DK1259485T3 - Benzamider og beslægtede inhibitorer for faktor Xa - Google Patents

Benzamider og beslægtede inhibitorer for faktor Xa

Info

Publication number
DK1259485T3
DK1259485T3 DK01918257T DK01918257T DK1259485T3 DK 1259485 T3 DK1259485 T3 DK 1259485T3 DK 01918257 T DK01918257 T DK 01918257T DK 01918257 T DK01918257 T DK 01918257T DK 1259485 T3 DK1259485 T3 DK 1259485T3
Authority
DK
Denmark
Prior art keywords
factor
benzamides
compounds
related inhibitors
compositions
Prior art date
Application number
DK01918257T
Other languages
Danish (da)
English (en)
Inventor
Penglie Zhang
Lingyan Wang
Wenrong Huang
Wenhao Li
Yonghong Song
Robert Scarborough
Bing-Yan Zhu
Erick Goldman
Jingmei Zuckett
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=DK1259485(T3) "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 DK1259485T3 publication Critical patent/DK1259485T3/da

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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
DK01918257T 2000-02-29 2001-02-28 Benzamider og beslægtede inhibitorer for faktor Xa DK1259485T3 (da)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
DK1259485T3 true DK1259485T3 (da) 2006-04-10

Family

ID=26881428

Family Applications (1)

Application Number Title Priority Date Filing Date
DK01918257T DK1259485T3 (da) 2000-02-29 2001-02-28 Benzamider og beslægtede inhibitorer for faktor Xa

Country Status (10)

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)
HK (1) HK1051539A1 (de)
WO (2) WO2001064643A2 (de)

Families Citing this family (220)

