AR079752A1 - Prodrogas de sales de amonio cuaternario - Google Patents

Prodrogas de sales de amonio cuaternario

Info

Publication number
AR079752A1
AR079752A1 ARP100104960A ARP100104960A AR079752A1 AR 079752 A1 AR079752 A1 AR 079752A1 AR P100104960 A ARP100104960 A AR P100104960A AR P100104960 A ARP100104960 A AR P100104960A AR 079752 A1 AR079752 A1 AR 079752A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
progenitor
tertiary
straight
Prior art date
Application number
ARP100104960A
Other languages
English (en)
Inventor
Blumberg Laura Cook
Julius F Remenar
Orn Almarsson
Original Assignee
Alkermes Inc
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 Alkermes Inc filed Critical Alkermes Inc
Publication of AR079752A1 publication Critical patent/AR079752A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • 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
    • A61K31/407—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 condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/452—Piperidinium derivatives
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/52—Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (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)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Los compuestos que constituyen las prodrogas apropiadas para usar en los métodos de la presente son sales de amonio cuaternario lábiles de drogas progenitoras que contienen aminas terciarias (o de drogas progenitoras de que contienen iminas terciarias), que se obtienen por medio de una derivatizacion con unidades de prodrogas unidas a aldehído que reducen la solubilidad de la prodroga al pH de referencia, con relacion a la droga progenitora. Las propiedades físicas, químicas y de solubilidad de estos derivados también pueden modularse mediante la seleccion del contraion X-. Los compuestos que son las prodrogas de la presente podrán usarse para tratar cualquier afeccion para cuyo tratamiento sea util una droga progenitora que contenga una amina terciaria o una droga progenitora que contenga una imina terciaria. Reivindicacion 1: Un método para la administracion sostenida de una droga madre que contiene una amina terciaria a un paciente, caracterizado porque comprende administrar un compuesto prodroga de formula (1) donde R1 es un grupo alquilo C5-24 de cadena lineal o ramificada, sustituido o no sustituido, alquenilo C5-24 de cadena lineal o ramificada, sustituido o no sustituido, alquinilo C5-24 de cadena lineal o ramificada, sustituido o no sustituido, un grupo alquilo que comprende al menos 3 átomos de carbono donde dicho grupo alquilo comprende un grupo C3-12 sustituido o no sustituido, un grupo arilo sustituido o no sustituido, o un grupo heteroarilo sustituido o no sustituido; R2 es hidrogeno, alquilo C1-6 de cadena lineal o ramificada, sustituido o no sustituido, o cicloalquilo C3-12 sustituido o no sustituido; R3, R4 y R5, junto con el átomo de nitrogeno al cual se encuentran unidos, forman una droga madre que contiene una amina terciaria o una droga madre que contiene una imina terciaria; y X- es un anion aceptable farmacéuticamente; donde luego de la administracion al paciente, la liberacion de la droga madre a partir de la prodroga es sostenida.
ARP100104960A 2010-01-07 2010-12-27 Prodrogas de sales de amonio cuaternario AR079752A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US29316310P 2010-01-07 2010-01-07
US29317110P 2010-01-07 2010-01-07
US29312410P 2010-01-07 2010-01-07
US29315310P 2010-01-07 2010-01-07

Publications (1)

Publication Number Publication Date
AR079752A1 true AR079752A1 (es) 2012-02-15

Family

ID=44277990

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100104960A AR079752A1 (es) 2010-01-07 2010-12-27 Prodrogas de sales de amonio cuaternario

Country Status (9)

Country Link
US (1) US9670200B2 (es)
EP (1) EP2521711B1 (es)
JP (2) JP6076740B2 (es)
AR (1) AR079752A1 (es)
AU (1) AU2010339689B2 (es)
CA (1) CA2798172C (es)
ES (1) ES2647361T3 (es)
TW (2) TWI568448B (es)
WO (1) WO2011084846A1 (es)

