公开(公告)号：US6011069A

公开(公告)日：2000-01-04

申请号：US767624

申请日：1996-12-17

申请人： Kohei Inomata ,  Toshihiro Takahashi ,  Hitoshi Inoue ,  Makoto Yanai ,  Hiroyuki Yamazaki ,  Masashi Suzuki ,  Tsutomu Takasawa ,  Kouji Kawamura ,  Norio Oshida ,  Hiroyuki Ikemoto ,  Takao Kishiye

发明人： Kohei Inomata ,  Toshihiro Takahashi ,  Hitoshi Inoue ,  Makoto Yanai ,  Hiroyuki Yamazaki ,  Masashi Suzuki ,  Tsutomu Takasawa ,  Kouji Kawamura ,  Norio Oshida ,  Hiroyuki Ikemoto ,  Takao Kishiye

IPC分类号： A61K31/137 ,  A01N33/02

CPC分类号： A61K31/137

摘要： There is disclosed a multidrug resistance inhibitor for overcoming a multidrug resistance of cancer, or an agent for enhancing the activity of anti-cancer agents, which comprises as an active ingredient a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein n is an integer of 5 to 12,R.sub.1 and R.sub.2 are each independently benzyl, of which a phenyl ring may be substituted by 1 to 5 substituents selected from hydroxy, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and halogen, and/or by methylenedioxy, with the proviso that R.sub.1 and R.sub.2 are simultaneously not a compound of formula (II) ##STR2##

摘要翻译： 公开了用于克服癌症的多药耐药性的多药耐药性抑制剂或增强抗癌剂活性的药剂，其包含作为活性成分的式（I）化合物或其药学上可接受的盐：其中n 为5〜12的整数，R 1和R 2各自独立地为苄基，其中苯环可被1〜5个选自羟基，（C 1 -C 4）烷基，（C 1 -C 4）烷氧基和卤素的取代基取代， /或亚甲二氧基，条件是R1和R2不是式（II）的化合物，

公开(公告)号：US5756475A

公开(公告)日：1998-05-26

申请号：US791165

申请日：1997-01-30

申请人： Kohei Inomata ,  Toshihiro Takahashi ,  Hitoshi Inoue ,  Makoto Yanai ,  Hiroyuki Yamazaki ,  Masashi Suzuki ,  Tsutomu Takasawa ,  Kouji Kawamura ,  Norio Oshida ,  Hiroyuki Ikemoto ,  Takao Kishiye

发明人： Kohei Inomata ,  Toshihiro Takahashi ,  Hitoshi Inoue ,  Makoto Yanai ,  Hiroyuki Yamazaki ,  Masashi Suzuki ,  Tsutomu Takasawa ,  Kouji Kawamura ,  Norio Oshida ,  Hiroyuki Ikemoto ,  Takao Kishiye

IPC分类号： C07C211/29 ,  C07C217/58 ,  C07D207/14 ,  C07D295/13 ,  C07D498/08 ,  A01N43/04 ,  A01N33/02 ,  C07C211/00

CPC分类号： C07D295/13 ,  C07C211/29 ,  C07C217/58 ,  C07D207/14 ,  C07C2101/04 ,  C07C2103/18 ,  Y10S514/937 ,  Y10S514/938

摘要： Isoprene derivatives of formula (I) ##STR1## wherein m is an integer of 0 to 3, n is an integer of 5 to 12, A is cyclo(C.sub.3 -C.sub.6)alkylene, phenylene, fluorenylene, pyrrolidinylene, piperazinylene, 9-aza-3-oxabicyclo�3.3.1!-nonylene, R.sub.1 and R.sub.2 are each independently benzyl, of which a phenyl ring may be substituted by 1 to 5 substituents selected from the group consisting of hydroxy, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and halogen, X is a single bond or a divalent radical of --(CH.sub.2).sub.p NH--, p is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof. Those compounds are useful as multidrug resistance inhibitors for overcoming multidrug resistance of cancer and agents for enhancing an activity of anti-cancer agents.

