公开(公告)号：US08793058B2

公开(公告)日：2014-07-29

申请号：US13121325

申请日：2010-10-12

申请人： Shuntaro Okazaki ,  Satoshi Yoshizaki ,  Masashi Shibayama ,  Kaoru Shokatsu ,  Hajime Kawakami

发明人： Shuntaro Okazaki ,  Satoshi Yoshizaki ,  Masashi Shibayama ,  Kaoru Shokatsu ,  Hajime Kawakami

IPC分类号： B60T7/12

CPC分类号： F02D11/105 ,  F02D37/02 ,  F02D41/0002 ,  F02D41/1475 ,  F02D2041/1431 ,  F02D2041/1432 ,  F02P5/1504 ,  Y02T10/42 ,  Y02T10/46

摘要： A control device for an internal combustion engine provided by the present invention is a control device which can satisfy both a requirement relating to exhaust gas performance of the internal combustion engine and a requirement relating to operation performance by properly regulating a change speed of a required air-fuel ratio, in the internal combustion engine which uses torque and an air-fuel ratio as control variables. The control device receives the requirement relating to the exhaust gas performance of the internal combustion engine, and calculates an air-fuel ratio which satisfies the requirement as a required air-fuel ratio. When a predetermined reduction condition is not satisfied, an original required air-fuel ratio is directly determined as a final required air-fuel ratio. However, when the reduction condition is satisfied, the change speed is reduced by processing the signal of the original required air-fuel ratio, and determines the required air-fuel ratio with the change speed reduced as the final required air-fuel ration. The reduction condition includes a condition that the change amount of the original required air-fuel ratio, in more detail, a change amount per calculation period is larger than a predetermined air-fuel ratio change determination value.

摘要翻译： 本发明提供的用于内燃机的控制装置是一种控制装置，其能够通过适当地调节所需空气的变速来满足与内燃机的废气性能有关的要求和与运行性能有关的要求 - 燃料比，在使用转矩和空燃比作为控制变量的内燃机中。 控制装置接收与内燃机的排气性能有关的要求，并且计算满足要求的空燃比作为所需的空燃比。 当不满足预定的减少条件时，原始所需的空燃比被直接确定为最终所需的空燃比。 然而，当满足减速条件时，通过处理原始所需空燃比的信号来降低变速，并且随着最终所需空燃比降低变速而确定所需的空燃比。 还原条件包括原始所需空燃比的变化量，更详细地说，每个计算周期的变化量大于预定的空燃比变化判定值的条件。

公开(公告)号：US07521454B2

公开(公告)日：2009-04-21

申请号：US11582452

申请日：2006-10-18

申请人： Yoshiaki Isobe ,  Haruhisa Ogita ,  Masanori Tobe ,  Haruo Takaku ,  Tetsuhiro Ogino ,  Ayumu Kurimoto ,  Hajime Kawakami

发明人： Yoshiaki Isobe ,  Haruhisa Ogita ,  Masanori Tobe ,  Haruo Takaku ,  Tetsuhiro Ogino ,  Ayumu Kurimoto ,  Hajime Kawakami

IPC分类号： A61P11/06 ,  A61P17/00 ,  A61P35/00 ,  C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  A61K31/52 ,  A61K31/522

CPC分类号： C07D473/00 ,  C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  C07D473/34

摘要： This invention relates to an adenine derivative, a tautomer thereof, or a pharmaceutically acceptable salt thereof represented by general formula (I): wherein X represents NR3 (wherein R3 represents a hydrogen atom or C1-3 alkyl) or the like; R1 represents substituted or unsubstituted alkyl or the like; R2 represents hydroxyl or the like; and Y represents a substituted or unsubstituted aromatic hetero ring or the like. Also, the present invention relates to pharmaceuticals such as an interferon inducer, antiviral agent, anticancer agent, type 2 helper T cell selective immune response inhibitor, antiallergic agent, and immune response modulator comprising the above derivative as an active ingredient.

摘要翻译： 本发明涉及由通式（I）表示的腺嘌呤衍生物，其互变异构体或其药学上可接受的盐：其中X表示NR 3（其中R 3表示氢原子或C 1-3烷基）等; R 1表示取代或未取代的烷基等; R2表示羟基等; Y表示取代或未取代的芳族杂环等。 此外，本发明涉及包含上述衍生物作为活性成分的药物，例如干扰素诱导剂，抗病毒剂，抗癌剂，2型辅助T细胞选择性免疫应答抑制剂，抗过敏剂和免疫应答调节剂。

公开(公告)号：US07396842B2

公开(公告)日：2008-07-08

申请号：US11111845

申请日：2005-04-22

申请人： Norio Fujiwara ,  Hitoshi Fujita ,  Fujio Antoku ,  Toshinari Sugasawa ,  Hajime Kawakami

