CY1116423T1 - Ενωσεις δις(φθοροαλκυλο)-1,4-βενζοδιαζεπινονης - Google Patents

Ενωσεις δις(φθοροαλκυλο)-1,4-βενζοδιαζεπινονης

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Publication number
CY1116423T1
CY1116423T1 CY20151100355T CY151100355T CY1116423T1 CY 1116423 T1 CY1116423 T1 CY 1116423T1 CY 20151100355 T CY20151100355 T CY 20151100355T CY 151100355 T CY151100355 T CY 151100355T CY 1116423 T1 CY1116423 T1 CY 1116423T1
Authority
CY
Cyprus
Prior art keywords
compounds
benzodiazepinone
fluoroalkyl
bis
ch2ch2cf3
Prior art date
Application number
CY20151100355T
Other languages
English (en)
Inventor
Claude Quesnelle
Soong-Hoon Kim
Francis Lee
Ashvinikumar Gavai
Original Assignee
Bristol-Myers Squibb Company
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 Bristol-Myers Squibb Company filed Critical Bristol-Myers Squibb Company
Publication of CY1116423T1 publication Critical patent/CY1116423T1/el

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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • 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
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/33Heterocyclic compounds
    • A61K31/555Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Αποκαλύπτονται ενώσεις του τύπου (I) ή προφάρμακα αυτών· όπου: η R1 είναι CH2CF3 ή CH2CH2CF3· η R2 είναι CH2CF3, CH2CH2CF3, ή CH2CH2CH2CF3· η R3 είναι Η ή CH3· έκαστη Ra είναι ανεξαρτήτως F, CI, -CN, -OCH3, και/ή NHCH2CH2OCH3· και z είναι μηδέν, 1 ή 2. Επίσης αποκαλύπτονται μέθοδοι χρήσης τέτοιων ενώσεων για αναστολή του υποδοχέα Notch, και φαρμακευτικές συνθέσεις που περιλαμβάνουν τέτοιες ενώσεις. Οι ενώσεις αυτές είναι χρήσιμες στη θεραπευτική αγωγή, πρόληψη, ή επιβράδυνση της εξέλιξης παθήσεων ή διαταραχών σε ποικιλία θεραπευτικών πεδίων, όπως καρκίνο.
CY20151100355T 2011-03-22 2015-04-17 Ενωσεις δις(φθοροαλκυλο)-1,4-βενζοδιαζεπινονης CY1116423T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161466238P 2011-03-22 2011-03-22
EP12711102.9A EP2688873B1 (en) 2011-03-22 2012-03-22 Bis(fluoroalkyl)-1,4-benzodiazepinone compounds

Publications (1)

Publication Number Publication Date
CY1116423T1 true CY1116423T1 (el) 2017-02-08

Family

ID=45894701

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20151100355T CY1116423T1 (el) 2011-03-22 2015-04-17 Ενωσεις δις(φθοροαλκυλο)-1,4-βενζοδιαζεπινονης

Country Status (32)

