KR101831675B1 - 벤질벤젠 sglt2 억제제의 결정형 - Google Patents

벤질벤젠 sglt2 억제제의 결정형 Download PDF

Info

Publication number
KR101831675B1
KR101831675B1 KR1020137000844A KR20137000844A KR101831675B1 KR 101831675 B1 KR101831675 B1 KR 101831675B1 KR 1020137000844 A KR1020137000844 A KR 1020137000844A KR 20137000844 A KR20137000844 A KR 20137000844A KR 101831675 B1 KR101831675 B1 KR 101831675B1
Authority
KR
South Korea
Prior art keywords
compound
mixture
crystalline form
pyran
solution
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
KR1020137000844A
Other languages
English (en)
Korean (ko)
Other versions
KR20130090875A (ko
Inventor
맹츄앙 차이
퀴안 리우
지 수
빈후아 엘브
브라이언 시드
자크 와이. 로베르제
Original Assignee
테라코스 서브, 엘엘씨
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=45097470&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR101831675(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 테라코스 서브, 엘엘씨 filed Critical 테라코스 서브, 엘엘씨
Publication of KR20130090875A publication Critical patent/KR20130090875A/ko
Application granted granted Critical
Publication of KR101831675B1 publication Critical patent/KR101831675B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic 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
    • A61K31/351Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic 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
    • C07D309/08Heterocyclic 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
    • C07D309/10Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00Processes for the preparation of sugar derivatives
    • C07H1/06Separation; Purification
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/04Carbocyclic radicals

Landscapes

  • 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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (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)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (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)
KR1020137000844A 2010-06-12 2011-06-10 벤질벤젠 sglt2 억제제의 결정형 Active KR101831675B1 (ko)

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
KR20130090875A KR20130090875A (ko) 2013-08-14
KR101831675B1 true KR101831675B1 (ko) 2018-02-23

Family

ID=45097470

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020137000844A Active KR101831675B1 (ko) 2010-06-12 2011-06-10 벤질벤젠 sglt2 억제제의 결정형

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)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SMT201600475T1 (it) * 2008-08-22 2017-03-08 Theracos Sub Llc Procedimenti per la preparazione di inibitori di 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
FI2981269T3 (fi) 2013-04-04 2023-09-27 Boehringer Ingelheim Vetmedica Gmbh Aineenvaihduntahäiriöiden hoito hevoseläimillä
CN105611920B (zh) 2013-10-12 2021-07-16 泰拉科斯萨普有限责任公司 羟基-二苯甲烷衍生物的制备
RS64990B1 (sr) 2013-12-17 2024-01-31 Boehringer Ingelheim Vetmedica Gmbh Sglt-2 inhibitor za primenu u lečenju metaboličkog poremećaja kod životinja iz roda mačaka
EA201891406A1 (ru) 2014-01-23 2018-12-28 Бёрингер Ингельхайм Ветмедика Гмбх Лечение метаболических расстройств у представителей собачьих
CN106133887B (zh) * 2014-03-27 2019-11-08 三菱电机株式会社 半导体装置、半导体装置的制造方法
NZ723781A (en) 2014-04-01 2022-09-30 Boehringer Ingelheim Vetmedica Gmbh Treatment of metabolic disorders in equine animals
US10555958B2 (en) 2014-09-25 2020-02-11 Boehringer Ingelheim Vetmedica Gmbh Combination treatment of SGLT2 inhibitors and dopamine agonists for preventing metabolic disorders in equine animals
ES2999279T3 (en) 2015-08-27 2025-02-25 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
US11031285B2 (en) 2017-10-06 2021-06-08 Invensas Bonding Technologies, Inc. Diffusion barrier collar for interconnects
US20190343853A1 (en) * 2018-04-25 2019-11-14 Theracos Sub, Llc Methods of treating hypertension
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
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
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
WO2024240632A1 (en) 2023-05-24 2024-11-28 Boehringer Ingelheim Vetmedica Gmbh Combination treatment and/or prevention of cardiac diseases in non-human mammals comprising one or more sglt-2 inhibitors and pimobendan and/or telmisartan

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010022313A2 (en) * 2008-08-22 2010-02-25 Theracos, Inc. Processes for the preparation of sglt2 inhibitors

