CN101068794B - 可用作离子通道调控剂的喹唑啉 - Google Patents

可用作离子通道调控剂的喹唑啉 Download PDF

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Publication number
CN101068794B
CN101068794B CN2005800374969A CN200580037496A CN101068794B CN 101068794 B CN101068794 B CN 101068794B CN 2005800374969 A CN2005800374969 A CN 2005800374969A CN 200580037496 A CN200580037496 A CN 200580037496A CN 101068794 B CN101068794 B CN 101068794B
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Prior art keywords
pain
compound according
tfa
ring
piperazin
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Expired - Fee Related
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CN2005800374969A
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Chinese (zh)
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CN101068794A (zh
Inventor
D·M·威尔森
A·P·特门
J·E·冈萨雷斯三世
L·T·D·范宁
T·D·纽伯特
P·克任尼特斯奇
P·乔什
D·J·赫雷
U·舍斯
J·S·博格
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D401/14—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 three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Compounds Of Unknown Constitution (AREA)
CN2005800374969A 2004-09-02 2005-08-31 可用作离子通道调控剂的喹唑啉 Expired - Fee Related CN101068794B (zh)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US60703604P 2004-09-02 2004-09-02
US60703304P 2004-09-02 2004-09-02
US60724504P 2004-09-02 2004-09-02
US60715004P 2004-09-02 2004-09-02
US60703704P 2004-09-02 2004-09-02
US60/607,150 2004-09-02
US60/607,033 2004-09-02
US60/607,036 2004-09-02
US60/607,037 2004-09-02
US60/607,245 2004-09-02
PCT/US2005/031146 WO2006028904A1 (en) 2004-09-02 2005-08-31 Quinazolines useful as modulators of ion channels

Publications (2)

Publication Number Publication Date
CN101068794A CN101068794A (zh) 2007-11-07
CN101068794B true CN101068794B (zh) 2012-12-19

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CN2005800374969A Expired - Fee Related CN101068794B (zh) 2004-09-02 2005-08-31 可用作离子通道调控剂的喹唑啉

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EP (1) EP1784393B1 (enExample)
JP (1) JP5014994B2 (enExample)
KR (1) KR20070057914A (enExample)
CN (1) CN101068794B (enExample)
AT (1) ATE435214T1 (enExample)
AU (1) AU2005282761B2 (enExample)
BR (1) BRPI0514893A (enExample)
CA (1) CA2578739A1 (enExample)
DE (1) DE602005015231D1 (enExample)
ES (1) ES2327945T4 (enExample)
IL (1) IL181700A0 (enExample)
MA (1) MA28909B1 (enExample)
MX (1) MX2007002582A (enExample)
NO (1) NO20071742L (enExample)
NZ (1) NZ589252A (enExample)
RU (1) RU2440991C2 (enExample)
WO (1) WO2006028904A1 (enExample)
ZA (1) ZA200702375B (enExample)

