PE20142185A1 - Pirrolidina-2-carboxamidas sustituidas - Google Patents

Pirrolidina-2-carboxamidas sustituidas

Info

Publication number
PE20142185A1
PE20142185A1 PE2014001419A PE2014001419A PE20142185A1 PE 20142185 A1 PE20142185 A1 PE 20142185A1 PE 2014001419 A PE2014001419 A PE 2014001419A PE 2014001419 A PE2014001419 A PE 2014001419A PE 20142185 A1 PE20142185 A1 PE 20142185A1
Authority
PE
Peru
Prior art keywords
chloro
phenyl
pyrrolidine
lower alkyl
substitute
Prior art date
Application number
PE2014001419A
Other languages
English (en)
Inventor
David Joseph Bartkovitz
Xin-Jie Chu
Binh Thanh Vu
Chunlin Zhao
Daniel Fishlock
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20142185A1 publication Critical patent/PE20142185A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—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 no double bonds between ring members or between ring members and non-ring members 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE: X ES H, F, CL, ENTRE OTROS; Y ES H, F, CL, ENTRE OTROS; Z ES ALCOXI INFERIOR; R1 ES ALQUILO INFERIOR, ALQUENILO INFERIOR, ARILO, ENTRE OTROS; R2 ES FENILO SUSTITUIDO; R3 ES H, ALQUILO INFERIOR O ALQUILO INFERIOR SUSTITUIDO; R4 SE ELIJE DE II, DONDE R5 ES ALQUILO INFERIOR, HETEROCICLO, CICLOALQUILO ENTRE OTROS Y R6 ES H O BENCILO. SON COMPUESTOS PREFERIDOS: 4-((2R,3S,4R,5S)-3-(3-CLORO-2-FLUORFENIL)-4-(4-CLORO-2-FLUORFENIL)-4-CIANO-5-NEOPENTILPIRROLIDINA-2-CARBOXAMIDO)-3-METOXIBENZOATO DE 1-(ETIL(ISOPROPIL)CARBAMOILOXI)ETILO; 4-{[(2R,3S,4R,5S)-3-(3-CLORO-2-FLUOR-FENIL)-4-(4-CLORO-2-FLUOR-FENIL)-4-CIANO-5-(2,2-DIMETIL-PROPIL)-PIRROLIDINA-2-CARBONIL]-AMINO}-3-METOXI-BENZOATO DE DI-TERT-BUTOXI-FOSFORILOXIMETILO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN INHIBIDOR DE LA MDM2 Y ES UTIL EN EL TRATAMIENTO DEL CANCER.
PE2014001419A 2012-03-15 2013-03-12 Pirrolidina-2-carboxamidas sustituidas PE20142185A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261611200P 2012-03-15 2012-03-15

Publications (1)

Publication Number Publication Date
PE20142185A1 true PE20142185A1 (es) 2014-12-29

Family

ID=47844360

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014001419A PE20142185A1 (es) 2012-03-15 2013-03-12 Pirrolidina-2-carboxamidas sustituidas

Country Status (28)

