AR073155A1 - Formas de ester metilico de cddo, composiciones farmaceuticas y metodo de preparacion de las mismas - Google Patents
Formas de ester metilico de cddo, composiciones farmaceuticas y metodo de preparacion de las mismasInfo
- Publication number
- AR073155A1 AR073155A1 ARP080103557A ARP080103557A AR073155A1 AR 073155 A1 AR073155 A1 AR 073155A1 AR P080103557 A ARP080103557 A AR P080103557A AR P080103557 A ARP080103557 A AR P080103557A AR 073155 A1 AR073155 A1 AR 073155A1
- Authority
- AR
- Argentina
- Prior art keywords
- methyl ester
- solid
- cddo methyl
- cddo
- vitreous
- Prior art date
Links
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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
- C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Steroid Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Glass Compositions (AREA)
Abstract
Un compuesto triterpenoide, 2-ciano-3,2-dioxoleana-1,9(11)-dien-28-oato de metilo (éster metílico de CDDO), tiene una forma solida vítrea no cristalina y una forma cristalina no hidratada que se puede preparar, por ejemplo, a partir de una solucion metanolica saturada. La forma vítrea despliega una mejorada biodisponibilidad respecto de la forma cristalina no hidratada. Cada forma del éster metílico de CDDO es un candidato superior para usar, típicamente en forma de dosis solida, para el tratamiento de una variedad de estados patologicos, en general asociados con inflamacion. Reivindicacion 1: Una forma solida vítrea de éster metílico de CDDO, caracterizada porque tiene un patron de difraccion de rayos X de polvo con un pico de halo a aproximadamente 13,5 s 2theta, tal como se muestra en la Figura 2C y a Tg. Reivindicacion 2: Una forma de solvato de dimetanol de éster metílico de CDDO, caracterizada porque tiene un patron de difraccion de rayos X de polvo con picos característicos tal como se muestra en la Tabla 18 y un patron de DSC tal como se muestra en la Figura 24. Reivindicacion 3: Una composicion farmacéutica en forma de dosificacion solida, caracterizada porque comprende (i) una cantidad terapéuticamente efectiva de la forma solida vítrea del éster metílico de CDDO de acuerdo con la reivindicacion 1 con (ii) un portador comestible. Reivindicacion 4: Un método para la produccion de la forma solida vítrea de éster metílico de CDDO de acuerdo con la reivindicacion 1, caracterizado porque comprende (a) preparar una forma de solvato de dimetanol de éster metílico de CDDO, que tiene un patron de difraccion de rayos X de polvo con picos característicos tal como se muestra en la Tabla 18 y un patron de DSC tal como se muestra en la Figura 24, y (b) secar la forma de solvato de dimetanol para obtener dicha forma solida vítrea. Reivindicacion 5: La forma solida vítrea de éster metílico de CDDO de acuerdo con la reivindicacion 1, caracterizada porque tiene un espectro de PDF con los picos característicos de la Figura 28 de aproximadamente 5 L a aproximadamente 20 L. Reivindicacion 9: La forma solida vítrea de éster metílico de CDDO de acuerdo con la reivindicacion 1, caracterizada porque tiene un valor de Tg en el rango de aproximadamente 120° C a aproximadamente 135s C. Reivindicacion 10: La forma solida vítrea de éster metílico de CDDO de acuerdo con la reivindicacion 1, caracterizada porque tiene un valor de Tg en el rango de aproximadamente 125s C a aproximadamente 130s C. Reivindicacion 11: Una composicion farmacéutica, caracterizada porque comprende (i) una cantidad terapéuticamente efectiva de éster metílico de CDDO y (ii) un excipiente que es un formador de cristales, de manera tal que dicha composicion tenga una Tg.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US95593907P | 2007-08-15 | 2007-08-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR073155A1 true AR073155A1 (es) | 2010-10-20 |
