RU2011108024A - 3-азабицикло(3.1.0) гексильные производные в качестве модуляторов метаботропных глутаматных рецепторов - Google Patents
3-азабицикло(3.1.0) гексильные производные в качестве модуляторов метаботропных глутаматных рецепторов Download PDFInfo
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Abstract
1. Соединение, имеющее формулу (I) ! , ! или его стереохимически изомерная форма, где ! R1 представляет собой С1-6алкил или С1-3алкил, замещенный С3-7циклоалкилом, галогено, фенилом или фенилом, замещенным галогено, трифторметилом или трифторметокси; !R2 представляет собой галогено, трифторметил, С1-3алкил или циклопропил; ! Х представляет собой ковалентную связь, О, NR3, NR3-CH2 или О-СН2; ! R3 представляет собой водород или С1-3алкил; и ! Ar представляет собой незамещенный фенил или фенил, замещенный n радикалами R4, ! где n равен 1, 2 или 3; ! где каждый R4 независимо выбран из группы, состоящей из галогено, С1-3алкила, гидроксиС1-3алкила, полигалогеноС1-3алкила, циано, гидроксила, амино, карбоксила, С1-3алкилоксиС1-3алкила, С1-3алкилокси, полигалогеноС1-3алкилокси, С1-3алкилкарбонила, моно- и ди(С1-3алкил)амино и морфолинила; ! или где два соседних радикала R4, взятые вместе, образуют бивалентный радикал формулы ! -N=CH-NH- (а), или ! -СН=СН-NH- (b), или ! -O-CH2-CH2-NH- (с); или ! его фармацевтически приемлемые соль присоединения или сольват. ! 2. Соединение по п.1 или его стереохимически изомерная форма, где ! R1 представляет собой С1-6алкил или C1-3алкил, замещенный С3-7циклоалкилом, фенилом или фенилом, замещенным галогено, трифторметилом или трифторметокси; ! R2 представляет собой галогено, трифторметил, C1-3алкил или циклопропил; ! Х представляет собой ковалентную связь, О, NR3, NR3-CH2 или O-CH2; ! R3 представляет собой водород или C1-3алкил; и ! Ar представляет собой незамещенный фенил или фенил, замещенный n радикалами R4, ! где n равен 1, 2 или 3; ! где каждый R4 независимо выбран из группы, состоящей из галогено, C1-3алкила, гидроксиС1-3алкила, полигалогеноС1-3алкила, циано, гидроксила, амино, к�
Claims (16)
1. Соединение, имеющее формулу (I)
или его стереохимически изомерная форма, где
R1 представляет собой С1-6алкил или С1-3алкил, замещенный С3-7циклоалкилом, галогено, фенилом или фенилом, замещенным галогено, трифторметилом или трифторметокси;
R2 представляет собой галогено, трифторметил, С1-3алкил или циклопропил;
Х представляет собой ковалентную связь, О, NR3, NR3-CH2 или О-СН2;
R3 представляет собой водород или С1-3алкил; и
Ar представляет собой незамещенный фенил или фенил, замещенный n радикалами R4,
где n равен 1, 2 или 3;
где каждый R4 независимо выбран из группы, состоящей из галогено, С1-3алкила, гидроксиС1-3алкила, полигалогеноС1-3алкила, циано, гидроксила, амино, карбоксила, С1-3алкилоксиС1-3алкила, С1-3алкилокси, полигалогеноС1-3алкилокси, С1-3алкилкарбонила, моно- и ди(С1-3алкил)амино и морфолинила;
или где два соседних радикала R4, взятые вместе, образуют бивалентный радикал формулы
-N=CH-NH- (а), или
-СН=СН-NH- (b), или
-O-CH2-CH2-NH- (с); или
его фармацевтически приемлемые соль присоединения или сольват.
