公开(公告)号：US4180655A

公开(公告)日：1979-12-25

申请号：US870884

申请日：1978-01-20

申请人： Tetsuo Suami ,  Tomoya Machinami ,  Takashi Hisamatsu

发明人： Tetsuo Suami ,  Tomoya Machinami ,  Takashi Hisamatsu

IPC分类号： C07H13/12 ,  C07H15/04 ,  C07H15/12 ,  C07H15/20

CPC分类号： C07H13/12 ,  C07H15/04 ,  C07H15/12 ,  Y10S514/908

摘要： New nitrosourea derivatives are provided, which possess a high inhibitory activity against the leukemia and tumors with a low toxicity and which are useful for pharmaceutical purposes. The compounds have the formula ##STR1## wherein A represents a glycosyl group, a monovalent residue of methyl glucoside or of alditol, a N-substituted carbamoyloxyalkyl group or a hydroxy-substituted cyclohexyl group when n is 1, or A represents a tetravalent residue of ribostamycin when n is 4 and R represents a lower alkyl or halo-alkyl group and are prepared by treating a compound of the formula ##STR2## with a nitrosating agent.

摘要翻译： 提供了新的亚硝基脲衍生物，其对白血病和低毒性的肿瘤具有高的抑制活性并且可用于制药目的。 所述化合物具有式（A）表示糖基，当n为1时甲基葡糖苷或糖醇的一价残基，N-取代氨基甲酰氧基烷基或羟基取代的环己基，或A表示四价残基 当n为4并且R代表低级烷基或卤代烷基时，为核糖霉素，并且通过用亚硝酸化剂处理式“IMAGE”的化合物来制备。

公开(公告)号：US4086415A

公开(公告)日：1978-04-25

申请号：US600206

申请日：1975-07-30

申请人： Tetsuo Suami ,  Tomoya Machinami ,  Takashi Hisamatsu

发明人： Tetsuo Suami ,  Tomoya Machinami ,  Takashi Hisamatsu

IPC分类号： C07H13/12 ,  A61K31/70 ,  A61K31/7024 ,  A61P35/00 ,  A61P35/02 ,  C07C67/00 ,  C07C239/00 ,  C07C275/68 ,  C07H15/12 ,  C07H15/23 ,  C07H11/02

CPC分类号： C07H15/12 ,  C07H15/23 ,  Y10S514/908

摘要： New nitrosourea derivatives are provided, which possess a high inhibitory activity against the leukemia and tumors with a low toxicity and which are useful for pharmaceutical purposes. The compounds have the formula ##STR1## WHEREIN A represents a glycosyl group, a monovalent residue of methyl glucoside or of alditol, a N-substituted carbamoyloxyalkyl group or a hydroxy-substituted cyclohexyl group when n is 1, or A represents a tetravalent residue of ribostamycin when n is 4 and R represents a lower alkyl or halo-alkyl group and are prepared by treating a compound of the formula ##STR2## WITH A NITROSATING AGENT.

摘要翻译： 提供了新的亚硝基脲衍生物，其对白血病和低毒性的肿瘤具有高的抑制活性并且可用于制药目的。 当n为1时，化合物具有下式：其中A表示糖基，甲基葡糖苷或糖醇的一价残基，N-取代的氨基甲酰氧基烷基或羟基取代的环己基，或A表示四价残基 当n为4并且R代表低级烷基或卤代烷基时，并且通过用硝基化剂处理式“化合物”制备的核糖霉素。

公开(公告)号：US5171746A

公开(公告)日：1992-12-15

申请号：US683176

申请日：1991-04-09

申请人： Tomoya Machinami ,  Kazue Yasufuku ,  Seiji Shibahara ,  Yasukatsu Yuda ,  Fumiya Hirano

发明人： Tomoya Machinami ,  Kazue Yasufuku ,  Seiji Shibahara ,  Yasukatsu Yuda ,  Fumiya Hirano

IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/443 ,  A61K31/445 ,  A61K31/454 ,  A61K31/535 ,  A61K31/5355 ,  A61P1/04 ,  C07D233/84 ,  C07D235/28 ,  C07D277/20 ,  C07D277/36 ,  C07D277/56 ,  C07D277/74 ,  C07D277/76 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D417/04 ,  C07D417/12

