HRP20120350T1 - Novi oblici cddo metilnog estera - Google Patents
Novi oblici cddo metilnog estera Download PDFInfo
- Publication number
- HRP20120350T1 HRP20120350T1 HRP20120350AT HRP20120350T HRP20120350T1 HR P20120350 T1 HRP20120350 T1 HR P20120350T1 HR P20120350A T HRP20120350A T HR P20120350AT HR P20120350 T HRP20120350 T HR P20120350T HR P20120350 T1 HRP20120350 T1 HR P20120350T1
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- Croatia
- Prior art keywords
- pharmaceutical preparation
- methyl ester
- cddo
- excipient
- glassy
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- WPTTVJLTNAWYAO-KPOXMGGZSA-N Bardoxolone methyl Chemical compound C([C@@]12C)=C(C#N)C(=O)C(C)(C)[C@@H]1CC[C@]1(C)C2=CC(=O)[C@@H]2[C@@H]3CC(C)(C)CC[C@]3(C(=O)OC)CC[C@]21C WPTTVJLTNAWYAO-KPOXMGGZSA-N 0.000 title claims abstract 11
- 239000007787 solid Substances 0.000 claims abstract 8
- 239000000843 powder Substances 0.000 claims abstract 3
- 125000001475 halogen functional group Chemical group 0.000 claims abstract 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 11
- 239000000546 pharmaceutical excipient Substances 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 3
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 229940041181 antineoplastic drug Drugs 0.000 claims 2
- 229920001577 copolymer Polymers 0.000 claims 2
- 230000009477 glass transition Effects 0.000 claims 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 2
- -1 organic acid salt Chemical class 0.000 claims 2
- 229920001282 polysaccharide Polymers 0.000 claims 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 2
- 102000004196 processed proteins & peptides Human genes 0.000 claims 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims 2
- 229920005613 synthetic organic polymer Polymers 0.000 claims 2
- BXGYYDRIMBPOMN-UHFFFAOYSA-N 2-(hydroxymethoxy)ethoxymethanol Chemical compound OCOCCOCO BXGYYDRIMBPOMN-UHFFFAOYSA-N 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 150000001719 carbohydrate derivatives Chemical class 0.000 claims 1
- 150000001720 carbohydrates Chemical class 0.000 claims 1
- 235000014633 carbohydrates Nutrition 0.000 claims 1
- 229920001531 copovidone Polymers 0.000 claims 1
- 238000001035 drying Methods 0.000 claims 1
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical group O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 1
- 229960005277 gemcitabine Drugs 0.000 claims 1
- 150000004676 glycans Chemical class 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229920003145 methacrylic acid copolymer Polymers 0.000 claims 1
- 229940117841 methacrylic acid copolymer Drugs 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229920001184 polypeptide Polymers 0.000 claims 1
- 239000005017 polysaccharide Substances 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 239000007909 solid dosage form Substances 0.000 claims 1
- 238000001228 spectrum Methods 0.000 claims 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
- A61K31/70—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
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- 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
Staklasto-kruti oblik CDDO metilnog estera, naznačen time da čiji rendgenski difraktogram praha ima amorfni halo na približno 13,5 °2θ, kao što je prikazano na Slici 2C, i koji ima Tg.Patent sadrži još 17 patentnih zahtjeva.
Claims (18)
1. Staklasto-kruti oblik CDDO metilnog estera, naznačen time da čiji rendgenski difraktogram praha ima amorfni halo na približno 13,5 °2θ, kao što je prikazano na Slici 2C, i koji ima Tg.
2. Dimetanolni solvat CDDO-metilnog estera, naznačen time da čiji rendgenski difraktogram praha ima karakteristične maksimume kako je prikazano u Tablici 18 i DSC signal kako je prikazano u Slici 24.
3. Farmaceutski pripravak u krutom doznom obliku, naznačen time da sadrži (i) terapijski učinkovitu količinu staklasto-krutog CDDO metil-estera iz Zahtjeva 1 i (ii) jestivi nosač.
4. Metoda za proizvodnju staklasto-krutog oblika CDDO-metilnog estera iz zahtjeva 1, naznačena time da obuhvaća (a) pripremu dimetanolnog solvata CDDO- metilnog estera, čiji rendgenski difraktogram praha ima maksimume kako je prikazano u Tablici 18 i DSC signal kako je prikazano na Slici 24, te (b) sušenje dimetanolnog solvata radi dobivanja navedenog staklasto-krutog oblika.
5. Staklasto-kruti oblik CDDO-metilnog estera iz Zahtjeva 1, naznačen time da ima PDF spektar s karakterističnim maksimumima iz Slike 28 od približno 5 Å do približno 20 Å.
6. Farmaceutski pripravak sukladno Zahtjevu 3 naznačen time da je za primjenu u liječenju kanceroznih stanja.
7. Farmaceutski pripravak sukladno Zahtjevu 6, naznačen time da dodatno sadrži drugi lijek protiv raka.
8. Farmaceutski pripravak sukladno Zahtjevu 7, naznačen time da drugi lijek protiv raka pripada skupini gemcitabina, a kancerozno stanje je rak gušterače.
9. Staklasto-kruti oblik CDDO-metilnog estera iz zahtjeva 1, naznačen time da ima staklište (Tg) između 120°C i 135°C.
10. Staklasto-kruti oblik CDDO-metilnog estera iz zahtjeva 1, naznačen time da ima staklište (Tg) između 125°C i 135°C.
11. Farmaceutski pripravak naznačen time da sadrži (i) terapijski učinkovitu količinu CDDO-metilnog estera i (ii) ekscipijent koji pomaže stvoriti staklastu fazu, tako da navedeni pripravak ima Tg.
12. Farmaceutski pripravak iz zahtjeva 11, naznačen time da je ekscipijent odabran iz skupine koja se sastoji od (A) ugljikohidrata, derivata ugljikohidrata ili polimera ugljikohidrata, (B) sintetskog organskog polimera, (C) soli organske kiseline, (D) proteina, polipeptida ili peptida i (E) polisaharida visoke molekularne težine.
13. Farmaceutski pripravak iz zahtjeva 12, naznačen time da je ekscipijent sintetski organski polimer.
14. Farmaceutski pripravak iz zahtjeva 13, naznačen time da je ekscipijent odabran iz skupine koja se sastoji od hidroksipropil metil celuloze, poli[1-(2-okso-1-pirolidinil)etilena ili njegovog kopolimera, te kopolimera metakrilne kiseline.
15. Farmaceutski pripravak iz Zahtjeva 14, naznačen time da je ekscipijent ftalatni ester hidroksipropil metil celuloze.
16. Farmaceutski pripravak iz Zahtjeva 14, naznačen time da je ekscipijent PVP/VA.
17. Farmaceutski pripravak iz Zahtjeva 14, naznačen time da je ekscipijent metakrilna kiselina–etil akrilatni kopolimer (1:1).
18. Farmaceutski pripravak iz Zahtjeva 13, naznačen time da je ekscipijent kopovidon.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US95593907P | 2007-08-15 | 2007-08-15 | |
PCT/US2008/009703 WO2009023232A1 (en) | 2007-08-15 | 2008-08-14 | Novel forms of cddo methyl ester |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20120350T1 true HRP20120350T1 (hr) | 2012-05-31 |
Family
ID=40351005
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20120350AT HRP20120350T1 (hr) | 2007-08-15 | 2012-04-18 | Novi oblici cddo metilnog estera |
HRP20161503TT HRP20161503T1 (hr) | 2007-08-15 | 2016-11-15 | Novi oblici cddo metilnog estera |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20161503TT HRP20161503T1 (hr) | 2007-08-15 | 2016-11-15 | Novi oblici cddo metilnog estera |
Country Status (29)
Country | Link |
---|---|
US (3) | US8088824B2 (hr) |
EP (2) | EP2187741B1 (hr) |
JP (4) | JP5005812B2 (hr) |
KR (2) | KR101544766B1 (hr) |
CN (2) | CN103254267B (hr) |
AR (2) | AR073155A1 (hr) |
AT (1) | ATE549035T1 (hr) |
AU (1) | AU2008287388B2 (hr) |
BR (1) | BRPI0815540A8 (hr) |
CA (2) | CA2696330C (hr) |
CL (1) | CL2008002417A1 (hr) |
CY (2) | CY1112864T1 (hr) |
DK (2) | DK2450057T3 (hr) |
EA (2) | EA023550B1 (hr) |
ES (2) | ES2382571T3 (hr) |
HK (1) | HK1143537A1 (hr) |
HR (2) | HRP20120350T1 (hr) |
HU (1) | HUE031866T2 (hr) |
IL (2) | IL203824A (hr) |
LT (1) | LT2450057T (hr) |
MX (1) | MX2010001628A (hr) |
NZ (1) | NZ583269A (hr) |
PL (2) | PL2187741T3 (hr) |
PT (2) | PT2450057T (hr) |
SG (2) | SG10201504650VA (hr) |
SI (2) | SI2187741T1 (hr) |
TW (2) | TWI419899B (hr) |
WO (1) | WO2009023232A1 (hr) |
ZA (1) | ZA201001066B (hr) |
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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 |
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ME03713B (me) | 2010-04-12 | 2021-01-20 | Reata Pharmaceuticals Inc | Bardoksolon meтil za lečenje gojaznosтi |
PL2651902T3 (pl) | 2010-12-17 | 2018-04-30 | Reata Pharmaceuticals, Inc. | Pirazolilowe i pirymidynylowe tricykliczne enony jako modulatory zapalenia o działaniu przeciwutleniającym |
UY33946A (es) | 2011-03-11 | 2012-08-31 | Reata Pharmaceuticals Inc | Derivados de c4-monometil triterpenoides y sus métodos de uso |
CN103156861B (zh) * | 2011-12-08 | 2015-11-25 | 陈丽梅 | 齐敦果酸衍生物及其可药用盐在治疗糖尿病眼病中的应用 |
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US8981144B2 (en) | 2012-05-08 | 2015-03-17 | Trustees Of Dartmouth College | Method for synthesizing 2-cyano-3,12-dioxoolean-1, 9(11)-dien-28-oic acid methyl ester and derivatives thereof |
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CA2884400A1 (en) * | 2012-09-10 | 2014-03-13 | Abbvie Inc. | Glycyrrhetinic acid derivatives and methods of use thereof |
US9278912B2 (en) | 2012-09-10 | 2016-03-08 | Reata Pharmaceuticals, Inc. | C13-hydroxy derivatives of oleanolic acid and methods of use thereof |
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AU2002243246A1 (en) * | 2000-11-28 | 2002-06-24 | Board Of Regents, The University Of Texas System | Cddo-compounds and combination therapies thereof |
CA2485565A1 (en) * | 2002-05-13 | 2004-08-05 | Trustees Of Dartmouth College | Inhibitors and methods of use thereof |
JP3618341B2 (ja) * | 2003-04-15 | 2005-02-09 | 山之内製薬株式会社 | 臭化物及びその結晶 |
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