发明人： Norio Fujiwara ,  Hitoshi Fujita ,  Fujio Antoku ,  Toshinari Sugasawa ,  Hajime Kawakami

IPC分类号： A61K31/44 ,  C07D417/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D277/42 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： A 5-membered cyclic compound of the formula: wherein X is oxygen or sulfur, R1 is hydrogen, substituted or unsubstituted alkyl, etc., R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc., Y1 is a direct bond, substituted or unsubstituted alkylene, —CO(CH2)n—, etc., the wavy line means (E)-configuration or (Z)-configuration, R3 is substituted or unsubstituted aryl, etc., Y2 is substituted or unsubstituted alkylene, etc., R4 is hydrogen, substituted or unsubstituted alkanoyl, substituted or unsubstituted alkyl, etc., R5 is hydrogen, etc., or a salt thereof, these compound being able to inhibit infiltration of leukocytes such as eosinophils and lymphocytes, by which being useful for the treatment of various kinds of inflammation.

摘要翻译： 下式的5元环状化合物：其中X是氧或硫，R 1是氢，取代或未取代的烷基等，R 2是氢，被取代的 或未取代的烷基，取代或未取代的芳基等，Y 1是直接键，取代或未取代的亚烷基，-CO（CH 2）n， （E）构型或（Z）构型，R 3是取代或未取代的芳基等。Y 2 - 是取代或未取代的亚烷基等，R 4是氢，取代或未取代的烷酰基，取代或未取代的烷基等，R 5是氢等，或 其盐，这些化合物能够抑制白细胞如嗜酸性粒细胞和淋巴细胞的浸润，由此可用于治疗各种炎症。

公开(公告)号：US06692926B1

公开(公告)日：2004-02-17

申请号：US09786681

申请日：2001-04-30

申请人： Toshinari Sugasawa ,  Jun Hidaka ,  Hajime Kawakami

发明人： Toshinari Sugasawa ,  Jun Hidaka ,  Hajime Kawakami

IPC分类号： C07K100

CPC分类号： C07K14/705 ,  A61K38/00

摘要： Transformed cells designed to express a recombinant human SMBP at an elevated level to the extent that its ligand-binding activity can be measured, and cellular membrane fractions thereof; recombinant human SMBPs isolated from the transformed cells or the cellular membrane fractions thereof; a screening system for human SMBP agonists/antagonists characterized by utilizing the transformed cells, the cellular membrane fractions thereof or the isolated recombinant human SMBPs; and human SMBP agonists or antagonists obtainable by the screening system, are provided by deleting the polythymidine sequence from the base sequence of the 3′-untranslated region.

摘要翻译： 设计用于在升高的水平上表达重组人SMBP至可测量其配体结合活性的程度的转化细胞及其细胞膜级分; 从转化细胞或其细胞膜级分分离的重组人SMBP; 其特征在于利用转化的细胞，其细胞膜级分或分离的重组人SMBP2的人SMBP激动剂/拮抗剂的筛选系统; 和通过筛选系统可获得的人SMBP激动剂或拮抗剂，通过从3'非翻译区的碱基序列中缺失多胸苷序列来提供。

公开(公告)号：US06329381B1

公开(公告)日：2001-12-11

申请号：US09555292

申请日：2000-05-26

申请人： Ayumu Kurimoto ,  Tetsuhiro Ogino ,  Hajime Kawakami

发明人： Ayumu Kurimoto ,  Tetsuhiro Ogino ,  Hajime Kawakami

IPC分类号： C07D47316

CPC分类号： C07D473/24 ,  C07D473/16 ,  C07D473/18

摘要： The present invention relates to a heterocyclic compound of the following general formula (I): wherein X is sulfur atom, oxygen atom or —NR3— (R3 may form a heterocyclic ring or a substituted heterocyclic ring with R1 via the nitrogen atom), R1 is alkyl group, substituted alkyl group, aryl group, substituted aryl group, heterocyclic group or substituted heterocyclic group, and R2 is hydrogen atom, halogen atom etc.; or its pharmaceutically acceptable salt and interferon inducers, antiviral agents, anticancer agents and therapeutic agents for immunologic diseases comprising the compound (I) or its pharmaceutically acceptable salt as active ingredients.

