HRP20171783T1 - Derivati imidazopirazinona - Google Patents

Derivati imidazopirazinona Download PDF

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Publication number
HRP20171783T1
HRP20171783T1 HRP20171783TT HRP20171783T HRP20171783T1 HR P20171783 T1 HRP20171783 T1 HR P20171783T1 HR P20171783T T HRP20171783T T HR P20171783TT HR P20171783 T HRP20171783 T HR P20171783T HR P20171783 T1 HRP20171783 T1 HR P20171783T1
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HR
Croatia
Prior art keywords
pharmaceutically acceptable
stereoisomers
atoms
tautomers
formula
Prior art date
Application number
HRP20171783TT
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English (en)
Inventor
Hans-Peter Buchstaller
Dieter Dorsch
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Merck Patent 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.)
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Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of HRP20171783T1 publication Critical patent/HRP20171783T1/hr

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    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/527Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/06Peri-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Lubricants (AREA)
  • Developing Agents For Electrophotography (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Claims (11)

1. Spojevi s formulom I [image] naznačeni time da R1 označava H ili metil, R2 označava A ili Het, A označava nerazgranati ili razgranati alkil s 1 - 8 C-atoma, pri čemu jedna ili dvije ne-susjedne CH- i/ili CH2-skupine mogu biti zamijenjene s N- ili O-atomima i/ili pri čemu 1-7 H-atoma mogu biti zamijenjeni s F ili Cl, Het označava pirimidil, piridil, piridazinil, pirazinil, piperidinil, pirolidinil, pirazolil, tiazolil, imidazolil, furanil, tiofenil, pirolil, oksazolil, triazolil, oksadiazolil ili tiadiazolil, svaki od kojih je nesupstituiran ili mono- ili disupstituiran s Hal, A, CN, OH i/ili OA, Hal označava F, Cl, Br ili I, pod uvjetom da, ako R1 je H, tada R2 nije 4-OMe, i njihove farmaceutski prihvatljive soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
2. Spojevi prema zahtjevu 1, naznačeni time da A označava nerazgranati ili razgranati alkil s 1 - 8 C-atoma, pri čemu jedna ili dvije ne-susjedne CH2-skupine mogu biti zamijenjene s O-atomima i/ili pri čemu 1-3 H-atoma mogu biti zamijenjeni s F, te njihovi farmaceutski prihvatljivi solvati, soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
3. Spojevi prema zahtjevu 1 ili 2, naznačeni time da Het označava pirimidil, piridil, piridazinil, pirazinil, piperidinil, pirolidinil, pirazolil, tiazolil, imidazolil, furanil, tiofenil, pirolil, oksazolil, triazolil, oksadiazolil ili tiadiazolil, svaki od kojih je nesupstituiran ili monosupstituiran s A, i njihovi farmaceutski prihvatljivi solvati, soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
4. Spojevi prema zahtjevu 1, naznačeni time da R1 označava H ili metil, R2 označava A ili Het, A označava nerazgranati ili razgranati alkil s 1 - 8 C-atoma, pri čemu jedna ili dvije ne-susjedne CH2-skupine mogu biti zamijenjene s O-atomima i/ili pri čemu 1-3 H-atomi mogu biti zamijenjeni s F, Het označava pirimidil, piridil, piridazinil, pirazinil, piperidinil, pirolidinil, pirazolil, tiazolil, imidazolil, furanil, tiofenil, pirolil, oksazolil, triazolil, oksadiazolil ili tiadiazolil, svaki od kojih je nesupstituiran ili monosupstituiran s A, i njihove farmaceutski prihvatljive soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
5. Spojevi prema zahtjevu 1, naznačeni time da su odabrani iz skupine koja sadrži [image] i njihovi farmaceutski prihvatljivi solvati, soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
6. Postupak za pripremanje spojeva s formulom I prema zahtjevima 1-5 i njihove farmaceutski prihvatljive soli, solvati, tautomeri i stereoizomeri, naznačen time da spoj s formulom II [image] u kojoj R1 i R2 imaju značenja navedena u zahtjevu 1, je debenziliran, i/ili baza ili kiselina s formulom I se pretvara u jednu njihovih soli.
7. Lijekovi naznačeni time da sadrže barem jedan spoj s formulom I prema zahtjevu 1 i/ili njihove farmaceutski prihvatljive soli, solvati, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima, i proizvoljno farmaceutski prihvatljiv nosač, pomoćno sredstvo ili prijenosnik.
8. Spojevi s formulom I prema zahtjevu 1 i njihove farmaceutski prihvatljive soli, solvati, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima, naznačeni time da su za uporabu za liječenje i/ili sprječavanje raka, multiple skleroze, kardiovaskularnih bolesti, ozljeda središnjeg živčanog sustava i različitih oblika upala.
9. Spojevi prema zahtjevu 8 naznačeni time da su za uporabu za liječenje i/ili sprječavanje bolesti odabranih iz skupine koju čine rak glave, vrata, oka, usta, grla, jednjaka, bronha, grkljana, ždrijela, prsa, kosti, pluća, debelog crijeva, rektuma, želuca, prostate, mokraćnog mjehura, uterine, grlića maternice, dojke, jajnika, testisa ili drugih reproduktivnih organa, kože, štitnjače, krvi, limfnih čvorova, bubrega, jetre, gušterače, mozga, središnjeg živčanog sustava, solidnih tumora i tumora krvi.
10. Lijekovi naznačeni time da sadrže barem jedan spoj s formulom I prema zahtjevu 1 i/ili njihove farmaceutski prihvatljive soli, solvati i stereoizomeri, uključujući njihove smjese u svim omjerima, te barem jedan dodatni aktivni sastojak lijeka.
11. Komplet (kit) naznačen time da sadrži odvojena pakiranja (a) učinkovite količine spoja s formulom I prema zahtjevu 1 i/ili njegove farmaceutski prihvatljive soli, solvati i stereoizomeri, uključujući njihove smjese u svim omjerima, i (b) učinkovite količine dodatnog aktivnog sastojka lijeka.
HRP20171783TT 2013-12-23 2017-11-16 Derivati imidazopirazinona HRP20171783T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13006052 2013-12-23
PCT/EP2014/003226 WO2015096884A1 (en) 2013-12-23 2014-12-03 Imidazopyrazinone derivatives
EP14808506.1A EP3087076B1 (en) 2013-12-23 2014-12-03 Imidazopyrazinone derivatives

