HUE028538T2 - Új kristályok és eljárás 5-({[2-amino-3-(4-karbamoil-2,6-dimetil-fenil)-propionil]-[1-(4-fenil-1H-imidazol-2-il) -etil]-amino}-metil)-2-metoxi-benzoesav elõállítására - Google Patents
Új kristályok és eljárás 5-({[2-amino-3-(4-karbamoil-2,6-dimetil-fenil)-propionil]-[1-(4-fenil-1H-imidazol-2-il) -etil]-amino}-metil)-2-metoxi-benzoesav elõállítására Download PDFInfo
- Publication number
- HUE028538T2 HUE028538T2 HUE08781434A HUE08781434A HUE028538T2 HU E028538 T2 HUE028538 T2 HU E028538T2 HU E08781434 A HUE08781434 A HU E08781434A HU E08781434 A HUE08781434 A HU E08781434A HU E028538 T2 HUE028538 T2 HU E028538T2
- Authority
- HU
- Hungary
- Prior art keywords
- amino
- phenyl
- imidazol
- ethyl
- propionyl
- Prior art date
Links
- 0 C[C@@](c1nc(-c2ccccc2)c[n]1)N(Cc(cc1)cc(C(*)=O)c1OC)C([C@@](*)Cc(c(C)c1)c(C)cc1C(N)=O)=O Chemical compound C[C@@](c1nc(-c2ccccc2)c[n]1)N(Cc(cc1)cc(C(*)=O)c1OC)C([C@@](*)Cc(c(C)c1)c(C)cc1C(N)=O)=O 0.000 description 1
Classifications
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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
- A61K31/60—Salicylic acid; Derivatives thereof
- A61K31/625—Salicylic acid; Derivatives thereof having heterocyclic substituents, e.g. 4-salicycloylmorpholine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/08—Antiallergic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
Claims (5)
- Szabadalmi. igényper?; ok L Biárás 5^(f|2-sffiífto~3<4-fc^bgmöÍr2,6^d:b»etlí“IVn!ií”pP5p:iopíi]-|l-(4-:fefisl-v;SB4ö5Ída^l-á'il)"et;sl^aíaioí?]-m^l^àâôlôxi-berszoesm. kmtalynj- teflonjának eJőá!iitá><mt, amely ísrtakoaziKá a következő lépéseket: ÿms mùzMh&ià sav kombinálása -- Í“'!fearií>' |«-8p»filtH:Î#-feO:4:Îfe*n: így 4<|}'áHÜ«íöö4^4- beoxoesav sóját aktijuk elő; és m dfep'-aminö-fetotoafhaotoh-^fe^ in<4il}y2~metOK?dv;jnzoe;5av sójának mosását szseveto Msiissal. így m 5”i {i2oKnino-;k(3-karbanwjk2,<S~ <is:m«ii:l~SÍónypíöpio8Íl-ÍI44-^ob4íí*imíia^oí4'4;íy«ií:í|-aíróaöymetil>4-s)őtósi-4>eozo<;sav ikerionját topjuk,
- 2. Az L igénypont szerinti eljárás. amely továbbá tartalmazza az S-( U2oroÍno43'4yarí)aou)il4,6oliít)etíkföB:ii}- propioo lij-jl -(4^ieí*ílrTM~i^l^K^I“3^>-^íÍi-amiÍBfeéf|:*-m€?t*iÉV2'-tóí#^5í.í--feei@>áá^é^!V itorioipápak vízzel való mosásának iétoséí,
- 3. Az i, igtoypPkí: smrnâ «garas, ahol a szé«vg:iea bázis náimim-híáumíá.
