JP4653100B2 - 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 - Google Patents

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 Download PDF

Info

Publication number
JP4653100B2
JP4653100B2 JP2006529848A JP2006529848A JP4653100B2 JP 4653100 B2 JP4653100 B2 JP 4653100B2 JP 2006529848 A JP2006529848 A JP 2006529848A JP 2006529848 A JP2006529848 A JP 2006529848A JP 4653100 B2 JP4653100 B2 JP 4653100B2
Authority
JP
Japan
Prior art keywords
group
carbon atoms
compound
general structure
branched
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.)
Expired - Fee Related
Application number
JP2006529848A
Other languages
English (en)
Japanese (ja)
Other versions
JP2007500734A5 (enExample
JP2007500734A (ja
Inventor
シュテュルツェベヒャー，イェルク
シュタインメツァー，トルステン
シュヴァイニッツ，アンドレア
シュテュルツェベヒャー，アンヌ
ウーラント，ケルスティン
Original Assignee
キュラサイト・ケミストリー・ゲーエムベーハー
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by キュラサイト・ケミストリー・ゲーエムベーハー filed Critical キュラサイト・ケミストリー・ゲーエムベーハー
Publication of JP2007500734A publication Critical patent/JP2007500734A/ja
Publication of JP2007500734A5 publication Critical patent/JP2007500734A5/ja
Application granted granted Critical
Publication of JP4653100B2 publication Critical patent/JP4653100B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2006529848A 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 Expired - Fee Related JP4653100B2 (ja)

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 JP2007500734A5 (enExample) 2007-04-19
JP4653100B2 true 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) EP2316830A3 (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 (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003219039A1 (en) * 2002-03-11 2003-09-22 Curacyte Ag 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
CA2576971A1 (en) * 2004-08-20 2006-03-02 Entremed, Inc. 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
EP2391617B1 (en) 2009-02-02 2015-11-11 Evotec AG Azetidines as histamine h3 receptor antagonists
SG175711A1 (en) 2009-05-18 2011-12-29 Orion Corp Protease inhibitors
ES2483802T3 (es) 2010-07-07 2014-08-07 The Medicines Company (Leipzig) Gmbh Inhibidores de serina proteasa
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
US11130780B2 (en) 2015-03-09 2021-09-28 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
EP3654968B1 (en) 2017-07-17 2023-08-16 Merck Sharp & Dohme LLC Metallo-beta-lactamase inhibitors and methods of use thereof
US12318382B2 (en) 2018-10-17 2025-06-03 Imbria Pharmaceuticals, Inc. Methods of treating rheumatic diseases using trimetazidine-based compounds
EP3976101A4 (en) 2019-05-31 2023-06-21 Imbria Pharmaceuticals, Inc. FIBROSIS TREATMENT METHODS USING COMPOUNDS THAT PROMOTE GLUCOSE OXIDATION
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
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
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)

* Cited by examiner, † Cited by third party
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
KR920703558A (ko) 1990-11-15 1992-12-18 원본미기재 메타-치환 페닐알라닌 유도체
WO1994018185A1 (de) * 1993-02-10 1994-08-18 Pentapharm Ag Piperazide von substituierten phenylalanin-derivativen als thrombin inhibitoren
CH689611A5 (de) * 1995-03-01 1999-07-15 Pentapharm Ag Urokinase-Inhibitoren.
BR9912327B1 (pt) * 1998-07-20 2013-11-12 Inibidores da uroquinase
US7745441B1 (en) 1998-09-18 2010-06-29 Wilex Ag Urokinase inhibitors
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

Also Published As

Publication number Publication date
EP2316830A2 (de) 2011-05-04
DE10322191B4 (de) 2014-02-27
US20070055065A1 (en) 2007-03-08
CA2525886C (en) 2013-01-08
JP2007500734A (ja) 2007-01-18
DE10322191A1 (de) 2004-12-09
WO2004101507A2 (de) 2004-11-25
WO2004101507A3 (de) 2006-03-23
US7772251B2 (en) 2010-08-10
US20110002992A1 (en) 2011-01-06
EP1651597A2 (de) 2006-05-03
AU2004238558A1 (en) 2004-11-25
CA2525886A1 (en) 2004-11-25
EP2316830A3 (de) 2011-08-17

Similar Documents

Publication Publication Date Title
US20110002992A1 (en) N-sulphonylated amino acid derivatives, method for the production and use thereof
US6262069B1 (en) 1-amino-7-isoquinoline derivatives as serine protease inhibitors
US7928137B2 (en) Meta-benzamidine derivatives as serine protease inhibitors
US6794507B2 (en) Compounds that inhibit factor Xa activity
CA2282399A1 (en) Thioaryl sulfonamide hydroxamic acid compounds
CA2355281A1 (en) Thrombin inhibitors
EP3297992B1 (en) Heterocyclicalkyl derivative compounds as selective histone deacetylase inhibitors and pharmaceutical compositions comprising the same
EP0822934B1 (en) Antithrombotic amidinotetrahydropyridylalanine derivatives
AU758237B2 (en) Thrombin inhibitors
JPH08301833A (ja) 選択的トロンビン抑制剤
AU4412701A (en) Arginine mimetics as factor xa inhibitors
JP2013503829A (ja) 特に医薬に使用するための新規な多機能ペプチダーゼインヒビター
US8569313B2 (en) Meta-substituted phenyl sulfonyl amides of secondary amino acid amides, the production thereof, and use thereof as matriptase inhibitors
JP4942481B2 (ja) 凝固因子Ｘａ阻害剤として用いるための塩基−置換ベンジルアミン類似体、それらの製法および使用
JP2004525134A (ja) ウロキナーゼ阻害剤
JPH03505583A (ja) 抗高血圧剤としてのアミノアルキルアミノカルボニルアミノジオールアミノ酸誘導体
MXPA00004241A (es) Nuevos compuestos de 2,3-metano-amino acido, un proceso para su preparacion y composiciones farmaceuticas que los contienen.
CA2369109A1 (en) Thrombin inhibitors
US20050267127A1 (en) Guanidino phenylalanin compounds used as urokinase inhibitors
CA2374654A1 (en) Thrombin inhibitors
CA2303832A1 (en) Thrombin inhibitors
EP3381907A1 (en) Symmetrical 2-aminophenyl-benzazolyl-5-acetate compounds and their use as anti-heparanase
JP2004523560A5 (enExample)

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20070301

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20070301

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20100422

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20100421

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20100721

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20100728

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20100823

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20100830

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20100917

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20100928

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20101022

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20101022

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20101117

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20101216

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20131224

Year of fee payment: 3

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20131224

Year of fee payment: 3

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313111

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20131224

Year of fee payment: 3

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees