PE20171333A1 - Sal de acido toluensulfonico (tosilato) de n-[3-[(4ar,7as)-2-amino-6-(5-fluoropirimidina-2-il)-4,4a,5,7-tetrahidropirrolo[3,4-d][1,3]tiazina-7a-il]-4-fluoro-fenil]-5-metoxi-pirazina-2-carboxamida - Google Patents

Sal de acido toluensulfonico (tosilato) de n-[3-[(4ar,7as)-2-amino-6-(5-fluoropirimidina-2-il)-4,4a,5,7-tetrahidropirrolo[3,4-d][1,3]tiazina-7a-il]-4-fluoro-fenil]-5-metoxi-pirazina-2-carboxamida

Info

Publication number
PE20171333A1
PE20171333A1 PE2017001211A PE2017001211A PE20171333A1 PE 20171333 A1 PE20171333 A1 PE 20171333A1 PE 2017001211 A PE2017001211 A PE 2017001211A PE 2017001211 A PE2017001211 A PE 2017001211A PE 20171333 A1 PE20171333 A1 PE 20171333A1
Authority
PE
Peru
Prior art keywords
tetrahydropyrrolo
thiazine
pyrazine
carboxamide
fluoro
Prior art date
Application number
PE2017001211A
Other languages
English (en)
Inventor
David Andrew Coates
Craig Daniel Wolfangel
Original Assignee
Lilly Co Eli
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of PE20171333A1 publication Critical patent/PE20171333A1/es

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Classifications

    • 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

Abstract

Se refiere a la forma cristalina de la sal de tosilato de N-[3-[(4aR,7aS)-2-amino-6-(5-fluoropirimidin-2-il)-4,4a,5,7-tetrahidropirrolo[3,4-d][1,3]tiazina-7a-il]-4-fluoro-fenil]-5-metoxi-pirazina-2-carboxamida de formula I, caracterizado porque comprende, en el espectro de difraccion de rayos X a un angulo de difraccion 2-theta, picos tales como: 5.0°, 19.6°, 13.8° y 18.5° ± 0.2° (2-theta). Tambien se refiere a una composicion farmaceutica. Dichos compuestos son utiles en el tratamiento del Alzheimer y trastornos que implican el peptido beta amiloide.
PE2017001211A 2015-01-30 2016-01-22 Sal de acido toluensulfonico (tosilato) de n-[3-[(4ar,7as)-2-amino-6-(5-fluoropirimidina-2-il)-4,4a,5,7-tetrahidropirrolo[3,4-d][1,3]tiazina-7a-il]-4-fluoro-fenil]-5-metoxi-pirazina-2-carboxamida PE20171333A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562109733P 2015-01-30 2015-01-30

Publications (1)

Publication Number Publication Date
PE20171333A1 true PE20171333A1 (es) 2017-09-13

Family

ID=55275232

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017001211A PE20171333A1 (es) 2015-01-30 2016-01-22 Sal de acido toluensulfonico (tosilato) de n-[3-[(4ar,7as)-2-amino-6-(5-fluoropirimidina-2-il)-4,4a,5,7-tetrahidropirrolo[3,4-d][1,3]tiazina-7a-il]-4-fluoro-fenil]-5-metoxi-pirazina-2-carboxamida

Country Status (41)

