RU96100754A - N - [[1- [4- / 4-FLUORPHENOXY / BUTYL] -4-PIPERIDINYL] -N-METHYLAMINO] -2-BENZOTHIAZOLOLES AS ANTI-ARITHM MEDICINE CLASS III - Google Patents

N - [[1- [4- / 4-FLUORPHENOXY / BUTYL] -4-PIPERIDINYL] -N-METHYLAMINO] -2-BENZOTHIAZOLOLES AS ANTI-ARITHM MEDICINE CLASS III

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Publication number
RU96100754A
RU96100754A RU96100754/04A RU96100754A RU96100754A RU 96100754 A RU96100754 A RU 96100754A RU 96100754/04 A RU96100754/04 A RU 96100754/04A RU 96100754 A RU96100754 A RU 96100754A RU 96100754 A RU96100754 A RU 96100754A
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RU
Russia
Prior art keywords
compound according
piperidinyl
methylamino
butyl
compound
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Application number
RU96100754/04A
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Russian (ru)
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RU2122546C1 (en
Inventor
Ян Питер Хейкантс Йозеф
Ян Мария Боргерс Марсель
Вильхельм Дорис
Original Assignee
Жансен Фармасетика Н.В.
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Application filed by Жансен Фармасетика Н.В. filed Critical Жансен Фармасетика Н.В.
Publication of RU96100754A publication Critical patent/RU96100754A/en
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Publication of RU2122546C1 publication Critical patent/RU2122546C1/en

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Claims (9)

1. Соединение, имеющее формулу I
Figure 00000001

где один из заместителей R1 и R2 представляет собой гидроксигруппу, тогда как другой обозначает водород, а также его фармацевтически приемлемые соли присоединения кислоты.1. The compound having the formula I
Figure 00000001

where one of the substituents R 1 and R 2 represents a hydroxy group, while the other denotes hydrogen, as well as its pharmaceutically acceptable acid addition salts. 2. Соединение по п.1, которое представляет собой 2-[[1-[4-)-4-фторфенокси)бутил] 4-пиперидинил] метиламино]-5-бензотиазолол или его фармацевтически приемлемую соль присоединения кислоты. 2. The compound according to claim 1, which is 2 - [[1- [4 -) - 4-fluorophenoxy) butyl] 4-piperidinyl] methylamino] -5-benzothiazolol or its pharmaceutically acceptable acid addition salt. 3. Соединение по п. 1, которое представляет собой 2-[[1-[4-(4-фторфенокси)бутил] -4-пиперидинил] метиламино]-6-бензотиазолол или его фармацевтически приемлемую соль добавления кислоты. 3. The compound according to claim 1, which is 2 - [[1- [4- (4-fluorophenoxy) butyl] -4-piperidinyl] methylamino] -6-benzothiazolol or its pharmaceutically acceptable acid addition salt. 4. Соединение по п. 1, которое представляет собой 2-[[1-[4-)4-фторфенокси)бутил]-4-пиперидинил]метиламино]-6-бензотиазолол (Z)-2-бутендиоат (1 : 1). 4. The compound according to claim 1, which is a 2 - [[1- [4-) 4-fluorophenoxy) butyl] -4-piperidinyl] methylamino] -6-benzothiazolol (Z) -2-bundioate (1: 1) . 5. Антиаритмическая композиция III класса, включающая фармацевтически приемлемый наполнитель и в качестве активного ингредиента терапевтически эффективное количество соединения по любому из пп.1 - 4. 5. An antiarrhythmic composition of class III, including a pharmaceutically acceptable excipient and, as an active ingredient, a therapeutically effective amount of a compound according to any one of claims 1 to 4. 6. Способ получения композиции по п.4, отличающийся тем, что включает тщательное перемешивание терапевтически эффективного количества соединения по пп.1 - 4 с фармацевтически приемлемым наполнителем. 6. A method of obtaining a composition according to claim 4, characterized in that it includes thoroughly mixing a therapeutically effective amount of a compound according to claims 1-4 with a pharmaceutically acceptable excipient. 7. Соединение по любому из пп.1 - 4, предназначенное для использования в медицине. 7. The compound according to any one of paragraphs.1 to 4, intended for use in medicine. 8. Соединение по любому из пп.1 - 4, предназначенное для использования в качестве антиаритмических средств III класса. 8. The compound according to any one of paragraphs.1 to 4, intended for use as an antiarrhythmic agent of class III. 9. Способ приготовления соединения по п.1, отличающийся тем, что осуществляют N-алкилирование промежуточного соединения формулы II в том случае, когда один из двух заместителей R1 и R2 представляет собой гидроксигруппу, а другой - водород, реагентом формулы III, в которой W обозначает отщепляемую реакционную группу
Figure 00000002

