MX2016005173A - Un polimorfo estable de la sal de (2r)-4-oxo-4-[3-(trifluorometil) -5,6-dihidro[1,2,4]triazolo[4,3-a]pirazin-7(8h)-il]-1-(2,4,5-trif luorofenil)butan-2-amina con acido l-tartarico. - Google Patents

Un polimorfo estable de la sal de (2r)-4-oxo-4-[3-(trifluorometil) -5,6-dihidro[1,2,4]triazolo[4,3-a]pirazin-7(8h)-il]-1-(2,4,5-trif luorofenil)butan-2-amina con acido l-tartarico.

Info

Publication number
MX2016005173A
MX2016005173A MX2016005173A MX2016005173A MX2016005173A MX 2016005173 A MX2016005173 A MX 2016005173A MX 2016005173 A MX2016005173 A MX 2016005173A MX 2016005173 A MX2016005173 A MX 2016005173A MX 2016005173 A MX2016005173 A MX 2016005173A
Authority
MX
Mexico
Prior art keywords
salt
tartaric acid
pyrazin
triazolo
butan
Prior art date
Application number
MX2016005173A
Other languages
English (en)
Inventor
Jindrich Richter
Ondrej Dammer
Lukas Krejcik
Petr Lehnert
Kamal Jarrah
Original Assignee
Zentiva Ks
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 Zentiva Ks filed Critical Zentiva Ks
Publication of MX2016005173A publication Critical patent/MX2016005173A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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
    • A61K31/395—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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255—Tartaric acid
    • 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

Landscapes

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

Abstract

La presente invención se refiere a un polimorfo estable (Forma Z1) de la sal de (2R)-4-oxo-4-[3-(trifluorometil)-5,6-dihidro[152, 4]triazolo[4,3-a]pirazin-7(8H)-il]-1-(2s4,5-trifluorofenil)butan- 2-amina (sitagliptina) con ácido L-tartárico, de la fórmula 1, la cual es una forma muy estable del ingrediente farmacéutico activo de productos medicinales proyectados especialmente para el tratamiento de la diabetes tipo 2. La presente invención también se refiere a un método para la preparación del polimorfo estable (Forma Z1) de la sal de sitagliptina con ácido L-tartárico, y al uso del mismo para la preparación de una composición farmacéutica.
MX2016005173A 2013-11-01 2014-10-30 Un polimorfo estable de la sal de (2r)-4-oxo-4-[3-(trifluorometil) -5,6-dihidro[1,2,4]triazolo[4,3-a]pirazin-7(8h)-il]-1-(2,4,5-trif luorofenil)butan-2-amina con acido l-tartarico. MX2016005173A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CZ2013-842A CZ2013842A3 (cs) 2013-11-01 2013-11-01 Stabilní polymorf soli (2R)-4-oxo-4-[3-(trifluorometyl)-5,6-dihydro[1,2,4]triazolo[4,3-α]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorofenyl)butan-2-aminu s kyselinou L-vinnou
PCT/CZ2014/000125 WO2015062562A1 (en) 2013-11-01 2014-10-30 A stable polymorph of the salt of (2r)-4-oxo-4-[3-(trifiuoromethyl)-5,6- dihydro[l,2,4]triazolo[4,3-a]pyrazin-7(8h)-yl]-l-(2,4,54rifluorophenyl)butan-2-amine with l-tartaric acid

Publications (1)

Publication Number Publication Date
MX2016005173A true MX2016005173A (es) 2016-07-08

Family

ID=52130030

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016005173A MX2016005173A (es) 2013-11-01 2014-10-30 Un polimorfo estable de la sal de (2r)-4-oxo-4-[3-(trifluorometil) -5,6-dihidro[1,2,4]triazolo[4,3-a]pirazin-7(8h)-il]-1-(2,4,5-trif luorofenil)butan-2-amina con acido l-tartarico.

Country Status (17)

Country Link
US (1) US9862723B2 (es)
EP (1) EP3063151B1 (es)
JP (1) JP2016535045A (es)
KR (1) KR20160078359A (es)
CN (1) CN105705505A (es)
CZ (1) CZ2013842A3 (es)
EA (1) EA030029B1 (es)
ES (1) ES2694350T3 (es)
IL (1) IL245263A0 (es)
LT (1) LT3063151T (es)
MX (1) MX2016005173A (es)
PL (1) PL3063151T3 (es)
PT (1) PT3063151T (es)
TR (1) TR201815737T4 (es)
UA (1) UA119655C2 (es)
WO (1) WO2015062562A1 (es)
ZA (1) ZA201602731B (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ27898U1 (cs) * 2015-01-13 2015-03-02 Zentiva, K.S. Krystalická modifikace 2 L-vínanu (3R)-3-amino-1-[3-(trifluormethyl)-6,8-dihydro-5H-[1,2,4,]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorfenyl)butan-1-onu
CZ27930U1 (cs) * 2015-01-13 2015-03-10 Zentiva, K.S. Krystalická modifikace 3 L-vínanu (3R)-3-amino-1-[3-(trifluormethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorfenyl)butan-1-onu

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
JO2625B1 (en) 2003-06-24 2011-11-01 ميرك شارب اند دوم كوربوريشن Phosphoric acid salts of dipeptidyl betidase inhibitor 4
EP1708571A4 (en) * 2004-01-16 2009-07-08 Merck & Co Inc NEW CRYSTALLINE SALTS OF A DIPEPTIDYLPEPTIDASE IV HEMMER
US20090221592A1 (en) 2005-07-25 2009-09-03 Ellison Martha E Dodecylsulfate Salt Of A Dipeptidyl Peptidase-Iv Inhibitor
EP2599781A1 (en) 2007-12-20 2013-06-05 Dr. Reddy's Laboratories Ltd. Processes for the preparation of sitagliptin and pharmaceutically acceptable salts thereof

