BRPI0411726A - composto, monoidrato, sal, composição farmacêutica, método para o tratamento de diabetes tipo 2, processo para preparar o composto, uso do composto, e, processo para a preparação do monoidrato cristalino - Google Patents

composto, monoidrato, sal, composição farmacêutica, método para o tratamento de diabetes tipo 2, processo para preparar o composto, uso do composto, e, processo para a preparação do monoidrato cristalino

Info

Publication number
BRPI0411726A
BRPI0411726A BRPI0411726-3A BRPI0411726A BRPI0411726A BR PI0411726 A BRPI0411726 A BR PI0411726A BR PI0411726 A BRPI0411726 A BR PI0411726A BR PI0411726 A BRPI0411726 A BR PI0411726A
Authority
BR
Brazil
Prior art keywords
compound
monohydrate
diabetes
treatment
preparing
Prior art date
Application number
BRPI0411726-3A
Other languages
English (en)
Inventor
Stephen Howard Cypes
Alex Minhua Chen
Russell R Ferlita
Karl Hansen
Ivan Lee
Vicky K Vydra
Robert M Wenslow
Original Assignee
Merck & Co 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33563839&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0411726(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of BRPI0411726A publication Critical patent/BRPI0411726A/pt
Publication of BRPI0411726B1 publication Critical patent/BRPI0411726B1/pt
Publication of BRPI0411726B8 publication Critical patent/BRPI0411726B8/pt

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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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

Landscapes

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

Abstract

"COMPOSTO, MONOIDRATO, SAL, COMPOSIçáO FARMACêUTICA, MéTODO PARA O TRATAMENTO DE DIABETES TIPO 2, PROCESSO PARA PREPARAR O COMPOSTO, USO DO COMPOSTO, E, PROCESSO PARA A PREPARAçãO DO MONOIDRATO CRISTALINO". O sal de di-hidrogeno fosfato de 4-oxo-4-¢3-(trifluorometil)5,6-diidro¢1,2,4!triazol ¢4,3-α!pirazin-7- (8H)-il!-1-(2,4,5trifluorofenil)butan-2-anfina é um inibidor potente de dipeptidil peptidase-IV e é útil para a prevenção e/ou o tratamento de diabetes melitus dependente de não -insulina, também referido como diabetes melitus tipo 2. A invenção refere-se também a um monoidrato cristalino do sal de di-hidrogeno fosfato, assim como a um processo para a sua preparação, a composições farmacêuticas contendo esta nova forma e a métodos de uso para o tratamento de diabetes, obesidade e pressão sangüínea elevada.
BRPI0411726A 2003-06-24 2004-06-18 composto monoidrato cristalino do sal de di-hidrogenofosfato de (2r)-4-oxo-4-[3-(trifluorometil)-5,6-diidro[1,2,4]triazol[4,3-a]pirazin-7-(8h)-il]-1 -(2,4,5-trifluorofenil) butan-2-amina, processo para preparar o composto, e, uso do composto BRPI0411726B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US48216103P 2003-06-24 2003-06-24
US60/482,161 2003-06-24
PCT/US2004/019683 WO2005003135A1 (en) 2003-06-24 2004-06-18 Phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor

Publications (3)

Publication Number Publication Date
BRPI0411726A true BRPI0411726A (pt) 2006-08-08
BRPI0411726B1 BRPI0411726B1 (pt) 2017-12-12
BRPI0411726B8 BRPI0411726B8 (pt) 2021-05-25

Family

ID=33563839

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0411726A BRPI0411726B8 (pt) 2003-06-24 2004-06-18 composto monoidrato cristalino do sal de di-hidrogenofosfato de (2r)-4-oxo-4-[3-(trifluorometil)-5,6-diidro[1,2,4]triazol[4,3-a]pirazin-7-(8h)-il]-1 -(2,4,5-trifluorofenil) butan-2-amina, processo para preparar o composto, e, uso do composto

Country Status (40)

