EA201690869A1 - СТАБИЛЬНЫЙ ПОЛИМОРФ СОЛИ (2R)-4-ОКСО-4-[3-(ТРИФТОРМЕТИЛ)-5,6-ДИГИДРО[1,2,4]ТРИАЗОЛО[4,3-α]ПИРАЗИН-7(8H)-ИЛ]-1-(2,4,5-ТРИФТОРФЕНИЛ)БУТАН-2-АМИНА И L-ВИННОЙ КИСЛОТЫ - Google Patents

СТАБИЛЬНЫЙ ПОЛИМОРФ СОЛИ (2R)-4-ОКСО-4-[3-(ТРИФТОРМЕТИЛ)-5,6-ДИГИДРО[1,2,4]ТРИАЗОЛО[4,3-α]ПИРАЗИН-7(8H)-ИЛ]-1-(2,4,5-ТРИФТОРФЕНИЛ)БУТАН-2-АМИНА И L-ВИННОЙ КИСЛОТЫ

Info

Publication number
EA201690869A1
EA201690869A1 EA201690869A EA201690869A EA201690869A1 EA 201690869 A1 EA201690869 A1 EA 201690869A1 EA 201690869 A EA201690869 A EA 201690869A EA 201690869 A EA201690869 A EA 201690869A EA 201690869 A1 EA201690869 A1 EA 201690869A1
Authority
EA
Eurasian Patent Office
Prior art keywords
salt
pyrazin
triazolo
butan
dihydro
Prior art date
Application number
EA201690869A
Other languages
English (en)
Other versions
EA030029B1 (ru
Inventor
Индржих Рихтер
Петр Легнерт
Камаль Ярраг
Ондрей Даммер
Лукас Крейцик
Original Assignee
Зентива, К.С.
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 Зентива, К.С. filed Critical Зентива, К.С.
Publication of EA201690869A1 publication Critical patent/EA201690869A1/ru
Publication of EA030029B1 publication Critical patent/EA030029B1/ru

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

Abstract

Стабильный полиморф (форма Z1) соли (2R)-4-оксо-4-[3-(трифторметил)-5,6-дигидро[1,2,4]триазоло[4,3-α]пиразин-7(8Н)-ил]-1-(2,4,5-трифторфенил)бутан-2-амина (ситаглиптин) и L-винной кислоты формулы 1, который представляет собой очень подходящую форму активного фармацевтического ингредиента лекарственных средств, главным образом предназначенных для лечения диабета 2 типа. Способ получения стабильного полиморфа (форма Z1) соли ситаглиптина и L-винной кислоты, а также его применение для получения фармацевтической композиции.
EA201690869A 2013-11-01 2014-10-30 СТАБИЛЬНЫЙ ПОЛИМОРФ СОЛИ (2R)-4-ОКСО-4-[3-(ТРИФТОРМЕТИЛ)-5,6-ДИГИДРО[1,2,4]ТРИАЗОЛО[4,3-α]ПИРАЗИН-7(8H)-ИЛ]-1-(2,4,5-ТРИФТОРФЕНИЛ)БУТАН-2-АМИНА И L-ВИННОЙ КИСЛОТЫ EA030029B1 (ru)

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 (2)

Publication Number Publication Date
EA201690869A1 true EA201690869A1 (ru) 2016-08-31
EA030029B1 EA030029B1 (ru) 2018-06-29

Family

ID=52130030

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201690869A EA030029B1 (ru) 2013-11-01 2014-10-30 СТАБИЛЬНЫЙ ПОЛИМОРФ СОЛИ (2R)-4-ОКСО-4-[3-(ТРИФТОРМЕТИЛ)-5,6-ДИГИДРО[1,2,4]ТРИАЗОЛО[4,3-α]ПИРАЗИН-7(8H)-ИЛ]-1-(2,4,5-ТРИФТОРФЕНИЛ)БУТАН-2-АМИНА И L-ВИННОЙ КИСЛОТЫ

Country Status (17)

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

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
WO2005072530A1 (en) 2004-01-16 2005-08-11 Merck & Co., Inc. Novel crystalline salts of a dipeptidyl peptidase-iv inhibitor
US20090221592A1 (en) * 2005-07-25 2009-09-03 Ellison Martha E Dodecylsulfate Salt Of A Dipeptidyl Peptidase-Iv Inhibitor
CN101903390A (zh) * 2007-12-20 2010-12-01 雷迪博士实验室有限公司 制备西他列汀及其药学上可接受的盐的方法

