PE20060401A1 - Derivados de n-(2-bencil)-2-fenil-butanamidas y propanamidas como moduladores del receptor de androgeno - Google Patents
Derivados de n-(2-bencil)-2-fenil-butanamidas y propanamidas como moduladores del receptor de androgenoInfo
- Publication number
- PE20060401A1 PE20060401A1 PE2005000631A PE2005000631A PE20060401A1 PE 20060401 A1 PE20060401 A1 PE 20060401A1 PE 2005000631 A PE2005000631 A PE 2005000631A PE 2005000631 A PE2005000631 A PE 2005000631A PE 20060401 A1 PE20060401 A1 PE 20060401A1
- Authority
- PE
- Peru
- Prior art keywords
- benzyl
- androgen receptor
- phenylbutanamide
- fluoro
- modulators
- Prior art date
Links
- 102000001307 androgen receptors Human genes 0.000 title 1
- 108010080146 androgen receptors Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- SLRMQYXOBQWXCR-UHFFFAOYSA-N 2154-56-5 Chemical class [CH2]C1=CC=CC=C1 SLRMQYXOBQWXCR-UHFFFAOYSA-N 0.000 abstract 1
- 206010002261 Androgen deficiency Diseases 0.000 abstract 1
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 1
- 208000029725 Metabolic bone disease Diseases 0.000 abstract 1
- 206010049088 Osteopenia Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 210000003205 muscle Anatomy 0.000 abstract 1
- HXCCXUWPISVJRA-UHFFFAOYSA-N n-[(2-fluoro-5-methylphenyl)methyl]-2-phenylbutanamide Chemical compound C=1C=CC=CC=1C(CC)C(=O)NCC1=CC(C)=CC=C1F HXCCXUWPISVJRA-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000849 selective androgen receptor modulator Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
- C07D295/205—Radicals derived from carbonic acid
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/12—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
- C07C233/13—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
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- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
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- C07C235/32—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 containing six-membered aromatic rings
- C07C235/34—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 containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
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- C07C271/12—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
- C07D213/61—Halogen atoms or nitro radicals
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
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- Child & Adolescent Psychology (AREA)
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- Urology & Nephrology (AREA)
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Abstract
REFERIDA A UN COMPUESTO DERIVADO DE FENILBUTANAMIDA DE FORMULA I, DONDE X ES CH O N; n ES 0, 1, 2 O 3; m ES 0, 1 O 2; R1, R4 Y R5 SON H, HALOGENO, CIANO, ENTRE OTROS; R2 Y R3 SON H, HALOGENO, CIANO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (S)-N-(2-FLUORO-5-(TRIFLUOROMETIL)BENCIL)-2-FENILBUTANAMIDA, N-(2-FLUORO-5-METILBENCIL)-2-FENILBUTANAMIDA, (S)-N-((2-FLUORO-5-(TRIFLUOROMETIL)PIRIDIN-3-IL)METIL)-2-FENILBUTANAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR DE ANDROGENO Y SON UTILES EN LA MEJORA DEL TONO MUSCULAR DEBILITADO Y EN EL TRATAMIENTO DE AFECCIONES PROVOCADAS POR DEFICIENCIA DE ANDROGENO, INCLUYENDO OSTEOPOROSIS, OSTEOPENIA, FRACTURA OSEA, ENTRE OTRAS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US57769804P | 2004-06-07 | 2004-06-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20060401A1 true PE20060401A1 (es) | 2006-05-15 |
Family
ID=35415107
