PE20050730A1 - Derivados de 2,5-dihidropirrol 2,2-disustituidos como inhibidores de quinesinas mitoticas - Google Patents

Derivados de 2,5-dihidropirrol 2,2-disustituidos como inhibidores de quinesinas mitoticas

Info

Publication number
PE20050730A1
PE20050730A1 PE2004000762A PE2004000762A PE20050730A1 PE 20050730 A1 PE20050730 A1 PE 20050730A1 PE 2004000762 A PE2004000762 A PE 2004000762A PE 2004000762 A PE2004000762 A PE 2004000762A PE 20050730 A1 PE20050730 A1 PE 20050730A1
Authority
PE
Peru
Prior art keywords
alkyl
methyl
hydroximethyl
pyrrol
difluorophenyl
Prior art date
Application number
PE2004000762A
Other languages
English (en)
Inventor
Paul J Coleman
Christopher D Cox
Robert M Garbaccio
George D Hartman
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 PE20050730A1 publication Critical patent/PE20050730A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632—Organic additives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 2,5-DIHIDROPIRROL 2,2-DISUSTITUIDOS DE FORMULA (I), EN DONDE R1 Y R2 SON INDEPENDIENTEMENTE H, ALQUILO(C1-C6), ARILO Y CICLOALQUILO, OPCIONALMENTE SUSTITUIDOS; R3 ES H, ALQUIL(C1-C10), ALQUIL(C1-C10)-O-Rd, COMO METILHIDROXI, ALQUIL(C1-C10)-(C=O)b-NRcRc', ENTRE OTROS; R4 ES HALO, OH, Ob-PERFLUOROALQUILO(C1-C6), ENTRE OTROS; R5 ES H, HALO, OH, Ob-PERFLUOROALQUILO(C1-C6), ENTRE OTROS; R10 ES F O -CH2F; R13 ES H O -CH2F, CON LA CONDICION DE QUE SI t ES 1, R13 SEA H; Rox ESTA AUSENTE O ES OXO. SON COMPUESTOS PREFERIDOS: (2S)-4-(2,5-DIFLUOROFENIL)-N-[(3S,4R)-3-FLUORO-1-METILPIPERIDIN-4-IL]-2-(HIDROXIMETIL)-N-METIL-2-FENIL-2,5-DIHIDRO-1H-PIRROL-1-CARBOXAMIDA, (2S)-4-(2,5-DIFLUOROFENIL)-N-[(2R,4R)-2-(FLUOROMETIL)-1-METILPIPERIDIN-4-IL]-2-(HIDROXIMETIL)-N-METIL-2-FENIL-2,5-DIHIDRO-1H-PIRROL-1-CARBOXAMIDA, (2S)-4-(2,5-DIFLUOROFENIL)-N-[(3S,4R)-3-FLUORO-1-METIL-1-OXIDOPIPERIDIN-4-IL]-2-(HIDROXIMETIL)-N-METIL-2-FENIL-2,5-DIHIDRO-1H-PIRROL-1-CARBOXAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON INHIBIDORES DE QUINESINAS MITOTICAS, EN PARTICULAR DE KSP, POR LO QUE SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS CELULARES, COMO CANCER, HIPERPLASIAS, REESTENOSIS, HIPERTROFIA CARDIACA, TRANSTORNOS INMUNES E INFLAMACION
PE2004000762A 2003-08-15 2004-08-06 Derivados de 2,5-dihidropirrol 2,2-disustituidos como inhibidores de quinesinas mitoticas PE20050730A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US49563703P 2003-08-15 2003-08-15
US51268003P 2003-10-20 2003-10-20
US56358604P 2004-04-19 2004-04-19

Publications (1)

Publication Number Publication Date
PE20050730A1 true PE20050730A1 (es) 2005-09-20

Family

ID=34222358

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004000762A PE20050730A1 (es) 2003-08-15 2004-08-06 Derivados de 2,5-dihidropirrol 2,2-disustituidos como inhibidores de quinesinas mitoticas

Country Status (13)

Country Link
US (1) US20050038074A1 (es)
KR (1) KR20060058716A (es)
AR (1) AR045342A1 (es)
BR (1) BRPI0413580A (es)
CO (1) CO5650252A2 (es)
EC (1) ECSP066362A (es)
IL (1) IL173513A0 (es)
IS (1) IS8276A (es)
MA (1) MA27986A1 (es)
NO (1) NO20061194L (es)
PE (1) PE20050730A1 (es)
TW (1) TW200510380A (es)
WO (1) WO2005019205A1 (es)

