公开(公告)号：US20130102587A1

公开(公告)日：2013-04-25

申请号：US13634732

申请日：2011-03-14

申请人： David Evans ,  Allison Carley ,  Alison Stewart ,  Michael Higginbottom ,  Edward Savory ,  Iain Simpson ,  Marianne Nilsson ,  Martin Haraldsson ,  Erik Nordling ,  Tobias Koolmeister

发明人： David Evans ,  Allison Carley ,  Alison Stewart ,  Michael Higginbottom ,  Edward Savory ,  Iain Simpson ,  Marianne Nilsson ,  Martin Haraldsson ,  Erik Nordling ,  Tobias Koolmeister

IPC分类号： C07D471/04 ,  C07D491/08 ,  C07D487/04

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/08 ,  C07D519/00

摘要： Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumour growth.

摘要翻译： 公开了抑制SSAO酶活性的化合物。 还公开了包含这些化合物的药物组合物以及这些化合物在治疗或预防其中抑制SSAO活性有益的医学病症中的用途，例如炎性疾病，免疫疾病和抑制肿瘤生长。

公开(公告)号：US09150574B2

公开(公告)日：2015-10-06

申请号：US14344417

申请日：2011-09-14

申请人： David Evans ,  Allison Carley ,  Alison Stewart ,  Michael Higginbottom ,  Edward Savory ,  Iain Simpson ,  Marianne Nilsson ,  Martin Haraldsson ,  Erik Nordling ,  Tobias Koolmeister

发明人： David Evans ,  Allison Carley ,  Alison Stewart ,  Michael Higginbottom ,  Edward Savory ,  Iain Simpson ,  Marianne Nilsson ,  Martin Haraldsson ,  Erik Nordling ,  Tobias Koolmeister

IPC分类号： C07D471/02 ,  A61K31/55 ,  C07D471/04

CPC分类号： C07D471/04

摘要： 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3-aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4-(dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; ethyl 1-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylic acid; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxamide; 4-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4yl}carbonyl)morpholine; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4-yl}carbonyl)piperazine; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}methanol; {4-[1-(4-methyl-phenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-2-yl}methanol; [(3R)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl]methanol; methyl 4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxylate; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxamide; 2-{4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}ethan-1-ol; methyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxylate; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxamide; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-2-yl}carbonyl)piperazine; 4-[1-(4-methylphenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]morpholine; 1-(4-chlorophenyl)-3-(piperidin-4-yl)-1H-pyrrolo[2,3-c]pyridin-4-ol; N-butyl-1-(4-chlorophenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridin-3-amine; 1-[4-(fluoromethyl)phenyl]-3-(oxan-4-yl)-1H-pyrazolo[3,4-c]pyridine; and 3-({4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-1-yl}methyl)pyridine are useful for the inhibition of SSAO activity.

公开(公告)号：US09227967B2

公开(公告)日：2016-01-05

申请号：US13634732

申请日：2011-03-14

申请人： David Evans ,  Allison Carley ,  Alison Stewart ,  Michael Higginbottom ,  Edward Savory ,  Iain Simpson ,  Marianne Nilsson ,  Martin Haraldsson ,  Erik Nordling ,  Tobias Koolmeister

发明人： David Evans ,  Allison Carley ,  Alison Stewart ,  Michael Higginbottom ,  Edward Savory ,  Iain Simpson ,  Marianne Nilsson ,  Martin Haraldsson ,  Erik Nordling ,  Tobias Koolmeister

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D498/08 ,  C07D519/00 ,  C07D491/08

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/08 ,  C07D519/00

摘要： Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.

摘要翻译： 公开了抑制SSAO酶活性的化合物。 还公开了包含这些化合物的药物组合物以及这些化合物在治疗或预防其中抑制SSAO活性有益的医学病症中的用途，例如炎性疾病，免疫疾病和抑制肿瘤生长。

公开(公告)号：US20140275063A1

公开(公告)日：2014-09-18

申请号：US14344436

申请日：2012-09-13

申请人： Allison Carley ,  Iain Simpson

发明人： Allison Carley ,  Iain Simpson

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： Compounds of formula (I) are inhibitors of Semicarbazide-sensitive amine oxidase R1—X—R2  (I) wherein R1, X and R2 are as defined in the claims.

摘要翻译： 式（I）化合物是氨基脲敏感性胺氧化酶R1-X-R2（Ⅰ）的抑制剂，其中R1，X和R2如权利要求中所定义。

公开(公告)号：US09353086B2

公开(公告)日：2016-05-31

申请号：US13878968

申请日：2011-10-13

申请人： Edward Daniel Savory ,  Alison Stewart ,  Allison Carley ,  Giles Brown ,  Iain Simpson ,  Kathryn Oliver ,  Lee Patient ,  Michael Higginbottom ,  Andrew Graham Cole

发明人： Edward Daniel Savory ,  Alison Stewart ,  Allison Carley ,  Giles Brown ,  Iain Simpson ,  Kathryn Oliver ,  Lee Patient ,  Michael Higginbottom ,  Andrew Graham Cole

IPC分类号： A61K31/55 ,  A61K31/551 ,  A61K31/439 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/12 ,  A61K45/06 ,  C07D401/12

CPC分类号： C07D471/08 ,  A61K45/06 ,  C07B59/002 ,  C07B2200/05 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Disclosed are compounds that are antagonists of the CXCR4 receptor.

摘要翻译： 公开了作为CXCR4受体的拮抗剂的化合物。

公开(公告)号：US20140357623A1

公开(公告)日：2014-12-04

申请号：US14344417

申请日：2011-09-14

申请人： David Evans ,  Allison Carley ,  Alison Stewart ,  Michael Higginbottom ,  Edward Savory ,  Iain Simpson ,  Marianne Nilsson ,  Martin Haraldsson ,  Erik Nordling ,  Tobias Koolmeister

发明人： David Evans ,  Allison Carley ,  Alison Stewart ,  Michael Higginbottom ,  Edward Savory ,  Iain Simpson ,  Marianne Nilsson ,  Martin Haraldsson ,  Erik Nordling ,  Tobias Koolmeister

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3-aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4-(dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; ethyl 1-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylic acid; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxamide; 4-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4 yl}carbonyl)morpholine; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4-yl}carbonyl)piperazine; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}methanol; {4-[1-(4-methyl-phenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-2-yl}methanol; [(3R)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl]methanol; methyl 4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxylate; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxamide; 2-{4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}ethan-1-ol; methyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxylate; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxamide; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-2-yl}carbonyl)piperazine; 4-[1-(4-methylphenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]morpholine; 1-(4-chlorophenyl)-3-(piperidin-4-yl)-1H-pyrrolo[2,3-c]pyridin-4-ol; N-butyl-1-(4-chlorophenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridin-3-amine; 1-[4-(fluoromethyl)phenyl]-3-(oxan-4-yl)-1H-pyrazolo[3,4-c]pyridine; and 3-({4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-1-yl}methyl)pyridine are useful for the inhibition of SSAO activity.