AR093767A1 - Compuestos de bis(fluoroalquil)-1,4-benzodiazepinona y profarmacos de estos - Google Patents

Compuestos de bis(fluoroalquil)-1,4-benzodiazepinona y profarmacos de estos

Info

Publication number
AR093767A1
AR093767A1 ARP130103390A ARP130103390A AR093767A1 AR 093767 A1 AR093767 A1 AR 093767A1 AR P130103390 A ARP130103390 A AR P130103390A AR P130103390 A ARP130103390 A AR P130103390A AR 093767 A1 AR093767 A1 AR 093767A1
Authority
AR
Argentina
Prior art keywords
profarms
fluoroalquil
benzodiazepinona
cyclopropyl
bis compounds
Prior art date
Application number
ARP130103390A
Other languages
English (en)
Inventor
Gill Patrice
A Quesnelle Claude
E Fink Brian
Zhao Yufen
Y Lee Francis
V Gavai Ashvinikumar
V Delucca George
Omalley Daniel
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=AR093767(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 AR093767A1 publication Critical patent/AR093767A1/es

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
    • 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
    • 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
    • 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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto caracterizado por la fórmula (1) y/o al menos una sal de aquel, en donde: R¹ es -CH₂CH₂CF₃; R² es -CH₂CH₂CF₃ o -CH₂CH₂CH₂CF₃; R³ es H, -CH₃ o Rˣ; R⁴ es H o Rʸ; Rˣ es: -CH₂OC(O)CH(CH₃)NH₂, -CH₂OC(O)CH(NH₂)CH(CH₃)₂, -CH₂OC(O)CH((CH(CH₃)₂)NHC(O)CH(NH₂)CH(CH₃)₂, o un compuesto del grupo de fórmulas (2); Rʸ es: -SCH₂CH(NH₂)C(O)OH, -SCH₂CH(NH₂)C(O)OCH₃ o -SCH₂CH(NH₂)C(O)OC(CH₃)₃; el anillo A es fenilo o piridinilo; cada Rᵃ es independientemente Cl, alquilo C₁₋₃, -CH₂OH, -CF₃, ciclopropilo, -OCH₃ y/u -O(ciclopropilo); cada Rᵇ es independientemente F, Cl, -CH₃, -CH₂OH, -CF₃, ciclopropilo y/u -OCH₃; y es 0, 1 ó 2; y z es 0, 1 ó 2; siempre que si el anillo A es fenilo y z es 0, entonces y es 1 ó 2 y al menos un Rᵃ es alquilo C₁₋₃, -CH₂OH, -CF₃, ciclopropilo u -O(ciclopropilo); siempre que si R³ es Rˣ, entonces R⁴ es H; y siempre que si R⁴ es Rʸ, entonces R³ es H o -CH₃.
ARP130103390A 2012-09-21 2013-09-20 Compuestos de bis(fluoroalquil)-1,4-benzodiazepinona y profarmacos de estos AR093767A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261703912P 2012-09-21 2012-09-21

Publications (1)

Publication Number Publication Date
AR093767A1 true AR093767A1 (es) 2015-06-24

Family

ID=49263506

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130103390A AR093767A1 (es) 2012-09-21 2013-09-20 Compuestos de bis(fluoroalquil)-1,4-benzodiazepinona y profarmacos de estos

Country Status (34)