Families Citing this family (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES3031438T3 (en) * 2009-06-25 2025-07-08 Alkermes Pharma Ireland Ltd Heterocyclic compounds for the treatment of neurological and psychological disorders
WO2010151711A1 (en) 2009-06-25 2010-12-29 Alkermes, Inc. Prodrugs of nh-acidic compounds
WO2011084850A1 (en) * 2010-01-07 2011-07-14 Alkermes, Inc. Prodrugs for the treatment of schizophrenia and bipolar disease
US20110166194A1 (en) * 2010-01-07 2011-07-07 Alkermes, Inc. Asenapine Prodrugs
WO2011084848A2 (en) 2010-01-07 2011-07-14 Alkermes, Inc. Prodrugs of heteraromatic compounds
CA2798172C (en) * 2010-01-07 2017-11-21 Alkermes Pharma Ireland Limited Quaternary ammonium salt prodrugs
WO2011084849A1 (en) * 2010-01-07 2011-07-14 Alkermes, Inc. Diaryldiazepine prodrugs for the treatment of neurological and psychological disorders
ES2691671T3 (es) 2010-06-24 2018-11-28 Alkermes Pharma Ireland Limited Profármacos de compuestos NH-acídicos: derivados de éster, carbonato, carbamato y fosfonato
DK2685979T3 (da) 2011-03-18 2016-12-19 Alkermes Pharma Ireland Ltd Injicerbare farmaceutiske sammensætninger, omfattende et vand-uopløseligt, antipsykotisk sorbitanlaurat og polysorbat 20.
ES2779225T3 (es) * 2011-04-08 2020-08-14 Sphaera Pharma Pte Ltd Reactivos de merilformilo sustituido y procedimiento de uso de los mismos para modificar propiedades fisicoquímicas y/o farmacocinéticas de compuestos
EP4215512A1 (en) 2011-06-20 2023-07-26 H. Lundbeck A/S Deuterated 1-piperazino-3-phenyl indanes for treatment of schizophrenia
US9907812B2 (en) 2011-06-22 2018-03-06 Vyome Biosciences Pvt. Ltd. Conjugate-based antifungal and antibacterial prodrugs
JO3227B1 (ar) 2011-09-08 2018-03-08 Otsuka Pharma Co Ltd مشتقات بنزو ثيوفين بها استبدال ببرازين كعوامل مضادة للذهان
US8426450B1 (en) 2011-11-29 2013-04-23 Helsinn Healthcare Sa Substituted 4-phenyl pyridines having anti-emetic effect
JP5952912B2 (ja) * 2011-12-15 2016-07-13 アルカーメス ファーマ アイルランド リミテッド 二級アミン化合物のプロドラッグ
AU2013235526B2 (en) 2012-03-19 2017-11-30 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising benzyl alcohol
NZ630703A (en) 2012-03-19 2017-02-24 Alkermes Pharma Ireland Ltd Pharmaceutical compositions comprising glycerol esters
EP2827868B8 (en) 2012-03-19 2019-12-18 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising fatty acid esters
NZ748572A (en) 2012-09-19 2020-07-31 Alkermes Pharma Ireland Ltd Pharmaceutical compositions having improved storage stability
EP2712611A1 (en) 2012-09-27 2014-04-02 B. Braun Melsungen AG Stabilized aqueous compositions of neuromuscular blocking agents
EP2968320B1 (en) * 2013-03-15 2020-11-11 Intra-Cellular Therapies, Inc. Organic compounds
US9487531B2 (en) 2013-04-17 2016-11-08 BioPharma Works LLC Compounds for treatment of pain
US10072018B2 (en) * 2013-04-17 2018-09-11 Biopharma Works Compounds for treatment of pain
WO2015143145A1 (en) 2014-03-20 2015-09-24 Alkermes Pharma Ireland Limited Aripiprazole formulations having increased injection speeds
EP4119539A1 (en) * 2015-09-23 2023-01-18 XWPharma Ltd. Prodrugs of gamma-hydroxybutyric acid, compositions and uses thereof
TWI759301B (zh) 2016-05-24 2022-04-01 美商安美基公司 聚乙二醇化卡非佐米化合物
US10683387B2 (en) 2016-10-04 2020-06-16 Massachusetts Institute Of Technology Bottlebrush copolymers and uses thereof
EP3558275A1 (en) 2016-12-20 2019-10-30 LTS Lohmann Therapie-Systeme AG Transdermal therapeutic system containing asenapine
