MX2016005567A - Profarmacos de antagonista de (s)-1-fenil-2-(piridin-2-il)etanamin a (nmda). - Google Patents

Profarmacos de antagonista de (s)-1-fenil-2-(piridin-2-il)etanamin a (nmda).

Info

Publication number
MX2016005567A
MX2016005567A MX2016005567A MX2016005567A MX2016005567A MX 2016005567 A MX2016005567 A MX 2016005567A MX 2016005567 A MX2016005567 A MX 2016005567A MX 2016005567 A MX2016005567 A MX 2016005567A MX 2016005567 A MX2016005567 A MX 2016005567A
Authority
MX
Mexico
Prior art keywords
nmda antagonist
prodrugs
antagonist prodrugs
nmda
ethanamine
Prior art date
Application number
MX2016005567A
Other languages
English (en)
Inventor
Michael Quirk
Dirk Reinhold Weigelt
Peter Roberto Bernstein
Michael Balestra
Gunnar Nordvall
Katharina Högdin
Per Jonas Malmborg
Annika Kers
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of MX2016005567A publication Critical patent/MX2016005567A/es

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Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • 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
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • C07K5/06095—Arg-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06147—Dipeptides with the first amino acid being heterocyclic and His-amino acid; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06156—Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención se refiere a profármacos de un antagonista de NMDA, (S)-1-fenil-2-(piridin-2-il)etanamina, útiles para el tratamiento de depresión (particularmente trastorno depresivo mayor) o dolor; composiciones que los comprenden, y métodos para elaborarlos.
MX2016005567A 2013-11-05 2014-10-30 Profarmacos de antagonista de (s)-1-fenil-2-(piridin-2-il)etanamin a (nmda). MX2016005567A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361899903P 2013-11-05 2013-11-05
PCT/GB2014/053236 WO2015067923A1 (en) 2013-11-05 2014-10-30 Nmda antagonist prodrugs

Publications (1)

Publication Number Publication Date
MX2016005567A true MX2016005567A (es) 2016-07-21

Family

ID=51947383

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2016005567A MX2016005567A (es) 2013-11-05 2014-10-30 Profarmacos de antagonista de (s)-1-fenil-2-(piridin-2-il)etanamin a (nmda).
MX2020011946A MX2020011946A (es) 2013-11-05 2014-10-30 Profarmacos de antagonista de (s)-1-fenil-2-(piridin-2-il)etanamin a (nmda).

Family Applications After (1)

Application Number Title Priority Date Filing Date
MX2020011946A MX2020011946A (es) 2013-11-05 2014-10-30 Profarmacos de antagonista de (s)-1-fenil-2-(piridin-2-il)etanamin a (nmda).

Country Status (24)

Country Link
US (4) US9822075B2 (es)
EP (3) EP3066091B1 (es)
JP (4) JP6479834B2 (es)
KR (2) KR102469167B1 (es)
CN (1) CN105683180B (es)
AR (1) AR098319A1 (es)
AU (1) AU2014345407B2 (es)
CA (1) CA2928004C (es)
CY (1) CY1121749T1 (es)
DK (1) DK3066091T3 (es)
ES (2) ES2733344T3 (es)
HR (1) HRP20191159T1 (es)
HU (1) HUE045001T2 (es)
LT (1) LT3066091T (es)
MX (2) MX2016005567A (es)
PL (1) PL3066091T3 (es)
PT (1) PT3066091T (es)
RS (1) RS58991B1 (es)
RU (1) RU2695372C2 (es)
SI (1) SI3066091T1 (es)
TR (1) TR201909632T4 (es)
TW (1) TW201609653A (es)
UY (1) UY35823A (es)
WO (1) WO2015067923A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI3066091T1 (sl) 2013-11-05 2019-09-30 Astrazeneca Ab NMDA antagonist predzdravila
WO2018098344A1 (en) * 2016-11-28 2018-05-31 Biohaven Pharmaceutical Holding Company Ltd. Prodrugs of lanicemine and their method of use
CN107578281B (zh) * 2017-08-31 2021-03-30 湖南大学 电子商务环境下用户优惠券行为预测方法及模型构建方法
US20230190719A1 (en) * 2020-06-23 2023-06-22 Biohaven Therapeutics Ltd. Topical formulations of (1s)-1-phenyl-2-pyridin-2-ylethanamine