* 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
CN1283626C (zh) * 2000-11-22 2006-11-08 安斯泰来制药有限公司 取代苯衍生物或其盐
AU2001297648A1 (en) * 2000-11-28 2002-08-28 Eli Lilly And Company Substituted carboxamides as inhibitors of factor xa
US7067539B2 (en) 2001-02-08 2006-06-27 Schering Corporation Cannabinoid receptor ligands
US7507767B2 (en) 2001-02-08 2009-03-24 Schering Corporation Cannabinoid receptor ligands
US7312235B2 (en) * 2001-03-30 2007-12-25 Millennium Pharmaceuticals, Inc. Benzamide inhibitors of factor Xa
WO2003000657A1 (fr) 2001-06-20 2003-01-03 Daiichi Pharmaceutical Co., Ltd. Derives de diamine
SE0102764D0 (sv) 2001-08-17 2001-08-17 Astrazeneca Ab Compounds
AUPR738301A0 (en) * 2001-08-30 2001-09-20 Starpharma Limited Chemotherapeutic agents
EP1429765A2 (de) 2001-09-14 2004-06-23 Methylgene, Inc. Histone deacetylase-hemmer
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
NZ532291A (en) 2001-11-14 2005-11-25 Schering Corp Cannabinoid receptor ligands
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
WO2003090680A2 (en) * 2002-04-23 2003-11-06 Axys Pharmaceuticals, Inc. Novel phenyl derivatives as inducers of apoptosis
EP1539693B9 (de) 2002-06-19 2008-10-08 Schering Corporation 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
AU2003283265B2 (en) 2002-10-18 2009-03-05 F. Hoffmann-La Roche Ag 4-piperazinyl benzenesulfonyl indoles with 5-HT6 receptor affinity
GB0226930D0 (en) 2002-11-19 2002-12-24 Astrazeneca Ab Chemical compounds
PT1569912E (pt) 2002-12-03 2015-09-15 Pharmacyclics Llc Derivados 2-(2-hidroxibifenil-3-il)-1h-benzoimidazole-5- carboxamidina como inibidores do fator viia
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
TW200505447A (en) 2003-02-07 2005-02-16 Daiichi Seiyaku Co Pyrazole derivative
TW200505902A (en) 2003-03-20 2005-02-16 Schering Corp Cannabinoid receptor ligands
WO2004087646A2 (de) 2003-04-03 2004-10-14 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
DE502004003688D1 (de) 2003-04-03 2007-06-14 Merck Patent Gmbh Pyrazolidin-1,2-dicarbonsäure-1-((phenyl)-amid)-2-((phenyl)-amid) derivate als koagulationsfaktor xa inhibitoren zur behandlung von thrombosen
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
NZ544756A (en) 2003-07-22 2009-09-25 Astex Therapeutics Ltd 3,4-Disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators
ATE352550T1 (de) 2003-09-19 2007-02-15 Astrazeneca Ab Chinazolinderivate
US7868205B2 (en) * 2003-09-24 2011-01-11 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
EP1670783A2 (de) * 2003-09-30 2006-06-21 Eli Lilly And Company Aromatische ether mit antithrombotischer wirkung
BRPI0415179A (pt) 2003-10-07 2006-11-28 Renovis Inc derivados de amida como ligandos de canal de ìon e composições farmacêuticas e métodos de empregar as mesmas
US7022695B2 (en) 2003-10-09 2006-04-04 Millennium Pharmaceuticals, Inc. Thioether-substituted benzamides as inhibitors of Factor Xa
WO2005063744A2 (en) * 2003-12-22 2005-07-14 K.U. Leuven Research & Development IMIDAZO[4,5-c]PYRIDINE COMPOUNDS AND METHODS OF ANTIVIRAL TREATMENT
NZ547696A (en) 2003-12-23 2009-12-24 Astex Therapeutics Ltd 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
CA2554310A1 (en) * 2004-02-18 2005-09-01 Astrazeneca Ab Benzamide derivatives and their use as glucokinase activating agents
AU2005214137B2 (en) * 2004-02-18 2008-05-29 Astrazeneca Ab Compounds
US7253204B2 (en) * 2004-03-26 2007-08-07 Methylgene Inc. Inhibitors of histone deacetylase
US7625949B2 (en) 2004-04-23 2009-12-01 Roche Palo Alto Llc Methods for treating retroviral infections
US7166738B2 (en) 2004-04-23 2007-01-23 Roche Palo Alto Llc Non-nucleoside reverse transcriptase inhibitors
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
