RU2001116117A - NEW PIPERAZINE AND PIPERIDINE COMPOUNDS - Google Patents

NEW PIPERAZINE AND PIPERIDINE COMPOUNDS

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Publication number
RU2001116117A
RU2001116117A RU2001116117/04A RU2001116117A RU2001116117A RU 2001116117 A RU2001116117 A RU 2001116117A RU 2001116117/04 A RU2001116117/04 A RU 2001116117/04A RU 2001116117 A RU2001116117 A RU 2001116117A RU 2001116117 A RU2001116117 A RU 2001116117A
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RU
Russia
Prior art keywords
formula
compound
compound according
compounds
methyl
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RU2001116117/04A
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Russian (ru)
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RU2225406C2 (en
Inventor
Рулоф В. Фенстра
М. ВАН ДЕР ХЕЙДЕН Йоханнес А.
Йоханнес МОС
Стефен К. ЛОНГ
Гербен М. ВИССЕР
Корнелис Г. Крусе
СХАРРЕНБУРГ Густаф Й. М. ВАН
Геррит П. ТОРОП
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Дюфар Интернэшнл Рисерч Бв
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Publication of RU2001116117A publication Critical patent/RU2001116117A/en
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Publication of RU2225406C2 publication Critical patent/RU2225406C2/en

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Claims (11)

1. Соединения формулы (I)1. The compounds of formula (I)
Figure 00000001
Figure 00000001
где S1 представляет водород, галоген, алкил(1-3С), CN, CF3, OCF3, SCF3, алкокси (1-3С), амино или моно- или диалкил(1-3С)замещенный амино, или гидрокси;where S 1 represents hydrogen, halogen, alkyl (1-3C), CN, CF 3 , OCF 3 , SCF 3 , alkoxy (1-3C), amino or mono- or dialkyl (1-3C) substituted amino, or hydroxy; Z представляет =С или -N;Z represents = C or —N; R1 и R2 независимо представляют Н или алкил(1-3С), или R1 и R2 вместе могут образовывать мостик из 2 или 3 атомов углерода,R 1 and R 2 independently represent H or alkyl (1-3C), or R 1 and R 2 together can form a bridge of 2 or 3 carbon atoms, R4 представляет водород или алкил(1-3С),R 4 represents hydrogen or alkyl (1-3C), Q представляет метил, этил, этил, замещенный одним или несколькими атомами фтора, или циклопропилметил, необязательно замещенный одним или несколькими атомами фтора,Q is methyl, ethyl, ethyl substituted with one or more fluorine atoms, or cyclopropylmethyl optionally substituted with one or more fluorine atoms, и их соли и пролекарства.and their salts and prodrugs.
2. Соединения по п.1, где S1, R1, R2 и R4 представляют водород, Q представляет метил или этил и Z имеет значение, определенное в п.1.2. The compounds of claim 1, wherein S 1 , R 1 , R 2, and R 4 are hydrogen, Q is methyl or ethyl, and Z is as defined in claim 1. 3. Соединения по п.2, где Z представляет -N.3. The compound of claim 2, wherein Z is —N. 4. Соединение по п.3, где Q представляет метил.4. The compound according to claim 3, where Q is methyl. 5. Способ получения соединении по п.1 реакцией взаимодействия соединения формулы (I), где Q представляет водород, с соединением формулы Q-Hal, где Q представляет метил или (необязательно фторированный)этил, (необязательно фторированный) циклопропилметил и Hal представляет галоген.5. A method for producing a compound according to claim 1 by reacting a compound of formula (I), where Q is hydrogen, with a compound of formula Q-Hal, where Q is methyl or (optionally fluorinated) ethyl, (optionally fluorinated) cyclopropylmethyl and Hal is halogen. 6. Способ получения соединений по п.1, где Z представляет -N, взаимодействием соединения формулы (II)6. The method of producing compounds according to claim 1, where Z is —N, by reacting a compound of formula (II)
Figure 00000002
Figure 00000002
с соединением формулы (III)with a compound of formula (III)
Figure 00000003
Figure 00000003
при этом в указанных формулах символы имеют значения, определенные в п.1.while in these formulas, the symbols have the meanings defined in paragraph 1.
7. Способ получения соединений формулы (I), где Z представляет =С, взаимодействием соединения формулы (IV)7. A method of obtaining compounds of formula (I), where Z represents = C, by the interaction of compounds of formula (IV)
Figure 00000004
Figure 00000004
с производным пиперидона, которое необязательно является R1 и/или R2 замещенным и имеет группу Q, с последующим дегидрированием и снятием защиты.with a piperidone derivative, which is optionally R 1 and / or R 2 substituted and has a Q group, followed by dehydrogenation and deprotection.
8. Фармацевтическая композиция, которая в качестве активного компонента содержит, по меньшей мере, одно соединение по п.1.8. The pharmaceutical composition, which as an active component contains at least one compound according to claim 1. 9. Способ получения фармацевтической композиции, отличающийся тем, что соединение по п.1 приводят в форму, подходящую для введения.9. A method of obtaining a pharmaceutical composition, characterized in that the compound according to claim 1 is brought into a form suitable for administration. 10. Способ лечения расстройств ЦНС, отличающийся тем, что используют соединение по п.1.10. A method of treating CNS disorders, characterized in that the compound according to claim 1 is used. 11. Способ лечения беспокойства и/или депрессии, отличающийся тем, что используют соединение по п.1.11. A method of treating anxiety and / or depression, characterized in that the compound according to claim 1 is used.
RU2001116117/04A 1998-11-13 1999-11-10 Alkyl-piperazinyl benzoxazolone and alkyl-piperidinyl benzoxazolone derivatives, method for their preparing and method for treatment RU2225406C2 (en)

