DK2505579T3 - Fremgangsmåder og forbindelser til fremstilling af dipeptidylpeptidase IV-inhibitorer og mellemprodukter deraf - Google Patents

Fremgangsmåder og forbindelser til fremstilling af dipeptidylpeptidase IV-inhibitorer og mellemprodukter deraf Download PDF

Info

Publication number
DK2505579T3
DK2505579T3 DK12162633.7T DK12162633T DK2505579T3 DK 2505579 T3 DK2505579 T3 DK 2505579T3 DK 12162633 T DK12162633 T DK 12162633T DK 2505579 T3 DK2505579 T3 DK 2505579T3
Authority
DK
Denmark
Prior art keywords
formula
acetic acid
added
decane
hydroxytricyclo
Prior art date
Application number
DK12162633.7T
Other languages
English (en)
Inventor
Truc Chi Vu
Sergei V Kolotuchin
Jianji Wang
Kwok Wong
Jurong Yu
John A Mazzullo Jr
Jason Zhu
Original Assignee
Astrazeneca Ab
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=32507798&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DK2505579(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Application granted granted Critical
Publication of DK2505579T3 publication Critical patent/DK2505579T3/da

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/74—Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C69/757—Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/28—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C62/00—Compounds having carboxyl groups bound to carbon atoms of rings other than six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C62/02—Saturated compounds containing hydroxy or O-metal groups
    • C07C62/06—Saturated compounds containing hydroxy or O-metal groups polycyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/62—Halogen-containing esters
    • C07C69/63—Halogen-containing esters of saturated acids
    • C07C69/635—Halogen-containing esters of saturated acids containing rings in the acid moiety
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/67—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids
    • C07C69/675—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids of saturated hydroxy-carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/56—Ring systems containing bridged rings
    • C07C2603/58—Ring systems containing bridged rings containing three rings
    • C07C2603/70—Ring systems containing bridged rings containing three rings containing only six-membered rings
    • C07C2603/74—Adamantanes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Indole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (4)

1. Fremgangsmåde til fremstilling af en cyclopropylfusioneret pyrrolidinbaseret inhibitor af dipeptidylpeptidase IV, der omfatter: (a) kobling af (aS)-a-[[(1,1-dimethylethoxy)carbonyl]amino]-3- hydroxytricyclo [3.3.1.13'7] decan-l-eddikesyre eller dens 1,4-diazabicyclo[2.2.2]octansalt til (IS,3S,5S)-2- azabicyclo[3.1.0]hexan-3-carboxamid til fremstilling af 3-(aminocarbonyl) -aS) -a- (3-hydroxytricyclo [3.3.1.13'7] dec-l-yl) -β-οχο-(IS,3S,5S)-2-azabicyclo[3.1.0]hexan-2-ethancarbaminsyre, 1,1-dimethylethylester; (b) dehydrering af 3-(aminocarbonyl) - (aS)-ex-(3- hydroxytricyclo [3.3.l.l3'7] dec-l-yl) - β-οχο- (lS,3S,5S)-2-azabicyclo[3.1.0]hexan-2-ethancarbaminsyre, 1,1-dimethylethylester til fremstilling af 3-cyano-(aS)-a- (3-hydroxytricyclo [3.3.1.13'7] dec-l-yl) - β-οχο- (lS,3S,5S)-2-azabicyclo[3.1.0]hexan-2-ethancarbaminsyre, 1,1-dimethylethylester; og (c) afbeskyttelse af 3-cyano-(aS)-a-(3- hydroxytricyclo [3.3.1.13'7]dec-l-yl)^-oxo-(lS,3S,5S)-2-azabicyclo[3.1.0]hexan-2-ethancarbaminsyre, 1,1-dimethylethylester til frembringelse af dipeptidylpeptidase IV-inhibitoren.
2. Fremgangsmåde til fremstilling af en fri baseforbindelse med struktur M'
M' som omfatter tilvejebringelse af en beskyttet forbindelse med struktur L
L og behandling af forbindelse L med saltsyre til frembringelse af det tilsvarende saltsyresalt L'
L' behandling af saltsyresaltet L' med saltsyre og natriumhydroxid til frembringelse af den fri baseforbindelse M' .
3. Fremgangsmåde ifølge krav 2, hvor forbindelse L frembringes ved
dehydrering af mellemprodukt K i nærvær af pyridin og trifluoreddikesyreanhydrid og efterfølgende hydrolysering af reaktionsproduktet i nærvær af en kraftig base til frembringelse af forbindelse L.
4. Fremgangsmåde til fremstilling af et monohydrat med struktur M"
WT der omfatter behandling af en fri base med strukturen
M' med vand til frembringelse af monohydratet M".
DK12162633.7T 2002-12-09 2003-12-04 Fremgangsmåder og forbindelser til fremstilling af dipeptidylpeptidase IV-inhibitorer og mellemprodukter deraf DK2505579T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US43181402P 2002-12-09 2002-12-09
EP03812799.9A EP1581487B1 (en) 2002-12-09 2003-12-04 Methods and compounds for producing dipeptidyl peptidase iv inhibitors and intermediates thereof

