RU95101044A - Применение комбинаций бензотиофена и прогестина для лечения остеопороза - Google Patents
Применение комбинаций бензотиофена и прогестина для лечения остеопорозаInfo
- Publication number
- RU95101044A RU95101044A RU95101044/14A RU95101044A RU95101044A RU 95101044 A RU95101044 A RU 95101044A RU 95101044/14 A RU95101044/14 A RU 95101044/14A RU 95101044 A RU95101044 A RU 95101044A RU 95101044 A RU95101044 A RU 95101044A
- Authority
- RU
- Russia
- Prior art keywords
- compound
- alkoxy
- formula
- progestin
- use according
- Prior art date
Links
- 239000000583 progesterone congener Substances 0.000 title claims 6
- FCEHBMOGCRZNNI-UHFFFAOYSA-N Benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 title 1
- 208000001132 Osteoporosis Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- ICTXHFFSOAJUMG-SLHNCBLASA-N Norethynodrel Chemical compound C1CC(=O)CC2=C1[C@H]1CC[C@](C)([C@](CC3)(O)C#C)[C@@H]3[C@@H]1CC2 ICTXHFFSOAJUMG-SLHNCBLASA-N 0.000 claims 3
- 125000005333 aroyloxy group Chemical class 0.000 claims 2
- 125000004104 aryloxy group Chemical class 0.000 claims 2
- 230000037396 body weight Effects 0.000 claims 2
- 125000005708 carbonyloxy group Chemical class [*:2]OC([*:1])=O 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- 206010065687 Bone loss Diseases 0.000 claims 1
- FRQMUZJSZHZSGN-HBNHAYAOSA-N Medroxyprogesterone Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2CC[C@]2(C)[C@@](O)(C(C)=O)CC[C@H]21 FRQMUZJSZHZSGN-HBNHAYAOSA-N 0.000 claims 1
- 229940053934 Norethindrone Drugs 0.000 claims 1
- VIKNJXKGJWUCNN-XGXHKTLJSA-N Norethisterone Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 VIKNJXKGJWUCNN-XGXHKTLJSA-N 0.000 claims 1
- 230000037182 bone density Effects 0.000 claims 1
- 229910052736 halogen Chemical class 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 229960004616 medroxyprogesterone Drugs 0.000 claims 1
- 229960000993 norethisterone Drugs 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 0 *C1C=C2SC(c3ccc(*)cc3)=C(C(c3ccc(*)cc3)=O)C2=CC1 Chemical compound *C1C=C2SC(c3ccc(*)cc3)=C(C(c3ccc(*)cc3)=O)C2=CC1 0.000 description 1
Claims (6)
1. Применение комбинации:
1) соединение формулы I
где R и R1 независимо - водород, гидроксил, C1 - C6-алкокси, C1 - C6-ацилокси, C1 - C6-алкокси-C2 - C6-ацилокси, R2-замещенный арилокси, R2-замещенный ароилокси, R3-замещенный карбонилокси или галоид;
R2 - C1 - C3-алкил, C1 - C3-алкокси, водород или галоид;
R3 - C1 - C6-алкокси или арилокси;
n = 2, 3 или 4;
p = 4, 5 или 6,
или его фармацевтически приемлемая соль или сольват; вместе с
2) прогестином, выбранным из медроксипрогестерона, норетинодрона или норетинодрела или его фармацевтически приемлемой соли, для сохранения или увеличения плотности кости или ингибирования потери костной массы.
1) соединение формулы I
где R и R1 независимо - водород, гидроксил, C1 - C6-алкокси, C1 - C6-ацилокси, C1 - C6-алкокси-C2 - C6-ацилокси, R2-замещенный арилокси, R2-замещенный ароилокси, R3-замещенный карбонилокси или галоид;
R2 - C1 - C3-алкил, C1 - C3-алкокси, водород или галоид;
R3 - C1 - C6-алкокси или арилокси;
n = 2, 3 или 4;
p = 4, 5 или 6,
или его фармацевтически приемлемая соль или сольват; вместе с
2) прогестином, выбранным из медроксипрогестерона, норетинодрона или норетинодрела или его фармацевтически приемлемой соли, для сохранения или увеличения плотности кости или ингибирования потери костной массы.
2. Применение по п.1, отличающееся тем, что соединением формулы I является соединение, в котором R и R1 выбраны из гидроксила, C1 - C6-ацилокси, C1 - C6-алкокси-C2 - C6-ацилокси, R2 - замещенного ароилокси или R3-замещенного карбонилокси, а выбранным прогестином является норетинодрон или норетинодрел.
3. Применение по п.2, отличающееся тем, что соединением формулы I является соединение, в котором R и R1 - гидроксил, n = 2 и p = 4 или 5, а выбранный прогестин - норетиндрон.
4. Применение по п.3, отличающееся тем, что соединением формулы I является соединение, в котором p = 5.
