RU2000113729A - HETEROCYCLIC COMPOUNDS FOR INHIBITING GASTRIC ACID SECRET, METHODS FOR PRODUCING THEM AND THEIR PHARMACEUTICAL COMPOSITIONS - Google Patents

HETEROCYCLIC COMPOUNDS FOR INHIBITING GASTRIC ACID SECRET, METHODS FOR PRODUCING THEM AND THEIR PHARMACEUTICAL COMPOSITIONS

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Publication number
RU2000113729A
RU2000113729A RU2000113729/04A RU2000113729A RU2000113729A RU 2000113729 A RU2000113729 A RU 2000113729A RU 2000113729/04 A RU2000113729/04 A RU 2000113729/04A RU 2000113729 A RU2000113729 A RU 2000113729A RU 2000113729 A RU2000113729 A RU 2000113729A
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Russia
Prior art keywords
compound according
pharmaceutically acceptable
acceptable salt
paragraphs
alkyl
Prior art date
Application number
RU2000113729/04A
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Russian (ru)
Other versions
RU2241000C2 (en
Inventor
Косрат АМИН
Микаэль Дальстрем
Петер Нордберг
Ингемар Старке
Original Assignee
Астразенека Аб
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Publication date
Priority claimed from SE9704404A external-priority patent/SE9704404D0/en
Application filed by Астразенека Аб filed Critical Астразенека Аб
Publication of RU2000113729A publication Critical patent/RU2000113729A/en
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Publication of RU2241000C2 publication Critical patent/RU2241000C2/en

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Claims (23)

1. Соединение формулы I
Figure 00000001

или его фармацевтически приемлемая соль,
в котором R1 представляет собой С1-С6алкил;
R2 представляет собой С1-С6алкил;
R3 представляет собой Н или галоген; и
Figure 00000002

представляет собой замещенный гетероцикл, выбранный из
Figure 00000003

Figure 00000004

Figure 00000005

Figure 00000006

Figure 00000007

или
Figure 00000008

где R4 представляет собой Н, СН3, CH2OH или CH2CN;
R5 представляет собой Н или С1-С6алкил;
R6 представляет собой Н, С1-С6алкил, арил, арилалкил, содержащий 1-2 атома углерода в алкильной части, С2-С6алкенил, галогено(С2-С6алкенил), С2-С6алкинил, С3-С7циклоалкил или галогено(С1-С6алкил);
R7 представляет собой Н, галоген, С1-С6алкил, C1-С6алкилтио или тиоциано;
n = 0 или 1;
Х представляет собой NH или О.1. The compound of formula I
Figure 00000001

or a pharmaceutically acceptable salt thereof,
in which R 1 represents a C 1 -C 6 alkyl;
R 2 represents C 1 -C 6 alkyl;
R 3 represents H or halogen; and
Figure 00000002

represents a substituted heterocycle selected from
Figure 00000003

Figure 00000004

Figure 00000005

Figure 00000006

Figure 00000007

or
Figure 00000008

where R 4 represents H, CH 3 , CH 2 OH or CH 2 CN;
R 5 represents H or C 1 -C 6 alkyl;
R 6 represents H, C 1 -C 6 alkyl, aryl, arylalkyl containing 1-2 carbon atoms in the alkyl part, C 2 -C 6 alkenyl, halogen (C 2 -C 6 alkenyl), C 2 -C 6 alkynyl C 3 -C 7 cycloalkyl or halogen (C 1 -C 6 alkyl);
R 7 represents H, halogen, C 1 -C 6 alkyl, C 1 -C 6 alkylthio or thiociano;
n is 0 or 1;
X represents NH or O. 2. Соединение по п. 1, или его фармацевтически приемлемая соль, в котором
Figure 00000009

представляет собой
Figure 00000010

где R4, R5 и Х такие, как определено в п. 1.2. The compound according to claim 1, or its pharmaceutically acceptable salt, in which
Figure 00000009

represents
Figure 00000010

where R 4 , R 5 and X are as defined in paragraph 1. 3. Соединение по п. 1, или его фармацевтически приемлемая соль, в котором
Figure 00000011

представляет собой
Figure 00000012

где R4, R6 и X такие, как определено в п. 1.3. The compound according to claim 1, or its pharmaceutically acceptable salt, in which
Figure 00000011

represents
Figure 00000012

where R 4 , R 6 and X are as defined in paragraph 1. 4. Соединение по п. 1, или его фармацевтически приемлемая соль, в котором
Figure 00000013