EP3558276B1 (en) 2016-12-20 2024-11-06 LTS Lohmann Therapie-Systeme AG Transdermal therapeutic system containing asenapine and polysiloxane or polyisobutylene
WO2018191477A1 (en) * 2017-04-14 2018-10-18 Kempharm, Inc. Dextrorphan prodrugs and processes for making and using them
WO2018191474A1 (en) * 2017-04-14 2018-10-18 Kempharm, Inc. Levorphanol prodrugs and processes for making and using them
US11234975B2 (en) 2017-04-14 2022-02-01 Kempharm, Inc. Levorphanol prodrugs and processes for making and using them
WO2019002204A1 (en) 2017-06-26 2019-01-03 Lts Lohmann Therapie-Systeme Ag TRANSDERMAL THERAPEUTIC SYSTEM CONTAINING ASENAPINE AND SILICONE-TYPE ACRYLIC HYBRID POLYMER
CN111263758A (zh) 2017-06-30 2020-06-09 麻省理工学院 支链的多官能大分子单体和相关聚合物及其用途
WO2019006425A1 (en) 2017-06-30 2019-01-03 Massachusetts Institute Of Technology IMAGING AGENTS OF BRUSH ARRAY STAR POLYMERS AND USES THEREOF
CN109422668B (zh) * 2017-08-25 2021-06-22 广州市恒诺康医药科技有限公司 一种长效雷沙吉兰前药及其制备方法和用途
EP3710063A1 (en) 2017-11-16 2020-09-23 Amgen Inc. Stable compositions of pegylated carfilzomib compounds
WO2019173230A1 (en) 2018-03-05 2019-09-12 Alkermes Pharma Ireland Limited Aripiprazole dosing strategy
EP3810099A1 (en) 2018-06-20 2021-04-28 LTS Lohmann Therapie-Systeme AG Transdermal therapeutic system containing asenapine
ES3010131T3 (en) 2018-06-20 2025-04-01 Lts Lohmann Therapie Systeme Ag Transdermal therapeutic system containing asenapine
US10988491B2 (en) 2018-08-17 2021-04-27 Massachusetts Institute Of Technology Degradable polymers of a cyclic silyl ether and uses thereof
US12030868B2 (en) 2018-10-13 2024-07-09 Pfizer Ireland Pharmaceuticals Prodrugs of CGRP antagonists
US11535600B2 (en) 2018-12-03 2022-12-27 H. Lundbeck A/S Prodrugs of 4-((1R,3S)-6-chloro-3-phenyl-2,3-dihydro-1H-inden-1-yl)-1,2,2-trimethylpiperazine and 4-((1R,3S)-6-chloro-3-(phenyl-d5)-2,3-dihydro-1H-inden-1-yl)-2,2-dimethyl-1-(methyl-d3)piperazine
EP3966212A1 (en) * 2019-05-07 2022-03-16 Bristol-Myers Squibb Company Prodrug compounds
WO2021076821A2 (en) * 2019-10-16 2021-04-22 Massachusetts Institute Of Technology Brush prodrugs and uses thereof
JP7483890B2 (ja) 2019-12-20 2024-05-15 エックスダブリューファーマ リミテッド ４－バリルオキシ酪酸の合成方法
WO2021141662A1 (en) 2020-01-10 2021-07-15 Massachusetts Institute Of Technology Proteolysis targeting chimeric molecules (protacs) with functional handles and uses thereof
AU2021293941B2 (en) 2020-06-18 2024-03-28 XWPharma Ltd. Pharmaceutical granulations of water-soluble active pharmaceutical ingredients
US11304906B2 (en) 2020-06-18 2022-04-19 XWPharma Ltd. Controlled release granulations of water-soluble active pharmaceutical ingredients
WO2022020621A1 (en) 2020-07-24 2022-01-27 XWPharma Ltd. Pharmaceutical compositions and pharmacokinetics of a gamma-hydroxybutyric acid derivative
US11395801B2 (en) 2020-10-05 2022-07-26 XWPharma Ltd. Modified release compositions of a gamma-hydroxybutyric acid derivative
WO2022183196A1 (en) 2021-02-24 2022-09-01 Oakwood Laboratories, Llc Microsphere formulations comprising lurasidone and methods for making and using the same
CN117098533A (zh) 2021-03-19 2023-11-21 凯瑞康宁公司 γ-羟基丁酸衍生物的组合释放型制剂的药物动力学
EP4452933A1 (en) 2021-12-20 2024-10-30 Massachusetts Institute of Technology Biomolecule-polymer-pharmaceutical agent conjugates for delivering the pharmaceutical agent
WO2024147146A1 (en) 2023-01-03 2024-07-11 Rajaram Samant Novel quaternary ammonium compounds (qacs) and process for preparation thereof
US12269818B2 (en) 2023-04-24 2025-04-08 Terran Biosciences Inc. Analogs of xanomeline

