ME02469B - Proces za pripremu jedinjenja koja su korisna kao inhibitori sglt2 - Google Patents

Proces za pripremu jedinjenja koja su korisna kao inhibitori sglt2

Info

Publication number
ME02469B
ME02469B MEP-2016-153A MEP2016153A ME02469B ME 02469 B ME02469 B ME 02469B ME P2016153 A MEP2016153 A ME P2016153A ME 02469 B ME02469 B ME 02469B
Authority
ME
Montenegro
Prior art keywords
ring
formula
compound
optionally substituted
zinc salt
Prior art date
Application number
MEP-2016-153A
Other languages
German (de)
English (en)
French (fr)
Inventor
Ioannis Nicolaos Houpis
Sebastien François Emmanuel Lemaire
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of ME02469B publication Critical patent/ME02469B/me

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61P3/08—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/02—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
    • C07H13/04—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals attached to acyclic carbon atoms
    • C07H13/06—Fatty acids

Landscapes

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

Claims (11)

1. Proces za pripremu jedinjenja formule (I)pri čemu su Prsten A, i Prsten B jedan od sledećih:(1) Prsten A je opciono supstituisani nezasićeni monociklični heterociklični prsten, i Prsten B je opciono supstituisani nezasićeni monociklični heterociklični prsten, opciono supstituisani nezasićeni fuzionisani heterobiciklični prsten, ili opciono supstituisani benzenov prsten; ili(2) Prsten A je opciono supstituisani benzenov prsten, i Prsten B je opciono supstituisani nezasićeni monociklični heterociklični prsten, ili opciono supstituisani nezasićeni fuzionisani heterobiciklični prsten pri čemu je Y povezan na heterociklični prsten fuzionisanog heterobicikličnog prstena; ili(3) Prsten A je opciono supstituisani nezasićeni fuzionisani heterobiciklični prsten, pri čemu su šećerni ostatak X- (šećer) i ostatak-Y-(prsten B), oba na istom heterocikličnom prstenu fuzionisanog heterobicikličnog prstena, i Prsten B je opciono supstituisani nezasićeni monociklični heterociklični prsten, opciono supstituisani nezasićeni fuzionisani heterobiciklični prsten, ili opciono supstituisani benzenov prsten;X je atom ugljenika;Y je -(CH2)n-; pri čemu je n 1 ili 2;obezbedjujući da je u Prstenu A, X deo nezasićene veze;ili njegova farmaceutski prihvatljiva so ili solvat; obuhvatajućireagovanje jedinjenja formule (V) pri čemu je LG1 odlazća grupa, sa smešom cinkove soli i organolitijumovog reagensa; u prvom ugljovodoničnom rastvaraču; na temperaturi u rasponu od oko -78°C do oko sobne temperature; da se dobije smeša odgovarajućeg jedinjenja formule (VI), pri čemu je M1 litijum i cinkova so;mešanje u smešu jedinjenja formule (VI) i cinkove soli u prvom etarskom rastvaraču; da se dobije odgovarajuće jedinjenje formule (VII), pri čemu je M2 cink reaktivnih vrsta;reagovanje jedinjenja formule (VII), sa jedinjenjem formule (VIII), pri čemu svaka Z je nezavisno izabrana kiseonik zaštitna grupa i pri čemu je LG2 odlazeća grupa; da se dobije odgovarajuće jedinjenje formule (IX);uklanjanje zaštite jedinjenja formule (IX); da se dobije odgovarajuće jedinjenje formule (I).
2. Proces prema patentnom zahtevu 1 za pripremu jedinjenja formule (IS) ili njegove farmaceutski prihvatljive soli ili solvata; koji sadrži reagovanje jedinjenja formule (V-S) pri čemu je LG1 odlazća grupa, sa smešom cinkove soli i organolitijumovog reagensa; u prvom ugljovodoničnom rastvaraču; na temperaturi u rasponu od oko -78°C do oko sobne temperature; da se dobije smeša odgovarajućeg jedinjenja formule (VI-S), pri čemu je M1 litijum i cinkova so; mešanje u smešu jedinjenja formule (VI-S) i cinkove soli u prvom etarskom rastvaraču; da se dobije odgovarajuće jedinjenje formule (VII-S), pri čemu je M2 cink reaktivnih vrsta; reagovanje jedinjenja formule (VII-S), pri čemu je M2 vrste cinka, sa jedinjenjem formule (VIII-S), pri čemu je svaka Z nezavisno izabrana kiseonik zaštitna grupa i pri čemu je LG2 odlazeća grupa; da se dobije odgovarajuće jedinjenje formule (IX-S); uklanjanje zaštite jedinjenja formule (IX-S); da se dobije odgovarajuće jedinjenje formule (I-S).
3. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu je cinkova so ZnBr2 i pri čemu je organo-litijumov reagens n-butil litijum.
4. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu su cinkova so, i organo-litijumov reagens prisutni u molarnom odnosu od oko 1:2.
5. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu su cinkova so, i organo-litijumov reagens prethodno mešani tokom perioda od oko 1 do oko 2 sata.
6. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu je prvi ugljovodonični rastvarač toluen.
7. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu je LG1 jod, zinkova so je ZnBr2, organolitijumov reagens je n-butil litijum, cinkova so i organo-litijumov reagens su pretrhodno-pomešani, prvi ugljovodonični rastvarač je toluen, i pri čemu je jedinjenje formule (V) reagovalo sa smešom cinkove soli i organolitijumovim reagensom na temperaturi od oko 0°C.
8. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu je prvi etarski rastvarač din-butil etar.
9. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu je prvi etarski rastvarač prisutan u količini u rasponu od oko 7% do oko 10% po zapremini.
10. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu je LG1 jod, Z je pivaloil i LG2 je brom.
11. Proces prema patentnom zahtevu 1, pri čemu X je atom ugljenika; Prsten A je izabran iz grupe koja se sastoji od 4-metilfenila i 4-hlorofenila; Y je -CH2- i vezan je na 3-poziciji Prstena A; i Prsten B je izabran iz grupe koja ses sastoji od 2-(5-(4-fluorofenil)-tienila) i 2-(5-(6-fluoro-pirid-3-il)-tienila). Janssen Phamaceutica NV., BE 2
MEP-2016-153A 2011-04-13 2012-04-12 Proces za pripremu jedinjenja koja su korisna kao inhibitori sglt2 ME02469B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161474936P 2011-04-13 2011-04-13
EP12715362.5A EP2697218B1 (en) 2011-04-13 2012-04-12 Process for the preparation of compounds useful as inhibitors of sglt2
PCT/EP2012/056649 WO2012140120A1 (en) 2011-04-13 2012-04-12 Process for the preparation of compounds useful as inhibitors of sglt2

