JP2007500734A5 - - Google Patents
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- Publication number
- JP2007500734A5 JP2007500734A5 JP2006529848A JP2006529848A JP2007500734A5 JP 2007500734 A5 JP2007500734 A5 JP 2007500734A5 JP 2006529848 A JP2006529848 A JP 2006529848A JP 2006529848 A JP2006529848 A JP 2006529848A JP 2007500734 A5 JP2007500734 A5 JP 2007500734A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- carbon atoms
- branched
- linear
- cyclic alkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000004432 carbon atom Chemical group C* 0.000 claims 40
- 125000006165 cyclic alkyl group Chemical group 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 125000002947 alkylene group Chemical group 0.000 claims 6
- 125000004181 carboxyalkyl group Chemical group 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000002577 pseudohalo group Chemical group 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000004414 alkyl thio group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 4
- -1 amino, cyano, amidino, guanidino Chemical group 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 108010091175 Matriptase Proteins 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 102100037942 Suppressor of tumorigenicity 14 protein Human genes 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000005418 aryl aryl group Chemical group 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 238000003745 diagnosis Methods 0.000 claims 1
- 150000002148 esters Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000002243 precursor Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 0 CC(C1OC1*(*)*)N(C)* Chemical compound CC(C1OC1*(*)*)N(C)* 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10322191.3A DE10322191B4 (de) | 2003-05-16 | 2003-05-16 | N-sulfonylierte Aminosäurederivate, Verfahren zu ihrer Herstellung und ihre Verwendung |
| PCT/EP2004/005291 WO2004101507A2 (de) | 2003-05-16 | 2004-05-17 | N-sulfonylierte aminosäurederivate und ihre verwendung als matriptase-inhibitoren |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007500734A JP2007500734A (ja) | 2007-01-18 |
| JP2007500734A5 true JP2007500734A5 (enExample) | 2007-04-19 |
| JP4653100B2 JP4653100B2 (ja) | 2011-03-16 |
Family
ID=33440914
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006529848A Expired - Fee Related JP4653100B2 (ja) | 2003-05-16 | 2004-05-17 | N−スルホニル化アミノ酸誘導体およびマトリプターゼ阻害剤としてのそれらの使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US7772251B2 (enExample) |
| EP (2) | EP1651597A2 (enExample) |
| JP (1) | JP4653100B2 (enExample) |
| AU (1) | AU2004238558A1 (enExample) |
| CA (1) | CA2525886C (enExample) |
| DE (1) | DE10322191B4 (enExample) |
| WO (1) | WO2004101507A2 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE399175T1 (de) * | 2002-03-11 | 2008-07-15 | Curacyte Ag | Hemmstoffe der urokinase, ihre herstellung und verwendung |
| DE10301300B4 (de) | 2003-01-15 | 2009-07-16 | Curacyte Chemistry Gmbh | Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein |
| DE10322191B4 (de) * | 2003-05-16 | 2014-02-27 | The Medicines Company (Leipzig) Gmbh | N-sulfonylierte Aminosäurederivate, Verfahren zu ihrer Herstellung und ihre Verwendung |
| DE10342108A1 (de) * | 2003-09-11 | 2005-04-14 | Curacyte Chemistry Gmbh | Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung |
| JP2008510726A (ja) * | 2004-08-20 | 2008-04-10 | エントレメッド インコーポレイテッド | プロテイナーゼ活性化受容体アンタゴニストを含む組成物および方法 |
| DE102005044319A1 (de) * | 2005-09-16 | 2007-03-22 | Curacyte Chemistry Gmbh | 2-(Aminomethyl)-5-Chlor-Benzylamid-Derivate und ihre Verwendung als Hemmstoffe des Gerinnungsfaktors Xa |
| JP5406722B2 (ja) | 2006-10-16 | 2014-02-05 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | ブラジキニン1受容体モジュレータとしての置換されたスルホンアミド誘導体 |
| DE102006050672A1 (de) * | 2006-10-24 | 2008-04-30 | Curacyte Discovery Gmbh | Hemmstoffe des Plasmins und des Plasmakallikreins |
