Pyrido[3,2-e]pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them
    2.
    发明授权
    Pyrido[3,2-e]pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them 失效
    吡啶并[3,2-e]吡嗪,它们用作磷酸二酯酶10的抑制剂,以及它们的制备方法

    公开(公告)号:US07550465B2

    公开(公告)日:2009-06-23

    申请号:US11753207

    申请日:2007-05-24

    CPC classification number: C07D471/14

    Abstract: The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating diseases of mammals including a human which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 10 activity in the central nervous system. More particularly, the invention relates to the treatment of neurologic and psychiatric disorders, for example psychosis and disorders comprising cognitive deficits as symptoms.

    Abstract translation: 本发明涉及吡啶并[3,2-e]吡嗪,其制备方法涉及包含这些化合物的药物制剂和作为磷酸二酯酶10抑制剂的这些化合物的药物用途,作为治疗疾病的活性化合物 包括可以通过使用根据本发明的化合物来抑制中枢神经系统中磷酸二酯酶10活性的人的哺乳动物。 更具体地说,本发明涉及治疗神经和精神疾病,例如精神病和包括认知缺陷的症状作为症状。

    1,3,5-tribsubstituted indazole derivatives, processes for preparing, and
for pharmacological treatment therewith
    5.
    发明授权
    1,3,5-tribsubstituted indazole derivatives, processes for preparing, and for pharmacological treatment therewith 失效
    1,3,5-三取代吲唑衍生物,制备方法和用于药物治疗

    公开(公告)号:US5776932A

    公开(公告)日:1998-07-07

    申请号:US821740

    申请日:1997-03-20

    Abstract: 1,3,5-trisubstituted indazole derivatives of the formula ##STR1## wherein R1 is H, (b) a C.sub.1-6 straight or branched, substituted or unsubstituted alkyl residue, (c) a C.sub.3-7 cycloalkyl residue, (d) an unsustituted or substituted phenyl, naphthyl, anthranyl, or fluorenyl residue, (e) a quinolin-2-ylmethoxy, or pyridin-2-ylmethoxy residue; X is O, or a --NH, --NH--(C.dbd.O)--NH--, --NH--(C.dbd.O)--O--, --NH--(C.dbd.O)--, or --NH--CH.sub.2 --(C.dbd.O)-- residue; Y is O, or S; R.sub.2 is H; Z is a SO, SO.sub.2, --(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --O--, --O--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--, --(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--NH--, --NH--(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CHOH--, --CHOH--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CH.dbd.CH--, or --CH.dbd.CH--(CH.sub.2).sub.p -- residue, wherein p is between 1 and 6; A is a phenyl, naphthyl, anthranyl, fluorenyl, thiophenyl, pyridinyl, isoxazolyl, benzimidazolyl, benz�1,3!dioxolyl, pyrimidyl, pyrimidine-2,4-dionyl, quinolinyl, quinoxazolinyl, morpholinyl, or pyrrolidinyl residue; and, R.sub.3, R.sub.4, and R.sub.5, the same or different, are defined in the specification; and pharmaceutically acceptable salts, stereoisomers, racemates, racemic modifications, and enantiomers thereof. The invention also relates to specific compounds, processes for preparing and for treating an allergic, asthmatic, inflamed condition of a host, or for modulating the immune system of a host.

    Abstract translation: 式(I)的1,3,5-三取代吲唑衍生物其中R 1是H,(b)C 1-6直链或支链,取代或未取代的烷基残基,(c)C 3-7环烷基残基, (d)未取代或取代的苯基,萘基,蒽基或芴基残基,(e)喹啉-2-基甲氧基或吡啶-2-基甲氧基残基; X是O,或-NH,-NH-(C = O)-NH-,-NH-(C = O)-O-,-NH-(C = O) - 或-NH-CH 2 - C = O) - 残基; Y是O或S; R2为H; Z是SO,SO 2, - (CH 2)p - , - (CH 2)p O-,-O-(CH 2)p - , - (CH 2)p - (C = O) - , - (C = O) (CH2)p-, - (CH2)p-(C = O)-NH-,-NH-(C = O) - (CH2)p-, - (CH2)p-CHOH-,-CHOH-(CH2 )对 - , - (CH 2)p -CH = CH-或-CH = CH-(CH 2)p - 残基,其中p为1至6; A是苯基,萘基,蒽基,芴基,噻吩基,吡啶基,异恶唑基,苯并咪唑基,苯并[1,3]二氧杂环戊烯基,嘧啶基,嘧啶-2,4-二酰基,喹啉基,喹唑啉基,吗啉基或吡咯烷基残基; 和R3,R4和R5相同或不同,在本说明书中定义; 和其药学上可接受的盐,立体异构体,外消旋体,外消旋体和其对映异构体。 本发明还涉及具体化合物,用于制备和治疗宿主的过敏性,哮喘,发炎状况或调节宿主免疫系统的方法。