Country Link
US (1) US7326708B2 (pt)
EP (1) EP1654263B2 (pt)
JP (1) JP4463768B2 (pt)
KR (2) KR101013431B1 (pt)
CN (1) CN100430397C (pt)
AR (2) AR044705A1 (pt)
AT (1) ATE373003T1 (pt)
AU (1) AU2004253889B2 (pt)
BR (1) BRPI0411726B8 (pt)
CA (1) CA2529400C (pt)
CO (1) CO5660266A2 (pt)
CR (1) CR8117A (pt)
CY (1) CY1106936T1 (pt)
DE (1) DE602004008938T3 (pt)
DK (1) DK1654263T4 (pt)
DO (1) DOP2004000941A (pt)
EA (1) EA009042B1 (pt)
EC (1) ECSP056245A (pt)
ES (1) ES2291907T5 (pt)
GE (1) GEP20084489B (pt)
HR (1) HRP20070534T4 (pt)
IL (1) IL172563A (pt)
IS (1) IS2792B (pt)
JO (1) JO2625B1 (pt)
MA (1) MA27861A1 (pt)
ME (1) ME00405B (pt)
MX (1) MXPA05013931A (pt)
MY (1) MY139595A (pt)
NO (1) NO335371B1 (pt)
NZ (1) NZ544026A (pt)
PE (1) PE20050696A1 (pt)
PL (1) PL1654263T5 (pt)
PT (1) PT1654263E (pt)
RS (1) RS51873B (pt)
SI (1) SI1654263T2 (pt)
TN (1) TNSN05329A1 (pt)
TW (1) TWI347185B (pt)
UA (1) UA86026C2 (pt)
WO (1) WO2005003135A1 (pt)
ZA (1) ZA200509933B (pt)

