA-N 0.000 claims 1
JGWIJSLXUUPLIV-HXUWFJFHSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-n-[(3r)-pyrrolidin-3-yl]acetamide Chemical compound C=1C=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=CC=1OCC(=O)N[C@@H]1CCNC1 JGWIJSLXUUPLIV-HXUWFJFHSA-N 0.000 claims 1
JGWIJSLXUUPLIV-FQEVSTJZSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-n-[(3s)-pyrrolidin-3-yl]acetamide Chemical compound C=1C=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=CC=1OCC(=O)N[C@H]1CCNC1 JGWIJSLXUUPLIV-FQEVSTJZSA-N 0.000 claims 1
HDDMDXLJFJALKN-UHFFFAOYSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-n-methylacetamide Chemical compound CNC(=O)COC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 HDDMDXLJFJALKN-UHFFFAOYSA-N 0.000 claims 1
OIJMDJNPWMWIRN-UHFFFAOYSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-n-prop-2-ynylacetamide Chemical compound C#CCNC(=O)COC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 OIJMDJNPWMWIRN-UHFFFAOYSA-N 0.000 claims 1
GKHIVNAUVKXIIY-UHFFFAOYSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-n-propan-2-ylacetamide Chemical compound CC(C)NC(=O)COC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 GKHIVNAUVKXIIY-UHFFFAOYSA-N 0.000 claims 1
TWTKNUYGDKCAQH-UHFFFAOYSA-N 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-n-pyridin-3-ylacetamide Chemical compound C=1C=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=CC=1OCC(=O)NC1=CC=CN=C1 TWTKNUYGDKCAQH-UHFFFAOYSA-N 0.000 claims 1
NGIJYBMRWWVDQV-UHFFFAOYSA-N 2-[4-(1h-indazol-5-ylamino)-7-methoxy-2-(3-phenylphenyl)quinazolin-6-yl]oxy-1-(4-methylpiperazin-1-yl)ethanone Chemical compound COC1=CC2=NC(C=3C=C(C=CC=3)C=3C=CC=CC=3)=NC(NC=3C=C4C=NNC4=CC=3)=C2C=C1OCC(=O)N1CCN(C)CC1 NGIJYBMRWWVDQV-UHFFFAOYSA-N 0.000 claims 1
NOJGCQJRKNOXPV-UHFFFAOYSA-N 3-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenyl]-1,1-dimethylurea Chemical compound CN(C)C(=O)NC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 NOJGCQJRKNOXPV-UHFFFAOYSA-N 0.000 claims 1
UJKGFTWFIUTUOC-UHFFFAOYSA-N 6-[2-(dimethylamino)ethoxy]-n-(1h-indazol-5-yl)-7-methoxy-2-(3-phenylphenyl)quinazolin-4-amine Chemical compound N=1C(NC=2C=C3C=NNC3=CC=2)=C2C=C(OCCN(C)C)C(OC)=CC2=NC=1C(C=1)=CC=CC=1C1=CC=CC=C1 UJKGFTWFIUTUOC-UHFFFAOYSA-N 0.000 claims 1
XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 claims 1
XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 claims 1
208000024172 Cardiovascular disease Diseases 0.000 claims 1
206010073306 Exposure to radiation Diseases 0.000 claims 1
206010016654 Fibrosis Diseases 0.000 claims 1
206010061218 Inflammation Diseases 0.000 claims 1
PCZOHLXUXFIOCF-UHFFFAOYSA-N Monacolin X Natural products C12C(OC(=O)C(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 PCZOHLXUXFIOCF-UHFFFAOYSA-N 0.000 claims 1
TUZYXOIXSAXUGO-UHFFFAOYSA-N Pravastatin Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(O)C=C21 TUZYXOIXSAXUGO-UHFFFAOYSA-N 0.000 claims 1
RYMZZMVNJRMUDD-UHFFFAOYSA-N SJ000286063 Natural products C12C(OC(=O)C(C)(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 RYMZZMVNJRMUDD-UHFFFAOYSA-N 0.000 claims 1
AJLFOPYRIVGYMJ-UHFFFAOYSA-N SJ000287055 Natural products C12C(OC(=O)C(C)CC)CCC=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 AJLFOPYRIVGYMJ-UHFFFAOYSA-N 0.000 claims 1
125000000304 alkynyl group Chemical group 0.000 claims 1
