JP6538556B2 - １−シアノ−２−（４−シクロプロピル−ベンジル）−４−（β−Ｄ−グルコピラノース−１−イル）−ベンゼンの結晶性錯体、その調製方法及び薬物を調製するためのその使用 - Google Patents

１−シアノ−２−（４−シクロプロピル−ベンジル）−４−（β−Ｄ−グルコピラノース−１−イル）−ベンゼンの結晶性錯体、その調製方法及び薬物を調製するためのその使用 Download PDF

Info

Publication number
JP6538556B2
JP6538556B2 JP2015523552A JP2015523552A JP6538556B2 JP 6538556 B2 JP6538556 B2 JP 6538556B2 JP 2015523552 A JP2015523552 A JP 2015523552A JP 2015523552 A JP2015523552 A JP 2015523552A JP 6538556 B2 JP6538556 B2 JP 6538556B2
Authority
JP
Japan
Prior art keywords
solution
benzene
glucopyranose
crystal
cyclopropyl
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2015523552A
Other languages
English (en)
Japanese (ja)
Other versions
JP2015522644A (ja
JP2015522644A5 (cg-RX-API-DMAC7.html
Inventor
マティアス エクハルト
マティアス エクハルト
ターニャ ブッツ
ターニャ ブッツ
ヒンメルスバッハ　フランク
フランク ヒンメルスバッハ
ハンス−ユルゲン マルティン
ハンス−ユルゲン マルティン
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Vetmedica GmbH
Original Assignee
Boehringer Ingelheim Vetmedica GmbH
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 Boehringer Ingelheim Vetmedica GmbH filed Critical Boehringer Ingelheim Vetmedica GmbH
Publication of JP2015522644A publication Critical patent/JP2015522644A/ja
Publication of JP2015522644A5 publication Critical patent/JP2015522644A5/ja
Application granted granted Critical
Publication of JP6538556B2 publication Critical patent/JP6538556B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
    • C07D309/10—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/04—Carbocyclic radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2015523552A 2012-07-26 2013-07-25 １−シアノ−２−（４−シクロプロピル−ベンジル）−４−（β−Ｄ−グルコピラノース−１−イル）−ベンゼンの結晶性錯体、その調製方法及び薬物を調製するためのその使用 Active JP6538556B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12177944 2012-07-26
EP12177944.1 2012-07-26
PCT/EP2013/065736 WO2014016381A1 (en) 2012-07-26 2013-07-25 CRYSTALLINE COMPLEX OF 1-CYANO-2-(4-CYCLOPROPYL-BENZYL)-4-(ß- D-GLUCOPYRANOS-1-YL)-BENZENE, METHODS FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2018089968A Division JP2018135384A (ja) 2012-07-26 2018-05-08 １−シアノ−２−（４−シクロプロピル−ベンジル）−４−（β−Ｄ−グルコピラノース−１−イル）−ベンゼンの結晶性錯体、その調製方法及び薬物を調製するためのその使用

Publications (3)

Publication Number Publication Date
JP2015522644A JP2015522644A (ja) 2015-08-06
JP2015522644A5 JP2015522644A5 (cg-RX-API-DMAC7.html) 2019-05-09
JP6538556B2 true JP6538556B2 (ja) 2019-07-03

Family

ID=48874313

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2015523552A Active JP6538556B2 (ja) 2012-07-26 2013-07-25 １−シアノ−２−（４−シクロプロピル−ベンジル）−４−（β−Ｄ−グルコピラノース−１−イル）−ベンゼンの結晶性錯体、その調製方法及び薬物を調製するためのその使用
JP2018089968A Pending JP2018135384A (ja) 2012-07-26 2018-05-08 １−シアノ−２−（４−シクロプロピル−ベンジル）−４−（β−Ｄ−グルコピラノース−１−イル）−ベンゼンの結晶性錯体、その調製方法及び薬物を調製するためのその使用

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2018089968A Pending JP2018135384A (ja) 2012-07-26 2018-05-08 １−シアノ−２−（４−シクロプロピル−ベンジル）−４−（β−Ｄ−グルコピラノース−１−イル）−ベンゼンの結晶性錯体、その調製方法及び薬物を調製するためのその使用

Country Status (23)

