EA201000946A1 - Бициклические производные для применения при лечении состояний, связанных с андрогенным рецептором - Google Patents
Бициклические производные для применения при лечении состояний, связанных с андрогенным рецепторомInfo
- Publication number
- EA201000946A1 EA201000946A1 EA201000946A EA201000946A EA201000946A1 EA 201000946 A1 EA201000946 A1 EA 201000946A1 EA 201000946 A EA201000946 A EA 201000946A EA 201000946 A EA201000946 A EA 201000946A EA 201000946 A1 EA201000946 A1 EA 201000946A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- conditions associated
- androgen receptor
- treatment
- bicyclic derivatives
- relates
- Prior art date
Links
- 102000001307 androgen receptors Human genes 0.000 title abstract 2
- 108010080146 androgen receptors Proteins 0.000 title abstract 2
- 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
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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (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
Изобретение касается бициклических соединений формулы Iгде переменные X, X, X, кольцо A, R, Rи m определены в описании. Настоящее изобретение также относится к способам получения таких соединений, фармацевтическим композициям, содержащим их, и к их применению для изготовления лекарственного средства для применения для предотвращения или лечения состояний, связанных с андрогенным рецептором.
Applications Claiming Priority (4)
| 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 | |
| PCT/GB2008/051206 WO2009081197A1 (en) | 2007-12-21 | 2008-12-18 | Bicyclic derivatives for use in the treatment of androgen receptor associated conditions |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201000946A1 true EA201000946A1 (ru) | 2010-12-30 |
| EA017144B1 EA017144B1 (ru) | 2012-10-30 |
Family
ID=40428336
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201000946A EA017144B1 (ru) | 2007-12-21 | 2008-12-18 | N-содержащие бициклические производные для применения при лечении состояний, связанных с андрогенным рецептором |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US8003649B2 (ru) |
| EP (1) | EP2235010A1 (ru) |
| JP (1) | JP2011507824A (ru) |
| KR (1) | KR20100099742A (ru) |
| CN (1) | CN101952286A (ru) |
| AR (1) | AR069911A1 (ru) |
| AU (1) | AU2008339572B2 (ru) |
| BR (1) | BRPI0821676A2 (ru) |
| CA (1) | CA2709514A1 (ru) |
| CL (1) | CL2008003846A1 (ru) |
| CO (1) | CO6331441A2 (ru) |
| CR (1) | CR11524A (ru) |
| DO (1) | DOP2010000195A (ru) |
| EA (1) | EA017144B1 (ru) |
| EC (1) | ECSP10010291A (ru) |
| IL (1) | IL206284A0 (ru) |
| NI (1) | NI201000110A (ru) |
| NZ (1) | NZ586913A (ru) |
| PE (1) | PE20091157A1 (ru) |
| TW (1) | TW200927121A (ru) |
| UY (1) | UY31559A1 (ru) |
| WO (1) | WO2009081197A1 (ru) |
| ZA (1) | ZA201004227B (ru) |
Families Citing this family (52)
| 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 |
| US8188083B2 (en) * | 2007-06-28 | 2012-05-29 | Abbott Laboratories | 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 |
| US8268872B2 (en) | 2008-02-22 | 2012-09-18 | Radius Health, Inc. | Selective androgen receptor modulators |
| BRPI0907844B8 (pt) | 2008-02-22 | 2021-05-25 | Radius Health Inc | compostos e método para modular um receptor de andrógeno, processos de preparação e composição farmacêutica dos mesmos e seus usos |
| 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 |
| US8586599B2 (en) | 2008-12-22 | 2013-11-19 | Merck Patent Gmbh | Polymorphic forms of 6-(1-methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one dihydrogenphosphate and processes of manufacturing thereof |