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EP98203871 1998-11-13
EP98203871.3 1998-11-13

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US (1) US6780864B1 (en)
EP (1) EP1131308B1 (en)
JP (1) JP3638874B2 (en)
KR (1) KR100619465B1 (en)
CN (1) CN1225462C (en)
AR (1) AR021256A1 (en)
AT (1) ATE267183T1 (en)
AU (1) AU756470B2 (en)
BR (1) BR9915293B1 (en)
CA (1) CA2350137C (en)
CZ (1) CZ299774B6 (en)
DE (1) DE69917478T2 (en)
DK (1) DK1131308T3 (en)
DZ (1) DZ2934A1 (en)
ES (1) ES2217833T3 (en)
HK (1) HK1039489A1 (en)
HU (1) HUP0104922A3 (en)
IL (2) IL143028A0 (en)
MX (1) MXPA01004854A (en)
NO (1) NO318888B1 (en)
NZ (1) NZ511584A (en)
PL (1) PL193685B1 (en)
RU (1) RU2225406C2 (en)
SI (1) SI1131308T1 (en)
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TW (1) TWI252230B (en)
UA (1) UA71590C2 (en)
WO (1) WO2000029397A1 (en)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA73981C2 (en) 2000-03-10 2005-10-17 Merck Patent Gmbh (r)-(-)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane for treatment of extrapyramidal movement disorders (variants), pharmaceutical composition and kit
DZ3370A1 (en) * 2000-05-12 2001-11-15 Solvay Pharm Bv PIPERAZINE AND PIPERIDINE COMPOUNDS
AU2001267421A1 (en) * 2000-05-12 2001-11-20 Solvay Pharmaceuticals B.V. Use of compounds having combined dopamine d2, 5-ht1a and alpha adrenoreceptor agonistic action for treating cns disorders
RU2283648C2 (en) * 2000-11-14 2006-09-20 Мерк Патент Гмбх New application of combined selective antagonists of dopamine d2 receptor and agonists of 5-нт 1a receptor
AR034206A1 (en) * 2001-02-16 2004-02-04 Solvay Pharm Bv A PROCEDURE FOR THE PREPARATION OF MESILATES OF PIPERAZINE DERIVATIVES AND SUCH MESILATES
US6800648B2 (en) 2001-04-26 2004-10-05 Wyeth Antipsychotic aminomethyl derivatives of 7,8-dihydro-3H-1,6,9-trioxa-3-AZA-cyclopenta[a]naphthalen-2-one
US6743796B2 (en) * 2001-05-07 2004-06-01 Wyeth Piperazinyl-isatins
DK1408964T3 (en) 2001-07-26 2007-05-21 Merck Patent Gmbh Hitherto unknown use of 2-5- (4-fluorophenyl) -3-pyridylmethylaminomethyl-chroman and physiologically acceptable salts thereof
EP1336406A1 (en) * 2002-02-14 2003-08-20 Solvay Pharmaceuticals B.V. Partial dopamine-D2 receptor agonist plus serotonin and/or noradrenaline inhibitory activity
AU2003244160A1 (en) * 2002-06-25 2004-01-06 Sumitomo Pharmaceuticals Co., Ltd. Novel benzoxazolinone derivative
US7435738B2 (en) 2003-08-18 2008-10-14 Solvay Pharmaceuticals, Inc. Stable crystalline form of bifeprunox mesylate (7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate)
US7596407B2 (en) 2004-03-26 2009-09-29 Solvay Pharmaceuticals, B.V. Transdermal iontophoretic delivery of piperazinyl-2(3H)-benzoxazolone compounds
EP1595542A1 (en) * 2004-03-26 2005-11-16 Solvay Pharmaceuticals B.V. Transdermal iontophoretic delivery of piperazinyl-2(3H)-benzoxazolone compounds