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) PH12015500414A1 (es)
PL (1) PL2897945T3 (es)
PT (1) PT2897945T (es)
RS (1) RS55779B1 (es)
SG (1) SG11201501573UA (es)
SI (1) SI2897945T1 (es)
TN (1) TN2015000102A1 (es)
TW (1) TWI614238B (es)
UY (1) UY35041A (es)
WO (1) WO2014047372A1 (es)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104854094A (zh) 2012-09-21 2015-08-19 百时美施贵宝公司 氟烷基二苯并二氮杂*酮化合物
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
EP2897944B1 (en) 2012-09-21 2016-10-26 Bristol-Myers Squibb Company Substituted 1,5-benzodiazepinone compounds
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
WO2014047374A1 (en) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Alkyl, fluoroalkyl-1,4-benzodiazepinone compounds
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
CN104797584A (zh) 2012-09-21 2015-07-22 百时美施贵宝公司 作为notch抑制剂的三环杂环化合物
EP2897941B1 (en) 2012-09-21 2016-09-07 Bristol-Myers Squibb Company Prodrugs of 1,4-benzodiazepinone compounds
US9242940B2 (en) 2012-09-21 2016-01-26 Bristol-Myers Squibb Company N-substituted bis(fluoroalkyl)-1,4-benzodiazepinone compounds
US9492469B2 (en) 2013-04-04 2016-11-15 Bristol-Myers Squibb Company Combination therapy for the treatment of proliferative diseases
EA033423B1 (ru) 2015-02-03 2019-10-31 Pfizer Циклопропанбензофуранилпиридопиразиндионы
BR112020022654A2 (pt) * 2018-05-06 2021-03-09 Ayala Pharmaceuticals Inc. Composições de combinação que compreendem compostos de bisfluoroalquil-1,4-benzodiazepinona e métodos de uso das mesmas
EP3790553A4 (en) * 2018-05-06 2022-04-20 Ayala Pharmaceuticals Inc. COMPOSITIONS CONTAINING CD20 INHIBITORS AND BISFLUORAKYL-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
MX2020012281A (es) * 2018-05-15 2021-01-29 Bristol Myers Squibb Co Composiciones que comprenden compuestos de bisfluoroalquil-1,4-ben zodiacepinona y metodos de uso de las mismas.
JP2021526517A (ja) * 2018-05-24 2021-10-07 アヤラ ファーマシューティカルズ インコーポレイテッド ビスフルオロアルキル−１，４−ベンゾジアゼピノン化合物および免疫療法剤を含む組成物ならびにそれらの使用方法
EP3860562A1 (en) 2018-10-02 2021-08-11 Frequency Therapeutics, Inc. Pharmaceutical compositions comprising otic therapeutic agents and related methods
TW202103692A (zh) 2019-04-08 2021-02-01 美商頻率醫療公司 用於治療聽力損失之組合物及方法
AU2021218456A1 (en) * 2020-02-16 2022-09-22 Ayala Pharmaceuticals Inc. Methods of preparing chiral benzodiazepinone derivatives
WO2022051442A1 (en) 2020-09-03 2022-03-10 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
US20240041884A1 (en) 2020-12-07 2024-02-08 Cellestia Biotech Ag Pharmaceutical Combinations for Treating Cancer
WO2022253794A2 (en) 2021-06-02 2022-12-08 Cellestia Biotech Ag Method for treating an autoimmune and inflammatory disease
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
WO2024036097A1 (en) 2022-08-12 2024-02-15 Nuvalent, Inc. Heteroaromatic macrocyclic ether compounds and isotopologues thereof

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
US5852010A (en) 1996-04-03 1998-12-22 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CA2250203A1 (en) 1996-04-03 1997-10-09 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
EP1129355B1 (en) 1998-11-12 2005-07-20 Bristol-Myers Squibb Pharma Company Use of radioligands to screen inhibitors of amyloid-beta peptide production
WO2000038618A2 (en) 1998-12-24 2000-07-06 Du Pont Pharmaceuticals Company SUCCINOYLAMINO BENZODIAZEPINES AS INHIBITORS OF Aβ PROTEIN PRODUCTION
ATE258439T1 (de) 1999-04-30 2004-02-15 Univ Michigan Verwendung von benzodiazepinen zur behandlung von apoptose-induzierten autoimmunerkrankungen
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
CA2387493A1 (en) 1999-10-08 2001-04-19 Lorin Andrew Thompson Amino lactam sulfonamides as inhibitors of a.beta. protein production
US6756511B2 (en) 2000-01-24 2004-06-29 Merck Sharp & Dohme Limited Gamma-secretase inhibitors
WO2001060826A2 (en) * 2000-02-17 2001-08-23 Bristol-Myers Squibb Pharma Company SUCCINOYLAMINO CARBOCYCLES AND HETEROCYCLES AS INHIBITORS OF Aβ PROTEIN PRODUCTION
US6495540B2 (en) 2000-03-28 2002-12-17 Bristol - Myers Squibb Pharma Company Lactams as inhibitors of A-β protein production
AU2001251147A1 (en) 2000-03-31 2001-10-15 Dupont Pharmaceuticals Company Succinoylamino heterocycles as inhibitors of abeta protein production
BR0107532A (pt) 2000-04-03 2004-11-03 Bristol Myers Squibb Pharma Co Composto, uso do composto, método para o tratamento de disfunções neurológicas associadas com a produção de b-amilóide, método de inibição da atividade de y-secretase e composição farmacêutica
MXPA02009729A (es) 2000-04-03 2003-03-27 Bristol Myers Squibb Pharma Co Lactamas ciclicas como inhibidores de la produccion de la proteina a-beta.
GB0008710D0 (en) 2000-04-07 2000-05-31 Merck Sharp & Dohme Therapeutic compounds
AU2001257006A1 (en) 2000-04-11 2001-10-23 Du Pont Pharmaceuticals Company Substituted lactams as inhibitors of abeta 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
BR0106717A (pt) 2000-06-01 2002-04-16 Bristol Myers Squibb Pharma Co Compostos, composição farmacêutica e usos dos compostos de lactama inovadora
US7001901B2 (en) 2002-08-27 2006-02-21 Bristol-Myers Squibb Company Tetrazolylpropionamides as inhibitors of Aβ protein production
WO2004026843A1 (en) * 2002-09-20 2004-04-01 Arrow Therapeutics Limited Benzodiazepine derivatives and pharmaceutical compositions containing them
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
EA017286B1 (ru) 2007-08-14 2012-11-30 Эли Лилли Энд Компани Ингибиторы гамма-секретазы
MA33076B1 (fr) 2008-01-11 2012-03-01 Hoffmann La Roche Utilisation d'un inhibiteur de la gamma-secretase pour le traitement du 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
AU2013317923A1 (en) 2015-05-07
UY35041A (es) 2014-03-31
CN104703976B (zh) 2017-03-08
SG11201501573UA (en) 2015-05-28
US8999918B2 (en) 2015-04-07
BR112015005817A2 (pt) 2017-07-04
LT2897945T (lt) 2017-03-27
JP6165255B2 (ja) 2017-07-19
DK2897945T3 (en) 2017-03-27
WO2014047372A1 (en) 2014-03-27
SI2897945T1 (sl) 2017-03-31
PH12015500414B1 (en) 2015-04-20
PE20150622A1 (es) 2015-05-11
US20150166489A1 (en) 2015-06-18
CO7310522A2 (es) 2015-06-30
CL2015000711A1 (es) 2015-09-04
CA2885574C (en) 2021-06-08
EA201590581A1 (ru) 2015-07-30
TWI614238B (zh) 2018-02-11
US9273014B2 (en) 2016-03-01
CN104703976A (zh) 2015-06-10
CA2885574A1 (en) 2014-03-27
PT2897945T (pt) 2017-03-07
TN2015000102A1 (en) 2016-06-29
HUE032038T2 (en) 2017-09-28
PL2897945T3 (pl) 2017-06-30
EA027281B1 (ru) 2017-07-31
NZ707171A (en) 2018-01-26
HRP20170352T8 (hr) 2017-05-19
KR20150056780A (ko) 2015-05-27
JP2015530411A (ja) 2015-10-15
CY1118739T1 (el) 2017-07-12
PH12015500414A1 (en) 2015-04-20
TW201418230A (zh) 2014-05-16
MA37929A1 (fr) 2018-06-29
AU2013317923B2 (en) 2017-06-29
EP2897945B1 (en) 2016-12-21
US20140087992A1 (en) 2014-03-27
ES2617591T3 (es) 2017-06-19
KR102155588B1 (ko) 2020-09-14
BR112015005817B1 (pt) 2022-10-04
IL237782A (en) 2017-03-30
MX367474B (es) 2019-08-23
EP2897945A1 (en) 2015-07-29
RS55779B1 (sr) 2017-07-31
MX2015003033A (es) 2015-06-10
MY185233A (en) 2021-04-30
MA37929B1 (fr) 2018-09-28
HRP20170352T1 (hr) 2017-05-05