| WO2010092371A1 (en) * | 2009-02-10 | 2010-08-19 | Astrazeneca Ab | Triazolo [4,3-b] pyridazine derivatives and their uses for prostate cancer |
| CN102482280A (zh) * | 2009-05-11 | 2012-05-30 | 阿斯利康(瑞典)有限公司 | 作为雄激素受体的配体的[1,2,4]三唑并[4,3-b]哒嗪 |
| WO2011008543A2 (en) * | 2009-06-29 | 2011-01-20 | University Of Delaware | Pan-antagonists for the androgen receptor and androgen receptor mutants associated with anti-androgen withdrawal |
| ME02437B (me) | 2009-10-23 | 2016-09-20 | Janssen Pharmaceutica Nv | Disupstituirani oktahidropirolo[3,4-c]piroli kao modulatori oreksin receptora |
| US8680275B2 (en) | 2009-10-23 | 2014-03-25 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
| EP2491031B1 (en) | 2009-10-23 | 2013-08-07 | Janssen Pharmaceutica N.V. | Fused heterocyclic compounds as orexin receptor modulators |
| WO2011082271A2 (en) | 2009-12-30 | 2011-07-07 | Arqule, Inc. | Substituted triazolo-pyrimidine compounds |
| EP2531029B1 (en) | 2010-02-04 | 2016-10-19 | Radius Health, Inc. | Selective androgen receptor modulators |
| SI2568806T1 (sl) | 2010-05-12 | 2016-09-30 | Radius Health, Inc. | Režimi zdravljenja |
| WO2011143365A1 (en) | 2010-05-13 | 2011-11-17 | 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 |
| EP2621901B1 (en) | 2010-09-28 | 2015-07-29 | Radius Health, Inc | Selective androgen receptor modulators |
| US9586962B2 (en) | 2011-04-20 | 2017-03-07 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators |
| US9175291B2 (en) | 2012-10-11 | 2015-11-03 | Isis Pharmaceuticals Inc. | Modulation of androgen receptor expression |
| 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 |
| JP5924453B2 (ja) * | 2013-06-10 | 2016-05-25 | アステラス製薬株式会社 | 二環式含窒素芳香族ヘテロ環アミド化合物 |
| NO2719005T3 (ru) | 2014-07-28 | 2018-01-20 | ||
| EP3034499A1 (en) * | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Novel FXR (NR1H4) modulating compounds |
| EP3034501A1 (en) * | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Hydroxy containing FXR (NR1H4) modulating compounds |
| US10363254B2 (en) * | 2015-03-31 | 2019-07-30 | University Of Vermont And State Agricultural College | Methods for treating cryptosporidiosis using triazolopyridazines |
| IL288321B2 (en) | 2016-03-10 | 2025-08-01 | Janssen Pharmaceutica Nv | Methods of treating depression using orexin-2 receptor antagonists |
| SG11201810600WA (en) | 2016-06-13 | 2018-12-28 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| PL3474841T3 (pl) | 2016-06-22 | 2022-07-11 | Ellipses Pharma Ltd | Sposoby leczenia nowotworu złośliwego piersi ar+ |
| EP4122464B1 (en) | 2017-03-28 | 2024-05-15 | Gilead Sciences, Inc. | Therapeutic combinations for treating liver diseases |
| CN110997670B (zh) * | 2017-08-04 | 2022-11-01 | 百时美施贵宝公司 | [1,2,4]三唑并[4,3-a]吡啶基取代的吲哚化合物 |
| 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 |
| RS65638B1 (sr) | 2018-11-14 | 2024-07-31 | Janssen Pharmaceutica Nv | Unapređene sintetičke metode pravljenja fuzionisanih heterocikličnih jedinjenja kao modulatora receptora oreksina |
| WO2020123670A1 (en) * | 2018-12-11 | 2020-06-18 | 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 |
| BR112021011762A2 (pt) | 2019-01-15 | 2021-11-03 | Gilead Sciences Inc | Compostos para modulação de fxr (nr1h4) |
| US12479816B2 (en) | 2019-02-08 | 2025-11-25 | University of Pittsburgh—of the Commonwealth System of Higher Education | 20-HETE formation inhibitors |