AU2005257999B2 (en) 2004-06-18 2011-12-08 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
CN101213194A (zh) 2004-08-03 2008-07-02 惠氏公司 可用于治疗心血管疾病的吲唑化合物
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
GB0423043D0 (en) * 2004-10-16 2004-11-17 Astrazeneca Ab Compounds
GB0423044D0 (en) * 2004-10-16 2004-11-17 Astrazeneca Ab Compounds
EP1802570A1 (de) 2004-10-16 2007-07-04 AstraZeneca AB Verfahren zur herstellung von phenoxybenzamidverbindungen
AU2005299771A1 (en) 2004-10-21 2006-05-04 High Point Pharmaceuticals, Llc Bissulfonamide compounds as agonists of GalR1, compositions, and methods of use
WO2006048152A2 (en) 2004-11-03 2006-05-11 F. Hoffmann-La Roche Ag Dicarboxamide derivatives and their use as factor xa inhibitors
WO2006057845A1 (en) 2004-11-24 2006-06-01 Eli Lilly And Company Aromatic ether derivatives useful as thrombin inhibitors
WO2006057868A1 (en) * 2004-11-29 2006-06-01 Eli Lilly And Company Antithrombotic diamides
EP1824831A2 (de) 2004-12-16 2007-08-29 Takeda San Diego, Inc. Histondeacetylase-inhibitoren
JP2008524335A (ja) * 2004-12-21 2008-07-10 ギリアド サイエンシズ， インコーポレイテッド イミダゾ［４，５−ｃ］ピリジン化合物および抗ウイルス処置法
TWI427077B (zh) 2004-12-30 2014-02-21 Astex Therapeutics Ltd 吡唑化合物及其用途和含有彼之藥學組成物
WO2006083477A2 (en) 2005-01-07 2006-08-10 Synta Pharmaceuticals Corp. Compounds for inflammation and immune-related uses
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.
BRPI0606480A (pt) 2005-01-21 2008-03-11 Astex Therapeutics Ltd compostos farmacêuticos
MX2007008781A (es) 2005-01-21 2007-09-11 Astex Therapeutics Ltd Compuestos farmaceuticos.
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
WO2006083003A1 (ja) * 2005-02-02 2006-08-10 Ajinomoto Co., Inc. 新規ベンズアミジン化合物
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
MX2007011105A (es) 2005-03-10 2007-10-08 Pfizer Compuestos de n-sulfonilaminofeniletil-2-fenoxiacetamida sustituidos.
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
WO2006125958A1 (en) * 2005-05-24 2006-11-30 Astrazeneca Ab 2-phenyl substituted imidazol [4 , 5b] pyridine/ pyrazine and purine derivatives as glucokinase modulators
TW200714597A (en) * 2005-05-27 2007-04-16 Astrazeneca Ab Chemical compounds
JP2008546751A (ja) 2005-06-22 2008-12-25 アステックス・セラピューティクス・リミテッド 医薬組成物
US8541461B2 (en) 2005-06-23 2013-09-24 Astex Therapeutics Limited Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators
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
CA2614746C (en) * 2005-07-09 2011-05-10 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
JP2009501236A (ja) * 2005-07-14 2009-01-15 タケダ サン ディエゴ インコーポレイテッド ヒストンデアセチラーゼ阻害剤
US9202182B2 (en) * 2005-08-11 2015-12-01 International Business Machines Corporation Method and system for analyzing business architecture
BRPI0615934A2 (pt) 2005-09-16 2011-05-31 Arrow Therapeutics Ltd composto ou um sal farmaceuticamente aceitável do mesmo, uso de um derivado de bifenila, composição farmacêutica, e, produto
AU2006303368B2 (en) 2005-10-19 2011-05-26 F. Hoffmann-La Roche Ag Non-Nucleoside Reverse Transcriptase Inhibitors
PE20070717A1 (es) * 2005-11-08 2007-08-17 Millennium Pharm Inc Sal de maleato y polimorfo de [2-({4-[(dimetilamino)iminometil]fenil}carbonilamino)-5-metoxifenil]-n-(5-cloro-(2-piridil))carboxamida
TW200738621A (en) 2005-11-28 2007-10-16 Astrazeneca Ab Chemical process
US8399442B2 (en) 2005-12-30 2013-03-19 Astex Therapeutics Limited Pharmaceutical compounds
JP2009525955A (ja) * 2006-01-13 2009-07-16 タケダ サン ディエゴ インコーポレイテッド ヒストンデアセチラーゼ阻害剤
EP1991226B1 (de) 2006-02-28 2013-03-20 Merck Sharp & Dohme Corp. Histondeacetylase-hemmer
TW200745049A (en) * 2006-03-23 2007-12-16 Astrazeneca Ab New crystalline forms
WO2007112367A2 (en) * 2006-03-27 2007-10-04 Portola Pharmaceuticals, Inc. Potassium channel modulators and platelet procoagulant activity