Family Cites Families (141)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA254853A (en) 1925-10-20 Wyatt Prentice Frank Radio train stop and telephone despatching system
US4499289A (en) 1982-12-03 1985-02-12 G. D. Searle & Co. Octahydronapthalenes
US4933438A (en) 1984-02-29 1990-06-12 University Of Florida Brain-specific analogues of centrally acting amines
US4613610A (en) 1984-06-22 1986-09-23 Sandoz Pharmaceuticals Corp. Cholesterol biosynthesis inhibiting pyrazole analogs of mevalonolactone and its derivatives
US4686237A (en) 1984-07-24 1987-08-11 Sandoz Pharmaceuticals Corp. Erythro-(E)-7-[3'-C1-3 alkyl-1'-(3",5"-dimethylphenyl)naphth-2'-yl]-3,5-dihydroxyhept-6-enoic acids and derivatives thereof
US4647576A (en) 1984-09-24 1987-03-03 Warner-Lambert Company Trans-6-[2-(substitutedpyrrol-1-yl)alkyl]-pyran-2-one inhibitors of cholesterol synthesis
US6150354A (en) 1987-01-15 2000-11-21 Bonnie Davis Compounds for the treatment of Alzheimer's disease
US4924024A (en) 1988-01-11 1990-05-08 E. R. Squibb & Sons, Inc. Phosphorus-containing squalene synthetase inhibitors, new intermediates and method
US4871721A (en) 1988-01-11 1989-10-03 E. R. Squibb & Sons, Inc. Phosphorus-containing squalene synthetase inhibitors
US5506219A (en) 1988-08-29 1996-04-09 E. R. Squibb & Sons, Inc. Pyridine anchors for HMG-CoA reductase inhibitors
US5753675A (en) 1989-03-03 1998-05-19 Novartis Pharmaceuticals Corporation Quinoline analogs of mevalonolactone and derivatives thereof
US5133974A (en) 1989-05-05 1992-07-28 Kv Pharmaceutical Company Extended release pharmaceutical formulations
CN1020944C (zh) 1990-01-30 1993-05-26 阿图尔-费希尔股份公司费希尔厂 紧固件
WO1992020327A1 (en) 1991-05-14 1992-11-26 Ernir Snorrason Treatment of fatigue syndrome with cholinesterase inhibitors
IT1250421B (it) 1991-05-30 1995-04-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato con proprieta' bio-adesive.
US5595872A (en) 1992-03-06 1997-01-21 Bristol-Myers Squibb Company Nucleic acids encoding microsomal trigyceride transfer protein
US5470845A (en) 1992-10-28 1995-11-28 Bristol-Myers Squibb Company Methods of using α-phosphonosulfonate squalene synthetase inhibitors including the treatment of atherosclerosis and hypercholesterolemia
WO1994011030A1 (en) 1992-11-13 1994-05-26 The Ohio State University Research Foundation C-glycoside analogues of n-(4-hydroxyphenyl)retinamide-o-glucuronide
US6537579B1 (en) 1993-02-22 2003-03-25 American Bioscience, Inc. Compositions and methods for administration of pharmacologically active compounds
US5739135A (en) 1993-09-03 1998-04-14 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
FR2710265B1 (fr) 1993-09-22 1995-10-20 Adir Composition pharmaceutique bioadhésive pour la libération contrôlée de principes actifs.
US5620997A (en) 1995-05-31 1997-04-15 Warner-Lambert Company Isothiazolones
US6548084B2 (en) 1995-07-20 2003-04-15 Smithkline Beecham Plc Controlled release compositions
US6245347B1 (en) 1995-07-28 2001-06-12 Zars, Inc. Methods and apparatus for improved administration of pharmaceutically active compounds
AU6966696A (en) 1995-10-05 1997-04-28 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
DE19541260A1 (de) 1995-11-06 1997-05-07 Lohmann Therapie Syst Lts Therapeutische Zubereitung zur transdermalen Applikation von Wirkstoffen durch die Haut
US5962440A (en) 1996-05-09 1999-10-05 Bristol-Myers Squibb Company Cyclic phosphonate ester inhibitors of microsomal triglyceride transfer protein and method
US5885983A (en) 1996-05-10 1999-03-23 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
US5827875A (en) 1996-05-10 1998-10-27 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