Publications (1)

Publication Number Publication Date
ME02469B true ME02469B (me) 2017-02-20

Family

ID=45976924

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2016-153A ME02469B (me) 2011-04-13 2012-04-12 Proces za pripremu jedinjenja koja su korisna kao inhibitori sglt2

Country Status (20)

Country Link
US (1) US10544135B2 (me)
EP (1) EP2697218B1 (me)
JP (1) JP5973551B2 (me)
KR (1) KR101913587B1 (me)
CN (1) CN103596944B (me)
AU (1) AU2012241897C1 (me)
CA (1) CA2832938C (me)
CY (1) CY1117989T1 (me)
DK (1) DK2697218T3 (me)
EA (1) EA028946B1 (me)
ES (1) ES2586846T3 (me)
HR (1) HRP20161062T1 (me)
HU (1) HUE030116T2 (me)
ME (1) ME02469B (me)
PL (1) PL2697218T3 (me)
PT (1) PT2697218T (me)
RS (1) RS55056B1 (me)
SI (1) SI2697218T1 (me)
SM (1) SMT201600274B (me)
WO (1) WO2012140120A1 (me)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014132940A1 (ja) 2013-02-26 2014-09-04 田辺三菱製薬株式会社 α－ハロテトラアシルグルコースの製造方法
CN104557894A (zh) * 2013-10-18 2015-04-29 上海信谊药厂有限公司 坎格列汀晶型及其制备方法
CN104672227A (zh) * 2013-11-28 2015-06-03 镇江新元素医药科技有限公司 一类新型sglt2抑制剂化合物及其药物组合物
EP2918579A1 (en) * 2014-03-14 2015-09-16 LEK Pharmaceuticals d.d. Synthesis of 2-arylmethyl-5-aryl-thiophene
CN103936725B (zh) * 2014-04-01 2016-07-27 天津大学 卡格列净的c晶型及其结晶制备方法
CN103980262B (zh) * 2014-04-01 2016-06-22 天津大学 卡格列净的b晶型及其结晶制备方法
CN103980261B (zh) * 2014-04-01 2016-06-29 天津大学 卡格列净的a晶型及其结晶制备方法
CN103980263B (zh) * 2014-04-17 2016-08-03 海门瑞一医药科技有限公司 卡格列净的合成工艺
EP2933255A1 (en) 2014-04-17 2015-10-21 LEK Pharmaceuticals d.d. Novel crystalline form of 1-(beta-D-glucopyranosyl)-4- methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene
EP2947077A1 (en) 2014-05-19 2015-11-25 LEK Pharmaceuticals d.d. Stereoselective synthesis of intermediates in the preparation of ß-C-arylglucosides
CN104109157B (zh) * 2014-08-04 2016-05-25 山东康美乐医药科技有限公司 卡格列净的制备方法
CN105440025B (zh) * 2014-09-25 2019-02-12 深圳翰宇药业股份有限公司 一种制备卡格列净及其中间体的方法及所述中间体
CN104817554A (zh) * 2014-11-10 2015-08-05 镇江新元素医药科技有限公司 一类葡萄糖苷衍生物及其药物组合物
CN104557895B (zh) * 2015-01-27 2017-10-31 江苏嘉逸医药有限公司 1‑(β‑D‑吡喃葡糖基)‑4‑甲基‑3‑[5‑(4‑氟苯基)‑2‑噻吩基甲基]苯的合成工艺
CN105884755B (zh) * 2015-02-14 2019-05-28 正大天晴药业集团股份有限公司 氘修饰的碳甙衍生物
CN106188022A (zh) * 2015-04-30 2016-12-07 上海医药工业研究院 伊格列净的制备方法
CN105153137A (zh) * 2015-09-17 2015-12-16 上海应用技术学院 一种艾格列净的制备方法
CN105503845A (zh) * 2015-12-01 2016-04-20 北京普德康利医药科技发展有限公司 去氟卡格列净化合物及其制备方法和应用
CN109988128B (zh) * 2017-12-29 2022-08-19 江苏扬农化工股份有限公司 一种呋喃醇衍生物的合成方法
CN110054657B (zh) * 2018-01-18 2021-06-29 亚宝药业集团股份有限公司 吡喃葡萄糖取代的吡唑化合物及其制备方法
CN109111490B (zh) * 2018-08-09 2021-02-23 浙江大学 卤代新戊酰基吡喃葡萄糖及其用于sglt2抑制剂的制备方法
CN114591313A (zh) * 2020-12-04 2022-06-07 南京圣鼎医药科技有限公司 一种卡格列净的制备方法
CN117980327A (zh) * 2021-11-03 2024-05-03 杭州多禧生物科技有限公司 抗体的特异性偶联

