公开(公告)号：US5763404A

公开(公告)日：1998-06-09

申请号：US466333

申请日：1995-06-06

申请人： Karl A. Folkers ,  Cyril Y. Bowers ,  Anders Ljungqvist ,  Pui-Fun Louisa Tang ,  Minoru Kubota ,  Dong-Mei Feng

发明人： Karl A. Folkers ,  Cyril Y. Bowers ,  Anders Ljungqvist ,  Pui-Fun Louisa Tang ,  Minoru Kubota ,  Dong-Mei Feng

IPC分类号： A61K38/04 ,  A61K38/00 ,  A61P15/00 ,  C07K7/06 ,  C07K7/23 ,  A61K38/24

CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S930/13

摘要： Antide is the decapeptide, N-Ac-D-2-Nal,D-pClPhe, D-3-Pal, Ser,NicLys, D-NicLys, Leu, ILys, Pro, D-Ala,NH.sub.2 which is an antagonist of luteinizing hormone releasing hormone (LHRH). This decapeptide, like others of the present invention, has high antiovulatory activity (AOA) and releases negligible histamine. Antide is scheduled for scale-up, safety testing and evaluation in the experimental primate and in clinical medicine. Numerous other peptides having structures related to Antide were prepared and tested. These peptides had variations primarily in positions 5, 6, 7, and 8. Of these, N-Ac-D-2-Nal, D-pClPhe,D-3-Pal,Ser,PicLys,cis-DPzACAla,Leu,ILys,Pro,D-Ala-NH.sub.2 was one of the most potent and had higher antiovulatory activity than Antide, i.e. 73%/0.25 ug and 100%/0.5 ug vs. 36%/0.5 ug and 100%/1.0 ug. Antide showed significant, (p

公开(公告)号：US5470947A

公开(公告)日：1995-11-28

申请号：US371552

申请日：1989-06-26

申请人： Karl A. Folkers ,  Anders Ljungqvist ,  Dong-Mei Feng ,  Minoru Kubota ,  Pui-Fun L. Tang ,  Cyril Y. Bowers

发明人： Karl A. Folkers ,  Anders Ljungqvist ,  Dong-Mei Feng ,  Minoru Kubota ,  Pui-Fun L. Tang ,  Cyril Y. Bowers

IPC分类号： A61K38/04 ,  A61K38/00 ,  A61P15/00 ,  C07K7/06 ,  C07K7/23

CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S930/13

摘要： Antide is the decapeptide, N--Ac--D--2--Nal,D--pClPhe, D--3--Pal, Ser,NicLys, D--NicLys, Leu, ILys, Pro, D--Ala,NH.sub.2 which is an antagonist of luteinizing hormone releasing hormone (LHRH). This decapeptide, like others of the present invention, has high antiovulatory activity (AOA) and releases negligible histamine. Antide is scheduled for scale-up, safety testing and evaluation in the experimental primate and in clinical medicine. Numerous other peptides having structures related to Antide were prepared and tested. These peptides had variations primarily in positions 5, 6, 7, and 8. Of these, N--Ac--D--2--Nal, D--pClPhe,D--3--Pal,Ser,PicLys,cis--DpzACAla, Leu,ILys,pro,D--Ala--NH.sub.2 was one of the most potent and had higher antiovulatory activity than Antide, i.e. 73%/0.25 ug and 100%/0.5 ug vs. 36%/0.5 ug and 100%/1.0 ug. Antide showed significant, (p

摘要翻译： Antide是黄素化拮抗剂的十肽，N-Ac-D-2-Nal，D-pClPhe，D-3-Pal，Ser，NicLys，D-NicLys，Leu，ILys，Pro，D-Ala，NH2 激素释放激素（LHRH）。 这种十肽与本发明的其它物质一样，具有高的抗疟药活性（AOA），释放出可忽略的组胺。 Antide计划在实验灵长类动物和临床医学中进行放大，安全测试和评估。 制备并测试了许多具有与Antide有关的结构的其它肽。 这些肽主要在第5,6,7和8号位置有变化。其中，N-Ac-D-2-Nal，D-pClPhe，D-3-Pal，Ser，PicLys，cis-DpzACAla，Leu，ILys ，pro-D-Ala-NH2是最有效的并且具有比Antide更高的抗肿瘤活性，即73％/ 0.25ug和100％/ 0.5ug，而36％/ 0.5ug和100％/1.0μg。 当在50ng激动剂[D-3-Qal6] -LHRH之前以10μg，44小时的剂量注射时，Antide显示显着的（p <0.001）作用持续时间。 Antide在600ug（73％）和1200μg（100％）下显示口服AOA，水和玉米油口服制剂之间的差异可以忽略不计。