US6512010B1 (en) 1996-07-15 2003-01-28 Alza Corporation Formulations for the administration of fluoxetine
US6011155A (en) 1996-11-07 2000-01-04 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US5760246A (en) 1996-12-17 1998-06-02 Biller; Scott A. Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method
WO1998031697A1 (en) 1997-01-15 1998-07-23 Sankyo Company, Limited Aryl c-glycoside compounds and sulfated esters thereof
WO1999012524A1 (en) 1997-09-11 1999-03-18 Nycomed Danmark A/S MODIFIED RELEASE MULTIPLE-UNITS COMPOSITIONS OF NON-STEROID ANTI-INFLAMMATORY DRUG SUBSTANCES (NSAIDs)
US6624200B2 (en) 1998-08-25 2003-09-23 Columbia Laboratories, Inc. Bioadhesive progressive hydration tablets
US6607751B1 (en) 1997-10-10 2003-08-19 Intellipharamaceutics Corp. Controlled release delivery device for pharmaceutical agents incorporating microbial polysaccharide gum
US6403597B1 (en) 1997-10-28 2002-06-11 Vivus, Inc. Administration of phosphodiesterase inhibitors for the treatment of premature ejaculation
US6248864B1 (en) 1997-12-31 2001-06-19 Adherex Technologies, Inc. Compounds and methods and modulating tissue permeability
US6613358B2 (en) 1998-03-18 2003-09-02 Theodore W. Randolph Sustained-release composition including amorphous polymer
US6312717B1 (en) 1998-07-07 2001-11-06 Bristol-Myers Squibb Company Method for treatment of anxiety and depression
US6197798B1 (en) 1998-07-21 2001-03-06 Novartis Ag Amino-benzocycloalkane derivatives
US20020009478A1 (en) 1998-08-24 2002-01-24 Douglas Joseph Dobrozsi Oral liquid mucoadhesive compositions
SE9802864D0 (sv) 1998-08-27 1998-08-27 Pharmacia & Upjohn Ab Transdermally administered tolterodine as antimuscarinic agent for the treatment of overactive bladder
US6069238A (en) 1998-09-30 2000-05-30 Eli Lilly And Company Spirocyclic C-glycosides
AU764866B2 (en) 1998-10-01 2003-09-04 Novartis Ag New sustained release oral formulations
US6283719B1 (en) * 1998-11-05 2001-09-04 Frantz Medical Development Ltd Detecting obstructions in enteral/parenteral feeding tubes and automatic removal of clogs therefrom
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US6548529B1 (en) 1999-04-05 2003-04-15 Bristol-Myers Squibb Company Heterocyclic containing biphenyl aP2 inhibitors and method
US7407978B2 (en) 1999-04-06 2008-08-05 Theracos, Inc. Heterocyclic analogs of diphenylethylene compounds
FR2792527B1 (fr) 1999-04-22 2004-08-13 Ethypharm Lab Prod Ethiques Microgranules de ketoprofene, procede de preparation et compositions pharmaceutiques
US6172081B1 (en) 1999-06-24 2001-01-09 Novartis Ag Tetrahydroisoquinoline 3-carboxamide derivatives
US6541020B1 (en) 1999-07-09 2003-04-01 Trimeris, Inc. Methods and compositions for administration of therapeutic reagents
DE19933926A1 (de) 1999-07-20 2001-01-25 Boehringer Ingelheim Pharma Biphenylderivate, ihre Herstellung und ihre Verwendung als Arzneimittel
US6562375B1 (en) 1999-08-04 2003-05-13 Yamanouchi Pharmaceuticals, Co., Ltd. Stable pharmaceutical composition for oral use
AU781048B2 (en) 1999-09-02 2005-05-05 Nostrum Pharmaceuticals, Inc. Controlled release pellet formulation
US6544548B1 (en) 1999-09-13 2003-04-08 Keraplast Technologies, Ltd. Keratin-based powders and hydrogel for pharmaceutical applications
US6515117B2 (en) 1999-10-12 2003-02-04 Bristol-Myers Squibb Company C-aryl glucoside SGLT2 inhibitors and method
PH12000002657B1 (en) * 1999-10-12 2006-02-21 Bristol Myers Squibb Co C-aryl glucoside SGLT2 inhibitors
US6080736A (en) 1999-10-27 2000-06-27 Janus Pharmaceuticals, Inc. Methods and compositions for treating and preventing anxiety and anxiety disorders using optically pure (R) tofisopam