Families Citing this family (180)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EE05643B1 (et) * 2001-02-24 2013-04-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Ksantiini derivaadid, nende valmistamine ja kasutamine ravimina
CN1723196A (zh) 2001-06-27 2006-01-18 史密丝克莱恩比彻姆公司 作为二肽酶抑制剂的氟代吡咯烷
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
CA2508947A1 (en) * 2002-12-20 2004-07-15 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
CA2518465A1 (en) * 2003-03-25 2004-10-14 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7638638B2 (en) 2003-05-14 2009-12-29 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
DE602004021603D1 (de) * 2003-07-25 2009-07-30 Conjuchem Biotechnologies Inc Insulinderivative mit langanhaltender wirkung und verfahren zu deren herstellung
US7678909B1 (en) 2003-08-13 2010-03-16 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7169926B1 (en) 2003-08-13 2007-01-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
KR20060041309A (ko) 2003-08-13 2006-05-11 다케다 야쿠힌 고교 가부시키가이샤 ４-피리미돈 유도체 및 펩티딜 펩티다제 저해제로서의 그의용도
US20060287528A1 (en) * 2003-09-02 2006-12-21 Wenslow Robert M Novel crystalline forms of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
WO2005030751A2 (en) * 2003-09-08 2005-04-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
JP2007505121A (ja) * 2003-09-08 2007-03-08 武田薬品工業株式会社 ジペプチジルぺプチダーゼ阻害剤
WO2005030127A2 (en) * 2003-09-23 2005-04-07 Merck & Co., Inc. Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
US20080227786A1 (en) * 2004-01-16 2008-09-18 Ferlita Russell R Novel Crystalline Salts of a Dipeptidyl Peptidase-IV Inhibitor
US7501426B2 (en) 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EA013427B1 (ru) * 2004-03-15 2010-04-30 Такеда Фармасьютикал Компани Лимитед Ингибиторы дипептидилпептидазы
JP2008501714A (ja) * 2004-06-04 2008-01-24 武田薬品工業株式会社 ジペプチジルペプチダーゼインヒビター
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
TW200608967A (en) 2004-07-29 2006-03-16 Sankyo Co Pharmaceutical compositions containing with diabetic agent
WO2006033848A1 (en) * 2004-09-15 2006-03-30 Merck & Co., Inc. Amorphous form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
DE102004054054A1 (de) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
EP1828192B1 (en) * 2004-12-21 2014-12-03 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
DOP2006000008A (es) 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
US20090221592A1 (en) * 2005-07-25 2009-09-03 Ellison Martha E Dodecylsulfate Salt Of A Dipeptidyl Peptidase-Iv Inhibitor
DE102005035891A1 (de) 2005-07-30 2007-02-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
TW200738245A (en) * 2005-08-22 2007-10-16 Sankyo Co Pharmaceutical composition containing FBPase inhibitor
AU2006290205B2 (en) * 2005-09-14 2012-12-13 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors for treating diabetes
PL1931350T5 (pl) * 2005-09-14 2021-11-15 Takeda Pharmaceutical Company Limited Podanie inhibitorów dipeptydylo-peptydazy
TW200745079A (en) * 2005-09-16 2007-12-16 Takeda Pharmaceuticals Co Polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and methods of use therefor
CA2622642C (en) 2005-09-16 2013-12-31 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
TW200745080A (en) * 2005-09-16 2007-12-16 Takeda Pharmaceuticals Co Polymorphs of tartrate salt of 2-[2-(3-(R)-amino-piperidin-1-yl)-5-fluoro-6-oxo-6H-pyrimidin-1-ylmethyl]-benzonitrile and methods of use therefor
TW200738266A (en) * 2005-09-29 2007-10-16 Sankyo Co Pharmaceutical agent containing insulin resistance improving agent
US20090156579A1 (en) * 2005-10-25 2009-06-18 Hasegawa Philip A Combination of a Dipeptidyl Peptidase-4 Inhibitor and an Anti-Hypertensive Agent for the Treatment of Diabetes and Hypertension
US20100029941A1 (en) * 2006-03-28 2010-02-04 Takeda Pharmaceutical Company Limited Preparation of (r)-3-aminopiperidine dihydrochloride
