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 (https=) | 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 (https=) |
| EP (2) | EP2316830A3 (https=) |
| JP (1) | JP4653100B2 (https=) |
| AU (1) | AU2004238558A1 (https=) |
| CA (1) | CA2525886C (https=) |
| DE (1) | DE10322191B4 (https=) |
| WO (1) | WO2004101507A2 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7838560B2 (en) * | 2002-03-11 | 2010-11-23 | The Medicines Company (Leipzig) Gmbh | Urokinase inhibitors, production and use thereof |
| 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 |
| US20060063930A1 (en) * | 2004-08-20 | 2006-03-23 | Agoston Gregory E | Compositions and methods comprising proteinase activated receptor antagonists |
| 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 |
| EP2086935A1 (de) | 2006-10-16 | 2009-08-12 | Grünenthal GmbH | Substituierte sulfonamid-derivate als bradykinin 1 rezeptor modulatoren |
| 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 |
| WO2010086403A1 (en) | 2009-02-02 | 2010-08-05 | Evotec Neurosciences Gmbh | Azetidines as histamine h3 receptor antagonists |
| US8722930B2 (en) | 2009-05-18 | 2014-05-13 | Orion Corporation | Protease inhibitors |
| EP2590945B1 (en) | 2010-07-07 | 2014-04-30 | 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 |
| EP2714716B1 (en) | 2011-06-02 | 2018-04-11 | Socpra Sciences Santé Et Humaines S.E.C. | Matriptase inhibitors and uses thereof against orthomyxoviridae infections |
| WO2016144654A1 (en) | 2015-03-09 | 2016-09-15 | Washington University | Inhibitors of growth factor activation enzymes |
| EP4092013A1 (en) | 2017-06-20 | 2022-11-23 | Imbria Pharmaceuticals, Inc. | Compositions and methods for increasing efficiency of cardiac metabolism |
| WO2019018186A1 (en) | 2017-07-17 | 2019-01-24 | Merck Sharp & Dohme Corp. | 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 |
| WO2020243120A1 (en) | 2019-05-31 | 2020-12-03 | Imbria Pharmaceuticals, Inc. | Methods of treating fibrosis using compounds that promote glucose oxidation |
| 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 |
| CA2073776A1 (en) | 1990-11-15 | 1992-05-16 | Joerg Stuerzebecher | Meta-substituted phenyl alanine derivatives |
| JPH07509731A (ja) * | 1993-02-10 | 1995-10-26 | ペンタファルム アクチェンゲゼルシャフト | トロンビン阻害剤としての置換されたフェニルアラニン誘導体のピペラジド |
| CH689611A5 (de) * | 1995-03-01 | 1999-07-15 | Pentapharm Ag | Urokinase-Inhibitoren. |
| ATE264103T1 (de) * | 1998-07-20 | 2004-04-15 | Wilex Ag | Urokinase-inhibitoren |
| ES2188003T3 (es) | 1998-09-18 | 2003-06-16 | Pentapharm Ag | Inhibidores de la uroquinasa. |
| US6797504B1 (en) | 2000-09-08 | 2004-09-28 | Dendreon San Diego Llc | Inhibitors of serine protease activity of matriptase or MTSP1 |
| WO2001097794A2 (en) | 2000-06-21 | 2001-12-27 | Georgetown University | 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 EP10013067A patent/EP2316830A3/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 EP EP04733311A patent/EP1651597A2/de not_active Withdrawn
- 2004-05-17 JP JP2006529848A patent/JP4653100B2/ja not_active Expired - Fee Related
- 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
-
2010
- 2010-07-01 US US12/829,185 patent/US20110002992A1/en not_active Abandoned
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