DK2346837T3 - Fremgangsmåder til fremstilling af quinazolinonderivater - Google Patents
Fremgangsmåder til fremstilling af quinazolinonderivater Download PDFInfo
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- DK2346837T3 DK2346837T3 DK09770937.2T DK09770937T DK2346837T3 DK 2346837 T3 DK2346837 T3 DK 2346837T3 DK 09770937 T DK09770937 T DK 09770937T DK 2346837 T3 DK2346837 T3 DK 2346837T3
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- DK
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- Prior art keywords
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- compound
- hydroxyethoxy
- dimethylphenyl
- halogen
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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
- C07D239/70—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
- C07D239/88—Oxygen atoms
- C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
-
- 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
- A61P9/10—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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- Urology & Nephrology (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Heart & Thoracic Surgery (AREA)
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- Plural Heterocyclic Compounds (AREA)
Claims (15)
1. Fremgangsmåde til fremstilling afen forbindelse med formlen I:
Formel I og solvater, hydrater, tautomere og farmaceutisk acceptable salte deraf, hvori: R-ι, R2, R3 og R4 indbyrdes uafhængigt er valgt blandt alkoxy, alkyl, amido, aryloxy, cycloalkyl, halogen, heterocyclyl, hydrogen og nitro; R6 er valgt blandt alkyl, alkoxy og halogen; R5 er hydrogen, eller R5 og R6 sammen med de carbonatomer, til hvilke de er bundet, kan danne en ring valgt blandt aryl, cycloalkyl og heterocyclyl; R8 er valgt blandt alkyl, alkoxy og halogen; W er C eller N, idet p er 0, når W er N, og p er 1, når W er C; omfattende a) omsætning af et aldehyd med formlen II:
Formel II hvori R5, R6 og R8 er defineret som ovenfor, med ethylencarbonat til dannelse af en forbindelse med formlen III:
Formel III og b) omsætning af forbindelsen med formlen III med en forbindelse med formlen IV:
Formel IV hvori Ri, R2, R3 og R4 er defineret som ovenfor, til fremstilling af forbindelsen med formlen I.
2. Fremgangsmåde ifølge krav 1, hvori R6 og R8 indbyrdes uafhængigt er valgt blandt alkyl og halogen; fortrinsvis hvori R6 og R8 hver især er methyl.
3. Fremgangsmåde ifølge krav 1 eller krav 2, hvori R1 og R3 indbyrdes uafhængigt er valgt blandt alkoxy, alkyl, halogen og hydrogen; fortrinsvis hvori og R3 hver især er methoxy.
4. Fremgangsmåde ifølge krav 1, hvori forbindelsen med formlen I er valgt blandt: 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)quinazolin-4(3H)-on; 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-on; 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-6,7-dimethoxyquinazolin-4(3H)-on; 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxypyrido[2,3-d]pyrimidin-4(3H)-on; N-(2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-4-oxo-3,4-dihydroquinazolin-6- yl)acetamid; 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethylquinazolin-4(3H)-on; 5,7-dichlor-2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)quinazolin-4(3H)-on; 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-6-methoxyquinazolin-4(3H)-on; 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5-methoxyquinazolin-4(3H)-on; og 6-brom-2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)quinazolin-4(3H)-on, og solvater, hydrater, tautomere og farmaceutisk acceptable salte deraf; fortrinsvis hvori forbindelsen med formlen I er 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-on, eller et solvat, et hydrat, en tautomer eller et farmaceutisk acceptabelt salt deraf.
5. Fremgangsmåde ifølge et hvilket som helst af kravene 1 til 4, som endvidere omfatter omsætning af forbindelsen med formlen I med en forbindelse med formlen V:
Formel V hvori R9 er valgt blandt alkyl, aryl, cycloalkyl, heteroaryl og heterocyclyl, til fremstilling af en forbindelse med formlen VI:
Formula VI og solvater, hydrater, tautomere og farmaceutisk acceptable salte deraf, hvori R2, R3, R4, R5, R6, Re og R9 er defineret som ovenfor.
6. Fremgangsmåde ifølge krav 5, hvori R9 er aryl substitueret med én eller flere grupper valgt blandt alkoxy, alkyl og halogen.
7. Fremgangsmåde ifølge et hvilket som helst af kravene 1 til 4, som endvidere omfatter c) omsætning af en forbindelse med formlen I med et reagens til at skabe en fraspaltelig gruppe R10 til dannelse af en forbindelse med formlen VII:
_ Formel VII _ hvori R10 er valgt blandt halogen, sulfonyl og phosphonium; Ri, R2, R3, R4, R5, R6 og R8 er defineret som ovenfor; og d) omsætning af forbindelsen med formlen VII med et nukleofilt reagens til dannelse af en forbindelse med formlen VIII:
Formel VIII og solvater, hydrater, tautomere og farmaceutisk acceptable salte deraf, hvori Ru er valgt blandt alkoxy, amido, amino, imido og heterocyclyl; og R^ R2, R3, R4, R5, R6 og R8 er defineret som ovenfor.
8. Fremgangsmåde ifølge krav 7, ved hvilken a) det reagens, der skaber den fraspaltelige gruppe, er valgt blandt thionylchlorid, methansulfonylchlorid, p-toluensulfonylchlorid og PPIVdiethylazodicarboxylat; og/eller b) R10 er valgt blandt chlorid, methansulfonyl, p-toluensulfonyl og triphenyl-phosphonium.
9. Fremgangsmåde ifølge krav 7 eller krav 8, ved hvilken a) det nukleofile reagens er valgt blandt et alkanolat, en amin, et azid og en heteroring med mindst ét nitrogenatom; og/eller b) Ru er valgt blandt methoxy, methylamino, morpholino, piperazino og piperidino.
10. Fremgangsmåde ifølge et hvilket som helst af kravene 7 til 9, hvori forbindelsen med formlen VIII er 2-(3,5-dimethyl-4-(2-(methylamino)ethoxy)phenyl)-5,7-dimethoxy-quinazolin-4(3H)-on eller et solvat, et hydrat, en tautomer eller et farmaceutisk acceptabelt salt deraf.
