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1. 发明授权

US5556855A N-heterocyclic substituted salicylic acids 失效
标题翻译： N-杂环取代的水杨酸
公开(公告)号：US5556855A
公开(公告)日：1996-09-17
申请号：US365869
申请日：1994-12-29
申请人： Hubert Agback , Leif Ahrgren , Thomas Berglindh , Martin Haraldsson , G oran Smedeg.ang.rd , Lars-Inge Olsson
发明人： Hubert Agback , Leif Ahrgren , Thomas Berglindh , Martin Haraldsson , G oran Smedeg.ang.rd , Lars-Inge Olsson
IPC分类号： A61K31/41 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/50 , A61K31/505 , A61K31/603 , A61P1/00 , A61P29/00 , A61P37/02 , A61P37/06 , C07D213/75 , C07D213/76 , C07D213/78 , C07D233/88 , C07D233/90 , C07D237/20 , C07D239/42 , C07D239/69 , C07D241/20 , C07D249/12 , C07D249/14 , C07D261/14 , C07D261/16 , C07D263/28 , C07D277/20 , C07D277/22 , C07D277/32 , C07D277/38 , C07D277/82
CPC分类号： C07D213/76 , C07D237/20 , C07D239/42 , C07D261/16 , C07D277/82
摘要： A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomic form, salts, solvates, C.sub.1-6 alkyl esters and pharmaceutical compositions of the compound. Ph.sup.1 and Ph.sup.2 are benzene rings with the proviso that carboxy and hydroxy are ortho to one another. Het includes an optionally substituted heterocyclic ring which includes conjugated double bonds and binds to nitrogen in NR. The compound is characterized in that A is a bridge which is stable against reduction because it is not azo, and in that R is hydrogen or lower alkyl.The invention also includes the preparation of the compound and its use as a drug, particularly for treating autoimmune diseases.
摘要翻译：式Het-NR-SO2-Ph2-A-Ph1（COOH）（OH）和互变异构形式的化合物，盐，溶剂合物，C 1-6烷基酯和该化合物的药物组合物。 Ph1和Ph2是苯环，条件是羧基和羟基彼此邻接。 Het包括任选取代的杂环，其包括共轭双键并与NR结合。该化合物的特征在于A是不是偶氮还原反应稳定的桥，其中R是氢或低级烷基。本发明还包括该化合物的制备及其作为药物的用途，特别是用于治疗自身免疫性疾病。

2. 发明授权

US5403930A Substituted salicylic acids 失效
标题翻译：取代水杨酸
公开(公告)号：US5403930A
公开(公告)日：1995-04-04
申请号：US132874
申请日：1993-10-07
申请人： Hubert Agback , Leif Ahrgren , Thomas Berglindh , Martin Haraldsson , Goran Smedeg.ang.rd , Lars-Inge Olsson
发明人： Hubert Agback , Leif Ahrgren , Thomas Berglindh , Martin Haraldsson , Goran Smedeg.ang.rd , Lars-Inge Olsson
IPC分类号： A61K31/41 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/50 , A61K31/505 , A61K31/603 , A61P1/00 , A61P29/00 , A61P37/02 , A61P37/06 , C07D213/75 , C07D213/76 , C07D213/78 , C07D233/88 , C07D233/90 , C07D237/20 , C07D239/42 , C07D239/69 , C07D241/20 , C07D249/12 , C07D249/14 , C07D261/14 , C07D261/16 , C07D263/28 , C07D277/20 , C07D277/22 , C07D277/32 , C07D277/38 , C07D277/82 , C07D237/26 , C07D211/56
CPC分类号： C07D213/76 , C07D237/20 , C07D239/42 , C07D261/16 , C07D277/82
摘要： A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomic form, salts, solvates, C.sub.1-6 alkyl esters and pharmaceutical compositions of the compound. Ph.sup.1 and Ph.sup.2 are benzene rings with the proviso that carboxy and hydroxy are ortho to one another. Het includes an optionally substituted heterocyclic ring which includes conjugated double bonds and binds to nitrogen in NR. The compound is characterized in that A is a bridge which is stable against reduction because it is not azo, and in that R is hydrogen or lower alkyl.The invention also includes the preparation of the compound and its use as a drug, particularly for treating autoimmune diseases.
摘要翻译：式Het-NR-SO2-Ph2-A-Ph1（COOH）（OH）和互变异构形式的化合物，盐，溶剂合物，C 1-6烷基酯和该化合物的药物组合物。 Ph1和Ph2是苯环，条件是羧基和羟基彼此邻接。 Het包括任选取代的杂环，其包括共轭双键并与NR结合。该化合物的特征在于A是不是偶氮还原反应稳定的桥，其中R是氢或低级烷基。本发明还包括该化合物的制备及其作为药物的用途，特别是用于治疗自身免疫性疾病。

