MX367474B - Compuestos de bis(fluoroalquil)-1,4-benzodiazepinona como inhibidores de notch. - Google Patents

Compuestos de bis(fluoroalquil)-1,4-benzodiazepinona como inhibidores de notch.

Info

Publication number
MX367474B
MX367474B MX2015003033A MX2015003033A MX367474B MX 367474 B MX367474 B MX 367474B MX 2015003033 A MX2015003033 A MX 2015003033A MX 2015003033 A MX2015003033 A MX 2015003033A MX 367474 B MX367474 B MX 367474B
Authority
MX
Mexico
Prior art keywords
compounds
fluoroalkyl
bis
notch inhibitors
benzodiazepinone compounds
Prior art date
Application number
MX2015003033A
Other languages
English (en)
Other versions
MX2015003033A (es
Inventor
E Fink Brian
Zhao Yufen
V Gavai Ashvinikumar
V Delucca George
O'malley Daniel
Gill Patrice
A Quesnelle Claude
Y Lee Francis
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=MX367474(B) "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 MX2015003033A publication Critical patent/MX2015003033A/es
Publication of MX367474B publication Critical patent/MX367474B/es

Links

Classifications

    • 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
    • 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)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)

Abstract

La presente invención se refiere a compuestos de la Fórmula (I) y/o sus sales: (ver Fórmula) en donde R1 es -CH2CH2CF3 R2 es -CH2CH2CF3 o -CH2CH2CH2CF3 R3 es H, -CH3 o Rx; R4 es H o Ry; el anillo A es fenilo o piridinilo; y Rx, Ry, Ra, Rb, y e z son como se definen en la presente. También se describen métodos para usar tales compuestos con el fin de inhibir el receptor de Notch, y composiciones farmacéuticas que comprenden tales compuestos. Estos compuestos son útiles para el tratamiento, la prevención o el enlentecimiento de la progresión de enfermedades o trastornos en varias áreas terapéuticas, tales como el cáncer; o como profármacos de tales compuestos.
MX2015003033A 2012-09-21 2013-09-20 Compuestos de bis(fluoroalquil)-1,4-benzodiazepinona como inhibidores de notch. MX367474B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261703912P 2012-09-21 2012-09-21
PCT/US2013/060790 WO2014047372A1 (en) 2012-09-21 2013-09-20 Bis(fluoroalkyl)-1,4-benzodiazepinone compounds as notch inhibitors

Publications (2)

Publication Number Publication Date
MX2015003033A MX2015003033A (es) 2015-06-10
MX367474B true MX367474B (es) 2019-08-23

Family

ID=49263506

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015003033A MX367474B (es) 2012-09-21 2013-09-20 Compuestos de bis(fluoroalquil)-1,4-benzodiazepinona como inhibidores de notch.

Country Status (35)