11. Fremgangsmåde til fremstilling af en forbindelse med formlen VIII:
Formel VIII og solvater, hydrater, tautomere og farmaceutisk acceptable salte deraf, hvori: Ri, R2, R3 og R4 indbyrdes uafhængigt er valgt blandt alkoxy, alkyl, amido, aryloxy, cycloalkyl, halogen, heterocyclyl, hydrogen og nitro; R6 er valgt blandt alkyl, alkoxy og halogen; R5 er hydrogen, eller R5 og R6 sammen med de carbonatomer, til hvilke de er bundet, kan danne en ring valgt blandt aryl, cycloalkyl og heterocyclyl; R8 er valgt blandt alkoxy, alkyl og halogen; R11 er valgt blandt alkoxy, amido, amino, imido og heterocyclyl; W er C eller N, idet p er 0, når W er N, og p er 1, når W er C; omfattende a) omsætning af et aldehyd med formlen II:
Formel II hvori R5, R6 og R8 er defineret som ovenfor, med ethylencarbonat til dannelse af en forbindelse med formlen III:
Formel III b) omsætning af forbindelsen med formlen III med et reagens til at skabe en fraspaltelig gruppe R12 til dannelse af en forbindelse med formlen IX:
Formel IX hvori R12 er valgt blandt halogen, sulfonyl og phosphonium; c) omsætning af forbindelsen med formlen VIII med et nukleofilt reagens til dannelse af en forbindelse med formlen X:
Formel X hvori R13 er valgt blandt alkoxy, amido, amino, imido og heterocyclyl; og d) omsætning af forbindelsen med formlen X med en forbindelse med formlen IV:
hvori R^ R2, R3 og R4 er defineret som ovenfor, til dannelse af forbindelsen med formlen VIII.
12. Fremgangsmåde ifølge krav 11, ved hvilken a) det reagens, der skaber den fraspaltelige gruppe, er valgt blandt thionylchlorid, methansulfonylchlorid, p-toluensulfonylchlorid og PPh3/diethylazodicarboxylat; og/eller b) R12 er valgt blandt chlorid, methansulfonyl, p-toluensulfonyl og triphenyl-phosphonium.
13. Fremgangsmåde ifølge krav 11 eller krav 12, ved hvilken a) det nukleofile reagens er valgt blandt et alkanolat, en amin, et azid og en heteroring med mindst ét nitrogenatom; og/eller b) R13 er valgt blandt methoxy, methylamino, morpholino, piperazino og piperidino.
14. Fremgangsmåde ifølge et hvilket som helst af kravene 11 til 13, ved hvilken R6 og Re hver især er methyl; og/eller R1 og R3 hver især er hydrogen.
15. Fremgangsmåde ifølge et hvilket som helst af kravene 11 til 14, ved hvilken forbindelsen med formlen VIII er 2-(3,5-dimethyl-4-(2-morpholinoethoxy)phenyl)-quinazolin-4(3H)-on eller et solvat, et hydrat, en tautomer, eller et farmaceutisk acceptabelt salt deraf.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7595208P | 2008-06-26 | 2008-06-26 | |
| PCT/US2009/048457 WO2009158404A1 (en) | 2008-06-26 | 2009-06-24 | Methods of preparing quinazolinone derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2346837T3 true DK2346837T3 (da) | 2015-04-20 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK09770937.2T DK2346837T3 (da) | 2008-06-26 | 2009-06-24 | Fremgangsmåder til fremstilling af quinazolinonderivater |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US8114995B2 (da) |
| EP (1) | EP2346837B8 (da) |
| JP (1) | JP5602728B2 (da) |
| KR (1) | KR101629356B1 (da) |
| CN (1) | CN101970416B (da) |
| AU (1) | AU2009262252B2 (da) |
| CA (1) | CA2711103C (da) |
| CY (1) | CY1116260T1 (da) |
| DK (1) | DK2346837T3 (da) |
| ES (1) | ES2532402T3 (da) |
| HK (1) | HK1160135A1 (da) |
| HR (1) | HRP20150477T8 (da) |
| IL (1) | IL206544A (da) |
| NZ (1) | NZ586440A (da) |
| PL (1) | PL2346837T3 (da) |
| PT (1) | PT2346837E (da) |
| RU (1) | RU2520098C2 (da) |
| SI (1) | SI2346837T1 (da) |
| WO (1) | WO2009158404A1 (da) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2584507C (en) * | 2004-10-20 | 2016-04-26 | Resverlogix Corp. | Flavanoids and isoflavanoids for the prevention and treatment of cardiovascular diseases |
| US8410109B2 (en) * | 2005-07-29 | 2013-04-02 | Resverlogix Corp. | Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices |
| NZ579355A (en) | 2007-02-01 | 2012-03-30 | Resverlogix Corp | 2-(Aryl)-4-oxo-quinazoline derivatives |
| ES2463097T3 (es) | 2009-01-08 | 2014-05-27 | Resverlogix Corp. | Compuestos para la prevención y el tratamiento de enfermedades cardiovasculares |
| CA2992231C (en) | 2009-03-18 | 2022-03-29 | Resverlogix Corp. | Phenyl-quinazolin-4(3h)-one and phenyl-pyrido[2,3-d]pyrimidin-4(3h)-one derivatives and compositions thereof useful as anti-inflammatory agents |
| PL2421533T3 (pl) | 2009-04-22 | 2019-05-31 | Resverlogix Corp | Nowe środki przeciwzapalne |
| AU2011298423B2 (en) | 2010-09-03 | 2015-11-05 | Bayer Intellectual Property Gmbh | Substituted fused pyrimidinones and dihydropyrimidinones |
| EP2714639A1 (en) * | 2011-05-26 | 2014-04-09 | Solvay Specialty Polymers Italy S.p.A. | Hydro-fluorocompounds |
| WO2013033268A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bivalent bromodomain ligands, and methods of using same |
| WO2013033269A1 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same |
| KR102011641B1 (ko) | 2011-11-01 | 2019-08-19 | 리스버로직스 코퍼레이션 | 치환된 퀴나졸리논을 위한 경구 즉시 방출 제형 |