а также при необходимости, превращение соединения формулы I в терапевтически активную метоксичную соль присоединения кислоты или, наоборот, превращение упомянутого соединения в виде соли присоединения кислоты в свободное основание путем обработки щелочью.9. The method of preparation of the compound according to claim 1, characterized in that N-alkylation of the intermediate compound of formula II is carried out in the case when one of the two substituents R 1 and R 2 is a hydroxy group, and the other is hydrogen, with a reagent of formula III wherein W denotes a leaving group
Figure 00000002

and, if necessary, the conversion of a compound of formula I into a therapeutically active methoxy acid addition salt or, conversely, the conversion of said compound in the form of an acid addition salt into a free base by treatment with alkali.
RU96100754A 1993-06-11 1994-06-06 N-[[1-[4-(fluorophenoxy)butyl]-4-piperidinyl]-n-methylamino]-2-benzthiazoles or their pharmaceutically acceptable acid salts, a method of synthesis, an antiarrhythmic composition of the third-class and a method of its preparing RU2122546C1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP93201685.0 1993-06-11
EP93201685 1993-06-11

Publications (2)

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RU96100754A true RU96100754A (en) 1998-03-27
RU2122546C1 RU2122546C1 (en) 1998-11-27

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RU96100754A RU2122546C1 (en) 1993-06-11 1994-06-06 N-[[1-[4-(fluorophenoxy)butyl]-4-piperidinyl]-n-methylamino]-2-benzthiazoles or their pharmaceutically acceptable acid salts, a method of synthesis, an antiarrhythmic composition of the third-class and a method of its preparing

Country Status (34)

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US (1) US5691354A (en)
EP (1) EP0701556B1 (en)
JP (1) JP3498145B2 (en)
KR (1) KR100337984B1 (en)
CN (1) CN1039120C (en)
AT (1) ATE159254T1 (en)
AU (1) AU678841B2 (en)
BG (1) BG62968B1 (en)
BR (1) BR9406765A (en)
CA (1) CA2163018A1 (en)
CZ (1) CZ285766B6 (en)
DE (1) DE69406284T2 (en)
DK (1) DK0701556T3 (en)
ES (1) ES2108471T3 (en)
FI (1) FI955916A (en)
GR (1) GR3025805T3 (en)
HU (1) HU221620B1 (en)
IL (1) IL109975A (en)
LV (1) LV11544B (en)
MY (1) MY111222A (en)
NO (1) NO305123B1 (en)
NZ (1) NZ268575A (en)
OA (1) OA10201A (en)
PH (1) PH31126A (en)
PL (1) PL176775B1 (en)
RO (1) RO115523B1 (en)
RU (1) RU2122546C1 (en)
SG (1) SG48821A1 (en)
SI (1) SI9420036A (en)
SK (1) SK281175B6 (en)
TW (1) TW282469B (en)
UA (1) UA41936C2 (en)
WO (1) WO1994029305A1 (en)
ZA (1) ZA944106B (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2398388A1 (en) * 2000-01-20 2001-07-26 Koji Kato Novel piperidine compound and pharmaceutical thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5010198A (en) * 1984-12-03 1991-04-23 Janssen Pharmaceutica N.V. Intermediates for the synthesis of benzoxazol- and benzothiazolamine derivatives, useful as anti-anoxic agents
CA1260474A (en) * 1984-12-03 1989-09-26 Raymond A. Stokbroekx Benzoxazol- and benzothiazolamine derivatives
US4861785A (en) * 1984-12-03 1989-08-29 Janssen Pharmaceutica N.V. Benzoxazol-and benzothiazolamine derivatives, useful as anti-anoxic agents
KR930005004B1 (en) * 1985-04-15 1993-06-11 쟈안센 파아마슈우티카 엔. 부이. Process for preparing substituted n-|(4-piperidinyl) alkyl¨ bicycle condensed oxazole and thiazolamines
US4749702A (en) * 1985-04-15 1988-06-07 Janssen Pharmaceutica N. V. Antidepressive substituted N-[(4-piperidinyl)alkyl] bicyclic condensed oxazol- and thiazolamines
ZW1992A1 (en) * 1991-02-25 1993-09-22 Janssen Pharmaceutica Nv 4-/(2-benzotiazolyl)methylamino/-b-/(3,4-difluorephenoxy)methyl/-1-piperidine ethanol

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