JP4809570B2 - 第ＶＩＩａ因子阻害剤である（チオ）尿素誘導体、その製造方法およびその使用 - Google Patents

第ＶＩＩａ因子阻害剤である（チオ）尿素誘導体、その製造方法およびその使用 Download PDF

Info

Publication number
JP4809570B2
JP4809570B2 JP2002501818A JP2002501818A JP4809570B2 JP 4809570 B2 JP4809570 B2 JP 4809570B2 JP 2002501818 A JP2002501818 A JP 2002501818A JP 2002501818 A JP2002501818 A JP 2002501818A JP 4809570 B2 JP4809570 B2 JP 4809570B2
Authority
JP
Japan
Prior art keywords
group
compound
formula
het
aryl
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
JP2002501818A
Other languages
English (en)
Japanese (ja)
Other versions
JP2003535844A (ja
JP2003535844A5 (OSRAM
Inventor
オトマール・クリングラー
マンフレート・シュードック
ハンス−ペーター・ネストラー
ハンス・マター
ヘルマン・シュロイダー
Original Assignee
サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング
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 サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング filed Critical サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング
Publication of JP2003535844A publication Critical patent/JP2003535844A/ja
Publication of JP2003535844A5 publication Critical patent/JP2003535844A5/ja
Application granted granted Critical
Publication of JP4809570B2 publication Critical patent/JP4809570B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/42—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96—Sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18—Fluorenes; Hydrogenated fluorenes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
JP2002501818A 2000-06-06 2001-05-26 第ＶＩＩａ因子阻害剤である（チオ）尿素誘導体、その製造方法およびその使用 Expired - Fee Related JP4809570B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP00112116A EP1162194A1 (en) 2000-06-06 2000-06-06 Factor VIIa inhibitory (thio)urea derivatives, their preparation and their use
EP00112116.9 2000-06-06
PCT/EP2001/006029 WO2001094301A2 (en) 2000-06-06 2001-05-26 Factor viia inhibitory (thio)urea derivatives, their preparation and their use

Publications (3)

Publication Number Publication Date
JP2003535844A JP2003535844A (ja) 2003-12-02
JP2003535844A5 JP2003535844A5 (OSRAM) 2008-05-15
JP4809570B2 true JP4809570B2 (ja) 2011-11-09

Family

ID=8168926

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2002501818A Expired - Fee Related JP4809570B2 (ja) 2000-06-06 2001-05-26 第ＶＩＩａ因子阻害剤である（チオ）尿素誘導体、その製造方法およびその使用

Country Status (29)

