JP2017532315A5 - - Google Patents
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- Publication number
- JP2017532315A5 JP2017532315A5 JP2017515186A JP2017515186A JP2017532315A5 JP 2017532315 A5 JP2017532315 A5 JP 2017532315A5 JP 2017515186 A JP2017515186 A JP 2017515186A JP 2017515186 A JP2017515186 A JP 2017515186A JP 2017532315 A5 JP2017532315 A5 JP 2017532315A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- halo
- cyano
- substituted
- Prior art date
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 34
- 150000001875 compounds Chemical class 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 15
- 150000001204 N-oxides Chemical class 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 11
- 125000004093 cyano group Chemical group *C#N 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000004043 oxo group Chemical group O=* 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 201000004810 Vascular dementia Diseases 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 230000004054 inflammatory process Effects 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 2
- 230000001363 autoimmune Effects 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 208000019425 cirrhosis of liver Diseases 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 201000008482 osteoarthritis Diseases 0.000 claims 2
- 230000002685 pulmonary effect Effects 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- UZGQPQRCHGAMQR-UHFFFAOYSA-N 1-[[5-[3-(4-fluorophenyl)imidazo[4,5-c]pyridin-2-yl]pyrimidin-2-yl]amino]-2-methylpropan-2-ol Chemical compound FC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)C=1C=NC(=NC=1)NCC(C)(O)C UZGQPQRCHGAMQR-UHFFFAOYSA-N 0.000 claims 1
- BSKKEARUDBJATB-UHFFFAOYSA-N 4-[4-[3-(4-chlorophenyl)imidazo[4,5-c]pyridin-2-yl]piperidin-1-yl]-1H-pyrimidin-6-one Chemical compound ClC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)C1CCN(CC1)C1=CC(NC=N1)=O BSKKEARUDBJATB-UHFFFAOYSA-N 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000022309 Alcoholic Liver disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 1
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 1
- WTRBRNHDYVTXRE-UHFFFAOYSA-N CC1=CC=C(C=C1)N1C2=C(C=CN=C2)N=C1C1=CN=C(NCC(C)(C)O)N=C1 Chemical compound CC1=CC=C(C=C1)N1C2=C(C=CN=C2)N=C1C1=CN=C(NCC(C)(C)O)N=C1 WTRBRNHDYVTXRE-UHFFFAOYSA-N 0.000 claims 1
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000021910 Cerebral Arterial disease Diseases 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 1
- JZKBCCBKRCEZAW-UHFFFAOYSA-N ClC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)C1CCN(CC1)C1=CC=NC=C1 Chemical compound ClC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)C1CCN(CC1)C1=CC=NC=C1 JZKBCCBKRCEZAW-UHFFFAOYSA-N 0.000 claims 1
- PABVYNYFCNWVDM-UHFFFAOYSA-N ClC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)CC=1C=NC=CC=1 Chemical compound ClC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)CC=1C=NC=CC=1 PABVYNYFCNWVDM-UHFFFAOYSA-N 0.000 claims 1
- CXJYKHJOOFQCAU-UHFFFAOYSA-N ClC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)CCCN1C=NC=C1 Chemical compound ClC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)CCCN1C=NC=C1 CXJYKHJOOFQCAU-UHFFFAOYSA-N 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- BRQIOVJAMQHKCN-UHFFFAOYSA-N FC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)C(=O)NCC1CCOCC1 Chemical compound FC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)C(=O)NCC1CCOCC1 BRQIOVJAMQHKCN-UHFFFAOYSA-N 0.000 claims 1
