MX2014004603A - Formas de dosificacion solidas de 2-amino-3-(4-(2-amino-6-((r)-1-( 4-cloro-2-(3-metil-1h-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pi rimidin-4-il)fenil) propanoato de (s)-etilo. - Google Patents

Formas de dosificacion solidas de 2-amino-3-(4-(2-amino-6-((r)-1-( 4-cloro-2-(3-metil-1h-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pi rimidin-4-il)fenil) propanoato de (s)-etilo.

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Publication number
MX2014004603A
MX2014004603A MX2014004603A MX2014004603A MX2014004603A MX 2014004603 A MX2014004603 A MX 2014004603A MX 2014004603 A MX2014004603 A MX 2014004603A MX 2014004603 A MX2014004603 A MX 2014004603A MX 2014004603 A MX2014004603 A MX 2014004603A
Authority
MX
Mexico
Prior art keywords
phenyl
amino
pyrazol
pyrimidin
chloro
Prior art date
Application number
MX2014004603A
Other languages
English (en)
Other versions
MX360191B (es
Inventor
Jinling Chen
Matthew S Deaver
Richard J Holl
Kalyan Nuguru
Original Assignee
Lexicon Pharmaceuticals 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 Lexicon Pharmaceuticals Inc filed Critical Lexicon Pharmaceuticals Inc
Publication of MX2014004603A publication Critical patent/MX2014004603A/es
Publication of MX360191B publication Critical patent/MX360191B/es

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2095Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2893Tablet coating processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se revelan formas de dosificación sólidas que comprenden 2-amino-3-(4-(2-amino-6-( (R)-1-(4-cloro-2-(3-metil-1H pirazol-1-il) fenil) -2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)pr opanoato de (S)-etilo (telotristat), también como métodos para fabricarlas y composiciones útiles en su manufactura.
MX2014004603A 2011-10-17 2012-10-16 Formas de dosificacion solidas de 2-amino-3-(4-(2-amino-6-((r)-1-( 4-cloro-2-(3-metil-1h-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pi rimidin-4-il)fenil) propanoato de (s)-etilo. MX360191B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161547894P 2011-10-17 2011-10-17
PCT/US2012/060338 WO2013059146A1 (en) 2011-10-17 2012-10-16 Solid dosage forms of (s)-ethyl 2-amino-3-(4-(2-amino-6-((r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate

Publications (2)

Publication Number Publication Date
MX2014004603A true MX2014004603A (es) 2014-05-12
MX360191B MX360191B (es) 2018-10-24

Family

ID=47116458

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2014004603A MX360191B (es) 2011-10-17 2012-10-16 Formas de dosificacion solidas de 2-amino-3-(4-(2-amino-6-((r)-1-( 4-cloro-2-(3-metil-1h-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pi rimidin-4-il)fenil) propanoato de (s)-etilo.

Country Status (19)

Country Link
US (4) US20130172376A1 (es)
EP (2) EP3763374A1 (es)
JP (1) JP6203182B2 (es)
KR (1) KR102047788B1 (es)
CN (1) CN103987381B (es)
AU (1) AU2012326383B2 (es)
BR (1) BR112014009308B1 (es)
CA (1) CA2851862C (es)
DK (1) DK2753306T3 (es)
ES (1) ES2835722T3 (es)
HU (1) HUE051585T2 (es)
IL (1) IL231958B (es)
MX (1) MX360191B (es)
PL (1) PL2753306T3 (es)
PT (1) PT2753306T (es)
RU (1) RU2661402C2 (es)
SG (1) SG11201401583YA (es)
UA (1) UA114412C2 (es)
WO (1) WO2013059146A1 (es)

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UA119247C2 (uk) 2013-09-06 2019-05-27 РОЙВЕНТ САЙЕНСИЗ ҐмбГ Спіроциклічні сполуки як інгібітори триптофангідроксилази
JP6577866B2 (ja) 2014-03-28 2019-09-18 日本碍子株式会社 モノリス型分離膜構造体及びその製造方法
US9611201B2 (en) 2015-03-05 2017-04-04 Karos Pharmaceuticals, Inc. Processes for preparing (R)-1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanol and 1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanone
CN108883377B (zh) 2016-03-31 2021-05-07 日本碍子株式会社 多孔质支撑体、多孔质支撑体的制造方法、分离膜结构体以及分离膜结构体的制造方法
TW201818964A (zh) 2016-09-30 2018-06-01 瑞士商諾伊曼特醫療公司 使用色胺酸羥化酶抑制劑之方法
EP3363798A1 (en) 2017-02-20 2018-08-22 Esteve Química, S.A. Amorphous form of telotristat etiprate
WO2021137160A1 (en) * 2019-12-31 2021-07-08 Pfizer R&D Uk Limited Stable immediate release tablet and capsule formulations of 1-((2s,5r)-5-((7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one

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GB9124807D0 (en) * 1991-11-22 1992-01-15 Wellcome Found Pharmaceutical formulations
EP1332757B1 (en) * 1998-05-27 2012-06-13 Merck Sharp & Dohme Corp. Efavirenz compressed tablet formulation
PE20000559A1 (es) * 1998-05-27 2000-07-05 Merck & Co Inc Formulacion de tabletas comprimidas de efavirenz
PA8576201A1 (es) * 2002-07-10 2004-05-26 Pfizer Prod Inc Composicion farmaceutica que tiene una distribucion y potencia uniforme de farmaco
WO2005021000A1 (en) * 2003-08-28 2005-03-10 Ranbaxy Laboratories Limited Solid oral dosage forms of gatifloxacin
HN2006020928A (es) * 2005-06-09 2011-02-16 Wyeth Corp "composiciones de tanaproget que contienen etinil estradiol"
JP2009542647A (ja) * 2006-07-05 2009-12-03 テバ ファーマシューティカル インダストリーズ リミティド メマンチン医薬組成物
UA99270C2 (en) 2006-12-12 2012-08-10 Лексикон Фармасьютикалз, Инк. 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use
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TWI439457B (zh) * 2007-09-28 2014-06-01 Lexicon Pharmaceuticals Inc (s)-2-胺基-3-(4-(2-胺基-6-((r)-1-(4-氯-2-(3-甲基-1h-吡唑-1-基)苯基)-2,2,2-三氟乙氧)-嘧啶-4-基)苯基)丙酸乙酯之固體形式與其使用方法
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Also Published As

Publication number Publication date
JP6203182B2 (ja) 2017-09-27
PT2753306T (pt) 2020-11-11
CN103987381A (zh) 2014-08-13
CA2851862C (en) 2020-04-14
RU2014119866A (ru) 2015-11-27
ES2835722T3 (es) 2021-06-23
CN103987381B (zh) 2017-07-04
US11406635B2 (en) 2022-08-09
AU2012326383A1 (en) 2014-04-24
EP3763374A1 (en) 2021-01-13
HUE051585T2 (hu) 2021-03-01
AU2012326383B2 (en) 2017-07-27
US20150157632A1 (en) 2015-06-11
US20210008068A1 (en) 2021-01-14
BR112014009308A2 (pt) 2017-04-11
DK2753306T3 (da) 2020-12-14
IL231958A0 (en) 2014-05-28
SG11201401583YA (en) 2014-09-26
IL231958B (en) 2018-06-28
NZ623423A (en) 2016-04-29
KR20140081872A (ko) 2014-07-01
EP2753306B1 (en) 2020-09-23
NZ717137A (en) 2017-10-27
US20190000843A1 (en) 2019-01-03
UA114412C2 (uk) 2017-06-12
RU2661402C2 (ru) 2018-07-16
JP2014532073A (ja) 2014-12-04
MX360191B (es) 2018-10-24
PL2753306T3 (pl) 2021-04-06
WO2013059146A1 (en) 2013-04-25
EP2753306A1 (en) 2014-07-16
US20130172376A1 (en) 2013-07-04
KR102047788B1 (ko) 2019-11-22
CA2851862A1 (en) 2013-04-25
BR112014009308B1 (pt) 2022-05-03

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