AR075383A1 - Derivados de triazolo[4,3-b]piridazina - Google Patents
Derivados de triazolo[4,3-b]piridazinaInfo
- Publication number
- AR075383A1 AR075383A1 ARP100100350A ARP100100350A AR075383A1 AR 075383 A1 AR075383 A1 AR 075383A1 AR P100100350 A ARP100100350 A AR P100100350A AR P100100350 A ARP100100350 A AR P100100350A AR 075383 A1 AR075383 A1 AR 075383A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cr3r4
- heteroatoms
- independently selected
- identically
- Prior art date
Links
Classifications
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
Abstract
Se refiere a procesos para la preparacion de dichos compuestos, composiciones farmacéuticas que los contienen y su uso en el tratamiento de afecciones asociadas con el receptor de androgenos, en particular el cáncer de prostata. Reivindicacion 1: Un compuesto caracterizado porque es de Formula 1, o una sal farmacéuticamente aceptable del mismo: en donde R1 representa haloalquilo C1-4; k representa 0, 1 o 2: n y p independientemente representan 1 o 2: Y representa N, C, CH o COH; la línea punteada representa un enlace simple cuando Y es N, CH o COH; la línea punteada representa un enlace doble cuando Y es C, L1 es un enlace directo y J es indolilo pirrolopiridinilo: L1 representa un enlace directo,-(CR3R4)t-, -(CR3R4)v-O-(CR3R4)v-, -N(R5)-(CH2)q-, -S-, -S(O)- o S(O)2-; R3 y R4, de forma idéntica o diferente en cada aparicion, representan hidrogeno o metilo; R5 representa hidrogeno o metilo: q, de forma idéntica o diferente en cada aparicion, representa 0, 1, 2, 3 o 4; t representa 1, 2 o 3; v, de forma idéntica o diferente en cada aparicion, representa 0, 1 o 2; j representa: arilo; cicloalquilo C3-6; un anillo heterocíclico de 4, 5, 6 o 7 miembros monocíclico que comprende 1, 2 o 3 heteroátomos que se seleccionan independientemente de O, N o S; Un anillo heteroarilo monocíclico de 5 o 6 miembros que comprende 1, 2, 3 o 4 heteroátomos que se seleccionan independientemente de O, N o S; o un sistema de anillos heteroarilo bicíclico de 9 o 10 miembros que comprende 1, 2, 3, 4 o 5 heteroátomos que se seleccionan independientemente de O, N o S; L2 representa un enlace directo. -(CR3R4)t-, -C(O)N(R5)-(CH2)q-, -C(O)N(R5)-(CH2)q- S(O)2-, -NR5C(O)-(CH2)q-, -C(O)-(CH2)q-, -O-(CR9R10)q-, -O-(CR3R4)q-NR5-(CH2)q-, -O-(CR3R4)q-C(O)NR5-(CH2)q-, -S-, -S(O)- o -S(O)2-; R9 y R10, de forma idéntica o diferente en cada aparicion, representan hidrogeno, metilo, etilo, isopropilo, ciclopropilo o metoximetilo: R2 representa: halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carboxi, alcoxi C1-6, ciano, oxo, fluoroalquilo C1-6, hidroxi, animo, N-alquil C1-4amino o N,N-di-alquil C1-4amino; arilo, en donde el anillo arilo está opcionalmente sustituido por 1, 2 o 3 sustituyentes que se seleccionan de R6; un anillo heterocíclico de 4, 5, 6 o 7 miembros monocíclico que comprende 1, 2 o 3 heteroátomos que se seleccionan independientemente de O, N o S y en donde el anillo heterocíclico está opcionalmente sustituido por 1, 2 o 3 sustituyentes que se seleccionan de R6; un anillo heteroarilo de 5 o 6 miembros monocíclico que comprende 1, 2, 3 o 4 heteroátomos que