- 4. Az 1. igénypont szerintkepf ás, ahol az iooMib&tő sas bMroklorid sav és ahol a # m 54ÍP*aiosa>4>>í4“ torbaaiOîl-S;<i4ifse:iÎ3-4niij'ptopioî»j!”fk-f4--Énn4li-imitogôl443)4i?kamiMpmetïi;}-2-'inetoxâ-be«zôosav hidreklosid í:6ja I, Az i. igénypont szerinti eljárás, ahol az eljárás tartalmazza a köveikeaii: lépéseket: hídfők lot id sav kombinálása á^jjS-terc^iMökifeáífeönitorioo-^^d^atbaKusll^^-^intöíil-fönílii'pröpiosilji·' [1 k4"|őn:ii-l:íí-|;í8:idazu! -2-Ü j-etil] -aminoj -met il )*2*metos t-benzosavval, Így áss .5-(|Pramá«>-3-|4^ karín r<> 36, nv t s 3 p >p ornP I (4 it d 1 íl i oa3..u í>í ' í i> an r ( rneiíií 7 t>\ .... n· ossv Iddroldoriíi sóját ifeapiak; az: '54|{p-atnino-.3-{-t-katbanK«'l-2,í-diitteui-fenn-t-propiotíílJ~P”{4~feniMH'imidazoi^.-^)Heíil^^n-iao}·-· timiil}4--mptoxi-berzosav sójának mosasa nátrittm-hidroKiddai, így a? >4![ssmn?;ű^-f4rkátoanto!~2,6-4ΐόΐί«ΐΗ··&ϊΙ^·^>ίο;ηοί;ίΐί·[ i-i44eaiMi'3-im>dazoi"u-;S}-einj-iin:;i;o>-metiO-2-;ae;;>\i--benzasav icerioaját topjuk:; és: az to {{J-antino^-fol-kartyamoil^^imetH-feniD-pmpjonill-f t -(4 ·reníl»lM4mida2ó:l~2-íl)-etöj-ssan-ino|“iaetiîi|“2-metoxl-beozossv Ikerionjának mosását vízzel.
- 6, Az 5. igénypont szerintii eljárás, ahol az, .«Ifádik tbSáhbá. M <|li%WÔI-ftiâ-tî^ïm»:p£mU>P-<4:~ffersïf-'-li^4im3dia^0ii^2-5!)^nj-'am«î»^Â^iÎJ^irïetôxi~'foéRX-i>es^V: iköríoígötíírk tárolását fe2:S% relatív páratartalom mellett 3i napig, igy az 5”í'|-jPSv8ö*ii«-©“-3--(4^-3íb^i^ii-2i6^áll^eti:í^if^íl>~ |a-optoti3|r[í yd'denlkl 3í-ltnidagol"á‘-íij--«í3ij--ami:iKtl~m:et3:i)-2-ínetöxl-be;n;oessv a kristályferm^jaí ifegjäjtik, amely por-ettogesídiffetkolós ríMbiánítal jellemzőit, atnély rendelkezik pór-tíMgendlfekelós csúcsokkal: kdriilfeeiid «.követezőknél:: 14,¾ 14,3 és !4J fek 2 théta. 7. A 6. i^ÿpig szerinti eljárás, aböl M ö ^iytea ps>rs4>m:ge?uÍiriPkcfos öfomkatial jellemzett, saaelÿ reaílelköxlk jííSMtmípnílíílhjkeíós csacsökkai köröfosfol s követkézdfcaék: 1¾¾ ki ,2,14,0, 14,5 ás 14,7 fok 2 IÄ. B. A 6. igényper szerinti eljárás, almi az tx 'kvMBïfimm pwsrttatgeetâ iftakÄ mintázattal |e!lei:aA;ti, rsMétarife ^»'•«^Speií.fiMKítóiS: «Äsrifcbl körlifbsM a kövötfcstoéfe ji,2y 14 ,1, i |j; %ô, 14,3, 14,7, 16,1 és 18,3 fok2#fom, 4, A® S, igénypont sWtmii eljárás, ahol ást eljárás tövábM: tarláimszza az 5-{{(2-8^ήίθ'3·Ηί445»Α»ϊ»ί«)1··2,δ-4smel;IP6il}i4Opi4ixiy;-'il44Piiil-lB'iswi<läzök24|)vetilpamiböpmei!l}'24öeioxi“befizo«»av ikeri:íá|ifo3& i#»!ásái aagyöbfe :îS:ibi 60% relatív páratartalom tpeieíi 3 sápig, így az 5~({(2-amrno-3444£á!fb«P!lPv6“ <1ïmeis]--feni|P|>Tie>pîonsihI l^^kmil-lllrimidaiaiO^ljHStHHminoHnetii^roetori^tenzxtesav p kristály firmáját kapjak, amely por-röntgenU*tlfokelús mhitázattftl jellemzett, amely rer-íJslkezik p»>r"rÉítg»Bd|jMíp-lós csáesökbaí k&nilibsllíl a kovelkezOkm'i.: ! t,ö,12,4 és 1.5:,2 fok2foétá. 10. A 9. laénypom szerimi eljárás, ahol a P krsstályforma: pöt~röt%eadií:fíafccióíí mlmáznttal jellemzett, amely rendelkezik por-rikUgendiÖrakcíós csúcsukkal kúrüihelÚ· s kíiveíkezÓkTKíl: 11,ö, 1:2,4, 14,9, 15,2 ás 22,1 fok 2 iMta, 11. A % tgépypsní: szerinti eljárit*, aW « $ Mstályforroa pur-rönfgendiitfokclös anirifozabakjejláíTizeil:, amely rendelkezik posH-ms^endlimakeios: cmfeökkst fcMfeelül a következeknél: 11,¾. 1:2,4, 14,9, 15,2, 22,1, 25-,6, 27,4 és 30,4 fok 2 tbfoa.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US94858407P | 2007-07-09 | 2007-07-09 |
