AR111252A1 - Compuestos de isoxazol carboxamida y usos de los mismos - Google Patents

Compuestos de isoxazol carboxamida y usos de los mismos

Info

Publication number
AR111252A1
AR111252A1 ARP180100694A ARP180100694A AR111252A1 AR 111252 A1 AR111252 A1 AR 111252A1 AR P180100694 A ARP180100694 A AR P180100694A AR P180100694 A ARP180100694 A AR P180100694A AR 111252 A1 AR111252 A1 AR 111252A1
Authority
AR
Argentina
Prior art keywords
alkyl
independently selected
optionally substituted
cycloalkyl
alkylene
Prior art date
Application number
ARP180100694A
Other languages
English (en)
Inventor
Rohan Eric John Beckwith
Hua Jiang
Ce Wang
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR111252A1 publication Critical patent/AR111252A1/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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, caracterizado porque: R¹ se selecciona entre fenilo, tienilo y furanilo, que son cada uno independientemente opcionalmente sustituidos por 1 - 2 F; L es alquileno C₅₋₆ opcionalmente sustituido con 1 - 4 sustituyentes seleccionados independientemente de alquilo C₁₋₆ y halógeno, en donde, opcionalmente, un sustituyente de alquilo C₁₋₆ se toma junto con los átomos de carbono a los que esta unido para formar un anillo de cicloalquilo de 3 miembros; R² y R³ se toman junto con el átomo de nitrógeno al que están unidos para formar un heterociclo de 4 a 10 miembros que comprende átomos de carbono y 1 - 3 heteroátomos seleccionados independientemente entre N y O, que está opcionalmente sustituido con 1 - 4 R⁴; cada R⁴ se selecciona independientemente a partir de alquilo C₁₋₆, cicloalquilo C₃₋₈, halógeno, (alquileno C₀₋₃)-CN, haloalquilo C₁₋₆, haloalcoxilo C₁₋₆, (alquileno C₀₋₆)-OR⁵, (=O), NH(C=O)R⁵, NH(C=O)OR⁷, NH(C=O)N(R⁵)₂, (C=O)N(R⁷)₂, (C=O)R⁵, (C=O)O(alquilo C₁₋₆), (C=O)O(cicloalquilo C₃₋₈), S(=O)₂R⁵, S(=O)₂N(R⁷)₂, NHS(=O)₂R⁵, fenilo opcionalmente sustituido por 1 - 3 R⁶ y heteroarilo de 5- a 6-miembros que comprende átomos de carbono y 1 - 3 heteroátomos seleccionados independientemente a partir de N, O y S opcionalmente sustituido por 1 - 3 R⁶; cada R⁵ se selecciona independientemente a partir de H, alquilo C₁₋₆ y cicloalquilo C₃₋₈; cada R⁶ se selecciona independientemente a partir de alquilo C₁₋₆, cicloalquilo C₃₋₈, halógeno, CN, haloalquilo C₁₋₆, haloalcoxilo C₁₋₆, OR⁵, N(R⁵)₂, NH(C=O)R⁵, (C=O)N(R⁵)₂, (C=O)R⁵, (C=O)OR⁵, S(=O)₂R⁵ y S(=O)₂N(R⁵)₂; y cada R⁷ se selecciona independientemente a partir de H, alquilo C₁₋₆, cicloalquilo C₃₋₈ opcionalmente sustituido por 1 - 2 OR⁵, (alquileno C₀₋₃)-CN y (alquileno C₀₋₃)-OR⁵.
ARP180100694A 2017-03-24 2018-03-23 Compuestos de isoxazol carboxamida y usos de los mismos AR111252A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2017078060 2017-03-24

Publications (1)

Publication Number Publication Date
AR111252A1 true AR111252A1 (es) 2019-06-19

Family

ID=61868561

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP180100694A AR111252A1 (es) 2017-03-24 2018-03-23 Compuestos de isoxazol carboxamida y usos de los mismos

Country Status (15)

Country Link
US (2) US20180271837A1 (es)
EP (1) EP3601276A1 (es)
JP (1) JP2020511486A (es)
KR (1) KR20190133703A (es)
CN (1) CN110461835A (es)
AR (1) AR111252A1 (es)
AU (1) AU2018237987B2 (es)
BR (1) BR112019019680A2 (es)
CA (1) CA3057423A1 (es)
EA (1) EA201992233A1 (es)
MX (1) MX2019011261A (es)
RU (1) RU2019133281A (es)
TW (1) TW201838989A (es)
UY (1) UY37641A (es)
WO (1) WO2018172997A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3743057A4 (en) 2018-01-26 2021-11-17 Massachusetts Eye & Ear Infirmary TREATMENT OF HEARING LOSS
JOP20210053A1 (ar) * 2018-09-21 2021-03-21 Novartis Ag مركبات أيزوكسازول كربوكساميد واستخداماتها
US20220192984A1 (en) 2018-10-02 2022-06-23 Frequency Therapeutics, Inc. Pharmaceutical compositions comprising otic therapeutic agents and related methods
MX2021012258A (es) 2019-04-08 2022-01-04 Frequency Therapeutics Inc Combinacion de chir99021 y acido valproico para tratar la perdida auditiva.

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1295799A (en) * 1918-06-14 1919-02-25 Samuel Gordon Sanborn Rotary wrench.
US5421818A (en) 1993-10-18 1995-06-06 Inner Ear Medical Delivery Systems, Inc. Multi-functional inner ear treatment and diagnostic system
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
US8870826B2 (en) 2004-05-24 2014-10-28 Auris Medical Llc Combined otic aspirator and medication dispenser
AU2009212135B2 (en) * 2008-02-07 2014-08-21 Massachusetts Eye & Ear Infirmary Compounds that enhance Atoh-1 expression
WO2014210159A1 (en) * 2013-06-26 2014-12-31 Proteostasis Therapeutics, Inc. Methods of modulating cftr activity
AU2015311816B2 (en) * 2014-09-03 2019-04-04 Massachusetts Institute Of Technology Compositions, systems, and methods for generating inner ear hair cells for treatment of hearing loss
WO2016054560A1 (en) * 2014-10-02 2016-04-07 Flatley Discovery Lab Isoxazole compounds and methods for the treatment of cystic fibrosis
AR105080A1 (es) * 2015-07-07 2017-09-06 Lilly Co Eli Compuestos inhibidores de la señalización de la vía de notch

Also Published As

Publication number Publication date
CA3057423A1 (en) 2018-09-27
US20180271837A1 (en) 2018-09-27
EP3601276A1 (en) 2020-02-05
US20220117945A1 (en) 2022-04-21
JP2020511486A (ja) 2020-04-16
KR20190133703A (ko) 2019-12-03
AU2018237987B2 (en) 2021-01-21
AU2018237987A1 (en) 2019-10-03
EA201992233A1 (ru) 2020-02-21
MX2019011261A (es) 2019-10-30
RU2019133281A (ru) 2021-04-26
BR112019019680A2 (pt) 2020-04-14
CN110461835A (zh) 2019-11-15
TW201838989A (zh) 2018-11-01
RU2019133281A3 (es) 2021-07-21
WO2018172997A1 (en) 2018-09-27
UY37641A (es) 2018-10-31

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