HRP20220446T1 - Lijekovi inhibitora membranskog antigena specifičnog za prostatu (psma) - Google Patents

Lijekovi inhibitora membranskog antigena specifičnog za prostatu (psma) Download PDF

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Publication number
HRP20220446T1
HRP20220446T1 HRP20220446TT HRP20220446T HRP20220446T1 HR P20220446 T1 HRP20220446 T1 HR P20220446T1 HR P20220446T T HRP20220446T T HR P20220446TT HR P20220446 T HRP20220446 T HR P20220446T HR P20220446 T1 HRP20220446 T1 HR P20220446T1
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Croatia
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compound
cr5r6
formula
disease
image
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HRP20220446TT
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English (en)
Inventor
Barbara Slusher
Rana RAIS
Marcela Krecmerova
Tomas Tichy
Pavel Majer
Andrej JANCARIK
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The Johns Hopkins University
Institute Of Organic Chemistry And Biochemistry As Cr, V.V.I.
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Application filed by The Johns Hopkins University, Institute Of Organic Chemistry And Biochemistry As Cr, V.V.I. filed Critical The Johns Hopkins University
Publication of HRP20220446T1 publication Critical patent/HRP20220446T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3808Acyclic saturated acids which can have further substituents on alkyl
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40Esters thereof
    • C07F9/4003Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006Esters of acyclic acids which can have further substituents on alkyl
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40Esters thereof
    • C07F9/4071Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4075Esters with hydroxyalkyl compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40Esters thereof
    • C07F9/4071Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4084Esters with hydroxyaryl compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40Esters thereof
    • C07F9/4071Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4087Esters with arylalkanols
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/44Amides thereof
    • C07F9/4461Amides thereof the amide moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4465Amides thereof the amide moiety containing a substituent or a structure which is considered as characteristic of aliphatic amines

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (12)

1. Spoj formule (I) ili formule (II): [image] [image] pri čemu: svaki R1, R3, i R4 je izabran od sljedećih: pivaloiloksimetil (POM) i izopropiloksikarboniloksimetil (POC), tako da ili oba R3, i R4 su svaki pivaloiloksimetil (POM), ili oba R3, i R4 su svaki izopropiloksikarboniloksimetil (POC), i svaki R2, je neovisno izabran iz grupe koja se sastoji od sljedećih: H, alkil, Ar, -(CR5R6)n-Ar, -(CR5R6)n-O-C(=O)-R7, -(CR5R6)n-C(=O)-O-R7, -(CR5R6)n-O-C(=O)-O-R7,-(CR5R6)n-O-R7, -(CR5R6)n-O-[(CR5R6)n-O]m-R7, -(CR5R6)n-Ar-O-C(=O)-R7, -Ar-C(=O)-O-(CR5R6)n-R7, -(CR5R6)n-NR8R9, i -(CR5R6)n-C(=O)-NR8R9; gdje: n je cijeli broj od 1 do 20; m je cijeli broj od 1 do 20; svaki R3' i R4' su neovisno H ili alkil; svaki R5 i R6 je neovisno izabran iz grupe koja se sastoji od sljedećih: H, alkil i alkilaril; svaki R7 je neovisno ravan ili razgranati alkil; Ar je aril, supstituirani aril, heteroaril ili supstituirani heteroaril; i R8 i R9 su svaki neovisno H ili alkil; i njihove farmaceutski prihvatljive soli.
2. Spoj prema zahtjevu 1, naznačen time što je spoj formule (I) izabran iz grupe koja se sastoji od: [image] i [image]
3. Spoj prema zahtjevu 1, naznačen time što spoj formule (I) je [image]
4. Spoj prema zahtjevu 1, naznačen time što spoj formule (I) je [image]
5. Spoj prema zahtjevu 1, naznačen time što spoj formule (I) je [image]
6. Spoj sljedeće formule [image]
7. Farmaceutska kompozicija koja sadrži spoj prema bilo kojem od zahtjeva 1-6 i farmaceutski prihvatljiv ekscipijens.
8. Spoj ili kompozicija prema bilo kojem od zahtjeva 1-7 za uporabu u liječenju bolesti ili stanja.
9. Spoj ili kompozicija za uporabu prema zahtjevu 8, naznačen time što je bolest ili stanje izabrano iz grupe koja se sastoji od sljedećih: neurodegenerativna bolest, multipla skleroza (MS), rak, angiogeneza i upalna bolest crijeva.
10. Spoj ili kompozicija za uporabu prema zahtjevu 9, naznačen time što je neurodegenerativna bolest izabrana iz grupe koja se sastoji od sljedećih: amiotrofna lateralna skleroza (ALS), Parkinsonova bolest (PD), Alzheimerova bolest (AD), Huntingtonova bolest, demencija sa Lewyjevim tijelima (DLB), shizofrenija, bol, epilepsija, moždani udar i traumatska povreda mozga (TBI).
11. Spoj ili kompozicija za uporabu prema zahtjevu 8, naznačen time što bolest ili stanje rezultira viškom aktivnosti PSMA.
12. Spoj ili kompozicija za uporabu prema zahtjevu 11, naznačen time što je višak aktivnosti PSMA inhibiran kada se primjenjuje spoj formule (I), spoj formule (II) ili njegova farmaceutska kompozicija.
HRP20220446TT 2014-08-06 2015-08-06 Lijekovi inhibitora membranskog antigena specifičnog za prostatu (psma) HRP20220446T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462033926P 2014-08-06 2014-08-06
EP15829215.1A EP3177632B1 (en) 2014-08-06 2015-08-06 Prodrugs of prostate specific membrane antigen (psma) inhibitor
PCT/US2015/044053 WO2016022827A1 (en) 2014-08-06 2015-08-06 Prodrugs of prostate specific membrane antigen (psma) inhibitor