229960005370 atorvastatin Drugs 0.000 claims 1
GPUADMRJQVPIAS-QCVDVZFFSA-M cerivastatin sodium Chemical compound [Na+].COCC1=C(C(C)C)N=C(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC([O-])=O)=C1C1=CC=C(F)C=C1 GPUADMRJQVPIAS-QCVDVZFFSA-M 0.000 claims 1
201000010099 disease Diseases 0.000 claims 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
230000004761 fibrosis Effects 0.000 claims 1
229960003765 fluvastatin Drugs 0.000 claims 1
230000004054 inflammatory process Effects 0.000 claims 1
230000005865 ionizing radiation Effects 0.000 claims 1
229960004844 lovastatin Drugs 0.000 claims 1
PCZOHLXUXFIOCF-BXMDZJJMSA-N lovastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 PCZOHLXUXFIOCF-BXMDZJJMSA-N 0.000 claims 1
QLJODMDSTUBWDW-UHFFFAOYSA-N lovastatin hydroxy acid Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(C)C=C21 QLJODMDSTUBWDW-UHFFFAOYSA-N 0.000 claims 1
FBIGUXNIHCMKNB-UHFFFAOYSA-N methyl 2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]anilino]-2-oxoacetate Chemical compound COC(=O)C(=O)NC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 FBIGUXNIHCMKNB-UHFFFAOYSA-N 0.000 claims 1
229950009116 mevastatin Drugs 0.000 claims 1
AJLFOPYRIVGYMJ-INTXDZFKSA-N mevastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=CCC[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 AJLFOPYRIVGYMJ-INTXDZFKSA-N 0.000 claims 1
BOZILQFLQYBIIY-UHFFFAOYSA-N mevastatin hydroxy acid Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CCC=C21 BOZILQFLQYBIIY-UHFFFAOYSA-N 0.000 claims 1
UPHYFHPRKDRKDY-UHFFFAOYSA-N n-(1h-indazol-5-yl)-7-methoxy-2-(3-phenylphenyl)-6-(2-pyrrolidin-1-ylethoxy)quinazolin-4-amine Chemical compound COC1=CC2=NC(C=3C=C(C=CC=3)C=3C=CC=CC=3)=NC(NC=3C=C4C=NNC4=CC=3)=C2C=C1OCCN1CCCC1 UPHYFHPRKDRKDY-UHFFFAOYSA-N 0.000 claims 1
ZSRJIYXCIMBXFA-UHFFFAOYSA-N n-(1h-indazol-5-yl)-7-methoxy-6-(2-morpholin-4-ylethoxy)-2-(3-phenylphenyl)quinazolin-4-amine Chemical compound COC1=CC2=NC(C=3C=C(C=CC=3)C=3C=CC=CC=3)=NC(NC=3C=C4C=NNC4=CC=3)=C2C=C1OCCN1CCOCC1 ZSRJIYXCIMBXFA-UHFFFAOYSA-N 0.000 claims 1
OJAYSJUGHYTKKF-UHFFFAOYSA-N n-(1h-indazol-5-yl)-7-methoxy-6-[2-(4-methylpiperazin-1-yl)ethoxy]-2-(3-phenylphenyl)quinazolin-4-amine Chemical compound COC1=CC2=NC(C=3C=C(C=CC=3)C=3C=CC=CC=3)=NC(NC=3C=C4C=NNC4=CC=3)=C2C=C1OCCN1CCN(C)CC1 OJAYSJUGHYTKKF-UHFFFAOYSA-N 0.000 claims 1
DTXWOTDWPWTGFL-UHFFFAOYSA-N n-(2,2-dimethylpropyl)-2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]acetamide Chemical compound CC(C)(C)CNC(=O)COC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 DTXWOTDWPWTGFL-UHFFFAOYSA-N 0.000 claims 1
GAMWZWDTPABWTE-UHFFFAOYSA-N n-(cyanomethyl)-2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]acetamide Chemical compound N#CCNC(=O)COC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 GAMWZWDTPABWTE-UHFFFAOYSA-N 0.000 claims 1
TYDXNFSXGZAXGM-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-6-(2-methoxyethoxy)quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=CC(OCCOC)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 TYDXNFSXGZAXGM-UHFFFAOYSA-N 0.000 claims 1
VURPHHPGBKTHTM-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-6-(2-methoxyethoxy)quinazolin-2-yl]phenyl]pyridine-3-carboxamide Chemical compound N1=C(NC=2C=C3C=NNC3=CC=2)C2=CC(OCCOC)=CC=C2N=C1C(C=1)=CC=CC=1NC(=O)C1=CC=CN=C1 VURPHHPGBKTHTM-UHFFFAOYSA-N 0.000 claims 1