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
PE20071221A1 (es) * 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
ES2354390T3 (es) * 2006-04-11 2011-03-14 Arena Pharmaceuticals, Inc. Procedimientos de uso del receptor gpr119 para identificar compuestos útiles para aumentar la masa ósea en un individuo.
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
CN102838599A (zh) 2006-05-04 2012-12-26 贝林格尔.英格海姆国际有限公司 多晶型
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
EP2056673A4 (en) * 2006-08-17 2010-06-16 Wellstat Therapeutics Corp COMBINATION TREATMENT FOR METABOLISM DISEASES
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
WO2008141021A1 (en) 2007-05-08 2008-11-20 Concert Pharmaceuticals, Inc. Deuterated derivatives of tetrahydrotriazolopyrazine compounds and their use as dpp-iv inhibitors
CN101357922B (zh) * 2007-08-02 2011-05-18 山东轩竹医药科技有限公司 新的dpp-iv抑制剂
PE20090938A1 (es) 2007-08-16 2009-08-08 Boehringer Ingelheim Int Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo
CN101397300B (zh) * 2007-09-04 2011-04-27 山东轩竹医药科技有限公司 二肽酶-ⅳ抑制剂衍生物
US8334385B2 (en) 2007-11-02 2012-12-18 Glenmark Generics Limited Process for the preparation of R-sitagliptin and its pharmaceutically acceptable salts thereof
US20090221595A1 (en) * 2007-11-26 2009-09-03 Nurit Perlman Crystalline form of sitagliptin
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
EP2249643A4 (en) * 2008-02-05 2013-10-09 Merck Sharp & Dohme PHARMACEUTICAL COMPOSITIONS OF A COMBINATION OF METFORMIN AND A DIPEPTIDYL PEPTIDASE IV HEMMER
CN101959406A (zh) * 2008-03-04 2011-01-26 默沙东公司 二甲双胍和二肽基肽酶-ⅳ抑制剂的组合的药物组合物
WO2009120746A2 (en) * 2008-03-25 2009-10-01 Teva Pharmaceutical Industries Ltd. Crystalline forms of sitagliptin phosphate
US20090247532A1 (en) * 2008-03-28 2009-10-01 Mae De Ltd. Crystalline polymorph of sitagliptin phosphate and its preparation
PE20091730A1 (es) 2008-04-03 2009-12-10 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
EP2146210A1 (en) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
US20090264476A1 (en) * 2008-04-18 2009-10-22 Mckelvey Craig CB-1 receptor modulator formulations
US8003672B2 (en) * 2008-04-21 2011-08-23 Merck Sharp & Dohme Corp. CB-1 receptor modulator formulations
RU2519717C2 (ru) 2008-07-03 2014-06-20 Рациофарм Гмбх Кристаллические соли ситаглиптина
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
KR20200118243A (ko) 2008-08-06 2020-10-14 베링거 인겔하임 인터내셔날 게엠베하 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료
MX370599B (es) 2008-08-15 2019-12-18 Boehringer Ingelheim Int Derivados de purina para su uso en el tratamiento de enfermedades relacionadas con fab.
EP2331545B1 (en) 2008-08-27 2013-10-02 Cadila Healthcare Limited Improved process for preparation of (2r)-4-oxo-4-[3- (trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-a]pyrazin- 7(8h)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine&new impurities in preparation thereof
BRPI0919288A2 (pt) 2008-09-10 2015-12-15 Boehring Ingelheim Internat Gmbh teriapia de combinação para tratamento de diabetes e condições relacionadas.
US8563517B2 (en) * 2008-09-12 2013-10-22 Cadila Pharmaceuticals Limited Dipeptidyl peptidase IV (DP-IV) compounds
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
EA022310B1 (ru) 2008-12-23 2015-12-30 Бёрингер Ингельхайм Интернациональ Гмбх Солевые формы органического соединения
AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
TWI466672B (zh) 2009-01-29 2015-01-01 Boehringer Ingelheim Int 小兒科病人糖尿病之治療
EP2218721A1 (en) 2009-02-11 2010-08-18 LEK Pharmaceuticals d.d. Novel salts of sitagliptin
NZ619520A (en) 2009-02-13 2015-06-26 Boehringer Ingelheim Int Antidiabetic medications comprising a dpp-4 inhibitor (linagliptin) optionally in combination with other antidiabetics
PL2395983T3 (pl) 2009-02-13 2020-09-07 Boehringer Ingelheim International Gmbh Kompozycja farmaceutyczna zawierająca inhibitor sglt2, inhibitor dpp-iv i ewentualnie dalszy środek przeciwcukrzycowy oraz jej zastosowania
