ATE311366T1 - Benzamide und ähnliche inhibitoren vom faktor xa - Google Patents

Benzamide und ähnliche inhibitoren vom faktor xa

Info

Publication number
ATE311366T1
ATE311366T1 AT01918257T AT01918257T ATE311366T1 AT E311366 T1 ATE311366 T1 AT E311366T1 AT 01918257 T AT01918257 T AT 01918257T AT 01918257 T AT01918257 T AT 01918257T AT E311366 T1 ATE311366 T1 AT E311366T1
Authority
AT
Austria
Prior art keywords
benzamide
inhibitors
compounds
similar factor
compositions
Prior art date
Application number
AT01918257T
Other languages
English (en)
Inventor
Bing-Yan Zhu
Penglie Zhang
Lingyan Wang
Wenrong Huang
Erick Goldman
Wenhao Li
Jingmei Zuckett
Yonghong Song
Robert Scarborough
Original Assignee
Millennium Pharm Inc
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=26881428&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ATE311366(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US09/663,420 external-priority patent/US6844367B1/en
Application filed by Millennium Pharm Inc filed Critical Millennium Pharm Inc
Application granted granted Critical
Publication of ATE311366T1 publication Critical patent/ATE311366T1/de

Links

Classifications

    • 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
    • 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
    • A61K31/60—Salicylic acid; Derivatives thereof
    • A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
    • A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/12—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines
    • C07C259/18—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines having carbon atoms of hydroxamidine groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C317/34—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
    • C07C317/38—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atom of at least one amino group being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfones
    • C07C317/40—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • 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
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
AT01918257T 2000-02-29 2001-02-28 Benzamide und ähnliche inhibitoren vom faktor xa ATE311366T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18574600P 2000-02-29 2000-02-29
US09/663,420 US6844367B1 (en) 1999-09-17 2000-09-15 Benzamides and related inhibitors of factor Xa
PCT/US2001/006255 WO2001064643A2 (en) 2000-02-29 2001-02-28 BENZAMIDES AND RELATED INHIBITORS OF FACTOR Xa

Publications (1)

Publication Number Publication Date
ATE311366T1 true ATE311366T1 (de) 2005-12-15

Family

ID=26881428

Family Applications (1)

Application Number Title Priority Date Filing Date
AT01918257T ATE311366T1 (de) 2000-02-29 2001-02-28 Benzamide und ähnliche inhibitoren vom faktor xa

Country Status (9)

Country Link
US (13) US6376515B2 (de)
EP (1) EP1259485B1 (de)
AT (1) ATE311366T1 (de)
AU (2) AU2001245353A1 (de)
CA (1) CA2401778C (de)
DE (1) DE60115394T2 (de)
DK (1) DK1259485T3 (de)
ES (1) ES2254385T3 (de)
WO (2) WO2001064643A2 (de)

