ZA200107890B - Prodrugs of thrombin inhibitors. - Google Patents

Prodrugs of thrombin inhibitors.

Info

Publication number
ZA200107890B
ZA200107890B ZA200107890A ZA200107890A ZA200107890B ZA 200107890 B ZA200107890 B ZA 200107890B ZA 200107890 A ZA200107890 A ZA 200107890A ZA 200107890 A ZA200107890 A ZA 200107890A ZA 200107890 B ZA200107890 B ZA 200107890B
Authority
ZA
South Africa
Prior art keywords
prodrugs
thrombin inhibitors
inhibitors
complement
substances
Prior art date
Application number
ZA200107890A
Other languages
English (en)
Inventor
Dorit Baucke
Helmut Mack
Werner Seitz
Wilfried Hornberger
Gisela Backfisch
Juergen DELZER
Original Assignee
Abbott Gmbh & Co Kg
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 Abbott Gmbh & Co Kg filed Critical Abbott Gmbh & Co Kg
Publication of ZA200107890B publication Critical patent/ZA200107890B/xx

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B43/00—Formation or introduction of functional groups containing nitrogen
    • 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • Biophysics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
ZA200107890A 1999-04-09 2001-09-26 Prodrugs of thrombin inhibitors. ZA200107890B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19915930 1999-04-09

Publications (1)

Publication Number Publication Date
ZA200107890B true ZA200107890B (en) 2003-11-26

Family

ID=7903946

Family Applications (2)

Application Number Title Priority Date Filing Date
ZA200107890A ZA200107890B (en) 1999-04-09 2001-09-26 Prodrugs of thrombin inhibitors.
ZA200107978A ZA200107978B (en) 1999-04-09 2001-09-28 Low-molecular inhibitors of complement proteases.

Family Applications After (1)

Application Number Title Priority Date Filing Date
ZA200107978A ZA200107978B (en) 1999-04-09 2001-09-28 Low-molecular inhibitors of complement proteases.

Country Status (22)

Country Link
US (1) US6683055B1 (hu)
EP (1) EP1169338B1 (hu)
JP (1) JP4489976B2 (hu)
KR (1) KR20010108477A (hu)
CN (1) CN1351609A (hu)
AT (1) ATE281466T1 (hu)
AU (1) AU4111700A (hu)
BG (1) BG105978A (hu)
BR (1) BR0009678A (hu)
CA (1) CA2369378A1 (hu)
CZ (1) CZ20013577A3 (hu)
DE (1) DE50008510D1 (hu)
HK (1) HK1045846A1 (hu)
HU (1) HUP0203167A3 (hu)
IL (1) IL145771A0 (hu)
MX (1) MXPA01010114A (hu)
NO (1) NO20014876L (hu)
PL (1) PL351441A1 (hu)
SK (1) SK14232001A3 (hu)
TR (1) TR200102913T2 (hu)
WO (1) WO2000061608A2 (hu)
ZA (2) ZA200107890B (hu)

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BR0009674A (pt) * 1999-04-09 2002-01-15 Basf Ag Composto, droga, e, uso de composto
US6586405B2 (en) 2000-08-11 2003-07-01 Corvas International, Inc. Non-covalent inhibitors of urokinase and blood vessel formation
NZ518195A (en) * 2000-08-11 2005-04-29 Corvas Int Inc Non-covalent inhibitors of urokinase and blood vessel formation
WO2003070229A2 (de) * 2002-02-22 2003-08-28 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Verwendung von proteinaseinhibitoren zur behandlung von autoimmunerkrankungen
CA2477604A1 (en) 2002-03-13 2003-09-25 Signum Biosciences, Inc. Modulation of protein methylation and phosphoprotein phosphate
JP4459629B2 (ja) 2002-04-12 2010-04-28 メルク エンド カムパニー インコーポレーテッド 二環式アミド
CA2524534C (en) * 2003-05-15 2012-12-11 Sek Chung Fung Methods and compositions for the prevention and treatment of sepsis
TW200519105A (en) * 2003-10-20 2005-06-16 Lg Life Science Ltd Novel inhibitors of DPP-IV, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent
CN1304568C (zh) * 2004-07-05 2007-03-14 中国人民解放军第二军医大学 新型人补体C1r样丝氨酸蛋白酶类似物,其编码序列及用途
US7923041B2 (en) 2005-02-03 2011-04-12 Signum Biosciences, Inc. Compositions and methods for enhancing cognitive function
US8221804B2 (en) * 2005-02-03 2012-07-17 Signum Biosciences, Inc. Compositions and methods for enhancing cognitive function
KR20080002832A (ko) * 2005-03-16 2008-01-04 얀센 파마슈티카 엔.브이. 보체 매개성 질병 및 이상을 치료하기 위한 신규한 티오펜설폭시민
WO2009132051A1 (en) 2008-04-21 2009-10-29 Signum Biosciences, Inc. Compounds, compositions and methods for making the same
CN102464701B (zh) * 2010-11-08 2015-10-21 上海医药工业研究院 一类新型化合物、其制备方法及用途
CN103987696B (zh) 2011-10-14 2016-12-21 百时美施贵宝公司 作为因子xia抑制剂的取代的四氢异喹啉化合物
ES2699226T3 (es) 2011-10-14 2019-02-08 Bristol Myers Squibb Co Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa
PL2766346T3 (pl) 2011-10-14 2017-09-29 Bristol-Myers Squibb Company Podstawione związki tetrahydroizochinoliny jako inhibitory czynnika XIA
US9315519B2 (en) 2012-10-12 2016-04-19 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
SI2906551T1 (en) 2012-10-12 2018-05-31 Bristol-Myers Squibb Company CRYSTALINOUS FORMATS OF XIA FACTOR INHIBITOR
WO2014059214A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EP2978751B1 (en) 2013-03-25 2018-12-05 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors
HUE040226T2 (hu) 2014-01-31 2019-02-28 Bristol Myers Squibb Co Makrociklusok heterociklusos P2' csoportokkal XIA faktor inhibitorokként
NO2760821T3 (hu) 2014-01-31 2018-03-10
WO2016036893A1 (en) 2014-09-04 2016-03-10 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
EP3941462A4 (en) * 2019-03-22 2023-04-05 Achillion Pharmaceuticals, Inc. PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT-MEDIED DISEASES

