CO6210719A2 - Forma criatalina del hemihidrato de 1-(beta-dglucopiranosil )-4-metil-3-[5-(4-fluorofenil)-2-tienilmetil]benceno - Google Patents
Forma criatalina del hemihidrato de 1-(beta-dglucopiranosil )-4-metil-3-[5-(4-fluorofenil)-2-tienilmetil]bencenoInfo
- Publication number
- CO6210719A2 CO6210719A2 CO09068422A CO09068422A CO6210719A2 CO 6210719 A2 CO6210719 A2 CO 6210719A2 CO 09068422 A CO09068422 A CO 09068422A CO 09068422 A CO09068422 A CO 09068422A CO 6210719 A2 CO6210719 A2 CO 6210719A2
- Authority
- CO
- Colombia
- Prior art keywords
- hemihydrate
- crystalline form
- benzene
- methyl
- further characterized
- Prior art date
Links
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
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- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
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- 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
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
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- 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
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- 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
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- 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
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
-
- 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
-
- 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
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
1.- Una forma cristalina del hemihidrato de 1-(ß-D-glucopiranosil)-4-metil-3-[5-(4-fluorofenil)-2-tienilmetil] benceno. 2.- La forma cristalina del hemihidrato de conformidad con la reivindicación 1, caracterizada además porque tiene un patrón de difracción de rayos X de polvo que comprende los siguientes valores 2? medidos utilizando radiación CuKa: 4.36 ± 0.2, 13.54 ± 0.2, 16,00 ± 0.2, 19.32 ± 0.2. y 20.80 ± 0.2. 3.- La forma cristalina del hemihidrato de conformidad con la reivindicación 1, caracterizada además porque tiene sustancialmente el mismo patrón de difracción de rayos X expuesto en la FIG. 1. 4.- La forma cristalina del hemihidrato de conformidad con la reivindicación 1, caracterizada además porque tiene sustancialmente el mismo espectro IR, expuesto en la FIG. 2. 5.- Un proceso para la preparación de una forma cristalina del hemihidrato de la reivindicación 1, que comprende preparar una solución de 1-(ß-D-glucopiranosil)-4-metil-3-[5-(4-fluorofenil)-2-tienilmetil] benceno y cristalizar dicho hemihidrato a partir de la solución mediante precipitación o recristalización. 6.- Una composición farmacéutica que comprende una cantidad efectiva de una forma cristalina del hemihidrato de la reivindicación 1 y un vehículo aceptable para uso farmacéutico. 7.- Un método para el tratamiento o retardo de la progresión o comienzo de la diabetes mellitus, retinopatía diabética, neuropatía diabética, nefropatía diabética, retraso en la curación de heridas, resistencia a la insulina, hiperglucemia, hiperinsulinemia, niveles sanguíneos elevados de ácidos grasos, niveles sanguíneos elevados de glicerol, hiperlipidemia, obesidad, hipertrigliceridernia, Síndrome X, complicaciones diabéticas, aterosclerosis o hipertensión, que comprende administrar una cantidad efectiva para uso terapéutico de una forma cristalina del hemihidrato de la reivindicación 1.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US86842606P | 2006-12-04 | 2006-12-04 | |
JP2006327019 | 2006-12-04 |
Publications (1)
Publication Number | Publication Date |
---|---|
CO6210719A2 true CO6210719A2 (es) | 2010-10-20 |
Family
ID=38973167
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CO09068422A CO6210719A2 (es) | 2006-12-04 | 2009-07-02 | Forma criatalina del hemihidrato de 1-(beta-dglucopiranosil )-4-metil-3-[5-(4-fluorofenil)-2-tienilmetil]benceno |
Country Status (34)
Country | Link |
---|---|
US (2) | US7943582B2 (es) |
EP (1) | EP2102224B2 (es) |
JP (1) | JP5159788B2 (es) |
KR (1) | KR101146095B1 (es) |
CN (3) | CN101573368B (es) |
AR (3) | AR064099A1 (es) |
AU (1) | AU2007329895C1 (es) |
BR (1) | BRPI0718882B8 (es) |
CA (1) | CA2671357C (es) |
CL (1) | CL2007003487A1 (es) |
CO (1) | CO6210719A2 (es) |
CR (1) | CR10861A (es) |
DK (1) | DK2102224T4 (es) |
EA (1) | EA017103B1 (es) |
EC (1) | ECSP099489A (es) |
ES (1) | ES2456640T5 (es) |
GT (1) | GT200900151A (es) |
IL (1) | IL199032A (es) |
ME (1) | ME01829B (es) |
MX (1) | MX2009005857A (es) |
MY (1) | MY153702A (es) |
NO (1) | NO344354B1 (es) |
NZ (1) | NZ577545A (es) |
PA (1) | PA8759401A1 (es) |
PE (3) | PE20081201A1 (es) |
PL (1) | PL2102224T5 (es) |
PT (1) | PT2102224E (es) |
RS (1) | RS53274B2 (es) |
SI (1) | SI2102224T2 (es) |
SV (1) | SV2009003285A (es) |
TW (1) | TWI403325B (es) |
UY (1) | UY30730A1 (es) |
WO (1) | WO2008069327A1 (es) |
ZA (1) | ZA200903941B (es) |
Families Citing this family (102)
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PT2200606T (pt) | 2007-09-10 | 2017-12-13 | Janssen Pharmaceutica Nv | Processo para a preparação de compostos úteis como inibidores de sglt |
HUE029970T2 (en) | 2008-08-22 | 2017-04-28 | Theracos Sub Llc | Method for producing SGLT2 inhibitors |
US9056850B2 (en) * | 2008-10-17 | 2015-06-16 | Janssen Pharmaceutica N.V. | Process for the preparation of compounds useful as inhibitors of SGLT |
SG173619A1 (en) | 2009-02-13 | 2011-09-29 | Boehringer Ingelheim Int | Pharmaceutical composition comprising a sglt2 inhibitor, a dpp-iv inhibitor and optionally a further antidiabetic agent and uses thereof |
US20110009347A1 (en) * | 2009-07-08 | 2011-01-13 | Yin Liang | Combination therapy for the treatment of diabetes |
WO2011003976A1 (en) * | 2009-07-10 | 2011-01-13 | Janssen Pharmaceutica Nv | CRYSTALLISATION PROCESS FOR 1-(ß-D-GLUCOPYRANOSYL)-4-METHYL-3-[5-(4-FLUOROPHENYL)-2-THIENYLMETHYL] BENZENE |
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CA2777528C (en) * | 2009-10-14 | 2018-09-18 | Janssen Pharmaceutica Nv | Process for the preparation of compounds useful as inhibitors of sglt2 |
WO2011070592A2 (en) | 2009-12-09 | 2011-06-16 | Panacea Biotec Ltd. | Novel sugar derivatives |
CN102115468B (zh) * | 2009-12-31 | 2014-06-11 | 上海特化医药科技有限公司 | 一种2,5-二取代噻吩化合物的合成方法 |
WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
JP2013523681A (ja) | 2010-03-30 | 2013-06-17 | 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 | Sglt2インヒビター及びppar−ガンマアゴニストを含む医薬組成物並びにその使用 |
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