RU2453543C2 - Новые производные пиридона, обладающие антагонистической активностью в отношении mch, и лекарственные средства, включающие такие соединения - Google Patents

Новые производные пиридона, обладающие антагонистической активностью в отношении mch, и лекарственные средства, включающие такие соединения Download PDF

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RU2453543C2
RU2453543C2 RU2009110446/04A RU2009110446A RU2453543C2 RU 2453543 C2 RU2453543 C2 RU 2453543C2 RU 2009110446/04 A RU2009110446/04 A RU 2009110446/04A RU 2009110446 A RU2009110446 A RU 2009110446A RU 2453543 C2 RU2453543 C2 RU 2453543C2
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RU2009110446/04A
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Дирк ШТЕНКАМП (DE)
Дирк Штенкамп
Штефан Георг МЮЛЛЕР (DE)
Штефан Георг Мюллер
Торстен ЛЕМАНН-ЛИНТЦ (DE)
Торстен Леманн-Линтц
Геральд Юрген РОТ (DE)
Геральд Юрген Рот
Йёрг КЛЕЙ (DE)
Йёрг Клей
Клаус РУДОЛЬФ (DE)
Клаус Рудольф
Армин ХЕККЕЛЬ (DE)
Армин Хеккель
Маркус ШИНДЛЕР (GB)
Маркус Шиндлер
Ральф ЛОТЦ (DE)
Ральф Лотц
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Бёрингер Ингельхайм Интернациональ Гмбх
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Abstract

Настоящее изобретение относится к соединениям общей формулы (I), где группы и радикалы R1, R2 независимо друг от друга обозначают Н, C1-8-алкил или С3-7-циклоалкил, причем алкильная или циклоалкильная группа может быть моно- или полизамещенной одинаковыми или различными группами R11; или R2 обозначает -СН2-или -СН2-СН2- мостик, который связан с группой Y, и R1 является таким, как определено выше, или обозначает группу, выбранную из С1-4-алкил-СО, С1-4-алкил-О-СО-, (С1-4-алкил)NH-CO- или (С1-4-алкил)2N-СО-, где алкильные группы могут быть моно- или полифторированы; или R1 и R2 образуют алкиленовый мостик такой, что R1R2N- обозначает группу, выбранную из: азетидин, пирролидин, пиперидин, азепан, 2,5-дигидро-1H-пиррол, 1,2,3,6-тетрагидропиридин, 2,3,4,7-тетрагидро-1H-азепин, 2,3,6,7-тетрагидро-1H-азепин, пиперазин, в котором свободная иминогруппа замещена R13, пиперидин-4-он, морфолин, тиоморфолин, 4-С1-4-алкоксииминопиперидин-1-ил и 4-гидроксииминопиперидин-1-ил; причем в случае, когда R1 и R2 образуют алкиленовый мостик, в алкиленовом мостике один или несколько атомов Н могут быть замещены одинаковыми или различными группами R14, и X обозначает С1-3-алкиленовый мостик, который может включать один, два или три одинаковых или различных С1-4-алкильных заместителей; и Y обозначает группу подформулы выбранной из: и ; где группа может быть монозамещенной заместителем R20; Z обозначает -СН2-СН2- или -C(=O)-CH2-; U, V оба обозначают СН, или одна из групп U, V обозначает N, а другая из U, V обозначает СН, где СН может быть замещена L; и L независимо друг от друга обозначает галоген, циано или С1-3-алкил; и k обозначает 0, 1 или 2; W выбран из группы, состоящей из -СН2-O- и -O-СН2-; В выбран из группы, состоящей из фенила, пи�

Description

Текст описания приведен в факсимильном виде.
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Claims (12)

