BRPI0921593B8 - processo para preparar compostos de 4-[2-(2-fluorofenoximetil)fenil]piperidina e compostos relacionados - Google Patents

processo para preparar compostos de 4-[2-(2-fluorofenoximetil)fenil]piperidina e compostos relacionados

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Publication number
BRPI0921593B8
BRPI0921593B8 BRPI0921593A BRPI0921593A BRPI0921593B8 BR PI0921593 B8 BRPI0921593 B8 BR PI0921593B8 BR PI0921593 A BRPI0921593 A BR PI0921593A BR PI0921593 A BRPI0921593 A BR PI0921593A BR PI0921593 B8 BRPI0921593 B8 BR PI0921593B8
Authority
BR
Brazil
Prior art keywords
compounds
preparing
fluorophenoxymethyl
phenyl
piperidine
Prior art date
Application number
BRPI0921593A
Other languages
English (en)
Inventor
Stangeland Eric
Rapta Miroslav
Original Assignee
Theravance Biopharma R&D Ip Llc
Theravance Inc
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 Theravance Biopharma R&D Ip Llc, Theravance Inc filed Critical Theravance Biopharma R&D Ip Llc
Publication of BRPI0921593A2 publication Critical patent/BRPI0921593A2/pt
Publication of BRPI0921593B1 publication Critical patent/BRPI0921593B1/pt
Publication of BRPI0921593B8 publication Critical patent/BRPI0921593B8/pt

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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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4465—Non condensed piperidines, e.g. piperocaine only substituted in position 4
    • 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
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • 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
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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    • C—CHEMISTRY; METALLURGY
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    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/08—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
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    • C07D211/06—Heterocyclic 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
    • C07D211/08—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/08—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32—Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms

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Abstract

processo para preparar compostos de 4 - [2 - (2 - fluorofenoximetil) fenil] piperidina. a invenção se relaciona aos processos e intermediários para preparação de compostos de fórmula (i) onde a, r¹, e r³-6 são como definidos no relatório descritivo, ou um sal dos mesmos. os compostos de fórmula (i) são inibidores da recaptação de serotonina e norepinefrina.
BRPI0921593A 2008-11-14 2009-11-13 processo para preparar compostos de 4-[2-(2-fluorofenoximetil)fenil]piperidina e compostos relacionados BRPI0921593B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11454108P 2008-11-14 2008-11-14
US61/114,541 2008-11-14
PCT/US2009/064304 WO2010056938A1 (en) 2008-11-14 2009-11-13 Process for preparing 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compounds

Publications (3)

Publication Number Publication Date
BRPI0921593A2 BRPI0921593A2 (pt) 2015-08-18
BRPI0921593B1 BRPI0921593B1 (pt) 2021-05-04
BRPI0921593B8 true BRPI0921593B8 (pt) 2021-05-25

Family

ID=41666409

Family Applications (3)

Application Number Title Priority Date Filing Date
BRPI0921595A BRPI0921595B8 (pt) 2008-11-14 2009-11-13 sal monocloridrato cristalino de 4-[2,4,6-(trifluorfenoximetil)fenil]piperidina, seu processo de preparo e usos
BRPI0921596-4A BRPI0921596B1 (pt) 2008-11-14 2009-11-13 Compostos de 4-[2-(2-fluorfenoximetil)fenil]piperidina, composição, método de preparação e uso relacionados
BRPI0921593A BRPI0921593B8 (pt) 2008-11-14 2009-11-13 processo para preparar compostos de 4-[2-(2-fluorofenoximetil)fenil]piperidina e compostos relacionados

Family Applications Before (2)

Application Number Title Priority Date Filing Date
BRPI0921595A BRPI0921595B8 (pt) 2008-11-14 2009-11-13 sal monocloridrato cristalino de 4-[2,4,6-(trifluorfenoximetil)fenil]piperidina, seu processo de preparo e usos
BRPI0921596-4A BRPI0921596B1 (pt) 2008-11-14 2009-11-13 Compostos de 4-[2-(2-fluorfenoximetil)fenil]piperidina, composição, método de preparação e uso relacionados

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US (22) US8304433B2 (pt)
EP (3) EP2358675B9 (pt)
JP (6) JP5529150B2 (pt)
KR (3) KR101685186B1 (pt)
CN (3) CN102209712B (pt)
AR (3) AR074128A1 (pt)
AU (3) AU2009313948B2 (pt)
BR (3) BRPI0921595B8 (pt)
CA (3) CA2739992C (pt)
CL (2) CL2011001088A1 (pt)
CO (2) CO6361988A2 (pt)
CY (3) CY1113622T1 (pt)
DK (3) DK2358675T3 (pt)
ES (3) ES2397247T3 (pt)
HK (3) HK1160449A1 (pt)
HR (3) HRP20120897T1 (pt)
IL (2) IL212230A (pt)
MX (3) MX2011005088A (pt)
MY (2) MY151229A (pt)
NZ (2) NZ592413A (pt)
PL (3) PL2358676T3 (pt)
PT (3) PT2358675E (pt)
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SG (1) SG171311A1 (pt)
SI (3) SI2358675T1 (pt)
SM (3) SMT201200063B (pt)
TW (3) TWI443087B (pt)
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ZA (1) ZA201103495B (pt)

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DK2358675T3 (da) 2008-11-14 2013-01-14 Theravance Inc 4-[2-(2-Fluorphenoxymethyl)phenyl]piperidinforbindelser
EP2523945A1 (en) 2010-01-11 2012-11-21 Theravance, Inc. 1 - (2 - phenoxymethylphenyl) piperazine compounds as serotonin and norepinephrine reuptake inhibitors
WO2011119461A1 (en) * 2010-03-22 2011-09-29 Theravance, Inc. 1-(2-phenoxymethylheteroaryl)piperidine and piperazine compounds
EP2560646B1 (en) * 2010-04-22 2014-12-17 Theravance Biopharma R&D IP, LLC Combination of a serotonin and norepinephrine reuptake inhibitor and an opioid agonist for the treatment of pain
CN103547580B (zh) 2011-03-22 2016-12-07 阿迪维纳斯疗法有限公司 取代的稠合三环化合物、其组合物及医药用途
US9544692B2 (en) * 2012-11-19 2017-01-10 Bitwave Pte Ltd. System and apparatus for boomless-microphone construction for wireless helmet communicator with siren signal detection and classification capability
CN115813923A (zh) * 2016-08-30 2023-03-21 施万生物制药研发Ip有限责任公司 用于治疗神经性起立性低血压的化合物
WO2019232010A1 (en) 2018-06-01 2019-12-05 Theravance Biopharma R&D Ip, Llc PROCESS FOR PREPARING 2-(1-(tert-BUTOXYCARBONYL)PIPERIDINE-4-YL)BENZOIC ACID
TW202345817A (zh) 2022-03-28 2023-12-01 美商施萬生物製藥研發 Ip有限責任公司 治療患有多系統萎縮之個體的方法
CN114957098B (zh) * 2022-06-02 2024-03-29 和鼎（南京）医药技术有限公司 一种制备喷他佐辛中间体的方法

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