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MD20140044A2 - 2-Tiopirimidinone şi utilizarea lor pentru tratamentul afecţiunilor cardiovasculare - Google Patents

2-Tiopirimidinone şi utilizarea lor pentru tratamentul afecţiunilor cardiovasculare Download PDF

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Publication number
MD20140044A2
MD20140044A2 MDA20140044A MD20140044A MD20140044A2 MD 20140044 A2 MD20140044 A2 MD 20140044A2 MD A20140044 A MDA20140044 A MD A20140044A MD 20140044 A MD20140044 A MD 20140044A MD 20140044 A2 MD20140044 A2 MD 20140044A2
Authority
MD
Moldova
Prior art keywords
inhibitors
thiopyrimidinones
treatment
cardiovascular diseases
prodrugs
Prior art date
Application number
MDA20140044A
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English (en)
Russian (ru)
Inventor
Филипп Альберт КАПРИНО
Эдвард Ли Конн
Дэвид Хепуорт
Дэниел Вэй-Шун КУН
Бенджамин Нейл РОКИ
Роджер Бенджамин Руггери
Джозеф Скотт ВАРМУС
Янь Чжан
Роберт Ли Дау
Мэтью Скотт ДАУЛИНГ
Суви Туула Марджукка ОРР
Мэтью Форрест САММОНС
Original Assignee
Pfizer Inc.
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Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47356235&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MD20140044(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Inc. filed Critical Pfizer Inc.
Publication of MD20140044A2 publication Critical patent/MD20140044A2/ro

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/56—One oxygen atom and one sulfur atom
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
    • A61K31/37—Coumarins, e.g. psoralen
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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  • Photoreceptors In Electrophotography (AREA)
  • Cephalosporin Compounds (AREA)

Abstract

Prezenta invenţie se referă la compuşi care inhibă mieloperoxidaza, la compoziţii farmaceutice care conţin asemenea inhibitori şi la utilizarea lor pentru tratamentul, de exemplu, al afecţiunilor cardiovasculare, inclusiv al sindromului coronarian acut.În calitate de inhibitori se propun 2-tiopirimidinone cu formula (I), sărurile lor farmaceutic acceptabile sau promedicamentele acestora, în care R1 şi R2 sunt definiţi în descrierea invenţiei:(I).
MDA20140044A 2011-11-11 2012-10-28 2-Tiopirimidinone şi utilizarea lor pentru tratamentul afecţiunilor cardiovasculare MD20140044A2 (ro)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161558605P 2011-11-11 2011-11-11
PCT/IB2012/055949 WO2013068875A1 (en) 2011-11-11 2012-10-28 2-thiopyrimidinones

Publications (1)

Publication Number Publication Date
MD20140044A2 true MD20140044A2 (ro) 2014-08-31

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ID=47356235

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MDA20140044A MD20140044A2 (ro) 2011-11-11 2012-10-28 2-Tiopirimidinone şi utilizarea lor pentru tratamentul afecţiunilor cardiovasculare

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US (4) US8835449B2 (ro)
EP (1) EP2776405A1 (ro)
JP (1) JP5731718B2 (ro)
KR (1) KR101650262B1 (ro)
CN (1) CN103917529B (ro)
AP (1) AP2014007621A0 (ro)
AR (1) AR088805A1 (ro)
AU (1) AU2012335220B2 (ro)
BR (1) BR112014011254A2 (ro)
CA (1) CA2853024C (ro)
CL (1) CL2014000996A1 (ro)
CO (1) CO6960543A2 (ro)
CR (1) CR20140179A (ro)
CU (1) CU20140049A7 (ro)
DO (1) DOP2014000098A (ro)
EA (1) EA027324B1 (ro)
EC (1) ECSP14004595A (ro)
GE (1) GEP201706656B (ro)
GT (1) GT201400090A (ro)
IL (2) IL232425A (ro)
MA (1) MA35638B1 (ro)
MD (1) MD20140044A2 (ro)
MX (1) MX351299B (ro)
NI (1) NI201400042A (ro)
PE (1) PE20161219A1 (ro)
PH (1) PH12014501032A1 (ro)
SG (1) SG11201401531RA (ro)
TN (1) TN2014000195A1 (ro)
TW (2) TWI526433B (ro)
UA (1) UA108713C2 (ro)
UY (1) UY34442A (ro)
WO (1) WO2013068875A1 (ro)
ZA (1) ZA201403589B (ro)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2386555A1 (en) 2010-05-13 2011-11-16 Almirall, S.A. New cyclohexylamine derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities
EP2592078A1 (en) 2011-11-11 2013-05-15 Almirall, S.A. New cyclohexylamine derivatives having beta2 adrenergic agonist and M3 muscarinic antagonist activities
PE20161219A1 (es) 2011-11-11 2016-11-17 Pfizer 2-tiopirimidinonas
EP2934594B1 (en) 2012-12-18 2019-09-04 Almirall, S.A. Cyclohexyl and quinuclidinyl carbamate derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities .
TWI643853B (zh) 2013-02-27 2018-12-11 阿爾米雷爾有限公司 同時具有β2腎上腺素受體促效劑和M3毒蕈鹼受體拮抗劑活性之2-氨基-1-羥乙基-8-羥基喹啉-2(1H)-酮衍生物之鹽類
TW201517906A (zh) 2013-07-25 2015-05-16 Almirall Sa 含有ｍａｂａ化合物和皮質類固醇之組合
TWI641373B (zh) 2013-07-25 2018-11-21 阿爾米雷爾有限公司 具有蕈毒鹼受體拮抗劑和β２腎上腺素受體促效劑二者之活性的２－胺基－１－羥乙基－８－羥基喹啉－２（１Ｈ）－酮衍生物之鹽
TW201617343A (zh) 2014-09-26 2016-05-16 阿爾米雷爾有限公司 具有β２腎上腺素促效劑及Ｍ３蕈毒拮抗劑活性之新穎雙環衍生物
US9616063B2 (en) 2014-12-01 2017-04-11 Astrazeneca Ab 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
BR112017022340A2 (pt) * 2015-05-05 2018-07-10 Pfizer 2-tiopirimidinonas
TW201930315A (zh) 2017-11-02 2019-08-01 德商艾庫瑞斯公司 具抗b型肝炎病毒(hbv)活性之新穎高活性胺基-噻唑取代之吲哚-2-甲醯胺
US11478533B2 (en) 2020-04-27 2022-10-25 Novo Nordisk A/S Semaglutide for use in medicine
UY40399A (es) 2022-08-18 2024-02-15 Astrazeneca Ab Inhibidores de mieloperoxidasa
WO2025172474A1 (en) 2024-02-15 2025-08-21 Astrazeneca Ab Inhibitors of myeloperoxidase

Family Cites Families (165)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4088751A (en) 1972-04-07 1978-05-09 Colgate-Palmolive Company Self-heating cosmetic
US4171429A (en) 1977-03-29 1979-10-16 Research Corporation Pyrimidine to pyrimidine transformation process
EP0028489B1 (en) 1979-11-05 1983-10-05 Beecham Group Plc Enzyme derivatives, and their preparation
JPS5770693A (en) 1980-10-22 1982-05-01 Fuji Photo Film Co Ltd Desensitizing composition
EP0422011A1 (de) 1988-05-05 1991-04-17 BASF Aktiengesellschaft Mittel auf der basis von uracil-derivaten zur wachstumsförderung und fettreduktion bei tieren
KR0155168B1 (ko) 1989-09-29 1998-11-16 미우라 아끼라 6-치환된 아시클로피리미딘 뉴클레오시드 유도체 및 이를 활성성분으로 함유하는 항비루스제
JPH0699170B2 (ja) 1990-01-19 1994-12-07 日東紡績株式会社 耐火被覆材
JPH0525144A (ja) 1991-04-15 1993-02-02 Nissan Chem Ind Ltd ウラシル誘導体及び有害生物防除剤
JPH0525142A (ja) 1991-07-12 1993-02-02 Nissan Chem Ind Ltd ウラシル誘導体及び有害生物防除剤
JPH0543555A (ja) 1991-08-13 1993-02-23 Nissan Chem Ind Ltd ウラシル誘導体及び有害生物防除剤
TW284688B (ro) 1991-11-20 1996-09-01 Takeda Pharm Industry Co Ltd
GB2263639A (en) 1992-01-28 1993-08-04 Merck & Co Inc Substituted pyrimidinones as neurotensin antagonists
JPH063761A (ja) 1992-06-19 1994-01-14 Fuji Photo Film Co Ltd ハロゲン化銀写真感光材料
US6444656B1 (en) 1992-12-23 2002-09-03 Biochem Pharma, Inc. Antiviral phosphonate nucleotides
KR0151811B1 (ko) 1993-12-21 1998-10-15 강박광 신규한 항바이러스성 2,4-피리미딘디온 유도체 및 그의 제조방법
JP3781200B2 (ja) 1994-04-27 2006-05-31 コニカミノルタホールディングス株式会社 ハロゲン化銀写真感光材料の処理方法
JP3261641B2 (ja) 1994-04-28 2002-03-04 コニカ株式会社 ハロゲン化銀写真感光材料の処理方法
US5612359A (en) 1994-08-26 1997-03-18 Bristol-Myers Squibb Company Substituted biphenyl isoxazole sulfonamides
MX9703518A (es) 1994-11-16 1997-08-30 Synaptic Pharma Corp Dihidropirimidinas y usos de las mismas.