2. Соединение по п.1 или его стереохимически изомерная форма, где
R1 представляет собой С1-6алкил или C1-3алкил, замещенный С3-7циклоалкилом, фенилом или фенилом, замещенным галогено, трифторметилом или трифторметокси;
R2 представляет собой галогено, трифторметил, C1-3алкил или циклопропил;
Х представляет собой ковалентную связь, О, NR3, NR3-CH2 или O-CH2;
R3 представляет собой водород или C1-3алкил; и
Ar представляет собой незамещенный фенил или фенил, замещенный n радикалами R4,
где n равен 1, 2 или 3;
где каждый R4 независимо выбран из группы, состоящей из галогено, C1-3алкила, гидроксиС1-3алкила, полигалогеноС1-3алкила, циано, гидроксила, амино, карбоксила, С1-3алкилоксиС1-3алкила, C1-3алкилокси, полигалогеноС1-3алкилокси, C1-3алкилкарбонила, моно- и ди(С1-3алкил)амино и морфолинила;
или где два соседних радикала R4, взятые вместе, образуют бивалентный радикал формулы
-N=CH-NH- (а), или
-CH=CH-NH- (b), или
-O-CH2-CH2-NH- (с); или
его фармацевтически приемлемые соль присоединения или сольват.
3. Соединение по п.1 или его стереохимически изомерная форма, где
R1 представляет собой 1-бутил, 2-метил-1-пропил, 3-метил-1-бутил, (циклопропил)метил или 2-(циклопропил)-1-этил;
R2 представляет собой хлоро;
Х представляет собой ковалентную связь или О-СН2; и
Ar представляет собой незамещенный фенил или фенил, замещенный n радикалами R4,
где n равен 1, 2 или 3;
где каждый R4 независимо выбран из группы, состоящей из галогено, трифторметила, морфолинила или гидроксиС1-3алкила;
или его фармацевтически приемлемые соль присоединения или сольват.
4. Соединение по п.1 или его стереохимически изомерная форма, где
R1 представляет собой 1-бутил, 2-метил-1-пропил, 3-метил-1-бутил, (циклопропил)метил или 2-(циклопропил)-1-этил;
R2 представляет собой хлоро;
Х представляет собой ковалентную связь или O-СН2; и
Ar представляет собой незамещенный фенил или фенил, замещенный n радикалами R4,
где n равен 2;
где каждый R4 независимо выбран из группы, состоящей из галогено;
или его фармацевтически приемлемые соль присоединения или сольват.
5. Соединение по п.1 или его стереохимически изомерная форма, где
R1 представляет собой 1-бутил, 3-метил-1-бутил, (циклопропил)метил или 2-(циклопропил)-1-этил;
R2 представляет собой хлоро;
Х представляет собой ковалентную связь или O-СН2; и
Ar представляет собой незамещенный фенил или 2,5-дихлорфенил;
или его фармацевтически приемлемые соль присоединения или сольват.
6. Соединение по п.1, выбранное из:
(2аα,3β,3аα)-1-бутил-3-хлор-4-[6-[(2,5-дихлор-феноксиметил)-3-аза-бицикло[3.1.0]гекс-3-ил]-1H-пиридин-2-она;
(2аα,3α,3аα)-1-бутил-3-хлор-4-[6-[(2,5-дихлор-феноксиметил)-3-аза-бицикло[3.1.0]гекс-3-ил]-1H-пиридин-2-она;
(2аα,3α,3аα)-1-бутил-3-хлор-4-(6-фенил-3-аза-бицикло[3.1.0]гекс-3-ил)-1H-пиридин-2-она;
(2аα,3α,3аα)-3-хлор-1-циклопропилметил-4-(6-фенил-3-аза-бицикло[3.1.0]гекс-3-ил)-1H-пиридин-2-она;
или его фармацевтически приемлемые соль присоединения или сольват.
7. Фармацевтическая композиция, содержащая терапевтически эффективное количество соединения по любому из пп.1-6 и фармацевтически приемлемый носитель или эксципиент.
8. Соединение по любому из пп.1-6 для применения в качестве лекарственного средства.
9. Применение соединения по любому из пп.1-6 или фармацевтической композиции по п.7 для изготовления лекарственного средства для лечения или предупреждения состояния у млекопитающего, включая человека, на лечение или предупреждение которого влияет нейромодуляторный эффект положительных аллостерических модуляторов метаботропного глутаматного рецептора 2 подтипа (mGluR2), или лечению или предупреждению которого он способствует.
