HK1061973A1 - Lactam-containing compounds and derivatives thereof as factor xa inhibitors - Google Patents

Lactam-containing compounds and derivatives thereof as factor xa inhibitors Download PDF

Info

Publication number
HK1061973A1
HK1061973A1 HK04105041.4A HK04105041A HK1061973A1 HK 1061973 A1 HK1061973 A1 HK 1061973A1 HK 04105041 A HK04105041 A HK 04105041A HK 1061973 A1 HK1061973 A1 HK 1061973A1
Authority
HK
Hong Kong
Prior art keywords
compound
mmol
phenyl
substituted
treating
Prior art date
Application number
HK04105041.4A
Other languages
English (en)
French (fr)
Chinese (zh)
Other versions
HK1061973B (en
Inventor
Wei Han
Michael J. Orwat
Donald Pinto
Mimi Quan
Yun-Long Li
X. Qiao Jennifer
Patrick Lam
Stephanie Koch
Original Assignee
Bristol-Myers Squibb Holdings Ireland Unlimited Company
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=23262376&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HK1061973(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol-Myers Squibb Holdings Ireland Unlimited Company filed Critical Bristol-Myers Squibb Holdings Ireland Unlimited Company
Publication of HK1061973A1 publication Critical patent/HK1061973A1/en
Publication of HK1061973B publication Critical patent/HK1061973B/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J1/00—Containers specially adapted for medical or pharmaceutical purposes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J1/00—Containers specially adapted for medical or pharmaceutical purposes
    • A61J1/03—Containers specially adapted for medical or pharmaceutical purposes for pills or tablets
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J1/00—Containers specially adapted for medical or pharmaceutical purposes
    • A61J1/05—Containers specially adapted for medical or pharmaceutical purposes for collecting, storing or administering blood, plasma or medical fluids ; Infusion or perfusion containers
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • 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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B65—CONVEYING; PACKING; STORING; HANDLING THIN OR FILAMENTARY MATERIAL
    • B65D—CONTAINERS FOR STORAGE OR TRANSPORT OF ARTICLES OR MATERIALS, e.g. BAGS, BARRELS, BOTTLES, BOXES, CANS, CARTONS, CRATES, DRUMS, JARS, TANKS, HOPPERS, FORWARDING CONTAINERS; ACCESSORIES, CLOSURES, OR FITTINGS THEREFOR; PACKAGING ELEMENTS; PACKAGES
    • B65D81/00—Containers, packaging elements, or packages, for contents presenting particular transport or storage problems, or adapted to be used for non-packaging purposes after removal of contents
    • B65D81/32—Containers, packaging elements, or packages, for contents presenting particular transport or storage problems, or adapted to be used for non-packaging purposes after removal of contents for packaging two or more different materials which must be maintained separate prior to use in admixture
    • B65D81/3216—Rigid containers disposed one within the other
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Mechanical Engineering (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)

Claims (29)

