WO2003103598A3 - Amidine derivatives for treating amyloidosis - Google Patents

Amidine derivatives for treating amyloidosis Download PDF

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Publication number
WO2003103598A3
WO2003103598A3 PCT/US2003/017992 US0317992W WO03103598A3 WO 2003103598 A3 WO2003103598 A3 WO 2003103598A3 US 0317992 W US0317992 W US 0317992W WO 03103598 A3 WO03103598 A3 WO 03103598A3
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WO
WIPO (PCT)
Prior art keywords
amyloid
formula
amidine derivatives
subject
amidine
Prior art date
Application number
PCT/US2003/017992
Other languages
French (fr)
Other versions
WO2003103598A2 (en
Inventor
Robert J Chalifour
Xianqi Kong
Xinfu Wu
Wenshuo Lu
Richard R Tidwell
David Boykin
Original Assignee
Univ North Carolina
Univ Georgia State Res Found
Robert J Chalifour
Xianqi Kong
Xinfu Wu
Wenshuo Lu
Richard R Tidwell
David Boykin
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 Univ North Carolina, Univ Georgia State Res Found, Robert J Chalifour, Xianqi Kong, Xinfu Wu, Wenshuo Lu, Richard R Tidwell, David Boykin filed Critical Univ North Carolina
Priority to AU2003251418A priority Critical patent/AU2003251418A1/en
Priority to EP03757414A priority patent/EP1572129A4/en
Priority to JP2004510719A priority patent/JP2006501160A/en
Priority to CA002488493A priority patent/CA2488493A1/en
Publication of WO2003103598A2 publication Critical patent/WO2003103598A2/en
Publication of WO2003103598A3 publication Critical patent/WO2003103598A3/en

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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A—HUMAN NECESSITIES
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
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    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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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    • 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

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Diabetes (AREA)
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  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
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Abstract

The present invention relates to the use of amidine compounds in the treatment of amyloid related diseases. In particular, the invention relates to a method of treating or preventing an amyloid-related disease in a subject comprising administering to the subject a therapeutic amount of an amidine compound. Among the compounds for use according to the invention are those according to the following Formulae, such that, when administered, amyloid fibril formation, neurodegeneration, or cellular toxicity is reduced or inhibited. Formula I, Formula II, Formula III.
PCT/US2003/017992 2002-06-07 2003-06-09 Amidine derivatives for treating amyloidosis WO2003103598A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
AU2003251418A AU2003251418A1 (en) 2002-06-07 2003-06-09 Amidine derivatives for treating amyloidosis
EP03757414A EP1572129A4 (en) 2002-06-07 2003-06-09 Amidine derivatives for treating amyloidosis
JP2004510719A JP2006501160A (en) 2002-06-07 2003-06-09 Amidine derivatives for the treatment of amyloidosis
CA002488493A CA2488493A1 (en) 2002-06-07 2003-06-09 Amidine derivatives for treating amyloidosis

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38700102P 2002-06-07 2002-06-07
US60/387,001 2002-06-07

Publications (2)

Publication Number Publication Date
WO2003103598A2 WO2003103598A2 (en) 2003-12-18
WO2003103598A3 true WO2003103598A3 (en) 2006-03-09

Family

ID=29736249

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/017992 WO2003103598A2 (en) 2002-06-07 2003-06-09 Amidine derivatives for treating amyloidosis

Country Status (6)

Country Link
EP (1) EP1572129A4 (en)
JP (1) JP2006501160A (en)
AU (1) AU2003251418A1 (en)
CA (1) CA2488493A1 (en)
NO (1) NO20040497L (en)
WO (1) WO2003103598A2 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003265967A1 (en) * 2003-09-05 2005-04-21 Georgia State University Research Foundation, Inc Novel amidine compounds for treating microbial infections
WO2005040132A1 (en) * 2003-10-24 2005-05-06 University Of North Carolina At Chapel Hill Dicationic triaryl analogs as anti-protozoan agents
WO2005079780A1 (en) * 2004-01-23 2005-09-01 Neurochem (International) Limited Amidine derivatives for treating amyloidosis
US7262223B2 (en) * 2004-01-23 2007-08-28 Neurochem (International) Limited Amidine derivatives for treating amyloidosis
CA2600570C (en) * 2005-03-14 2011-12-06 Transtech Pharma, Inc. Benzazole derivatives, compositions, and methods of use as .beta.-secretase inhibitors
AU2006201739A1 (en) * 2005-05-05 2006-11-23 The University Of North Carolina At Chapel Hill Synthesis and antiprotozoal activity of dicationic 3,5-diphenylisoxazoles
SI2247558T1 (en) * 2008-02-14 2022-07-29 Eli Lilly And Company Novel imaging agents for detecting neurological dysfunction
FR2933692B1 (en) * 2008-07-10 2022-12-02 Univ Nancy 1 Henri Poincare NEW COMPOUNDS, THEIR USE AS MEDICINES, AND METHOD FOR PREPARING THEM
CA2786891C (en) 2009-02-20 2017-08-01 Meisho.Co.,Ltd Immunopotentiating composition and process for producing same

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003017994A1 (en) * 2001-08-31 2003-03-06 Neurochem (International) Limited Amidine derivatives for treating amyloidosis

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6635668B1 (en) * 1998-07-22 2003-10-21 The University Of North Carolina At Chapel Hill Imidazoline receptor binding compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003017994A1 (en) * 2001-08-31 2003-03-06 Neurochem (International) Limited Amidine derivatives for treating amyloidosis

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP1572129A4 *

Also Published As

Publication number Publication date
JP2006501160A (en) 2006-01-12
EP1572129A2 (en) 2005-09-14
EP1572129A4 (en) 2007-03-28
CA2488493A1 (en) 2003-12-18
WO2003103598A2 (en) 2003-12-18
NO20040497L (en) 2004-04-14
AU2003251418A1 (en) 2003-12-22

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