ES2894903T3 - Profármacos antagonistas de NMDA - Google Patents

Profármacos antagonistas de NMDA Download PDF

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Publication number
ES2894903T3
ES2894903T3 ES19166031T ES19166031T ES2894903T3 ES 2894903 T3 ES2894903 T3 ES 2894903T3 ES 19166031 T ES19166031 T ES 19166031T ES 19166031 T ES19166031 T ES 19166031T ES 2894903 T3 ES2894903 T3 ES 2894903T3
Authority
ES
Spain
Prior art keywords
pyridin
phenyl
ethanamine
pyrrolidine
compound
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES19166031T
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English (en)
Spanish (es)
Inventor
Gunnar Nordvall
Katharina Högdin
Per Jonas Malmborg
Annika Kers
Dirk Weigelt
Peter Bernstein
Michael Quirk
Michael Balestra
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AstraZeneca AB
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.)
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Publication date
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Publication of ES2894903T3 publication Critical patent/ES2894903T3/es
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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
    • C07D213/36Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40Acylated substituent nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4402Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043Leu-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052Val-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06086Dipeptides with the first amino acid being basic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06086Dipeptides with the first amino acid being basic
    • C07K5/06095Arg-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06104Dipeptides with the first amino acid being acidic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06147Dipeptides with the first amino acid being heterocyclic and His-amino acid; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06156Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal 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)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
ES19166031T 2013-11-05 2014-10-30 Profármacos antagonistas de NMDA Active ES2894903T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361899903P 2013-11-05 2013-11-05

Publications (1)

Publication Number Publication Date
ES2894903T3 true ES2894903T3 (es) 2022-02-16

Family

ID=51947383

Family Applications (3)

Application Number Title Priority Date Filing Date
ES14802476T Active ES2733344T3 (es) 2013-11-05 2014-10-30 Profármacos antagonistas de NMDA
ES19166031T Active ES2894903T3 (es) 2013-11-05 2014-10-30 Profármacos antagonistas de NMDA
ES21196371T Active ES2999064T3 (en) 2013-11-05 2014-10-30 Nmda antagonist prodrugs

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES14802476T Active ES2733344T3 (es) 2013-11-05 2014-10-30 Profármacos antagonistas de NMDA

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES21196371T Active ES2999064T3 (en) 2013-11-05 2014-10-30 Nmda antagonist prodrugs

Country Status (25)

Country Link
US (4) US9822075B2 (OSRAM)
EP (3) EP3066091B1 (OSRAM)
JP (4) JP6479834B2 (OSRAM)
KR (2) KR102336426B1 (OSRAM)
CN (2) CN105683180B (OSRAM)
AR (1) AR098319A1 (OSRAM)
AU (1) AU2014345407B2 (OSRAM)
CA (1) CA2928004C (OSRAM)
CY (1) CY1121749T1 (OSRAM)
DK (1) DK3066091T3 (OSRAM)
ES (3) ES2733344T3 (OSRAM)
HR (2) HRP20241784T1 (OSRAM)
HU (2) HUE045001T2 (OSRAM)
LT (1) LT3066091T (OSRAM)
MX (2) MX377276B (OSRAM)
PL (2) PL3066091T3 (OSRAM)
PT (1) PT3066091T (OSRAM)
RS (2) RS58991B1 (OSRAM)
RU (1) RU2695372C2 (OSRAM)
SI (1) SI3066091T1 (OSRAM)
SM (1) SMT202500023T1 (OSRAM)
TR (1) TR201909632T4 (OSRAM)
TW (1) TW201609653A (OSRAM)
UY (1) UY35823A (OSRAM)
WO (1) WO2015067923A1 (OSRAM)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105683180B (zh) 2013-11-05 2020-01-21 阿斯利康(瑞典)有限公司 Nmda拮抗剂前药
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
KR20230026449A (ko) * 2020-06-23 2023-02-24 바이오하벤 테라퓨틱스 리미티드 (1s)-1-페닐-2-피리딘-2-일레탄아민의 국소 제형
WO2025137661A1 (en) * 2023-12-22 2025-06-26 Biohaven Therapeutics Ltd. Combination treatment of neurological disorders

