CA2385589A1 - Inhibiteurs du facteur xa - Google Patents

Inhibiteurs du facteur xa Download PDF

Info

Publication number
CA2385589A1
CA2385589A1 CA002385589A CA2385589A CA2385589A1 CA 2385589 A1 CA2385589 A1 CA 2385589A1 CA 002385589 A CA002385589 A CA 002385589A CA 2385589 A CA2385589 A CA 2385589A CA 2385589 A1 CA2385589 A1 CA 2385589A1
Authority
CA
Canada
Prior art keywords
group
4alkyl
substituted
compound
conh2
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA002385589A
Other languages
English (en)
Inventor
Bing-Yan Zhu
Zhaozhong Jon Jia
Robert M. Scarborough
James Kanter
Yonghong Song
Wenrong Huang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Millennium Pharmaceuticals Inc
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of CA2385589A1 publication Critical patent/CA2385589A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • C07D213/78—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
    • 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
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Facsimile Image Signal Circuits (AREA)
  • Controls And Circuits For Display Device (AREA)
  • Dot-Matrix Printers And Others (AREA)

Abstract

L'invention concerne de nouveaux composés, leurs sels et des compositions les contenant, efficaces contre le facteur Xa mammalien. Ces composés sont utilisés i<i>n vivo</i> et <i>in vitro</i> pour prévenir ou traiter les troubles de la coagulation.
CA002385589A 1999-09-17 2000-09-15 Inhibiteurs du facteur xa Abandoned CA2385589A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US15433299P 1999-09-17 1999-09-17
US60/154,332 1999-09-17
PCT/US2000/025195 WO2001019798A2 (fr) 1999-09-17 2000-09-15 INHIBITEURS DU FACTEUR Xa

Publications (1)

Publication Number Publication Date
CA2385589A1 true CA2385589A1 (fr) 2001-03-22

Family

ID=22550934

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002385589A Abandoned CA2385589A1 (fr) 1999-09-17 2000-09-15 Inhibiteurs du facteur xa

Country Status (16)

Country Link
EP (1) EP1216231A2 (fr)
JP (1) JP2003509412A (fr)
CN (1) CN1390206A (fr)
AU (1) AU781880B2 (fr)
BR (1) BR0014078A (fr)
CA (1) CA2385589A1 (fr)
CZ (1) CZ2002959A3 (fr)
HU (1) HUP0203954A2 (fr)
IL (1) IL148698A0 (fr)
MX (1) MX228790B (fr)
NO (1) NO20021230L (fr)
NZ (1) NZ517828A (fr)
RU (1) RU2002110295A (fr)
TR (1) TR200201413T2 (fr)
WO (1) WO2001019798A2 (fr)
ZA (4) ZA200202116B (fr)