| PL2906531T3 (pl) | 2012-10-15 | 2018-04-30 | Resverlogix Corp. | Związki użyteczne w syntezie związków benzamidowych |
| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| EP2935253B1 (en) | 2012-12-21 | 2018-08-01 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| AU2014249192B2 (en) | 2013-03-11 | 2017-12-21 | The Regents Of The University Of Michigan | BET bromodomain inhibitors and therapeutic methods using the same |
| CN103570632B (zh) * | 2013-07-22 | 2015-09-30 | 成都理工大学 | 无催化剂的4(3h)-喹唑啉酮的合成方法 |
| CN103613550A (zh) * | 2013-11-29 | 2014-03-05 | 成都理工大学 | 4(3h)-喹唑啉酮的绿色合成方法 |
| CN107074861A (zh) | 2014-02-28 | 2017-08-18 | 密执安大学评议会 | 作为bet溴结构域抑制剂的9h嘧啶并[4，5‑b]吲哚和相关类似物 |
| WO2016138332A1 (en) | 2015-02-27 | 2016-09-01 | The Regents Of The University Of Michigan | 9h-pyrimido [4,5-b] indoles as bet bromodomain inhibitors |
| JP6903585B2 (ja) | 2015-03-13 | 2021-07-14 | レスバーロジックス コーポレイション | 補体関連疾患の治療のための組成物および治療方法 |
| WO2016196065A1 (en) | 2015-05-29 | 2016-12-08 | Genentech, Inc. | Methods and compositions for assessing responsiveness of cancers to bet inhibitors |
| CN108349911B (zh) | 2015-09-07 | 2022-05-13 | 浙江华海药业股份有限公司 | 可释放一氧化氮的前药分子 |
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| JP7001614B2 (ja) | 2016-04-06 | 2022-02-03 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | リガンド依存性の標的タンパク質分解のための単官能性中間体 |
| US11192898B2 (en) | 2016-04-06 | 2021-12-07 | The Regents Of The University Of Michigan | MDM2 protein degraders |
| EP3442976B1 (en) | 2016-04-12 | 2022-07-20 | The Regents of The University of Michigan | Bet protein degraders |
| EP3490579A1 (en) | 2016-07-27 | 2019-06-05 | Hartis-Pharma SA | Therapeutic combinations to treat red blood cell disorders |
| JP7035027B2 (ja) | 2016-09-13 | 2022-03-14 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｂｅｔタンパク質分解物質としての縮合１，４－ジアゼピン |
| CN110062759B (zh) | 2016-09-13 | 2022-05-24 | 密执安大学评议会 | 作为bet蛋白降解剂的稠合的1,4-氧氮杂䓬 |
| EP3309154A1 (en) * | 2016-10-13 | 2018-04-18 | Universite De Geneve | New compounds and uses thereof for detection of target molecules in a sample |
| CN110049981A (zh) * | 2016-12-09 | 2019-07-23 | 苏州科睿思制药有限公司 | 一种溴结构域蛋白抑制剂药物的晶型及其制备方法和用途 |
| US11046709B2 (en) | 2017-02-03 | 2021-06-29 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as BET bromodomain inhibitors |
| US11267822B2 (en) | 2017-09-13 | 2022-03-08 | The Regents Of The University Of Michigan | BET bromodomain protein degraders with cleavable linkers |
| CA3102178A1 (en) | 2018-06-13 | 2019-12-19 | Dybly Ag | Preparation of condensed triazepine derivatives and their use as bet inhibitors |
| CN112424200B (zh) | 2018-07-25 | 2022-09-20 | 正大天晴药业集团股份有限公司 | 作为溴区结构域蛋白抑制剂的亚氨基砜类化合物、药物组合物及其医药用途 |
| CN109897009B (zh) * | 2019-03-15 | 2022-06-28 | 深圳晶泰科技有限公司 | 一种Apabetalone水合物晶型及其制备方法 |
| CN115710202B (zh) * | 2021-08-23 | 2024-05-03 | 江西同和药业股份有限公司 | 一种阿帕他酮关键中间体的制备方法及其应用 |
Family Cites Families (187)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2065593A (en) | 1936-12-29 | Water-soluble diazoimino com | ||
| FR472489A (fr) | 1914-02-20 | 1914-12-08 | Stas Motor Ges M B H | Bague de garniture métallique pour pistons |
| FR803619A (fr) | 1935-03-23 | 1936-10-05 | Ig Farbenindustrie Ag | Acide du type dihydroxystilbène-dicarboxylique et son procédé de préparation |
| US2065900A (en) | 1935-03-23 | 1936-12-29 | Gen Aniline Works Inc | Dihydroxystilbene-dicarboxylic acid and a process of preparing it |
| DE637259C (de) | 1935-03-24 | 1936-10-27 | I G Farbenindustrie Akt Ges | Verfahren zur Darstellung einer Dioxystilbendicarbonsaeure |
| FR803201A (fr) | 1935-07-08 | 1936-09-25 | Ste Ind Chim Bale | Préparation d'acides sulfoniques |
| US2071329A (en) | 1935-08-22 | 1937-02-23 | Solvay Process Co | Method of recovering phthalic anhydride |
| DE652772C (de) | 1935-11-07 | 1937-11-08 | I G Farbenindustrie Akt Ges | Verfahren zur Herstellung von N-Dihydroazinen der Anthrachinonreihe |
| GB728767A (en) | 1951-10-12 | 1955-04-27 | Wander Ag Dr A | 2-substituted chromone compounds, and a method of making same |
| US3251837A (en) | 1962-09-14 | 1966-05-17 | Pfizer & Co C | Derivatives of 1, 2, 4-benzothiadiazine-1, 1-dioxides |
| GB1179019A (en) | 1967-05-23 | 1970-01-28 | Produits Chimique Soc Et | Polynicotinic Esters of Flavonoids |
| FR6928M (da) | 1967-11-24 | 1969-05-05 | ||
| US3600394A (en) | 1968-05-17 | 1971-08-17 | Searle & Co | 2-aminoalkyl-3-arylisocarbostyrils |
| US3773946A (en) | 1969-09-02 | 1973-11-20 | Parke Davis & Co | Triglyceride-lowering compositions and methods |
| US3930024A (en) | 1969-09-02 | 1975-12-30 | Parke Davis & Co | Pharmaceutical compositions and methods |
| FR2244493A1 (en) | 1973-08-09 | 1975-04-18 | Pluripharm | Flavonoid amino-acid salts - for treatment of haemorrhage, circulatory disorders and atherosclerosis |
| DE2349024A1 (de) | 1973-09-26 | 1975-04-10 | Schering Ag | 6beta,7beta-epoxy-1alpha,2alphamethylen-d-homo-4-pregnen-3,20-dione |
| US5098903A (en) * | 1980-03-07 | 1992-03-24 | Board Of Regents Of The University Of Oklahoma | Diphenylcyclopropyl analogs as antiestrogenic and antitumor agents |
