HRP20211557T1 - Pripravci i postupci povezani s piridinoilpiperidinskim agonistima 5-ht1f - Google Patents
Pripravci i postupci povezani s piridinoilpiperidinskim agonistima 5-ht1f Download PDFInfo
- Publication number
- HRP20211557T1 HRP20211557T1 HRP20211557TT HRP20211557T HRP20211557T1 HR P20211557 T1 HRP20211557 T1 HR P20211557T1 HR P20211557T T HRP20211557T T HR P20211557TT HR P20211557 T HRP20211557 T HR P20211557T HR P20211557 T1 HRP20211557 T1 HR P20211557T1
- Authority
- HR
- Croatia
- Prior art keywords
- dihydrate
- pharmaceutical preparation
- benzamide
- trifluoro
- carbonyl
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims 2
- 239000000556 agonist Substances 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- YSWVIKAWHDUJFE-UHFFFAOYSA-N piperidin-1-yl(pyridin-2-yl)methanone Chemical compound C=1C=CC=NC=1C(=O)N1CCCCC1 YSWVIKAWHDUJFE-UHFFFAOYSA-N 0.000 title 1
- 150000004683 dihydrates Chemical class 0.000 claims 7
- 239000000825 pharmaceutical preparation Substances 0.000 claims 4
- 238000002441 X-ray diffraction Methods 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- KXDAEFPNCMNJSK-UHFFFAOYSA-N benzene carboxamide Natural products NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 1
- QKIMTLNRLDSKFU-UHFFFAOYSA-N butanedioic acid tetrahydrate Chemical compound C(CCC(=O)O)(=O)O.O.O.O.O QKIMTLNRLDSKFU-UHFFFAOYSA-N 0.000 claims 1
- MSOIHUHNGPOCTH-UHFFFAOYSA-N butanedioic acid;2,4,6-trifluoro-n-[6-(1-methylpiperidine-4-carbonyl)pyridin-2-yl]benzamide Chemical compound OC(=O)CCC(O)=O.C1CN(C)CCC1C(=O)C1=CC=CC(NC(=O)C=2C(=CC(F)=CC=2F)F)=N1.C1CN(C)CCC1C(=O)C1=CC=CC(NC(=O)C=2C(=CC(F)=CC=2F)F)=N1 MSOIHUHNGPOCTH-UHFFFAOYSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004128 high performance liquid chromatography Methods 0.000 claims 1
- 239000012535 impurity Substances 0.000 claims 1
- XEDHVZKDSYZQBF-UHFFFAOYSA-N lasmiditan Chemical compound C1CN(C)CCC1C(=O)C1=CC=CC(NC(=O)C=2C(=CC(F)=CC=2F)F)=N1 XEDHVZKDSYZQBF-UHFFFAOYSA-N 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 238000005550 wet granulation 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
- A61K31/33—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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (9)
1. Dihidrat hemisukcinatne soli 2,4,6-trifluor-N-[6-(1-metilpiperidin-4-karbonil)piridin-2-il]benzamida (Oblik D), naznačen time što ima difrakcija rendgenskih zraka koja sadrži maksimume na 18,7, 26,5, 27,0, 27,5 i 27,8 stupnjeva 2θ, ± 0,2 stupnjeva, uz upotrebu zračenja Cu-Kα.
2. Dihidrat u skladu s patentnim zahtjevom 1, naznačen time što difrakcija rendgenskih zraka sadrži jedan ili više sljedećih dodatnih maksimuma na 8,5, 9,7, 11,9, 13,8, 14,0, 15,4, 15,5, 15,8, 17,0, 17,3, 17,7, 18,0, 18,9, 19,3, 19,8, 20,0, 20,8, 21,4, 21,6, 21,9, 22,4, 22,7, 23,0, 24,1, 24,3, 24,7, 25,6, 25,9, 26,1, 26,4, 28,4, 29,1, 29,6, 29,8 ili 31,9 stupnjeva 2θ uz upotrebu zračenja Cu-Kα.
3. Dihidrat u skladu s patentnim zahtjevom 1, dodatno naznačen time što ima parametre jedinične ćelije na 100 Kelvina od otprilike a = 25,08 Å, b = 10,08 Å, c = 20,84 Å, α =90°, β = 123,71, a kut γ = 90°.
4. Dihidrat u skladu s patentnim zahtjevom 1, naznačen time što ga se dobiva postupkom koji se sastoji u mokrom granuliranju amorfnog 2,4,6-trifluor-N-[6-(1-metilpiperidin-4-karbonil)piridin-2-il]benzamid-hemisukcinata.
5. Farmaceutski pripravak, naznačen time što sadrži dihidrat u skladu s bilo kojim od patentnih zahtjeva 1 do 4, kao i farmaceutski prihvatljivi nosač.
6. Farmaceutski pripravak u skladu s patentnim zahtjevom 5, naznačen time što navedeni dihidrat uglavnom ne sadrži nečistoće.
