ES2733344T3 - Profármacos antagonistas de NMDA - Google Patents

Profármacos antagonistas de NMDA Download PDF

Info

Publication number
ES2733344T3
ES2733344T3 ES14802476T ES14802476T ES2733344T3 ES 2733344 T3 ES2733344 T3 ES 2733344T3 ES 14802476 T ES14802476 T ES 14802476T ES 14802476 T ES14802476 T ES 14802476T ES 2733344 T3 ES2733344 T3 ES 2733344T3
Authority
ES
Spain
Prior art keywords
phenyl
pyridin
ethanamine
mmol
pyrrolidin
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
ES14802476T
Other languages
English (en)
Spanish (es)
Inventor
Gunnar Nordvall
Katharina Högdin
Per Jonas Malmborg
Annika Kers
Dirk Weigelt
Peter Bernstein
Michael Quirk
Michael Balestra
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
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.)
Filing date
Publication date
Application filed by AstraZeneca AB filed Critical AstraZeneca AB
Application granted granted Critical
Publication of ES2733344T3 publication Critical patent/ES2733344T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • 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)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (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)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
ES14802476T 2013-11-05 2014-10-30 Profármacos antagonistas de NMDA Active ES2733344T3 (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
ES2733344T3 true ES2733344T3 (es) 2019-11-28

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 After (2)

Application Number Title Priority Date Filing Date
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

Country Status (25)

Country Link
US (4) US9822075B2 (enExample)
EP (3) EP3066091B1 (enExample)
JP (4) JP6479834B2 (enExample)
KR (2) KR102336426B1 (enExample)
CN (2) CN111187202B (enExample)
AR (1) AR098319A1 (enExample)
AU (1) AU2014345407B2 (enExample)
CA (1) CA2928004C (enExample)
CY (1) CY1121749T1 (enExample)
DK (1) DK3066091T3 (enExample)
ES (3) ES2733344T3 (enExample)
HR (2) HRP20191159T1 (enExample)
HU (2) HUE070532T2 (enExample)
LT (1) LT3066091T (enExample)
MX (2) MX394633B (enExample)
PL (2) PL4001272T3 (enExample)
PT (1) PT3066091T (enExample)
RS (2) RS58991B1 (enExample)
RU (1) RU2695372C2 (enExample)
SI (1) SI3066091T1 (enExample)
SM (1) SMT202500023T1 (enExample)
TR (1) TR201909632T4 (enExample)
TW (1) TW201609653A (enExample)
UY (1) UY35823A (enExample)
WO (1) WO2015067923A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102336426B1 (ko) 2013-11-05 2021-12-08 아스트라제네카 아베 Nmda 길항제 전구약물
US11358935B2 (en) 2016-11-28 2022-06-14 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
BR112022025900A2 (pt) 2020-06-23 2023-01-10 Biohaven Therapeutics Ltd Formulações tópicas de (1s)-1-fenil-2-piridin-2-iletanamina
CN122421958A (zh) * 2023-12-22 2026-07-17 拜奥海芬治疗学有限公司 神经性障碍的组合治疗

Family Cites Families (19)

* 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
ES2083972T3 (es) * 1988-08-12 1996-05-01 Astra Ab Arilalquil-aminas y -amidas con propiedades anticonvulsivas y neuroprotectoras.
ES2142320T3 (es) 1991-10-30 2000-04-16 Astra Ab Derivados de 2-pirazinil-etilamina y su uso como productos farmaceuticos.
NZ251384A (en) * 1992-04-03 1996-10-28 Fisons Corp (s)-enantiomer of 1-phenyl-2-(2-pyridinyl) ethylamine and medicaments
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
AU2002310409C1 (en) 2001-06-11 2008-04-17 Xenoport, Inc. Orally administered dosage forms of GABA analog prodrugs having reduced toxicity
GB0310593D0 (en) * 2003-05-08 2003-06-11 Leuven K U Res & Dev Peptidic prodrugs
CA2551859C (en) 2003-12-30 2011-10-04 Xenoport, Inc. Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
EP1929030A2 (en) * 2005-09-08 2008-06-11 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
CA2710538A1 (en) 2008-01-25 2009-07-30 Xenoport, Inc. Crystalline form of a (3s)-aminomethyl-5-methyl-hexanoic acid prodrug and methods of use
WO2010017504A1 (en) * 2008-08-07 2010-02-11 Xenoport, Inc. Methods of synthesizing 1-(acyloxy)-alkyl carbamate prodrugs
US9062094B2 (en) * 2010-01-22 2015-06-23 Ascendis Pharma As 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
KR102336426B1 (ko) 2013-11-05 2021-12-08 아스트라제네카 아베 Nmda 길항제 전구약물