Country Link
US (1) US6743790B2 (OSRAM)
EP (2) EP1162194A1 (OSRAM)
JP (1) JP4809570B2 (OSRAM)
KR (1) KR101011345B1 (OSRAM)
CN (1) CN1208314C (OSRAM)
AR (1) AR030936A1 (OSRAM)
AU (2) AU7749401A (OSRAM)
BR (1) BR0111264A (OSRAM)
CA (1) CA2410862C (OSRAM)
CZ (1) CZ20023963A3 (OSRAM)
DE (1) DE60139320D1 (OSRAM)
DK (1) DK1299354T3 (OSRAM)
EE (1) EE200200617A (OSRAM)
ES (1) ES2330412T3 (OSRAM)
HR (1) HRP20020961A2 (OSRAM)
HU (1) HUP0301631A2 (OSRAM)
IL (2) IL153220A0 (OSRAM)
MX (1) MXPA02009789A (OSRAM)
MY (1) MY129363A (OSRAM)
NO (1) NO328546B1 (OSRAM)
NZ (1) NZ522960A (OSRAM)
PL (1) PL359584A1 (OSRAM)
PT (1) PT1299354E (OSRAM)
RU (1) RU2286337C2 (OSRAM)
SK (1) SK17032002A3 (OSRAM)
TW (1) TWI283662B (OSRAM)
WO (1) WO2001094301A2 (OSRAM)
YU (1) YU89202A (OSRAM)
ZA (1) ZA200209018B (OSRAM)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2483228C (en) 2002-04-27 2011-07-05 Merck Patent Gesellschaft Mit Beschraenkter Haftung Carboxamides
JP2005535710A (ja) * 2002-08-09 2005-11-24 トランス　テック　ファーマ，インコーポレイテッド アリールおよびヘテロアリール化合物ならびに凝固を調節する方法
AU2004249671A1 (en) * 2003-05-20 2004-12-29 Genentech, Inc. Benzofuran inhibitors of factor VIIa
WO2004113278A2 (en) * 2003-05-20 2004-12-29 Genentech, Inc. Acylsulfamide inhibitors of factor viia
US7208601B2 (en) * 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
JP2007501844A (ja) * 2003-08-08 2007-02-01 トランス　テック　ファーマ，インコーポレイテッド アリール及びヘテロアリール化合物、組成物並びに使用方法
WO2005014532A1 (en) * 2003-08-08 2005-02-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions and methods of use
JP4478157B2 (ja) * 2004-10-13 2010-06-09 エーザイ・アール・アンド・ディー・マネジメント株式会社 ヒドラジド誘導体
TW200630337A (en) * 2004-10-14 2006-09-01 Euro Celtique Sa Piperidinyl compounds and the use thereof
WO2006089952A1 (en) * 2005-02-24 2006-08-31 Novo Nordisk Health Care Ag Amidino-compounds por stabilizing factor vii polypeptide formulations
JP2008531525A (ja) * 2005-02-24 2008-08-14 ノボ ノルディスク ヘルス ケア アクチェンゲゼルシャフト Ｖｉｉ因子ポリペプチド製剤を安定化する化合物
JP2008531524A (ja) * 2005-02-24 2008-08-14 ノボ ノルディスク ヘルス ケア アクチェンゲゼルシャフト Ｖｉｉ因子ポリペプチド製剤を安定化する化合物
ES2553160T3 (es) 2005-06-17 2015-12-04 Novo Nordisk Health Care Ag Reducción y derivatización selectivas de proteínas Factor VII transformadas por ingeniería que comprenden al menos una cisteína no nativa
KR101362024B1 (ko) 2006-03-24 2014-02-11 에자이 알앤드디 매니지먼트 가부시키가이샤 트리아졸론 유도체
US8247442B2 (en) * 2006-03-29 2012-08-21 Purdue Pharma L.P. Benzenesulfonamide compounds and their use
WO2007118854A1 (en) * 2006-04-13 2007-10-25 Euro-Celtique S.A. Benzenesulfonamide compounds and the use thereof
US8791264B2 (en) * 2006-04-13 2014-07-29 Purdue Pharma L.P. Benzenesulfonamide compounds and their use as blockers of calcium channels
US8399486B2 (en) * 2007-04-09 2013-03-19 Purdue Pharma L.P. Benzenesulfonyl compounds and the use thereof
US7807690B2 (en) * 2007-09-21 2010-10-05 Eisai R&D Management Co., Ltd. 2,3-dihydro-iminoisoindole derivatives
WO2009040659A2 (en) * 2007-09-28 2009-04-02 Purdue Pharma L.P. Benzenesulfonamide compounds and the use thereof
AU2012329098B2 (en) 2011-10-26 2017-08-03 Allergan, Inc. Amide derivatives of N-urea substituted amino acids as formyl peptide receptor like-1 (FPRL-1) receptor modulators
CN104302630A (zh) * 2012-04-16 2015-01-21 阿勒根公司 作为甲酰肽受体2调节剂的(2-脲基乙酰氨基)烷基衍生物
EP2906236A1 (en) * 2012-10-10 2015-08-19 Novo Nordisk Health Care AG Liquid pharmaceutical composition of factor vii polypeptide
CA3114477A1 (en) 2013-03-06 2014-09-12 Allergan, Inc. Use of agonists of formyl peptide receptor 2 for treating dermatological diseases
KR102290134B1 (ko) 2013-03-06 2021-08-17 알러간, 인코포레이티드 안구 염증성 질환을 치료하기 위한 포르밀 펩타이드 수용체 2의 작용제의 용도