CPC分类号： C07D417/04 ,  C07D235/28 ,  C07D277/36 ,  C07D277/56 ,  C07D277/74 ,  C07D277/76 ,  C07D417/12

摘要： A thiazole or imidazole derivative having the general formula (I): ##STR1## wherein: R.sup.1 and R.sup.2, which may be the same or different, each independently represent a hydrogen atom, or a phenyl or heteroaryl group, or R.sup.1 and R.sup.2 may together form a benzene ring which may be optionally substituted by a halogen atom or a lower alkyl optionally substituted by a halogen atom, lower alkoxy or nitro group;A represents a sulfur atom or --NH--;B represents a lower alkoxy group optionally substituted by a halogen atom; a five- or six-membered saturated heterocyclic ring containing one nitrogen or oxygen atom which ring may be optionally substituted; a six-membered saturated heterocyclic ring containing one oxygen atom plus one nitrogen atom; a group --XR.sup.3 where X represents a group --NR.sup.4 wherein R.sup.3 and R.sup.4, which may be the same or different, each independently represent a lower alkyl group; or a group --NHC(.dbd.Y)R.sup.5 where Y represents an oxygen or sulfur atom or a group .dbd.NCN or .dbd.CHNO.sub.2, and R.sup.5 represents a group --NHR.sup.6 or --SR.sup.6 wherein R.sup.6 represents a lower alkyl group optionally substituted by a halogen atom;m is an integer from 1 to 4; andn is an integer from 0 to 2;and their pharmacologically acceptable salts. The compounds have an antiulcerative activity.

公开(公告)号：US5190952A

公开(公告)日：1993-03-02

申请号：US549136

申请日：1990-07-05

申请人： Nobuto Minowa ,  Tomoya Machinami ,  Seiji Shibahara ,  Keiichi Imamura ,  Michiaki Iwata ,  Masaru Shimura ,  Shigeharu Inouye

发明人： Nobuto Minowa ,  Tomoya Machinami ,  Seiji Shibahara ,  Keiichi Imamura ,  Michiaki Iwata ,  Masaru Shimura ,  Shigeharu Inouye

IPC分类号： C07D215/22 ,  A01N43/42 ,  A01N47/06 ,  A01N53/00 ,  C07D215/233 ,  C07D215/56 ,  C07D219/06 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07D215/233 ,  A01N43/42 ,  A01N47/06 ,  A01N53/00 ,  C07D215/56 ,  C07D219/06 ,  C07D405/12 ,  C07D409/12

摘要： A 4-acyloxyquinoline derivative represented by the general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.18 alkyl, C.sub.2 -C.sub.18 alkenyl, C.sub.3 -C.sub.10 cycloalkyl which may be optionally substituted, phenylloweralkyl, phenoxyloweralkyl, aryl group, a group OR.sup.4, where R.sup.4 represents a lower alkyl or aryl group, or a group ##STR2## where X represents an oxygen or a sulphur atom; R.sup.2 represents a hydrogen atom, a lower alkyl alkyl group or a group --COOR.sup.5 where R.sup.5 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl or C.sub.2 -C.sub.10 alkenyl group, provided that R.sup.1 does not represent OR.sup.4 when R.sup.2 is a hydrogen atom and R.sup.3 is methyl; R.sup.2 and R.sup.3 together represent a group (CH.sub.2).sub.m, wherein m is 3 or 4, and W represents a hydrogen atom, 1 to 4 halogen atoms, a lower alkyl or lower alkoxy group which may be the same or different and with which the left-hand nucleus is substituted, provided that the compound wherein R.sup.1 represents methyl, R.sup.2, R.sup.3 and W each represent a hydrogen atom is excluded.

公开(公告)号：US5399566A

公开(公告)日：1995-03-21

申请号：US752557

申请日：1991-09-10

申请人： Kiyoaki Katano ,  Hiroko Ogino ,  Eiki Shitara ,  Hiromi Watanabe ,  Jun Nagura ,  Naomi Osada ,  Yasuyuki Ichimaru ,  Fukio Konno ,  Tomoya Machinami ,  Takashi Tsuruoka

发明人： Kiyoaki Katano ,  Hiroko Ogino ,  Eiki Shitara ,  Hiromi Watanabe ,  Jun Nagura ,  Naomi Osada ,  Yasuyuki Ichimaru ,  Fukio Konno ,  Tomoya Machinami ,  Takashi Tsuruoka

