ECSP11011257A - Derivados de triazolo [4,3-b] piridazina y sus usos para el cáncer de próstata - Google Patents

Derivados de triazolo [4,3-b] piridazina y sus usos para el cáncer de próstata

Info

Publication number
ECSP11011257A
ECSP11011257A EC2011011257A ECSP11011257A ECSP11011257A EC SP11011257 A ECSP11011257 A EC SP11011257A EC 2011011257 A EC2011011257 A EC 2011011257A EC SP11011257 A ECSP11011257 A EC SP11011257A EC SP11011257 A ECSP11011257 A EC SP11011257A
Authority
EC
Ecuador
Prior art keywords
prostate cancer
piridazine
triazol derivatives
relates
triazol
Prior art date
Application number
EC2011011257A
Other languages
English (en)
Inventor
Gregory Richard Carr
Robert Hugh Bradbury
Alfred Arthur Rabow
Korupoju Srinivasa Rao
Harikrishna Tumma
Original Assignee
Astrazeneca
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Astrazeneca filed Critical Astrazeneca
Publication of ECSP11011257A publication Critical patent/ECSP11011257A/es

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La invención se refiere a compuestos bicíclicos de Fórmula I; en donde , R1, R2, L1, L2, J, Y, k, n, p y r son tal como se definen en la descripción. La presente invención también se refiere a procesos para la preparación de dichos compuestos, composiciones farmacéuticas que los contienen y su uso en el tratamiento de afecciones asociadas con el receptor de andrógenos, en particular el cáncer de próstata.
EC2011011257A 2009-02-10 2011-08-10 Derivados de triazolo [4,3-b] piridazina y sus usos para el cáncer de próstata ECSP11011257A (es)

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
ECSP11011257A true ECSP11011257A (es) 2011-09-30

Family

ID=42115693

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2011011257A ECSP11011257A (es) 2009-02-10 2011-08-10 Derivados de triazolo [4,3-b] piridazina y sus usos para el cáncer de próstata

Country Status (26)

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)
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 (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2010247190A1 (en) * 2009-05-11 2011-11-10 Astrazeneca Ab [1,2,4] triazolo [4,3-b] pyridazines as ligands of the androgen receptor
HRP20191982T4 (hr) 2011-11-30 2023-01-06 Astrazeneca Ab Kombinacijsko liječenje 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
US9745253B2 (en) 2015-03-13 2017-08-29 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
US10722527B2 (en) 2015-04-10 2020-07-28 Capsugel Belgium Nv Abiraterone acetate lipid formulations
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
AU2020266604A1 (en) * 2019-05-02 2021-11-18 Constellation Pharmaceuticals, Inc. Modulators of TREX1
US20220218701A1 (en) * 2019-05-31 2022-07-14 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
WO2024137968A1 (en) * 2022-12-21 2024-06-27 Capulus Therapeutics, Llc Androgen receptor modulators and methods for their use

