RU2002120906A - Производные пиперидина и пиперазина - Google Patents

Производные пиперидина и пиперазина Download PDF

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RU2002120906A
RU2002120906A RU2002120906/04A RU2002120906A RU2002120906A RU 2002120906 A RU2002120906 A RU 2002120906A RU 2002120906/04 A RU2002120906/04 A RU 2002120906/04A RU 2002120906 A RU2002120906 A RU 2002120906A RU 2002120906 A RU2002120906 A RU 2002120906A
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Карл-Аугуст АККЕРМАНН (DE)
Карл-Аугуст АККЕРМАНН
Хеннинг БЁТТХЕР (DE)
Хеннинг БЁТТХЕР
Хельмут ПРЮХЕР (DE)
Хельмут ПРЮХЕР
Кристоф ВАН-АМСТЕРДАМ (DE)
Кристоф ВАН-АМСТЕРДАМ
Кристоф ЗЕЙФРИД (DE)
Кристоф Зейфрид
Хартмут ГРАЙНЕР (DE)
Хартмут Грайнер
Герд БАРТОШИК (DE)
Герд Бартошик
Юрген ХАРТИНГ (DE)
Юрген Хартинг
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Мерк Патент ГмбХ (DE)
Мерк Патент Гмбх
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Claims (10)