    Selective congestion control mechanism for information networks
    6.
    发明授权
    Selective congestion control mechanism for information networks 失效
    信息网络选择性拥塞控制机制

    公开(公告)号:US5768258A

    公开(公告)日:1998-06-16

    申请号:US624597

    申请日:1996-04-17

    Abstract: This invention is an implementation of a congestion control mechanism, especially for ATM networks supporting data services or other nonreserved bandwidth traffic, e.g. in multimedia applications. It reacts immediately upon detection of a traffic bottleneck by selectively and temporarily holding back the data traffic that is to pass the bottleneck (5). A congested node (3) transmits congestion notifications (36) containing routing label information and deferment information to upstream nodes (2), thus enabling selective, temporary throttling action. If congestions persist, further notifications may be spread backwards step by step, eventually reaching the sources. A specific implementation is given for PRIZMA type switching nodes.

    Abstract translation: PCT No.PCT / EP93 / 02937 371日期:1996年4月17日 102(e)日期1996年4月17日PCT提交1993年10月23日PCT公布。 公开号WO95 / 11557 日期1995年04月27日本发明是拥塞控制机制的实现,特别是对于支持数据业务或其他非保留带宽业务的ATM网络,例如, 在多媒体应用中。 通过选择性地和临时地阻止通过瓶颈(5)的数据流量,在检测到流量瓶颈时立即作出反应。 拥塞节点(3)将包含路由标签信息和延迟信息的拥塞通知(36)发送到上游节点(2),从而实现选择性的临时限制动作。 如果拥塞持续存在,则进一步的通知可能会逐步向后传播,最终到达源。 给PRIZMA型交换节点给出了具体的实现。

    Apparatus for impregnating reinforcing fiber materials with a resinous
binder material
    7.
    发明授权
    Apparatus for impregnating reinforcing fiber materials with a resinous binder material 失效
    用树脂粘合剂材料浸渍增强纤维材料的装置

    公开(公告)号:US4530733A

    公开(公告)日:1985-07-23

    申请号:US559885

    申请日:1984-01-25

    CPC classification number: D06B19/0017 C08J5/24 D06B1/14 Y10T156/1715

    Abstract: Reinforcing fiber materials such as rovings, webbings, and other fiber maials are impregnated with a resinous binder material in such a manner that gaseous inclusions are avoided whereby a surprising increase in the strength of the fiber compound material is achieved. For this purpose the liquid resinous binder material is applied substantially only to one side of the reinforcing material which is then moved through an absorbing zone in which the liquid resinous binder material penetrates the reinforcing material substantially completely as a result of a predetermined residence time and temperature in the absorbing zone. Gas inclusions are removed by adsorption and/or by expulsion. The gas adsorbing and expulsion zone is a chamber in which a plurality of guide rollers are arranged so as to cause the impregnated material to repeatedly reverse its moving direction, whereby the sequential and repeated penetration of the reinforcing material by the resinous material and the removal of gas inclusions are enhanced. Further, the precise weight ratio adjustment of resin to fiber material is enhanced by moving the impregnated material in a substantially vertical orientation through a fulling station. The vertical orientation facilitates the flow off of excess resin.

    Abstract translation: 加强纤维材料如粗纱,网带和其它纤维材料用树脂粘合剂材料浸渍,以避免气态夹杂物,从而实现纤维复合材料的强度令人惊讶的增加。 为此,液态树脂粘合剂材料基本上仅施加到增强材料的一侧,然后通过吸收区域移动,其中液态树脂粘合剂材料基本上完全渗透加固材料,这是由于预定的停留时间和温度 在吸收区。 通过吸附和/或通过排出除去气体夹杂物。 气体吸附和排出区是其中布置多个导辊以使浸渍材料反复地反转其移动方向的室,由此通过树脂材料的顺序和重复的增强材料的渗透以及去除 气体夹杂物增强。 此外,通过使浸渍的材料以大致垂直的方向移动通过充气站,来提高树脂与纤维材料的精确重量比调整。 垂直方向有助于流过多余的树脂。

