公开(公告)号：US6090802A

公开(公告)日：2000-07-18

申请号：US95925

申请日：1998-06-12

申请人： Isao Kawamoto ,  Yasuo Shimoji ,  Katsuya Ishikawa ,  Katsuhiko Kojima ,  Hiroshi Yasuda ,  Satoshi Ohya ,  Yukio Utsui

发明人： Isao Kawamoto ,  Yasuo Shimoji ,  Katsuya Ishikawa ,  Katsuhiko Kojima ,  Hiroshi Yasuda ,  Satoshi Ohya ,  Yukio Utsui

IPC分类号： C07D477/20 ,  A61K31/409

CPC分类号： C07D477/20

摘要： A 1-methylcarbapenem compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.2 represents hydrogen or an ester residue; and A represents a group of the formula (A1) ##STR2## wherein n is 0, 1 or 2, P is 0, 1 or 2, R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl and R.sup.4 is a group (Q2) ##STR3## wherein B is phenylene, phenylene(C.sub.1 -C.sub.3)alkyl, cyclohexylene, cyclohexylene(C.sub.1 -C.sub.3)alkyl or C.sub.1 -C.sub.5 alkylene, R.sup.7 is hydrogen or C.sub.1 -C.sub.4 alkyl, and R.sup.14 is a group --C(.dbd.NH)R.sup.8, wherein R.sup.8 is hydrogen or C.sub.1 -C.sub.4 alkyl or a group --NR.sup.9 R.sup.10, wherein R.sup.9 and R.sup.10 are the same or different and are hydrogen or C.sub.1 -C.sub.4 alkyl; or a pharmacologically acceptable salt thereof.

摘要翻译： 由下式（I）表示的1-甲基碳青霉烯化合物：其中R1表示氢或C1-C4烷基; R2代表氢或酯残基; 并且A表示式（A1）的基团，其中n为0,1或2，P为0,1或2，R3为氢或C1-C4烷基，R4为基团（Q2），其中B为亚苯基，亚苯基 （C1-C3）烷基，亚环己基，亚环己基（C1-C3）烷基或C1-C5亚烷基，R7是氢或C1-C4烷基，R14是基团-C（= NH）R8，其中R8是氢或C1 -C4烷基或-NR9R10基团，其中R9和R10相同或不同，为氢或C1-C4烷基; 或其药理学上可接受的盐。

公开(公告)号：US5977097A

公开(公告)日：1999-11-02

申请号：US176804

申请日：1998-10-22

申请人： Isao Kawamoto ,  Katsuya Ishikawa ,  Katsuhiko Kojima ,  Yasuo Shimoji ,  Satoshi Ohya ,  Munetsugu Morimoto

发明人： Isao Kawamoto ,  Katsuya Ishikawa ,  Katsuhiko Kojima ,  Yasuo Shimoji ,  Satoshi Ohya ,  Munetsugu Morimoto

IPC分类号： A61K31/403 ,  A61P31/04 ,  C07D477/20 ,  A61K31/40 ,  C07D487/04

CPC分类号： C07D477/20

摘要： A 1-methylcarbapenem compound represented by the following formula: ##STR1## [wherein R.sup.1 represents a hydrogen atom or a lower alkyl group, R.sup.2 represents a hydrogen atom or a lower alkyl group, R.sup.3 represents a hydrogen atom, a lower alkyl group, a lower alkyl group which has a substituent, a cycloalkyl group or a group of formula --C(.dbd.NH)R.sup.4 (in which R.sup.4 represents a hydrogen atom, a lower alkyl group or an amino group)]; or a pharmacologically acceptable salt or derivative thereof. The 1-methylcarbapenem compounds of the present invention exhibit excellent antibacterial activity and are therefore effective as a preventive or remedy of infections.

摘要翻译： 由下式表示的1-甲基碳青霉烯化合物：其中，R 1表示氢原子或低级烷基，R 2表示氢原子或低级烷基，R 3表示氢原子，低级烷基，低级烷基 具有取代基，环烷基或式-C（= NH）R 4（其中R 4表示氢原子，低级烷基或氨基）的基团]。 或其药理学上可接受的盐或其衍生物。 本发明的1-甲基碳青霉烯化合物表现出优异的抗菌活性，因此作为感染的预防或补救是有效的。

公开(公告)号：US06924279B2

公开(公告)日：2005-08-02

申请号：US10351944

申请日：2003-01-27

申请人： Isao Kawamoto ,  Yasuo Shimoji ,  Hiroshi Fukuhara

发明人： Isao Kawamoto ,  Yasuo Shimoji ,  Hiroshi Fukuhara

IPC分类号： A61K31/407 ,  A61P31/04 ,  C07D477/20

CPC分类号： C07D477/20 ,  A61K31/407

摘要： This invention provides crystalline forms of a 1-methylcarbapenem derivative of formula (I) or of pharmaceutically acceptable salts thereof. The crystalline forms of the 1-methylcarbapenem derivative exhibit excellent antibiotic activity against various bacterial strains and sufficient stability for practical use.