SG173815A1 (en) 2009-02-26 2011-09-29 Codexis Inc Transaminase biocatalysts
CA2757241A1 (en) 2009-03-30 2010-10-14 Teva Pharmaceutical Industries Ltd. Solid state forms of sitagliptin salts
WO2010122578A2 (en) * 2009-04-20 2010-10-28 Msn Laboratories Limited Process for the preparation of sitagliptin and its intermediates
AU2010247193B2 (en) * 2009-05-11 2016-05-19 Tianish Laboratories Private Limited Sitagliptin synthesis
WO2010131035A1 (en) * 2009-05-11 2010-11-18 Generics [Uk] Limited Novel crystalline polymorph of sitagliptin dihydrogen phosphate
CN101899047B (zh) * 2009-05-26 2016-01-20 盛世泰科生物医药技术(苏州)有限公司 作为二肽基肽酶抑制剂用于治疗或预防糖尿病的β-氨基四氢吡嗪、四氢嘧啶和四氢吡啶
CN101899048B (zh) * 2009-05-27 2013-04-17 上海恒瑞医药有限公司 (R)-7-[3-氨基-4-(2,4,5-三氟-苯基)-丁酰]-3-三氟甲基-5,6,7,8-四氢-咪唑并[1,5-a]吡嗪-1-羧酸甲酯的盐
ES2644992T3 (es) 2009-06-22 2017-12-01 Codexis, Inc. Reacciones de transaminasa
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
AU2010283689B2 (en) 2009-08-13 2016-07-14 Sandoz Ag Crystalline compound of 7-[(3R)-3-amino-1-oxo-4-(2, 4, 5-trifluorphenyl)butyl]-5, 6, 7, 8-tetrahydro-3-(tri fluormethyl)-1, 2, 4 -triazolo[4,3-a]pyrazine
EP2295083A1 (de) 2009-09-15 2011-03-16 Ratiopharm GmbH Pharmazeutische Zusammensetzung mit den Wirkstoffen Metformin und Sitagliptin oder Vildagliptin
NZ599298A (en) 2009-11-27 2014-11-28 Boehringer Ingelheim Int Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin
US9305057B2 (en) * 2009-12-28 2016-04-05 Oracle International Corporation Extensible indexing framework using data cartridges
KR101156587B1 (ko) * 2010-02-19 2012-06-20 한미사이언스 주식회사 시타글립틴의 제조방법 및 이에 사용되는 아민염 중간체
EP2547339A1 (en) 2010-03-18 2013-01-23 Boehringer Ingelheim International GmbH Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions
WO2011123641A1 (en) 2010-03-31 2011-10-06 Teva Pharmaceutical Industries Ltd. Solid state forms of sitagliptin salts
MX2012011631A (es) 2010-04-06 2013-01-18 Arena Pharm Inc Moduladores del receptor gpr119 y el tratamiento de trastornos relacionados con el mismo.
WO2011138421A1 (en) 2010-05-05 2011-11-10 Boehringer Ingelheim International Gmbh Combination therapy
NZ603319A (en) 2010-06-24 2015-04-24 Boehringer Ingelheim Int Diabetes therapy
ES2860676T3 (es) * 2010-07-23 2021-10-05 Gruenenthal Gmbh Sales o cocristales de 3- (3-dimetilamino-1-etil-2-metil-propil) -fenol
US8932836B2 (en) 2010-08-16 2015-01-13 Codexis, Inc. Biocatalysts and methods for the synthesis of (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine
WO2012025944A2 (en) 2010-08-27 2012-03-01 Usv Limited Sitagliptin, salts and polymorphs thereof
MX2013003184A (es) 2010-09-22 2013-06-07 Arena Pharm Inc Moduladores del receptor gpr119 y el tratamiento de transtornos relacionados con el mismo.
CN101973997B (zh) * 2010-09-30 2012-06-06 浙江大学 一种磷酸西他列汀侧链的制备方法
CN103201260B (zh) * 2010-11-11 2015-05-27 莱德克斯制药有限公司 药物衍生物
AR083878A1 (es) 2010-11-15 2013-03-27 Boehringer Ingelheim Int Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento
CN102485718B (zh) * 2010-12-03 2014-03-26 浙江海翔药业股份有限公司 西他列汀的中间体及其制备方法
WO2012076973A2 (en) 2010-12-09 2012-06-14 Aurobindo Pharma Limited Novel salts of dipeptidyl peptidase iv inhibitor
US9108972B2 (en) 2011-03-03 2015-08-18 Cadila Healthcare Limited Salts of DPP-IV inhibitor
SI2691083T1 (sl) 2011-03-29 2017-12-29 Krka, D.D., Novo Mesto Farmacevtski sestavek sitagliptina
WO2012135570A1 (en) 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145361A1 (en) 2011-04-19 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140038889A1 (en) 2011-04-22 2014-02-06 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
US20140051714A1 (en) 2011-04-22 2014-02-20 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
US8524936B2 (en) 2011-05-18 2013-09-03 Milan Soukup Manufacturing process for sitagliptin from L-aspartic acid