1. Соединения формулы I
Figure 00000001
в которой R1 и R2 каждый, независимо друг от друга, представляют собой фенильный или нафтильный радикал, который может быть незамещенным или замещенным R3, R4 и/или R5 либо обозначают Het1,
R3, R4 и R5 каждый, независимо друг от друга, обозначают Hal, A, OA, ОН, CN, NO2, NH2, NHA, NA2, NH-ацил, ацил, -SA, -SOA, SO2A, COOA или фенил,
Х обозначает СН или N,
Y обозначает SO2, если Х=N или S, SO или SO2, если Х=СН,
Het1 обозначает ненасыщенную гетероциклическую кольцевую систему, которая может быть незамещенной, либо монозамещенной, бизамещенной или тризамещенной Hal, A, CN, CONH2, CH2COOA, фенил-SO2, ацилом, OA или ОН, и которая содержит один, два или три одинаковых или различных гетероатомов, таких, как азот, кислород и сера,
А обозначает алкил, содержащий 1-6 атомов углерода,
alk обозначает алкилен, содержащий 1-6 атомов углерода, и
Hal обозначает F, CI, Br или I,
где Het1 ≠ 2,1,3-бензоксадиазолил или 2,1,3-бензотиадиазолил, и их физиологически приемлемые соли и сольваты.
2. Соединения по п.1
a) 8-{4-[2-(4-фторфенил)этил]пиперазин-1-сульфонил)хинолин;
b) 4-(4-фторфенилсульфонил)-1-[2-(4-фторфенил)этил]пиперидин;
с) 2-хлор-6-{1-[2-(4-фторфенил)этил]пиперидин-4-сульфонил}пиридин;
d) 4-(2-метоксифенилсульфанил)-1-[2-(4-фторфенил)этил]пиперидин;
e) 4-(4-метилфенилсульфинил)-1-[2-(4-фторфенил)этил]пиперидин;
f) 4-(3-циано-1Н-индол-5-сульфонил)-1-[2-(4-фторфенил)этил]-пиперазин и их физиологически приемлемые соли и сольваты.
3. Способ получения соединений формулы I по п.1, в которой Х обозначает N, отличающийся тем, что
а) проводят реакцию соединения формулы II
Figure 00000002
в которой R1 и alk соответствуют определениям, приведенным в п.1, с соединением формулы III
R2Y-L III
в которой L обозначает Cl, Br, I или свободную, либо активно функционально модифицированную группу ОН,
а R2 и Y соответствуют определениям, приведенным в п.1, или
b) если это желательно, один из радикалов R1 и/или R2 преобразуют в другой радикал R1 и/или R2 при помощи, например, отщепления группы ОА, что приводит к образованию группы ОН, и/или преобразуют группу СНО в группу CN, и/или
полученное основание формулы 1 преобразуют в одну из его солей при помощи обработки кислотой.
4. Способ получения соединений формулы I по п.1, в которой Х обозначает СН, отличающийся тем, что
а) проводят реакцию соединения формулы IV
Figure 00000003
в которой R2 соответствует определению, приведенному в п.1, с соединением формулы V
R1-alk-L V
в которой L обозначает Cl, Br, I или свободную, либо активно функционально модифицированную группу ОН, а R1 и alk соответствуют определениям, приведенным в п.1,
и затем производят окисление продукта этой реакции, или
b) если это желательно, один из радикалов R1 и/или R2 преобразуют в другой радикал R1 и/или R2 при помощи, например, отщепления группы ОА, которое приводит к образованию группы ОН, и/или посредством преобразования группы СНО в группу CN, и/или
полученное основание формулы I преобразуют в одну из его солей при помощи обработки кислотой.
5. Соединения формулы I по п.1 и их физиологически приемлемые соли и сольваты в качестве медицинских препаратов.
6. Соединения формулы I
Figure 00000004
в которой R1 и R2 каждый, независимо друг от друга, обозначают фенильный или нафтильный радикал, который может быть незамещенным или замещенным R3, R4 и/или R5
или обозначают Het1,
R3, R4 и R5 каждый, независимо друг от друга, обозначают Hal, A, OA, ОН, CN, NO2, NH2, NHA, NA2, NH-ацил, ацил, -SA, -SOA, SO2A, COOA или фенил,
Х обозначает СН или N,
Y обозначает SO2 если Х=М, или S, SO или SO2, если Х=СН,
Het1 обозначает ненасыщенную гетероциклическую кольцевую систему, которая может быть незамещенной, или монозамещенной, бизамещенной, либо тризамещенной Hal, A, CN, CONH2, CH2COOA, фенил-SO2, ацилом, OA или ОН, и содержащую один, два или три одинаковых или различных гетероатомов, таких, как азот, кислород и сера,
А обозначает алкил, содержащий 1 -6 атомов углерода,
alk обозначает алкилен, содержащий 1-6 атомов углерода, и
Hal обозначает F, CI, Br или I,
и их физиологически приемлемые соли и сольваты в качестве медицинских препаратов, оказывающих антагонистическое действие на рецептор 5-НТ2А.
7. Медицинские препараты по пп.5 или 6 для лечения психозов, шизофрении, депрессии, неврологических расстройств, расстройств памяти, болезни Паркинсона, бокового амиотрофического склероза, болезни Альцгеймера, болезни Хантингтона, расстройств аппетита, таких, как ненормально повышенное чувство голода, невротическая потеря аппетита, предменструального синдрома и/или для положительного воздействия на навязчиво-невротические расстройства (OCD).
8. Фармацевтические композиции, включающие, по крайней мере, один медицинский препарат по пп.5 или 6 и, возможно также, носители и/или вспомогательные вещества и возможно - другие активные ингредиенты.
9. Применение соединений по п.1 и/или их физиологически приемлемых солей и сольватов для производства медицинских препаратов, оказывающих антагонистическое действие на рецептор 5-НТ2A.
10. Применение соединений по п.9 для производства медицинских препаратов, предназначенных для лечения психозов, шизофрении, депрессии, неврологических расстройств, расстройств памяти, болезни Паркинсона, бокового амиотрофического склероза, болезни Альцгеймера, болезни Хантингтона, расстройств аппетита, таких, как ненормально повышенное чувство голода, невротическая потеря аппетита, предменструального синдрома и/или для положительного воздействия на навязчиво-невротические расстройства (OCD).
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2483068C2 (ru) * 2007-08-07 2013-05-27 Эбботт Гмбх Унд Ко.Кг Соединения хинолина, пригодные для лечения нарушений, являющихся ответом на модуляцию рецептора 5-ht6 серотонина

