RU96100074A - AGONISTS / ANTAGONISTS ESTROGEN, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT OF DISEASES - Google Patents

AGONISTS / ANTAGONISTS ESTROGEN, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT OF DISEASES

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RU96100074A
RU96100074A RU96100074/04A RU96100074A RU96100074A RU 96100074 A RU96100074 A RU 96100074A RU 96100074/04 A RU96100074/04 A RU 96100074/04A RU 96100074 A RU96100074 A RU 96100074A RU 96100074 A RU96100074 A RU 96100074A
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compound according
effective amount
phenyl
mammal
treatment
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RU96100074/04A
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RU2130454C1 (en
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О.Камерон Кимберли
А.Дасилва Жардине Поль
Л.Розати Роберт
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Пфайзер Инк.
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Claims (1)

1. Соединение общей формулы
Figure 00000001

где А - СН2 или NR;
В, D и Е независимо - СН или N;
Y обозначает фенил, необязательно замещенный 1 - 3 заместителями, независимо выбранными из R4; нафил, необязательно замещенный 1 - 3 заместителями, независимо выбранными из R4; С3 - С8-циклоалкил, необязательно замещенный 1 - 2 заместителями, независимо выбранными из R4; С3 - С8-циклоалкенил, необязательно замещенный 1-2 заместителями, независимо выбранными из R4; пятичленный гетероцикл, содержащий до двух гетероатомов, выбранных из группы, состоящий из -О-, -NR2 - и - S(O)n -, необязательно замещенный 1 - 3 заместителями, независимо выбранными из R4; шестичленный гетероцикл, содержащий до двух гетероатомов, выбранных из группы, состоящей из -О-, -NR2- и -S(O)n-, необязательно замещенный 1 - 3 заместителями, независимо выбранными из R4, или бициклическая кольцевая система, содержащая пяти- или шестичленный гетероцикл сконденсированный с фенильным кольцом, где гетероцикл содержит до двух гетероатомов, выбранных из группы, включающей -О-, -NR2- и -S(O)n- , необязательно замещенная 1 - 3 заместителями, независимо выбранными из R4;
Z1 - -(CH2)p W(CH2)q-, -O(CH2)p CR5R6-, -O(CH2)pW(CH2)q, -OCH R2CHR3 - или -SCHR2CHR3-;
G - NR7 R8,
Figure 00000002

где n = 0,1 или 2;
m = 1,2 или 3;
Z2 - NH-, -O-, -S- или -CH2-, необязательно сконденсированный по смежным углеродным атомам с одним или двумя фенильными кольцами и необязательно независимо замещенный по углероду 1 - 3 заместителями и необязательно независимо по азоту химически приемлемым заместителем, выбранным из R4, или бициклический амин, содержащий 5 - 12 атомов углерода, либо связанный мостиковой связью, либо конденсированный и необязательно замещенный 1 - 3 заместителями, независимо выбранными из R4;
или Z1 и G в комбинации могут представлять
Figure 00000003

W - -CH2-, -CH = CH-, -O-, -NR2-, -S(O)n-,
Figure 00000004

-CR2(OH)-, -CONR2-, -NR2CO-,
Figure 00000005

или -C≡C- ;
R - водород или С1 - С6 - алкил;
R2 и R3 независимо - водород или С1 - С4 алкил;
R4 - водород, галоген, С1 - С6 - алкил, С1 - С4 - алкокси, С1 - С4 - ацилокси, С1 - С4 - алкилтио, С1 - С4 - алкилсульфинил, С1 - С4 - алкилсульфонил, гидрокси(С1 - С4)алкил, арил (С1 - С4)алкил, -СО2Н, -CN, -СОNНОR, -SO2NHR, -NH2, С1 - С4-алкиламино, С1 - С4 - диалкиламино, -NHSO2R, - NO2 -арил или -ОН,
R5 и R6 независимо С1 - С8 - алкил или вместе образуют С3 - С1 0-карбоциклическое кольцо,
R7 и R8 независимо - фенил, (в) С3 - С1 0-карбоцикл, насыщенный или ненасыщенный, C3 - С1 0 - гетероцикл, содержащий до двух гетероатомов, выбранных из -О-, -N- и S-, H, С1 - С6 - алкил или образуют 3 - 8 - членный азот, содержащий цикл с R5 или R6;
R7 и R8 в форме либо линейной, либо циклической, могут необязательно содержать до трех заместителей, независимо выбранных из С1 - С6-алкила, галогена, алкокси-, гидрокси- и карбоксигруппы, цикл, образованный R7 и R8, может необязательно быть сконденсирован с фенильным кольцом;
e = 0, 1 или 2;
m = 1, 2 или 3;
n = 0, 1 или 2;
p = 0, 1, 2 или 3;
q = 0, 1, 2 или 3;
и их оптические и геометрические изомеры, а также их нетоксичные фармакологически приемлемые соли кислотного присоединения, N - окиси, эфиры и четвертичные аммониевые соли.1. The compound of the General formula
Figure 00000001

