RS20060146A - Malonamide derivatives blocking the activity of gama-secretase - Google Patents

Malonamide derivatives blocking the activity of gama-secretase

Info

Publication number
RS20060146A
RS20060146A YUP-2006/0146A YUP20060146A RS20060146A RS 20060146 A RS20060146 A RS 20060146A YU P20060146 A YUP20060146 A YU P20060146A RS 20060146 A RS20060146 A RS 20060146A
Authority
RS
Serbia
Prior art keywords
lower alkyl
halogen
hydrogen
cycloalkyl
phenyl
Prior art date
Application number
YUP-2006/0146A
Other languages
English (en)
Inventor
Alexander Flohr
Guido Galley
Roland Jakob-Roetne
Eric Argiros Kitas
Jens-Uwe Peters
Wolfgang Wostl
Original Assignee
F.Hoffmann-La Roche Ag.,
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 F.Hoffmann-La Roche Ag., filed Critical F.Hoffmann-La Roche Ag.,
Publication of RS20060146A publication Critical patent/RS20060146A/sr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16Benzazepines; Hydrogenated benzazepines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/557Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/558Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/18Dibenzazepines; Hydrogenated dibenzazepines
    • C07D223/20Dibenz [b, e] azepines; Hydrogenated dibenz [b, e] azepines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D273/00Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D313/00Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
    • C07D313/02Seven-membered rings
    • C07D313/06Seven-membered rings condensed with carbocyclic rings or ring systems
    • C07D313/10Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
    • C07D313/14[b,f]-condensed

Landscapes

  • 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)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Ovaj pronalazak se odnosi na derivate malonamida formule (I), u kojoj R1 označava jednu od sledećih grupa (formula a), b), c), d)); R2 označava niži alkil, niži alkinil, -(CH2)n-O-niži alkil, -(CH2)n-S-niži alkil, -(CH2)n-CN, -(CR'R")n-CF3, -(CR'R")n-CHF2, -(CR'R")n-CH2F-(CH2)n-C(O)O-niži alkil, -(CH2)n-halogen, ili označava -(CH2)n-cikloalkil, koji je opciono supstituisan sa jednim ili više supstituenata, koji su odabrani iz grupe koja se sastoji od fenila, halogena ili CF3; R',R" svaki nezavisno od n i jedan od drugog označava vodonik, niži alkil, niži alkoksi, halogen ili hidroksi; R3,R4 svaki nezavisno jedan od drugog označava vodonik, niži alkil, niži alkoksi, fenil ili halogen; R5 označava vodonik, niži alkil, - (CH2) n-CF3 ili - (CH2) n-cikloalkil; R6 označava vodonik ili halogen; R7 označava vodonik ili niži alkil; R8 označava vodonik, niži alkil, niži alkinil, -(CH2)n- CF3, -(CH2)n-cikloalkil ili -(CH2)n-fenil, koji je opciono supstituisan halogenom; R9 označava vodonik, niži alkil, -C(O)H, -C(O)-niži alkil, -C(O)-CF3, -C(O)-CH2F, -C(O)CHF2, -C(O)-cikloalkil, -C(O)-(CH2)n-O-niži alkil, -C(O)O(CH2)n-cikloalkil, -C(O)-fenil, koji je opciono supstituisan sa jednim ili više supstituenata koji su odabrani iz grupe koja se sastoji od halogena ili -C(O)O nižeg alkila, ili označava -S(O)2-niži alkil, -S(O)2-CF3, -(CH2)n-cikloalkil ili označava -(CH2)n-fenil, koji je opciono supstituisan halogenom; n iznosi 0, 1, 2, 3 ili 4; i na njihove farmaceutski prihvatljive kiselinske adicione soli, optički čiste enantiomere, racemate ili dijastereomerne smeše. Ova jedinjenja se mogu primeniti za lečenje Alchajmerove bolesti.
YUP-2006/0146A 2003-09-09 2004-08-31 Malonamide derivatives blocking the activity of gama-secretase RS20060146A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP03019683 2003-09-09
PCT/EP2004/009700 WO2005023772A1 (en) 2003-09-09 2004-08-31 Malonamide derivatives blocking the activity of gama-secretase

Publications (1)

Publication Number Publication Date
RS20060146A true RS20060146A (en) 2008-06-05

Family

ID=34224068

Family Applications (1)

Application Number Title Priority Date Filing Date
YUP-2006/0146A RS20060146A (en) 2003-09-09 2004-08-31 Malonamide derivatives blocking the activity of gama-secretase

Country Status (35)

