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AR090602A1 - AMIDAS CICLICAS Y HETEROCICLOS COMO INHIBIDORES DE MetAP-2 - Google Patents

AMIDAS CICLICAS Y HETEROCICLOS COMO INHIBIDORES DE MetAP-2

Info

Publication number
AR090602A1
AR090602A1 ARP130101102A ARP130101102A AR090602A1 AR 090602 A1 AR090602 A1 AR 090602A1 AR P130101102 A ARP130101102 A AR P130101102A AR P130101102 A ARP130101102 A AR P130101102A AR 090602 A1 AR090602 A1 AR 090602A1
Authority
AR
Argentina
Prior art keywords
atoms
mono
unsubstituted
cooa
hal
Prior art date
Application number
ARP130101102A
Other languages
English (en)
Inventor
Dr Zenke Frank
Dr Heinrich Timo
Dra Krier Mireille
Dra Friese-Hamim Manja
Seenisamy Jeyaprakashnarayanan
Original Assignee
Merck Patent Ges Mit Beschränkter Haftung
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 Ges Mit Beschränkter Haftung filed Critical Merck Patent Ges Mit Beschränkter Haftung
Publication of AR090602A1 publication Critical patent/AR090602A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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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
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    • 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
    • A61K31/402—1-aryl substituted, e.g. piretanide
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    • 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
    • A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
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    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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Abstract

Los compuestos de la fórmula (1) en donde R es NR²R⁴, Alk, C(=CH₂)[C(R⁴)₂]ₙAr², Het², O[C(R⁴)₂]ₙAr² u OA; X es CO o CH₂; Y es CO o CH₂; R¹ es H, [C(R⁴)₂]ₙAr¹, (CH₂)ₙHet, (CH₂)ₙCyc, [C(R⁴)₂]ₙCOOH, [C(R⁴)₂]ₙCONHAr¹, [C(R⁴)₂]ₙCONH₂, [C(R⁴)₂]ₙNHA, [C(R⁴)₂]ₙNA₂, O[C(R⁴)₂]ₙAr¹, [C(R⁴)₂]ₙOR⁷, [C(R⁴)₂]ₙCOO(CH₂)ₙAr¹, [C(R⁴)₂]ₙCOOA, [C(R⁴)₂]ₙCONH[C(R⁴)₂]ₚCON(R⁴)₂ o [C(R⁴)₂]ₙCONHCR⁴[(CH₂)ₙN(R⁴)₂]CON(R⁴)₂; R² es H, [C(R⁴)₂]ₙAr², (CH₂)ₙCOHet¹, (CH₂)ₙCOAr², (CH₂)ₘNA₂ O (CH₂)ₙHet; R³ es OH u OCOA; 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 esta reemplazado por N(CH₂)ₘOH ó SO₂; R⁵, R⁶ son cada uno, de modo independiente entre sí, H, F o A; R⁵ y R⁶ también son juntos alquileno con 2, 3, 4 ó 5 átomos de C, en donde un grupo CH₂ también puede estar reemplazado por NCOA u O; R⁷ es H o A; Ar¹ es fenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, OH, OA, CONH₂, CONHA, CONA₂, NHSO₂A, CONHCyc, NHSO₂Cyc, CONHAr², COHet¹ y/o NASO₂A; Ar² es fenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con Hal, A, CONH₂, y/u OAr³; Ar³ es fenilo no sustituido o monosustituido con NH₂; Het es un heterociclo mono- o bicíclico saturado, insaturado o aromático no sustituido o mono-, di- o trisustituido con Hal, A, OA, CN, NH₂, NHA, NA₂, NO₂, CN, COOH, COOA, (CH₂)ₙCONH₂, (CH₂)ₙCONHA, (CH₂)ₙCONA₂, NHCOA, COA, CHO, Het¹, SO₂A, SO₂NH₂, SO₂NHA, SO₂NA₂, CONHNH₂, CONHAr³, =O y/o Ar³ con 1 a 4 átomos de N y/u O y/o S; Het¹ es un heterociclo monocíclico saturado no sustituido o mono-, di- o trisustituido con =O y/o COOA con 1 a 4 átomos de N y/u O y/o S; Het² es isoindolilo; 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, o Cyc; Alk es alquenilo con 2, 3, 4, 5 ó 6 átomos de C; Cyc es alquilo cíclico no sustituido o mono-, di- o trisustituido con NHCOA, NHSO₂, OH, OA, A, NH₂, NHA, NA₂, COOA, COOH y/o CONHA con 3 - 7 átomos de C; Hal es F, Cl, Br o I; m es 1, 2, 3 ó 4; n es 0, 1, 2, 3 ó 4; p es 1, 2 ó 3; así como sus sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la metionina-amino-peptidasa y se pueden usar para el tratamiento de tumores.
ARP130101102A 2012-04-04 2013-04-04 AMIDAS CICLICAS Y HETEROCICLOS COMO INHIBIDORES DE MetAP-2 AR090602A1 (es)