US6461631B1 (en) 1999-11-16 2002-10-08 Atrix Laboratories, Inc. Biodegradable polymer composition
DE19963234A1 (de) 1999-12-27 2002-01-24 Boehringer Ingelheim Pharma Substituierte Piperazinderivate, ihre Herstellung und ihre Verwendung als Arzneimittel
WO2001047501A1 (en) 1999-12-29 2001-07-05 Nanodelivery, Inc. Drug delivery system exhibiting permeability control
EP1259484B1 (en) 2000-01-18 2005-05-18 Novartis AG Carboxamides useful as inhibitors of microsomal triglyceride transfer protein and of apolipoprotein b secretion
WO2001054694A1 (en) 2000-01-28 2001-08-02 Bristol-Myers Squibb Company Tetrahydropyrimidone inhibitors of fatty acid binding protein and method
US6555519B2 (en) 2000-03-30 2003-04-29 Bristol-Myers Squibb Company O-glucosylated benzamide SGLT2 inhibitors and method
US6683056B2 (en) 2000-03-30 2004-01-27 Bristol-Myers Squibb Company O-aryl glucoside SGLT2 inhibitors and method
US6589549B2 (en) 2000-04-27 2003-07-08 Macromed, Incorporated Bioactive agent delivering system comprised of microparticles within a biodegradable to improve release profiles
US6524621B2 (en) 2000-05-01 2003-02-25 Aeropharm Technology Inc. Core formulation
US6432969B1 (en) 2000-06-13 2002-08-13 Novartis Ag N-(substituted glycyl)-2 cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6482440B2 (en) 2000-09-21 2002-11-19 Phase 2 Discovery, Inc. Long acting antidepressant microparticles
AU2002215218A1 (en) 2000-11-17 2002-05-27 Takeda Chemical Industries Ltd. Isoxazole derivatives
WO2002040448A1 (en) 2000-11-20 2002-05-23 Bristol-Myers Squibb Company Pyridone derivatives as ap2 inhibitors
TWI255817B (en) 2001-02-14 2006-06-01 Kissei Pharmaceutical Glucopyranosyloxybenzylbenzene derivatives and medicinal use thereof
US6524615B2 (en) 2001-02-21 2003-02-25 Kos Pharmaceuticals, Incorporated Controlled release pharmaceutical composition
US6936590B2 (en) 2001-03-13 2005-08-30 Bristol Myers Squibb Company C-aryl glucoside SGLT2 inhibitors and method
DE60209343T2 (de) 2001-04-11 2006-10-26 Bristol-Myers Squibb Co. Aminosäurekomplexe von c-arylglycosiden zur behandlung von diabetes und verfahren
US6869947B2 (en) 2001-07-03 2005-03-22 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
EP1414461A4 (en) 2001-07-13 2005-10-26 Bristol Myers Squibb Co PYRAZINONE INHIBITORS OF FATTY ACID BINDING PROTEIN AND METHOD
EP1432720A1 (en) 2001-09-05 2004-06-30 Bristol-Myers Squibb Company O-pyrazole glucoside sglt2 inhibitors and method of use
JP2003080635A (ja) * 2001-09-12 2003-03-19 Teijin Meton Kk 合成樹脂複合構造体、それからなる浴室構成品及びその製造方法
EP1443919A4 (en) 2001-11-16 2006-03-22 Bristol Myers Squibb Co DOUBLE INHIBITORS OF THE FATTY ACID BINDING PROTEIN OF THE ADIPOCYTES AND THE FATTY ACID BINDING PROTEIN OF KERATINOCYTES
US6727261B2 (en) 2001-12-27 2004-04-27 Hoffman-La Roche Inc. Pyrido[2,1-A]Isoquinoline derivatives
MXPA04009229A (es) 2002-03-22 2004-11-26 Kissei Pharmaceutical Cristales derivados de glucopiranosiloxibencil benceno.
US6710040B1 (en) 2002-06-04 2004-03-23 Pfizer Inc. Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors
CA2494179C (en) 2002-08-08 2012-04-24 Kissei Pharmaceutical Co., Ltd. Pyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate for production thereof
RU2322449C2 (ru) 2002-08-09 2008-04-20 Тайсо Фармасьютикал Ко., Лтд. ПРОИЗВОДНЫЕ АРИЛ 5-ТИО-β-D-ГЛЮКОПИРАНОЗИДА И ТЕРАПЕВТИЧЕСКИЕ СРЕДСТВА ПРИ ДИАБЕТЕ, СОДЕРЖАЩИЕ ИХ
US6700238B1 (en) * 2002-08-13 2004-03-02 Wei Tong Generator gas shield and related method
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