VLFJNCVNWVVWAV-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-6-(2-piperidin-1-ylethoxy)quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=CC(OCCN4CCCCC4)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 VLFJNCVNWVVWAV-UHFFFAOYSA-N 0.000 claims 1
HTROFVQKJODSCL-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-6-(2-pyrrolidin-1-ylethoxy)quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=CC(OCCN4CCCC4)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 HTROFVQKJODSCL-UHFFFAOYSA-N 0.000 claims 1
WIWLMHOAKGHQBF-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-6-[2-(2-oxopyrrolidin-1-yl)ethoxy]quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=CC(OCCN4C(CCC4)=O)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 WIWLMHOAKGHQBF-UHFFFAOYSA-N 0.000 claims 1
OYYKFTMPIAGPIG-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-6-[2-(4-methylpiperazin-1-yl)ethoxy]quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=CC(OCCN4CCN(C)CC4)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 OYYKFTMPIAGPIG-UHFFFAOYSA-N 0.000 claims 1
OJZHJTAYYVFECQ-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-6-[2-[2-methoxyethyl(methyl)amino]ethoxy]quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=CC(OCCN(C)CCOC)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 OJZHJTAYYVFECQ-UHFFFAOYSA-N 0.000 claims 1
GONSFGGIXZMLDJ-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-7-methoxy-6-(2-methoxyethoxy)quinazolin-2-yl]phenyl]-2-morpholin-4-ylacetamide Chemical compound N1=C2C=C(OC)C(OCCOC)=CC2=C(NC=2C=C3C=NNC3=CC=2)N=C1C(C=1)=CC=CC=1NC(=O)CN1CCOCC1 GONSFGGIXZMLDJ-UHFFFAOYSA-N 0.000 claims 1
RBMZTABDHRMSMI-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-7-methoxy-6-(2-methoxyethoxy)quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=C(OC)C(OCCOC)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 RBMZTABDHRMSMI-UHFFFAOYSA-N 0.000 claims 1
XXYKKTKWQIXFIP-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-7-methoxy-6-(2-methoxyethoxy)quinazolin-2-yl]phenyl]pyridine-3-carboxamide Chemical compound N1=C2C=C(OC)C(OCCOC)=CC2=C(NC=2C=C3C=NNC3=CC=2)N=C1C(C=1)=CC=CC=1NC(=O)C1=CC=CN=C1 XXYKKTKWQIXFIP-UHFFFAOYSA-N 0.000 claims 1
RYOMMGAHCJKUDG-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-7-methoxy-6-(2-pyrrolidin-1-ylethoxy)quinazolin-2-yl]phenyl]-2-morpholin-4-ylacetamide Chemical compound COC1=CC2=NC(C=3C=C(NC(=O)CN4CCOCC4)C=CC=3)=NC(NC=3C=C4C=NNC4=CC=3)=C2C=C1OCCN1CCCC1 RYOMMGAHCJKUDG-UHFFFAOYSA-N 0.000 claims 1
KMBVJJHZAZTAPG-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=C(OC)C(OCCCN4CCOCC4)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 KMBVJJHZAZTAPG-UHFFFAOYSA-N 0.000 claims 1
AHBQWQVXLLQFCO-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-2-yl]phenyl]pyridine-3-carboxamide Chemical compound COC1=CC2=NC(C=3C=C(NC(=O)C=4C=NC=CC=4)C=CC=3)=NC(NC=3C=C4C=NNC4=CC=3)=C2C=C1OCCCN1CCOCC1 AHBQWQVXLLQFCO-UHFFFAOYSA-N 0.000 claims 1
QPNLSVHQZIBOLE-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-2-yl]phenyl]pyridine-4-carboxamide Chemical compound COC1=CC2=NC(C=3C=C(NC(=O)C=4C=CN=CC=4)C=CC=3)=NC(NC=3C=C4C=NNC4=CC=3)=C2C=C1OCCCN1CCOCC1 QPNLSVHQZIBOLE-UHFFFAOYSA-N 0.000 claims 1