5. Применение по п.2, отличающееся тем, что R и R1 - гидроксил, n = 2 и p = 5, а выбранный прогестин - норетинодрел.
6. Применение по п.1, отличающееся тем, что количество соединения формулы I составляет от 0,1 до примерно 1000 мг/кг массы тела, а назначаемое количество выбранного прогестина - от примерно 0,01 до 500 мг/кг массы тела.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/189,399 | 1994-01-28 | ||
US08/189,399 US5591753A (en) | 1994-01-28 | 1994-01-28 | Combination treatment for osteoporosis |
Publications (2)
Publication Number | Publication Date |
---|---|
RU95101044A true RU95101044A (ru) | 1997-11-27 |
RU2181048C2 RU2181048C2 (ru) | 2002-04-10 |
Family
ID=22697178
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU95101044/14A RU2181048C2 (ru) | 1994-01-28 | 1995-01-26 | Применение комбинации бензотиофена и прогестина для лечения остеопороза |
Country Status (17)
Country | Link |
---|---|
US (2) | US5591753A (ru) |
EP (1) | EP0665015A3 (ru) |
JP (1) | JPH07267858A (ru) |
KR (1) | KR950031068A (ru) |
CN (1) | CN1084617C (ru) |
AU (1) | AU692811B2 (ru) |
CA (1) | CA2140952A1 (ru) |
CZ (1) | CZ290045B6 (ru) |
HU (1) | HUT72633A (ru) |
IL (1) | IL112455A (ru) |
NO (1) | NO950275L (ru) |
NZ (1) | NZ270386A (ru) |
PH (1) | PH31553A (ru) |
RU (1) | RU2181048C2 (ru) |
TW (1) | TW401296B (ru) |
UA (1) | UA29451C2 (ru) |
ZA (1) | ZA95556B (ru) |
Families Citing this family (30)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5811447A (en) | 1993-01-28 | 1998-09-22 | Neorx Corporation | Therapeutic inhibitor of vascular smooth muscle cells |
US6515009B1 (en) | 1991-09-27 | 2003-02-04 | Neorx Corporation | Therapeutic inhibitor of vascular smooth muscle cells |
USRE38968E1 (en) | 1992-07-28 | 2006-02-07 | Eli Lilly And Company | Methods for inhibiting bone loss using 6-hydroxy-2-(4-hydroxyphenyl)-benzo[b]thien-3-yl-4-[2-(piperidin-1-yl) ethoxyphenylimethanone hydrochloride |
USRE39049E1 (en) | 1992-07-28 | 2006-03-28 | Eli Lilly And Company | Methods for inhibiting bone loss |
TW366342B (en) | 1992-07-28 | 1999-08-11 | Lilly Co Eli | The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss |
US6491938B2 (en) | 1993-05-13 | 2002-12-10 | Neorx Corporation | Therapeutic inhibitor of vascular smooth muscle cells |
US6319914B1 (en) | 1993-11-05 | 2001-11-20 | Apollo Biopharmaceuticals, Inc. | Cytoprotective effect of polycyclic phenolic compounds |
US5478847A (en) | 1994-03-02 | 1995-12-26 | Eli Lilly And Company | Methods of use for inhibiting bone loss and lowering serum cholesterol |
PL181304B1 (pl) * | 1994-07-22 | 2001-07-31 | Lilly Co Eli | Preparat farmaceutyczny do hamowania zmniejszania masy kosci PL PL PL PL PL PL PL PL PL PL |
IL120263A0 (en) * | 1996-02-28 | 1997-06-10 | Pfizer | Combination therapy to prevent bone loss-progesterone and estrogen agonists |
IL120270A0 (en) * | 1996-02-28 | 1997-06-10 | Pfizer | Combination therapy to treat osteoporosis |
IL120265A0 (en) * | 1996-02-28 | 1997-06-10 | Pfizer | Combination therapy to treat osteoporosis - polyphosphonates or progestins and estrogen agonists |
AU6959898A (en) | 1997-04-11 | 1998-11-11 | David J. Grainger | Compounds and therapies for the prevention of vascular and non-vascular pathol ogies |
WO1998048806A1 (en) * | 1997-04-25 | 1998-11-05 | Eli Lilly And Company | Indene compounds having activity as serms |
US6653297B1 (en) * | 1997-07-03 | 2003-11-25 | Medical College Of Hampton Roads | Control of selective estrogen receptor modulators |
US6326392B1 (en) | 1997-11-06 | 2001-12-04 | American Home Products Corporation | Anti-estrogen plus progestin containing oral contraceptives |
US6096781A (en) | 1997-11-14 | 2000-08-01 | Eli Lilly And Company | 2-arylbenzo[B]thiophenes useful for the treatment of estrogen deprivation syndrome |
US6054446A (en) | 1997-12-24 | 2000-04-25 | Sri International | Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use |
AU3171099A (en) * | 1998-04-17 | 1999-11-08 | Senga Pharmaceutical Laboratory Inc. | 1-heteroindene derivatives and medicinal composition containing the same |