US6268369B1 (en) 1994-11-16 2001-07-31 Synaptic Pharmaceutical Corporation 5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
US6228861B1 (en) 1995-11-16 2001-05-08 Synaptic Pharmaceutical Corporation Dihydropyrimidines and uses thereof
WO1997017969A1 (en) 1995-11-16 1997-05-22 Synaptic Pharmaceutical Corporation Dihydropyrimidines and uses thereof
US5719190A (en) 1996-02-28 1998-02-17 Pfizer Inc. Inhibition of myeloperoxidase activity
US6245773B1 (en) 1996-05-16 2001-06-12 Synaptic Pharmaceutical Corporation 5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
CA2253862A1 (en) 1996-05-16 1997-11-20 Wai C. Wong Dihydropyrimidines and uses thereof
US6172066B1 (en) 1996-05-16 2001-01-09 Synaptic Pharmaceutical Corporation Dihydropyrimidines and uses thereof
WO1997041097A2 (en) 1996-12-31 1997-11-06 Dr. Reddy's Research Foundation Novel heterocyclic compounds process for their preparation and pharmaceutical compositions containing them and their use in the treatment of diabetes and related diseases
DE19647380A1 (de) 1996-11-15 1998-05-20 Hoechst Ag 5-Ring-Heterocyclen als Inhibitoren der Leukozytenadhäsion und VLA-4-Antagonisten
WO1998024782A2 (en) 1996-12-05 1998-06-11 Amgen Inc. Substituted pyrimidine compounds and their use
IL130181A0 (en) 1996-12-05 2000-06-01 Amgen Inc Substituted pyrimidone and pyridone compounds and methods of use
US6096753A (en) 1996-12-05 2000-08-01 Amgen Inc. Substituted pyrimidinone and pyridone compounds and methods of use
TW536540B (en) 1997-01-30 2003-06-11 Bristol Myers Squibb Co Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe
DE19731784A1 (de) 1997-07-24 1999-02-04 Bayer Ag Substituierte N-Aryl-N-thioxocarbonyl-sulfonamide
US6211370B1 (en) 1998-01-13 2001-04-03 Harvard University Asymmetric cycloaddition reactions
US6130340A (en) 1998-01-13 2000-10-10 President And Fellows Of Harvard College Asymmetric cycloaddition reactions
AU4084599A (en) 1998-05-18 1999-12-06 Oklahoma Medical Research Foundation Resveratrol inhibition of myeloperoxidase
TR200100149T2 (tr) 1998-07-06 2001-10-22 Bristol-Myers Squibb Company Dual anjiyotensin endotelin alıcı antagonistleri olarak bifenil-sülfonamitler
CA2252144A1 (en) 1998-10-16 2000-04-16 University Of Alberta Dual action anticancer prodrugs
DE19918725A1 (de) 1999-04-24 2000-10-26 Bayer Ag Substituierte N-Cyano-sulfonsäureanilide
CZ20013904A3 (cs) * 1999-05-01 2002-04-17 Smithkline Beecham Plc Pyrimidinonové sloučeniny
WO2000075136A1 (en) 1999-06-02 2000-12-14 Janssen Pharmaceutica N.V. Aminoalkyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
IT1307786B1 (it) * 1999-07-22 2001-11-19 Bracco Spa Analoghi di ceramidi, processo per la loro preparazione e loro usocome antitumorali.