| IL64542A0 (en) | 1981-12-15 | 1982-03-31 | Yissum Res Dev Co | Long-chain alpha,omega-dicarboxylic acids and derivatives thereof and pharmaceutical compositions containing them |
| JPS60136512A (ja) | 1983-12-26 | 1985-07-20 | Eisai Co Ltd | 脂質代謝改善剤 |
| DE3423166A1 (de) | 1984-06-22 | 1986-01-02 | Epis S.A., Zug | Alpha-, omega-dicarbonsaeuren, verfahren zu ihrer herstellung und arzneimittel, die diese verbindungen enthalten |
| CA1281720C (en) | 1984-11-08 | 1991-03-19 | Makoto Sunagawa | Carbapenem compounds and production thereof |
| DE3515882A1 (de) | 1985-05-03 | 1986-11-06 | Dr. Karl Thomae Gmbh, 7950 Biberach | Arzneimittel, enthaltend pyridinone mit antithrombotischen wirkungen und verfahren zu ihrer herstellung |
| DE3601417A1 (de) | 1986-01-20 | 1987-07-23 | Nattermann A & Cie | 2'-alkyl-(alkenyl-) substituierte quercetine |
| DE3774801D1 (de) | 1986-08-29 | 1992-01-09 | Ciba Geigy Ag | Verfahren zur herstellung von aromatischen ether- und thioetherverbindungen. |
| ES2053508T3 (es) | 1986-11-24 | 1994-08-01 | Fujisawa Pharmaceutical Co | Compuestos de acidos 3-pirrolidinil-tio-1-azabiciclo(3.2.0)hept-2-eno-2-carboxilicos. |
| GB8804058D0 (en) | 1988-02-22 | 1988-03-23 | Fujisawa Pharmaceutical Co | 3-alkenyl-1-azabicyclo(3 2 0)hept-2-ene-2-carboxylic acid compounds |
| US4925838A (en) | 1988-03-18 | 1990-05-15 | Fujisawa Pharmaceutical Company, Ltd. | 3-pyrrolidinylthio-1-azabicyclo[3.2.0]-hept-2-ene-2-carboxylic acid compounds |
| US4963544A (en) | 1988-05-23 | 1990-10-16 | Fujisawa Pharmaceutical Company, Ltd. | 3-pyrrolidinylthio-1-azabicyclo[3.2.0]-hept-2-ene-2-carboxylic acid compounds |
| GB8926981D0 (en) | 1988-12-23 | 1990-01-17 | Ici Plc | Heterocyclic derivatives |
| KR920701167A (ko) | 1989-07-07 | 1992-08-11 | 에릭 에스. 딕커 | 약제학적 활성 화합물 |
| IE64358B1 (en) | 1989-07-18 | 1995-07-26 | Ici Plc | Diaryl ether heterocycles |
| GB9018134D0 (en) | 1989-09-29 | 1990-10-03 | Ici Plc | Heterocyclic derivatives |
| KR950002885B1 (ko) | 1990-06-05 | 1995-03-28 | 토레이가부시키가이샤 | 인돌 유도체 |
| JP2999579B2 (ja) | 1990-07-18 | 2000-01-17 | 武田薬品工業株式会社 | Ｄｎａおよびその用途 |
| GB9025832D0 (en) | 1990-11-28 | 1991-01-09 | Ashwell Geoffrey J | Novel films for nonlinear optical applications |
| IE913866A1 (en) | 1990-11-28 | 1992-06-03 | Ici Plc | Aryl derivatives |
| US5141970A (en) * | 1990-12-10 | 1992-08-25 | Loctite (Ireland) Limited | Method of forming high-temperature resistant polymers |
| US5126351A (en) | 1991-01-24 | 1992-06-30 | Glaxo Inc. | Antitumor compounds |
| MX9200299A (es) | 1991-02-07 | 1992-12-01 | Roussel Uclaf | Nuevos derivados biciclicos nitrogenados, su procedimiento de preparacion los nuevos compuestos intermedios obtenidos su aplicacion como medicamentos y las composiciones farmaceuticas que los contienen. |
| WO1992018123A2 (en) | 1991-04-10 | 1992-10-29 | Octamer, Inc. | A method for inhibition of retroviral replication |
| US5480883A (en) | 1991-05-10 | 1996-01-02 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| CA2102780C (en) | 1991-05-10 | 2007-01-09 | Alfred P. Spada | Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase |
| US5124337A (en) | 1991-05-20 | 1992-06-23 | Schering Corporation | N-acyl-tetrahydroisoquinolines as inhibitors of acyl-coenzyme a:cholesterol acyl transferase |
| US5223506A (en) | 1991-06-04 | 1993-06-29 | Glaxo Inc. | Cyclic antitumor compounds |
| PT100905A (pt) | 1991-09-30 | 1994-02-28 | Eisai Co Ltd | Compostos heterociclicos azotados biciclicos contendo aneis de benzeno, ciclo-hexano ou piridina e de pirimidina, piridina ou imidazol substituidos e composicoes farmaceuticas que os contem |
| US5250679A (en) | 1991-10-18 | 1993-10-05 | Genentech, Inc. | Nonpeptidyl platelet aggregation inhibitors having specificity for the GPIIb III.sub. receptor |
| FR2689127B1 (fr) | 1992-03-31 | 1994-05-06 | Adir Cie | Nouvelles 3', 5' -ditertbutyl-4'-hydroxy flavones, leur procede de preparation et les compositions pharmaceutiques les renfermant. |
| DE4215587A1 (de) | 1992-05-12 | 1993-11-18 | Bayer Ag | Sulfonylbenzyl-substituierte Benzo- und Pyridopyridone |
| DE4215588A1 (de) | 1992-05-12 | 1993-11-18 | Bayer Ag | Biphenylmethyl-substituierte Pyridone |
| GB9218334D0 (en) | 1992-08-28 | 1992-10-14 | Ici Plc | Heterocyclic compounds |
| AU5850894A (en) | 1992-12-23 | 1994-07-19 | Procept, Inc. | Novel agents for inhibition of hiv infectivity and use therefor |
| JPH0725761A (ja) | 1993-07-09 | 1995-01-27 | Kureha Chem Ind Co Ltd | 軟骨保護剤 |
| WO1995003277A1 (fr) | 1993-07-23 | 1995-02-02 | Zaidan Hojin Biseibutsu Kagaku Kenkyukai | Nouveau derive de pyrrolidine |
| US5707547A (en) | 1993-08-03 | 1998-01-13 | Sumitomo Chemical Company, Limited | Trans-olefin compounds, method for production thereof, liquid crystal composition containing the same as active ingredient, and liquid crystal element using said composition |
| ATE207922T1 (de) | 1994-02-25 | 2001-11-15 | Banyu Pharma Co Ltd | Carbapenem-derivate |
