ZA200610417B - 2-[(Hetero)aryl]-benzoxazole compounds and derivatives, compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding - Google Patents
2-[(Hetero)aryl]-benzoxazole compounds and derivatives, compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding Download PDFInfo
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- ZA200610417B ZA200610417B ZA200610417A ZA200610417A ZA200610417B ZA 200610417 B ZA200610417 B ZA 200610417B ZA 200610417 A ZA200610417 A ZA 200610417A ZA 200610417 A ZA200610417 A ZA 200610417A ZA 200610417 B ZA200610417 B ZA 200610417B
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- ZA
- South Africa
- Prior art keywords
- compound
- cooh
- alkyl
- transthyretin
- hydrogen
- Prior art date
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- 125000002971 oxazolyl group Chemical group 0.000 description 1
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- JRKICGRDRMAZLK-UHFFFAOYSA-L peroxydisulfate Chemical class [O-]S(=O)(=O)OOS([O-])(=O)=O JRKICGRDRMAZLK-UHFFFAOYSA-L 0.000 description 1
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- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 1
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- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
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- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- CRDYSYOERSZTHZ-UHFFFAOYSA-M selenocyanate Chemical compound [Se-]C#N CRDYSYOERSZTHZ-UHFFFAOYSA-M 0.000 description 1
- DUIOPKIIICUYRZ-UHFFFAOYSA-N semicarbazide Chemical compound NNC(N)=O DUIOPKIIICUYRZ-UHFFFAOYSA-N 0.000 description 1
- AWUCVROLDVIAJX-GSVOUGTGSA-N sn-glycerol 3-phosphate Chemical compound OC[C@@H](O)COP(O)(O)=O AWUCVROLDVIAJX-GSVOUGTGSA-N 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
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- 125000005017 substituted alkenyl group Chemical group 0.000 description 1
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- 125000003107 substituted aryl group Chemical group 0.000 description 1
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- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical class [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
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- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
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- 229940034208 thyroxine Drugs 0.000 description 1
- XUIIKFGFIJCVMT-UHFFFAOYSA-N thyroxine-binding globulin Natural products IC1=CC(CC([NH3+])C([O-])=O)=CC(I)=C1OC1=CC(I)=C(O)C(I)=C1 XUIIKFGFIJCVMT-UHFFFAOYSA-N 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical class CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
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- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001052 transient effect Effects 0.000 description 1
- 229910052723 transition metal Inorganic materials 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical class CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
- NQPDZGIKBAWPEJ-UHFFFAOYSA-M valerate Chemical class CCCCC([O-])=O NQPDZGIKBAWPEJ-UHFFFAOYSA-M 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
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Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D307/91—Dibenzofurans; Hydrogenated dibenzofurans
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D263/57—Aryl or substituted aryl radicals
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/40—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/42—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by saturated carbon chains
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/52—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
- C07C229/54—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C229/56—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in ortho-position
- C07C229/58—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in ortho-position having the nitrogen atom of at least one of the amino groups further bound to a carbon atom of a six-membered aromatic ring, e.g. N-phenyl-anthranilic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/52—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
- C07C229/54—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C229/60—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in meta- or para- positions
-
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- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
- C07C251/32—Oximes
- C07C251/34—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C251/48—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atom of at least one of the oxyimino groups bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C39/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring
- C07C39/24—Halogenated derivatives
- C07C39/367—Halogenated derivatives polycyclic non-condensed, containing only six-membered aromatic rings as cyclic parts, e.g. halogenated poly-hydroxyphenylalkanes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C65/21—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups
- C07C65/24—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups polycyclic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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ZA200610417A ZA200610417B (en) | 2004-05-20 | 2006-12-12 | 2-[(Hetero)aryl]-benzoxazole compounds and derivatives, compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding |
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US (5) | US20050261365A1 (fr) |
EP (3) | EP1768968A1 (fr) |
JP (2) | JP2007538103A (fr) |
KR (2) | KR20070032700A (fr) |
CN (2) | CN101198598A (fr) |
AU (2) | AU2005244999A1 (fr) |
BR (2) | BRPI0510142A (fr) |
CA (2) | CA2566688A1 (fr) |
MX (1) | MXPA06013381A (fr) |
RU (1) | RU2371440C2 (fr) |
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CA2438032C (fr) * | 2003-03-14 | 2013-05-07 | University Of Pittsburgh | Derives de benzothiazole et compositions et utilisations connexes |
AR044503A1 (es) | 2003-03-18 | 2005-09-14 | Merck & Co Inc | Triazoles sustituidos con biarilo como bloqueantes del canal de sodio |
CN101468965A (zh) | 2003-03-24 | 2009-07-01 | 默克公司 | 联芳基取代的6元杂环钠通道阻滞剂 |
JP2004302049A (ja) | 2003-03-31 | 2004-10-28 | Hodogaya Chem Co Ltd | 感光性樹脂組成物 |
JP2006522130A (ja) | 2003-04-03 | 2006-09-28 | メルク エンド カムパニー インコーポレーテッド | ナトリウムチャンネル遮断薬としてのビアリール置換ピラゾール |
US20070060584A1 (en) | 2003-04-18 | 2007-03-15 | Chakravarty Prasun K | Biaryl substituted thiazoles, oxazoles and imidazoles as sodium channel blockers |
JP3687660B2 (ja) | 2003-04-22 | 2005-08-24 | 松下電工株式会社 | マッサージ機 |
EP1620413A2 (fr) | 2003-04-30 | 2006-02-01 | Cytokinetics, Inc. | Composes, compositions et procedes |
WO2005113523A1 (fr) * | 2004-05-20 | 2005-12-01 | Foldrx Pharmaceuticals, Inc. | Composés 2-(hétéroaryl)benzoxazoles et dérivés, compositions et procédés servant à stabiliser la transthyrétine et à inhiber le mauvais repliement de la transthyrétine |
-
2005
- 2005-05-20 WO PCT/US2005/017612 patent/WO2005113523A1/fr active Application Filing
- 2005-05-20 EP EP05751051A patent/EP1768968A1/fr not_active Withdrawn
- 2005-05-20 EP EP05754418A patent/EP1755585A4/fr not_active Withdrawn
- 2005-05-20 JP JP2007527513A patent/JP2007538103A/ja active Pending
- 2005-05-20 JP JP2007527448A patent/JP2007538095A/ja active Pending
- 2005-05-20 BR BRPI0510142-5A patent/BRPI0510142A/pt not_active IP Right Cessation
- 2005-05-20 AU AU2005244999A patent/AU2005244999A1/en not_active Abandoned
- 2005-05-20 CA CA002566688A patent/CA2566688A1/fr not_active Abandoned
- 2005-05-20 US US11/134,527 patent/US20050261365A1/en not_active Abandoned
- 2005-05-20 WO PCT/US2005/017929 patent/WO2005112913A1/fr active Application Filing
- 2005-05-20 KR KR1020067026735A patent/KR20070032700A/ko not_active Application Discontinuation
- 2005-05-20 CN CNA2005800244880A patent/CN101198598A/zh active Pending
- 2005-05-20 RU RU2006145074/04A patent/RU2371440C2/ru not_active IP Right Cessation
- 2005-05-20 BR BRPI0510033-0A patent/BRPI0510033A/pt not_active IP Right Cessation
- 2005-05-20 US US11/134,628 patent/US7868033B2/en active Active
- 2005-05-20 MX MXPA06013381A patent/MXPA06013381A/es not_active Application Discontinuation
- 2005-05-20 CN CNA2005800217239A patent/CN1976693A/zh active Pending
- 2005-05-20 WO PCT/US2005/019184 patent/WO2005118511A2/fr active Application Filing
- 2005-05-20 AU AU2005245470A patent/AU2005245470A1/en not_active Abandoned
- 2005-05-20 KR KR1020067026787A patent/KR20070013335A/ko not_active Application Discontinuation
- 2005-05-20 EP EP20100179645 patent/EP2314584A1/fr not_active Withdrawn
- 2005-05-20 US US11/134,848 patent/US20050272704A1/en not_active Abandoned
- 2005-05-20 US US11/596,832 patent/US20080319175A1/en not_active Abandoned
- 2005-05-20 CA CA002566923A patent/CA2566923A1/fr not_active Abandoned
-
2006
- 2006-12-12 ZA ZA200610417A patent/ZA200610417B/en unknown
-
2010
- 2010-12-28 US US12/979,733 patent/US8338459B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
CN101198598A (zh) | 2008-06-11 |
WO2005118511A3 (fr) | 2006-02-09 |
US20080319175A1 (en) | 2008-12-25 |
WO2005118511A2 (fr) | 2005-12-15 |
BRPI0510142A (pt) | 2007-10-02 |
CA2566688A1 (fr) | 2005-12-01 |
RU2006145074A (ru) | 2008-06-27 |
WO2005113523A1 (fr) | 2005-12-01 |
US20050272704A1 (en) | 2005-12-08 |
JP2007538103A (ja) | 2007-12-27 |
WO2005112913A1 (fr) | 2005-12-01 |
KR20070013335A (ko) | 2007-01-30 |
CN1976693A (zh) | 2007-06-06 |
AU2005245470A1 (en) | 2005-12-01 |
EP1768968A1 (fr) | 2007-04-04 |
WO2005112913B1 (fr) | 2006-02-09 |
RU2371440C2 (ru) | 2009-10-27 |
US20110092545A1 (en) | 2011-04-21 |
BRPI0510033A (pt) | 2007-10-02 |
JP2007538095A (ja) | 2007-12-27 |
EP2314584A1 (fr) | 2011-04-27 |
EP1755585A4 (fr) | 2009-04-01 |
US7868033B2 (en) | 2011-01-11 |
MXPA06013381A (es) | 2007-03-01 |
US20050282780A1 (en) | 2005-12-22 |
US8338459B2 (en) | 2012-12-25 |
EP1755585A1 (fr) | 2007-02-28 |
AU2005244999A1 (en) | 2005-12-01 |
US20050261365A1 (en) | 2005-11-24 |
KR20070032700A (ko) | 2007-03-22 |
CA2566923A1 (fr) | 2005-12-01 |
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