IPC分类号： C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/69 ,  C07D213/70 ,  C07D213/80 ,  C07D221/04 ,  C07D401/10 ,  C07D401/12 ,  A61K31/44

CPC分类号： C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/69 ,  C07D213/70 ,  C07D213/80 ,  C07D221/04 ,  C07D401/10 ,  C07D401/12

摘要： The invention provides compounds represented by the following formula (I) ##STR1## or a pharmaceutically acceptable salts thereof wherein A represents ##STR2## B represents a carboxy or tetrazolyl group; and X represents --O--, --NH-- or --S(O).sub.t --.The compounds possess angiotensin II antagonism, and may be used as an antihypertensive agent, a therapeutic agent to congestive heart failure, an antianxiety agent and a cognitive enhancing agent.

摘要翻译： PCT No.PCT / JP91 / 00822 Sec。 371日期1991年9月10日 102（e）1991年9月10日PCT PCT 1991年6月19日PCT公布。 No.W091 / 19697 PCT出版物 1991年12月26日，本发明提供由下式（I）表示的化合物或其药学上可接受的盐，其中A表示羧基或四唑基; X表示-O - ， - NH-或-S（O）t - 。 该化合物具有血管紧张素II拮抗作用，可用作抗高血压药，充血性心力衰竭的治疗剂，抗焦虑剂和认知增强剂。

公开(公告)号：US5079255A

公开(公告)日：1992-01-07

申请号：US544671

申请日：1990-06-27

申请人： Kiyoaki Katano ,  Tamako Tomomoto ,  Hiroko Ogino ,  Yamazaki Naoki ,  Fumiya Hirano ,  Yasukatsu Yuda ,  Fukio Konno ,  Motohiro Nishio ,  Tomoya Machinami ,  Seiji Shibahara ,  Takashi Tsuruoka ,  Shigeharu Inouye

发明人： Kiyoaki Katano ,  Tamako Tomomoto ,  Hiroko Ogino ,  Yamazaki Naoki ,  Fumiya Hirano ,  Yasukatsu Yuda ,  Fukio Konno ,  Motohiro Nishio ,  Tomoya Machinami ,  Seiji Shibahara ,  Takashi Tsuruoka ,  Shigeharu Inouye

IPC分类号： C07D487/04 ,  A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P1/04 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07D471/04 ,  C07D513/04

摘要： Compounds of the general formula (I): ##STR1## and pharmaceutically acceptable salts thereof, in which A, B, C and D each represent --CH.dbd. or --N.dbd., with the proviso that at least one of them is --N.dbd.;X represents --NH--, --O-- or --S--;Y represents --(CH.sub.2).sub.p -- wherein p is an integer from 0 to 4, --C(CH.sub.3).sub.2 --, --CH.sub.2 CH.dbd.CH--, --CH.sub.2 CO--, --CF.sub.2 -- or --CH.sub.2 COCH.sub.2 --;R.sup.1 represents a hydrogen atom, a C.sub.1-4 alkyl group, a halogen atom or a C.sub.1-4 alkoxy group;R.sup.2 represents a hydrogen atom, a hydroxyl group, a saturated or unsaturated C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a carboxyl group, a saturated or unsaturated C.sub.1-12 alkoxycarbonyl group which may be optionally substituted, a cycloalkoxycarbonyl group, a saturated or unsaturated five- or six-membered heterocyclic group containing at least one nitrogen atom optionally with one or more nitrogen and/or oxygen atoms, which may be optionally condensed and/or substituted, --CONR.sup.3 R.sup.4, --NR.sup.3 R.sup.4, --OCOR.sup.3 or --NHCONHR.sup.3 wherein R.sup.3 and R.sup.4, which may be the same or different, represent a C.sub.1-6 alkyl group which may be optionally substituted or a cycloalkyl group, andm and n each represent an integer from 0 to 2.