ATE440826T1 (en) * 2004-05-27 2009-09-15 Ucb Pharma Sa BENZOXAZOLONE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND THEIR APPLICATIONS
US7405216B2 (en) 2004-08-18 2008-07-29 Solvay Pharmaceuticals, B.V. Stable crystalline form of bifeprunox mesylate (7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate)
US7423040B2 (en) 2005-02-18 2008-09-09 Irene Eijgendaal Stable crystalline form of bifeprunox mesylate, dosage forms thereof and methods for using same
US7964604B2 (en) 2005-02-18 2011-06-21 Solvay Pharmaceuticals B.V. Bifeprunox mesylate maintenance dose compositions and methods for using the same
US7750013B2 (en) 2005-08-22 2010-07-06 Solvay Pharmaceuticals, B.V. N-oxides as prodrugs of piperazine and piperidine derivatives
AR058022A1 (en) * 2005-08-22 2008-01-23 Solvay Pharm Bv DERIVATIVES OF BENZOOXAZOLES, PHARMACEUTICAL COMPOSITIONS AND ITS USE FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS.
ES2318783T3 (en) * 2005-08-22 2009-05-01 Solvay Pharmaceuticals B.V. N-OXIDES AS PROPHARMACES OF PIPERAZINE AND PIPERADINE DERIVATIVES.
US8106056B2 (en) 2006-06-16 2012-01-31 Solvay Pharmaceuticals B.V. Combination preparations comprising bifeprunox and a dopamine agonist
US7786126B2 (en) 2006-06-16 2010-08-31 Solvay Pharmaceuticals B.V. Combination preparations comprising SLV308 and a dopamine agonist
UY32934A (en) 2009-10-12 2011-05-31 Abbott Healthcare Products Bv PARDOPRUNOX MONOHIDRATE
WO2018039642A1 (en) 2016-08-26 2018-03-01 Exciva Ug (Haftungsbeschränkt) Compositions and methods thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2567884B1 (en) 1984-07-19 1987-03-06 Roussel Uclaf NEW INDOLE DERIVATIVES, THEIR PREPARATION, THEIR APPLICATION AS MEDICAMENTS AND THE COMPOSITIONS CONTAINING THEM
EP0190472B1 (en) * 1984-12-21 1989-07-12 Duphar International Research B.V New pharmaceutical compositions having anti-psychotic properties
EP0189612B1 (en) * 1984-12-21 1992-11-04 Duphar International Research B.V New pharmaceutical compositions having a psychotropic activity
DK148392D0 (en) * 1992-12-09 1992-12-09 Lundbeck & Co As H Heterocyclic Compounds
ZA954689B (en) 1994-06-08 1996-01-29 Lundbeck & Co As H 4-Aryl-1-(indanmethyl dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl) piperidines tetrahydropyridines or piperazines
JP3155008B2 (en) * 1994-07-26 2001-04-09 ファイザー・インコーポレーテッド 4-indole derivatives as serotonin agonists and antagonists
ATE340173T1 (en) * 1996-03-29 2006-10-15 Duphar Int Res PIPERAZINE AND PIPERIDINE DERIVATIVES
EP0900792B1 (en) 1997-09-02 2003-10-29 Duphar International Research B.V Piperazine and piperidine derivatives as 5-HT1A and dopamine D2-receptor (ant)agonists

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