摘要翻译： 式（I）的异戊二烯衍生物其中m为0〜3的整数，n为5〜12的整数，A为环（C 3〜C 6）亚烷基，亚苯基，亚芴基，吡咯烷基， 9-氮杂-3-氧杂双环[3.3.1] - 亚芳基，R 1和R 2各自独立地为苄基，其中苯环可被1至5个选自羟基，（C 1 -C 4）烷基 ，（C1-C4）烷氧基和卤素，X是 - （CH2）pNH-的单键或二价基团，p是0-3的整数，或其药学上可接受的盐。 那些化合物可用作克服癌症多药耐药性和增强抗癌药活性的药物的多药耐药性抑制剂。

公开(公告)号：US5380723A

公开(公告)日：1995-01-10

申请号：US228505

申请日：1994-04-15

申请人： Toshihiro Takahashi ,  Hitoshi Inoue ,  Masato Horigome ,  Kenichi Momose ,  Masanori Sugita ,  Kouichi Katsuyama ,  Chikako Suzuki ,  Shinji Nagai ,  Masao Nagase ,  Koichi Nakamaru

发明人： Toshihiro Takahashi ,  Hitoshi Inoue ,  Masato Horigome ,  Kenichi Momose ,  Masanori Sugita ,  Kouichi Katsuyama ,  Chikako Suzuki ,  Shinji Nagai ,  Masao Nagase ,  Koichi Nakamaru

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/454 ,  A61K31/47 ,  A61K31/4725 ,  A61K31/5377 ,  A61P1/04 ,  C07D209/14 ,  C07D209/16 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D403/14 ,  C07D413/14

CPC分类号： C07D401/14 ,  C07D209/16

摘要： Disclosed are indole derivatives of formula (I) ##STR1## wherein X and Y each independently represent H or --CH.sub.2 CH.sub.2 R; R represents pyridyl or substituted amino of NR.sub.1 R.sub.2 ;R.sub.1 represents H or C.sub.1 -C.sub.6 alkyl;R.sub.2 represents 2-(3-indolyl)ethyl or aralkyl; orR.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached may form an N-containing 5 to 6 membered hetero ring, an N, O-containing hetero ring, which hetero ring may be fused with benzene;n is an integer of 4 to 8;with the proviso that X and Y both do not represent H or piperizinoethyl when n is 4, or pharmaceuticaly acceptable acid addition salts thereof. They are useful as an antiulcer agent.

摘要翻译： 公开了式（I）的吲哚衍生物其中X和Y各自独立地表示H或-CH 2 CH 2 R; R代表NR1R2的吡啶基或取代氨基; R1代表H或C1-C6烷基; R2代表2-（3-吲哚基）乙基或芳烷基; 或R 1和R 2与它们所连接的氮原子一起可以形成含N的5至6元杂环，含N，O的杂环，该杂环可以与苯稠合; n为4〜8的整数， 条件是当n为4时X和Y都不表示H或哌嗪子基，或其药学上可接受的酸加成盐。 它们作为抗溃疡剂是有用的。

公开(公告)号：US5326879A

公开(公告)日：1994-07-05

申请号：US949028

申请日：1992-09-22

申请人： Toshihiro Takahashi ,  Hitoshi Inoue ,  Masato Horigome ,  Kenichi Momose ,  Masanori Sugita ,  Kouichi Katsuyama ,  Chikako Suzuki ,  Shinji Nagai ,  Masao Nagase ,  Koichi Nakamaru

发明人： Toshihiro Takahashi ,  Hitoshi Inoue ,  Masato Horigome ,  Kenichi Momose ,  Masanori Sugita ,  Kouichi Katsuyama ,  Chikako Suzuki ,  Shinji Nagai ,  Masao Nagase ,  Koichi Nakamaru

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/454 ,  A61K31/47 ,  A61K31/4725 ,  A61K31/5377 ,  A61P1/04 ,  C07D209/14 ,  C07D209/16 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D403/06

CPC分类号： C07D401/14 ,  C07D209/16

摘要： Disclosed are indole derivatives of formula (I) ##STR1## wherein X and Y each independently represent H or --CH.sub.2 CH.sub.2 R;R represents pyridyl or substituted amino of NR.sub.1 R.sub.2 ;R.sub.1 represents H or C.sub.1 -C.sub.6 alkyl;R.sub.2 represents 2-(3-indolyl)ethyl or aralkyl; orR.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached may form an N-containing 5 to 6 membered hetero ring, an N, O-containing hetero ring, which hetero ring may be fused with benzene;n is an integer of 4 to 8;with the proviso that X and Y both do not represent H or piperizinoethyl when n is 4, or pharmaceuticaly acceptable acid addition salts thereof. They are useful as an antiulcer agent.

