ECSP10010291A - Derivados bicíclicos para usar en el tratamiento de afecciones asociadas con el receptor de andrógeno - Google Patents
Derivados bicíclicos para usar en el tratamiento de afecciones asociadas con el receptor de andrógenoInfo
- Publication number
- ECSP10010291A ECSP10010291A EC2010010291A ECSP10010291A ECSP10010291A EC SP10010291 A ECSP10010291 A EC SP10010291A EC 2010010291 A EC2010010291 A EC 2010010291A EC SP10010291 A ECSP10010291 A EC SP10010291A EC SP10010291 A ECSP10010291 A EC SP10010291A
- Authority
- EC
- Ecuador
- Prior art keywords
- treatment
- bicyclic derivatives
- androgen
- affections
- receiver
- Prior art date
Links
- 239000003098 androgen Substances 0.000 title 1
- 102000001307 androgen receptors Human genes 0.000 abstract 1
- 108010080146 androgen receptors Proteins 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La invención se refiere a los compuestos bicíclicos de Fórmula (I), donde los números enteros X1, X2, X3, el Anillo A, R4, R5 y m son como los definidos en la descripción. La presente invención también se relaciona con procesos para la preparación de tales compuestos, composiciones farmacéuticas que los contienen y su uso en la fabricación de un medicamento para su uso en la prevención o tratamiento de afecciones asociadas con el receptor de andrógeno.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1575507P | 2007-12-21 | 2007-12-21 | |
| US9609008P | 2008-09-11 | 2008-09-11 | |
| US10780408P | 2008-10-23 | 2008-10-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP10010291A true ECSP10010291A (es) | 2010-07-30 |
Family
ID=40428336
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2010010291A ECSP10010291A (es) | 2007-12-21 | 2010-06-21 | Derivados bicíclicos para usar en el tratamiento de afecciones asociadas con el receptor de andrógeno |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US8003649B2 (es) |
| EP (1) | EP2235010A1 (es) |
| JP (1) | JP2011507824A (es) |
| KR (1) | KR20100099742A (es) |
| CN (1) | CN101952286A (es) |
| AR (1) | AR069911A1 (es) |
| AU (1) | AU2008339572B2 (es) |
| BR (1) | BRPI0821676A2 (es) |
| CA (1) | CA2709514A1 (es) |
| CL (1) | CL2008003846A1 (es) |
| CO (1) | CO6331441A2 (es) |
| CR (1) | CR11524A (es) |
| DO (1) | DOP2010000195A (es) |
| EA (1) | EA017144B1 (es) |
| EC (1) | ECSP10010291A (es) |
| IL (1) | IL206284A0 (es) |
| NI (1) | NI201000110A (es) |
| NZ (1) | NZ586913A (es) |
| PE (1) | PE20091157A1 (es) |
| TW (1) | TW200927121A (es) |
| UY (1) | UY31559A1 (es) |
| WO (1) | WO2009081197A1 (es) |
| ZA (1) | ZA201004227B (es) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008013791A2 (en) * | 2006-07-24 | 2008-01-31 | University Of Delaware | Pan-antagonists for the androgen receptor and androgen receptor mutants associated with anti-androgen withdrawal |
| DE102007026341A1 (de) | 2007-06-06 | 2008-12-11 | Merck Patent Gmbh | Benzoxazolonderivate |
| WO2009005675A1 (en) * | 2007-06-28 | 2009-01-08 | Abbott Laboratories | Novel triazolopyridazines |
| DE102007032507A1 (de) | 2007-07-12 | 2009-04-02 | Merck Patent Gmbh | Pyridazinonderivate |
| DE102007061963A1 (de) | 2007-12-21 | 2009-06-25 | Merck Patent Gmbh | Pyridazinonderivate |
| MX2010009162A (es) | 2008-02-22 | 2010-12-21 | Radius Health Inc | Moduladores selectivos del receptor de androgeno. |