Country Link
US (1) US9145434B2 (cg-RX-API-DMAC7.html)
EP (3) EP2877460B1 (cg-RX-API-DMAC7.html)
JP (2) JP6538556B2 (cg-RX-API-DMAC7.html)
CN (2) CN104470908A (cg-RX-API-DMAC7.html)
AR (1) AR091908A1 (cg-RX-API-DMAC7.html)
AU (1) AU2013294947B2 (cg-RX-API-DMAC7.html)
BR (1) BR112015001327B1 (cg-RX-API-DMAC7.html)
CA (1) CA2878698C (cg-RX-API-DMAC7.html)
DK (2) DK3351539T3 (cg-RX-API-DMAC7.html)
EA (2) EA201600506A1 (cg-RX-API-DMAC7.html)
ES (2) ES2937665T3 (cg-RX-API-DMAC7.html)
FI (1) FI3351539T3 (cg-RX-API-DMAC7.html)
HR (2) HRP20230081T1 (cg-RX-API-DMAC7.html)
HU (1) HUE061450T2 (cg-RX-API-DMAC7.html)
LT (1) LT3351539T (cg-RX-API-DMAC7.html)
MX (1) MX357906B (cg-RX-API-DMAC7.html)
PL (2) PL2877460T3 (cg-RX-API-DMAC7.html)
PT (2) PT2877460T (cg-RX-API-DMAC7.html)
RS (1) RS63881B1 (cg-RX-API-DMAC7.html)
SG (1) SG11201500574QA (cg-RX-API-DMAC7.html)
SI (2) SI2877460T1 (cg-RX-API-DMAC7.html)
TW (1) TW201418275A (cg-RX-API-DMAC7.html)
WO (1) WO2014016381A1 (cg-RX-API-DMAC7.html)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9145434B2 (en) 2012-07-26 2015-09-29 Boehringer Ingelheim International Gmbh Crystalline complex of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(ss-d-glucopyranos-1-yl)-benzene, methods for its preparation and the use thereof for preparing medicaments
PL2981269T3 (pl) 2013-04-04 2024-02-05 Boehringer Ingelheim Vetmedica Gmbh Leczenie zaburzeń metabolicznych u zwierząt koniowatych
ES2859905T3 (es) 2013-12-17 2021-10-04 Boehringer Ingelheim Vetmedica Gmbh Inhibidores de SGLT2 para el tratamiento de trastornos metabólicos en animales felinos
US10603300B2 (en) * 2014-01-23 2020-03-31 Boehringer Ingelheim Vetmedica Gmbh Treatment of metabolic disorders in canine animals
ES2811261T3 (es) * 2014-04-01 2021-03-11 Boehringer Ingelheim Vetmedica Gmbh Tratamiento de trastornos metabólicos en animales equinos
CN103965020B (zh) * 2014-05-06 2015-09-09 启东东岳药业有限公司 制备5-碘-2-溴苄醇的方法
ES2991763T3 (es) 2014-09-25 2024-12-04 Boehringer Ingelheim Vetmedica Gmbh Tratamiento de combinación de inhibidores de SGLT2 y agonistas de dopamina para la prevención de trastornos metabólicos en animales equinos
PT3202772T (pt) * 2014-09-30 2020-11-20 Jiangsu Hengrui Medicine Co Cristal de um complexo de l-prolina/inibidor do cotransportador de sódio-glicose 2
CZ2015110A3 (cs) * 2015-02-18 2016-08-31 Zentiva, K.S. Pevné formy empagliflozinu
CN107995862B8 (zh) 2015-08-27 2021-12-03 勃林格殷格翰维特梅迪卡有限公司 包含sglt-2抑制剂之液态药物组合物
WO2017203457A1 (en) * 2016-05-26 2017-11-30 Dr. Reddy's Laboratories Limited Solid state forms of empagliflozin
KR102226465B1 (ko) * 2016-05-28 2021-03-11 하이난 수안주 파마 코포레이션 리미티드 나트륨-글루코스 공수송체 2에 대한 억제제의 결정형
CN111511725B (zh) * 2017-12-19 2024-04-09 勃林格殷格翰维特梅迪卡有限公司 1-氰基-2-(4-环丙基-苄基)-4-(β-D-吡喃葡萄糖-1-基)-苯、L-脯氨酸和水的1:1:1共晶体的合成
UY38969A (es) 2019-11-28 2021-05-31 Boehringer Ingelheim Vetmedica Gmbh Uso de inhibidores de sglt-2 en el secado de mamíferos no humanos
CN118615450A (zh) 2020-02-17 2024-09-10 勃林格殷格翰动物保健有限公司 Sglt-2抑制剂用于预防和/或治疗猫科动物的心脏疾病的用途
CA3223537A1 (en) 2021-07-28 2023-02-02 Boehringer Ingelheim Vetmedica Gmbh Use of sglt-2 inhibitors for the prevention and/or treatment of cardiac diseases in non-human mammals excluding felines, in particular canines
EP4376819A1 (en) 2021-07-28 2024-06-05 Boehringer Ingelheim Vetmedica GmbH Use of sglt-2 inhibitors for the prevention and/or treatment of hypertension in non-human mammals
JP2024525981A (ja) 2021-07-28 2024-07-12 ベーリンガー インゲルハイム フェトメディカ ゲーエムベーハー ヒト以外の哺乳動物における腎疾患の予防及び／又は治療のためのｓｇｌｔ－２阻害剤の使用
JP2025516857A (ja) 2022-05-25 2025-05-30 ベーリンガー インゲルハイム フェトメディカ ゲーエムベーハー Ｓｇｌｔ－２阻害薬を含む水性医薬組成物
AU2024233233A1 (en) 2023-03-06 2025-09-11 Boehringer Ingelheim Vetmedica Gmbh Systems for delivery of liquid pharmaceutical compositions in particular comprising one or more sglt-2 inhibitor(s)
WO2024223388A1 (en) 2023-04-24 2024-10-31 Boehringer Ingelheim Vetmedica Gmbh Crystalline complexes between velagliflozin and selected co-crystal forming agents, methods for their preparation and the use thereof for preparing medicaments
TW202508593A (zh) 2023-05-24 2025-03-01 德商百靈佳殷格翰維美迪加股份有限公司 包含一或多種sglt-2抑制劑及匹莫苯坦(pimobendan)及/或替米沙坦(telmisartan)之非人類哺乳動物心臟病之組合治療及/或預防
WO2024240633A1 (en) 2023-05-24 2024-11-28 Boehringer Ingelheim Vetmedica Gmbh Combination treatment and/or prevention of renal diseases and/or hypertension in non-human mammals comprising one or more sglt-2 inhibitors and telmisartan