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JP4823894B2 (ja) 2004-04-09 2011-11-24 中外製薬株式会社 新規水溶性プロドラッグ
US7928107B2 (en) 2004-09-02 2011-04-19 Vertex Pharmaceuticals Incorporated Quinazolines useful as modulators of ion channels
TW200744603A (en) 2005-08-22 2007-12-16 Chugai Pharmaceutical Co Ltd Novel anticancer concomitant drug
KR20080066039A (ko) * 2005-10-19 2008-07-15 추가이 세이야쿠 가부시키가이샤 신규 수용성 프로드러그를 함유하는 췌장암, 난소암 또는 간암의 예방 또는 치료제
MX2008006303A (es) * 2005-11-14 2009-02-26 Vertex Pharma Quinazolinas de utilidad como moduladores de canales ionicos regulados por voltaje.
AU2006329202A1 (en) * 2005-12-21 2007-06-28 Painceptor Pharma Corporation Compositions and methods for modulating gated ion channels
WO2007146284A2 (en) 2006-06-12 2007-12-21 Vertex Pharmaceuticals Incorporated Thienopyrimidines useful as modulators of ion channels
AU2007328336B2 (en) 2006-12-01 2014-04-17 President And Fellows Of Harvard College Compounds and methods for enzyme-mediated tumor imaging and therapy
WO2008147864A2 (en) * 2007-05-22 2008-12-04 Xenon Pharmaceuticals Inc. Methods of using piperazine compounds in treating sodium channel-mediated diseases or conditions
WO2008157500A1 (en) * 2007-06-17 2008-12-24 Kalypsys, Inc. Aminoquinazoline cannabinoid receptor modulators for treatment of disease
WO2012046132A1 (en) 2010-10-05 2012-04-12 Purdue Pharma L.P. Quinazoline compounds as sodium channel blockers
WO2012068096A2 (en) 2010-11-15 2012-05-24 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
EP2670722B1 (en) 2011-01-31 2016-10-12 Council of Scientific & Industrial Research Chiral 1-(4-methylphenylmethyl)-5-oxo-{n-[(3-t-butoxycarbonyl-aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamides as inhibitors of collagen induced platelet activation and adhesion
HRP20161412T1 (hr) 2011-06-27 2016-12-02 Newron Pharmaceuticals S.P.A. Fluorirani derivati arilalkilaminokarboksamida
PL3438096T3 (pl) * 2016-04-01 2021-05-17 Impact Therapeutics, Inc Sposób wytwarzania 1-(arylometylo)chinazolino-2,4(1H,3H)-dionu
CN111094233B (zh) 2017-08-09 2024-03-15 戴纳立制药公司 化合物、组合物及方法
PT3676297T (pt) 2017-09-01 2023-08-29 Denali Therapeutics Inc Compostos, composições e métodos
US20210130308A1 (en) * 2018-03-23 2021-05-06 Denali Therapeutics Inc. Modulators of eukaryotic initiation factor 2
JPWO2020017569A1 (ja) * 2018-07-17 2021-12-02 日本ケミファ株式会社 Ｔ型カルシウムチャネル阻害剤
CA3129609A1 (en) 2019-02-13 2020-08-20 Denali Therapeutics Inc. Eukaryotic initiation factor 2b modulators
MA54959A (fr) 2019-02-13 2021-12-22 Denali Therapeutics Inc Composés, compositions et procédés
BR112022006692A2 (pt) * 2019-10-10 2022-07-12 Esteve Pharmaceuticals Sa Composto de fórmula geral (i); processo para a preparação de compostos de fórmula (i); uso dos compostos de fórmula iia, iib, iii, iv, v, vi, vii, viia, viii, ix, xii, xiii, xiv, xv, xvi, xvii, xviii ou xix; e composição farmacêutica
PH12022551379A1 (en) 2019-12-06 2023-05-03 Vertex Pharma Substituted tetrahydrofurans as modulators of sodium channels
DK4347031T3 (da) 2021-06-04 2025-12-01 Vertex Pharma N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler
CN119757730A (zh) * 2024-12-24 2025-04-04 浙江省海洋水产研究所 一种河豚毒素的胶体金检测卡

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MXPA04005510A (es) * 2001-12-07 2006-02-24 Vertex Pharma Compuestos basados en pirimidina utiles como inhibidores de gsk-3.
AR045445A1 (es) * 2003-08-05 2005-10-26 Vertex Pharma Compuestos ihinibidores de canales ionicos regulados por voltaje
JP5112297B2 (ja) * 2005-05-20 2013-01-09 バーテックス ファーマシューティカルズ インコーポレイテッド イオンチャネルのモジュレーターとして有用なキノリン誘導体

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WO2004078733A1 (en) * 2003-03-03 2004-09-16 Vertex Pharmaceuticals Incorporated Quinazolines useful as modulators of ion channels

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WO2006028904A1 (en) 2006-03-16
CA2578739A1 (en) 2006-03-16
EP1784393A1 (en) 2007-05-16
WO2006028904A9 (en) 2006-06-22
NZ589252A (en) 2012-06-29
RU2440991C2 (ru) 2012-01-27
CN101068794A (zh) 2007-11-07
IL181700A0 (en) 2007-07-04
DE602005015231D1 (de) 2009-08-13
ATE435214T1 (de) 2009-07-15
AU2005282761B2 (en) 2012-02-02
MA28909B1 (fr) 2007-10-01
BRPI0514893A (pt) 2007-11-27
HK1104544A1 (en) 2008-01-18
RU2007111897A (ru) 2008-10-10
JP2008511670A (ja) 2008-04-17
AU2005282761A1 (en) 2006-03-16
NO20071742L (no) 2007-04-02
EP1784393B1 (en) 2009-07-01
ZA200702375B (en) 2009-03-25
JP5014994B2 (ja) 2012-08-29
ES2327945T4 (es) 2010-07-02
MX2007002582A (es) 2008-01-14
ES2327945T3 (es) 2009-11-05
KR20070057914A (ko) 2007-06-07

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