представляет собой
Figure 00000014

где R4, R5, R6 и Х такие, как определено в п. 1.4. The compound according to claim 1, or its pharmaceutically acceptable salt, in which
Figure 00000013

represents
Figure 00000014

where R 4 , R 5 , R 6 and X are as defined in claim 1. 5. Соединение по п. 1, или его фармацевтически приемлемая соль, в котором
Figure 00000015

представляет собой
Figure 00000016

где R4, R5, R7 и Х такие, как определено в п. 1.5. The compound according to claim 1, or its pharmaceutically acceptable salt, in which
Figure 00000015

represents
Figure 00000016

where R 4 , R 5 , R 7 and X are as defined in claim 1. 6. Соединение по п. 1, или его фармацевтически приемлемая соль, в котором
Figure 00000017

представляет собой
Figure 00000018

где R4, R5 и Х такие, как определено в п. 1.6. The compound according to claim 1, or its pharmaceutically acceptable salt, in which
Figure 00000017

represents
Figure 00000018

where R 4 , R 5 and X are as defined in paragraph 1. 7. Соединение по п. 1, или его фармацевтически приемлемая соль, в котором
Figure 00000019

представляет собой
Figure 00000020

где R4 и Х такие, как определено в п. 1.7. The compound according to claim 1, or its pharmaceutically acceptable salt, in which
Figure 00000019

represents
Figure 00000020

where R 4 and X are as defined in paragraph 1. 8. Соединение по п. 1, или его фармацевтически приемлемая соль, в котором R1 и R2 независимо представляют собой СН3 или СН2СН3.8. The compound according to claim 1, or its pharmaceutically acceptable salt, in which R 1 and R 2 independently represent CH 3 or CH 2 CH 3 . 9. Соединение по п. 2, которое представляет собой 2,3-диметил-8-(2,6-диметилбензиламино)имидазо[1,2-а] пиразин
Figure 00000021

или его фармацевтически приемлемую соль.9. The compound of claim 2, which is 2,3-dimethyl-8- (2,6-dimethylbenzylamino) imidazo [1,2-a] pyrazine
Figure 00000021

or a pharmaceutically acceptable salt thereof. 10. Соединение по п. 2, которое представляет собой 2,3-диметил-8-(2,6-диметилбензилокси)имидазо[1,2-а] пиразин
Figure 00000022

или его фармацевтически приемлемую соль.10. The compound according to claim 2, which is 2,3-dimethyl-8- (2,6-dimethylbenzyloxy) imidazo [1,2-a] pyrazine
Figure 00000022

or a pharmaceutically acceptable salt thereof. 11. Способ получения соединения по любому из пп. 1-10, при котором соединения общей формулы II
Figure 00000023

где X1 представляет собой ОН или NH2,
подвергают взаимодействию с соединением общей формулы III
Figure 00000024

где R1, R3 и R4 такие, как определено для формулы I;
Y1 представляет собой отщепляемую группу.11. A method of obtaining a compound according to any one of paragraphs. 1-10, in which the compounds of General formula II
Figure 00000023

where X 1 represents OH or NH 2 ,
reacted with a compound of general formula III
Figure 00000024

where R 1 , R 3 and R 4 are as defined for formula I;
Y 1 represents a leaving group. 12. Способ получения соединения по любому из пп. 1-10, при котором соединения общей формулы IV
Figure 00000025

где X2 представляет собой отщепляемую группу,
подвергают взаимодействию с соединением общей формулы V
Figure 00000026

где R1, R3 и R4 такие, как определено для формулы I;
Y2 представляет собой NH2 или ОН.12. A method of obtaining a compound according to any one of paragraphs. 1-10, in which the compounds of General formula IV
Figure 00000025

where X 2 represents a leaving group,
reacted with a compound of general formula V
Figure 00000026