公开(公告)号：US5294629A

公开(公告)日：1994-03-15

申请号：US037671

申请日：1993-03-25

申请人： Tomoya Machinami ,  Kazue Yasufuku ,  Seiji Shibahara ,  Fumiya Hirano ,  Yasukatsu Yuda ,  Motohiro Nishio ,  Yuji Matsuhashi ,  Takashi Tsuruoka ,  Kiyoaki Katano ,  Shigeharu Inoye

发明人： Tomoya Machinami ,  Kazue Yasufuku ,  Seiji Shibahara ,  Fumiya Hirano ,  Yasukatsu Yuda ,  Motohiro Nishio ,  Yuji Matsuhashi ,  Takashi Tsuruoka ,  Kiyoaki Katano ,  Shigeharu Inoye

IPC分类号： C07D235/28 ,  C07D277/74 ,  A61K31/415 ,  A61K31/425 ,  C07D277/76

CPC分类号： C07D235/28 ,  C07D277/74

摘要： A novel benzothiazole or benzimidazole derivative represented by formula (I) ##STR1## wherein X represents a sulfur atom or a NH group; R.sup.1 represents a hydrogen atom, a lower alkoxy group, a chlorine atom, a bromine atom or an iodine atom; R.sup.2 represents a hydrogen atom a substituted or unsubstituted lower alkyl group, a vinyl group, an aryl group or an acyl group; m is an integer of 1, 2 or 3; and n is an integer of 0, 1 or 2, which shows an excellent acid secretion suppressing effect and gastric mucosa protecting effect, and an antiulcer agent containing the same as an active ingredient.

摘要翻译： 由式（I）表示的新型苯并噻唑或苯并咪唑衍生物其中X表示硫原子或NH基团; R1表示氢原子，低级烷氧基，氯原子，溴原子或碘原子; R2代表氢原子取代或未取代的低级烷基，乙烯基，芳基或酰基; m为1,2或3的整数; n为0或1或2的整数，表现出优异的酸分泌抑制效果和胃粘膜保护作用，以及含有作为活性成分的抗溃疡剂。

公开(公告)号：US5200407A

公开(公告)日：1993-04-06

申请号：US716621

申请日：1991-06-14

申请人： Kiyoaki Katano ,  Tamako Tomomoto ,  Hiroko Ogino ,  Naoki Yamazaki ,  Fumiya Hirano ,  Yasukatsu Yuda ,  Fukio Konno ,  Motohiro Nishio ,  Tomoya Machinami ,  Seiji Shibahara ,  Takashi Tsuruoka ,  Shigeharu Inouye

发明人： Kiyoaki Katano ,  Tamako Tomomoto ,  Hiroko Ogino ,  Naoki Yamazaki ,  Fumiya Hirano ,  Yasukatsu Yuda ,  Fukio Konno ,  Motohiro Nishio ,  Tomoya Machinami ,  Seiji Shibahara ,  Takashi Tsuruoka ,  Shigeharu Inouye

IPC分类号： C07D471/04 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07D471/04 ,  C07D513/04

摘要： Compounds of the general formula (I): ##STR1## and pharmaceutically acceptable salts thereof, in which A, B, C and D each represent --CH.dbd. or --N.dbd., with the proviso that at least one of them is --N.dbd.;X represents --NH--, --O-- or --S--;Y represents --(CH.sub.2).sub.p -- wherein p is an integer from 0 to 4, --C(CH.sub.3).sub.2 --, --CH.sub.2 CH.dbd.CH--, --CH.sub.2 CO--, --CF.sub.2 -- or --CH.sub.2 COCH.sub.2 --;R.sup.1 represents a hydrogen atom, a C.sub.1-4 alkyl group, a halogen atom or a C.sub.1-4 alkoxy group;R.sup.2 represents a hydrogen atom, a hydroxyl group, a saturated or unsaturated C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a carboxyl group, a saturated or unsaturated C.sub.1-12 alkoxycarbonyl group which may be optionally substituted, a cycloalkoxycarbonyl group, a saturated or unsaturated five- or six-membered heterocyclic group containing at least one nitrogen atom optionally with one or more nitrogen and/or oxygen atoms, which may be optionally condensed and/or substituted, --CONR.sup.3 R.sup.4, --NR.sup.3 R.sup.4, --OCOR.sup.3 or --NHCONHR.sup.3 wherein R.sup.3 and R.sup.4, which may be the same or different, represent a C.sub.1-6 alkyl group which may be optionally substituted or a cycloalkyl group, andm and n each represent an integer from 0 to 2.