摘要翻译： 本发明涉及以下通式（I）的杂环化合物：其中X是硫原子，氧原子或-NR 3 - （R 3可以通过氮原子与R 1形成杂环或取代的杂环），R 1 是烷基，取代的烷基，芳基，取代的芳基，杂环基或取代的杂环基，R 2是氢原子，卤素原子等;或其药学上可接受的盐和干扰素诱导剂，抗病毒剂，抗癌剂和治疗剂 包含化合物（I）或其药学上可接受的盐作为活性成分的免疫疾病。

公开(公告)号：US4482573A

公开(公告)日：1984-11-13

申请号：US550583

申请日：1983-11-10

申请人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

发明人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

IPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  C07C93/08

CPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  Y10S514/929

摘要： Diphenylalkanoether and diphenylalkanone oximeether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4) alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylamino and N-(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.4) alkyl group or, when taken together with the adjacent nitrogen atom to which they are attached, represent a nitrogen-containing 5 to 7-membered saturated heterocyclic group optionally having an oxygen atom or an additional nitrogen atom as the hetero atom in addition to the said nitrogen atom and, in case of having the additional nitrogen atom, bearing a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, and ar(C.sub.1 -C.sub.4)alkyl group or a phenyl group thereon), ##STR3## is a group of the formula: ##STR4## or the formula: ##STR5## A.sup.1 is a C.sub.2 -C.sub.6 alkylene group and A.sup.2 is a C.sub.2 -C.sub.4 alkylene group, and non-toxic, pharmaceutically acceptable acid addition salts thereof, which have cerebral vasodilating activity and antihypoxic activity.

公开(公告)号：US4382936A

公开(公告)日：1983-05-10

申请号：US259179

申请日：1981-04-30

申请人： Junki Katsube ,  Keiichi Ono ,  Hajime Kawakami

发明人： Junki Katsube ,  Keiichi Ono ,  Hajime Kawakami

IPC分类号： C07D461/00 ,  A61K31/445 ,  C07D471/14 ,  C07D471/22 ,  A61K31/435

CPC分类号： C07D471/14 ,  C07D461/00 ,  Y10S514/929

摘要： A compound of the formula: ##STR1## wherein R.sup.1 is a C.sub.1 -C.sub.6 alkyl group and R is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, and their salts, which are useful as cerebral vasodilator; and a compound of the formula: ##STR2## wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, R.sup.3 is a hydrogen atom or the formula: --CO.sub.2 R.sup.1 (R.sup.1 is a C.sub.1 -C.sub.6 alkyl group) and W is an oxygen atom, an imino group or ##STR3## but not an imino group in case that R.sup.3 is a hydrogen atom, which are intermediates of the compound (I), useful per se as cerebral vasodilator and/or antihypertensive agents.

摘要翻译： 下式的化合物：其中R1是C1-C6烷基，R是氢原子或C1-C6烷基，它们的盐可用作脑血管扩张剂; 和下式的化合物：其中R 2是氢原子或C 1 -C 6烷基，R 3是氢原子或式-CO 2 R 1（R 1是C 1 -C 6烷基）和W 在R3是氢原子的情况下是氧原子，亚氨基或亚氨基，而不是亚氨基，它是作为脑血管扩张剂和/或抗高血压药物的化合物（I）的中间体。

公开(公告)号：US08666635B2

公开(公告)日：2014-03-04

申请号：US13513978

申请日：2010-12-27

申请人： Shuntaro Okazaki ,  Satoshi Yoshizaki ,  Masashi Shibayama ,  Kaoru Shokatsu ,  Hajime Kawakami

发明人： Shuntaro Okazaki ,  Satoshi Yoshizaki ,  Masashi Shibayama ,  Kaoru Shokatsu ,  Hajime Kawakami

IPC分类号： F02D43/04

CPC分类号： F02D43/04 ,  F02D37/02 ,  F02D41/0002 ,  F02D41/0295 ,  F02D41/1497 ,  F02D2041/1431 ,  F02D2200/0814 ,  F02D2200/1004 ,  F02D2250/21 ,  Y02T10/42

摘要： A control device for an internal combustion engine provided by the present invention is a control device which can satisfy a requirement concerning exhaust gas performance of the internal combustion engine, a requirement concerning fuel economy performance, and a requirement concerning operation performance with an excellent balance by properly regulating a change speed of a required air-fuel ratio and an ignition timing. The present control device keeps the ignition timing at an optimal ignition timing if a predetermined permission condition is not satisfied. However, when the permission condition is satisfied, the present control device controls the ignition timing so as to compensate for a difference which occurs between torque which is estimated from an operation of an actuator for air quantity control and required torque by the ignition timing. Further, if a predetermined lessening condition is not satisfied, the present control device determines an original required air-fuel ratio directly as a final required air-fuel ratio. However, if the lessening condition is satisfied, the present control device processes a signal of the original required air-fuel ratio to lessen a change speed thereof, and determines a required air-fuel ratio the change speed of which is lessened as a final required air-fuel ratio. The permission condition includes the required air-fuel ratio changing in a rich direction, and a change amount thereof being larger than a predetermined determination reference value, and the lessening condition includes the change amount of the required air-fuel ratio being larger than a determination reference value, and the permission condition being unsatisfied.