se seleccionan independientemente de O, N o S y en donde el anillo heteroarilo está opcionalmente sustituido por 1, 2 o 3 sustituyentes que se seleccionan de R6: o un sistema de anillos heteroarilo bicíclico de 9 o 10 miembros que comprenden 1, 2, 3, 4 o 5 heteroátomos que se seleccionan independientemente de O, N o S y en donde el anillo heterocíclico está opcionalmente sustituido por 1, 2 o 3 sustituyentes que se seleccionan de R6; R6 representa amino, halo, alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcanoilo C2-6, alcoxi C1-6 alquilo C1-6, carboxi, ciano, oxo, fluoroalquilo C1-6, hidroxi, hidroxialquilo C1-6, alquil C1-6 sulfanilo, alquil C1-6 sulfinilo, alquil C1-6 sulfonilo, oxetan-3-ilcarbonilo, N-alquil C1-4 amino N,N-di-alquil C1-4 amino o -C(O)NR7R8 en donde R7 y R8 independientemente representan hidrogeno o metilo; y r representa 0, 1, 2 o 3.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US15122109P | 2009-02-10 | 2009-02-10 | |
US18776609P | 2009-06-17 | 2009-06-17 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR075383A1 true AR075383A1 (es) | 2011-03-30 |
Family
ID=42115693
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100100350A AR075383A1 (es) | 2009-02-10 | 2010-02-09 | Derivados de triazolo[4,3-b]piridazina |
Country Status (27)
Country | Link |
---|---|
US (2) | US8258140B2 (es) |
EP (1) | EP2396333B1 (es) |
JP (1) | JP5059977B2 (es) |
KR (1) | KR20110113755A (es) |
CN (1) | CN102388048B (es) |
AR (1) | AR075383A1 (es) |
AU (1) | AU2010212590B2 (es) |
CA (1) | CA2749926A1 (es) |
CL (1) | CL2011001920A1 (es) |
CO (1) | CO6410299A2 (es) |
CR (1) | CR20110427A (es) |
CU (1) | CU20110158A7 (es) |
DO (1) | DOP2011000258A (es) |
EA (1) | EA019647B1 (es) |
EC (1) | ECSP11011257A (es) |
ES (1) | ES2427917T3 (es) |
HK (1) | HK1164870A1 (es) |
IL (1) | IL214112A0 (es) |
MX (1) | MX2011008452A (es) |
NI (1) | NI201100156A (es) |
PE (1) | PE20120603A1 (es) |
SG (1) | SG172986A1 (es) |
SV (1) | SV2011003993A (es) |
TW (1) | TW201033215A (es) |
UY (1) | UY32426A (es) |
WO (1) | WO2010092371A1 (es) |
ZA (1) | ZA201106625B (es) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
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AU2010247190A1 (en) * | 2009-05-11 | 2011-11-10 | Astrazeneca Ab | [1,2,4] triazolo [4,3-b] pyridazines as ligands of the androgen receptor |
RS59493B2 (sr) | 2011-11-30 | 2023-02-28 | Astrazeneca Ab | Kombinacioni tretman raka |
AU2013204533B2 (en) | 2012-04-17 | 2017-02-02 | Astrazeneca Ab | Crystalline forms |
WO2014036897A1 (zh) | 2012-09-04 | 2014-03-13 | 上海恒瑞医药有限公司 | 咪唑啉类衍生物、其制备方法及其在医药上的应用 |
WO2015042170A1 (en) | 2013-09-17 | 2015-03-26 | Wayne State University | Compositions and uses of combinations of dim-related indoles and selected anti-androgen compounds |
NO2719005T3 (es) * | 2014-07-28 | 2018-01-20 | ||
WO2016149099A1 (en) | 2015-03-13 | 2016-09-22 | Forma Therapeutics, Inc. | Alpha-cinnamide compounds and compositions as hdac8 inhibitors |
US10363254B2 (en) * | 2015-03-31 | 2019-07-30 | University Of Vermont And State Agricultural College | Methods for treating cryptosporidiosis using triazolopyridazines |
