HRP20230249T1 - Derivati 4-pirazin-2-ilmetil-morfolina i njihova uporaba kao lijeka - Google Patents

Derivati 4-pirazin-2-ilmetil-morfolina i njihova uporaba kao lijeka Download PDF

Info

Publication number
HRP20230249T1
HRP20230249T1 HRP20230249TT HRP20230249T HRP20230249T1 HR P20230249 T1 HRP20230249 T1 HR P20230249T1 HR P20230249T T HRP20230249T T HR P20230249TT HR P20230249 T HRP20230249 T HR P20230249T HR P20230249 T1 HRP20230249 T1 HR P20230249T1
Authority
HR
Croatia
Prior art keywords
image
following structure
compound
enantiomer
treatment
Prior art date
Application number
HRP20230249TT
Other languages
English (en)
Inventor
Riccardo Giovannini
Angelo Ceci
Cornelia Dorner-Ciossek
Roland Pfau
Dieter Wiedenmayer
Original Assignee
Boehringer Ingelheim International Gmbh
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 Boehringer Ingelheim International Gmbh filed Critical Boehringer Ingelheim International Gmbh
Publication of HRP20230249T1 publication Critical patent/HRP20230249T1/hr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Claims (22)

1. Spoj, naznačen time, da je predstavljen formulom A [image] u kojoj R1 predstavlja metil, etil, propil, izo-propil, ciklopropil, H3CCH2CH2CH2, ciklobutil; R2 predstavlja fenil koji je opcionalno supstituiran s 1, 2 ili 3 supstitenta odabrana iz skupine koju čine fluor, klor, metil, etil, ciklopropil.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da R1 predstavlja metil, etil; R2 predstavlja [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] .
3. (S)-enantiomer prema bilo kojem od patentnih zahtjeva 1 do 2, to jest spoj, naznačen time, da se bira iz skupine koju čine: [image] [image] [image] [image]
4. (S)-enantiomer prema bilo kojem od patentnih zahtjeva 1 to 3, naznačen time, da ima sljedeću strukturu: [image]
5. (S)-enantiomer prema bilo kojem od patentnih zahtjeva 1 to 3, naznačen time, da ima sljedeću strukturu: [image]
6. (S)-enantiomer prema bilo kojem od patentnih zahtjeva 1 to 3, naznačen time, da ima sljedeću strukturu: [image]
7. (S)-enantiomer prema bilo kojem od patentnih zahtjeva 1 to 3, naznačen time, da ima sljedeću strukturu: [image]
8. (S)-enantiomer prema bilo kojem od patentnih zahtjeva 1 to 3, naznačen time, da ima sljedeću strukturu: [image]
9. (S)-enantiomer prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da ima sljedeću strukturu: [image]
10. (S)-enantiomer prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da ima sljedeću strukturu: [image]
11. (S)-enantiomer prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da ima sljedeću strukturu: [image]
12. (S)-enantiomer prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da ima sljedeću strukturu: [image]
13. (S)-enantiomer prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da ima sljedeću strukturu: [image]
14. Farmaceutski prihvatljiva sol, naznačena time, da je od spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 13.
15. Spoj prema bilo kojem od patentnih zahtjeva 1 do 14, naznačen time, da je za uporabu kao lijek.
16. Spoj prema bilo kojem od patentnih zahtjeva 1 do 14, naznačen time, da je za uporabu u liječenju i/ili prevenciji bipolarnog poremećaja I u obliku depresije, hipomanije, manije, i u miješanom obliku; bipolarnog poremećaja II; depresivnih poremećaja; velikog depresivnog poremećaja sa ili bez pratećeg anksioznog distresa, miješanih značajki, melankolijskih značajki, netipičnih značajki, psihotičkih značajki koje se podudaraju s raspoloženjem, psihotičkih značajki koja se ne podudaraju s raspoloženjem, katatonije.
17. Spoj prema bilo kojem od patentnih zahtjeva 1 do 14, naznačen time, da je za uporabu u liječenju i/ili prevenciji jednokratne depresivne epizode ili periodičnog velikog depresivnog poremećaja, manjeg depresivnog poremećaja, depresivnog poremećaja s postporođajnim napadom, depresivnih poremećaja s psihotičnim simptomima.
18. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 15 do 17, naznačen time, da se spoj primjenjuje kao dodatak uz liječenje s nekim drugim antidepresivnim lijekom.
19. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 15 do 17, naznačen time, da se spoj primjenjuje kao dodatak u terapiji poremećaja ponašanja.
20. Spoj prema bilo kojem od patentnih zahtjeva 1 do 14, naznačen time, da je za uporabu u liječenju akutne i kronične boli koja se odnosi na neuropatiju, fiziološke procese i fizičke poremećaje, bolest mišićno-koštanog sustava i vezivnog tkiva, poremećaje kod živaca, korjena živaca i pleksusa.
21. Spoj prema bilo kojem od patentnih zahtjeva 1 do 14, naznačen time, da je za uporabu u liječenju dijabetičke neuropatije, polineuropatije, bolova u donjem dijelu leđa, bolova u zglobovima, reumatizma, mijalgije, sindroma fantomskog ekstremiteta s bolovima, sindroma karpalnog kanala.
22. Farmaceutski pripravak, naznačen time, da sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 14, u mješavini s farmaceutski prihvatljivim pomoćnim sredstvom, razrjeđivačem i/ili nosačem.
HRP20230249TT 2018-10-17 2019-10-16 Derivati 4-pirazin-2-ilmetil-morfolina i njihova uporaba kao lijeka HRP20230249T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18200943 2018-10-17
PCT/EP2019/078027 WO2020079039A1 (en) 2018-10-17 2019-10-16 4-pyrazin-2-ylmethyl-morpholine derivatives and the use thereof as medicament
EP19786343.4A EP3867244B1 (en) 2018-10-17 2019-10-16 4-pyrazin-2-ylmethyl-morpholine derivatives and the use thereof as medicament