Families Citing this family (229)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6822267B1 (en) * 1997-08-20 2004-11-23 Advantest Corporation Signal transmission circuit, CMOS semiconductor device, and circuit board
DK1259485T3 (da) * 2000-02-29 2006-04-10 Millennium Pharm Inc Benzamider og beslægtede inhibitorer for faktor Xa
AU776053B2 (en) 2000-03-31 2004-08-26 Astellas Pharma Inc. Diazepan derivatives or salts thereof
TWI290136B (en) 2000-04-05 2007-11-21 Daiichi Seiyaku Co Ethylenediamine derivatives
WO2002010154A2 (en) 2000-07-27 2002-02-07 Eli Lilly And Company Substituted heterocyclic amides
EP1336605B1 (de) * 2000-11-22 2006-04-12 Astellas Pharma Inc. Substituierte phenolderivate und deren salze als hemmstoffe von koagulations faktor x
US7163938B2 (en) 2000-11-28 2007-01-16 Eli Lilly And Company Substituted carboxamides
US7507767B2 (en) 2001-02-08 2009-03-24 Schering Corporation Cannabinoid receptor ligands
US7067539B2 (en) 2001-02-08 2006-06-27 Schering Corporation Cannabinoid receptor ligands
US7312235B2 (en) * 2001-03-30 2007-12-25 Millennium Pharmaceuticals, Inc. Benzamide inhibitors of factor Xa
US7365205B2 (en) 2001-06-20 2008-04-29 Daiichi Sankyo Company, Limited Diamine derivatives
SE0102764D0 (sv) 2001-08-17 2001-08-17 Astrazeneca Ab Compounds
AUPR738301A0 (en) * 2001-08-30 2001-09-20 Starpharma Limited Chemotherapeutic agents
MXPA04002397A (es) 2001-09-14 2004-12-02 Methylgene Inc Inhibidores de histona deacetilasa.
US6897220B2 (en) * 2001-09-14 2005-05-24 Methylgene, Inc. Inhibitors of histone deacetylase
US7868204B2 (en) * 2001-09-14 2011-01-11 Methylgene Inc. Inhibitors of histone deacetylase
CN100567266C (zh) 2001-11-14 2009-12-09 先灵公司 类大麻苷受体配体
EP1314733A1 (de) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indol-2-carbonsäureamide als Faktor-Xa-Hemmer
US7030141B2 (en) * 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
EP1456175A1 (de) * 2001-12-07 2004-09-15 Eli Lilly And Company Substituierte heterozyklische karboxamide mit antithrombotischer aktivität
AU2003223708A1 (en) * 2002-04-23 2003-11-10 Axys Pharmaceuticals, Inc. Novel phenyl derivatives as inducers of apoptosis
DE60319714T2 (de) 2002-06-19 2009-04-02 Schering Corp. Agonisten des cannabinoidrezeptors
AR040336A1 (es) 2002-06-26 2005-03-30 Glaxo Group Ltd Compuesto de piperidina, uso del mismo para la fabricacion de un medicamento, composicion farmaceutica que lo comprende y procedimiento para preparar dicho compuesto
GB0215293D0 (en) 2002-07-03 2002-08-14 Rega Foundation Viral inhibitors
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
EP1556037B1 (de) 2002-10-18 2006-11-02 F. Hoffmann-La Roche Ag 4-piperazinylbenzolsulfonyl-indole mit 5-ht6 rezeptor-affinität
GB0226930D0 (en) 2002-11-19 2002-12-24 Astrazeneca Ab Chemical compounds
CA2507707C (en) 2002-12-03 2011-06-21 Axys Pharmaceuticals, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
TWI299664B (en) 2003-01-06 2008-08-11 Osi Pharm Inc (2-carboxamido)(3-amino)thiophene compounds
US7696225B2 (en) 2003-01-06 2010-04-13 Osi Pharmaceuticals, Inc. (2-carboxamido)(3-Amino) thiophene compounds
WO2004069824A1 (ja) 2003-02-07 2004-08-19 Daiichi Pharmaceutical Co., Ltd. ピラゾール誘導体
AR043633A1 (es) 2003-03-20 2005-08-03 Schering Corp Ligandos de receptores de canabinoides
DE502004009440D1 (de) * 2003-04-03 2009-06-10 Merck Patent Gmbh Pyrrolidin-1,2-dicarbonsäure-1-(phenylamid)-2-(4-(3-oxo-morpholin-4-yl)-phenylamid) derivate und verwandte verbindungen als inhibitoren des koagulationsfaktors xa zur behandlung von thromboembolischen erkrankungen
MXPA05010445A (es) * 2003-04-03 2005-11-04 Merck Patent Gmbh Derivados de azaprolina.
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
BRPI0412259B1 (pt) 2003-07-22 2019-08-20 Astex Therapeutics Limited Compostos de 1H-pirazol 3,4-dissubstituídos como moduladores de quinases dependentes de ciclina (CDK), seus usos, processo para a preparação dos mesmos e composição farmacêutica
ATE352550T1 (de) 2003-09-19 2007-02-15 Astrazeneca Ab Chinazolinderivate
CA2539117A1 (en) 2003-09-24 2005-04-07 Methylgene Inc. Inhibitors of histone deacetylase
SE0302573D0 (sv) * 2003-09-26 2003-09-26 Astrazeneca Ab Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
US7511066B2 (en) * 2003-09-30 2009-03-31 Eli Lilly And Company Antithrombotic aromatic ethers
JP4667384B2 (ja) 2003-10-07 2011-04-13 レノビス， インコーポレイテッド イオンチャネルリガンドとしてのアミド誘導体および薬学的組成物、ならびにこれらを使用する方法
KR20060110288A (ko) * 2003-10-09 2006-10-24 밀레니엄 파머슈티컬스 인코퍼레이티드 인자 ｘａ 의 저해제로서의 티오에테르-치환 벤즈아미드
ES2381890T3 (es) * 2003-12-22 2012-06-01 K.U.Leuven Research & Development Compuesto de imidazo[4,5-c]piridina y métodos de tratamiento antiviral
AU2004303602C1 (en) 2003-12-23 2009-05-28 Astex Therapeutics Limited Pyrazole derivatives as protein kinase modulators
US20050165015A1 (en) * 2004-01-23 2005-07-28 Ncube Mghele V. Vanilloid receptor ligands and their use in treatments
