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AR083402A1 - Pirrolidinonas como inhibidores de metap-2 - Google Patents

Pirrolidinonas como inhibidores de metap-2

Info

Publication number
AR083402A1
AR083402A1 ARP110103781A ARP110103781A AR083402A1 AR 083402 A1 AR083402 A1 AR 083402A1 AR P110103781 A ARP110103781 A AR P110103781A AR P110103781 A ARP110103781 A AR P110103781A AR 083402 A1 AR083402 A1 AR 083402A1
Authority
AR
Argentina
Prior art keywords
hal
atoms
mono
cooa
coa
Prior art date
Application number
ARP110103781A
Other languages
English (en)
Inventor
Michel Calderini
Djordje Musil
Frank Zenke
Timo Heinrich
Original Assignee
Merck Patent Gmbh
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 Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR083402A1 publication Critical patent/AR083402A1/es

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    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
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    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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Abstract

Los compuestos de la formula (1) en donde R1 es [C(R4)2]nAr1, (CH2)nHet, (CH2)nCyc, un resto de fórmula (2) o A; R2 es [C(R4)2]nAr2, CH[B(OH)2]CH2Het, un resto de fórmula (3), (CH2)nHet, (CH2)nCyc, CH(CCH)fenilo o A; R3 es OH, Hal, NH2, CN, CF3, CHF2 o N3; R4 es H o alquilo con 1, 2, 3 ó 4 átomos de C; R2 y R4 también son juntos alquileno con 2, 3, 4 ó 5 átomos de C, en donde un grupo CH2 también puede estar sustituido con NH, NA, N-COA, N-(CH2)nAr3, N-(CH2)nHet2, CH-A, CH-O-(CH2)nAr3, N-SO2A u O y/o puede estar sustituido con A; Ar1 es fenilo, naftilo o bifenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHSO2A, COA, CHO, Het1, SO2NH2 y/o SO2A; Ar2 es fenilo, naftilo o bifenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHSO2A, COA, CHO, Het1, SO2NH2 y/o SO2A; Ar3 es fenilo no sustituido o mono-, di- o trisustituido con Hal, OH, OA y/o A; Het es un heterociclo saturado, insaturado o aromático mono- o bicíclico no sustituido o mono-, di- o trisustituido con Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, COOH, COOA, (CH2)nCONH2, (CH2)nCONHA, (CH2)nCONA2, NHCOA, NHSO2A, COA, CHO, Het1, SO2NH2, SO2A y/u =O con 1 a 4 átomos de N y/u O y/o S; Het1 es un heterociclo saturado, insaturado o aromático monocíclico no sustituido o mono-, di- o trisustituido con Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, COOH y/o COOA con 1 a 4 átomos de N y/u O y/o S; Het2 es piridilo, pirimidinilo, furilo, tienilo, imidazolilo, pirrolilo, oxazolilo, oxadiazolilo, isoxazolilo, tiazolilo, triazolilo, tetrazolilo o tiadiazol; A es alquilo no ramificado o ramificado con 1 - 10 átomos de C, en donde 1 - 7 átomos de H pueden estar reemplazados por F, Cl, Br, OH, CHO, COA, COOA, CN, CONA2, CONHA y/o CONH2, y/o en donde uno o dos grupos no adyacentes CH y/o CH2 pueden estar reemplazados por O, N y/o NR4, o Cyc; Cyc es alquilo cíclico con 3 - 7 átomos de C; Hal es F, Cl, Br o I; n es 0, 1, 2, 3 ó 4; así como sus sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones, composición farmacéutica y proceso de preparación. Son inhibidores de la metionina-amino-peptidasa y se pueden usar para el tratamiento de tumores.
ARP110103781A 2010-10-13 2011-10-13 Pirrolidinonas como inhibidores de metap-2 AR083402A1 (es)

