RU2009107917A - Аминоизохинолиновый ингибитор тромбина с улучшенной биодоступностью - Google Patents

Аминоизохинолиновый ингибитор тромбина с улучшенной биодоступностью Download PDF

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Publication number
RU2009107917A
RU2009107917A RU2009107917/04A RU2009107917A RU2009107917A RU 2009107917 A RU2009107917 A RU 2009107917A RU 2009107917/04 A RU2009107917/04 A RU 2009107917/04A RU 2009107917 A RU2009107917 A RU 2009107917A RU 2009107917 A RU2009107917 A RU 2009107917A
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RU
Russia
Prior art keywords
amino
compound according
pharmaceutically acceptable
isochinoline
compound
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RU2009107917/04A
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English (en)
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RU2437879C2 (ru
Inventor
Роберт ДЖИЛФИЛЛАН (GB)
Роберт ДЖИЛФИЛЛАН
Дэвид Джонатан БЕННЕТТ (GB)
Дэвид Джонатан БЕННЕТТ
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Н.В. Органон (Nl)
Н.В. Органон
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Application filed by Н.В. Органон (Nl), Н.В. Органон filed Critical Н.В. Органон (Nl)
Publication of RU2009107917A publication Critical patent/RU2009107917A/ru
Application granted granted Critical
Publication of RU2437879C2 publication Critical patent/RU2437879C2/ru

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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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

1. Соединение, представляющее собой N-(2-оксо-2-пропоксиэтил)-β-фенил-D-фенилаланил-N-[(1-амино-6-изохинолинил)метил]-L-пролинамид, или его фармацевтически приемлемая соль. ! 2. Соединение по п.1 в виде дигидрохлорида. ! 3. Фармацевтическая композиция, содержащая соединение по п.1 и фармацевтически приемлемые вспомогательные вещества. ! 4. Соединение по п.1 для применения в терапии. ! 5. Применение соединения по п.1 для производства лекарственного средства для лечения или профилактики заболеваний, опосредованных тромбином. ! 6. Соединение, представляющее собой N-(карбоксиметил)-β-фенил-D-фенилаланил-N-[(1-амино-6-изохинолинил)метил]-L-пролинамид, или его фармацевтически приемлемая соль.

Claims (6)

1. Соединение, представляющее собой N-(2-оксо-2-пропоксиэтил)-β-фенил-D-фенилаланил-N-[(1-амино-6-изохинолинил)метил]-L-пролинамид, или его фармацевтически приемлемая соль.
2. Соединение по п.1 в виде дигидрохлорида.
3. Фармацевтическая композиция, содержащая соединение по п.1 и фармацевтически приемлемые вспомогательные вещества.
4. Соединение по п.1 для применения в терапии.
5. Применение соединения по п.1 для производства лекарственного средства для лечения или профилактики заболеваний, опосредованных тромбином.
6. Соединение, представляющее собой N-(карбоксиметил)-β-фенил-D-фенилаланил-N-[(1-амино-6-изохинолинил)метил]-L-пролинамид, или его фармацевтически приемлемая соль.
RU2009107917/04A 2006-08-08 2007-08-06 Аминоизохинолиновый ингибитор тромбина с улучшенной биодоступностью RU2437879C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06118608 2006-08-08
EP06118608.6 2006-08-08

Publications (2)

Publication Number Publication Date
RU2009107917A true RU2009107917A (ru) 2010-09-20
RU2437879C2 RU2437879C2 (ru) 2011-12-27

Family

ID=37561257

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2009107917/04A RU2437879C2 (ru) 2006-08-08 2007-08-06 Аминоизохинолиновый ингибитор тромбина с улучшенной биодоступностью

Country Status (21)

Country Link
US (1) US8299091B2 (ru)
EP (1) EP2054402B1 (ru)
JP (1) JP5271904B2 (ru)
KR (1) KR20090048496A (ru)
CN (1) CN101511816B (ru)
AR (1) AR062215A1 (ru)
AU (1) AU2007283596B2 (ru)
BR (1) BRPI0715384A2 (ru)
CA (1) CA2659154A1 (ru)
CL (1) CL2007002294A1 (ru)
CO (1) CO6150148A2 (ru)
IL (1) IL196783A (ru)
MX (1) MX2009001384A (ru)
MY (1) MY143949A (ru)
NO (1) NO20090448L (ru)
NZ (1) NZ574550A (ru)
PE (1) PE20080526A1 (ru)
RU (1) RU2437879C2 (ru)
TW (1) TWI389899B (ru)
WO (1) WO2008017650A1 (ru)
ZA (1) ZA200900903B (ru)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20150047597A (ko) * 2012-08-27 2015-05-04 어레이 바이오파마 인크. 과증식성 질환의 치료를 위한 세린/트레오닌 키나아제 억제제

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4115468A1 (de) * 1991-05-11 1992-11-12 Behringwerke Ag Amidinophenylalaninderivate, verfahren zu deren herstellung, deren verwendung und diese enthaltende mittel als antikoagulantien
GB9322976D0 (en) * 1993-11-08 1994-01-05 Pfizer Ltd Therapeutic agents
US5523308A (en) * 1995-06-07 1996-06-04 Costanzo; Michael J. Peptidyl heterocycles useful in the treatment of thrombin related disorders
NZ336046A (en) * 1996-12-06 2000-10-27 Cortech Inc Serine protease inhibitors containing substituted oxadiazole, thiadiazole and triazole peptide derivatives
IL123986A (en) * 1997-04-24 2011-10-31 Organon Nv Medicinal compounds
TW575567B (en) 1998-10-23 2004-02-11 Akzo Nobel Nv Serine protease inhibitor
EP1303491A1 (en) * 2000-07-12 2003-04-23 Akzo Nobel N.V. Thrombin inhibitors comprising an aminoisoquinoline group

Also Published As

Publication number Publication date
CA2659154A1 (en) 2008-02-14
JP5271904B2 (ja) 2013-08-21
BRPI0715384A2 (pt) 2013-06-18
WO2008017650A1 (en) 2008-02-14
AU2007283596A1 (en) 2008-02-14
IL196783A (en) 2013-03-24
AR062215A1 (es) 2008-10-22
CL2007002294A1 (es) 2008-04-18
CN101511816B (zh) 2013-01-02
ZA200900903B (en) 2010-06-30
TWI389899B (zh) 2013-03-21
NO20090448L (no) 2009-02-05
KR20090048496A (ko) 2009-05-13
EP2054402A1 (en) 2009-05-06
US20100305153A1 (en) 2010-12-02
JP2010500321A (ja) 2010-01-07
PE20080526A1 (es) 2008-06-13
MX2009001384A (es) 2009-04-30
AU2007283596B2 (en) 2012-07-05
TW200821294A (en) 2008-05-16
NZ574550A (en) 2010-09-30
CO6150148A2 (es) 2010-04-20
RU2437879C2 (ru) 2011-12-27
EP2054402B1 (en) 2013-11-27
MY143949A (en) 2011-07-29
US8299091B2 (en) 2012-10-30
CN101511816A (zh) 2009-08-19
IL196783A0 (en) 2009-11-18

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PC43 Official registration of the transfer of the exclusive right without contract for inventions

Effective date: 20120326

PC43 Official registration of the transfer of the exclusive right without contract for inventions

Effective date: 20130917

PC43 Official registration of the transfer of the exclusive right without contract for inventions

Effective date: 20140402

MM4A The patent is invalid due to non-payment of fees

Effective date: 20140807