公开(公告)号：US07666888B2

公开(公告)日：2010-02-23

申请号：US11779599

申请日：2007-07-18

申请人： Michael D. Bartberger ,  Christopher H. Fotsch ,  Martin Haraldsson ,  David St. Jean ,  Lars Johansson ,  Marianne Nilsson ,  Lori Sutin ,  Katrina Flyrén

发明人： Michael D. Bartberger ,  Christopher H. Fotsch ,  Martin Haraldsson ,  David St. Jean ,  Lars Johansson ,  Marianne Nilsson ,  Lori Sutin ,  Katrina Flyrén

IPC分类号： A61K31/422 ,  A61K31/4155 ,  C07D261/06 ,  C07D231/10

CPC分类号： C07D403/06 ,  C07D413/06 ,  C07D413/12

摘要： Compounds of formula I and IV are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorder: wherein the variables A-B, R1, R2, m, and Q are described herein.

摘要翻译： 描述了式I和IV的化合物，并具有治疗效用，特别是在治疗糖尿病，肥胖症和相关病症和病症中：其中本文描述了变量A-B，R1，R2，m和Q。

公开(公告)号：US20080021022A1

公开(公告)日：2008-01-24

申请号：US11779599

申请日：2007-07-18

申请人： Michael Bartberger ,  Christopher Fotsch ,  Martin Haraldsson ,  David St. Jean ,  Lars Johansson ,  Marianne Nilsson ,  Lori Sutin ,  Katrina Flyren

发明人： Michael Bartberger ,  Christopher Fotsch ,  Martin Haraldsson ,  David St. Jean ,  Lars Johansson ,  Marianne Nilsson ,  Lori Sutin ,  Katrina Flyren

IPC分类号： A61K31/42 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/497 ,  A61K31/499 ,  A61K31/5377 ,  A61K31/541 ,  A61P17/02 ,  A61P19/10 ,  A61P25/28 ,  A61P27/06 ,  A61P3/04 ,  A61P3/10 ,  A61P37/00 ,  A61P9/12 ,  C07D261/08 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14

CPC分类号： C07D403/06 ,  C07D413/06 ,  C07D413/12

摘要： Compounds of formula I and IV are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorder: wherein the variables A-B, R1, R2, m, and Q are described herein.

摘要翻译： 描述了式I和IV的化合物，并且具有治疗效用，特别是在治疗糖尿病，肥胖症和相关病症和病症中：其中变量AB，R 1，R 2， >，m和Q。

公开(公告)号：US20120010188A1

公开(公告)日：2012-01-12

申请号：US13132143

申请日：2009-12-04

申请人： Marianne Nilsson ,  Martin Haraldsson ,  Sofia Henriksson ,  Rikard Emond ,  Edward Daniel Savory ,  Iain David Simpson

发明人： Marianne Nilsson ,  Martin Haraldsson ,  Sofia Henriksson ,  Rikard Emond ,  Edward Daniel Savory ,  Iain David Simpson

IPC分类号： A61K31/437 ,  C07D413/14 ,  A61K31/5377 ,  A61P29/00 ,  A61P37/00 ,  A61P19/02 ,  A61P7/00 ,  A61P1/00 ,  A61P1/04 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  A61P11/06 ,  A61P11/00 ,  A61P17/00 ,  A61P17/06 ,  A61P1/16 ,  A61P3/10 ,  A61P9/04 ,  C07D471/04

CPC分类号： C07D498/04 ,  A61K31/4188 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/519 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： The invention relates to compounds of formula (I): and their pharmaceutically acceptable salts and solvates, 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 or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.

摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐和溶剂化物，其是SSAO活性的抑制剂。 本发明还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或预防其中SSAO活性抑制是有益的医学病症的用途，例如炎性疾病和免疫疾病。

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：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：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：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：US07132436B2

公开(公告)日：2006-11-07

申请号：US10296552

申请日：2001-05-22

申请人： Guido Kurz ,  Marianne Nilsson

发明人： Guido Kurz ,  Marianne Nilsson

IPC分类号： C07D277/52 ,  C07D409/12 ,  A61K31/426 ,  A61K31/427

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D277/52 ,  C07D277/56 ,  C07D277/84 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D491/08 ,  C07D513/04

摘要： The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

公开(公告)号：US07074788B2

公开(公告)日：2006-07-11

申请号：US10302329

申请日：2002-11-22

申请人： Guido Kurz ,  Marianne Nilsson ,  Jerk Vallgårda ,  Meredith Williams

发明人： Guido Kurz ,  Marianne Nilsson ,  Jerk Vallgårda ,  Meredith Williams

IPC分类号： C07D417/06 ,  A61K31/5377

CPC分类号： A61K31/381 ,  A61K31/433 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D285/08 ,  C07D285/135 ,  C07D333/36 ,  C07D409/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

公开(公告)号：US20060287374A1

公开(公告)日：2006-12-21

申请号：US11511224

申请日：2006-08-29

申请人： Tjeerd Barf ,  Marianne Nilsson ,  Jerk Vallgarda ,  Guido Kurz

发明人： Tjeerd Barf ,  Marianne Nilsson ,  Jerk Vallgarda ,  Guido Kurz

IPC分类号： A61K31/427 ,  A61K31/426 ,  C07D417/02

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D277/52 ,  C07D277/56 ,  C07D277/84 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D491/08 ,  C07D513/04

摘要： The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.