Also Published As

Publication number Publication date
US20160251360A1 (en) 2016-09-01
US9862723B2 (en) 2018-01-09
LT3063151T (lt) 2018-12-10
CZ2013842A3 (cs) 2015-05-13
EA030029B1 (ru) 2018-06-29
UA119655C2 (uk) 2019-07-25
CN105705505A (zh) 2016-06-22
EP3063151B1 (en) 2018-08-29
KR20160078359A (ko) 2016-07-04
MX2016005173A (es) 2016-07-08
WO2015062562A1 (en) 2015-05-07
ZA201602731B (en) 2017-07-26
IL245263A0 (en) 2016-06-30
ES2694350T3 (es) 2018-12-20
JP2016535045A (ja) 2016-11-10
TR201815737T4 (tr) 2018-11-21
PL3063151T3 (pl) 2019-05-31
EP3063151A1 (en) 2016-09-07
PT3063151T (pt) 2018-11-19

Similar Documents

Publication Publication Date Title
MX2020011079A (es) Forma cristalina de sulfato acido de (s)-n-(5-((r)-2-(2,5-difluoro fenil)-pirrolidin-1-il)-pirazolo[1,5-a]-pirimidin-3-il)-3-hidroxi pirrolidina-1-carboxamida.
NZ629511A (en) Novel crystalline form of sitagliptin sulfate
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
EA201300908A1 (ru) ПРОИЗВОДНЫЕ 6-ЦИКЛОБУТИЛ-1,5-ДИГИДРОПИРАЗОЛО[3,4d]ПИРИМИДИН-4-ОНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE9A
EA201300620A1 (ru) ПРОИЗВОДНЫЕ ИМИДАЗО[1,2-b]ПИРИДАЗИНА И ИМИДАЗО[4,5-b]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ JAK
EA201170771A1 (ru) Органические соединения
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
CL2012003227A1 (es) Compuestos macrociclicos que comprenden en el ciclo una porcion pirazolo[1,5-a]pirimidina, inhibidores de quinasa trk; composicion farmaceutica; proceso de preparación; y metodo para tratar un trastorno seleccionado de dolor, cancer, inflamacion, enfermedad neurodegenerativa o infeccion por trypanosoma cruzi.
EA201170962A1 (ru) Препарат разагилина с отсроченным высвобождением действующего вещества
EA201201664A1 (ru) Производные 6-циклоалкил-1,5-дигидропипазоло[3,4-d]пиримидин-4-она и их применение в качестве ингибиторов pde9a
DOP2010000263A (es) Derivados de imidazo-[1,2-b]-piridazina para el tratamiento de enfermedad mediada por cinasa de tirosina c-met
WO2012034055A3 (en) Compounds as c-met kinase inhibitors
PE20120534A1 (es) PIRIMIDINAS FUSIONADAS COMO INHIBIDORES DE Akt
RU2015148189A (ru) ПРОИЗВОДНЫЕ 2-АМИДОПИРИДО[4, 3-d]ПИРИМИДИН-5-ОНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ WEE-1
EA201591804A1 (ru) Производные 2-((4-амино-3-(3-фтор-5-гидроксифенил)-1h-пиразоло[3,4-d]пиримидин-1-ил)метил)-3-(2-(трифторметил)бензил)хиназолин-4(3h)-она и их применение в качестве ингибиторов фосфоинозитид-3-киназы
HRP20190814T1 (hr) 7-benzil-4-(2-metilbenzil)-2,4,6,7,8,9-heksahidroimidazo[1,2-a]pirido[3,4-e]pirimidin-5(1h)-on, njegove soli i postupci uporabe
MX339302B (es) 3-(quinolin-6-il-tio)-[1,2,4]-triazolo-[4,3-a]-piridinas 6-sustituidas como cinasas de tirosina.
EA201690183A1 (ru) Замещенные пиразолопиридинамины
RU2015102772A (ru) Бензодиазелипы для мелкоклеточного рака легкого
GEP20196969B (en) New therapeutical composition containing apomorphine as active ingredient
PE20171104A1 (es) Pirazolpiridinaminas como inhibidores de mknk1 y mknk2
AR084832A1 (es) Derivado cristalino de oxazina
AR079136A1 (es) Formas polimorfas de (4,6-diamino-2-(1-(2-fluorobencil)-1h- pirazolo (3,4-b) piridin -3-il)piridin -5-il) carbamato de metilo
EA201490045A1 (ru) Дейтерированные 1-пиперазино-3-фенилинданы, применяемые для лечения шизофрении
EA201071352A1 (ru) Трициклические азотсодержащие соединения и их применение в качестве бактерицидных средств

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KG TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): KZ RU