RU99127433A - ERGOLINE DERIVATIVES AND THEIR APPLICATION AS ANTAGONISTS OF SOMATOSTATIN RECEPTORS - Google Patents

ERGOLINE DERIVATIVES AND THEIR APPLICATION AS ANTAGONISTS OF SOMATOSTATIN RECEPTORS

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Publication number
RU99127433A
RU99127433A RU99127433/04A RU99127433A RU99127433A RU 99127433 A RU99127433 A RU 99127433A RU 99127433/04 A RU99127433/04 A RU 99127433/04A RU 99127433 A RU99127433 A RU 99127433A RU 99127433 A RU99127433 A RU 99127433A
Authority
RU
Russia
Prior art keywords
formula
free base
denotes
compound
pharmaceutically acceptable
Prior art date
Application number
RU99127433/04A
Other languages
Russian (ru)
Other versions
RU2191776C2 (en
Inventor
Пауль ПФЭФФЛИ
Петер Нойманн
Роберт Свобода
Петер ШТЮТЦ
Original Assignee
Новартис Аг
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB9711043.1A external-priority patent/GB9711043D0/en
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of RU99127433A publication Critical patent/RU99127433A/en
Application granted granted Critical
Publication of RU2191776C2 publication Critical patent/RU2191776C2/en

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Claims (10)

1. Соединение формулы I
Figure 00000001

где R1 обозначает водород, C1-C4алкил или группу формулы
Figure 00000002

в которой n равно 1-4 и R7 обозначает фтор, хлор, гидрокси, C1-C4алкил или C1-C4алкокси;
R2 обозначает водород, хлор, бром, йод, С1-C4алкил или C1-C4алкилтио,
R3 обозначает водород или C1-C4алкил;
R4 обозначает (I) группу формулы
Figure 00000003

или
Figure 00000004

где R8 обозначает фтор, хлор, нитро или пиано, и R11 обозначает C1-C4алкил или С2-С8алкенил, или (II) группу формулы
Figure 00000005

или
Figure 00000006

где радикалы Х независимо друг от друга обозначают О или S, и R5 и R6 каждый обозначает водород или вместе образуют дополнительную связь
между двумя атомами углерода, к которым они присоединены, в форме свободного основания или в форме кислотно-аддитивной соли.1. The compound of formula I
Figure 00000001

where R 1 denotes hydrogen, C 1 -C 4 alkyl or a group of the formula
Figure 00000002

in which n is 1-4 and R 7 denotes fluorine, chlorine, hydroxy, C 1 -C 4 alkyl or C 1 -C 4 alkoxy;
R 2 denotes hydrogen, chlorine, bromine, iodine, C 1 -C 4 alkyl or C 1 -C 4 alkylthio,
R 3 is hydrogen or C 1 -C 4 alkyl;
R 4 means (I) a group of the formula
Figure 00000003

or
Figure 00000004

where R 8 denotes fluorine, chlorine, nitro or piano, and R 11 denotes C 1 -C 4 alkyl or C 2 -C 8 alkenyl, or (II) a group of the formula
Figure 00000005

or
Figure 00000006

where the radicals X independently of one another denote O or S, and R 5 and R 6 each denotes hydrogen or together form an additional bond
between the two carbon atoms to which they are attached, in the form of a free base or in the form of an acid addition salt. 2. Соединение формулы I по п.1, в котором R4 обозначает группу формулы (г), в форме свободного основания или в форме кислотно-аддитивной соли.2. The compound of formula I according to claim 1, in which R 4 denotes a group of formula (g), in the form of a free base or in the form of an acid addition salt. 3. Соединение формулы I по п.1, в котором R4 обозначает группу формулы (д), в форме свободного основания или в форме кислотно-аддитивной соли.3. The compound of formula I according to claim 1, in which R 4 denotes a group of formula (d), in the form of a free base or in the form of an acid addition salt. 4. Способ получения соединения формулы I по п.1 или его соли, который включает взаимодействие соединения формулы II
Figure 00000007

где R1, R2, R3, R5 и R6 имеют значения, указанные в п.1, а М обозначает Н или щелочной металл, с соединением формулы III
Figure 00000008

где R4 имеет значения, указанные в п.1, и восстановление полученного таким путем соединения формулы I в форме свободного основания или в форме кислотно-аддитивной соли.4. The method of obtaining the compounds of formula I according to claim 1 or its salt, which includes the interaction of the compounds of formula II
Figure 00000007

where R 1 , R 2 , R 3 , R 5 and R 6 have the meanings indicated in paragraph 1, and M denotes H or an alkali metal, with a compound of formula III
Figure 00000008

