AR069911A1 - 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
- AR069911A1 AR069911A1 ARP080105584A ARP080105584A AR069911A1 AR 069911 A1 AR069911 A1 AR 069911A1 AR P080105584 A ARP080105584 A AR P080105584A AR P080105584 A ARP080105584 A AR P080105584A AR 069911 A1 AR069911 A1 AR 069911A1
- Authority
- AR
- Argentina
- Prior art keywords
- 6alkyl
- methyl
- monocyclic
- heteroatoms independently
- independently selected
- Prior art date
Links
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 presente se relaciona con procesos para la preparacion de tales compuestos, composiciones farmacéuticas que los contienen y su uso en la fabricacion de un medicamento para su uso en la prevencion o tratamiento de afecciones asociadas con el receptor de androgeno. Reivindicacion 1: Un compuesto caracterizado porque es de Formula (1), o una sal farmacéuticamente aceptable del mismo, para su uso como un medicamento donde X3 representa CH o N; representa difluorometil, trifluorometil o cloro(difluoro)metil; Y representa CH, COH o N; R14, de manera idéntica o diferente en cada aparicion, representa hidrogeno o metil; n y p independientemente representan 1 o 2; L1 representa un enlace directo, -(CR9R10)t, -(CR9R10)v-O-(CR9R10)v, -N(R11)-(CH2)q-,-S-(O)- o -S(O)2-; R9 y R10, de manera idéntica o diferente en cada aparicion, representan hidrogeno o metil; q, de manera idéntica o diferente en cada aparicion, representa 0, 1, 2 o 3; t representa 1, 2 o 3; v, de manera idéntica o diferente en cada aparicion, representa 0, 1 o 2; J representa: aril; un anillo carbocíclico de 3 a 6 miembros monocíclico totalmente saturado; un anillo heterocíclico de 4, 5, 6 o 7 miembros monocíclico el cual comprende 1, 2, 3 o 4 heteroátomos independientemente seleccionados de O, N o S; un anillo heteroaril de 5 o 6 miembros monocíclico que comprende 1, 2, 3 o 4 heteroátomos independientemente seleccionados de O, N o S; o un sistema de anillos heteroaril de 9 o 10 miembros bicíclico que comprende 1, 2, 3, 4 o 5 heteroátomos independientemente seleccionados de O, N o S; L3 representa un enlace directo, -(CR9R10)t-, C(O)N(R11)-(CH2)q-, C(O)N(R11)-(CH2)q-S(O)2-, -NR11C (O)-(CH2)q, -C(O)(CH2)q-, -O-(CH2)q-, -O-(CH2)q-NR11-(CH2)q-, -O-(CH2)q-C(O)NR11-(CH2)q-, -S-, -S(O)- o -S(O)2-; R11 representa hidrogeno o metil; R12 representa: halo, C1-6alquil, C2-6alquenil, C2-6alquinil, carboxi, C1-6alcoxi, ciano, oxo, fluoroC1-6alquil, hidroxi, amino, N-C1-4alquiIamino o N,N-di-C1-4aIquilamino; aril, donde el anillo aril está opcionalmente sustituido por 1, 2 o 3 sustituyentes seleccionados de R13; un anillo heteroaril de 5 o 6 miembros monocíclico el cual comprende 1, 2, 3 o 4 heteroátomos independientemente seleccionados de O, N o S y donde el anillo heteroaril está opcionalmente sustituido por 1, 2 o 3 sustituyentes seleccionados de R13; o un anillo heterocíclico de 4, 5, 6 o 7 miembros monocíclico el cual comprende 1, 2, 3 o 4 heteroátomos independientemente seleccionados de O, N o S y donde el anillo heterocíclico está opcionalmente sustituido por 1, 2 o 3 sustituyentes seleccionados de R13; R13 representa amino, halo, C1-6alquil, C2-6alquenil, C2-6alquinil, C1-6alcoxi, C2-6alcanoil, C1-6alcoxiC1-6alquil, carboxi, ciano, oxo, fluoroC1-6alquiI, hidroxi, hidroxiC1-6alquil, C1-6alquilsulfanil, C1-6alquilsulfinil, C1-6alquilsulfonil, N-C1-4alquilamino, N,N-di-C1-4alquilamino o -C(O)NR14R15 donde R14 y R15 independientemente representan hidrogeno o metil; y r representa 0, 1, 2 o 3.