CA2554686A1 (en) * 2004-02-18 2005-09-01 Astrazeneca Ab Compounds
US20080280872A1 (en) * 2004-02-18 2008-11-13 Craig Johnstone Benzamide Derivatives and Their Use as Glucokinase Activating Agents
US7253204B2 (en) 2004-03-26 2007-08-07 Methylgene Inc. Inhibitors of histone deacetylase
US7166738B2 (en) 2004-04-23 2007-01-23 Roche Palo Alto Llc Non-nucleoside reverse transcriptase inhibitors
US7625949B2 (en) 2004-04-23 2009-12-01 Roche Palo Alto Llc Methods for treating retroviral infections
TW200600086A (en) * 2004-06-05 2006-01-01 Astrazeneca Ab Chemical compound
US7696352B2 (en) * 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
CA2565437A1 (en) 2004-06-18 2006-01-05 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
PA8640701A1 (es) 2004-08-03 2006-09-08 Wyeth Corp Indazoles utiles para tratamiento de enfermedades cardiovascular
KR101269869B1 (ko) * 2004-09-24 2013-06-07 네오메드 인스티튜트 벤즈이미다졸 유도체, 그를 함유하는 조성물, 그의 제조방법 및 그의 용도
GB0422556D0 (en) * 2004-10-11 2004-11-10 Syngenta Participations Ag Novel insecticides
KR20070085371A (ko) 2004-10-16 2007-08-27 아스트라제네카 아베 페녹시 벤즈아미드 화합물의 제조 방법
GB0423043D0 (en) * 2004-10-16 2004-11-17 Astrazeneca Ab Compounds
GB0423044D0 (en) * 2004-10-16 2004-11-17 Astrazeneca Ab Compounds
JP2008517930A (ja) 2004-10-21 2008-05-29 トランス テック ファーマ，インコーポレイテッド ＧａｌＲ１のアゴニストとしてのビススルホンアミド化合物、組成物、及び使用法
ATE496030T1 (de) 2004-11-03 2011-02-15 Hoffmann La Roche Dicarbonsäureamidderivate und deren verwendung als inhibitoren von faktor xa
EP1817287B1 (de) 2004-11-24 2010-02-10 Eli Lilly And Company Aromatische etherderivate als thrombin-hemmer
US7666866B2 (en) * 2004-11-29 2010-02-23 Eli Lilly And Company Antithrombotic diamides
WO2006066133A2 (en) 2004-12-16 2006-06-22 Takeda San Diego, Inc. Histone deacetylase inhibitors
PT1841765E (pt) * 2004-12-21 2009-05-14 Gilead Sciences Inc Anticorpos para mcp-1 humano
US8110573B2 (en) 2004-12-30 2012-02-07 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of CDK, GSK and aurora kinases
TWI441819B (zh) 2005-01-07 2014-06-21 Synta Pharmaceuticals Corp 用於炎症及免疫相關用途之化合物
CA2594477C (en) 2005-01-21 2016-07-12 Astex Therapeutics Limited Pharmaceutical compounds
KR101345002B1 (ko) 2005-01-21 2013-12-31 아스텍스 테라퓨틱스 리미티드 제약 화합물
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
EP1847527A4 (de) * 2005-02-02 2009-04-08 Ajinomoto Kk Neue benzamidinverbindungen
US7576099B2 (en) 2005-02-28 2009-08-18 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
WO2006095263A1 (en) 2005-03-10 2006-09-14 Pfizer Japan Inc. Substituted n-sulfonylaminophenylethyl-2-phenoxy acetamide compounds
US7264402B2 (en) * 2005-03-10 2007-09-04 Corning Cable Systems Llc Multi-fiber optic receptacle and plug assembly
EP1896436A2 (de) 2005-05-11 2008-03-12 Takeda San Diego, Inc. Inhibitoren der histondeacetylase
JP2008542247A (ja) * 2005-05-24 2008-11-27 アストラゼネカ アクチボラグ グルコキナーゼモジュレーターとしての２−フェニル置換イミダゾール［４，５ｂ］ピリジン／ピラジンおよびプリン誘導体
TW200714597A (en) * 2005-05-27 2007-04-16 Astrazeneca Ab Chemical compounds
WO2006136821A1 (en) 2005-06-22 2006-12-28 Astex Therapeutics Limited Pharmaceutical compounds
US8541461B2 (en) 2005-06-23 2013-09-24 Astex Therapeutics Limited Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators
NZ575512A (en) 2005-07-09 2009-11-27 Astrazeneca Ab Heteroaryl benzamide derivatives for use as GLK activators in the treatment of diabetes
US20080234273A1 (en) * 2005-07-09 2008-09-25 Mckerrecher Darren Heteroaryl Benzamide Derivatives for Use as Glk Activators in the Treatment of Diabetes
US20110053910A1 (en) * 2005-07-09 2011-03-03 Mckerrecher Darren 2 -heterocyclyloxybenzoyl amino heterocyclyl compounds as modulators of glucokinase for the treatment of type 2 diabetes
ZA200800901B (en) * 2005-07-14 2010-05-26 Takeda San Diego Inc Histone deacetylase inhibitors
US9202182B2 (en) * 2005-08-11 2015-12-01 International Business Machines Corporation Method and system for analyzing business architecture
HRP20100542T1 (hr) 2005-09-16 2010-11-30 Arrow Therapeutics Limited Derivati bifenila i njihova uporaba za liječenje hepatitisa c
KR20080056220A (ko) 2005-10-19 2008-06-20 에프. 호프만-라 로슈 아게 페닐-아세트아마이드 ｎｎｒｔ 저해제
NZ592533A (en) * 2005-11-08 2012-08-31 Millennium Pharm Inc METHOD FOR THE PREPARATION OF N-(5-CHLORO-2-PYRIDINYL)-2-[[4-[(DIMETHYLAMINO) IMINOMETHYL] BENZOYL] AMINO]-5-METHOXY-BENZAMIDE, A FACTOR Xa INHIBITOR
TW200738621A (en) * 2005-11-28 2007-10-16 Astrazeneca Ab Chemical process
JP5474354B2 (ja) 2005-12-30 2014-04-16 アステックス、セラピューティックス、リミテッド 医薬化合物
EP1976835A2 (de) * 2006-01-13 2008-10-08 Takeda San Diego, Inc. Histondeacetylase-inhibitoren
CA2642813A1 (en) 2006-02-28 2007-09-07 Merck & Co., Inc. Inhibitors of histone deacetylase
TW200745049A (en) * 2006-03-23 2007-12-16 Astrazeneca Ab New crystalline forms
US20090186810A1 (en) * 2006-03-27 2009-07-23 Portola Pharmaceuticals, Inc. Potassium channel modulators and platelet procoagulant activity