US7713978B2 (en) 2006-03-31 2010-05-11 Nigel Paul King Compounds
AU2007234843B2 (en) * 2006-04-07 2013-07-11 Methylgene Inc. Inhibitors of histone deacetylase
TW200808769A (en) * 2006-04-18 2008-02-16 Astrazeneca Ab Therapeutic compounds
CA2651303A1 (en) 2006-05-05 2007-11-15 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
EP2049119A2 (de) 2006-06-29 2009-04-22 Astex Therapeutics Limited Pharmazeutische kombinationen von 1-cyclopropyl-3-[3-(5-morphoolin-4-ylmethyl-1h-benzoimidazol-2-yl)-1h-1-pyrazol-4-yl]-harnstoff
US20110159111A1 (en) * 2006-06-29 2011-06-30 Astex Therapeutics Limited Pharmaceutical combinations
TWI360549B (en) * 2006-07-07 2012-03-21 Gilead Sciences Inc Novel pyridazine compound and use thereof
TW200825063A (en) * 2006-10-23 2008-06-16 Astrazeneca Ab Chemical compounds
TW200825060A (en) * 2006-10-26 2008-06-16 Astrazeneca Ab Chemical compounds
WO2008057972A1 (en) * 2006-11-02 2008-05-15 Millennium Pharmaceuticals, Inc. Methods of synthesizing pharmaceutical salts of a factor xa inhibitor
EP2084127A1 (de) 2006-11-13 2009-08-05 Pfizer Products Inc. Diaryl-, dipyridinyl- und arylpyridinylderivate und anwendungen davon
WO2008073670A2 (en) * 2006-12-08 2008-06-19 Millennium Pharmaceuticals, Inc. Unit dose formulations and methods of treating thrombosis with an oral factor xa inhibitor
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
US20080293704A1 (en) * 2007-01-05 2008-11-27 Millennium Pharmaceuticals, Inc. FACTOR Xa INHIBITORS
UY30892A1 (es) * 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
WO2008112939A2 (en) * 2007-03-13 2008-09-18 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
AU2008239659B2 (en) * 2007-04-13 2013-09-05 Millennium Pharmaceuticals, Inc. Combination anticoagulant therapy with a compound that acts as a factor Xa inhibitor
EP2586439A1 (de) * 2007-05-02 2013-05-01 Portola Pharmaceuticals, Inc. Kombinationstherapie mit einer Verbindung als Thrombozyt-ADP-Rezeptor-Hemmer
UA99466C2 (en) 2007-07-06 2012-08-27 Гилиад Сайенсиз, Инк. Crystalline pyridazine compound
EP2915564B1 (de) 2007-09-28 2020-11-04 Portola Pharmaceuticals, Inc. Gegenmittel für Faktor-XA-Hemmer und Verfahren zur Verwendung davon
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
AU2009278929B2 (en) 2008-08-04 2012-07-05 Astrazeneca Ab Pyrazolo [3,4] pyrimidin-4-yl derivatives and their uses to treat diabetes and obesity
EP2364165B1 (de) 2008-11-14 2018-01-03 Portola Pharmaceuticals, Inc. Antidote für faktor-xa-inhibitoren und verfahren zu ihrer verwendung in kombination mit blutgerinnungsmitteln
EP4242206A1 (de) * 2009-01-30 2023-09-13 Novartis AG Kristallines n-{(1-s)-2-amino-1-[(3-fluorphenyl)methyl]ethyl}-5-chlor-4-(4-chlor-1-methyl-1h-pyrazol-5-yl)-2-thiophencarboxamid hydrochlorid
GB0902434D0 (en) * 2009-02-13 2009-04-01 Astrazeneca Ab Chemical process
GB0902406D0 (en) * 2009-02-13 2009-04-01 Astrazeneca Ab Crystalline polymorphic form
AU2010223919B2 (en) 2009-03-13 2016-03-31 Les Laboratoires Servier Methods and compositions for cell-proliferation-related disorders
EP3604510A1 (de) 2009-03-30 2020-02-05 Portola Pharmaceuticals, Inc. Gegenmittel für faktor-xa-inhibitoren und verfahren zur verwendung davon
JP5756457B2 (ja) 2009-04-06 2015-07-29 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調節剤、治療組成物および関連する使用方法
AR076220A1 (es) 2009-04-09 2011-05-26 Astrazeneca Ab Derivados de pirazol [4,5 - e] pirimidina
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
SG10201403696UA (en) 2009-06-29 2014-10-30 Agios Pharmaceuticals Inc Therapeutic compounds and compositions
JP6163304B2 (ja) * 2009-07-15 2017-07-12 ポートラ ファーマシューティカルズ， インコーポレイテッド 第Ｘａ因子インヒビターの解毒剤の単位用量処方物およびその使用方法
US20110086853A1 (en) * 2009-10-08 2011-04-14 William Brown Therapeutic Compounds
