ME02390B - Inhibitori beta sekretaze - Google Patents

Inhibitori beta sekretaze

Info

Publication number
ME02390B
ME02390B MEP-2016-74A MEP201674A ME02390B ME 02390 B ME02390 B ME 02390B ME P201674 A MEP201674 A ME P201674A ME 02390 B ME02390 B ME 02390B
Authority
ME
Montenegro
Prior art keywords
disease
pharmaceutically acceptable
acceptable salt
dementia
disorder
Prior art date
Application number
MEP-2016-74A
Other languages
German (de)
English (en)
French (fr)
Inventor
Yuri Bukhtiyarov
Salvacion Cacatian
Lawrence Wayne Dillard
Cornelia Dorner-Ciossek
Klaus Fuchs
Lanqi Jia
Deepak S Lala
Angel Morales-Ramos
Georg Rast
Jonathan Reeves
Suresh B Singh
Shankar Venkatraman
Zhenrong Xu
Jing Yuan
Yi Zhao
Yajun Zheng
Original Assignee
Boehringer Ingelheim Int
Vitae Pharmaceuticals Inc
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 Int, Vitae Pharmaceuticals Inc filed Critical Boehringer Ingelheim Int
Publication of ME02390B publication Critical patent/ME02390B/me

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    • 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
    • A61K31/495—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
    • 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
    • A61K31/41—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
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/46—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C229/50—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms being part of the same condensed ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
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    • C07C313/02—Sulfinic acids; Derivatives thereof
    • C07C313/06—Sulfinamides
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    • C07C331/00—Derivatives of thiocyanic acid or of isothiocyanic acid
    • C07C331/02—Thiocyanates
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/587—Unsaturated compounds containing a keto groups being part of a ring
    • C07C49/687—Unsaturated compounds containing a keto groups being part of a ring containing halogen
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    • C07C49/587—Unsaturated compounds containing a keto groups being part of a ring
    • C07C49/703—Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C49/587—Unsaturated compounds containing a keto groups being part of a ring
    • C07C49/753—Unsaturated compounds containing a keto groups being part of a ring containing ether groups, groups, groups, or groups
    • C07C49/755—Unsaturated compounds containing a keto groups being part of a ring containing ether groups, groups, groups, or groups a keto group being part of a condensed ring system with two or three rings, at least one ring being a six-membered aromatic ring
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D405/02—Heterocyclic 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
    • C07D405/06—Heterocyclic 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 only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
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    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/93—Spiro compounds
    • C07C2603/94—Spiro compounds containing "free" spiro atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychology (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (14)