where R 1 , R 3 and R 4 are as defined for formula I;
Y 2 represents NH 2 or OH. 13. Соединение по любому из пп. 1-10 для использования в терапии. 13. The compound according to any one of paragraphs. 1-10 for use in therapy. 14. Фармацевтический препарат, содержащий в качестве активного ингредиента соединение по любому из пп. 1-10 в сочетании с фармацевтически приемлемым разбавителем или носителем. 14. A pharmaceutical preparation containing, as an active ingredient, a compound according to any one of paragraphs. 1-10 in combination with a pharmaceutically acceptable diluent or carrier. 15. Применение соединения по любому из пп. 1-10 для изготовления лекарства для ингибирования секреции желудочной кислоты. 15. The use of compounds according to any one of paragraphs. 1-10 for the manufacture of a medicament for inhibiting the secretion of gastric acid. 16. Применение соединения по любому из пп. 1-10 для изготовления лекарства для лечения желудочно-кишечных воспалительных заболеваний. 16. The use of compounds according to any one of paragraphs. 1-10 for the manufacture of a medicament for the treatment of gastrointestinal inflammatory diseases. 17. Применение соединения по любому из пп. 1-10 для изготовления лекарства для лечения или профилактики состояний, в которые вовлечена инфекция Helicobacter pylori слизистой оболочки желудка человека, причем указанная соль адаптирована для введения в комбинации с по меньшей мере одним противомикробным агентом. 17. The use of compounds according to any one of paragraphs. 1-10 for the manufacture of a medicament for the treatment or prophylaxis of conditions in which a Helicobacter pylori infection of a human gastric mucosa is involved, said salt being adapted for administration in combination with at least one antimicrobial agent. 18. Способ ингибирования секреции желудочной кислоты, при котором млекопитающему, включая человека, нуждающемуся в таком ингибировании, вводят эффективное количество соединения по любому из пп. 1-10. 18. A method of inhibiting the secretion of gastric acid, in which a mammal, including a human in need of such inhibition, is administered an effective amount of a compound according to any one of claims. 1-10. 19. Способ лечения желудочно-кишечных воспалительных заболеваний, при котором млекопитающему, включая человека, нуждающемуся в таком ингибировании, вводят эффективное количество соединения по любому из пп. 1-10. 19. A method of treating gastrointestinal inflammatory diseases, in which a mammal, including a human in need of such inhibition, is administered an effective amount of a compound according to any one of claims. 1-10. 20. Способ лечения или профилактики состояний, в которые вовлечена инфекция Helicobacter pylori слизистой оболочки желудка человека, при котором млекопитающему, включая человека, нуждающемуся в таком лечении, вводят эффективное количество соединения по любому из пп. 1-10, причем указанную соль вводят в комбинации с по меньшей мере одним противомикробным агентом. 20. A method of treating or preventing conditions in which a Helicobacter pylori infection of the human gastric mucosa is involved, in which an effective amount of a compound according to any one of claims is administered to a mammal, including a person in need of such treatment. 1-10, wherein said salt is administered in combination with at least one antimicrobial agent. 21. Фармацевтический препарат для использования в ингибировании секреции желудочной кислоты, в котором активный ингредиент представляет собой соединение по любому из пп. 1-10. 21. A pharmaceutical preparation for use in inhibiting the secretion of gastric acid, in which the active ingredient is a compound according to any one of paragraphs. 1-10. 22. Фармацевтический препарат для использования в лечении желудочно-кишечных воспалительных заболеваний, в котором активный ингредиент представляет собой соединение по любому из пп. 1-10. 22. A pharmaceutical preparation for use in the treatment of gastrointestinal inflammatory diseases, in which the active ingredient is a compound according to any one of paragraphs. 1-10. 23. Фармацевтический препарат для использования в лечении или профилактике состояний, в которые вовлечено инфицирование Helicobacter pylori слизистой оболочки желудка человека, в котором активный ингредиент представляет собой соединение по любому из пп. 1-10 в комбинации с по меньшей мере одним противомикробным агентом. 23. A pharmaceutical preparation for use in the treatment or prophylaxis of conditions involving Helicobacter pylori infection of the human gastric mucosa, in which the active ingredient is a compound according to any one of claims. 1-10 in combination with at least one antimicrobial agent.
RU2000113729/04A 1997-11-28 1998-11-18 Heterocyclic compounds with substituted phenyl group, method for their preparing (variants), pharmaceutical preparations based on thereof and method for inhibition of gastric acid secretion RU2241000C2 (en)

Applications Claiming Priority (2)

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SE9704404A SE9704404D0 (en) 1997-11-28 1997-11-28 New compounds
SE9704404-4 1997-11-28

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