MX2018016386A - Proceso de preparacion de un inhibidor de inmunoproteasoma de peptido epoxicetona, y precursores del mismo. - Google Patents

Proceso de preparacion de un inhibidor de inmunoproteasoma de peptido epoxicetona, y precursores del mismo.

Info

Publication number
MX2018016386A
MX2018016386A MX2018016386A MX2018016386A MX2018016386A MX 2018016386 A MX2018016386 A MX 2018016386A MX 2018016386 A MX2018016386 A MX 2018016386A MX 2018016386 A MX2018016386 A MX 2018016386A MX 2018016386 A MX2018016386 A MX 2018016386A
Authority
MX
Mexico
Prior art keywords
precursors
preparing
peptide epoxyketone
immunoproteasome inhibitor
epoxyketone immunoproteasome
Prior art date
Application number
MX2018016386A
Other languages
English (en)
Inventor
Mcminn Dustin
Johnson Henry
Dalziel Sean
Original Assignee
Kezar Life Sciences
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 Kezar Life Sciences filed Critical Kezar Life Sciences
Publication of MX2018016386A publication Critical patent/MX2018016386A/es

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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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C229/36—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D301/00—Preparation of oxiranes
    • C07D301/02—Synthesis of the oxirane ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/12—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/12—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C07D303/32—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/38—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D303/46—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals by amide or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Epoxy Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

En el presente documento se describen métodos para preparar [(2S,3R)-N-[(2S)-3-(ciclopent-1-en-1-il)-1-[(2R)-2-metiloxiran-2- il]-1-oxopropan-2-il]-3-hidroxi-3-(4-metoxifenil)-2-[(2S)-2-[2-(m orfolin-4-il)acetamido]propanamido]propanamida(compuesto "G"): (ver Fórmula) y precursores del mismo.
MX2018016386A 2016-06-29 2017-06-29 Proceso de preparacion de un inhibidor de inmunoproteasoma de peptido epoxicetona, y precursores del mismo. MX2018016386A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662356178P 2016-06-29 2016-06-29
PCT/US2017/039975 WO2018005781A1 (en) 2016-06-29 2017-06-29 Process of preparing a peptide epoxyketone immunoproteasome inhibitor, and precursors thereof

Publications (1)

Publication Number Publication Date
MX2018016386A true MX2018016386A (es) 2019-09-09

Family

ID=59351085

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2018016386A MX2018016386A (es) 2016-06-29 2017-06-29 Proceso de preparacion de un inhibidor de inmunoproteasoma de peptido epoxicetona, y precursores del mismo.

Country Status (17)

Country Link
US (3) US10781192B2 (es)
EP (2) EP4296257A3 (es)
JP (2) JP7065044B2 (es)
KR (2) KR102571568B1 (es)
CN (1) CN109641860A (es)
AR (1) AR108919A1 (es)
AU (1) AU2017290147B2 (es)
BR (1) BR112018077250A2 (es)
CA (1) CA3029418A1 (es)
CL (1) CL2018003873A1 (es)
CO (1) CO2019000866A2 (es)
EA (1) EA201990157A1 (es)
IL (2) IL302234A (es)
MX (1) MX2018016386A (es)
SG (1) SG11201811506UA (es)
TW (1) TWI751177B (es)
WO (1) WO2018005781A1 (es)

Family Cites Families (25)