| US8268872B2 (en) | 2008-02-22 | 2012-09-18 | Radius Health, Inc. | Selective androgen receptor modulators |
| DE102008019907A1 (de) | 2008-04-21 | 2009-10-22 | Merck Patent Gmbh | Pyridazinonderivate |
| DE102008028905A1 (de) | 2008-06-18 | 2009-12-24 | Merck Patent Gmbh | 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate |
| MX2011006682A (es) | 2008-12-22 | 2011-07-13 | Merck Patent Gmbh | Nuevas formas polimorficas de dihidrogeno-fosfato de 6-(1-metil-1h-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirim idin-2-il]-bencil}-2h-piridazin-3-ona y procesos para su preparacion. |
| CN102388048B (zh) | 2009-02-10 | 2014-07-30 | 阿斯利康(瑞典)有限公司 | 三唑并[4,3-b]哒嗪衍生物及其用于前列腺癌的用途 |
| SG175726A1 (en) * | 2009-05-11 | 2011-12-29 | Astrazeneca Ab | [1,2,4] triazolo [4,3-b] pyridazines as ligands of the androgen receptor |
| US8450374B2 (en) * | 2009-06-29 | 2013-05-28 | University Of Delaware | Pan-antagonists for the androgen receptor and androgen receptor mutants associated with anti-androgen withdrawal |
| WO2011050202A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
| EP2491034B1 (en) | 2009-10-23 | 2013-12-18 | Janssen Pharmaceutica, N.V. | Fused heterocyclic compounds as orexin receptor modulators |
| ES2585806T3 (es) * | 2009-10-23 | 2016-10-10 | Janssen Pharmaceutica N.V. | Octahidropirrolo [3,4-c] pirroles disustituidos como moduladores de receptores de orexina |
| WO2011082271A2 (en) | 2009-12-30 | 2011-07-07 | Arqule, Inc. | Substituted triazolo-pyrimidine compounds |
| CA2788907A1 (en) | 2010-02-04 | 2011-08-11 | Radius Health, Inc. | Selective androgen receptor modulators |
| PT2568806T (pt) | 2010-05-12 | 2016-08-05 | Radius Health Inc | Regimes terapêuticos |
| NZ603876A (en) | 2010-05-13 | 2015-02-27 | Amgen Inc | Nitrogen heterocyclic compounds useful as pde10 inhibitors |
| US9006450B2 (en) | 2010-07-01 | 2015-04-14 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
| US8642632B2 (en) | 2010-07-02 | 2014-02-04 | Radius Health, Inc. | Selective androgen receptor modulators |
| ES2550319T3 (es) | 2010-09-28 | 2015-11-06 | Radius Health, Inc | Moduladores selectivos del receptor de andrógenos |
| WO2012145581A1 (en) | 2011-04-20 | 2012-10-26 | Janssen Pharmaceutica Nv | Disubstituted octahy-dropyrrolo [3,4-c] pyrroles as orexin receptor modulators |
| AR092982A1 (es) | 2012-10-11 | 2015-05-13 | Isis Pharmaceuticals Inc | Modulacion de la expresion de receptores androgenicos |
| US9422290B2 (en) * | 2012-11-13 | 2016-08-23 | Boehringer Ingelheim International Gmbh | Triazolopyridazine |
| US9266891B2 (en) | 2012-11-16 | 2016-02-23 | Boehringer Ingelheim International Gmbh | Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors |
| HUP1300139A2 (en) * | 2013-03-06 | 2014-09-29 | Richter Gedeon Nyrt | Phenoxypiperidine h3 antagonists |
| ES2718550T3 (es) | 2013-05-13 | 2019-07-02 | Glaxosmithkline Llc | Análogos de urea con puente sustituidos como moduladores de sirtuinas |
| AU2014279240A1 (en) * | 2013-06-10 | 2016-01-07 | Astellas Pharma Inc. | Bicyclic nitrogen-containing aromatic heterocyclic amide compound |
| NO2719005T3 (es) | 2014-07-28 | 2018-01-20 | ||
| EP3034501A1 (en) * | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Hydroxy containing FXR (NR1H4) modulating compounds |
