WO2011153953A1 - Crystalline form of benzylbenzene sglt2 inhibitor - Google Patents
Crystalline form of benzylbenzene sglt2 inhibitor Download PDFInfo
- Publication number
- WO2011153953A1 WO2011153953A1 PCT/CN2011/075554 CN2011075554W WO2011153953A1 WO 2011153953 A1 WO2011153953 A1 WO 2011153953A1 CN 2011075554 W CN2011075554 W CN 2011075554W WO 2011153953 A1 WO2011153953 A1 WO 2011153953A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- crystalline form
- solvent
- mixture
- xrpd
- compound
- Prior art date
Links
- DIVLHXCRCGXYFE-TWZFXSIXSA-N OC[C@H](C[C@@H](C1)O)O[C@H]1C1C=CC(Cl)=C(Cc(cc2)ccc2OCCOC2CC2)C1 Chemical compound OC[C@H](C[C@@H](C1)O)O[C@H]1C1C=CC(Cl)=C(Cc(cc2)ccc2OCCOC2CC2)C1 DIVLHXCRCGXYFE-TWZFXSIXSA-N 0.000 description 1
- CDPAQRCAQDPXFZ-NGYIFUPDSA-N OC[C@H](C[C@@H](C1)O)O[C@H]1c(cc1Cc(cc2)ccc2OCCOC2CC2)ccc1Cl Chemical compound OC[C@H](C[C@@H](C1)O)O[C@H]1c(cc1Cc(cc2)ccc2OCCOC2CC2)ccc1Cl CDPAQRCAQDPXFZ-NGYIFUPDSA-N 0.000 description 1
Classifications
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- 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
-
- 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
- C07H1/00—Processes for the preparation of sugar derivatives
- C07H1/06—Separation; Purification
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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)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (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)
Abstract
Description
Claims
Priority Applications (24)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PL11791943T PL2580225T3 (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene sglt2 inhibitor |
JP2013513540A JP5842191B2 (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene SGLT2 inhibitor |
MYPI2012005263A MY184925A (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene sglt2 inhibitor |
ES11791943.1T ES2683123T3 (en) | 2010-06-12 | 2011-06-10 | Crystal form of the benzylbenzene SGLT2 inhibitor |
CN201180028665.8A CN102933592B (en) | 2010-06-12 | 2011-06-10 | The crystalline form of ditane SGLT2 inhibitor |
CA2800379A CA2800379C (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene sglt2 inhibitor |
EP11791943.1A EP2580225B1 (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene sglt2 inhibitor |
DK11791943.1T DK2580225T3 (en) | 2010-06-12 | 2011-06-10 | CRYSTALLIC FORM OF BENZYLBENZEN-SGLT2 INHIBITORS |
MX2012014423A MX342665B (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene sglt2 inhibitor. |
RU2013101580/04A RU2569491C2 (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzyl-benzene sglt inhibitor |
MA35549A MA34371B1 (en) | 2010-06-12 | 2011-06-10 | CRYSTALLINE FORM OF SGL T2 INHIBITOR OF BENZYL-BENZENE TYPE |
RS20181044A RS57653B1 (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene sglt2 inhibitor |
BR112012031616A BR112012031616A2 (en) | 2010-06-12 | 2011-06-10 | crystalline form of benzylbenzene inhibitor sglt2 |
AU2011264220A AU2011264220B2 (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene SGLT2 inhibitor |
SI201131551T SI2580225T1 (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene sglt2 inhibitor |
KR1020137000844A KR101831675B1 (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene sglt2 inhibitor |
LTEP11791943.1T LT2580225T (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene sglt2 inhibitor |
NZ605570A NZ605570A (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene sglt2 inhibitor |
SG2012089710A SG186206A1 (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene sglt2 inhibitor |
UAA201300352A UA108887C2 (en) | 2010-06-12 | 2011-10-06 | CRYSTAL FORM OF BENZYL-BENZOLE INHIBITOR SGLT2 |
IL223205A IL223205B (en) | 2010-06-12 | 2012-11-22 | Crystalline form of benzylbenzene sglt2 inhibitor |
ZA2013/00004A ZA201300004B (en) | 2010-06-12 | 2013-01-02 | Cyrstalline form of benzylbenzene sglt2 inhibitor |
CY181100972T CY1120690T1 (en) | 2010-06-12 | 2018-09-20 | CRYSTAL FORM OF BENZYLOVENZOLE SUBSTANCE OF SGLT2 |
HRP20181695TT HRP20181695T1 (en) | 2010-06-12 | 2018-10-17 | Crystalline form of benzylbenzene sglt2 inhibitor |
Applications Claiming Priority (2)
