HUE026059T2 - N-[5-[4-(5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oxazol-2-il)-1H-indazol-6-il]-2-(metiloxi)-3-piridinil]metánszulfonamid polimorfjai és sói - Google Patents

N-[5-[4-(5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oxazol-2-il)-1H-indazol-6-il]-2-(metiloxi)-3-piridinil]metánszulfonamid polimorfjai és sói Download PDF

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Publication number
HUE026059T2
HUE026059T2 HUE11755311A HUE11755311A HUE026059T2 HU E026059 T2 HUE026059 T2 HU E026059T2 HU E11755311 A HUE11755311 A HU E11755311A HU E11755311 A HUE11755311 A HU E11755311A HU E026059 T2 HUE026059 T2 HU E026059T2
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HU
Hungary
Prior art keywords
polymorph
salt
methyl
xrpd
dimethyl
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HUE11755311A
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English (en)
Inventor
Julie Nicole Hamblin
Paul Spencer Jones
Suzanne Elaine Keeling
Joelle Le
Charlotte Jane Mitchell
Nigel James Parr
Robert David Willacy
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Glaxosmithkline Ip Dev Ltd
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Publication of HUE026059T2 publication Critical patent/HUE026059T2/hu

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (5)

  1. Szabadalmi Igátypntok 1. ^^2^,*5’i-2.6-dimeíí3-^-mö3í¥íí:!3rí;MÍí^eít|}: -í:>3-i>xS^0;N2~5l)-? //-íTída^í:-!@-ií|-2^metíí»3íií>-3>'pír:5<l|r!l!lfaeláesz;üií<n^raid polimorf a (II ίφ$&amp;%. -üEzal jetifemszvé, hogy Ρ..2.±0,|-β&amp;1 lévó osöosoí (22&amp;) tamlínazo XRPD Mintazmot biztosa
  2. 2. Az 1, sgényponi szar-mti puli morf. azzal jmtemBzve, hogy alapystóea az I. táblázat szerint meghatározott óshosökat tartalmazó XRPD mimazaíöí biztosit: L tábiázaí
  3. 3. Az I, vagy 2. igósy|Xmt szm-jnb polimorf azzal jelfeotezw, hogy :aZ: ^ áfával alspvatöett megegyezd XRPD miatázato? biztosi!. 4#iP^4-{5-Hl2Ä,6.<?)-2>6-dimetiU.morIb{iftinmefil)-K3-owr>IO-il)-l^M^6*{n-2*<«,oet}bx^ 3-pirÂfîJmetànszmibnainid polimorfja <01. formád, azzal jolleínezvo, hogy --vö {· — tartalmazó XRPD mimázatot biztosít. ,%;M ?- lgéoyp)í!t: szertftó; polimorf, azzal jeltemazg«, hogy # * táblázat ^erim megháíáröZOíl sysksofeat tartalmazó XRPD mintázatot biztos0: 2. táblázat
    6. A 4.. -vagy 5. igénypont szetmti. polimorf azzal jellemezve, hogy a. 2'. ábrával: alapvetően megegyező XRPD: mlötázatoí biztosit, ?. ^45'|4-í5--(i{2/c6Áá-0.6-<i:!me(:ib4'níör:föli:8Í!:jrset:il j-I J~a>eaZ9;Í-24l)-:l/f-i:sd3Zöl-b-!lj-2-(S5elí:löí;í>-^g>?rldmiî]î««lâr!S/«ironamîd polimorffá <IV, forma), azzal jellemezve, bogy köritlbdöl 5,8-0¾¾ levő tsfai (°2S)·tartalmazó XRPD mintázatot biztosit 8. A 7. igénypont szerinti pslîmofC azzal jellemezve, bogy alapvetően a 3. táblázat szériái megbatározott csúcsokat tartalmazó XRPD mintázatot biztosit: 3. táblázat
    %A 7, vagy 8. igém pont szerinti polimorf azzal jellemezve, begy a 3;. ábrával alapvetően megegyező XRPD mintázatot biztosit. |Ö. 5-[ 4^(3 - í 6S>- 2,6-d í metíl --4 -r« orfe Iî ώ iä ί I ί | -1,3 -oíí<3 ^:oí -Æ * ä í > - 5 //-^áxsil-fö-íll-S-ímeíiloxií)- 3^)irtdini]jrasÉiíSí«JÉffiáSí:id soja, amely ä következő so: nátrium* tozilat, maieát>: bemipamoáb berni·· nálisliodis;mf#nát,; ntóídíilébszulfonáí, feeml-feileSildisztdlosak Smáíiábn^szóllönát |>tapszijit|s. kmicfeßamät. hemkzeóakáí, keßtjriJeszöidlakFdlk: ki.öyö^ÄSszetl: készítmény. amely táttálotazzíi az |*tfi igénypontok bármelyike ,áM rá^Asp polimorfot vagy sót# egy: vagy több gyógyszerészeti leg eílögslbató segédanyagot.
  4. 12. Az t~ i 0. igénypontok bármelyike altat megbatározott polimorf vagy só gyógyászati terápiában történő alkalmazásra. 13:, Az. 1-1:0:. Igénypontok, bármelyike által megbatározott pofeorf vagy só: nem megfelelő; PB-kináz aktivitás: állít! médiáit rendellenesség kezelésében történő alkalmazásra:..
  5. 14, Az 1:-1(1. igénypontok bármelyike által meghatározott polimorf vagy só alkalmazása nem megtelélő PD-ksnáz aktivitás által médiáit rendellenesség kezelésére: szolgáló gyógy szer előáll kására.
HUE11755311A 2010-09-08 2011-09-06 N-[5-[4-(5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oxazol-2-il)-1H-indazol-6-il]-2-(metiloxi)-3-piridinil]metánszulfonamid polimorfjai és sói HUE026059T2 (hu)

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US38074810P 2010-09-08 2010-09-08

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HUE11755311A HUE026059T2 (hu) 2010-09-08 2011-09-06 N-[5-[4-(5-{[(2R,6S)-2,6-dimetil-4-morfolinil]metil}-1,3-oxazol-2-il)-1H-indazol-6-il]-2-(metiloxi)-3-piridinil]metánszulfonamid polimorfjai és sói

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US (1) US8735390B2 (hu)
EP (1) EP2614058B1 (hu)
JP (1) JP5965402B2 (hu)
DK (1) DK2614058T3 (hu)
ES (1) ES2548036T3 (hu)
HR (1) HRP20151017T1 (hu)
HU (1) HUE026059T2 (hu)
PL (1) PL2614058T3 (hu)
PT (1) PT2614058E (hu)
RS (1) RS54286B1 (hu)
SI (1) SI2614058T1 (hu)
SM (1) SMT201500223B (hu)
WO (1) WO2012032067A1 (hu)

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EP2614058A1 (en) 2013-07-17
US8735390B2 (en) 2014-05-27
JP5965402B2 (ja) 2016-08-03
PT2614058E (pt) 2015-10-27
PL2614058T3 (pl) 2015-12-31
US20130165441A1 (en) 2013-06-27
DK2614058T3 (en) 2015-09-28
WO2012032067A1 (en) 2012-03-15
EP2614058B1 (en) 2015-07-08
JP2013537175A (ja) 2013-09-30
ES2548036T3 (es) 2015-10-13
SMT201500223B (it) 2015-10-30
RS54286B1 (en) 2016-02-29
HRP20151017T1 (hr) 2015-10-23

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