Publications (1)

Publication Number Publication Date
DK2505579T3 true DK2505579T3 (da) 2015-01-19

Family

ID=32507798

Family Applications (4)

Application Number Title Priority Date Filing Date
DK03812799.9T DK1581487T3 (da) 2002-12-09 2003-12-04 Fremgangsmåder og forbindelser til produktion af dipeptidylpeptidase iv-inhibitorer og mellemprodukter deraf
DK12162624.6T DK2517706T3 (da) 2002-12-09 2003-12-04 Fremgangsmåder og forbindelser til produktion af dipeptidylpeptidase iv-inhibitorer og mellemprodukter deraf
DK12162633.7T DK2505579T3 (da) 2002-12-09 2003-12-04 Fremgangsmåder og forbindelser til fremstilling af dipeptidylpeptidase IV-inhibitorer og mellemprodukter deraf
DK12162626.1T DK2505578T3 (da) 2002-12-09 2003-12-04 Fremgangsmåder og forbindelser til fremstilling af dipeptidylpeptidase IV-inhibitorer og mellemprodukter deraf

Family Applications Before (2)

Application Number Title Priority Date Filing Date
DK03812799.9T DK1581487T3 (da) 2002-12-09 2003-12-04 Fremgangsmåder og forbindelser til produktion af dipeptidylpeptidase iv-inhibitorer og mellemprodukter deraf
DK12162624.6T DK2517706T3 (da) 2002-12-09 2003-12-04 Fremgangsmåder og forbindelser til produktion af dipeptidylpeptidase iv-inhibitorer og mellemprodukter deraf

Family Applications After (1)

Application Number Title Priority Date Filing Date
DK12162626.1T DK2505578T3 (da) 2002-12-09 2003-12-04 Fremgangsmåder og forbindelser til fremstilling af dipeptidylpeptidase IV-inhibitorer og mellemprodukter deraf

Country Status (17)

Country Link
US (4) US7420079B2 (da)
EP (5) EP2792672A3 (da)
JP (6) JP4886193B2 (da)
KR (1) KR20050088309A (da)
CN (3) CN102070451B (da)
AU (1) AU2003297647A1 (da)
BR (1) BR0317139A (da)
CA (1) CA2508619A1 (da)
DK (4) DK1581487T3 (da)
ES (4) ES2484915T3 (da)
IL (1) IL192912A0 (da)
MX (1) MXPA05005970A (da)
PL (1) PL377123A1 (da)
PT (4) PT1581487E (da)
SI (4) SI2505578T1 (da)
TW (2) TW200914419A (da)
WO (1) WO2004052850A2 (da)