Family Cites Families (150)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2799241A (en) 1949-01-21 1957-07-16 Wisconsin Alumni Res Found Means for applying coatings to tablets or the like
US4160861A (en) 1977-10-03 1979-07-10 Merck & Co., Inc. Method for the separation of antibiotic macrolides
US4584369A (en) 1981-07-31 1986-04-22 Sloan-Kettering Institute For Cancer Research Anti-leukemic beta-glycosyl C-nucleosides
JPS5939889A (ja) 1982-08-30 1984-03-05 Noguchi Kenkyusho ２，４，６↓−トリ↓−０↓−アセチル↓−３↓−デオキシ↓−ヘキソノ↓−１，５↓−ラクトンの製造方法
JP2544609B2 (ja) 1986-10-07 1996-10-16 和光純薬工業株式会社 Ｔｃｎｑ錯体
US4863957A (en) 1987-12-21 1989-09-05 Rorer Pharmaceutical Corporation Novel HMG-CoA reductase inhibitors
CA1327013C (en) 1988-06-23 1994-02-15 Peter Rex Brawn Cosmetic composition
JP2786896B2 (ja) 1988-08-19 1998-08-13 ワーナー―ランバート・コンパニー 置換されたジヒドロイソキノリノンおよび関連化合物
DK0472502T3 (da) 1990-08-24 1995-10-09 Spirig Ag Fremgangsmåde til fremstilling af pellets
JPH04253974A (ja) 1991-02-05 1992-09-09 Ishihara Sangyo Kaisha Ltd スルホニル尿素系化合物、それらの製造方法及びそれらを含有する除草剤
EP0517969A1 (en) 1991-06-10 1992-12-16 AUSIMONT S.p.A. Process for increasing the bleaching efficiency of an inorganic persalt or of hydrogen peroxide
US5149838A (en) 1991-09-20 1992-09-22 Merck & Co., Inc. Intermediates for substituted azetidinones useful as anti-inflammatory and antidegenerative agents
US5610294A (en) 1991-10-11 1997-03-11 The Du Pont Merck Pharmaceutical Company Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
CN1071924A (zh) 1991-10-29 1993-05-12 纳幕尔杜邦公司 除草的三唑羧酸酰胺
GB9208161D0 (en) 1992-04-14 1992-05-27 Pfizer Ltd Indoles
US5334225A (en) 1992-07-15 1994-08-02 Kao Corporation Keratinous fiber dye composition containing a 2-substituted amino-5-alkylphenol derivative coupler
US5731292A (en) 1992-11-12 1998-03-24 Tanabe Seiyaku Co., Ltd. Dihydrochalcone derivatives which are hypoglycemic agents
CA2102591C (en) 1992-11-12 2000-12-26 Kenji Tsujihara Hypoglycemic agent
DE4243279A1 (de) 1992-12-21 1994-06-23 Bayer Ag Substituierte Triole
US6297363B1 (en) 1993-02-12 2001-10-02 Nomura Co., Ltd. Glycoside indoles
JP3342727B2 (ja) 1993-03-01 2002-11-11 株式会社小松製作所 制振鋼板の曲げ加工方法および曲げ加工装置
JP3187611B2 (ja) 1993-05-17 2001-07-11 キヤノン株式会社 液晶性化合物、これを含む液晶組成物、それを有する液晶素子、それらを用いた表示方法および表示装置
JPH07242526A (ja) 1994-03-03 1995-09-19 Sogo Yatsukou Kk 化粧料
US5830873A (en) 1994-05-11 1998-11-03 Tanabe Seiyaku Co., Ltd. Propiophenone derivative and a process for preparing the same
EP0732921A4 (en) 1994-09-30 1998-09-02 Ohio State Res Found C-GLYCOSIDANOLOGIST OF N- (4-HYDROXYPHENYL) RETINAMIDE-O-GLUCURONIDE
US5780483A (en) 1995-02-17 1998-07-14 Smithkline Beecham Corporation IL-8 receptor antagonists
JP2002500618A (ja) 1995-10-31 2002-01-08 イーライ・リリー・アンド・カンパニー 抗血栓性ジアミン
JP3059088B2 (ja) 1995-11-07 2000-07-04 田辺製薬株式会社 プロピオフェノン誘導体およびその製法
US5723495A (en) 1995-11-16 1998-03-03 The University Of North Carolina At Chapel Hill Benzamidoxime prodrugs as antipneumocystic agents
JPH09263549A (ja) 1996-01-25 1997-10-07 Fujisawa Pharmaceut Co Ltd ベンゼン誘導体の製造法
IL121525A0 (en) 1996-08-26 1998-02-08 Tanabe Seiyaku Co Process for preparing optically active benzothiazepine compound and intermediate therefor
ATE216704T1 (de) 1996-12-26 2002-05-15 Tanabe Seiyaku Co Propiophenonderivate und verfahren zu ihrer herstellung
US6153632A (en) 1997-02-24 2000-11-28 Rieveley; Robert B. Method and composition for the treatment of diabetes
WO1998042347A1 (en) 1997-03-25 1998-10-01 Takeda Chemical Industries, Ltd. Pharmaceutical composition containing a phosphorylamide and an ayntibiotic
WO1999047128A1 (en) 1998-03-19 1999-09-23 Bristol-Myers Squibb Company Biphasic controlled release delivery system for high solubility pharmaceuticals and method
EP1087931A1 (de) 1998-06-18 2001-04-04 MERCK PATENT GmbH Verfahren zur symmetrischen und unsymmetrischen disubstitution von carbonsäureamiden mit organotitanaten und grignard-reagenzien