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4727151A (en) 1974-06-24 1988-02-23 Interx Research Corporation Labile quaternary ammonium salts as prodrugs
US3998815A (en) 1974-06-24 1976-12-21 Interx Research Corporation 1-hydrocarbonoyloxymethyl-3-carbamoyl or 3-carboethoxy-pyridinium salts
US4264765A (en) * 1980-02-20 1981-04-28 Abbott Laboratories Salts of erythromycin A esters
US4804663A (en) 1985-03-27 1989-02-14 Janssen Pharmaceutica N.V. 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
GB8513754D0 (en) 1985-05-31 1985-07-03 Jones T R Anti-cancer quinazoline derivatives
GB8607683D0 (en) 1986-03-27 1986-04-30 Ici Plc Anti-tumor agents
US5158952A (en) 1988-11-07 1992-10-27 Janssen Pharmaceutica N.V. 3-[2-[4-(6-fluoro-1,2-benzisoxozol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9 tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a]pyrimidin-4-one, compositions and method of use
US5364866A (en) 1989-05-19 1994-11-15 Hoechst-Roussel Pharmaceuticals, Inc. Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analetics
TW226016B (es) 1991-12-30 1994-07-01 Sterling Winthrop Inc
US5312925A (en) 1992-09-01 1994-05-17 Pfizer Inc. Monohydrate of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one-hydrochloride
US5497763A (en) 1993-05-21 1996-03-12 Aradigm Corporation Disposable package for intrapulmonary delivery of aerosolized formulations
US5508269A (en) 1994-10-19 1996-04-16 Pathogenesis Corporation Aminoglycoside formulation for aerosolization
US6083922A (en) 1996-04-02 2000-07-04 Pathogenesis, Corp. Method and a tobramycin aerosol formulation for treatment prevention and containment of tuberculosis
US5767068A (en) 1997-02-13 1998-06-16 Pathogenesis Corporation Pure biologically active colistin, its components and a colistin formulation for treatment of pulmonary infections
US6180095B1 (en) 1997-12-17 2001-01-30 Enzon, Inc. Polymeric prodrugs of amino- and hydroxyl-containing bioactive agents
KR20010033811A (ko) 1997-12-31 2001-04-25 토마스 안 빅토리아 2차 및 3차 아민을 함유하는 약제의 물에 용해가능한프로드럭 및 그것의 제조방법
ATE346841T1 (de) 1998-08-26 2006-12-15 Aventis Pharma Ltd Azabicyclo-verbindungen welche die inhibition der zell adhesion modulieren
ATE342959T1 (de) * 2000-07-14 2006-11-15 Transform Pharmaceuticals Inc System und verfahren zum optimieren des gewebebarrieretransfers von verbindungen
US20060293217A1 (en) * 2001-03-19 2006-12-28 Praecis Pharmaceuticals, Inc. Pharmaceutical formulations for sustained release
WO2002074247A2 (en) * 2001-03-19 2002-09-26 Praecis Pharmaceuticals Incorporated Pharmaceutical formulations for sustained release
WO2005063206A1 (en) * 2003-12-23 2005-07-14 Alza Corporation Methods and dosage forms for increasing solubility of drug compositions for controlled delivery
CN1917882A (zh) 2004-02-13 2007-02-21 辉瑞产品公司 非典型抗精神病药物与促肾上腺皮质激素释放因子拮抗剂的治疗剂组合
EP1787648A4 (en) 2004-09-03 2010-06-23 Dainippon Sumitomo Pharma Co MEDICAL COMPOSITION FOR PERCUTANEOUS PEROSPIRON MANAGEMENT
KR20070084123A (ko) 2004-10-15 2007-08-24 엔.브이.오가논 양극성 장애 및 관련 증상의 치료
ES2390353T3 (es) 2005-06-13 2012-11-12 Dainippon Sumitomo Pharma Co., Ltd. Preparación de disolución
US20070154546A1 (en) * 2005-12-30 2007-07-05 Zhang Jack Y Sustained release pharmaceutical compositions
CL2007002684A1 (es) 2006-09-15 2008-06-27 Astrazeneca Ab Targacept Inc Combinacion que comprende un antipsicotico y (2s)-(4e)-n-metil-5-[3-(5-isopropoxipiridin)il]-4-penten-2-amina; composicion farmaceutica que la comprende; kit farmaceutico; y uso para tratar perjuicio cognitivo y/o trastorno psicoticos.
CN101677971A (zh) * 2007-03-19 2010-03-24 阿卡蒂亚药品公司 5-ht2a反向激动剂和拮抗剂与抗精神病药物的组合
WO2009111540A1 (en) 2008-03-04 2009-09-11 Medivation Neurology, Inc. Methods for preparing pyridylethyl-substituted carbolines
ES3031438T3 (en) 2009-06-25 2025-07-08 Alkermes Pharma Ireland Ltd Heterocyclic compounds for the treatment of neurological and psychological disorders
WO2010151711A1 (en) 2009-06-25 2010-12-29 Alkermes, Inc. Prodrugs of nh-acidic compounds
WO2011084850A1 (en) * 2010-01-07 2011-07-14 Alkermes, Inc. Prodrugs for the treatment of schizophrenia and bipolar disease
WO2011084849A1 (en) * 2010-01-07 2011-07-14 Alkermes, Inc. Diaryldiazepine prodrugs for the treatment of neurological and psychological disorders
WO2011084848A2 (en) 2010-01-07 2011-07-14 Alkermes, Inc. Prodrugs of heteraromatic compounds
CA2798172C (en) * 2010-01-07 2017-11-21 Alkermes Pharma Ireland Limited Quaternary ammonium salt prodrugs
US20110166194A1 (en) 2010-01-07 2011-07-07 Alkermes, Inc. Asenapine Prodrugs
ES2691671T3 (es) 2010-06-24 2018-11-28 Alkermes Pharma Ireland Limited Profármacos de compuestos NH-acídicos: derivados de éster, carbonato, carbamato y fosfonato