Also Published As

Publication number Publication date
PT3063151T (pt) 2018-11-19
KR20160078359A (ko) 2016-07-04
EP3063151A1 (en) 2016-09-07
WO2015062562A1 (en) 2015-05-07
ES2694350T3 (es) 2018-12-20
US20160251360A1 (en) 2016-09-01
EP3063151B1 (en) 2018-08-29
UA119655C2 (uk) 2019-07-25
CZ2013842A3 (cs) 2015-05-13
CN105705505A (zh) 2016-06-22
EA201690869A1 (ru) 2016-08-31
IL245263A0 (en) 2016-06-30
JP2016535045A (ja) 2016-11-10
LT3063151T (lt) 2018-12-10
PL3063151T3 (pl) 2019-05-31
US9862723B2 (en) 2018-01-09
ZA201602731B (en) 2017-07-26
EA030029B1 (ru) 2018-06-29
TR201815737T4 (tr) 2018-11-21

Similar Documents

Publication Publication Date Title
WO2018033853A3 (en) Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
NZ629511A (en) Novel crystalline form of sitagliptin sulfate
IL291489A (en) Preparation of (s)-4-(8-amino-3-(1-but-2-inoyl-pyrrolidin-2-yl)imidazo[5,1-a]pyrazin-1-yl)-n-(pyridine- 2-l) Benzamide and its acceptable pharmaceutical salts
MY164274A (en) Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof
BR112014032338A2 (pt) cristais de sal
HRP20182007T1 (hr) Derivati 3-okso-2,3,5,8-tetrahidro-[1,2,4]triazolo[4,3-a]pirimidina za liječenje respiratornih bolesti
EA201300908A1 (ru) ПРОИЗВОДНЫЕ 6-ЦИКЛОБУТИЛ-1,5-ДИГИДРОПИРАЗОЛО[3,4d]ПИРИМИДИН-4-ОНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE9A
EP3489238B8 (en) Pharmaceutical compositions of 6h-pyrido[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5-one and [1,2,4]triazolo[1,5-c]pteridin-5(6h)-one derivatives as pde1 inhibitors for treating e.g. neurological disorders
WO2012143416A3 (en) 7 - (3,5 - dimethyl - 4 - isoxazolyl) - 8 - (methyloxy) - 1h - imidazo [4,5 -c] quinoline derivatives
NZ601754A (en) Pyrrolopyrimidine compounds as inhibitors of cdk4/6
NZ703111A (en) Novel 3,5-disubstitued-3h-imidazo[4,5-b]pyridine and 3,5- disubstitued -3h-[1,2,3]triazolo[4,5-b] pyridine compounds as modulators of protein kinases
MX339302B (es) 3-(quinolin-6-il-tio)-[1,2,4]-triazolo-[4,3-a]-piridinas 6-sustituidas como cinasas de tirosina.
MX2020002711A (es) Proceso para preparacion de 7-(4,7-diazaespiro[2.5]octan-7-il)-2-( 2,8-dimetilimidazo[1,2-b]piridazin-6-il)pirido[1,2-a]pirimidin-4- ona.
MX2021004487A (es) Nuevas formas de derivados de pirido[1,2-a]pirimidin-4-ona, su formulacion y su proceso de elaboracion.
MX2012001529A (es) Derivados de 3-heteroaril-metil-imidazo-[1,2-b]-piridazin-6-ilo como moduladores de cinasa de tirosina c-met.
PH12015501536A1 (en) Novel salts of dpp-iv inhibitor
MX2016005173A (es) Un polimorfo estable de la sal de (2r)-4-oxo-4-[3-(trifluorometil) -5,6-dihidro[1,2,4]triazolo[4,3-a]pirazin-7(8h)-il]-1-(2,4,5-trif luorofenil)butan-2-amina con acido l-tartarico.
ECSP13012599A (es) Hidrato de tartrato DE 1-{(2S)-2-amino-4-[2,4-bis(trifluorometil)-5,8-di-hidropirido[3,4-d]pirimidin-7(6H)-il]-4-oxobutil}-5,5-difluoro-piperidin-2-ona
MY165623A (en) 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indol acetic acid derivatives and their use as prostaglandin d2 receptor modulators
WO2014193881A8 (en) Crystalline form of n,n-dicyclopropyl-4-(1,5-dimethyl-1 h-pyrazol-3-ylamino)-6-ethyl-1 -methyl-1,6-dihyrdroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide for the treatment of myeloproliferative disorders
MX2023004924A (es) Nuevo tratamiento de la atrofia muscular espinal (sma).
WO2015145333A8 (en) Process for the preparation of sitagliptin and its intermediate
TN2013000146A1 (en) Salt(s) of 7-cyclopentyl-2 -(5-piperazin-1-yl-pyridin-2-ylamino)-7h-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof
MX2016007494A (es) Tratamiento de la esclerosis multiple con un derivado de 1,2,4-triazolo [1,5-a] piridina.
PL395783A1 (pl) Pochodna 1,2,4-triazolo[3,4-b]-1,3,4-tiadiazolu - 3-(3-chlorofenylo)-6-(4-chlorofenylo)amino-[1,2,4]triazolo[3,4-b]-1,3,4-tiadiazol, sposób jej wytwarzania oraz jej pierwsze zastosowanie medyczne