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 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2011153953A1 true WO2011153953A1 (en) | 2011-12-15 |
Family
ID=45097470
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/CN2010/073865 WO2011153712A1 (en) | 2010-06-12 | 2010-06-12 | Crystalline form of benzylbenzene sglt2 inhibitor |
PCT/CN2011/075554 WO2011153953A1 (en) | 2010-06-12 | 2011-06-10 | Crystalline form of benzylbenzene sglt2 inhibitor |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/CN2010/073865 WO2011153712A1 (en) | 2010-06-12 | 2010-06-12 | Crystalline form of benzylbenzene sglt2 inhibitor |
Country Status (31)
Country | Link |
---|---|
US (4) | US8987323B2 (en) |
EP (1) | EP2580225B1 (en) |
JP (1) | JP5842191B2 (en) |
KR (1) | KR101831675B1 (en) |
CN (1) | CN102933592B (en) |
AR (1) | AR121997A2 (en) |
AU (1) | AU2011264220B2 (en) |
BR (1) | BR112012031616A2 (en) |
CA (1) | CA2800379C (en) |
CO (1) | CO6640246A2 (en) |
CY (1) | CY1120690T1 (en) |
DK (1) | DK2580225T3 (en) |
ES (1) | ES2683123T3 (en) |
HR (1) | HRP20181695T1 (en) |
HU (1) | HUE040355T2 (en) |
IL (1) | IL223205B (en) |
LT (1) | LT2580225T (en) |
MA (1) | MA34371B1 (en) |
MX (1) | MX342665B (en) |
MY (1) | MY184925A (en) |
NZ (1) | NZ605570A (en) |
PL (1) | PL2580225T3 (en) |
PT (1) | PT2580225T (en) |
RS (1) | RS57653B1 (en) |
RU (1) | RU2569491C2 (en) |
SG (1) | SG186206A1 (en) |
SI (1) | SI2580225T1 (en) |
TW (1) | TWI589295B (en) |
UA (1) | UA108887C2 (en) |
WO (2) | WO2011153712A1 (en) |
ZA (1) | ZA201300004B (en) |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2015522644A (en) * | 2012-07-26 | 2015-08-06 | 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Boehringer Ingelheim Vetmedica GmbH | Crystalline complex of 1-cyano-2- (4-cyclopropyl-benzyl) -4- (β-D-glucopyranose-1-yl) -benzene, process for its preparation and its use for preparing drugs |
WO2019209998A1 (en) * | 2018-04-25 | 2019-10-31 | Theracos Sub, Llc | Methods of treating hypertension |
WO2021165177A1 (en) | 2020-02-17 | 2021-08-26 | Boehringer Ingelheim Vetmedica Gmbh | Use of sglt-2 inhibitors for the prevention and/or treatment of cardiac diseases in felines |
WO2022076328A1 (en) | 2020-10-05 | 2022-04-14 | Theracos Sub, Llc | Pharmaceutical formulations |
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NZ604897A (en) * | 2008-08-22 | 2014-03-28 | Theracos Sub Llc | Processes for the preparation of sglt2 inhibitors |
WO2011153712A1 (en) | 2010-06-12 | 2011-12-15 | Theracos, Inc. | Crystalline form of benzylbenzene sglt2 inhibitor |
EP4245765A3 (en) | 2013-04-04 | 2024-03-20 | Boehringer Ingelheim Vetmedica GmbH | Treatment of metabolic disorders in equine animals |
WO2015051484A1 (en) | 2013-10-12 | 2015-04-16 | Theracos, Inc. | Preparation of hydroxy-benzylbenzene derivatives |
CN105828815B (en) | 2013-12-17 | 2020-03-27 | 勃林格殷格翰动物保健有限公司 | Treatment of metabolic disorders in felines |
PL3485890T3 (en) | 2014-01-23 | 2023-08-28 | Boehringer Ingelheim Vetmedica Gmbh | Sglt2 inhibitors for treatment of metabolic disorders in canine animals |
JP6115684B2 (en) * | 2014-03-27 | 2017-04-19 | 三菱電機株式会社 | Semiconductor device and method for manufacturing semiconductor device |
DK3125882T3 (en) | 2014-04-01 | 2020-06-29 | Boehringer Ingelheim Vetmedica Gmbh | TREATMENT OF METABOLIC DISORDERS IN ANIMAL ANIMALS |
EP3197429A1 (en) * | 2014-09-25 | 2017-08-02 | Boehringer Ingelheim Vetmedica GmbH | Combination treatment of sglt2 inhibitors and dopamine agonists for preventing metabolic disorders in equine animals |
US10220017B2 (en) | 2015-08-27 | 2019-03-05 | Boehringer Ingelheim Vetmedica Gmbh | Liquid pharmaceutical compositions comprising SGLT-2 inhibitors |
CN108239055B (en) * | 2016-12-23 | 2023-07-18 | 杭州领业医药科技有限公司 | THR 1442L-aspartic acid eutectic crystal, preparation method and pharmaceutical composition thereof |
US11031285B2 (en) | 2017-10-06 | 2021-06-08 | Invensas Bonding Technologies, Inc. | Diffusion barrier collar for interconnects |
GB202213849D0 (en) * | 2022-09-22 | 2022-11-09 | Macfarlan Smith Ltd | Crystalline forms of bexagliflozin, processes for the preparation and use thereof |
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