ATE428698T1 - Die aktivität von gamma-secretase blockierende malonamidderivate - Google Patents

Die aktivität von gamma-secretase blockierende malonamidderivate

Info

Publication number
ATE428698T1
ATE428698T1 AT04764665T AT04764665T ATE428698T1 AT E428698 T1 ATE428698 T1 AT E428698T1 AT 04764665 T AT04764665 T AT 04764665T AT 04764665 T AT04764665 T AT 04764665T AT E428698 T1 ATE428698 T1 AT E428698T1
Authority
AT
Austria
Prior art keywords
secretase
gamma
activity
malonamide derivatives
blocking
Prior art date
Application number
AT04764665T
Other languages
English (en)
Inventor
Alexander Flohr
Guido Galley
Roland Jakob-Roetne
Eric Kitas
Jens-Uwe Peters
Wolfgang Wostl
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Application granted granted Critical
Publication of ATE428698T1 publication Critical patent/ATE428698T1/de

Links

Classifications

    • 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)
AT04764665T 2003-09-09 2004-08-31 Die aktivität von gamma-secretase blockierende malonamidderivate ATE428698T1 (de)

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
ATE428698T1 true ATE428698T1 (de) 2009-05-15

Family

ID=34224068

Family Applications (1)

Application Number Title Priority Date Filing Date
AT04764665T ATE428698T1 (de) 2003-09-09 2004-08-31 Die aktivität von gamma-secretase blockierende malonamidderivate

Country Status (34)