Country Link
US (2) US8629136B2 (el)
EP (1) EP2688873B1 (el)
JP (1) JP5873923B2 (el)
KR (1) KR101948347B1 (el)
CN (1) CN103717576B (el)
AR (1) AR085471A1 (el)
AU (1) AU2012230904B2 (el)
BR (1) BR112013024059B1 (el)
CA (1) CA2830902C (el)
CL (1) CL2013002690A1 (el)
CO (1) CO6771446A2 (el)
CY (1) CY1116423T1 (el)
DK (1) DK2688873T3 (el)
EA (1) EA022530B1 (el)
ES (1) ES2534080T3 (el)
HK (1) HK1189218A1 (el)
HR (1) HRP20150273T1 (el)
IL (1) IL228534A (el)
MA (1) MA35036B1 (el)
MX (1) MX2013010420A (el)
MY (1) MY161233A (el)
PE (1) PE20140626A1 (el)
PL (1) PL2688873T3 (el)
PT (1) PT2688873E (el)
RS (1) RS53843B1 (el)
SG (1) SG193555A1 (el)
SI (1) SI2688873T1 (el)
SM (1) SMT201500091B (el)
TN (1) TN2013000372A1 (el)
TW (1) TWI530489B (el)
UY (1) UY33961A (el)
WO (1) WO2012129353A1 (el)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8883145B2 (en) 2009-10-16 2014-11-11 Oncomed Pharmaceuticals, Inc. Methods of treatment with DLL4 antagonists and an anti-hypertensive agent
US8858941B2 (en) 2011-09-23 2014-10-14 Oncomed Pharmaceuticals, Inc. VEGF/DLL4 binding agents and uses thereof
WO2014047392A1 (en) * 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Fluoroalkyl-1,4-benzodiazepinone compounds
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
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
EP2897942B1 (en) * 2012-09-21 2016-08-31 Bristol-Myers Squibb Company Fluoroalkyl and fluorocycloalkyl 1,4-benzodiazepinone compounds as notch inhibitors
US9187434B2 (en) 2012-09-21 2015-11-17 Bristol-Myers Squibb Company Substituted 1,5-benzodiazepinones compounds
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
EP2897941B1 (en) * 2012-09-21 2016-09-07 Bristol-Myers Squibb Company Prodrugs of 1,4-benzodiazepinone compounds
WO2014047390A1 (en) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Tricyclic heterocyclic compounds as notch inhibitors
EP2897938B1 (en) 2012-09-21 2017-03-15 Bristol-Myers Squibb Company Fluoroalkyl dibenzodiazepinone compounds
EP2914961A4 (en) 2012-10-31 2016-04-20 Oncomed Pharm Inc METHODS AND MONITORING A TREATMENT BY AN ANTAGONIST OF DLL4
EP2981267A1 (en) * 2013-04-04 2016-02-10 Bristol-Myers Squibb Company Combination therapy for the treatment of proliferative diseases
KR20160099081A (ko) 2013-07-26 2016-08-19 업데이트 파마 인코포레이트 비산트렌의 치료 효과 개선용 조합 방법
CN103435562B (zh) * 2013-08-26 2016-02-24 华东理工大学 6-取代苯并二氮卓-2,4-二酮类化合物及其用途
WO2016070051A2 (en) 2014-10-31 2016-05-06 Oncomed Pharmaceuticals, Inc. Combination therapy for treatment of disease
WO2016066115A1 (zh) * 2014-10-31 2016-05-06 厦门大学 取代杂环衍生物、其制备方法和用途
CN104356082B (zh) * 2014-10-31 2016-07-13 厦门大学 一类取代杂环衍生物及其制备方法
CN104352488B (zh) * 2014-10-31 2016-08-31 厦门大学 一类取代杂环衍生物在制备治疗疼痛药物中的应用
CN104892532B (zh) * 2015-05-20 2017-09-08 成都理工大学 手性3‑取代1,3,4,5‑四氢‑1,4‑苯二氮*‑2‑酮的合成工艺
LT3324977T (lt) 2015-07-22 2022-10-25 Enanta Pharmaceuticals, Inc. Benzodiazepino dariniai kaip rsv inhibitoriai
CN109071644B (zh) 2015-09-23 2023-09-19 昂考梅德药品有限公司 治疗癌症的方法和组合物
CN108699077B (zh) 2016-01-15 2021-03-02 英安塔制药有限公司 作为rsv抑制剂的杂环化合物
BR112018068565A2 (pt) 2016-03-15 2019-02-12 Oryzon Genomics, S.A. combinações de inibidores de lsd1 para uso no tratamento de tumores sólidos
US10358441B2 (en) 2017-02-16 2019-07-23 Enanta Pharmaceuticals, Inc. Processes for the preparation of benzodiazepine derivatives
US20200055948A1 (en) 2017-04-28 2020-02-20 Novartis Ag Cells expressing a bcma-targeting chimeric antigen receptor, and combination therapy with a gamma secretase inhibitor
US20200179511A1 (en) 2017-04-28 2020-06-11 Novartis Ag Bcma-targeting agent, and combination therapy with a gamma secretase inhibitor
US10752598B2 (en) 2017-06-07 2020-08-25 Enanta Pharmaceuticals, Inc. Aryldiazepine derivatives as RSV inhibitors
WO2019006295A1 (en) 2017-06-30 2019-01-03 Enanta Pharmaceuticals, Inc. HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
