BR9916678A - Inibidores de trombina - Google Patents

Inibidores de trombina

Info

Publication number
BR9916678A
BR9916678A BR9916678-0A BR9916678A BR9916678A BR 9916678 A BR9916678 A BR 9916678A BR 9916678 A BR9916678 A BR 9916678A BR 9916678 A BR9916678 A BR 9916678A
Authority
BR
Brazil
Prior art keywords
thrombin inhibitors
relates
anticoagulants
useful
formula
Prior art date
Application number
BR9916678-0A
Other languages
English (en)
Inventor
Koo Lee
Won Hyuk Jung
Cheol Won Park
Sang Koo Lee
Sun Hwa Lee
Hee Dong Park
Original Assignee
Lg Ci Ltd
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 Lg Ci Ltd filed Critical Lg Ci Ltd
Publication of BR9916678A publication Critical patent/BR9916678A/pt

Links

Classifications

    • 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
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • C07D205/085—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams with a nitrogen atom directly attached in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
    • C07K5/0222—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2 with the first amino acid being heterocyclic, e.g. Pro, Trp
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Saccharide Compounds (AREA)

Abstract

Patente de Invenção: <B>"INIBIDORES DE TROMBINA"<D>. A presente invenção refere-se a inibidores de trombina da fórmula (I), em que A, B, C, D, E, F e n têm o significado dado na descrição, que são úteis como anticoagulantes. Em particular, esta invenção refere-se a derivados de peptídeo tendo alta atividade antitrombótica e alta biodisponibilidade oral.
BR9916678-0A 1998-12-29 1999-12-29 Inibidores de trombina BR9916678A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
KR19980060266 1998-12-29
KR1019990033490A KR20000047461A (ko) 1998-12-29 1999-08-14 트롬빈 억제제
PCT/KR1999/000830 WO2000039124A1 (en) 1998-12-29 1999-12-29 Thrombin inhibitors

Publications (1)

Publication Number Publication Date
BR9916678A true BR9916678A (pt) 2001-10-16

Family

ID=26634497

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9916678-0A BR9916678A (pt) 1998-12-29 1999-12-29 Inibidores de trombina

Country Status (22)