AR060213A1 (es) 2006-03-31 2008-06-04 Glaxo Group Ltd Compuesto de piperazinil - piridinil -bencensulfonamida , su uso para fabricar un medicamento proceso para la preparacion del mismo composicion farmaceutica que lo comprende y proceso para prepararla
CN101466670B (zh) * 2006-04-07 2013-04-17 梅特希尔基因公司 组蛋白脱乙酰酶抑制剂
TW200808769A (en) * 2006-04-18 2008-02-16 Astrazeneca Ab Therapeutic compounds
EP2016072B1 (de) 2006-05-05 2014-07-16 Millennium Pharmaceuticals, Inc. Faktor-xa-hemmer
JP5523829B2 (ja) 2006-06-29 2014-06-18 アステックス、セラピューティックス、リミテッド 複合薬剤
WO2008001101A2 (en) * 2006-06-29 2008-01-03 Astex Therapeutics Limited Pharmaceutical combinations
HRP20090078A2 (en) * 2006-07-07 2009-06-30 Gilead Sciences Novel pyridazine compound and use thereof
TW200825063A (en) * 2006-10-23 2008-06-16 Astrazeneca Ab Chemical compounds
SA07280576B1 (ar) * 2006-10-26 2011-06-22 استرازينيكا ايه بي مركبات بنزويل أمينو سيكليل غير متجانسة بأعتبارها عوامل منشطة للجلوكوكيناز
EP2404906B1 (de) 2006-11-02 2015-07-15 Millennium Pharmaceuticals, Inc. Verfahren zur Synthetisierung pharmazeutischer Salze aus einem Faktor XA-Hemmer
CN101583593A (zh) 2006-11-13 2009-11-18 辉瑞产品公司 二芳基、二吡啶基和芳基-吡啶基衍生物及其用途
PT2101760E (pt) * 2006-12-08 2013-05-07 Millennium Pharm Inc Formulações de dose unitária e métodos de tratamento da trombose com um inibidor oral do fator xa
AR064625A1 (es) * 2006-12-21 2009-04-15 Astrazeneca Ab Forma cristalina de 3-{[5-(azetidin-1-ilcarbonil)pirazin-2-il]oxi}-5-[(1-metiletil)oxi]-n-1h-pirazol-3-ilbenzamida
JP2010515691A (ja) * 2007-01-05 2010-05-13 ミレニアム・ファーマシューティカルズ・インコーポレイテッド 第Ｘａ因子阻害剤
UY30892A1 (es) * 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
US8618324B2 (en) * 2007-03-13 2013-12-31 Board Of Regents, The University Of Texas System Composition and method for making oligo-benzamide compounds
GB0704932D0 (en) 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
BRPI0809655B8 (pt) * 2007-04-13 2021-05-25 Millennium Pharm Inc uso de um composto e um agente terapêutico,composição farmacêutica,e,kit
ES2467468T3 (es) * 2007-05-02 2014-06-12 Portola Pharmaceuticals, Inc. Terapia de combinación con un compuesto que actúa como inhibidor del receptor de ADP plaquetario
UA99466C2 (en) 2007-07-06 2012-08-27 Гилиад Сайенсиз, Инк. Crystalline pyridazine compound
DK2915564T3 (da) 2007-09-28 2021-02-08 Alexion Pharma Inc Antidoter mod faktor XA-inhibitorer og fremgangsmåder til anvendelse deraf
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
MX2011001333A (es) 2008-08-04 2011-03-15 Astrazeneca Ab Derivados de pirazolo [3, 4] pirimidin-4-ilo y sus usos para tratar la diabetes y obesidad.
US8455439B2 (en) 2008-11-14 2013-06-04 Portola Pharmaceuticals, Inc. Antidotes for factor Xa inhibitors and methods of using the same in combination with blood coagulating agents
UA106740C2 (uk) * 2009-01-30 2014-10-10 Глаксосмітклайн Ллс Кристалічний гідрохлорид n-{(1s)-2-аміно-1-[(3-фторфеніл)метил]етил}-5-хлор-4-(4-хлор-1-метил-1h-піразол-5-іл)-2-тіофенкарбоксаміду
GB0902406D0 (en) * 2009-02-13 2009-04-01 Astrazeneca Ab Crystalline polymorphic form
GB0902434D0 (en) * 2009-02-13 2009-04-01 Astrazeneca Ab Chemical process
CN108524505A (zh) 2009-03-13 2018-09-14 安吉奥斯医药品有限公司 用于细胞增殖相关病症的方法和组合物
PL3604510T3 (pl) 2009-03-30 2025-07-28 Alexion Pharmaceuticals, Inc. Antidota na inhibitory czynnika xa i sposoby ich stosowania
CN102448951B (zh) 2009-04-06 2017-05-10 安吉奥斯医药品有限公司 丙酮酸激酶m2调节剂、治疗组合物和相关使用方法
AR076221A1 (es) * 2009-04-09 2011-05-26 Astrazeneca Ab Derivado de pirazol [4,5-e] pirimidina y su uso para tratar diabetes y obesidad
AR076220A1 (es) 2009-04-09 2011-05-26 Astrazeneca Ab Derivados de pirazol [4,5 - e] pirimidina
PT2448582T (pt) 2009-06-29 2017-07-10 Agios Pharmaceuticals Inc Compostos e composições terapêuticas
CN102625712B (zh) 2009-07-15 2017-07-25 博尔托拉制药公司 用于因子xa抑制剂的解毒剂的单位剂量制剂及其使用方法
US20110086853A1 (en) * 2009-10-08 2011-04-14 William Brown Therapeutic Compounds
EP3561077B1 (de) 2009-10-21 2022-12-21 Les Laboratoires Servier Verfahren für zellproliferationsbedingte erkrankungen
EP2513094B1 (de) * 2009-12-17 2015-12-16 Millennium Pharmaceuticals, Inc. Salze und kristalline formen eines faktor-xa-inhibitors
EP2513058B1 (de) 2009-12-17 2016-11-09 Millennium Pharmaceuticals, Inc. Verfahren zur synthese von faktor-xa-hemmern
WO2011075602A1 (en) 2009-12-17 2011-06-23 Millennium Pharmaceuticals, Inc. Methods of preparing factor xa inhibitors and salts thereof
EA015918B1 (ru) * 2010-03-03 2011-12-30 Дмитрий Геннадьевич ТОВБИН УРЕТАНЫ, МОЧЕВИНЫ, АМИДЫ И РОДСТВЕННЫЕ ИНГИБИТОРЫ ФАКТОРА Xa
KR20130115108A (ko) 2010-05-28 2013-10-21 더 보드 오브 리전츠 오브 더 유니버시티 오브 텍사스 시스템 올리고－벤즈아미드 화합물 및 이의 용도
ES2547890T3 (es) * 2010-07-07 2015-10-09 Ardelyx, Inc. Compuestos y métodos para inhibir el transporte de fosfato
WO2012054110A2 (en) 2010-07-07 2012-04-26 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
