RU96124822A - Cross-linked polymers for the removal of bile salts from the human body - Google Patents

Cross-linked polymers for the removal of bile salts from the human body

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Publication number
RU96124822A
RU96124822A RU96124822/04A RU96124822A RU96124822A RU 96124822 A RU96124822 A RU 96124822A RU 96124822/04 A RU96124822/04 A RU 96124822/04A RU 96124822 A RU96124822 A RU 96124822A RU 96124822 A RU96124822 A RU 96124822A
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Russia
Prior art keywords
alkyl
ion
alkyl group
cross
linked polymers
Prior art date
Application number
RU96124822/04A
Other languages
Russian (ru)
Other versions
RU2146266C1 (en
Inventor
В. Харри Мэндевилл III
Стефен Рэндалл Хольмс-Фарли
Original Assignee
Джелтекс Фармасьютикэлс, Инк.
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Priority claimed from US08/258,477 external-priority patent/US5624963A/en
Application filed by Джелтекс Фармасьютикэлс, Инк. filed Critical Джелтекс Фармасьютикэлс, Инк.
Publication of RU96124822A publication Critical patent/RU96124822A/en
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Publication of RU2146266C1 publication Critical patent/RU2146266C1/en

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Claims (6)

1. Способ выведения желчных камней из организма человека, основанный на использовании ионообменных смол, отличающийся тем, что в качестве ионообменной смолы используют терапевтически эффективное количество продукта реакции одного или нескольких поперечно сшитых полимеров, имеющих повторяющееся структурное звено общей формулы
Figure 00000001

или солей и сополимеров на их основе,
где n - целое сило;
R1 - H или C1 - C8 алкильная группа;
M -
Figure 00000002

или -Z-R2; Z - O, NR3, S или (CH2)m; m = 0 - 10; R3 - H или C1 - C8 алкильная группа; R2 -
Figure 00000003

Figure 00000004

где p = 0 - 10;
R4, R5, R6 - каждый, независимо, H или C1 - C8 алкильная или арильная группа,
и по меньшей мере одного алкилирующего агента.1. The method of removing gallstones from the human body, based on the use of ion-exchange resins, characterized in that as the ion-exchange resin using a therapeutically effective amount of the reaction product of one or more cross-linked polymers having a repeating structural unit of the General formula
Figure 00000001

or salts and copolymers based on them,
where n is a whole force;
R 1 is H or C 1 is a C 8 alkyl group;
M -
Figure 00000002

or -ZR 2 ; Z is O, NR 3 , S or (CH 2 ) m ; m is 0-10; R 3 is H or C 1 is a C 8 alkyl group; R 2 -
Figure 00000003

Figure 00000004

where p = 0 - 10;
R 4 , R 5 , R 6 each, independently, H or C 1 - C 8 alkyl or aryl group,
and at least one alkylating agent. 2. Способ по п.1, отличающийся тем, что используют алкилирующий агент общей формулы RX, где R - C1 - C20 алкил, C1 - C20 гидроксиалкил, C1 - C20 аралкил, C1 - C20 алкиламмоний, или C1 - C20 алкиламидная группа, X - одна или более электрофильных групп.2. The method according to claim 1, characterized in that an alkylating agent of the general formula RX is used, where R is C 1 - C 20 alkyl, C 1 - C 20 hydroxyalkyl, C 1 - C 20 aralkyl, C 1 - C 20 alkylammonium, or a C 1 - C 20 alkylamide group, X is one or more electrophilic groups. 3. Способ по п. 1, отличающийся тем, что используют полимер, взаимодействующий по меньшей мере с двумя алкилирующими агентами, причем один из алкилирующих агентов имеет формулу RX, где R является C1 - C20 алкильной группой и X - одна или несколько электрофильных групп, а другой алкилирующий агент имеет формулу R'X, где R' является C1 - C20 алкил аммониевой группой и X - одна или несколько электрофильных групп.3. The method according to p. 1, characterized in that they use a polymer that interacts with at least two alkylating agents, one of the alkylating agents having the formula RX, where R is a C 1 - C 20 alkyl group and X is one or more electrophilic groups, and the other alkylating agent has the formula R'X, where R 'is a C 1 - C 20 alkyl ammonium group and X is one or more electrophilic groups. 4. Терапевтическая композиция, используемая для приготовления препарата для выведения желчных камней на основе ионообменных смол, отличающаяся тем, что в качестве ионообменной смолы она содержит терапевтически эффективное количество продукта реакции одного или более поперечно сшитых полимеров, содержащих повторяющееся структурное звено общей формулы
Figure 00000005

или солей и сополимеров на их основе,
где n - целое число; R1 - H или C1 - C8 алкильная группа;
M -
Figure 00000006

или -Z-R2; Z - O, NR3, S или (CH2)m; m = 0 - 10; R3 - H или C1 - C8 алкильная группа; R2 -
Figure 00000007