Families Citing this family (133)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002533465A (ja) 1998-12-23 2002-10-08 デュポン ファーマシューティカルズ カンパニー Ｘａ因子阻害剤としての窒素を含む複素二環類
AU776053B2 (en) 2000-03-31 2004-08-26 Astellas Pharma Inc. Diazepan derivatives or salts thereof
TWI288745B (en) 2000-04-05 2007-10-21 Daiichi Seiyaku Co Ethylenediamine derivatives
US7160878B2 (en) 2000-07-27 2007-01-09 Eli Lilly And Company Substituted heterocyclic amides
ATE323071T1 (de) 2000-11-22 2006-04-15 Astellas Pharma Inc Substituierte phenolderivate und deren salze als hemmstoffe von koagulations faktor x
EP1379506A2 (fr) 2000-11-28 2004-01-14 Eli Lilly And Company Carboxamides substitues
US6998408B2 (en) 2001-03-23 2006-02-14 Bristol-Myers Squibb Pharma Company 6-5, 6-6, or 6-7 Heterobicycles as factor Xa inhibitors
CA2444571A1 (fr) 2001-04-18 2002-10-31 Bristol-Myers Squibb Company 1, 4, 5, 6-tetrahydropyrazolo-¬3, 4-c|-pyridine-7-ones comme inhiteurs du facteur xa
EP1379244A4 (fr) 2001-04-18 2006-03-15 Bristol Myers Squibb Co 1,4,5,6-tetrahydropyrazolo- 3,4-c]-pyridin-7-ones utilisees comme inhibiteurs du facteur xa
EP1414449A4 (fr) 2001-05-22 2005-04-06 Bristol Myers Squibb Co Inhibiteurs bicycliques du facteur xa
US7365205B2 (en) 2001-06-20 2008-04-29 Daiichi Sankyo Company, Limited Diamine derivatives
ES2329881T3 (es) 2001-09-21 2009-12-02 Bristol-Myers Squibb Company Compuestos que contienen lactama y derivados de los mismos como inhibidores del factor xa.
TWI331526B (en) 2001-09-21 2010-10-11 Bristol Myers Squibb Pharma Co Lactam-containing compounds and derivatives thereof as factor xa inhibitors
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
TW200302225A (en) 2001-12-04 2003-08-01 Bristol Myers Squibb Co Substituted amino methyl factor Xa inhibitors
AU2002350217A1 (en) 2001-12-04 2003-06-17 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
US7449457B2 (en) 2001-12-07 2008-11-11 Eli Lilly And Company Substituted heterocyclic carboxamides with antithrombotic activity
US7312214B2 (en) 2002-05-10 2007-12-25 Bristol-Myers Squibb Company 1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors
EP2402309A1 (fr) 2002-05-24 2012-01-04 Millennium Pharmaceuticals, Inc. Inhibiteurs de CCR9 et leurs procédés d'utilisation
EP1517898A1 (fr) * 2002-06-29 2005-03-30 Zentaris GmbH Aryl- et heteroarylcarbonylpiperazines et leur utilisation dans le traitement de maladies tumorales benignes et malignes
DE60304718T2 (de) 2002-08-06 2007-04-26 Astrazeneca Ab Kondensierte pyridine und pyrimidine mit tie2 (tek) aktivität
US7420055B2 (en) 2002-11-18 2008-09-02 Chemocentryx, Inc. Aryl sulfonamides
US7227035B2 (en) 2002-11-18 2007-06-05 Chemocentryx Bis-aryl sulfonamides
KR100874292B1 (ko) 2002-11-18 2008-12-18 케모센트릭스 아릴 술폰아마이드
US7741519B2 (en) 2007-04-23 2010-06-22 Chemocentryx, Inc. Bis-aryl sulfonamides
EP2982668A3 (fr) 2002-12-03 2016-04-13 Pharmacyclics LLC Dérivés de 2-(2-hydroxybiphényl-3-yl)-1h-benzoimidazole-5-carboxamidine en tant qu'inhibiteurs du facteur viia inhibitors pour le traitement de maladies thromboemboliques
US7429581B2 (en) 2002-12-23 2008-09-30 Sanofi-Aventis Deutschland Gmbh Pyrazole-derivatives as factor Xa inhibitors
BR0317659A (pt) * 2002-12-23 2005-12-06 Aventis Pharma Gmbh Derivados de pirazol como inibidores de fator xa
EP1479678A1 (fr) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Derivés du pyrazole en tant qu'inhibiteurs du facteur Xa
