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WO2001019798A3 - Inhibitors of factor xa - Google Patents

Inhibitors of factor xa Download PDF

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Publication number
WO2001019798A3
WO2001019798A3 PCT/US2000/025195 US0025195W WO0119798A3 WO 2001019798 A3 WO2001019798 A3 WO 2001019798A3 US 0025195 W US0025195 W US 0025195W WO 0119798 A3 WO0119798 A3 WO 0119798A3
Authority
WO
WIPO (PCT)
Prior art keywords
substituted
heterocyclic ring
ring system
compounds
factor
Prior art date
Application number
PCT/US2000/025195
Other languages
French (fr)
Other versions
WO2001019798A2 (en
Inventor
Bing-Yan Zhu
Zhaozhong Jon Jia
Wenrong Huang
Yonghong Song
James Kanter
Robert M Scarborough
Original Assignee
Cor Therapeutics 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
Priority to IL14869800A priority Critical patent/IL148698A0/en
Priority to NZ517828A priority patent/NZ517828A/en
Priority to HU0203954A priority patent/HUP0203954A2/en
Priority to JP2001523378A priority patent/JP2003509412A/en
Priority to EP00963451A priority patent/EP1216231A2/en
Priority to CA002385589A priority patent/CA2385589A1/en
Application filed by Cor Therapeutics Inc filed Critical Cor Therapeutics Inc
Priority to BR0014078-3A priority patent/BR0014078A/en
Priority to MXPA02002762 priority patent/MX228790B/en
Priority to AU74866/00A priority patent/AU781880B2/en
Publication of WO2001019798A2 publication Critical patent/WO2001019798A2/en
Publication of WO2001019798A3 publication Critical patent/WO2001019798A3/en
Priority to NO20021230A priority patent/NO20021230L/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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  • Hydrogenated Pyridines (AREA)

Abstract

Compounds of formula A Q D E G J X in which D is a direct link, a substituted or unsubsituted phenyl or naphtyl gourp or a heterocyclic ring system; G is substituted or unsubstituted phenyl or a heterocyclic ring system; X is a substituted or unsubstituted phenyl or naphtyl group or a heterocyclic ring system; and the other variables are as defined in the claims, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed, The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
PCT/US2000/025195 1999-09-17 2000-09-15 INHIBITORS OF FACTOR Xa WO2001019798A2 (en)

Priority Applications (10)

Application Number Priority Date Filing Date Title
NZ517828A NZ517828A (en) 1999-09-17 2000-09-15 Inhibitors having activity against mammalian factor Xa
HU0203954A HUP0203954A2 (en) 1999-09-17 2000-09-15 Inhibitors of factor xa
JP2001523378A JP2003509412A (en) 1999-09-17 2000-09-15 Factor Xa inhibitor
EP00963451A EP1216231A2 (en) 1999-09-17 2000-09-15 INHIBITORS OF FACTOR Xa
CA002385589A CA2385589A1 (en) 1999-09-17 2000-09-15 Inhibitors of factor xa
IL14869800A IL148698A0 (en) 1999-09-17 2000-09-15 INHIBITORS OF FACTOR Xa
BR0014078-3A BR0014078A (en) 1999-09-17 2000-09-15 Xa factor inhibitors
MXPA02002762 MX228790B (en) 1999-09-17 2000-09-15 Inhibitors of factor xa.
AU74866/00A AU781880B2 (en) 1999-09-17 2000-09-15 Inhibitors of factor Xa
NO20021230A NO20021230L (en) 1999-09-17 2002-03-12 Factor Xa inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15433299P 1999-09-17 1999-09-17
US60/154,332 1999-09-17

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WO2001019798A2 WO2001019798A2 (en) 2001-03-22
WO2001019798A3 true WO2001019798A3 (en) 2001-10-25

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

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