FR2796945B1 (fr) * 1999-07-30 2002-06-28 Sod Conseils Rech Applic Nouveaux derives d'hydantoines, de thiohydantoines, de pyrimidinediones et de thioxopyrimidinones, leurs procedes de preparation et leur application a titre de medicaments
JP2001131133A (ja) 1999-08-23 2001-05-15 Sankyo Co Ltd 新規ミエロペルオキシダーゼ阻害物質およびその製造方法
MY125533A (en) 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
GB2362101A (en) 2000-05-12 2001-11-14 Astrazeneca Ab Treatment of chronic obstructive pulmonary disease
GB0013655D0 (en) 2000-06-05 2000-07-26 Prolifix Ltd Therapeutic compounds
JO2352B1 (en) 2000-06-22 2006-12-12 جانسين فارماسيوتيكا ان. في Compounds for the treatment of non-adaptation of the bottom of the uterus
US6720324B2 (en) 2000-07-05 2004-04-13 Synaptic Pharmaceutical Corporation Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof
AU783403B2 (en) 2000-07-05 2005-10-20 H. Lundbeck A/S Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof
DE60102304T2 (de) 2000-07-14 2005-02-17 Akzo Nobel N.V. Stabilisatorensystem, das hydroxysäuren enthält
DE10034800A1 (de) 2000-07-18 2002-01-31 Bayer Ag Substituierte Benzostickstoffheterocyclen
DE10034803A1 (de) 2000-07-18 2002-01-31 Bayer Ag Substituierte Sulfonsäureanilide
CA2416303A1 (en) 2000-07-31 2002-02-07 Brandeis University Kinetic resolutions of chiral 2- and 3-substituted carboxylic acids
US6562967B2 (en) 2000-07-31 2003-05-13 Brandeis University Kinetic resolutions of chiral 2-and-3-substituted carboxylic acids
WO2003011799A1 (en) 2000-07-31 2003-02-13 Brandeis University Kinetic resolutions of chirat 3- and 3-substituted carboxylic acids
US20030087873A1 (en) 2000-10-18 2003-05-08 Lieven Stuyver Modified nucleosides for the treatment of viral infections and abnormal cellular proliferation
EP2180064A3 (en) 2000-10-18 2010-08-11 Pharmasset, Inc. Multiplex quantification of nucleic acids in diseased cells
DE10108995A1 (de) 2001-02-23 2002-09-05 Abbott Gmbh & Co Kg Substituierte Pyrimidinon-Derivate als Liganden von Integrinrezeptoren
AU2002252183A1 (en) 2001-03-06 2002-09-19 Biocryst Pharmaceuticals, Inc. Nucleosides, preparation thereof and use as inhibitors of rna viral polymerases
WO2002090575A1 (en) 2001-05-08 2002-11-14 Astrazeneca Ab An assay for detecting inhibitors of the enzyme mueloperokidase
WO2003016275A1 (fr) 2001-08-10 2003-02-27 Shionogi & Co., Ltd. Agent antiviral
MXPA04003167A (es) 2001-10-03 2004-07-08 Pharmacia Corp Compuestos heterociclicos insaturados de 6 miembros utiles para la inhibicion selectiva de la cascada de coagulacion.
