PE20090806A1 - Derivados de triazol que son antagonistas de smo - Google Patents

Derivados de triazol que son antagonistas de smo

Info

Publication number
PE20090806A1
PE20090806A1 PE2008000654A PE2008000654A PE20090806A1 PE 20090806 A1 PE20090806 A1 PE 20090806A1 PE 2008000654 A PE2008000654 A PE 2008000654A PE 2008000654 A PE2008000654 A PE 2008000654A PE 20090806 A1 PE20090806 A1 PE 20090806A1
Authority
PE
Peru
Prior art keywords
ilo
methyl
triazol
oxadiazole
bicycle
Prior art date
Application number
PE2008000654A
Other languages
English (en)
Inventor
James M Balkovec
Sherman T Waddell
Rolf Thieringer
Original Assignee
Merck & Co Inc
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 Merck & Co Inc filed Critical Merck & Co Inc
Publication of PE20090806A1 publication Critical patent/PE20090806A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245Oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

REFERIDA A UN DERIVADO DE TRIAZOL DE FORMULA (I), DONDE DOS DE X, Y, Z SON N Y EL OTRO ES O; R1 Y R2 JUNTOS FORMAN CICLOBUTILO OPCIONALMENTE SUSTITUIDO CON FLUOR Y R3 ES H O F; O R1 ES METILO, R2 ES METILO O FLUOR Y R3 ES F. SON COMPUESTOS PREFERIDOS: 5-(1,1-DIFLUOROETIL)-3-(4-{4-METIL-5-[2-(TRIFLUOROMETIL)FENIL]-4H-1,2,4-TRIAZOL-3-ILO}BICICLO[2.2.2]OCT-1-ILO)-1,2,4-OXADIAZOL, 5-(3,3-DIFLUOROCICLOBUTIL)-3-(4-{4-METIL-5-[2-(TRIFLUOROMETIL)FENIL]-4H-1,2,4-TRIAZOL-3-ILO}BICICLO[2.2.2]OCT-1-ILO)-1,2,4-OXADIAZOL, 5-(1-FLUORO-1-METILETIL)-3-(4-{4-METIL-5-[2-(TRIFLUOROMETIL)FENIL]-4H-1,2,4-TRIAZOL-3-ILO}BICICLO[2.2.2]OCT-1-ILO)-1,2,4-OXADIAZOL, ENTRE OTROS. DICHOS COMPUESTOS INHIBEN LA VIA DE TRANSDUCCION DE SENALES DE HEDGEHOG SONIC, PARTICULARMENTE SMOTHENED (Smo) Y SON UTILES EN EL TRATAMIENTO DE CANCERES DE PROSTATA, PANCREATICOS, DE HUESOS, ENTRE OTROS
PE2008000654A 2007-04-18 2008-04-15 Derivados de triazol que son antagonistas de smo PE20090806A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US92501807P 2007-04-18 2007-04-18

Publications (1)

Publication Number Publication Date
PE20090806A1 true PE20090806A1 (es) 2009-06-27

Family

ID=39433852

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000654A PE20090806A1 (es) 2007-04-18 2008-04-15 Derivados de triazol que son antagonistas de smo

Country Status (12)

Country Link
US (1) US7691887B2 (es)
EP (1) EP2136803B1 (es)
JP (1) JP5498936B2 (es)
CN (1) CN101663033B (es)
AR (1) AR066063A1 (es)
AT (1) ATE555785T1 (es)
AU (1) AU2008241527B2 (es)
CA (1) CA2683946C (es)
CL (1) CL2008001074A1 (es)
PE (1) PE20090806A1 (es)
TW (1) TW200901987A (es)
WO (1) WO2008130552A1 (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI433674B (zh) 2006-12-28 2014-04-11 Infinity Discovery Inc 環杷明(cyclopamine)類似物類
KR20100137416A (ko) * 2007-12-27 2010-12-30 인피니티 파마슈티칼스, 인코포레이티드 암 치료법
CN101917853B (zh) 2007-12-27 2014-03-19 无限药品股份有限公司 立体选择性还原的方法
US20100297118A1 (en) * 2007-12-27 2010-11-25 Macdougall John Therapeutic Cancer Treatments
GB0813740D0 (en) * 2008-07-28 2008-09-03 Angeletti P Ist Richerche Biologica Therapeutic compounds
EP2334683B1 (en) * 2008-08-29 2017-03-22 MSD Italia S.r.l. Saturated bicyclic heterocyclic derivatives as smo antagonists
CA2769795C (en) 2009-08-05 2020-01-07 Infinity Pharmaceuticals, Inc. Enzymatic transamination of cyclopamine analogs
WO2011063309A1 (en) * 2009-11-20 2011-05-26 Infinity Pharmaceuticals, Inc. Methods and compositions for treating hedgehog-associated cancers
US9376447B2 (en) 2010-09-14 2016-06-28 Infinity Pharmaceuticals, Inc. Transfer hydrogenation of cyclopamine analogs
KR20160061911A (ko) 2013-04-08 2016-06-01 데니스 엠. 브라운 최적하 투여된 화학 화합물의 치료 효과
CN104324039A (zh) * 2014-10-20 2015-02-04 付茜 一种治疗人身体表面脂肪瘤的药剂及使用方法
AU2016271468B2 (en) 2015-06-04 2020-01-02 Sol-Gel Technologies Ltd. Topical formulations for delivery of hedgehog inhibitor compounds and use thereof
CN108623446A (zh) * 2017-03-24 2018-10-09 北京艾德旺科技发展有限公司 一种合成3,3-二氟环丁烷甲酸的方法

