ME02728B - Jedinjenja i njihova upotreba kao bace inhibitori - Google Patents

Jedinjenja i njihova upotreba kao bace inhibitori

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Publication number
ME02728B
ME02728B MEP-2017-115A MEP11517A ME02728B ME 02728 B ME02728 B ME 02728B ME P11517 A MEP11517 A ME P11517A ME 02728 B ME02728 B ME 02728B
Authority
ME
Montenegro
Prior art keywords
pharmaceutically acceptable
compound
disease
acceptable salt
alzheimer
Prior art date
Application number
MEP-2017-115A
Other languages
German (de)
English (en)
French (fr)
Inventor
Gabor Csjernyik
Sofia Karlström
Annika Kers
Karin Kolmodin
Martin Nylöf
Liselotte Öhberg
Laszlo Rakos
Lars Sandberg
Fernando Sehgelmeble
Peter Söderman
Britt-Marie Swahn
Berg Stefan Von
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46314249&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME02728(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of ME02728B publication Critical patent/ME02728B/me

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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • C07D401/10—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 carbon chain containing aromatic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • 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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
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  • Neurosurgery (AREA)
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  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Furan Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pyridine Compounds (AREA)

Claims (6)

1.Jedinjenje koje je (1r,1'R,4R)-4-metoksi-5"-metil-6'-[5-(prop-1-in-1-il)piridin-3-il]-3'H-dispiro[cikloheksan-1,2'-inden-1',2"-imidazol]-4"-amin: ili njegova farmaceutski prihvatljiva so.
2.Farmaceutski sastav koji se sastoji od aktivnih sastojaka terapeutski efektivnih količina jedinjenja prema patentnom zahtevu 1, ili njegova farmaceutski prihvatljiva so, u vezi sa bar jednim farmaceutski prihvatljivim ekscipijentom, nosiocem ili razblaživačem.
3.Jedinjenje prema patentnom zahtevu 1, ili njegova farmaceutski prihvatljiva so za upotrebu kao lek.
4.Jedinjenje ili njegova farmaceutski prihvatljiva so prema patentnom zahtevu 1 za upotrebu kao metod lečenja ili sprečavanja Aβ-povezanih patologija, gde je navedena Aβ-povezana patologija Daunov sindrom, β-amiloidna angiopatija, cerebralna amiloidna angiopatija, nasledno cerebralno krvarenje, poremećaji povezani sa kognitivnim oštećenjem, MCI ("blago kognitivno oštećenje"), Alchajmerova bolest, gubitak pamćenja, simptomi nedostatka pažnje povezani sa Alchajmerovom bolešću, neurodegeneracija povezana sa Alchajmerovom bolešću, demencija mešovitog vaskularnog porekla, demencija degenerativnog porekla, presenilna demencija, senilna demencija, demencije povezane sa Parkinsonovom bolešću, progresivna supranuklearna paraliza ili kortikalna bazalna degeneracija.
5.Jedinjenje ili njegova farmaceutski prihvatljiva so za upotrebu prema patentnom zahtevu 4, gde je navedena β-povezana patologija Alchajmerova bolest.
6.Jedinjenje ili njegova farmaceutski prihvatljiva za upotrebu prema patentnim zahtevima 4 ili 5, gde je navedena upotreba u kombinaciji sa bar jednim kongitivnim poboljšavajućim agensom, agensom za poboljšavanje memorije ili inhibitorom holinesteraze.
MEP-2017-115A 2010-12-22 2011-12-21 Jedinjenja i njihova upotreba kao bace inhibitori ME02728B (me)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201061425852P 2010-12-22 2010-12-22
US201161529620P 2011-08-31 2011-08-31
PCT/SE2011/051555 WO2012087237A1 (en) 2010-12-22 2011-12-21 Compounds and their use as bace inhibitors
EP11850232.7A EP2655378B1 (en) 2010-12-22 2011-12-21 Compounds and their use as bace inhibitors

Publications (1)

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ME02728B true ME02728B (me) 2017-10-20

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US (6) US8415483B2 (me)
EP (2) EP3176172B1 (me)
JP (3) JP6180325B2 (me)
KR (1) KR101916975B1 (me)
CN (2) CN103380133B (me)
AR (1) AR084553A1 (me)
AU (3) AU2011345389B2 (me)
BR (1) BR112013016030B1 (me)
CA (1) CA2822378C (me)
CL (1) CL2013001849A1 (me)
CO (1) CO6781485A2 (me)
CR (1) CR20130308A (me)
CY (1) CY1119211T1 (me)
DK (1) DK2655378T3 (me)
DO (3) DOP2013000147A (me)
EA (2) EA032687B1 (me)
EC (1) ECSP13012708A (me)
ES (2) ES2780928T3 (me)
GT (1) GT201300165A (me)
HR (1) HRP20170723T1 (me)
HU (1) HUE033274T2 (me)
LT (1) LT2655378T (me)
ME (1) ME02728B (me)
MX (1) MX342477B (me)
MY (1) MY178156A (me)
NI (1) NI201300055A (me)
NZ (2) NZ612041A (me)
PE (2) PE20141191A1 (me)
PH (2) PH12017500851A1 (me)
PL (1) PL2655378T3 (me)
PT (1) PT2655378T (me)
RS (1) RS55961B1 (me)
SA (2) SA111330107B1 (me)
SG (2) SG10201602241SA (me)
SI (1) SI2655378T1 (me)
SM (1) SMT201700243T1 (me)
TW (2) TWI633092B (me)
UY (1) UY33829A (me)
WO (1) WO2012087237A1 (me)
ZA (1) ZA201305495B (me)

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US8415483B2 (en) * 2010-12-22 2013-04-09 Astrazeneca Ab Compounds and their use as BACE inhibitors
WO2013054108A1 (en) 2011-10-10 2013-04-18 Astrazeneca Ab Mono-fluoro beta-secretase inhibitors
US8779355B2 (en) 2011-12-28 2014-07-15 Quest Diagnostics Investments, Inc. Methods for detecting lacosamide by mass spectrometry
PE20142376A1 (es) 2012-01-26 2015-01-17 Hoffmann La Roche Fluormetil-5,6-dihidro-4h-[1,3]oxazinas
TWI557112B (zh) 2012-03-05 2016-11-11 百靈佳殷格翰國際股份有限公司 β－分泌酶抑制劑
AR091203A1 (es) 2012-05-30 2015-01-21 Astellas Pharma Inc Compuestos de cromano
US9000183B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors
US9000185B2 (en) * 2012-06-20 2015-04-07 Astrazeneca Ab Cycloalkyl ether compounds and their use as BACE inhibitors
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