摘要翻译： 公开了式（I）的吲哚衍生物代表H或-CH 2 CH 2 R; R代表NR1R2的吡啶基或取代氨基; R1代表H或C1-C6烷基; R2代表2-（3-吲哚基）乙基或芳烷基; 或R 1和R 2与它们所连接的氮原子一起可以形成含N的5至6元杂环，含N，O的杂环，该杂环可以与苯稠合; n为4〜8的整数， 条件是当n为4时X和Y都不表示H或哌嗪子基，或其药学上可接受的酸加成盐。 它们作为抗溃疡剂是有用的。

公开(公告)号：US5252580A

公开(公告)日：1993-10-12

申请号：US947169

申请日：1992-09-18

申请人： Toshihiro Takahashi ,  Hitoshi Inoue ,  Masato Horigome ,  Kenichi Momose ,  Masanori Sugita ,  Kouichi Katsuyama ,  Chikako Suzuki ,  Shinji Nagai ,  Masao Nagase ,  Koichi Nakamaru

发明人： Toshihiro Takahashi ,  Hitoshi Inoue ,  Masato Horigome ,  Kenichi Momose ,  Masanori Sugita ,  Kouichi Katsuyama ,  Chikako Suzuki ,  Shinji Nagai ,  Masao Nagase ,  Koichi Nakamaru

IPC分类号： A61K31/395 ,  A61K31/435 ,  A61K31/437 ,  A61P1/04 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D519/00 ,  A61K31/445 ,  C07D401/06

CPC分类号： C07D471/04

摘要： Disclosed are indole derivatives of formula (I) ##STR1## wherein Y represents H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or halogen;Z represents --CH.sub.2 N(R.sub.5)--;R represents H or --CH.sub.2 CH.sub.2 X where X represents pyridyl, aralkyloxy or substituted amino of NR.sub.6 R.sub.7 where R.sub.6 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl, C.sub.1 -C.sub.6 alkoxycarbonyl, aralkyloxycarbonyl or halogenated C.sub.1 -C.sub.6 alkoxycarbonyl and R.sub.7 represents H, C.sub.1 -C.sub.6 alkyl or aralkyl, or together with R.sub.2 may form a ring of --(CH.sub.2).sub.n -- (n is 1-4) or ##STR2## R.sub.1 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl or arylsulfonyl; R.sub.2 represents C.sub.1 -C.sub.6 alkyl, hydroxy, C.sub.1 -C.sub.6 alkoxy or aralkyloxy;R.sub.3 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl or halogenated C.sub.1 -C.sub.6 alkyl;R.sub.4 and R.sub.5 may be the same or different and each represents H, C.sub.1 -C.sub.6 alkyl or aralkyl or both may together form a ring of --(CH.sub.2).sub.m -- (m is 3 or 4);or pharmaceutically acceptable acid addition salts thereof. They are useful as an antiulcer agent.

公开(公告)号：US20080194826A1

公开(公告)日：2008-08-14

申请号：US12077687

申请日：2008-03-20

申请人： Ryuuta Fukutomi ,  Hitoshi Inoue ,  Koji Kawamura ,  Takuya Kishimoto ,  Masashi Suzuki ,  Rie Shibayama ,  Kazuko Kojima ,  Kouichirou Hagihara

发明人： Ryuuta Fukutomi ,  Hitoshi Inoue ,  Koji Kawamura ,  Takuya Kishimoto ,  Masashi Suzuki ,  Rie Shibayama ,  Kazuko Kojima ,  Kouichirou Hagihara

IPC分类号： C07D401/12 ,  C07D211/58

CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14

摘要： A compound represented the general formula (V): wherein X is CH or N; and Ya is a group of the general formula selected from:

摘要翻译： 化合物为通式（Ⅴ）：其中X为CH或N; 并且Y a a是选自以下的通式的基团：

公开(公告)号：US20050085508A1

公开(公告)日：2005-04-21

申请号：US10492065

申请日：2002-10-08

申请人： Ryuuta Fukutomi ,  Hitoshi Inoue ,  Koji Kawamura ,  Takuya Kishimoto ,  Masashi Suzuki ,  Rie Shibayama ,  Kazuko Kojima ,  Kouichirou Hagihara

发明人： Ryuuta Fukutomi ,  Hitoshi Inoue ,  Koji Kawamura ,  Takuya Kishimoto ,  Masashi Suzuki ,  Rie Shibayama ,  Kazuko Kojima ,  Kouichirou Hagihara

IPC分类号： A61P1/04 ,  A61P1/08 ,  A61P1/10 ,  A61P17/04 ,  A61P43/00 ,  C07D211/58 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  A61K31/445

CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14

摘要： There are provided novel 4-(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is CH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N—R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxycarbonyl group, or the like. The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid μ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by μ receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.

摘要翻译： 提供由通式（I）表示的新型4-（2-糠酰基）氨基哌啶，其合成中间体，其制备方法和含有它们的药物。 在上式中，X是CH或N，Y是下列通式（II），式（II-a）或式（III）的基团：其中a，b和c各自为0〜 6; Z是CH 2或NH; W为O或S; T是O或N-R 15，其中R 15是H，C 1 -C 6烷基，苄基或苯乙基; R 1是H，C 1 -C 6烷氧基羰基，苄氧基羰基等。 根据本发明的4-（2-糠酰基）氨基哌啶衍生物具有阿片样物质μ拮抗活性，可用于治疗或预防由mu受体激动剂引起的副作用，其选自便秘，恶心/呕吐或瘙痒， 或用于治疗或预防特发性便秘，术后肠梗阻，麻痹性肠梗阻，肠易激综合征或慢性瘙痒。

公开(公告)号：US07375115B2

公开(公告)日：2008-05-20

申请号：US10492065

申请日：2002-10-08

申请人： Ryuuta Fukutomi ,  Hitoshi Inoue ,  Koji Kawamura ,  Takuya Kishimoto ,  Masashi Suzuki ,  Rie Shibayama ,  Kazuko Kojima ,  Kouichirou Hagihara

发明人： Ryuuta Fukutomi ,  Hitoshi Inoue ,  Koji Kawamura ,  Takuya Kishimoto ,  Masashi Suzuki ,  Rie Shibayama ,  Kazuko Kojima ,  Kouichirou Hagihara

IPC分类号： A01N43/40 ,  C07D401/00

CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14

摘要： There are provided novel 4(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is OH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N—R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxy-carbonyl group, or the like. The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid μ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by μ receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.

摘要翻译： 提供由通式（I）表示的新型4（2-糠酰基）氨基哌啶，其合成中间体，其制备方法和含有它们的药物。 在上式中，X为OH或N，Y为下列通式（II），式（II-a）或式（III）的基团：其中a，b和c各自为0〜 6; Z是CH 2或NH; W为O或S; T是O或N-R 15，其中R 15是H，C 1 -C 6烷基，苄基或苯乙基; R 1是H，C 1 -C 6烷氧基羰基，苄氧基羰基等。 根据本发明的4-（2-糠酰基）氨基哌啶衍生物具有阿片样物质μ拮抗活性，可用于治疗或预防由mu受体激动剂引起的副作用，其选自便秘，恶心/呕吐或瘙痒， 或用于治疗或预防特发性便秘，术后肠梗阻，麻痹性肠梗阻，肠易激综合征或慢性瘙痒。

公开(公告)号：US6048882A

公开(公告)日：2000-04-11

申请号：US875759

申请日：1997-08-08

申请人： Tatsuya Ohwaki ,  Masako Yamada ,  Hiroyuki Yamazaki ,  Hitoshi Inoue ,  Yoshiyuki Tahara ,  Shigeo Kawase

发明人： Tatsuya Ohwaki ,  Masako Yamada ,  Hiroyuki Yamazaki ,  Hitoshi Inoue ,  Yoshiyuki Tahara ,  Shigeo Kawase