| EP3034499A1 (en) | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Novel FXR (NR1H4) modulating compounds |
| EP3285764B1 (en) * | 2015-03-31 | 2024-03-27 | University of Vermont and State Agricultural College | Triazolopyridazines for treating cryptosporidiosis |
| HRP20220642T1 (hr) | 2016-03-10 | 2022-06-24 | Janssen Pharmaceutica Nv | Postupci za liječenje depresije uporabom antagonista receptora oreksina 2 |
| BR112018075734A2 (pt) | 2016-06-13 | 2019-04-02 | Gilead Sciences, Inc. | composto, composição farmacêutica, método para tratar um paciente com uma doença ou condição mediada pelo menos em parte por fxr, e, uso de um composto. |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences, Inc. | Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds |
| RS63311B1 (sr) | 2016-06-22 | 2022-07-29 | Ellipses Pharma Ltd | Ar+ metode lečenja raka dojke |
| CN110461328A (zh) | 2017-03-28 | 2019-11-15 | 吉利德科学公司 | 治疗肝疾病的治疗组合 |
| ES2921020T3 (es) * | 2017-08-04 | 2022-08-16 | Bristol Myers Squibb Co | Compuestos de indol sustituidos con [1,2,4]triazolo[4,3-a]piridinilo |
| GB201716871D0 (en) * | 2017-10-13 | 2017-11-29 | Inst Of Cancer Research: Royal Cancer Hospital | Compounds |
| GB201806663D0 (en) * | 2018-04-24 | 2018-06-06 | Avexxin As | 2-Oxothiazole compositions for treatment of fibrotic disease |
| SMT202400265T1 (it) | 2018-11-14 | 2024-07-09 | Janssen Pharmaceutica Nv | Metodi di sintesi migliorati per realizzare composti eterociclici fusi come modulatori del recettore per l'oressina |
| US12521386B2 (en) * | 2018-12-11 | 2026-01-13 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of the androgen receptor activity and/or expression and uses thereof |
| CN109942574B (zh) * | 2019-01-11 | 2022-04-01 | 成都阿奇生物医药科技有限公司 | 天奇替尼及其制备方法和用途 |
| EP4360632B1 (en) | 2019-01-15 | 2025-10-29 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
| WO2020163689A1 (en) | 2019-02-08 | 2020-08-13 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | 20-hete formation inhibitors |
| US11524005B2 (en) | 2019-02-19 | 2022-12-13 | Gilead Sciences, Inc. | Solid forms of FXR agonists |
| EP4010325A1 (en) | 2019-08-07 | 2022-06-15 | Janssen Pharmaceutica NV | Improved synthetic methods of making (2h-1,2,3-triazol-2-yl)phenyl compounds as orexin receptor modulators |
| EP4023649A1 (en) * | 2020-12-30 | 2022-07-06 | Industrial Technology Research Institute | Androgen receptor binding bifunctional molecules |
| US20240262832A1 (en) * | 2021-04-30 | 2024-08-08 | Vanqua Bio, Inc. | Small molecule modulators of glucocerebrosidase activity and uses thereof |
| WO2024189472A1 (en) | 2023-03-14 | 2024-09-19 | Janssen Pharmaceutica Nv | Improved synthetic methods of making substituted pyrimidine intermediates for synthesis of orexin receptor modulators |
| AU2024376208A1 (en) * | 2023-11-10 | 2026-04-30 | Suven Life Sciences Limited | Piperidine substituted compounds as muscarinic m4 receptor positive allosteric modulators (m4 pams) |
| CN121181498A (zh) * | 2025-09-03 | 2025-12-23 | 遵义医科大学第五附属(珠海)医院 | 一种醚类芳基哌嗪衍生物及其制备方法和应用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL346795A1 (en) | 1998-09-22 | 2002-02-25 | Yamanouchi Pharma Co Ltd | Cyanophenyl derivatives |