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7291626B1 (en) 1998-04-09 2007-11-06 John Hopkins University School Of Medicine Inhibitors of hedgehog signaling pathways, compositions and uses related thereto
JP4368683B2 (ja) 2002-02-01 2009-11-18 メルク エンド カムパニー インコーポレーテッド 糖尿病、肥満症および脂質代謝異常の治療に有用な11−ベータ−ヒドロキシステロイドデヒドロゲナーゼ1阻害剤
JO2397B1 (en) 2002-12-20 2007-06-17 ميرك شارب اند دوم كوربوريشن Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors
JP4499106B2 (ja) 2003-05-29 2010-07-07 メルク・シャープ・エンド・ドーム・コーポレイション 11−ベータ−水酸化ステロイド脱水素酵素−1の阻害剤としてのトリアゾール誘導体
US8067608B2 (en) 2003-09-29 2011-11-29 The Johns Hopkins University Hedgehog pathway antagonists
CN101018783B (zh) 2004-04-30 2012-11-21 遗传技术研究公司 Hedgehog信号传导途径的喹喔啉抑制剂
ATE472531T1 (de) 2004-08-06 2010-07-15 Merck Sharp & Dohme Sulfonylverbindungen als hemmer von 11-beta- hydroxysteroiddehydrogenase-1
BRPI0514444A (pt) 2004-08-27 2008-06-10 Infinity Pharmaceuticals Inc análogos de ciclopamina e métodos de uso destes
CN102964294A (zh) 2004-09-02 2013-03-13 遗传技术研究公司 Hedgehog信号转导的吡啶基抑制剂
KR20070083836A (ko) 2004-10-28 2007-08-24 아이알엠 엘엘씨 헷지혹 경로 조절제로서의 화합물 및 조성물
NZ555419A (en) 2004-11-03 2009-07-31 Curis Inc Mediators of the hedgehog gene signaling pathways, compositions and uses related thereto
EP1940393B1 (en) * 2005-10-20 2012-07-25 Merck Sharp & Dohme Corp. Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1

Also Published As

Publication number Publication date
CA2683946C (en) 2013-01-22
WO2008130552A1 (en) 2008-10-30
US7691887B2 (en) 2010-04-06
JP2010524937A (ja) 2010-07-22
AU2008241527A1 (en) 2008-10-30
ATE555785T1 (de) 2012-05-15
CL2008001074A1 (es) 2009-06-05
EP2136803A1 (en) 2009-12-30
CA2683946A1 (en) 2008-10-30
EP2136803B1 (en) 2012-05-02
US20080262051A1 (en) 2008-10-23
CN101663033A (zh) 2010-03-03
JP5498936B2 (ja) 2014-05-21
AR066063A1 (es) 2009-07-22
CN101663033B (zh) 2013-01-16
TW200901987A (en) 2009-01-16
AU2008241527B2 (en) 2014-02-13

Similar Documents

Publication Publication Date Title
PE20090806A1 (es) Derivados de triazol que son antagonistas de smo
PE20030200A1 (es) Bencimidazol como inhibidores de las map quinasas
PE20061038A1 (es) Derivados del 1,5-difenil-1h-pirazol-3-il) oxadiazol como agentes antagonistas cb1 y su preparacion
NZ602099A (en) Stat3 inhibitor containing quinolinecarboxamide derivative as active ingredient
PE20070460A1 (es) Derivados de carboxamida como antagonista del receptor muscarinico
PE20040936A1 (es) Derivados de triazol como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1
JP2015533157A5 (es)
JP2005536458A5 (es)
PE20081704A1 (es) Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta-9 desaturasa
PE20110235A1 (es) Combinaciones farmaceuticas que comprenden linagliptina y metmorfina
PE20051173A1 (es) Compuestos azabiciclico (3.1.0) hexanos como moduladores de receptores de dopamina d3
PE20080545A1 (es) Isoxazolinas insecticidas
RU2009118602A (ru) Производное индола
JP2006517220A5 (es)
PE20110308A1 (es) 1,2,5-oxadiazoles como inhibidores de indolamina 2,3-dioxigenasa
PE20070427A1 (es) Compuestos derivados de benzimidazoles sustituidos como inhibidores de tirosina quinasas
PE20090974A1 (es) Mezclas fungicidas
PE20040649A1 (es) Procedimiento para la preparacion de benzoilureas heterociclicamente sustituidas
PE20091523A1 (es) Derivados de tiazol como inhibidores de la enzima fosfatidilinositol 3-cinasa (pi3k)
PE20060729A1 (es) Compuestos heterociclicos como moduladores o inhibidores de la actividad de miostatina
NZ598685A (en) Heterocylcic derivatives as inhibitors of glutaminyl cyclase
PE20081378A1 (es) Derivados de 1,2,4-triazol como moduladores de mglur5
EA200900913A1 (ru) Производное триазола в качестве ингибитора hsp90
RU2014107463A (ru) Селективные ингибиторы протеинкиназ
PE20070640A1 (es) Compuestos derivados de pirazol-isoquinolina urea como inhibidores de la cinasa p38

Legal Events

Date Code Title Description
FC Refusal