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    • 154. 发明授权
    • Thrombin receptor antagonists
    • 凝血酶受体拮抗剂
    • US07713999B2
    • 2010-05-11
    • US11733635
    • 2007-04-10
    • Samuel ChackalamannilMartin C. ClasbyWilliam J. GreenleeYuguang WangYan XiaEnrico P. VeltriMariappan V. Chelliah
    • Samuel ChackalamannilMartin C. ClasbyWilliam J. GreenleeYuguang WangYan XiaEnrico P. VeltriMariappan V. Chelliah
    • A61K31/443C07D307/78
    • C07D405/06C07D405/14C07D417/14
    • Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond;  represents an optional double bond, n is 0-2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1-C6)alkyl, (C3-C8)cycloalkyl, —OH, (C1-C6)alkoxy, R27-aryl(C1-C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms, Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
    • 具有下式的杂环取代的三环或其药学上可接受的盐,其中:虚线表示任选的单键; 表示可选的双键,n为0-2; Q是环烷基,任选被R 13和R 14取代; R 13和R 14独立地选自(C 1 -C 6)烷基,(C 3 -C 8)环烷基,-OH,(C 1 -C 6)烷氧基,R 27 - 芳基(C 1 -C 6)烷基,杂芳基,杂芳基烷基,杂环基,杂环基烷基,卤素 和卤代烷基; 或R 13和R 14一起形成3-6个原子的螺环或异环环,Het是单或双环任选取代的杂芳基; 和B是键,亚烷基或任选取代的亚烯基或亚炔基,其中剩余的取代基如说明书中所定义,以及含有它们的药物组合物和治疗与血栓形成,动脉粥样硬化,再狭窄有关的疾病的方法, 高血压,心绞痛,心律失常,心力衰竭和癌症。 还要求与其它心血管药物联合治疗。
    • 159. 发明授权
    • Adenosine A2a receptor antagonists
    • 腺苷A2a受体拮抗剂
    • US06630475B2
    • 2003-10-07
    • US09865071
    • 2001-05-24
    • Bernard R. NeustadtNeil LindoWilliam J. GreenleeDeen TulshianLisa S. SilvermanYan XiaCraig D. BoyleSamuel Chackalamannil
    • Bernard R. NeustadtNeil LindoWilliam J. GreenleeDeen TulshianLisa S. SilvermanYan XiaCraig D. BoyleSamuel Chackalamannil
    • C07D40314
    • C07D487/14
    • Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted  m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—,  phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula I.
    • 具有结构式I的化合物或其药学上可接受的盐,其中R是任选取代的苯基,环烯基或杂芳基; X是亚烷基或-C(O)CH 2 - ; Y是-N(R 2)CH 2 CH 2 N(R) 3) - ,-OCH 2 CH 2 N(R 2) - , - O - , - S - , - CH 2 S - , - (CH 2)2 -NH-或任选地被取代的n和n是2-3,并且Q是氮 或任选取代的碳; 和Z是任选取代的苯基,苯基烷基或杂芳基,二苯基甲基,R 6 -C(O) - ,R 6 -SO 2 - ,R 6 -OC(O) - ,R 7 -N C(O) - ,R 7 -N(R 8)-C(S) - ,苯基-CH(OH) - 或苯基-C(= NOR 2) ; 或当Q为CH时,为苯基氨基或吡啶基氨基; 或Z和Y一起是取代的哌啶基或取代的苯基; 和R 2,R 3,R 6,R 7和R 8如说明书中所定义,其用于治疗帕金森病,单独使用或与其它药剂组合 用于治疗帕金森病,以及包含它们的药物组合物; 还公开了制备可用于制备式I化合物的中间体的方法。
    • 160. 发明授权
    • Rotor for a dynamoelectric machine
    • 转子用于电动机
    • US6091168A
    • 2000-07-18
    • US218653
    • 1998-12-22
    • David G. HalseyHassan MansirRobert GrennanWilliam J. GreenleeDam Nguyen
    • David G. HalseyHassan MansirRobert GrennanWilliam J. GreenleeDam Nguyen
    • H02K1/24H02K1/32H02K9/02H02K9/00
    • H02K1/32H02K1/24H02K9/02
    • Losses in efficiency of operation of a dynamoelectric machine as a result of eddy current losses and poor coolant efficiency and/or disruption of the magnetic circuit in a rotor by coolant passages is avoided in a dynamoelectric machine including a stator (18) in which a rotor (16) is journaled. The rotor includes a stack (16) of thin laminations (17) made of a ferromagnetic material to define a rotor body. The rotor body includes a plurality of equally angularly spaced poles (58) separated by recesses (64). Coolant passages (76) located in the rotor at or just radially inward of the base (72) of each pole (58) and substantially radially outward of the rotational axis (56) of the rotor (14) to maximize cooling efficiency of the poles (58) without disrupting the magnetic circuit in the rotor. Slots (80) are placed in the tips (70) of the poles (58) of selected laminations (17) and extend generally radially inward to reduce eddy current losses.
    • 在包括定子(18)的电动机中避免了由于涡流损失和冷却剂效率差和/或由冷却剂通道引起的转子中的磁路的破坏导致的电动机的操作效率的损失,其中转子 (16)记录。 转子包括由铁磁材料制成的薄的叠片(17)的叠层(16),以形成转子体。 转子主体包括由凹部(64)分开的多个等角度间隔的极(58)。 冷却剂通道(76)位于转子的每一极(58)的基部(72)处或位于转子的径向内侧,并且基本上位于转子(14)的旋转轴线(56)的径向外侧,以使极点的冷却效率最大化 (58),而不破坏转子中的磁路。 狭槽(80)被放置在所选择的叠片(17)的极(58)的尖端(70)中,并且大致径向向内延伸以减少涡流损耗。