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012174164A2 (en) * 2011-06-15 2012-12-20 Metabolex, Inc. Agonists of gpr131 and uses thereof
MX348130B (es) 2011-06-24 2017-05-26 Merck Sharp & Dohme Transaminasas inmovilizadas y procedimiento para la preparacion y uso de transaminasa inmovilizada.
CA2840814A1 (en) 2011-06-29 2013-01-03 Ranbaxy Laboratories Limited Solid dispersions of sitagliptin and processes for their preparation
EP2726075A4 (en) 2011-06-29 2014-11-19 Merck Sharp & Dohme NEW CRYSTALLINE FORMS OF A DIPEPTIDYL-PEPTIDASE IV HEMMER
EP2726483A1 (en) 2011-06-30 2014-05-07 Ranbaxy Laboratories Limited Novel salts of sitagliptin
CA2841552C (en) 2011-07-15 2020-06-23 Boehringer Ingelheim International Gmbh Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions
SI2736909T1 (sl) 2011-07-27 2017-08-31 Farma Grs, D.O.O. Proces za pripravo sitagliptina in njegovih farmacevtsko sprejemljivih soli
US9593109B2 (en) 2011-08-26 2017-03-14 Cymabay Therapeutics, Inc. Bicyclic agonists of GPR131 and uses thereof
EP2753328A1 (en) 2011-09-07 2014-07-16 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Dpp-iv inhibitor formulations
PL2578208T3 (pl) 2011-10-06 2014-10-31 Sanovel Ilac Sanayi Ve Ticaret As Stałe formulacje dawkowane inhibitora DPP-IV
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
CN106905321A (zh) 2011-10-14 2017-06-30 劳乐斯实验室私营有限公司 新的西他列汀盐、其制备方法及其药物组合物
WO2013084210A1 (en) 2011-12-08 2013-06-13 Ranbaxy Laboratories Limited Amorphous form of sitagliptin salts
ES2421956B1 (es) 2012-03-02 2014-09-29 Moehs Ibérica S.L. Nueva forma cristalina de sulfato de sitagliptina
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
EP3685839A1 (en) 2012-05-14 2020-07-29 Boehringer Ingelheim International GmbH Linagliptin for use in the treatment of albuminuria and kidney related diseases
US20130303554A1 (en) 2012-05-14 2013-11-14 Boehringer Ingelheim International Gmbh Use of a dpp-4 inhibitor in sirs and/or sepsis
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
CN103421011B (zh) * 2012-05-25 2017-08-08 浙江海翔药业股份有限公司 一种制备磷酸西他列汀无水晶型i的方法
EP2882752A1 (en) 2012-08-08 2015-06-17 Cipla Limited Process for the preparation of sitagliptin and intermediate compounds
CN102898387B (zh) * 2012-09-26 2015-01-07 浙江工业大学 管道化连续生产n-[(2z)-哌嗪-2-亚基]-2,2,2-三氟乙酰肼的方法
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
HUE042206T2 (hu) 2013-02-28 2019-06-28 Codexis Inc Módosított transzamináz polipeptidek ipari biokatalízishez
EP2961838B1 (en) 2013-02-28 2018-04-18 Merck Sharp & Dohme Corp. Immobilized transaminases and process for making and using immobilized transaminase
EP2970927A4 (en) 2013-03-15 2016-10-12 Merck Sharp & Dohme IMMOBILIZED KETOREDUCASTASES AND METHOD FOR THE PRODUCTION AND USE OF IMMOBILIZED KETOREDUCASTASES
IN2013MU00916A (pt) 2013-03-20 2015-06-26 Cadila Healthcare Ltd
WO2014147641A2 (en) * 2013-03-21 2014-09-25 Laurus Labs Private Limited Sitagliptin pterostilbene phosphate salt, process for the preparation and pharmaceutical composition thereof
WO2015001568A2 (en) * 2013-07-01 2015-01-08 Laurus Labs Private Limited Sitagliptin lipoate salt, process for the preparation and pharmaceutical composition thereof
CN103387577A (zh) * 2013-07-29 2013-11-13 迪沙药业集团山东迪沙药业有限公司 西格列汀碱的不对称合成方法
CN103483218B (zh) * 2013-09-24 2015-06-03 浙江永太科技股份有限公司 一种1-(氯乙酰基)-2-(三氟乙酰基)肼的制备方法
CZ2013842A3 (cs) * 2013-11-01 2015-05-13 Zentiva, K.S. 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
ES2704501T3 (es) 2013-12-17 2019-03-18 Sun Pharmaceutical Ind Ltd Procedimiento para la preparación de fumarato de sitagliptina cristalino
IN2014MU00212A (pt) 2014-01-21 2015-08-28 Cadila Healthcare Ltd
EP3102187B1 (en) 2014-02-03 2020-03-25 Galenicum Health S.L. Stable pharmaceutical compositions containing sitagliptin in the form of immediate release tablets
IN2014MU00651A (pt) 2014-02-25 2015-10-23 Cadila Healthcare Ltd
