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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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
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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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Classifications

    • 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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (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 (enExample)
EP (1) EP2580225B1 (enExample)
JP (1) JP5842191B2 (enExample)
KR (1) KR101831675B1 (enExample)
CN (1) CN102933592B (enExample)
AR (1) AR121997A2 (enExample)
AU (1) AU2011264220B2 (enExample)
BR (1) BR112012031616A2 (enExample)
CA (1) CA2800379C (enExample)
CO (1) CO6640246A2 (enExample)
CY (1) CY1120690T1 (enExample)
DK (1) DK2580225T3 (enExample)
ES (1) ES2683123T3 (enExample)
HR (1) HRP20181695T1 (enExample)
HU (1) HUE040355T2 (enExample)
IL (1) IL223205B (enExample)
LT (1) LT2580225T (enExample)
MA (1) MA34371B1 (enExample)
MX (1) MX342665B (enExample)
MY (1) MY184925A (enExample)
NZ (1) NZ605570A (enExample)
PH (1) PH12012502395A1 (enExample)
PL (1) PL2580225T3 (enExample)
PT (1) PT2580225T (enExample)
RS (1) RS57653B1 (enExample)
RU (1) RU2569491C2 (enExample)
SG (1) SG186206A1 (enExample)
SI (1) SI2580225T1 (enExample)
SM (1) SMT201800475T1 (enExample)
TW (1) TWI589295B (enExample)
UA (1) UA108887C2 (enExample)
WO (2) WO2011153712A1 (enExample)
ZA (1) ZA201300004B (enExample)

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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
ES2959444T3 (es) * 2013-04-04 2024-02-26 Boehringer Ingelheim Vetmedica Gmbh Tratamiento de trastornos metabólicos en animales equinos
WO2015051484A1 (en) * 2013-10-12 2015-04-16 Theracos, Inc. Preparation of hydroxy-benzylbenzene derivatives
EP3082829B1 (en) 2013-12-17 2021-02-17 Boehringer Ingelheim Vetmedica GmbH Sglt2 inhibitors for the treatment of metabolic disorders in feline animals
EA032558B1 (ru) 2014-01-23 2019-06-28 Бёрингер Ингельхайм Ветмедика Гмбх Лечение метаболических расстройств у представителей собачьих
US9887131B2 (en) * 2014-03-27 2018-02-06 Mitsubishi Electric Corporation Semiconductor device having a Pd-containing adhesion layer
DK3721882T3 (da) 2014-04-01 2024-10-21 Boehringer Ingelheim Vetmedica Gmbh Behandling af hypofyse pars intermedia-dysfunktion hos hestedyr
KR102539788B1 (ko) * 2014-09-25 2023-06-07 베링거잉겔하임베트메디카게엠베하 말과 동물의 대사 장애를 예방하기 위한 sglt2 억제제와 도파민 작용제의 병용 치료
MX389367B (es) 2015-08-27 2025-03-20 Boehringer Ingelheim Vetmedica Gmbh Composiciones farmaceuticas liquidas que comprenden inhibidores de sglt-2.
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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US12274689B2 (en) 2019-03-14 2025-04-15 Increvet, Inc. Compound for the management of feline diabetes
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
KR102716551B1 (ko) 2019-04-26 2024-10-15 메르크 파텐트 게엠베하 경화막의 제조방법 및 이의 용도
KR20220143732A (ko) 2020-02-17 2022-10-25 베링거잉겔하임베트메디카게엠베하 고양이과에서 심장 질환을 예방 및/또는 치료하기 위한 sglt-2 억제제의 사용
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GB202213849D0 (en) * 2022-09-22 2022-11-09 Macfarlan Smith Ltd Crystalline forms of bexagliflozin, processes for the preparation and use thereof
CN118206515A (zh) * 2022-12-16 2024-06-18 广东东阳光药业股份有限公司 吡喃葡萄糖基衍生物的晶型及其用途
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