- DDGRQNROCYUUTL-UHFFFAOYSA-N FC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)C1=CC2=C(NC=N2)C=C1 Chemical compound FC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)C1=CC2=C(NC=N2)C=C1 DDGRQNROCYUUTL-UHFFFAOYSA-N 0.000 claims 1
- YPKKKJIPVFMHGZ-UHFFFAOYSA-N FC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)C=1C=C2CC(NC2=CC=1)=O Chemical compound FC1=CC=C(C=C1)N1C(=NC2=C1C=NC=C2)C=1C=C2CC(NC2=CC=1)=O YPKKKJIPVFMHGZ-UHFFFAOYSA-N 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010051379 Systemic Inflammatory Response Syndrome Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 230000005856 abnormality Effects 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000018093 autoimmune cholangitis Diseases 0.000 claims 1
- 230000009787 cardiac fibrosis Effects 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 208000019069 chronic childhood arthritis Diseases 0.000 claims 1
- 230000005494 condensation Effects 0.000 claims 1
- 238000009833 condensation Methods 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 239000000835 fiber Substances 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 208000026278 immune system disease Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000000968 intestinal effect Effects 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 208000012947 ischemia reperfusion injury Diseases 0.000 claims 1
- 208000023589 ischemic disease Diseases 0.000 claims 1
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
- 201000004595 synovitis Diseases 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 230000004614 tumor growth Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1416444.6A GB201416444D0 (en) | 2014-09-17 | 2014-09-17 | New compounds |
| GB1416444.6 | 2014-09-17 | ||
| PCT/GB2015/052691 WO2016042332A1 (en) | 2014-09-17 | 2015-09-17 | Imidazo[4,5-c]pyridine derived ssao inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017532315A JP2017532315A (ja) | 2017-11-02 |
| JP2017532315A5 true JP2017532315A5 (enExample) | 2019-08-15 |
| JP6589246B2 JP6589246B2 (ja) | 2019-10-16 |
Family
ID=51869759
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017515186A Expired - Fee Related JP6589246B2 (ja) | 2014-09-17 | 2015-09-17 | イミダゾ［４，５‐ｃ］ピリジン由来のｓｓａｏ阻害剤 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US11530208B2 (enExample) |
| EP (1) | EP3194389B1 (enExample) |
| JP (1) | JP6589246B2 (enExample) |
| CN (1) | CN107074853B (enExample) |
| AU (1) | AU2015316611B2 (enExample) |
| BR (1) | BR112017005324A2 (enExample) |
| CA (1) | CA2961424A1 (enExample) |
| DK (1) | DK3194389T3 (enExample) |
| ES (1) | ES2744548T3 (enExample) |
| GB (1) | GB201416444D0 (enExample) |
| HU (1) | HUE045827T2 (enExample) |
| IL (1) | IL251166B (enExample) |
| PL (1) | PL3194389T3 (enExample) |
| PT (1) | PT3194389T (enExample) |
| WO (1) | WO2016042332A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201304526D0 (en) * | 2013-03-13 | 2013-04-24 | Proximagen Ltd | New compounds |
| GB201416446D0 (en) * | 2014-09-17 | 2014-10-29 | Proximagen Ltd | New enzyme inhibitor compounds |
| WO2018027892A1 (en) | 2016-08-12 | 2018-02-15 | Eli Lilly And Company | Amino pyrimidine ssao inhibitors |
| WO2018148856A1 (en) * | 2017-02-14 | 2018-08-23 | Eli Lilly And Company | Diazaspirodecanyl-pyrimidine compounds useful as ssao inhibitors |
| AU2021332217A1 (en) | 2020-08-25 | 2023-05-11 | Eli Lilly And Company | Polymorphs of an ssao inhibitor |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002038153A1 (en) * | 2000-11-09 | 2002-05-16 | Biovitrum Ab | New use of 4, 5, 6, 7-tetrahydroimidazo-[4,5-c]pyridine derivatives |
