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公开(公告)号:US5583148A
公开(公告)日:1996-12-10
申请号:US729986
申请日:1991-07-15
申请人: Wayne K. Anderson , Dennis C. Dean
发明人: Wayne K. Anderson , Dennis C. Dean
IPC分类号: A61K31/44 , A61P31/04 , A61P35/00 , C07D401/04 , C07D403/04 , C07D487/04 , C07D219/08 , A61K31/435 , C07D215/10 , C07D217/10
CPC分类号: C07D401/04 , C07D487/04
摘要: This invention relates to new pyridyl, quinoline and acridine bis-acyloxymethyl compounds; to compositions comprising these compounds; and to processes for their utility as fungicides, bactericides and as inhibitors of the growth of cancer in warm-blooded animals. In accordance with this invention, new bis-acyloxymethyl derivatives are provided of the formula: ##STR1## wherein B is selected from substituted and unsubstituted alkyl, cycloalkyl, aryl, alkenyl, cycloalkenyl and alkynyl; A is selected from hydrogen and B; or, A and B together comprise a pyrrolizine; L is selected from ##STR2## wherein Y is selected from hydrogen or ##STR3## each R and Z is independently selected from hydrogen or substituted and unsubstituted alkyl, cycloalkyl, aryl, alkenyl, cycloalkenyl, alkynyl, amine group, each Z' is independently selected from hydrogen and substituted or unsubstituted alkyl; M is Z or is selected from halogen, nitro, hydroxyl, nitrile and substituted or unsubstituted, carboxylic acid group, carboxylic acid ester group, carboxylic acid amide group, sulfonic acid group and sulfonic acid amide group; ether group, thioether group, acylated hydroxyl, sulfonylamide, sulfonylurea, sulfoxide group, sulfone group and mixtures thereof; each n is the same and is 0 or 1; q is from 0-4; and, X is the anion of an acid.
摘要翻译: 本发明涉及新的吡啶基,喹啉和吖啶双酰氧基甲基化合物; 包含这些化合物的组合物; 以及作为杀真菌剂,杀菌剂和作为温血动物癌症生长抑制剂的作用的方法。 根据本发明,新的双酰氧基甲基衍生物由下式提供:其中B选自取代和未取代的烷基,环烷基,芳基,烯基,环烯基和炔基; A选自氢和B; 或者,A和B一起包含吡咯嗪; 每个R和Z独立地选自氢或取代和未取代的烷基,环烷基,芳基,烯基,环烯基,炔基,胺基,每个Z'独立地选自氢 和取代或未取代的烷基; M为Z或选自卤素,硝基,羟基,腈和取代或未取代的羧酸基,羧酸酯基,羧酸酰胺基,磺酸基和磺酸酰胺基; 醚基,硫醚基,酰化羟基,磺酰胺,磺酰脲,亚砜基,砜基及其混合物; 每个n相同,为0或1; q为0-4; 而X是酸的阴离子。
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公开(公告)号:US06838291B2
公开(公告)日:2005-01-04
申请号:US09904045
申请日:2001-07-12
申请人: John W. Butcher , David A. Claremon , Thomas M. Connolly , Jerzy Karczewski , Kenneth S. Koblan , Matthew J. Kostura , Nigel J. Liverton , Dennis C. Dean , David G. Melillo
发明人: John W. Butcher , David A. Claremon , Thomas M. Connolly , Jerzy Karczewski , Kenneth S. Koblan , Matthew J. Kostura , Nigel J. Liverton , Dennis C. Dean , David G. Melillo
IPC分类号: G01N33/566 , A61K51/04 , C07D491/10 , C07D491/107 , C07D491/20 , C07F7/18 , C12N15/09 , C12Q1/02 , G01N33/58 , G01N33/60 , G01N33/68 , G01N33/534 , G01N33/567
CPC分类号: G01N33/6872 , A61K51/0455 , A61K51/0476 , C07B2200/05 , C07D491/10 , C07F7/1804 , G01N33/60
摘要: The present invention is directed to the radioligand compound, [35S]-radiolabeled (+)-N-[1′-(6-cyano-1,2,3,4-tetrahydro-2(R)-naphthalenyl)-3,4-dihydro-4(R)-hydoxyspiro[2H-1-benzopyran-2,4′-piperidin]-6-yl]methanesulfonamide. Also within the scope of this invention is a method for identifying compounds that bind to the IKr channel, and may have antiarrhythmic activity.