Families Citing this family (127)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0487425A (ja) * 1990-07-31 1992-03-19 Fujitsu Ltd 回線切り替え装置
US7420079B2 (en) * 2002-12-09 2008-09-02 Bristol-Myers Squibb Company Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof
US6995183B2 (en) 2003-08-01 2006-02-07 Bristol Myers Squibb Company Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
KR20170005163A (ko) 2003-11-17 2017-01-11 노파르티스 아게 디펩티딜 펩티다제 ⅳ 억제제의 용도
EP2165703A3 (en) 2004-01-20 2012-03-28 Novartis Pharma AG Direct compression formulation and process
TW200538122A (en) 2004-03-31 2005-12-01 Bristol Myers Squibb Co Process for preparing a dipeptidyl peptidase Ⅳ inhibitor and intermediates employed therein
US7741082B2 (en) * 2004-04-14 2010-06-22 Bristol-Myers Squibb Company Process for preparing dipeptidyl peptidase IV inhibitors and intermediates therefor
TW200536827A (en) 2004-05-04 2005-11-16 Bristol Myers Squibb Co Enzymatic ammonolysis process for the preparation of intermediates for DPP IV inhibitors
US7214702B2 (en) * 2004-05-25 2007-05-08 Bristol-Myers Squibb Company Process for producing a dipeptidyl peptidase IV inhibitor
DE102004035978A1 (de) * 2004-07-23 2006-03-16 Justus-Liebig-Universität Giessen Aminoadamantan-Verbindungen
US20060035954A1 (en) * 2004-08-11 2006-02-16 Sharma Padam N Ammonolysis process for the preparation of intermediates for DPP IV inhibitors
US7250529B2 (en) 2004-09-17 2007-07-31 Albemarle Corporation Synthesis process for 2-(3-hydroxy-1-adamantyl)-2-oxoacetic acid
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
WO2006107963A2 (en) * 2005-04-06 2006-10-12 Novartis Ag Process for preparing dipeptide amides
US7205432B2 (en) * 2005-05-31 2007-04-17 Kemfine Oy Process for the preparation of adamantane derivatives
FI120765B (fi) * 2005-05-31 2010-02-26 Kemfine Group Ltd Menetelmä adamantaanijohdannaisten valmistamiseksi
MY152185A (en) 2005-06-10 2014-08-29 Novartis Ag Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation
DK1942898T4 (da) 2005-09-14 2014-06-02 Takeda Pharmaceutical Dipeptidylpeptidase-inhibitorer til behandling af diabetes
KR101368988B1 (ko) 2005-09-16 2014-02-28 다케다 야쿠힌 고교 가부시키가이샤 디펩티딜 펩티다제 억제제
GB0526291D0 (en) 2005-12-23 2006-02-01 Prosidion Ltd Therapeutic method
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
EP2007734A1 (en) 2006-04-12 2008-12-31 Probiodrug AG Enzyme inhibitors
CN101415676A (zh) * 2006-04-17 2009-04-22 住友化学株式会社 N-叔丁氧基羰基-2-吡咯烷酮类及其制造方法
JP5272324B2 (ja) * 2006-04-17 2013-08-28 住友化学株式会社 Ｎ−ｔｅｒｔ−ブトキシカルボニル−２−ピロリジノン類およびその製造方法
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
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
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
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
JP5667440B2 (ja) 2007-04-18 2015-02-12 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体
PE20090696A1 (es) * 2007-04-20 2009-06-20 Bristol Myers Squibb Co Formas cristalinas de saxagliptina y procesos para preparar las mismas
AU2008270438B2 (en) 2007-07-02 2013-10-10 F. Hoffmann-La Roche Ag Imidazole derivatives as CCR2 receptor antagonists