Publications (1)
Publication Number | Publication Date |
---|---|
HUE028538T2 true HUE028538T2 (hu) | 2016-12-28 |
Family
ID=39926468
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HUE08781434A HUE028538T2 (hu) | 2007-07-09 | 2008-07-07 | Új kristályok és eljárás 5-({[2-amino-3-(4-karbamoil-2,6-dimetil-fenil)-propionil]-[1-(4-fenil-1H-imidazol-2-il) -etil]-amino}-metil)-2-metoxi-benzoesav elõállítására |
HUS1700011C HUS1700011I1 (hu) | 2007-07-09 | 2017-03-02 | Új kristályok és eljárás 5-({[2-amino-3-(4-karbamoil-2,6-dimetil-fenil)-propionil]-[1-(4-fenil-1H-imidazol-2-il) -etil]-amino}-metil)-2-metoxi-benzoesav elõállítására |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HUS1700011C HUS1700011I1 (hu) | 2007-07-09 | 2017-03-02 | Új kristályok és eljárás 5-({[2-amino-3-(4-karbamoil-2,6-dimetil-fenil)-propionil]-[1-(4-fenil-1H-imidazol-2-il) -etil]-amino}-metil)-2-metoxi-benzoesav elõállítására |
Country Status (25)
Country | Link |
---|---|
US (7) | US7994206B2 (hu) |
EP (1) | EP2176234B1 (hu) |
JP (5) | JP5702140B2 (hu) |
KR (2) | KR101690161B1 (hu) |
CN (3) | CN101730685A (hu) |
AU (1) | AU2008275270C1 (hu) |
BR (1) | BRPI0813632A2 (hu) |
CA (1) | CA2695126C (hu) |
CO (1) | CO6260079A2 (hu) |
CR (1) | CR11260A (hu) |
EA (1) | EA020024B1 (hu) |
EC (1) | ECSP109863A (hu) |
ES (1) | ES2567077T3 (hu) |
HK (1) | HK1141519A1 (hu) |
HU (2) | HUE028538T2 (hu) |
IL (1) | IL203081A (hu) |
MX (1) | MX339569B (hu) |
MY (1) | MY174681A (hu) |
NI (1) | NI201000001A (hu) |
NZ (1) | NZ582420A (hu) |
PH (1) | PH12016502561A1 (hu) |
SG (1) | SG185941A1 (hu) |
UA (1) | UA104713C2 (hu) |
WO (1) | WO2009009480A2 (hu) |
ZA (1) | ZA201000921B (hu) |
Families Citing this family (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7412462B2 (en) | 2000-02-18 | 2008-08-12 | Burnside Acquisition, Llc | Data repository and method for promoting network storage of data |
NZ582420A (en) | 2007-07-09 | 2011-11-25 | Janssen Pharmaceutica Nv | Novel crystals and process of making 5-({ [2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino} -methyl)-2-methoxy- benzoic acid |
US9675587B2 (en) * | 2013-03-14 | 2017-06-13 | Allergan Holdings Unlimited Company | Opioid receptor modulator dosage formulations |
EP3325450A1 (en) * | 2015-07-23 | 2018-05-30 | Teva Pharmaceuticals International GmbH | Solid state forms of eluxadoline |
WO2017114446A1 (zh) * | 2015-12-31 | 2017-07-06 | 苏州晶云药物科技有限公司 | 艾沙度林的新晶型及其制备方法 |
EP3272741A1 (en) | 2016-07-21 | 2018-01-24 | Euticals S.P.A. | New stable solvate crystalline forms of eluxadoline |
WO2017191650A1 (en) * | 2016-05-03 | 2017-11-09 | Msn Laboratories Private Limited | Process for the preparation of 5-[[[(2s)-2-amino-3-[4-(aminocarbonyl)-2,6-dimethylphenyl]-1-oxopropyl][(1s)-1-(4-phenyl-1h-imidazol-2-yl)ethyl]amino]methyl-2-methoxybenzoic acid and its polymorphs thereof |