JLDIMPXARFWITP-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-7-methoxy-6-[2-(2-oxopyrrolidin-1-yl)ethoxy]quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=C(OC)C(OCCN4C(CCC4)=O)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 JLDIMPXARFWITP-UHFFFAOYSA-N 0.000 claims 1
GKZABRRCVROKDJ-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)-7-methoxy-6-[2-(4-methylpiperazin-1-yl)ethoxy]quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=C(OC)C(OCCN4CCN(C)CC4)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 GKZABRRCVROKDJ-UHFFFAOYSA-N 0.000 claims 1
HAXOAIWDRNEKDR-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenyl]-2-methoxyacetamide Chemical compound COCC(=O)NC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 HAXOAIWDRNEKDR-UHFFFAOYSA-N 0.000 claims 1
LDIKNSCDPZFMMA-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenyl]-2-morpholin-4-ylacetamide Chemical compound C=1C=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=CC=1NC(=O)CN1CCOCC1 LDIKNSCDPZFMMA-UHFFFAOYSA-N 0.000 claims 1
WJLFPIPGQZWAJR-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenyl]-3-(4-propan-2-ylpiperazin-1-yl)propanamide Chemical compound C1CN(C(C)C)CCN1CCC(=O)NC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 WJLFPIPGQZWAJR-UHFFFAOYSA-N 0.000 claims 1
FKGASPODRFALEE-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenyl]-4-methylpiperazine-1-carboxamide Chemical compound C1CN(C)CCN1C(=O)NC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 FKGASPODRFALEE-UHFFFAOYSA-N 0.000 claims 1
LEKUVGYHAACMPX-UHFFFAOYSA-N n-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenyl]piperidine-4-carboxamide Chemical compound C=1C=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=CC=1NC(=O)C1CCNCC1 LEKUVGYHAACMPX-UHFFFAOYSA-N 0.000 claims 1
YFIAGILPWYUJOO-UHFFFAOYSA-N n-[3-[6-[2-(3-hydroxypyrrolidin-1-yl)ethoxy]-4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=CC(OCCN4CC(O)CC4)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 YFIAGILPWYUJOO-UHFFFAOYSA-N 0.000 claims 1
IGLWQEHCFIZYNV-UHFFFAOYSA-N n-[3-[6-[2-(dimethylamino)-2-oxoethoxy]-4-(1h-indazol-5-ylamino)-7-methoxyquinazolin-2-yl]phenyl]pyridine-3-carboxamide Chemical compound N=1C(NC=2C=C3C=NNC3=CC=2)=C2C=C(OCC(=O)N(C)C)C(OC)=CC2=NC=1C(C=1)=CC=CC=1NC(=O)C1=CC=CN=C1 IGLWQEHCFIZYNV-UHFFFAOYSA-N 0.000 claims 1
PNLVKNQWPPYODW-UHFFFAOYSA-N n-[3-[6-[2-(dimethylamino)ethoxy]-4-(1h-indazol-5-ylamino)-7-methoxyquinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=C(OC)C(OCCN(C)C)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 PNLVKNQWPPYODW-UHFFFAOYSA-N 0.000 claims 1
JIIRSFCNUVXFCS-UHFFFAOYSA-N n-[3-[6-[2-(dimethylamino)ethoxy]-4-(1h-indazol-5-ylamino)-7-methoxyquinazolin-2-yl]phenyl]pyridine-3-carboxamide Chemical compound N=1C(NC=2C=C3C=NNC3=CC=2)=C2C=C(OCCN(C)C)C(OC)=CC2=NC=1C(C=1)=CC=CC=1NC(=O)C1=CC=CN=C1 JIIRSFCNUVXFCS-UHFFFAOYSA-N 0.000 claims 1
PQKDTUQQZKJBBH-UHFFFAOYSA-N n-[3-[6-[2-(dimethylamino)ethoxy]-4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=CC(OCCN(C)C)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 PQKDTUQQZKJBBH-UHFFFAOYSA-N 0.000 claims 1
QRCUDOKSMFUXGE-UHFFFAOYSA-N n-[3-[6-[2-(dimethylamino)ethoxy]-4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenyl]pyridine-3-carboxamide Chemical compound N1=C(NC=2C=C3C=NNC3=CC=2)C2=CC(OCCN(C)C)=CC=C2N=C1C(C=1)=CC=CC=1NC(=O)C1=CC=CN=C1 QRCUDOKSMFUXGE-UHFFFAOYSA-N 0.000 claims 1