Also Published As

Publication number Publication date
AU2010339689A1 (en) 2012-07-19
US20110178068A1 (en) 2011-07-21
JP2015155477A (ja) 2015-08-27
EP2521711A1 (en) 2012-11-14
US9670200B2 (en) 2017-06-06
JP6076740B2 (ja) 2017-02-08
TWI568448B (zh) 2017-02-01
CA2798172C (en) 2017-11-21
TW201618810A (zh) 2016-06-01
JP2013516465A (ja) 2013-05-13
EP2521711B1 (en) 2017-08-16
CA2798172A1 (en) 2011-07-14
TW201125585A (en) 2011-08-01
ES2647361T3 (es) 2017-12-21
WO2011084846A1 (en) 2011-07-14
TWI623325B (zh) 2018-05-11
AU2010339689B2 (en) 2015-02-19
EP2521711A4 (en) 2013-06-19

Similar Documents

Publication Publication Date Title
AR079752A1 (es) Prodrogas de sales de amonio cuaternario
CY1124882T1 (el) Αναλογα 1,4-διϋποκατεστημενης πυριδαζινης και μεθοδοι για την θεραπευτικη αγωγη καταστασεων συναφων με ανεπαρκεια smn
AR082499A1 (es) Compuestos utiles para trastornos del sistema nervioso, inflamatorios, estomacales y como analgesicos
CY1119642T1 (el) Csf-1r αναστολεις για την θεραπεια ογκων του εγκεφαλου
EA201490445A1 (ru) Циклопропанаминовое соединение
CY1118842T1 (el) Αναισθητικες ενωσεις και σχετιζομενες μεθοδοι χρησεις
BR112015015812A2 (pt) derivados de pirimidina fundidos a pirido ou pirrolo como inibidores de autotaxina para tratamento de dor
EA201490569A1 (ru) Полиморфная форма гидрохлорида придопидина
EA201390723A1 (ru) Аминозамещенные производные бисфенилпентановой кислоты в качестве ингибиторов nep
ECSP15012804A (es) Alcoxipirazoles como activadores de guanilato ciclasa soluble
AR078121A1 (es) Compuestos de sales de amonio cuaternario y composiciones farmaceuticas
AR061584A1 (es) Uso de 2-aminotetralinas sustituidas para la fabricacion de un medicamento para la prevencion, alivio y/o tratamiento de diversos tipos de dolor
HRP20191857T1 (hr) Inhibitori replikacije virusa
EA201370184A1 (ru) Гетероарильные производные
MX2016008665A (es) Derivado basado en 1,2-naftoquinona y metodo de preparacion del mismo.
NZ603465A (en) Antimalarial drug which contains 5-aminolevulinic acid or derivative thereof as active ingredient
CR20150419A (es) Derivados sustituidos del ácido bisfenil butanóico fosfónico como inhibidores de la nep
CO6231027A2 (es) Metodos e intermediarios para preparar compuestos de lactama lactoma de 8 atomos de carbono activos como inhibidores de renina
JO3263B1 (ar) مشتق إندان سلفاميد جديد
MA38854B1 (fr) Dérivés amides utilisés en tant qu'antagonistes des récepteurs de l'acide lysophosphatidique
AR072880A1 (es) Derivados nitrogenados de la pancratistatina
RU2016116036A (ru) Производное циклического амина и его фармацевтическое применение
JP2018508537A5 (es)
CO6680697A2 (es) Compuestos heterociclicos para tratar o prevenir transtornos causado por neurotransmisión reducida de serotonina, norepinefrina o dopamina
BR112015002921A2 (pt) derivados de ariletinila.

Legal Events

Date Code Title Description
FC Refusal