摘要翻译： 本发明提供式（I）的1-甲基碳青霉烯衍生物或其药学上可接受的盐的结晶形式。 1-甲基碳青霉烯衍生物的结晶形式对各种细菌菌株表现出优异的抗生素活性，并且在实际应用中具有足够的稳定性。

公开(公告)号：US4527915A

公开(公告)日：1985-07-09

申请号：US615901

申请日：1984-05-29

申请人： Koichi Ikariishi ,  Toshiaki Kitano ,  Masanori Shinohara ,  Yasuo Shimoji

发明人： Koichi Ikariishi ,  Toshiaki Kitano ,  Masanori Shinohara ,  Yasuo Shimoji

IPC分类号： B21B31/07 ,  F16C19/38 ,  F16C33/80 ,  F16J15/447

CPC分类号： F16C19/388 ,  B21B31/07 ,  F16C13/02 ,  F16C33/768 ,  F16C33/7813 ,  F16C33/80

摘要： A sealed multi-row roller bearing device for rolling mills, wherein the opposite ends of the inner race are extended, and a plurality of inner annular bodies which are of one of the groups of elements defining labyrinths are fitted on the extension of the inner race, while outer annular bodies which are of the other group of elements defining labyrinths are removably connected to the end of the outer race.

摘要翻译： 一种用于轧机的密封多列滚子轴承装置，其中内圈的相对端延伸，并且具有限定迷宫的元件组中的一组的多个内环形体安装在内圈的延伸部 而另一组元件限定迷宫的外部环形体可拆卸地连接到外圈的端部。

公开(公告)号：US5086057A

公开(公告)日：1992-02-04

申请号：US691542

申请日：1991-04-25

申请人： Kazuhiko Sasagawa ,  Yo Takiguchi ,  Jun Ohsuri ,  Yasuo Shimoji

发明人： Kazuhiko Sasagawa ,  Yo Takiguchi ,  Jun Ohsuri ,  Yasuo Shimoji

IPC分类号： A61K31/505 ,  A61K31/535 ,  A61P1/00 ,  A61P1/14 ,  A61P7/06 ,  C07D487/14

CPC分类号： C07D487/14 ,  A61K31/505 ,  A61K31/535

摘要： Compounds of formula (I): ##STR1## [in which: Y represents a group of formula ##STR2## the dotted line is a double of single bond; R.sup.1 is hydrogen, alkyl or aryl; R.sup.2 is hydrogen or halogen; R.sup.3 is alkyl or cycloalkyl; R.sup.4 is hydrogen, alkyl, hydroxy or halogen; and R.sup.6 is hydrogen, optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or aralkyl;]and pharmaceutically acceptable salts thereof are valuable in the treatment of cachexia. Certain of these compounds are novel.

公开(公告)号：US5002942A

公开(公告)日：1991-03-26

申请号：US384261

申请日：1989-07-21

申请人： Hiroaki Yanagisawa ,  Koichi Fujimoto ,  Yasuo Shimoji ,  Takuro Kanazaki ,  Hiroyuki Koike ,  Hiroshi Nishino

发明人： Hiroaki Yanagisawa ,  Koichi Fujimoto ,  Yasuo Shimoji ,  Takuro Kanazaki ,  Hiroyuki Koike ,  Hiroshi Nishino

IPC分类号： C07D281/10 ,  C07D417/04 ,  C07D417/06

CPC分类号： C07D417/04 ,  C07D281/10 ,  C07D417/06

摘要： Compounds of formula (I): ##STR1## in which: R.sup.1 is aryl or aromatic heterocyclic; R.sup.2 and R.sup.3 are hydrogen, alkyl, alkoxy, halogen, phenyl, phenoxy, C.sub.1 -C.sub.6 alkylthio, phenylthio, C.sub.1 -C.sub.6 haloalkyl, cyano or nitro, or together are alkylene optionally containing oxygen; R.sup.4 is hydrogen, aliphatic acyl, cycloalkylcarbonyl, cycloalkoxycarbonyl, aromatic acyl, alkoxycarbonyl or benzyloxycarbonyl; R.sup.5 and R.sup.6 are alkyl; and X is oxygen, sulfur or methylene, have calcium channel blocking activity and can serve for the treatment or prophylaxis of cardiovascular diseases and disorders. They may be prepared by reacting a corresponding compound where R.sup.4 is hydrogen and the aminoethyl group is replaced by hydrogen with a compound providing the aminoethyl group and the, if required, acylating the product.