EP1433788A1 (fr) * 2002-12-23 2004-06-30 Aventis Pharma Deutschland GmbH Dérivés de pyrazole en tant qu'inhibiteurs du facteur Xa
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
MXPA05008367A (es) 2003-02-07 2005-11-04 Daiichi Seiyaku Co Derivados de pirazol.
US7122557B2 (en) 2003-03-18 2006-10-17 Bristol-Myers Squibb Company Sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds as factor Xa inhibitors
CA2525325A1 (fr) * 2003-05-01 2004-11-18 Abbott Laboratories Pyrazole-amides et sulfonamides modulateurs des canaux sodiques
US20040220170A1 (en) * 2003-05-01 2004-11-04 Atkinson Robert N. Pyrazole-amides and sulfonamides as sodium channel modulators
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
WO2005012256A1 (fr) 2003-07-22 2005-02-10 Astex Therapeutics Limited Composes 1h-pyrazole 3,4-disubstitues et leur utilisation en tant que kinases dependant des cyclines (cdk) et modulateurs de la glycogene synthase kinase-3 (gsk-3)
SE0302573D0 (sv) 2003-09-26 2003-09-26 Astrazeneca Ab Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
CA2541949A1 (fr) 2003-10-07 2005-05-26 Renovis, Inc. Derives d'amide utilises comme ligands du canal ionique et compositions pharmaceutiques et methodes d'utilisation de ces derives
EP2228369A1 (fr) 2003-12-23 2010-09-15 Astex Therapeutics Ltd. Derives de pyrazole comme modulateurs de proteine kinase
CA2560510C (fr) 2004-03-18 2009-10-13 Pfizer Inc. Sulfamides n-(1-arylpyrazol-4yl) et leur utilisation en tant qu'anti-parasitaires
US7868037B2 (en) 2004-07-14 2011-01-11 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7772271B2 (en) 2004-07-14 2010-08-10 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
WO2006019831A1 (fr) 2004-07-14 2006-02-23 Ptc Therapeutics, Inc. Procedes pour le traitement de l'hepatite c
US7645881B2 (en) 2004-07-22 2010-01-12 Ptc Therapeutics, Inc. Methods for treating hepatitis C
AU2005271737A1 (en) 2004-08-03 2006-02-16 Wyeth Indazoles useful in treating cardiovascular diseases
BRPI0515483A (pt) 2004-09-20 2008-07-22 Xenon Pharmaceuticals Inc derivados heterocìclicos para o tratamento de doenças mediadas por enzimas estearoil-coa desaturase
AU2005286647A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
CA2580856A1 (fr) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Derives heterocycliques et leur utilisation en tant qu'inhibiteurs de la stearoyl-coa desaturase
EP1799667B1 (fr) 2004-09-20 2013-03-20 Xenon Pharmaceuticals Inc. Derives heterocycliques et leur utilisation comme agents therapeutiques
TW200626139A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
US7951805B2 (en) 2004-09-20 2011-05-31 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase
CN101083992A (zh) 2004-09-20 2007-12-05 泽农医药公司 抑制人硬脂酰CoA去饱和酶的哒嗪衍生物
ES2380709T3 (es) 2004-09-24 2012-05-17 Astrazeneca Ab Derivados de bencimidazol, composiciones que los contienen, su preparación y usos
US7381732B2 (en) * 2004-10-26 2008-06-03 Bristol-Myers Squibb Company Pyrazolobenzamides and derivatives as factor Xa inhibitors
US8110573B2 (en) 2004-12-30 2012-02-07 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of CDK, GSK and aurora kinases
US8202999B2 (en) 2005-01-07 2012-06-19 Synta Pharmaceuticals Corp. Compounds for inflammation and immune-related uses
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
MX2007008781A (es) 2005-01-21 2007-09-11 Astex Therapeutics Ltd Compuestos farmaceuticos.
BRPI0606480A (pt) 2005-01-21 2008-03-11 Astex Therapeutics Ltd compostos farmacêuticos
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.