7. Farmaceutski pripravak u skladu s patentnim zahtjevom 6, naznačen time što navedeni dihidrat ima kemijsku čistoću veću od 98,0%, što je određeno HPLC-om.
8. Farmaceutski pripravak u skladu s patentnim zahtjevom 5, naznačen time što dodatno sadrži bezvodni čvrsti kristalni oblik hemisukcinatne soli 2,4,6-trifluor-N-[6-(1-metilpiperidin-4-karbonil)piridin-2-il]benzamida (Oblik A).
9. Dihidrat u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što je namijenjen upotrebi u liječenju migrene.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662430662P | 2016-12-06 | 2016-12-06 | |
| EP17829372.6A EP3551617B1 (en) | 2016-12-06 | 2017-12-05 | Compositions and methods related to pyridinoylpiperidine 5-ht1f agonists |
| PCT/US2017/064652 WO2018106657A1 (en) | 2016-12-06 | 2017-12-05 | Compositions and methods related to pyridinoylpiperidine 5-ht1f agonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20211557T1 true HRP20211557T1 (hr) | 2022-01-07 |
Family
ID=60972336
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20211557TT HRP20211557T1 (hr) | 2016-12-06 | 2017-12-05 | Pripravci i postupci povezani s piridinoilpiperidinskim agonistima 5-ht1f |
Country Status (38)
| Country | Link |
|---|---|
| US (1) | US11053214B2 (hr) |
| EP (1) | EP3551617B1 (hr) |
| JP (3) | JP2020500936A (hr) |
| KR (3) | KR20190075130A (hr) |
| CN (3) | CN115385894A (hr) |
| AU (1) | AU2017373784B2 (hr) |
| BR (1) | BR112019010934A2 (hr) |
| CA (1) | CA3043772C (hr) |
| CL (1) | CL2019001426A1 (hr) |
| CO (1) | CO2019005290A2 (hr) |
| CR (1) | CR20190251A (hr) |
| CY (1) | CY1124540T1 (hr) |
| DK (1) | DK3551617T3 (hr) |
| DO (1) | DOP2019000139A (hr) |
| EA (1) | EA201991112A1 (hr) |
| EC (1) | ECSP19040190A (hr) |
| ES (1) | ES2889476T3 (hr) |
| HR (1) | HRP20211557T1 (hr) |
| HU (1) | HUE056820T2 (hr) |
| IL (1) | IL266598B2 (hr) |
| JO (1) | JOP20190129B1 (hr) |
| LT (1) | LT3551617T (hr) |
| MA (1) | MA52920B1 (hr) |
| MD (1) | MD3551617T2 (hr) |
| MX (2) | MX2021014139A (hr) |
| MY (1) | MY196855A (hr) |
| NZ (1) | NZ752906A (hr) |
| PE (1) | PE20191134A1 (hr) |
| PH (1) | PH12019501252A1 (hr) |
| PL (1) | PL3551617T3 (hr) |
| PT (1) | PT3551617T (hr) |
| RS (1) | RS62415B1 (hr) |
| SI (1) | SI3551617T1 (hr) |
| TN (1) | TN2019000174A1 (hr) |
| TW (1) | TWI671290B (hr) |
| UA (1) | UA124433C2 (hr) |
| WO (1) | WO2018106657A1 (hr) |
| ZA (1) | ZA201903449B (hr) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR119319A1 (es) * | 2019-07-09 | 2021-12-09 | Lilly Co Eli | Procesos e intermediario para la preparación a gran escala de hemisuccinato de 2,4,6-trifluoro-n-[6-(1-metil-piperidina-4-carbonil)-piridin-2-il]-benzamida y preparación de acetato de 2,4,6-trifluoro-n-[6-(1-metil-piperidina-4-carbonil)-piridin-2-il]-benzamida |
| CN111004214B (zh) * | 2019-11-22 | 2021-06-08 | 广东东阳光药业有限公司 | 吡啶酰基哌啶衍生物及其用途 |
| EP4333815A1 (en) | 2021-05-07 | 2024-03-13 | Eli Lilly And Company | Taste masked compostions of 2,4,6-trifluoro- n-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2- ylj-benzamide hemisuccinate, and orally disentegrating tablet comprising the same |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US5011472A (en) | 1988-09-06 | 1991-04-30 | Brown University Research Foundation | Implantable delivery system for biological factors |
| TWI263497B (en) | 2002-03-29 | 2006-10-11 | Lilly Co Eli | Pyridinoylpiperidines as 5-HT1F agonists |
| US20060178349A1 (en) * | 2005-01-24 | 2006-08-10 | Pozen Inc. | Compositions and therapeutic methods utilizing a combination of a 5-HT1F inhibitor and an NSAID |
| AU2010232497B2 (en) * | 2009-04-02 | 2016-05-19 | Colucid Pharmaceuticals, Inc. | Composition of 2,4,6-trifluoro-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-benzamide |