Country Link
US (1) US10080758B2 (es)
EP (1) EP3250575B1 (es)
JP (2) JP6723250B2 (es)
KR (1) KR101950129B1 (es)
CN (1) CN107108657B (es)
AR (1) AR103406A1 (es)
AU (1) AU2016211827B2 (es)
BR (1) BR112017012149A2 (es)
CA (1) CA2969475C (es)
CL (1) CL2017001899A1 (es)
CO (1) CO2017007810A2 (es)
CR (1) CR20170287A (es)
CY (1) CY1122548T1 (es)
DK (1) DK3250575T3 (es)
DO (1) DOP2017000159A (es)
EA (1) EA031330B1 (es)
EC (1) ECSP17048768A (es)
ES (1) ES2768782T3 (es)
GT (1) GT201700166A (es)
HR (1) HRP20192240T1 (es)
HU (1) HUE048029T2 (es)
IL (1) IL252754A0 (es)
LT (1) LT3250575T (es)
MA (1) MA41420B1 (es)
MD (1) MD3250575T2 (es)
ME (1) ME03581B (es)
MX (1) MX2017009713A (es)
NZ (1) NZ732381A (es)
PE (1) PE20171333A1 (es)
PH (1) PH12017501356A1 (es)
PL (1) PL3250575T3 (es)
PT (1) PT3250575T (es)
RS (1) RS59730B1 (es)
SG (1) SG11201706038PA (es)
SI (1) SI3250575T1 (es)
SV (1) SV2017005478A (es)
TN (1) TN2017000332A1 (es)
TW (1) TWI574969B (es)
UA (1) UA119581C2 (es)
WO (1) WO2016122968A1 (es)
ZA (1) ZA201703937B (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR103406A1 (es) * 2015-01-30 2017-05-10 Lilly Co Eli Sal de tosilato
WO2019094608A1 (en) 2017-11-08 2019-05-16 Denali Therapeutics Inc. Anti-bace1 antibodies and methods of use thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
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-
NZ585671A (en) * 2007-12-07 2012-06-29 Pfizer Tosylate salt of trans-n-isobutyl-3-fluoro-3- [3-fluoro-4- (pyrrolidin-1-yl-methyl) -phenyl] cyclobut anecarboxamide
EP2233474B1 (en) * 2008-01-18 2015-08-05 Eisai R&D Management 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
AR103406A1 (es) * 2015-01-30 2017-05-10 Lilly Co Eli Sal de tosilato

Also Published As

Publication number Publication date
KR101950129B1 (ko) 2019-02-19
MA41420B1 (fr) 2020-02-28
ME03581B (me) 2020-07-20
ES2768782T3 (es) 2020-06-23
SI3250575T1 (sl) 2019-12-31
EA031330B1 (ru) 2018-12-28
DOP2017000159A (es) 2017-07-31
PL3250575T3 (pl) 2020-06-01
CA2969475A1 (en) 2016-08-04
AU2016211827B2 (en) 2018-04-26
CA2969475C (en) 2019-06-18
CN107108657A (zh) 2017-08-29
CL2017001899A1 (es) 2018-03-23
EP3250575B1 (en) 2019-11-20
GT201700166A (es) 2018-11-23
PT3250575T (pt) 2020-01-16
AU2016211827A1 (en) 2017-06-22
SV2017005478A (es) 2018-02-09
JP2019142902A (ja) 2019-08-29
RS59730B1 (sr) 2020-02-28
ZA201703937B (en) 2019-01-30
EA201791229A1 (ru) 2017-11-30
EP3250575A1 (en) 2017-12-06
BR112017012149A2 (pt) 2018-01-02
MX2017009713A (es) 2017-11-17
SG11201706038PA (en) 2017-08-30
JP6723250B2 (ja) 2020-07-15
NZ732381A (en) 2018-05-25
ECSP17048768A (es) 2017-11-30
AR103406A1 (es) 2017-05-10
US20170368071A1 (en) 2017-12-28
TW201636354A (zh) 2016-10-16
TN2017000332A1 (en) 2019-01-16
JP2018503666A (ja) 2018-02-08
CO2017007810A2 (es) 2017-10-20
CR20170287A (es) 2017-07-20
PH12017501356A1 (en) 2017-12-11
KR20170097782A (ko) 2017-08-28
UA119581C2 (uk) 2019-07-10
CY1122548T1 (el) 2021-01-27
HRP20192240T1 (hr) 2020-03-06
DK3250575T3 (da) 2020-01-20
TWI574969B (zh) 2017-03-21
MD3250575T2 (ro) 2020-03-31
HUE048029T2 (hu) 2020-05-28
CN107108657B (zh) 2021-10-08
LT3250575T (lt) 2020-02-10
US10080758B2 (en) 2018-09-25
WO2016122968A1 (en) 2016-08-04
IL252754A0 (en) 2017-08-31

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