1. Соединения общей формулы I:
Figure 00000228

где R1, R2 независимо друг от друга обозначают Н, С1-8-алкил или С3-7-циклоалкил, причем алкильная или циклоалкильная группа может быть моно- или полизамещенной одинаковыми или различными группами R11;
или
R2 обозначает -СН2- или -СН2-СН2- мостик, который связан с группой Y, и R1 является таким, как определено выше, или обозначает группу, выбранную из С1-4-алкил-СО-, С1-4-алкил-О-СО-, (С1-4-алкил)NH-СО- или (С1-4алкил)2N-СО-, где алкильные группы могут быть моно- или полифторированы; или
R1 и R2 образуют алкиленовый мостик такой, что R1R2N- обозначает группу, выбранную из: азетидин, пирролидин, пиперидин, азепан, 2,5-дигидро-1Н-пиррол, 1,2,3,6-тетрагидропиридин, 2,3,4,7-тетрагидро-1Н-азепин, 2,3,6,7-тетрагидро-1Н-азепин, пиперазин, в котором свободная иминогруппа замещена R13, пиперидин-4-он, морфолин, тиоморфолин, 4-С1-4-алкоксииминопиперидин-1-ил и 4-гидроксииминопиперидин-1-ил; причем в случае, когда R1 и R2 образуют алкиленовый мостик, в алкиленовом мостике один или несколько атомов Н могут быть замещены одинаковыми или различными группами R14, и
X обозначает С1-3-алкиленовый мостик, который может включать один, два или три одинаковых или различных С1-4-алкильных заместителей; и Y обозначает группу подформулы, выбранной из:
Figure 00000229
и
Figure 00000230
;
где группа может быть монозамещенной заместителем R20;
Z обозначает -СН2-СН2- или -С(=O)-СН2-;
U, V оба обозначают СН, или одна из групп U, V обозначает N, а другая из U, V обозначает СН, где СН может быть замещена L; и
L независимо друг от друга обозначает галоген, циано или С1-3-алкил; и k обозначает 0, 1 или 2;
W выбран из группы, состоящей из -СН2-O- и -O-СН2-;
В выбран из группы, состоящей из фенила, пиридила, пиридазинила, пиразинила, пиримидинила, пирролила, пиразолила, имидазолила, триазолила, тетразолила, фурила, тиофенила и тиазолила; каждая из которых может быть моно- или полизамещена одинаковыми или различными заместителями R20; и
R11 обозначает галоген, С1-6-алкил, R15-O-, R15-O-CO, R15-CO-O, циано, R16R17N-, R18R19N-CO- или С3-7-циклоалкил, причем в описанных выше группах один или несколько атомов С могут быть замещены независимо друг от друга заместителями, выбранными из F;
R13 имеет одно из значений, указанных для R17 или обозначает формил; R14 обозначает галоген, циано, С1-6-алкил, R15-O-, R15-O-CO-, R15-CO-, R15CO-O-, R16R17N-, HCO-NR15-, R18R19N-CO-, R18R19N-CO-NH-, R15-O-C1-3-алкил, R15-О-СО-С1-3-алкил-, R15-SO2-NH-, R15-SO2-N(C1-3-алкил)-, R15-O-CO-NH-C1-3-алкил-, R15-SO2-NH-C1-3-алкил-, R15-CO-С1-3-алкил-, R15-CO-O-С1-3-алкил-, R16R17N-C1-3-алкил-, R18R19N-CO-С1-3-алкил-,
R15 обозначает H, С1-4-алкил, С3-7-циклоалкил, С3-7-циклоалкил-С1-3-алкил,
R16 обозначает H, С1-4-алкил, С3-7-циклоалкил, ω-гидрокси-С2-3-алкил, ω-(С1-4-алкокси)-С2-3-алкил, амино-С2-6-алкил, С1-4-алкиламино-С2-6-алкил, ди-(С1-4-алкил)амино-С2-6-алкил,
R17 имеет одно из значений, указанных для R16, или обозначает С1-4-алкилкарбонил, С1-4-алкоксикарбонил;
R18, R19 независимо друг от друга обозначают Н или С1-6-алкил, где R18, R19 могут быть связаны с образованием С3-6-алкиленового мостика;
R20 обозначает галоген, гидрокси, циано, нитро, C1-6-алкил, гидрокси-С1-3-алкил или С1-4-алкокси; и
причем в описанных выше группах и радикалах, особенно в L, W, X, Z, R11, R13 -R20, в каждом случае один или несколько атомов С дополнительно могут быть моно- или полизамещены F, и/или в каждом случае один или два атома С независимо друг от друга дополнительно могут быть монозамещены Сl или Br, и/или в каждом случае одно или несколько фенильных колец дополнительно могут включать независимо друг от друга один, два или три заместителя, выбранных из группы F, Cl, Br, I, циано, С1-4-алкила, С1-4-алкокси, дифторметила, трифторметила, гидрокси, амино, С1-3-алкиламино, ди-(С1-3-алкил)амино, ацетиламино, аминокарбонила, дифторметокси, трифторметокси, амино-С1-3-алкила, C1-3-алкиламино-С1-3-алкил- и ди-(С1-3-алкил)амино-С1-3-алкила, и/или могут быть монозамещены нитро, и их соли.
2. Соединения по п.1, отличающиеся тем, что группы R1, R2 независимо друг от друга выбраны из группы, состоящей из Н, С1-4-алкила, С3-7-циклоалкил-С1-3-алкила, гидрокси-С1-4-алкила, С3-7-циклоалкила, гидрокси-С3-7-циклоалкила, дигидрокси-С3-6-алкила, С1-4-алокси-С2-3-алкила, гидрокси-С1-4-алкокси-С2-3-алкила, С1-4-алкокси- С1-4-алкокси-С2-3-алкила, причем алкильные, циклоалкильные или циклоалкилалкильные группы могут быть дополнительно моно- или дизамещены гидрокси и/или гидрокси-С1-3-алкилом, и/или моно- или полизамещены F или C1-3-алкилом, и/или монозамещены CF3, Br, Сl или CN.
3. Соединения по п.1, отличающиеся тем, что R1 и R2 вместе с атомом N, с которым они связаны, образуют гетероциклическую группу, которая выбрана из следующих значений: азетидин, пирролидин, пиперидин, пиперазин, в котором свободная иминогруппа замещена R13, и морфолин; причем один или несколько атомом Н могут быть замещены одинаковыми или различными группами R14, и группы R13, R14 являются такими, как определено в п.1.
Figure 00000231
4. Соединения по п.1, отличающиеся тем, что подформула выбрана из группы, состоящей из:
Figure 00000232
Figure 00000233
Figure 00000234

