EA200500648A1 - Галогенированные селективные модуляторы андрогеновых рецепторов и способы их применения - Google Patents
Галогенированные селективные модуляторы андрогеновых рецепторов и способы их примененияInfo
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- EA200500648A1 EA200500648A1 EA200500648A EA200500648A EA200500648A1 EA 200500648 A1 EA200500648 A1 EA 200500648A1 EA 200500648 A EA200500648 A EA 200500648A EA 200500648 A EA200500648 A EA 200500648A EA 200500648 A1 EA200500648 A1 EA 200500648A1
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- androgen receptors
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- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
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- C07C233/02—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C233/04—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C233/07—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
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- C07C235/16—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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Abstract
Настоящее изобретение предоставляет класс веществ, направленных на андрогеновые рецепторы (ARTA). Эти вещества определяют новый подкласс соединений, являющихся селективными модуляторами андрогеновых рецепторов (SARM). Некоторые соединения SARM, как оказалось, обладают неожиданной андрогенной и анаболической активностью нестероидных лигандов андрогеновых рецепторов. Другие соединения SARM, как оказалось, обладают неожиданной антиандрогенной активностью нестероидных лигандов андрогеновых рецепторов. Соединения SARM, сами по себе или в виде композиции, применимы для: а) мужской контрацепции; b) лечения целого ряда гормонзависимых расстройств, например расстройств, связанных с возрастным снижением уровня андрогенов у мужчин (ADAM), таких как усталость, депрессия, пониженное либидо, половая дисфункция, нарушения эрекции, гипогонадизм, остеопороз, выпадение волос, анемия, ожирение, саркопения, остеопения, остеопороз, доброкачественная гиперплазия простаты, изменения настроения и сознания и рак простаты; с) лечения расстройств, связанных со снижением уровня андрогенов у женщин (ADIF), таких как половая дисфункция, пониженное сексуальное либидо, гипогонадизм, саркопения, остеопения, остеопороз, изменения в сознании и настроении, депрессия, анемия, выпадение волос, ожирение, эндометриоз, рак молочной железы, рак матки и рак яичников; d) лечения и/или предупреждения острой и/или хронической гипотрофии мышц; е) предупреждения и/или лечения сухости глаз; f) пероральной андроген-заместительной терапии; g) снижения встречаемости, приостановки или регрессии рака простаты; и/или h) индукции апоптоза в раковых клетках.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US10/270,732 US6998500B2 (en) | 2000-08-24 | 2002-10-16 | Selective androgen receptor modulators and methods of use thereof |
US10/371,213 US7026500B2 (en) | 2000-08-24 | 2003-02-24 | Halogenated selective androgen receptor modulators and methods of use thereof |
PCT/US2003/032507 WO2004035736A2 (en) | 2002-10-16 | 2003-10-14 | Halogenated selective androgen receptor modulators and methods of use thereof |
Publications (2)
Publication Number | Publication Date |
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EA200500648A1 true EA200500648A1 (ru) | 2006-06-30 |
EA011744B1 EA011744B1 (ru) | 2009-06-30 |
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ID=32109809
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
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EA200500648A EA011744B1 (ru) | 2002-10-16 | 2003-10-14 | Галогенированные селективные модуляторы андрогеновых рецепторов и способы их применения |
EA200700854A EA014932B1 (ru) | 2002-10-16 | 2003-10-14 | Способы лечения состояний, связанных с падением уровня андрогенов у женщин (adif) |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
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EA200700854A EA014932B1 (ru) | 2002-10-16 | 2003-10-14 | Способы лечения состояний, связанных с падением уровня андрогенов у женщин (adif) |
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US (1) | US7026500B2 (ru) |
EP (3) | EP2305636A1 (ru) |
JP (4) | JP4764719B2 (ru) |
KR (3) | KR101068779B1 (ru) |
CN (3) | CN100999481A (ru) |
AT (1) | ATE430125T1 (ru) |
AU (1) | AU2003287074B2 (ru) |
BR (1) | BR0314891A (ru) |
CA (3) | CA2502355A1 (ru) |
CY (1) | CY1109858T1 (ru) |
DE (1) | DE60327456D1 (ru) |
DK (1) | DK1558565T3 (ru) |
EA (2) | EA011744B1 (ru) |
ES (1) | ES2324606T3 (ru) |
GE (2) | GEP20094820B (ru) |
HK (1) | HK1080070A1 (ru) |
HR (2) | HRP20050334A2 (ru) |
IL (2) | IL182880A0 (ru) |
MX (1) | MXPA05004076A (ru) |
PT (1) | PT1558565E (ru) |
SI (1) | SI1558565T1 (ru) |
TW (1) | TWI332955B (ru) |
WO (1) | WO2004035736A2 (ru) |
Families Citing this family (81)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7759520B2 (en) * | 1996-11-27 | 2010-07-20 | University Of Tennessee Research Foundation | Synthesis of selective androgen receptor modulators |
US20070173546A1 (en) * | 2000-08-24 | 2007-07-26 | Dalton James T | Selective androgen receptor modulators and method of use thereof |
US7855229B2 (en) * | 2000-08-24 | 2010-12-21 | University Of Tennessee Research Foundation | Treating wasting disorders with selective androgen receptor modulators |
US7919647B2 (en) | 2000-08-24 | 2011-04-05 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and methods of use thereof |
US20030232792A1 (en) * | 2000-08-24 | 2003-12-18 | Dalton James T. | Selective androgen receptor modulators and methods of use thereof |
US20040260108A1 (en) * | 2001-06-25 | 2004-12-23 | Dalton James T. | Metabolites of selective androgen receptor modulators and methods of use thereof |
US7645898B2 (en) * | 2000-08-24 | 2010-01-12 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and method of use thereof |
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