Country Link
US (2) US8999918B2 (es)
EP (1) EP2897945B1 (es)
JP (1) JP6165255B2 (es)
KR (1) KR102155588B1 (es)
CN (1) CN104703976B (es)
AR (1) AR093767A1 (es)
AU (1) AU2013317923B2 (es)
BR (1) BR112015005817B1 (es)
CA (1) CA2885574C (es)
CL (1) CL2015000711A1 (es)
CO (1) CO7310522A2 (es)
CY (1) CY1118739T1 (es)
DK (1) DK2897945T3 (es)
EA (1) EA027281B1 (es)
ES (1) ES2617591T3 (es)
HR (1) HRP20170352T8 (es)
HU (1) HUE032038T2 (es)
IL (1) IL237782A (es)
LT (1) LT2897945T (es)
MA (1) MA37929B1 (es)
MX (1) MX367474B (es)
MY (1) MY185233A (es)
NZ (1) NZ707171A (es)
PE (1) PE20150622A1 (es)
PH (1) PH12015500414B1 (es)
PL (1) PL2897945T3 (es)
PT (1) PT2897945T (es)
RS (1) RS55779B1 (es)
SG (1) SG11201501573UA (es)
SI (1) SI2897945T1 (es)
SM (1) SMT201700153T1 (es)
TN (1) TN2015000102A1 (es)
TW (1) TWI614238B (es)
UY (1) UY35041A (es)
WO (1) WO2014047372A1 (es)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014047374A1 (en) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Alkyl, fluoroalkyl-1,4-benzodiazepinone 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
US9249157B2 (en) 2012-09-21 2016-02-02 Bristol-Myers Squibb Company Tricyclic heterocycle compounds
EP2897954B1 (en) 2012-09-21 2016-10-26 Bristol-Myers Squibb Company Fluoroalkyl-1,4-benzodiazepinone compounds
US9187434B2 (en) 2012-09-21 2015-11-17 Bristol-Myers Squibb Company Substituted 1,5-benzodiazepinones compounds
JP2015533811A (ja) 2012-09-21 2015-11-26 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｎ−置換ビス（フルオロアルキル）１，４−ベンゾジアゼピノン化合物
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
WO2014047397A1 (en) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Fluoroalkyl and fluorocycloalkyl 1,4-benzodiazepinone compounds as notch|inhibitors
WO2014047370A1 (en) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Fluoroalkyl dibenzodiazepinone compounds
US9492469B2 (en) 2013-04-04 2016-11-15 Bristol-Myers Squibb Company Combination therapy for the treatment of proliferative diseases
MX368391B (es) 2015-02-03 2019-09-30 Pfizer Ciclopropabenzofuranil-piridopirazindionas novedosas.
US20220339162A1 (en) * 2018-05-06 2022-10-27 Ayala Pharmaceuticals Inc. Bisfluoroalkyl-1,4-benzodiazepinone compounds for treating desmoid tumors
KR20210005714A (ko) * 2018-05-06 2021-01-14 아얄라 파마큐티컬즈 아이엔씨. 비스플루오로알킬-1,4-벤조디아제피논 화합물을 포함하는 조합 조성물 및 이의 사용 방법
EP3790553A4 (en) * 2018-05-06 2022-04-20 Ayala Pharmaceuticals Inc. COMPOSITIONS COMPRISING CD20 INHIBITORS AND BISFLUOROALKYL-1,4-BENZODIAZEPINONE COMPOUNDS AND METHODS OF USE THEREOF
US20210220372A1 (en) * 2018-05-15 2021-07-22 Bristol-Myers Squibb Company Compositions comprising bisfluoroalkyl-1,4-benzodiazepinone compounds and methods of use thereof
CA3100394A1 (en) 2018-05-15 2019-11-21 Ayala Pharmaceuticals Inc. Compositions comprising bisfluoroalkyl-l,4-benzodiazepinone compounds for treating adenoid cystic carcinoma
CN112203661A (zh) * 2018-05-24 2021-01-08 艾雅拉制药公司 包含双氟烷基-1,4-苯并二氮杂*酮化合物与免疫治疗剂的组合物和其使用方法
US20220192984A1 (en) 2018-10-02 2022-06-23 Frequency Therapeutics, Inc. Pharmaceutical compositions comprising otic therapeutic agents and related methods
CA3136424A1 (en) 2019-04-08 2020-10-15 Frequency Therapeutics, Inc. Combination of chir99021 and valproic acid for treating hearing loss
EP4107148A4 (en) * 2020-02-16 2024-05-15 Ayala Pharmaceuticals Inc. PROCESS FOR PREPARING CHIRAL BENZODIAZEPINONE DERIVATIVES
EP4208162A4 (en) * 2020-09-03 2024-08-21 Bristol-Myers Squibb Company Polymorphs of bis(fluoroalkyl)-1,4-benzodiazepinone compounds and uses thereof
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
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
EP4255409A1 (en) 2020-12-07 2023-10-11 Cellestia Biotech AG Pharmaceutical combinations for treating cancer
EP4346816A2 (en) 2021-06-02 2024-04-10 Cellestia Biotech AG Compounds for use in a method for treating an autoimmune and inflammatory disease
EP4429661A1 (en) 2021-11-08 2024-09-18 Cellestia Biotech AG Pharmaceutical combinations for treating cancer
EP4223292A1 (en) 2022-02-07 2023-08-09 Cellestia Biotech AG Pharmaceutical combinations for treating cancer
WO2024036097A1 (en) 2022-08-12 2024-02-15 Nuvalent, Inc. Heteroaromatic macrocyclic ether compounds and isotopologues thereof
EP4642758A1 (en) * 2022-12-28 2025-11-05 Immunome, Inc. Intermediate salt for the preparation of bis(fluoroalkyl) benzodiazepinone compounds
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025072117A1 (en) 2023-09-25 2025-04-03 Nuvalent, Inc. Heteroaromatic macrocyclic ether compounds and isotopologues thereof
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

