BRPI0414241A - composto, composição farmacêutica, métodos para ativar receptores 5-ht1f em um mamìfero, para inibir o extravasamento de proteìna neuronal em um mamìfero e para tratar ou prevenir enxaqueca em um mamìfero, e, uso de um composto - Google Patents

composto, composição farmacêutica, métodos para ativar receptores 5-ht1f em um mamìfero, para inibir o extravasamento de proteìna neuronal em um mamìfero e para tratar ou prevenir enxaqueca em um mamìfero, e, uso de um composto

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Publication number
BRPI0414241A
BRPI0414241A BRPI0414241-1A BRPI0414241A BRPI0414241A BR PI0414241 A BRPI0414241 A BR PI0414241A BR PI0414241 A BRPI0414241 A BR PI0414241A BR PI0414241 A BRPI0414241 A BR PI0414241A
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Brazil
Prior art keywords
mammal
alkyl
hydrogen
compound
substituted
Prior art date
Application number
BRPI0414241-1A
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English (en)
Inventor
Maris-Jesus Blanco-Pillado
Michael Philip Cohen
Sandra Ann Filla
Kevin John Hudziak
Daniel Timothy Kohlman
Dana Rae Benesh
Frantz Victor
Yao-Chang Xu
Bai-Ping Ying
Deanna Piatt Zacherl
Deyi Zhang
Brian Michael Mathes
Original Assignee
Lilly Co Eli
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Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of BRPI0414241A publication Critical patent/BRPI0414241A/pt

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    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4468Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
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    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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Abstract

"COMPOSTO, COMPOSIçãO FARMACêUTICA, MéTODOS PARA ATIVAR RECEPTORES 5-HT~ 1F~ EM UM MAMìFERO, PARA INIBIR O EXTRAVASAMENTO DE PROTEìNA NEURONAL EM UM MAMìFERO E PARA TRATAR OU PREVENIR ENXAQUECA EM UM MAMìFERO, E, USO DE UM COMPOSTO". A presente invenção diz respeito a compostos da fórmula I: ou um sal de adição de ácido farmaceuticamente aceitável destes, onde; X é C(R¬ 3c¬= ou N=; R¬ 1¬ é alquila C~ 2~-C~ 6~, alquila C~ 2~-C~ 6~ substituído, cicloalquila C~ 3~-C~ 7~, cicloalquila C~ 3~-C~ 7~ substituído, fenila, fenila substituído, heterociclo, ou heterociclo substituído; R¬ 2¬ é hidrogênio, n-alquila C~ 1~-C~ 3~, cicloaquila C~ 3~-C~ 6~-alquila C~ 1~-C~ 3~, ou um grupo da fórmula II contanto que quando R¬ 1¬ é alquila C~ 2~-C~6~ ou alquila C~ 2~-C~ 6~ substituída, R¬ 2¬ é hidrogênio ou metila; R¬ 3a¬, R¬ 3b¬ , e, quando X é C(R¬ 3c¬)=, R¬ 3c¬, são cada um independentemente hidrogênio, flúor, ou metila, contanto que não mais do que um de R¬ 3a¬ , R¬ 3b¬ , e R¬ 3c¬ possa ser outro além de hidrogênio; R¬ 4¬ é hidrogênio ou alquila C~ 1~-C~ 3~; R¬ 5¬ é hidrogênio, alquila C~ 1~-C~ 3~, ou cicloalquilcarbonila C~ 3~-C~ 6~, contanto que quando R¬ 3a¬ for outro que não hidrogênio, R¬ 5¬ é hidrogênio; R¬ 6¬ é hidrogênio ou alquila C~ 1~-C~ 6~; e n é um número inteiro de 1 a 6 inclusive. Os compostos da presente invenção são úteis para ativar os receptores 5-HT~ 1F~, inibir extravasamento de proteína neuronal, e para o tratamento ou prevenção de enxaqueca em um mamífero.
BRPI0414241-1A 2003-09-12 2004-09-03 composto, composição farmacêutica, métodos para ativar receptores 5-ht1f em um mamìfero, para inibir o extravasamento de proteìna neuronal em um mamìfero e para tratar ou prevenir enxaqueca em um mamìfero, e, uso de um composto BRPI0414241A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US50278003P 2003-09-12 2003-09-12
PCT/US2004/025607 WO2005035499A1 (en) 2003-09-12 2004-09-03 Substituted 2-carbonylamino-6-piperidinaminopyridines and substituted 1-carbonylamino-3-piperidinaminobenzenes as 5-ht1f agonists

Publications (1)

Publication Number Publication Date
BRPI0414241A true BRPI0414241A (pt) 2006-11-07

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BRPI0414241-1A BRPI0414241A (pt) 2003-09-12 2004-09-03 composto, composição farmacêutica, métodos para ativar receptores 5-ht1f em um mamìfero, para inibir o extravasamento de proteìna neuronal em um mamìfero e para tratar ou prevenir enxaqueca em um mamìfero, e, uso de um composto

Country Status (30)

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US (3) US7291632B2 (pt)
EP (1) EP1663971B1 (pt)
JP (1) JP4700614B2 (pt)
KR (1) KR100777875B1 (pt)
CN (1) CN1849307B (pt)
AR (1) AR045619A1 (pt)
AT (1) ATE538093T1 (pt)
AU (1) AU2004280320B2 (pt)
BR (1) BRPI0414241A (pt)
CA (1) CA2537936C (pt)
CR (1) CR8275A (pt)
CY (1) CY1112475T1 (pt)
DK (1) DK1663971T3 (pt)
EA (1) EA011274B1 (pt)
EC (1) ECSP066415A (pt)
ES (1) ES2379665T3 (pt)
IL (1) IL173521A (pt)
MA (1) MA28212A1 (pt)
MX (1) MXPA06002767A (pt)
MY (1) MY144623A (pt)
NO (1) NO20061584L (pt)
NZ (1) NZ545049A (pt)
PE (1) PE20050350A1 (pt)
PL (1) PL1663971T3 (pt)
PT (1) PT1663971E (pt)
SI (1) SI1663971T1 (pt)
TW (1) TWI340740B (pt)
UA (1) UA82711C2 (pt)
WO (1) WO2005035499A1 (pt)
ZA (1) ZA200602072B (pt)

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TWI826514B (zh) 2018-09-04 2023-12-21 美商美國禮來大藥廠 用於預防偏頭痛之拉米迪坦(lasmiditan)長期夜間投藥
TWI776175B (zh) 2019-07-09 2022-09-01 美商美國禮來大藥廠 大規模製備2,4,6-三氟-n-[6-(1-甲基-哌啶-4-羰基)-吡啶-2-基]-苯甲醯胺半琥珀酸鹽的方法及中間體,以及2,4,6-三氟-n-[6-(1-甲基-哌啶-4-羰基)-吡啶-2-基]-苯甲醯胺醋酸鹽之製備
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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
CN114728929A (zh) * 2019-11-22 2022-07-08 广东东阳光药业有限公司 吡啶亚甲基哌啶衍生物及其用途
CN113045540B (zh) * 2019-12-27 2024-02-13 上海天慈国际药业有限公司 一种拉司米地坦的制备方法
WO2026005536A1 (ko) * 2024-06-28 2026-01-02 주식회사 대웅제약 신규한 화합물, 및 이를 포함하는 암 또는 자가 면역 질환의 예방 또는 치료용 약학적 조성물

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