FR2780403B3 (fr) 1998-06-24 2000-07-21 Sanofi Sa Nouvelle forme de l'irbesartan, procedes pour obtenir ladite forme et compositions pharmaceutiques en contenant
JP2000034239A (ja) 1998-07-16 2000-02-02 Asahi Glass Co Ltd トリフルオロメチル化芳香族化合物の製造方法
JP3857429B2 (ja) 1998-07-17 2006-12-13 ポーラ化成工業株式会社 含硫黄抗真菌剤
US6069238A (en) 1998-09-30 2000-05-30 Eli Lilly And Company Spirocyclic C-glycosides
DE69926148D1 (en) 1998-11-09 2005-08-18 Black James Foundation Gastrin und cholecystokinin rezeptor ligande
WO2000028989A1 (en) 1998-11-12 2000-05-25 Smithkline Beecham P.L.C. Pharmaceutical composition for modified release of an insulin sensitiser and another antidiabetic agent
US20020032164A1 (en) 1998-12-30 2002-03-14 Dale Roderic M. K. Antimicrobial compounds and methods for their use
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
PH12000002657B1 (en) 1999-10-12 2006-02-21 Bristol Myers Squibb Co C-aryl glucoside SGLT2 inhibitors
US6515117B2 (en) 1999-10-12 2003-02-04 Bristol-Myers Squibb Company C-aryl glucoside SGLT2 inhibitors and method
JP3450810B2 (ja) 2000-01-31 2003-09-29 キヤノン株式会社 脂肪族ポリエステル、脂肪族ポリエステルの製造方法およびセルロースの再資源化方法
JP4456768B2 (ja) 2000-02-02 2010-04-28 壽製薬株式会社 Ｃ−配糖体を含有する薬剤
US6627611B2 (en) 2000-02-02 2003-09-30 Kotobuki Pharmaceutical Co Ltd C-glycosides and preparation of thereof as antidiabetic agents
WO2001064669A1 (en) 2000-03-03 2001-09-07 Pfizer Products Inc. Pyrazole ether derivatives as anti-inflammatory/analgesic agents
ES2254376T3 (es) 2000-03-17 2006-06-16 Kissei Pharmaceutical Co., Ltd. Derivados glucopiranosiloxibencilbenceno, preparaciones medicinales que los contienen e intermediarios para la preparacion de los indicados derivados.
US6683056B2 (en) 2000-03-30 2004-01-27 Bristol-Myers Squibb Company O-aryl glucoside SGLT2 inhibitors and method
US6555519B2 (en) 2000-03-30 2003-04-29 Bristol-Myers Squibb Company O-glucosylated benzamide SGLT2 inhibitors and method
GB0011098D0 (en) 2000-05-08 2000-06-28 Black James Foundation Pharmaceutical compositions comprising protpn pump inhibitors and gastrin/cholecystokinin receptor ligands
EP1172362A1 (de) 2000-07-11 2002-01-16 Basf Aktiengesellschaft Azadioxacycloalkene und ihre Verwendung zur Bekämpfung von Schadpilzen und tierischen Schädlingen
KR100426030B1 (ko) 2000-07-22 2004-04-03 (주) 한켐 락톤계 당화합물에서의 키랄성 전환방법
AU2001296961A1 (en) 2000-09-29 2002-04-08 Bayer Pharmaceuticals Corporation 17-beta-hydroxysteroid dehydrogenase-ii inhibitors
WO2002036602A1 (en) 2000-11-02 2002-05-10 Ajinomoto Co., Inc. Novel pyrazole derivatives and diabetes remedies containing the same
JP2002167430A (ja) 2000-12-01 2002-06-11 Canon Inc 脂肪族ポリエステル、脂肪族ポリエステルの製造方法およびデンプンの資源化方法
US6476352B2 (en) 2000-12-18 2002-11-05 General Electric Company Laser beam stop sensor and method for automatically detecting the presence of laser beam stop material using a laser beam stop sensor
SK287786B6 (sk) 2000-12-28 2011-09-05 Kissei Pharmaceutical Co., Ltd. Glukopyranosyloxypyrazolový derivát, farmaceutická kompozícia alebo kombinácia s jeho obsahom a ich použitie
EP1364957B1 (en) 2001-02-26 2008-12-31 Kissei Pharmaceutical Co., Ltd. Glycopyranosyloxypyrazole derivatives and medicinal use thereof
WO2002068440A1 (en) 2001-02-27 2002-09-06 Kissei Pharmaceutical Co., Ltd. Glycopyranosyloxypyrazole derivatives and medicinal use thereof
WO2002070020A2 (en) 2001-03-02 2002-09-12 University Of Western Ontario Polymer precursors of radiolabeled compounds, and methods of making and using the same
US6936590B2 (en) 2001-03-13 2005-08-30 Bristol Myers Squibb Company C-aryl glucoside SGLT2 inhibitors and method
DK1385856T3 (da) 2001-04-11 2006-05-15 Bristol Myers Squibb Co Aminosyrekomplekser af C-aryl-glucosider til behandling af diabetes og fremgangsmåder