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
WO1997036879A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
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
NZ525513A (en) 1998-08-07 2004-09-24 Pont Pharmaceuticals Du Succinoylamino lactams as inhibitors of Abeta protein production
HRP990246A2 (en) * 1998-08-07 2000-06-30 Du Pont Pharm Co Succinoylamino benzodiazepines as inhibitors of a beta protein production
WO2000028331A1 (en) * 1998-11-12 2000-05-18 Du Pont Pharmaceuticals Company Use of radioligands to screen inhibitors of amyloid-beta peptide 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
BR9917082A (pt) * 1998-12-24 2001-11-06 Du Pont Pharm Co Compostos inibidores da produção de proteìnas a"beta", método de tratamento de disfunções neurológicas associadas com a produção de "beta"-amilóide, composição farmacêutica e, método de inibição da atividade de y-secretase
EP2062583B1 (en) 1999-04-30 2012-12-26 The Regents of the University of Michigan Therapeutic applications of pro-apoptotic benzodiazepines
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 (en) 1999-10-08 2001-04-19 Bristol-Myers Squibb Pharma Company AMINO LACTAM SULFONAMIDES AS INHIBITORS OF Aβ PROTEIN PRODUCTION
WO2001053255A1 (en) 2000-01-24 2001-07-26 Merck Sharp & Dohme Limited 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
JP2003529594A (ja) 2000-03-31 2003-10-07 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サクシノイルアミノ複素環
WO2001074783A1 (en) 2000-04-03 2001-10-11 Dupont Pharmaceuticals Company Cyclic lactams as inhibitors of a βετα protein production
AU2001253108A1 (en) 2000-04-03 2001-10-15 Bristol-Myers Squibb Pharma Company Cyclic lactams as inhibitors of a-beta protein production
GB0008710D0 (en) 2000-04-07 2000-05-31 Merck Sharp & Dohme Therapeutic compounds
CA2404273A1 (en) 2000-04-11 2001-10-18 Bristol-Myers Squibb Pharma Company Substituted lactams as inhibitors of a.beta. protein production
AU2001261728A1 (en) 2000-05-17 2001-11-26 Bristol-Myers Squibb Pharma Company Use of small molecule radioligands 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
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
NZ541324A (en) 2003-02-04 2008-10-31 Hoffmann La Roche Malonamide derivatives as gamma-secretase inhibitors
GB0312365D0 (en) 2003-05-30 2003-07-02 Univ Aston Novel 3-substituted-1, 4-benzodiazepines
DE602004020680D1 (de) 2003-09-09 2009-05-28 Hoffmann La Roche Die aktivität von gamma-secretase blockierende malonamidderivate
EP1795198A1 (en) 2005-12-09 2007-06-13 Hubrecht Laboratorium Treatment of Barret's esophagus
US8188069B2 (en) 2007-08-14 2012-05-29 Eli Lilly And Company Azepine derivatives as gamma-secretase inhibitors
BRPI0906831A2 (pt) 2008-01-11 2019-09-24 Hoffmann La Roche uso de um inibidor de gama-secretase para tratamento de câncer
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
JP2015533811A (ja) * 2012-09-21 2015-11-26 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｎ−置換ビス（フルオロアルキル）１，４−ベンゾジアゼピノン化合物