Publications (1)

Publication Number Publication Date
HRP20230249T1 true HRP20230249T1 (hr) 2023-04-14

Family

ID=63878518

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20230249TT HRP20230249T1 (hr) 2018-10-17 2019-10-16 Derivati 4-pirazin-2-ilmetil-morfolina i njihova uporaba kao lijeka

Country Status (35)

Country Link
US (2) US11166958B2 (hr)
EP (1) EP3867244B1 (hr)
JP (1) JP7093468B2 (hr)
KR (1) KR20210079325A (hr)
CN (1) CN112888685B (hr)
AR (1) AR116711A1 (hr)
AU (1) AU2019362330B2 (hr)
BR (1) BR112021004993A2 (hr)
CA (1) CA3113308A1 (hr)
CL (1) CL2021000858A1 (hr)
CO (1) CO2021004612A2 (hr)
CR (1) CR20210184A (hr)
DK (1) DK3867244T3 (hr)
DO (1) DOP2021000069A (hr)
EA (1) EA202191014A1 (hr)
EC (1) ECSP21027009A (hr)
ES (1) ES2940184T3 (hr)
FI (1) FI3867244T3 (hr)
HR (1) HRP20230249T1 (hr)
HU (1) HUE061891T2 (hr)
IL (1) IL282142B2 (hr)
JO (1) JOP20210075A1 (hr)
LT (1) LT3867244T (hr)
MA (1) MA53898B1 (hr)
MX (1) MX2021004418A (hr)
PE (1) PE20211278A1 (hr)
PH (1) PH12021550834A1 (hr)
PL (1) PL3867244T3 (hr)
PT (1) PT3867244T (hr)
RS (1) RS63988B1 (hr)
SA (1) SA521421756B1 (hr)
SG (1) SG11202103806VA (hr)
SI (1) SI3867244T1 (hr)
TW (1) TWI828779B (hr)
WO (1) WO2020079039A1 (hr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3980401A1 (en) * 2019-06-04 2022-04-13 Boehringer Ingelheim International GmbH Purine derivatives, as nr2b negative modulators and the use thereof as medicament, in particular for treating depressive disorders

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6495561B2 (en) 1999-10-29 2002-12-17 Merck & Co., Inc. 2-cyclohexyl imidazopyridine NMDA/NR2B antagonists
AU2002338334B8 (en) 2001-04-03 2008-09-18 Merck & Co., Inc. N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B antagonists
MXPA04000737A (es) * 2001-07-24 2004-07-08 Richter Gedeon Vegyeszet Derivados de piperidina como antagonistas receptores de nmda.
US7855201B2 (en) * 2005-12-06 2010-12-21 Merck Sharp & Dohme. Corp. Morpholine carboxamide prokineticin receptor antagonists
US20110319416A1 (en) * 2009-01-28 2011-12-29 Emory University Subunit Selective NMDA Receptor Antagonists For The Treatment Of Neurological Conditions
WO2012128582A2 (en) 2011-03-23 2012-09-27 Hyundai Pharm Co., Ltd. A COMPOUND FOR INHIBITING HUMAN 11-β-HYDROXY STEROID DEHYDROGENASE TYPE 1, AND A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
KR101684816B1 (ko) 2012-10-18 2016-12-20 에프. 호프만-라 로슈 아게 mGluR5 수용체 활성의 조절제로서 에틴일 유도체
US9676757B2 (en) 2014-02-27 2017-06-13 Merck Patent Gmbh Heterocyclic compounds as NaV channel inhibitors and uses thereof
WO2016029146A1 (en) 2014-08-22 2016-02-25 University Of Washington Specific inhibitors of methionyl-trna synthetase
WO2017066368A1 (en) * 2015-10-14 2017-04-20 Bristol-Myers Squibb Company Selective nr2b antagonists

