[go: up one dir, main page]

MX2020001891A - Derivados del acido boronico. - Google Patents

Derivados del acido boronico.

Info

Publication number
MX2020001891A
MX2020001891A MX2020001891A MX2020001891A MX2020001891A MX 2020001891 A MX2020001891 A MX 2020001891A MX 2020001891 A MX2020001891 A MX 2020001891A MX 2020001891 A MX2020001891 A MX 2020001891A MX 2020001891 A MX2020001891 A MX 2020001891A
Authority
MX
Mexico
Prior art keywords
acid derivatives
boronic acid
immunoproteasome
activity
diseases
Prior art date
Application number
MX2020001891A
Other languages
English (en)
Inventor
Esdar Christina
Klein Markus
Schadt Oliver
Original Assignee
Merck Patent Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of MX2020001891A publication Critical patent/MX2020001891A/es

Links

Classifications

    • 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
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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
    • A61K31/69—Boron compounds
    • 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
    • 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
    • A61K47/02—Inorganic compounds
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • 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
    • 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
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
    • 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
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61K9/0031—Rectum, anus
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/282—Organic compounds, e.g. fats
    • A61K9/2826—Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Dermatology (AREA)
  • Inorganic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención se relaciona con derivados del ácido a-amino borónico. Estos compuestos son útiles para inhibir la actividad del inmunoproteasoma (LMP7) y para el tratamiento y/o prevención de las afecciones médicas afectadas por la actividad del inmunoproteasoma, tales como enfermedades inflamatorias y autoinmunes, enfermedades neurodegenerativas, enfermedades proliferativas y cáncer.
MX2020001891A 2017-08-24 2018-08-21 Derivados del acido boronico. MX2020001891A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP17187636 2017-08-24
PCT/EP2018/072485 WO2019038250A1 (en) 2017-08-24 2018-08-21 BORONIC ACID DERIVATIVES

Publications (1)

Publication Number Publication Date
MX2020001891A true MX2020001891A (es) 2020-03-24

Family

ID=59699569

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2020001891A MX2020001891A (es) 2017-08-24 2018-08-21 Derivados del acido boronico.

Country Status (15)

Country Link
US (2) US11274109B2 (es)
EP (1) EP3672977B1 (es)
JP (1) JP7189203B2 (es)
KR (1) KR20200040295A (es)
CN (1) CN111183142B (es)
AU (1) AU2018321118B2 (es)
CA (1) CA3073611A1 (es)
DK (1) DK3672977T3 (es)
ES (1) ES2927283T3 (es)
IL (1) IL272806B2 (es)
MX (1) MX2020001891A (es)
PL (1) PL3672977T3 (es)
PT (1) PT3672977T (es)
TW (1) TWI791595B (es)
WO (1) WO2019038250A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022073994A1 (en) 2020-10-05 2022-04-14 Merck Patent Gmbh Lmp7-selective inhibitors for the treatment of blood disorders and solid tumors
JP2024529468A (ja) * 2021-07-29 2024-08-06 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規の［（１ｒ）－２－（１－ベンゾフラン－３－イル）－１－｛［（１ｓ，２ｒ，４ｒ）－７－オキサビシクロ［２．２．１］ヘプタン－２－イル］ホルムアミド｝エチル］ボロン酸の結晶性形態、その付加物、および得るためのプロセス
WO2023061445A1 (zh) 2021-10-14 2023-04-20 首药控股(北京)股份有限公司 硼酸衍生物
WO2023232830A1 (en) 2022-06-02 2023-12-07 Merck Patent Gmbh Boronic acid adducts