WO2011050210A1 (en) 2009-10-21 2011-04-28 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
CA2784921A1 (en) * 2009-12-17 2011-07-14 Millennium Pharmaceuticals, Inc. Salts and crystalline forms of a factor xa inhibitor
US8742120B2 (en) 2009-12-17 2014-06-03 Millennium Pharmaceuticals, Inc. Methods of preparing factor xa inhibitors and salts thereof
ES2610145T3 (es) 2009-12-17 2017-04-26 Millennium Pharmaceuticals, Inc. Procedimientos de síntesis de inhibidores del factor Xa
EA015918B1 (ru) * 2010-03-03 2011-12-30 Дмитрий Геннадьевич ТОВБИН УРЕТАНЫ, МОЧЕВИНЫ, АМИДЫ И РОДСТВЕННЫЕ ИНГИБИТОРЫ ФАКТОРА Xa
CA2800811C (en) 2010-05-28 2019-02-26 The Board Of Regents Of The University Of Texas System Oligo-benzamide compounds and their use
EP2590965B1 (de) 2010-07-07 2016-04-20 Ardelyx, Inc. Verbindungen und verfahren zur hemmung eines phosphattransports
WO2012006473A1 (en) * 2010-07-07 2012-01-12 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
EP2590656B1 (de) 2010-07-07 2017-11-15 Ardelyx, Inc. Verbindungen und verfahren zur hemmung eines phosphattransports
JP5827328B2 (ja) 2010-07-07 2015-12-02 アーデリクス，インコーポレーテッド リン酸輸送を阻害する化合物及び方法
AR082804A1 (es) 2010-09-01 2013-01-09 Portola Pharm Inc Formas cristalinas de un inhibidor del factor xa
TW201240664A (en) 2010-09-01 2012-10-16 Portola Pharm Inc Methods and formulations of treating thrombosis with betrixaban and a P-glycoprotein inhibitor
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
MX336022B (es) 2010-12-21 2016-01-06 Agios Pharmaceuticals Inc Activadores de pkm2 bicíclicos.
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
WO2012098089A1 (en) 2011-01-19 2012-07-26 Bayer Pharma Aktiengesellschaft Binding proteins to inhibitors of coagulation factors
GB201104267D0 (en) 2011-03-14 2011-04-27 Cancer Rec Tech Ltd Pyrrolopyridineamino derivatives
BR112013028422B8 (pt) 2011-05-03 2022-01-11 Agios Pharmaceuticals Inc Ativadores de piruvato cinase para uso em terapia
US9404081B2 (en) 2011-05-03 2016-08-02 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in therapy
AU2012250958B8 (en) 2011-05-04 2017-02-09 Merck Sharp & Dohme Corp. Amino-pyridine-containing Spleen Tyrosine Kinase (Syk) inhibitors
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
JP2014528404A (ja) 2011-10-03 2014-10-27 レスピバート・リミテツド ｐ３８ＭＡＰキナーゼ阻害剤としての１−ピラゾリル−３−（４−（（２−アニリノピリミジン−４−イル）オキシ）ナフタレン−１−イル）尿素
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
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
US8754124B2 (en) 2011-11-23 2014-06-17 Board Of Regents, 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
KR102089239B1 (ko) 2012-04-24 2020-03-16 버텍스 파마슈티칼스 인코포레이티드 Dna-pk 억제제
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
JP2015531395A (ja) 2012-10-04 2015-11-02 ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ ピロロ［３，２−ｃ］ピリジントロポミオシン関連キナーゼ阻害剤
US9200268B2 (en) * 2012-12-27 2015-12-01 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
US20140346397A1 (en) 2012-12-27 2014-11-27 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
ES2900061T3 (es) 2013-03-12 2022-03-15 Vertex Pharma Inhibidores de DNA-PK
EP2970190A1 (de) 2013-03-14 2016-01-20 Respivert Limited Kinaseinhibitoren
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
CN105593215B (zh) 2013-07-11 2019-01-15 安吉奥斯医药品有限公司 用于治疗癌症的作为idh2突变体抑制剂的2,4-或4,6-二氨基嘧啶化合物
WO2015003360A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US9579324B2 (en) 2013-07-11 2017-02-28 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
JP6408569B2 (ja) 2013-10-17 2018-10-17 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ｄｎａ−ｐｋ阻害剤としての（ｓ）−ｎ−メチル−８−（１−（（２’−メチル−［４，５’−ビピリミジン］−６−イル）アミノ）プロパン−２−イル）キノリン−４−カルボキサミドおよびその重水素化誘導体の共結晶
