HRP20181567T2 - Kristalni metiltioninij klorid hidrati – dio 2 - Google Patents
Kristalni metiltioninij klorid hidrati – dio 2 Download PDFInfo
- Publication number
- HRP20181567T2 HRP20181567T2 HRP20181567TT HRP20181567T HRP20181567T2 HR P20181567 T2 HRP20181567 T2 HR P20181567T2 HR P20181567T T HRP20181567T T HR P20181567TT HR P20181567 T HRP20181567 T HR P20181567T HR P20181567 T2 HRP20181567 T2 HR P20181567T2
- Authority
- HR
- Croatia
- Prior art keywords
- methylthioninium chloride
- chloride monohydrate
- cukα
- hydrates
- wavelength
- Prior art date
Links
- LXQCLHQAJVBFGN-UHFFFAOYSA-N 2-methylthionin-1-ium;chloride;hydrate Chemical class O.[Cl-].CC1=CC=CC=CC=C[SH+]1 LXQCLHQAJVBFGN-UHFFFAOYSA-N 0.000 title claims 6
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- XQAXGZLFSSPBMK-UHFFFAOYSA-M [7-(dimethylamino)phenothiazin-3-ylidene]-dimethylazanium;chloride;trihydrate Chemical compound O.O.O.[Cl-].C1=CC(=[N+](C)C)C=C2SC3=CC(N(C)C)=CC=C3N=C21 XQAXGZLFSSPBMK-UHFFFAOYSA-M 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 229960000907 methylthioninium chloride Drugs 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- 239000007787 solid Substances 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 208000005176 Hepatitis C Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000034799 Tauopathies Diseases 0.000 claims 1
- 241000710886 West Nile virus Species 0.000 claims 1
- 238000007664 blowing Methods 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 238000000354 decomposition reaction Methods 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000001914 filtration Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000001291 vacuum drying Methods 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
- C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
- C07D279/18—[b, e]-condensed with two six-membered rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4515—Non condensed piperidines, e.g. piperocaine having a butyrophenone group in position 1, e.g. haloperidol
-
- 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
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
- C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
- C07D279/18—[b, e]-condensed with two six-membered rings
- C07D279/22—[b, e]-condensed with two six-membered rings with carbon atoms directly attached to the ring nitrogen atom
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Crystals, And After-Treatments Of Crystals (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Steroid Compounds (AREA)
Claims (6)
1. Kristalni metiltioninij klorid monohidrat u Obliku E, naznačen time, da ima slijedeće karakteristične maksimume u difraktogramu rendgenske difrakcije praha (koristeći CuKα kao izvor radijacije, na valnoj duljini od 1.54180 Å):
[image]
2. Spoj prema zahtjevu 1, naznačen time, da ima slijedeće karakteristične maksimume u difraktogramu rendgenske difrakcije praha (koristeći CuKα kao izvor radijacije, na valnoj duljini od 1.54180 Å):
[image]
ili ne pokazuje termalni događaj sve do temperature dekompozicije od 220°C, kada se zagrijava brzinom od 100°C po minuti diferencijalnom pretražnom kalorimetrijom.
3. Postupak za dobivanje metiltioninij klorid monohidrata u Obliku E prema zahtjevu 1 ili zahtjevu 2, naznačen time, da se metiltioninij klorid koji sadrži vodu ili mješavina različitih hidrata ili specifičnih hidrata metiltioninij klorida, suspendira i miješa na ambijentalnoj temperaturi u suhom otapalu, poželjno u izopropanolu, da bi se stvorio Oblik E, a krutina se izolira filtracijom; i ostatak otapala se ukloni iz krutine ili vakuumskim sušenjem ili upuhivanjem suhog plina.
4. Farmaceutski pripravak, naznačen time, da sadrži metiltioninij klorid monohidrat u Obliku E prema zahtjevu 1 ili zahtjevu 2, i opcionalno farmaceutski prihvatljiv nosač, ekscipijent ili razrjeđivač.
5. Metiltioninij klorid monohidrat u Obliku E prema zahtjevu 1 ili zahtjevu 2, naznačen time, da služi za uporabu u postupku liječenja ljudskog ili životinjskog tijela putem terapije.