摘要翻译： 本发明提供的用于内燃机的控制装置是能够满足内燃机排气性能要求的控制装置，关于燃油经济性的要求，以及具有良好平衡的运行性能的要求 适当地调节所需空燃比和点火正时的变化速度。 如果不满足预定的允许条件，则本控制装置将点火正时保持在最佳点火时间。 然而，当允许条件满足时，本控制装置控制点火正时，以便补偿由用于空气量控制的致动器的操作估计的转矩与由点火正时所需的转矩之间发生的转矩之间的差异。 此外，如果不满足预定的减小条件，则本控制装置将原始所需的空燃比直接确定为最终所需的空燃比。 然而，如果减轻条件满足，则本控制装置处理原始所需空燃比的信号以减小其变化速度，并且确定其变化速度作为最终要求减小的所需空燃比 空燃比。 允许条件包括在丰富方向上所需的空燃比变化，并且其变化量大于预定的确定基准值，并且减小条件包括所需空燃比的变化量大于确定 参考值，许可条件不满足。

公开(公告)号：US08649957B2

公开(公告)日：2014-02-11

申请号：US13520502

申请日：2011-01-24

申请人： Satoshi Yoshizaki ,  Shuntaro Okazaki ,  Masashi Shibayama ,  Kaoru Shokatsu ,  Hajime Kawakami

发明人： Satoshi Yoshizaki ,  Shuntaro Okazaki ,  Masashi Shibayama ,  Kaoru Shokatsu ,  Hajime Kawakami

IPC分类号： F02D9/02 ,  F02D41/14 ,  F02D41/30

CPC分类号： F02D41/0235 ,  F01N2430/06 ,  F01N2550/00 ,  F02D41/027 ,  F02D2200/08 ,  F02D2250/18

摘要： A control device is provided that generates a target air-fuel ratio by lessening a change speed of a required air-fuel ratio of an internal combustion engine. However, when a deterioration degree of a catalyst which is disposed in an exhaust passage of the internal combustion engine is a predetermined reference or more, lessening of the change speed of the required air-fuel ratio is stopped, or a lessening degree of the change speed of the required air-fuel ratio is decreased. The control device calculates a target air quantity for realizing the required torque under the target air-fuel ratio. For calculation of the target air quantity, data in which relationship of torque generated by the internal combustion engine and an air quantity taken into a cylinder is fixed by being related to an air-fuel ratio can be used.

摘要翻译： 提供一种控制装置，其通过减小内燃机的所需空燃比的变化速度来产生目标空燃比。 然而，当设置在内燃机的排气通道中的催化剂的劣化程度为预定的参考值或更大时，停止所需空燃比的变化速度的减小或变化的减小程度 所需空燃比的速度降低。 控制装置在目标空燃比下，计算出实现所需转矩的目标空气量。 为了计算目标空气量，可以使用通过与空燃比相关的方式固定由内燃机产生的扭矩和吸入气缸的空气量的关系的数据。

公开(公告)号：US20130297186A1

公开(公告)日：2013-11-07

申请号：US13520502

申请日：2011-01-24

申请人： Satoshi Yoshizaki ,  Shuntaro Okazaki ,  Masashi Shibayama ,  Kaoru Shokatsu ,  Hajime Kawakami

发明人： Satoshi Yoshizaki ,  Shuntaro Okazaki ,  Masashi Shibayama ,  Kaoru Shokatsu ,  Hajime Kawakami

IPC分类号： F02D41/02

CPC分类号： F02D41/0235 ,  F01N2430/06 ,  F01N2550/00 ,  F02D41/027 ,  F02D2200/08 ,  F02D2250/18

摘要： A control device is provided that generates a target air-fuel ratio by lessening a change speed of a required air-fuel ratio of an internal combustion engine. However, when a deterioration degree of a catalyst which is disposed in an exhaust passage of the internal combustion engine is a predetermined reference or more, lessening of the change speed of the required air-fuel ratio is stopped, or a lessening degree of the change speed of the required air-fuel ratio is decreased. The control device calculates a target air quantity for realizing the required torque under the target air-fuel ratio. For calculation of the target air quantity, data in which relationship of torque generated by the internal combustion engine and an air quantity taken into a cylinder is fixed by being related to an air-fuel ratio can be used.

摘要翻译： 提供一种控制装置，其通过减小内燃机的所需空燃比的变化速度来产生目标空燃比。 然而，当设置在内燃机的排气通道中的催化剂的劣化程度为预定的参考值或更大时，停止所需空燃比的变化速度的减小或变化的减小程度 所需空燃比的速度降低。 控制装置在目标空燃比下，计算出实现所需转矩的目标空气量。 为了计算目标空气量，可以使用通过与空燃比相关的方式固定由内燃机产生的扭矩和吸入气缸的空气量的关系的数据。