| WO2011123654A1 (en) * | 2010-04-02 | 2011-10-06 | Colucid Pharmaceuticals, Inc. | Compositions and methods of synthesis of pyridinoylpiperidine 5-ht1f agonists |
| WO2012163365A1 (en) | 2011-06-01 | 2012-12-06 | Concit Pharma Aps | Combinations of serotonin receptor agonists for treatment of movement disorders |
| CN113121498A (zh) | 2016-07-15 | 2021-07-16 | 杭州领业医药科技有限公司 | 一种受体激动剂的晶型及其制备方法和药物组合物 |
| TWI754772B (zh) | 2017-09-06 | 2022-02-11 | 美商美國禮來大藥廠 | 用於治療偏頭痛之拉米迪坦(lasmiditan)與cgrp拮抗劑之組合療法 |
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2017
- 2017-12-05 JP JP2019551251A patent/JP2020500936A/ja active Pending
- 2017-12-05 MX MX2021014139A patent/MX2021014139A/es unknown
- 2017-12-05 MY MYPI2019003189A patent/MY196855A/en unknown
- 2017-12-05 TN TNP/2019/000174A patent/TN2019000174A1/en unknown
- 2017-12-05 PE PE2019001167A patent/PE20191134A1/es unknown
- 2017-12-05 HU HUE17829372A patent/HUE056820T2/hu unknown
- 2017-12-05 DK DK17829372.6T patent/DK3551617T3/da active
- 2017-12-05 CN CN202210944373.9A patent/CN115385894A/zh active Pending
- 2017-12-05 UA UAA201905483A patent/UA124433C2/uk unknown
- 2017-12-05 BR BR112019010934A patent/BR112019010934A2/pt active Search and Examination
- 2017-12-05 KR KR1020197016255A patent/KR20190075130A/ko active Application Filing
- 2017-12-05 MX MX2019006520A patent/MX2019006520A/es unknown
- 2017-12-05 CA CA3043772A patent/CA3043772C/en active Active
- 2017-12-05 EA EA201991112A patent/EA201991112A1/ru unknown
- 2017-12-05 TW TW106142535A patent/TWI671290B/zh active
- 2017-12-05 KR KR1020227046438A patent/KR20230008257A/ko not_active Application Discontinuation
- 2017-12-05 CN CN202210944298.6A patent/CN115385893A/zh active Pending
- 2017-12-05 HR HRP20211557TT patent/HRP20211557T1/hr unknown
- 2017-12-05 AU AU2017373784A patent/AU2017373784B2/en active Active
- 2017-12-05 SI SI201730881T patent/SI3551617T1/sl unknown
- 2017-12-05 WO PCT/US2017/064652 patent/WO2018106657A1/en active Application Filing
- 2017-12-05 RS RS20211233A patent/RS62415B1/sr unknown
- 2017-12-05 EP EP17829372.6A patent/EP3551617B1/en active Active
- 2017-12-05 CR CR20190251A patent/CR20190251A/es unknown
- 2017-12-05 PL PL17829372T patent/PL3551617T3/pl unknown
- 2017-12-05 MD MDE20191169T patent/MD3551617T2/ro unknown
- 2017-12-05 JO JOP/2019/0129A patent/JOP20190129B1/ar active
- 2017-12-05 PT PT17829372T patent/PT3551617T/pt unknown
- 2017-12-05 LT LTEPPCT/US2017/064652T patent/LT3551617T/lt unknown
- 2017-12-05 IL IL266598A patent/IL266598B2/en unknown
- 2017-12-05 KR KR1020217025499A patent/KR20210102497A/ko not_active Application Discontinuation
- 2017-12-05 MA MA52920A patent/MA52920B1/fr unknown
- 2017-12-05 NZ NZ752906A patent/NZ752906A/en unknown
- 2017-12-05 US US16/467,208 patent/US11053214B2/en active Active
- 2017-12-05 CN CN201780075750.7A patent/CN110291079A/zh active Pending
- 2017-12-05 ES ES17829372T patent/ES2889476T3/es active Active
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2019
- 2019-05-23 CO CONC2019/0005290A patent/CO2019005290A2/es unknown
- 2019-05-27 CL CL2019001426A patent/CL2019001426A1/es unknown
- 2019-05-30 DO DO2019000139A patent/DOP2019000139A/es unknown
- 2019-05-30 ZA ZA2019/03449A patent/ZA201903449B/en unknown
- 2019-06-06 PH PH12019501252A patent/PH12019501252A1/en unknown
- 2019-06-06 EC ECSENADI201940190A patent/ECSP19040190A/es unknown
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2021
- 2021-09-22 JP JP2021153729A patent/JP2022000451A/ja active Pending
- 2021-10-05 CY CY20211100864T patent/CY1124540T1/el unknown
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2023
- 2023-06-26 JP JP2023104019A patent/JP2023123678A/ja active Pending
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