Country Link
US (1) US7160875B2 (de)
EP (1) EP1711470B1 (de)
JP (2) JP4571639B2 (de)
KR (3) KR100834177B1 (de)
CN (1) CN100593539C (de)
AR (1) AR045609A1 (de)
AT (1) ATE428698T1 (de)
AU (1) AU2004270361B2 (de)
BR (1) BRPI0413533A (de)
CA (1) CA2537440C (de)
CO (1) CO5660268A2 (de)
CR (1) CR8264A (de)
CY (1) CY1109225T1 (de)
DE (1) DE602004020680D1 (de)
DK (1) DK1711470T3 (de)
EA (1) EA009940B1 (de)
EC (1) ECSP066414A (de)
ES (1) ES2322652T3 (de)
HR (1) HRP20090266T1 (de)
IL (1) IL173905A (de)
MA (1) MA28034A1 (de)
MX (1) MXPA06002562A (de)
MY (1) MY141308A (de)
NO (1) NO20061047L (de)
NZ (1) NZ545538A (de)
PL (1) PL1711470T3 (de)
PT (1) PT1711470E (de)
RS (1) RS20060146A (de)
SI (1) SI1711470T1 (de)
TN (1) TNSN06077A1 (de)
TW (1) TW200519092A (de)
UA (1) UA83501C2 (de)
WO (1) WO2005023772A1 (de)
ZA (1) ZA200601989B (de)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1592684B1 (de) * 2003-02-04 2008-07-30 F. Hoffmann-La Roche Ag Malonamidderivate als gamma-secretaseinhibitoren
UA83501C2 (uk) * 2003-09-09 2008-07-25 Ф.Хоффманн-Ля Рош Аг ПОХІДНІ МАЛОНАМІДУ, ЩО БЛОКУЮТЬ АКТИВНІСТЬ γ-СЕКРЕТАЗИ
RU2356895C2 (ru) * 2003-10-06 2009-05-27 Ф.Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ЗАМЕЩЕННОГО ДИБЕНЗОАЗЕПИНА И БЕНЗОДИАЗЕПИНА, ПОЛЕЗНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ γ-СЕКРЕТАЗЫ
US7211573B2 (en) 2004-12-08 2007-05-01 Hoffmann-La Roche Inc. Malonamide derivatives
CA2645756C (en) * 2006-03-27 2013-12-31 F. Hoffmann-La Roche Ag Malonamide derivatives as gamma secretase inhibitors
CN101516859B (zh) * 2006-09-20 2012-07-04 霍夫曼-拉罗奇有限公司 4-氧代-2,3,4,5-四氢-苯并[b][1,4]二氮杂*衍生物
EP2109604A1 (de) * 2007-02-02 2009-10-21 F. Hoffmann-Roche AG 6-oxo-6,7-dihydro-5h-dibenzo[b,d]azepin-7-ylderivate
CA2679985A1 (en) * 2007-03-15 2008-09-18 F. Hoffmann-La Roche Ag Malonamides as orexin antagonists
US7579464B2 (en) * 2007-05-25 2009-08-25 Hoffmann-La Roche Inc. Process for preparation of enantiomerically pure compounds
CN101909633B (zh) * 2008-01-11 2012-05-30 霍夫曼-拉罗奇有限公司 γ-分泌酶抑制剂用于治疗癌症的应用
US8741889B2 (en) 2008-01-11 2014-06-03 Hoffmann-La Roche Inc Method of treating non-small cell lung cancer and colon cancer with gamma-secretase inhibitor
US8309299B2 (en) 2010-05-19 2012-11-13 Hoffmann-La Roche Inc. Combination therapy and method for assessing resistance to treatment
WO2012040444A2 (en) * 2010-09-24 2012-03-29 Bristol-Myers Squibb Company Treatment of patients with incipient alzheimer's disease
WO2012050370A2 (ko) * 2010-10-15 2012-04-19 성균관대학교산학협력단 감마-세크레타제 저해제를 유효성분으로 함유하는 류마티스성 관절염의 예방 또는 치료용 조성물
KR101330184B1 (ko) 2010-10-15 2013-11-15 성균관대학교산학협력단 감마-세크레타제 저해제를 유효성분으로 함유하는 류마티스성 관절염의 예방 또는 치료용 조성물
US20120114638A1 (en) 2010-11-08 2012-05-10 John Boylan Combination therapy
US20120184529A1 (en) 2011-01-14 2012-07-19 Demario Mark D Combination therapy
US20120225860A1 (en) 2011-03-02 2012-09-06 John Frederick Boylan Method for administration of a gamma secretase inhibitor
TWI530489B (zh) 2011-03-22 2016-04-21 必治妥美雅史谷比公司 雙(氟烷基)-1,4-苯二氮呯酮化合物
AR087107A1 (es) 2011-07-27 2014-02-12 Lilly Co Eli Compuesto inhibidor de la señalizacion de la trayectoria notch
JP2015529253A (ja) 2012-09-21 2015-10-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Notch阻害剤としてのフルオロアルキルおよびフルオロシクロアルキル1,4−ベンゾジアゼピノン化合物
JP2015534553A (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 置換1,5−ベンゾジアゼピノン化合物
US9133126B2 (en) 2012-09-21 2015-09-15 Bristol-Myers Squibb Company Fluoroalkyl dibenzoazepinone compounds
JP2015531792A (ja) 2012-09-21 2015-11-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 1,4−ベンゾジアゼピノン化合物のプロドラッグ
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
CN104822677A (zh) 2012-09-21 2015-08-05 百时美施贵宝公司 氟烷基-1,4-苯并二氮杂*酮化合物
US9242941B2 (en) 2012-09-21 2016-01-26 Bristol-Myers Squibb Company Alkyl, fluoroalkyl-1,4-benzodiazepinone compounds
EP2897946B1 (de) 2012-09-21 2016-11-16 Bristol-Myers Squibb Company N-substituierte bis(fluoralkyl)-1,4-benzodiazepinonverbindungen
JP2015529251A (ja) 2012-09-21 2015-10-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Notch阻害剤としての三環系複素環式化合物
CN105101968A (zh) 2013-04-04 2015-11-25 百时美施贵宝公司 治疗增殖性疾病的组合疗法
EP2932966A1 (de) 2014-04-16 2015-10-21 Novartis AG Gammasekretasehemmer zur Behandlung von Atemwegserkrankungen
MX378973B (es) * 2015-10-30 2025-03-10 Pipeline Therapeutics Inc Compuestos de dibenzo-azepina y su uso en el tratamiento de enfermedades y trastornos óticos.
IL267253B2 (en) * 2016-12-16 2023-04-01 Pipeline Therapeutics Inc Methods for treating cochlear synaptopathy
EP3615055A1 (de) 2017-04-28 2020-03-04 Novartis AG Zellen, die einen auf bcma abzielenden chimären antigenrezeptor exprimieren, und kombinationsbehandlung mit einem gamma-sekretase-inhibitor
EP3615068A1 (de) 2017-04-28 2020-03-04 Novartis AG Auf bcma abzielender wirkstoff und kombinationstherapie mit einem gamma-sekretase-inhibitor
WO2019034532A1 (en) * 2017-08-15 2019-02-21 Bayer Aktiengesellschaft 4-oxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-7-carboxamides
BR112020024351A2 (pt) 2018-06-01 2021-02-23 Novartis Ag moléculas de ligação contra bcma e usos das mesmas
CA3144324A1 (en) 2019-06-24 2020-12-30 Novartis Ag Dosing regimen and combination therapies for multispecific antibodies targeting b-cell maturation antigen
WO2022020658A1 (en) * 2020-07-23 2022-01-27 Purdue Research Foundation Notch signaling inhibitors for treating obesity and metabolic disorders
CN117881667A (zh) * 2021-08-31 2024-04-12 巴斯夫欧洲公司 含有稠环系的除草剂丙二酰胺
CN119095890A (zh) 2022-11-04 2024-12-06 株式会社Lg化学 全息图记录介质和包括其的光学元件
CN116621721B (zh) * 2023-04-12 2025-03-18 珠海市柏瑞医药科技有限公司 一种壬二酰胺的制备方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0675886T3 (da) * 1992-12-10 2000-09-18 Pfizer Aminomethylensubstituerede ikke-aromatiske heterocykler og deres anvendelse som substance P-antagonister
US5672598A (en) * 1995-03-21 1997-09-30 The Procter & Gamble Company Lactam-containing hydroxamic acids
CA2404273A1 (en) * 2000-04-11 2001-10-18 Bristol-Myers Squibb Pharma Company Substituted lactams as inhibitors of a.beta. protein production
GB0012671D0 (en) * 2000-05-24 2000-07-19 Merck Sharp & Dohme Therapeutic agents
EP1592684B1 (de) * 2003-02-04 2008-07-30 F. Hoffmann-La Roche Ag Malonamidderivate als gamma-secretaseinhibitoren
UA83501C2 (uk) * 2003-09-09 2008-07-25 Ф.Хоффманн-Ля Рош Аг ПОХІДНІ МАЛОНАМІДУ, ЩО БЛОКУЮТЬ АКТИВНІСТЬ γ-СЕКРЕТАЗИ