公开(公告)号：US4935491A

公开(公告)日：1990-06-19

申请号：US88431

申请日：1987-08-24

申请人： Karl Folkers ,  Anders Ljungqvist ,  Dong-Mei Feng ,  Cyril Y. Bowers ,  Pui-Fun L. Tang ,  Minoru Kubota

发明人： Karl Folkers ,  Anders Ljungqvist ,  Dong-Mei Feng ,  Cyril Y. Bowers ,  Pui-Fun L. Tang ,  Minoru Kubota

IPC分类号： A61K38/04 ,  A61K38/00 ,  A61P15/00 ,  C07K7/06 ,  C07K7/23

CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S930/13

摘要： The objective of the research was the achievement of antagonists of the luteinizing hormone releasing hormone (LHRH) which would have adequate antagonistic activity to prevent ovulation, and yet would not have a pronounced structural feature to release a histamine, in vivo. Some existing antagonists of LHRH produced edema of the face and extremities in rats. This recent recognition of the edematogenic and anaphylactoid activities of an antagonist of LHRH necessitated new structural changes if such antagonists were to be considered for potential use as contraceptive agents in the human. Consequently, 57 peptides have been designed, synthesized and bioassayed toward achieving a potent antagonist which releases negligible histamine. Since there was no predictable structural sequence which offered assurance of such achievement, it was necessary to design, synthesize and bioassay a very large number of peptides having diverse structural changes toward ultimately discovering an antagonist with the necessary potency of antiovulatory activity and the necessary negligible release of histamine. Ultimately, this objective was achieved, and this application describes the diverse and unpredictable many positive steps which finally led to the objectives.

摘要翻译： 研究的目标是实现促黄体激素释放激素（LHRH）的拮抗剂，其具有足够的拮抗活性以防止排卵，并且在体内不具有释放组胺的显着结构特征。 一些现有的LHRH拮抗剂在大鼠中产生了四肢的水肿。 最近对LHRH拮抗剂引起的血液发生和过敏性活性的认识需要新的结构改变，如果这样的拮抗剂被认为可能用作人类的避孕药。 因此，已经设计，合成和生物测定了57种肽，以实现释放可忽略的组胺的有效拮抗剂。 由于没有可预测的结构序列来提供这种成就的保证，所以有必要设计，合成和生物测定大量具有不同结构变化的肽，以最终发现拮抗剂具有必需的抗疟药活性和必需的可忽略的释放 的组胺。 最终，这个目标已经实现，这个应用程序描述了最终导致目标的多样化和不可预测的许多积极步骤。

公开(公告)号：US4721775A

公开(公告)日：1988-01-26

申请号：US771546

申请日：1985-08-26

申请人： Karl Folkers ,  Cyril Y. Bowers ,  Pui-Fun L. Tang ,  Minoru Kubota

发明人： Karl Folkers ,  Cyril Y. Bowers ,  Pui-Fun L. Tang ,  Minoru Kubota

IPC分类号： A61K38/00 ,  C07K7/23 ,  C07K7/20

CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S930/13

摘要： The chemical structure of the luteinizing hormone releasing hormone (LHRH) was elucidatd in 1971. Since then, a very large number of international investigators synthesized more than 100 monosubstituted and about 14 disubstituted analogs of LHRH. All of these analogs were synthesized from natural amino acids having the L-configuration. Not one of these approximately 114 analogs showed agonist activity equivalent to that of LHRH. Two of the 114 were about 60% as active, and neither one has had any utility. We have investigated the six individual L-amino acids which occur in positions 5, 7, and 8 of the four naturally occurring LHRH's which exist in porcine/ovine, salmon, and chicken tissue. There are a total of 16 peptides with these structural features, and we have discovered that not only one but five of these peptides are not only equivalent in certain assays in activity to LHRH, but that two of the five are surprisingly superior to LHRH in activity, and that two of the five have a unique and unpredictable dissociation of activity for the release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). These five peptides are:A. p-Glu His Trp Ser His Gly Leu Arg Pro Gly-NH.sub.2,B. p-Glu His Trp Ser His Gly Trp Arg Pro Gly-NH.sub.2,C. p-Glu His Trp Ser His Gly Trp Gln Pro Gly-NH.sub.2,D. p-Glu His Trp Ser His Gly Trp Leu Pro Gly-NH.sub.2,E. p-Glu His Trp Ser Tyr Gly Trp Arg Pro Gly-NH.sub.2,Peptide C might be the naturally occurring as FSHRH, because of its dissociated release of LH and FSH. The discovery for the first time of decapeptides with L-amino acids equal to or more potent than LHRH was based on about 14 years of background. Our new peptides are particularly useful in medical fields for pituitary stimulation and inhibition, for enhancement or inhibition of fertility in humans and animals, for the therapy of hormone-dependent tumors, for special effects on sexual behavior in humans and animals, and for design of new categories of superagonists and antagonists. Extrapituitary effects by these new peptides may be observed on the central nervous system or reproductive organs of humans and animals that are different from those of LHRH. The latter will be especially true if some of these new peptides are found to be native peptides such as FSH-RH or the LHRH-like peptides that have been detected in the gonads that are yet to be identified. The reason for believing this projection is possible is that some of these peptides have high or unique LH and FSH releasing activity in the LHRH radioreceptor assay, as exemplified by the biological activities of peptide C.