摘要翻译： 通式（I）的化合物：其中A，B，C和D各自表示-CH =或-N =，条件是其中至少一个为 -N =; X表示-NH-，-O-或-S-; Y表示 - （CH 2）p - ，其中p是0至4的整数，-C（CH 3）2 - ， - CH 2 CH = CH - ， - CH 2 CO - ， - CF 2 - 或-CH 2 COCH 2 - R1表示氢原子，C1-4烷基，卤素原子或C1-4烷氧基; R2表示氢原子，羟基，饱和或不饱和的C1-6烷基，C1-6烷氧基，羧基，可以任意取代的饱和或不饱和的C 1-12烷氧基羰基，环烷氧基羰基， 含有至少一个氮原子的饱和或不饱和五元或六元杂环基，任选具有一个或多个氮和/或氧原子，其可以任选地被缩合和/或取代，-CONR 3 R 4，-NR 3 R 4，-OCOR 3或 - NHCONHR 3其中R3和R4可以相同或不同，表示可以被任意取代的C 1-6烷基或环烷基，m和n各自表示0〜2的整数。

公开(公告)号：US5185347A

公开(公告)日：1993-02-09

申请号：US700985

申请日：1991-05-16

申请人： Kiyoaki Katano ,  Tamako Tomomoto ,  Hiroko Ogino ,  Fumiya Hirano ,  Yasukatsu Yuda ,  Fukio Konno ,  Tomoya Machinami ,  Takashi Tsuruoka ,  Shigeharu Inoye

发明人： Kiyoaki Katano ,  Tamako Tomomoto ,  Hiroko Ogino ,  Fumiya Hirano ,  Yasukatsu Yuda ,  Fukio Konno ,  Tomoya Machinami ,  Takashi Tsuruoka ,  Shigeharu Inoye

IPC分类号： C07D401/12 ,  A61K31/4427 ,  A61K31/445 ,  A61P1/04 ,  C07D235/28 ,  C07D401/14

CPC分类号： C07D235/28

摘要： A piperidine compound represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group having from 1 to 4 carbon atoms, a lower alkoxy group having from 1 to 4 carbon atoms, a hydroxymethyl group, --CO.sub.2 R.sup.3, or ##STR2## wherein R.sup.3 represents a hydrogen atom or a lower alkyl group having from 1 to 4 carbon atoms; R.sup.4 represents a hydroxyl group, a lower alkoxy group having from 1 to 4 carbon atoms or --NR.sup.6 R.sup.7 (wherein R.sup.6 and R.sup.7, which may be the same or different, each represent a hydrogen atom or a lower alkyl group having from 1 to 4 carbon atoms); and R.sup.5 represents a hydrogen atom, a lower alkanoyl group having from 1 to 4 carbon atoms, or a chlorobenzoyl group; R.sup.2 represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms, a substituted or unsubstituted benzyl group, or a (2,2,6,6-tetramethylpiperidin-1-yl)ethyl group; and n represents 0 or an integer of 1 or 2,and an antiulcer composition containing said piperidine compound.

公开(公告)号：US5194617A

公开(公告)日：1993-03-16

申请号：US807946

申请日：1991-12-10

申请人： Nobuto Minowa ,  Tomoya Machinami ,  Takashi Shomura ,  Masaji Sezaki ,  Toru Sasaki ,  Seiji Shibahara ,  Shigeharu Inouye

发明人： Nobuto Minowa ,  Tomoya Machinami ,  Takashi Shomura ,  Masaji Sezaki ,  Toru Sasaki ,  Seiji Shibahara ,  Shigeharu Inouye

IPC分类号： C07D215/22 ,  C07D215/233

CPC分类号： C07D215/233

摘要： 2,3-disubstituted-4-hydroxyquinoline derivatives of the general formula (I): ##STR1## [wherein R.sup.1 represents a hydrogen atom or R.sup.3 CO-- (wherein R.sup.3 is a lower alkyl group); R.sup.2 represents a hydrogen atom, --CH.sub.3 or --C.sub.2 H.sub.5 ; A represents ##STR2## and W represents a hydrogen atom, or 1- 4 halogen atoms or alkyl groups which are substituted at the nucleus and may be the same or different] have a strong antagonistic action on leukotriene D.sub.4.

摘要翻译： （I）的2,3-二取代-4-羟基喹啉衍生物：其中R1表示氢原子或R3CO-（其中R3是低级烷基）; R 2表示氢原子，-CH 3或-C 2 H 5; A表示 ，W表示氢原子或1-4个卤原子或在核上被取代且可相同或不同的烷基对白三烯D4具有强拮抗作用。