| US5798344A (en) | 1994-03-08 | 1998-08-25 | Otsuka Pharmaceutical Factory, Inc. | Phosphonic ester derivatives of quinazolinones |
| FR2718329B1 (fr) | 1994-03-21 | 2002-09-20 | Rhone Poulenc Rorer Sa | Lapin transgénique sensibilisé aux dyslipoprotéinémies. |
| US6048903A (en) | 1994-05-03 | 2000-04-11 | Robert Toppo | Treatment for blood cholesterol with trans-resveratrol |
| US6168776B1 (en) | 1994-07-19 | 2001-01-02 | University Of Pittsburgh | Alkyl, alkenyl and alkynyl Chrysamine G derivatives for the antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition |
| GB2292149A (en) | 1994-08-09 | 1996-02-14 | Ferring Res Ltd | Peptide inhibitors of pro-interleukin-1beta converting enzyme |
| IL115256A0 (en) | 1994-11-14 | 1995-12-31 | Warner Lambert Co | 6-Aryl pyrido (2,3-d) pyrimidines and naphthyridines and their use |
| US5446071A (en) | 1994-11-18 | 1995-08-29 | Eli Lilly And Company | Methods for lowering serum cholesterol |
| JP4140981B2 (ja) | 1994-12-26 | 2008-08-27 | 東菱薬品工業株式会社 | 再狭窄症及び動脈硬化症治療薬 |
| US5648387A (en) | 1995-03-24 | 1997-07-15 | Warner-Lambert Company | Carboxyalkylethers, formulations, and treatment of vascular diseases |
| WO1996031206A2 (en) | 1995-04-07 | 1996-10-10 | Warner-Lambert Company | Flavones and coumarins as agents for the treatment of atherosclerosis |
| EP0747051B1 (en) | 1995-06-07 | 2002-07-24 | Eli Lilly And Company | Treatment of diseases by inducing BEF-1 transcription factor |
| US5922866A (en) | 1995-08-30 | 1999-07-13 | Otsuka Pharmaceutical Factory, Inc. | Process for preparing quinazolin-4-one derivatives |
| WO1997010221A1 (en) | 1995-09-15 | 1997-03-20 | Torrey Pines Institute For Molecular Studies | Synthesis of quinazolinone libraries |
| US5783577A (en) | 1995-09-15 | 1998-07-21 | Trega Biosciences, Inc. | Synthesis of quinazolinone libraries and derivatives thereof |
| EA199800393A1 (ru) | 1995-10-23 | 1998-12-24 | Займодженетикс, Инк. | Композиции и способы их применение для лечения поражения костей |
| RU2135494C1 (ru) | 1995-12-01 | 1999-08-27 | Санкио Компани Лимитед | Гетероциклические соединения и композиция на их основе, проявляющая антагонистическое действие в отношении рецепторов тахикинина |
| US5756736A (en) | 1996-01-26 | 1998-05-26 | Syntex (U.S.A.) Inc. | Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative |
| US5763608A (en) | 1996-02-05 | 1998-06-09 | Hoechst Celanese Corporation | Process for preparing pyrimidine derivatives |
| WO1997028118A1 (en) | 1996-02-05 | 1997-08-07 | Hoechst Celanese Corporation | Process for preparing anthranilic acids |
| US5739330A (en) | 1996-02-05 | 1998-04-14 | Hoechst Celanese Corporation | Process for preparing quinazolones |
| AU710070C (en) | 1996-02-12 | 2001-08-30 | Rutgers, The State University Of New Jersey | Coralyne analogs as topoisomerase inhibitors |
| JPH1029979A (ja) * | 1996-04-12 | 1998-02-03 | Ajinomoto Co Inc | 新規ピリジン誘導体 |
| WO1997048694A1 (en) | 1996-06-20 | 1997-12-24 | Board Of Regents, The University Of Texas System | Compounds and methods for providing pharmacologically active preparations and uses thereof |
| US5854264A (en) | 1996-07-24 | 1998-12-29 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| KR100213895B1 (ko) | 1996-10-14 | 1999-08-02 | 박원훈 | 감귤류 과피 추출물, 이로부터 분리 정제된 헤스페리딘 또는 나린진을 포함하는 심혈관 질환 예방및 치료제 조성물 |
| DE19651099A1 (de) | 1996-12-09 | 1998-06-10 | Consortium Elektrochem Ind | Mehrkomponentensystem zum Verändern, Abbau oder Bleichen von Lignin, ligninhaltigen Materialien oder ähnlichen Stoffen sowie Verfahren zu seiner Anwendung |
| IL119971A (en) | 1997-01-07 | 2003-02-12 | Yissum Res Dev Co | Pharmaceutical compositions containing dicarboxylic acids and derivatives thereof and some novel dicarboxylic acids |
| AR012634A1 (es) | 1997-05-02 | 2000-11-08 | Sugen Inc | Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion |
| JP4362638B2 (ja) | 1997-05-13 | 2009-11-11 | オクテイマー・インコーポレイテッド | ｐＡＤＰＲＴインヒビターを用いる炎症および炎症性疾患の処置法 |
| US5908861A (en) | 1997-05-13 | 1999-06-01 | Octamer, Inc. | Methods for treating inflammation and inflammatory disease using pADPRT inhibitors |
| PT988038E (pt) | 1997-06-02 | 2002-12-31 | Janssen Pharmaceutica Nv | Derivados (imidazol-5-il)metil-2-quinolinona como inibidores da proliferacao de celulas dos musculos lisos |
| IL121165A0 (en) | 1997-06-26 | 1997-11-20 | Yissum Res Dev Co | Pharmaceutical compositions containing carboxylic acids and derivatives thereof |
| WO1999011634A1 (en) | 1997-08-29 | 1999-03-11 | Takeda Chemical Industries, Ltd. | Triazine derivatives, their production and use |
| US6635642B1 (en) | 1997-09-03 | 2003-10-21 | Guilford Pharmaceuticals Inc. | PARP inhibitors, pharmaceutical compositions comprising same, and methods of using same |
| US6239114B1 (en) | 1997-09-26 | 2001-05-29 | Kgk Synergize | Compositions and methods for treatment of neoplastic diseases with combinations of limonoids, flavonoids and tocotrienols |
| DE69839887D1 (de) | 1997-10-02 | 2008-09-25 | Eisai R&D Man Co Ltd | Kondensierte pyridinderivate |