EP2590510B1 (de) 2010-07-07 2016-09-28 Ardelyx, Inc. Verbindungen und verfahren zur hemmung eines phosphattransports
WO2012006474A2 (en) 2010-07-07 2012-01-12 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
AR082804A1 (es) 2010-09-01 2013-01-09 Portola Pharm Inc Formas cristalinas de un inhibidor del factor xa
AR082803A1 (es) 2010-09-01 2013-01-09 Portola Pharm Inc Metodos y formulaciones para el tratamiento de la trombosis con betrixaban y un inhibidor de la glicoproteina p
JP5837091B2 (ja) 2010-12-17 2015-12-24 アジオス ファーマシューティカルズ， インコーポレイテッド ピルビン酸キナーゼｍ２（ｐｋｍ２）調節剤としての新規ｎ−（４−（アゼチジン−１−カルボニル）フェニル）−（ヘテロ−）アリールスルホンアミド誘導体
US9328077B2 (en) 2010-12-21 2016-05-03 Agios Pharmaceuticals, Inc Bicyclic PKM2 activators
TWI549947B (zh) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
JP2014506448A (ja) 2011-01-19 2014-03-17 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 凝固因子の阻害剤に対する結合タンパク質
GB201104267D0 (en) 2011-03-14 2011-04-27 Cancer Rec Tech Ltd Pyrrolopyridineamino derivatives
CN108451955B (zh) 2011-05-03 2022-02-01 安吉奥斯医药品有限公司 用于治疗的丙酮酸激酶活化剂
WO2012151452A1 (en) 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc Pyruvate kinase activators for use in therapy
JP5934782B2 (ja) 2011-05-04 2016-06-15 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． アミノ−ピリジン含有脾臓チロシンキナーゼ（Ｓｙｋ）阻害薬
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN102827170A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
US20150224091A1 (en) 2011-08-31 2015-08-13 Portola Pharmaceuticals, Inc. Prevention and treatment of thrombosis in medically ill patients
EP2578582A1 (de) 2011-10-03 2013-04-10 Respivert Limited 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl) Harnstoffe als p38 MAP Kinasehemmer
US9108950B2 (en) 2011-10-03 2015-08-18 Respivert, Ltd. 1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl) ureas as p38 MAP kinase inhibitors
WO2013078288A1 (en) 2011-11-23 2013-05-30 The Board Of Regents Of The University Of Texas System Oligo-benzamide compounds for use in treating cancers
WO2013078277A1 (en) 2011-11-23 2013-05-30 The Board Of Regents Of The University Of Texas System Oligo-benzamide compounds and their use in treating cancers
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
RS61664B1 (sr) 2012-04-24 2021-04-29 Vertex Pharma Inhibitori dna-pk
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
GB201216018D0 (en) 2012-09-07 2012-10-24 Cancer Rec Tech Ltd Pharmacologically active compounds
CA2885259A1 (en) 2012-10-04 2014-04-10 Pfizer Limited Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors
US20140346397A1 (en) 2012-12-27 2014-11-27 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
US9200268B2 (en) 2012-12-27 2015-12-01 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
FR3000895B1 (fr) 2013-01-11 2017-02-24 Laboratoire Francais Du Fractionnement Et Des Biotechnologies Sa Utilisation d'antidotes d'inhibiteurs de la coagulation indiques dans la prevention ou le traitement de pathologies thromboemboliques
SI3527563T1 (sl) 2013-03-12 2022-01-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK
WO2014140582A1 (en) 2013-03-14 2014-09-18 Respivert Limited Kinase inhibitors
AU2014287121B2 (en) 2013-07-11 2018-11-15 Agios Pharmaceuticals, Inc. 2,4- or 4,6-diaminopyrimidine compounds as IDH2 mutants inhibitors for the treatment of cancer
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
WO2015003360A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
EA201300843A1 (ru) * 2013-08-01 2015-04-30 Арсений Валерьевич Айбушев Карбамоилфенильные производные для остановки, предотвращения и профилактики кровотечений или усиления системы гемостаза
GB201314452D0 (en) 2013-08-13 2013-09-25 Ostara Biomedical Ltd Embryo implantation
EP3054936B1 (de) 2013-10-10 2023-10-18 Eastern Virginia Medical School 4-((2-hydroxy-3-methoxybenzyl)amino)benzolsulfonamid-derivate als 12-lipoxygenase-inhibitoren
SI3424920T1 (sl) 2013-10-17 2020-08-31 Vertex Pharmaceuticals Incorporated Kokristali (s)-n-metil-8-(1-((2'-metil-(4,5'-bipirimidin)-6-il)amino)propan-2-il) kinolin-4-karboksamida in devterirani derivati le-teh kot inhibitorji dna-pk
US9636298B2 (en) 2014-01-17 2017-05-02 Methylgene Inc. Prodrugs of compounds that enhance antifungal activity and compositions of said prodrugs
TWI664967B (zh) 2014-02-14 2019-07-11 英商瑞斯比維特有限公司 新穎化合物（一）
EA036325B1 (ru) 2014-03-14 2020-10-27 Аджиос Фармасьютикалз, Инк. Фармацевтическая композиция на основе твердой дисперсии ингибитора idh1
DE102014108210A1 (de) 2014-06-11 2015-12-17 Dietrich Gulba Rodentizid
CN107073082B (zh) 2014-08-20 2021-04-30 博尔托拉制药公司 Xa因子解毒剂的冻干制剂
GB201501302D0 (en) 2015-01-27 2015-03-11 Ostara Biomedical Ltd Embryo implantation
SMT202300344T1 (it) 2015-06-11 2023-11-13 Agios Pharmaceuticals Inc Metodi di utilizzo degli attivatori della piruvato chinasi
