PE20091157A1 - Derivados biciclicos para usar en el tratamiento de afecciones asociadas con el receptor de androgeno - 155 - Google Patents
Derivados biciclicos para usar en el tratamiento de afecciones asociadas con el receptor de androgeno - 155Info
- Publication number
- PE20091157A1 PE20091157A1 PE2008002119A PE2008002119A PE20091157A1 PE 20091157 A1 PE20091157 A1 PE 20091157A1 PE 2008002119 A PE2008002119 A PE 2008002119A PE 2008002119 A PE2008002119 A PE 2008002119A PE 20091157 A1 PE20091157 A1 PE 20091157A1
- Authority
- PE
- Peru
- Prior art keywords
- treatment
- androgen receptor
- triazolo
- conditions associated
- compounds
- Prior art date
Links
- 102000001307 androgen receptors Human genes 0.000 title abstract 3
- 108010080146 androgen receptors Proteins 0.000 title abstract 3
- -1 AMINO Chemical class 0.000 abstract 3
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 2
- 206010060862 Prostate cancer Diseases 0.000 abstract 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- QPAXMPYBNSHKAK-UHFFFAOYSA-N chloro(difluoro)methane Chemical group F[C](F)Cl QPAXMPYBNSHKAK-UHFFFAOYSA-N 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- HDOWRFHMPULYOA-UHFFFAOYSA-N piperidin-4-ol Chemical compound OC1CCNCC1 HDOWRFHMPULYOA-UHFFFAOYSA-N 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
SE REFIERE A COMPUESTOS BICICLICOS DE FORMULA (Ic) DONDE X3 ES CH O N; R4 ES C2F2, CF3 O CClF2; Y ES CH, COH O N; R14 ES H O CH3; n Y p SON CADA UNO 1 O 2; L1 ES UN ENLACE DIRECTO, -S-, -S(O)-, -S(O)2-, ENTRE OTROS; J ES ARILO, UN ANILLO CARBOCICLICO DE 3 A 6 MIEMBROS MONOCICLICO, HETEROCICLICO DE 4 A 7 MIEMBROS, ENTRE OTROS; L3 ES -C(O)-(CH2)q, -O-(CH2)q, (CH2)q, ENTRE OTROS, DONDE q ES DE 0 A 3; R12 ES OH, HALO, AMINO, CN, OXO, ENTRE OTROS; r ES DE 0 A 3. SON COMPUESTOS PREFERIDOS: 4-[[4-[3-(TRIFLUOROMETIL)-[1,2,4]TRIAZOLO[4,3-b]PIRIDAZIN-6-IL]PIPERAZIN-1-IL]METIL]BENZONITRILO, 3-(TRIFLUOROMETIL)-6-[4-[[3-(TRIFLUOROMETIL)FENIL]METIL]PIPERAZIN-1-IL]-[1,2,4]TRIAZOLO[4,3-b]PIRIDAZINA, 4-PIRIDIN-3-IL-1-[3-(TRIFLUOROMETIL)-[1,2,4]TRIAZOLO[4,3-b]PIRIDAZIN-6-IL]PIPERIDIN-4-OL, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON LIGANDOS DEL RECEPTOR DE ANDROGENO (AR) SIENDO UTILES EN EL TRATAMIENTO DEL CANCER DE PROSTATA
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 |
|---|---|
| PE20091157A1 true PE20091157A1 (es) | 2009-09-03 |
Family
ID=40428336
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008002119A PE20091157A1 (es) | 2007-12-21 | 2008-12-18 | Derivados biciclicos para usar en el tratamiento de afecciones asociadas con el receptor de androgeno - 155 |
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 (51)
| 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 |
| US8067448B2 (en) | 2008-02-22 | 2011-11-29 | 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 |
| MY160526A (en) | 2008-12-22 | 2017-03-15 | Merck Patent Gmbh | Novel 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 |
| MX2011012055A (es) * | 2009-05-11 | 2011-12-06 | Astrazeneca Ab | [1,2,4] triazolo [4,3-b] piridazinas como ligandos del receptor de androgeno. |
| 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 |
| RS54945B1 (sr) | 2009-10-23 | 2016-11-30 | Janssen Pharmaceutica Nv | Disupstituisani oktahidropirolo[3,4-c]piroli kao oreksin receptor modulatori |
| WO2011050200A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
| US9062044B2 (en) | 2009-10-23 | 2015-06-23 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators |
| WO2011082271A2 (en) | 2009-12-30 | 2011-07-07 | Arqule, Inc. | Substituted triazolo-pyrimidine compounds |
| WO2011097496A1 (en) | 2010-02-04 | 2011-08-11 | Radius Health, Inc. | Selective androgen receptor modulators |
| MX342898B (es) | 2010-05-12 | 2016-10-18 | Radius Health Inc * | Regimen terapéutico de la sal de diclorhidrato del (r) -6-(2-(etil (4-2(etilamino) etil) bencil) amino)-4-metoxifenil)-5, 6,7,8-tetrahidronaftaleno-2-ol. |
| MA34300B1 (fr) | 2010-05-13 | 2013-06-01 | Amgen Inc | Composés azotés hétérocycliques convenant comme inhibiteurs de la pde10 |
| 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 |