公开(公告)号：US09281880B2

公开(公告)日：2016-03-08

申请号：US14239088

申请日：2012-08-13

申请人： Alvaro Ruiz Delgado ,  Takashi Onodera ,  Hiromichi Tomeba ,  Hiroshi Nakano ,  Minoru Kubota

发明人： Alvaro Ruiz Delgado ,  Takashi Onodera ,  Hiromichi Tomeba ,  Hiroshi Nakano ,  Minoru Kubota

IPC分类号： H04W4/00 ,  H04B7/04 ,  H04B7/06 ,  H04L25/03

CPC分类号： H04B7/0456 ,  H04B7/0452 ,  H04B7/0689 ,  H04L2025/03802

摘要： A wireless reception device is notified of whether a multi-user MIMO signal transmitted from a wireless transmission device has undergone linear precoding or non-linear precoding without increasing the amount of control information. A wireless transmission device having a plurality of transmit antennas 303, for transmitting spatially multiplexed signals to a plurality of wireless reception devices includes a group construction unit 307 configured to classify the wireless reception devices into a plurality of groups and to determine a precoding scheme for each of the groups, a selection unit 315 configured to select one group from among the groups, and a precoding unit 323 configured to precode transmit data addressed to each of wireless reception devices belonging to the selected group, using a precoding scheme determined for the selected group.

摘要翻译： 从无线发送装置发送的多用户MIMO信号是否已经经历了线性预编码或非线性预编码，而不增加控制信息量，通知无线接收装置。 具有用于将空间复用信号发送到多个无线接收装置的多个发送天线303的无线发送装置包括：组构建单元307，被配置为将无线接收装置分类为多个组，并且确定每个 组成的选择单元315，被配置为从组中选择一组;以及预编码单元323，被配置为使用为所选择的组确定的预编码方案来对寻址到​​属于所选择的组的无线接收装置中的每一个的发送数据进行预编码 。

公开(公告)号：US09209874B2

公开(公告)日：2015-12-08

申请号：US13882556

申请日：2011-10-24

申请人： Takashi Onodera ,  Hiromichi Tomeba ,  Shimpei To ,  Hiroshi Nakano ,  Alvaro Ruiz Delgado ,  Minoru Kubota

发明人： Takashi Onodera ,  Hiromichi Tomeba ,  Shimpei To ,  Hiroshi Nakano ,  Alvaro Ruiz Delgado ,  Minoru Kubota

IPC分类号： H04B7/02 ,  H04B7/04 ,  H04B7/06 ,  H04L25/03

CPC分类号： H04B7/0456 ,  H04B7/0417 ,  H04B7/0632 ,  H04B7/0689 ,  H04B7/0697 ,  H04L25/03942

摘要： The present invention switches an interference suppression system between a linear precoding and a nonlinear precoding in accordance with a communication environment. A wireless transmission apparatus is provided with a plurality of transmission antenna units (303), and multiplexes spatially and transmits a plurality of series of data with respect to at least one wireless reception apparatus, and includes a selection unit (307) configured to select any one precoding system from a plurality of types of precoding systems and a precoding unit (315) configured to carry out precoding with respect to the plurality of series of data using the selected precoding system. In addition, the selection unit selects either of a first precoding system carrying out linear processing with respect to the plurality of series of data or a second precoding system carrying out nonlinear processing with respect to the plurality of series of data.