公开(公告)号：US4716162A

公开(公告)日：1987-12-29

申请号：US755474

申请日：1985-07-16

申请人： Kuniyuki Tomita ,  Yasuo Shimoji ,  Seiji Kumakura ,  Hiroyuki Koike ,  Nobuyoshi Iwata ,  Yasuhiro Morisawa

发明人： Kuniyuki Tomita ,  Yasuo Shimoji ,  Seiji Kumakura ,  Hiroyuki Koike ,  Nobuyoshi Iwata ,  Yasuhiro Morisawa

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/435 ,  A61K31/475 ,  A61K31/535 ,  A61K31/55 ,  A61P7/10 ,  A61P9/06 ,  A61P25/28 ,  C07D209/18 ,  C07D209/26 ,  C07D471/06 ,  C07D487/04 ,  C07D487/06 ,  A61K31/495 ,  C07D401/14 ,  C07D471/04

CPC分类号： C07D471/06 ,  C07D209/26 ,  C07D487/04 ,  C07D487/06

摘要： Fused ring compounds of formula (I): ##STR1## (where R.sup.1 -R.sup.4, X.sup.1 and X.sup.2 represent hydrogen or various substituents, n and m are 1-3 and 2-7 respectively, the dotted lines are double or single bonds and Y is one oxygen or two hydrogens) have magnificent anti-arrhythmic activity, diuretic activity and the ability to improve brain function.

摘要翻译： 式（I）的稠环化合物：其中R 1 -R 4，X 1和X 2表示氢或各种取代基，n和m分别为1-3和2-7，虚线是双重或单数 键和Y是一个氧或两个氢）具有宏伟的抗心律失常活性，利尿活性和改善脑功能的能力。

公开(公告)号：US5646171A

公开(公告)日：1997-07-08

申请号：US465369

申请日：1995-06-05

申请人： Hiroaki Yanagisawa ,  Yoshiya Amemiya ,  Yasuo Shimoji ,  Takuro Kanazaki ,  Hiroyuki Koike ,  Toshio Sada

发明人： Hiroaki Yanagisawa ,  Yoshiya Amemiya ,  Yasuo Shimoji ,  Takuro Kanazaki ,  Hiroyuki Koike ,  Toshio Sada

IPC分类号： C07D233/90 ,  C07D403/10 ,  C07D405/12 ,  C07D405/14 ,  C07F7/18 ,  C07D405/08 ,  C07D257/04 ,  A61K31/415 ,  A61K31/41

CPC分类号： C07D403/10 ,  C07D233/90 ,  C07D405/12 ,  C07D405/14 ,  C07F7/1856

摘要： An angiotensin II antagonist of the formula: ##STR1## in which: R.sub.p.sup.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or C.sub.1 -C.sub.6 alkanoyl; R.sub.p.sup.2 represents a single bond, C.sub.1 -C.sub.4 alkylene or C.sub.1 -C.sub.4 alkylidene; R.sub.p.sup.3 and R.sub.p.sup.4 are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.6 alkyl; R.sub.p.sup.5 represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, naphthyl, benzyl, diphenylmethyl, naphthylmethyl, alkanoyloxyalkyl, cycloalkanecarbonyloxyalkyl, alkoxycarbonyloxyalkyl, cycloalkyloxycarbonyloxyalkyl, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methyl, (5-alkyl-2-oxo-1,3-dioxolen-4-yl)methyl or phthalaidyl; R.sub.p.sup.6 represents a carboxy or a tetrazol-5-yl; and X.sub.p represents an oxygen or sulfur, and pharmaceutically acceptable salts thereof. The compounds have hypotensive activity and can thus be used for the treatment and prophylaxis of hypertension.

摘要翻译： 一种下式的血管紧张素II拮抗剂：其中：Rp1表示氢，C1-C6烷基，C3-C6环烷基或C1-C6烷酰基; Rp2表示单键，C1-C4亚烷基或C1-C4亚烷基; Rp3和Rp4独立地选自氢和C1-C6烷基; R 5表示氢，C 1 -C 4烷基，苯基，萘基，苄基，二苯基甲基，萘基甲基，烷酰氧基烷基，环烷基羰氧基烷基，烷氧基羰氧基烷基，环烷氧基羰基氧基烷基，（5-苯基-2-氧代-1,3-二氧杂环戊烯-4-基） - 烷基-2-氧代-1,3-二氧杂环戊烯-4-基）甲基或邻苯二甲酰基; Rp6表示羧基或四唑-5-基; Xp表示氧或硫，以及其药学上可接受的盐。 这些化合物具有降血压活性，因此可用于治疗和预防高血压。

