CN101500575A - 可用作离子通道调控剂的噻吩并嘧啶 - Google Patents

可用作离子通道调控剂的噻吩并嘧啶 Download PDF

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Publication number
CN101500575A
CN101500575A CNA2007800297622A CN200780029762A CN101500575A CN 101500575 A CN101500575 A CN 101500575A CN A2007800297622 A CNA2007800297622 A CN A2007800297622A CN 200780029762 A CN200780029762 A CN 200780029762A CN 101500575 A CN101500575 A CN 101500575A
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China
Prior art keywords
ring
compound according
pain
optionally substituted
cor
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Pending
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CNA2007800297622A
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English (en)
Chinese (zh)
Inventor
L·T·D·范宁
P·乔希
P·克雷尼特斯基
A·特明
D·威尔逊
张玉连
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Publication of CN101500575A publication Critical patent/CN101500575A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20—Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Surgery (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CNA2007800297622A 2006-06-12 2007-06-12 可用作离子通道调控剂的噻吩并嘧啶 Pending CN101500575A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US81276506P 2006-06-12 2006-06-12
US60/812,765 2006-06-12

Publications (1)

Publication Number Publication Date
CN101500575A true CN101500575A (zh) 2009-08-05

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Country Link
US (1) US8883781B2 (enExample)
EP (1) EP2043654A2 (enExample)
JP (1) JP2009539988A (enExample)
KR (1) KR20090021218A (enExample)
CN (1) CN101500575A (enExample)
AU (1) AU2007258313A1 (enExample)
CA (1) CA2654842A1 (enExample)
IL (1) IL195861A0 (enExample)
MX (1) MX2008015908A (enExample)
NO (1) NO20090157L (enExample)
RU (1) RU2009100159A (enExample)
WO (1) WO2007146284A2 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103328481A (zh) * 2010-09-14 2013-09-25 莱西肯医药有限公司 背板胶质乙酰酯酶的抑制剂及其应用方法
CN103492392A (zh) * 2011-04-01 2014-01-01 森申有限公司 噻吩并[2,3-d]嘧啶衍生物及其用于治疗心律失常的用途

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DE102005003632A1 (de) 2005-01-20 2006-08-17 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Katheter für die transvaskuläre Implantation von Herzklappenprothesen
US8052750B2 (en) 2006-09-19 2011-11-08 Medtronic Ventor Technologies Ltd Valve prosthesis fixation techniques using sandwiching
US7896915B2 (en) 2007-04-13 2011-03-01 Jenavalve Technology, Inc. Medical device for treating a heart valve insufficiency
ES2903231T3 (es) 2008-02-26 2022-03-31 Jenavalve Tech Inc Stent para el posicionamiento y anclaje de una prótesis valvular en un sitio de implantación en el corazón de un paciente
US9044318B2 (en) 2008-02-26 2015-06-02 Jenavalve Technology Gmbh Stent for the positioning and anchoring of a valvular prosthesis
SMT201700456T1 (it) * 2009-07-27 2017-11-15 Gilead Sciences Inc Composti eterociclici fusi come modulatori dei canali ionici
US10856978B2 (en) 2010-05-20 2020-12-08 Jenavalve Technology, Inc. Catheter system
CA2799459A1 (en) 2010-05-25 2011-12-01 Jenavalve Technology Inc. Prosthetic heart valve and transcatheter delivered endoprosthesis comprising a prosthetic heart valve and a stent
JP5858586B2 (ja) 2010-07-02 2016-02-10 ギリアード サイエンシーズ， インコーポレイテッド イオンチャネルモジュレーターとしての縮合複素環式化合物
TWI577670B (zh) 2011-05-10 2017-04-11 基利科學股份有限公司 充當離子通道調節劑之稠合雜環化合物
TWI478908B (zh) 2011-07-01 2015-04-01 Gilead Sciences Inc 作為離子通道調節劑之稠合雜環化合物
NO3175985T3 (enExample) 2011-07-01 2018-04-28
GB201114212D0 (en) * 2011-08-18 2011-10-05 Ucb Pharma Sa Therapeutic agents
AR090037A1 (es) * 2011-11-15 2014-10-15 Xention Ltd Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio
WO2015028209A1 (en) 2013-08-30 2015-03-05 Jenavalve Technology Gmbh Radially collapsible frame for a prosthetic valve and method for manufacturing such a frame
WO2016150806A1 (en) 2015-03-20 2016-09-29 Jenavalve Technology, Inc. Heart valve prosthesis delivery system and method for delivery of heart valve prosthesis with introducer sheath
EP3288495B1 (en) 2015-05-01 2019-09-25 JenaValve Technology, Inc. Device with reduced pacemaker rate in heart valve replacement
US10221191B2 (en) 2015-12-22 2019-03-05 SHY Therapeutics LLC Compounds for the treatment of cancer and inflammatory disease
JP7081749B2 (ja) 2016-05-13 2022-06-07 イエナバルブ テクノロジー インク 心臓弁プロテーゼ送達システム
CN109862893B (zh) * 2016-11-07 2023-02-17 范德比尔特大学 毒蕈碱型乙酰胆碱受体m4的正向别构调节剂
US11008335B2 (en) * 2016-11-07 2021-05-18 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor M4
WO2018138658A1 (en) 2017-01-27 2018-08-02 Jenavalve Technology, Inc. Heart valve mimicry
JP7514005B2 (ja) 2017-06-21 2024-07-10 シャイ・セラピューティクス・エルエルシー がん、炎症性疾患、ラソパシー、及び線維性疾患の治療のためのｒａｓスーパーファミリーと相互作用する化合物
EP3898609A1 (en) 2018-12-19 2021-10-27 Shy Therapeutics LLC Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
WO2024102411A1 (en) 2022-11-09 2024-05-16 Jenavalve Technology, Inc. Catheter system for sequential deployment of an expandable implant

