公开(公告)号：US5462957A

公开(公告)日：1995-10-31

申请号：US365128

申请日：1994-12-28

申请人： Koichi Niimura ,  Yuko Ikeda ,  Akira Kato ,  Takao Ando

发明人： Koichi Niimura ,  Yuko Ikeda ,  Akira Kato ,  Takao Ando

IPC分类号： A61K31/41 ,  A61K31/415 ,  A61P31/04 ,  A61P31/10 ,  A61P35/00 ,  A61P43/00 ,  C07D249/08 ,  C07D307/33 ,  C07D333/38 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D493/10 ,  C07D495/10 ,  C07D521/00

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

摘要： Azole derivatives (including stereoisomers and pharmaceutically acceptable salts) of the formula: ##STR1## wherein R.sub.1 and R.sub.2 each are H or C.sub.1 -C.sub.4 alkyl; R.sub.3 is H, OH, CN, halogen, haloalkyl, C.sub.1 -C.sub.4 alkyl or phenyl, and if there are two or more R.sub.3 groups, such R.sub.3 groups may be the same or different; n is an integer from 0 to 5; Y is N or CH; and X is O, S or NH have antimycotic and aromatase inhibitory activities. Compositions containing the azole derivatives and a method of treating mycosis and estrogen-dependent diseases by administering effective quantities of the azole derivatives are also disclosed.

公开(公告)号：US5432190A

公开(公告)日：1995-07-11

申请号：US183339

申请日：1994-01-19

申请人： Koichi Niimura ,  Yuko Ikeda ,  Akira Kato ,  Takao Ando

发明人： Koichi Niimura ,  Yuko Ikeda ,  Akira Kato ,  Takao Ando

IPC分类号： A61K31/41 ,  A61K31/415 ,  A61P31/04 ,  A61P31/10 ,  A61P35/00 ,  A61P43/00 ,  C07D249/08 ,  C07D307/33 ,  C07D333/38 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D493/10 ,  C07D495/10 ,  C07D521/00 ,  A61K31/34 ,  A61K31/38 ,  A61K31/40

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

摘要： Azole derivatives (including stereoisomers and pharmaceutically acceptable salts) of the formula: ##STR1## wherein R.sub.1 and R.sub.2 each are H or C.sub.1 -C.sub.4 alkyl; R.sub.3 is H, OH, CN, halogen, haloalkyl, C.sub.1 -C.sub.4 alkyl or phenyl, and if there are two or more R.sub.3 groups, such R.sub.3 groups may be the same or different; n is an integer from 0 to 5; Y is N or CH; and X is O, S or NH have antimycotic and aromatase inhibitory activities. Compositions containing the azole derivatives and a method of treating mycosis and estrogen-dependent diseases by administering effective quantities of the azole derivatives are also disclosed.

摘要翻译： 式：-C 1-4烷基的唑衍生物（包括立体异构体和药学上可接受的盐） R3是H，OH，CN，卤素，卤代烷基，C1-C4烷基或苯基，如果有两个或更多个R 3基团，则这样的R 3基团可以相同或不同; n为0〜5的整数， Y为N或CH; X是O，S或NH具有抗真菌和芳香酶抑制活性。 还公开了含有唑衍生物的组合物和通过施用有效量的唑衍生物治疗真菌病和雌激素依赖性疾病的方法。

公开(公告)号：US5324740A

公开(公告)日：1994-06-28

申请号：US67052

申请日：1993-05-26

申请人： Koichi Niimura ,  Yuko Ikeda ,  Akira Kato ,  Takao Ando

发明人： Koichi Niimura ,  Yuko Ikeda ,  Akira Kato ,  Takao Ando

IPC分类号： A61K31/41 ,  A61K31/415 ,  A61P31/04 ,  A61P31/10 ,  A61P35/00 ,  A61P43/00 ,  C07D249/08 ,  C07D307/33 ,  C07D333/38 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D493/10 ,  C07D495/10 ,  C07D521/00