| US6184249B1 (en) | 1998-12-18 | 2001-02-06 | Biophysica, Inc. | Androgen receptor suppressors in the therapy and diagnosis of prostate cancer, alopecia and other hyper-androgenic syndromes |
| US6472415B1 (en) | 1998-12-18 | 2002-10-29 | Biophysica, Inc. | Androgen receptor suppressors in the therapy and diagnosis of prostate cancer, alopecia and other hyper-androgenic syndromes |
| EP1796669B1 (en) | 2004-10-01 | 2010-09-22 | Merck Sharp & Dohme Corp. | Aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes |
| WO2008109104A1 (en) * | 2007-03-07 | 2008-09-12 | The Regents Of The University Of California | Bivalent inhibitors of akt protein kinase |
-
2008
- 2008-12-18 BR BRPI0821676-2A patent/BRPI0821676A2/pt not_active IP Right Cessation
- 2008-12-18 KR KR1020107016410A patent/KR20100099742A/ko not_active Withdrawn
- 2008-12-18 AU AU2008339572A patent/AU2008339572B2/en not_active Ceased
- 2008-12-18 EP EP08863828A patent/EP2235010A1/en not_active Withdrawn
- 2008-12-18 US US12/338,405 patent/US8003649B2/en not_active Expired - Fee Related
- 2008-12-18 CA CA2709514A patent/CA2709514A1/en not_active Abandoned
- 2008-12-18 PE PE2008002119A patent/PE20091157A1/es not_active Application Discontinuation
- 2008-12-18 WO PCT/GB2008/051206 patent/WO2009081197A1/en not_active Ceased
- 2008-12-18 EA EA201000946A patent/EA017144B1/ru not_active IP Right Cessation
- 2008-12-18 NZ NZ586913A patent/NZ586913A/en not_active IP Right Cessation
- 2008-12-18 CN CN200880127073XA patent/CN101952286A/zh active Pending
- 2008-12-18 JP JP2010538919A patent/JP2011507824A/ja active Pending
- 2008-12-19 AR ARP080105584A patent/AR069911A1/es not_active Application Discontinuation
- 2008-12-19 CL CL2008003846A patent/CL2008003846A1/es unknown
- 2008-12-19 TW TW097149898A patent/TW200927121A/zh unknown
- 2008-12-19 UY UY31559A patent/UY31559A1/es not_active Application Discontinuation
-
2010
- 2010-06-10 IL IL206284A patent/IL206284A0/en unknown
- 2010-06-14 ZA ZA2010/04227A patent/ZA201004227B/en unknown
- 2010-06-21 DO DO2010000195A patent/DOP2010000195A/es unknown
- 2010-06-21 EC EC2010010291A patent/ECSP10010291A/es unknown
- 2010-06-21 NI NI201000110A patent/NI201000110A/es unknown
- 2010-06-21 CO CO10074454A patent/CO6331441A2/es not_active Application Discontinuation
- 2010-06-21 CR CR11524A patent/CR11524A/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| DOP2010000195A (es) | 2010-08-31 |
| WO2009081197A1 (en) | 2009-07-02 |
| EP2235010A1 (en) | 2010-10-06 |
| US20100016279A1 (en) | 2010-01-21 |
| TW200927121A (en) | 2009-07-01 |
| NZ586913A (en) | 2012-06-29 |
| CL2008003846A1 (es) | 2010-02-05 |
| UY31559A1 (es) | 2009-08-03 |
| ZA201004227B (en) | 2011-10-26 |
| AR069911A1 (es) | 2010-03-03 |
| KR20100099742A (ko) | 2010-09-13 |
| US8003649B2 (en) | 2011-08-23 |
| JP2011507824A (ja) | 2011-03-10 |
| AU2008339572B2 (en) | 2012-05-10 |
| BRPI0821676A2 (pt) | 2015-06-16 |
| EA201000946A1 (ru) | 2010-12-30 |
| NI201000110A (es) | 2012-05-14 |
| CO6331441A2 (es) | 2011-10-20 |
| CA2709514A1 (en) | 2009-07-02 |
| EA017144B1 (ru) | 2012-10-30 |
| CR11524A (es) | 2010-08-05 |
| PE20091157A1 (es) | 2009-09-03 |
| IL206284A0 (en) | 2010-12-30 |
| CN101952286A (zh) | 2011-01-19 |
| AU2008339572A1 (en) | 2009-07-02 |
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