ES2523873T3 - Administración de un inhibidor parcial de la oxidación de ácidos grasos, tal como ranolazina, para el tratamiento de la diabetes - Google Patents
Administración de un inhibidor parcial de la oxidación de ácidos grasos, tal como ranolazina, para el tratamiento de la diabetes Download PDFInfo
- Publication number
- ES2523873T3 ES2523873T3 ES03755446.6T ES03755446T ES2523873T3 ES 2523873 T3 ES2523873 T3 ES 2523873T3 ES 03755446 T ES03755446 T ES 03755446T ES 2523873 T3 ES2523873 T3 ES 2523873T3
- Authority
- ES
- Spain
- Prior art keywords
- diabetic
- mammal
- prediabetic
- alkyl
- level
- 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.)
- Expired - Lifetime
Links
- 206010012601 diabetes mellitus Diseases 0.000 title abstract 12
- XKLMZUWKNUAPSZ-UHFFFAOYSA-N N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide Chemical compound COC1=CC=CC=C1OCC(O)CN1CCN(CC(=O)NC=2C(=CC=CC=2C)C)CC1 XKLMZUWKNUAPSZ-UHFFFAOYSA-N 0.000 title 1
- 229940081730 Partial fatty acid oxidation inhibitor Drugs 0.000 title 1
- 229960000213 ranolazine Drugs 0.000 title 1
- 241000124008 Mammalia Species 0.000 abstract 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 5
- 206010018429 Glucose tolerance impaired Diseases 0.000 abstract 5
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 abstract 1
- 206010012689 Diabetic retinopathy Diseases 0.000 abstract 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- -1 aminocarbonylmethyl Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 235000012000 cholesterol Nutrition 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 239000008103 glucose Substances 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000036470 plasma concentration Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Chemical group 0.000 abstract 1
- 239000011593 sulfur Chemical group 0.000 abstract 1
Classifications
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Pulmonology (AREA)
- Otolaryngology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Uso de un compuesto de Fórmula I:**Fórmula** en la que: R1, R2, R3, R4 y R5 son cada uno independientemente hidrógeno, alquilo C1-4, alcoxi C1-4, ciano, trifluorometilo, halo, alquiltio C1-4, alquilsulfinilo C1-4, alquilsulfonilo C1-4 o N-alquilamido opcionalmente sustituido, siempre que cuando R1 sea metilo, R4 no sea metilo; o R2 y R3 formen juntos -OCH2O-; R6, R7, R8, R9 y R10 son cada uno independientemente hidrógeno, acilo que tiene un grupo alquilo C1-4, aminocarbonilmetilo, ciano, alquilo C1-4, alcoxi C1-4, trifluorometilo, halo, C1-4 alquitio, alquilsulfinilo C1-4, 15 alquilsulfonilo C1-4 o dialquilamino C1-4; o R6 y R7 forman juntos -CH>=CH-CH>=CH-; o R7 y R8 forman juntos -OCH2O-; R11 y R12 son cada uno independientemente hidrógeno o alquilo C1-4; y W es oxígeno o azufre; o una sal farmacéuticamente aceptable o éster del mismo, o un isómero del mismo para la preparación de una composición farmacéutica para (i) tratar la diabetes en un mamífero, (ii) reducir el nivel de HbA1c en plasma en un mamífero diabético, no diabético o prediabético, (iii) reducir el nivel de glucosa en plasma en un mamífero diabético, no diabético o prediabético, (iv) reducir el nivel total de colesterol en plasma en un mamífero diabético, no diabético o prediabético, (v) retrasar la aparición de retinopatía diabética en un mamífero diabético, no diabético o prediabético, o (vi) aumentar el nivel en plasma de colesterol de HDL en un mamífero diabético, no diabético o prediabético.
Description
Claims (1)
-
imagen1 imagen2
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38278102P | 2002-05-21 | 2002-05-21 | |
| US382781P | 2002-05-21 | ||
| US45933203P | 2003-03-31 | 2003-03-31 | |
| US459332P | 2003-03-31 | ||
| PCT/US2003/016277 WO2003099281A2 (en) | 2002-05-21 | 2003-05-21 | Administration of a partial fatty acid inhibitor such as ranolazine for the treatment of diabetes |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2523873T3 true ES2523873T3 (es) | 2014-12-02 |
Family
ID=29586970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES03755446.6T Expired - Lifetime ES2523873T3 (es) | 2002-05-21 | 2003-05-21 | Administración de un inhibidor parcial de la oxidación de ácidos grasos, tal como ranolazina, para el tratamiento de la diabetes |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US20040063717A1 (es) |
| EP (2) | EP1505977B1 (es) |
| JP (1) | JP4546824B2 (es) |
| KR (1) | KR101030943B1 (es) |
| CN (1) | CN100551370C (es) |
| AU (1) | AU2003248558B8 (es) |
| BR (1) | BR0311161A (es) |
| CA (1) | CA2486712C (es) |
| ES (1) | ES2523873T3 (es) |
| HK (1) | HK1073441A1 (es) |
