DE60219911D1 - Pyrrolidin-2-on derivate als faktor xa inhibitoren - Google Patents

Pyrrolidin-2-on derivate als faktor xa inhibitoren

Info

Publication number
DE60219911D1
DE60219911D1 DE60219911T DE60219911T DE60219911D1 DE 60219911 D1 DE60219911 D1 DE 60219911D1 DE 60219911 T DE60219911 T DE 60219911T DE 60219911 T DE60219911 T DE 60219911T DE 60219911 D1 DE60219911 D1 DE 60219911D1
Authority
DE
Germany
Prior art keywords
factor
pyrrolidin
inhibitors
derivatives
amelioration
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
DE60219911T
Other languages
English (en)
Other versions
DE60219911T2 (de
Inventor
Chuen Chan
Julie Nicole Hamblin
Henry Anderson Kelly
Nigel Paul King
Andrew Mcmurtrie Mason
Vipulkumar Kantibhai Patel
Stefan Senger
Gita Punjabhai Shah
Nigel Stephen Watson
Helen Elisabeth Weston
Caroline Whitworth
Robert John Young
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Glaxo Group Ltd
Original Assignee
Glaxo Group 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 Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of DE60219911D1 publication Critical patent/DE60219911D1/de
Application granted granted Critical
Publication of DE60219911T2 publication Critical patent/DE60219911T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • 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
    • 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
    • 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
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • 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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0043—Nose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
DE60219911T 2001-06-08 2002-06-06 Pyrrolidin-2-on derivate als faktor xa inhibitoren Expired - Lifetime DE60219911T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0114004.5A GB0114004D0 (en) 2001-06-08 2001-06-08 Chemical compounds
GB0114004 2001-06-08
PCT/GB2002/002586 WO2002100886A1 (en) 2001-06-08 2002-06-06 Pyrrolidin-2-one derivatives as inhibitors of factor xa

Publications (2)

Publication Number Publication Date
DE60219911D1 true DE60219911D1 (de) 2007-06-14
DE60219911T2 DE60219911T2 (de) 2008-01-17

Family

ID=9916208

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60219911T Expired - Lifetime DE60219911T2 (de) 2001-06-08 2002-06-06 Pyrrolidin-2-on derivate als faktor xa inhibitoren

Country Status (8)

Country Link
US (3) US7084139B2 (de)
EP (2) EP1839659A3 (de)
JP (1) JP4358616B2 (de)
AT (1) ATE361315T1 (de)
DE (1) DE60219911T2 (de)
ES (1) ES2284877T3 (de)
GB (1) GB0114004D0 (de)
WO (1) WO2002100886A1 (de)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0100902D0 (sv) * 2001-03-15 2001-03-15 Astrazeneca Ab Compounds
SE0100903D0 (sv) * 2001-03-15 2001-03-15 Astrazeneca Ab Compounds
GB0114005D0 (en) * 2001-06-08 2001-08-01 Glaxo Group Ltd Chemical compounds
SE0103710D0 (sv) * 2001-11-07 2001-11-07 Astrazeneca Ab Compounds
SE0202539D0 (sv) * 2002-08-27 2002-08-27 Astrazeneca Ab Compounds
GB0228533D0 (en) * 2002-12-06 2003-01-15 Glaxo Group Ltd Crystalline form
GB0228552D0 (en) * 2002-12-06 2003-01-15 Glaxo Group Ltd Chemical compounds
US20050119266A1 (en) * 2003-10-01 2005-06-02 Yan Shi Pyrrolidine and piperidine derivatives as factor Xa inhibitors
EP1732885A1 (de) * 2004-02-23 2006-12-20 Trustees Of Tufts College Lactame als konformationsgehinderte peptidomimetische inhibitoren
SE0401762D0 (sv) * 2004-07-05 2004-07-05 Astrazeneca Ab Novel compounds
SE0401763D0 (sv) * 2004-07-05 2004-07-05 Astrazeneca Ab Compounds
US7648992B2 (en) * 2004-07-05 2010-01-19 Astrazeneca Ab Hydantoin derivatives for the treatment of obstructive airway diseases
SE0403085D0 (sv) * 2004-12-17 2004-12-17 Astrazeneca Ab Novel componds
SE0403086D0 (sv) 2004-12-17 2004-12-17 Astrazeneca Ab Compounds
MX2009002669A (es) * 2006-09-12 2009-03-24 Glaxo Group Ltd Composicion farmaceutica que comprende una pluralidad de mini-comprimidos que comprenden un inhibidor del factor xa.
TW200831488A (en) * 2006-11-29 2008-08-01 Astrazeneca Ab Novel compounds
DE102007028406A1 (de) 2007-06-20 2008-12-24 Bayer Healthcare Ag Substituierte Oxazolidinone und ihre Verwendung
DE102007028407A1 (de) 2007-06-20 2008-12-24 Bayer Healthcare Ag Substituierte Oxazolidinone und ihre Verwendung
DE102007028319A1 (de) 2007-06-20 2008-12-24 Bayer Healthcare Ag Substituierte Oxazolidinone und ihre Verwendung
EP3078378B1 (de) 2015-04-08 2020-06-24 Vaiomer Verwendung von faktor-xa-inhibitoren zur regulierung von glykämie
CN113563255B (zh) * 2020-04-29 2023-08-18 成都倍特药业股份有限公司 瑞芬沙星中间体的制备方法
CN112250611B (zh) * 2020-11-27 2022-04-22 济南大学 一种-2-(2,5-二氟苯基)吡咯烷盐酸盐的合成方法