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Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8575349B2 (en) * 2010-11-22 2013-11-05 International Flavors & Fragrances Inc. Derivatives of 1-alkyl-6-oxo-piperidine-3-carboxylic acids and 1-alkyl-5-oxo-pyrrolidine-3-carboxylic acids and their uses as cooling compounds
EP2573073B1 (en) * 2011-09-26 2014-10-22 Sanofi Pyrazoloquinolinone derivatives, preparation thereof and therapeutic use thereof
JP6042060B2 (ja) * 2011-09-26 2016-12-14 サノフイ ピラゾロキノリノン誘導体、その調製および治療上の使用
DE102012006884A1 (de) * 2012-04-04 2013-10-10 Merck Patent Gmbh Cyclische Amide als MetAP-2 Inhibitoren
JPWO2015037716A1 (ja) * 2013-09-12 2017-03-02 住友化学株式会社 含窒素飽和複素環化合物
HUE042064T2 (hu) * 2014-08-04 2019-06-28 Merck Patent Gmbh Pirrolidinon-származékok MetAP-2 inhibitorokként
WO2017004797A1 (en) * 2015-07-08 2017-01-12 Eli Lilly And Company Pyrrolidinone compounds
WO2017084096A1 (en) * 2015-11-20 2017-05-26 Eli Lilly And Company Pyrrolidinone compounds
WO2017219083A1 (en) * 2016-06-21 2017-12-28 The University Of Melbourne Activators of hiv latency
WO2018098781A1 (en) * 2016-12-01 2018-06-07 Eli Lilly And Company Pyrrolidinone compounds
US11365194B2 (en) * 2017-09-27 2022-06-21 Kagoshima University Analgesic drug using PAC1 receptor antagonistic drug
CN108409630B (zh) * 2018-02-07 2021-01-15 宁波大学 一种水相中3-羟基-2-吲哚酮衍生物的制备方法
MX2021008712A (es) * 2019-01-22 2021-08-19 Merck Patent Gmbh Derivados heterociclicos.
EP3994134B9 (en) 2019-07-03 2024-06-26 Merck Patent GmbH Process for manufacturing (s)-3-hydroxy-1-(1h-indol-5-yl)-2-oxo-pyrrolidine-3-carboxylic acid 3,5-difluoro-benzylamide
CN112480100B (zh) * 2019-09-11 2022-10-14 康威(广州)生物科技有限公司 吡咯烷酮衍生物
CN110759843A (zh) * 2019-09-30 2020-02-07 东北师范大学 一种氟叠氮取代的四元杂环化合物的制备和应用
KR20230038219A (ko) 2020-07-09 2023-03-17 메르크 파텐트 게엠베하 메티오닌 아미노펩티다아제 2 억제제 및 vegfr/vegf 억제제의 조합
CN112851561A (zh) * 2021-01-29 2021-05-28 南京艾美斐生物医药科技有限公司 一种nr6a1蛋白受体抑制剂及其制备和应用
AU2022252615A1 (en) * 2021-03-28 2023-10-12 Canwell Biotech Limited Metap-2 inhibitors, pharmaceutical compositions and therapeutic methods thereof
WO2023144053A1 (en) 2022-01-26 2023-08-03 Merck Patent Gmbh Heterocyclic derivatives

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5747469A (en) 1991-03-06 1998-05-05 Board Of Regents, The University Of Texas System Methods and compositions comprising DNA damaging agents and p53
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
PE20011222A1 (es) 2000-04-14 2001-12-07 Abbott Lab Hidrazidas y alcoxiamidas inhibidoras de la angiogenesis
US20070161570A1 (en) 2000-11-01 2007-07-12 Praecis Pharmaceuticals, Inc. Methionine aminopeptidase-2 inhibitors and methods of use thereof
AU2002306907A1 (en) 2001-04-03 2002-10-21 Smithkline Beecham Corporation Method for inhibiting metap2
US20030225054A1 (en) * 2002-06-03 2003-12-04 Jingwu Duan Combined use of tace inhibitors and COX2 inhibitors as anti-inflammatory agents
US7355053B2 (en) 2002-10-18 2008-04-08 Basf Aktiengesellschaft 1-phenylpyrrolidine-2-one-3-carboxamides
JP2006104280A (ja) 2004-10-04 2006-04-20 Toyo Tire & Rubber Co Ltd 高熱伝導性加硫ゴム成形体及びダイアフラム
EP1864971A4 (en) * 2005-03-31 2010-02-10 Takeda Pharmaceutical PROPHYLACTIC / THERAPEUTIC AGENT AGAINST DIABETES
US20070123508A1 (en) * 2005-05-27 2007-05-31 Roger Olsson PAR2-modulating compounds and their use
UY31984A (es) * 2008-07-16 2010-02-26 Boehringer Ingelheim Int DERIVADOS DE 1-(3,4-difluorobencil)-6-oxo-1,6-dihidropirimidin-5-carboxamidas N-sustituidas y de 2-(3,4-difluorobencil)-3-oxo-2,3-dihidro-1H-pirazol-4-carboxamidas N-sustituidas.
EP2521719B1 (en) 2010-01-08 2015-07-29 Zafgen, Inc. Fumagillol type compounds and methods of making and using same
WO2011085198A1 (en) 2010-01-08 2011-07-14 Zafgen Corporation Metap-2 inhibitor for use in treating benign prostatic hypertrophy (bph)

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