EP1389621A4 (en) 2001-04-27 2005-05-11 Ajinomoto Kk N-SUBSTITUTED PYRAZOLYL-O-GLYCOSIDE DERIVATIVES AND DIABETES CONTAINING THEREOF
GB0112122D0 (en) 2001-05-18 2001-07-11 Lilly Co Eli Heteroaryloxy 3-substituted propanamines
US7105556B2 (en) 2001-05-30 2006-09-12 Bristol-Myers Squibb Company Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
US7271153B2 (en) 2001-06-20 2007-09-18 Kissei Pharmaceutical Co., Ltd. Nitrogenous heterocyclic derivatives, medicinal compositions containing the same, medicinal uses thereof, and intermediates therefor
JP4115105B2 (ja) 2001-07-02 2008-07-09 協和醗酵工業株式会社 ピラゾール誘導体
WO2003011880A1 (fr) 2001-07-31 2003-02-13 Kissei Pharmaceutical Co., Ltd. Derive de glucopyranosyloxybenzylbenzene, composition medicinale contenant ce derive, usage medicinal de cette composition et produit intermediaire pour produire cette composition
US20030191121A1 (en) 2001-08-09 2003-10-09 Miller Ross A. Piperazine carboxamide intermediates of HIV protease inhibitors and processes for their preparation
US20030087843A1 (en) 2001-09-05 2003-05-08 Washburn William N. O-pyrazole glucoside SGLT2 inhibitors and method of use
ATE312940T1 (de) 2001-10-24 2005-12-15 Michael Burton Chromogenischen enzymsubstraten und verfahren zum nachweis von beta-d-ribofuranosidase-wirksamkeit
CA2465186A1 (en) 2001-11-08 2003-05-15 Sepracor, Inc. Methods for treating depression and other cns disorders using enantiomerically enriched desmethyl- and didesmethyl-metabolites of citalopram
PT1443915E (pt) 2001-11-16 2006-11-30 Bioform Medical Inc Composições farmacêuticas e cosméticas contendo aldeídos aromáticos com grupos oxilo
JP2003238417A (ja) 2002-02-18 2003-08-27 Nippon Shoyaku Kenkyusho:Kk フロレチン配糖体の安定化組成物、該安定化組成物を含有する糖尿病予防・治療剤、および保健食品
US6617313B1 (en) 2002-03-13 2003-09-09 Council Of Scientific And Industrial Research Glucopyranoside and process of isolation thereof from pterocarpus marsupium pharmaceutical composition containing the same and use thereof
US6562791B1 (en) 2002-03-29 2003-05-13 Council Of Scientific And Industrial Research Glucopyranoside, process for isolation thereof, pharmaceutical composition containing same and use thereof
JP2003313168A (ja) 2002-04-18 2003-11-06 Kirin Brewery Co Ltd Ｂｃｌ−２阻害活性を有する化合物およびその化合物のスクリーニング方法
JP4523775B2 (ja) 2002-04-18 2010-08-11 アストラゼネカ・アクチエボラーグ 複素環化合物
DE10231370B4 (de) 2002-07-11 2006-04-06 Sanofi-Aventis Deutschland Gmbh Thiophenglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel
TWI254635B (en) 2002-08-05 2006-05-11 Yamanouchi Pharma Co Ltd Azulene derivative and salt thereof
MXPA05000725A (es) 2002-08-09 2005-04-08 Taisho Pharma Co Ltd Procedimiento para la produccion selectiva de aril-5-tio-??-d-aldohexopiranosidos.
WO2004019958A1 (ja) 2002-08-27 2004-03-11 Kissei Pharmaceutical Co., Ltd. ピラゾール誘導体、それを含有する医薬組成物及びその医薬用途
US7074826B2 (en) 2002-10-07 2006-07-11 Encore Pharmaceuticals, Inc. R-NSAID esters and their use
IN192749B (me) 2002-11-15 2004-05-15 Ranbaxy Lab Ltd
DE10258007B4 (de) 2002-12-12 2006-02-09 Sanofi-Aventis Deutschland Gmbh Aromatische Fluorglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel
DE10258008B4 (de) 2002-12-12 2006-02-02 Sanofi-Aventis Deutschland Gmbh Heterocyclische Fluorglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel
PL378324A1 (pl) 2003-01-03 2006-03-20 Bristol-Myers Squibb Company Sposób wytwarzania C-aryloglukozydowych inhibitorów SGLT2
GB0301259D0 (en) 2003-01-20 2003-02-19 Novartis Ag Organic compounds
WO2004076470A2 (en) 2003-02-27 2004-09-10 Bristol-Myers Squibb Company A non-cryogenic process for forming glycosides
ATE510834T1 (de) 2003-03-14 2011-06-15 Astellas Pharma Inc C-glykosid-derivate zur behandlung von diabetes
JP2004300102A (ja) 2003-03-31 2004-10-28 Kissei Pharmaceut Co Ltd 縮合複素環誘導体、それを含有する医薬組成物およびその医薬用途