CL2008002427A1 (es) 2007-08-16 2009-09-11 Boehringer Ingelheim Int Composicion farmaceutica que comprende 1-cloro-4-(b-d-glucopiranos-1-il)-2-[4-((s)-tetrahidrofurano-3-iloxi)bencil]-benceno combinado con 1-[(4-metilquinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(r)-aminopiperidin-1-il)xantina; y su uso para tratar diabetes mellitus tipo 2.
US8338450B2 (en) * 2007-09-21 2012-12-25 Lupin Limited Compounds as dipeptidyl peptidase IV (DPP IV) inhibitors
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
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
BRPI0917675A2 (pt) 2008-08-15 2015-12-01 Boehringer Ingelheim Int compostos orgânicos para cura de ferida
WO2010059639A2 (en) * 2008-11-19 2010-05-27 Auspex Pharmaceuticals, Inc. Hydroxyadamantyl inhibitors of dipeptidylpeptidase iv
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
AR075204A1 (es) 2009-01-29 2011-03-16 Boehringer Ingelheim Int Inhibidores de dpp-4 y composiciones farmaceuticas que los comprenden, utiles para tratar enfermedades metabolicas en pacientes pediatricos, particularmente diabetes mellitus tipo 2
CN104906582A (zh) 2009-02-13 2015-09-16 勃林格殷格翰国际有限公司 包含sglt2抑制剂、dpp-iv抑制剂和任选的另一种抗糖尿病药的药物组合物及其用途
CN106177958A (zh) 2009-02-13 2016-12-07 勃林格殷格翰国际有限公司 包含dpp‑4抑制剂(利拉列汀)任选地组合其它抗糖尿病药的抗糖尿病药物
EA201101231A1 (ru) * 2009-03-27 2012-06-29 Бристол-Майерс Сквибб Компани Способы предотвращения или снижения риска смертности
US8796466B2 (en) 2009-03-30 2014-08-05 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CN102459610B (zh) * 2009-04-08 2014-12-17 阿斯利康(瑞典)有限公司 表达pdh和fdh酶的遗传稳定性质粒
PL2417107T3 (pl) * 2009-04-09 2016-02-29 Sandoz Ag Krystaliczne postacie saksagliptyny
GB2483614B (en) 2009-06-18 2014-12-03 Lupin Ltd 2-Amino-2- [8-(dimethyl carbamoyl)- 8-aza- bicyclo [3.2.1] oct-3-yl]-exo- ethanoyl derivatives as potent dpp-iv inhibitors
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
SG178953A1 (en) 2009-09-11 2012-04-27 Probiodrug Ag Heterocylcic derivatives as inhibitors of glutaminyl cyclase
US20110274648A1 (en) 2009-11-11 2011-11-10 Bristol-Myers Squibb Company Hepatitis C Virus Inhibitors
US20110269956A1 (en) * 2009-11-11 2011-11-03 Bristol-Myers Squibb Company Hepatitis C Virus Inhibitors
AU2010323068B2 (en) 2009-11-27 2015-09-03 Boehringer Ingelheim International Gmbh Treatment of genotyped diabetic patients with DPP-IV inhibitors such as linagliptin
US8377980B2 (en) 2009-12-16 2013-02-19 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
FR2956400A1 (fr) 2010-02-15 2011-08-19 Finorga Procede de preparation de composes adamantyles
US9181233B2 (en) 2010-03-03 2015-11-10 Probiodrug Ag Inhibitors of glutaminyl cyclase
AU2011226074B2 (en) 2010-03-10 2015-01-22 Vivoryon Therapeutics N.V. Heterocyclic inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5)
WO2011113947A1 (en) 2010-03-18 2011-09-22 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
EP2368874A1 (en) 2010-03-26 2011-09-28 Sandoz AG Racemisation of (R)-N-Boc-3-hydroxyadamant-1-yl glycine
CN102918027A (zh) 2010-04-06 2013-02-06 艾尼纳制药公司 Gpr119受体调节剂和对与所述受体有关的障碍的治疗