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5411981A (en) * 1991-01-09 1995-05-02 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
USRE35956E (en) * 1991-01-09 1998-11-10 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
FR2693461B1 (fr) 1992-07-08 1994-09-02 Roussel Uclaf Nouvelles phénylimidazolidines substituées, leur procédé de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant.
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
DE69720965T2 (de) 1996-02-13 2004-02-05 Astrazeneca Ab Chinazolinderivate und deren verwendung als vegf hemmer
NZ331191A (en) 1996-03-05 2000-03-27 Zeneca Ltd 4-anilinoquinazoline derivatives and pharmaceutical compositions thereof
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
PT1154774E (pt) 1999-02-10 2005-10-31 Astrazeneca Ab Derivados de quinazolina como inibidores de angiogenese
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
AU2001258628A1 (en) 2000-05-31 2001-12-11 Astrazeneca Ab Indole derivatives with vascular damaging activity
UA73993C2 (uk) 2000-06-06 2005-10-17 Астразенека Аб Хіназолінові похідні для лікування пухлин та фармацевтична композиція
MXPA02012903A (es) 2000-07-07 2004-07-30 Angiogene Pharm Ltd Derivados de colquinol como inhibidores de angiogenesis.
MXPA02012905A (es) 2000-07-07 2004-07-30 Angiogene Pharm Ltd Derivados de colquinol como agentes de dano vascular..
SI1474420T1 (sl) 2002-02-01 2012-06-29 Astrazeneca Ab Spojine kinazolina
US20040102360A1 (en) * 2002-10-30 2004-05-27 Barnett Stanley F. Combination therapy
US20050124625A1 (en) 2003-10-21 2005-06-09 Salvati Mark E. Piperazine derivatives and their use as modulators of nuclear hormone receptor function
US7388027B2 (en) 2004-03-04 2008-06-17 Bristol-Myers Squibb Company Bicyclic compounds as modulators of androgen receptor function and method
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
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
US7572807B2 (en) * 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
KR20080080584A (ko) * 2005-11-30 2008-09-04 버텍스 파마슈티칼스 인코포레이티드 ｃ-Ｍｅｔ의 억제제 및 이의 용도
JP5171649B2 (ja) 2006-02-10 2013-03-27 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 選択的アンドローゲン受容体モジュレーターとして有用な、二環式イミダゾール又はチアジアゾール複素環
EP1991223B1 (en) 2006-02-10 2010-07-14 Janssen Pharmaceutica, N.V. Novel imidazolopyrazole derivatives useful as selective androgen receptor modulators
CA2651979A1 (en) * 2006-05-30 2007-12-06 Pfizer Products Inc. Triazolopyridazine derivatives
AU2007279595A1 (en) 2006-08-04 2008-02-07 Takeda Pharmaceutical Company Limited Fused heterocyclic derivative and use thereof
JP2010503648A (ja) * 2006-09-14 2010-02-04 アストラゼネカ アクチボラグ 増殖性疾患の治療のためのｐｉ３ｋ及びｍｔｏｒ阻害剤としての２−ベンゾイミダゾリル−６−モルホリノ−４−（アゼチジン、ピロリジン、ピペリジン、又はアゼピン）ピリミジン誘導体
WO2008044033A1 (en) 2006-10-11 2008-04-17 Astrazeneca Ab Amide derivatives
KR101083177B1 (ko) * 2006-10-23 2011-11-11 에스지엑스 파마슈티컬스, 인코포레이티드 트리아졸로-피리다진 단백질 키나제 조정제
WO2008109104A1 (en) * 2007-03-07 2008-09-12 The Regents Of The University Of California Bivalent inhibitors of akt protein kinase
WO2009005675A1 (en) 2007-06-28 2009-01-08 Abbott Laboratories Novel triazolopyridazines
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.
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
CA2709514A1 (en) 2007-12-21 2009-07-02 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

Also Published As

Publication number Publication date
AU2010212590A1 (en) 2011-08-04
DOP2011000258A (es) 2011-09-30
HK1164870A1 (en) 2012-09-28
US8258140B2 (en) 2012-09-04
ZA201106625B (en) 2013-02-27
CU20110158A7 (es) 2012-02-15
EA201101180A1 (ru) 2012-03-30
JP2012517462A (ja) 2012-08-02
UY32426A (es) 2010-09-30
CO6410299A2 (es) 2012-03-30
SG172986A1 (en) 2011-08-29
JP5059977B2 (ja) 2012-10-31
EA019647B1 (ru) 2014-05-30
IL214112A0 (en) 2011-08-31
ES2427917T3 (es) 2013-11-04
PE20120603A1 (es) 2012-06-14
AR075383A1 (es) 2011-03-30
MX2011008452A (es) 2011-12-16
SV2011003993A (es) 2012-01-06
CL2011001920A1 (es) 2011-10-21
CN102388048A (zh) 2012-03-21
WO2010092371A1 (en) 2010-08-19
US20100267699A1 (en) 2010-10-21
CR20110427A (es) 2011-09-21
TW201033215A (en) 2010-09-16
CN102388048B (zh) 2014-07-30
CA2749926A1 (en) 2010-08-19
AU2010212590B2 (en) 2013-01-10
NI201100156A (es) 2012-03-19
EP2396333B1 (en) 2013-07-03
KR20110113755A (ko) 2011-10-18
EP2396333A1 (en) 2011-12-21
US20130203714A1 (en) 2013-08-08