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.
BRPI0611187A2 (pt) 2005-06-03 2010-08-24 Xenon Pharmaceuticals Inc derivados aminotiazàis como inibidores da estearoil-coa desaturase humana
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
EP1928866A1 (fr) 2005-09-05 2008-06-11 Ranbaxy Laboratories Limited Indazoles substitues utilises en tant qu'inhibiteurs de phosphodiesterase de type-iv
US7915286B2 (en) 2005-09-16 2011-03-29 Ranbaxy Laboratories Limited Substituted pyrazolo [3,4-b] pyridines as phosphodiesterase inhibitors
GB0521244D0 (en) 2005-10-19 2005-11-30 Astrazeneca Ab Benzamide compounds
US8399442B2 (en) 2005-12-30 2013-03-19 Astex Therapeutics Limited Pharmaceutical compounds
TW200745049A (en) 2006-03-23 2007-12-16 Astrazeneca Ab New crystalline forms
TW200808769A (en) 2006-04-18 2008-02-16 Astrazeneca Ab Therapeutic compounds
CA2655933C (fr) 2006-06-23 2014-09-09 Alethia Biotherapeutics Inc. Sequences de polynucleotides et de polypeptides impliquees dans le cancer
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
WO2008059335A1 (fr) 2006-11-13 2008-05-22 Pfizer Products Inc. Dérivés diaryle, dipyridinyle et aryl-pyridinyle et leurs utilisations
EP1958947A1 (fr) 2007-02-15 2008-08-20 Ranbaxy Laboratories Limited Inhibiteurs de la phosphodiestérase de type 4
GB0704932D0 (en) 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
NZ580162A (en) * 2007-04-13 2012-10-26 Millennium Pharm Inc Combination anticoagulant therapy with a compound that acts as a factor xa inhibitor
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
WO2010060186A1 (fr) 2008-11-03 2010-06-03 Alethia Biotherapeutics Inc. Anticorps qui bloquent spécifiquement l’activité biologique d’un antigène tumoral
ES2740424T3 (es) 2009-03-13 2020-02-05 Agios Pharmaceuticals Inc Métodos y composiciones para trastornos relacionados con la proliferación celular
EP2417123A2 (fr) 2009-04-06 2012-02-15 Agios Pharmaceuticals, Inc. Compositions thérapeutiques et procédés d'utilisation associés
BRPI1010024A2 (pt) 2009-06-05 2019-09-24 Link Medicine Corp derivados de aminopirrolidinona e uso dos mesmos
CN102481300B (zh) 2009-06-29 2015-04-15 安吉奥斯医药品有限公司 治疗性化合物和组合物
EP2491145B1 (fr) 2009-10-21 2016-03-09 Agios Pharmaceuticals, Inc. Procédés et compositions pour des troubles relatifs à la prolifération cellulaire
WO2011057145A2 (fr) 2009-11-05 2011-05-12 University Of Notre Dame Du Lac Composés d'imidazo[1,2-a]pyridine, leur synthèse et procédés pour les utiliser
NZ603156A (en) 2010-03-30 2014-10-31 Verseon Corp Multisubstituted aromatic compounds as inhibitors of thrombin
CN101870636B (zh) * 2010-04-01 2013-01-23 大唐(杭州)医药化工有限公司 2-溴-6-氟萘的制备方法
US9221792B2 (en) 2010-12-17 2015-12-29 Agios Pharmaceuticals, Inc N-(4-(azetidine-1-carbonyl) phenyl)-(hetero-) arylsulfonamide derivatives as pyruvate kinase M2 (PMK2) modulators
JP6092118B2 (ja) 2010-12-21 2017-03-08 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 ニ環式ｐｋｍ２活性化剤
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
DK3173427T3 (da) 2011-03-31 2019-08-05 Adc Therapeutics Sa Antistoffer mod nyre-associeret antigen 1 og antigen-bindende fragmenter deraf
CA2834692A1 (fr) 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc. Activateurs de la pyruvate kinase destines a une utilisation therapeutique
DK2704721T3 (en) 2011-05-03 2018-07-09 Agios Pharmaceuticals Inc Pyruvate kinase activators for therapeutic use
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