JP2006516257A (ja) 2003-01-03 2006-06-29 ブリストル−マイヤーズ スクイブ カンパニー C−アリールグルコシドsglt2阻害剤の製造法
JP4222450B2 (ja) 2003-03-14 2009-02-12 アステラス製薬株式会社 C−グリコシド誘導体又はその塩
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
WO2005012242A2 (en) 2003-08-01 2005-02-10 Janssen Pharmaceutica Nv Substituted benzimidazole-, benztriazole-, and benzimidazolone-o-glucosides
RS53365B (sr) 2003-08-01 2014-10-31 Mitsubishi Tanabe Pharma Corporation Nova jedinjenja koja imaju inhibitorno dejstvo na transporter glukoze zavisan od natrijuma
US7094763B2 (en) 2003-08-01 2006-08-22 Janssen Pharaceutica, N.V. Substituted fused heterocyclic C-glycosides
US7375090B2 (en) 2003-08-26 2008-05-20 Boehringer Ingelheim International Gmbh Glucopyranosyloxy-pyrazoles, pharmaceutical compositions containing these compounds, the use thereof and processed for the preparation thereof
CA2539032A1 (en) 2003-08-26 2005-03-10 Boehringer Ingelheim International Gmbh Glucopyranosyloxy-pirazoles, drugs containing said compounds the use and production method thereof
DE10361133A1 (de) 2003-12-22 2005-07-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Glucopyranosyloxy-substituierte Aromaten, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US7371732B2 (en) 2003-12-22 2008-05-13 Boehringer Ingelheim International Gmbh Glucopyranosyloxy-substituted aromatic compounds, medicaments containing such compounds, their use and process for their manufacture
AU2005219779B2 (en) 2004-03-04 2011-04-14 Kissei Pharmaceutical Co., Ltd. Fused heterocycle derivative, medicinal composition containing the same, and medicinal use thereof
CN103467423B (zh) 2004-03-16 2016-03-16 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
US20070185197A1 (en) 2004-03-31 2007-08-09 Hideki Fujikura Phenol derivative, medicinal composition containing the same, and medicinal use thereof
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
DE102004034690A1 (de) 2004-07-17 2006-02-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Methyliden-D-xylopyranosyl-und Oxo-D-xylopyranosyl-substituierte Phenyle, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
TW200606129A (en) 2004-07-26 2006-02-16 Chugai Pharmaceutical Co Ltd Novel cyclohexane derivative, its prodrug, its salt and diabetic therapeutic agent containing the same
CA2574451A1 (en) 2004-07-27 2006-02-02 Boehringer Ingelheim International Gmbh D-glucopyranosyl phenyl-substituted cyclene, medicaments containing these compounds, their use, and method for the production thereof
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
AR051446A1 (es) 2004-09-23 2007-01-17 Bristol Myers Squibb Co Glucosidos de c-arilo como inhibidores selectivos de transportadores de glucosa (sglt2)
DE102004048388A1 (de) 2004-10-01 2006-04-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg D-Pyranosyl-substituierte Phenyle, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
EP1828216B1 (en) 2004-12-16 2008-09-10 Boehringer Ingelheim International GmbH Glucopyranosyl-substituted benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
TW200637839A (en) 2005-01-07 2006-11-01 Taisho Pharmaceutical Co Ltd 1-thio-d-glucitol derivatives
TW200637869A (en) 2005-01-28 2006-11-01 Chugai Pharmaceutical Co Ltd The spiroketal derivatives and the use as therapeutical agent for diabetes of the same
WO2006089872A1 (en) 2005-02-23 2006-08-31 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituted ( (hetero)arylethynyl-benzyd-benzene derivatives and use thereof as sodium-dependent glucose cotransporter 2 (sglt2) inhibitors
AR053710A1 (es) 2005-04-11 2007-05-16 Xenon Pharmaceuticals Inc Compuestos espiroheterociclicos y sus usos como agentes terapeuticos