US8541596B2 (en) 2010-04-21 2013-09-24 Probiodrug Ag Inhibitors
WO2011138421A1 (en) 2010-05-05 2011-11-10 Boehringer Ingelheim International Gmbh Combination therapy
EP2539321A1 (en) 2010-05-05 2013-01-02 Assia Chemical Industries Ltd. Saxagliptin intermediates, saxagliptin polymorphs, and processes for preparation thereof
KR20190050871A (ko) 2010-06-24 2019-05-13 베링거 인겔하임 인터내셔날 게엠베하 당뇨병 요법
WO2012031124A2 (en) 2010-09-03 2012-03-08 Bristol-Myers Squibb Company Drug formulations using water soluble antioxidants
WO2012028721A1 (en) 2010-09-03 2012-03-08 Sandoz Ag PROCESS FOR THE REDUCTIVE AMINATION OF α-KETO CARBOXYLIC ACIDS
BR112013008100A2 (pt) 2010-09-22 2016-08-09 Arena Pharm Inc "moduladores do receptor de gpr19 e o tratamento de distúrbios relacionados a eles."
EP2619195A1 (en) 2010-09-24 2013-07-31 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
EP2608788A1 (en) 2010-10-04 2013-07-03 Assia Chemical Industries Ltd. Polymorphs of saxagliptin hydrochloride and processes for preparing them
EP2670397B1 (en) 2011-02-01 2020-05-13 Bristol-Myers Squibb Company Pharmaceutical formulations including an amine compound
ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
WO2012135570A1 (en) 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140066369A1 (en) 2011-04-19 2014-03-06 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
US20140038889A1 (en) 2011-04-22 2014-02-06 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012162507A1 (en) 2011-05-24 2012-11-29 Apicore, Llc Process for preparing saxagliptin and its novel intermediates useful in the synthesis thereof
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2013081100A1 (ja) * 2011-11-30 2013-06-06 積水メディカル株式会社 アダマンチルヒダントイン化合物
ITMI20120842A1 (it) * 2012-05-16 2013-11-17 Chemelectiva S R L Intermedi utili per la preparazione di saxagliptina e processo per la loro preparazione
WO2013175395A2 (en) * 2012-05-21 2013-11-28 Dr. Reddys Laboratories Limited Improved process for preparation of saxagliptin and its salts
US8664443B2 (en) 2012-05-23 2014-03-04 Divi's Laboratories Ltd. Process for the preparation of (1S, 3S, 5S)-2-[2(S)-2-amino-2-(3-hydroxy-1-adamantan-1-yl) acetyl]-2-azabicyclo [3.1.0] hexane-3-carbonitrile
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
ES2690321T3 (es) 2012-05-24 2018-11-20 Apotex Inc. Sales de saxagliptina con ácidos orgánicos
EP2867206A2 (en) 2012-07-02 2015-05-06 Ranbaxy Laboratories Limited Saxagliptin salts
CN103539724B (zh) * 2012-07-12 2017-09-26 博瑞生物医药（苏州）股份有限公司 沙格列汀单一立体异构体的新晶型和纯化方法
WO2014057495A1 (en) 2012-10-11 2014-04-17 Lee Pharma Limited A process for industrial preparation of [(s)-n-tert butoxycarbonyl-3-hydroxy]adamantylglycine
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
WO2014108830A1 (en) 2013-01-10 2014-07-17 Wockhardt Limited A process for preparing pharmaceutically acceptable salt of saxagliptin
CN104098481B (zh) * 2013-04-10 2016-05-11 浙江九洲药物科技有限公司 一种沙格列汀中间体的制备方法
CN103265473A (zh) * 2013-06-04 2013-08-28 上海同昌生物医药科技有限公司 一种生产沙格列汀的方法
CN104370769B (zh) * 2013-08-14 2017-05-31 重庆博腾制药科技股份有限公司 一种制备羟基金刚烷甘氨酸衍生物的方法