Also Published As

Publication number Publication date
HUE045001T2 (hu) 2019-12-30
CN105683180B (zh) 2020-01-21
EP4001272B1 (en) 2024-11-13
US20190152914A1 (en) 2019-05-23
EP3066091A1 (en) 2016-09-14
EP4001272C0 (en) 2024-11-13
KR20210148443A (ko) 2021-12-07
CA2928004C (en) 2022-04-12
ES2999064T3 (en) 2025-02-24
CN105683180A (zh) 2016-06-15
SI3066091T1 (sl) 2019-09-30
HUE070532T2 (hu) 2025-06-28
PT3066091T (pt) 2019-07-11
JP2021100950A (ja) 2021-07-08
HRP20191159T1 (hr) 2019-10-04
JP2016535098A (ja) 2016-11-10
CY1121749T1 (el) 2020-07-31
RU2016119493A3 (enExample) 2018-06-29
US12516023B2 (en) 2026-01-06
AU2014345407A1 (en) 2016-06-02
BR112016009949A8 (pt) 2020-04-14
JP7234278B2 (ja) 2023-03-07
AU2014345407B2 (en) 2018-10-18
US10815199B2 (en) 2020-10-27
SMT202500023T1 (it) 2025-03-12
RS66369B1 (sr) 2025-01-31
AR098319A1 (es) 2016-05-26
KR102336426B1 (ko) 2021-12-08
KR20160079094A (ko) 2016-07-05
RS58991B1 (sr) 2019-08-30
JP6856737B2 (ja) 2021-04-07
MX2020011946A (es) 2022-08-10
MX2016005567A (es) 2016-07-21
JP2019081781A (ja) 2019-05-30
JP6633233B2 (ja) 2020-01-22
US20180037550A1 (en) 2018-02-08
US9822075B2 (en) 2017-11-21
TR201909632T4 (tr) 2019-07-22
US20160280647A1 (en) 2016-09-29
MX377276B (es) 2025-03-07
PL3066091T3 (pl) 2019-10-31
RU2016119493A (ru) 2017-12-07
CN111187202B (zh) 2025-01-21
EP3066091B1 (en) 2019-04-03
ES2894903T3 (es) 2022-02-16
HRP20241784T1 (hr) 2025-02-28
LT3066091T (lt) 2019-07-10
MX394633B (es) 2025-03-24
CN111187202A (zh) 2020-05-22
JP2020055857A (ja) 2020-04-09
JP6479834B2 (ja) 2019-03-06
UY35823A (es) 2015-04-30
EP4001272A1 (en) 2022-05-25
RU2695372C2 (ru) 2019-07-23
US10207994B2 (en) 2019-02-19
TW201609653A (zh) 2016-03-16
US20210040039A1 (en) 2021-02-11
KR102469167B1 (ko) 2022-11-22
CA2928004A1 (en) 2015-05-14
WO2015067923A1 (en) 2015-05-14
DK3066091T3 (da) 2019-07-15
PL4001272T3 (pl) 2025-02-10
EP3564234B1 (en) 2021-09-29
EP3564234A1 (en) 2019-11-06

Similar Documents

Publication Publication Date Title
US12516023B2 (en) NMDA antagonist prodrugs
KR101413955B1 (ko) 아지리디닐-에포틸론 화합물
HK40076024A (en) Nmda antagonist prodrugs
HK40076024B (en) Nmda antagonist prodrugs
HK40014361B (en) Nmda antagonist prodrugs
HK40014361A (en) Nmda antagonist prodrugs
WO2019217465A1 (en) Calpain modulators and therapeutic uses thereof background
HK1226721A1 (en) Nmda antagonist prodrugs
HK1226721B (en) Nmda antagonist prodrugs
BR112016009949B1 (pt) Composto pró-fármaco antagonista de nmda, composição farmacêutica, e, uso de um composto