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5273982A (en) * 1990-03-09 1993-12-28 Hoffmann-La Roche Inc. Acetic acid derivatives
US5506134A (en) 1990-10-22 1996-04-09 Corvas International, Inc. Hypridoma and monoclonal antibody which inhibits blood coagulation tissue factor/factor VIIa complex
JPH06505978A (ja) * 1991-02-05 1994-07-07 スミスクライン・ビーチャム・コーポレイション 芳香族エステルまたはアミドを含有する抗凝集性ペプチド
US5788965A (en) 1991-02-28 1998-08-04 Novo Nordisk A/S Modified factor VII
US5833982A (en) 1991-02-28 1998-11-10 Zymogenetics, Inc. Modified factor VII
JP3387948B2 (ja) * 1992-12-04 2003-03-17 富山化学工業株式会社 新規なフェニルアラニン誘導体またはその塩
US5314902A (en) 1993-01-27 1994-05-24 Monsanto Company Urea derivatives useful as platelet aggregation inhibitors
DE4309867A1 (de) * 1993-03-26 1994-09-29 Cassella Ag Neue Harnstoffderivate, ihre Herstellung und Verwendung
GB9313269D0 (en) * 1993-06-28 1993-08-11 Zeneca Ltd Allophanic acid derivatives
GB9313268D0 (en) * 1993-06-28 1993-08-11 Zeneca Ltd Chemical compounds
WO1995008550A1 (en) * 1993-09-24 1995-03-30 Abbott Laboratories Endothelin antagonists
CA2174516A1 (en) * 1993-10-19 1995-04-27 Yoshiharu Ikeda 2,3-diaminopropionic acid derivative
US5674894A (en) * 1995-05-15 1997-10-07 G.D. Searle & Co. Amidine derivatives useful as platelet aggregation inhibitors and vasodilators
EP0880320A4 (en) * 1996-01-30 1999-06-16 Merck & Co Inc FARNESYL-PROTEIN TRANSFERASE INHIBITORS
IL135488A0 (en) * 1997-11-18 2001-05-20 Teijin Ltd Cyclic amine derivatives
EP0987274A1 (en) * 1998-09-15 2000-03-22 Hoechst Marion Roussel Deutschland GmbH Factor VIIa Inhibitors

Also Published As

Publication number Publication date
ES2330412T3 (es) 2009-12-10
PL359584A1 (en) 2004-08-23
KR101011345B1 (ko) 2011-01-28
WO2001094301A2 (en) 2001-12-13
AR030936A1 (es) 2003-09-03
YU89202A (sh) 2006-05-25
JP2003535844A (ja) 2003-12-02
NZ522960A (en) 2004-05-28
AU2001277494B2 (en) 2006-05-04
US6743790B2 (en) 2004-06-01
US20020052417A1 (en) 2002-05-02
NO20025810D0 (no) 2002-12-03
IL153220A0 (en) 2003-07-06
DK1299354T3 (da) 2009-11-16
EP1299354B1 (en) 2009-07-22
EE200200617A (et) 2004-04-15
HUP0301631A2 (hu) 2003-09-29
SK17032002A3 (sk) 2003-05-02
CZ20023963A3 (cs) 2003-03-12
EP1162194A1 (en) 2001-12-12
ZA200209018B (en) 2003-10-08
IL153220A (en) 2008-11-03
MY129363A (en) 2007-03-30
AU7749401A (en) 2001-12-17
KR20030007911A (ko) 2003-01-23
CA2410862A1 (en) 2001-12-13
BR0111264A (pt) 2003-06-17
MXPA02009789A (es) 2003-03-12
CA2410862C (en) 2009-11-10
NO20025810L (no) 2002-12-03
NO328546B1 (no) 2010-03-15
EP1299354A2 (en) 2003-04-09
TWI283662B (en) 2007-07-11
HK1055941A1 (en) 2004-01-30
WO2001094301A3 (en) 2002-04-04
RU2286337C2 (ru) 2006-10-27
DE60139320D1 (de) 2009-09-03
CN1208314C (zh) 2005-06-29
CN1427818A (zh) 2003-07-02
PT1299354E (pt) 2009-10-01
HRP20020961A2 (en) 2004-12-31

Similar Documents

Publication Publication Date Title
JP4809570B2 (ja) 第ＶＩＩａ因子阻害剤である（チオ）尿素誘導体、その製造方法およびその使用
AU2001277494A1 (en) Factor viia inhibitory (thio)urea derivatives, their preparation and their use
JP4274522B2 (ja) Ｘａ因子阻害剤としてのグアニジンおよびアミジン誘導体
US6664393B2 (en) N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
JP5016178B2 (ja) 抗血栓活性を有するマロンアミドおよびマロンアミド酸エステル誘導体、それらの製造および使用
SK17592001A3 (sk) Inhibítory faktora VIIa, spôsob ich prípravy a farmaceutická kompozícia, ktorá ich obsahuje
AU2001293824A1 (en) Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation and their use

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20080319

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20080319

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20090929

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20101222

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20110104

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20110401

RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7422

Effective date: 20110401

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20110411

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110624

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: 20110726

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: 20110819

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

Free format text: PAYMENT UNTIL: 20140826

Year of fee payment: 3

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees