MA37929A1 - Composés bis(fluoroalkyl) -1,4-benzodiazépinones en tant qu'inhibiteurs de notch - Google Patents

Composés bis(fluoroalkyl) -1,4-benzodiazépinones en tant qu'inhibiteurs de notch

Info

Publication number
MA37929A1
MA37929A1 MA37929A MA37929A MA37929A1 MA 37929 A1 MA37929 A1 MA 37929A1 MA 37929 A MA37929 A MA 37929A MA 37929 A MA37929 A MA 37929A MA 37929 A1 MA37929 A1 MA 37929A1
Authority
MA
Morocco
Prior art keywords
compounds
fluoroalkyl
bis
notch inhibitors
benzodiazepinone compounds
Prior art date
Application number
MA37929A
Other languages
English (en)
Other versions
MA37929B1 (fr
Inventor
Ashvinikumar V Gavai
George V Delucca
Daniel O'malley
Patrice Gill
Claude A Quesnelle
Brian E Fink
Yufen Zhao
Francis Y Lee
Original Assignee
Bristol Myers Squibb Co
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=49263506&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MA37929(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of MA37929A1 publication Critical patent/MA37929A1/fr
Publication of MA37929B1 publication Critical patent/MA37929B1/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic 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
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24—Oxygen atoms
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds 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
    • A61K31/573—Compounds 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
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic 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
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic 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
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24—Oxygen atoms
    • C07D243/26—Preparation from compounds already containing the benzodiazepine skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C07F9/12—Esters of phosphoric acids with hydroxyaryl compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)

Abstract

L'invention concerne des composés de formule (i) et/ou des sels de ceux-ci : formule (i) dans laquelle r1 représente ch2ch2cf3; r2 représente ch2ch2cf3ou ch2ch2ch2cf3; r3 représente h, ch3, ou rx; r4 représente h ou ry; le cycle a représente phényle ou pyridinyle ; et rx, ry, ra, rb, y et z sont tels que définis dans la description. L'invention concerne également des méthodes d'utilisation desdits composés pour inhiber le récepteur notch, et des compositions pharmaceutiques comprenant ces composés. Ces composés sont utiles dans le traitement, la prévention ou le ralentissement de la progression de maladies ou de troubles dans divers domaines thérapeutiques, comme le cancer ; ou en tant que promédicaments desdits composés.
MA37929A 2012-09-21 2013-09-20 Composés bis(fluoroalkyl) -1,4-benzodiazépinones en tant qu'inhibiteurs de notch MA37929B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261703912P 2012-09-21 2012-09-21
PCT/US2013/060790 WO2014047372A1 (fr) 2012-09-21 2013-09-20 Composés bis(fluoroalkyl) -1,4-benzodiazépinones en tant qu'inhibiteurs de notch

Publications (2)

Publication Number Publication Date
MA37929A1 true MA37929A1 (fr) 2018-06-29
MA37929B1 MA37929B1 (fr) 2018-09-28

Family

ID=49263506

Family Applications (1)

Application Number Title Priority Date Filing Date
MA37929A MA37929B1 (fr) 2012-09-21 2013-09-20 Composés bis(fluoroalkyl) -1,4-benzodiazépinones en tant qu'inhibiteurs de notch

Country Status (35)

Country Link
US (2) US8999918B2 (fr)
EP (1) EP2897945B1 (fr)
JP (1) JP6165255B2 (fr)
KR (1) KR102155588B1 (fr)
CN (1) CN104703976B (fr)
AR (1) AR093767A1 (fr)
AU (1) AU2013317923B2 (fr)
BR (1) BR112015005817B1 (fr)
CA (1) CA2885574C (fr)
CL (1) CL2015000711A1 (fr)
CO (1) CO7310522A2 (fr)
CY (1) CY1118739T1 (fr)
DK (1) DK2897945T3 (fr)
EA (1) EA027281B1 (fr)
ES (1) ES2617591T3 (fr)
HR (1) HRP20170352T8 (fr)
HU (1) HUE032038T2 (fr)
IL (1) IL237782A (fr)
LT (1) LT2897945T (fr)
MA (1) MA37929B1 (fr)
MX (1) MX367474B (fr)
MY (1) MY185233A (fr)
NZ (1) NZ707171A (fr)
PE (1) PE20150622A1 (fr)
PH (1) PH12015500414A1 (fr)
PL (1) PL2897945T3 (fr)
PT (1) PT2897945T (fr)
RS (1) RS55779B1 (fr)
SG (1) SG11201501573UA (fr)
SI (1) SI2897945T1 (fr)
SM (1) SMT201700153T1 (fr)
TN (1) TN2015000102A1 (fr)
TW (1) TWI614238B (fr)
UY (1) UY35041A (fr)
WO (1) WO2014047372A1 (fr)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2897960B1 (fr) 2012-09-21 2016-08-03 Bristol-Myers Squibb Company Composés hétérocycliques tricycliques utilisables en tant qu'inhibiteurs du récepteur notch
WO2014047369A1 (fr) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Composés de 1,5-benzodiazépinone substituée
US9242940B2 (en) 2012-09-21 2016-01-26 Bristol-Myers Squibb Company N-substituted bis(fluoroalkyl)-1,4-benzodiazepinone compounds
EP2897947B1 (fr) 2012-09-21 2016-10-26 Bristol-Myers Squibb Company Composés d'alkyl, fluoroalkyl-1, 4-benzodiazepinone
WO2014047397A1 (fr) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Composés de fluoralkyl- et de fluorocycloalkyl-1,4-benzodiazépinone utilisables en tant qu'inhibiteurs du récepteur notch
WO2014047391A1 (fr) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Promédicaments de composés 1,4-benzodiazépinones
EP2897954B1 (fr) 2012-09-21 2016-10-26 Bristol-Myers Squibb Company Composés fluoroalkyl-1,4-benzodiazépinones
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
WO2014047370A1 (fr) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Composés fluoroalkyl benzodiazépinones
WO2014165718A1 (fr) 2013-04-04 2014-10-09 Bristol-Myers Squibb Company Traitement combiné pour le traitement de maladies prolifératives
MX368391B (es) 2015-02-03 2019-09-30 Pfizer Ciclopropabenzofuranil-piridopirazindionas novedosas.
CA3099479A1 (fr) 2018-05-06 2019-11-14 Ayala Pharmaceuticals Inc. Compositions de combinaison comprenant des composes de bisfluoroalkyle-1,4-benzodiazepinone et leurs procedes d'utilisation
US20220339162A1 (en) * 2018-05-06 2022-10-27 Ayala Pharmaceuticals Inc. Bisfluoroalkyl-1,4-benzodiazepinone compounds for treating desmoid tumors
WO2019215585A1 (fr) * 2018-05-06 2019-11-14 Ayala Pharmaceuticals Inc. Compositions comprenant des inhibiteurs de cd20 et des composés de bisfluoroalkyl-1,4-benzodiazépinone et leurs procédés d'utilisation
CN118750499A (zh) * 2018-05-15 2024-10-11 艾雅拉制药公司 用于治疗腺样囊性癌的包含双氟烷基-1,4-苯并二氮杂䓬酮化合物的组合物
EP3793563A4 (fr) * 2018-05-15 2022-02-23 Bristol-Myers Squibb Company Compositions comprenant des composés de bisfluoroalkyl-1,4-benzodiazépinone et méthodes d'utilisation associées
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
TW202034900A (zh) 2018-10-02 2020-10-01 美商頻率醫療公司 有關耳用治療劑之醫藥組成物及方法
KR20220007050A (ko) 2019-04-08 2022-01-18 프리퀀시 테라퓨틱스, 인크. 난청을 치료하기 위한 chir99021과 발프로산의 조합
CA3171651A1 (fr) * 2020-02-16 2021-08-19 Ayala Pharmaceuticals Inc. Procedes de preparation de derives chiraux de benzodiazepinone
MX2023002612A (es) * 2020-09-03 2023-05-16 Bristol Myers Squibb Co Polimorfos de compuestos de bis(fluoroalquilo)-1,4-benzodiazepinon a y usos de los mismos.
CN112142629B (zh) * 2020-10-10 2021-09-14 西北工业大学 3-氨基磺酰基丙氨酸的制备方法
EP4255409A1 (fr) 2020-12-07 2023-10-11 Cellestia Biotech AG Combinaisons pharmaceutiques pour le traitement du cancer
EP4008324A1 (fr) 2020-12-07 2022-06-08 Cellestia Biotech AG Combinaisons comprenant un inhibiteur d'une protéine anti-apoptotique, telle que bcl-2, bcl-xl, bclw ou mcl-1, et un inhibiteur de voie de signalisation notch pour le traitement du cancer
US20240269120A1 (en) 2021-06-02 2024-08-15 Cellestia Biotech Ag Method for Treating an Autoimmune and Inflammatory Disease
WO2023079132A1 (fr) 2021-11-08 2023-05-11 Cellestia Biotech Ag Combinaisons pharmaceutiques pour le traitement du cancer
EP4223292A1 (fr) 2022-02-07 2023-08-09 Cellestia Biotech AG Combinaisons pharmaceutiques pour le traitement du cancer
EP4508052A4 (fr) * 2022-04-11 2026-04-01 Prism Biolab Co Ltd Nouveaux composés à cycles fusionnés à sept éléments
WO2024036097A1 (fr) 2022-08-12 2024-02-15 Nuvalent, Inc. Composés d'éther macrocycliques hétéroaromatiques et isotopologues de ceux-ci
US20260028319A1 (en) * 2022-12-28 2026-01-29 Immunome, Inc. Intermediate salt for the preparation of bis(fluoroalkyl) benzodiazepinone compounds
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
WO2025072117A1 (fr) 2023-09-25 2025-04-03 Nuvalent, Inc. Composés d'éther macrocycliques hétéroaromatiques et isotopologues de ceux-ci
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
CN117447393A (zh) * 2023-10-26 2024-01-26 浙江雅辰药物科技股份有限公司 一种瑞马唑仑中间体的制备方法
WO2025171296A1 (fr) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Inhibiteurs de ras
WO2025240847A1 (fr) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Inhibiteurs de ras
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (fr) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Compositions thérapeutiques et procédés de gestion d'effets liés au traitement
WO2026006747A1 (fr) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Inhibiteurs de ras
WO2026015801A1 (fr) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Méthodes de traitement d'une maladie ou d'un trouble liés à ras
WO2026015790A1 (fr) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Méthodes de traitement d'une maladie ou d'un trouble lié à ras
WO2026015796A1 (fr) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Méthodes de traitement d'une maladie ou d'un trouble lié à ras
WO2026015825A1 (fr) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Utilisation d'un inhibiteur de ras pour traiter le cancer du pancréas
WO2026050446A1 (fr) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Inhibiteurs de ras
WO2026072904A2 (fr) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions et méthodes de traitement du cancer du poumon