US9636298B2 (en) 2014-01-17 2017-05-02 Methylgene Inc. Prodrugs of compounds that enhance antifungal activity and compositions of said prodrugs
CN106164067B (zh) 2014-02-14 2019-09-10 瑞斯比维特有限公司 作为抗炎化合物的芳族杂环化合物
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
LT3307271T (lt) 2015-06-11 2023-10-25 Agios Pharmaceuticals, Inc. Piruvatkinazės aktyvatorių panaudojimo būdai
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
PL3362066T3 (pl) 2015-10-15 2022-05-02 Les Laboratoires Servier Terapia skojarzona do leczenia nowotworów złośliwych
AU2016338552B2 (en) 2015-10-15 2022-04-28 Les Laboratoires Servier Combination therapy for treating malignancies
WO2017091757A1 (en) 2015-11-24 2017-06-01 Portola Pharmaceuticals, Inc. Isotopically enriched betrixaban
EP3405196B1 (de) 2016-01-22 2019-12-04 Janssen Pharmaceutica NV Neue n-phenylpyrimidin-2-aminsubstituierte cyanoindolinderivate als nik-inhibitoren
JP6916796B2 (ja) 2016-01-22 2021-08-11 ヤンセン ファーマシューティカ エヌ．ベー． Ｎｉｋ阻害剤としての新たな６員のヘテロ芳香族置換シアノインドリン誘導体
EP3419650B1 (de) 2016-02-24 2021-06-02 Alexion Pharmaceuticals, Inc. Lyophilisierte formulierungen für faktor-xa-antidot
RU2698202C2 (ru) * 2016-06-01 2019-08-23 Закрытое акционерное общество "ФАРМА ВАМ" СПОСОБ ПОЛУЧЕНИЯ ПРЯМОГО ИНГИБИТОРА ФАКТОРА Ха
DK3472314T3 (da) 2016-06-17 2021-07-26 Alexion Pharma Inc Fremstilling af faktor-xa-derivater
CN109689645B (zh) 2016-06-30 2022-06-03 杨森制药有限公司 作为nik抑制剂的氰基吲哚啉衍生物
KR102517352B1 (ko) 2016-06-30 2023-03-31 잔센파마슈티카엔.브이. Nik 억제제로서의 헤테로방향족 유도체
PT3507291T (pt) 2016-09-02 2021-08-30 Cyclerion Therapeutics Inc Estimulantes de sgc bicíclicos fundidos
TW201815418A (zh) 2016-09-27 2018-05-01 Vertex Pharma 使用dna破壞劑及dna-pk抑制劑之組合治療癌症的方法
WO2018069936A1 (en) 2016-10-13 2018-04-19 Mylan Laboratories Limited Polymorphs and solid dispersion of betrixaban and methods for the preparation thereof
AU2018218521C1 (en) 2017-02-07 2022-06-09 Oblique Therapeutics Ab Heterocyclylsulfonyl-substituted pyridines and their use in the treatment of cancer
MX2019009356A (es) 2017-02-07 2019-09-19 Oblique Therapeutics Ab Sulfinilpiridinas y su uso en el tratamiento del cancer.
RU2019128063A (ru) 2017-02-07 2021-03-09 Облик Терапьютикс Аб Углеводородсульфонилзамещенные пиридины и их применение при лечении рака
US11028067B2 (en) 2017-02-07 2021-06-08 Oblique Therapeutics Ab Heteroarylsulfonyl-substituted pyridines and their use in the treatment of cancer
WO2018229796A2 (en) 2017-06-14 2018-12-20 Mylan Laboratories Limited A process for betrixaban hydrochloride and betrixaban maleate salt
US10647661B2 (en) 2017-07-11 2020-05-12 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
MX2020003671A (es) 2017-10-06 2020-08-03 Forma Therapeutics Inc Inhibicion de peptidasa especifica de ubiquitina 30.
HUE059450T2 (hu) 2017-10-27 2022-11-28 Boehringer Ingelheim Int Piridin származékok és ezek terápiás alkalmazásai TRPC6 inhibitorokként
MX2020011294A (es) 2018-04-26 2020-11-18 Pfizer Derivados de 2-amino-piridina o 2-amino-pirimidina como inhibidores de cinasa dependientes de ciclina.
GB201807014D0 (en) 2018-04-30 2018-06-13 Univ Leeds Innovations Ltd Factor xlla inhibitors
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
GB201810581D0 (en) 2018-06-28 2018-08-15 Ctxt Pty Ltd Compounds
EP4218934A1 (de) 2018-10-05 2023-08-02 Forma Therapeutics, Inc. Hemmung von ubiquitin-spezifischer protease 30 (usp40)
PE20220808A1 (es) 2019-06-18 2022-05-20 Pfizer Derivados de benzisoxazol sulfonamida
EP4069691A1 (de) 2019-12-06 2022-10-12 Vertex Pharmaceuticals Incorporated Substituierte tetrahydrofurane als modulatoren von natriumkanälen
TWI794742B (zh) 2020-02-18 2023-03-01 美商基利科學股份有限公司 抗病毒化合物
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
EP4323362A1 (de) 2021-04-16 2024-02-21 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

