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：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：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：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：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：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：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：US20100022590A1

公开(公告)日：2010-01-28

申请号：US12321096

申请日：2009-01-15

申请人： Styrbjörn Byström ,  Martin Haraldsson ,  Lars Johansson ,  Jan Tejbrant

发明人： Styrbjörn Byström ,  Martin Haraldsson ,  Lars Johansson ,  Jan Tejbrant

IPC分类号： A61K31/445 ,  C07D413/06

CPC分类号： C07D413/06

摘要： The present invention relates to novel isoxazole compounds of formula (I), and pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides thereof, which are modulators of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the preparation of a medicament for the treatment of glaucoma.

摘要翻译： 本发明涉及式（I）的新型异恶唑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，其为1型11β-羟类固醇脱氢酶（11beta-HSD1 ）。 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在制备用于治疗青光眼的药物中的用途。

公开(公告)号：US20190152943A1

公开(公告)日：2019-05-23

申请号：US15772650

申请日：2016-11-11

申请人： Sonia Lain ,  Catherine Drummond ,  Ingeborg van Leeuwen ,  Martin Haraldsson ,  Lars Johansson ,  Lars Sandberg ,  Ulrika Yngve

发明人： Sonia Lain ,  Catherine Drummond ,  Ingeborg van Leeuwen ,  Martin Haraldsson ,  Lars Johansson ,  Lars Sandberg ,  Ulrika Yngve

IPC分类号： C07D401/12 ,  A61P35/00 ,  A61P31/14 ,  A61K45/06 ,  A61K31/4439 ,  C07D417/12 ,  A61K31/427 ,  C07D413/12 ,  A61K31/422 ,  C07D403/12 ,  A61K31/497 ,  C07D405/12 ,  A61K31/416 ,  C07D409/12 ,  C07D471/04 ,  A61K31/437 ,  A61K31/5377 ,  A61K31/506

摘要： There is herein provided a compound of formula I (I) or a pharmaceutically acceptable salt thereof, for use in the treatment of cancer and/or the treatment or prevention of a viral infection, wherein A1, A2, L1, R1, R2 and n have meanings as provided in the description.

公开(公告)号：US06124354A

公开(公告)日：2000-09-26

申请号：US230164

申请日：1999-04-12

申请人： Eva .ANG.kerblom ,  Martin Haraldsson ,  Rolf Johansson ,  Katarina Beierlein ,  Birger Sjoberg ,  Erik Ringberg ,  Birgitta Weinz

发明人： Eva .ANG.kerblom ,  Martin Haraldsson ,  Rolf Johansson ,  Katarina Beierlein ,  Birger Sjoberg ,  Erik Ringberg ,  Birgitta Weinz

IPC分类号： C07D295/08 ,  A61K31/216 ,  A61K31/357 ,  A61K31/381 ,  A61K31/40 ,  A61K31/439 ,  A61K31/445 ,  A61K31/46 ,  A61P1/00 ,  A61P13/00 ,  A61P13/10 ,  C07C219/12 ,  C07D207/12 ,  C07D211/22 ,  C07D317/72 ,  C07D319/18 ,  C07D333/24 ,  C07D409/12 ,  C07D451/06 ,  C07D451/10 ,  C07D451/14 ,  C07D453/02 ,  C07D487/08

CPC分类号： C07D409/12 ,  C07C219/12 ,  C07D207/12 ,  C07D211/22 ,  C07D317/72 ,  C07D333/24 ,  C07D451/06 ,  C07D453/02 ,  C07D487/08 ,  C07C2101/04

摘要： This invention relates to the use of 2-(diisopropylamino)-ethyl-1-phenyl-cyclopentane-carboxylate or 2-(diisopropylamino)-ethyl-1-phenyl-cyclohexane-carboxylate, or a pharmaceutically accceptable salt thereof, for treatment of urinary incontinence or irritable bowel syndrome (IBS).

摘要翻译： PCT No.PCT / SE97 / 01310 Sec。 371日期1999年4月12日 102（e）1999年4月12日PCT PCT 1997年7月23日PCT公布。 第WO98 / 04517号公报 日期：1998年2月5日本发明涉及2-（二异丙基氨基） - 乙基-1-苯基 - 环戊烷羧酸酯或2-（二异丙基氨基） - 乙基-1-苯基 - 环己烷羧酸酯或其药学上可接受的盐 用于治疗尿失禁或肠易激综合征（IBS）。