SOCMHMWQDVOXGG-SANMLTNESA-N n-[3-[6-[2-[(3s)-3-(dimethylamino)pyrrolidin-1-yl]ethoxy]-4-(1h-indazol-5-ylamino)-7-methoxyquinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=C(OC)C(OCCN4C[C@H](CC4)N(C)C)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 SOCMHMWQDVOXGG-SANMLTNESA-N 0.000 claims 1
ZGJCPUWSTXPZNG-UHFFFAOYSA-N n-[3-[6-[3-(dimethylamino)propoxy]-4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenyl]butanamide Chemical compound CCCC(=O)NC1=CC=CC(C=2N=C3C=CC(OCCCN(C)C)=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 ZGJCPUWSTXPZNG-UHFFFAOYSA-N 0.000 claims 1
XDLFYTCCWCUIQC-UHFFFAOYSA-N n-cyclobutyl-2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]acetamide Chemical compound C=1C=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=CC=1OCC(=O)NC1CCC1 XDLFYTCCWCUIQC-UHFFFAOYSA-N 0.000 claims 1
KABJHFCHTPNPDM-UHFFFAOYSA-N n-cyclohexyl-2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]acetamide Chemical compound C=1C=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=CC=1OCC(=O)NC1CCCCC1 KABJHFCHTPNPDM-UHFFFAOYSA-N 0.000 claims 1
XCQHNDAIHGGNJC-UHFFFAOYSA-N n-ethyl-2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]acetamide Chemical compound CCNC(=O)COC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 XCQHNDAIHGGNJC-UHFFFAOYSA-N 0.000 claims 1
MJGAFLMZUQBXAZ-UHFFFAOYSA-N n-tert-butyl-2-[3-[4-(1h-indazol-5-ylamino)quinazolin-2-yl]phenoxy]acetamide Chemical compound CC(C)(C)NC(=O)COC1=CC=CC(C=2N=C3C=CC=CC3=C(NC=3C=C4C=NNC4=CC=3)N=2)=C1 MJGAFLMZUQBXAZ-UHFFFAOYSA-N 0.000 claims 1
230000001613 neoplastic effect Effects 0.000 claims 1
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
229960002797 pitavastatin Drugs 0.000 claims 1
VGYFMXBACGZSIL-MCBHFWOFSA-N pitavastatin Chemical compound OC(=O)C[C@H](O)C[C@H](O)\C=C\C1=C(C2CC2)N=C2C=CC=CC2=C1C1=CC=C(F)C=C1 VGYFMXBACGZSIL-MCBHFWOFSA-N 0.000 claims 1
229960002965 pravastatin Drugs 0.000 claims 1
TUZYXOIXSAXUGO-PZAWKZKUSA-N pravastatin Chemical compound C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC(O)=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@H](O)C=C21 TUZYXOIXSAXUGO-PZAWKZKUSA-N 0.000 claims 1
DRYRBWIFRVMRPV-UHFFFAOYSA-N quinazolin-4-amine Chemical compound C1=CC=C2C(N)=NC=NC2=C1 DRYRBWIFRVMRPV-UHFFFAOYSA-N 0.000 claims 1
238000001959 radiotherapy Methods 0.000 claims 1
229960000672 rosuvastatin Drugs 0.000 claims 1
BPRHUIZQVSMCRT-VEUZHWNKSA-N rosuvastatin Chemical compound CC(C)C1=NC(N(C)S(C)(=O)=O)=NC(C=2C=CC(F)=CC=2)=C1\C=C\[C@@H](O)C[C@@H](O)CC(O)=O BPRHUIZQVSMCRT-VEUZHWNKSA-N 0.000 claims 1
229960002855 simvastatin Drugs 0.000 claims 1
RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 claims 1
229910052717 sulfur Inorganic materials 0.000 claims 1
208000037816 tissue injury Diseases 0.000 claims 1
101000669917 Homo sapiens Rho-associated protein kinase 1 Proteins 0.000 abstract 3
102100039313 Rho-associated protein kinase 1 Human genes 0.000 abstract 3
239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 abstract 1
230000002401 inhibitory effect Effects 0.000 abstract 1
230000003285 pharmacodynamic effect Effects 0.000 abstract 1
238000011282 treatment Methods 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)