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
DE3207033C2 (de) 1981-02-27 1984-09-13 Torii & Co., Ltd., Tokyo Amidinverbindungen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Mittel
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
WO1994013693A1 (en) 1992-12-15 1994-06-23 Corvas International, Inc. NOVEL INHIBITORS OF FACTOR Xa
US5610335A (en) 1993-05-26 1997-03-11 Cornell Research Foundation Microelectromechanical lateral accelerometer
EP0798295B1 (de) 1994-12-02 2003-02-26 Yamanouchi Pharmaceutical Co. Ltd. Neues amidinonaphthylderivat oder dessen salz
AU707323B2 (en) 1995-03-10 1999-07-08 Berlex Laboratories, Inc. Benzamidine derivatives 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
CA2264942A1 (en) 1996-09-09 1998-03-12 Smithkline Beecham Corporation Compounds and methods
DE69720773T2 (de) * 1996-12-23 2004-01-29 Bristol Myers Squibb Pharma Co SAUERSTOFF ODER SCHWEFEL ENTHALTENDE 5-GLIEDRIGE HETEROAROMATISHE DERIVATIVE ALS FACTOR Xa HEMMER
PL334250A1 (en) 1996-12-23 2000-02-14 Du Pont Pharm Co Nitrogen containing hetero-aromatic compounds and inhibitors of xa factor
EP0993448A1 (de) * 1997-06-19 2000-04-19 The Du Pont Merck Pharmaceutical Company (amidino)6-gliedrige aromaten als factor xa inhibitoren
IL133627A0 (en) 1997-06-26 2001-04-30 Lilly Co Eli Antithrombotic agents
JP2002512633A (ja) 1997-06-26 2002-04-23 イーライ・リリー・アンド・カンパニー 抗血栓剤
AU8270698A (en) * 1997-06-26 1999-01-19 Eli Lilly And Company Antithrombotic agents
IL133623A0 (en) 1997-06-26 2001-04-30 Lilly Co Eli Antithrombotic agents
US5919779A (en) 1997-08-11 1999-07-06 Boehringer Ingelheim Pharmaceuticals, Inc. 5,6-Heteroaryl-dipyrido(2,3-B:3', 2'-F) azepines and their use in the prevention or treatment of HIV infection
EP1020434A4 (de) 1997-08-27 2000-11-15 Kissei Pharmaceutical 3-amidinoanilin-derivate, inhibitoren des aktivierten blutgerinnungsfaktors x und zwischenpodukte zur herstellung beider
US6140351A (en) 1997-12-19 2000-10-31 Berlex Laboratories, Inc. Ortho-anthranilamide derivatives as anti-coagulants
PT1040108E (pt) 1997-12-19 2004-06-30 Schering Ag Derivados de orto-antranilamida como anticoagulantes
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
CN1333769A (zh) 1998-12-09 2002-01-30 美国家庭用品有限公司 疱疹病毒的硫脲抑制剂
PT1137645E (pt) 1998-12-09 2004-09-30 Wyeth Corp Inibidores virus de herpes a base de tioureia alfa-metilbenzilada contendo um grupo fenilenodiamina
KR20010089559A (ko) 1998-12-09 2001-10-06 이곤 이 버그 허프스 바이러스의 티오우레아 억제제
AU2353900A (en) 1998-12-09 2000-06-26 Wyeth Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing a substituted phenylenediamine group
KR20010087413A (ko) 1998-12-09 2001-09-15 이곤 이 버그 헤르페스 바이러스의 아세트아마이드 및 치환아세트아마이드-함유 티오우레아 억제제
BR9916046A (pt) 1998-12-09 2001-10-02 American Home Prod Composto, composição farmacêutica, e, processos para inibir a replicação de um vìrus herpes e para tratamento de um paciente que sofra de uma infecção do vìrus herpes
WO2000034269A1 (en) 1998-12-09 2000-06-15 American Home Products Corporation Thiourea inhibitors of herpes viruses
DE69919212T2 (de) 1998-12-23 2005-07-28 Eli Lilly And Co., Indianapolis Aromatische amiden
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
KR100760434B1 (ko) 1999-09-17 2007-10-04 밀레니엄 파머슈티컬스 인코퍼레이티드 벤즈아미드 및 관련된 Ｘａ 인자의 억제제
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. 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
CA2456173A1 (en) * 2001-07-31 2003-02-13 Wayne State University Quinoline derivatives and use thereof as antitumor agents
US7022695B2 (en) * 2003-10-09 2006-04-04 Millennium Pharmaceuticals, Inc. Thioether-substituted benzamides as inhibitors of Factor Xa
US7696352B2 (en) * 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
AU2005257999B2 (en) * 2004-06-18 2011-12-08 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
PE20070717A1 (es) * 2005-11-08 2007-08-17 Millennium Pharm Inc Sal de maleato y polimorfo de [2-({4-[(dimetilamino)iminometil]fenil}carbonilamino)-5-metoxifenil]-n-(5-cloro-(2-piridil))carboxamida
WO2007112367A2 (en) 2006-03-27 2007-10-04 Portola Pharmaceuticals, Inc. Potassium channel modulators and platelet procoagulant activity
CA2651303A1 (en) * 2006-05-05 2007-11-15 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
WO2008073670A2 (en) * 2006-12-08 2008-06-19 Millennium Pharmaceuticals, Inc. Unit dose formulations and methods of treating thrombosis with an oral factor xa inhibitor
US20080293704A1 (en) * 2007-01-05 2008-11-27 Millennium Pharmaceuticals, Inc. FACTOR Xa INHIBITORS
AU2008239659B2 (en) * 2007-04-13 2013-09-05 Millennium Pharmaceuticals, Inc. Combination anticoagulant therapy with a compound that acts as a factor Xa inhibitor
EP2586439A1 (de) * 2007-05-02 2013-05-01 Portola Pharmaceuticals, Inc. Kombinationstherapie mit einer Verbindung als Thrombozyt-ADP-Rezeptor-Hemmer