摘要翻译： 本发明根据通信环境在线性预编码和非线性预编码之间切换干扰抑制系统。 一种无线发送装置具备多个发送天线单元（303），在空间上进行多路复用，并相对于至少一个无线接收装置发送多个数据序列，并具有选择单元（307） 一种来自多种类型的预编码系统的预编码系统和预编码单元（315），其被配置为使用所选择的预编码系统对多个数据系列进行预编码。 此外，选择单元选择对多个数据系列进行线性处理的第一预编码系统或对多个数据系列执行非线性处理的第二预编码系统。

公开(公告)号：US09185577B2

公开(公告)日：2015-11-10

申请号：US13700754

申请日：2011-05-13

申请人： Hiromichi Tomeba ,  Minoru Kubota ,  Takashi Onodera ,  Shimpei To ,  Kozue Hirata ,  Hiroshi Nakano

发明人： Hiromichi Tomeba ,  Minoru Kubota ,  Takashi Onodera ,  Shimpei To ,  Kozue Hirata ,  Hiroshi Nakano

IPC分类号： H04W24/02 ,  H04B7/04 ,  H04L1/06 ,  H04L25/497 ,  H04J11/00 ,  H04L27/26

CPC分类号： H04W24/02 ,  H04B7/0452 ,  H04J11/0033 ,  H04L1/0625 ,  H04L1/0656 ,  H04L25/4975 ,  H04L27/2601

摘要： To realize transmission performances equivalent to those of an MU-MIMO BLAST ZF-THP system without increasing a signal processing amount in a base station apparatus in a downlink MU-MIMO transmission system. A transmission apparatus is provided with a plurality of transmission antennas, generates a transmission signal addressed to each reception apparatus based on information indicating spatial correlation of channels to and from a plurality of reception apparatuses, space-multiplexes the generated each transmission signal in the same wireless resource, and transmits it to each reception apparatus. The transmission apparatus includes: an ordering determination part 601 which determines an order in which a transmission signal addressed to each reception apparatus is generated based on information indicating spatial correlation of channels; a linear filter generation part 603 which generates a linear filter based on the determined order; a THP part 605 which performs a THP process by using the determined order and the linear filter; and a linear filter multiplication part 607 which multiplies an output of the THP part 605 by the linear filter.

摘要翻译： 实现与MIMO-MIMO BLAST ZF-THP系统相当的传输性能，而不增加下行MU-MIMO传输系统中的基站装置中的信号处理量。 发送装置具有多个发送天线，基于表示与多个接收装置的频道的频道的空间相关性的信息，生成发往各接收装置的发送信号，对同一无线电中产生的各发送信号进行空间复用 资源，并将其发送到每个接收装置。 传输装置包括：排序确定部分601，其基于指示信道的空间相关性的信息来确定寻址到每个接收装置的发送信号的顺序; 线性滤波器生成部603，其基于所确定的次序生成线性滤波器; 通过使用确定的顺序执行THP处理的THP部件605和线性滤波器; 线性滤波器乘法部607，其将THP部605的输出与线性滤波器相乘。

公开(公告)号：US09166658B2

公开(公告)日：2015-10-20

申请号：US13877368

申请日：2011-10-03

申请人： Shimpei To ,  Takashi Onodera ,  Hiroshi Nakano ,  Hiromichi Tomeba ,  Minoru Kubota ,  Kozue Hirata ,  Alvaro Ruiz Delgado

发明人： Shimpei To ,  Takashi Onodera ,  Hiroshi Nakano ,  Hiromichi Tomeba ,  Minoru Kubota ,  Kozue Hirata ,  Alvaro Ruiz Delgado

IPC分类号： H04W4/00 ,  H04B7/04 ,  H04B7/06

CPC分类号： H04B7/0417 ,  H04B7/0452 ,  H04B7/065

摘要： A wireless communication system in which a base station apparatus having a plurality of transmission antennas and one or more terminal apparatuses communicate with each other is provided with at least two methods of a first feedback method and a second feedback method regarding propagation path information at the time of reception. In accordance with a communication condition between the base station apparatus and the terminal apparatus, or the function of the terminal apparatus, the terminal apparatus performs feedback by one of the two methods of the first feedback method and the second feedback method. The base station apparatus performs spatial multiplexing transmission on the basis of the propagation path information that has been fed back. Thus, in a system in which CSI is fed back for MIMO transmission, desired transmission characteristics can be efficiently obtained.