ES2863500T3 (es) | 2015-04-10 | 2021-10-11 | Capsugel Belgium Nv | Formulaciones lipídicas de acetato de abiraterona |
US11664093B2 (en) * | 2019-01-17 | 2023-05-30 | The Board Of Trustees Of The University Of Illinois | Extrapolative prediction of enantioselectivity enabled by computer-driven workflow, new molecular representations and machine learning |
JP7183842B2 (ja) * | 2019-02-08 | 2022-12-06 | 富士通株式会社 | 結合自由エネルギー計算の前処理方法、前処理装置及び前処理プログラム、並びに、結合自由エネルギーの算出方法 |
WO2020223590A1 (en) * | 2019-05-02 | 2020-11-05 | Constellation Pharmaceuticals, Inc. | Modulators of trex1 |
WO2020243378A1 (en) * | 2019-05-31 | 2020-12-03 | United States Government As Represented By The Department Of Veterans Affairs | Compositions and methods comprising endothelin a receptor antagonists and androgen therapies |
TWI813106B (zh) * | 2020-12-30 | 2023-08-21 | 財團法人工業技術研究院 | 雄性激素受體結合分子及其用途 |
AU2022291768A1 (en) | 2021-06-16 | 2023-11-30 | Celgene Corporation | Azetidinyl compounds comprising a carboxylic acid group for the treatment of neurodegenerative diseases |
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USRE35956E (en) | 1991-01-09 | 1998-11-10 | Roussel Uclaf | Phenylimidazolidines having antiandrogenic activity |
US5411981A (en) | 1991-01-09 | 1995-05-02 | Roussel Uclaf | Phenylimidazolidines having antiandrogenic activity |
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CN1597671A (zh) * | 2004-07-20 | 2005-03-23 | 贵州大学 | 喹唑啉衍生物及制备方法和生物活性 |
CN101031300A (zh) * | 2004-10-01 | 2007-09-05 | 默克公司 | 用于治疗或预防糖尿病的作为二肽基肽酶-ⅳ抑制剂的氨基哌啶化合物 |
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US7655683B2 (en) | 2006-02-10 | 2010-02-02 | Janssen Pharmaceutica Nv | Imidazolopyrazole derivatives useful as selective androgen receptor modulators |
JP2009538899A (ja) * | 2006-05-30 | 2009-11-12 | ファイザー・プロダクツ・インク | トリアゾロピリダジン誘導体 |
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JP2010507577A (ja) * | 2006-10-23 | 2010-03-11 | エスジーエックス ファーマシューティカルズ、インコーポレイテッド | トリアゾロピリダジンタンパク質キナーゼモジュレーター |
WO2008109104A1 (en) * | 2007-03-07 | 2008-09-12 | The Regents Of The University Of California | Bivalent inhibitors of akt protein kinase |
US8188083B2 (en) | 2007-06-28 | 2012-05-29 | Abbott Laboratories | Triazolopyridazines |
FR2919870B1 (fr) | 2007-08-09 | 2014-05-16 | Sanofi Aventis | Nouveaux derives de 6-triazolopyridazine-sulfanyl benzothiazole et benzothiazole et benzimidazole, procede, compositions pharmaceutiques et nouvelle utilisation comme inhibiteurs de cmet |
PA8792501A1 (es) * | 2007-08-09 | 2009-04-23 | Sanofi Aventis | Nuevos derivados de 6-triazolopiridacina-sulfanil benzotiazol y bencimidazol,su procedimiento de preparación,su aplicación como medicamentos,composiciones farmacéuticas y nueva utilización principalmente como inhibidores de met. |
NZ586913A (en) | 2007-12-21 | 2012-06-29 | Astrazeneca Ab | Bicyclic derivatives for use in the treatment of androgen receptor associated conditions |
AU2010247190A1 (en) | 2009-05-11 | 2011-11-10 | Astrazeneca Ab | [1,2,4] triazolo [4,3-b] pyridazines as ligands of the androgen receptor |
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2010
- 2010-02-08 EP EP10703945.5A patent/EP2396333B1/en active Active