  1. Verbindung, welche durch Formel (1) dargestellt wird: oder ein pharmazeutisch verträgliches Salz davon.
  2. Verbindung gemäß Anspruch 1, welche durch Formel (1) dargestellt wird.
  3. Pharmazeutische Zusammensetzung, umfassend: einen pharmazeutisch verträglichen Träger und eine therapeutisch wirksame Menge der Verbindung der Formel (1) nach Anspruch 1 oder ein pharmazeutisch verträgliches Salz davon.
  4. Pharmazeutische Zusammensetzung, umfassend: den pharmazeutisch verträglichen Träger und eine therapeutisch wirksame Menge der Verbindung nach Anspruch 2.
  5. Verbindung nach Anspruch 1 oder 2 zur Verwendung in der Therapie.
  6. Pharmazeutische Zusammensetzung nach Anspruch 3 oder 4 zur Verwendung in der Therapie.
  7. Verbindung nach Anspruch 1 oder 2 zur Verwendung beim Behandeln einer thromboembolischen Erkrankung.
  8. Pharmazeutische Zusammensetzung nach Anspruch 3 oder 4 zur Verwendung beim Behandeln einer thromboembolischen Erkrankung.
  9. Verwendung einer Verbindung nach Anspruch 1 oder 2 bei der Herstellung eines Medikaments zur Verwendung beim Behandeln einer thromboembolischen Erkrankung.
  10. Verwendung einer pharmazeutischen Zusammensetzung nach Anspruch 3 oder 4 bei der Herstellung eines Medikaments zur Verwendung beim Behandeln einer thromboembolischen Erkrankung.
  11. Verbindung zur Verwendung beim Behandeln einer thromboembolischen Erkrankung gemäß Anspruch 7 oder Verwendung einer Verbindung gemäß Anspruch 9, wobei die thromboembolische Erkrankung aus der Gruppe, bestehend aus arteriellen kardiovaskulären thromboembolischen Erkrankungen, venösen kardiovaskulären thromboembolischen Erkrankungen und thromboembolischen Erkrankungen in den Kammern des Herzens, ausgewählt ist.
  12. Verbindung zur Verwendung beim Behandeln einer thromboembolischen Erkrankung gemäß Anspruch 7 oder Verwendung einer Verbindung gemäß Anspruch 9, wobei die thromboembolische Erkrankung ausgewählt ist aus instabiler Angina, einem akuten Koronarsyndrom, erstem Myokardinfarkt, wiederkehrendem Myokardinfarkt, ischämischem plötzlichen Tod, transitorischer ischämischer Attacke, Schlaganfall, Atherosklerose, peripherer arterieller Verschlußkrankheit, venöser Thrombose, tiefer Venenthrombose, Thrombophlebitis, arterieller Embolie, Koronararterienthrombose, Hirnarterienthrombose, Hirnembolie, Nierenembolie, Lungenembolie und Thrombose, resultierend aus (a) Klappenprothesen oder anderen Implantaten, (b) Dauerkathetern, (c) Stents, (d) kardiopulmonalem Bypass, (e) Hämodialyse oder (f) anderen Verfahrensweisen, bei welchen Blut einer künstlichen Oberfläche ausgesetzt wird, die Thrombose fördert.
  13. Verbindung zur Verwendung beim Behandeln einer thromboembolischen Erkrankung gemäß Anspruch 12 oder Verwendung einer Verbindung gemäß Anspruch 12, wobei die thromboembolische Erkrankung ein akutes Koronarsyndrom ist.
  14. Verbindung zur Verwendung beim Behandeln einer thromboembolischen Erkrankung gemäß Anspruch 12 oder Verwendung einer Verbindung gemäß Anspruch 12, wobei die thromboembolische Erkrankung ischämischer plötzlicher Tod, transitorische ischämische Attacke oder Schlaganfall ist.