Country Link
US (2) US6492402B1 (pt)
EP (1) EP1140918B1 (pt)
JP (1) JP3847092B2 (pt)
KR (2) KR20000047461A (pt)
CN (1) CN1149210C (pt)
AT (1) ATE273305T1 (pt)
AU (1) AU765417B2 (pt)
BR (1) BR9916678A (pt)
CA (1) CA2355281A1 (pt)
CZ (1) CZ20012429A3 (pt)
DE (1) DE69919397T2 (pt)
DK (1) DK1140918T3 (pt)
ES (1) ES2226482T3 (pt)
HK (1) HK1044936A1 (pt)
HU (1) HUP0104500A3 (pt)
IL (1) IL143545A (pt)
NO (1) NO321739B1 (pt)
NZ (1) NZ513174A (pt)
RU (1) RU2221808C2 (pt)
TR (1) TR200101899T2 (pt)
WO (1) WO2000039124A1 (pt)
ZA (1) ZA200104780B (pt)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ515026A (en) * 1999-04-09 2003-10-31 Abbott Gmbh & Co Heterocyclic amidine derivatives useful as prodrugs of thrombin inhibitors
DE19934066A1 (de) * 1999-07-23 2001-01-25 Basf Ag Verfahren zur Herstellung von 4-Cyano-2-aminomethylthiazol
DE19933861A1 (de) 1999-07-23 2001-01-25 Basf Ag Verfahren zur Herstellung von 2-Aminomethyl-4-cyano-thiazol
DE10049937A1 (de) * 2000-10-06 2002-04-11 Knoll Ag Niedermolekulare Inhibitoren von Serinproteasen mit Polyhydroxyalkyl- und Polyhydroxycycloalkylresten
KR100447421B1 (ko) * 2001-04-04 2004-09-07 주식회사 엘지생명과학 5-(아미노메틸)-2-티오펜카보니트릴 염산염의 연속반응에의한 새로운 제조방법
US20050113309A1 (en) * 2002-03-22 2005-05-26 Aeri Kim Crystalline forms(2s)-n-5[amino(imino)methyl]-2-thienylmethyl-1-(2r)-2[(carboxymethyl) amino]-3,3-diphenylpropanoyl-2-pyrrolidinecarboxamide nh2o
EP1497283A4 (en) * 2002-03-22 2006-01-11 Lg Life Sciences Ltd (2S) -N-5-AMINO (IMINO) METHYL-2-THIENYL METHYL-1- (2R) -2- (CARBOXYMETHYL) AMINO) 3,3-DIPHENYLPROPANOYL -2-PYRROLIDINE CARBOXAMIDE MALEIC ACID SALT AND PROCESS OF PREPARATION CORRESPONDING
AU2003245060A1 (en) * 2002-06-27 2004-01-19 Lg Life Sciences Ltd. Peptidic thrombin inhibitor compound
US7097967B2 (en) 2002-10-24 2006-08-29 Lg Life Sciences Ltd. Method of predicting drug-food interaction
US7399870B2 (en) * 2004-03-30 2008-07-15 Wyeth Synthesis of pyrrole-2-carbonitriles
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
US7678917B2 (en) * 2005-09-01 2010-03-16 Hoffman-La Roche Inc. Factor Xa inhibitors
CN109053523B (zh) 2005-10-07 2022-03-25 埃克塞利希斯股份有限公司 作为用于治疗增生性疾病的mek抑制剂的吖丁啶
US7951823B2 (en) 2006-05-23 2011-05-31 Irm Llc Compounds and compositions as channel activating protease inhibitors
US20080287687A1 (en) 2006-11-03 2008-11-20 Ajinomoto Co. Inc Production method of diphenylalanine-Ni (II) complex
EA016327B1 (ru) 2007-02-09 2012-04-30 Айрм Ллк Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы
WO2008135525A2 (en) * 2007-05-02 2008-11-13 Boehringer Ingelheim International Gmbh Substituted azetidines, manufacturing and use thereof as medicaments
RU2017144535A (ru) * 2010-03-30 2019-02-18 Версеон Корпорейшн Мультизамещенные ароматические соединения в качестве ингибиторов тромбина
EP2632898A4 (en) 2010-10-29 2014-04-02 Biogen Idec Inc HETEROCYCLIC TYROSINE KINASE HEMMER
CR20200237A (es) 2012-10-12 2020-07-26 Exelixis Inc Proceso novedoso para la elaboración de compuestos para su uso en el tratamiento del cáncer (diviisional 2015-0245)
KR20150132148A (ko) 2013-03-15 2015-11-25 베르선 코포레이션 세린 프로타아제 억제제로서의 다중 치환된 방향족 화합물
US9951025B2 (en) 2013-03-15 2018-04-24 Verseon Corporation Halogenopyrazoles as inhibitors of thrombin
KR20170048410A (ko) 2014-09-17 2017-05-08 베르선 코포레이션 세린 프로테아제 저해제로서의 피라졸릴-치환된 피리돈 화합물
MX2017011000A (es) 2015-02-27 2017-10-20 Verseon Corp Compuestos de pirazol sustituidos como inhibidores de serina proteasa.
WO2017035401A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amide compounds for treatment of immune and inflammatory disorders
WO2017035405A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amino compounds for treatment of immune and inflammatory disorders
AU2018227849B2 (en) 2017-03-01 2022-04-28 Achillion Pharmaceuticals, Inc. Aryl, heteroary, and heterocyclic pharmaceutical compounds for treatment of medical disorders
WO2018160891A1 (en) 2017-03-01 2018-09-07 Achillion Pharmaceutical, Inc. Pharmaceutical compounds for treatment of medical disorders
SG11202010925UA (en) * 2018-05-29 2020-12-30 Omeros Corp Masp-2 inhibitors and methods of use
AU2019336238A1 (en) 2018-09-06 2021-04-08 Achillion Pharmaceuticals, Inc. Morphic forms of Complement factor D inhibitors
AU2019346464A1 (en) 2018-09-25 2021-04-08 Achillion Pharmaceuticals, Inc. Morphic forms of complement factor D inhibitors
WO2020198062A1 (en) * 2019-03-22 2020-10-01 Achillion Pharmaceuticals, Inc. Pharmaceutical compounds for the treatment of complement mediated disorders
CA3159172A1 (en) 2019-12-04 2021-06-10 Michael Cicirelli Masp-2 inhibitors and methods of use
WO2023183405A2 (en) * 2022-03-22 2023-09-28 Alexion Pharmaceuticals, Inc. Pharmaceutical compounds for the treatment of complement mediated disorders