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US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5340736A (en) 1991-05-13 1994-08-23 The President & Fellows Of Harvard College ATP-dependent protease and use of inhibitors for same in the treatment of cachexia and muscle wasting
AU4499697A (en) 1996-09-13 1998-04-02 New York University Method for treating parasitic diseases with proteasome inhibitors
JP5354836B2 (ja) 2002-11-06 2013-11-27 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド プロテアソームインヒビターを使用する癌を処置するための方法および組成物
PT1948678E (pt) 2005-11-09 2013-07-16 Onyx Therapeutics Inc Compostos para inibição de enzimas
US7691852B2 (en) 2006-06-19 2010-04-06 Onyx Therapeutics, Inc. Compounds for enzyme inhibition
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KR20170040374A (ko) 2007-10-04 2017-04-12 오닉스 세라퓨틱스, 인크. 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성
CN101525370A (zh) * 2008-03-06 2009-09-09 海南建邦制药科技有限公司 一种新型高效多肽合成缩合剂
MX2011004225A (es) 2008-10-21 2011-06-21 Onyx Therapeutics Inc Terapia de combinacion con epoxicetonas peptidicas.
TWI504598B (zh) 2009-03-20 2015-10-21 Onyx Therapeutics Inc 結晶性三肽環氧酮蛋白酶抑制劑
WO2011060179A1 (en) 2009-11-13 2011-05-19 Onyx Therapeutics, Inc Use of peptide epoxyketones for metastasis suppression
US8697646B2 (en) 2010-04-07 2014-04-15 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor
US8609610B2 (en) 2011-02-18 2013-12-17 Trustees Of Dartmouth College Inhibitors of the trypsin-like site of the proteasome and methods of use thereof
US20140187771A1 (en) 2011-05-02 2014-07-03 Gilead Sciences, Inc. Amorphous solid salts
EP2662094B1 (en) 2012-05-08 2024-04-17 Onyx Therapeutics, Inc. Cylodextrin Complexation Methods for Formulating Peptide Proteasome Inhibitors
JP6176259B2 (ja) 2012-06-29 2017-08-09 日産化学工業株式会社 立体選択的なエポキシケトン化合物の製造方法
CA2892368A1 (en) 2012-10-11 2014-04-17 F. Hoffmann-La Roche Ag Ketoamide immunoproteasome inhibitors
EP2906582A1 (en) 2012-10-12 2015-08-19 F. Hoffmann-La Roche AG Macrocyclic ketoamide immunoproteasome inhibitors
TW201422255A (zh) * 2012-10-24 2014-06-16 Onyx Therapeutics Inc 用於蛋白酶體抑制劑之調整釋放製劑
JP2016515127A (ja) * 2013-03-14 2016-05-26 オニキス セラピューティクス， インク．Ｏｎｙｘ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． ジペプチド及びトリペプチドエポキシケトンプロテアーゼ阻害剤
KR102365509B1 (ko) * 2013-03-14 2022-02-21 오닉스 세라퓨틱스, 인크. 트리펩타이드 에폭시 케톤 프로테이스 억제제
AR095426A1 (es) * 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
CN104710507B (zh) * 2013-12-11 2018-08-14 深圳翰宇药业股份有限公司 一种卡非佐米的制备方法
CN104230857A (zh) 2014-08-19 2014-12-24 上海皓元生物医药科技有限公司 卡非佐米(Carfilzomib)的中间体化合物的制备方法及其中间体化合物

Also Published As

Publication number Publication date
JP7065044B2 (ja) 2022-05-11
CL2018003873A1 (es) 2019-06-21
US20190194155A1 (en) 2019-06-27
KR20190025945A (ko) 2019-03-12
EA201990157A1 (ru) 2019-05-31
TW201800397A (zh) 2018-01-01
CA3029418A1 (en) 2018-01-04
US11498907B2 (en) 2022-11-15
IL263771B2 (en) 2023-09-01
TWI751177B (zh) 2022-01-01
AU2017290147B2 (en) 2021-09-09
KR20230056798A (ko) 2023-04-27
EP4296257A2 (en) 2023-12-27
EP3478669B1 (en) 2023-08-30
AU2017290147A1 (en) 2019-01-17
WO2018005781A1 (en) 2018-01-04
JP7392031B2 (ja) 2023-12-05
SG11201811506UA (en) 2019-01-30
JP2022105081A (ja) 2022-07-12
BR112018077250A2 (pt) 2019-04-02
IL302234A (en) 2023-06-01
US10781192B2 (en) 2020-09-22
CN109641860A (zh) 2019-04-16
IL263771B1 (en) 2023-05-01
EP3478669A1 (en) 2019-05-08
AR108919A1 (es) 2018-10-10
KR102571568B1 (ko) 2023-08-25
EP4296257A3 (en) 2024-03-20
CO2019000866A2 (es) 2019-04-12
IL263771A (en) 2019-01-31
US20230135100A1 (en) 2023-05-04
KR102524751B1 (ko) 2023-04-21
US20200407334A1 (en) 2020-12-31
JP2019527677A (ja) 2019-10-03

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