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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China
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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English (en)
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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Publication of CN101068794A publication Critical patent/CN101068794A/zh
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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
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P23/00—Anaesthetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61P25/22—Anxiolytics
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    • A61P25/24—Antidepressants
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • 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
    • C07D401/12—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Psychiatry (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
US60724504P 2004-09-02 2004-09-02
US60703304P 2004-09-02 2004-09-02
US60715004P 2004-09-02 2004-09-02
US60703604P 2004-09-02 2004-09-02
US60703704P 2004-09-02 2004-09-02
US60/607,036 2004-09-02
US60/607,245 2004-09-02
US60/607,037 2004-09-02
US60/607,033 2004-09-02
US60/607,150 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

Family

ID=35517001

Family Applications (1)

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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

Country Status (18)

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

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Publication number Priority date Publication date Assignee Title
RU2413731C2 (ru) 2004-04-09 2011-03-10 Чугаи Сейяку Кабусики Кайся Новые растворимые в воде пролекарства
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
CA2626330A1 (en) * 2005-10-19 2007-04-26 Chugai Seiyaku Kabushiki Kaisha Preventive or therapeutic agents for pancreatic cancer, ovarian cancer, or liver cancer comprising a novel water-solube prodrug
ES2377988T3 (es) 2005-11-14 2012-04-03 Vertex Pharmaceuticals, Inc. Quinazolinas útiles como moduladores de canales iónicos controlados por voltaje
EP1968968A1 (en) * 2005-12-21 2008-09-17 PainCeptor Pharma Corp. Compositions and methods for modulating gated ion channels
EP2043654A2 (en) * 2006-06-12 2009-04-08 Vertex Pharmaceuticals, Inc. Thienopyrimidines useful as modulators of ion channels
CA2707449A1 (en) 2006-12-01 2009-06-12 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
US20090209536A1 (en) * 2007-06-17 2009-08-20 Kalypsys, Inc. Aminoquinazoline cannabinoid receptor modulators for treatment of disease
EP2625169B1 (en) 2010-10-05 2015-03-25 Purdue Pharma L.P. Quinazoline compounds as sodium channel blockers
US20140080810A1 (en) 2010-11-15 2014-03-20 Exelixis, Inc. Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture
WO2012104866A1 (en) 2011-01-31 2012-08-09 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
ES2602140T3 (es) 2011-06-27 2017-02-17 Newron Pharmaceuticals S.P.A. Derivados de arilalquilaminocarboxamida fluorados
EP3438096B1 (en) * 2016-04-01 2020-12-02 Impact Therapeutics, Inc Manufacturing process for 1-(arylmethyl) quinazoline-2,4 (1h, 3h)-dione
CA3071024A1 (en) 2017-08-09 2019-02-14 Denali Therapeutics Inc. Compounds, compositions and methods
CN111201245B (zh) 2017-09-01 2024-04-05 戴纳立制药公司 化合物、组合物和方法
WO2019183589A1 (en) * 2018-03-23 2019-09-26 Denali Therapeutics Inc. Modulators of eukaryotic initiation factor 2
CA3106470A1 (en) * 2018-07-17 2020-01-23 Nippon Chemiphar Co., Ltd. T-type calcium channel blocker
SG11202108552QA (en) 2019-02-13 2021-09-29 Denali Therapeutics Inc Compounds, compositions and methods
EP3924341A4 (en) 2019-02-13 2022-11-02 Denali Therapeutics Inc. Compounds, compositions and methods
US12479830B2 (en) * 2019-10-10 2025-11-25 Esteve Pharmaceuticals, S.A. Homopiperazinyl and homopiperidinyl quinazolin-4(3H)-one derivatives having multimodal activity against pain
CA3164134A1 (en) 2019-12-06 2021-06-10 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofurans as modulators of sodium channels
SI4347031T1 (sl) 2021-06-04 2026-01-30 Vertex Pharmaceuticals Incorporated N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov
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

Citations (2)

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WO2001032632A2 (en) * 1999-11-01 2001-05-10 Eli Lilly And Company Pharmaceutically active 4-substituted pyrimidine derivatives
WO2004078733A1 (en) * 2003-03-03 2004-09-16 Vertex Pharmaceuticals Incorporated Quinazolines useful as modulators of ion channels

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JPH083144A (ja) * 1994-06-21 1996-01-09 Chugai Pharmaceut Co Ltd キナゾリン及びキノリン誘導体
GB9718972D0 (en) * 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
SE0004055D0 (sv) * 2000-11-06 2000-11-06 Astrazeneca Ab N-type calcium channel antagonists for the treatment of pain
SE0004054D0 (sv) * 2000-11-06 2000-11-06 Astrazeneca Ab N-type calcium channel antagonists for the treatment of pain
DE60236322D1 (de) * 2001-12-07 2010-06-17 Vertex Pharma Verbindungen auf pyrimidin-basis als gsk-3-hemmer
ZA200601859B (en) * 2003-08-05 2008-03-26 Vertex Pharma Condensed pyrimidine compounds as inhibitors of voltagegated ion channels
WO2006127329A1 (en) * 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Quinoline derivatives useful as modulators of ion channels

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001032632A2 (en) * 1999-11-01 2001-05-10 Eli Lilly And Company Pharmaceutically active 4-substituted pyrimidine derivatives
WO2004078733A1 (en) * 2003-03-03 2004-09-16 Vertex Pharmaceuticals Incorporated Quinazolines useful as modulators of ion channels

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

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