WO2017221213A1 (en) * | 2016-06-23 | 2017-12-28 | Sun Pharmaceutical Industries Limited | Processes for the preparation of eluxadoline |
WO2018020450A2 (en) | 2016-07-28 | 2018-02-01 | Lupin Limited | Process for the preparation of eluxadoline |
CZ2016548A3 (cs) | 2016-09-07 | 2018-03-14 | Zentiva, K.S. | Pevné formy eluxadolinu |
WO2018047131A1 (en) * | 2016-09-09 | 2018-03-15 | Sun Pharmaceutical Industries Limited | Amorphous eluxadoline |
WO2018055528A2 (en) * | 2016-09-20 | 2018-03-29 | Sun Pharmaceutical Industries Limited | Processes for the preparation of eluxadoline |
WO2018069770A1 (en) * | 2016-10-14 | 2018-04-19 | Allergan Holdings Unlimited Company | Methods of treatment using eluxadoline |
WO2018138272A1 (en) | 2017-01-27 | 2018-08-02 | Quimica Sintetica, S. A. | Eluxadoline crystalline form and process for the preparation thereof |
EP3573958A1 (en) | 2017-01-27 | 2019-12-04 | Quimica Sintetica, S.A. | Eluxadoline crystalline forms and processes for their preparation |
WO2018198101A2 (en) * | 2017-04-25 | 2018-11-01 | Sun Pharmaceutical Industries Limited | Processes for the preparation of crystalline form of eluxadoline |
WO2019008604A1 (en) | 2017-07-07 | 2019-01-10 | Cipla Limited | NEW FORMS OF MU-OPIOID RECEPTOR AGONIST |
CA3018321A1 (en) * | 2017-09-25 | 2019-03-25 | Apotex Inc. | Novel crystalline form of eluxadoline |
US10298921B1 (en) * | 2018-02-27 | 2019-05-21 | Looking Glass Factory, Inc. | Superstereoscopic display with enhanced off-angle separation |
WO2020039333A1 (en) | 2018-08-20 | 2020-02-27 | Allergan Holdings Unlimited Company | Polymorphs of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid |
WO2021198780A1 (en) * | 2020-03-30 | 2021-10-07 | Allergan Holdings Unlimited Company | Forms of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2003065441A (ja) | 2001-08-28 | 2003-03-05 | Japan Matekkusu Kk | パッキン材料及びこの材料を用いたグランドパッキン |
SI2653465T1 (sl) * | 2004-03-15 | 2016-10-28 | Janssen Pharmaceutica N.V. | Modulatorji opiodnih receptorjev |
EA015512B1 (ru) * | 2005-03-14 | 2011-08-30 | Янссен Фармацевтика, Н.В. | Способ получения опиоидных модуляторов |
NZ582420A (en) | 2007-07-09 | 2011-11-25 | Janssen Pharmaceutica Nv | Novel crystals and process of making 5-({ [2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino} -methyl)-2-methoxy- benzoic acid |
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2008
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- 2008-07-07 JP JP2010516175A patent/JP5702140B2/ja not_active Expired - Fee Related
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- 2010-02-09 CR CR11260A patent/CR11260A/es not_active Application Discontinuation
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- 2017-03-02 HU HUS1700011C patent/HUS1700011I1/hu unknown
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2018
- 2018-04-03 JP JP2018071317A patent/JP2018123144A/ja active Pending
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