| US6982286B2 (en) | 2001-07-12 | 2006-01-03 | Biotie Therapies Corp. | Carbocyclic hydrazino inhibitors of copper-containing amine oxidases |
| AU2004263525A1 (en) | 2003-08-08 | 2005-02-17 | La Jolla Pharmaceutical Co. | Inhibitors of semicarbazide-sensitive amine oxidase (SSAO) and VAP-1 mediated adhesion useful for treatment of diseases |
| US7405300B2 (en) | 2003-09-04 | 2008-07-29 | Aventis Pharmaveuticals Inc. | Substituted indoles as inhibitors of poly (ADP-ribose) polymerase (PARP) |
| US20070293548A1 (en) | 2006-03-31 | 2007-12-20 | Wang Eric Y | Inhibitors of semicarbazide-sensitive amine oxidase (SSAO) and VAP-1 mediated adhesion useful for treatment and prevention of diseases |
| US7947723B2 (en) | 2008-02-01 | 2011-05-24 | Spelman College | Synthesis and anti-proliferative effect of benzimidazole derivatives |
| US8263616B2 (en) * | 2008-09-16 | 2012-09-11 | Proximagen Ltd | 4,5,6,7-tetrahydroimidazo[4,5-c]pyridine compounds |
| EP2328895B1 (en) * | 2008-09-16 | 2013-03-27 | Proximagen Limited | Pyrazolo[4,3-c]pyridine compounds and their use as inhibitors of SSAO |
| WO2010064020A1 (en) | 2008-12-04 | 2010-06-10 | Proximagen Ltd. | Imidazopyridine compounds |
| WO2010117935A1 (en) | 2009-04-06 | 2010-10-14 | Schering Corporation | Compounds and methods for antiviral treatment |
| GB201004311D0 (en) | 2010-03-15 | 2010-04-28 | Proximagen Ltd | New enzyme inhibitor compounds |
| EP2518071A1 (en) * | 2011-04-29 | 2012-10-31 | Almirall, S.A. | Imidazopyridine derivatives as PI3K inhibitors |
| JP5796130B2 (ja) | 2011-09-14 | 2015-10-21 | プロクシマゲン リミテッド | 新規な酵素阻害剤化合物 |
| GB201115853D0 (en) | 2011-09-14 | 2011-10-26 | Proximagen Ltd | New enzyme inhibitor compounds |
| WO2013078254A1 (en) | 2011-11-22 | 2013-05-30 | Array Biopharma Inc. | Bicyclic heteroaryl derivatives as kinase inhibitors |
| GB201304526D0 (en) * | 2013-03-13 | 2013-04-24 | Proximagen Ltd | New compounds |
| GB201304527D0 (en) | 2013-03-13 | 2013-04-24 | Proximagen Ltd | New compounds |
| GB201404498D0 (en) * | 2014-03-13 | 2014-04-30 | Proximagen Ltd | New compounds |
| WO2015189534A1 (en) | 2014-06-12 | 2015-12-17 | Proximagen Limited | Vap-1 inhibitors for treating muscular dystrophy |
| GB201416446D0 (en) * | 2014-09-17 | 2014-10-29 | Proximagen Ltd | New enzyme inhibitor compounds |
| HK1256174A1 (zh) * | 2015-12-07 | 2019-09-13 | Benevolentai Cambridge Limited | 用於治疗疼痛的 vap-1 抑制剂 |
| GB201709136D0 (en) * | 2017-06-08 | 2017-07-26 | Proximagen Ltd | New therapeutic uses of enzyme inhibitors |
-
2014
- 2014-09-17 GB GBGB1416444.6A patent/GB201416444D0/en not_active Ceased
-
2015
- 2015-09-17 PL PL15770605T patent/PL3194389T3/pl unknown
- 2015-09-17 CA CA2961424A patent/CA2961424A1/en not_active Abandoned
- 2015-09-17 JP JP2017515186A patent/JP6589246B2/ja not_active Expired - Fee Related
- 2015-09-17 WO PCT/GB2015/052691 patent/WO2016042332A1/en not_active Ceased
- 2015-09-17 HU HUE15770605A patent/HUE045827T2/hu unknown
- 2015-09-17 BR BR112017005324A patent/BR112017005324A2/pt not_active IP Right Cessation
- 2015-09-17 EP EP15770605.2A patent/EP3194389B1/en not_active Not-in-force
- 2015-09-17 PT PT15770605T patent/PT3194389T/pt unknown
- 2015-09-17 DK DK15770605.2T patent/DK3194389T3/da active
- 2015-09-17 US US15/506,847 patent/US11530208B2/en active Active
- 2015-09-17 AU AU2015316611A patent/AU2015316611B2/en not_active Ceased
- 2015-09-17 ES ES15770605T patent/ES2744548T3/es active Active
- 2015-09-17 CN CN201580056356.XA patent/CN107074853B/zh not_active Expired - Fee Related
-
2017
- 2017-03-14 IL IL251166A patent/IL251166B/en active IP Right Grant
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