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

摘要： Azole derivatives (including stereoisomers and pharmaceutically acceptable salts) of the formula: ##STR1## wherein R.sub.1 and R.sub.2 each are H or C.sub.1 -C.sub.4 alkyl; R.sub.3 is H, OH, CN, halogen, haloalkyl, C.sub.1 -C.sub.4 alkyl or phenyl, and if there are two or more R.sub.3 groups, such R.sub.3 groups may be the same or different; n is an integer from 0 to 5; Y is N or CH; and X is O, S or NH have antimycotic and aromatase inhibitory activities. Compositions containing the azole derivatives and a method of treating mycosis and estrogen-dependent diseases by administering effective quantities of the azole derivatives are also disclosed.

摘要翻译： C4烷基的唑衍生物（包括立体异构体和药学上可接受的盐） R3是H，OH，CN，卤素，卤代烷基，C1-C4烷基或苯基，如果有两个或更多个R 3基团，则这样的R 3基团可以相同或不同; n为0〜5的整数， Y为N或CH; X是O，S或NH具有抗真菌和芳香酶抑制活性。 还公开了含有唑衍生物的组合物和通过施用有效量的唑衍生物治疗真菌病和雌激素依赖性疾病的方法。

公开(公告)号：US5726196A

公开(公告)日：1998-03-10

申请号：US623914

申请日：1996-03-28

申请人： Koichi Niimura ,  Akira Kato ,  Junko Miyagawa ,  Yuko Ikeda

发明人： Koichi Niimura ,  Akira Kato ,  Junko Miyagawa ,  Yuko Ikeda

IPC分类号： C07D249/08 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/4196 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07D233/56 ,  C07D233/60 ,  C07D405/06 ,  C07D521/00

CPC分类号： C07D231/12 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/4196 ,  C07D233/56 ,  C07D249/08

摘要： The disclosure describes a pharmaceutical composition comprising an aromatase-inhibiting effective amount of a compound selected from the group consisting of compounds of the formula (I): ##STR1## including their stereoisomers and salts thereof, wherein R.sup.1 is halogen or phenyl; m is 0, 1, 2 or 3; k and n each are independently 0, 1 or 2; R.sup.2 and R.sup.3 each are independently H or OH; R.sup.6 and R.sup.7 each are independently H or C.sub.1-4 alkyl; R.sup.8 and R.sup.9 each are H or R.sup.8 and R.sup.9 form --C(R.sup.4) (R.sup.5)--C(R.sup.11) (R12)-- bond wherein R.sup.4, R.sup.5, R.sup.11 and R.sup.12 each are independently H or C.sub.1-4 alkyl; Y is N or CH; and R.sup.10 is H or halogen, or R.sup.10 combines with R.sup.2 to form --O-- bond, with proviso that if R.sup.8 and R.sup.9 form --C (R.sup.4) (R.sup.5)--C(R.sup.11) (R.sup.12)-- bond R.sup.3, R.sup.6 and R.sup.7 each are H, and k and n each are 1, then R.sup.2 and R.sup.10 form --O-- bond, and a pharmaceutically acceptable carrier or diluent.

摘要翻译： 本公开描述了一种药物组合物，其包含芳香酶抑制有效量的选自式（I）的化合物的化合物：包括其立体异构体和盐的其中R 1是卤素或苯基; m为0,1,2或3; k和n各自独立地为0,1或2; R2和R3各自独立地为H或OH; R6和R7各自独立地为H或C1-4烷基; R8和R9各自为H或R8，R9为-C（R4）（R5）-C（R11）（R12） - 键，其中R4，R5，R11和R12各自独立地为H或C1-4烷基; Y为N或CH; R 10为H或卤素，或R 10与R 2结合形成-O-键，条件是如果R 8和R 9形成-C（R 4）（R 5）-C（R 11）（R 12） - 键R 3，R 6和R 7 各自为H，并且k和n各自为1，则R 2和R 10形成-O-键，以及药学上可接受的载体或稀释剂。