Family Cites Families (19)

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IL92011A0 (en) 1988-10-19 1990-07-12 Abbott Lab Heterocyclic peptide renin inhibitors
DE4035961A1 (de) 1990-11-02 1992-05-07 Thomae Gmbh Dr K Cyclische iminoderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
DE4121947A1 (de) * 1991-07-03 1993-01-07 Basf Ag 2-(3-(4-amidino-phenyl))-propionsaeurederivate, ihre herstellung und verwendung
US5703208A (en) * 1994-06-17 1997-12-30 Corvas International, Inc. 3-amino-2-oxo-1-piperidineacetic derivatives as enzyme inhibitors
EP0937073A2 (de) * 1996-10-11 1999-08-25 Cor Therapeutics, Inc. Selektive inhibitoren des faktor xa
US6602864B1 (en) 1996-12-13 2003-08-05 Aventis Pharma Deutschland Gmbh Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds
ATE224192T1 (de) 1996-12-13 2002-10-15 Aventis Pharma Inc Sulfonsäure oder sulfonylamino n-(heteroaralkyl)- azaheterocyclylamid verbindungen
US6281227B1 (en) * 1996-12-13 2001-08-28 Aventis Pharma Deutschland Gmbh Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds
US6187797B1 (en) * 1996-12-23 2001-02-13 Dupont Pharmaceuticals Company Phenyl-isoxazoles as factor XA Inhibitors
IL123986A (en) 1997-04-24 2011-10-31 Organon Nv Medicinal compounds
US6060491A (en) * 1997-06-19 2000-05-09 Dupont Pharmaceuticals 6-membered aromatics as factor Xa inhibitors
BR9815377A (pt) 1997-09-30 2001-01-16 Daiichi Pharmaceutical Co Ltda Derivados de sulfonil
HUP0101810A3 (en) 1998-01-27 2002-05-28 Aventis Pharm Prod Inc Substituted oxoazaheterocyclyl factor xa inhibitors and pharmaceutical compositions containing them
AU1926700A (en) 1998-12-31 2000-07-24 Aventis Pharmaceuticals Inc. 3-(thio-substituted amido)-lactams useful as inhibitors of matrix metalloproteinase
WO2000047563A1 (en) * 1999-02-09 2000-08-17 Bristol-Myers Squibb Co. LACTAM INHIBITORS OF FXa AND METHOD
KR20020004971A (ko) 1999-03-16 2002-01-16 이경하 치환 프로린 유도체 및 이들을 함유하고 있는 의약 조성물
WO2000069465A1 (fr) 1999-05-12 2000-11-23 Ono Pharmaceutical Co., Ltd. Agents anticancereux contenant des antagonistes de ep1 en tant que principe actif
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HUP0304058A2 (hu) 2001-01-30 2004-04-28 Bristol-Myers Squibb Company Xa faktor szulfonamid-laktám inhibitorok és alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények

Also Published As

Publication number Publication date
JP2005508868A (ja) 2005-04-07
GB0114004D0 (en) 2001-08-01
ES2284877T3 (es) 2007-11-16
US20040152697A1 (en) 2004-08-05
US7282497B2 (en) 2007-10-16
EP1395606B1 (de) 2007-05-02
US7084139B2 (en) 2006-08-01
US20060160885A1 (en) 2006-07-20
EP1839659A2 (de) 2007-10-03
DE60219911T2 (de) 2008-01-17
EP1839659A3 (de) 2011-05-04
US7226929B2 (en) 2007-06-05
WO2002100886A8 (en) 2004-02-05
US20060160886A1 (en) 2006-07-20
WO2002100886A1 (en) 2002-12-19
EP1395606A1 (de) 2004-03-10
JP4358616B2 (ja) 2009-11-04
ATE361315T1 (de) 2007-05-15

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