EA201101180A1 - Производные триазоло[4,3-в]пиридазина и их применение для рака предстательной железы - Google Patents

Производные триазоло[4,3-в]пиридазина и их применение для рака предстательной железы

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Publication number
EA201101180A1
EA201101180A1 EA201101180A EA201101180A EA201101180A1 EA 201101180 A1 EA201101180 A1 EA 201101180A1 EA 201101180 A EA201101180 A EA 201101180A EA 201101180 A EA201101180 A EA 201101180A EA 201101180 A1 EA201101180 A1 EA 201101180A1
Authority
EA
Eurasian Patent Office
Prior art keywords
prostate cancer
pyridazin
triazolo
derivatives
application
Prior art date
Application number
EA201101180A
Other languages
English (en)
Other versions
EA019647B1 (ru
Inventor
Роберт Хью Брэдбери
Грегори Ричард Карр
Алфред Артур Рейбоу
Сриниваза Рао-Коруподжу
Харикришна Тумма
Original Assignee
Астразенека Аб
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 Астразенека Аб filed Critical Астразенека Аб
Publication of EA201101180A1 publication Critical patent/EA201101180A1/ru
Publication of EA019647B1 publication Critical patent/EA019647B1/ru

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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

Изобретение охватывает бициклические соединения формулы (I)где, R, R, L, L, J, Y, k, n, p и r имеют значения, указанные в описании. Настоящее изобретение также относится к способам получения таких соединений, фармацевтическим композициям, которые их содержат, и к их применению для лечения состояний, связанных с андрогеновым рецептором, в особенности рака предстательной железы.
EA201101180A 2009-02-10 2010-02-08 ПРОИЗВОДНЫЕ ТРИАЗОЛО[4,3-b]ПИРИДАЗИНА И ИХ ПРИМЕНЕНИЕ ДЛЯ ЛЕЧЕНИЯ РАКА ПРЕДСТАТЕЛЬНОЙ ЖЕЛЕЗЫ EA019647B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US15122109P 2009-02-10 2009-02-10
US18776609P 2009-06-17 2009-06-17
PCT/GB2010/050191 WO2010092371A1 (en) 2009-02-10 2010-02-08 Triazolo [4,3-b] pyridazine derivatives and their uses for prostate cancer

Publications (2)

Publication Number Publication Date
EA201101180A1 true EA201101180A1 (ru) 2012-03-30
EA019647B1 EA019647B1 (ru) 2014-05-30

Family

ID=42115693

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201101180A EA019647B1 (ru) 2009-02-10 2010-02-08 ПРОИЗВОДНЫЕ ТРИАЗОЛО[4,3-b]ПИРИДАЗИНА И ИХ ПРИМЕНЕНИЕ ДЛЯ ЛЕЧЕНИЯ РАКА ПРЕДСТАТЕЛЬНОЙ ЖЕЛЕЗЫ

Country Status (27)