AU2003902263A0 (en) 2003-05-12 2003-05-29 Fujisawa Pharmaceutical Co., Ltd. Monosaccharide compounds
WO2004113359A1 (ja) 2003-06-20 2004-12-29 Kissei Pharmaceutical Co., Ltd. ピラゾール誘導体、それを含有する医薬組成物及びその製造中間体
NZ545447A (en) 2003-07-23 2010-03-26 Synta Pharmaceuticals Corp Compounds for inflammation and immune-related uses
EP1679965A4 (en) 2003-08-01 2009-05-27 Janssen Pharmaceutica Nv SUBSTITUTED ANELLIERED HETEROCYCLIC C-GLYCOSIDES
WO2005012243A2 (en) 2003-08-01 2005-02-10 Janssen Pharmaceutica N.V. Substituted indole-o-glucosides
UA86042C2 (en) 2003-08-01 2009-03-25 Янссен Фармацевтика Н.В. Substituted indazole-o-glucosides
US8785403B2 (en) 2003-08-01 2014-07-22 Mitsubishi Tanabe Pharma Corporation Glucopyranoside compound
AU2004261663A1 (en) 2003-08-01 2005-02-10 Janssen Pharmaceutica N.V. Substituted benzimidazole-, benztriazole-, and benzimidazolone-O-glucosides
CA2549017A1 (en) 2003-08-01 2005-02-10 Mona Patel Substituted indazole-o-glucosides
CN104109155A (zh) * 2003-08-01 2014-10-22 田边三菱制药株式会社 新颖化合物
WO2005058845A2 (en) 2003-12-19 2005-06-30 Novo Nordisk A/S Novel glucagon antagonists/inverse agonists
US7157584B2 (en) 2004-02-25 2007-01-02 Takeda Pharmaceutical Company Limited Benzimidazole derivative and use thereof
EA011158B1 (ru) 2004-03-16 2009-02-27 Бёрингер Ингельхайм Интернациональ Гмбх Замещённые глюкопиранозилом бензольные производные, содержащие эти соединения лекарственные средства, их применение и способ их получения
US7393836B2 (en) 2004-07-06 2008-07-01 Boehringer Ingelheim International Gmbh D-xylopyranosyl-substituted phenyl derivatives, medicaments containing such compounds, their use and process for their manufacture
WO2006010557A1 (de) 2004-07-27 2006-02-02 Boehringer Ingelheim International Gmbh D-glucopyranosyl-phenyl-substituierte cyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
WO2006018150A1 (de) 2004-08-11 2006-02-23 Boehringer Ingelheim International Gmbh D-xylopyranosyl-phenyl-substituierte cyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
TW200637839A (en) 2005-01-07 2006-11-01 Taisho Pharmaceutical Co Ltd 1-thio-d-glucitol derivatives
US20090124702A1 (en) 2005-01-25 2009-05-14 Pechetti Siva Satya Krishna Babu Pharmaceutical Compositions of Metformin
AR053329A1 (es) 2005-01-31 2007-05-02 Tanabe Seiyaku Co Derivados de indol utiles como inhibidores de los transportadores de glucosa dependientes del sodio (sglt)
JP5264183B2 (ja) 2005-02-23 2013-08-14 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング グルコピラノシル置換（（ヘテロ）アリールエチニル−ベンジル）−ベンゼン誘導体及びナトリウム依存性グルコース共輸送体２（ｓｇｌｔ２）インヒビターとしてのそれらの使用
WO2006108842A1 (en) 2005-04-15 2006-10-19 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituted (heteroaryloxy-benzyl)-benzene derivatives as sglt inhibitors
US7772191B2 (en) 2005-05-10 2010-08-10 Boehringer Ingelheim International Gmbh Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein
EP1910390B1 (en) 2005-07-27 2010-05-19 Boehringer Ingelheim International GmbH Glucopyranosyl-substituted ((hetero)cycloalyklethynyl-benzyl)-benzene derivatives and use thereof as sodium-dependent glucose cotransporter (sglt) inhibitors
JP5175191B2 (ja) 2005-08-30 2013-04-03 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング グリコピラノシル置換ベンジルベンゼン誘導体、該化合物を含有する医薬品及びその使用と製造方法
AR056195A1 (es) 2005-09-15 2007-09-26 Boehringer Ingelheim Int Procedimientos para preparar derivados de (etinil-bencil)-benceno sustituidos de glucopiranosilo y compuestos intermedios de los mismos
CA2640090A1 (en) 2006-01-25 2007-08-02 Synta Pharmaceuticals Corp. Substituted aromatic compounds for inflammation and immune-related uses
JP2007230999A (ja) 2006-01-31 2007-09-13 Kyoto Univ 置換芳香族ニトリル化合物およびその製造方法
TWI370818B (en) 2006-04-05 2012-08-21 Astellas Pharma Inc Cocrystal of c-glycoside derivative and l-proline