Similar Documents

Publication Publication Date Title
ECSP11011257A (es) Derivados de triazolo [4,3-b] piridazina y sus usos para el cáncer de próstata
CR20110610A (es) Nuevos derivados de pirimidina y sus usos en el tratamiento del cáncer y otras enfermedades
UY32611A (es) Compuestos de 1-cianoetilheterociclilcarboxamida sustituidos 750
GT201300137A (es) Derivados de imidazo [1,2-b] piridazina e imidazo [4,5-b] piridina como inhibidores de jak
CO6612210A2 (es) Conjugados de dimeros de pirrolo(1.4) benzodiazepina como agentes anticancerosos
AR091837A1 (es) Compuestos para inmunoterapia dirigida
ECSP11011390A (es) Compuestos espiro-amidas sustituidas
UY33503A (es) Imidazo [1,2-a]pirimidinas y piridinas sustituidas
CL2012001714A1 (es) Compuestos derivados de pirrol[3.4-b]piridin-5-ona, inhibidores de pi3k; composicion farmaceutica que los comprende; y uso para el tratamiento de enfermedades tales como alzheimer, epilepsia, esclerosis multiple, parkinson, entre otras.
CL2007001711A1 (es) Compuestos derivados de pirazolopiridina sustituida;composicion farmaceutica que los comprende;metodo de preparacion de los compuestos ,compuestos intermediarios;y su uso en el tratamiento de enfermedades,tales como tumores,artritis reumatoide,enfermedades del crecimiento vascular desregulado, entre otras.
UY32918A (es) Nuevos compuestos de 2-piridona
UY31905A (es) Derivados de benzoxazinona, procesos de preparación, composiciones farmacéuticas conteniéndolos y aplicaciones.
HN2012000261A (es) Derivados de 5-fluoro-2-oxopirimidina-1(2h)-carboxilato
CU20110205A7 (es) [1,2,4] triazolo [4,3-b] piridazinas como ligandos del receptor de andrógenos
CO6341625A2 (es) Derivados de indol como agentes anticáncer
UY32744A (es) Derivados de 2-carboxamida-7-piperazinil-benzofurano 774
CL2012000478A1 (es) Formas cristalinas de 4,5,6,7-tetrahidro-11-metoxi-2-[(4-metil-1-piperazinil)metil]-1h-ciclopenta[alfa]pirrolo[3,4-c]carbazol-1,3(2h)-diona; composicion farmaceutica; y uso en el tratamiento de cancer.
CL2011001850A1 (es) Uso de un compuesto nitrogenado heterociclico sustituido para el tratamiento de cánceres tales como cáncer de colon o mieloma múltiple;composición farmacéutica que comprende al compuesto.
PY1132289A (es) DERIVADOS DE 6,7-DIHIDRO-3H-OXAZOLO [3,4-a] PIRAZIN-5,8-DIONA Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
UY32154A (es) Derivados de isoquinolinona, procesos para su preparacion, composiciones farmaceuticas que los contiene y su uso en terapia
UY32412A (es) DERIVADOS DE 4-AMINO-7,8-DIHIDROPIRIMIDO [4,3-d] PIRIMIDIN-5 (6H)-ONA
CR11640A (es) Derivados de azetidina y ciclobutano como inhibidores de jak