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2258141T3 (es) 2001-04-11 2006-08-16 Bristol-Myers Squibb Company Complejos de aminoacidos de glucosidos c-arilo para el tratamiento de la diabetes y procedimiento.
US7927613B2 (en) * 2002-02-15 2011-04-19 University Of South Florida Pharmaceutical co-crystal compositions
EP1581543A4 (en) * 2003-01-03 2008-03-19 Bristol Myers Squibb Co METHODS FOR PRODUCING SGLT2 GLYCOSIS C-ARYL INHIBITORS
CN103435581B (zh) * 2004-03-16 2015-08-19 贝林格尔.英格海姆国际有限公司 吡喃葡萄糖基取代的苯基衍生物、含该化合物的药物、其用途及其制造方法
ATE491700T1 (de) * 2005-09-08 2011-01-15 Boehringer Ingelheim Int KRISTALLINE FORMEN VON 1-CHLORO-4-(ß-D-
ATE517099T1 (de) * 2006-02-15 2011-08-15 Boehringer Ingelheim Int Glucopyranosyl-substituierte benzonitril-derivate,pharmazeutische zusammensetzungen mit derartigen verbindungen, ihre verwendung und herstellungsverfahren dafür
TWI370818B (en) * 2006-04-05 2012-08-21 Astellas Pharma Inc Cocrystal of c-glycoside derivative and l-proline
PE20080697A1 (es) * 2006-05-03 2008-08-05 Boehringer Ingelheim Int Derivados de benzonitrilo sustituidos con glucopiranosilo, composiciones farmaceuticas que contienen compuestos de este tipo, su uso y procedimiento para su fabricacion
US7919598B2 (en) 2006-06-28 2011-04-05 Bristol-Myers Squibb Company Crystal structures of SGLT2 inhibitors and processes for preparing same
TW200817424A (en) 2006-08-04 2008-04-16 Daiichi Sankyo Co Ltd Benzylphenyl glucopyranoside derivatives
PE20090185A1 (es) 2007-03-22 2009-02-28 Bristol Myers Squibb Co Formulaciones farmaceuticas que contienen un inhibidor sglt2
EP2147008A2 (en) * 2007-05-18 2010-01-27 Bristol-Myers Squibb Company Crystal structures of sglt2 inhibitors and processes for preparing same
CN103319445B (zh) * 2007-12-27 2016-01-20 阿斯利康公司 Sglt2抑制剂的晶体结构及其制备方法
CN102177147A (zh) * 2008-08-22 2011-09-07 泰拉科斯有限公司 制备sglt2抑制剂的方法
AU2009286380B2 (en) 2008-08-28 2011-09-15 Pfizer Inc. Dioxa-bicyclo[3.2.1.]octane-2,3,4-triol derivatives
US20100167988A1 (en) 2008-10-22 2010-07-01 Auspex Pharmaceuticals, Inc. Ethoxyphenylmethyl inhibitors of sglt2
WO2011153712A1 (en) * 2010-06-12 2011-12-15 Theracos, Inc. Crystalline form of benzylbenzene sglt2 inhibitor
US9145434B2 (en) 2012-07-26 2015-09-29 Boehringer Ingelheim International Gmbh Crystalline complex of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(ss-d-glucopyranos-1-yl)-benzene, methods for its preparation and the use thereof for preparing medicaments
PL2981269T3 (pl) 2013-04-04 2024-02-05 Boehringer Ingelheim Vetmedica Gmbh Leczenie zaburzeń metabolicznych u zwierząt koniowatych