| WO1999021548A1 (en) | 1997-10-28 | 1999-05-06 | Korea Institute Of Science And Technology | Naringin and naringenin as inhibitor of acyl coa-cholesterol-o-acyltransferase, inhibitor of macrophage-lipid complex accumulation on the arterial wall and preventive or treating agent for hepatic diseases |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| DE19756388A1 (de) | 1997-12-18 | 1999-06-24 | Hoechst Marion Roussel De Gmbh | Substituierte 2-Aryl-4-amino-chinazoline |
| EP1049767B1 (en) | 1998-01-08 | 2005-08-17 | Aventis Pharmaceuticals Inc. | A transgenic rabbit that expresses a functional human lipoprotein (a) |
| US6414037B1 (en) | 1998-01-09 | 2002-07-02 | Pharmascience | Pharmaceutical formulations of resveratrol and methods of use thereof |
| US6022901A (en) | 1998-05-13 | 2000-02-08 | Pharmascience Inc. | Administration of resveratrol to prevent or treat restenosis following coronary intervention |
| CA2345311A1 (en) | 1998-09-24 | 2000-03-30 | Kazutoshi Watanabe | Hydroxyflavone derivatives as tau protein kinase 1 inhibitors |
| EP1123702A1 (en) | 1998-10-19 | 2001-08-16 | Eisai Co., Ltd. | Analgesics |
| CN1327384A (zh) | 1998-10-20 | 2001-12-19 | 韩国科学技术研究院 | 作为血浆高密度脂蛋白浓度增高剂的生物类黄酮 |
| WO2000035865A2 (en) | 1998-12-17 | 2000-06-22 | Tularik Inc. | Tubulin-binding agents |
| US6291456B1 (en) | 1998-12-30 | 2001-09-18 | Signal Pharmaceuticals, Inc. | Compounds and methods for modulation of estrogen receptors |
| US6399633B1 (en) | 1999-02-01 | 2002-06-04 | Aventis Pharmaceuticals Inc. | Use of 4-H-1-benzopryan-4-one derivatives as inhibitors of smooth muscle cell proliferation |
| TR200102522T2 (tr) | 1999-03-15 | 2001-12-21 | Abbott Laboratories | Antibakteryel etkinliğe sahip olan 6-0-ikameli makrolidler. |
| US6969720B2 (en) | 1999-03-17 | 2005-11-29 | Amr Technology, Inc. | Biaryl substituted purine derivatives as potent antiproliferative agents |
| US6054435A (en) | 1999-03-19 | 2000-04-25 | Abbott Laboratories | 6-O-substituted macrolides having antibacterial activity |
| IL145922A0 (en) | 1999-04-28 | 2002-07-25 | Aventis Pharma Gmbh | Di-aryl acid derivatives as ppar receptor ligands |
| US6835755B1 (en) | 1999-06-24 | 2004-12-28 | University Of Pretoria | Naphthoquinone derivatives and their use in the treatment and control of tuberculosis |
| DE19934799B4 (de) | 1999-07-28 | 2008-01-24 | Az Electronic Materials (Germany) Gmbh | Chiral-smektische Flüssigkristallmischung und ihre Verwendung in Aktivmatrix-Displays mit hohen Kontrastwerten |
| JP2001131151A (ja) | 1999-11-02 | 2001-05-15 | Shionogi & Co Ltd | オレフィン誘導体の新規用途 |
| JP5278983B2 (ja) | 1999-11-17 | 2013-09-04 | 塩野義製薬株式会社 | アミド化合物の新規用途 |
| WO2001042231A2 (en) | 1999-12-06 | 2001-06-14 | Welichem Biotech Inc. | Polyhydroxystilbenes and stilbene oxides as antisoriatic agents and protein kinase inhibitors |
| FR2804679B1 (fr) | 2000-02-07 | 2002-04-26 | Clariant France Sa | Nouveaux composes phenoliques derives des dialcoxyethanals, leur procede de preparation et leur application |
| JP2003522810A (ja) | 2000-02-17 | 2003-07-29 | アップルトン ペーパーズ インコーポレイテッド | アルコキシ又はアリルメトキシエタンの製造方法 |
| WO2003018008A1 (fr) | 2000-02-25 | 2003-03-06 | Shionogi & Co., Ltd. | Agent d'accélération de l'expression de apo ai |
| WO2001083456A1 (fr) | 2000-04-27 | 2001-11-08 | Yamanouchi Pharmaceutical Co., Ltd. | Derives d'heteroaryle condenses |
| US6653332B2 (en) | 2000-05-03 | 2003-11-25 | Tularik Inc. | Combination therapeutic compositions and method of use |
| US6548694B2 (en) * | 2000-05-23 | 2003-04-15 | Hoffman-La Roche Inc. | N-(4-carbamimidoyl-phenyl)-glycine derivatives |
| JP2001335476A (ja) | 2000-05-29 | 2001-12-04 | Shionogi & Co Ltd | 三環化合物の新規用途 |
| WO2003024441A1 (fr) | 2001-09-14 | 2003-03-27 | Shionogi & Co., Ltd. | Nouvelle utilisation de composes tricycliques |
| US6541522B2 (en) | 2000-08-16 | 2003-04-01 | Insmed Incorporated | Methods of using compositions containing hypotriglyceridemically active stilbenoids |
| CA2356544C (en) | 2000-10-03 | 2006-04-04 | Warner-Lambert Company | Pyridotriazines and pyridopyridazines |
| MXPA03003002A (es) | 2000-10-05 | 2004-12-06 | Fujisawa Pharmaceutical Co | Compuestos de benzamina como inhibidores de la secrecion de la apo b. |
| CN1479721A (zh) | 2000-10-11 | 2004-03-03 | ͨ��ҽ�ƹ�˾ | 用于胆固醇治疗和相关应用的亚砜和双亚砜化合物和组合物 |
| MXPA03003022A (es) | 2000-10-11 | 2003-07-14 | Esperion Therapeutics Inc | Compuestos de sulfuro y disulfuro y composiciones para el control del colesterol y usos relacionados. |
| CN1285601C (zh) | 2000-11-30 | 2006-11-22 | 佳能株式会社 | 发光器件和显示器 |
| AU2002239508B9 (en) | 2000-12-07 | 2005-09-08 | Gilead Palo Alto, Inc. | Substituted 1, 3, 5-triazines and pyrimidines as ABCA-1 elevating compounds against coronary artery disease or atherosclerosis |
| KR100472694B1 (ko) | 2000-12-30 | 2005-03-07 | 한국생명공학연구원 | 플라바논 유도체 및 이를 포함하는 혈중 지질 농도 관련질환의 예방 및 치료용 조성물 |
| JP2002249483A (ja) | 2001-02-21 | 2002-09-06 | Koei Chem Co Ltd | アリール置換複素環式化合物の製造法 |
| JP4256679B2 (ja) | 2001-03-16 | 2009-04-22 | ノボゲン リサーチ ピーティーワイ リミテッド | 再狭窄の治療方法 |