CN106349228B (zh) 2015-07-17 2019-07-09 广东东阳光药业有限公司 取代的喹唑啉酮类化合物及其制备方法和用途
GB201514021D0 (en) 2015-08-07 2015-09-23 Arner Elias Set Jeno Novel Pyridines and their use in the treatment of cancer
GB201517523D0 (en) 2015-10-05 2015-11-18 Ostara Biomedical Ltd Methods and compositions for managing reproduction
ES2897959T3 (es) 2015-10-15 2022-03-03 Servier Lab Terapia de combinación para tratar neoplasias malignas
UA123401C2 (uk) 2015-10-15 2021-03-31 Аджиос Фармасьютікалз, Інк. Комбінована терапія для лікування злоякісних пухлин
WO2017091757A1 (en) 2015-11-24 2017-06-01 Portola Pharmaceuticals, Inc. Isotopically enriched betrixaban
WO2017125530A1 (en) 2016-01-22 2017-07-27 Janssen Pharmaceutica Nv New substituted cyanoindoline derivatives as nik inhibitors
CN109311846B (zh) 2016-01-22 2021-03-19 杨森制药有限公司 作为nik抑制剂的新的6元杂芳族取代的氰基吲哚衍生物
CN108883160B (zh) 2016-02-24 2022-06-28 博尔托拉制药公司 因子xa解毒剂的冻干制剂
RU2698202C2 (ru) * 2016-06-01 2019-08-23 Закрытое акционерное общество "ФАРМА ВАМ" СПОСОБ ПОЛУЧЕНИЯ ПРЯМОГО ИНГИБИТОРА ФАКТОРА Ха
PE20190661A1 (es) 2016-06-17 2019-05-08 Portola Pharm Inc Preparacion de derivados del factor xa
CN109641882B (zh) 2016-06-30 2022-10-28 杨森制药有限公司 作为nik抑制剂的杂芳族衍生物
WO2018002219A1 (en) 2016-06-30 2018-01-04 Janssen Pharmaceutica Nv Cyanoindoline derivatives as nik inhibitors
CR20220309A (es) 2016-09-02 2022-09-16 Cyclerion Therapeutics Inc Estimuladores de sgc
KR20190062485A (ko) 2016-09-27 2019-06-05 버텍스 파마슈티칼스 인코포레이티드 Dna-손상제 및 dna-pk 저해제의 조합을 사용한 암 치료 방법
WO2018069936A1 (en) 2016-10-13 2018-04-19 Mylan Laboratories Limited Polymorphs and solid dispersion of betrixaban and methods for the preparation thereof
KR20190115011A (ko) 2017-02-07 2019-10-10 오블리크 세러퓨틱스 에이비 설피닐피리딘 및 암의 치료에서 이의 용도
CA3051538A1 (en) 2017-02-07 2018-08-16 Oblique Therapeutics Ab Heterocyclylsulfonyl-substituted pyridines and their use in the treatment of cancer
MA47458A (fr) 2017-02-07 2019-12-18 Oblique Therapeutics Ab Pyridines à substitution hydrocarbylsulfonyle et leur utilisation dans le traitement du cancer
JP2020507625A (ja) 2017-02-07 2020-03-12 オブリーク セラピューティクス アーベー ヘテロアリールスルホニル置換ピリジンおよび癌の治療におけるそれらの使用
WO2018229796A2 (en) 2017-06-14 2018-12-20 Mylan Laboratories Limited A process for betrixaban hydrochloride and betrixaban maleate salt
UY37806A (es) 2017-07-11 2020-01-31 Vertex Pharma Carboxamidas como moduladores de los canales de sodio
US11247987B2 (en) 2017-10-06 2022-02-15 Forma Therapeutics, Inc. Inhibiting ubiquitin specific peptidase 30
PL3786160T3 (pl) 2017-10-27 2022-10-24 Boehringer Ingelheim International Gmbh Pochodne pirydyny i ich zastosowania terapeutyczne jako inhibitory trpc6
CN118286225A (zh) 2018-04-26 2024-07-05 辉瑞公司 作为细胞周期蛋白依赖性激酶抑制剂的2-氨基-吡啶或2-氨基-嘧啶衍生物
GB201807014D0 (en) 2018-04-30 2018-06-13 Univ Leeds Innovations Ltd Factor xlla inhibitors
ES2988920T3 (es) 2018-05-17 2024-11-22 Forma Therapeutics Inc Compuestos bicíclicos fusionados útiles como inhibidores de la peptidasa 30 específica de ubiquitina
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
GB201810092D0 (en) 2018-06-20 2018-08-08 Ctxt Pty Ltd Compounds
GB201810581D0 (en) 2018-06-28 2018-08-15 Ctxt Pty Ltd Compounds
MX2021002981A (es) 2018-10-05 2021-05-14 Forma Therapeutics Inc Pirrolinas fusionadas que actuan como inhibidores de la proteasa 30 especifica de la ubiquitina (usp30).
US12441703B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
WO2020146612A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
PL4299135T3 (pl) 2019-06-18 2025-11-12 Pfizer Inc. Pochodne benzizoksazolosulfonamidu
HUE069128T2 (hu) 2019-12-06 2025-02-28 Vertex Pharma Szubsztituált tetrahidrofurán vegyületek mint nátriumcsatornák modulátorai
TWI883391B (zh) 2020-02-18 2025-05-11 美商基利科學股份有限公司 抗病毒化合物
TWI874791B (zh) 2020-02-18 2025-03-01 美商基利科學股份有限公司 抗病毒化合物
AR121356A1 (es) 2020-02-18 2022-05-11 Gilead Sciences Inc Compuestos antivirales
WO2022211680A1 (ru) * 2021-03-30 2022-10-06 Общество С Ограниченной Ответственностью "Фармадиол" Способ получения антикоагулянта n-(5-хлорпиридин-2-ил)-2-({4-[этан-имидоил(метил)амино]бензоил}амино)-5-метилбензамид гидрохлорида
EP4070658A1 (de) 2021-04-06 2022-10-12 BIORoxx GmbH Verwendung von blutgerinnungshemmenden verbindungen als rodentizide
EP4323362B1 (de) 2021-04-16 2025-05-07 Gilead Sciences, Inc. Verfahren zur herstellung von carbanukleosiden mit amiden
GB202107722D0 (en) 2021-05-28 2021-07-14 Lunac Therapeutics Ltd Factor XIIA Inhibitors
AU2022284886A1 (en) 2021-06-04 2023-11-30 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamides as modulators of sodium channels
CA3228162A1 (en) 2021-08-18 2023-02-23 Gilead Sciences, Inc. Phospholipid compounds and methods of making and using the same
IL321433A (en) 2022-12-16 2025-08-01 Astrazeneca Ab Purines 2,6,9 trimethylated
NL2036011B1 (en) 2023-10-12 2025-04-30 Synapse Res Institute Molecules for reversing anti-coagulant activity of direct oral anticoagulants