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2005000631A PE20060401A1 (es) | 2004-06-07 | 2005-06-03 | Derivados de n-(2-bencil)-2-fenil-butanamidas y propanamidas como moduladores del receptor de androgeno |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US7629367B2 (es) |
| EP (1) | EP1755572B1 (es) |
| JP (1) | JP4881865B2 (es) |
| CN (1) | CN1976902A (es) |
| AR (1) | AR049140A1 (es) |
| AT (1) | ATE545631T1 (es) |
| AU (1) | AU2005251766B9 (es) |
| BR (1) | BRPI0511862A (es) |
| CA (1) | CA2569124C (es) |
| CR (1) | CR8777A (es) |
| EC (1) | ECSP067061A (es) |
| IL (1) | IL179843A0 (es) |
| MA (1) | MA28677B1 (es) |
| MX (1) | MXPA06014235A (es) |
| MY (1) | MY147997A (es) |
| NO (1) | NO20070085L (es) |
| NZ (1) | NZ551738A (es) |
| PE (1) | PE20060401A1 (es) |
| RU (1) | RU2378255C2 (es) |
| SG (1) | SG169398A1 (es) |
| TW (1) | TW200610755A (es) |
| UA (1) | UA87854C2 (es) |
| WO (1) | WO2005120477A2 (es) |
| ZA (1) | ZA200609673B (es) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA87854C2 (en) | 2004-06-07 | 2009-08-25 | Мерк Энд Ко., Инк. | N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators |
| WO2006060108A1 (en) * | 2004-10-29 | 2006-06-08 | Merck & Co., Inc. | N-(pyridin-3-yl)-2-phenylbutanamides as androgen receptor modulators |
| US20090088458A1 (en) * | 2005-08-02 | 2009-04-02 | Meissner Robert S | N-(Pyridin-4-Yl)-2-Phenylbutanamides as Androgen Receptor Modulators |
| BRPI0620844A2 (pt) * | 2005-12-30 | 2011-11-29 | Ranbaxy Lab Ltd | compostos antagonistas dos receptores muscarìnicos, seus métodos de preparação, composições farmacêuticas compreendendo os mesmos, usos dos referidos compostos na preparação de medicamentos |
| US20090275515A1 (en) * | 2006-10-18 | 2009-11-05 | Yuntae Kim | 2-hydroxy-2-phenylthiophenylpropionamides as androgen receptor modulators |
| CN101945853B (zh) | 2007-12-21 | 2014-08-20 | 配体药物公司 | 选择性雄激素受体调节剂(sarm)及其应用 |
| US20090197947A1 (en) * | 2008-02-01 | 2009-08-06 | The Research Foundation Of State University Of New York | Medicaments and methods for lowering plasma lipid levels and screening drugs |
| WO2009136629A1 (ja) * | 2008-05-09 | 2009-11-12 | あすか製薬株式会社 | 生活習慣病予防・治療剤 |
| AU2011264858B2 (en) | 2010-06-10 | 2016-04-21 | Seragon Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
| US9282979B2 (en) | 2010-06-24 | 2016-03-15 | DePuy Synthes Products, Inc. | Instruments and methods for non-parallel disc space preparation |
| FR2982261B1 (fr) * | 2011-11-04 | 2014-06-13 | Galderma Res & Dev | Nouveaux amides, et leur utilisation pharmaceutique ou cosmetique |
| BR112014014124A2 (pt) | 2011-12-14 | 2017-08-22 | Seragon Pharmaceutical Inc | Moduladores do receptor de estrogênio fluorados e usos dos mesmos |
| CN103288669B (zh) * | 2013-07-01 | 2015-06-24 | 南开大学 | 一种阿卓乳酸酰胺衍生物及应用 |
| US9868705B2 (en) | 2013-09-27 | 2018-01-16 | The Board Of Trustees Of The University Of Illinois | Tetra-aryl cyclobutane inhibitors of androgen receptor action for the treatment of hormone refractory cancer |
| WO2015108988A2 (en) | 2014-01-17 | 2015-07-23 | Ligand Pharmaceuticals, Inc. | Methods and compositions for modulating hormone levels |
| US10806720B2 (en) | 2015-04-21 | 2020-10-20 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10441570B2 (en) | 2015-04-21 | 2019-10-15 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) Ligands and methods of use thereof |
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- 2005-06-03 AT AT05756622T patent/ATE545631T1/de active
- 2005-06-03 CA CA2569124A patent/CA2569124C/en not_active Expired - Fee Related
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- 2005-06-03 CN CNA2005800185774A patent/CN1976902A/zh active Pending
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