Also Published As

Publication number Publication date
AR116711A1 (es) 2021-06-02
TW202031262A (zh) 2020-09-01
CO2021004612A2 (es) 2021-04-30
CN112888685B (zh) 2023-09-22
MA53898A (fr) 2022-01-26
US11166958B2 (en) 2021-11-09
LT3867244T (lt) 2023-03-10
HUE061891T2 (hu) 2023-09-28
IL282142A (en) 2021-05-31
SA521421756B1 (ar) 2023-02-12
US20210393644A1 (en) 2021-12-23
KR20210079325A (ko) 2021-06-29
ECSP21027009A (es) 2021-05-31
AU2019362330A1 (en) 2021-04-08
EA202191014A1 (ru) 2021-11-09
MX2021004418A (es) 2021-07-06
SG11202103806VA (en) 2021-05-28
PL3867244T3 (pl) 2023-05-22
CN112888685A (zh) 2021-06-01
EP3867244B1 (en) 2023-01-18
IL282142B1 (en) 2023-12-01
WO2020079039A1 (en) 2020-04-23
DK3867244T3 (da) 2023-05-01
SI3867244T1 (sl) 2023-04-28
JOP20210075A1 (ar) 2023-01-30
PE20211278A1 (es) 2021-07-19
JP2022505080A (ja) 2022-01-14
US20200121691A1 (en) 2020-04-23
ES2940184T3 (es) 2023-05-04
BR112021004993A2 (pt) 2021-06-08
CA3113308A1 (en) 2020-04-23
CR20210184A (es) 2021-05-26
PT3867244T (pt) 2023-02-22
CL2021000858A1 (es) 2021-10-01
DOP2021000069A (es) 2021-05-31
FI3867244T3 (fi) 2023-03-20
RS63988B1 (sr) 2023-03-31
JP7093468B2 (ja) 2022-06-29
IL282142B2 (en) 2024-04-01
TWI828779B (zh) 2024-01-11
EP3867244A1 (en) 2021-08-25
PH12021550834A1 (en) 2021-10-04
AU2019362330B2 (en) 2024-03-28
MA53898B1 (fr) 2023-03-31

Similar Documents

Publication Publication Date Title
RU2018110647A (ru) Арильные, гетероарильные и гетероциклические соединения для лечения заболеваний
Tafur et al. Anestesia total intravenosa: de la farmacéutica a la farmacocinética
HRP20211906T1 (hr) Dalargin za upotrebu u liječenju akutne respiratorne virusne infekcije
JP2018188483A5 (hr)
RS52256B (en) THERAPEUTIC USES OF COMPOUNDS WITH COMBINED SERT, 5-HT3 AND 5-HT1A ACTIVITIES
JP2016528301A5 (hr)
EA201690069A1 (ru) Применение высоких доз придопидина для лечения болезни хантингтона
RU2016105581A (ru) Способ лечения острого, хронического и подострого кашля и непреодолимого желания откашляться
HRP20202051T1 (hr) Aril supstituirani pirimidini za uporabu kod infekcije virusom influence
HRP20191869T1 (hr) Fluoroindol derivati kao pozitivni alosterički modulatori muskarinskog m1 receptora
HRP20240173T1 (hr) Fluorofenil beta-hidroksietilamini i njihova upotreba u liječenju hiperglikemije
JP2019529541A5 (hr)
JP2017533972A5 (hr)
BRPI0411079A (pt) composições farmacêuticas compreendendo atorvastatina, fabricadas sem granulação
HRP20230249T1 (hr) Derivati 4-pirazin-2-ilmetil-morfolina i njihova uporaba kao lijeka
JP2021506971A5 (hr)
HRP20211726T1 (hr) Derivati imidazopiridina i njihova uporaba kao lijeka
US20160106774A1 (en) Liquid pharmaceutical composition containing piroxicam and hyaluronic acid for the treatment of osteoarthritis
RU2016105310A (ru) Пиперазин-замещенные мостиковые производные спиро[2.4]гептана в качестве агонистов alx рецептора
BR112019018185A2 (pt) composição para tratar uma doença de articulação humana, e, kit.
EA201591653A1 (ru) Композиции для лечения глазных расстройств с применением дипиридамола
BR112014004339A2 (pt) suspensão oral
EA201990419A1 (ru) Слаборастворимый комплекс или его сольват, фармацевтическая композиция и их применение
JP2019529569A5 (hr)
EA202192894A1 (ru) Новые ингибиторы глутаминилциклаз и их применение для лечения различных заболеваний