WO2015031595A1 (en) * 2013-08-28 2015-03-05 Amneal Pharmaceuticals Llc A process for preparation of saxagliptin and its hydrochloride salt
CN103450071A (zh) * 2013-09-05 2013-12-18 南京工业大学 一种医药中间体2-氮杂双环[3.1.0]己烷-2,3-二碳酸叔丁酯的不对称合成方法
CN103435533A (zh) * 2013-09-09 2013-12-11 嘉兴学院 具有环丙烷结构的s-脯氨醇手性有机小分子化合物及其合成方法
CN103450074A (zh) * 2013-09-09 2013-12-18 嘉兴学院 具有环丙烷结构的r-脯氨醇手性有机小分子化合物及其合成方法
CN103435536A (zh) * 2013-09-09 2013-12-11 嘉兴学院 具有环丙烷结构s-脯氨酸的吡咯衍生物及其制备方法
CN103467361A (zh) * 2013-09-09 2013-12-25 嘉兴学院 具有环丙烷结构s-脯氨酸的吗啉衍生物及其制备方法
CN103467362A (zh) * 2013-09-09 2013-12-25 嘉兴学院 具有环丙烷结构s-二苯基脯氨醇类手性有机小分子化合物及其合成方法
CN103467360A (zh) * 2013-09-09 2013-12-25 嘉兴学院 具有环丙烷结构r-脯氨酸的吗啉衍生物及其制备方法
CN103435534A (zh) * 2013-09-09 2013-12-11 嘉兴学院 具有环丙烷结构s-脯氨酸的制备方法
CN103435535A (zh) * 2013-09-09 2013-12-11 嘉兴学院 具有环丙烷结构r-脯氨酸的制备方法
CN103450073A (zh) * 2013-09-09 2013-12-18 嘉兴学院 具有环丙烷结构r-二苯基脯氨醇类手性有机小分子化合物及其合成方法
CN104649953A (zh) * 2013-11-25 2015-05-27 天津市汉康医药生物技术有限公司 一种沙格列汀倍半水合物化合物
WO2015087262A1 (en) 2013-12-11 2015-06-18 Ranbaxy Laboratories Limited Process for the preparation of saxagliptin and its intermediates
CN104829444A (zh) * 2014-02-12 2015-08-12 上海医药工业研究院 一种α-溴代三环[3.3.1.13,7]癸烷-1-乙酸的后处理方法
CN103910669B (zh) * 2014-04-04 2015-10-21 苏州景泓生物技术有限公司 沙格列汀关键中间体的制备方法
CN103951588B (zh) * 2014-04-30 2016-10-05 淮海工学院 一种合成沙格列汀中间体n-叔丁氧羰基-3-羟基-1-金刚烷基-d-甘氨酸的方法
CN104109100A (zh) * 2014-05-29 2014-10-22 上海应用技术学院 一种金刚烷氨基酸酯化合物的合成方法
CN105315189A (zh) * 2014-05-29 2016-02-10 上海医药工业研究院 一种制备（5s）-5-氨基羰基-4,5-二氢-1h-吡咯-1-羧酸-1（1,1-二甲基乙基）酯的方法
CN104098487A (zh) * 2014-07-31 2014-10-15 天津民祥生物医药科技有限公司 一种n-叔丁氧羰基-3-羟基-1-金刚烷基甘氨酸的制备方法
CN104098505A (zh) * 2014-07-31 2014-10-15 天津民祥生物医药科技有限公司 一种沙格列汀的制备方法
WO2016026827A1 (en) * 2014-08-20 2016-02-25 Sandoz Ag Crystalline boc-s-hadgly and process for its preparation
CN104293844B (zh) * 2014-08-26 2017-10-10 苏州永健生物医药有限公司 一种特拉匹韦中间体的合成方法
GB201415598D0 (en) 2014-09-03 2014-10-15 Univ Birmingham Elavated Itercranial Pressure Treatment
CN105503698A (zh) * 2014-09-26 2016-04-20 深圳翰宇药业股份有限公司 一种合成沙格列汀及其中间体的方法
AU2016229982B2 (en) 2015-03-09 2020-06-18 Intekrin Therapeutics, Inc. Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy
CN104817476B (zh) * 2015-03-25 2020-09-11 重庆医科大学 一种制备非天然氨基酸的方法
CN105037245B (zh) * 2015-08-03 2017-04-12 沧州那瑞化学科技有限公司 一种沙格列汀中间体的制备方法
CN105112469B (zh) * 2015-09-24 2018-07-27 福建省微生物研究所 酶催化不对称转氨基反应制备沙格列汀手性中间体的方法
CN106554301B (zh) * 2015-09-30 2018-09-21 深圳翰宇药业股份有限公司 一种沙格列汀关键中间体的制备方法
KR101715682B1 (ko) 2015-10-29 2017-03-13 경동제약 주식회사 삭사글립틴의 제조를 위한 신규 중간체, 이의 제조방법 및 이를 이용한 삭사글립틴의 제조방법
DE102016116130A1 (de) 2016-08-30 2018-03-01 Universität Bielefeld Verfahren zur Herstellung chiraler Aminonitrile
EP3606527A1 (en) 2017-04-03 2020-02-12 Coherus Biosciences, Inc. Ppar-gamma agonist for treatment of progressive supranuclear palsy
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa
EP3807894A1 (en) 2018-06-14 2021-04-21 AstraZeneca UK Limited Methods for lowering blood sugar with a dipeptidyl peptidase-4 inhibitor pharmaceutical composition
CN111170927B (zh) * 2020-04-10 2020-08-04 上海翰森生物医药科技有限公司 一种沙格列汀中间体的制备方法
CN114621068A (zh) * 2022-03-31 2022-06-14 沧州那瑞化学科技有限公司 3-羟基-1-金刚烷甲基酮的制备方法及合成沙格列汀的方法

