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公开(公告)号：US06489480B2
公开(公告)日：2002-12-03
申请号：US09734443
申请日：2000-12-11
申请人： George Rodriguez
发明人： George Rodriguez
IPC分类号： C07D20908
CPC分类号： C07D207/325 , C07D205/04 , C07D209/08 , C07D295/073 , C07F5/027 , C08F4/65916 , C08F4/65927 , C08F10/06 , C08F110/02 , C08F110/06 , C08F4/65908 , C08F2500/12 , C08F2500/03
摘要： This description addresses fluorinated amine compounds meeting the general formula R′iArF—ER2, where ArF is a fluoroaryl group, E is nitrogen or phosphorous, each R is independently a C1-C20 hydrocarbyl group; or the two Rs may connect to form an unsubstituted or substituted C2-C20 cycloaliphatic group, R′ is a C1-C20 hydrocarbyl or halogenated hydrocarbyl, and i is 0, 1 or 2. These compounds may be protonated with strong Bronsted acids to form protonated amine compounds that are useful for the preparation of organometallic catalyst-cocatalyst compounds comprising noncoordinating or weakly coordinating anions. The resulting organometallic catalyst-cocatalyst complexes can be effectively used as olefin polymerization catalysts. High number-average molecular weight polymers at high rates of productivity were observed from the use of metallocene catalyst complexes prepared with [N-pentafluorophenyl pyrrolidinium][tetrakis(pentafluorophenyl)borate] of [N-pentafluorophenyl pyrrolidinium][chloride].
摘要翻译： 该描述涉及满足通式R'ArF-ER2的氟化胺化合物，其中ArF是氟代芳基，E是氮或磷，每个R独立地是C1-C20烃基; 或两个R可连接形成未取代或取代的C 2 -C 20脂环族基团，R'为C 1 -C 20烃基或卤代烃基，且i为0,1或2.这些化合物可用强烈的布朗斯台德酸质子化形成 可用于制备包含非配位或弱配位阴离子的有机金属催化剂 - 助催化剂化合物的质子化胺化合物。 所得到的有机金属催化剂 - 助催化剂配合物可以有效地用作烯烃聚合催化剂。 使用由[N-五氟苯基吡咯烷鎓] [氯化物]的[N-五氟苯基吡咯烷鎓] [四（五氟苯基）硼酸盐]制备的茂金属催化剂配合物，观察到高生产率的高数均分子量聚合物。
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2.发明授权公开(公告)号：US06407261B1
公开(公告)日：2002-06-18
申请号：US09647470
申请日：2000-09-27
IPC分类号： C07D20908
CPC分类号： C07C313/04 , C07D209/08 , C07D209/88
摘要： A process for preparing 4-hydroxy carbazoles useful as intermediates for preparing compounds that are useful for inhibiting sPLA2 and novel intermediates.
摘要翻译： 用作制备可用于抑制sPLA2和新型中间体的化合物的中间体的4-羟基咔唑的制备方法。
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3.发明授权公开(公告)号：US06350749B1
公开(公告)日：2002-02-26
申请号：US09601866
申请日：2000-08-08
IPC分类号： C07D20908
CPC分类号： C07D221/04 , C07D209/06 , C07D209/88 , C07D215/38 , C07D215/60 , C07D231/56 , C07D237/28 , C07D239/74 , C07D261/20 , C07D307/79 , C07D307/84 , C07D401/04 , C07D405/04 , C07D409/04 , C07D417/04
摘要： The present invention is to provide a compound of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic heterocyclic ring, the ring B an optionally substituted 5- to 6-membered aromatic homocyclic ring or an optionally substituted 5- to 6-membered aromatic heterocyclic ring, R1 is a hydrogen atom, a hydroxy group or a lower alkyl group, and n is 0 or 1, or a salt thereof, which is effective for the prevention or treatment of ischemic cardiac disease, etc., and which is useful as an agent for preventing or treating ischemic cardiac disease, etc. such as myocardial infarction, arrhythmia, etc.
摘要翻译： 本发明提供下式的化合物：其中环A为任选取代的5至6元芳族杂环，环B为任选取代的5至6元芳族碳环或任选取代的5 至6元芳族杂环，R 1为氢原子，羟基或低级烷基，n为0或1，或其盐对预防或治疗缺血性心脏病有效等。 可用作预防或治疗心肌梗死，心律失常等缺血性心脏病等的药剂。
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公开(公告)号：US06756398B1
公开(公告)日：2004-06-29
申请号：US10111028
申请日：2002-04-18
申请人： Michael Balestra , David Gurley , James Rosamond
发明人： Michael Balestra , David Gurley , James Rosamond
IPC分类号： C07D20908
CPC分类号： C07D209/08 , A61K31/404 , A61K45/06
摘要： Compounds of Formula I wherein R1a, R1b, R2b, R3b, R3a, R2a, B1, B2, Z, A2 and A1 are as defined in the specification, enantiomers thereof, pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially for treatment of conditions associated with reductions in nicotinic transmission. Compounds of the invention enhance the efficacy of agonists at nicotinic receptors.