Country Link
US (1) US8993614B2 (es)
EP (1) EP2825528B1 (es)
JP (1) JP6125546B2 (es)
KR (1) KR20140138165A (es)
CN (1) CN104271554B (es)
AR (1) AR090328A1 (es)
AU (1) AU2013203662B2 (es)
BR (1) BR112014018959A8 (es)
CA (1) CA2860781A1 (es)
CL (1) CL2014001858A1 (es)
CO (1) CO6990736A2 (es)
CR (1) CR20140399A (es)
DK (1) DK2825528T3 (es)
EA (1) EA025557B1 (es)
ES (1) ES2634290T3 (es)
HK (1) HK1200830A1 (es)
HU (1) HUE032864T2 (es)
IL (1) IL234173A (es)
MX (1) MX2014010942A (es)
NZ (1) NZ626505A (es)
PE (1) PE20142185A1 (es)
PH (1) PH12014501542A1 (es)
PL (1) PL2825528T3 (es)
SG (1) SG11201404344XA (es)
SI (1) SI2825528T1 (es)
TW (1) TWI586648B (es)
UA (1) UA113541C2 (es)
WO (1) WO2013135648A1 (es)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2869101A1 (en) 2012-05-30 2013-12-05 F. Hoffmann-La Roche Ag Substituted pyrrolidine-2-carboxamides
WO2014100065A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
BR112015029976A2 (pt) * 2013-06-24 2017-07-25 Hoffmann La Roche formulação farmacêutica, formulação liofilizada farmacêutica e preparações novas, métodos e usos
RU2016101514A (ru) 2013-07-03 2017-08-08 Ф. Хоффманн-Ля Рош Аг ЭКСПРЕССИЯ мРНК ГЕНОВ ДЛЯ ПЕРСОНАЛИЗАЦИИ ПРОТИВООПУХОЛЕВОЙ ТЕРАПИИ ПАЦИЕНТОВ АНТАГОНИСТОМ MDM2
AR097584A1 (es) 2013-09-12 2016-03-23 Hoffmann La Roche Terapia de combinación de anticuerpos contra el csf-1r humano y anticuerpos contra el pd-l1 humano
HUE049434T2 (hu) * 2013-12-05 2020-09-28 Hoffmann La Roche Akut mielogén leukémia (AML) új, kombinált kezelése
US9657351B2 (en) 2013-12-06 2017-05-23 Hoffman-La Roche Inc. MRNA-based gene expression for personalizing patient cancer therapy with an MDM2 antagonist
US10227298B2 (en) * 2014-04-15 2019-03-12 Hoffmann-La Roche Inc. Solid forms of a pharmaceutically active compound
CN106536478A (zh) * 2014-05-22 2017-03-22 悉尼大学 ω‑3类似物
US20170227544A1 (en) * 2014-10-10 2017-08-10 Hoffmann-La Roche Inc. Methods for personalizing patient cancer therapy with an mdm2 antagonist
CN104496822B (zh) * 2014-12-15 2016-10-26 扬州三友合成化工有限公司 一种1-氯乙基环己基丙基碳酸酯的制备方法
MY189692A (en) 2015-05-07 2022-02-26 Memorial Sloan Kettering Cancer Center Anti-ox40 antibodies and methods of use thereof
KR20180083944A (ko) 2015-12-02 2018-07-23 아게누스 인코포레이티드 항체 및 이의 사용 방법
JP2019522633A (ja) 2016-05-20 2019-08-15 ジェネンテック， インコーポレイテッド Ｐｒｏｔａｃ抗体コンジュゲート及び使用方法
CN107698598B (zh) * 2016-08-08 2019-06-21 肖飞 螺环吲哚酮聚乙二醇碳酸酯类化合物和其组合物、制备方法及用途
EP3498712B1 (en) * 2016-08-08 2024-01-03 Jiangsu Yayo Biotechnology Co. Ltd Spirocyclic indolone polyethylene glycol carbonate compound, composition, preparation method and use thereof
WO2018036852A1 (en) 2016-08-25 2018-03-01 F. Hoffmann-La Roche Ag Intermittent dosing of an anti-csf-1r antibody in combination with macrophage activating agent
WO2018089628A1 (en) 2016-11-09 2018-05-17 Agenus Inc. Anti-ox40 antibodies, anti-gitr antibodies, and methods of use thereof
EP3558360A1 (en) 2016-12-22 2019-10-30 F. Hoffmann-La Roche AG Treatment of tumors with an anti-csf-1r antibody in combination with an anti-pd-l1 antibody after failure of anti-pd-l1/pd1 treatment
EP3727364A4 (en) * 2017-12-20 2021-08-11 Angex Pharmaceutical, Inc. CARBAMATE AND UREA COMPOUNDS AS MULTIKINASE INHIBITORS
CN114230561B (zh) * 2020-09-09 2024-03-19 中国人民解放军海军军医大学 一种mdm2抑制剂类小分子化合物及用途
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0720857B2 (ja) 1988-08-11 1995-03-08 テルモ株式会社 リポソームおよびその製法
EP0452179B1 (en) 1990-03-28 1996-06-12 Nippon Oil And Fats Company, Limited Polymer-combined drug for gastric treatment and a method for producing the drug
US5681811A (en) 1993-05-10 1997-10-28 Protein Delivery, Inc. Conjugation-stabilized therapeutic agent compositions, delivery and diagnostic formulations comprising same, and method of making and using the same
GB9317618D0 (en) 1993-08-24 1993-10-06 Royal Free Hosp School Med Polymer modifications
KR100361933B1 (ko) 1993-09-08 2003-02-14 라 졸라 파마슈티칼 컴파니 화학적으로정의된비중합성결합가플랫폼분자및그것의콘주게이트
WO1995016465A1 (en) 1993-12-14 1995-06-22 Sandoz Ltd. Pharmaceutical compositions containing alkyl polyoxyalkylene carboxylates