US7919598B2 (en) 2006-06-28 2011-04-05 Bristol-Myers Squibb Company Crystal structures of SGLT2 inhibitors and processes for preparing same
TWI418556B (zh) 2006-07-27 2013-12-11 Mitsubishi Tanabe Pharma Corp 吲哚衍生物
CA2656847A1 (en) 2006-08-15 2008-02-21 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituted cyclopropylbenzene derivatives, pharmaceutical compositions containing such compounds, their use as sglt inhibitors and process for their manufacture
CA2664095A1 (en) * 2006-09-21 2008-03-27 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituted difluorobenzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
AR063569A1 (es) 2006-11-06 2009-02-04 Boehringer Ingelheim Int Derivados de benzil- benzonitrilo sustituidos con glucopiranosilo medicamentos que contienen a compuestos de este tipo su uso u procedimiento para su fabricacion
CL2007003227A1 (es) 2006-11-09 2008-07-04 Boehringer Ingelheim Int Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo en combinacion con uno o mas agentes terapeuticos; y uso para el tratamiento de diabetes mellitus, obesidad e hiperglucemia entre otras.
UY30730A1 (es) * 2006-12-04 2008-07-03 Mitsubishi Tanabe Pharma Corp Forma cristalina del hemihidrato de 1-(b (beta)-d-glucopiranosil) -4-metil-3-[5-(4-fluorofenil) -2-tienilmetil]benceno
NZ577391A (en) 2006-12-04 2011-11-25 Janssen Pharmaceutica Nv Thienyl-containing glycopyranosyl derivatives as antidiabetics
EP1956023A1 (en) 2007-02-06 2008-08-13 Lonza Ag Method for lithium exchange reactions
TW200904405A (en) 2007-03-22 2009-02-01 Bristol Myers Squibb Co Pharmaceutical formulations containing an SGLT2 inhibitor
JP5424571B2 (ja) 2007-04-12 2014-02-26 協和発酵キリン株式会社 トピラマート含有固形製剤
US20090047514A1 (en) 2007-08-15 2009-02-19 Allen David P Thermal Activated Pressure Sensitive Adhesive and Method for Producing the Same and Product therewith
AU2008288770B2 (en) 2007-08-23 2014-06-12 Theracosbio, Llc Benzylbenzene derivatives and methods of use
MX2010002695A (es) 2007-09-10 2010-04-01 Janssen Pharmaceutica Nv Proceso para la preparacion de compuestos utiles como inhibidores de transportador de glucosa dependiente de sodio (sglt).
CL2008003653A1 (es) 2008-01-17 2010-03-05 Mitsubishi Tanabe Pharma Corp Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica.
PE20140960A1 (es) 2008-04-03 2014-08-15 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
WO2010009243A1 (en) 2008-07-15 2010-01-21 Theracos, Inc. Deuterated benzylbenzene derivatives and methods of use
MX2011001855A (es) 2008-08-22 2011-03-24 Theracos Inc Procesos para la preparacion de inhibidores de sglt2.
US9056850B2 (en) 2008-10-17 2015-06-16 Janssen Pharmaceutica N.V. Process for the preparation of compounds useful as inhibitors of SGLT
WO2010045656A2 (en) 2008-10-17 2010-04-22 Nectid, Inc. Novel sglt2 inhibitor dosage forms
MX339194B (es) 2009-02-13 2016-05-16 Boehringer Ingelheim Int Composicion farmaceutica que comprende un inhibidor de sglt2, un inhibidor de dpp-iv y opcionalmente otro agente antidiabetico, y usos de la misma.
MX356518B (es) 2009-04-24 2018-05-31 Iceutica Pty Ltd Producción de nanopartículas encapsuladas en fracciones de alto volumen.
US20110009347A1 (en) 2009-07-08 2011-01-13 Yin Liang Combination therapy for the treatment of diabetes
WO2011047113A1 (en) * 2009-10-14 2011-04-21 Janssen Pharmaceutica Nv Process for the preparation of compounds useful as inhibitors of sglt2
US8163704B2 (en) 2009-10-20 2012-04-24 Novartis Ag Glycoside derivatives and uses thereof
NZ703128A (en) 2010-05-11 2016-04-29 Janssen Pharmaceutica Nv Pharmaceutical formulations comprising 1 - (beta-d-glucopyranosyl) - 2 -thienylmethylbenzene derivatives as inhibitors of sglt
CA2804506C (en) 2010-07-06 2018-08-21 Janssen Pharmaceutica Nv Formulation for co-therapy treatment of diabetes