BR0213129A (pt) 2001-10-03 2004-08-10 Pharmacia Corp Pró-drogas de compostos policìclicos substituìdos, úteis para inibição seletiva da cascata da coagulação
JP2005519866A (ja) 2001-10-03 2005-07-07 ファルマシア・コーポレーション 凝固カスケードの選択阻害に有用な６員複素環式化合物
JP2005525413A (ja) 2001-10-03 2005-08-25 ファルマシア・コーポレーション 凝固カスケードの選択的抑制に有用な置換５員多環状化合物
AU2003205536A1 (en) 2002-01-11 2003-07-24 Statens Serum Institut Anti-retroviral 5,6-disubstituted acyclopyrimidine nucleoside derivatives
IL163659A0 (en) 2002-02-27 2005-12-18 Pfizer Prod Inc Acc inhibitors
US20030232813A1 (en) 2002-04-10 2003-12-18 Orchid Chemicals & Pharmaceuticals Limited Novel amino substituted pyrimidinone derivatives
AR039385A1 (es) 2002-04-19 2005-02-16 Astrazeneca Ab Derivados de tioxantina como inhibidores de la mieloperoxidasa
CA2486090C (en) 2002-05-16 2011-07-05 Bayer Cropscience Gmbh Pyridine carboxamide derivatives and their use as pesticides
EP1394241A1 (en) 2002-08-07 2004-03-03 Rohm And Haas Company Cyclic thioureas as additives for lubricating oils
EP1394242A3 (en) 2002-08-07 2004-04-21 Rohm And Haas Company Cyclic thioureas and their use as additives for lubricating oils
AU2003274652A1 (en) 2002-10-23 2004-05-13 Obetherapy Biotechnology Compounds, compositions and methods for modulating fat metabolism
US20050096319A1 (en) 2003-02-21 2005-05-05 Balzarini Jan M.R. Identification of compounds that inhibit replication of human immunodeficiency virus
HK1079984A1 (zh) 2003-02-21 2006-04-21 Tripep Ab 抑制hiv复制的甘氨酰胺衍生物
WO2004089927A1 (en) 2003-04-07 2004-10-21 Cortical Pty Ltd Novel methods for the treatment of inflammatory diseases
SE0301232D0 (sv) * 2003-04-25 2003-04-25 Astrazeneca Ab Novel use
US7485604B2 (en) 2003-05-27 2009-02-03 Fujifilm Corporation Lubricant composition and method for using and preparing thereof
US7572581B2 (en) 2003-06-30 2009-08-11 Roche Molecular Systems, Inc. 2′-terminator nucleotide-related methods and systems
US7947817B2 (en) 2003-06-30 2011-05-24 Roche Molecular Systems, Inc. Synthesis and compositions of 2'-terminator nucleotides
NZ547907A (en) 2003-12-22 2010-07-30 Gilead Sciences Inc 4'-Substituted carbovir-and abacavir-derivatives as well as related compounds with HIV and HCV antiviral activity
BRPI0418639B8 (pt) 2004-03-15 2021-05-25 Takeda Pharmaceutical compostos inibidores de dipeptidil peptidase, assim como composição farmacêutica contendo os mesmos
WO2005116014A1 (en) 2004-05-12 2005-12-08 Pfizer Products Inc. Proline derivatives and their use as dipeptidyl peptidase iv inhibitors
US7745125B2 (en) 2004-06-28 2010-06-29 Roche Molecular Systems, Inc. 2′-terminator related pyrophosphorolysis activated polymerization
US7928207B2 (en) 2004-06-28 2011-04-19 Roche Molecular Systems, Inc Synthesis and compositions of nucleic acids comprising 2′-terminator nucleotides
EP1616874A1 (en) 2004-07-14 2006-01-18 Universiteit Gent Mono- and bicyclic compounds with therapeutic activity and pharmaceutical compositions including them
US7485729B2 (en) 2004-08-12 2009-02-03 King Industries, Inc. Organometallic compositions and coating compositions
WO2006022899A2 (en) 2004-08-12 2006-03-02 King Industries, Inc. Organometallic compositions and coating compositions