10. Применение соединения по любому из пп.1-6 или фармацевтической композиции по п.7 для изготовления лекарственного средства для лечения или предупреждения расстройства центральной нервной системы, выбранного из группы, состоящей из тревожных расстройств, психотических расстройств, расстройств личности, расстройств, вызванных приемом психоактивных веществ, расстройств пищевого поведения, расстройств настроения, мигрени, эпилепсии или судорожных расстройств, расстройств детского возраста, когнитивных расстройств, нейродегенерации, нейротоксичности и ишемии.
11. Применение по п.10, где расстройство центральной нервной системы представляет собой тревожное расстройство, выбранное из группы, состоящей из агорафобии, генерализованного тревожного расстройства, обсессивно-компульсивного расстройства, панического расстройства, посттравматического стрессового расстройства, социальной фобии и других фобий.
12. Применение по п.10, где расстройство центральной нервной системы представляет собой психотическое расстройство, выбранное из группы, состоящей из шизофрении, бредового расстройства, шизоаффективного расстройства, шизофреноформного расстройства и психотического расстройства, вызванного приемом психоактивных веществ.
13. Применение по п.10, где расстройство центральной нервной системы представляет собой расстройство настроения, выбранное из группы, состоящей из биполярных расстройств (I и II типа), циклотимического расстройства, депрессии, дистимического расстройства, большого депрессивного расстройства и расстройства настроения, вызванного приемом психоактивных веществ.
14. Применение по п.10, где расстройство центральной нервной системы выбрано из группы, состоящей из тревоги, шизофрении, мигрени, депрессии и эпилепсии.
15. Применение соединения по любому из пп.1-6 в комбинации с ортостерическим агонистом mGluR2 для изготовления лекарственного средства для лечения или предупреждения состояния, охарактеризованного в любом из пп.9-14.
16. Продукт, содержащий
а) соединение по любому из пп.1-6; и
б) ортостерический агонист mGluR2,
в качестве комбинированного препарата для одновременного, раздельного или последовательного применения в лечении или предупреждении состояния у млекопитающего, на лечение или предупреждение которого влияет нейромодуляторный эффект аллостерических модуляторов mGluR2, или лечению или предупреждению которого он способствует.
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PCT/EP2009/006326 WO2010025890A1 (en) | 2008-09-02 | 2009-09-01 | 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors |
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TW200900065A (en) | 2007-03-07 | 2009-01-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives |
TW200845978A (en) | 2007-03-07 | 2008-12-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
JP5433579B2 (ja) | 2007-09-14 | 2014-03-05 | ジャンセン ファーマシューティカルズ, インコーポレイテッド. | 1,3−二置換−4−フェニル−1h−ピリジン−2−オン |
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NZ584152A (en) | 2007-09-14 | 2011-11-25 | Ortho Mcneil Janssen Pharm | 1,3-disubstituted 4-(aryl-x-phenyl)-1h-pyridin-2-ones |
MX2010005110A (es) | 2007-11-14 | 2010-09-09 | Ortho Mcneil Janssen Pharm | Derivados de imidazo[1,2-a]piridina y su uso como moduladores alostericos positivos de los receptores de glutamato metabotropico 2. |
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ES2439291T3 (es) | 2014-01-22 |
MX2011002042A (es) | 2011-06-20 |
JP2012501352A (ja) | 2012-01-19 |
CN102143955A (zh) | 2011-08-03 |
JP5547194B2 (ja) | 2014-07-09 |
RU2510396C2 (ru) | 2014-03-27 |
EP2344470A1 (en) | 2011-07-20 |
US8691849B2 (en) | 2014-04-08 |
CA2735764A1 (en) | 2010-03-11 |
WO2010025890A1 (en) | 2010-03-11 |
BRPI0918055A2 (pt) | 2015-12-01 |
CN102143955B (zh) | 2013-08-14 |
AU2009289784B2 (en) | 2012-03-22 |
US20110306642A1 (en) | 2011-12-15 |
EP2344470B1 (en) | 2013-11-06 |
AU2009289784A1 (en) | 2010-03-11 |
CA2735764C (en) | 2016-06-14 |
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