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 |
|---|---|
| AR069911A1 true AR069911A1 (es) | 2010-03-03 |
Family
ID=40428336
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080105584A AR069911A1 (es) | 2007-12-21 | 2008-12-19 | 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 (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7550505B2 (en) * | 2006-07-24 | 2009-06-23 | 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 |
| AU2009215843B2 (en) | 2008-02-22 | 2011-09-08 | Ellipses Pharma Ltd | Selective androgen receptor modulators |
| 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 |
| EA019320B1 (ru) | 2008-12-22 | 2014-02-28 | Мерк Патент Гмбх | Новые полиморфные формы дигидрофосфата 6-(1-метил-1h-пиразол-4-ил)-2-{3-[5-(2-морфолин-4-илэтокси)пиримидин-2-ил]бензил}-2h-пиридазин-3-она и способы их получения |
| WO2010092371A1 (en) * | 2009-02-10 | 2010-08-19 | Astrazeneca Ab | Triazolo [4,3-b] pyridazine derivatives and their uses for prostate cancer |
| CA2759884A1 (en) * | 2009-05-11 | 2010-11-18 | Astrazeneca Ab | [1,2,4] triazolo [4,3-b] pyridazines as ligands of the androgen receptor |
| 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 |
| US8680275B2 (en) | 2009-10-23 | 2014-03-25 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
| JP5848251B2 (ja) | 2009-10-23 | 2016-01-27 | ヤンセン ファーマシューティカ エヌ．ベー． | オレキシン受容体調節因子としての縮合複素環式化合物 |
| ME02437B (me) | 2009-10-23 | 2016-09-20 | Janssen Pharmaceutica Nv | Disupstituirani oktahidropirolo[3,4-c]piroli kao modulatori oreksin receptora |
| US8343977B2 (en) | 2009-12-30 | 2013-01-01 | Arqule, Inc. | Substituted triazolo-pyrimidine compounds |
| US8987319B2 (en) | 2010-02-04 | 2015-03-24 | Radius Health, Inc. | Selective androgen receptor modulators |
| SI2568806T1 (sl) | 2010-05-12 | 2016-09-30 | Radius Health, Inc. | Režimi zdravljenja |
| SG185515A1 (en) * | 2010-05-13 | 2012-12-28 | 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 |
| AU2011312490B2 (en) | 2010-09-28 | 2015-06-25 | Radius Pharmaceuticals, Inc. | Selective androgen receptor modulators |
| WO2012145581A1 (en) | 2011-04-20 | 2012-10-26 | Janssen Pharmaceutica Nv | Disubstituted octahy-dropyrrolo [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 |
| JP6376707B2 (ja) | 2013-05-13 | 2018-08-22 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ | サーチュイン調節剤としての置換架橋尿素類似体 |
| CA2914982A1 (en) * | 2013-06-10 | 2014-12-18 | 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 |
| WO2016161125A1 (en) * | 2015-03-31 | 2016-10-06 | University Of Vermont And State Agricultural College | Methods for treating cryptosporidiosis using triazolopyridazines |
| CR20180433A (es) | 2016-03-10 | 2018-11-07 | Janssen Pharmaceutica Nv | Métodos para tratar la depresión con antagonistas del receptor de orexina-2 |
| KR102269305B1 (ko) | 2016-06-13 | 2021-06-25 | 길리애드 사이언시즈, 인코포레이티드 | Fxr (nr1h4) 조정 화합물 |
| CA2968836A1 (en) | 2016-06-13 | 2017-12-13 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
| PT3474841T (pt) | 2016-06-22 | 2022-06-20 | Radius Health Inc | Métodos de tratamento do cancro de mama ar+ |
| ES2927019T3 (es) | 2017-03-28 | 2022-11-02 | Gilead Sciences Inc | Combinaciones terapéuticas para el tratamiento de enfermedades hepáticas |
