PE20120603A1 - Derivados de triazolo[4,3-b]piridazina y sus usos para el cancer de prostata - Google Patents

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

Info

Publication number
PE20120603A1
PE20120603A1 PE2011001469A PE2011001469A PE20120603A1 PE 20120603 A1 PE20120603 A1 PE 20120603A1 PE 2011001469 A PE2011001469 A PE 2011001469A PE 2011001469 A PE2011001469 A PE 2011001469A PE 20120603 A1 PE20120603 A1 PE 20120603A1
Authority
PE
Peru
Prior art keywords
triazolo
pyridazine
dihydro
prostate cancer
compounds
Prior art date
Application number
PE2011001469A
Other languages
English (en)
Inventor
Robert Hugh Bradbury
Gregory Richard Carr
Alfred Arthur Rabow
Korupoju Srinivasa Rao
Harikrishna Tumma
Original Assignee
Astrazeneca Ab
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 Ab filed Critical Astrazeneca Ab
Publication of PE20120603A1 publication Critical patent/PE20120603A1/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

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE TRIAZOLO[4,3-b]PIRIDAZINA DE FORMULA (I) DONDE R1 ES HALOALQUILO(C1-C4); k ES DE 0 A 2; n Y p SON CADA UNO 1 O 2; Y ES N, C, CH O COH; LAS LINEAS PUNTEADAS SON UN ENLACE SIMPLE O DOBLE; L1 ES UN ENLACE DIRECTO, -(CR3R4)t-, -S-, -S(O)-, ENTRE OTROS, EN DONDE R3 Y R4 SON CADA UNO H O METILO; t ES DE 1 A 3; J ES ARILO, CICLOALQUILO(C3-C6), UN ANILLO HETEROCICLICO DE 4 A 7 MIEMBROS, ENTRE OTROS; L2 ES UN ENLACE DIRECTO, -S(O)-, -S(O)2-, ENTRE OTROS; R2 ES HALO, ALQUILO(C1-C6), CARBOXI, CN, AMINO, ENTRE OTROS; r ES DE 0 A 3. SON COMPUESTOS PREFERIDOS: 6-[4-(4-FLUOROBENCIL)PIPERAZIN-1-IL]-3-(TRIFLUOROMETIL)-7,8-DIHIDRO[1,2,4]TRIAZOLO[4,3-b]PIRIDAZINA; 6-[4-(1H-INDOL-3-IL)-3,6-DIHIDROPIRIDIN-1(2H)-IL]-3-(TRIFLUOROMETIL)-7,8-DIHIDRO[1,2,4]TRIAZOLO[4,3-b]PIRIDAZINA; 6-(4-{4-[2-(4-ACETILPIPERAZIN-1-IL)ETOXI]FENIL}PIPERIDIN-1-IL)-3-(TRIFLUOROMETIL)-7,8-DIHIDRO[1,2,4]TRIAZOLO[4,3-b]PIRIDAZINA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON LIGANDOS DEL RECEPTOR DE ANDROGENOS (AR) SIENDO UTILES EN EL TRATAMIENTO DE CANCER DE PROSTATA
PE2011001469A 2009-02-10 2010-02-08 Derivados de triazolo[4,3-b]piridazina y sus usos para el cancer de prostata PE20120603A1 (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
PE20120603A1 true PE20120603A1 (es) 2012-06-14

Family

ID=42115693

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2011001469A PE20120603A1 (es) 2009-02-10 2010-02-08 Derivados de triazolo[4,3-b]piridazina y sus usos para el cancer de prostata

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2759884A1 (en) * 2009-05-11 2010-11-18 Astrazeneca Ab [1,2,4] triazolo [4,3-b] pyridazines as ligands of the androgen receptor
DK2785349T4 (da) 2011-11-30 2023-01-09 Astrazeneca Ab Kombinationsbehandling af cancer
AU2013204533B2 (en) 2012-04-17 2017-02-02 Astrazeneca Ab Crystalline forms
LT2894151T (lt) 2012-09-04 2021-09-10 Shanghai Hengrui Pharmaceutical Co. Ltd. Imidazolino dariniai, jų gamybos būdai ir jų naudojimas medicinoje
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
CR20170420A (es) 2015-03-13 2017-10-03 Forma Therapeutics Inc Compuestos y composiciones de alfa-cinamida como inhibidores de hdac8
EP3285764B1 (en) 2015-03-31 2024-03-27 University of Vermont and State Agricultural College Triazolopyridazines for treating cryptosporidiosis
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
CN114341125A (zh) * 2019-05-02 2022-04-12 星座制药公司 Trex1调节剂
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
US20220227771A1 (en) * 2020-12-30 2022-07-21 Industrial Technology Research Institute Androgen receptor binding molecule and use thereof
CA3217423A1 (en) 2021-06-16 2022-12-22 Jeffrey M. Schkeryantz Azetidinyl compounds comprising a carboxylic acid group for the treatment of neurodegenerative diseases