Publications (1)

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HRP20171783T1 true HRP20171783T1 (hr) 2017-12-29

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HRP20171783TT HRP20171783T1 (hr) 2013-12-23 2017-11-16 Derivati imidazopirazinona

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US (1) US9718826B2 (hr)
EP (1) EP3087076B1 (hr)
JP (1) JP6446461B2 (hr)
KR (1) KR20160101188A (hr)
CN (1) CN105829317B (hr)
AU (1) AU2014372896B2 (hr)
CA (1) CA2934663A1 (hr)
DK (1) DK3087076T3 (hr)
ES (1) ES2654403T3 (hr)
HR (1) HRP20171783T1 (hr)
HU (1) HUE037606T2 (hr)
IL (1) IL246406A0 (hr)
LT (1) LT3087076T (hr)
MX (1) MX364859B (hr)
NO (1) NO3087076T3 (hr)
PL (1) PL3087076T3 (hr)
PT (1) PT3087076T (hr)
RS (1) RS56746B1 (hr)
RU (1) RU2672885C2 (hr)
SG (1) SG11201605189YA (hr)
SI (1) SI3087076T1 (hr)
TW (1) TWI637956B (hr)
WO (1) WO2015096884A1 (hr)

Families Citing this family (7)

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Publication number Priority date Publication date Assignee Title
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
TW201822637A (zh) 2016-11-07 2018-07-01 德商拜耳廠股份有限公司 用於控制動物害蟲的經取代磺醯胺類
CN108403697A (zh) * 2018-05-02 2018-08-17 吉林大学 吡嗪酮类小分子抑制剂在制备抗肿瘤药物中的应用
WO2020049017A1 (en) * 2018-09-07 2020-03-12 Merck Patent Gmbh 5-morpholin-4-yl-pyrazolo[4,3-b]pyridine derivatives
JP7433403B1 (ja) 2022-12-06 2024-02-19 本田技研工業株式会社 内燃機関及び鞍乗型車両

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JP2005089352A (ja) * 2003-09-16 2005-04-07 Kissei Pharmaceut Co Ltd 新規なイミダゾ[1,5−a]ピラジン誘導体、それを含有する医薬組成物およびそれらの用途
CN101468988A (zh) * 2007-12-26 2009-07-01 上海恒瑞医药有限公司 哌嗪类衍生物,其制备方法及其在医药上的应用
WO2011089400A1 (en) * 2010-01-22 2011-07-28 Centro Nacional De Investigaciones Oncológicas (Cnio) Inhibitors of pi3 kinase
NZ630489A (en) 2012-03-28 2016-04-29 Merck Patent Gmbh Bicyclic pyrazinone derivatives
RS55062B1 (sr) * 2012-05-04 2016-12-30 Merck Patent Gmbh Pirolotriazinon derivati

Also Published As

Publication number Publication date
EP3087076A1 (en) 2016-11-02
KR20160101188A (ko) 2016-08-24
TWI637956B (zh) 2018-10-11
CA2934663A1 (en) 2015-07-02
MX2016008042A (es) 2016-09-16
SG11201605189YA (en) 2016-07-28
LT3087076T (lt) 2017-12-27
ES2654403T3 (es) 2018-02-13
NO3087076T3 (hr) 2018-02-24
HUE037606T2 (hu) 2018-09-28
RU2016130148A (ru) 2018-01-30
AU2014372896A1 (en) 2016-08-04
US9718826B2 (en) 2017-08-01
IL246406A0 (en) 2016-08-31
JP6446461B2 (ja) 2018-12-26
MX364859B (es) 2019-05-09
EP3087076B1 (en) 2017-09-27
US20170002010A1 (en) 2017-01-05
RU2672885C2 (ru) 2018-11-20
CN105829317B (zh) 2019-03-29
PL3087076T3 (pl) 2018-01-31
WO2015096884A1 (en) 2015-07-02
CN105829317A (zh) 2016-08-03
SI3087076T1 (en) 2018-01-31
RU2016130148A3 (hr) 2018-07-25
DK3087076T3 (da) 2017-11-13
PT3087076T (pt) 2018-01-03
TW201605862A (zh) 2016-02-16
JP2017500353A (ja) 2017-01-05
AU2014372896B2 (en) 2018-08-16
RS56746B1 (sr) 2018-03-30

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