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0007907D0 (en) * 2000-03-31 2000-05-17 Merck Sharp & Dohme Therapeutic agents
AU2002360561A1 (en) * 2001-12-11 2003-06-23 Sepracor, Inc. 4-substituted piperidines, and methods of use thereof
DE10201550A1 (de) * 2002-01-17 2003-07-31 Merck Patent Gmbh Phenoxy-Piperidine
WO2003062224A1 (en) * 2002-01-17 2003-07-31 Eli Lilly And Company Aza-cyclic compounds as modulators of acetylcholine receptors
OA12792A (en) 2002-03-13 2006-07-10 Janssen Pharmaceutica Nv Sulfonyl-derivatives as novel inhibitors of histone deacetylase.
ATE460933T1 (de) * 2002-05-24 2010-04-15 Carl-Fr Coester Pharmazeutische wirkstoffkombination sowie deren verwendung
US7378525B2 (en) 2002-12-23 2008-05-27 Millennium Pharmaceuticals, Inc. CCR8 inhibitors
US7491827B2 (en) 2002-12-23 2009-02-17 Millennium Pharmaceuticals, Inc. Aryl sulfonamides useful as inhibitors of chemokine receptor activity
TW200510311A (en) 2002-12-23 2005-03-16 Millennium Pharm Inc CCr8 inhibitors
GB0311349D0 (en) * 2003-05-16 2003-06-25 Merck Sharp & Dohme Therapeutic agents, compositions, preparations and uses
WO2005063247A1 (en) * 2003-12-22 2005-07-14 Amgen Inc. Aryl sulfonamide compounds and uses related thereto
MXPA06012143A (es) * 2004-04-20 2007-05-15 Amgen Inc Arilsulfonamidas y usos relacionados con las mismas.
TWI391387B (zh) * 2004-05-12 2013-04-01 Eisai R&D Man Co Ltd 具有哌啶環之吲哚衍生物
US20050282818A1 (en) * 2004-06-22 2005-12-22 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
GB0419192D0 (en) 2004-08-27 2004-09-29 Merck Sharp & Dohme Therapeutic agents
EP1847535A4 (en) * 2005-02-04 2011-03-09 Eisai R&D Man Co Ltd 1- (piperidin-4-yl) -1H-indole derivatives
GB0504828D0 (en) * 2005-03-09 2005-04-13 Merck Sharp & Dohme Therapeutic agents
JP4932717B2 (ja) * 2005-05-11 2012-05-16 エーザイ・アール・アンド・ディー・マネジメント株式会社 ピペリジン環を有するインドール誘導体の製造方法
JPWO2006121104A1 (ja) * 2005-05-11 2008-12-18 エーザイ・アール・アンド・ディー・マネジメント株式会社 ピペリジン環を有するインドール誘導体の結晶およびその製法
US8071602B2 (en) * 2005-08-09 2011-12-06 M's Science Corporation Piperidine and piperazine derivatives
NZ567629A (en) 2005-09-23 2011-08-26 Ms Science Corp Piperazine derivatives useful in the treatment of discorders of the central nervous system
ES2355607T3 (es) 2006-01-27 2011-03-29 M's Science Corporation Derivados de piperidina y piperazina.
US20070238876A1 (en) * 2006-04-10 2007-10-11 Neera Tewari Process for the preparation of aripiprazole
US20110281890A1 (en) * 2008-03-19 2011-11-17 M's Science Corporation Piperidine and piperazine derivatives

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2439195A2 (fr) * 1978-10-16 1980-05-16 Synthelabo Derives du naphtalene et leur application en therapeutique
ZA848275B (en) * 1983-12-28 1985-08-28 Degussa New piridine-2-ethers or pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring
US4695575A (en) * 1984-11-13 1987-09-22 Janssen Pharmaceutica, N.V. 4-[(bicycle heterocyclyl)-methyl and -hetero]-piperidines
US5643995A (en) * 1987-06-11 1997-07-01 Amoco Corporation Method for improving the processabilty of polyphthalamides
JPH01131158A (ja) * 1987-08-03 1989-05-24 Ss Pharmaceut Co Ltd 置換アルキルピペラジン誘導体
PH25458A (en) * 1987-08-24 1991-07-01 Eisai Co Ltd Piperidine derivatives, therapeutic, preventive agents
FR2642069B1 (fr) * 1989-01-20 1991-04-12 Rhone Poulenc Sante Nouveaux derives du benzopyranne, leur preparation et les compositions pharmaceutiques qui les contiennent
JP2983257B2 (ja) * 1990-06-22 1999-11-29 三井化学株式会社 新規複素環式化合物及び医薬組成物
JP3036789B2 (ja) * 1990-06-22 2000-04-24 三井化学株式会社 新規な複素環式化合物及び医薬組成物
US5418242A (en) * 1993-05-18 1995-05-23 Laboratoires Upsa Piperidinylthioindole derivatives, their methods of preparation and pharmaceutical compositions in which they are present, useful especially as analgesics
US5567711A (en) * 1995-04-19 1996-10-22 Abbott Laboratories Indole-3-carbonyl and indole-3-sulfonyl derivatives as platelet activating factor antagonists
GB9901147D0 (en) * 1999-01-19 1999-03-10 Merck Sharp & Dohme Therapeutic agents

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2483068C2 (ru) * 2007-08-07 2013-05-27 Эбботт Гмбх Унд Ко.Кг Соединения хинолина, пригодные для лечения нарушений, являющихся ответом на модуляцию рецептора 5-ht6 серотонина

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