  15. Verbindung zur Verwendung beim Behandeln einer thromboembolischen Erkrankung gemäß Anspruch 12 oder Verwendung einer Verbindung gemäß Anspruch 12, wobei die thromboembolische Erkrankung tiefe Venenthrombose ist.
  16. Verbindung zur Verwendung beim Behandeln einer thromboembolischen Erkrankung gemäß Anspruch 12 oder Verwendung einer Verbindung gemäß Anspruch 12, wobei die thromboembolische Erkrankung Lungenembolie ist.
  17. Pharmazeutische Zusammensetzung zur Verwendung beim Behandeln einer thromboembolischen Erkrankung gemäß Anspruch 8 oder Verwendung einer pharmazeutischen Zusammensetzung gemäß Anspruch 10, wobei die thromboembolische Erkrankung aus der Gruppe, bestehend aus arteriellen kardiovaskulären thromboembolischen Erkrankungen, venösen kardiovaskulären thromboembolischen Erkrankungen und thromboembolischen Erkrankungen in den Kammern des Herzens, ausgewählt ist.
  18. Pharmazeutische Zusammensetzung zur Verwendung beim Behandeln einer thromboembolischen Erkrankung gemäß Anspruch 8 oder Verwendung einer pharmazeutischen Zusammensetzung gemäß Anspruch 10, wobei die thromboembolische Erkrankung ausgewählt ist aus instabiler Angina, einem akuten Koronarsyndrom, erstem Myokardinfarkt, wiederkehrendem Myokardinfarkt, ischämischem plötzlichen Tod, transitorischer ischämischer Attacke, Schlaganfall, Atherosklerose, peripherer arterieller Verschlußkrankheit, venöser Thrombose, tiefer Venenthrombose, Thrombophlebitis, arterieller Embolie, Koronararterienthrombose, Hirnarterienthrombose, Hirnembolie, Nierenembolie, Lungenembolie und Thrombose, resultierend aus (a) Klappenprothesen oder anderen Implantaten, (b) Dauerkathetern, (c) Stents, (d) kardiopulmonalem Bypass, (e) Hämodialyse oder (f) anderen Verfahrensweisen, bei welchen Blut einer künstlichen Oberfläche ausgesetzt wird, die Thrombose fördert.
  19. Pharmazeutische Zusammensetzung zur Verwendung beim Behandeln einer thromboembolischen Erkrankung gemäß Anspruch 18 oder Verwendung einer pharmazeutischen Zusammensetzung gemäß Anspruch 18, wobei die thromboembolische Erkrankung ein akutes Koronarsyndrom ist.
  20. Pharmazeutische Zusammensetzung zur Verwendung beim Behandeln einer thromboembolischen Erkrankung gemäß Anspruch 18 oder Verwendung einer pharmazeutischen Zusammensetzung gemäß Anspruch 18, wobei die thromboembolische Erkrankung ischämischer plötzlicher Tod, transitorische ischämische Attacke oder Schlaganfall ist.
  21. Pharmazeutische Zusammensetzung zur Verwendung beim Behandeln einer thromboembolischen Erkrankung gemäß Anspruch 18 oder Verwendung einer pharmazeutischen Zusammensetzung gemäß Anspruch 18, wobei die thromboembolische Erkrankung tiefe Venenthrombose ist.
  22. Pharmazeutische Zusammensetzung zur Verwendung beim Behandeln einer thromboembolischen Erkrankung gemäß Anspruch 18 oder Verwendung einer pharmazeutischen Zusammensetzung gemäß Anspruch 18, wobei die thromboembolische Erkrankung Lungenembolie ist.
