RU97112857A - NEW IMMUNOTHERAPEUTIC ARILAMIDES - Google Patents

NEW IMMUNOTHERAPEUTIC ARILAMIDES

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Publication number
RU97112857A
RU97112857A RU97112857/04A RU97112857A RU97112857A RU 97112857 A RU97112857 A RU 97112857A RU 97112857/04 A RU97112857/04 A RU 97112857/04A RU 97112857 A RU97112857 A RU 97112857A RU 97112857 A RU97112857 A RU 97112857A
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Russia
Prior art keywords
carbon atoms
substituted
alkyl containing
compound
phenyl
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RU97112857/04A
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Russian (ru)
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RU2162839C2 (en
Inventor
Мюллер Джордж
Шир Мэри
И.Стирлинг Дэвид
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Селджин Корпорейшн
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Priority claimed from US08/366,618 external-priority patent/US5801195A/en
Application filed by Селджин Корпорейшн filed Critical Селджин Корпорейшн
Publication of RU97112857A publication Critical patent/RU97112857A/en
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Publication of RU2162839C2 publication Critical patent/RU2162839C2/en

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Claims (11)

1. Соединение, имеющее формулу
Figure 00000001

где Аr обозначает (i) линейный, разветвленный или циклический, не замещенный алкил, содержащий от 1 до 12 атомов углерода, (ii) линейный разветвленный или циклический, замещенный алкил, содержащий от 1 до 12 атомов углерода; iii) фенил; iv) фенил, замещенный одним или несколькими заместителями, каждый из которых, независимо, выбран из группы, состоящей из нитро, циано, трифторметила, карбэтокси, карбометокси, карбопропокси, ацетила, карбамоила, ацетокси, карбокси, гидрокси, амино, замещенной амино группы, алкила, содержащего от 1 до 10 атомов углерода, алкокси, содержащего от 1 до 10 атомов углерода, или галогена; v) гетероцикл; или vi) гетероцикл, замещенный одним или несколькими заместителями, каждый из которых, независимо, выбран из нитро, циано, трифторметила, карбэтокси, карбометокси, карбопропокси, ацетила, карбамоила, ацетокси, карбокси, гидрокси, амино, алкила, содержащего от 1 до 10 атомов углерода, алкокси, содержащего от 1 до 10 атомов углерода, или галогена;
R обозначает -Н, алкил, содержащий от 1 до 10 атомов углерода, -СН2ОН, -СН2СН2ОН или-CH2COZ, где Z обозначает алкокси, содержащий от 1 до 10 атомов углерода, бензилокси или NHR1, где R1 обозначает Н или алкил, содержащий от 1 до 10 атомов углерода; и Y обозначает i) фенил или гетероциклическое кольцо,
незамещенное или замещенное одним или несколькими заместителями, каждый из которых, независимо, выбран из группы, состоящей из нитро, циано, трифторметила, карбэтокси, карбометокси, карбопропокси, ацетила, карбамоила, ацетокси, карбокси, гидрокси, амино, алкила, содержащего от 1 до 10 атомов углерода, алкокси, содержащего от 1 до 10 атомов углерода, или галогена; или ii) нафтил.1. The compound having the formula
Figure 00000001

where Ar is (i) linear, branched or cyclic, unsubstituted alkyl containing from 1 to 12 carbon atoms, (ii) linear, branched or cyclic, substituted alkyl containing from 1 to 12 carbon atoms; iii) phenyl; iv) phenyl substituted with one or more substituents, each independently selected from the group consisting of nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, substituted amino groups, alkyl containing from 1 to 10 carbon atoms, alkoxy containing from 1 to 10 carbon atoms, or halogen; v) heterocycle; or vi) a heterocycle substituted with one or more substituents, each independently selected from nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkyl containing from 1 to 10 carbon atoms, alkoxy containing from 1 to 10 carbon atoms, or halogen;
R is —H, alkyl containing from 1 to 10 carbon atoms, —CH 2 OH, —CH 2 CH 2 OH or —CH 2 COZ, where Z is alkoxy containing from 1 to 10 carbon atoms, benzyloxy or NHR 1 , where R 1 denotes H or alkyl containing from 1 to 10 carbon atoms; and Y is i) a phenyl or heterocyclic ring,
unsubstituted or substituted by one or more substituents, each of which is independently selected from the group consisting of nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkyl containing from 1 to 10 carbon atoms, alkoxy containing from 1 to 10 carbon atoms, or halogen; or ii) naphthyl. 2. Соединение по п. 1, в котором Аr обозначает фенил, замещенный двумя метокси группами. 2. The compound of claim 1, wherein Ar is phenyl substituted with two methoxy groups. 3. Соединение по п. 2, в котором R обозначает СН2CO2CH3.3. The compound of claim 2, wherein R is CH 2 CO 2 CH 3 . 4. Соединение по п. 2, в котором Y обозначает фенил. 4. The compound of claim 2, wherein Y is phenyl. 5. Соединение по п. 2, в котором Y обозначает нафтил. 5. The compound of claim 2, wherein Y is naphthyl. 6. Соединение по п. 2, в котором Y обозначает пиридил. 6. The compound of claim 2, wherein Y is pyridyl. 7. Способ снижения уровня ФНОКα у млекопитающих, который включает введение им эффективного количества соединения формулы
Figure 00000002