公开(公告)号：US5286737A

公开(公告)日：1994-02-15

申请号：US945178

申请日：1992-09-16

申请人： Akira Kato ,  Junko Miyagawa ,  Yuko Ikeda ,  Koichi Niimura

发明人： Akira Kato ,  Junko Miyagawa ,  Yuko Ikeda ,  Koichi Niimura

IPC分类号： A61K31/41 ,  A61K31/415 ,  A61P35/00 ,  A61P43/00 ,  C07D233/60 ,  C07D249/08

CPC分类号： A61K31/415 ,  A61K31/41

摘要： This invention provides a method of inhibiting aromatase and treating of estrogen-dependent diseases in a patient by administering azole derivatives as nonsteroidal inhibitors. The azole derivative has the formula ##STR1## where R.sub.1 a is hydrogen or a (C.sub.1 -C.sub.5) alkyl; R.sub.2 is a hydrogen or a (C.sub.1 -C.sub.5) alkyl; R.sub.3 is any of a halogen, a (C.sub.1 -C.sub.5)alkyl, a haloalkyl, a phenyl, a cyano, or nitro; n is 0 to 5; and Y is a nitrogen atom or CH.

摘要翻译： 本发明提供一种通过施用唑类衍生物作为非甾体抑制剂来抑制芳香酶和治疗患者雌激素依赖性疾病的方法。 唑衍生物具有式（* CHEMICAL STRUCTURE *），其中R a a是氢或（C 1 -C 5）烷基; R2是氢或（C1-C5）烷基; R3是卤素，（C1-C5）烷基，卤代烷基，苯基，氰基或硝基中的任何一种; n为0〜5; Y是氮原子或CH。

公开(公告)号：US5789432A

公开(公告)日：1998-08-04

申请号：US325161

申请日：1994-10-21

申请人： Koichi Niimura ,  Akira Kato ,  Junko Miyagawa ,  Yuko Ikeda

发明人： Koichi Niimura ,  Akira Kato ,  Junko Miyagawa ,  Yuko Ikeda

IPC分类号： C07D249/08 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/4196 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07D233/56 ,  C07D233/60 ,  C07D405/06 ,  C07D521/00 ,  A61K21/415

CPC分类号： C07D231/12 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/4196 ,  C07D233/56 ,  C07D249/08

摘要： The disclosure describes a pharmaceutical composition comprising an aromatase-inhibiting effective amount of a compound selected from the group consisting of compounds of the formula (I): ##STR1## including their stereoisomers and salts thereof, wherein R.sup.1 is halogen or phenyl; m is 0, 1, 2 or 3; k and n each are independently 0, 1 or 2; R.sup.2 and R.sup.3 each are independently H or OH; R.sup.6 and R.sup.7 each are independently H or C.sub.1-4 alkyl; R.sup.8 and R.sup.9 each are H or R.sup.8 and R.sup.9 form --C(R.sup.4) (R.sup.5)--C(R.sup.11) (R.sup.12)-- bond wherein R.sup.4, R.sup.5, R.sup.11 and R.sup.12 each are independently H or C.sub.1-4 alkyl; Y is N or CH; and R.sup.10 is H or halogen, or R.sup.10 combines with R.sup.2 to form --O-- bond, with proviso that if R.sup.8 and R.sup.9 form --C(R.sup.4) (R.sup.5)--C(R.sup.11) (R.sup.2)-- bond, R.sup.3, R.sup.6 and R.sup.7 each are H, and k and n each are 1, then R.sup.2 and R.sup.10 form --O-- bond, and a pharmaceutically acceptable carrier or diluent.