| CN110997670B (zh) * | 2017-08-04 | 2022-11-01 | 百时美施贵宝公司 | [1,2,4]***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 |
| MA54250A (fr) | 2018-11-14 | 2022-02-23 | Janssen Pharmaceutica Nv | Procédés synthétiques améliorés de production de composés hétérocycliques fusionnés utilisés en tant que modulateurs du récepteur de l'orexine |
| 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 |
| EP4360632A3 (en) | 2019-01-15 | 2024-06-19 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
| KR20210129128A (ko) | 2019-02-19 | 2021-10-27 | 길리애드 사이언시즈, 인코포레이티드 | Fxr 효능제의 고체 형태 |
| CN114685601A (zh) * | 2020-12-30 | 2022-07-01 | 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 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU754529B2 (en) | 1998-09-22 | 2002-11-21 | 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 |
| US7884104B2 (en) * | 2004-10-01 | 2011-02-08 | 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 EA EA201000946A patent/EA017144B1/ru not_active IP Right Cessation
- 2008-12-18 PE PE2008002119A patent/PE20091157A1/es not_active Application Discontinuation
- 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 BR BRPI0821676-2A patent/BRPI0821676A2/pt 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 AU AU2008339572A patent/AU2008339572B2/en not_active Ceased
- 2008-12-18 WO PCT/GB2008/051206 patent/WO2009081197A1/en active Application Filing
- 2008-12-18 KR KR1020107016410A patent/KR20100099742A/ko not_active Application Discontinuation
- 2008-12-18 JP JP2010538919A patent/JP2011507824A/ja active Pending
- 2008-12-18 EP EP08863828A patent/EP2235010A1/en not_active Withdrawn
- 2008-12-19 TW TW097149898A patent/TW200927121A/zh unknown
- 2008-12-19 UY UY31559A patent/UY31559A1/es not_active Application Discontinuation
- 2008-12-19 CL CL2008003846A patent/CL2008003846A1/es unknown
- 2008-12-19 AR ARP080105584A patent/AR069911A1/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 CR CR11524A patent/CR11524A/es not_active Application Discontinuation
- 2010-06-21 EC EC2010010291A patent/ECSP10010291A/es unknown
- 2010-06-21 DO DO2010000195A patent/DOP2010000195A/es unknown
- 2010-06-21 NI NI201000110A patent/NI201000110A/es unknown
- 2010-06-21 CO CO10074454A patent/CO6331441A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CN101952286A (zh) | 2011-01-19 |
| PE20091157A1 (es) | 2009-09-03 |
| US8003649B2 (en) | 2011-08-23 |
| IL206284A0 (en) | 2010-12-30 |
| ZA201004227B (en) | 2011-10-26 |
| ECSP10010291A (es) | 2010-07-30 |
| DOP2010000195A (es) | 2010-08-31 |
| BRPI0821676A2 (pt) | 2015-06-16 |
| EP2235010A1 (en) | 2010-10-06 |
| CO6331441A2 (es) | 2011-10-20 |
| WO2009081197A1 (en) | 2009-07-02 |
| JP2011507824A (ja) | 2011-03-10 |
| AU2008339572A1 (en) | 2009-07-02 |
| KR20100099742A (ko) | 2010-09-13 |
| AU2008339572B2 (en) | 2012-05-10 |
| NI201000110A (es) | 2012-05-14 |
| UY31559A1 (es) | 2009-08-03 |
| NZ586913A (en) | 2012-06-29 |
| EA201000946A1 (ru) | 2010-12-30 |
| CL2008003846A1 (es) | 2010-02-05 |
| CA2709514A1 (en) | 2009-07-02 |
| TW200927121A (en) | 2009-07-01 |
| EA017144B1 (ru) | 2012-10-30 |
| US20100016279A1 (en) | 2010-01-21 |
| CR11524A (es) | 2010-08-05 |
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