where a is CH 2 or NR;
B, D and E are independently CH or N;
Y is phenyl, optionally substituted with 1 to 3 substituents independently selected from R 4 ; nafil, optionally substituted with 1 to 3 substituents independently selected from R 4 ; C 3 - C 8 -cycloalkyl, optionally substituted with 1 to 2 substituents independently selected from R 4 ; C 3 - C 8 -cycloalkenyl, optionally substituted with 1-2 substituents independently selected from R 4 ; a five-membered heterocycle containing up to two heteroatoms selected from the group consisting of -O-, -NR 2 - and - S (O) n -, optionally substituted with 1 to 3 substituents independently selected from R 4 ; a six-membered heterocycle containing up to two heteroatoms selected from the group consisting of —O—, —NR 2 - and —S (O) n -, optionally substituted with 1 to 3 substituents independently selected from R 4 , or a bicyclic ring system containing a five- or six-membered heterocycle condensed with a phenyl ring, where the heterocycle contains up to two heteroatoms selected from the group consisting of -O-, -NR 2 - and -S (O) n -, optionally substituted with 1 to 3 substituents independently selected from R 4 ;
Z 1 - - (CH 2 ) p W (CH 2 ) q -, -O (CH 2 ) p CR 5 R 6 -, -O (CH 2 ) p W (CH 2 ) q , -OCH R 2 CHR 3 - or -SCHR 2 CHR 3 -;
G - NR 7 R 8 ,
Figure 00000002

where n = 0.1 or 2;
m = 1.2 or 3;
Z 2 - NH-, -O-, -S-, or -CH 2 -, optionally condensed on adjacent carbon atoms with one or two phenyl rings and optionally independently substituted on carbon with 1 to 3 substituents and optionally independently nitrogen with a chemically acceptable substituent, selected from R 4 , or a bicyclic amine containing 5 to 12 carbon atoms, either bridged or fused and optionally substituted with 1 to 3 substituents independently selected from R 4 ;
or Z 1 and G in combination can represent
Figure 00000003

W - -CH 2 -, -CH = CH-, -O-, -NR 2 -, -S (O) n -,
Figure 00000004

-CR 2 (OH) -, -CONR 2 -, -NR 2 CO-,
Figure 00000005

or -C≡C-;
R is hydrogen or C 1 - C 6 - alkyl;
R 2 and R 3 are independently hydrogen or C 1 - C 4 alkyl;
R 4 is hydrogen, halogen, C 1 - C 6 - alkyl, C 1 - C 4 - alkoxy, C 1 - C 4 - acyloxy, C 1 - C 4 - alkylthio, C 1 - C 4 - alkylsulfinyl, C 1 - C 4 - alkylsulfonyl, hydroxy (C 1 - C 4 ) alkyl, aryl (C 1 - C 4 ) alkyl, -CO 2 H, -CN, -CONHOR, -SO 2 NHR, -NH 2 , C 1 - C 4 -alkylamino, C 1 - C 4 - dialkylamino, -NHSO 2 R, - NO 2 -aryl or -OH,
R 5 and R 6 are independently C 1 - C 8 - alkyl or together form a C 3 - C 1 0 carbocyclic ring,
R 7 and R 8 are independently phenyl, (c) C 3 - C 1 0 -carbocycle, saturated or unsaturated, C 3 - C 1 0 is a heterocycle containing up to two heteroatoms selected from -O-, -N- and S -, H, C 1 - C 6 - alkyl or form 3 to 8 - membered nitrogen containing a cycle with R 5 or R 6 ;
R 7 and R 8 in the form of either linear or cyclic, may optionally contain up to three substituents independently selected from C 1 -C 6 -alkyl, halogen, alkoxy, hydroxy and carboxy, the cycle formed by R 7 and R 8 , may optionally be condensed with a phenyl ring;
e = 0, 1 or 2;
m = 1, 2 or 3;
n = 0, 1 or 2;
p = 0, 1, 2 or 3;
q = 0, 1, 2 or 3;
and their optical and geometric isomers, as well as their non-toxic pharmacologically acceptable acid addition salts, N-oxides, ethers, and quaternary ammonium salts. 2. Соединение по п.1 общей формулы
Figure 00000006

