公开(公告)号：US4751227A

公开(公告)日：1988-06-14

申请号：US844013

申请日：1986-03-26

申请人： Motosuke Yamanaka ,  Kazutoshi Miyake ,  Shinji Suda ,  Hideto Ohhara ,  Toshiaki Ogawa

发明人： Motosuke Yamanaka ,  Kazutoshi Miyake ,  Shinji Suda ,  Hideto Ohhara ,  Toshiaki Ogawa

IPC分类号： C07D213/64 ,  A61K31/435 ,  A61K31/437 ,  A61K31/44 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  C07D213/78 ,  C07D471/04

CPC分类号： C07D471/04

摘要： 5-(6-Imidazo[1,2-a]pyridyl)pyridine derivatives represented by general formula: ##STR1## wherein X represents hydrogen atom or methyl group; Y represents cyano group, carboxamido group, hydrogen atom, amino group or a halogen atom; Z represents hydrogen atom or a lower alkyl group; W represents hydrogen atom or a lower alkyl group; R.sup.1 represents hydrogen atom, a lower alkyl group, phenyl group, a group shown by formula: --CH.sub.2 R.sup.4 in which R.sup.4 is a lower alkoxy group, or a group shown by formula: ##STR2## in which R.sup.5 and R.sup.6 are hydrogen atom or a lower alkyl group R.sup.2 represents hydrogen atom or a halogen atom; and R.sup.3 represents hydrogen atom, a lower alkyl group or a halogen atom; or a tautomer thereof; and pharmacologically acceptable salts thereof are disclosed. The 5-(6-imidazo[1,2-a]pyridyl)pyridine derivatives are effective for treating congestive heart failures.

摘要翻译： 5-（6-咪唑并[1,2-a]吡啶基）吡啶衍生物，其通式如下：其中X代表氢原子或甲基; Y表示氰基，甲酰胺基，氢原子，氨基或卤素原子; Z表示氢原子或低级烷基; W表示氢原子或低级烷基; R1表示氢原子，低级烷基，苯基，其中R4表示低级烷氧基的式-CH2R4表示的基团，或由下式表示的基团：其中R5和R6为氢原子或 低级烷基R2表示氢原子或卤素原子; R3代表氢原子，低级烷基或卤原子; 或其互变异构体; 及其药理学上可接受的盐。 5-（6-咪唑并[1,2-a]吡啶基）吡啶衍生物对于治疗充血性心力衰竭是有效的。

公开(公告)号：US5444083A

公开(公告)日：1995-08-22

申请号：US468147

申请日：1990-01-22

申请人： Motosuke Yamanaka ,  Tomonori Hoshiko ,  Shinji Suda ,  Naoki Yoneda ,  Nobuyuki Mori ,  Mitsumasa Shino ,  Hiroki Ishihara ,  Mamoru Saito ,  Toshiyuki Matsuoka

发明人： Motosuke Yamanaka ,  Tomonori Hoshiko ,  Shinji Suda ,  Naoki Yoneda ,  Nobuyuki Mori ,  Mitsumasa Shino ,  Hiroki Ishihara ,  Mamoru Saito ,  Toshiyuki Matsuoka

IPC分类号： C07D207/06 ,  A61K31/40 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04 ,  C07D409/06

CPC分类号： C07D207/08 ,  C07D207/12 ,  C07D207/14 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04 ,  C07D409/06

摘要： A pyrrolidine compound having the following formula and a pharmacologically acceptable salt thereof is disclosed. It is useful in the pharmaceutical field. ##STR1## in which X is hydrogen, a halogen, or a lower alkyl, Y is --(CH2)n--, n being zero, 1 or 2, --S(O)p--, p being zero, 1 or 2, --O--, or --NH-- and R is phenyl, a substituent-having phenyl, naphtyl, a substituent-having naphthyl, a heteroaryl or a substituent-having heteroaryl.