Country Link
US (1) US7160875B2 (sr)
EP (1) EP1711470B1 (sr)
JP (2) JP4571639B2 (sr)
KR (3) KR20070087233A (sr)
CN (1) CN100593539C (sr)
AR (1) AR045609A1 (sr)
AT (1) ATE428698T1 (sr)
AU (1) AU2004270361B2 (sr)
BR (1) BRPI0413533A (sr)
CA (1) CA2537440C (sr)
CO (1) CO5660268A2 (sr)
CR (1) CR8264A (sr)
CY (1) CY1109225T1 (sr)
DE (1) DE602004020680D1 (sr)
DK (1) DK1711470T3 (sr)
EA (1) EA009940B1 (sr)
EC (1) ECSP066414A (sr)
ES (1) ES2322652T3 (sr)
HK (1) HK1099014A1 (sr)
HR (1) HRP20090266T1 (sr)
IL (1) IL173905A (sr)
MA (1) MA28034A1 (sr)
MX (1) MXPA06002562A (sr)
MY (1) MY141308A (sr)
NO (1) NO20061047L (sr)
NZ (1) NZ545538A (sr)
PL (1) PL1711470T3 (sr)
PT (1) PT1711470E (sr)
RS (1) RS20060146A (sr)
SI (1) SI1711470T1 (sr)
TN (1) TNSN06077A1 (sr)
TW (1) TW200519092A (sr)
UA (1) UA83501C2 (sr)
WO (1) WO2005023772A1 (sr)
ZA (1) ZA200601989B (sr)

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AU2007229550B2 (en) * 2006-03-27 2012-03-08 F. Hoffmann-La Roche Ag Malonamide derivatives as gamma secretase inhibitors
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US7579464B2 (en) * 2007-05-25 2009-08-25 Hoffmann-La Roche Inc. Process for preparation of enantiomerically pure compounds
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KR101330184B1 (ko) 2010-10-15 2013-11-15 성균관대학교산학협력단 감마-세크레타제 저해제를 유효성분으로 함유하는 류마티스성 관절염의 예방 또는 치료용 조성물
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CN104854097A (zh) 2012-09-21 2015-08-19 百时美施贵宝公司 N-取代的二(氟烷基)-1,4-苯并二氮杂*酮化合物
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CN104968648A (zh) 2012-09-21 2015-10-07 百时美施贵宝公司 1,4-苯并二氮杂*酮化合物的前药
CN104797569A (zh) 2012-09-21 2015-07-22 百时美施贵宝公司 取代的1,5-苯并二氮杂*酮化合物
TWI614238B (zh) 2012-09-21 2018-02-11 必治妥美雅史谷比公司 雙(氟烷基)-1,4-苯并二氮呯酮化合物及其前藥
JP2015534554A (ja) 2012-09-21 2015-12-03 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company アルキル,フルオロアルキル−1,4−ベンゾジアゼピノン化合物
EP2897954B1 (en) 2012-09-21 2016-10-26 Bristol-Myers Squibb Company Fluoroalkyl-1,4-benzodiazepinone compounds
JP2016515625A (ja) 2013-04-04 2016-05-30 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 増殖性疾患を治療するための併用療法
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NZ741553A (en) * 2015-10-30 2019-08-30 Inception 3 Inc Dibenzo azepine compounds and their use in the treatment of otic diseases and disorders
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DE602004020680D1 (de) * 2003-09-09 2009-05-28 Hoffmann La Roche Die aktivität von gamma-secretase blockierende malonamidderivate

Also Published As

Publication number Publication date
PT1711470E (pt) 2009-05-21
ZA200601989B (en) 2007-05-30
JP4571639B2 (ja) 2010-10-27
PL1711470T3 (pl) 2009-09-30
JP2007505063A (ja) 2007-03-08
SI1711470T1 (sl) 2009-08-31
HRP20090266T1 (en) 2009-06-30
BRPI0413533A (pt) 2006-10-10
EP1711470B1 (en) 2009-04-15
CN100593539C (zh) 2010-03-10
TNSN06077A1 (fr) 2007-10-03
CO5660268A2 (es) 2006-07-31
TW200519092A (en) 2005-06-16
JP2010229153A (ja) 2010-10-14
AU2004270361B2 (en) 2009-06-25
EA200600503A1 (ru) 2006-08-25
CN1875005A (zh) 2006-12-06
CA2537440A1 (en) 2005-03-17
ATE428698T1 (de) 2009-05-15
HK1099014A1 (en) 2007-08-03
AU2004270361A1 (en) 2005-03-17
KR20060054455A (ko) 2006-05-22
MY141308A (en) 2010-04-16
IL173905A (en) 2011-05-31
UA83501C2 (uk) 2008-07-25
ECSP066414A (es) 2006-09-18
MXPA06002562A (es) 2006-06-20
NO20061047L (no) 2006-04-04
DK1711470T3 (da) 2009-06-08
US20050054633A1 (en) 2005-03-10
MA28034A1 (fr) 2006-07-03
US7160875B2 (en) 2007-01-09
EP1711470A1 (en) 2006-10-18
DE602004020680D1 (de) 2009-05-28
ES2322652T3 (es) 2009-06-24
WO2005023772A1 (en) 2005-03-17
CA2537440C (en) 2012-07-10
KR100834177B1 (ko) 2008-05-30
KR20070087690A (ko) 2007-08-28
CY1109225T1 (el) 2014-07-02
KR20070087233A (ko) 2007-08-27
AR045609A1 (es) 2005-11-02
IL173905A0 (en) 2006-07-05
NZ545538A (en) 2008-12-24
EA009940B1 (ru) 2008-04-28
KR100838852B1 (ko) 2008-06-16
CR8264A (es) 2008-09-22

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