公开(公告)号：US5616599A

公开(公告)日：1997-04-01

申请号：US378650

申请日：1995-01-26

申请人： Hiroaki Yanagisawa ,  Koichi Fujimoto ,  Yoshiya Amemiya ,  Yasuo Shimoji ,  Takuro Kanazaki ,  Hiroyuki Koike ,  Toshio Sada

发明人： Hiroaki Yanagisawa ,  Koichi Fujimoto ,  Yoshiya Amemiya ,  Yasuo Shimoji ,  Takuro Kanazaki ,  Hiroyuki Koike ,  Toshio Sada

IPC分类号： C07D233/90 ,  C07D403/10 ,  C07D405/12 ,  C07D405/14 ,  C07F7/18 ,  C07D257/04 ,  A61K31/41 ,  A61K31/415

CPC分类号： C07D403/10 ,  C07D233/90 ,  C07D405/12 ,  C07D405/14 ,  C07F7/1856

摘要： Compounds of the following formula (I) or the formula (I).sub.p : ##STR1## wherein R.sup.1 is alkyl or alkenyl; R.sup.2 and R.sup.3 are hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl, or aryl fused to cycloalkyl; R.sup.4 is hydrogen, alkyl, alkanoyl, alkenoyl, arylcarbonyl, alkoxycarbonyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydrothienyl, tetrahydrofuryl, a group of formula --SiR.sup.a R.sup.b R.sup.c, in which R.sup.a, R.sup.b and R.sup.c are alkyl or aryl, alkoxymethyl, (alkoxyalkoxy)methyl, haloalkoxymethyl, aralkyl, aryl or alkanoyloxymethoxycarbonyl; R.sup.5 is carboxy or --CONR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 hydrogens or alkyl, or R.sup.8 and R.sup.9 together form alkylene; R.sup.6 is hydrogen, alkyl, alkoxy or halogen; R.sup.7 is carboxy or tetrazol-5-yl; R.sub.p.sup.1 is hydrogen, alkyl, cycloalkyl or alkanoyl; R.sub.p.sup.2 is a single bond, alkylene or alkylidene; R.sub.p.sup.3 and R.sub.p.sup.4 are each hydrogen or alkyl; R.sub.p.sup.6 is carboxy or tetrazol-5-yl; and X.sub.p is oxygen or sulfur; and pharmaceutically acceptable salts and esters thereof. The compounds are AII receptor antagonists and thus have hypotensive activity and can be used for the treatment and prophylaxis of hypertension. The compounds may be prepared by reacting a biphenylmethyl compound with an imidazole compound.

摘要翻译： 下式（I）或式（I）的化合物p：其中R 1是烷基或链烯基; R2和R3是与环烷基稠合的氢，烷基，烯基，环烷基，芳烷基，芳基或芳基; R4是氢，烷基，烷酰基，烯酰基，芳基羰基，烷氧基羰基，四氢吡喃基，四氢噻喃基，四氢噻吩基，四氢呋喃基，式-SiRaRbRc的基团，其中R a，R b和R c是烷基或芳基，烷氧基甲基，（烷氧基烷氧基）甲基，卤代烷氧基甲基， 芳烷基，芳基或烷酰氧基甲氧基羰基; R5是羧基或-CONR8R9，其中R8和R9的氢或烷基，或R8和R9一起形成亚烷基; R6是氢，烷基，烷氧基或卤素; R7是羧基或四唑-5-基; Rp1为氢，烷基，环烷基或烷酰基; Rp2是单键，亚烷基或亚烷基; Rp3和Rp4各自为氢或烷基; Rp6是羧基或四唑-5-基; Xp为氧或硫; 及其药学上可接受的盐和酯。 化合物是AII受体拮抗剂，因此具有低血压活性，可用于治疗和预防高血压。 该化合物可以通过使联苯甲基化合物与咪唑化合物反应来制备。

公开(公告)号：US5055479A

公开(公告)日：1991-10-08

申请号：US365851

申请日：1989-06-14

申请人： Yo Takiguchi ,  Jun Ohsumi ,  Yasuo Shimoji ,  Kazuhiko Sasagawa

发明人： Yo Takiguchi ,  Jun Ohsumi ,  Yasuo Shimoji ,  Kazuhiko Sasagawa

IPC分类号： A61K31/505 ,  A61K31/535 ,  A61P1/00 ,  A61P1/14 ,  A61P7/06 ,  C07D487/14

CPC分类号： C07D487/14 ,  A61K31/505 ,  A61K31/535

摘要： Compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are valuable in the treatment of cachexia.