6. Metiltioninij klorid monohidrat u Obliku E prema zahtjevu 1 ili zahtjevu 2, naznačen time, da je za uporabu u postupku liječenja stanja bolesti, na primjer u liječenju tauopatije, Alzheimerove bolesti (AD), raka kože, melanoma, hepatitisa C, HIV-a ili virusa Zapadnog Nila.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24539109P | 2009-09-24 | 2009-09-24 | |
| EP15176967.6A EP2963024B1 (en) | 2009-09-24 | 2010-09-23 | Crystalline methylthioninium chloride hydrates - part 2 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HRP20181567T1 HRP20181567T1 (hr) | 2018-11-30 |
| HRP20181567T2 true HRP20181567T2 (hr) | 2022-09-30 |
Family
ID=43415329
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20181567TT HRP20181567T2 (hr) | 2009-09-24 | 2010-09-23 | Kristalni metiltioninij klorid hidrati – dio 2 |
| HRP20231201TT HRP20231201T1 (hr) | 2009-09-24 | 2010-09-23 | Kristalni metiltionij klorid hidrati |
| HRP20210086TT HRP20210086T1 (hr) | 2009-09-24 | 2021-01-19 | Kristalni metiltioninij-klorid-hidrati |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20231201TT HRP20231201T1 (hr) | 2009-09-24 | 2010-09-23 | Kristalni metiltionij klorid hidrati |
| HRP20210086TT HRP20210086T1 (hr) | 2009-09-24 | 2021-01-19 | Kristalni metiltioninij-klorid-hidrati |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US8765742B2 (hr) |
| EP (4) | EP3378856B1 (hr) |
| JP (1) | JP5806217B2 (hr) |
| KR (3) | KR20170061177A (hr) |
| CN (2) | CN102666511B (hr) |
| AU (1) | AU2010299571B2 (hr) |
| BR (4) | BR122019022631B8 (hr) |
| CA (4) | CA3141737C (hr) |
| DK (4) | DK2963024T3 (hr) |
| ES (4) | ES2689029T3 (hr) |
| FI (1) | FI3792254T3 (hr) |
| HK (2) | HK1167653A1 (hr) |
| HR (3) | HRP20181567T2 (hr) |
| MX (2) | MX2012003083A (hr) |
| MY (1) | MY159782A (hr) |
| PL (4) | PL2480541T3 (hr) |
| PT (4) | PT2480541E (hr) |
| SG (1) | SG10201408584UA (hr) |
| SI (4) | SI2963024T1 (hr) |
| WO (1) | WO2011036558A2 (hr) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9925282B2 (en) | 2009-01-29 | 2018-03-27 | The General Hospital Corporation | Cromolyn derivatives and related methods of imaging and treatment |
| EP2480540B1 (en) * | 2009-09-24 | 2017-11-29 | WisTa Laboratories Ltd. | Methylthioninium chloride pentahydrate, preparation and pharmaceutical use thereof |
| US10058530B2 (en) | 2012-10-25 | 2018-08-28 | The General Hospital Corporation | Combination therapies for the treatment of Alzheimer's disease and related disorders |
| EP3563849A3 (en) * | 2012-10-25 | 2020-02-12 | The General Hospital Corporation | Combination therapies for the treatment of alzheimer's disease and related disorders |
| US10525005B2 (en) | 2013-05-23 | 2020-01-07 | The General Hospital Corporation | Cromolyn compositions and methods thereof |
| EP3060205A4 (en) | 2013-10-22 | 2017-06-28 | The General Hospital Corporation | Cromolyn derivatives and related methods of imaging and treatment |
| US10765755B1 (en) | 2013-11-20 | 2020-09-08 | University Of South Florida | Preparation and characterization of methylene blue nanoparticles for Alzheimer's disease and other tauopathies |
| MY201804A (en) | 2016-07-25 | 2024-03-19 | Wista Laboratories Ltd | Administration and dosage of diaminophenothiazines |
| CA3033079A1 (en) | 2016-08-31 | 2018-03-08 | The General Hospital Corporation | Macrophages/microglia in neuro-inflammation associated with neurodegenerative diseases |
| GB201614834D0 (en) | 2016-09-01 | 2016-10-19 | Wista Lab Ltd | Treatment of dementia |
| WO2019017995A1 (en) | 2017-07-20 | 2019-01-24 | Aztherapies, Inc. | FORMULATIONS OF CROMOLYNE SODIUM POWDER AND IBUPROFEN |
| CN113038944A (zh) | 2018-07-02 | 2021-06-25 | 通用医疗公司 | 色甘酸钠和α-乳糖的粉末化制剂 |
| WO2023232764A1 (en) | 2022-05-31 | 2023-12-07 | Wista Laboratories Ltd. | Treatment of neurodegenerative disorders utilising methylthioninium (mt)-containing compounds |
| WO2024061971A1 (en) | 2022-09-21 | 2024-03-28 | Wista Laboratories Ltd. | Novel formulations and vehicles |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9506197D0 (en) | 1995-03-27 | 1995-05-17 | Hoffmann La Roche | Inhibition of tau-tau association. |
| GB0101049D0 (en) | 2001-01-15 | 2001-02-28 | Univ Aberdeen | Materials and methods relating to protein aggregation in neurodegenerative disease |
| GB0322756D0 (en) | 2003-09-29 | 2003-10-29 | Univ Aberdeen | Methods of chemical synthesis |
| JP5186212B2 (ja) * | 2004-09-23 | 2013-04-17 | ウィスタ ラボラトリーズ リミテッド | メチルチオニニウム塩化物（ｍｔｃ）などのジアミノフェノチアジニウム化合物を化学合成および精製する方法 |
| WO2006032879A2 (en) | 2004-09-23 | 2006-03-30 | Wista Laboratories Ltd. | Methods of chemical synthesis and purification of diaminophenothiazinium compounds including methylthioninium chloride (mtc) |
| CN104119294B (zh) * | 2006-03-29 | 2018-10-30 | 维斯塔实验室有限公司 | 3,7-二氨基-10h-吩噻嗪化合物的制备方法 |
| CN103735554B (zh) | 2006-03-29 | 2018-03-20 | 维斯塔实验室有限公司 | 蛋白聚集抑制剂 |
| CN101631780A (zh) * | 2007-04-03 | 2010-01-20 | 普罗瑟塔生物谐成公司 | 用于抗病毒治疗的吩噻嗪衍生物 |
| US7603854B2 (en) | 2007-04-10 | 2009-10-20 | Illinois Tool Works Inc. | Pneumatically self-regulating valve |
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2010
- 2010-09-23 PT PT107715161T patent/PT2480541E/pt unknown
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- 2010-09-23 US US13/497,686 patent/US8765742B2/en active Active
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- 2010-09-23 KR KR1020187022958A patent/KR20180094126A/ko not_active Application Discontinuation
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2021
- 2021-01-19 HR HRP20210086TT patent/HRP20210086T1/hr unknown
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