1. Jedinjenje predstavljeno strukturnom formulom izabranom između:
2. Jedinjenje prema zahtevu 1 ili njegova farmaceutski prihvatljiva so za primenu kao lek.
3.Farmaceutska kompozicija koja sadrži najmanje jedno jedinjenje prema zahtevu 1 ili njegovu farmaceutski prihvatljivu so u smeši sa farmaceutski prihvatljivim adjuvansom, rastvaračem i/ili nosačem .
4.Jedinjenje prema zahtevu 1 ili njegova farmaceutski prihvatljiva so za primenu u lečenju poremećaja ili bolesti posredovanih sa BACE1.
5.Jedinjenje ili njegova farmaceutski prihvatljiva so za primenu prema zahtevu 4, pri čemu su poremećaji ili bolesti posredovani sa BACE1 izabrani iz grupe koja se sastoji od neurodegenerativnog poremećaja , opadanja kognitivnih sposobnosti, kognitivnog oštećenja , demencije i bolesti karakterisane proizvodnjom 13-amiloidnih depozita ili neurofibrilarnih spletova.
6.Jedinjenje ili njegova farmaceutski prihvatljiva so za primenu prema zahtevu 5, pri čemu je poremećaj ili bolest izabrana iz grupe koja se sastoji od Alchajmerove bolesti, Trizomije 21 (Daunov sindrom}, nasledne cerebralne hemoragije sa amiloidozom holandskog tipa (HCHWA-0), senilne demencije, cerebralne amiloidne angiopatije, degenerativne demencije, demencija mešovitog vaskularnog i degenerativnog porekla, demencije povezane sa Parkinsonovom bolesti, demencije povezane sa progresivnom supranuklearnom paralizom, demencije povezane sa kortikalnom bazalnom degeneracijom, Alchajmerove bolesti tipa sa difuznim Levijevim telima, suve senilnemakularne degeneracije (AMD), i glaukoma.
7.Jedinjenje ili njegova farmaceutski prihvatljiva so za primenu prema zahtevu 6, pri čemu je poremećaj ili bolest Alchajmerova bolest
8.Jedinjenje ili njegova farmaceutski prihvatljiva so za primenu prema zahtevu 6, pri čemu je poremećaj ili bolest glaukom.
9.Primena jedinjenja prema zahtevu 1 ili njegove farmaceutski prihvatljive soli za proizvodnjuleka za lečenje poremećaja posredovanog sa BACE1 kod subjekta.
10.Pri mena jedin jenja prema zahtevu 9 ili njegove farmaceutski prihvatljive soli, pri čemu su bolest ili poremećaj posredovani sa BACE1 izabrani iz grupe koja se sastoji od neurodegenerativnog poremećaja, opadanja kognitivnih sposobnosti, kognitivnog oštećenja, demencije i bolesti karakterisane proizvodnjom 13-amiloidnih depozita ili neurofibrilarnih spletova.
11.Primena jedin jenja prema zahtevu 1 O ili njegove farmaceutski prihvatljive soli, pri čemu su bolest ili poremećaj izabrani iz grupe koja se sastoji od Alchajmerove bolesti, Trizomije 21(Daunov sindrom), nasledne cerebralne hemoragije sa amiloidozom holandskog tipa (HCHWA-0), senilne demencije, cerebralne amiloidne angiopatije, degenerativne demencije, demencija mešovitog vaskularnog i degenerativnog porekla, demencije povezane sa Parkinsonovom bolesti, demencije povezane sa progresivnom supranuklearnom paralizom, demencije povezane sa kortikalnom bazalnom degeneracijom, Alchajmerove bolesti tipa sa difuznim Levijevim telima, suve senilne makularne degeneracije (AMD), i glaukoma.
12.Primena jedinjenja prema zahtevu 11 ili njegove farmaceutski prihvatljive soli, pri čemu je bolest ili poremećaj Alchajmerova bolest.
13.Primena jedinjenja prema zahtevu 11 ili njegove farmaceutski prihvatljive soli, pri čemu je bolest ili poremećaj glaukom.
14.Jedinjenje izabrano iz grupe koja se sastoji od:ili njegova so.
MEP-2016-74A 2012-03-05 2013-03-04 Inhibitori beta sekretaze ME02390B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261606786P 2012-03-05 2012-03-05
EP13710937.7A EP2822930B1 (en) 2012-03-05 2013-03-04 Inhibitors of beta-secretase
PCT/US2013/028796 WO2013134085A1 (en) 2012-03-05 2013-03-04 Inhibitors of beta-secretase

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ME02390B true ME02390B (me) 2016-09-20

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US (4) US8981112B2 (me)
EP (1) EP2822930B1 (me)
JP (1) JP6161643B2 (me)
KR (1) KR20140138774A (me)
CN (1) CN104271558B (me)
AP (1) AP4029A (me)
AR (1) AR090241A1 (me)
AU (2) AU2013230523B2 (me)
BR (1) BR112014021269A2 (me)
CA (1) CA2864143C (me)
CL (1) CL2014002334A1 (me)
CO (1) CO7091177A2 (me)
CY (1) CY1117543T1 (me)
DK (1) DK2822930T3 (me)
EA (1) EA024995B1 (me)
EC (1) ECSP14020640A (me)
ES (1) ES2568928T3 (me)
GE (1) GEP20176799B (me)
HR (1) HRP20160415T1 (me)
HU (1) HUE027289T2 (me)
IL (1) IL233887A (me)
IN (1) IN2014DN06710A (me)
MA (1) MA35945B1 (me)
ME (1) ME02390B (me)
MX (1) MX353432B (me)
MY (1) MY171091A (me)
NZ (1) NZ629239A (me)
PE (1) PE20141972A1 (me)
PH (1) PH12014501963B1 (me)
PL (1) PL2822930T3 (me)
RS (1) RS54730B1 (me)
SG (1) SG11201404600VA (me)
SI (1) SI2822930T1 (me)
SM (1) SMT201600114B (me)
TN (1) TN2014000326A1 (me)
TW (1) TWI557112B (me)
UA (1) UA113641C2 (me)
UY (1) UY34654A (me)
WO (1) WO2013134085A1 (me)
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