IPC分类号： C07C211/27 ,  C07C211/29 ,  C07C215/50 ,  C07C217/58 ,  C07D213/38 ,  C07D307/52 ,  C07D317/58 ,  C07D317/66 ,  C07D333/20 ,  A61K31/34 ,  A61K31/36

CPC分类号： C07D213/38 ,  C07C211/27 ,  C07C211/29 ,  C07C215/50 ,  C07C217/58 ,  C07D307/52 ,  C07D317/58 ,  C07D317/66 ,  C07D333/20

摘要： Hepatic diseases can be prevented or treated by administering an isoprenylamine derivative represented by the general formula (II) ##STR1## [wherein n represents an integer of 4-12, m represents an integer of 0-3, Ar represents a phenyl group, a furyl group, a thienyl group or a pyridyl group, said group being optionally substituted with one or more of an alkyl group of 1-4 carbon atoms, and alkoxy group of 1-4 carbon atoms, a methylenedioxy group, a hydroxy group or a halogen atom, and R represents a hydrogen atom or an alkyl group of 1-4 carbon atoms] or a pharmacologically acceptable salt thereof at a daily dose of 0.01-500 .mu.g/kg.A lipid emulsion of the compound (II) is particularly useful and can be administered at a remarkably lowered dose as compared with other pharmaceutical preparations.

摘要翻译： PCT No.PCT / JP96 / 00255 Sec。 371日期：1997年8月8日 102（e）日期1997年8月8日PCT提交1996年2月7日PCT公布。 出版物WO96 / 24575 日期：1996年8月15日可以通过施用通式（II）表示的异戊二烯胺衍生物[其中n表示4-12的整数，m表示0-3的整数，Ar表示苯基 ，呋喃基，噻吩基或吡啶基，所述基团任选被一个或多个1-4个碳原子的烷基和1-4个碳原子的烷氧基，亚甲二氧基，羟基 或卤素原子，R表示氢原子或1-4个碳原子的烷基]或其​​药理学上可接受的盐，日剂量为0.01-500μg/ kg。 化合物（II）的脂质乳剂特别有用，与其它药物制剂相比，可以以显着降低的剂量给药。

公开(公告)号：US20130137055A1

公开(公告)日：2013-05-30

申请号：US13503259

申请日：2010-09-07

申请人： Makoto Hirano ,  Hitoshi Inoue

发明人： Makoto Hirano ,  Hitoshi Inoue

IPC分类号： F27B3/20

CPC分类号： F27B3/205 ,  C03B5/235 ,  F23C5/28 ,  F23C2900/07021 ,  F23D14/22 ,  F23D23/00 ,  F27D7/02 ,  F27D17/004 ,  F27D17/008 ,  F27D99/0033

摘要： A combustion device for a melting furnace, capable of heating a melting target object and the ceiling portion of the furnace with the radiant heat of the flame, including a combustion space above the location of the melting target object, including a fuel injection nozzle having a plurality of fuel injecting portions, which portions include orifices disposed side by side horizontally relative to the direction of fuel injection, and formed side by side vertically relative to the same. The orifices are formed radially side by side as seen laterally, with a direction along a middle angle in the angular range between the fuel injection direction of the uppermost fuel injection orifice and the fuel injection direction of the lowermost fuel injection orifice being directed obliquely upwards. The fuel injection orifices of the upper fuel injecting portion are formed radially side by side as seen in the plane view.

摘要翻译： 一种用于熔化炉的燃烧装置，其能够利用火焰的辐射热加热熔化物体和熔炉的顶部，包括在熔化目标物体的位置上方的燃烧空间，包括具有 多个燃料喷射部分，这些部分包括相对于燃料喷射方向水平并排布置的孔，并且相对于其相互垂直并排地形成。 这些孔径向并排地形成，如横向看到的那样，在最上面的燃料喷射孔的燃料喷射方向和最下面的燃料喷射孔的燃料喷射方向之间的角度范围内沿着中角的方向倾斜向上指向。 上部燃料喷射部的燃料喷射孔在平面图中看到的径向并排地形成。