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3325478A (en) * 1964-11-17 1967-06-13 Du Pont alpha-amino-1-adamantylmethyl penicillins
US3646066A (en) * 1970-03-25 1972-02-29 Squibb & Sons Inc Adamantylamino-tetrahydronaphthyl-oxypropanols and ester derivatives
SU910605A1 (ru) * 1980-06-23 1982-03-07 Киевский Ордена Ленина Политехнический Институт Им.50-Летия Великой Октябрьской Социалистической Революции Способ получени @ -амино-1-адамантилуксусной кислоты
EP0140503A1 (en) 1983-08-16 1985-05-08 Genentech, Inc. An efficient process for preparing L-amino acids in bacteria
JPS62200861A (ja) 1986-02-28 1987-09-04 Toshiba Corp 画像形成装置
JPH06102027B2 (ja) * 1987-08-13 1994-12-14 財団法人相模中央化学研究所 Ｌ−２−アミノ−４−フェニル酪酸の製造方法
CA2008702A1 (en) 1989-02-27 1990-08-27 Ronald L. Hanson Process for transformation of hydroxyketo acids to hydroxyamino acids
IL120873A0 (en) 1996-05-24 1997-09-30 Tanabe Seiyaku Co Process for preparing optically active 2-halogen-3-hydroxypropionic acid ester
US6093330A (en) * 1997-06-02 2000-07-25 Cornell Research Foundation, Inc. Microfabrication process for enclosed microstructures
US6068991A (en) * 1997-12-16 2000-05-30 Bristol-Myers Squibb Company High expression Escherichia coli expression vector
WO2000004179A1 (en) 1998-07-15 2000-01-27 Bristol-Myers Squibb Company Stereoselective reductive amination of ketones
US6395767B2 (en) * 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
JP3942846B2 (ja) * 2001-06-21 2007-07-11 独立行政法人科学技術振興機構 組織特異的トランスポーター阻害剤
ES2344057T3 (es) 2002-10-23 2010-08-17 Bristol-Myers Squibb Company Inhibidores de la dipeptidil peptidasa iv basados en nitrilos de glicina.
US7420079B2 (en) * 2002-12-09 2008-09-02 Bristol-Myers Squibb Company Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof
US6995183B2 (en) * 2003-08-01 2006-02-07 Bristol Myers Squibb Company Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
KR20170005163A (ko) 2003-11-17 2017-01-11 노파르티스 아게 디펩티딜 펩티다제 ⅳ 억제제의 용도
TW200538122A (en) * 2004-03-31 2005-12-01 Bristol Myers Squibb Co Process for preparing a dipeptidyl peptidase Ⅳ inhibitor and intermediates employed therein
US7741082B2 (en) * 2004-04-14 2010-06-22 Bristol-Myers Squibb Company Process for preparing dipeptidyl peptidase IV inhibitors and intermediates therefor
TW200536827A (en) * 2004-05-04 2005-11-16 Bristol Myers Squibb Co Enzymatic ammonolysis process for the preparation of intermediates for DPP IV inhibitors
US7214702B2 (en) * 2004-05-25 2007-05-08 Bristol-Myers Squibb Company Process for producing a dipeptidyl peptidase IV inhibitor