    Connecting rod for an engine
    8.
    发明授权
    Connecting rod for an engine 失效
    发动机连杆

    公开(公告)号:US4414860A

    公开(公告)日:1983-11-15

    申请号:US217040

    申请日:1980-12-16

    CPC classification number: F16C7/026 B60G2206/11 B60G2206/7101 Y10T74/2162

    Abstract: A connecting rod assembly includes an axially elongated member with openi spaced apart in the axial direction. The axis of the openings extend perpendicularly to the axis of the member. A connecting rod shaft extends in the axial direction of the member between the two openings. A fiber reinforced plastics material belt extends around the first and second openings and also around the connecting rod shaft. Oblique cuts are formed in the belt on opposite sides of the connecting rod shaft adjacent one of the openings. A highly heat-resistant adhesive is placed in the oblique cuts for splicing the belt together.

    Abstract translation: 连杆组件包括沿轴向间隔开的开口的轴向细长构件。 开口的轴线垂直于构件的轴线延伸。 连杆轴在两个开口之间沿构件的轴向方向延伸。 纤维增强塑料材料带围绕第一和第二开口以及围绕连杆轴延伸。 在与连接杆轴相邻的一个开口的相对侧上的皮带中形成斜切口。 将高耐热粘合剂放置在倾斜切口中,以将皮带拼接在一起。

    Shear transfer element
    9.
    发明授权
    Shear transfer element 失效
    剪切转印元件

    公开(公告)号:US4201815A

    公开(公告)日:1980-05-06

    申请号:US972223

    申请日:1978-12-22

    Abstract: Shear transfer elements can be formed by winding or weaving unidirectional fibers on a support structure. In a winding operation the support structure consists of two intersecting planes of winding mandrels with the planes arranged in angularly spaced relation. Each plane has two pair of mandrels with the mandrels in each pair located on the opposite sides of the line of intersection between the two planes. After the fibers are wound on the mandrels, each mandrel is axially disposed in the opposite direction relative to the other mandrel in the pair and also to the adjacent mandrel in the other pair in the same plane. Next, the fibers are pressed to form the shear transfer element. In a weaving operation, the support structure consists of a pair of pivotally interconnected frames. The fibers are woven onto holders on the sides of each frame extending parallel to the pivot axis of the frames. After placement of the fibers on the frames, the frames are pivoted apart and the fibers are pressed to form the shear transfer element.

    Abstract translation: 剪切转印元件可以通过在支撑结构上缠绕或编织单向纤维来形成。 在卷绕操作中,支撑结构由缠绕心轴的两个相交平面组成,其中平面以角度间隔的关系布置。 每个平面具有两对心轴,其中每对中的心轴位于两个平面之间的相交线的相对侧上。 在纤维缠绕在心轴上之后,每个心轴相对于该对中的另一个心轴在相反方向上轴向地设置,并且在同一平面中的另一对中相邻的心轴。 接下来,将纤维压制以形成剪切传递元件。 在编织操作中,支撑结构由一对枢转互连的框架组成。 纤维被编织到平行于框架的枢转轴线延伸的每个框架的侧面上的保持器上。 在将纤维放置在框架上之后,框架枢转分开,并且将纤维压制以形成剪切传递元件。

    Pyrido[3,2-e]pyrazines, their use as inhibitors of phospohodiesterase 10, and processes for preparing them
    10.
    发明申请
    Pyrido[3,2-e]pyrazines, their use as inhibitors of phospohodiesterase 10, and processes for preparing them 审中-公开
    吡啶并[3,2-e]吡嗪,它们用作磷酸二酯酶10的抑制剂,以及它们的制备方法

    公开(公告)号:US20090239874A1

    公开(公告)日:2009-09-24

    申请号:US12454537

    申请日:2009-05-19

    CPC classification number: C07D471/14

    Abstract: The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating diseases of mammals including a human which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 10 activity in the central nervous system. More particularly, the invention relates to the treatment of neurologic and psychiatric disorders, for example psychosis and disorders comprising cognitive deficits as symptoms.

    Abstract translation: 本发明涉及吡啶并[3,2-e]吡嗪,其制备方法涉及包含这些化合物的药物制剂和作为磷酸二酯酶10抑制剂的这些化合物的药物用途,作为治疗疾病的活性化合物 包括可以通过使用根据本发明的化合物来抑制中枢神经系统中磷酸二酯酶10活性的人的哺乳动物。 更具体地说,本发明涉及治疗神经和精神疾病,例如精神病和包括认知缺陷的症状作为症状。

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