DE4435087A1 (de) 1994-09-30 1996-04-04 Deutsches Krebsforsch Konjugat zur Behandlung von Infektions-, Autoimmun- und Hauterkrankungen
WO1998032466A1 (en) 1997-01-29 1998-07-30 Polymasc Pharmaceuticals Plc Pegylation process
AU9402198A (en) 1997-09-26 1999-04-23 Becton Dickinson & Company Preparing conjugates using polyethylene glycol linkers
US6165509A (en) 1998-09-01 2000-12-26 University Of Washington Pegylated drug complexed with bioadhesive polymer suitable for drug delivery and methods relating thereto
US6294192B1 (en) 1999-02-26 2001-09-25 Lipocine, Inc. Triglyceride-free compositions and methods for improved delivery of hydrophobic therapeutic agents
US6713454B1 (en) 1999-09-13 2004-03-30 Nobex Corporation Prodrugs of etoposide and etoposide analogs
AU2001268228A1 (en) 2000-06-08 2001-12-17 La Jolla Pharmaceutical Company Multivalent platform molecules comprising high molecular weight polyethylene oxide
US20040171808A1 (en) 2001-05-30 2004-09-02 Kazunori Kataoka Method of bonding substance to be incorporated into polymer terminal
US6939874B2 (en) * 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
US7144978B2 (en) 2002-01-15 2006-12-05 Pan Asia Bio Co., Ltd. Multidrop tree branching functional polyethylene glycol, methods of preparing and using same
MEP35608A (en) 2002-01-18 2011-02-10 Biogen Idec Inc Polyalkylene polymer compounds and uses thereof
US7482376B2 (en) 2003-07-03 2009-01-27 3-Dimensional Pharmaceuticals, Inc. Conjugated complement cascade inhibitors
EP1729814A2 (en) 2004-04-01 2006-12-13 Cardiome Pharma Corp. Pegylated ion channel modulating compounds
TW200616604A (en) 2004-08-26 2006-06-01 Nicholas Piramal India Ltd Nitric oxide releasing prodrugs containing bio-cleavable linker
CA2584510C (en) 2004-10-25 2013-05-28 Intezyne Technologies, Incorporated Heterobifunctional poly(ethylene glycol) and uses thereof
NZ561215A (en) 2005-02-22 2010-12-24 Univ Michigan Small molecule inhibitors of MDM2 and uses thereof
US7560588B2 (en) 2006-04-27 2009-07-14 Intezyne Technologies, Inc. Poly(ethylene glycol) containing chemically disparate endgroups
WO2008109783A2 (en) 2007-03-06 2008-09-12 The Regents Of The University Of California Detecting spin perturbations using magnetic resonance imaging
JP2008308690A (ja) 2007-06-13 2008-12-25 Bio-Cancer Treatment Internatl Ltd ポリ（エチレングリコール）機能性誘導体およびその製造方法
WO2009128789A1 (en) 2008-04-17 2009-10-22 Agency For Science, Technology And Research Vesicles for intracellular drug delivery
WO2009155431A1 (en) 2008-06-18 2009-12-23 University Of Louisville Research Foundation, Inc. Methods for targeted cancer treatment and detection
WO2010007626A1 (en) 2008-07-14 2010-01-21 Biocon Limited A method of synthesizing a substantially monodispersed mixture of oligomers
EP2328619B1 (en) 2008-08-22 2016-12-07 Baxalta GmbH Polymeric benzyl carbonate-derivatives
US8354444B2 (en) 2008-09-18 2013-01-15 Hoffmann-La Roche Inc. Substituted pyrrolidine-2-carboxamides
RU2506257C2 (ru) 2008-09-18 2014-02-10 Ф.Хоффманн-Ля Рош Аг Замещенные пирролидин-2-карбоксамиды
WO2010151269A1 (en) 2009-06-26 2010-12-29 Biotic Laboratories, Inc. Para-xylylene based multilayer drug elution devices
US20110118283A1 (en) 2009-11-17 2011-05-19 Qingjie Ding Substituted Pyrrolidine-2-Carboxamides
US20120065210A1 (en) 2010-09-15 2012-03-15 Xin-Jie Chu Substituted hexahydropyrrolo[1,2-c]imidazolones
CN101991860B (zh) 2010-11-08 2013-06-19 中国药科大学 泊洛沙姆-羧酸类药物偶联物及其制备方法与应用
WO2012065022A2 (en) 2010-11-12 2012-05-18 The Regents Of The University Of Michigan Spiro-oxindole mdm2 antagonists
JP5918274B2 (ja) 2011-02-02 2016-05-18 オンタリオ インスティテュート フォー キャンサー リサーチ 薬物送達のためのセルロース系ナノ粒子
US9212258B2 (en) 2011-02-23 2015-12-15 The Board Of Trustees Of The University Of Illinois Amphiphilic dendron-coils, micelles thereof and uses
CN102247602B (zh) 2011-06-13 2013-01-02 中山大学 一种超分子水凝胶双重药物载体及其制备方法和应用
WO2013033476A1 (en) 2011-08-30 2013-03-07 Quanta Biodesign, Ltd. Branched discrette peg constructs
CA2869101A1 (en) * 2012-05-30 2013-12-05 F. Hoffmann-La Roche Ag Substituted pyrrolidine-2-carboxamides