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US (4) US9988407B2 (hr)
EP (1) EP3177632B1 (hr)
CA (1) CA2961880C (hr)
CY (1) CY1125201T1 (hr)
DK (1) DK3177632T3 (hr)
ES (1) ES2908411T3 (hr)
HR (1) HRP20220446T1 (hr)
HU (1) HUE058072T2 (hr)
LT (1) LT3177632T (hr)
PL (1) PL3177632T3 (hr)
PT (1) PT3177632T (hr)
RS (1) RS63082B1 (hr)
SI (1) SI3177632T1 (hr)
WO (1) WO2016022827A1 (hr)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4374924A2 (en) 2013-10-18 2024-05-29 Novartis AG Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer
US10172873B2 (en) * 2014-08-06 2019-01-08 The Johns Hopkins University Methods for treating inflammatory bowel disease using prostate specific membrane antigen (PSMA) inhibitors
LT3177632T (lt) 2014-08-06 2022-04-25 The Johns Hopkins University Prostatos specifinio membraninio antigeno (psma) inhibitoriaus provaistai
JP2020530007A (ja) * 2017-04-11 2020-10-15 ザ・ジョンズ・ホプキンス・ユニバーシティ Psma標的化ガンイメージングまたは放射線療法中の健康組織保護のための2−pmpaのプロドラッグ
GB201810965D0 (en) * 2018-07-04 2018-08-15 Univ College Cardiff Consultants Ltd Phosphoantigen prodrug compounds
WO2020030954A1 (en) 2018-08-09 2020-02-13 Integrative Medicine Clinic, Sia Theranostics-like protein sanps conjugated to integrin and pmsa targeting peptides and therapy of prostate cancer
US20210323985A1 (en) * 2018-09-21 2021-10-21 Endocyte, Inc. Shielding agents and their use

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US6071965A (en) * 1996-06-17 2000-06-06 Guilford Pharmaceuticals Inc. Phosphinic alkanoic acid derivatives
DE60238435D1 (de) 2001-10-26 2011-01-05 Scripps Research Inst Gezielte thrombose durch gewebefaktor polypeptiden
US20060046978A1 (en) 2004-08-31 2006-03-02 Morphochem Ag Novel compounds that inhibit dipeptidyl peptidase (DPP-IV) and neprilysin (NEP) and/or angiotensin converting enzyme (ACE)
US9422234B2 (en) 2007-11-30 2016-08-23 The Johns Hopkins University Prostate specific membrane antigen (PSMA) targeted nanoparticles for therapy of prostate cancer
US10172873B2 (en) * 2014-08-06 2019-01-08 The Johns Hopkins University Methods for treating inflammatory bowel disease using prostate specific membrane antigen (PSMA) inhibitors
LT3177632T (lt) * 2014-08-06 2022-04-25 The Johns Hopkins University Prostatos specifinio membraninio antigeno (psma) inhibitoriaus provaistai

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LT3177632T (lt) 2022-04-25
US11932664B2 (en) 2024-03-19
CY1125201T1 (el) 2024-02-16
US20200399298A1 (en) 2020-12-24
HUE058072T2 (hu) 2022-07-28
CA2961880A1 (en) 2016-02-11
US20170226141A1 (en) 2017-08-10
EP3177632A4 (en) 2018-04-04
ES2908411T3 (es) 2022-04-29
US10544176B2 (en) 2020-01-28
US20230115651A1 (en) 2023-04-13
DK3177632T3 (da) 2022-03-21
US20180244705A1 (en) 2018-08-30
PT3177632T (pt) 2022-03-21
RS63082B1 (sr) 2022-04-29
CA2961880C (en) 2022-09-27
PL3177632T3 (pl) 2022-06-13
US11325931B2 (en) 2022-05-10
WO2016022827A1 (en) 2016-02-11
SI3177632T1 (sl) 2022-05-31
US9988407B2 (en) 2018-06-05
EP3177632B1 (en) 2022-01-12
EP3177632A1 (en) 2017-06-14

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