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE7909514L (sv) 1979-11-16 1981-05-17 Astra Laekemedel Ab Nya halofenyl-pyridyl-allylaminderivat
US4769466A (en) * 1987-02-06 1988-09-06 Pennwalt Corporation 2-aminoacetamide pyridinyl derivatives
DE68925933T2 (de) * 1988-08-12 1996-08-14 Fisons Corp Arylalkylamine und -amide mit krampflösender und nervenschützender Wirkung
JP3120810B2 (ja) 1992-04-03 2000-12-25 アストラゼネカ・アクチエボラーグ 神経変性疾患を治療するための化合物の製造方法
SE9901077D0 (sv) 1999-03-23 1999-03-23 Astra Ab Novel use
SE9901340D0 (sv) 1999-04-15 1999-04-15 Astra Pharma Prod Novel process
US6613879B1 (en) * 1999-05-14 2003-09-02 Boehringer Ingelheim Pharma Kg FAP-activated anti-tumour compounds
PA8525601A1 (es) 2000-08-21 2002-04-25 Hoffmann La Roche Profarmacos de (3s,4s)-4-bencil-1-[2-(4-hidroxi-bencenosulfonil)-etil]-piperidin-3-ol
CN1533270A (zh) 2001-06-11 2004-09-29 ʲŵ�������޹�˾ 具有降低毒性的gaba类似物前药的口服给药剂型
GB0310593D0 (en) 2003-05-08 2003-06-11 Leuven K U Res & Dev Peptidic prodrugs
EP1716115B1 (en) 2003-12-30 2013-02-27 XenoPort, Inc. Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
WO2007030577A2 (en) * 2005-09-08 2007-03-15 Shire Llc Prodrugs of t3 and t4 with enhanced bioavailability
CN101246417B (zh) 2007-02-13 2010-09-29 艾威梯科技(北京)有限公司 音频数据流输入/输出无间断软件切换的方法和系统
JP5563483B2 (ja) 2008-01-25 2014-07-30 ゼノポート，インコーポレイティド アシロキシアルキルカルバメートプロドラッグの合成に使用されるアシロキシアルキルチオカーボネートの鏡像異性的な分解
US8299291B2 (en) 2008-08-07 2012-10-30 Xenoport, Inc. Methods of synthesizing 1-(acyloxy)-alkyl carbamate prodrugs
EP2525830B1 (en) * 2010-01-22 2016-05-11 Ascendis Pharma A/S Dipeptide-based prodrug linkers for aliphatic amine-containing drugs
US8580850B2 (en) * 2011-08-11 2013-11-12 Xenoport, Inc. Anhydrous and hemihydrate crystalline forms of an (R)-baclofen prodrug, methods of synthesis and methods of use
SI3066091T1 (sl) 2013-11-05 2019-09-30 Astrazeneca Ab NMDA antagonist predzdravila

Also Published As

Publication number Publication date
RU2016119493A3 (es) 2018-06-29
ES2894903T3 (es) 2022-02-16
EP3066091B1 (en) 2019-04-03
TR201909632T4 (tr) 2019-07-22
ES2733344T3 (es) 2019-11-28
SI3066091T1 (sl) 2019-09-30
EP3564234B1 (en) 2021-09-29
KR102469167B1 (ko) 2022-11-22
CN111187202A (zh) 2020-05-22
JP6479834B2 (ja) 2019-03-06
EP4001272A1 (en) 2022-05-25
CN105683180A (zh) 2016-06-15
BR112016009949A8 (pt) 2020-04-14
UY35823A (es) 2015-04-30
DK3066091T3 (da) 2019-07-15
HRP20191159T1 (hr) 2019-10-04
EP4001272C0 (en) 2024-11-13
MX2020011946A (es) 2022-08-10
RS58991B1 (sr) 2019-08-30
JP6856737B2 (ja) 2021-04-07
US20160280647A1 (en) 2016-09-29
US20180037550A1 (en) 2018-02-08
AU2014345407B2 (en) 2018-10-18
TW201609653A (zh) 2016-03-16
PL3066091T3 (pl) 2019-10-31
RU2695372C2 (ru) 2019-07-23
CY1121749T1 (el) 2020-07-31
PT3066091T (pt) 2019-07-11
EP3564234A1 (en) 2019-11-06
EP3066091A1 (en) 2016-09-14
CN105683180B (zh) 2020-01-21
JP2019081781A (ja) 2019-05-30
AR098319A1 (es) 2016-05-26
KR102336426B1 (ko) 2021-12-08
US10815199B2 (en) 2020-10-27
CA2928004C (en) 2022-04-12
WO2015067923A1 (en) 2015-05-14
JP2021100950A (ja) 2021-07-08
JP7234278B2 (ja) 2023-03-07
JP2020055857A (ja) 2020-04-09
US9822075B2 (en) 2017-11-21
KR20160079094A (ko) 2016-07-05
CA2928004A1 (en) 2015-05-14
US20210040039A1 (en) 2021-02-11
HUE045001T2 (hu) 2019-12-30
JP6633233B2 (ja) 2020-01-22
US20190152914A1 (en) 2019-05-23
RU2016119493A (ru) 2017-12-07
AU2014345407A1 (en) 2016-06-02
LT3066091T (lt) 2019-07-10
EP4001272B1 (en) 2024-11-13
KR20210148443A (ko) 2021-12-07
JP2016535098A (ja) 2016-11-10
US10207994B2 (en) 2019-02-19

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