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Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105764887A (zh) * 2013-09-12 2016-07-13 住友化学株式会社 含氮饱和杂环化合物
WO2015130958A1 (en) * 2014-02-26 2015-09-03 Howard University 5-oxopyrrolidine derivatives as hiv integrase inhibitors
CN106255679B (zh) * 2014-02-27 2019-09-06 默克专利有限公司 用作nav通道抑制剂的杂环化合物及其用途
CA2957154C (en) * 2014-08-04 2023-01-10 Merck Patent Gmbh Pyrrolidinone derivatives as metap-2 inhibitors
WO2016100940A1 (en) 2014-12-19 2016-06-23 The Broad Institute, Inc. Dopamine d2 receptor ligands
WO2016100823A1 (en) 2014-12-19 2016-06-23 The Broad Institute, Inc. Dopamine d2 receptor ligands
AU2016218840A1 (en) * 2015-02-15 2017-08-31 Jiangsu Hengrui Medicine Co., Ltd. Ligand-cytotoxicity drug conjugate, preparing method therefor, and application thereof
WO2017005069A1 (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
WO2018098781A1 (en) * 2016-12-01 2018-06-07 Eli Lilly And Company Pyrrolidinone compounds
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
EP3750885A4 (en) * 2018-02-06 2021-10-27 Shanghai Haihe Pharmaceutical Co., Ltd. COMPOUND PRESENTING AN INHIBITORING ACTIVITY OF BET, ITS PREPARATION PROCESS AND ITS USE
WO2019195658A1 (en) 2018-04-05 2019-10-10 Dana-Farber Cancer Institute, Inc. Sting levels as a biomarker for cancer immunotherapy
EP3833661A1 (en) 2018-08-09 2021-06-16 Valo Early Discovery, Inc. Carboxamides as ubiquitin-specific protease inhibitors
CN110963957B (zh) * 2018-09-28 2021-10-22 深圳恩多凯医药科技有限公司 N-芳香酰胺类化合物及其制备方法和用途
CA3127268A1 (en) * 2019-01-22 2020-07-30 Merck Patent Gmbh Heterocyclic derivatives
KR102281485B1 (ko) 2019-06-19 2021-07-28 주식회사 오쎄인 시안화아크릴레이트의 점도 변화에 따른 물성변화를 통한 골대체용 복합재료의 제조방법 및 그것의 조성물
HUE066832T2 (hu) * 2019-07-03 2024-09-28 Merck Patent Gmbh Eljárás (S)-3-hidroxi-1-(1H-indol-5-il)-2-oxo-pirrolidin-3-karbonsav 3,5-difluor-benzilamid elõállítására
US20220305048A1 (en) 2019-08-26 2022-09-29 Dana-Farber Cancer Institute, Inc. Use of heparin to promote type 1 interferon signaling
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
US20230248695A1 (en) 2020-07-09 2023-08-10 Merck Patent Gmbh Combinations of cancer therapeutics
CN111728969B (zh) * 2020-08-25 2021-03-19 广州市万千粉丝化妆品有限公司 抗衰老抗氧化的化合物在制备药物或者抗衰老化妆品中的用途
US20240158348A1 (en) * 2021-02-16 2024-05-16 Fmc Corporation Herbicidal cyclic amides n-substituted with a haloalkylsulfonylanilide group
CN117412952A (zh) * 2021-03-28 2024-01-16 康崴新药有限公司 Metap-2抑制剂、药物组合物及其治疗方法
WO2023144053A1 (en) 2022-01-26 2023-08-03 Merck Patent Gmbh Heterocyclic derivatives