摘要翻译： 本公开描述了一种药物组合物，其包含芳香酶抑制有效量的选自式（I）的化合物的化合物：包括其立体异构体和盐的其中R 1是卤素或苯基; m为0,1,2或3; k和n各自独立地为0,1或2; R2和R3各自独立地为H或OH; R6和R7各自独立地为H或C1-4烷基; R8和R9各自为H或R8，R9为-C（R4）（R5）-C（R11）（R12） - 键，其中R4，R5，R11和R12各自独立地为H或C1-4烷基; Y为N或CH; R 10为H或卤素，或R 10与R 2结合形成-O-键，条件是如果R 8和R 9形成-C（R 4）（R 5）-C（R 11）（R 2） - 键，则R 3，R 6和 R7各自为H，k和n各自为1，则R2和R10形成-O-键，以及药学上可接受的载体或稀释剂。

公开(公告)号：US5407952A

公开(公告)日：1995-04-18

申请号：US120758

申请日：1993-09-15

申请人： Kochi Niimura ,  Yuko Ikeda ,  Akira Kato ,  Takao Ando

发明人： Kochi Niimura ,  Yuko Ikeda ,  Akira Kato ,  Takao Ando

IPC分类号： A61K31/41 ,  A61K31/415 ,  A61P31/04 ,  A61P31/10 ,  A61P35/00 ,  A61P43/00 ,  C07D249/08 ,  C07D307/33 ,  C07D333/38 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D493/10 ,  C07D495/10 ,  C07D521/00 ,  A01N43/653

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

摘要： Azole derivatives (including stereoisomers and pharmaceutically acceptable salts) of the formula: ##STR1## wherein R.sub.1 and R.sub.2 each are H or C.sub.1 -C.sub.4 alkyl; R.sub.3 is H, OH, CN, halogen, haloalkyl, C.sub.1 -C.sub.4 alkyl or phenyl, and if there are two or more R.sub.3 groups, such R.sub.3 groups may be the same or different; n is an integer from 0 to 5; Y is N or CH; and X is O, S or NH have antimycotic and aromatase inhibitory activities. Compositions containing the azole derivatives and a method of treating mycosis and estrogen-dependent diseases by administering effective quantities of the azole derivatives are also disclosed.

摘要翻译： C4烷基的唑衍生物（包括立体异构体和药学上可接受的盐） R3是H，OH，CN，卤素，卤代烷基，C1-C4烷基或苯基，如果有两个或更多个R 3基团，则这样的R 3基团可以相同或不同; n为0〜5的整数， Y为N或CH; X是O，S或NH具有抗真菌和芳香酶抑制活性。 还公开了含有唑衍生物的组合物和通过施用有效量的唑衍生物治疗真菌病和雌激素依赖性疾病的方法。

公开(公告)号：US09523141B2

公开(公告)日：2016-12-20

申请号：US14356502

申请日：2012-11-06

申请人： Kota Washio ,  Akira Kato ,  Toshiji Mukai ,  Alok Singh ,  Hidetoshi Somekawa

发明人： Kota Washio ,  Akira Kato ,  Toshiji Mukai ,  Alok Singh ,  Hidetoshi Somekawa

IPC分类号： C22C23/04 ,  C22F1/06 ,  C22C1/02 ,  C22C23/00 ,  C22F1/00

CPC分类号： C22F1/06 ,  C22C1/02 ,  C22C23/00 ,  C22C23/04 ,  C22F1/00

摘要： Provided is an Mg alloy and a method for producing same able to demonstrate high strength without requiring an expensive rare earth element (RE). The high-strength Mg alloy containing Ca and Zn within a solid solubility limit and the remainder having a chemical composition comprising Mg and unavoidable impurities is characterized in comprising equiaxial crystal particles, there being a segregated area of Ca and Zn along the (c) axis of a Mg hexagonal lattice within the crystal particle, and having a structure in which the segregated area is lined up by Mg3 atomic spacing in the (a) axis of the Mg hexagonal lattice. The method for producing the high-strength Mg alloy is characterized in that Ca and Zn are added to Mg in a compounding amount corresponding to the above composition and, after homogenization heat treating an ingot formed by dissolution and casting, the above structure is formed by subjecting the ingot to hot processing.

