CAS: 98977-34-5; 1-Tert-Butyl 3-Ethyl 4-Oxopiperidine-1,3-Dicarboxylate

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CAS号24424-99-5 二碳酸二叔丁酯 | CAS号1454-53-1 1-苄基-3-乙氧羰基-4-哌啶酮盐酸盐 | CAS号4644-61-5 4-哌啶酮-3-甲酸乙酯盐酸盐 | CAS号52763-21-0 N-苄基-3-氧代哌啶-4-羧... | CAS号67848-59-3 4-氧代-3-哌啶甲酸乙酯 | CAS号79099-07-3 1-B°C-4-哌啶酮 | CAS号105-58-8 碳酸二乙酯 | CAS号4755-77-5 草酰氯单乙酯 | CAS号7646-93-7 硫酸氢钾 | CAS号41276-30-6 1-苄基-4-哌啶酮-3-羧酸乙酯 | CAS号79099-07-3 1-B°C-4-哌啶酮 | CAS号86447-11-2 1-B°C-1,2,5,6-四... | CAS号152559-30-3 3-羟基-6,7-二氢-1H-... | CAS号154548-45-5 4-氧代-哌啶-1,3-二羧酸苄基乙酯 | CAS号126114-09-8 1-叔丁基 3-乙基 5,6-... | CAS号932035-01-3 N-B°C-4-胺基哌啶-3-甲酸乙酯 | CAS号947403-75-0 1-叔丁基 3-乙基 4-氨基...

1-苄基-4-哌啶酮-3-羧酸乙酯置于palladium On Activated Charcoal 氢气,碳酸氢钠,Sodium Chloride体系中,用 乙醇,氯仿,水 作为反应溶剂,20.0~60.0 °C,344.74 Kpa 条件下,反应生成 1-N-Boc-4-氧代-3-哌啶羧酸乙酯
参考文献:Design And Syntheses Of Melanocortin Subtype-4 Receptor Agonists. Part 2: Discovery Of The Dihydropyridazinone Motif
标题:Design And Syntheses Of Melanocortin Subtype-4 Receptor Agonists. Part 2: Discovery Of The Dihydropyridazinone Motif
摘要:Optimization Of The Biological Activity Of A New Class Of Non-Peptidyl,Pyridazinone Derived Human Melanocortin Subtype-4 Receptor Agonists Is Disclosed. (C) 2005 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2005.06.033

专利信息

专利号:US-6867202-B1
优先权日:1997-06-25
标 题 :Treatment of insulin resistance
发明人：CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL
权利人:PFIZER
摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.

专利号:EP-1404682-B1
优先权日:2001-06-29
标题:Method of inhibiting ptp 1b and/or t-cell ptp and/or other ptpases with an asp residue at position 48
发明人：HANSEN THOMAS KRUSE; OLSEN OLE HVILSTED; PETERSEN ANDERS KLARSKOV; LAU JESPER; ANDERSEN HENRIK SUNE; MOLLER NIELS PETER HUNDAHL
权利人:NOVO NORDISK AS
摘要:This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al., Proc. Natl. Acad. Sci. USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1. This invention also relates to (I) the design and selection of inhibitors, which bind to the active site of PTP1B and/or TC-PTP and/or PTPases having an aspartic acid (Asp) in position 48 (II) the synthesis of said inhibitors, methods for their preparation and (III) to compositions comprising the inhibitor compounds.

专利号:US-2003064979-A1
优先权日:2001-06-29
标题 :Method of inhibiting PTP 1B and /or T-cell PTP and/or other PTPases with an Asp residue at position 48
发明人：HANSEN THOMAS KRUSE; OLSEN OLE HVILSTED; PETERSEN ANDERS KLARSKOV; LAU JESPER; ANDERSEN HENRIK SUNE; MOLLER NIELS PETER HUNDAHL
摘要:This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al, Proc Natl Acad Sci USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1 n n n This invention also relates to (I) the design and selection of inhibitors, which bind to the active site of PTP1B and/or TC-PTP and/or PTPases having an aspartic acid (Asp) in position 48 (II) the synthesis of said inhibitors, methods for their preparation and (III) to compositions comprising the inhibitor compounds.

专利号:US-6936600-B2
优先权日:1999-04-01
标题:Sorbitol dehrydrogenase inhibitors
发明人：CHU-MOYER MARGARET Y; MYLARI BANAVARA L; ZEMBROWSKI WILLIAM J
权利人:PFIZER
摘要:This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, n n nwherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula I and to processes for preparing those intermediates.

专利号:US-8518952-B2
优先权日:2008-08-06
标题 :6 substituted 2-heterocyclylamino pyrazine compounds as CHK-1 inhibitors
发明人：BRAGANZA JOHN FREDERICK; COLLINS MICHAEL RAYMOND; KATH JOHN CHARLES; NINKOVIC SACHA; LI HUI; RICHTER DANIEL TYLER
权利人:BRAGANZA JOHN FREDERICK; COLLINS MICHAEL RAYMOND; KATH JOHN CHARLES; NINKOVIC SACHA; LI HUI; RICHTER DANIEL TYLER; PFIZER
摘要:The present invention is directed to compounds of formula (I), n nand pharmaceutically acceptable salts thereof, their synthesis, and their use as CHK-1 inhibitors.