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DE3738910A1 (de) 1987-11-17 1989-05-24 Basf Ag Tributylammoniumsalz von 1,1-dicyano-2-hydroxy-3-chlorprop-1-en, ein verfahren zu seiner herstellung sowie ein verfahren zur herstellung von 2-amino-4-chlor-3-cyano-5-formylthiophen
AU675981B2 (en) * 1992-12-02 1997-02-27 Bristol-Myers Squibb Company Guanidinyl-substituted heterocyclic thrombin inhibitors
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
DE4421052A1 (de) 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
DE4443390A1 (de) * 1994-12-06 1996-06-13 Basf Ag Neue dipeptidische p-Amidinobenzylamide mit N-terminalen Sulfonyl- bzw. Aminosulfonylresten
US5932567A (en) 1995-02-10 1999-08-03 Basf Aktiengesellschaft Thrombin inhibitors
WO1996025426A1 (de) 1995-02-17 1996-08-22 Basf Aktiengesellschaft Neue dipeptidische amidine als thrombin-inhibitoren
AR005245A1 (es) * 1995-12-21 1999-04-28 Astrazeneca Ab Prodrogas de inhibidores de trombina, una formulación farmaceutica que las comprende, el uso de dichas prodrogas para la manufactura de un medicamento y un procedimiento para su preparacion
DE19632772A1 (de) * 1996-08-14 1998-02-19 Basf Ag Neue Benzamidine
DE19632773A1 (de) 1996-08-14 1998-02-19 Basf Ag Neue Thrombininhibitoren
DE19635674A1 (de) 1996-09-03 1998-03-05 Basf Ag Verfahren zur Herstellung von Amidinen
US6653340B1 (en) * 1997-06-03 2003-11-25 Biocryst Pharmaceuticals, Inc. Compounds useful in the complement, coagulat and kallikrein pathways and method for their preparation
EP1049673A1 (de) * 1998-01-26 2000-11-08 Basf Aktiengesellschaft Heterocyclische amidine als kallikrein protease inhibitoren
CN1289341A (zh) * 1998-01-26 2001-03-28 Basf公司 凝血酶抑制剂

Also Published As

Publication number Publication date
HK1045846A1 (zh) 2002-12-13
MXPA01010114A (es) 2002-07-30
TR200102913T2 (tr) 2002-01-21
KR20010108477A (ko) 2001-12-07
NO20014876D0 (no) 2001-10-08
JP2002542164A (ja) 2002-12-10
US6683055B1 (en) 2004-01-27
JP4489976B2 (ja) 2010-06-23
ZA200107978B (en) 2003-03-26
HUP0203167A3 (en) 2003-09-29
IL145771A0 (en) 2002-07-25
PL351441A1 (en) 2003-04-22
EP1169338A2 (de) 2002-01-09
HUP0203167A2 (hu) 2003-02-28
DE50008510D1 (de) 2004-12-09
CA2369378A1 (en) 2000-10-19
WO2000061608A3 (de) 2001-01-11
CZ20013577A3 (cs) 2002-07-17
CN1351609A (zh) 2002-05-29
EP1169338B1 (de) 2004-11-03
WO2000061608A2 (de) 2000-10-19
SK14232001A3 (sk) 2002-06-04
AU4111700A (en) 2000-11-14
BG105978A (bg) 2002-07-31
NO20014876L (no) 2001-12-04
ATE281466T1 (de) 2004-11-15
BR0009678A (pt) 2002-01-22

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