Family Cites Families (34)

* 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
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
US5852010A (en) 1996-04-03 1998-12-22 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
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
EP1313426A2 (fr) 1998-12-24 2003-05-28 Bristol-Myers Squibb Pharma Company Benzodiazepines succinoylamino utilisees comme inhibiteurs de la production de proteine a-beta
EP2359831A3 (fr) 1999-04-30 2012-02-01 The Regents of the University of Michigan Applications thérapeutiques de benzodiazépines pro-apoptotiques
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
WO2001027108A1 (fr) 1999-10-08 2001-04-19 Bristol-Myers Squibb Pharma Company AMINO SULFONAMIDES DE LACTAME UTILISES COMME INHIBITEURS DE LA PRODUCTION DE PROTEINE A$g(b)
CA2397543A1 (fr) 2000-01-24 2001-07-26 Timothy Harrison Inhibiteurs de la gamma-secretase
US6525044B2 (en) 2000-02-17 2003-02-25 Bristol-Myers Squibb Company Succinoylamino carbocycles and heterocycles as inhibitors of a-β protein production
US6495540B2 (en) 2000-03-28 2002-12-17 Bristol - Myers Squibb Pharma Company Lactams as inhibitors of A-β protein production
EP1268454A1 (fr) 2000-03-31 2003-01-02 Bristol-Myers Squibb Pharma Company Heterocycles succinoylamino en tant qu'inhibiteurs de la production de la beta-proteine
JP2004508289A (ja) 2000-04-03 2004-03-18 デュポン　ファーマシューティカルズ　カンパニー Ａβタンパク質産生の阻害剤としての環状ラクタム
CN1436175A (zh) 2000-04-03 2003-08-13 布里斯托尔-迈尔斯斯奎布药品公司 作为Aβ－蛋白生产抑制剂的环状内酰胺
GB0008710D0 (en) 2000-04-07 2000-05-31 Merck Sharp & Dohme Therapeutic compounds
CA2404273A1 (fr) 2000-04-11 2001-10-18 Bristol-Myers Squibb Pharma Company Lactames substitues utilises en tant qu'inhibiteurs de production de proteine a.beta.
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
EP1268450A1 (fr) 2000-06-01 2003-01-02 Bristol-Myers Squibb Pharma Company Lactames substitues par des succinates cycliques en tant qu'inhibiteurs de la production de la proteine beta
US7001901B2 (en) 2002-08-27 2006-02-21 Bristol-Myers Squibb Company Tetrazolylpropionamides as inhibitors of Aβ protein production
BR0314595A (pt) * 2002-09-20 2005-08-09 Arrow Therapeutics Ltd Uso de um derivado de benzodiazepina ou um sal farmaceuticamente aceitável deste, inalador ou nebulisador, produto, usos de um produto e de um composto ou sal farmaceuticamente aceitável deste, derivado de benzodiazepina, composto, e, composição farmacêutica
EP1592684B1 (fr) 2003-02-04 2008-07-30 F. Hoffmann-La Roche Ag Derives de malonamide utilises comme inhibiteurs de la gamma-secretase
GB0312365D0 (en) 2003-05-30 2003-07-02 Univ Aston Novel 3-substituted-1, 4-benzodiazepines
KR100834177B1 (ko) 2003-09-09 2008-05-30 에프. 호프만-라 로슈 아게 감마-세크리테이즈의 활성을 차단하는 말론아미드 유도체
EP1795198A1 (fr) 2005-12-09 2007-06-13 Hubrecht Laboratorium Traitement de l'esophage de Barret
MX2010001754A (es) 2007-08-14 2010-05-14 Lilly Co Eli Derivados de azepina como inhibidores de gamma secretasa.
AU2009203776A1 (en) 2008-01-11 2009-07-16 F. Hoffmann-La Roche Ag Use of a gamma-secretase inhibitor for treating cancer
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
US9242940B2 (en) * 2012-09-21 2016-01-26 Bristol-Myers Squibb Company N-substituted bis(fluoroalkyl)-1,4-benzodiazepinone compounds

Also Published As

Publication number Publication date
IL237782A (en) 2017-03-30
US20150166489A1 (en) 2015-06-18
US8999918B2 (en) 2015-04-07
WO2014047372A1 (fr) 2014-03-27
AR093767A1 (es) 2015-06-24
JP6165255B2 (ja) 2017-07-19
JP2015530411A (ja) 2015-10-15
EA027281B1 (ru) 2017-07-31
LT2897945T (lt) 2017-03-27
HRP20170352T1 (hr) 2017-05-05
NZ707171A (en) 2018-01-26
PE20150622A1 (es) 2015-05-11
CA2885574A1 (fr) 2014-03-27
HRP20170352T8 (hr) 2017-05-19
PH12015500414B1 (en) 2015-04-20
CN104703976A (zh) 2015-06-10
EP2897945B1 (fr) 2016-12-21
TWI614238B (zh) 2018-02-11
AU2013317923A1 (en) 2015-05-07
UY35041A (es) 2014-03-31
SI2897945T1 (sl) 2017-03-31
DK2897945T3 (en) 2017-03-27
MX367474B (es) 2019-08-23
EP2897945A1 (fr) 2015-07-29
SMT201700153T1 (it) 2017-05-08
EA201590581A1 (ru) 2015-07-30
PL2897945T3 (pl) 2017-06-30
BR112015005817B1 (pt) 2022-10-04
TN2015000102A1 (en) 2016-06-29
AU2013317923B2 (en) 2017-06-29
CY1118739T1 (el) 2017-07-12
CL2015000711A1 (es) 2015-09-04
RS55779B1 (sr) 2017-07-31
KR20150056780A (ko) 2015-05-27
MY185233A (en) 2021-04-30
SG11201501573UA (en) 2015-05-28
MA37929B1 (fr) 2018-09-28
ES2617591T3 (es) 2017-06-19
US20140087992A1 (en) 2014-03-27
TW201418230A (zh) 2014-05-16
MX2015003033A (es) 2015-06-10
BR112015005817A2 (pt) 2017-07-04
PT2897945T (pt) 2017-03-07
HUE032038T2 (en) 2017-09-28
CN104703976B (zh) 2017-03-08
CO7310522A2 (es) 2015-06-30
US9273014B2 (en) 2016-03-01
PH12015500414A1 (en) 2015-04-20
KR102155588B1 (ko) 2020-09-14
CA2885574C (fr) 2021-06-08