Similar Documents

Publication Publication Date Title
AR093767A1 (es) Compuestos de bis(fluoroalquil)-1,4-benzodiazepinona y profarmacos de estos
AR101815A1 (es) Compuestos y composiciones como inhibidores de quinasa
AR105388A1 (es) Ligandos de difosfina a base de benceno para alcoxicarbonilación
AR093515A1 (es) Triazolopirazinas
AR098912A1 (es) Inhibidores de syk
BR112017006253A2 (pt) novos compostos
MX2015015786A (es) Compuestos de n-(tetrazol-5-il)- y n-(triazol-5-il) arilcarboxamida sustituidos y su uso como herbicidas.
AR099177A1 (es) Determinadas (2s)-n-[(1s)-1-ciano-2-feniletil]-1,4-oxazepan-2-carboxamidas como inhibidores de dipeptidil peptidasa 1
AR094309A1 (es) Compuesto heterociclico fusionado y uso del mismo para el control de plagas
MX2014013074A (es) Compuestos de n- (tetrazol-5-il) - y n- (triazol-5-il) arilcarboxamida sustituidos y su uso como herbicidas.
AR096837A1 (es) Heterociclos tricíclicos como inhibidores de proteínas bet
AR080057A1 (es) Piridinas disustituidas como anticancerigenos
AR099400A1 (es) Compuesto heterocíclico fusionado
AR100233A1 (es) Composición de limpieza
AR098908A1 (es) Compuesto de (6s,9as)-n-bencil-6-[(4-hidroxifenil)metil]-4,7-dioxo-8-({6-[3-(piperazin-1-il)azetidin-1-il]piridin-2-il}metil)-2-(prop-2-en-1-il)-octahidro-1h-pirazino[2,1-c][1,2,4]triazina-1-carboxamida
AR097866A1 (es) Derivados de 4-azaindol
AR086829A1 (es) Compuestos heterociclicos fusionados como moduladores del canal ionico
JP2014510816A5 (es)
AR091770A1 (es) Indolcarbonitrilos moduladores selectivos de receptores androgenicos
EA201591486A1 (ru) Соединения имидазопиридина
AR090474A1 (es) Compuestos de tetrahidropirrolotiazina
AR095523A1 (es) Derivados piridin-4-ilo
AR097253A1 (es) Derivado de pirazolilpirazol sustituido y el uso del mismo como herbicida
AR099581A1 (es) Compuestos de aminocarbonilcarbamato
MA38884A1 (fr) Composé de triazolopyridine, compositions et procédés d'utilisation associés

Legal Events

Date Code Title Description
FB Suspension of granting procedure