Figure 00000235
,
Figure 00000236
,
где R1 обозначает Н, С1-4-алкил или С1-4-алкилкарбонил, причем алкильная группа может быть моно- или полифторирована, L1 определен как R20 и kl обозначает 0 или 1.
5. Соединения по п.1, отличающиеся тем, что X обозначает -СН2-, -СН2-СН2- или -СН2-СН2-СН2- мостиковую группу, где один или два атома водорода могут быть замещены одинаковыми или различными C1-3-алкильными группами.
6. Соединения по п.1, отличающиеся тем, что группа Y обозначает
Figure 00000229
;
где группа может быть монозамещенной заместителем R20.
7. Соединения по п.1, отличающиеся тем, что группа Z обозначает -С(=O)-СН2-.
8. Соединения по п.1, отличающиеся тем, что группа W обозначает -O-СН2-.
9. Соединения по п.1, отличающиеся тем, что группа В выбрана из группы, состоящей из фенила и пиридила, где указанная группа В может быть моно- или полизамещена одинаковыми или различными заместителями R20.
10. Соединения по п.1, в виде их физиологически приемлемых солей.
11. Фармацевтическая композиция, обладающая антагонистической активностью в отношении рецептора МСН, содержащая соединение по одному или нескольким пп.1-9 или его соль, необязательно вместе с одним или несколькими инертными носителями и/или разбавителями.
12. Соединение, выбранное из группы состоящей из:
5-Бензилокси-2-{2-[4-(3-гидрокси-3-метилпирролидин-1-илметил)фенил]-2-оксоэтил}-2Н-пиридазин-3-он,
5-Бензилокси-2-{2-[4-((R)-3-гидроксипирролидин-1-илметил)фенил]-2-оксоэтил}-2Н-пиридазин-3-он,
5-Бензилокси-2-{2-[4-(4-гидроксипиперидин-1-илметил)фенил]-2-оксоэтил}-2Н-пиридазин-3-он,
5-(5-Хлорпиридин-2-илметокси)-2-[2-оксо-2-(4-пиперидин-1-илметилфенил)этил]-2Н-пиридазин-3-он,
6-Бензилокси-3-{2-[4-(4-гидрокси-4-метилпиперидин-1-илметил)фенил]-2-оксоэтил}-3Н-пиримидин-4-он,
5-Бензилокси-2-[2-оксо-2-(1,2,3,4-тетрагидроизохинолин-7-ил)этил]-2Н-пиридазин-3-он,
5-(5-Бромпиридин-2-илметокси)-2-[2-оксо-2-(1,2,3,4-тетрагидроизохинолин-7-ил)этил]-2Н-пиридазин-3-он,
5-(5-Бромпиридин-2-илметокси)-2-[2-(2-метил-1,2,3,4-тетрагидроизохинолин-7-ил)-2-оксоэтил]-2Н-пиридазин-3-он,
5-Бензилокси-2-[2-(2,3-дигидро-1Н-изоиндол-5-ил)-2-оксоэтил]-2Н-пиридазин-3-он и
5-Бензилокси-2-[2-(2-метил-2,3-дигидро-1Н-изоиндол-5-ил)-2-оксоэтил]-2Н-пиридазин-3-он.
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Publication number Priority date Publication date Assignee Title
US7344702B2 (en) 2004-02-13 2008-03-18 Bristol-Myers Squibb Pharma Company Contrast agents for myocardial perfusion imaging
AU2009204048B2 (en) 2008-01-11 2013-08-01 Albany Molecular Research, Inc. (1-azinone) -substituted pyridoindoles as MCH antagonists
WO2009103478A1 (en) * 2008-02-19 2009-08-27 Boehringer Ingelheim International Gmbh Pyridone and pyridazinone derivatives as mch antagonists
CA2967254C (en) 2008-02-29 2019-03-26 Lantheus Medical Imaging, Inc. Contrast agents for applications including imaging cancer
CA2726588C (en) 2008-06-03 2019-04-16 Karl Kossen Compounds and methods for treating inflammatory and fibrotic disorders
UY32442A (es) 2009-02-13 2010-09-30 Sanofi Aventis Nuevos indanos sustituidos, procesos para su preparacion y uso de los mismos como un medicamento
