HRP20192240T1 - TOSILATNA SOL N-[3-[(4aR,7aS)-2-AMINO-6-(5-FLUOROPIRIMIDIN-2-IL)-4,4a,5,7-TETRAHIDROPIROLO[3,4-d][1,3]TIAZIN-7a-IL]-4-FLUOROFENIL]-5-METOKSIPIRAZIN-2-KARBOKSAMIDA - Google Patents
TOSILATNA SOL N-[3-[(4aR,7aS)-2-AMINO-6-(5-FLUOROPIRIMIDIN-2-IL)-4,4a,5,7-TETRAHIDROPIROLO[3,4-d][1,3]TIAZIN-7a-IL]-4-FLUOROFENIL]-5-METOKSIPIRAZIN-2-KARBOKSAMIDA Download PDFInfo
- Publication number
- HRP20192240T1 HRP20192240T1 HRP20192240TT HRP20192240T HRP20192240T1 HR P20192240 T1 HRP20192240 T1 HR P20192240T1 HR P20192240T T HRP20192240T T HR P20192240TT HR P20192240 T HRP20192240 T HR P20192240T HR P20192240 T1 HRP20192240 T1 HR P20192240T1
- Authority
- HR
- Croatia
- Prior art keywords
- tosylate salt
- tetrahydropyrrolo
- fluoropyrimidin
- thiazin
- carboxamide
- Prior art date
Links
- 125000005490 tosylate group Chemical class 0.000 title claims 4
- VQSRKMNBWMHJKY-YTEVENLXSA-N n-[3-[(4ar,7as)-2-amino-6-(5-fluoropyrimidin-2-yl)-4,4a,5,7-tetrahydropyrrolo[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]-5-methoxypyrazine-2-carboxamide Chemical compound C1=NC(OC)=CN=C1C(=O)NC1=CC=C(F)C([C@@]23[C@@H](CN(C2)C=2N=CC(F)=CN=2)CSC(N)=N3)=C1 VQSRKMNBWMHJKY-YTEVENLXSA-N 0.000 title claims 2
- 150000001875 compounds Chemical class 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 238000002441 X-ray diffraction Methods 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000001228 spectrum Methods 0.000 claims 1
- 238000002560 therapeutic procedure 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P25/28—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- 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
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (7)
1. Spoj, naznačen time što je tosilatna sol N-[3-[(4aR,7aS)-2-amino-6-(5-fluorpirimidin-2-il)-4,4a,5,7-tetrahidropirolo[3,4-d][1,3]tiazin-7a-il]-4-fluorfenil]-5-metoksipirazin-2-karboksamida.
2. Tosilatna sol u skladu s patentnim zahtjevom 1, naznačena time što je kristalna.
3. Tosilatna sol u skladu s bilo patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačena time što ima značajan maksimum u spektru difrakcije rendgenskih zraka, pod kutom difrakcije 2θ od 5,0°, u kombinaciji s jednim ili više maksimuma, koje se bira iz skupine koju čine 19,6°, 13,8°, te 18,5°; uz toleranciju za kutove difrakcije od 0,2 stupnjeva.
4. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što je namijenjen upotrebi u terapiji.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što je namijenjen upotrebi u liječenju Alzheimerove bolesti.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što je namijenjen upotrebi u liječenju napredovanja od blagog kognitivnog poremećaja do Alzheimerove bolesti.
7. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, kao i jedan ili više farmaceutski prihvatljivih nosača, razrjeđivača ili pomoćnih tvari.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562109733P | 2015-01-30 | 2015-01-30 | |
| PCT/US2016/014423 WO2016122968A1 (en) | 2015-01-30 | 2016-01-22 | Tosylate salt of n-[3-[(4ar,7as)-2-amino-6-(5-fluoropyrimidin-2-yl)-4,4a,5,7-tetrahydropyrrolo[3,4-d][1,3]thiazin-7a-yl]-4-fluoro-phenyl]-5-methoxy-pyrazine-2-carboxamide |
| EP16702654.1A EP3250575B1 (en) | 2015-01-30 | 2016-01-22 | Tosylate salt of n-[3-[(4ar,7as)-2-amino-6-(5-fluoropyrimidin-2-yl)-4,4a,5,7-tetrahydropyrrolo[3,4-d][1,3]thiazin-7a-yl]-4-fluoro-phenyl]-5-methoxy-pyrazine-2-carboxamide. |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20192240T1 true HRP20192240T1 (hr) | 2020-03-06 |
Family
ID=55275232
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20192240TT HRP20192240T1 (hr) | 2015-01-30 | 2019-12-12 | TOSILATNA SOL N-[3-[(4aR,7aS)-2-AMINO-6-(5-FLUOROPIRIMIDIN-2-IL)-4,4a,5,7-TETRAHIDROPIROLO[3,4-d][1,3]TIAZIN-7a-IL]-4-FLUOROFENIL]-5-METOKSIPIRAZIN-2-KARBOKSAMIDA |
Country Status (41)