摘要翻译： 公开了具有下式的吡咯烷化合物及其药理学上可接受的盐。 它在制药领域是有用的。 其中X是氢，卤素或低级烷基，Y是 - （CH 2）n - ，n是0,1或2，-S（O）p - ，p是0,1或2， -O-或-NH-，R是苯基，具有取代基的苯基，萘基，具有取代基的萘基，杂芳基或具有取代基的杂芳基。

公开(公告)号：US5082850A

公开(公告)日：1992-01-21

申请号：US571313

申请日：1990-08-22

申请人： Hitoshi Oinuma ,  Motosuke Yamanaka ,  Kazutoshi Miyake ,  Tomonori Hoshiko ,  Norio Minami ,  Tadao Shoji ,  Yoshiharu Daiku ,  Kohei Sawada ,  Kenichi Nomoto

发明人： Hitoshi Oinuma ,  Motosuke Yamanaka ,  Kazutoshi Miyake ,  Tomonori Hoshiko ,  Norio Minami ,  Tadao Shoji ,  Yoshiharu Daiku ,  Kohei Sawada ,  Kenichi Nomoto

IPC分类号： C07D211/14 ,  C07D211/32 ,  C07D211/54 ,  C07D213/38 ,  C07D401/06

CPC分类号： C07D401/06 ,  C07D211/14 ,  C07D211/32 ,  C07D211/54 ,  C07D213/38 ,  Y10S514/821

摘要： A piperidine compound has the generic formula and is useful to treat arrhythmia. ##STR1## in which R1 is a lower alkyl and W is: ##STR2## X is --S--, --SO-- or --SO2--, R2 is hydrogen or --(CH2)n--Y, n is an integer of 1 to 5, Y is an aryl, pyridyl or a substituted pyridyl, X' is --CO-- or --CH(OH)--,p is an integer of 1 to 4, R12 is hydrogen or a lower alkyl, Y' is --(CH2)m--A, m is 1 or 2, A is an aryl, a substituted aryl, pyridyl or a substituted pyridyl, R12 and Y may form a 5- or 6-membered ring or a 5- or 6-membered ring having one or more substituents andR22 is hydrogen, a halogen, a lower alkyl, a lower alkoxy or hydroxy.

公开(公告)号：US4996215A

公开(公告)日：1991-02-26

申请号：US408106

申请日：1989-09-15

申请人： Hitoshi Oinuma ,  Motosuke Yamanaka ,  Kazutoshi Miyake ,  Tomonori Hoshiko ,  Norio Minami ,  Tadao Shoji ,  Yoshiharu Daiku ,  Kohei Sawada ,  Kenichi Nomoto

发明人： Hitoshi Oinuma ,  Motosuke Yamanaka ,  Kazutoshi Miyake ,  Tomonori Hoshiko ,  Norio Minami ,  Tadao Shoji ,  Yoshiharu Daiku ,  Kohei Sawada ,  Kenichi Nomoto

IPC分类号： C07D473/08 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/451 ,  A61K31/50 ,  A61K31/505 ,  A61P9/06 ,  C07D207/08 ,  C07D211/22 ,  C07D211/28 ,  C07D211/32 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D417/04 ,  C07D417/06 ,  C07D471/04 ,  C07D473/10

CPC分类号： C07D401/04 ,  C07D211/28 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/10

摘要： A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R.sup.1 is a lower alkyl or a tolyl, R.sup.2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R.sup.3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH.sub.2 -- or --CHOH--, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, --CH.sub.2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## l being 1 or 2, --A--B, A being --(CH.sub.2).sub.n --, n being an integer of 1 to 5, a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkane having lower alkyl, phenyl or hydroxyl group(s) bonded directly to one or more carbon atoms constituting said alkane by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof, a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkene having a double bond formed between carbon atoms adjacent to each other by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof, --(CH.sub.2).sub.k --S--, k being an integer of 2 to 5, --(CH.sub.2).sub.p --CO--, p being an integer of 1 to 4, B being cyano, --NR.sub.4 R.sub.5, a heterocyclic ring or a condensed aromatic ring.