摘要翻译： 具有多个发送天线和一个以上的终端装置的基站装置相互通信的无线通信系统具备关于该时刻的传播路径信息的第一反馈方法和第二反馈方法的至少两种方法 的接待。 根据基站装置与终端装置之间的通信条件或终端装置的功能，终端装置通过第一反馈方法和第二反馈方法的两种方法之一进行反馈。 基站装置根据反馈的传播路径信息进行空间复用传输。 因此，在反馈用于MIMO传输的系统中，可以有效地获得期望的传输特性。

公开(公告)号：US08644424B2

公开(公告)日：2014-02-04

申请号：US13201234

申请日：2010-02-12

申请人： Takashi Yoshimoto ,  Minoru Kubota ,  Naoki Okamoto ,  Hiroshi Suzuki ,  Kazuhiko Fukawa ,  Satoshi Suyama

发明人： Takashi Yoshimoto ,  Minoru Kubota ,  Naoki Okamoto ,  Hiroshi Suzuki ,  Kazuhiko Fukawa ,  Satoshi Suyama

IPC分类号： H03D3/00

CPC分类号： H04L27/3863 ,  H04L27/0014 ,  H04L27/2337 ,  H04L2027/0026

摘要： A receiver apparatus receiving a quadrature-modulated, modulated wave, includes: a real-zero signal generator for adding a sinusoidal wave to the modulated wave to generate a real-zero signal; an in-phase and quadrature component detector for extracting an in-phase component signal and a quadrature component signal from the real-zero signal; a real-zero sequence generator for generating a real-zero sequence as a sequence of time points at which the in-phase component and quadrature component signals become zero; and a signal reconstruction unit for reproducing the in-phase component and quadrature component from the real-zero sequence. It is possible to provide a receiving apparatus that enables decoding of a received signal with high precision even when sufficient linearity cannot be secured in the analog circuit of the receiver apparatus.

摘要翻译： 一种接收正交调制调制波的接收机装置，包括：实零信号发生器，用于将正弦波加到调制波上以产生实零信号; 同相和正交分量检测器，用于从实零信号中提取同相分量信号和正交分量信号; 用于产生实零序列作为同相分量和正交分量信号变为零的时间点序列的实零序列发生器; 以及信号重建单元，用于从实零序列再现同相分量和正交分量。 即使在接收装置的模拟电路中不能确保足够的线性度的情况下，也能够提供能够高精度地对接收信号进行解码的接收装置。

公开(公告)号：US20130121277A1

公开(公告)日：2013-05-16

申请号：US13700756

申请日：2011-05-27

申请人： Shimpei To ,  Takashi Onodera ,  Kozue Hirata ,  Hiroshi Nakano ,  Hiromichi Tomeba ,  Minoru Kubota

发明人： Shimpei To ,  Takashi Onodera ,  Kozue Hirata ,  Hiroshi Nakano ,  Hiromichi Tomeba ,  Minoru Kubota

IPC分类号： H04B7/06

CPC分类号： H04B7/0697 ,  H04B7/0617

摘要： When signals received by receiving antennas included in each terminal are subjected to MMSE combining, it is configured that each terminal is able to grasp position of desired signal in signal vector obtained after combining. A base station 100 receives by a receiving antenna 23 from the terminal apparatus channel state information between a transmitting antenna 16 and spatial multiplexing object antennas included in each terminal apparatus. A transmit weight calculation unit 19 calculates a transmit weight for performing spatial multiplexing transmission to the terminal apparatus based on the channel state information. Transmit weight multiplication unit s 12 and 18 multiplies an information signal addressed to each terminal apparatus to be performed spatial multiplexing by the transmit weight. A signal multiplexing unit 13 multiplexes the information signal multiplied by the transmit weight and an information to specify the information signal that needs to be demodulated by each terminal apparatus.

摘要翻译： 当通过每个终端中包含的接收天线接收到的信号进行MMSE组合时，配置为每个终端能够在组合后获得的信号向量中掌握期望信号的位置。 基站100由发送天线16和各终端装置中包含的空间复用对象天线之间的终端装置信道状态信息由接收天线23接收。 发送权重计算单元19基于信道状态信息计算用于对终端装置执行空间复用传输的发送权重。 发送权重乘法单元12和18将寻址到每个终端设备的信息信号乘以发送权重进行空间复用。 信号复用单元13将乘以发送权重的信息信号和用于指定每个终端装置需要解调的信息信号的信息进行复用。