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
JP4471404B2 (ja) 1996-02-13 2010-06-02 アストラゼネカ ユーケイ リミテッド Ｖｅｇｆインヒビターとしてのキナゾリン誘導体
PT885198E (pt) 1996-03-05 2002-06-28 Astrazeneca Ab Derivados de 4-anilinoquinazolina
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
KR100838617B1 (ko) 1999-02-10 2008-06-16 아스트라제네카 아베 혈관형성 억제제로서의 퀴나졸린 유도체
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
BR0111230A (pt) 2000-05-31 2003-06-10 Astrazeneca Ab Composto, e, uso e processo para a preparação do mesmo
UA73993C2 (uk) 2000-06-06 2005-10-17 Астразенека Аб Хіназолінові похідні для лікування пухлин та фармацевтична композиція
AU2001266233B2 (en) 2000-07-07 2006-06-29 Angiogene Pharmaceuticals Limited Colchinol derivatives as vascular damaging agents
CZ200331A3 (cs) 2000-07-07 2003-04-16 Angiogene Pharmaceuticals Limited Deriváty kolchinolu jako inhibitory angiogeneze, způsob jejich přípravy a farmaceutická kompozice, která je obsahuje
ES2381781T3 (es) 2002-02-01 2012-05-31 Astrazeneca Ab Compuestos de quinazolina
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
CA2582447C (en) * 2004-10-01 2012-04-17 Merck & Co., Inc. Aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
US7572807B2 (en) 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
NZ568666A (en) * 2005-11-30 2011-09-30 Vertex Pharma [1,2,4]Triazolo[3,4-b][1,3,4]thiadiazole derivative as inhibitors of c-Met
CA2642205C (en) 2006-02-10 2015-01-27 Janssen Pharmaceutica N.V. Bicyclic imidazole or thiadiazole heterocycles useful as selective androgen receptor modulators
EP1991223B1 (en) 2006-02-10 2010-07-14 Janssen Pharmaceutica, N.V. Novel imidazolopyrazole derivatives useful as selective androgen receptor modulators
WO2007138472A2 (en) * 2006-05-30 2007-12-06 Pfizer Products Inc. Triazolopyridazine derivatives
TW200817409A (en) 2006-08-04 2008-04-16 Takeda Pharmaceutical Fused heterocyclic derivative and use thereof
CN101563339A (zh) * 2006-09-14 2009-10-21 阿斯利康(瑞典)有限公司 作为 p i 3 k和 m t o r抑制剂用于治疗增殖性疾病的 2 -苯并咪唑基 - 6 -吗啉代 - 4 - (氮杂环丁烷、吡咯烷、哌啶或氮杂)嘧啶衍生物
WO2008044033A1 (en) 2006-10-11 2008-04-17 Astrazeneca Ab Amide derivatives
AU2007309237B2 (en) * 2006-10-23 2012-03-22 Sgx Pharmaceuticals, Inc. Triazolo-pyridazine protein kinase modulators
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
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.
EP2235010A1 (en) 2007-12-21 2010-10-06 AstraZeneca AB Bicyclic derivatives for use in the treatment of androgen receptor associated conditions
CA2759884A1 (en) 2009-05-11 2010-11-18 Astrazeneca Ab [1,2,4] triazolo [4,3-b] pyridazines as ligands of the androgen receptor

Also Published As

Publication number Publication date
ECSP11011257A (es) 2011-09-30
AR075383A1 (es) 2011-03-30
MX2011008452A (es) 2011-12-16
AU2010212590B2 (en) 2013-01-10
TW201033215A (en) 2010-09-16
US20100267699A1 (en) 2010-10-21
DOP2011000258A (es) 2011-09-30
JP2012517462A (ja) 2012-08-02
HK1164870A1 (en) 2012-09-28
AU2010212590A1 (en) 2011-08-04
CL2011001920A1 (es) 2011-10-21
US8258140B2 (en) 2012-09-04
WO2010092371A1 (en) 2010-08-19
CO6410299A2 (es) 2012-03-30
NI201100156A (es) 2012-03-19
CU20110158A7 (es) 2012-02-15
US20130203714A1 (en) 2013-08-08
UY32426A (es) 2010-09-30
EP2396333B1 (en) 2013-07-03
EA019647B1 (ru) 2014-05-30
ZA201106625B (en) 2013-02-27
EP2396333A1 (en) 2011-12-21
CN102388048B (zh) 2014-07-30
CN102388048A (zh) 2012-03-21
CR20110427A (es) 2011-09-21
ES2427917T3 (es) 2013-11-04
KR20110113755A (ko) 2011-10-18
JP5059977B2 (ja) 2012-10-31
EA201101180A1 (ru) 2012-03-30
IL214112A0 (en) 2011-08-31
CA2749926A1 (en) 2010-08-19
SV2011003993A (es) 2012-01-06
SG172986A1 (en) 2011-08-29

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