3. Соединение по п.2, в котором G представляет
Figure 00000007

Figure 00000008

4. Соединение по п.3, в котором R4 - H, OH, F или Cl.2. The compound according to claim 1 of the general formula
Figure 00000006

3. The compound according to claim 2, in which G represents
Figure 00000007

Figure 00000008

4. The compound according to claim 3, in which R 4 is H, OH, F or Cl. 5. Соединение по п.4, в котором В и Е - CH. 5. The compound according to claim 4, in which B and E - CH. 6. Соединение по п.4, в котором В обозначает N и Е - CH. 6. The compound according to claim 4, in which B represents N and E is CH. 7. Соединение по п.4, в котором В обозначает СН и Е - N. 7. The compound according to claim 4, in which B represents CH and E - N. 8. Соединение по п.1, представляющее собой цис-6-(4-фтор-фенил)-5-[4-(2 пиперидин-1-ил-этокси)-фенил]-5,6,7,8 тетрагидронафталин-2-ол. 8. The compound according to claim 1, which is cis-6- (4-fluoro-phenyl) -5- [4- (2 piperidin-1-yl-ethoxy) -phenyl] -5,6,7,8 tetrahydronaphthalene 2-ol. 9. Соединение по п. 1, представляющее собой (-) цис-6-фенил-5-[4-(2-пирролидин-1-ил-этокси)-фенил]-5,6,7,8 тетрагидронафталин-2-ол. 9. The compound according to claim 1, which is (-) cis-6-phenyl-5- [4- (2-pyrrolidin-1-yl-ethoxy) -phenyl] -5,6,7,8 tetrahydronaphthalen-2- ol 10. Соединение по п.1, представляющее собой цис-6-фенил-5-[4-(2-пирролидин-1-ил-этокси)-фенил]-5,6,7,8-тетрагидронафталин-2-ол. 10. The compound according to claim 1, which is cis-6-phenyl-5- [4- (2-pyrrolidin-1-yl-ethoxy) -phenyl] -5,6,7,8-tetrahydronaphthalen-2-ol. 11. Соединение по п. 1, представляющее собой цис- 1-[6'-пирролидиноэтокси-3'-пиридил]-2-фенил-6-гидрокси-1,2,3,4-тетрагидронафталин. 11. The compound according to claim 1, which is cis-1- [6'-pyrrolidinoethoxy-3'-pyridyl] -2-phenyl-6-hydroxy-1,2,3,4-tetrahydronaphthalene. 12. Соединение по п.1, представляющее собой 1-(4'-пирролидиноэтоксифенил)-2-(4'-фторфенил)-6 гидрокси-1,2,3,4-тетрагидроизохинолин. 12. The compound according to claim 1, which is 1- (4'-pyrrolidinoethoxyphenyl) -2- (4'-fluorophenyl) -6 hydroxy-1,2,3,4-tetrahydroisoquinoline. 13. Соединение по п.1, представляющее собой цис-6-(4'-гидроксифенил)-5-[4-(2-пиперидин-1-ил-этокси)-фенил]-5,6,7,8 тетрагидронафталин-2-ол. 13. The compound according to claim 1, which represents cis-6- (4'-hydroxyphenyl) -5- [4- (2-piperidin-1-yl-ethoxy) -phenyl] -5,6,7,8 tetrahydronaphthalene 2-ol. 14. Соединение по п.1, представляющее собой 1-(4'-пирролидиноэтоксифенил)-2-фенил-6-гидрокси-1,2,3,4-тетрагидроизохинолин. 14. The compound according to claim 1, which is 1- (4'-pyrrolidinoethoxyphenyl) -2-phenyl-6-hydroxy-1,2,3,4-tetrahydroisoquinoline. 15. Фармацевтическая композиция, содержащая эффективное количество соединения по п.1 и фармацевтически приемлемый носитель. 15. A pharmaceutical composition comprising an effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier. 16. Фармацевтическая композиция по п.15 для лечения или профилактики остеопороза, содержащая эффективное количество соединения по п.1 и фармацевтически приемлемый носитель. 16. The pharmaceutical composition according to p. 15 for the treatment or prevention of osteoporosis, containing an effective amount of the compound according to claim 1 and a pharmaceutically acceptable carrier. 17. Фармацевтическая композиция по п.15 для лечения или предупреждения сердечно-сосудистого заболевания или (гипер)холестеринемии, содержащая эффективное количество соединения по п.1 и фармацевтически приемлемый носитель. 17. The pharmaceutical composition according to claim 15 for treating or preventing a cardiovascular disease or (hyper) cholesterolemia, comprising an effective amount of the compound according to claim 1 and a pharmaceutically acceptable carrier. 18. Фармацевтическая композиция по п.15 для лечения или предупреждения заболевания простаты, содержащая эффективное количество соединения по п.1, фармацевтически приемлемый носитель. 18. The pharmaceutical composition according to p. 15 for the treatment or prevention of prostate disease, containing an effective amount of a compound according to claim 1, a pharmaceutically acceptable carrier. 19. Фармацевтическая композиция по п.15 для снижения уровня холестерина сыворотки, содержащая эффективное количество соединения по п.1 и фармацевтически приемлемый носитель. 19. The pharmaceutical composition according to claim 15 for lowering serum cholesterol, comprising an effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier. 20. Фармацевтическая композиция по п.15 для лечения или предупреждения ожирения, содержащая эффективное количество соединения по п.1 и фармацевтически приемлемый носитель. 