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：US20130289020A1

公开(公告)日：2013-10-31

申请号：US13878968

申请日：2011-10-13

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

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

IPC分类号： C07D401/14 ,  C07D401/12 ,  C07D471/08 ,  C07D413/14 ,  C07D471/04 ,  C07D405/14 ,  C07D417/14

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：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：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.

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：US20130324556A1

公开(公告)日：2013-12-05

申请号：US13981960

申请日：2012-01-27

申请人： Joe William Boyd ,  Paul Meo ,  Michael Higginbottom ,  Iain Simpson ,  David Mark Mountford ,  Edward Daniel Savory

发明人： Joe William Boyd ,  Paul Meo ,  Michael Higginbottom ,  Iain Simpson ,  David Mark Mountford ,  Edward Daniel Savory

IPC分类号： C07D211/16 ,  C07D211/18 ,  C07D401/06 ,  C07D211/46 ,  C07D471/04 ,  C07D211/54 ,  C07D211/62 ,  C07D295/215 ,  C07D207/06 ,  C07D413/04 ,  C07D211/22 ,  C07D211/58

CPC分类号： C07D211/16 ,  C07D207/06 ,  C07D211/18 ,  C07D211/20 ,  C07D211/22 ,  C07D211/46 ,  C07D211/54 ,  C07D211/58 ,  C07D211/62 ,  C07D295/185 ,  C07D295/192 ,  C07D295/215 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D471/04

摘要： A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrate thereof Wherein Y, Z, R3, U, R4, m and n are as defined in the claims.

摘要翻译： 式（I）化合物或其药学上可接受的盐，溶剂化物或水合物。其中Y，Z，R3，U，R4，m和n如权利要求中所定义。

公开(公告)号：US20130252951A1

公开(公告)日：2013-09-26

申请号：US13876220

申请日：2011-09-26

申请人： Joe William Boyd ,  Paul Meo ,  Michael Higginbottom ,  Iain Simpson ,  David Mountford ,  Edward Daniel Savory

发明人： Joe William Boyd ,  Paul Meo ,  Michael Higginbottom ,  Iain Simpson ,  David Mountford ,  Edward Daniel Savory

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： The compounds of formula (I) are antagonists of the CCR2 receptor Wherein R1-7 and A are as defined in the claims.

摘要翻译： 式（I）化合物是CCR2受体的拮抗剂，其中R1-7和A如权利要求中所定义。

公开(公告)号：US20110207746A1

公开(公告)日：2011-08-25

申请号：US13062318

申请日：2009-09-16

申请人： Edward Daniel Savory ,  Michael Higginbottom ,  Kathryn Oliver ,  VietAnh Anne Horgan

发明人： Edward Daniel Savory ,  Michael Higginbottom ,  Kathryn Oliver ,  VietAnh Anne Horgan

IPC分类号： A61K31/497 ,  C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P37/06 ,  A61P19/02 ,  A61P25/28 ,  A61P1/00 ,  A61P9/10 ,  A61P11/06 ,  A61P11/00 ,  A61P9/00 ,  A61P17/00 ,  A61P17/06 ,  A61P1/16 ,  A61P3/10 ,  A61P9/04

CPC分类号： C07D471/04 ,  A61K31/437

摘要： The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.

摘要翻译： 本发明涉及作为SSAO活性抑制剂的式（I）化合物及其药学上可接受的盐，溶剂合物，水合物，几何异构体，互变异构体，旋光异构体或N-氧化物。 本发明进一步涉及包含这些化合物的药物组合物以及这些化合物用于治疗其中SSAO活性抑制是有益的医学病症如炎性疾病和免疫疾病的用途。

公开(公告)号：US20120302583A1

公开(公告)日：2012-11-29

申请号：US13567146

申请日：2012-08-06

申请人： Edward Daniel Savory ,  Michael Higginbottom ,  Kathryn Oliver ,  Viet-Anh Anne Horgan

发明人： Edward Daniel Savory ,  Michael Higginbottom ,  Kathryn Oliver ,  Viet-Anh Anne Horgan

IPC分类号： A61K31/437 ,  A61K31/497 ,  A61P29/00 ,  A61P37/00 ,  A61P19/02 ,  A61P1/00 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  A61P11/00 ,  A61P17/00 ,  A61P3/10 ,  A61P1/16 ,  A61P9/04 ,  A61P1/04 ,  A61P11/06 ,  A61P9/00 ,  A61P17/06 ,  A61K31/444

CPC分类号： C07D471/04 ,  A61K31/437

摘要： The present invention relates to a method for the treatment or prevention of inflammation, an inflammatory disease, an immune or an autoimmune disorder, which comprises administering to a mammal in need of such treatment an effective amount of a compound compound of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity.

摘要翻译： 本发明涉及治疗或预防炎症，炎性疾病，免疫或自身免疫性疾病的方法，其包括向需要这种治疗的哺乳动物施用有效量的式（I）化合物和 其药学上可接受的盐，溶剂化物，水合物，几何异构体，互变异构体，光学异构体或N-氧化物，其是SSAO活性的抑制剂。