公开(公告)号：US5741902A

公开(公告)日：1998-04-21

申请号：US464341

申请日：1995-06-05

申请人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

发明人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/18 ,  C07D501/26 ,  C07D501/28 ,  C07D501/34 ,  C07D501/36 ,  C07D501/40

CPC分类号： C07D501/00

摘要： A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl, fluorine-substituted lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms, or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

公开(公告)号：US5563265A

公开(公告)日：1996-10-08

申请号：US393074

申请日：1995-02-23

申请人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

发明人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/18 ,  C07D501/26 ,  C07D501/28 ,  C07D501/34 ,  C07D501/36 ,  C07D501/60

CPC分类号： C07D501/00

摘要： A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl, fluorine-substituted lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms, or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

摘要翻译： 由下式（1）表示的7-酰基-3-取代氨基甲酰氧基头孢烯化合物：其中A表示-CH =或-N =基团; R1表示羟基，低级烷氧基，氟取代的低级烷氧基或被保护的羟基; R2和R3相同或不同，分别表示低级烷基，羟基取代的低级烷基，氨基甲酰取代的低级烷基或氰基取代的低级烷基，R2是氢原子，R3是低级烷氧基或烷基 任选地被一个或多个卤素原子取代，或者“IMAGE”是指含有一个氮原子或吗啉基的4-6元杂环基，所述杂环基或吗啉基任选被一个或多个低级烷基 ，羟基和/或羟基取代的低级烷基; R4表示羧基或被保护的羧基; 或其药学上可接受的盐; 及其制备方法; 以及含有上述头孢烯化合物的抗菌组合物。

公开(公告)号：US5162347A

公开(公告)日：1992-11-10

申请号：US703208

申请日：1991-05-20

申请人： Hitoshi Oinuma ,  Motosuke Yamanaka ,  Kazutoshi Miyake ,  Tomonori Hoshiko ,  Norio Minami ,  Tadao Shoji ,  Yoshiharu Daiku ,  Kohei Sawada ,  Kenichi Nomoto

发明人： Hitoshi Oinuma ,  Motosuke Yamanaka ,  Kazutoshi Miyake ,  Tomonori Hoshiko ,  Norio Minami ,  Tadao Shoji ,  Yoshiharu Daiku ,  Kohei Sawada ,  Kenichi Nomoto

IPC分类号： C07D211/14 ,  C07D211/32 ,  C07D211/54 ,  C07D213/38 ,  C07D401/06

CPC分类号： C07D401/06 ,  C07D211/14 ,  C07D211/32 ,  C07D211/54 ,  C07D213/38

摘要： A piperidine compound has the generic formula and is useful to treat arrhythmia. ##STR1## in which R1 is a lower alkyl and W is: ##STR2## X is --S--, --SO-- or --SO2--, R2 is hydrogen or --(CH2)n--Y, n is an integer of 1 to 5, Y is an aryl, pyridyl or a substituted pyridyl, X' is --CO-- or --CH(OH)--,p is an integer of 1 to 4, R12 is hydrogen or a lower alkyl, Y' is --(CH2)m--A, m is 1 or 2, A is an aryl, a substituted aryl, pyridyl or a substituted pyridyl, R12 and Y may form a 5- or 6-membered ring or a 5- or 6-membered ring having one or more substituents andR22 is hydrogen, a halogen, a lower alkyl, a lower alkoxy or hydroxy.

摘要翻译： 哌啶化合物具有通用的结构，可用于治疗心律失常。 （3）X是-S-，-SO-或-SO 2 - ，R 2（R 2），其中R 1是低级烷基，W是： 是氢或 - （CH 2）n Y，n是1至5的整数，Y是芳基，吡啶基或取代的吡啶基，X'是-CO-或-CH（OH） - ，p是1〜 4，R 12是氢或低级烷基，Y'是 - （CH 2）mA，m是1或2，A是芳基，取代的芳基，吡啶基或取代的吡啶基，R 12和Y可以形成5-或6 环或具有一个或多个取代基的5或6元环，R 22是氢，卤素，低级烷基，低级烷氧基或羟基。

公开(公告)号：US5118689A

公开(公告)日：1992-06-02

申请号：US594079

申请日：1990-10-09

申请人： Hitoshi Oinuma ,  Motosuke Yamanaka ,  Kazutoshi Miyake ,  Tomonori Hoshiko ,  Norio Minami ,  Tadao Shoji ,  Yoshiharu Daiku ,  Kohei Sawada ,  Kenichi Nomoto