摘要翻译： 提供一种Mg合金及其制造方法，能够显示高强度而不需要昂贵的稀土元素（RE）。 含有固溶度极限中的Ca和Zn的高强度Mg合金和其中包含Mg和不可避免的杂质的化学组成的其余部分的特征在于包括等轴晶体颗粒，沿着（c）轴具有Ca和Zn的偏析面积 的晶体粒子内的Mg六角形晶格，并且具有在Mg六方晶格的（a）轴上偏析区域被Mg 3原子间隔排列的结构。 高强度Mg合金的制造方法的特征在于，以与上述组成相对应的配合量将Mg和Ca添加到Mg中，在通过溶解和铸造形成的锭均质化热处理后，上述结构通过 对锭进行热加工。

公开(公告)号：US08792308B2

公开(公告)日：2014-07-29

申请号：US13634403

申请日：2011-03-23

申请人： Akira Kato ,  Takushi Hagita ,  Tadashi Yasuoka

发明人： Akira Kato ,  Takushi Hagita ,  Tadashi Yasuoka

IPC分类号： G04C11/02

CPC分类号： G05G5/005 ,  G04R20/06

摘要： Provided is a radio-controlled watch capable of performing leap second correction even when information on a leap second is not received from a satellite. Provided is a radio-controlled watch that adjusts time by receiving a signal containing time information from a satellite, the radio-controlled watch being configured to: store a leap second correction value to be used for leap second correction with respect to the time information; display a numerical value corresponding to the leap second correction value; receive an instruction operation of changing the leap second correction value from a user in a state in which the numerical value is displayed; and change the leap second correction value in response to the received instruction operation.

摘要翻译： 提供了即使在没有从卫星接收到关于闰秒的信息的情况下也能够执行闰秒校正的无线电控制的手表。 提供一种无线电控制手表，其通过从卫星接收到包含时间信息的信号来调整时间，该无线电控制手表被配置为：存储用于相对于时间信息的闰秒校正的闰秒校正值; 显示对应于闰秒校正值的数值; 在显示数值的状态下接收从用户改变闰秒校正值的指令操作; 并且响应于接收到的指令操作来改变闰秒校正值。

公开(公告)号：US08653067B2

公开(公告)日：2014-02-18

申请号：US12597470

申请日：2008-04-23

申请人： Naotake Kobayashi ,  Kazuo Ueda ,  Naohiro Itoh ,  Gaku Sakaguchi ,  Akira Kato ,  Akihiro Hori ,  Hidekazu Haraguchi ,  Ken Yasui

发明人： Naotake Kobayashi ,  Kazuo Ueda ,  Naohiro Itoh ,  Gaku Sakaguchi ,  Akira Kato ,  Akihiro Hori ,  Hidekazu Haraguchi ,  Ken Yasui

IPC分类号： A61K31/554 ,  A61K31/541 ,  A61K31/426 ,  A61K31/506 ,  C07D417/02 ,  C07D279/06 ,  C07D277/18 ,  C07D239/02

CPC分类号： C07D471/04 ,  A61K9/0019 ,  A61K9/1623 ,  A61K9/2018 ,  A61K31/426 ,  A61K31/506 ,  A61K31/535 ,  A61K31/54 ,  A61K31/541 ,  A61K31/554 ,  C07D239/14 ,  C07D265/08 ,  C07D277/18 ,  C07D279/06 ,  C07D281/02 ,  C07D285/36 ,  C07D295/155 ,  C07D295/192 ,  C07D405/04 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  A61K2300/00

摘要： A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I); wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene, etc.; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b are each independently a hydrogen atom, halogen, hydroxy, etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 1 to 3; and R5 is a hydrogen atom, optionally substituted lower alkyl, etc.; its pharmaceutically acceptable salt, or a solvate thereof as an active ingredient.

摘要翻译： 一种用于治疗含有由通式（I）表示的化合物的阿尔茨海默病的药物组合物; 其中环A是任选取代的碳环基团或任选取代的杂环基团; E为低级亚烷基等; X是S，O或NR1; R1是氢原子或低级烷基; R2a，R2b，R3a，R3b，R4a和R4b各自独立地为氢原子，卤素，羟基等; n和m各自独立地为0〜3的整数， n + m为1〜3的整数， R5为氢原子，任意取代的低级烷基等; 其药学上可接受的盐或其溶剂合物作为活性成分。