where R 4 has the meanings indicated in claim 1 and the reduction of the compound of formula I thus obtained in the form of the free base or in the form of an acid addition salt. 5. Соединение по любому из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотно-аддитивной соли, предназначенное для применения в качестве лекарственного средства. 5. The compound according to any one of claims 1 to 3 in the form of a free base or in the form of a pharmaceutically acceptable acid additive salt, intended for use as a medicine. 6. Соединение по любому из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотно-аддитивной соли, предназначенное для лечения депрессии, состояния тревоги, биполярных нарушений и дефицита внимания и нарушений, связанных с гиперактивностью (ДВНГ). 6. The compound according to any one of claims 1 to 3 in the form of a free base or in the form of a pharmaceutically acceptable acid additive salt, intended for the treatment of depression, anxiety, bipolar disorders and attention deficit disorders and disorders associated with hyperactivity (DVNG). 7. Фармацевтическая композиция, содержащая соединение по любому из пп. 1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотно-аддитивной соли в сочетании с фармацевтическим носителем или растворителем. 7. A pharmaceutical composition comprising a compound according to any one of claims. 1-3 in free base form or in the form of a pharmaceutically acceptable acid addition salt in combination with a pharmaceutical carrier or diluent. 8. Применение соединения по любому из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотно-аддитивной соли в качестве лекарственного средства, предназначенного для лечения депрессии, состояния тревоги, биполярных нарушений и ДВНГ. 8. The use of compounds according to any one of claims 1 to 3 in the form of a free base or in the form of a pharmaceutically acceptable acid additive salt as a drug intended for the treatment of depression, anxiety, bipolar disorders and DVNG. 9. Применение соединения по любому из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотно-аддитивной соли для приготовления лекарственного средства, предназначенного для лечения депрессии, состояния тревоги, биполярных нарушений и ДВНГ. 9. The use of compounds according to any one of claims 1 to 3 in the form of a free base or in the form of a pharmaceutically acceptable acid additive salt for the preparation of a medicinal product intended for the treatment of depression, anxiety, bipolar disorders and DVNG. 10. Способ лечения депрессии, состояния тревоги, биполярных нарушений и ДВНГ у пациента, нуждающегося в таком лечении, включающий введение пациенту терапевтически эффективного количества соединения по любому из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотно-аддитивной соли. 10. A method of treating depression, anxiety, bipolar disorder and DVNG in a patient in need of such treatment, comprising administering to the patient a therapeutically effective amount of a compound according to any one of claims 1 to 3 in the form of a free base or in the form of a pharmaceutically acceptable acid addition salt.
RU99127433/04A 1997-05-29 1998-05-27 Ergoline derivatives, method of their synthesis, pharmaceutical composition RU2191776C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9711043.1 1997-05-29
GBGB9711043.1A GB9711043D0 (en) 1997-05-29 1997-05-29 Organic compounds

Publications (2)

Publication Number Publication Date
RU99127433A true RU99127433A (en) 2001-09-10
RU2191776C2 RU2191776C2 (en) 2002-10-27

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Country Status (24)

Country Link
US (1) US6221870B1 (en)
EP (1) EP0986558A2 (en)
JP (1) JP2001527580A (en)
KR (1) KR20010013103A (en)
CN (1) CN1259946A (en)
AR (1) AR012870A1 (en)
AU (1) AU727841B2 (en)
BR (1) BR9809491A (en)
CA (1) CA2288810A1 (en)
CO (1) CO4950561A1 (en)
CZ (1) CZ289466B6 (en)
GB (1) GB9711043D0 (en)
HU (1) HUP0002311A3 (en)
ID (1) ID22916A (en)
IL (1) IL132571A0 (en)
NO (1) NO995482D0 (en)
NZ (1) NZ500386A (en)
PE (1) PE74899A1 (en)
PL (1) PL336502A1 (en)
RU (1) RU2191776C2 (en)
SK (1) SK160899A3 (en)
TR (1) TR199902848T2 (en)
WO (1) WO1998054183A2 (en)
ZA (1) ZA984560B (en)

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KR20140042868A (en) 2011-06-23 2014-04-07 맵 파마슈티컬스, 인코포레이티드 Novel fluoroergoline analogs
EP2793580A4 (en) 2011-12-19 2015-05-20 Map Pharmaceuticals Inc Novel iso-ergoline derivatives
US8946420B2 (en) 2011-12-21 2015-02-03 Map Pharmaceuticals, Inc. Neuromodulatory compounds
US9012640B2 (en) 2012-06-22 2015-04-21 Map Pharmaceuticals, Inc. Cabergoline derivatives
TWI523863B (en) 2012-11-01 2016-03-01 艾普森藥品公司 Somatostatin-dopamine chimeric analogs
WO2014070965A2 (en) 2012-11-01 2014-05-08 Ipsen Pharma S.A.S Somatostatin analogs and dimers thereof
US9657020B2 (en) 2015-01-20 2017-05-23 Xoc Pharmaceuticals, Inc. Ergoline compounds and uses thereof
BR112017015510A2 (en) 2015-01-20 2018-01-30 Xoc Pharmaceuticals Inc compound of formula (i), method of treatment and / or prevention, d2 receptor agonizing method in one individual, d3 receptor antagonizing method in one individual, 5-ht1d receptor agonizing method in one individual, 5-ht1a receptor agonization in one individual, selective 5-ht1d receptor agonizing method instead of 5-ht1b receptor in one individual, 5-ht2c re-receptor selective agonizing method instead of 5-ht2a or 5 receptor -ht2b in one individual, method of 5-ht2c receptor agonization in one individual, method of providing functional antagonist activity at 5-ht2b receptor or 5-ht7 receptor, and, method of providing functional antagonist activity at adrenergic receptors in one individual
CA3064274A1 (en) 2017-06-01 2018-12-06 Xoc Pharmaceuticals, Inc. Ergoline derivatives for use in medicine
JP7099717B2 (en) 2019-09-30 2022-07-12 株式会社理研バイオ Somatostatin receptor

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