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
IL112795A (en) * 1994-03-04 2001-01-28 Astrazeneca Ab Derivatives of peptides as antithrombotic drugs, their preparation, and pharmaceutical preparations containing them
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
CZ237697A3 (cs) 1995-02-10 1998-04-15 Basf Aktiengesellschaft Derivát peptidického p-amidinobenzylamidu jako inhibitor thrombinu a meziprodukty pro jeho přípravu
US5914319A (en) 1995-02-27 1999-06-22 Eli Lilly And Company Antithrombotic agents
US5710130A (en) * 1995-02-27 1998-01-20 Eli Lilly And Company Antithrombotic agents
IL123986A (en) * 1997-04-24 2011-10-31 Organon Nv Medicinal compounds
EP1051431A1 (de) * 1998-01-26 2000-11-15 Basf Aktiengesellschaft Thrombininhibitoren
AU2424499A (en) * 1998-01-26 1999-08-09 Basf Aktiengesellschaft Heterocyclic amidines as callicrein protease inhibitors

Also Published As

Publication number Publication date
US20030134801A1 (en) 2003-07-17
CN1332737A (zh) 2002-01-23
KR100462974B1 (ko) 2004-12-23
CZ20012429A3 (cs) 2001-10-17
HUP0104500A2 (hu) 2002-04-29
JP3847092B2 (ja) 2006-11-15
CN1149210C (zh) 2004-05-12
HK1044936A1 (zh) 2002-11-08
CA2355281A1 (en) 2000-07-06
ZA200104780B (en) 2003-06-12
IL143545A (en) 2005-08-31
DE69919397D1 (de) 2004-09-16
NZ513174A (en) 2003-10-31
IL143545A0 (en) 2002-04-21
ATE273305T1 (de) 2004-08-15
NO20013220L (no) 2001-08-27
NO321739B1 (no) 2006-06-26
AU1895100A (en) 2000-07-31
WO2000039124A1 (en) 2000-07-06
AU765417B2 (en) 2003-09-18
JP2002533460A (ja) 2002-10-08
RU2221808C2 (ru) 2004-01-20
HUP0104500A3 (en) 2002-06-28
ES2226482T3 (es) 2005-03-16
KR20000047461A (ko) 2000-07-25
US6864249B2 (en) 2005-03-08
DK1140918T3 (da) 2004-12-20
NO20013220D0 (no) 2001-06-27
EP1140918B1 (en) 2004-08-11
TR200101899T2 (tr) 2001-12-21
EP1140918A1 (en) 2001-10-10
DE69919397T2 (de) 2005-07-28
US6492402B1 (en) 2002-12-10
KR20010086468A (ko) 2001-09-12

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Legal Events

Date Code Title Description
B25A Requested transfer of rights approved

Free format text: LLG LIFE SCIENCES LTD. (KR)

B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 5A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO PUBLICADO NA RPI 1942 DE 25/03/2008.