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4508724A (en) 1984-02-03 1985-04-02 A. H. Robins Company, Inc. Aryloxymethylpyrrolidinols and piperidinols having antidepressant, antiarrhythmic or hypotensive activity
JPS63208590A (ja) 1987-02-24 1988-08-30 Yamanouchi Pharmaceut Co Ltd ヘテロ環式スピロ化合物及びその製造法
US5173484A (en) 1988-02-05 1992-12-22 Bayer Aktiengesellschaft Quinolone- and naphthyridone carboxylic acid derivatives, process for their production, antibacterial compositions and feed additives containing them
DE3814517A1 (de) 1988-02-05 1989-08-17 Bayer Ag Chinolon- und naphthyridoncarbonsaeurederivate, verfahren zu ihrer herstellung und sie enthaltende antibakterielle mittel und futterzusatzstoffe
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
US20080234247A1 (en) 1999-05-25 2008-09-25 Sepracor, Inc. Heterocyclic analgesic compounds and methods of use thereof
US6635661B2 (en) 2000-05-25 2003-10-21 Sepracor Inc. Heterocyclic analgesic compounds and methods of use thereof
WO2000071518A2 (en) 1999-05-25 2000-11-30 Sepracor, Inc. Heterocyclic analgesic compounds and their use
US7361666B2 (en) 1999-05-25 2008-04-22 Sepracor, Inc. Heterocyclic analgesic compounds and methods of use thereof
US6677332B1 (en) 1999-05-25 2004-01-13 Sepracor, Inc. Heterocyclic analgesic compounds and methods of use thereof
AR028537A1 (es) 2000-04-14 2003-05-14 Abbott Lab Hidrazidas y alcoxiamidas inhibidoras de la angiogénesis
AU2001216218A1 (en) 2000-05-25 2001-12-11 Sepracor, Inc. Heterocyclic analgesic compounds and method of use thereof
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
US7259157B2 (en) 2001-04-03 2007-08-21 Merck & Co., Inc. N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
JP4398866B2 (ja) 2002-10-18 2010-01-13 ビーエーエスエフ ソシエタス・ヨーロピア １−フェニルピロリジン−２−オン−３−カルボキサミド
JP2008502689A (ja) 2004-06-15 2008-01-31 グラクソ　グループ　リミテッド 抗菌剤
US20070123508A1 (en) * 2005-05-27 2007-05-31 Roger Olsson PAR2-modulating compounds and their use
CL2008001002A1 (es) 2007-04-11 2008-10-17 Actelion Pharmaceuticals Ltd Compuestos derivados de oxazolidinona; composicion farmaceutica que comprende a dichos compuestos; y su uso para preparar un medicamento para tratar una infeccion bacteriana.
DE102008027574A1 (de) * 2008-06-10 2009-12-17 Merck Patent Gmbh Neue Pyrrolidinderivate als MetAP-2 Inhibitoren
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)
WO2012033956A1 (en) 2010-09-08 2012-03-15 Mithridion, Inc. Cognition enhancing compounds and compositions, methods of making, and methods of treating
DE102010048374A1 (de) 2010-10-13 2012-04-19 Merck Patent Gmbh Pyrrolidinone als MetAP-2 Inhibitoren

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