US20060100226A1 (en) 2004-09-10 2006-05-11 Sikorski James A 2-Thiopyrimidinones as therapeutic agents
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006070292A2 (en) 2004-10-12 2006-07-06 Queen's University At Kingston Pyrimidine compounds as anti-ictogenic and/or anti-epileptogenic agents
SE0402591D0 (sv) 2004-10-25 2004-10-25 Astrazeneca Ab Novel use
MY140748A (en) 2004-12-06 2010-01-15 Astrazeneca Ab Novel pyrrolo [3,2-d] pyrimidin-4-one derivatives and their use in therapy
US20060194821A1 (en) 2005-02-18 2006-08-31 The Brigham And Women's Hospital, Inc. Compounds inhibiting the aggregation of superoxide dismutase-1
EP1731911A1 (fr) 2005-06-07 2006-12-13 Institut National De La Sante Et De La Recherche Medicale (Inserm) Procédé utile pour la détection d'encéphalopathies
US7399786B2 (en) 2005-06-30 2008-07-15 Bexel Pharmaceuticals, Inc. Derivatives of amino acids for treatment of obesity and related disorders
US20100105145A1 (en) 2005-07-01 2010-04-29 Dako Denmark A/S Method of simultaneously visualizing multiple biological targets
WO2007023390A2 (en) 2005-07-01 2007-03-01 Dako Denmark A/S Immunohistochemistry detection method
CN101282962A (zh) 2005-08-12 2008-10-08 先灵公司 用于治疗炎性疾病的化合物
CA2630884A1 (en) 2005-11-30 2007-06-07 Vertex Pharmaceuticals Incorporated Inhibitors of c-met and uses thereof
GEP20105033B (en) 2005-12-28 2010-06-25 Takeda Pharmaceuticals Co Therapeutic agent for diabetes
DE102006000649A1 (de) 2006-01-03 2007-07-05 Degussa Gmbh Universell einsetzbare Zusammensetzungen
DE102006000651A1 (de) 2006-01-03 2007-07-12 Degussa Gmbh Präparation aus Ionischen Flüssigkeiten und Harzen
JP5025142B2 (ja) 2006-02-27 2012-09-12 株式会社東芝 モータ制御装置
JP5025144B2 (ja) 2006-02-28 2012-09-12 Ｊｘ日鉱日石エネルギー株式会社 内燃機関用潤滑油組成物
TW200806667A (en) 2006-04-13 2008-02-01 Astrazeneca Ab New compounds
PT2463283E (pt) 2006-04-20 2014-08-27 Pfizer Prod Inc Compostos heterocíclicos de fenil amido condensados para a prevenção e tratamento de doenças mediadas pela glucoquinase
TW200808649A (en) 2006-05-31 2008-02-16 Du Pont Process for purifying perfluorinated products
TW200804383A (en) * 2006-06-05 2008-01-16 Astrazeneca Ab New compounds
EP2029603A1 (en) 2006-06-05 2009-03-04 Astra Zeneca AB Pyrrolo[3,2-d]pyrimidin-4-one derivative as myeloperoxidase inhibitor
EP2048145B9 (en) 2006-08-04 2011-05-04 Toyama Chemical Co., Ltd. Protein kinase c activity enhancer containing alkyl ether derivative or salt thereof
WO2008023249A1 (en) 2006-08-24 2008-02-28 Chemfit Speciality Chemicals (Pty) Ltd Polyvinylchloride composition
US20100055071A1 (en) 2006-11-21 2010-03-04 Martin Robert Leivers Anti-Viral Compounds
ATE552262T1 (de) 2006-11-29 2012-04-15 Pfizer Prod Inc Spiroketone als inhibitoren von acetyl-coa- carboxylase
US20080153697A1 (en) 2006-12-22 2008-06-26 E. I. Dupont De Nemours And Company Mixtures of ammonia and ionic liquids
US8633186B2 (en) 2007-06-08 2014-01-21 Senomyx Inc. Modulation of chemosensory receptors and ligands associated therewith
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
WO2009005693A1 (en) 2007-06-29 2009-01-08 Gilead Sciences, Inc. Novel hiv reverse transcriptase inhibitors