CA2700988A 2006-09-27 2007-09-27 Inhibiteurs de la rho kinase Abandoned CA2700988A1 (fr)

Applications Claiming Priority (7)

Application Number	Priority Date	Filing Date	Title
US84769406P	2006-09-27	2006-09-27
US60/847,694		2006-09-28
US85012506P	2006-10-05	2006-10-05
US85012706P	2006-10-05	2006-10-05
US60/850,126		2006-10-05
US60/850,127		2006-10-05
PCT/US2007/021093 WO2008054599A2 (fr)	2006-09-27	2007-09-27	Inhibiteurs de la rho kinase

Publications (1)

Publication Number	Publication Date
CA2700988A1 true CA2700988A1 (fr)	2008-05-08

Family

ID=39344830

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
CA2700988A Abandoned CA2700988A1 (fr)	2006-09-27	2007-09-27	Inhibiteurs de la rho kinase

Country Status (3)

Country	Link
CA (1)	CA2700988A1 (fr)
PE (1)	PE20080972A1 (fr)
WO (1)	WO2008054599A2 (fr)

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WO2024078553A1 (fr) *	2022-10-13	2024-04-18	北京泰德制药股份有限公司	Procédé de traitement de la pneumoconiose

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US7645878B2 (en) *	2002-03-22	2010-01-12	Bayer Healthcare Llc	Process for preparing quinazoline Rho-kinase inhibitors and intermediates thereof

2007
- 2007-09-27 WO PCT/US2007/021093 patent/WO2008054599A2/fr active Application Filing
- 2007-09-27 CA CA2700988A patent/CA2700988A1/fr not_active Abandoned
- 2007-10-16 PE PE2007001317A patent/PE20080972A1/es not_active Application Discontinuation

Also Published As

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WO2008054599A3 (fr)	2008-11-20
WO2008054599A2 (fr)	2008-05-08
PE20080972A1 (es)	2008-10-04

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