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CA2133815A1 (en) * 1993-10-12 1995-04-13 Jeffrey Alan Dodge Inhibition of phosphatidylinositol 3-kinase with viridin, demethoxyviridin, viridiol, demethoxyviridiol, virone, wortmannolone, and analogs thereof
US6608053B2 (en) * 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
WO2001083456A1 (en) * 2000-04-27 2001-11-08 Yamanouchi Pharmaceutical Co., Ltd. Condensed heteroaryl derivatives
ES2217956B1 (es) 2003-01-23 2006-04-01 Almirall Prodesfarma, S.A. Nuevos derivados de 4-aminotieno(2,3-d)pirimidin-6-carbonitrilo.
CL2004000409A1 (es) * 2003-03-03 2005-01-07 Vertex Pharma Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu
MXPA06000051A (es) * 2003-07-02 2006-03-21 Vertex Pharma Pirimidinas utiles como moduladores de canales ionicos dependientes de voltaje.
EP1663994B1 (en) * 2003-08-05 2012-03-07 Vertex Pharmaceuticals Incorporated Tetrahydroquinazoline compounds as inhibitors of voltage-gated ion channels
CN101068794B (zh) * 2004-09-02 2012-12-19 沃泰克斯药物股份有限公司 可用作离子通道调控剂的喹唑啉
EP1806347A4 (en) * 2004-10-08 2009-07-01 Astellas Pharma Inc PYRIMIDINE DERIVATIVES FUSED WITH AN AROMATIC RING
US7666901B2 (en) * 2004-10-13 2010-02-23 Wyeth Analogs of 17-hydroxywortmannin as PI3K inhibitors
GB0423653D0 (en) * 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103328481A (zh) * 2010-09-14 2013-09-25 莱西肯医药有限公司 背板胶质乙酰酯酶的抑制剂及其应用方法
CN103492392A (zh) * 2011-04-01 2014-01-01 森申有限公司 噻吩并[2,3-d]嘧啶衍生物及其用于治疗心律失常的用途
CN103492392B (zh) * 2011-04-01 2015-11-25 森申有限公司 噻吩并[2,3-d]嘧啶衍生物及其用于治疗心律失常的用途

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JP2009539988A (ja) 2009-11-19
AU2007258313A1 (en) 2007-12-21
US8883781B2 (en) 2014-11-11
CA2654842A1 (en) 2007-12-21
MX2008015908A (es) 2009-01-28
RU2009100159A (ru) 2010-07-20
EP2043654A2 (en) 2009-04-08
NO20090157L (no) 2009-01-12
WO2007146284A3 (en) 2008-04-03
IL195861A0 (en) 2009-09-01
US20070287717A1 (en) 2007-12-13
KR20090021218A (ko) 2009-02-27
WO2007146284A2 (en) 2007-12-21

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