SK14232001A3 - Nízkomolekulové inhibítory komplementárnych proteáz - Google Patents

Nízkomolekulové inhibítory komplementárnych proteáz Download PDF

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Publication number
SK14232001A3
SK14232001A3 SK1423-2001A SK14232001A SK14232001A3 SK 14232001 A3 SK14232001 A3 SK 14232001A3 SK 14232001 A SK14232001 A SK 14232001A SK 14232001 A3 SK14232001 A3 SK 14232001A3
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SK
Slovakia
Prior art keywords
alkyl
thioph
alkylaryl
cycloalkyl
pyr
Prior art date
Application number
SK1423-2001A
Other languages
English (en)
Slovak (sk)
Inventor
Heinz Hillen
Martin Schmidt
Helmut Mack
Werner Seitz
Andreas Haupt
Johann-Christian Zechel
Andreas Kling
Original Assignee
Basf Aktiengesellschaft
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 Basf Aktiengesellschaft filed Critical Basf Aktiengesellschaft
Publication of SK14232001A3 publication Critical patent/SK14232001A3/sk

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B43/00Formation or introduction of functional groups containing nitrogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal 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)
SK1423-2001A 1999-04-09 2000-03-28 Nízkomolekulové inhibítory komplementárnych proteáz SK14232001A3 (sk)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19915930 1999-04-09
PCT/EP2000/002710 WO2000061608A2 (de) 1999-04-09 2000-03-28 Niedermolekulare inhibitoren von komplementproteasen

Publications (1)

Publication Number Publication Date
SK14232001A3 true SK14232001A3 (sk) 2002-06-04

Family

ID=7903946

Family Applications (1)

Application Number Title Priority Date Filing Date
SK1423-2001A SK14232001A3 (sk) 1999-04-09 2000-03-28 Nízkomolekulové inhibítory komplementárnych proteáz

Country Status (22)

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

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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 (cs) 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

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
ZA200107890B (en) 2003-11-26
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
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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