EP1874787B1 (en) 2005-04-15 2009-12-30 Boehringer Ingelheim International GmbH Glucopyranosyl-substituted (heteroaryloxy-benzyl)-benzene derivatives as sglt inhibitors
UA91546C2 (uk) 2005-05-03 2010-08-10 Бьорінгер Інгельхайм Інтернаціональ Гмбх КРИСТАЛІЧНА ФОРМА 1-ХЛОР-4-(β-D-ГЛЮКОПІРАНОЗ-1-ИЛ)-2-[4-((S)-ТЕТРАГІДРОФУРАН-3-ІЛОКСИ)-БЕНЗИЛ]-БЕНЗОЛУ, СПОСІБ ЇЇ ОДЕРЖАННЯ ТА ЇЇ ЗАСТОСУВАННЯ ПРИ ПРИГОТУВАННІ ЛІКАРСЬКИХ ЗАСОБІВ
US7723309B2 (en) 2005-05-03 2010-05-25 Boehringer Ingelheim International Gmbh Crystalline forms of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((R)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments
US7772191B2 (en) 2005-05-10 2010-08-10 Boehringer Ingelheim International Gmbh Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein
WO2007000445A1 (en) 2005-06-29 2007-01-04 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituted benzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
JP2007007628A (ja) * 2005-07-04 2007-01-18 Hokkaido Univ セメントコンクリートの中性化促進方法
TW200726755A (en) 2005-07-07 2007-07-16 Astellas Pharma Inc A crystalline choline salt of an azulene derivative
WO2007014894A2 (en) 2005-07-27 2007-02-08 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituted ( (hetero) cycloalyklethynyl-benzyl) -benzene derivatives and use thereof as sodium-dependent glucose cotransporter (sglt) inhibitors
GB0516156D0 (en) 2005-08-05 2005-09-14 Eisai London Res Lab Ltd JNK 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
WO2007028814A1 (en) 2005-09-08 2007-03-15 Boehringer Ingelheim International Gmbh CRYSTALLINE FORMS OF 1-CHLORO-4-(ß-D-GLUCOPYRANOS-1-YL)-2-(4-ETHYNYL-BENZYL)-BENZENE, METHODS FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS
TWI370818B (en) 2006-04-05 2012-08-21 Astellas Pharma Inc Cocrystal of c-glycoside derivative and l-proline
JP5067644B2 (ja) 2006-05-19 2012-11-07 大正製薬株式会社 C−フェニルグリシト−ル化合物
US7803778B2 (en) 2006-05-23 2010-09-28 Theracos, Inc. Glucose transport inhibitors and methods of use
US7919598B2 (en) 2006-06-28 2011-04-05 Bristol-Myers Squibb Company Crystal structures of SGLT2 inhibitors and processes for preparing same
US20080027014A1 (en) 2006-07-28 2008-01-31 Tanabe Seiyaku Co., Ltd. Novel SGLT inhibitors
JP2010507629A (ja) * 2006-10-27 2010-03-11 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 4−(β−D−グルコピラノス−1−イル)−1−メチル−2−[4−((S)−テトラヒドロフラン−3−イルオキシ)−ベンジル]−ベンゼンの結晶形、その製造方法及び医薬品を製造するための使用
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
AU2008232419B2 (en) 2007-04-02 2013-06-20 Theracos, Inc. Benzylic glycoside derivatives and methods of use
US20080287529A1 (en) * 2007-05-18 2008-11-20 Bristol-Myers Squibb Company Crystal structures of sglt2 inhibitors and processes for preparing same
UA107175C2 (uk) * 2007-07-26 2014-12-10 Спосіб і сполука, призначені для одержання інгібіторів контранспортера натрій-глюкози 2 типу, варіанти
UA99924C2 (en) * 2007-08-23 2012-10-25 Теракос, Инк. Benzylbenzol derivatives and using thereof
NO2200606T3 (enExample) 2007-09-10 2018-03-24
CL2009000309A1 (es) * 2008-02-13 2009-06-26 Sanofi Aventis Derivados fluoroglicosidos aromaticos, composicion farmaceutica que contenga estos compuestos, procedimiento para prepararla y su uso en el tratamiento de la diabetes tipo 1 y 2.
TWI523652B (zh) 2008-07-15 2016-03-01 泰瑞克公司 氘化苄基苯衍生物及使用方法
TW201023858A (en) * 2008-09-18 2010-07-01 Ortho Mcneil Janssen Pharm Synergistic combinations of a macrocyclic inhibitor of HCV and a nucleoside
WO2011153712A1 (en) * 2010-06-12 2011-12-15 Theracos, Inc. Crystalline form of benzylbenzene sglt2 inhibitor