Also Published As

Publication number Publication date
AU2012241897B2 (en) 2016-12-01
RS55056B1 (sr) 2016-12-30
US10544135B2 (en) 2020-01-28
DK2697218T3 (en) 2016-07-25
JP2014510776A (ja) 2014-05-01
SMT201600274B (it) 2016-08-31
HUE030116T2 (en) 2017-04-28
EP2697218B1 (en) 2016-05-25
CA2832938C (en) 2019-09-03
ES2586846T3 (es) 2016-10-19
EP2697218A1 (en) 2014-02-19
EA201391522A1 (ru) 2014-03-31
JP5973551B2 (ja) 2016-08-23
HRP20161062T1 (hr) 2016-12-16
CY1117989T1 (el) 2017-05-17
US20190194177A1 (en) 2019-06-27
PL2697218T3 (pl) 2016-11-30
AU2012241897C1 (en) 2017-05-11
AU2012241897A1 (en) 2013-10-24
KR101913587B1 (ko) 2018-10-31
CN103596944B (zh) 2017-02-22
CA2832938A1 (en) 2012-10-18
KR20140026467A (ko) 2014-03-05
SI2697218T1 (sl) 2016-07-29
WO2012140120A1 (en) 2012-10-18
CN103596944A (zh) 2014-02-19
PT2697218T (pt) 2016-07-13
EA028946B1 (ru) 2018-01-31

Similar Documents

Publication Publication Date Title
HRP20161062T1 (hr) Proces za pripremu spojeva koji su korisni kao inhibitori sglt2
ME02634B (me) Proces za pripremu jedinjenja koja su korisna kao inhibitori sglt2
CA3097949A1 (en) Hpk1 inhibitors, preparation method and application thereof
HRP20171914T1 (hr) Postupak za dobivanje spojeva koji su korisni kao inhibitori sglt
BRPI0916995B8 (pt) compostos orgânicos, seu uso, e composição farmacêutica
AR078168A1 (es) Derivados de piperidinas y piperazinas, procesos para prepararlos y sus usos como moduladores de gpr119
Zhao et al. Selective synthesis of pyrazolo [5, 1-a] isoquinolines via 1, 3-dipolar cycloaddition reaction
CA2908542A1 (en) Novel compounds for selective histone deacetylase inhibitors, and pharmaceutical composition comprising the same
JP2013543842A5 (me)
RU2015119366A (ru) Смоляная смесь на основе смолы из сложных виниловых эфиров уретана и ее применение
NO20064309L (no) Azabicyklo(3.1.0)heksanderivater anvendelige som modulatorer for dopamin D3 receptorer
HRP20211193T1 (hr) Postupak za sintezu 2-hidroksi-6-((2-(1-izopropil-1h-pirazol-5-yl)-piridin-3-yl)metoksi)benzaldehida
TW200734337A (en) Phenoxypiperidines and analogs thereof useful as histamine H3 antagonists
JP2013047277A5 (me)
CA2844855A1 (en) Pim kinase inhibitors and preparation methods and use in medicinal manufacture thereof
MX2007005189A (es) Derivados de quinuclidina y su uso como antagonistas del receptor muscarinico m3.
DK2091948T3 (da) Nye inhibitorer af glutaminylcyclase
AU2007319151A1 (en) Sulfoximines as kinase inhibitors
PE20170664A1 (es) Agonistas del receptor de apelina(apj) y usos de los mismos
JP2010504286A5 (me)
AR075367A1 (es) Inhibidores de glucosilceramida sintasa
ES2714705T3 (es) Inhibidor de PDE4 novedoso
PE20090103A1 (es) DERIVADOS DE PIRIDINA Y PIRIMIDINA COMO ANTAGONISTAS DEL mGluR2
JP2016527184A5 (me)
ME01491B (me) Novi derivati dihidroindolona, postupak za njihovu pripremu i farmaceutski spojevi koji ih sadržavaju