US10851115B2 (en) 2017-06-30 2020-12-01 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as RSV inhibitors
EP3438128B1 (en) * 2017-08-04 2020-05-20 Alzheimur 2012 S.L. Anti-presenilin antibody for use in the prevention and/or treatment of cancer
EP3687543B1 (en) 2017-09-29 2024-03-20 Enanta Pharmaceuticals, Inc. Combinations of pharmaceutical agents as rsv inhibitors
US10501422B2 (en) 2017-11-13 2019-12-10 Enanta Pharmaceuticals, Inc. Processes for the resolution of benzodiazepin-2-one and benzoazepin-2-one derivatives
US10647711B2 (en) 2017-11-13 2020-05-12 Enanta Pharmaceuticals, Inc. Azepin-2-one derivatives as RSV inhibitors
US10975094B2 (en) 2018-04-11 2021-04-13 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as RSV inhibitors
WO2019215585A1 (en) * 2018-05-06 2019-11-14 Ayala Pharmaceuticals Inc. Compositions comprising cd20 inhibitors and bisfluoroalkyl-1,4-benzodiazepinone compounds and methods of use thereof
CA3099479A1 (en) * 2018-05-06 2019-11-14 Ayala Pharmaceuticals Inc. Combination compositions comprising bisfluoroalkyl-1,4- benzodiazepinone compounds and methods of use thereof
WO2019222298A1 (en) * 2018-05-15 2019-11-21 Bristol-Myers Squibb Company Compositions comprising bisfluoroalkyl-1,4-benzodiazepinone compounds and methods of use thereof
AU2019271044A1 (en) * 2018-05-15 2021-01-14 Ayala Pharmaceuticals Inc. Compositions comprising bisfluoroalkyl-l,4-benzodiazepinone compounds for treating adenoid cystic carcinoma
SG11202011589WA (en) * 2018-05-24 2020-12-30 Ayala Pharmaceuticals Inc Compositions comprising bisfluoroalkyl-1,4-benzodiazepinone compounds and immunotherapeutics and methods of use thereof
CU20200089A7 (es) 2018-06-01 2021-07-02 Novartis Ag Moléculas de unión contra bcma
JP2022525893A (ja) 2019-03-18 2022-05-20 エナンタ ファーマシューティカルズ インコーポレイテッド Rsv阻害剤としてのベンゾジアゼピン誘導体
US11179400B2 (en) 2019-04-09 2021-11-23 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as RSV inhibitors
BR112021022966A2 (pt) * 2019-05-15 2022-01-04 Ayala Pharmaceuticals Inc Método para reduzir o tamanho do tumor
JP2022538237A (ja) 2019-06-24 2022-09-01 ノバルティス アーゲー B細胞成熟抗原を標的にする多重特異性抗体のための投与計画及び組み合わせ治療
US11505558B1 (en) 2019-10-04 2022-11-22 Enanta Pharmaceuticals, Inc. Antiviral heterocyclic compounds
JP2022550436A (ja) 2019-10-04 2022-12-01 エナンタ ファーマシューティカルズ インコーポレイテッド 抗ウイルス性複素環化合物
UY39032A (es) 2020-01-24 2021-07-30 Enanta Pharm Inc Compuestos heterocíclicos como agentes antivirales
US11534439B2 (en) 2020-07-07 2022-12-27 Enanta Pharmaceuticals, Inc. Dihydroquinoxaline and dihydropyridopyrazine derivatives as RSV inhibitors
WO2022051442A1 (en) 2020-09-03 2022-03-10 Bristol-Myers Squibb Company Polymorphs of bis(fluoroalkyl)-1,4-benzodiazepinone compounds and uses thereof
US11945824B2 (en) 2020-10-19 2024-04-02 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as anti-viral agents
EP4008324A1 (en) 2020-12-07 2022-06-08 Cellestia Biotech AG Combinations comprising an inhibitor of an anti-apoptotic protein, such as bcl-2, bcl-xl, bclw or mcl-1, and a notch signaling pathway inhibitor for treating cancer
US20240041884A1 (en) 2020-12-07 2024-02-08 Cellestia Biotech Ag Pharmaceutical Combinations for Treating Cancer
MX2023009961A (es) 2021-02-26 2023-09-05 Enanta Pharm Inc Compuestos heterociclicos antivirales.
TW202313020A (zh) 2021-06-02 2023-04-01 瑞士商西萊絲蒂亞生物科技股份有限公司 自體免疫及發炎性疾病的治療方法
WO2023079132A1 (en) 2021-11-08 2023-05-11 Cellestia Biotech Ag Pharmaceutical combinations for treating cancer
EP4223292A1 (en) 2022-02-07 2023-08-09 Cellestia Biotech AG Pharmaceutical combinations for treating cancer
WO2024145306A1 (en) * 2022-12-28 2024-07-04 Ayala Pharmaceuticals Inc. Intermediate salt for the preparation of bis(fluoroalkyl) benzodiazepinone compounds