Family
ID=40351005
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080103557A AR073155A1 (es) | 2007-08-15 | 2008-08-14 | Formas de ester metilico de cddo, composiciones farmaceuticas y metodo de preparacion de las mismas |
| ARP200100825A AR119704A2 (es) | 2007-08-15 | 2020-03-25 | Forma sólida vítrea de éster metílico de cddo, método para obtenerla, y composiciones farmacéuticas relacionadas |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP200100825A AR119704A2 (es) | 2007-08-15 | 2020-03-25 | Forma sólida vítrea de éster metílico de cddo, método para obtenerla, y composiciones farmacéuticas relacionadas |
Country Status (29)
| Country | Link |
|---|---|
| US (3) | US8088824B2 (es) |
| EP (2) | EP2187741B1 (es) |
| JP (4) | JP5005812B2 (es) |
| KR (2) | KR101544766B1 (es) |
| CN (2) | CN103254267B (es) |
| AR (2) | AR073155A1 (es) |
| AT (1) | ATE549035T1 (es) |
| AU (1) | AU2008287388B2 (es) |
| BR (1) | BRPI0815540A8 (es) |
| CA (2) | CA2696330C (es) |
| CL (1) | CL2008002417A1 (es) |
| CY (2) | CY1112864T1 (es) |
| DK (2) | DK2450057T3 (es) |
| EA (2) | EA023550B1 (es) |
| ES (2) | ES2382571T3 (es) |
| HK (1) | HK1143537A1 (es) |
| HR (2) | HRP20120350T1 (es) |
| HU (1) | HUE031866T2 (es) |
| IL (2) | IL203824A (es) |
| LT (1) | LT2450057T (es) |
| MX (1) | MX2010001628A (es) |
| NZ (1) | NZ583269A (es) |
| PL (2) | PL2187741T3 (es) |
| PT (2) | PT2450057T (es) |
| SG (2) | SG10201504650VA (es) |
| SI (2) | SI2187741T1 (es) |
| TW (2) | TWI419899B (es) |
| WO (1) | WO2009023232A1 (es) |
| ZA (1) | ZA201001066B (es) |
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|---|---|---|---|---|
| US6326507B1 (en) * | 1998-06-19 | 2001-12-04 | Trustees Of Dartmouth College | Therapeutic compounds and methods of use |
| US7435755B2 (en) | 2000-11-28 | 2008-10-14 | The Trustees Of Dartmouth College | CDDO-compounds and combination therapies thereof |
| EP1465615B1 (en) | 2002-01-15 | 2012-08-01 | Trustees of Dartmouth College | Tricyclic-bis-enone derivatives and methods of use thereof |
| US8921340B2 (en) | 2006-11-17 | 2014-12-30 | Trustees Of Dartmouth College | Methods for using synthetic triterpenoids in the treatment of bone or cartilage diseases or conditions |
| JP2010510243A (ja) | 2006-11-17 | 2010-04-02 | トラスティーズ オブ ダートマス カレッジ | 三環系−ビス−エノン（ｔｂｅ）の合成および生物学的活性 |
| WO2008064132A2 (en) | 2006-11-17 | 2008-05-29 | Trustees Of Dartmouth College | Synthetic triterpenoids and tricyclic-bis-enones for use in stimulating bone and cartilage growth |
| US8088824B2 (en) * | 2007-08-15 | 2012-01-03 | Reata Pharmaceuticals Inc. | Forms of CDDO methyl ester |
| RS58486B1 (sr) * | 2008-01-11 | 2019-04-30 | Reata Pharmaceuticals Inc | Sintetički triterpenoidi i metode njihove upotrebe u tretmanu bolesti |
| BRPI0911422B8 (pt) | 2008-04-18 | 2021-05-25 | Reata Pharmaceuticals Inc | compostos moduladores inflamatórios antioxidantes, composição farmacêutica e usos dos mesmos |
| PL2276493T3 (pl) * | 2008-04-18 | 2019-05-31 | Reata Pharmaceuticals Inc | Antyoksydacyjne modulatory stanu zapalnego: pochodne kwasu oleanolowego z amino- i innymi modyfikacjami przy C-17 |
| CN102066397B (zh) | 2008-04-18 | 2013-09-11 | 里亚塔医药公司 | 包含抗炎症药效团的化合物以及使用方法 |
| CN102164941B (zh) | 2008-04-18 | 2015-05-27 | 里亚塔医药公司 | 抗氧化剂炎症调节剂:具有饱和c环的齐墩果酸衍生物 |
| TW201004627A (en) | 2008-04-18 | 2010-02-01 | Reata Pharmaceuticals Inc | Antioxidant inflammation modulators: novel derivatives of oleanolic acid |
| AU2009274037B2 (en) | 2008-07-22 | 2015-07-09 | Trustees Of Dartmouth College | Monocyclic cyanoenones and methods of use thereof |
| KR101483203B1 (ko) * | 2009-02-13 | 2015-01-15 | 리아타 파마슈티컬즈, 아이엔씨. | 무정형 ｃｄｄｏ-ｍｅ를 포함하는, 지연 방출형 경구 투여 조성물 |
| US8759535B2 (en) | 2010-02-18 | 2014-06-24 | High Point Pharmaceuticals, Llc | Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof |
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| CN102875634B (zh) * | 2012-10-24 | 2014-08-20 | 苏州晶云药物科技有限公司 | 2-氰基-3,12-二氧代齐墩果-1,9(11)-二烯-28-酸甲酯的几种晶型 |
| EP2977381B1 (en) | 2013-03-19 | 2018-09-26 | Daiichi Sankyo Company, Limited | Terpenoid derivative |
| TW201936625A (zh) | 2013-04-24 | 2019-09-16 | 美商艾伯維有限公司 | 甲基巴多索龍之2,2-二氟丙醯胺衍生物、其多晶形及其使用方法 |
| SG10201906113RA (en) * | 2013-08-23 | 2019-08-27 | Reata Pharmaceuticals Inc | Methods of treating and preventing endothelial dysfunction using bardoxolone methyl or analogs thereof |
| WO2016033132A1 (en) | 2014-08-26 | 2016-03-03 | Trustees Of Dartmouth College | Pyridyl analogs of 1-(2-cyano-3,12-dioxooleana-1,9(11)dien-28-oyl) imidazole |
| US10189791B2 (en) | 2014-08-26 | 2019-01-29 | Trustees Of Dartmouth College | Pyridyl analogs of 1-(2-cyano-3,12-dioxooleana-1,9(11)dien-28-oyl) imidazole |
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| US11591302B2 (en) | 2014-12-19 | 2023-02-28 | Geistlich Pharm A Ag | Processes for preparing oxathiazin-like compounds |
| HRP20220313T1 (hr) | 2014-12-19 | 2022-05-13 | Geistlich Pharma Ag | Procesi za pripremu spojeva sličnih oksatiazinu |
| JP6748652B2 (ja) | 2015-02-12 | 2020-09-02 | リアタ ファーマシューティカルズ インコーポレイテッド | 抗酸化性炎症調節剤としてのイミダゾリル三環式エノン |
| PL3317281T3 (pl) * | 2015-07-02 | 2020-11-02 | Acerta Pharma B.V. | Postacie stałe i formulacje (s)-4-(8-amino-3-(1-(but-2-ynoilo)pirolidyn-2-ylo)imidazo[1,5-a]-pirazyn-1-ylo)-n-(pirydyn-2-ylo)benzamidu |
| EA201890767A1 (ru) | 2015-09-23 | 2019-09-30 | Рита Фармасьютикалз, Инк. | C4-модифицированные производные олеаноловой кислоты для ингибирования il-17 и других применений |
| US10953020B2 (en) | 2016-11-08 | 2021-03-23 | Reata Pharmaceuticals, Inc. | Methods of treating Alport syndrome using bardoxolone methyl or analogs thereof |
| TWI831738B (zh) | 2016-12-16 | 2024-02-11 | 美商瑞塔醫藥有限責任公司 | 用於抑制ＲＯＲγ及其他用途的嘧啶三環烯酮衍生物 |
| WO2019014412A1 (en) | 2017-07-13 | 2019-01-17 | Pliva Hrvatska D.O.O. | NOVEL CRYSTALLINE POLYMORPHIC FORMS OF METHYL BARDOXOLONE |
| CN112654610A (zh) | 2018-06-15 | 2021-04-13 | 里亚塔医药公司 | 用于抑制IL-17和RORγ的吡唑和咪唑化合物 |
| TW202038918A (zh) | 2018-11-27 | 2020-11-01 | 日商協和麒麟股份有限公司 | 醫藥組合物 |
| US20230255982A1 (en) | 2020-05-09 | 2023-08-17 | Reata Pharmaceuticals Holdings, LLC | Methods of treating covid-19 using bardoxolone methyl or analogs thereof |
| EP4259155A1 (en) | 2020-12-11 | 2023-10-18 | Reata Pharmaceuticals Holdings, LLC | Synthetic triterpenoids for use in therapy |
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2008
- 2008-08-13 US US12/191,176 patent/US8088824B2/en active Active
- 2008-08-14 AU AU2008287388A patent/AU2008287388B2/en active Active
- 2008-08-14 BR BRPI0815540A patent/BRPI0815540A8/pt not_active Application Discontinuation
- 2008-08-14 HU HUE12153605A patent/HUE031866T2/en unknown
- 2008-08-14 AR ARP080103557A patent/AR073155A1/es unknown
- 2008-08-14 PL PL08795303T patent/PL2187741T3/pl unknown
- 2008-08-14 CA CA2696330A patent/CA2696330C/en active Active
- 2008-08-14 SI SI200830650T patent/SI2187741T1/sl unknown
- 2008-08-14 PT PT121536056T patent/PT2450057T/pt unknown
- 2008-08-14 CL CL2008002417A patent/CL2008002417A1/es unknown
- 2008-08-14 MX MX2010001628A patent/MX2010001628A/es active IP Right Grant
- 2008-08-14 SI SI200831728A patent/SI2450057T1/sl unknown
- 2008-08-14 DK DK12153605.6T patent/DK2450057T3/en active
- 2008-08-14 SG SG10201504650VA patent/SG10201504650VA/en unknown
- 2008-08-14 TW TW097130947A patent/TWI419899B/zh active
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