AR075402A1 (es) 2009-02-13 2011-03-30 Sanofi Aventis Derivados heterociclicos oxigenados y/o nitrogenados de tetrahidronaftaleno, medicamentos que los contienen y uso de los mismos en el tratamiento de trastornos metabolicos, tales como obesidad,entre otros.
WO2011003012A1 (en) 2009-07-01 2011-01-06 Albany Molecular Research, Inc. Azinone-substituted azapolycycle mch-1 antagonists, methods of making, and use thereof
WO2011003007A1 (en) 2009-07-01 2011-01-06 Albany Molecular Research, Inc. Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine mch-1 antagonists, methods of making, and use thereof
WO2011003005A1 (en) 2009-07-01 2011-01-06 Albany Molecular Research, Inc. Azinone-substituted azepino[b]indole and pyrido-pyrrolo-azepine mch-1 antagonists, methods of making, and use thereof
WO2011003021A1 (en) 2009-07-01 2011-01-06 Albany Molecular Research, Inc. Azinone-substituted azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine mch-1 antagonists, methods of making, and use thereof
US20110021570A1 (en) 2009-07-23 2011-01-27 Nancy-Ellen Haynes Pyridone glucokinase activators
SG10201500929XA (en) 2010-02-08 2015-04-29 Lantheus Medical Imaging Inc Methods and apparatus for synthesizing imaging agents, and intermediates thereof
WO2012088038A2 (en) 2010-12-21 2012-06-28 Albany Molecular Research, Inc. Piperazinone-substituted tetrahydro-carboline mch-1 antagonists, methods of making, and uses thereof
US8993765B2 (en) 2010-12-21 2015-03-31 Albany Molecular Research, Inc. Tetrahydro-azacarboline MCH-1 antagonists, methods of making, and uses thereof
EP2753605B1 (en) 2011-09-09 2019-03-27 Lantheus Medical Imaging, Inc. Compositions, methods, and systems for the synthesis and use of imaging agents
JP6129850B2 (ja) 2012-01-12 2017-05-17 武田薬品工業株式会社 Ｍｃｈ受容体拮抗剤としてのベンゾイミダゾール誘導体
US8933079B2 (en) 2012-03-07 2015-01-13 Boehringer Ingelheim International Gmbh Pyridone and pyridazinone derivatives as anti-obesity agents
EP2848622A4 (en) 2012-05-10 2015-11-04 Takeda Pharmaceutical AROMATIC RING CONNECTION
KR102057877B1 (ko) 2012-07-18 2019-12-20 노스 앤드 사우스 브라더 파마시 인베스트먼트 컴파니 리미티드 질소함유 헤테로고리 유도체 및 그의 약물에서의 용도
AU2013203000B9 (en) 2012-08-10 2017-02-02 Lantheus Medical Imaging, Inc. Compositions, methods, and systems for the synthesis and use of imaging agents
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
AU2014366049B2 (en) 2013-12-19 2018-04-05 Sunshine Lake Pharma Co., Ltd. Nitrogenous heterocyclic derivatives and their application in drugs
EP3126362B1 (en) 2014-04-02 2022-01-12 Intermune, Inc. Anti-fibrotic pyridinones
US9783159B1 (en) 2014-07-21 2017-10-10 State Farm Mutual Automobile Insurance Company Methods of theft prevention or mitigation
CN117538462B (zh) * 2024-01-10 2024-03-26 地奥集团成都药业股份有限公司 一种氨氯地平贝那普利胶囊有关物质的检测方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2004118719A (ru) * 2001-11-22 2005-03-27 Оно Фармасьютикал Ко., Лтд. (Jp) Производные пиперидин-2-она и фармацевтические композиции, содержащие такие соединения в качестве активного ингредиента