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5324726A (en) 1989-12-18 1994-06-28 Merck & Co., Inc. Benzodiazepine analogs
US5852010A (en) 1996-04-03 1998-12-22 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2000507587A (ja) * 1996-04-03 2000-06-20 メルク エンド カンパニー インコーポレーテッド ファルネシルタンパク質トランスフェラーゼ阻害剤
US6635632B1 (en) 1996-12-23 2003-10-21 Athena Neurosciences, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
HRP990246A2 (en) 1998-08-07 2000-06-30 Du Pont Pharm Co Succinoylamino benzodiazepines as inhibitors of a beta protein production
NZ525513A (en) 1998-08-07 2004-09-24 Pont Pharmaceuticals Du Succinoylamino lactams as inhibitors of Abeta protein production
US6737038B1 (en) 1998-11-12 2004-05-18 Bristol-Myers Squibb Company Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging
AU1618000A (en) 1998-11-12 2000-05-29 Du Pont Pharmaceuticals Company Use of radioligands to screen inhibitors of amyloid-beta peptide production
CA2347671A1 (en) 1998-12-24 2000-07-06 Dupont Pharmaceuticals Company Succinoylamino benzodiazepines as inhibitors of a.beta. protein production
JP5127096B2 (ja) 1999-04-30 2013-01-23 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン アポトーシスにより誘導される自己免疫疾患を処置するためのベンゾジアゼピンの使用
US6960576B2 (en) 1999-09-13 2005-11-01 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production
US6503902B2 (en) 1999-09-13 2003-01-07 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of a β protein production
WO2001027091A1 (en) 1999-10-08 2001-04-19 Du Pont Pharmaceuticals Company AMINO LACTAM SULFONAMIDES AS INHIBITORS OF Aβ PROTEIN PRODUCTION
CZ20022332A3 (cs) * 2000-01-07 2003-01-15 Transform Pharmaceuticals, Inc. Sestava vzorků
EP1254108A1 (en) 2000-01-24 2002-11-06 MERCK SHARP & DOHME LTD. Gamma-secretase inhibitors
JP2003523345A (ja) 2000-02-17 2003-08-05 ブリストル−マイヤーズ スクイブ ファーマ カンパニー Aβタンパク質産生の阻害剤としてのスクシノイルアミノ炭素環および複素環
US6495540B2 (en) 2000-03-28 2002-12-17 Bristol - Myers Squibb Pharma Company Lactams as inhibitors of A-β protein production
EP1268454A1 (en) 2000-03-31 2003-01-02 Bristol-Myers Squibb Pharma Company Succinoylamino heterocycles as inhibitors of a-beta protein production
AU2001253090A1 (en) 2000-04-03 2001-10-15 Bristol-Myers Squibb Pharma Company Cyclic lactams as inhibitors of abeta protein production
WO2001074784A1 (en) 2000-04-03 2001-10-11 Dupont Pharmaceuticals Company CYCLIC LACTAMS AS INHIBITORS OF A-β PROTEIN PRODUCTION
GB0008710D0 (en) 2000-04-07 2000-05-31 Merck Sharp & Dohme Therapeutic compounds
EP1289966A1 (en) 2000-04-11 2003-03-12 Bristol-Myers Squibb Pharma Company SUBSTITUTED LACTAMS AS INHIBITORS OF A$g(b) PROTEIN PRODUCTION
US6878363B2 (en) 2000-05-17 2005-04-12 Bristol-Myers Squibb Pharma Company Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging
GB0012671D0 (en) * 2000-05-24 2000-07-19 Merck Sharp & Dohme Therapeutic agents
CN1386118A (zh) 2000-06-01 2002-12-18 布里斯托尔-迈尔斯斯奎布药品公司 作为Aβ蛋白产生抑制剂的被环状琥珀酸酯取代的内酰胺类化合物
US7001901B2 (en) 2002-08-27 2006-02-21 Bristol-Myers Squibb Company Tetrazolylpropionamides as inhibitors of Aβ protein production
PL375860A1 (en) 2002-09-20 2005-12-12 Arrow Therapeutics Limited Benzodiazepine derivatives and pharmaceutical compositions containing them
ATE402934T1 (de) 2003-02-04 2008-08-15 Hoffmann La Roche Malonamidderivate als gamma-secretaseinhibitoren
GB0312365D0 (en) 2003-05-30 2003-07-02 Univ Aston Novel 3-substituted-1, 4-benzodiazepines
EP1711470B1 (en) 2003-09-09 2009-04-15 F. Hoffmann-La Roche Ag Malonamide derivatives blocking the activtiy of gamma-secretase
EP1795198A1 (en) 2005-12-09 2007-06-13 Hubrecht Laboratorium Treatment of Barret's esophagus
EP1996182A4 (en) 2006-02-27 2009-08-12 Univ Johns Hopkins CANCER TREATMENT WITH GAMMA SECRETASE INHIBITORS
MX2008012136A (es) 2006-03-27 2008-10-03 Hoffmann La Roche Derivados de malonamida como inhibidores de gama secretasa.
JP5001372B2 (ja) 2006-09-20 2012-08-15 エフ.ホフマン−ラ ロシュ アーゲー 4−オキソ−2,3,4,5−テトラヒドロ−ベンゾ[b][1,4]ジアゼピン誘導体
BRPI0815135A2 (pt) 2007-08-14 2015-02-03 Lilly Co Eli Derivados de azepina como inibidores de gama secretase.
MA33076B1 (fr) 2008-01-11 2012-03-01 Hoffmann La Roche Utilisation d'un inhibiteur de la gamma-secretase pour le traitement du cancer
US8637493B2 (en) 2009-11-12 2014-01-28 University Of Massachusetts Methods for treating glioblastoma
US20120225860A1 (en) 2011-03-02 2012-09-06 John Frederick Boylan Method for administration of a gamma secretase inhibitor

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