| US9765075B2 (en) * | 2013-05-13 | 2017-09-19 | Glaxosmithkline Llc | Substituted bridged urea analogs as sirtuin modulators |
| HK1220446A1 (en) * | 2013-06-10 | 2017-05-05 | 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 |
| DK3426251T3 (da) | 2016-03-10 | 2022-06-20 | Janssen Pharmaceutica Nv | Fremgangsmåder til behandling af depression under anvendelse af orexin-2-receptorantagonister |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| 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. |
| CA3027563C (en) | 2016-06-22 | 2024-07-02 | Ellipses Pharma Ltd | AR+ METHODS FOR BREAST CANCER TREATMENT |
| ES2927019T3 (es) | 2017-03-28 | 2022-11-02 | Gilead Sciences Inc | Combinaciones terapéuticas para el tratamiento de enfermedades hepáticas |
| 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 |
| CR20210240A (es) | 2018-11-14 | 2021-06-08 | Janssen Pharmaceutica Nv | Métodos sintéticos mejorados para elaborar compuestos heterocíclicos fusionados como moduladores del receptor de orexina |
| 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 |
| DK3911647T3 (da) | 2019-01-15 | 2024-02-26 | Gilead Sciences Inc | Isoxazol-forbindelse som FXR-agonist og farmaceutiske sammensætninger, der omfatter en sådan |
| US12479816B2 (en) | 2019-02-08 | 2025-11-25 | University of Pittsburgh—of the Commonwealth System of Higher Education | 20-HETE formation inhibitors |
| JP2022519906A (ja) | 2019-02-19 | 2022-03-25 | ギリアード サイエンシーズ, インコーポレイテッド | Fxrアゴニストの固体形態 |
| 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 |
| 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 |
|---|---|---|---|---|
| JP3390744B2 (ja) | 1998-09-22 | 2003-03-31 | 山之内製薬株式会社 | シアノフェニル誘導体 |
| 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 |
| JP4797021B2 (ja) * | 2004-10-01 | 2011-10-19 | メルク・シャープ・エンド・ドーム・コーポレイション | 糖尿病の治療または予防用のジペプチジルペプチダ−ゼ−iv阻害剤としてのアミノピペリジン |
| 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 JP JP2010538919A patent/JP2011507824A/ja active Pending
- 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 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 BR BRPI0821676-2A patent/BRPI0821676A2/pt not_active IP Right Cessation
- 2008-12-18 PE PE2008002119A patent/PE20091157A1/es not_active Application Discontinuation
- 2008-12-18 EP EP08863828A patent/EP2235010A1/en not_active Withdrawn
- 2008-12-18 KR KR1020107016410A patent/KR20100099742A/ko not_active Withdrawn
- 2008-12-18 US US12/338,405 patent/US8003649B2/en not_active Expired - Fee Related
- 2008-12-18 AU AU2008339572A patent/AU2008339572B2/en not_active Ceased
- 2008-12-18 CA CA2709514A patent/CA2709514A1/en not_active Abandoned
- 2008-12-19 TW TW097149898A patent/TW200927121A/zh unknown
- 2008-12-19 AR ARP080105584A patent/AR069911A1/es not_active Application Discontinuation
- 2008-12-19 UY UY31559A patent/UY31559A1/es not_active Application Discontinuation
- 2008-12-19 CL CL2008003846A patent/CL2008003846A1/es unknown
-
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 NI NI201000110A patent/NI201000110A/es unknown
- 2010-06-21 EC EC2010010291A patent/ECSP10010291A/es unknown
- 2010-06-21 CR CR11524A patent/CR11524A/es not_active Application Discontinuation
- 2010-06-21 CO CO10074454A patent/CO6331441A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| TW200927121A (en) | 2009-07-01 |
| ZA201004227B (en) | 2011-10-26 |
| ECSP10010291A (es) | 2010-07-30 |
| DOP2010000195A (es) | 2010-08-31 |
| UY31559A1 (es) | 2009-08-03 |
| EA017144B1 (ru) | 2012-10-30 |
| WO2009081197A1 (en) | 2009-07-02 |
| EA201000946A1 (ru) | 2010-12-30 |
| CR11524A (es) | 2010-08-05 |
| CN101952286A (zh) | 2011-01-19 |
| CA2709514A1 (en) | 2009-07-02 |
| CL2008003846A1 (es) | 2010-02-05 |
| JP2011507824A (ja) | 2011-03-10 |
| AR069911A1 (es) | 2010-03-03 |
| CO6331441A2 (es) | 2011-10-20 |
| US20100016279A1 (en) | 2010-01-21 |
| NI201000110A (es) | 2012-05-14 |
| US8003649B2 (en) | 2011-08-23 |
| KR20100099742A (ko) | 2010-09-13 |
| BRPI0821676A2 (pt) | 2015-06-16 |
| NZ586913A (en) | 2012-06-29 |
| AU2008339572B2 (en) | 2012-05-10 |
| IL206284A0 (en) | 2010-12-30 |
| AU2008339572A1 (en) | 2009-07-02 |
| EP2235010A1 (en) | 2010-10-06 |
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| FC | Refusal |