- 2010-02-08 PE PE2011001469A patent/PE20120603A1/es not_active Application Discontinuation
- 2010-02-08 JP JP2011549665A patent/JP5059977B2/ja active Active
- 2010-02-08 ES ES10703945T patent/ES2427917T3/es active Active
- 2010-02-08 CA CA2749926A patent/CA2749926A1/en not_active Abandoned
- 2010-02-08 EA EA201101180A patent/EA019647B1/ru not_active IP Right Cessation
- 2010-02-08 KR KR1020117019968A patent/KR20110113755A/ko not_active Application Discontinuation
- 2010-02-08 AU AU2010212590A patent/AU2010212590B2/en not_active Ceased
- 2010-02-08 MX MX2011008452A patent/MX2011008452A/es active IP Right Grant
- 2010-02-08 SG SG2011051034A patent/SG172986A1/en unknown
- 2010-02-08 WO PCT/GB2010/050191 patent/WO2010092371A1/en active Application Filing
- 2010-02-08 CN CN201080016898.1A patent/CN102388048B/zh active Active
- 2010-02-09 UY UY0001032426A patent/UY32426A/es not_active Application Discontinuation
- 2010-02-09 TW TW099104022A patent/TW201033215A/zh unknown
- 2010-02-09 AR ARP100100350A patent/AR075383A1/es unknown
- 2010-02-09 US US12/702,603 patent/US8258140B2/en active Active
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2011
- 2011-07-14 IL IL214112A patent/IL214112A0/en unknown
- 2011-08-09 NI NI201100156A patent/NI201100156A/es unknown
- 2011-08-09 CL CL2011001920A patent/CL2011001920A1/es unknown
- 2011-08-10 SV SV2011003993A patent/SV2011003993A/es unknown
- 2011-08-10 CU CU20110158A patent/CU20110158A7/es unknown
- 2011-08-10 EC EC2011011257A patent/ECSP11011257A/es unknown
- 2011-08-10 DO DO2011000258A patent/DOP2011000258A/es unknown
- 2011-08-10 CR CR20110427A patent/CR20110427A/es unknown
- 2011-08-16 CO CO11103913A patent/CO6410299A2/es not_active Application Discontinuation
- 2011-09-09 ZA ZA2011/06625A patent/ZA201106625B/en unknown
-
2012
- 2012-06-08 HK HK12105648.1A patent/HK1164870A1/xx not_active IP Right Cessation
- 2012-08-01 US US13/564,029 patent/US20130203714A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
JP5059977B2 (ja) | 2012-10-31 |
TW201033215A (en) | 2010-09-16 |
ECSP11011257A (es) | 2011-09-30 |
US20100267699A1 (en) | 2010-10-21 |
CN102388048A (zh) | 2012-03-21 |
DOP2011000258A (es) | 2011-09-30 |
SG172986A1 (en) | 2011-08-29 |
EP2396333A1 (en) | 2011-12-21 |
NI201100156A (es) | 2012-03-19 |
IL214112A0 (en) | 2011-08-31 |
JP2012517462A (ja) | 2012-08-02 |
US20130203714A1 (en) | 2013-08-08 |
MX2011008452A (es) | 2011-12-16 |
HK1164870A1 (en) | 2012-09-28 |
CN102388048B (zh) | 2014-07-30 |
EA201101180A1 (ru) | 2012-03-30 |
ZA201106625B (en) | 2013-02-27 |
AU2010212590B2 (en) | 2013-01-10 |
US8258140B2 (en) | 2012-09-04 |
CO6410299A2 (es) | 2012-03-30 |
SV2011003993A (es) | 2012-01-06 |
WO2010092371A1 (en) | 2010-08-19 |
CR20110427A (es) | 2011-09-21 |
PE20120603A1 (es) | 2012-06-14 |
AU2010212590A1 (en) | 2011-08-04 |
KR20110113755A (ko) | 2011-10-18 |
ES2427917T3 (es) | 2013-11-04 |
CL2011001920A1 (es) | 2011-10-21 |
EP2396333B1 (en) | 2013-07-03 |
EA019647B1 (ru) | 2014-05-30 |
CA2749926A1 (en) | 2010-08-19 |
UY32426A (es) | 2010-09-30 |
CU20110158A7 (es) | 2012-02-15 |
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