ES2533863T3 (es) 2007-06-29 2015-04-15 Korea Research Institute Of Chemical Technology Inhibidores novedosos de la transcriptasa inversa de VIH
US20090036425A1 (en) 2007-08-02 2009-02-05 Pfizer Inc Substituted bicyclolactam compounds
JP5043555B2 (ja) 2007-08-08 2012-10-10 株式会社カネカ 硬化性組成物
US20090054468A1 (en) 2007-08-23 2009-02-26 Astrazeneca Ab New Use 938
US20090053176A1 (en) 2007-08-23 2009-02-26 Astrazeneca Ab New Combination 937
KR20100095430A (ko) 2007-11-02 2010-08-30 메틸진 인크. 히스톤 탈아세틸화효소의 저해물질
GB0722680D0 (en) 2007-11-19 2007-12-27 Topotarget As Therapeutic compounds and their use
JP2009167179A (ja) 2007-12-21 2009-07-30 Daiichi Sankyo Co Ltd 環状アミン化合物を含有する医薬
EP2268616A1 (en) 2008-03-21 2011-01-05 Chlorion Pharma, Inc. Substituted pyrrolidine and piperidine compounds, derivatives thereof, and methods for treating pain
WO2009120872A2 (en) 2008-03-26 2009-10-01 Ada Technologies, Inc. High performance batteries with carbon nanomaterials and ionic liquids
EP3042660A3 (en) 2008-04-15 2016-10-26 RFS Pharma, LLC. Nucleoside derivatives for treatment of caliciviridae infections, including norovirus infections
WO2009137508A1 (en) 2008-05-05 2009-11-12 Ada Technologies, Inc. High performance carbon nanocomposites for ultracapacitors
JP5435592B2 (ja) 2008-05-28 2014-03-05 ファイザー・インク ピラゾロスピロケトンアセチルＣｏＡカルボキシラーゼ阻害剤
US20110009443A1 (en) 2008-05-28 2011-01-13 Kevin Daniel Freeman-Cook Pyrazolospiroketone Acetyl-Coa Carboxylase Inhibitors
US20110130365A1 (en) 2008-07-29 2011-06-02 Benbow John W Fluorinated Heteroaryls
WO2010023594A1 (en) 2008-08-28 2010-03-04 Pfizer Inc. Dioxa-bicyclo[3.2.1.]octane-2,3,4-triol derivatives
GB0818063D0 (en) * 2008-10-02 2008-11-05 Univ Dundee Compounds
JP5206367B2 (ja) 2008-11-27 2013-06-12 コニカミノルタエムジー株式会社 ウレア化合物を含む有機圧電材料
WO2010086820A1 (en) 2009-02-02 2010-08-05 Pfizer Inc. 4-amino-5-oxo-7, 8-dihydropyrimido [5,4-f] [1,4] oxazepin-6 (5h) -yl) phenyl derivatives, pharmaceutical compositions and uses thereof
US20110319379A1 (en) 2009-03-11 2011-12-29 Corbett Jeffrey W Substituted Indazole Amides And Their Use As Glucokinase Activators
DK2406253T3 (da) 2009-03-11 2013-08-12 Pfizer Benzofuranylderivater anvendt som glucokinase-inhibitorer
JP2012520868A (ja) 2009-03-20 2012-09-10 ファイザー・インク ３−オキサ−７−アザビシクロ［３．３．１］ノナン
US20120129818A1 (en) 2009-04-23 2012-05-24 Desikan Rajagopal Compositions and Methods for Treatment of Cardiovascular Disease
US20100272783A1 (en) 2009-04-24 2010-10-28 Novabay Pharmaceuticals, Inc. Methods of Treating Infections of the Nail
WO2010128414A1 (en) 2009-05-08 2010-11-11 Pfizer Inc. Gpr 119 modulators
CA2759843A1 (en) 2009-05-08 2010-11-10 Pfizer Inc. Gpr 119 modulators
JP2012528120A (ja) 2009-05-27 2012-11-12 ユニヴェルシテ リブル ドゥ ブリュッセル ミエロペルオキシダーゼ阻害３−アルキル−５−フルオロインドール誘導体
WO2010138901A1 (en) 2009-05-29 2010-12-02 Biogen Idec Ma Inc Carboxylic acid-containing compounds, derivatives thereof, and related methods of use
SG175995A1 (en) 2009-06-05 2011-12-29 Pfizer L- ( piperidin-4-yl) -pyrazole derivatives as gpr 119 modulators
JP5732453B2 (ja) 2009-06-25 2015-06-10 アルカーメス ファーマ アイルランド リミテッド Ｎｈ酸性化合物のプロドラッグ
US8431576B2 (en) 2009-06-25 2013-04-30 Alkermes Pharma Ireland Limited Heterocyclic compounds for the treatment of neurological and psychological disorders