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006040646A1 (en) * 2004-10-14 2006-04-20 Pfizer, Inc. Benzimidazole or indole amides as inhibitors of pin1
EP2318419B2 (en) 2008-06-17 2024-10-30 Takeda Pharmaceutical Company Limited Boronate ester compounds and pharmaceutical compositions thereof
EP2793900B1 (en) * 2011-12-22 2018-08-22 Ares Trading S.A. Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors
CA2866135A1 (en) 2012-03-02 2014-09-06 Dr. Reddy's Laboratories Limited Pharmaceutical compositions comprising boronic acid compounds
KR101782235B1 (ko) 2012-12-03 2017-09-26 에프. 호프만-라 로슈 아게 치환된 트라이아졸 붕소산 화합물
KR102333718B1 (ko) * 2013-03-15 2021-12-01 데시페라 파마슈티칼스, 엘엘씨. 항암 및 항-증식 활성을 나타내는 n-아실-n'-(피리딘-2-일) 우레아 및 유사체
AU2015327411B2 (en) 2014-10-01 2020-01-02 Merck Patent Gmbh Boronic acid derivatives
KR102457840B1 (ko) 2014-10-01 2022-10-21 메르크 파텐트 게엠베하 보론산 유도체
ES2876287T3 (es) 2014-10-01 2021-11-12 Merck Patent Gmbh Derivados del ácido borónico.
KR102450583B1 (ko) 2014-10-01 2022-10-04 메르크 파텐트 게엠베하 보론산 유도체
CN106008572B (zh) * 2016-05-23 2018-08-17 成都千禧莱医药科技有限公司 一类二肽硼酸化合物及制备方法和用途

Also Published As

Publication number Publication date
EP3672977A1 (en) 2020-07-01
IL272806A (en) 2020-04-30
BR112020003368A2 (pt) 2020-08-18
IL272806B1 (en) 2023-05-01
TWI791595B (zh) 2023-02-11
CA3073611A1 (en) 2019-02-28
PT3672977T (pt) 2022-09-23
IL272806B2 (en) 2023-09-01
JP7189203B2 (ja) 2022-12-13
US11274109B2 (en) 2022-03-15
CN111183142A (zh) 2020-05-19
US20200354382A1 (en) 2020-11-12
WO2019038250A1 (en) 2019-02-28
AU2018321118A1 (en) 2020-04-09
CN111183142B (zh) 2023-06-16
DK3672977T3 (da) 2022-09-26
TW201920208A (zh) 2019-06-01
US11858951B2 (en) 2024-01-02
AU2018321118B2 (en) 2023-06-15
JP2020531510A (ja) 2020-11-05
RU2020111001A (ru) 2021-09-24
ES2927283T3 (es) 2022-11-03
US20220153761A1 (en) 2022-05-19
KR20200040295A (ko) 2020-04-17
EP3672977B1 (en) 2022-06-22
PL3672977T3 (pl) 2022-09-26
RU2020111001A3 (es) 2022-02-28

Similar Documents

Publication Publication Date Title
PH12020550901A1 (en) Macrocyclic compounds for treating disease
CY1120862T1 (el) Παραγοντες επαγωγης αποπτωσης για τη θεραπευτικη αγωγη καρκινου και ανοσων και αυτοανοσων ασθενειων
PH12017501921A1 (en) Novel compounds
PH12016502179A1 (en) Inhibitors of lysine specific demethylase-1
PH12015502414A1 (en) Enhancer of zeste homolog 2 inhibitors
GEP20217328B (en) Bispecific molecules having immunoreactivity with pd-1 and ctla-4, and methods of use thereof
PH12015502028A1 (en) Ido inhibitors
MX2017012738A (es) Inhibidores de indolamina 2.3-dioxigenasa (ido) para el tratamiento de cancer.
MX2016002075A (es) Inhibidores de indolamina 2,3-dioxigenasa (ido).
MX2016000295A (es) Inhibidores de indoleamina 2,3-dioxigenasa (ido).
EA201691857A1 (ru) Соединения, применимые в качестве иммуномодуляторов
EA201690027A1 (ru) Ингибиторы ido
MX2023002507A (es) Inhibidores de cd73.
EA201591599A1 (ru) Ингибиторы ido
PH12018500423A1 (en) Inhibitors of ezh2
MX2020006237A (es) Compuestos para el tratamiento de enfermedades relacionadas con la expresion de dux4.
MX2021000214A (es) Derivados de acido boronico.
MX2020001891A (es) Derivados del acido boronico.
NZ761519A (en) Nlrp3 modulators
PH12018502314A1 (en) Enhancer of zeste homolog 2 inhibitors
SA521422152B1 (ar) Vanin مركبات عطرية غير متجانسة كمثبطات
PH12021550269A1 (en) Heteroaromatic compounds as vanin inhibitors
ZA202204941B (en) Cd73 inhibitors
MX2021006490A (es) Compuestos heteroaromaticos como inhibidores de vanina.
EA202091327A1 (ru) Макроциклические соединения для лечения заболеваний