20. The pharmaceutical composition according to claim 15 for treating or preventing obesity, comprising an effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier. 21. Фармацевтическая композиция по п.15 для лечения или предупреждения эндометриоза, включающая эффективное количество соединения по п.1 и фармацевтически приемлемый носитель. 21. The pharmaceutical composition according to claim 15 for the treatment or prevention of endometriosis, comprising an effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier. 22. Фармацевтическая композиция по п.15 для лечения или предупреждения рака молочной железы, включающая эффективное количество соединения по п.1 и фармацевтически приемлемого носителя. 22. The pharmaceutical composition according to claim 15 for treating or preventing breast cancer, comprising an effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier. 23. Способ лечения или предупреждения остеопороза у млекопитающих, который включает введение нуждающимся в таком лечении млекопитающим эффективного количества соединения по п.1. 23. A method of treating or preventing osteoporosis in a mammal, which comprises administering to an mammal in need of such treatment an effective amount of a compound according to claim 1. 24. Способ лечения или предупреждения сердечно-сусудистых заболеваний или (гипер)липемии у млекопитающих, который включает введение млекопитающему, нуждающемуся в таком лечении, эффективного количества соединения по п. 1. 24. A method of treating or preventing cardiovascular diseases or (hyper) lipemia in mammals, which comprises administering to a mammal in need of such treatment an effective amount of the compound according to claim 1. 25. Способ лечения или предупреждения заболевания простаты у млекопитающего, включающий введение млекопитающему, нуждающемуся в таком лечении, эффективнго количества соединения по п.1. 25. A method of treating or preventing a prostate disease in a mammal, comprising administering to a mammal in need of such treatment an effective amount of a compound according to claim 1. 26. Способ снижения уровня холестерина сыворотки у млекопитающих, включающий введение млекопитающему, наждающему в такой обработке, эффективного количества соединения по п.1. 26. A method of reducing serum cholesterol in a mammal, comprising administering to a mammal, in such a treatment, an effective amount of the compound according to claim 1. 27. Способ лечения или предупреждения ожирения у млекопитающего, включающий введение млекопитающему, нуждающемуся в таком лечении, эффективного количества соединения по п.1. 27. A method of treating or preventing obesity in a mammal, comprising administering to a mammal in need of such treatment an effective amount of the compound according to claim 1. 28. Способ лечения или предупреждения рака молочной железы у млекопитающего, включающий введение млекопитающему нуждающемуся в таком лечении, эффективного количества соединения по п.1. 28. A method of treating or preventing breast cancer in a mammal, comprising administering to a mammal in need of such treatment an effective amount of the compound according to claim 1. 29. Способ лечения или предупреждения эндометриоза у млекопитающего, включающий введение млекопитающему, нуждающемуся в таком лечении, эффективного количества соединения по п.1. 29. A method of treating or preventing endometriosis in a mammal, comprising administering to a mammal in need of such treatment an effective amount of the compound according to claim 1. 30. Промежуточное соединение, пригодное для использования в получении соединения по п.1, представляющее собой 1-{2-[4-(6-метокси-3,4-дигидронафталин-1-ил)фенокси]-этил}-прирролидин или 1-{2-[4-(2-бром-6-метокси-3,4-дигидронафталин-1-ил)-фенокси]-этил}пир- ролидин. 30. Intermediate compound suitable for use in obtaining a compound according to claim 1, which is 1- {2- [4- (6-methoxy-3,4-dihydronaphthalen-1-yl) phenoxy] ethyl} -prirrolidine or 1 - {2- [4- (2-bromo-6-methoxy-3,4-dihydronaphthalen-1-yl) -phenoxy] -ethyl} pyrrolidine.
RU96100074A 1995-01-09 1996-01-05 Compound, pharmaceutical composition, method of treatment and prophylaxis of endometritis, intermediate compound RU2130454C1 (en)

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US08/369,954 US5552412A (en) 1995-01-09 1995-01-09 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis

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