Similar Documents

Publication Publication Date Title
MA37929B1 (fr) Composés bis(fluoroalkyl) -1,4-benzodiazépinones en tant qu'inhibiteurs de notch
MA35036B1 (fr) Composés bis(fluoroalkyl)-1,4-benzodiazépinone
MA37762A1 (fr) Composés n-aryltriazole utilisés comme antagonistes de lpar
MA37764A1 (fr) Composés n-alkyltriazole utilisés comme antagonistes de lpar
MA42295B1 (fr) Composés de la benzoxazépin oxazolidinone et procédé pour leur utilisation
MA37891A1 (fr) Alcoxypyrazoles comme activateurs de guanylate cyclase soluble
MA35184B1 (fr) Antagonistes de trpv4
MA38227A1 (fr) Nouveaux composés bicycliques et leur utilisation en tant qu'agents antibactériens et inhibiteurs de ?-lactamase
MA47043A1 (fr) Composés indole carboxamides utiles comme inhibiteurs de kinase
MA37142A3 (fr) Dérivés de dihydro-benzo-oxazine et de dihydro-pyrido-oxazine
MA42410A (fr) Oxystérols et leurs méthodes d'utilisation
TN2015000347A1 (fr) Azabenzimidazoles servant d'inhibiteurs d'isoenzymes pde4 pour le traitement de troubles du snc et d'autres troubles
MA43979B1 (fr) Dérivés de 1h-indazole-3-carboxamide et composés similaires en tant qu'inhibiteurs du facteur d pour le traitement de maladies characterisés par une activité aberrante du système complémentaire, comme p.E. Troubles immunologiques
MA35576B1 (fr) Nouveaux composés
MA30932B1 (fr) Spirocetones servant d'inhibiteurs d'acetyl-coa -carboxylase
MA38398B1 (fr) Composés biaryle amides en tant qu'inhibiteurs de kinase
MA46229B1 (fr) Composés d'hétéroaryle carboxamide en tant qu'inhibiteurs de ripk2
MA37765A1 (fr) Composés de pyrazole substitués utilisés comme antagonistes de lpar
MA31170B1 (fr) Dérivés de 2-amino-5,7-dihydro-6h-pyrrolo[3,4-d]pyrimidine servant d'inhibiteurs de la hsp-90 pour le traitement du cancer
MA37831B1 (fr) Dérivés d'azaindole agissant comme inhibiteur de pi3k
MA38810A1 (fr) Inhibiteurs de rorc2 méthodes d'utilisation associées
MA39165A1 (fr) Dérivés de benzimidazole-proline pour leurs utilisations dans le traitement du syndrome des etats crepusculaires
MA38425A1 (fr) Composés bicycliques pour une utilisation comme agonistes selectifs pour le recepteur s1p1
MA39229A1 (fr) Pyrrolidines, térahydrofuranes et cyclopentanes substitués utiles en tant qu'antagonistes des récepteurs des orexines
MA38206A1 (fr) Pyridyl-hydrazones pour le traitement de la tuberculose et de maladies associées