где Аr обозначает (i) линейный, разветвленный или циклический, не замещенный алкил, содержащий от 1 до 12 атомов углерода, (ii) линейный разветвленный или циклический, замещенный алкил, содержащий от 1 до 12 атомов углерода; iii) фенил; iv) фенил, замещенный одним или несколькими заместителями, каждый из которых, независимо, выбран из группы, состоящей из нитро, циано, трифторметила, карбэтокси, карбометокси, карбопропокси, ацетила, карбамоила, ацетокси, карбокси, гидрокси, амино, замещенной амино группы, алкила, содержащего от 1 до 10 атомов углерода, алкокси, содержащего от 1 до 10 атомов углерода, или галогена; v) гетероцикл; или vi) гетероцикл, замещенный одним или несколькими заместителями, каждый из которых, независимо, выбран из нитро, циано, трифторметила, карбэтокси, карбометокси, карбопропокси, ацетила, карбамоила, ацетокси, карбокси, гидрокси, амино, алкила, содержащего от 1 до 10 атомов углерода, алкокси, содержащего от 1 до 10 атомов углерода, или галогена;
R обозначает -Н, алкил, содержащий от 1 до 10 атомов углерода, -СН2ОН, -СН2СН2ОН или -CH2COZ, где Z обозначает алкокси, содержащий от 1 до 10 атомов углерода, бензилокси или NHR1, где R1 обозначает Н или алкил, содержащий от 1 до 10 атомов углерода; и Y обозначает i) фенил или гетероциклическое кольцо,
незамещенное или замещенное одним или несколькими заместителями, каждый из которых, независимо, выбран из группы, состоящей из группы, состоящей из нитро, циано, трифторметила, карбэтокси, карбометокси, карбопропокси, ацетила, карбамоила, ацетокси, карбокси, гидрокси, амино, алкила, содержащего от 1 до 10 атомов углерода, алкокси, содержащего от 1 до 10 атомов углерода, или галогена; или ii) нафтил.7. A method of reducing the level of TNFα in mammals, which includes the introduction of an effective amount of a compound of the formula
Figure 00000002

where Ar is (i) linear, branched or cyclic, unsubstituted alkyl containing from 1 to 12 carbon atoms, (ii) linear, branched or cyclic, substituted alkyl containing from 1 to 12 carbon atoms; iii) phenyl; iv) phenyl substituted with one or more substituents, each independently selected from the group consisting of nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, substituted amino groups, alkyl containing from 1 to 10 carbon atoms, alkoxy containing from 1 to 10 carbon atoms, or halogen; v) heterocycle; or vi) a heterocycle substituted with one or more substituents, each independently selected from nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkyl containing from 1 to 10 carbon atoms, alkoxy containing from 1 to 10 carbon atoms, or halogen;
R is —H, alkyl containing from 1 to 10 carbon atoms, —CH 2 OH, —CH 2 CH 2 OH or —CH 2 COZ, where Z is alkoxy containing from 1 to 10 carbon atoms, benzyloxy or NHR 1 , where R 1 denotes H or alkyl containing from 1 to 10 carbon atoms; and Y is i) a phenyl or heterocyclic ring,
unsubstituted or substituted by one or more substituents, each independently selected from the group consisting of nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkyl, containing from 1 to 10 carbon atoms, alkoxy containing from 1 to 10 carbon atoms, or halogen; or ii) naphthyl. 8. Способ ингибирования ФНОКα-активируемой репликации ретровирусов у млекопитающих, который включает введение им эффективного количества соединения по п. 1. 8. A method of inhibiting TNFα-activated replication of retroviruses in mammals, which comprises administering to them an effective amount of a compound according to claim 1. 9. Способ ингибирования ФНОКα-активируемой репликации ретровирусов у млекопитающих, который включает введение им эффективного количества соединения по п. 2. 9. A method of inhibiting TNFα-activated replication of retroviruses in mammals, which comprises administering to them an effective amount of a compound according to claim 2. 10. Фармацевтическая композиция, включающая количество соединения по п. 1, эффективное при введении в разовой или многократной дозе для ингибирования ФНОКα. 10. A pharmaceutical composition comprising an amount of a compound according to claim 1, effective when administered in a single or multiple dose to inhibit TNFα. 11. Фармацевтическая композиция, включающая количество соединения по п. 2 эффективное при введении в разовой или многократной дозе для ингибирования ФНОКα. 11. A pharmaceutical composition comprising an amount of a compound according to claim 2 effective when administered in a single or multiple dose to inhibit TNFα.
RU97112857/04A 1994-12-30 1995-11-20 Arylamides, pharmaceutical composition and method of inhibition of tnf2-activated retrovirus replication RU2162839C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/366,618 US5801195A (en) 1994-12-30 1994-12-30 Immunotherapeutic aryl amides
US08/366,618 1994-12-30

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RU97112857A true RU97112857A (en) 1999-06-27
RU2162839C2 RU2162839C2 (en) 2001-02-10

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EP (1) EP0800505B1 (en)
JP (2) JP4052665B2 (en)
KR (1) KR100374088B1 (en)
AT (1) ATE206107T1 (en)
AU (1) AU717100B2 (en)
CA (1) CA2208746C (en)
CZ (1) CZ203797A3 (en)
DE (1) DE69522961T2 (en)
DK (1) DK0800505T3 (en)
ES (1) ES2165927T3 (en)
FI (1) FI972710A (en)
HU (1) HUT77125A (en)
NZ (4) NZ501631A (en)
PL (1) PL182057B1 (en)
PT (1) PT800505E (en)
RU (1) RU2162839C2 (en)
SK (1) SK86797A3 (en)
WO (1) WO1996020915A1 (en)

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