ES2950384T3 (es) 2014-02-28 2023-10-09 Boehringer Ingelheim Int Uso médico de un inhibidor de DPP-4
WO2015153485A1 (en) 2014-04-01 2015-10-08 The Research Foundation For The State University Of New York Electrode materials for group ii cation-based batteries
CA2945681A1 (en) * 2014-04-17 2015-10-22 Merck Sharp & Dohme Corp. Sitagliptin tannate complex
JP6574474B2 (ja) 2014-07-21 2019-09-11 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． キラルジペプチジルペプチダーゼ−ｉｖ阻害剤の製造方法
EP3242879B1 (en) 2015-01-08 2019-12-11 Lee Pharma Ltd. Novel process for the preparation of dipeptidyl peptidase-4 (dpp-4) enzyme inhibitor
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
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
HK1249847A1 (zh) 2015-03-09 2018-11-16 Intekrin Therapeutics, Inc. 用於治疗非酒精性脂肪肝疾病和/或脂肪营养不良的方法
WO2016162877A1 (en) * 2015-04-09 2016-10-13 Finochem Limited Harman "a process for preparing 7-[(3r)-3-amino-l-oxo-4-(2,4,5trifluorophenyl)butyi]- 5,6,7,8-tetrahydro-3-(trifluoromethyl)-l,2,4-triazolo[4,3-a]pyrazine hydrochloride monohydrate and its crystalline form"
US9732035B2 (en) * 2015-07-24 2017-08-15 Newlink Genetics Corporation Salts and prodrugs of 1-methyl-D-tryptophan
CN105017260B (zh) * 2015-07-30 2017-04-19 新发药业有限公司 一种西他列汀中间体三唑并吡嗪衍生物的制备方法
CN105175422B (zh) * 2015-09-18 2018-04-20 深圳市海滨制药有限公司 一种磷酸西格列汀晶体及其制备方法和用途
KR20170036288A (ko) 2015-09-24 2017-04-03 주식회사 종근당 시타글립틴의 신규염 및 이의 제조방법
WO2017211979A1 (en) 2016-06-10 2017-12-14 Boehringer Ingelheim International Gmbh Combinations of linagliptin and metformin
MX2016016260A (es) 2016-12-08 2018-06-07 Alparis Sa De Cv Nuevas formas solidas de sitagliptina.
KR20200036808A (ko) 2017-04-03 2020-04-07 코히러스 바이오사이언시스, 인크. 진행성 핵상 마비 치료를 위한 PPARγ 작용제
EP3456320A1 (de) * 2017-09-15 2019-03-20 Stada Arzneimittel Ag Dpp-4-inhibitor-mono-zusammensetzung
US11096890B2 (en) 2017-09-29 2021-08-24 Merck Sharp & Dohme Corp. Chewable dosage forms containing sitagliptin and metformin
CN109651373A (zh) * 2017-10-11 2019-04-19 江苏瑞科医药科技有限公司 一种西格列汀磷酸盐单水合物晶型的制备方法
KR20190060235A (ko) 2017-11-24 2019-06-03 제일약품주식회사 시타글립틴 캄실산염의 제조방법
TR201722603A2 (tr) 2017-12-28 2019-07-22 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Metformi̇n ve si̇tagli̇pti̇n i̇çeren sicak eri̇tme ekstrüzyonu i̇le gerçekleşti̇ri̇len tablet formülasyonlari
EP4045048A4 (en) 2019-10-14 2023-05-24 Santa Farma Ilaç Sanayi A.S. ORAL FORMULATIONS WITH SITAGLIPTIN HCI MONOHYDRATE WITH IMPROVED PHARMACEUTICAL PROPERTIES
EP3811930A1 (en) 2019-10-24 2021-04-28 Authenda Pharmaceuticals AG Oral gliptin compositions and method for preparation thereof
CN113061594B (zh) 2019-12-31 2023-11-24 弈柯莱生物科技(集团)股份有限公司 转氨酶突变体、固定化转氨酶及用于制备西他列汀的用途
CN114262331A (zh) * 2020-09-16 2022-04-01 江苏万邦生化医药集团有限责任公司 一种西格列汀磷酸盐一水合物的制备方法
AU2022263996A1 (en) 2021-04-27 2023-11-02 Aardvark Therapeutics, Inc. Combination of bitter receptor agonist and gut-signaling compound
EP4604931A1 (en) 2022-10-21 2025-08-27 Merck Sharp & Dohme LLC Compositions of a dipeptidyl peptidase-iv inhibitor and an antioxidant
CN115671109A (zh) * 2022-11-23 2023-02-03 辽宁康辰诺信医药科技有限公司 磷酸西格列汀的用途
EP4630568A1 (en) 2022-12-09 2025-10-15 KRKA, D.D., Novo Mesto Process for the preparation of sitagliptin
CN116064457B (zh) 2022-12-16 2025-08-19 浙江工业大学 一种ω-转氨酶突变体及其应用
EP4431087A1 (en) 2023-03-14 2024-09-18 Sanovel Ilac Sanayi Ve Ticaret A.S. A film coated tablet of sitagliptin or a pharmaceutically acceptable salt thereof
CN116473971A (zh) * 2023-05-11 2023-07-25 宙晟智维生命科学(上海)有限公司 一种含西格列汀的药物组合物的制备方法及包衣片
EP4563143A1 (en) 2023-11-30 2025-06-04 Sanovel Ilac Sanayi ve Ticaret A.S. A bilayer tablet formulation of metformin and sitagliptin comprising antioxidant
EP4566593A1 (en) 2023-11-30 2025-06-11 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi A tablet comprising an extended-release formulation for metformin and immediate release formulation comprising sitagliptin