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2095619A (en) 1937-10-12 Aryl oxides
CH428747A (de) * 1961-09-11 1967-01-31 Wander Ag Dr A Verfahren zur Herstellung neuer Harnstoff- und Thioharnstoffderivate
GB1047245A (de) * 1963-02-15
JPS6033389B2 (ja) * 1979-02-22 1985-08-02 日産化学工業株式会社 複素環エ−テル系フェノシキ脂肪酸誘導体、その製造法および該誘導体を含有する除草剤
GB2095239B (en) 1981-02-27 1985-03-06 Torii & Co Ltd Novel amidine compounds
US4500714A (en) * 1981-10-15 1985-02-19 Chugai Seiyaku Kabushiki Kaisha 3-Substituted-ureido-N-pyridyl benzamides
US4588587A (en) 1983-03-01 1986-05-13 Pennsylvania Hospital Method of treatment to inhibit metastasis
JPS59181257A (ja) 1983-03-31 1984-10-15 Chugai Pharmaceut Co Ltd ウレイドベンズアミド誘導体
JPS648675A (en) 1987-06-30 1989-01-12 Mitsubishi Electric Corp Formation of schottky gate
JP2668231B2 (ja) 1987-12-29 1997-10-27 大日精化工業株式会社 電子写真感光体
AU606808B2 (en) * 1988-06-29 1991-02-14 Otsuka Pharmaceutical Factory, Inc. Arylcarboxamide substituted by alkylphosphonates, process for preparing the same and a pharmaceutical composition containing the same
JPH0418675A (ja) 1990-05-11 1992-01-22 Ricoh Co Ltd 回路図入力装置
GB9816837D0 (en) * 1998-08-04 1998-09-30 Zeneca Ltd Amide derivatives
ZA928276B (en) 1991-10-31 1993-05-06 Daiichi Seiyaku Co Aromatic amidine derivates and salts thereof.
US5612360A (en) 1992-06-03 1997-03-18 Eli Lilly And Company Angiotensin II antagonists
CA2151044A1 (en) 1992-12-15 1994-06-23 Terence K. Brunck Novel inhibitors for factor xa
US5610335A (en) 1993-05-26 1997-03-11 Cornell Research Foundation Microelectromechanical lateral accelerometer
PT798295E (pt) 1994-12-02 2003-07-31 Yamanouchi Pharma Co Ltd Novo derivado de amidinonaftilo ou sal deste
CA2214685C (en) 1995-03-10 2008-05-20 Berlex Laboratories, Inc. Benzamidine derivatives their preparation and their use as anti-coagulants
EP0742208A1 (de) 1995-05-05 1996-11-13 Grelan Pharmaceutical Co., Ltd. 2-Ureido-benzamid-Derivate
US5849759A (en) 1995-12-08 1998-12-15 Berlex Laboratories, Inc. Naphthyl-substituted benzimidazole derivatives as anti-coagulants
US5994375A (en) 1996-02-12 1999-11-30 Berlex Laboratories, Inc. Benzamidine derivatives substituted by amino acid and hydroxy acid derivatives and their use as anti-coagulants
AU4064597A (en) 1996-08-16 1998-03-06 Du Pont Pharmaceuticals Company Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof
WO1998009630A1 (en) 1996-09-09 1998-03-12 Smithkline Beecham Corporation Compounds and methods
CA2276034A1 (en) 1996-12-23 1998-07-02 Mimi Lifen Quan Oxygen or sulfur containing 5-membered heteroaromatics as factor xa inhibitors
CZ225699A3 (cs) 1996-12-23 2000-09-13 Du Pont Pharmaceuticals Company Dusíkaté heteroaromatické sloučeniny jako inhibitory faktoru Xa
EP0993448A1 (de) 1997-06-19 2000-04-19 The Du Pont Merck Pharmaceutical Company (amidino)6-gliedrige aromaten als factor xa inhibitoren
EP0999834B1 (de) 1997-06-26 2005-10-12 Eli Lilly And Company Antithrombosemittel
IL133621A0 (en) 1997-06-26 2001-04-30 Lilly Co Eli Antithrombotic agents
WO1999000127A1 (en) * 1997-06-26 1999-01-07 Eli Lilly And Company Antithrombotic agents
ES2241151T3 (es) 1997-06-26 2005-10-16 Eli Lilly And Company Agentes antitromboticos.
EP1001782A4 (de) 1997-08-11 2002-01-30 Boehringer Ingelheim Pharma 5,6-HETEROARYL-DIPYRIDO (2-3-b:3',2'-f) AZEPINE UND DEREN VERWENDUNG ZUR PROPHYLAXE UND BEHANDLUNG VON HIV-INFEKTIONEN
CN1268116A (zh) 1997-08-27 2000-09-27 橘生药品工业株式会社 3－脒基苯胺衍生物,活化血凝固因子x抑制剂和制备这些物质的中间体
US6140351A (en) 1997-12-19 2000-10-31 Berlex Laboratories, Inc. Ortho-anthranilamide derivatives as anti-coagulants
ATE260103T1 (de) 1997-12-19 2004-03-15 Schering Ag Ortho-anthranilamide derivate als antikoagulantien
EP0937711A1 (de) * 1998-02-18 1999-08-25 Roche Diagnostics GmbH Neue Thiobenzamide, Verfahren zu ihrer Herstellung sowie diese enthaltende Arzneimittel
JPH11302177A (ja) 1998-04-27 1999-11-02 Otsuka Pharmaceut Factory Inc 腎炎治療剤
WO2000034269A1 (en) 1998-12-09 2000-06-15 American Home Products Corporation Thiourea inhibitors of herpes viruses
WO2000034238A1 (en) 1998-12-09 2000-06-15 American Home Products Corporation Thiourea inhibitors of herpes viruses
IL143183A0 (en) 1998-12-09 2002-04-21 American Home Prod Alpha-methylbenzyl-containing thiourea inhibitors of herpres viruses containing a phenylenediamine group
CZ20012063A3 (cs) 1998-12-09 2001-10-17 American Home Products Corporation Thiomočovinové sloučeniny obsahující heterocyklický karboxamid a substituovanou fenylendiaminovou skupinu jako inhibitory herpes virů
PL349217A1 (en) 1998-12-09 2002-07-01 American Home Prod Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing phenylenediamine group
IL143204A0 (en) 1998-12-09 2002-04-21 American Home Prod Acetamide and substituted acetamide-containing thiourea inhibitors of herpes viruses
WO2000034268A1 (en) 1998-12-09 2000-06-15 American Home Products Corporation Thiourea inhibitors of herpes viruses
JP2002533454A (ja) 1998-12-23 2002-10-08 イーライ・リリー・アンド・カンパニー 芳香族アミド類
BR0014076A (pt) 1999-09-17 2002-10-15 Millennium Pharm Inc Benzamidas e inibidores correlatos do fator xa
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
US6720317B1 (en) 1999-09-17 2004-04-13 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
US6844367B1 (en) 1999-09-17 2005-01-18 Millennium Pharmaceuticals, Inc. Benzamides and related inhibitors of factor Xa
DK1259485T3 (da) 2000-02-29 2006-04-10 Millennium Pharm Inc Benzamider og beslægtede inhibitorer for faktor Xa
AU776053B2 (en) 2000-03-31 2004-08-26 Astellas Pharma Inc. Diazepan derivatives or salts thereof
US6373515B1 (en) * 2000-08-09 2002-04-16 Hewlett-Packard Company Variable resolution transition placement device
US7312235B2 (en) 2001-03-30 2007-12-25 Millennium Pharmaceuticals, Inc. Benzamide inhibitors of factor Xa
PL367340A1 (en) * 2001-07-31 2005-02-21 Wayne State University Quinoline derivatives and use thereof as antitumor agents
KR20060110288A (ko) * 2003-10-09 2006-10-24 밀레니엄 파머슈티컬스 인코퍼레이티드 인자 ｘａ 의 저해제로서의 티오에테르-치환 벤즈아미드
CA2565437A1 (en) * 2004-06-18 2006-01-05 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
US7696352B2 (en) * 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
NZ592533A (en) * 2005-11-08 2012-08-31 Millennium Pharm Inc METHOD FOR THE PREPARATION OF N-(5-CHLORO-2-PYRIDINYL)-2-[[4-[(DIMETHYLAMINO) IMINOMETHYL] BENZOYL] AMINO]-5-METHOXY-BENZAMIDE, A FACTOR Xa INHIBITOR
US20090186810A1 (en) 2006-03-27 2009-07-23 Portola Pharmaceuticals, Inc. Potassium channel modulators and platelet procoagulant activity
EP2016072B1 (de) * 2006-05-05 2014-07-16 Millennium Pharmaceuticals, Inc. Faktor-xa-hemmer
PT2101760E (pt) * 2006-12-08 2013-05-07 Millennium Pharm Inc Formulações de dose unitária e métodos de tratamento da trombose com um inibidor oral do fator xa
JP2010515691A (ja) * 2007-01-05 2010-05-13 ミレニアム・ファーマシューティカルズ・インコーポレイテッド 第Ｘａ因子阻害剤
BRPI0809655B8 (pt) * 2007-04-13 2021-05-25 Millennium Pharm Inc uso de um composto e um agente terapêutico,composição farmacêutica,e,kit
ES2467468T3 (es) * 2007-05-02 2014-06-12 Portola Pharmaceuticals, Inc. Terapia de combinación con un compuesto que actúa como inhibidor del receptor de ADP plaquetario