| EP1385501A2 (en) | 2001-04-11 | 2004-02-04 | Atherogenics, Inc. | Probucol monoesters and their use to increase plasma hdl cholesterol levels and improve hdl functionality |
| US6890915B2 (en) | 2001-05-25 | 2005-05-10 | Bristol-Myers Squibb Pharma Company | Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE) |
| WO2003007959A1 (en) | 2001-07-16 | 2003-01-30 | Fujisawa Pharmaceutical Co., Ltd. | Quinoxaline derivatives which have parp inhibitory action |
| JP2005504047A (ja) | 2001-08-13 | 2005-02-10 | チバ スペシャルティ ケミカルズ ホールディング インコーポレーテッド | 紫外線吸収剤 |
| US8124625B2 (en) | 2001-09-14 | 2012-02-28 | Shionogi & Co., Ltd. | Method of enhancing the expression of apolipoprotein AI using olefin derivatives |
| US7429593B2 (en) | 2001-09-14 | 2008-09-30 | Shionogi & Co., Ltd. | Utilities of amide compounds |
| US6835469B2 (en) | 2001-10-17 | 2004-12-28 | The University Of Southern California | Phosphorescent compounds and devices comprising the same |
| US7166368B2 (en) | 2001-11-07 | 2007-01-23 | E. I. Du Pont De Nemours And Company | Electroluminescent platinum compounds and devices made with such compounds |
| US7250512B2 (en) | 2001-11-07 | 2007-07-31 | E. I. Du Pont De Nemours And Company | Electroluminescent iridium compounds having red-orange or red emission and devices made with such compounds |
| US6541045B1 (en) | 2002-01-04 | 2003-04-01 | Nutraceutical Corporation | Herbal composition and method for combating inflammation |
| WO2003064399A1 (fr) | 2002-01-28 | 2003-08-07 | Ube Industries, Ltd. | Procede de production de derive de quinazolin-4-one |
| EP1478357B1 (en) | 2002-02-19 | 2007-01-31 | Pfizer Italia S.r.l. | Tricyclic pyrazole derivatives, process for their preparation and their use as antitumor agents |
| MY140680A (en) | 2002-05-20 | 2010-01-15 | Bristol Myers Squibb Co | Hepatitis c virus inhibitors |
| TW200401770A (en) | 2002-06-18 | 2004-02-01 | Sankyo Co | Fused-ring pyrimidin-4(3H)-one derivatives, processes for the preparation and uses thereof |
| KR20040001144A (ko) | 2002-06-27 | 2004-01-07 | 김대경 | 신규한 적혈구 세포질형 포스포리파아제 에이 투 효소,그에 대한 항체, 이들의 용도 및 제조 방법 |
| US20040033480A1 (en) | 2002-08-15 | 2004-02-19 | Wong Norman C.W. | Use of resveratrol to regulate expression of apolipoprotein A1 |
| US20050080021A1 (en) | 2002-08-15 | 2005-04-14 | Joseph Tucker | Nitric oxide donating derivatives of stilbenes, polyphenols and flavonoids for the treatment of cardiovascular disorders |
| US20050080024A1 (en) | 2002-08-15 | 2005-04-14 | Joseph Tucker | Nitric oxide donating derivatives for the treatment of cardiovascular disorders |
| AU2003265659A1 (en) | 2002-08-23 | 2004-03-11 | University Of Connecticut | Novel biphenyl and biphenyl-like cannabinoids |
| EP1407774A1 (en) | 2002-09-10 | 2004-04-14 | LION Bioscience AG | 2-Amino-4-quinazolinones as LXR nuclear receptor binding compounds |
| EP1398032A1 (en) | 2002-09-10 | 2004-03-17 | PheneX Pharmaceuticals AG | 4-Oxo-quinazolines as LXR nuclear receptor binding compounds |
| EP1558581A4 (en) | 2002-10-07 | 2007-07-25 | Bristol Myers Squibb Co | DERIVATIVES OF TRIAZOLONE AND TRIAZOLETHIONE |
| WO2004037176A2 (en) | 2002-10-21 | 2004-05-06 | Bristol-Myers Squibb Company | Quinazolinones and derivatives thereof as factor xa inhibitors |
| WO2004039795A2 (en) | 2002-10-29 | 2004-05-13 | Fujisawa Pharmaceutical Co., Ltd. | Amide compounds for the treatment of hyperlipidemia |
| EP1418164A1 (en) | 2002-11-07 | 2004-05-12 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | New stilbene derivatives and their use as aryl hydrocarbon receptor ligand antagonists |
| EP1565475B1 (en) | 2002-11-18 | 2009-04-08 | F. Hoffmann-La Roche Ag | Diazinopyrimidines and their use as protein kinase inhibitors |
| US7244727B2 (en) | 2002-11-22 | 2007-07-17 | Japan Tobacco Inc. | Fused bicyclic nitrogen-containing heterocycles |
| CN100418954C (zh) | 2002-12-13 | 2008-09-17 | 弗·哈夫曼-拉罗切有限公司 | 3h-喹唑啉-4-酮衍生物 |
| ITRM20020629A1 (it) | 2002-12-19 | 2004-06-20 | Sigma Tau Ind Farmaceuti | Uso di acidi alfa-feniltiocarbossilici e alfa-fenilossicarbossilici ad attivita' ipoglicemizzante e/o ipolipidemizzante. |
| ES2361924T3 (es) | 2002-12-20 | 2011-06-24 | X-Ceptor Therapeutics, Inc. | Derivados de isoquinolinona y su uso como agentes terapéuticos. |
| JP2004203751A (ja) | 2002-12-24 | 2004-07-22 | Pfizer Inc | 置換６，６−ヘテロ二環式誘導体 |
| EP1577288B1 (en) | 2002-12-26 | 2014-07-23 | Eisai R&D Management Co., Ltd. | Selective estrogen receptor modulators |
| WO2004065392A1 (en) | 2003-01-24 | 2004-08-05 | Smithkline Beecham Corporation | Condensed pyridines and pyrimidines and their use as alk-5 receptor ligands |
| WO2004072042A2 (en) | 2003-02-12 | 2004-08-26 | Carex S.A. | Quinoline derivative and their use for modulation of lxr activity |
| JP2006522124A (ja) | 2003-04-03 | 2006-09-28 | 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 | プロテインキナーゼのインヒビターとして有用な組成物 |
| AU2004230928B2 (en) | 2003-04-09 | 2010-12-02 | Exelixis, Inc. | Tie-2 modulators and methods of use |