| DE102007010815B3 (de) | 2007-03-06 | 2008-07-31 | Curacyte Discovery Gmbh | Meta-substituierte Phenylsulfonylamide sekundärer Aminosäureamide, ihre Herstellung und Verwendung als Hemmstoffe der Matriptase |
| JP5260976B2 (ja) * | 2008-02-08 | 2013-08-14 | 東ソー株式会社 | 血液凝固第viii因子c2ドメインタンパク質の製造方法 |
| US8912176B2 (en) | 2009-02-02 | 2014-12-16 | Evotec Ag | Azetidines as histamine H3 receptor antagonists |
| KR20120058468A (ko) | 2009-05-18 | 2012-06-07 | 오리온 코포레이션 | 프로테아제 억제제 |
| US8921319B2 (en) | 2010-07-07 | 2014-12-30 | The Medicines Company (Leipzig) Gmbh | Serine protease inhibitors |
| EP2655399B1 (en) | 2010-12-21 | 2017-09-27 | The Medicines Company (Leipzig) GmbH | Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors iia and xa |
| WO2012162828A1 (en) * | 2011-06-02 | 2012-12-06 | Socpra Sciences Santé Et Humaines S.E.C. | Matriptase inhibitors and uses thereof against orthomyxoviridae infections |
| US11130780B2 (en) | 2015-03-09 | 2021-09-28 | Washington University | Inhibitors of growth factor activation enzymes |
| KR102704242B1 (ko) | 2017-06-20 | 2024-09-09 | 임브리아 파마슈티칼스, 인크. | 심장 대사의 효율을 증가시키기 위한 조성물 및 방법 |
| EP3654968B1 (en) | 2017-07-17 | 2023-08-16 | Merck Sharp & Dohme LLC | Metallo-beta-lactamase inhibitors and methods of use thereof |
| WO2020081361A1 (en) | 2018-10-17 | 2020-04-23 | Imbria Pharmaceuticals, Inc. | Methods of treating rheumatic diseases using trimetazidine-based compounds |
| US11780811B2 (en) | 2020-06-30 | 2023-10-10 | Imbria Pharmaceuticals, Inc. | Methods of synthesizing 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate |
| US11530184B2 (en) | 2020-06-30 | 2022-12-20 | Imbria Pharmaceuticals, Inc. | Crystal forms of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate |
| US11883396B2 (en) | 2021-05-03 | 2024-01-30 | Imbria Pharmaceuticals, Inc. | Methods of treating kidney conditions using modified forms of trimetazidine |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3942114C2 (de) * | 1988-12-26 | 1997-09-04 | Hiroyoshi Hidaka | Verbindungen mit einer Wirkung für eine gleichmäßige Gefäßmuskelentspannung und pharmazeutische Zusammensetzung, die diese enthält |
| WO1992008709A1 (de) | 1990-11-15 | 1992-05-29 | Pentapharm Ag | Meta-substituierte phenylalanin-derivate |
| US5607937A (en) * | 1993-02-10 | 1997-03-04 | Pentapharm Ag | Piperazides of substituted phenylalanine derivatives as thrombin inhibitors |
| CH689611A5 (de) | 1995-03-01 | 1999-07-15 | Pentapharm Ag | Urokinase-Inhibitoren. |
| EP1264828B1 (de) * | 1998-07-20 | 2004-04-14 | Wilex AG | Urokinase-Inhibitoren |
| EP1114024B1 (de) | 1998-09-18 | 2002-11-27 | Pentapharm A.G. | Urokinase-inhibitoren |
| US6797504B1 (en) | 2000-09-08 | 2004-09-28 | Dendreon San Diego Llc | Inhibitors of serine protease activity of matriptase or MTSP1 |
| EP1355637A2 (en) | 2000-06-21 | 2003-10-29 | Georgetown University Medical Center | Inhibitors of matriptase for the treatment of cancer |
| AU2003206945A1 (en) * | 2002-02-22 | 2003-09-09 | Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften E.V. | Use of proteinase inhibitors in the treatment of autoimmune diseases |
| DE10322191B4 (de) * | 2003-05-16 | 2014-02-27 | The Medicines Company (Leipzig) Gmbh | N-sulfonylierte Aminosäurederivate, Verfahren zu ihrer Herstellung und ihre Verwendung |
-
2003
- 2003-05-16 DE DE10322191.3A patent/DE10322191B4/de not_active Expired - Fee Related
-
2004
- 2004-05-17 EP EP04733311A patent/EP1651597A2/de not_active Withdrawn
- 2004-05-17 US US10/555,821 patent/US7772251B2/en not_active Expired - Fee Related
- 2004-05-17 AU AU2004238558A patent/AU2004238558A1/en not_active Abandoned
- 2004-05-17 CA CA2525886A patent/CA2525886C/en not_active Expired - Fee Related
- 2004-05-17 WO PCT/EP2004/005291 patent/WO2004101507A2/de not_active Ceased
- 2004-05-17 EP EP10013067A patent/EP2316830A3/de not_active Withdrawn
- 2004-05-17 JP JP2006529848A patent/JP4653100B2/ja not_active Expired - Fee Related
-
2010
- 2010-07-01 US US12/829,185 patent/US20110002992A1/en not_active Abandoned
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