  23. Verbindung und ein zweites therapeutisches Mittel zur Verwendung beim Behandeln einer thrombolytischen Erkrankung, wobei die Verbindung eine Verbindung nach Anspruch 2 ist, und das zweite therapeutische Mittel mindestens ein Mittel, ausgewählt aus einem zweiten Faktor-Xa-Hemmer, einem antikoagulierenden Mittel, einem Antithrombozytenmittel, einem Thrombin hemmenden Mittel, einem thrombolytischen Mittel und einem fibrinolytischen Mittel, ist.
  24. Verwendung einer Verbindung und eines zweiten therapeutischen Mittels bei der Herstellung eines Medikaments zur Verwendung beim Behandeln einer thrombolytischen Erkrankung, wobei die Verbindung eine Verbindung nach Anspruch 2 ist, und das zweite therapeutische Mittel mindestens ein Mittel, ausgewählt aus einem zweiten Faktor-Xa-Hemmer, einem antikoagulierenden Mittel, einem Antithrombozytenmittel, einem Thrombin hemmenden Mittel, einem thrombolytischen Mittel und einem fibrinolytischen Mittel, ist.
  25. Verbindung und ein zweites therapeutisches Mittel zur Verwendung beim Behandeln einer thrombolytischen Erkrankung gemäß Anspruch 23 oder Verwendung einer Verbindung und eines zweiten therapeutischen Mittels gemäß Anspruch 24, wobei das zweite therapeutische Mittel mindestens ein Mittel, ausgewählt aus Warfarin, unfraktioniertem Heparin, Heparin mit niedrigem Molekulargewicht, synthetischem Pentasaccharid, Hirudin, Argatroban, Aspirin, Ibuprofen, Naproxen, Sulindac, Indomethacin, Mefenamat, Droxicam, Diclofenac, Sulfinpyrazon, Piroxicam, Ticlopidin, Clopidogrel, Tirofiban, Eptifibatid, Abciximab, Melagatran, Disulfatohirudin, Gewebeplasminogenaktivator, modifiziertem Gewebeplasminogenaktivator, Anistreplase, Urokinase und Streptokinase, ist.
  26. Verbindung und ein zweites therapeutisches Mittel zur Verwendung beim Behandeln einer thrombolytischen Erkrankung gemäß Anspruch 23 oder Verwendung einer Verbindung und eines zweiten therapeutischen Mittels gemäß Anspruch 24, wobei das zweite therapeutische Mittel mindestens ein Antithrombozytenmittel ist.
  27. Verbindung und ein zweites therapeutisches Mittel zur Verwendung beim Behandeln einer thrombolytischen Erkrankung gemäß Anspruch 26 oder Verwendung einer Verbindung und eines zweiten therapeutischen Mittels gemäß Anspruch 26, wobei das zweite therapeutische Mittel mindestens eines von Aspirin und Clopidogrel ist.
  28. Verbindung und ein zweites therapeutisches Mittel zur Verwendung beim Behandeln einer thrombolytischen Erkrankung gemäß Anspruch 27 oder Verwendung einer Verbindung und eines zweiten therapeutischen Mittels gemäß Anspruch 27, wobei das Antithrombozytenmittel Clopidogrel ist.
  29. Verbindung und ein zweites therapeutisches Mittel zur Verwendung beim Behandeln einer thrombolytischen Erkrankung gemäß Anspruch 27 oder Verwendung einer Verbindung und eines zweiten therapeutischen Mittels gemäß Anspruch 27, wobei das Antithrombozytenmittel Aspirin ist.
HK04105041.4A 2001-09-21 2002-09-17 Lactam-containing compounds and derivatives thereof as factor xa inhibitors HK1061973B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US324165 1981-11-23
US32416501P 2001-09-21 2001-09-21
PCT/US2002/029491 WO2003026652A1 (en) 2001-09-21 2002-09-17 Lactam-containing compounds and derivatives thereof as factor xa inhibitors