RS58918B1 (sr) 2012-01-09 2019-08-30 Adc Therapeutics Sa Agensi za tretman trostruko negativnog raka dojke
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
CN103483242A (zh) * 2012-06-15 2014-01-01 上海朴颐化学科技有限公司 4-(2’-吡啶基)苄基肼及其中间体的制备方法
WO2014053968A1 (fr) 2012-10-04 2014-04-10 Pfizer Limited Inhibiteurs de kinase associée à la tropomyosine pyrrolo[3,2-c]pyridine
CN105209440B (zh) 2013-03-15 2019-07-23 维颂公司 作为凝血酶抑制剂的卤代吡唑
BR112015022340A2 (pt) 2013-03-15 2017-07-18 Verseon Corp método para tratamento ou prevenção de uma doença ou distúrbio relacionado à calicreína em um sujeito, composto, e, composição farmacêutica
WO2015003355A2 (fr) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Composés thérapeutiquement actifs et leurs méthodes d'utilisation
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 (fr) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Composés thérapeutiquement actifs et leurs méthodes d'utilisation
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
EP3054936B1 (fr) 2013-10-10 2023-10-18 Eastern Virginia Medical School Dérivés de 4-((2-hydroxy-3-méthoxybenzyl)amino)benzènesulfonamide comme inhibiteur de la 12-lipoxygénase
KR102400737B1 (ko) 2014-03-14 2022-05-20 아지오스 파마슈티컬스 아이엔씨. 치료적으로 활성인 화합물의 약제학적 조성물
DK3154947T3 (en) * 2014-06-11 2018-06-18 Bayer Cropscience Ag PROCEDURE FOR PREPARING 3,5-BIS (HALOGENAL COOL) PYRAZOLES BY ACYLATION OF KETIMINES
CN104016944B (zh) * 2014-06-16 2016-05-18 山东大学 N-(2-(胺甲基)苯基)噻唑-4-甲酰胺衍生物及其制备方法与应用
AU2015317522A1 (en) 2014-09-17 2017-03-23 Verseon Corporation Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
MX2017011000A (es) 2015-02-27 2017-10-20 Verseon Corp Compuestos de pirazol sustituidos como inhibidores de serina proteasa.
US11234976B2 (en) 2015-06-11 2022-02-01 Agios Pharmaceuticals, Inc. Methods of using pyruvate kinase activators
WO2016202756A1 (fr) 2015-06-18 2016-12-22 Bayer Pharma Aktiengesellschaft Composés 2-(1h-pyrazol-1-yl)-1h-benzimidazole substitués
MX2018003294A (es) 2015-09-17 2019-04-25 J Miller Marvin Compuestos heterociclicos que contienen bencilamina y composiciones utiles contra infeccion por micobacterias.
EP4403173A3 (fr) 2015-10-15 2024-10-09 Les Laboratoires Servier Polythérapie pour le traitement de tumeurs malignes
CN108697698B (zh) 2015-10-15 2021-12-03 阿吉奥斯制药公司 用于治疗恶性肿瘤的组合疗法
EA202090871A1 (ru) 2017-10-06 2020-07-03 Форма Терапьютикс, Инк. Ингибирование убиквитин-специфической пептидазы 30
CN118084940A (zh) 2018-02-13 2024-05-28 吉利德科学公司 Pd-1/pd-l1抑制剂
CA3093130C (fr) 2018-04-19 2023-10-17 Gilead Sciences, Inc. Inhibiteurs pd-1/pd-l1
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.
CN112513036B (zh) 2018-05-17 2024-05-24 福马治疗有限公司 用作泛素特异性肽酶30抑制剂的稠合双环化合物
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
CR20210013A (es) 2018-07-13 2021-02-26 Gilead Sciences Inc Inhibidores de pd-1/pd-l1
AU2019356011A1 (en) 2018-10-05 2021-04-01 Forma Therapeutics, Inc. Fused pyrrolines which act as ubiquitin-specific protease 30 (USP30) inhibitors
CA3117199C (fr) 2018-10-24 2024-03-19 Gilead Sciences, Inc. Inhibiteurs de pd-1/pd-l1
SI3986890T1 (sl) 2019-06-18 2024-03-29 Ctxt Pty Ltd Derivati benzisoksazol sulfonamida
WO2021113627A1 (fr) 2019-12-06 2021-06-10 Vertex Pharmaceuticals Incorporated Tétrahydrofuranes substitués en tant que modulateurs de canaux sodiques
JP2024522292A (ja) 2021-06-04 2024-06-13 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 ナトリウムチャネルのモジュレーターとしてのｎ－（ヒドロキシアルキル（ヘテロ）アリール）テトラヒドロフランカルボキサミド