Also Published As

Publication number Publication date
LT2897945T (lt) 2017-03-27
WO2014047372A1 (en) 2014-03-27
TWI614238B (zh) 2018-02-11
CA2885574A1 (en) 2014-03-27
JP2015530411A (ja) 2015-10-15
TN2015000102A1 (en) 2016-06-29
CN104703976A (zh) 2015-06-10
KR20150056780A (ko) 2015-05-27
AU2013317923B2 (en) 2017-06-29
US20140087992A1 (en) 2014-03-27
JP6165255B2 (ja) 2017-07-19
BR112015005817B1 (pt) 2022-10-04
US9273014B2 (en) 2016-03-01
PE20150622A1 (es) 2015-05-11
BR112015005817A2 (pt) 2017-07-04
DK2897945T3 (en) 2017-03-27
TW201418230A (zh) 2014-05-16
MA37929A1 (fr) 2018-06-29
NZ707171A (en) 2018-01-26
PL2897945T3 (pl) 2017-06-30
AR093767A1 (es) 2015-06-24
CN104703976B (zh) 2017-03-08
IL237782A (en) 2017-03-30
MY185233A (en) 2021-04-30
EA027281B1 (ru) 2017-07-31
PH12015500414A1 (en) 2015-04-20
PT2897945T (pt) 2017-03-07
EP2897945A1 (en) 2015-07-29
SMT201700153T1 (it) 2017-05-08
MX2015003033A (es) 2015-06-10
US20150166489A1 (en) 2015-06-18
HRP20170352T1 (hr) 2017-05-05
HRP20170352T8 (hr) 2017-05-19
AU2013317923A1 (en) 2015-05-07
KR102155588B1 (ko) 2020-09-14
MA37929B1 (fr) 2018-09-28
CO7310522A2 (es) 2015-06-30
SG11201501573UA (en) 2015-05-28
CY1118739T1 (el) 2017-07-12
ES2617591T3 (es) 2017-06-19
EA201590581A1 (ru) 2015-07-30
SI2897945T1 (sl) 2017-03-31
CL2015000711A1 (es) 2015-09-04
UY35041A (es) 2014-03-31
EP2897945B1 (en) 2016-12-21
US8999918B2 (en) 2015-04-07
CA2885574C (en) 2021-06-08
PH12015500414B1 (en) 2015-04-20
RS55779B1 (sr) 2017-07-31
HUE032038T2 (en) 2017-09-28

Similar Documents

Publication Publication Date Title
MX367474B (es) Compuestos de bis(fluoroalquil)-1,4-benzodiazepinona como inhibidores de notch.
UY35012A (es) Alcoxipirazoles como activadores de guanilato ciclasa soluble
TN2013000372A1 (en) Bis(fluoroalkyl)-1,4-benzodiazepinone compounds
DOP2015000158A (es) Inhibidores de prmt5 y sus usos
CU20150014A7 (es) Análogos de piridazina 1,4-disustituida y métodos para el tratamiento de condiciones relacionadas con la deficiencia de smn
MX361815B (es) Compuestos pirazolopirimidinicos como inhibidores de cinasas.
ECSP14013222A (es) Indazoles
UY33557A (es) Inhibidores de oxadiazol de la produccion de leucotrieno
PH12014502733A1 (en) Neprilysin inhibitors
UY35898A (es) ?compuestos inhibidores de syk y composiciones que los comprenden?.
DOP2014000012A (es) Nuevos compuestos de 4-piperidinilo para uso como inhibidores de la tankirasa
UY33539A (es) Compuestos químicos alk
PE20150666A1 (es) Inhibidores de serina/treonina cinasa
EA201492023A1 (ru) Регуляторы пути комплемента и их применение
CO6771439A2 (es) Inhibidores de benzodioxano de la producción de leucotrieno
UY36875A (es) Composiciones inhibidoras de bromodominios para el tratamiento de diversas enfermedades
UY35551A (es) Derivados heteroarilos como inhibidores de aldosterona sintasa
MX2019003026A (es) Compuestos de heteroarilcarboxamida como inhibidores de ripk2.
GT201400242A (es) "nuevos compuestos de pirazol"
MX2016004841A (es) Compuestos de pirimidina substituidos y su uso como inhibidores de la tirosina cinasa del bazo (syk).
ECSP13012548A (es) Inhibidores de oxadiazol de la producción de leucotrienos.
TR201908822T4 (tr) Yeni flavonoid bileşikleri ve bunların kullanımları.
EA201491307A1 (ru) Терапевтическое применение имидазопиридиновых производных соединений
AR086791A1 (es) Moduladores alostericos positivos del receptor de acetilcolina nicotinico
CU20100127A7 (es) Derivados de tiazol usados como inhibidores de pi 3-cinasa

Legal Events

Date Code Title Description
FG Grant or registration