Publications (2)

Publication Number Publication Date
HK1061973A1 true HK1061973A1 (en) 2004-10-15
HK1061973B HK1061973B (en) 2010-02-05

Family

ID=

Also Published As

Publication number Publication date
CL2008002717A1 (es) 2009-01-09
US9975891B2 (en) 2018-05-22
HU228195B1 (hu) 2013-01-28
CN101357914A (zh) 2009-02-04
RS51444B (sr) 2011-04-30
US20100119510A1 (en) 2010-05-13
AU2008207537B2 (en) 2010-11-04
US20170050964A1 (en) 2017-02-23
MY137830A (en) 2009-03-31
IS2824B (is) 2013-03-15
KR100909141B1 (ko) 2009-07-23
CY2011016I1 (el) 2017-11-14
NZ531616A (en) 2006-12-22
FR11C0042I1 (de) 2011-04-11
LU91888I9 (de) 2019-01-03
IS7184A (is) 2004-03-16
US7531535B2 (en) 2009-05-12
US7960411B2 (en) 2011-06-14
ES2329881T3 (es) 2009-12-02
WO2003026652A1 (en) 2003-04-03
US7691846B2 (en) 2010-04-06
CA2461202C (en) 2011-07-12
ZA200402184B (en) 2005-07-27
RU2345993C2 (ru) 2009-02-10
HUP0402463A2 (hu) 2005-04-28
JP2009079059A (ja) 2009-04-16
JP4249621B2 (ja) 2009-04-02
IS3006B (is) 2018-11-15
CA2726702A1 (en) 2003-04-03
PL373299A1 (pl) 2005-08-22
US20150210691A1 (en) 2015-07-30
HRP20040280B1 (hr) 2013-09-30
CY2011016I2 (el) 2017-11-14
CA2461202A1 (en) 2003-04-03
US20090176758A1 (en) 2009-07-09
NO2011021I1 (no) 2011-09-26
PL204263B1 (pl) 2009-12-31
LTC1427415I2 (lt) 2023-10-10
US20050267097A1 (en) 2005-12-01
CH1427415H1 (de) 2023-12-21
HUS1300014I1 (hu) 2017-10-30
AR037092A1 (es) 2004-10-20
KR100908176B1 (ko) 2009-07-16
MEP58108A (bs) 2011-05-10
US8470854B2 (en) 2013-06-25
US20140113892A1 (en) 2014-04-24
IL160693A (en) 2011-06-30
ME00384B (me) 2011-05-10
CN1578660A (zh) 2005-02-09
HRP20080382A2 (en) 2008-12-31
LTPA2011012I1 (lt) 2012-07-25
BRPI0212726B1 (pt) 2015-11-24
RS20080517A (sr) 2009-07-15
US20120201816A1 (en) 2012-08-09
JP4889705B2 (ja) 2012-03-07
AU2008207537A1 (en) 2008-09-18
MEP8708A (bs) 2010-06-10
CO5560567A2 (es) 2005-09-30
RU2004112191A (ru) 2005-10-10
MXPA04002526A (es) 2004-05-31
DE122011100050I1 (de) 2012-03-15
PL204653B1 (pl) 2010-01-29
ME00090B (me) 2010-10-10
IS8803A (is) 2009-02-26
US7338963B2 (en) 2008-03-04
CN102617567A (zh) 2012-08-01
NO20083684L (no) 2004-05-03
NO20041163L (no) 2004-05-03
ATE544750T1 (de) 2012-02-15
EP1427415B1 (de) 2009-08-12
EP1427415A1 (de) 2004-06-16
CN104744461A (zh) 2015-07-01
AU2002341693B2 (en) 2008-05-29
CY1110509T1 (el) 2015-04-29
BR0212726A (pt) 2004-08-03
US20080090807A1 (en) 2008-04-17
BE2011C034I2 (de) 2021-11-22
EP2105436B1 (de) 2012-02-08
CN110894196A (zh) 2020-03-20
JP2005507889A (ja) 2005-03-24
NO328558B1 (no) 2010-03-22
ATE439360T1 (de) 2009-08-15
US20200140436A1 (en) 2020-05-07
KR20080075927A (ko) 2008-08-19
DK1427415T3 (da) 2009-11-23
AU2008207537B8 (en) 2011-12-08
NO2011021I2 (no) 2012-06-25
US8188120B2 (en) 2012-05-29
BRPI0212726B8 (pt) 2021-05-25
LU91888I2 (fr) 2011-12-19
HUP0402463A3 (en) 2011-07-28
US20180244673A1 (en) 2018-08-30
FR11C0042I2 (fr) 2013-01-11
GEP20074098B (en) 2007-05-10
UA78232C2 (uk) 2007-03-15
US20110212930A1 (en) 2011-09-01
IL203533A (en) 2011-12-29
PT1427415E (pt) 2009-10-29
RU2008134413A (ru) 2010-02-27
EP1427415A4 (de) 2005-11-02
EP2105436A1 (de) 2009-09-30
RS20040227A (xx) 2006-12-15
HRP20040280A2 (hr) 2007-09-30
DE60233335D1 (de) 2009-09-24
CN1578660B (zh) 2010-11-24
KR20040041167A (ko) 2004-05-14
AR067965A2 (es) 2009-10-28
NO2023030I1 (no) 2023-08-17
IL160693A0 (en) 2004-08-31
SI1427415T1 (sl) 2009-12-31

Similar Documents

Publication Publication Date Title
EP1427415B1 (de) Lactamhaltige verbindungen und ihre derivate als faktor-xa-hemmer
US6989391B2 (en) Lactam-containing compounds and derivatives thereof as factor Xa inhibitors
US7115627B2 (en) Glycinamides as factor Xa inhibitors
US6949550B2 (en) Substituted amino methyl factor Xa inhibitors
HK1061973B (en) Lactam-containing compounds and derivatives thereof as factor xa inhibitors
HK1133646A (en) Lactam-containing compounds and derivatives thereof as factor xa inhibitors

Legal Events

Date Code Title Description
PE Patent expired

Effective date: 20220916