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0946508B1 (fr) * 1996-12-23 2009-09-23 Bristol-Myers Squibb Pharma Company COMPOSES HETEROAROMATIQUES CONTENANT DE L'AZOTE, UTILISES EN TANT QU'INHIBITEURS DU FACTEUR Xa
JP2001506271A (ja) * 1996-12-23 2001-05-15 デュポン ファーマシューティカルズ カンパニー Ｘａ因子阻害剤としての酸素またはイオウを含む複素環式芳香族化合物
CA2293824A1 (fr) * 1997-06-19 1998-12-23 Mimi Lifen Quan Agents aromatiques a six membres amidino utiles en tant qu'inhibiteurs du facteur xa

Also Published As

Publication number Publication date
IL148698A0 (en) 2002-09-12
AU7486600A (en) 2001-04-17
MX228790B (es) 2005-06-30
BR0014078A (pt) 2002-12-31
EP1216231A2 (fr) 2002-06-26
HUP0203954A2 (hu) 2003-03-28
NO20021230L (no) 2002-05-21
WO2001019798A2 (fr) 2001-03-22
AU781880B2 (en) 2005-06-16
MXPA02002762A (es) 2003-10-14
ZA200202117B (en) 2004-02-25
ZA200306488B (en) 2004-04-28
ZA200306490B (en) 2004-05-26
CN1390206A (zh) 2003-01-08
WO2001019798A3 (fr) 2001-10-25
ZA200202116B (en) 2004-02-10
RU2002110295A (ru) 2003-12-10
NO20021230D0 (no) 2002-03-12
JP2003509412A (ja) 2003-03-11
CZ2002959A3 (cs) 2002-07-17
TR200201413T2 (tr) 2003-02-21
NZ517828A (en) 2003-10-31

Similar Documents

Publication Publication Date Title
CA2385589A1 (fr) Inhibiteurs du facteur xa
US6632815B2 (en) Inhibitors of factor Xa
CA2385592C (fr) Benzamides et inhibiteurs correspondants du facteur xa
CA2401778C (fr) Benzamides et inhibiteurs associes du facteur xa
US6720317B1 (en) Inhibitors of factor Xa
US6844367B1 (en) Benzamides and related inhibitors of factor Xa
CA2374650A1 (fr) Inhibiteurs du facteur xa
WO2001012600A1 (fr) INHIBITEURS DU FACTEUR Xa
CA2374641A1 (fr) Inhibiteurs du facteur xa
CA2361428A1 (fr) Inhibiteurs du facteur xa
CA2374820A1 (fr) Inhibiteurs du facteur xa
US20030069250A1 (en) Benzamide inhibitors of factor Xa
CA2371904A1 (fr) Inhibiteurs du facteur xa
WO2002079145A1 (fr) Composes de benzamide, inhibiteurs ddu factor xa
CA2392576A1 (fr) Inhibiteurs du facteur xa a base d&#39;acides .beta.-amines, aspartiques et diaminopropioniques
WO2002026718A2 (fr) Inhibiteurs du facteur xa à base de pyrimidine-4-one bicyclique
EP1322637A2 (fr) Inhibiteurs du facteur xa a base d&#39;amidinos quaternaires
CA2422873A1 (fr) Amides piperazine-2-un comme inhibiteurs du facteur xa

Legal Events

Date Code Title Description
FZDE Discontinued