发明人： Hitoshi Oinuma ,  Motosuke Yamanaka ,  Kazutoshi Miyake ,  Tomonori Hoshiko ,  Norio Minami ,  Tadao Shoji ,  Yoshiharu Daiku ,  Kohei Sawada ,  Kenichi Nomoto

IPC分类号： C07D473/08 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/451 ,  A61K31/50 ,  A61K31/505 ,  A61P9/06 ,  C07D207/08 ,  C07D211/22 ,  C07D211/28 ,  C07D211/32 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D417/04 ,  C07D417/06 ,  C07D471/04 ,  C07D473/10

CPC分类号： C07D401/04 ,  C07D211/28 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/10

摘要： A new piperidine compound is pharmacologically effective for treatment of arrythmia and has the formula: ##STR1## in which R.sup.1 is lower alkyl or tolyl; R.sup.2 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl or cycloalkylalkyl; X is --CO--, --CH.sub.2 -- or --CHOH--; the sum of g plus h equals the integer 3 or 4 with g and h being 1, 2 or 3; A is substituted or unsubstituted alkylene, alkenylene, --(CH.sub.2).sub.k --S--, wherein k is an integer of 2 to 5, or --(CH.sub.2).sub.p CO--, wherein p is an integer of 1 to 4; and B is a compound having at least one heterocyclic ring containing a nitrogen atom.

公开(公告)号：US4791202A

公开(公告)日：1988-12-13

申请号：US81778

申请日：1987-08-05

申请人： Motosuke Yamanaka ,  Kazutoshi Miyake ,  Shinji Suda ,  Hideto Ohhara ,  Toshiaki Ogawa

发明人： Motosuke Yamanaka ,  Kazutoshi Miyake ,  Shinji Suda ,  Hideto Ohhara ,  Toshiaki Ogawa

IPC分类号： C07D213/64 ,  A61K31/435 ,  A61K31/437 ,  A61K31/44 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  C07D213/78 ,  C07D471/04

CPC分类号： C07D471/04

摘要： 5-(6-Imidazo[1,2-a]pyridyl)pyridine derivatives represented by general formula: ##STR1## wherein X represents hydrogen atom or methyl group; Y represents cyano group, carboxamido group, hydrogen atom, amino group or a halogen atom; Z represents hydrogen atom or a lower alkyl group; W represents hydrogen atom or a lower alkyl group; R.sup.1 represents hydrogen atom, a lower alkyl group, phenyl group, a group shown by formula: --CH.sub.2 R.sup.4 in which R.sup.4 is a lower alkoxy group, or a group shown by formula: ##STR2## in which R.sup.5 and R.sup.6 are hydrogen atom or a lower alkyl group; R.sup.2 represents hydrogen atom or a halogen atom; and R.sup.3 represents hydrogen atom, a lower alkyl group or a halogen atom; or a tautomer thereof; and pharmacologically acceptable salts thereof are disclosed. The 5-(6-imidazo[1,2-a]pyridyl) pyridine derivatives are effective for treating congestive heart failures.

公开(公告)号：US5604217A

公开(公告)日：1997-02-18

申请号：US463353

申请日：1995-06-05

申请人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

发明人： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/18 ,  C07D501/26 ,  C07D501/28 ,  C07D501/34 ,  C07D501/36

CPC分类号： C07D501/00

摘要： A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl, fluorine-substituted lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

摘要翻译： 由下式（1）表示的7-酰基-3-取代氨基甲酰氧基头孢烯化合物：其中A表示-CH =或-N =基团; R1表示羟基，低级烷氧基，氟取代的低级烷氧基或被保护的羟基; R2和R3相同或不同，分别表示低级烷基，羟基取代的低级烷基，氨基甲酰取代的低级烷基或氰基取代的低级烷基，R2是氢原子，R3是低级烷氧基或烷基 任选地被一个或多个卤素原子取代，或者“IMAGE”是指含有一个氮原子或吗啉基的4-6元杂环基，所述杂环基或吗啉基任选被一个或多个低级烷基取代， 羟基和/或羟基取代的低级烷基; R4表示羧基或被保护的羧基; 或其药学上可接受的盐; 及其制备方法; 以及含有上述头孢烯化合物的抗菌组合物。