摘要翻译： R 1，R 1b，R 2b，R 3b，R 3a，R 2a，B 1，B 2，Z，A 2中的式I化合物， 和A 1如本说明书中所定义，其对映异构体，其药学上可接受的盐，制备方法，含有它们的药物组合物及其在治疗中的用途，特别是用于治疗与烟碱传递减少有关的病症。 本发明的化合物增强了激动剂在烟碱受体上的功效。
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公开(公告)号：US06380238B1
公开(公告)日：2002-04-30
申请号：US09786154
申请日：2001-03-01
申请人： David Reginald Adams , Jonathan Mark Bentley , Jonathan Richard Anthony Roffey , Richard John Hamlyn , Suneel Gaur , Matthew Alexander James Duncton , David Bebbington , Nathaniel Julius Monck , Claire Elizabeth Dawson , Robert Mark Pratt , Ashley Roger George
发明人： David Reginald Adams , Jonathan Mark Bentley , Jonathan Richard Anthony Roffey , Richard John Hamlyn , Suneel Gaur , Matthew Alexander James Duncton , David Bebbington , Nathaniel Julius Monck , Claire Elizabeth Dawson , Robert Mark Pratt , Ashley Roger George
IPC分类号： C07D20908
CPC分类号： C07D401/04 , C07D209/08 , C07D401/12 , C07D409/04 , C07D409/12
摘要： For use in therapy a chemical compound of formula (I), wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, heterocyclyl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, wherein at least one of R4 to R7 is a substituent group other than hydrogen, and pharmaceutically acceptable salts and prodrugs thereof, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and especially for the treatment of obesity; chemical compounds of formula (I) other than compounds wherein R7 is hydroxy.
摘要翻译： 用于治疗式（I）化合物，其中R 1至R 3独立地选自氢和烷基; R4至R7独立地选自氢，卤素，羟基，烷基，芳基，杂环基，烷氧基，芳氧基，烷硫基，芳硫基，烷基磺酰基，烷基磺酰基，芳基磺酰基，芳基磺酰基，氨基，单烷基氨基，二烷基氨基，硝基，氰基，甲醛， ，氨基羰基，单烷基氨基羰基，二烷基氨基羰基，烷氧基羰基氨基，氨基羰基氧基，单烷基氨基羰基氧基，二烷基氨基羰基氧基，单烷基氨基羰基氨基和二烷基氨基羰基氨基，其中R4至R7中的至少一个是氢以外的取代基，及其药学上可接受的盐和前药，特别是用于治疗 中枢神经系统; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症，睡眠呼吸暂停，特别是治疗肥胖症; 式（I）的化合物，其中R 7是羟基的化合物。
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公开(公告)号：US06489475B2
公开(公告)日：2002-12-03
申请号：US09784434
申请日：2001-02-15
申请人： Hiroshi Matsui , Shoji Kamiya
发明人： Hiroshi Matsui , Shoji Kamiya
IPC分类号： C07D20908
CPC分类号： C07D231/12 , A61K31/404 , A61K31/47 , C07D209/08 , C07D215/06 , C07D215/26 , C07D233/56 , C07D249/08 , C07D401/12 , Y10S514/824 , Y10S514/866
摘要： Heterocyclic derivatives of the formula (I) wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and method of producing them. Pharmaceutical compositions containing the heterocyclic derivative or a pharmaceutically acceptable salt thereof, particularly, ACAT inhibitors and lipoperoxidation inhibitors. The heterocyclic derivatives and pharmaceutically acceptable salts thereof of the present invention show superior ACAT inhibitory activity and lipoperoxidation inhibitory activity, and are useful as ACAT inhibitors and hyperlipemia inhibitors. To be specific, they are useful for the prevention and treatment of arteriosclerotic lesions of arteriosclerosis, hyperlipemia and diabetes, as well as ischemic diseases of brain, heart and the like.
摘要翻译： 式（I）的杂环衍生物，其中每个符号如说明书中所定义，其药学上可接受的盐及其制备方法。 含有杂环衍生物或其药学上可接受的盐，特别是ACAT抑制剂和脂质过氧化抑制剂的药物组合物。 本发明的杂环衍生物及其药学上可接受的盐显示出优异的ACAT抑制活性和脂质过氧化抑制活性，并且可用作ACAT抑制剂和高脂血症抑制剂。 具体而言，它们可用于预防和治疗动脉硬化，高脂血症和糖尿病的动脉硬化病变，以及脑，心脏等的缺血性疾病。
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公开(公告)号：US06339094B1
公开(公告)日：2002-01-15
申请号：US09463640
申请日：2000-01-27
IPC分类号： C07D20908
CPC分类号： C07D401/12 , C07D209/14 , C07D413/12 , C07D417/12
摘要： This invention provides a series of substituted propanamines useful as tachykinin receptor antagonists. This invention also provides methods employing these substituted propanamines as well as pharmaceutical formulations comprising these compounds.
摘要翻译： 本发明提供了一系列用作速激肽受体拮抗剂的取代丙胺。 本发明还提供了使用这些取代的丙胺的方法以及包含这些化合物的药物制剂。
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