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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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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
JP5639895B2 (ja) 2007-12-27 2014-12-10 インフィニティ ファーマスーティカルズ、インク. 立体選択的還元方法
US20100297118A1 (en) * 2007-12-27 2010-11-25 Macdougall John Therapeutic Cancer Treatments
KR20100137416A (ko) * 2007-12-27 2010-12-30 인피니티 파마슈티칼스, 인코포레이티드 암 치료법
GB0813740D0 (en) * 2008-07-28 2008-09-03 Angeletti P Ist Richerche Biologica Therapeutic compounds
AU2009286528B2 (en) * 2008-08-29 2014-07-17 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
CN105492011A (zh) 2013-04-08 2016-04-13 丹尼斯·M·布朗 不理想给药化学化合物的治疗增效
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
MX387917B (es) 2015-06-04 2025-03-19 Pellepharm Inc Formulaciones topicas para suministrar compuestos inhibidores de hedgehog y uso de los mismos.
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
US7329683B2 (en) 2002-02-01 2008-02-12 Merck & Co., Inc. 11-β-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
JO2397B1 (en) * 2002-12-20 2007-06-17 ميرك شارب اند دوم كوربوريشن Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors
WO2004106294A2 (en) 2003-05-29 2004-12-09 Merck & Co., Inc. Triazole derivatives as inhibitors of 11-beta hydroxysteroid dehydrogenase-1
WO2005033288A2 (en) 2003-09-29 2005-04-14 The Johns Hopkins University Hedgehog pathway antagonists
WO2006078283A2 (en) 2004-04-30 2006-07-27 Genentech, Inc. Quinoxaline inhibitors of hedgehog signalling
WO2006017542A1 (en) 2004-08-06 2006-02-16 Merck & Co., Inc. Sulfonyl compounds as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
ES2578728T3 (es) 2004-08-27 2016-07-29 Infinity Pharmaceuticals, Inc. Proceso para la preparación de compuestos análogos de ciclopamina
KR20130083488A (ko) 2004-09-02 2013-07-22 제넨테크, 인크. 헤지호그 신호전달에 대한 피리딜 억제제
US20090209573A1 (en) 2004-10-28 2009-08-20 Irm Llc Compounds and compositions as hedgehog pathway modulators
EP1807074B1 (en) 2004-11-03 2013-10-23 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
NI200800069A (es) * 2005-10-20 2008-06-25 Merck & Co Inc Derivados de triazol como inhibidores de 11-beta-hidroxiesteroide-deshidrogenasa-1

Also Published As

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

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