HRP20160415T1 - Inhibitori beta-sekretaze - Google Patents

Inhibitori beta-sekretaze Download PDF

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Publication number
HRP20160415T1
HRP20160415T1 HRP20160415TT HRP20160415T HRP20160415T1 HR P20160415 T1 HRP20160415 T1 HR P20160415T1 HR P20160415T T HRP20160415T T HR P20160415TT HR P20160415 T HRP20160415 T HR P20160415T HR P20160415 T1 HRP20160415 T1 HR P20160415T1
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Croatia
Prior art keywords
disease
pharmaceutically acceptable
acceptable salt
disorder
image
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HRP20160415TT
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English (en)
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
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Boehringer Ingelheim International Gmbh
Vitae Pharmaceuticals, Inc.
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Application filed by Boehringer Ingelheim International Gmbh, Vitae Pharmaceuticals, Inc. filed Critical Boehringer Ingelheim International Gmbh
Publication of HRP20160415T1 publication Critical patent/HRP20160415T1/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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/46Compounds 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
    • C07C229/50Compounds 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
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
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    • C07C313/00Sulfinic acids; Sulfenic acids; Halides, esters or anhydrides thereof; Amides of sulfinic or sulfenic acids, i.e. compounds having singly-bound oxygen atoms of sulfinic or sulfenic groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C331/00Derivatives of thiocyanic acid or of isothiocyanic acid
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    • C07C49/755Unsaturated 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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Claims (14)

1. Spoj, naznačen time što je prikazan strukturnom formulom koju se bira između: [image] [image] [image] ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi kao medikament.
3. Farmaceutski pripravak, naznačen time što sadrži najmanje jedan spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, u smjesi s farmaceutski prihvatljivim adjuvansom, razrjeđivačem i/ili podlogom.
4. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u liječenju poremećaja ili bolesti povezane s BACE1.
5. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 4, gdje se poremećaj ili bolest povezanu s BACE1 bira iz skupine koju čine neurodegenerativni poremećaj, slabljenje kognitivnih funkcija, kognitivni deficit, demencija, naznačen time što je za bolest karakteristična proizvodnja β-amiloidnih naslaga ili neurofibrilarnih klupka.
6. Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 5, gdje se poremećaj ili bolest bira iz skupine koju čine Alzheimerova bolest, trisomija 21 (Downov Sindrom), nasljedno krvarenje u mozgu uz amiloidozu nizozemskog tipa (HCHWA-D), staračka demencija, cerebralna amiloidna angiopatija, degenerativna demencija, demencije miješano vaskularog i degenerativnog podrijetla, demencija povezana s Parkinsonovom bolešću, demencija povezana s progresivnom supranuklearnom paralizom, demencija povezana s kortikobazalnom degeneracijom, Alzheimerova bolest s difuznim Lewyjevim tijelima, suha staračka degeneracija makule (AMD), te glaukom.
7. Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 6, gdje je poremećaj ili bolest Alzheimerova bolest.
8. Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 6, gdje je poremećaj ili bolest glaukom.
9. Upotreba spoja u skladu s patentnim zahtjevom 1, ili njegove farmaceutski prihvatljive soli, naznačena time što je spoj namijenjen proizvodnji medikamenta za liječenje poremećaja povezanog s BACE1 kod subjekta.
10. Upotreba spoja u skladu s patentnim zahtjevom 9, ili njegova farmaceutski prihvatljiva sol, gdje se bolest ili poremećaj povezan s BACE1 bira iz skupine koju čine neurodegenerativni poremećaj, slabljenje kognitivnih funkcija, kognitivni deficit, demencija, naznačena time što je za bolest karakteristična proizvodnja β-amiloidnih naslaga ili neurofibrilarnih klupka.
11. Upotreba spoja u skladu s patentnim zahtjevom 10, ili njegova farmaceutski prihvatljiva sol, naznačena time što se poremećaj ili bolest bira iz skupine koju čine Alzheimerova bolest, trisomija 21 (Down Sindrom), nasljedno krvarenje u mozgu uz amiloidozu nizozemskog tipa (HCHWA-D), staračka demencija, cerebralna amiloidna angiopatija, degenerativna demencija, demencije miješano vaskularog i degenerativnog podrijetla, demencija povezana s Parkinsonovom bolešću, demencija povezana s progresivnom supranuklearnom paralizom, demencija povezana s kortikobazalnom degeneracijom, Alzheimerova bolest s difuznim Lewyjevim tijelima, suha staračka degeneracija makule (AMD), te glaukom.
12. Upotreba spoja u skladu s patentnim zahtjevom 11, ili njegova farmaceutski prihvatljiva sol, naznačena time što je bolest ili poremećaj Alzheimerova bolest.
13. Upotreba spoja u skladu s patentnim zahtjevom 11, ili njegova farmaceutski prihvatljiva sol, naznačena time što je bolest ili poremećaj glaukom.
14. Spoj, naznačen time što ga se bira iz skupine koju čine: [image] [image] [image] [image] [image] [image] [image] ili njihove soli.
HRP20160415TT 2012-03-05 2016-04-20 Inhibitori beta-sekretaze HRP20160415T1 (hr)

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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HRP20160415T1 true HRP20160415T1 (hr) 2016-06-03

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US (4) US8981112B2 (hr)
EP (1) EP2822930B1 (hr)
JP (1) JP6161643B2 (hr)
KR (1) KR20140138774A (hr)
CN (1) CN104271558B (hr)
AP (1) AP4029A (hr)
AR (1) AR090241A1 (hr)
AU (2) AU2013230523B2 (hr)
BR (1) BR112014021269A2 (hr)
CA (1) CA2864143C (hr)
CL (1) CL2014002334A1 (hr)
CO (1) CO7091177A2 (hr)
CY (1) CY1117543T1 (hr)
DK (1) DK2822930T3 (hr)
EA (1) EA024995B1 (hr)
EC (1) ECSP14020640A (hr)
ES (1) ES2568928T3 (hr)
HK (1) HK1205739A1 (hr)
HR (1) HRP20160415T1 (hr)
HU (1) HUE027289T2 (hr)
IL (1) IL233887A (hr)
IN (1) IN2014DN06710A (hr)
MA (1) MA35945B1 (hr)
ME (1) ME02390B (hr)
MX (1) MX353432B (hr)
MY (1) MY171091A (hr)
NZ (1) NZ629239A (hr)
PE (1) PE20141972A1 (hr)
PH (1) PH12014501963B1 (hr)
PL (1) PL2822930T3 (hr)
RS (1) RS54730B1 (hr)
SG (1) SG11201404600VA (hr)
SI (1) SI2822930T1 (hr)
SM (1) SMT201600114B (hr)
TN (1) TN2014000326A1 (hr)
TW (1) TWI557112B (hr)
UA (1) UA113641C2 (hr)
UY (1) UY34654A (hr)
WO (1) WO2013134085A1 (hr)
ZA (1) ZA201405846B (hr)

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