Figure 00000008

где p = 0 - 10;
R4, R5, R6 каждый, независимо, H или C1 - C8 алкильная или арильная группа,
и по меньшей мере одного алкилирующего агента на фармацевтически приемлемом носителе.4. The therapeutic composition used to prepare a preparation for the removal of gallstones based on ion-exchange resins, characterized in that it contains a therapeutically effective amount of a reaction product of one or more cross-linked polymers containing a repeating structural unit of the general formula
Figure 00000005

or salts and copolymers based on them,
where n is an integer; R 1 is H or C 1 is a C 8 alkyl group;
M -
Figure 00000006

or -ZR 2 ; Z is O, NR 3 , S or (CH 2 ) m ; m is 0-10; R 3 is H or C 1 is a C 8 alkyl group; R 2 -
Figure 00000007

Figure 00000008

where p = 0 - 10;
R 4 , R 5 , R 6 each, independently, H or C 1 - C 8 alkyl or aryl group,
and at least one alkylating agent on a pharmaceutically acceptable carrier. 5. Полимерная композиция, используемая для приготовления препарата для выведения желчных камней на основе ионообменных смол, отличающаяся тем, что в качестве ионообменной смолы она содержит терапевтически эффективное количество продукта реакции одного или более поперечно сшитых полимеров, содержащих повторяющееся структурное звено общей формулы
Figure 00000009

или солей и сополимеров на их основе,
где n - целое число; R1 - H или C1 - C8 алкильная группа;
M - это
Figure 00000010

или -Z-R2; Z - O, NR3, S или (CH2)m; m = 0 - 10; R3 - H или C1 - C8 алкильная группа; R2 -
Figure 00000011

Figure 00000012

где p = 0 - 10;
R4, R5, R6 - каждый, независимо, H или C1 - C8 алкильная или арильная группа,
и по меньшей мере одного алкилирующего агента.5. The polymer composition used to prepare the preparation for the removal of gallstones based on ion-exchange resins, characterized in that as the ion-exchange resin it contains a therapeutically effective amount of a reaction product of one or more cross-linked polymers containing a repeating structural unit of the general formula
Figure 00000009

or salts and copolymers based on them,
where n is an integer; R 1 is H or C 1 is a C 8 alkyl group;
M is
Figure 00000010

or -ZR 2 ; Z is O, NR 3 , S or (CH 2 ) m ; m is 0-10; R 3 is H or C 1 is a C 8 alkyl group; R 2 -
Figure 00000011

Figure 00000012

where p = 0 - 10;
R 4 , R 5 , R 6 each, independently, H or C 1 - C 8 alkyl or aryl group,
and at least one alkylating agent. 6. Полимерная композиция, используемая для приготовления препарата для выведения желчных камней на основе ионообменных смол, отличающаяся тем, что в качестве ионообменной смолы она содержит терапевтически эффективное количество одного или более поперечно сшитых полимеров, содержащих повторяющееся структурное звено общей формулы
Figure 00000013

или сополимер на их основе,
где n - целое число; R - H или C1 - C8 алкильная группа;
L - -NH-, или
Figure 00000014

G -
Figure 00000015

R2, R3, R4 каждый, независимо, H или C1 - C8 алкильная или арильная группа.6. The polymer composition used to prepare the preparation for the removal of gallstones based on ion-exchange resins, characterized in that as the ion-exchange resin it contains a therapeutically effective amount of one or more cross-linked polymers containing a repeating structural unit of the general formula
Figure 00000013

or a copolymer based on them,
where n is an integer; R is H or C 1 -C 8 alkyl group;
L is -NH-, or
Figure 00000014

G -
Figure 00000015

R 2 , R 3 , R 4 each, independently, H or C 1 - C 8 alkyl or aryl group.
RU96124822A 1994-06-10 1995-05-24 Method of sequestering bile acid salts from body, therapeutic and polymer compositions for implementation of this method RU2146266C1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/258,477 US5624963A (en) 1993-06-02 1994-06-10 Process for removing bile salts from a patient and compositions therefor
US08/258,477 1994-06-10
PCT/US1995/006542 WO1995034588A1 (en) 1994-06-10 1995-05-24 Cross-linked polymers for removing bile salts from a patient

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RU96124822A true RU96124822A (en) 1999-04-10
RU2146266C1 RU2146266C1 (en) 2000-03-10

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EP (1) EP0764177B1 (en)
JP (1) JPH10501264A (en)
CN (1) CN1136855C (en)
AT (1) ATE205508T1 (en)
AU (1) AU694777B2 (en)
CA (1) CA2192592C (en)
DE (1) DE69522687T2 (en)
DK (1) DK0764177T3 (en)
ES (1) ES2164152T3 (en)
HK (1) HK1001611A1 (en)
MX (1) MX9606172A (en)
NZ (1) NZ285979A (en)
PT (1) PT764177E (en)
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WO (1) WO1995034588A1 (en)

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