| JP2004307440A (ja) | 2003-04-10 | 2004-11-04 | Kyorin Pharmaceut Co Ltd | ２−アミノ‐１，３‐プロパンジオール誘導体とその付加塩 |
| EP2033654B1 (en) | 2003-04-16 | 2012-05-16 | Bristol-Myers Squibb Company | Process for resolving a mixture of alkyl ester enantiomers using an enzyme |
| EP1633718B1 (en) | 2003-06-17 | 2012-06-06 | Millennium Pharmaceuticals, Inc. | COMPOSITIONS AND METHODS FOR INHIBITING TGF-s |
| EP1637523A4 (en) | 2003-06-18 | 2009-01-07 | Ube Industries | PROCESS FOR PRODUCING A PYRIMIDIN-4-ONE COMPOUND |
| US20050043300A1 (en) | 2003-08-14 | 2005-02-24 | Pfizer Inc. | Piperazine derivatives |
| AU2004279644A1 (en) | 2003-10-10 | 2005-04-21 | Resverlogix Corp. | Treatment of diseases associated with the egr-1 enhancer element |
| CN1893951A (zh) | 2003-12-19 | 2007-01-10 | 默克公司 | 有丝分裂驱动蛋白抑制剂 |
| WO2005066162A1 (en) | 2003-12-23 | 2005-07-21 | Human Biomolecular Research Institute | Synthetic compounds and derivatives as modulators of smoking or nicotine ingestion and lung cancer |
| TW200536830A (en) | 2004-02-06 | 2005-11-16 | Chugai Pharmaceutical Co Ltd | 1-(2H)-isoquinolone derivative |
| AU2005247808B2 (en) | 2004-05-31 | 2011-02-10 | Msd K.K. | Quinazoline derivative |
| WO2006012577A2 (en) | 2004-07-22 | 2006-02-02 | Bayer Pharmaceuticals Corporation | Quinazolinone derivatives useful for the regulation of glucose homeostasis and food intake |
| US20070218155A1 (en) | 2004-08-20 | 2007-09-20 | Kuhrts Eric H | Methods and compositions for treating dyslipidaemia |
| CA2584507C (en) | 2004-10-20 | 2016-04-26 | Resverlogix Corp. | Flavanoids and isoflavanoids for the prevention and treatment of cardiovascular diseases |
| WO2006071095A1 (en) | 2004-12-31 | 2006-07-06 | Sk Chemicals Co., Ltd. | Quinazoline derivatives for the treatment and prevention of diabetes and obesity |
| CR9465A (es) | 2005-03-25 | 2008-06-19 | Surface Logix Inc | Compuestos mejorados farmacocineticamente |
| US8410109B2 (en) | 2005-07-29 | 2013-04-02 | Resverlogix Corp. | Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices |
| JP2009520700A (ja) | 2005-12-21 | 2009-05-28 | ペインセプター ファーマ コーポレーション | 依存性イオンチャネルを調節するための組成物および方法 |
| NZ579355A (en) | 2007-02-01 | 2012-03-30 | Resverlogix Corp | 2-(Aryl)-4-oxo-quinazoline derivatives |
| EP2005941A3 (de) | 2007-06-01 | 2009-04-01 | Henkel AG & Co. KGaA | Zellverjüngende Zusammensetzungen |
| ES2463097T3 (es) | 2009-01-08 | 2014-05-27 | Resverlogix Corp. | Compuestos para la prevención y el tratamiento de enfermedades cardiovasculares |
-
2009
- 2009-06-24 ES ES09770937.2T patent/ES2532402T3/es active Active
- 2009-06-24 SI SI200931175T patent/SI2346837T1/sl unknown
- 2009-06-24 WO PCT/US2009/048457 patent/WO2009158404A1/en active Application Filing
- 2009-06-24 DK DK09770937.2T patent/DK2346837T3/da active
- 2009-06-24 NZ NZ586440A patent/NZ586440A/en unknown
- 2009-06-24 PT PT97709372T patent/PT2346837E/pt unknown
- 2009-06-24 AU AU2009262252A patent/AU2009262252B2/en active Active
- 2009-06-24 CA CA2711103A patent/CA2711103C/en active Active
- 2009-06-24 CN CN200980106586.7A patent/CN101970416B/zh active Active
- 2009-06-24 US US12/490,877 patent/US8114995B2/en active Active
- 2009-06-24 RU RU2010131833/04A patent/RU2520098C2/ru active
- 2009-06-24 EP EP09770937.2A patent/EP2346837B8/en active Active
- 2009-06-24 KR KR1020107018284A patent/KR101629356B1/ko active IP Right Grant
- 2009-06-24 PL PL09770937T patent/PL2346837T3/pl unknown
- 2009-06-24 JP JP2011516584A patent/JP5602728B2/ja active Active
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2010
- 2010-06-22 IL IL206544A patent/IL206544A/en active IP Right Grant
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2012
- 2012-01-26 HK HK12100731.0A patent/HK1160135A1/xx unknown
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2015
- 2015-05-04 HR HRP20150477TT patent/HRP20150477T8/hr unknown
- 2015-05-11 CY CY20151100414T patent/CY1116260T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RU2010131833A (ru) | 2012-08-10 |
| US8114995B2 (en) | 2012-02-14 |
| JP5602728B2 (ja) | 2014-10-08 |
| SI2346837T1 (sl) | 2015-05-29 |
| NZ586440A (en) | 2011-07-29 |
| AU2009262252A1 (en) | 2009-12-30 |
| CA2711103A1 (en) | 2009-12-30 |
| AU2009262252B2 (en) | 2013-05-02 |
| KR101629356B1 (ko) | 2016-06-13 |
| US20100004448A1 (en) | 2010-01-07 |
| IL206544A (en) | 2014-07-31 |
| EP2346837B8 (en) | 2015-04-15 |
| IL206544A0 (en) | 2010-12-30 |
| CN101970416B (zh) | 2014-05-28 |
| HRP20150477T1 (en) | 2015-06-05 |
| CY1116260T1 (el) | 2017-02-08 |
| EP2346837B1 (en) | 2015-03-04 |
| RU2520098C2 (ru) | 2014-06-20 |
| CA2711103C (en) | 2016-08-09 |
| CN101970416A (zh) | 2011-02-09 |
| HRP20150477T8 (hr) | 2016-10-21 |
| KR20110036525A (ko) | 2011-04-07 |
| WO2009158404A1 (en) | 2009-12-30 |
| PL2346837T3 (pl) | 2015-07-31 |
| ES2532402T3 (es) | 2015-03-26 |
| HK1160135A1 (en) | 2012-08-10 |
| PT2346837E (pt) | 2015-04-02 |
| JP2011526287A (ja) | 2011-10-06 |
| EP2346837A1 (en) | 2011-07-27 |
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