| WO2020172075A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| CN114685601B (zh) * | 2020-12-30 | 2024-10-18 | 财团法人工业技术研究院 | 雄性激素受体结合分子及其用途 |
| MX2023012882A (es) * | 2021-04-30 | 2024-01-17 | Vanqua Bio Inc | Moduladores de moleculas peque?as de la actividad de la glucocerebrosidasa y sus usos. |
| 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 |
| WO2025099660A1 (en) * | 2023-11-10 | 2025-05-15 | Suven Life Sciences Limited | Piperidine substituted compounds as muscarinic m4 receptor positive allosteric modulators (m4 pams) |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000017163A1 (en) | 1998-09-22 | 2000-03-30 | Yamanouchi Pharmaceutical Co., Ltd. | Cyanophenyl derivatives |
| 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 |
| 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 |
| ATE481969T1 (de) | 2004-10-01 | 2010-10-15 | Merck Sharp & Dohme | Aminopiperidine als dipeptidylpeptidase-iv- inhibitoren zur behandlung oder prävention von 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 US US12/338,405 patent/US8003649B2/en not_active Expired - Fee Related
- 2008-12-18 KR KR1020107016410A patent/KR20100099742A/ko not_active Withdrawn
- 2008-12-18 WO PCT/GB2008/051206 patent/WO2009081197A1/en not_active Ceased
- 2008-12-18 BR BRPI0821676-2A patent/BRPI0821676A2/pt not_active IP Right Cessation
- 2008-12-18 EP EP08863828A patent/EP2235010A1/en not_active Withdrawn
- 2008-12-18 NZ NZ586913A patent/NZ586913A/en not_active IP Right Cessation
- 2008-12-18 JP JP2010538919A patent/JP2011507824A/ja active Pending
- 2008-12-18 PE PE2008002119A patent/PE20091157A1/es not_active Application Discontinuation
- 2008-12-18 AU AU2008339572A patent/AU2008339572B2/en not_active Ceased
- 2008-12-18 EA EA201000946A patent/EA017144B1/ru not_active IP Right Cessation
- 2008-12-18 CN CN200880127073XA patent/CN101952286A/zh active Pending
- 2008-12-18 CA CA2709514A patent/CA2709514A1/en not_active Abandoned
- 2008-12-19 AR ARP080105584A patent/AR069911A1/es not_active Application Discontinuation
- 2008-12-19 CL CL2008003846A patent/CL2008003846A1/es unknown
- 2008-12-19 UY UY31559A patent/UY31559A1/es not_active Application Discontinuation
- 2008-12-19 TW TW097149898A patent/TW200927121A/zh unknown
-
2010
- 2010-06-10 IL IL206284A patent/IL206284A0/en unknown
- 2010-06-14 ZA ZA2010/04227A patent/ZA201004227B/en 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 DO DO2010000195A patent/DOP2010000195A/es unknown
- 2010-06-21 CR CR11524A patent/CR11524A/es not_active Application Discontinuation
- 2010-06-21 EC EC2010010291A patent/ECSP10010291A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2008339572B2 (en) | 2012-05-10 |
| ZA201004227B (en) | 2011-10-26 |
| CN101952286A (zh) | 2011-01-19 |
| NI201000110A (es) | 2012-05-14 |
| WO2009081197A1 (en) | 2009-07-02 |
| US20100016279A1 (en) | 2010-01-21 |
| KR20100099742A (ko) | 2010-09-13 |
| UY31559A1 (es) | 2009-08-03 |
| EP2235010A1 (en) | 2010-10-06 |
| IL206284A0 (en) | 2010-12-30 |
| AR069911A1 (es) | 2010-03-03 |
| CL2008003846A1 (es) | 2010-02-05 |
| CR11524A (es) | 2010-08-05 |
| TW200927121A (en) | 2009-07-01 |
| PE20091157A1 (es) | 2009-09-03 |
| CO6331441A2 (es) | 2011-10-20 |
| NZ586913A (en) | 2012-06-29 |
| CA2709514A1 (en) | 2009-07-02 |
| DOP2010000195A (es) | 2010-08-31 |
| JP2011507824A (ja) | 2011-03-10 |
| AU2008339572A1 (en) | 2009-07-02 |
| US8003649B2 (en) | 2011-08-23 |
| EA017144B1 (ru) | 2012-10-30 |
| ECSP10010291A (es) | 2010-07-30 |
| BRPI0821676A2 (pt) | 2015-06-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM RU |