Also Published As

Publication number Publication date
DE60115394T2 (de) 2006-10-19
US20160317511A1 (en) 2016-11-03
US20090131411A1 (en) 2009-05-21
WO2001064642A2 (en) 2001-09-07
US20180036296A1 (en) 2018-02-08
WO2001064643A3 (en) 2002-04-04
US9108922B2 (en) 2015-08-18
CA2401778C (en) 2010-12-21
US20130172310A1 (en) 2013-07-04
US20060241153A1 (en) 2006-10-26
US7727981B2 (en) 2010-06-01
US6376515B2 (en) 2002-04-23
US20050261346A1 (en) 2005-11-24
US20020002183A1 (en) 2002-01-03
US20070021472A1 (en) 2007-01-25
US20100298284A1 (en) 2010-11-25
US20030162690A1 (en) 2003-08-28
EP1259485A2 (de) 2002-11-27
ES2254385T3 (es) 2006-06-16
US7314874B2 (en) 2008-01-01
AU2001250783A1 (en) 2001-09-12
WO2001064642A3 (en) 2002-05-02
US8518977B2 (en) 2013-08-27
EP1259485B1 (de) 2005-11-30
CA2401778A1 (en) 2001-09-07
WO2001064643A2 (en) 2001-09-07
US20120083602A1 (en) 2012-04-05
US8063036B2 (en) 2011-11-22
US7727982B2 (en) 2010-06-01
US20140377247A1 (en) 2014-12-25
AU2001245353A1 (en) 2001-09-12
DE60115394D1 (de) 2006-01-05
US6835739B2 (en) 2004-12-28
US20040097561A1 (en) 2004-05-20
US7342013B2 (en) 2008-03-11
HK1051539A1 (en) 2003-08-08
US10179124B2 (en) 2019-01-15
US8691847B2 (en) 2014-04-08
US9629831B2 (en) 2017-04-25
ATE311366T1 (de) 2005-12-15

Similar Documents

Publication Publication Date Title
DK1259485T3 (da) Benzamider og beslægtede inhibitorer for faktor Xa
WO2001056989A3 (en) Inhibitors of factor xa
NZ511927A (en) Phenylglycine derivatives
WO2002026712A3 (en) Quaternary amines and related inhibitors of factor xa
BG106013A (en) New compounds and compositions as protease inhibitors
NO20021229D0 (no) Benzamider og lignende inhibitorer for faktor Xa
TR200201505T2 (tr) Terapötik maddeler olarak pirazolopirimidinler
BR0014078A (pt) Inibidores de fator xa
ATE359271T1 (de) Phenylderivate
MY133897A (en) N-(4-carb-amimidophenyl) glycineamide derivatives
WO2000071516A3 (en) INHIBITORS OF FACTOR Xa
ATE368643T1 (de) Faktor xa benzamidin inhibitoren
DE60230127D1 (de) Inhibitoren von integrin alpha-v-beta-6
DE60121461D1 (de) Kondensierte pyridoindolderivate
WO2001057021A3 (en) 2-[1H]-QUINOLONE AND 2-[1H]-QUINOXALONE INHIBITORS OF FACTOR Xa
WO2001072708A3 (en) OXINDOLE INHIBITORS OF FACTOR Xa
WO2002026720A3 (en) PIPERAZINE BASED INHIBITORS OF FACTOR Xa
MX9709910A (es) Compuestos que contienen arginina e imitaciones de arginina, su uso y composiciones que los contienen.
SE0302756D0 (sv) Novel Compounds
ATE369348T1 (de) Zyklisierte benzamid-neurokinin-antagonisten zur verwendung in therapie
DE69803383T2 (de) Selektive inhibitoren des faktors x, eine azepinonstruktur enthaltend
WO2002006280A3 (en) INHIBITORS OF FACTOR Xa
WO2002026718A3 (en) Bicyclic pyrimidin-4-one based inhibitors of factor xa
WO2002026731A3 (en) Quaternary amidino based inhibitors of factor xa
SE9902387D0 (sv) New pharmaceutically active compounds