| IL (4) | IL165304A0 (es) |
| MX (1) | MXPA04011530A (es) |
| NO (1) | NO330336B1 (es) |
| NZ (1) | NZ536678A (es) |
| RU (1) | RU2320343C2 (es) |
| WO (1) | WO2003099281A2 (es) |
| ZA (1) | ZA200409331B (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8822473B2 (en) | 2002-05-21 | 2014-09-02 | Gilead Sciences, Inc. | Method of treating diabetes |
| CA2486712C (en) | 2002-05-21 | 2012-01-03 | Cv Therapeutics, Inc. | Method of treating diabetes |
| AU2006203890A1 (en) * | 2005-01-06 | 2006-07-13 | Gilead Sciences, Inc. | Sustained release pharmaceutical formulations comprising ranolazine |
| JP2010518170A (ja) * | 2007-02-13 | 2010-05-27 | ギリアード・パロ・アルト・インコーポレイテッド | 冠微小血管疾患の処置のためのラノラジンの使用 |
| EP2136780A1 (en) * | 2007-02-13 | 2009-12-30 | CV Therapeutics Inc. | Use of ranolazine for the treatment of cardiovascular diseases |
| US20080193530A1 (en) * | 2007-02-13 | 2008-08-14 | Brent Blackburn | Use of ranolazine for the treatment of non-coronary microvascular diseases |
| US20090111826A1 (en) * | 2007-02-13 | 2009-04-30 | Louis Lange | Use of ranolazine for the treatment of cardiovascular diseases |
| WO2008116083A1 (en) * | 2007-03-22 | 2008-09-25 | Cv Therapeutics, Inc. | Use of ranolazine for elevated brain-type natriuretic peptide |
| JP2010523713A (ja) * | 2007-04-12 | 2010-07-15 | ギリアード・パロ・アルト・インコーポレイテッド | インスリン分泌を増強するためのラノラジン |
| CA2687381A1 (en) * | 2007-05-31 | 2008-12-04 | Cv Therapeutics, Inc. | Method of treating diabetes |
| KR20100033490A (ko) * | 2007-05-31 | 2010-03-30 | 질레드 팔로 알토 인코포레이티드 | 상승된 뇌-형 나트륨이뇨 펩티드에 대한 라놀라진 |
| US20090012103A1 (en) * | 2007-07-05 | 2009-01-08 | Matthew Abelman | Substituted heterocyclic compounds |
| WO2009100380A1 (en) * | 2008-02-06 | 2009-08-13 | Cv Therapeutics, Inc. | Use of ranolazine for treating pain |
| US20110250273A1 (en) * | 2008-12-11 | 2011-10-13 | Melford Scientific, LLC | Compositions of proton pump inhibitors, kits and methods of their use to treat diabetes |
| US20100292217A1 (en) * | 2009-05-14 | 2010-11-18 | Gilead Palo Alto, Inc. | Ranolazine for the treatment of cns disorders |
| JO3183B1 (ar) * | 2010-01-29 | 2018-03-08 | Regeneron Pharma | طرق لمعالجة أمراض المناعة الذاتية مضادات dll4 |
| TW201717919A (zh) | 2015-07-02 | 2017-06-01 | 國際藥品股份公司 | 雷諾多重壓縮錠劑 |
| WO2018001582A1 (en) | 2016-06-30 | 2018-01-04 | Interquim, S.A. | Ranolazine multiple compressed tablets |
| CN110812344A (zh) * | 2019-12-17 | 2020-02-21 | 卓和药业集团有限公司 | 一种治疗糖尿病合并心绞痛的药物组合物及制备方法 |
| GR1010510B (el) * | 2022-06-07 | 2023-07-20 | Ελπεν Α.Ε. Φαρμακευτικη Βιομηχανια, | Στερεες φαρμακοτεχνικες μορφες παρατεταμενης αποδεσμευσης ρανολαζινης |
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-
2003
- 2003-05-21 CA CA2486712A patent/CA2486712C/en not_active Expired - Fee Related
- 2003-05-21 WO PCT/US2003/016277 patent/WO2003099281A2/en active Application Filing
- 2003-05-21 CN CNB038113236A patent/CN100551370C/zh not_active Expired - Fee Related
- 2003-05-21 JP JP2004506805A patent/JP4546824B2/ja not_active Expired - Fee Related
- 2003-05-21 MX MXPA04011530A patent/MXPA04011530A/es active IP Right Grant
- 2003-05-21 AU AU2003248558A patent/AU2003248558B8/en not_active Ceased
- 2003-05-21 EP EP03755446.6A patent/EP1505977B1/en not_active Expired - Lifetime
- 2003-05-21 ES ES03755446.6T patent/ES2523873T3/es not_active Expired - Lifetime
- 2003-05-21 EP EP10011229A patent/EP2332540A1/en not_active Withdrawn
- 2003-05-21 KR KR1020047018803A patent/KR101030943B1/ko active IP Right Grant
- 2003-05-21 NZ NZ536678A patent/NZ536678A/en not_active IP Right Cessation
- 2003-05-21 RU RU2004133670/14A patent/RU2320343C2/ru not_active IP Right Cessation
- 2003-05-21 US US10/443,314 patent/US20040063717A1/en not_active Abandoned
- 2003-05-21 BR BR0311161-0A patent/BR0311161A/pt not_active Application Discontinuation
- 2003-05-21 IL IL16530403A patent/IL165304A0/xx unknown
-
2004
- 2004-11-18 IL IL165304A patent/IL165304A/en active IP Right Grant
- 2004-11-19 ZA ZA2004/09331A patent/ZA200409331B/en unknown
- 2004-12-20 NO NO20045554A patent/NO330336B1/no not_active IP Right Cessation
-
2005
- 2005-08-16 HK HK05107050.7A patent/HK1073441A1/xx not_active IP Right Cessation
-
2010
- 2010-04-07 US US12/755,931 patent/US8314104B2/en not_active Expired - Fee Related
-
2011
- 2011-06-28 IL IL213809A patent/IL213809A0/en unknown
- 2011-06-28 IL IL213806A patent/IL213806A0/en unknown
-
2012
- 2012-10-18 US US13/655,252 patent/US8883750B2/en not_active Expired - Fee Related
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2014
- 2014-09-03 US US14/476,650 patent/US20140378465A1/en not_active Abandoned
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