DK2155681T3 - Fremgangsmåde til fremstilling af sammensætninger til modulering af kinasekaskade og fremgangsmåder til anvendelse deraf - Google Patents

Fremgangsmåde til fremstilling af sammensætninger til modulering af kinasekaskade og fremgangsmåder til anvendelse deraf Download PDF

Info

Publication number
DK2155681T3
DK2155681T3 DK08754559.6T DK08754559T DK2155681T3 DK 2155681 T3 DK2155681 T3 DK 2155681T3 DK 08754559 T DK08754559 T DK 08754559T DK 2155681 T3 DK2155681 T3 DK 2155681T3
Authority
DK
Denmark
Prior art keywords
phenyl
pyridin
morpholinoethoxy
compound
cancer
Prior art date
Application number
DK08754559.6T
Other languages
English (en)
Inventor
Daniel Coughlin
Jeremy A Cody
Jonathan Gale
David G Hangauer Jr
Debasis Patra
Grant J Palmer
Jonathon Salsbury
Paul K Isbester
Original Assignee
Athenex 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39688868&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DK2155681(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US12/005,792 external-priority patent/US7851470B2/en
Application filed by Athenex Inc filed Critical Athenex Inc
Application granted granted Critical
Publication of DK2155681T3 publication Critical patent/DK2155681T3/da

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (11)

1. Sammensætning, der omfatter 2-(5-(4-(2-morpholinethoxy)phenyl)pyridin-2-yl)-V-benzylacetamid- (KX2-391) mesylatsalt, hvor KX2-391-mesylatsaltet har en urenhed, der er større end 98,0 %, 99,0 %, 99,5 %, 99,6 % eller 99,7% bestemt ved HPLC.
2. Sammensætning ifølge krav 1, hvor sammensætningen indeholder mindre end 2 % af en urenhed udvalgt fra ethylchlorid, ethanol, ethylacetat, heptan, anisol, palladium og kombinationer deraf.
3. Sammensætning ifølge krav 1 eller 2, der endvidere omfatter en farmaceutisk acceptabel bærer eller excipiens.
4. Fremgangsmåde til fremstilling af 2-(5-(4-(2-morpholinethoxy)phenyl)pyridin-2-yl)-V-benzylacetamidmesylat, hvilken fremgangsmåde omfatter følgende trin: etablering af kontakt mellem 2-(5-(4-(2-morpholinethoxy)phenyl)pyridin-2-yl)-A-benzylacetamid og methansulfonsyre for at opnå 2-(5-(4-(2-morpholinethoxy)phenyl)pyridin-2-yl)- A-benzy 1 acetam idmesylat.
5. Fremgangsmåde ifølge krav 4, der omfatter følgende trin: (1) omsætning af 4-(2-chlorethyl)morpholin med 4-bromphenol for at opnå 4-(2-(4-bromphenoxy)ethyl)morpholin; (2) kobling af 4-(2-(4-bromphenoxy)ethyl)morpholin med 6-fluorpyridin-3-yl-3-borsyre for at opnå 4-(2-(4-(6-fluorpyridin-3-yl)phenoxy)ethyl)morpholin; (3) omsætning af 4-(2-(4-(6-fluorpyridin-3-yl)phenoxy)ethyl)morpholin