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* Cited by examiner, † Cited by third party
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EP1515949B1 (en) 2002-06-14 2007-03-14 Merck & Co., Inc. Mitotic kinesin inhibitors
KR20050010515A (ko) * 2002-06-14 2005-01-27 머크 앤드 캄파니 인코포레이티드 유사분열 키네신 억제제
WO2005018547A2 (en) 2003-08-15 2005-03-03 Merck & Co., Inc. Mitotic kinesin inhibitors
SI1664026T1 (sl) * 2003-08-15 2009-04-30 Merck & Co Inc Inhibitorji mitotiäśnega kinezina
US7638549B2 (en) 2003-08-15 2009-12-29 Merck & Co. Inc. Mitotic kinesin inhibitors
WO2005102996A2 (en) * 2004-04-19 2005-11-03 Merck & Co., Inc. A process for the preparation of 2,2-disubstituted pyrroles
WO2006123182A2 (en) 2005-05-17 2006-11-23 Merck Sharp & Dohme Limited Cyclohexyl sulphones for treatment of cancer
KR20080110783A (ko) * 2006-03-07 2008-12-19 어레이 바이오파마 인크. 헤테로바이시클릭 피라졸 화합물 및 사용 방법
BRPI0818605A2 (pt) 2007-10-19 2015-04-22 Schering Corp Derivados de 1,3,4-tiadiazl espiro-condensados para inibir a atividade de ksp cinesima
EP2413932A4 (en) 2009-04-01 2012-09-19 Merck Sharp & Dohme INHIBITORS OF AKT ACTIVITY
BR112012008849A2 (pt) 2009-10-14 2015-09-22 Schering Corp composto, composição farmacêutica, e, uso de um composto
EP2584903B1 (en) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
JP6043285B2 (ja) 2010-08-02 2016-12-14 サーナ・セラピューティクス・インコーポレイテッドＳｉｒｎａ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． 低分子干渉核酸（ｓｉＮＡ）を用いたカテニン（カドヘリン結合型タンパク質）β１（ＣＴＮＮＢ１）遺伝子発現のＲＮＡ干渉媒介性阻害
HUE044815T2 (hu) 2010-08-17 2019-11-28 Sirna Therapeutics Inc Hepatitisz B vírus (HBV) génexpressziójának RNS-interferencia közvetített gátlása, rövid interferáló nukleinsav (SINS) alkalmazásával
EP2613782B1 (en) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
US9260471B2 (en) 2010-10-29 2016-02-16 Sirna Therapeutics, Inc. RNA interference mediated inhibition of gene expression using short interfering nucleic acids (siNA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP3919620A1 (en) 2012-05-02 2021-12-08 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
US9233979B2 (en) 2012-09-28 2016-01-12 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
BR112015012295A8 (pt) 2012-11-28 2023-03-14 Merck Sharp & Dohme Uso de um inibidor de wee1, e, kit para identificar um paciente com câncer
BR112015013611A2 (pt) 2012-12-20 2017-11-14 Merck Sharp & Dohme composto, e, composição farmacêutica
EP2951180B1 (en) 2013-01-30 2018-05-02 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
EP3041938A1 (en) 2013-09-03 2016-07-13 Moderna Therapeutics, Inc. Circular polynucleotides
JOP20190055A1 (ar) 2016-09-26 2019-03-24 Merck Sharp & Dohme أجسام مضادة ضد cd27
JP7160833B2 (ja) 2017-04-13 2022-10-25 サイロパ ビー．ブイ． 抗ｓｉｒｐアルファ抗体
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2019148412A1 (en) 2018-02-01 2019-08-08 Merck Sharp & Dohme Corp. Anti-pd-1/lag3 bispecific antibodies
EP3833667B1 (en) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5 inhibitors
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US20230108452A1 (en) 2019-12-17 2023-04-06 Merck Sharp & Dohme Llc Prmt5 inhibitors

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6057342A (en) * 1996-08-16 2000-05-02 Dupont Pharmaceutical Co. Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof
US6440686B1 (en) * 2000-06-15 2002-08-27 Cytokinetics, Inc. Methods for screening and therapeutic applications of kinesin modulators
CA2467916A1 (en) * 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
EP1515949B1 (en) * 2002-06-14 2007-03-14 Merck & Co., Inc. Mitotic kinesin inhibitors
KR20050010515A (ko) * 2002-06-14 2005-01-27 머크 앤드 캄파니 인코포레이티드 유사분열 키네신 억제제
US7235580B2 (en) * 2002-10-18 2007-06-26 Merck & Co., Inc. Mitotic kinesin inhibitors

Also Published As

Publication number Publication date
TW200510380A (en) 2005-03-16
NO20061194L (no) 2006-05-05
WO2005019205A1 (en) 2005-03-03
AR045342A1 (es) 2005-10-26
IL173513A0 (en) 2006-07-05
MA27986A1 (fr) 2006-07-03
IS8276A (is) 2006-01-31
BRPI0413580A (pt) 2006-10-17
ECSP066362A (es) 2006-10-31
KR20060058716A (ko) 2006-05-30
US20050038074A1 (en) 2005-02-17
CO5650252A2 (es) 2006-06-30

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