Also Published As

Publication number Publication date
WO2014016381A1 (en) 2014-01-30
ES2937665T3 (es) 2023-03-30
US20140031540A1 (en) 2014-01-30
US9145434B2 (en) 2015-09-29
JP2015522644A (ja) 2015-08-06
CN108774200A (zh) 2018-11-09
CA2878698A1 (en) 2014-01-30
MX2015000962A (es) 2015-04-16
MX357906B (es) 2018-07-30
RS63881B1 (sr) 2023-02-28
AR091908A1 (es) 2015-03-11
AU2013294947A1 (en) 2015-01-22
SI2877460T1 (sl) 2018-12-31
LT3351539T (lt) 2023-02-10
BR112015001327A2 (pt) 2017-07-04
DK3351539T3 (da) 2023-01-30
CA2878698C (en) 2021-03-23
PL3351539T3 (pl) 2023-03-06
JP2018135384A (ja) 2018-08-30
FI3351539T3 (fi) 2023-02-19
HRP20181972T1 (hr) 2019-01-25
EA201500038A1 (ru) 2015-07-30
ES2694675T3 (es) 2018-12-26
PT3351539T (pt) 2023-01-17
EA025438B1 (ru) 2016-12-30
TW201418275A (zh) 2014-05-16
PT2877460T (pt) 2018-12-19
EP3351539B1 (en) 2022-11-09
PL2877460T3 (pl) 2019-04-30
BR112015001327B1 (pt) 2022-08-16
AU2013294947B2 (en) 2017-03-30
EP3351539A1 (en) 2018-07-25
EP4166548A1 (en) 2023-04-19
HRP20230081T1 (hr) 2023-03-17
SG11201500574QA (en) 2015-02-27
EA201600506A1 (ru) 2017-03-31
SI3351539T1 (sl) 2023-03-31
EP2877460B1 (en) 2018-09-12
DK2877460T3 (en) 2019-01-07
HUE061450T2 (hu) 2023-07-28
EP2877460A1 (en) 2015-06-03
CN104470908A (zh) 2015-03-25

Similar Documents

Publication Publication Date Title
JP6538556B2 (ja) １−シアノ−２−（４−シクロプロピル−ベンジル）−４−（β−Ｄ−グルコピラノース−１−イル）−ベンゼンの結晶性錯体、その調製方法及び薬物を調製するためのその使用
JP5345846B2 (ja) １−クロロ−４−（β−Ｄ−グルコピラノス−１−イル）−２−（４−エチニル−ベンジル）−ベンゼンの結晶形態、その製造方法及び薬剤製造のためのそれらの使用
JP4226070B2 (ja) １−クロロ−４−（β−Ｄ−グルコピラノース−１−イル）−２−［４−（（Ｓ）−テトラヒドロフラン−３−イルオキシ）−ベンジル］−ベンゼンの結晶性形態、その調製方法及び薬物を調製するためのその使用
JP5091853B2 (ja) １−クロロ−４−（β−Ｄ−グルコピラノス−１−イル）−２−［４−（（Ｒ）−テトラヒドロフラン−３−イルオキシ）ベンジル］ベンゼンの結晶形、その調製方法及び薬剤を調製するための使用
JP5159788B2 (ja) １−（β−Ｄ−グルコピラノシル）−４−メチル−３−［５−（４−フルオロフェニル）−２−チエニルメチル］ベンゼン１／２水和物の結晶形
CA2667550A1 (en) Crystalline form of 4-(.beta.-d-glucopyranos-1-yl)-1-methyl-2-[4-((s)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160722

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20160722

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20170524

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20170525

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170824

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20180109

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180508

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20180515

A912 Re-examination (zenchi) completed and case transferred to appeal board

Free format text: JAPANESE INTERMEDIATE CODE: A912

Effective date: 20180615

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20190304

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20190322

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20190606

R150 Certificate of patent or registration of utility model

Ref document number: 6538556

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250