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010022313A2 (en) * 2008-08-22 2010-02-25 Theracos, Inc. Processes for the preparation of sglt2 inhibitors

Also Published As

Publication number Publication date
PH12012502395A1 (en) 2013-03-25
CA2800379C (en) 2018-05-01
US10981942B2 (en) 2021-04-20
AU2011264220B2 (en) 2015-05-21
RS57653B1 (sr) 2018-11-30
SG186206A1 (en) 2013-01-30
US20200239510A1 (en) 2020-07-30
WO2011153712A1 (en) 2011-12-15
US10533032B2 (en) 2020-01-14
WO2011153953A1 (en) 2011-12-15
AU2011264220A1 (en) 2013-01-24
HUE040355T2 (hu) 2019-03-28
JP5842191B2 (ja) 2016-01-13
DK2580225T3 (en) 2018-09-03
UA108887C2 (xx) 2015-06-25
MY184925A (en) 2021-04-30
RU2569491C2 (ru) 2015-11-27
ES2683123T3 (es) 2018-09-25
US20180118773A1 (en) 2018-05-03
HRP20181695T1 (hr) 2018-12-14
JP2013528190A (ja) 2013-07-08
MX342665B (es) 2016-10-07
KR20130090875A (ko) 2013-08-14
RU2013101580A (ru) 2014-07-20
IL223205B (en) 2020-05-31
SI2580225T1 (sl) 2018-10-30
TWI589295B (zh) 2017-07-01
CN102933592B (zh) 2016-03-16
EP2580225A1 (en) 2013-04-17
MX2012014423A (es) 2013-05-01
US20150266915A1 (en) 2015-09-24
TW201212924A (en) 2012-04-01
PL2580225T3 (pl) 2019-02-28
US20120238510A1 (en) 2012-09-20
CO6640246A2 (es) 2013-03-22
NZ605570A (en) 2014-03-28
CY1120690T1 (el) 2019-12-11
LT2580225T (lt) 2018-08-10
US20140011754A9 (en) 2014-01-09
CN102933592A (zh) 2013-02-13
PT2580225T (pt) 2018-10-26
EP2580225B1 (en) 2018-07-18
ZA201300004B (en) 2017-08-30
US8987323B2 (en) 2015-03-24
EP2580225A4 (en) 2013-11-06
MA34371B1 (fr) 2013-07-03
BR112012031616A2 (pt) 2017-05-16
CA2800379A1 (en) 2011-12-15
US9834573B2 (en) 2017-12-05
SMT201800475T1 (it) 2018-11-09
AR121997A2 (es) 2022-08-03

Similar Documents

Publication Publication Date Title
US10981942B2 (en) Crystalline form of benzylbenzene SGLT2 inhibitor
EP2187742B1 (en) (2s,3r,4r,5s,6r)-2-(4-chloro-3-benzylphenyl)-6-(hydroxymethyl)tetrahydro-2h-pyran-3,4,5-triol derivatives for use in the treatment of diabetes
KR101654231B1 (ko) Sglt2 억제제의 제조방법
CA2707909C (en) Benzylphenyl cyclohexane derivatives and methods of use
HK1184150A (en) Crystalline form of benzylbenzene sglt2 inhibitor
HK1184150B (en) Crystalline form of benzylbenzene sglt2 inhibitor
HK1142229B (en) (2s,3r,4r,5s,6r)-2-(4-chloro-3-benzylphenyl)-6-(hydroxymethyl)tetrahydro-2h-pyran-3,4,5-triol derivatives for use in the treatment of diabetes
HK1142229A (en) (2s,3r,4r,5s,6r)-2-(4-chloro-3-benzylphenyl)-6-(hydroxymethyl)tetrahydro-2h-pyran-3,4,5-triol derivatives for use in the treatment of diabetes

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20130111

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
N231 Notification of change of applicant
PN2301 Change of applicant

Patent event date: 20151030

Comment text: Notification of Change of Applicant

Patent event code: PN23011R01D

A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20160610

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20171123

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20180126

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20180219

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20180220

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
PR1001 Payment of annual fee

Payment date: 20210115

Start annual number: 4

End annual number: 4

PR1001 Payment of annual fee

Payment date: 20230117

Start annual number: 6

End annual number: 6

PR1001 Payment of annual fee

Payment date: 20240109

Start annual number: 7

End annual number: 7

PR1001 Payment of annual fee

Payment date: 20250106

Start annual number: 8

End annual number: 8