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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)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (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 (xx)
EP (1) EP1169338B1 (xx)
JP (1) JP4489976B2 (xx)
KR (1) KR20010108477A (xx)
CN (1) CN1351609A (xx)
AT (1) ATE281466T1 (xx)
AU (1) AU4111700A (xx)
BG (1) BG105978A (xx)
BR (1) BR0009678A (xx)
CA (1) CA2369378A1 (xx)
CZ (1) CZ20013577A3 (xx)
DE (1) DE50008510D1 (xx)
HK (1) HK1045846A1 (xx)
HU (1) HUP0203167A3 (xx)
IL (1) IL145771A0 (xx)
MX (1) MXPA01010114A (xx)
NO (1) NO20014876L (xx)
PL (1) PL351441A1 (xx)
SK (1) SK14232001A3 (xx)
TR (1) TR200102913T2 (xx)
WO (1) WO2000061608A2 (xx)
ZA (2) ZA200107890B (xx)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7144902B1 (en) * 1999-04-09 2006-12-05 Abbott Gmbh & Co. Kg Prodrugs of thrombin inhibitors
ATE360028T1 (de) * 2000-08-11 2007-05-15 Dendreon Corp Nicht-kovalente urokinase-und angiogenese- inhibitoren
WO2002014349A2 (en) * 2000-08-11 2002-02-21 Corvas International, Inc. Non-covalent inhibitors of urokinase and blood vessel formation
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
AU2003220222A1 (en) 2002-03-13 2003-09-29 Signum Biosciences, Inc. Modulation of protein methylation and phosphoprotein phosphate
WO2003086288A2 (en) 2002-04-12 2003-10-23 Merck & Co., Inc. Bicyclic amides
JP4768620B2 (ja) * 2003-05-15 2011-09-07 ジェネンテック， インコーポレイテッド 敗血症の予防及び治療のための方法及び組成物
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
CA2601777A1 (en) * 2005-02-03 2006-08-10 Signum Biosciences, Inc. Compositions and methods for enhancing cognitive function
AU2006227778A1 (en) * 2005-03-16 2006-09-28 Janssen Pharmaceutica N.V. Novel thiophene sulfoximines for treating complement-mediated diseases and conditions
US9486441B2 (en) 2008-04-21 2016-11-08 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
EP2899183B1 (en) 2011-10-14 2018-09-19 Bristol-Myers Squibb Company Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors
WO2013056034A1 (en) 2011-10-14 2013-04-18 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
HRP20170784T8 (hr) 2011-10-14 2018-05-18 Bristol-Myers Squibb Company Supstituirani spojevi tetrahidroizohinolina kao inhbitori xia faktora
EP2906541B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US9315519B2 (en) 2012-10-12 2016-04-19 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
HRP20180465T1 (hr) 2012-10-12 2018-05-04 Bristol-Myers Squibb Company Kristalni oblici inhibitora faktora xia
JP6479763B2 (ja) 2013-03-25 2019-03-06 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 第ｘｉａ因子阻害剤としての置換アゾール含有のテトラヒドロイソキノリン
UY35971A (es) 2014-01-31 2015-07-31 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Macrociclos con grupos p2? aromáticos como inhibidores del factor xia
NO2760821T3 (xx) 2014-01-31 2018-03-10
CN107074821B (zh) 2014-09-04 2020-05-22 百时美施贵宝公司 为fxia抑制剂的二酰胺大环化合物
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
JP7635138B2 (ja) * 2019-03-22 2025-02-25 アキリオン ファーマシューティカルズ， インコーポレーテッド 補体媒介性障害の治療のための医薬化合物
CN116437913A (zh) * 2020-09-23 2023-07-14 艾其林医药公司 用于治疗补体介导的病症的药物化合物

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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
HUP9800634A3 (en) 1995-02-10 2000-04-28 Abbott Gmbh & Co Kg P-amidino-benzylamide derivatives as thrombin inhibitors, intermediates and use thereof
KR100388185B1 (ko) * 1995-02-17 2003-11-28 애보트 게엠베하 운트 콤파니 카게 트롬빈 억제제로서의 신규 디펩티드 아미딘
TWI238827B (en) * 1995-12-21 2005-09-01 Astrazeneca Ab Prodrugs of thrombin inhibitors
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
CN1289341A (zh) * 1998-01-26 2001-03-28 Basf公司 凝血酶抑制剂
EP1049673A1 (de) * 1998-01-26 2000-11-08 Basf Aktiengesellschaft Heterocyclische amidine als kallikrein protease inhibitoren

Also Published As

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

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