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6479692B1 (en) * 2001-05-02 2002-11-12 Nobex Corporation Methods of synthesizing acylanilides including bicalutamide and derivatives thereof
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
US20060287528A1 (en) * 2003-09-02 2006-12-21 Wenslow Robert M Novel crystalline forms of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
WO2005030127A2 (en) * 2003-09-23 2005-04-07 Merck & Co., Inc. Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
US20080227786A1 (en) 2004-01-16 2008-09-18 Ferlita Russell R Novel Crystalline Salts of a Dipeptidyl Peptidase-IV Inhibitor
WO2006033848A1 (en) 2004-09-15 2006-03-30 Merck & Co., Inc. Amorphous form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor

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Free format text: PROCESSO INPI NO 52402.006669/2023-81 9A VARA FEDERAL DO RIO DE JANEIRO - PROCEDIMENTO COMUM NO 5064194-46.2023.4.02.5101/RJ AUTOR: SUN FARMACEUTICA DO BRASIL LTDA REU: INPI-INSTITUTO NACIONAL DA PROPRIEDADE INDUSTRIAL REU: MERCK SHARP AND DOHME LLC. SENTENCA: HOMOLOGO, POR SENTENCA, PARA QUE PRODUZA OS SEUS JURIDICOS E LEGAIS EFEITOS, O ACORDO FIRMADO ENTRE A AUTORA E A EMPRESA RE, CONFORME PECA DO EVENTO 55, EM QUE A DEMANDANTE "RENUNCIA A PRETENSAO FORMULADA NA ACAO", SEM OPOSICAO DO INPI (EVENTO 60), JULGANDO EXTINTO O PROCESSO, COM RESOLUCAO DO MERITO, NOS MOLDES DO ARTIGO 487, III, "B" E "C" DO CODIGO DE PROCESSO CIVIL. TRANSITADO EM JULGADO - DATA: 17/06/2025.