US6069153A (en) * | 1998-05-12 | 2000-05-30 | American Home Products Corporation | Indenoindoles and benzocarbazoles as estrogenic agents |
US6479535B1 (en) | 1998-05-15 | 2002-11-12 | Wyeth | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations |
US7005428B1 (en) | 1998-06-11 | 2006-02-28 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
US6465445B1 (en) | 1998-06-11 | 2002-10-15 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
US6265393B1 (en) | 1998-08-07 | 2001-07-24 | Heinrichs William Leroy | Prevention of endometriosis signs or symptons |
US6258826B1 (en) | 1998-10-13 | 2001-07-10 | Eli Lilly And Company | Pharmaceutical formulations and applications thereof for the treatment of estrogen deprivation syndrome |
AU777770C (en) | 1999-05-04 | 2005-11-10 | Strakan International Limited | Androgen glycosides and androgenic activity thereof |
US6159959A (en) * | 1999-05-06 | 2000-12-12 | American Home Products Corporation | Combined estrogen and antiestrogen therapy |
HUP0401268A2 (hu) | 2001-07-31 | 2004-11-29 | Pfizer Products Inc. | Ösztrogén agonisták/antagonisták, ösztrogének és progesztinek kombinációját tartalmazó gyógyszerkészítmények, valamint eljárás ezek előállítására |
US20060106010A1 (en) * | 2003-05-27 | 2006-05-18 | Black Larry J | Methods for inhibiting bone loss |
US20050107350A1 (en) * | 2003-08-22 | 2005-05-19 | Pharmacia Corporation | Method for the treatment or prevention of bone disorders with a cyclooxygenase-2 inhibitor alone and in combination with a bone disorder treatment agent and compositions therewith |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4133814A (en) * | 1975-10-28 | 1979-01-09 | Eli Lilly And Company | 2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents |
US4418068A (en) * | 1981-04-03 | 1983-11-29 | Eli Lilly And Company | Antiestrogenic and antiandrugenic benzothiophenes |
US4380635A (en) * | 1981-04-03 | 1983-04-19 | Eli Lilly And Company | Synthesis of acylated benzothiophenes |
US4425339A (en) * | 1981-04-09 | 1984-01-10 | Syntex (U.S.A.) Inc. | Treatment of menopausal symptoms |
ZA87332B (en) * | 1986-02-27 | 1987-08-26 | Warner Lambert Co | Compositions containing fixed combinations |
US5075321A (en) * | 1987-03-24 | 1991-12-24 | University Of Pennsylvania | Methods of treating diseases characterized by interactions of IgG-containing immune complexes with macrophage Fc receptors using antiestrogenic benzothiophenes |
JP3157882B2 (ja) * | 1991-11-15 | 2001-04-16 | 帝国臓器製薬株式会社 | 新規なベンゾチオフエン誘導体 |
AU3126593A (en) * | 1991-11-25 | 1993-06-28 | Healthguard, Incorporated | Multistage coaxial encapsulated filter assembly |
TW366342B (en) * | 1992-07-28 | 1999-08-11 | Lilly Co Eli | The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss |
-
1994
- 1994-01-28 US US08/189,399 patent/US5591753A/en not_active Expired - Fee Related
-
1995
- 1995-01-24 TW TW084100589A patent/TW401296B/zh not_active IP Right Cessation
- 1995-01-24 ZA ZA95556A patent/ZA95556B/xx unknown
- 1995-01-24 CZ CZ1995176A patent/CZ290045B6/cs not_active IP Right Cessation
- 1995-01-24 CA CA002140952A patent/CA2140952A1/en not_active Abandoned
- 1995-01-24 UA UA95018071A patent/UA29451C2/ru unknown
- 1995-01-24 NZ NZ270386A patent/NZ270386A/en unknown
- 1995-01-24 AU AU11390/95A patent/AU692811B2/en not_active Ceased
- 1995-01-25 HU HU9500229A patent/HUT72633A/hu unknown
- 1995-01-25 PH PH49830A patent/PH31553A/en unknown
- 1995-01-25 NO NO950275A patent/NO950275L/no unknown
- 1995-01-25 KR KR1019950001289A patent/KR950031068A/ko active IP Right Grant
- 1995-01-25 EP EP95300439A patent/EP0665015A3/en not_active Withdrawn
- 1995-01-26 RU RU95101044/14A patent/RU2181048C2/ru active
- 1995-01-26 CN CN95101458A patent/CN1084617C/zh not_active Expired - Fee Related
- 1995-01-26 IL IL11245595A patent/IL112455A/xx not_active IP Right Cessation
- 1995-01-26 JP JP7010490A patent/JPH07267858A/ja not_active Withdrawn
-
1996
- 1996-08-20 US US08/700,184 patent/US5646137A/en not_active Expired - Fee Related
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