摘要翻译: 本发明涉及放射性配体化合物[35 S] - 放射性标记的(+) - N- [1' - (6-氰基-1,2,3,4-四氢-2(R) - 萘基) -3,4-二氢-4(R) - 氧代氧杂螺[2H-1-苯并吡喃-2,4'-哌啶] -6-基]甲磺酰胺。 本发明的范围也是用于鉴定结合IKr通道的化合物的方法,并且可能具有抗心律失常活性。
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公开(公告)号:US5830433A
公开(公告)日:1998-11-03
申请号:US768368
申请日:1996-12-17
申请人: Dennis C. Dean , David G. Melillo , Ravi Nargund , Leonardus Van Der Ploeg , Sheng-Shung Pong , James M. Schaeffer , Roy G. Smith
发明人: Dennis C. Dean , David G. Melillo , Ravi Nargund , Leonardus Van Der Ploeg , Sheng-Shung Pong , James M. Schaeffer , Roy G. Smith
IPC分类号: A61K51/04 , C07K5/06 , A61K51/00 , C07D471/10
CPC分类号: C07K5/06034 , A61K51/0455 , A61K2123/00
摘要: The present invention is directed to �.sup.35 S!-N-�1(R)-�(1,2-dihydro-1-methanesulfonylspiro�3H-indole-3,4'-piperidin!-1'-yl)carbonyl!-2-(phenylmethyloxy)ethyl!-2-amino-2-methylpropanamide, and pharmaceutically acceptable salts thereof. This �.sup.35 S! radioligand is useful in identifying and characterizing cellular receptors which play a role in the activity of growth hormone secretatogogues. In addition, this �.sup.35 S! radioligand is useful in assays which test compounds for growth hormone secretagogue activity.
摘要翻译: 本发明涉及[35S] -N- [1(R) - [(1,2-二氢-1-甲磺酰基螺[3H-吲哚-3,4'-哌啶] -1'-基)羰基] 2-(苯基甲氧基)乙基] -2-氨基-2-甲基丙酰胺及其药学上可接受的盐。 该[35S]放射性配体可用于鉴定和表征在生长激素分泌蛋白酶活性中起作用的细胞受体。 此外,该[35S]放射性配体可用于测试化合物用于生长激素促分泌素活性的测定。
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公开(公告)号:US06753410B2
公开(公告)日:2004-06-22
申请号:US09797820
申请日:2001-03-02
申请人: Alan John Nadin , Joseph George Neduvelil , Mohinder K. Sardana , Jules A. Shafer , Stephen J. Gardell , Ming-Tain Lai , Yueming Li , Bruce D. Dorsey , Dennis C. Dean
发明人: Alan John Nadin , Joseph George Neduvelil , Mohinder K. Sardana , Jules A. Shafer , Stephen J. Gardell , Ming-Tain Lai , Yueming Li , Bruce D. Dorsey , Dennis C. Dean
IPC分类号: C07K508
CPC分类号: C07K5/0207 , A61K38/00 , A61K38/55
摘要: The present invention is directed to compounds and pharmaceutical compositions comprising the compounds which are inhibitors of the enzyme gamma secretase and which are useful in the treatment or prevention of diseases in which the beta-amyloid peptide is involved, such as Alzheimer's disease.
摘要翻译: 本发明涉及化合物和药物组合物,其包含作为γ-分泌酶抑制剂的化合物,其可用于治疗或预防涉及β-淀粉样蛋白肽的疾病,例如阿尔茨海默氏病。
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