CA2800379C - Crystalline form of benzylbenzene sglt2 inhibitor - Google Patents

Crystalline form of benzylbenzene sglt2 inhibitor Download PDF

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Publication number
CA2800379C
CA2800379C CA2800379A CA2800379A CA2800379C CA 2800379 C CA2800379 C CA 2800379C CA 2800379 A CA2800379 A CA 2800379A CA 2800379 A CA2800379 A CA 2800379A CA 2800379 C CA2800379 C CA 2800379C
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CA
Canada
Prior art keywords
crystalline form
compound
mixture
cyclopropoxyethoxy
chloro
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CA2800379A
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English (en)
French (fr)
Other versions
CA2800379A1 (en
Inventor
Mengzhuang Cai
Qian Liu
Ge Xu
Binhua Lv
Brian Seed
Jacques Y. Roberge
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.)
Theracosbio LLC
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THERACOS SUB LLC
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Application filed by THERACOS SUB LLC filed Critical THERACOS SUB LLC
Publication of CA2800379A1 publication Critical patent/CA2800379A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C07H1/06—Separation; Purification
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrane Compounds (AREA)
CA2800379A 2010-06-12 2011-06-10 Crystalline form of benzylbenzene sglt2 inhibitor Active CA2800379C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/CN2010/073865 WO2011153712A1 (en) 2010-06-12 2010-06-12 Crystalline form of benzylbenzene sglt2 inhibitor
CNPCT/CN2010/073865 2010-06-12
PCT/CN2011/075554 WO2011153953A1 (en) 2010-06-12 2011-06-10 Crystalline form of benzylbenzene sglt2 inhibitor

Publications (2)

Publication Number Publication Date
CA2800379A1 CA2800379A1 (en) 2011-12-15
CA2800379C true CA2800379C (en) 2018-05-01

Family

ID=45097470

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2800379A Active CA2800379C (en) 2010-06-12 2011-06-10 Crystalline form of benzylbenzene sglt2 inhibitor

Country Status (33)

Country Link
US (4) US8987323B2 (https=)
EP (1) EP2580225B1 (https=)
JP (1) JP5842191B2 (https=)
KR (1) KR101831675B1 (https=)
CN (1) CN102933592B (https=)
AR (1) AR121997A2 (https=)
AU (1) AU2011264220B2 (https=)
BR (1) BR112012031616A2 (https=)
CA (1) CA2800379C (https=)
CO (1) CO6640246A2 (https=)
CY (1) CY1120690T1 (https=)
DK (1) DK2580225T3 (https=)
ES (1) ES2683123T3 (https=)
HR (1) HRP20181695T1 (https=)
HU (1) HUE040355T2 (https=)
IL (1) IL223205B (https=)
LT (1) LT2580225T (https=)
MA (1) MA34371B1 (https=)
MX (1) MX342665B (https=)
MY (1) MY184925A (https=)
NZ (1) NZ605570A (https=)
PH (1) PH12012502395A1 (https=)
PL (1) PL2580225T3 (https=)
PT (1) PT2580225T (https=)
RS (1) RS57653B1 (https=)
RU (1) RU2569491C2 (https=)
SG (1) SG186206A1 (https=)
SI (1) SI2580225T1 (https=)
SM (1) SMT201800475T1 (https=)
TW (1) TWI589295B (https=)
UA (1) UA108887C2 (https=)
WO (2) WO2011153712A1 (https=)
ZA (1) ZA201300004B (https=)

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MX2011001855A (es) * 2008-08-22 2011-03-24 Theracos Inc Procesos para la preparacion de inhibidores de 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
DK2981269T3 (da) * 2013-04-04 2023-10-23 Boehringer Ingelheim Vetmedica Gmbh Behandling af stofskifteforstyrrelser hos hestedyr
WO2015051484A1 (en) * 2013-10-12 2015-04-16 Theracos, Inc. Preparation of hydroxy-benzylbenzene derivatives
MX376097B (es) 2013-12-17 2025-03-07 Boehringer Ingelheim Vetmedica Gmbh Inhibidores de sglt2 para usarse en el tratamiento o prevención de trastornos metabólicos en animales felinos.
CA2932674C (en) 2014-01-23 2023-01-24 Boehringer Ingelheim Vetmedica Gmbh Treatment of metabolic disorders in canine animals
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AU2016310535B2 (en) 2015-08-27 2021-08-19 Boehringer Ingelheim Vetmedica Gmbh Liquid pharmaceutical compositions comprising SGLT-2 inhibitors
CN108239055B (zh) * 2016-12-23 2023-07-18 杭州领业医药科技有限公司 一种thr1442 l-天冬氨酸共晶、其制备方法及药物组合物
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WO2019209998A1 (en) * 2018-04-25 2019-10-31 Theracos Sub, Llc Methods of treating hypertension
CN113613719A (zh) 2019-03-14 2021-11-05 印可瑞维特有限公司 控制猫糖尿病的化合物
KR20250136439A (ko) 2019-04-26 2025-09-16 메르크 파텐트 게엠베하 경화막의 제조방법 및 이의 용도
JP2020183506A (ja) * 2019-04-26 2020-11-12 メルク、パテント、ゲゼルシャフト、ミット、ベシュレンクテル、ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ ＧｍｂＨ 硬化膜の製造方法、およびその使用
JP7423800B2 (ja) 2020-02-17 2024-01-29 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 ネコにおける心臓疾患の予防および／または治療のためのｓｇｌｔ－２阻害剤の使用
WO2022073151A1 (en) 2020-10-05 2022-04-14 Theracos Sub, Llc Pharmaceutical formulations
GB202213849D0 (en) * 2022-09-22 2022-11-09 Macfarlan Smith Ltd Crystalline forms of bexagliflozin, processes for the preparation and use thereof
TW202440535A (zh) * 2022-12-16 2024-10-16 大陸商廣東東陽光藥業股份有限公司 吡喃葡萄糖基衍生物的晶型及其用途
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

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