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI574969B (zh) * | 2015-01-30 | 2017-03-21 | 美國禮來大藥廠 | 甲苯磺酸鹽 |
| WO2019094608A1 (en) | 2017-11-08 | 2019-05-16 | Denali Therapeutics Inc. | Anti-bace1 antibodies and methods of use thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AT401651B (de) * | 1994-06-14 | 1996-11-25 | Biochemie Gmbh | 7-(2-(2-aminothiazol-4-yl)-2-(z)- hydroximinoacetamido)-3-n,n- dimethylcarbamoyloxymethyl-3-cephem-4- |
| KR20100075679A (ko) * | 2007-12-07 | 2010-07-02 | 화이자 인코포레이티드 | 트랜스-ｎ-이소부틸-3-플루오로-3-[3-플루오로-4-(피롤리딘-1-일메틸)-페닐]-사이클로부탄카복스아미드의 토실레이트 염 |
| MY160690A (en) * | 2008-01-18 | 2017-03-15 | Eisai R&D Man Co Ltd | Condensed aminodihydrothiazine derivative |
| TWI593692B (zh) | 2013-03-12 | 2017-08-01 | 美國禮來大藥廠 | 四氫吡咯并噻嗪化合物 |
| TWI570127B (zh) * | 2014-09-15 | 2017-02-11 | 美國禮來大藥廠 | 結晶型N-[3-[(4aR,7aS)-2-胺基-6-(5-氟嘧啶-2-基)-4,4a,5,7-四氫吡咯并[3,4-d][1,3]噻嗪-7a-基]-4-氟-苯基]-5-甲氧基-吡嗪-2-甲醯胺、其用途及醫藥組合物 |
| TWI574969B (zh) * | 2015-01-30 | 2017-03-21 | 美國禮來大藥廠 | 甲苯磺酸鹽 |
-
2016
- 2016-01-13 TW TW105100973A patent/TWI574969B/zh not_active IP Right Cessation
- 2016-01-13 AR ARP160100076A patent/AR103406A1/es unknown
- 2016-01-22 ES ES16702654T patent/ES2768782T3/es active Active
- 2016-01-22 DK DK16702654.1T patent/DK3250575T3/da active
- 2016-01-22 EA EA201791229A patent/EA031330B1/ru not_active IP Right Cessation
- 2016-01-22 MA MA41420A patent/MA41420B1/fr unknown
- 2016-01-22 MX MX2017009713A patent/MX2017009713A/es unknown
- 2016-01-22 BR BR112017012149-2A patent/BR112017012149A2/pt not_active Application Discontinuation
- 2016-01-22 UA UAA201707108A patent/UA119581C2/uk unknown
- 2016-01-22 ME MEP-2019-347A patent/ME03581B/me unknown
- 2016-01-22 AU AU2016211827A patent/AU2016211827B2/en not_active Ceased
- 2016-01-22 PT PT167026541T patent/PT3250575T/pt unknown
- 2016-01-22 LT LTEP16702654.1T patent/LT3250575T/lt unknown
- 2016-01-22 MD MDE20170309T patent/MD3250575T2/ro unknown
- 2016-01-22 JP JP2017540253A patent/JP6723250B2/ja active Active
- 2016-01-22 TN TNP/2017/000332A patent/TN2017000332A1/en unknown
- 2016-01-22 SI SI201630517T patent/SI3250575T1/sl unknown
- 2016-01-22 RS RS20191663A patent/RS59730B1/sr unknown
- 2016-01-22 SG SG11201706038PA patent/SG11201706038PA/en unknown
- 2016-01-22 PE PE2017001211A patent/PE20171333A1/es unknown
- 2016-01-22 CN CN201680005234.2A patent/CN107108657B/zh active Active
- 2016-01-22 US US15/535,523 patent/US10080758B2/en active Active
- 2016-01-22 CR CR20170287A patent/CR20170287A/es unknown
- 2016-01-22 PL PL16702654T patent/PL3250575T3/pl unknown
- 2016-01-22 NZ NZ732381A patent/NZ732381A/en not_active IP Right Cessation
- 2016-01-22 WO PCT/US2016/014423 patent/WO2016122968A1/en active Application Filing
- 2016-01-22 EP EP16702654.1A patent/EP3250575B1/en active Active
- 2016-01-22 HU HUE16702654A patent/HUE048029T2/hu unknown
- 2016-01-22 KR KR1020177020943A patent/KR101950129B1/ko active IP Right Grant
- 2016-01-22 CA CA2969475A patent/CA2969475C/en not_active Expired - Fee Related
-
2017
- 2017-06-07 IL IL252754A patent/IL252754A0/en unknown
- 2017-06-08 ZA ZA2017/03937A patent/ZA201703937B/en unknown
- 2017-07-03 DO DO2017000159A patent/DOP2017000159A/es unknown
- 2017-07-06 SV SV2017005478A patent/SV2017005478A/es unknown
- 2017-07-25 CL CL2017001899A patent/CL2017001899A1/es unknown
- 2017-07-27 GT GT201700166A patent/GT201700166A/es unknown
- 2017-07-28 EC ECIEPI201748768A patent/ECSP17048768A/es unknown
- 2017-07-28 PH PH12017501356A patent/PH12017501356A1/en unknown
- 2017-08-01 CO CONC2017/0007810A patent/CO2017007810A2/es unknown
-
2019
- 2019-04-10 JP JP2019074951A patent/JP2019142902A/ja not_active Ceased
- 2019-12-12 HR HRP20192240TT patent/HRP20192240T1/hr unknown
-
2020
- 2020-01-15 CY CY20201100033T patent/CY1122548T1/el unknown
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