Country Link
US (2) US8258140B2 (ru)
EP (1) EP2396333B1 (ru)
JP (1) JP5059977B2 (ru)
KR (1) KR20110113755A (ru)
CN (1) CN102388048B (ru)
AR (1) AR075383A1 (ru)
AU (1) AU2010212590B2 (ru)
CA (1) CA2749926A1 (ru)
CL (1) CL2011001920A1 (ru)
CO (1) CO6410299A2 (ru)
CR (1) CR20110427A (ru)
CU (1) CU20110158A7 (ru)
DO (1) DOP2011000258A (ru)
EA (1) EA019647B1 (ru)
EC (1) ECSP11011257A (ru)
ES (1) ES2427917T3 (ru)
HK (1) HK1164870A1 (ru)
IL (1) IL214112A0 (ru)
MX (1) MX2011008452A (ru)
NI (1) NI201100156A (ru)
PE (1) PE20120603A1 (ru)
SG (1) SG172986A1 (ru)
SV (1) SV2011003993A (ru)
TW (1) TW201033215A (ru)
UY (1) UY32426A (ru)
WO (1) WO2010092371A1 (ru)
ZA (1) ZA201106625B (ru)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20120034645A (ko) * 2009-05-11 2012-04-12 아스트라제네카 아베 안드로겐 수용체의 리간드로서 ［１,２,４］트리아졸로［４,３?ｂ］피리다진
CA2856646C (en) 2011-11-30 2020-01-14 Astrazeneca Ab Combination treatment of cancer
AU2013204533B2 (en) 2012-04-17 2017-02-02 Astrazeneca Ab Crystalline forms
RS61242B1 (sr) 2012-09-04 2021-01-29 Shanghai hengrui pharmaceutical co ltd Derivati imidazolina, postupci njihove pripreme i njihove primene u medicini
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 (ru) * 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
WO2016162229A1 (en) 2015-04-10 2016-10-13 Capsugel Belgium N.V. 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
EP3962907A1 (en) * 2019-05-02 2022-03-09 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
IL308122A (en) 2021-06-16 2023-12-01 Celgene Corp Azetidinyl compounds consisting of 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
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.
US5411981A (en) * 1991-01-09 1995-05-02 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
TR199801530T2 (xx) 1996-02-13 1998-11-23 Zeneca Limited VEGF �nhibit�rleri olarak kinazolin t�revleri.
JP4464466B2 (ja) 1996-03-05 2010-05-19 アストラゼネカ・ユーケイ・リミテッド ４―アニリノキナゾリン誘導体
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
CZ306810B6 (cs) 1999-02-10 2017-07-19 Astrazeneca Ab Použití chinazolinového derivátu jako inhibitoru angiogeneze
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
WO2001092224A1 (en) 2000-05-31 2001-12-06 Astrazeneca Ab Indole derivatives with vascular damaging activity
UA73993C2 (ru) 2000-06-06 2005-10-17 Астразенека Аб Хиназолиновые производные для лечения опухолей и фармацевтическая композиция
IL153484A0 (en) 2000-07-07 2003-07-06 Angiogene Pharm Ltd Colchinol derivatives as angiogenesis inhibitors
BR0112225A (pt) 2000-07-07 2003-05-06 Angiogene Pharm Ltd Composto, composição farmacêutica, uso de um composto, e, processo papa preparar um composto
US7268230B2 (en) 2002-02-01 2007-09-11 Astrazeneca Ab Quinazoline compounds
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
AU2005292134B2 (en) * 2004-10-01 2010-12-23 Merck Sharp & Dohme Corp. 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
AU2006320580B2 (en) * 2005-11-30 2011-06-23 Vertex Pharmaceuticals Incorporated Inhibitors of c-Met and uses thereof
DE602007007734D1 (de) 2006-02-10 2010-08-26 Janssen Pharmaceutica Nv Neue imidazolopyrazolderivate als selektive androgen-rezeptor-modulatoren
AU2007215004B2 (en) 2006-02-10 2012-03-01 Janssen Pharmaceutica N.V. Bicyclic imidazole or thiadiazole heterocycles useful as selective androgen receptor modulators
EP2032578A2 (en) * 2006-05-30 2009-03-11 Pfizer Products Incorporated Triazolopyridazine derivatives
JP5238697B2 (ja) 2006-08-04 2013-07-17 武田薬品工業株式会社 縮合複素環誘導体およびその用途
US20100022534A1 (en) * 2006-09-14 2010-01-28 Astrazeneca 2-benzimidazolyl-6-morpholino-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008044033A1 (en) 2006-10-11 2008-04-17 Astrazeneca Ab Amide derivatives
PT2081937E (pt) * 2006-10-23 2012-10-15 Sgx Pharmaceuticals Inc Moduladores de proteína-cinase de triazolo-piridazina
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
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
US8003649B2 (en) * 2007-12-21 2011-08-23 Astrazeneca Ab Bicyclic derivatives for use in the treatment of androgen receptor associated conditions-155
KR20120034645A (ko) 2009-05-11 2012-04-12 아스트라제네카 아베 안드로겐 수용체의 리간드로서 ［１,２,４］트리아졸로［４,３?ｂ］피리다진

Also Published As

Publication number Publication date
EP2396333B1 (en) 2013-07-03
HK1164870A1 (en) 2012-09-28
AR075383A1 (es) 2011-03-30
IL214112A0 (en) 2011-08-31
ES2427917T3 (es) 2013-11-04
CL2011001920A1 (es) 2011-10-21
CU20110158A7 (es) 2012-02-15
KR20110113755A (ko) 2011-10-18
DOP2011000258A (es) 2011-09-30
CN102388048B (zh) 2014-07-30
TW201033215A (en) 2010-09-16
WO2010092371A1 (en) 2010-08-19
AU2010212590B2 (en) 2013-01-10
SG172986A1 (en) 2011-08-29
CR20110427A (es) 2011-09-21
US8258140B2 (en) 2012-09-04
ZA201106625B (en) 2013-02-27
EA019647B1 (ru) 2014-05-30
CN102388048A (zh) 2012-03-21
JP5059977B2 (ja) 2012-10-31
SV2011003993A (es) 2012-01-06
ECSP11011257A (es) 2011-09-30
NI201100156A (es) 2012-03-19
AU2010212590A1 (en) 2011-08-04
PE20120603A1 (es) 2012-06-14
CA2749926A1 (en) 2010-08-19
MX2011008452A (es) 2011-12-16
UY32426A (es) 2010-09-30
US20100267699A1 (en) 2010-10-21
EP2396333A1 (en) 2011-12-21
US20130203714A1 (en) 2013-08-08
CO6410299A2 (es) 2012-03-30
JP2012517462A (ja) 2012-08-02

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