EA200101135A1 - Способ ингибирования агрегации амилоидных белков и визуализации амилоидных отложений - Google Patents

Способ ингибирования агрегации амилоидных белков и визуализации амилоидных отложений

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Publication number
EA200101135A1
EA200101135A1 EA200101135A EA200101135A EA200101135A1 EA 200101135 A1 EA200101135 A1 EA 200101135A1 EA 200101135 A EA200101135 A EA 200101135A EA 200101135 A EA200101135 A EA 200101135A EA 200101135 A1 EA200101135 A1 EA 200101135A1
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EA
Eurasian Patent Office
Prior art keywords
amyloid
visualization
proteins
formula
inhibiting aggregation
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EA200101135A
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English (en)
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EA004632B1 (ru
Inventor
Коринн Элизабет Оджелли-Зэфрэн
Марк Роберт Барвиан
Кристофер Франклин Бигг
Шелли Энн Глейз
Шуничиро Хачийя
Джон Стивен Кейли
Такенори Кимура
Йингджи Лай
Аннетт Тереза Сэккэб
Марк Джеймс Суто
Лари Кразуэлл Уокер
Томоюки Ясунага
Ниан Жуанг
Original Assignee
Уорнер-Ламберт Компани
Яманучи Фармасьютикал Компани, Лтд.
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Application filed by Уорнер-Ламберт Компани, Яманучи Фармасьютикал Компани, Лтд. filed Critical Уорнер-Ламберт Компани
Publication of EA200101135A1 publication Critical patent/EA200101135A1/ru
Publication of EA004632B1 publication Critical patent/EA004632B1/ru

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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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • 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
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    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
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    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/402—1-aryl substituted, e.g. piretanide
    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • 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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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
    • C07C229/62—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 groups and at least two carboxyl groups bound to carbon atoms of the same six-membered aromatic ring
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    • 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
    • C07C229/64—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 the carbon skeleton being further substituted by singly-bound oxygen atoms
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    • C07C233/00—Carboxylic acid amides
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    • C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/42—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/43—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
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    • C07D233/66—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 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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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
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  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Pyrrole Compounds (AREA)
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Abstract

В настоящем изобретении предложен способ лечения болезни Альцгеймера с помощью соединения формулы (I). Также предложен способ ингибирования агрегации амилоидных белков с помощью соединения формулы (I) и способ визуализации амилоидных отложений, а также новые соединения формулы (I).Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200101135A 1999-06-10 2000-05-31 Ингибиторы агрегации амилоидных белков, их применение (варианты), композиция на их основе и способ визуализации амилоидных отложений EA004632B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13855099P 1999-06-10 1999-06-10
PCT/US2000/015071 WO2000076489A2 (en) 1999-06-10 2000-05-31 Method of inhibiting amyloid protein aggregation and imaging amyloid deposits

Publications (2)

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EA200101135A1 true EA200101135A1 (ru) 2002-06-27
EA004632B1 EA004632B1 (ru) 2004-06-24

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EP (1) EP1225886A2 (ru)
JP (1) JP2003504310A (ru)
KR (1) KR20020008224A (ru)
CN (1) CN1378446A (ru)
AP (1) AP2002002387A0 (ru)
AU (1) AU775157B2 (ru)
BG (1) BG106293A (ru)
BR (1) BR0011728A (ru)
CA (1) CA2375551A1 (ru)
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DZ (1) DZ3252A1 (ru)
EA (1) EA004632B1 (ru)
EE (1) EE200100673A (ru)
GE (1) GEP20053423B (ru)
HK (1) HK1048258A1 (ru)
HR (1) HRP20020026A2 (ru)
HU (1) HUP0202508A3 (ru)
IL (1) IL146971A0 (ru)
IS (1) IS6193A (ru)
MA (1) MA26805A1 (ru)
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PL (1) PL352430A1 (ru)
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TR (1) TR200103551T2 (ru)
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EP2135610A1 (en) 2008-06-20 2009-12-23 Laboratorios Almirall, S.A. Combination comprising DHODH inhibitors and methotrexate
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EP2239256A1 (en) 2009-03-13 2010-10-13 Almirall, S.A. Sodium salt of 5-cyclopropyl-2-{[2-(2,6-difluorophenyl)pyrimidin-5-yl]amino}benzoic acid as DHODH inhibitor
EP2228367A1 (en) * 2009-03-13 2010-09-15 Almirall, S.A. Addition salts of amines containing hydroxyl and/or carboxylic groups with amino nicotinic acid derivatives as DHODH inhibitors
EP2314577A1 (en) 2009-10-16 2011-04-27 Almirall, S.A. Process for manufacturing 2-[(3,5-difluoro-3'-methoxy-1,1'-biphenyl-4-yl)amino]nicotinic acid
WO2011101787A1 (en) * 2010-02-16 2011-08-25 Università Degli Studi Di Siena Non peptidic 14-3-3 inhibitors and the use thereof
AU2011332198A1 (en) * 2010-11-24 2013-07-11 Allergan, Inc. Modulators of S1P receptors
CN108530310A (zh) * 2017-03-02 2018-09-14 中国科学院上海药物研究所 2-(取代苯杂基)芳香甲酸类fto抑制剂，其制备方法及其应用
EP3680232A4 (en) * 2017-08-07 2021-08-11 Hiroshima University NEW COMBINATION BASED ON ANTHRANIC ACID AND PIN1 INHIBITOR, THERAPEUTIC FOR INFLAMMATORY DISEASES AND THERAPEUTIC FOR CANCER WITH IT

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CA2375551A1 (en) 2000-12-21
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SK17632001A3 (sk) 2003-03-04
AU5455300A (en) 2001-01-02
AU775157B2 (en) 2004-07-22
EA004632B1 (ru) 2004-06-24
HRP20020026A2 (en) 2003-08-31
ZA200109794B (en) 2003-07-01
TR200103551T2 (tr) 2002-12-23
HK1048258A1 (zh) 2003-03-28
BR0011728A (pt) 2002-02-26
IS6193A (is) 2001-12-07
NO20015995L (no) 2002-02-04
GEP20053423B (en) 2005-01-25
WO2000076489A2 (en) 2000-12-21
HUP0202508A2 (hu) 2002-12-28
DZ3252A1 (ru) 2000-12-21
YU86701A (sh) 2004-09-03
NZ515621A (en) 2004-05-28
MXPA01012318A (es) 2002-07-22
PL352430A1 (en) 2003-08-25
KR20020008224A (ko) 2002-01-29
AP2002002387A0 (en) 2002-03-31
BG106293A (en) 2002-06-28
IL146971A0 (en) 2002-08-14
EE200100673A (et) 2003-02-17
CN1378446A (zh) 2002-11-06
WO2000076489A3 (en) 2002-05-30
HUP0202508A3 (en) 2003-03-28
JP2003504310A (ja) 2003-02-04
MA26805A1 (fr) 2004-12-20
OA11963A (en) 2006-04-17
NO20015995D0 (no) 2001-12-07

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