med acetonitril for at opnå 2-(5-(4-(2-morpholinethoxy)phenyl)pyridin-2-yl)acetonitril; (4) omdannelse af 2-(5-(4-(2-morpholinethoxy)phenyl)pyridin-2-yl)acetonitril til methyl 2-(5-(4-(2-morpholinethoxy)phenyl)pyridin-2-yl)acetat; (5) omsætning af methyl 2-(5-(4-(2-morpholinethoxy)phenyl)pyridin-2-yl)acetat med benzylamin for at opnå 2-(5-(4-(2-morpholinethoxy)phenyl)pyridin-2-yl)-A-benzylacetamid og (6) etablering af kontakt mellem 2-(5-(4-(2-morpholinethoxy)phenyl)pyridin-2-yl)-A -benzylacetamid og methansulfonsyre for at opnå 2-(5-(4-(2-morpholinethoxy)phenyl)pyridin-2-yl)-A-benzylacetamidmesylat.
6. Sammensætning ifølge et hvilket som helst af kravene 1-3 til anvendelse i behandlingen af en sygdom eller forstyrrelse udvalgt fra celleproliferationsforstyrrelser, hyperproliferative forstyrrelser, cancere, præcancere, osteoporose, kardiovaskulære forstyrrelser, immunsystemdysfunktion, type Π-diabetes, fedme, hørenedsættelse, apopleksi, oftalmisk sygdom, aterosklerose, neuropatisk smerte, hepatitis B, autoimmun sygdom og transplantatafvisning.
7. Sammensætning til anvendelse ifølge krav 6, hvor canceren er brystcancer, ovariecancer, hjemecancer, levercancer, pancreascancer, coloncancer, lungecancer eller prostatacancer.
8. Sammensætning til anvendelse ifølge krav 6, hvor canceren er malign melanom-hudcancer, ikke-melanom-hudcancer, hæmatologisk tumor, hæmatologisk malignitet, leukæmi hos børn, lymfom, multipelt myelom, Hodgkins sygdom, lymfom af lymfocytisk oprindelse, lymfom af kutan oprindelse, akut leukæmi, kronisk leukæmi, lymfoblastisk leukæmi, akut myelocytisk leukæmi, kronisk myelocytisk leukæmi, plasmacelleneoplasme, lymfoid neoplasme eller en cancer forbundet med AIDS.
9. Sammensætning til anvendelse ifølge krav 6, hvor den oftalmiske sygdom er makuladedegeneration, retinopati eller makulaødem.
10. Sammensætning til anvendelse ifølge krav 6, hvor den autoimmune sygdom er rheumatoid arthritis, multipel sklerose eller lupus.
11. Sammensætning til anvendelse ifølge et hvilket som helst af kravene 6-10, der er formuleret til oral eller topisk administration.
DK08754559.6T 2007-05-17 2008-05-19 Fremgangsmåde til fremstilling af sammensætninger til modulering af kinasekaskade og fremgangsmåder til anvendelse deraf DK2155681T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US93075807P 2007-05-17 2007-05-17
US12/005,792 US7851470B2 (en) 2006-12-28 2007-12-28 Composition and methods for modulating a kinase cascade
PCT/US2008/006419 WO2008144045A1 (en) 2007-05-17 2008-05-19 Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof

Publications (1)

Publication Number Publication Date
DK2155681T3 true DK2155681T3 (da) 2018-08-06

Family

ID=39688868

Family Applications (1)

Application Number Title Priority Date Filing Date
DK08754559.6T DK2155681T3 (da) 2007-05-17 2008-05-19 Fremgangsmåde til fremstilling af sammensætninger til modulering af kinasekaskade og fremgangsmåder til anvendelse deraf

Country Status (8)

Country Link
EP (1) EP2155681B1 (da)
JP (3) JP5679811B2 (da)
CN (1) CN101687798B (da)
AU (1) AU2008254500B2 (da)
CA (1) CA2686267C (da)
DK (1) DK2155681T3 (da)
ES (1) ES2682108T3 (da)
WO (1) WO2008144045A1 (da)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI457336B (zh) * 2006-12-28 2014-10-21 Kinex Pharmaceuticals Llc 調節激酶級聯之組成物及方法
EP2217229B1 (en) * 2007-10-20 2020-10-14 Athenex, Inc. Pharmaceutical compositions for modulating a kinase cascade and methods of use thereof
WO2011129936A2 (en) 2010-04-16 2011-10-20 Kinex Pharmaceuticals, Llc Compositions and methods for the prevention and treatment of cancer
CA2883144C (en) 2012-08-30 2023-01-17 Kinex Pharmaceuticals, Llc N-(3-fluorobenzyl)-2-(5-(4-morpholinophenyl)pyridin-2-yl) acetamide as protein|tyrosine kinase modulators
ES2928593T3 (es) * 2015-01-19 2022-11-21 Univ Keio Agentes terapéuticos para el deterioro auditivo del oído interno
CN106902358B (zh) * 2015-12-21 2020-07-10 广州市香雪制药股份有限公司 口服制剂及其制备方法
FI3592355T3 (fi) 2017-03-10 2026-02-13 Atnx Spv Llc KX2-391/KX-01 käytettäväksi aktiinisen keratoosin hoidossa
CN113354575B (zh) * 2021-06-07 2022-09-27 河南应用技术职业学院 一种特班布林的合成方法
CN113499761B (zh) * 2021-06-15 2022-03-15 广东省农业科学院农业生物基因研究中心 一种固定化金属离子亲和色谱填料、色谱柱及其制备方法
IL314266A (en) * 2022-01-14 2024-09-01 Wuhan Humanwell Innovative Drug Res And Development Center Limited Company A diaryl compound as a dual-target tubulin/SRC inhibitor
CN115073362A (zh) * 2022-08-04 2022-09-20 重庆迈德凯医药有限公司 一种替尼布林的合成方法
WO2026022219A1 (en) 2024-07-24 2026-01-29 Almirall, S.A. Injectable formulations comprising tirbanibulin

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE59108246D1 (de) * 1990-07-09 1996-11-07 Jenapharm Gmbh UNGESÄTTIGTE 15-DEHYDRO-17alpha-CYANOMETHYL-17beta- HYDROXYSTEROIDE
DE4236103A1 (de) * 1992-10-26 1994-04-28 Hoechst Ag Verfahren zur Kreuzkupplung von aromatischen Boronsäuren mit aromatischen Halogenverbindungen oder Perfluoralkylsulfonaten
ATE348829T1 (de) * 2001-02-06 2007-01-15 Pfizer Prod Inc Pharmazeutische zusammensetzungen zur behandlung von störungen des zns oder anderen erkrankungen
ES2382068T3 (es) * 2004-12-28 2012-06-05 Kinex Pharmaceuticals, Llc Composiciones y métodos para tratar trastornos de proliferación celular
BRPI0609309A2 (pt) * 2005-04-14 2010-03-09 Novartis Vaccines & Diagnostic 2-amino-quinazolin-5-onas como inibidores hsp90 com utilidade no tratamento de doenças proliferativas

Also Published As

Publication number Publication date
JP6329871B2 (ja) 2018-05-23
EP2155681A1 (en) 2010-02-24
JP2015028068A (ja) 2015-02-12
CN101687798A (zh) 2010-03-31
CA2686267A1 (en) 2008-11-27
JP2010527361A (ja) 2010-08-12
AU2008254500A1 (en) 2008-11-27
ES2682108T3 (es) 2018-09-18
JP2017193587A (ja) 2017-10-26
EP2155681B1 (en) 2018-05-02
CA2686267C (en) 2015-10-06
AU2008254500B2 (en) 2014-01-23
WO2008144045A1 (en) 2008-11-27
JP5679811B2 (ja) 2015-03-04
CN101687798B (zh) 2012-08-15

Similar Documents

Publication Publication Date Title
DK2114934T3 (da) Sammensætning og fremgangsmåder til modulering af en kinasekaskade
US8293739B2 (en) Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof
US10323001B2 (en) Compositions for modulating a kinase cascade and methods of use thereof
DK2155681T3 (da) Fremgangsmåde til fremstilling af sammensætninger til modulering af kinasekaskade og fremgangsmåder til anvendelse deraf
US20240343691A1 (en) Compositions for modulating a kinase cascade and methods of use thereof
AU2014202221B2 (en) Process for the Preparation of Compositions for Modulating a Kinase Cascade and Methods of Use Thereof
AU2014200559B2 (en) Composition and Methods for Modulating a Kinase Cascade
HK1141530A (en) Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof
HK1141530B (en) Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof
HK1136570B (en) Composition and methods for modulating a kinase cascade