3. 发明授权

US5302718A Compounds containing an amino salicylic acid moiety linked to a sulphapyridine moiety via stable bridge 失效
标题翻译：含有氨基水杨酸部分的化合物通过稳定的桥连接到磺酰吡啶部分
公开(公告)号：US5302718A
公开(公告)日：1994-04-12
申请号：US973753
申请日：1992-11-09
申请人： Hubert Agback , Leif Ahrgren , Thomas Berglindh , Martin Haraldsson , Goran Smedegard , Lars-Inge Olsson
发明人： Hubert Agback , Leif Ahrgren , Thomas Berglindh , Martin Haraldsson , Goran Smedegard , Lars-Inge Olsson
IPC分类号： A61K31/41 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/50 , A61K31/505 , A61K31/603 , A61P1/00 , A61P29/00 , A61P37/02 , A61P37/06 , C07D213/75 , C07D213/76 , C07D213/78 , C07D233/88 , C07D233/90 , C07D237/20 , C07D239/42 , C07D239/69 , C07D241/20 , C07D249/12 , C07D249/14 , C07D261/14 , C07D261/16 , C07D263/28 , C07D277/20 , C07D277/22 , C07D277/32 , C07D277/38 , C07D277/82 , C07D237/26 , C07D211/56
CPC分类号： C07D213/76 , C07D237/20 , C07D239/42 , C07D261/16 , C07D277/82
摘要： A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomeric form, salts, solvates, C.sub.1-6 alkyl esters and pharmaceutical compositions of the compound. Ph.sup.1 and Ph.sup.2 are benzene rings with the proviso that carboxy and hydroxy are ortho to one another. Het includes an optionally substituted heterocyclic ring which includes conjugated double bonds and binds to nitrogen in NR. The compound is characterized in that A is a bridge which is stable against reduction because it is not azo, and in that R is hydrogen or lower alkyl.The invention also includes the preparation of the compound and its use as a drug, particularly for treating autoimmune diseases.
摘要翻译：式Het-NR-SO2-Ph2-A-Ph1（COOH）（OH）和互变异构形式的化合物，盐，溶剂合物，C 1-6烷基酯和该化合物的药物组合物。 Ph1和Ph2是苯环，条件是羧基和羟基彼此邻接。 Het包括任选取代的杂环，其包括共轭双键并与NR结合。该化合物的特征在于，A是不是偶氮的还原反应稳定的桥，其中R是氢或低级烷基。本发明还包括该化合物的制备及其作为药物的用途，特别是用于治疗自身免疫性疾病。

4. 发明申请

US20130102587A1 New Enzyme Inhibitor Compounds 有权
标题翻译：新型酶抑制剂化合物
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。

5. 发明授权

US06124354A Arylcycloalkane carboxylic esters, their use, pharmaceutical compositions and preparation 失效
标题翻译：芳基环烷羧酸酯，其用途，药物组合物和制剂
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）。

6. 发明授权

US09227967B2 Inhibitor compounds of semicarbazide-sensitive amine oxidases 有权
标题翻译：氨基脲敏感性胺氧化酶抑制剂化合物
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。

7. 发明申请

US20100022590A1 Novel compounds 审中-公开
标题翻译：新型化合物
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。

8. 发明申请

US20190152943A1 TETRAHYDROINDAZOLES AND MEDICAL USES THEREOF 审中-公开
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.

9. 发明申请

US20120010188A1 Imidazopyridine Compounds 审中-公开
标题翻译：咪唑并吡啶化合物
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。

10. 发明授权

US09150574B2 Enzyme inhibitor compounds 有权
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.

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