Also Published As

Publication number Publication date
AU2013203662A1 (en) 2013-10-03
DK2825528T3 (en) 2017-08-14
CO6990736A2 (es) 2014-07-10
EA201491623A1 (ru) 2014-12-30
TW201341357A (zh) 2013-10-16
EP2825528B1 (en) 2017-05-24
EP2825528A1 (en) 2015-01-21
HK1200830A1 (en) 2015-08-14
US8993614B2 (en) 2015-03-31
ES2634290T3 (es) 2017-09-27
CN104271554A (zh) 2015-01-07
AR090328A1 (es) 2014-11-05
BR112014018959A8 (pt) 2017-07-11
NZ626505A (en) 2016-04-29
KR20140138165A (ko) 2014-12-03
BR112014018959A2 (es) 2017-06-20
JP2015512890A (ja) 2015-04-30
EA025557B1 (ru) 2017-01-30
CR20140399A (es) 2014-10-07
AU2013203662B2 (en) 2016-04-14
PL2825528T3 (pl) 2017-09-29
CA2860781A1 (en) 2013-09-19
SG11201404344XA (en) 2014-10-30
WO2013135648A1 (en) 2013-09-19
PH12014501542B1 (en) 2014-09-22
PH12014501542A1 (en) 2014-09-22
HUE032864T2 (en) 2017-11-28
UA113541C2 (xx) 2017-02-10
SI2825528T1 (sl) 2017-08-31
CN104271554B (zh) 2016-11-23
TWI586648B (zh) 2017-06-11
US20130244958A1 (en) 2013-09-19
CL2014001858A1 (es) 2014-09-26
JP6125546B2 (ja) 2017-05-10
IL234173A (en) 2017-08-31
MX2014010942A (es) 2014-11-14

Similar Documents

Publication Publication Date Title
PE20142185A1 (es) Pirrolidina-2-carboxamidas sustituidas
PE20170664A1 (es) Agonistas del receptor de apelina(apj) y usos de los mismos
PE20110367A1 (es) DERIVADOS DE 4-CIANO-4-FENIL-PIRROLIDIN-2-CARBOXAMIDAS SUSTITUIDAS COMO INHIBIDORES DE LA INTERACCION p53-MDM2
PE20151274A1 (es) Inhibidores de erk y sus usos
PE20141075A1 (es) 4-aril-n-fenil-1,3,5-triazin-2-aminas que contienen un grupo sulfoximina
PE20091656A1 (es) Compuestos heterociclicos como inhibidores de la cinasa raf
PE20180177A1 (es) Derivados de 1-(het) arilsulfonil-(pirrolidin o piperidin)-2-carboxamida y su uso como antagonistas de trpa1
NZ631477A (en) Substituted pyrrolidine-2-carboxamides
PE20140192A1 (es) Derivados de bencimidazol como inhibidores de cinasa pi3
PE20121354A1 (es) Inhibidores del virus de la hepatitis c
PE20080404A1 (es) Derivados bencil-amino-piperidina como inhibidores de cetp
PE20081783A1 (es) Nuevas 2-aminooxazolinas como ligandos de taar1
PE20161225A1 (es) 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer
PE20090772A1 (es) Derivados de bencimidazol
PE20131377A1 (es) Triazina-oxadiazoles
PE20110298A1 (es) Derivados de picolinamida como inhibidores de cinasa
PE20090709A1 (es) Compuestos heterociclico de 5 miembros
PE20120517A1 (es) Inhibidores del virus de la hepatitis c
PE20142099A1 (es) Derivados de sulfonamida
PE20160843A1 (es) Pirrolidinonas herbicidas
PE20141824A1 (es) Compuestos terapeuticamente activos y sus metodos de uso
PE20090727A1 (es) DERIVADOS DE AMIDA COMO INHIBIDORES DE NaV1.7
PE20121500A1 (es) 2-amino-5,5-difluor-5,6-dihidro-4h-oxazinas como inhibidores de bace 1 y/o bace 2
PE20110062A1 (es) N-(3-(3,5-dimetoxifenetil)-1h-pirazol-5-il)-4-(3,4-dimetilpiperazin-1-il)benzamida y sales del mismo
PE20170947A1 (es) 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1

Legal Events

Date Code Title Description
FC Refusal