WO2011003018A2 (en) 2009-07-01 2011-01-06 Cornell University Halogenated 2-deoxy-lactones, 2'-deoxy--nucleosides, and derivatives thereof
WO2011005611A1 (en) 2009-07-09 2011-01-13 Merck Sharp & Dohme Corp. Neuromedin u receptor agonists and uses thereof
DE102009037300A1 (de) 2009-08-14 2011-02-17 Merck Patent Gmbh Tetracyanoborate als Schmierstoffe
EP2501696B1 (en) 2009-10-15 2016-12-28 Guerbet Imaging agents and their use for the diagnostic in vivo of neurodegenerative diseases, notably alzheimer's disease and derivative diseases
WO2011057220A2 (en) 2009-11-09 2011-05-12 Northwestern University Compositions and methods for treating lymphoma
FR2953145B1 (fr) 2009-11-30 2013-07-19 Inst Francais Du Petrole Solution absorbante contenant un inhibiteur de degradation derive de la pyrimidine ou de la triazine et procede d'absorption de composes acides contenus dans un effluent gazeux
WO2011094890A1 (en) 2010-02-02 2011-08-11 Argusina Inc. Phenylalanine derivatives and their use as non-peptide glp-1 receptor modulators
US20130085133A1 (en) 2010-02-08 2013-04-04 Sourthern Research Institute Office of Commercialization and Intellectual Prop. Anti-viral treatment and assay to screenfor anti-viral agent
JP5816635B2 (ja) 2010-03-05 2015-11-18 カリオファーム セラピューティクス，インコーポレイテッド 核輸送調節剤およびその使用
US8592427B2 (en) 2010-06-24 2013-11-26 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
WO2012016133A2 (en) 2010-07-29 2012-02-02 President And Fellows Of Harvard College Ros1 kinase inhibitors for the treatment of glioblastoma and other p53-deficient cancers
ES2352926B1 (es) 2010-12-07 2012-01-12 Universidad De Granada Fenucil deuterado y derivados, procedimiento para su preparación y usos de los mismos.
PE20161219A1 (es) 2011-11-11 2016-11-17 Pfizer 2-tiopirimidinonas
JP6003761B2 (ja) 2013-03-27 2016-10-05 富士ゼロックス株式会社 送風管、送風装置及び画像形成装置
BR112017022340A2 (pt) * 2015-05-05 2018-07-10 Pfizer 2-tiopirimidinonas

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US8835449B2 (en) 2014-09-16
TW201518281A (zh) 2015-05-16
EA027324B1 (ru) 2017-07-31
EA201490688A1 (ru) 2014-10-30
TWI480269B (zh) 2015-04-11
IL232425A (en) 2016-11-30
ZA201403589B (en) 2015-06-24
TN2014000195A1 (fr) 2015-09-30
KR101650262B1 (ko) 2016-08-22
IL249039A0 (en) 2017-01-31
AP2014007621A0 (en) 2014-05-31
PH12014501032A1 (en) 2014-10-20
DOP2014000098A (es) 2014-07-31
JP2014533261A (ja) 2014-12-11
US20130296351A1 (en) 2013-11-07
CN103917529A (zh) 2014-07-09
US9873673B2 (en) 2018-01-23
CN103917529B (zh) 2016-08-17
TW201332979A (zh) 2013-08-16
MX2014005721A (es) 2014-05-28
AU2012335220B2 (en) 2017-06-01
TWI526433B (zh) 2016-03-21
AU2012335220A1 (en) 2014-05-01
MX351299B (es) 2017-10-10
NI201400042A (es) 2014-10-01
HK1196603A1 (zh) 2014-12-19
ECSP14004595A (es) 2015-11-30
JP5731718B2 (ja) 2015-06-10
CU20140049A7 (es) 2014-08-28
US20160304469A1 (en) 2016-10-20
IL232425A0 (en) 2014-06-30
NZ624453A (en) 2015-12-24
CL2014000996A1 (es) 2014-07-04
IL249039B (en) 2018-07-31
MA35638B1 (fr) 2014-11-01
PE20161219A1 (es) 2016-11-17
UA108713C2 (xx) 2015-05-25
US20130123230A1 (en) 2013-05-16
WO2013068875A1 (en) 2013-05-16
SG11201401531RA (en) 2014-07-30

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