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
SG52662A1 (en) * 1988-08-12 1998-09-28 Astra Ab Arylkalkyl-amines and -amides having anticonvulsant and neuroprotective properties
UA29437C2 (uk) 1992-04-03 2000-11-15 Астра АБ (s)-альфа-феніл-2-піридинетанамін або його сіль з неорганічною кислотою, які мають протисудомну активність, спосіб їх отримання, лікарський препарат на їх основі та спосіб лікування судом
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
US6407235B1 (en) 2000-08-21 2002-06-18 Hoffmann-La Roche Inc. Prodrug acid esters of [2-(4-benzyl-3-hydroxy-piperidin-1-yl)-ethansulfonyl]phenol
JP4216713B2 (ja) * 2001-06-11 2009-01-28 ゼノポート,インコーポレイティド Gaba類似体のプロドラッグ、組成物およびその使用
GB0310593D0 (en) 2003-05-08 2003-06-11 Leuven K U Res & Dev Peptidic prodrugs
JP4927563B2 (ja) 2003-12-30 2012-05-09 ゼノポート,インコーポレイティド アシルオキシアルキルカルバメートプロドラッグ及び中間体の合成
CA2621847A1 (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
ES2601852T3 (es) 2008-01-25 2017-02-16 Xenoport, Inc. Forma cristalina de sales de calcio de ácidos (3S)-aminometil-5-metil-hexanoicos y métodos de uso
US8299291B2 (en) 2008-08-07 2012-10-30 Xenoport, Inc. Methods of synthesizing 1-(acyloxy)-alkyl carbamate prodrugs
WO2011089216A1 (en) * 2010-01-22 2011-07-28 Ascendis Pharma As Dipeptide-based prodrug linkers for aliphatic amine-containing drugs
WO2013023155A1 (en) * 2011-08-11 2013-02-14 Xenoport, Inc. Anhydrous and hemihydrate crystalline forms of an (r)-baclofen prodrug, methods of synthesis and methods of use
CN105683180B (zh) 2013-11-05 2020-01-21 阿斯利康(瑞典)有限公司 Nmda拮抗剂前药

Also Published As

Publication number Publication date
CN105683180B (zh) 2020-01-21
CA2928004A1 (en) 2015-05-14
PT3066091T (pt) 2019-07-11
TW201609653A (zh) 2016-03-16
EP3564234A1 (en) 2019-11-06
MX394633B (es) 2025-03-24
US20210040039A1 (en) 2021-02-11
UY35823A (es) 2015-04-30
JP2021100950A (ja) 2021-07-08
EP4001272C0 (en) 2024-11-13
ES2733344T3 (es) 2019-11-28
AR098319A1 (es) 2016-05-26
CN111187202B (zh) 2025-01-21
HUE070532T2 (hu) 2025-06-28
US10815199B2 (en) 2020-10-27
SMT202500023T1 (it) 2025-03-12
ES2999064T3 (en) 2025-02-24
JP2019081781A (ja) 2019-05-30
KR102336426B1 (ko) 2021-12-08
EP4001272A1 (en) 2022-05-25
DK3066091T3 (da) 2019-07-15
RS66369B1 (sr) 2025-01-31
EP3066091A1 (en) 2016-09-14
HRP20191159T1 (hr) 2019-10-04
HUE045001T2 (hu) 2019-12-30
MX377276B (es) 2025-03-07
EP4001272B1 (en) 2024-11-13
CN111187202A (zh) 2020-05-22
US9822075B2 (en) 2017-11-21
US20190152914A1 (en) 2019-05-23
JP6633233B2 (ja) 2020-01-22
EP3564234B1 (en) 2021-09-29
LT3066091T (lt) 2019-07-10
US20180037550A1 (en) 2018-02-08
PL4001272T3 (pl) 2025-02-10
CN105683180A (zh) 2016-06-15
HRP20241784T1 (hr) 2025-02-28
WO2015067923A1 (en) 2015-05-14
KR20210148443A (ko) 2021-12-07
US10207994B2 (en) 2019-02-19
KR20160079094A (ko) 2016-07-05
JP6479834B2 (ja) 2019-03-06
AU2014345407A1 (en) 2016-06-02
RS58991B1 (sr) 2019-08-30
RU2016119493A (ru) 2017-12-07
SI3066091T1 (sl) 2019-09-30
KR102469167B1 (ko) 2022-11-22
BR112016009949A8 (pt) 2020-04-14
CA2928004C (en) 2022-04-12
JP2016535098A (ja) 2016-11-10
MX2020011946A (es) 2022-08-10
CY1121749T1 (el) 2020-07-31
JP7234278B2 (ja) 2023-03-07
JP6856737B2 (ja) 2021-04-07
JP2020055857A (ja) 2020-04-09
MX2016005567A (es) 2016-07-21
TR201909632T4 (tr) 2019-07-22
RU2695372C2 (ru) 2019-07-23
PL3066091T3 (pl) 2019-10-31
US20160280647A1 (en) 2016-09-29
RU2016119493A3 (OSRAM) 2018-06-29
EP3066091B1 (en) 2019-04-03
AU2014345407B2 (en) 2018-10-18

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