Also Published As

Publication number Publication date
AU2003297647A1 (en) 2004-06-30
CN102070451A (zh) 2011-05-25
ES2525593T3 (es) 2014-12-26
ES2484915T3 (es) 2014-08-12
WO2004052850A3 (en) 2006-03-02
EP2792672A3 (en) 2014-11-26
JP2016040282A (ja) 2016-03-24
CN102942482B (zh) 2015-11-18
EP2505579A2 (en) 2012-10-03
EP2505579A3 (en) 2013-08-07
TW200512191A (en) 2005-04-01
PT2517706E (pt) 2014-09-05
EP2792672A2 (en) 2014-10-22
SI2517706T1 (sl) 2014-09-30
JP5860007B2 (ja) 2016-02-16
PT2505579E (pt) 2015-01-02
KR20050088309A (ko) 2005-09-05
US20130012723A1 (en) 2013-01-10
EP2505578A2 (en) 2012-10-03
EP2505579B1 (en) 2014-11-05
SI2505578T1 (sl) 2014-12-31
DK2517706T3 (da) 2014-09-08
DK2505578T3 (da) 2014-12-08
US20050090539A1 (en) 2005-04-28
ES2494793T3 (es) 2014-09-16
US7705033B2 (en) 2010-04-27
SI1581487T1 (sl) 2014-09-30
PT1581487E (pt) 2014-09-08
JP5511582B2 (ja) 2014-06-04
EP2505578A3 (en) 2013-07-31
CN1791401A (zh) 2006-06-21
PT2505578E (pt) 2014-12-17
WO2004052850A2 (en) 2004-06-24
EP2517706A3 (en) 2013-03-20
CA2508619A1 (en) 2004-06-24
DK1581487T3 (da) 2014-07-28
JP2006516121A (ja) 2006-06-22
JP2011006441A (ja) 2011-01-13
JP2013153748A (ja) 2013-08-15
EP1581487B1 (en) 2014-06-04
US20090018311A1 (en) 2009-01-15
US8278462B2 (en) 2012-10-02
CN102070451B (zh) 2015-07-15
US20100274025A1 (en) 2010-10-28
TW200914419A (en) 2009-04-01
EP1581487A4 (en) 2007-08-08
EP1581487A2 (en) 2005-10-05
JP4886193B2 (ja) 2012-02-29
EP2517706B1 (en) 2014-06-25
IL192912A0 (en) 2009-02-11
EP2505578B1 (en) 2014-09-24
MXPA05005970A (es) 2005-08-18
BR0317139A (pt) 2005-11-29
JP5730341B2 (ja) 2015-06-10
JP2014012689A (ja) 2014-01-23
JP2011006440A (ja) 2011-01-13
ES2526138T3 (es) 2015-01-07
US7420079B2 (en) 2008-09-02
EP2517706A2 (en) 2012-10-31
CN102942482A (zh) 2013-02-27
SI2505579T1 (sl) 2015-01-30
JP5345986B2 (ja) 2013-11-20
CN1791401B (zh) 2012-10-03
PL377123A1 (pl) 2006-01-23

Similar Documents

Publication Publication Date Title
DK2505579T3 (da) Fremgangsmåder og forbindelser til fremstilling af dipeptidylpeptidase IV-inhibitorer og mellemprodukter deraf
US8809024B2 (en) Process for preparing dipeptidyl peptidase IV inhibitors and intermediates therefor