Also Published As

Publication number Publication date
US20050054633A1 (en) 2005-03-10
ECSP066414A (es) 2006-09-18
RS20060146A (sr) 2008-06-05
DK1711470T3 (da) 2009-06-08
AU2004270361B2 (en) 2009-06-25
US7160875B2 (en) 2007-01-09
ZA200601989B (en) 2007-05-30
BRPI0413533A (pt) 2006-10-10
CO5660268A2 (es) 2006-07-31
HRP20090266T1 (en) 2009-06-30
SI1711470T1 (sl) 2009-08-31
JP2010229153A (ja) 2010-10-14
CA2537440C (en) 2012-07-10
HK1099014A1 (zh) 2007-08-03
KR100834177B1 (ko) 2008-05-30
KR20070087690A (ko) 2007-08-28
MY141308A (en) 2010-04-16
WO2005023772A1 (en) 2005-03-17
CY1109225T1 (el) 2014-07-02
PT1711470E (pt) 2009-05-21
KR20060054455A (ko) 2006-05-22
EP1711470B1 (de) 2009-04-15
TNSN06077A1 (fr) 2007-10-03
EP1711470A1 (de) 2006-10-18
KR20070087233A (ko) 2007-08-27
CN1875005A (zh) 2006-12-06
MXPA06002562A (es) 2006-06-20
UA83501C2 (uk) 2008-07-25
IL173905A0 (en) 2006-07-05
PL1711470T3 (pl) 2009-09-30
EA009940B1 (ru) 2008-04-28
CN100593539C (zh) 2010-03-10
NO20061047L (no) 2006-04-04
NZ545538A (en) 2008-12-24
ES2322652T3 (es) 2009-06-24
DE602004020680D1 (de) 2009-05-28
IL173905A (en) 2011-05-31
EA200600503A1 (ru) 2006-08-25
CR8264A (es) 2008-09-22
AU2004270361A1 (en) 2005-03-17
CA2537440A1 (en) 2005-03-17
JP4571639B2 (ja) 2010-10-27
JP2007505063A (ja) 2007-03-08
KR100838852B1 (ko) 2008-06-16
AR045609A1 (es) 2005-11-02
MA28034A1 (fr) 2006-07-03
TW200519092A (en) 2005-06-16

Similar Documents

Publication Publication Date Title
ATE428698T1 (de) Die aktivität von gamma-secretase blockierende malonamidderivate
ITMI20030709A1 (it) Miscele di stabilizzanti.
DE602004020156D1 (de) Verwaltung von Rahmenbursts
NO20043696L (no) Gamma-sekretaseinhibitorer
NL1025404A1 (nl) Pyrazolo-triazine verbindingen en gebruik daarvan.
DE60328426D1 (de) Gestaltung der Verschlusselemente
EP1583997A4 (de) Photoresistentfernung
DE602004019294D1 (de) Tetrahydronaphthalin- und harnstoffderivate
IS7729A (is) Bensónaþýridín með PDE 3/4 tálmunarvirkni
DK3587433T3 (da) Modificerede nukleotider
DE60304102D1 (de) Hautreinigungszusammensetzung
CY2017048I1 (el) Νεες φαρμακευτικες χρησεις των παραγωγων σταυροσπορινης
EP1500371A4 (de) Ultraschallgerät
IS8941A (is) Efnasambönd með bólgueyðandi virkni
NO20044916L (no) Preparater av sulfinylacetamid
ATE370929T1 (de) Cyclohexyl-harnstoff-derivate
DE60326190D1 (de) des Körpers
EP1486553A4 (de) Neues entparaffinierungshilfsmittel
FR2843451B1 (fr) Fronde du type lance-pierres
IS7943A (is) Ný amínóbensófenónefnasambönd
ITMI20041199A1 (it) Composizioni di coloranti e loro utilizzo
EP1589100A4 (de) Transkriptioneller aktivator
FI20021817A0 (fi) Kanyyli
ITCR20020004V0 (it) Portamonete
TH103167B (th) สารผสมและแอคติวิตีต้านไวรัสของอนุพันธ์อะซาอินโดลออกโซอะซีติกพิเพอราซีนซึ่งถูกแทนที่

Legal Events

Date Code Title Description
UEP Publication of translation of european patent specification

Ref document number: 1711470

Country of ref document: EP