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1218336A2 (en) 1999-09-20 2002-07-03 Takeda Chemical Industries, Ltd. Melanin concentrating hormone antagonist
EP1285651B1 (en) 2000-04-28 2010-09-01 Takeda Pharmaceutical Company Limited Melanin concentrating hormone antagonists
CA2474239A1 (en) 2002-01-18 2003-07-24 Pharmacia Corporation Substituted pyridazinones as inhibitors of p38
KR100705519B1 (ko) * 2002-02-14 2007-04-10 파마시아 코포레이션 Ｐ３８ ｍａｐ 키나제의 조절제로서의 치환된 피리디논
DE10238865A1 (de) 2002-08-24 2004-03-11 Boehringer Ingelheim International Gmbh Neue Carbonsäureamid-Verbindungen mit MCH-antagonistischer Wirkung, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE10250708A1 (de) 2002-10-31 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
DE10250743A1 (de) 2002-10-31 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Amid-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
US7183287B2 (en) 2003-04-03 2007-02-27 Pharmacia Corporation Substituted pyrimidinones
WO2005007632A1 (en) 2003-07-18 2005-01-27 Pharmacia Corporation Substituted pyridazinones as inhibitors of p38
CL2004002050A1 (es) 2003-08-13 2005-06-03 Pharmacia Corp Sa Organizada B Compuestos derivados de piridinonas sustituidas; su uso en el tratamiento de afecciones causadas o exacerbadas por actividad p38 map kinasa y/o tnf no regulada, tales como inflamaciones, tumores, sida y otros.
DE10360745A1 (de) 2003-12-23 2005-07-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Amid-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
US7732456B2 (en) 2004-03-05 2010-06-08 Banyu Pharmaceutical Co., Ltd. Pyridone derivative
DE102004010893A1 (de) 2004-03-06 2005-09-22 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue ß-Ketoamid-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
DE102004017935A1 (de) 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
DE102004017933A1 (de) 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
DE102004017934A1 (de) 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
DE102004017932A1 (de) 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
DE102004017930A1 (de) 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
WO2007018248A1 (ja) 2005-08-10 2007-02-15 Banyu Pharmaceutical Co., Ltd. ピリドン化合物
US7875633B2 (en) 2005-08-24 2011-01-25 Banyu Pharmaceutical Co., Ltd. Phenylpyridone derivative
WO2007029847A1 (ja) 2005-09-07 2007-03-15 Banyu Pharmaceutical Co., Ltd. 二環性芳香族置換ピリドン誘導体
EP1943231A1 (en) 2005-10-26 2008-07-16 Boehringer Ingelheim International Gmbh (hetero)aryl compounds with mch antagonistic activity and medicaments comprising these compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2004118719A (ru) * 2001-11-22 2005-03-27 Оно Фармасьютикал Ко., Лтд. (Jp) Производные пиперидин-2-она и фармацевтические композиции, содержащие такие соединения в качестве активного ингредиента

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DYKE Н J ЕТ AL: "Recent developments in the discovery of MCH-1R antagonists for the treatment of obesity - an update" EXPERT OPINION ON THERAPEUTIC PATENTS, ASHLEY PUBLICATIONS, GB, v. 15, № 10, October 2005, p. 1303-1313. *

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