Also Published As

Publication number Publication date
AU2001250783A1 (en) 2001-09-12
US20090131411A1 (en) 2009-05-21
US8063036B2 (en) 2011-11-22
US20120083602A1 (en) 2012-04-05
US20140377247A1 (en) 2014-12-25
CA2401778A1 (en) 2001-09-07
DK1259485T3 (da) 2006-04-10
US10179124B2 (en) 2019-01-15
US9108922B2 (en) 2015-08-18
CA2401778C (en) 2010-12-21
US20040097561A1 (en) 2004-05-20
WO2001064642A3 (en) 2002-05-02
US20130172310A1 (en) 2013-07-04
US20030162690A1 (en) 2003-08-28
US6835739B2 (en) 2004-12-28
DE60115394D1 (de) 2006-01-05
US20100298284A1 (en) 2010-11-25
US20180036296A1 (en) 2018-02-08
US7342013B2 (en) 2008-03-11
US7314874B2 (en) 2008-01-01
US20160317511A1 (en) 2016-11-03
US8518977B2 (en) 2013-08-27
US7727982B2 (en) 2010-06-01
US9629831B2 (en) 2017-04-25
WO2001064643A2 (en) 2001-09-07
US20020002183A1 (en) 2002-01-03
WO2001064642A2 (en) 2001-09-07
US8691847B2 (en) 2014-04-08
EP1259485A2 (de) 2002-11-27
US20060241153A1 (en) 2006-10-26
WO2001064643A3 (en) 2002-04-04
US7727981B2 (en) 2010-06-01
AU2001245353A1 (en) 2001-09-12
HK1051539A1 (en) 2003-08-08
DE60115394T2 (de) 2006-10-19
US20050261346A1 (en) 2005-11-24
US6376515B2 (en) 2002-04-23
EP1259485B1 (de) 2005-11-30
ES2254385T3 (es) 2006-06-16
US20070021472A1 (en) 2007-01-25

Similar Documents

Publication Publication Date Title
ATE311366T1 (de) Benzamide und ähnliche inhibitoren vom faktor xa
WO2000071493A3 (en) INHIBITORS OF FACTOR Xa
BR0014078A (pt) Inibidores de fator xa
BG106586A (en) Pyrazolopyramidines as therapeutic agents
WO2001056989A3 (en) Inhibitors of factor xa
ZA200306419B (en) Phenyl derivatives.
WO2000071515A3 (en) INHIBITORS OF FACTOR Xa
BG106013A (en) New compounds and compositions as protease inhibitors
NZ511927A (en) Phenylglycine derivatives
CY1112024T1 (el) Αναστολεις υποδοχεων adp αιμοπεταλιων
NO20021229D0 (no) Benzamider og lignende inhibitorer for faktor Xa
WO2002026712A3 (en) Quaternary amines and related inhibitors of factor xa
ES2421948T3 (es) Compuestos y composiciones para suministrar agentes activos
DE60230127D1 (de) Inhibitoren von integrin alpha-v-beta-6
DE60324544D1 (de) Muskarin antagonisten
DE60221505D1 (de) FAKTOR Xa BENZAMIDIN INHIBITOREN
WO2001072708A3 (en) OXINDOLE INHIBITORS OF FACTOR Xa
MA28279A1 (fr) Derives d'indole et utilisation de ceux-ci comme inhibiteurs de kinase, notamment des inhibiteurs de ikk2
YU87202A (sh) Derivati arilmetilamina koji se koriste kao inhibitori triptaze
WO2001057021A3 (en) 2-[1H]-QUINOLONE AND 2-[1H]-QUINOXALONE INHIBITORS OF FACTOR Xa
WO2002026720A3 (en) PIPERAZINE BASED INHIBITORS OF FACTOR Xa
SE0302756D0 (sv) Novel Compounds
MX9709910A (es) Compuestos que contienen arginina e imitaciones de arginina, su uso y composiciones que los contienen.
ATE369348T1 (de) Zyklisierte benzamid-neurokinin-antagonisten zur verwendung in therapie
DE69803383D1 (de) Selektive inhibitoren des faktors x, eine azepinonstruktur enthaltend

Legal Events

Date Code Title Description
UEP Publication of translation of european patent specification

Ref document number: 1259485

Country of ref document: EP