公开(公告)号：US4873253A

公开(公告)日：1989-10-10

申请号：US31738

申请日：1987-03-30

申请人： Shosuke Okamoto ,  Yoshio Okada ,  Akiko Okunomiya ,  Taketoshi Naito ,  Yoshio Kimura ,  Morihiko Yamada ,  Norio Ohno ,  Yasuhiro Katsuura ,  Hiroshi Nojima ,  Takashi Shishikura

发明人： Shosuke Okamoto ,  Yoshio Okada ,  Akiko Okunomiya ,  Taketoshi Naito ,  Yoshio Kimura ,  Morihiko Yamada ,  Norio Ohno ,  Yasuhiro Katsuura ,  Hiroshi Nojima ,  Takashi Shishikura

IPC分类号： C07D211/60 ,  C07D211/62 ,  C07D213/64 ,  C07D213/643 ,  C07D213/75 ,  C07D213/80 ,  C07D233/88 ,  C07D239/42 ,  C07D257/06 ,  C07D277/46 ,  C07D295/185

CPC分类号： C07D213/643 ,  C07D211/60 ,  C07D211/62 ,  C07D213/75 ,  C07D213/80 ,  C07D233/88 ,  C07D239/42 ,  C07D257/06 ,  C07D277/46 ,  C07D295/185

摘要： A phenylalanine derivative having the formula (I): ##STR1## wherein A represents ##STR2## B represents ##STR3## wherein m is 0, 1, or 2 and n is 3, 4, or 5; X represents (a) hydroxy, (b) nitro, (c) amino, (d) phenoxy which may be substituted with (i) halogen or (ii) nitro, (e) c.sub.1 -C.sub.4 alkyloxy which may be substituted wit (i) phenyl or (ii) benzoyl, (f) benzoyl, (g) pyridyloxy which may be substituted with (i) halogen or (ii) nitro, or (h) c.sub.1 -C.sub.4 alkyl which may by substituted with halogen;Y represents ##STR4## or --OR.sup.3 wherein R.sup.1 R.sup.2 are independently (a) hydrogen, (b) phenyl which may be substituted with (i) benzoyl, (ii) C.sub.1 -C.sub.4 alkylcarbonyl, (iii) C.sub.1 -C.sub.4 alkyl which may be further substituted with C.sub.1 -C.sub.4 alkoxycarbonyl or hydroxycarbonyl, (iv) C.sub.2 -C.sub.5 alkenyl which may be further substituted with hydroxycarbonyl or C.sub.1 -C.sub.4 alkoxycarbonyl, (v) C.sub.1 -C.sub.4 alkoxycarbonyl, or (vi) amidino, (c) pyridyl which may be substituted with halogen or carboxyl (d) imidazolyl, (e) pyrimidyl, (f) tetrazolyl, (g) thiazolyl which may be substituted with C.sub.1 -C.sub.4 alkyl which may be further substituted with C.sub.1 -C.sub.4 alkoxycarbonyl, (h) C.sub.1 -C.sub.6 alkyl which may be substituted with C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkoxycarbonyl, phenyl, or benzoyl, (i) C.sub.5 -C.sub.7 cycloalkyl which may be substituted with C.sub.1 -C.sub.4 alkoxycarbonyl or (j) R.sup.1 and R.sup.2 may form, with the nitrogen atom attached thereto, (i) pyperazyl which may be substituted on the nitrogen atom with C.sub.1 -C.sub.4 alkyl which may be further substituted with phenyl, (ii) piperidino which may be substituted with carboxyl or C.sub.1 -C.sub.4 alkoxycarbonyl, (iii) pyrrolidyl which may be substituted with C.sub.1 -C.sub.4 alkoxycarbonyl, or (iv) morpholyl; andR.sup.3 represents (a) hydrogen, (b) C.sub.1 -C.sub.6 alkyl which may be substituted with (i) C.sub.1 -C.sub.4 alkoxy, (ii) pehnyl, or (iii) pyridyl, or (c) pyridyl; or a pharmaceutically acceptable acid salt thereof.This phenylalanine derivative is effective as a proteinase.

公开(公告)号：US4895842A

公开(公告)日：1990-01-23

申请号：US912480

申请日：1986-09-29

申请人： Shosuke Okamoto ,  Yoshio Okada ,  Akiko Okunomiya ,  Taketoshi Naito ,  Yoshio Kimura ,  Morihiko Yamada ,  Norio Ohno ,  Yasuhiro Katsuura ,  Yumi Seki

发明人： Shosuke Okamoto ,  Yoshio Okada ,  Akiko Okunomiya ,  Taketoshi Naito ,  Yoshio Kimura ,  Morihiko Yamada ,  Norio Ohno ,  Yasuhiro Katsuura ,  Yumi Seki

IPC分类号： A61K38/00 ,  C07D211/16 ,  C07D211/32 ,  C07D211/62 ,  C07D213/30 ,  C07D213/40 ,  C07D213/64 ,  C07D213/643 ,  C07D213/75 ,  C07D239/42 ,  C07D295/185 ,  C07D307/14 ,  C07D401/12 ,  C07K5/065

CPC分类号： C07D213/30 ,  C07D211/16 ,  C07D211/32 ,  C07D211/62 ,  C07D213/40 ,  C07D213/643 ,  C07D213/75 ,  C07D239/42 ,  C07D295/185 ,  C07D307/14 ,  C07D401/12 ,  C07K5/06078 ,  A61K38/00

摘要： A phenylalanine derivative having the formula (I): ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen provided that both R.sup.1 and R.sup.2 are not hydrogen at the same time;C.sub.1 -C.sub.8 alkyl which may be substituted with hydroxy, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 alkylmercapto, C.sub.1 -C.sub.4 alkoxy, carbamoyl, sulfamoyl, pyridyl, or phenyl which may further be substituted with nitro, C.sub.1 -C.sub.4 alkoxy, or halogen;C.sub.6 -C.sub.8 cycloalkyl which may be substituted with hydroxy, C.sub.1 -C.sub.4 alkoxy, hydroxylcarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, or C.sub.1 -C.sub.4 alkyl;phenyl which may be substituted with halogen, nitro, trifluoromethyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 C.sub.4 alkylmercapto, C.sub.1 -C.sub.4 alkylcarbonyl, phenylcarbonyl, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, carbamoyl, sulfamoyl, amidino, pyridylcarbonyl, or C.sub.1 -C.sub.6 alkyl which may further be substituted with C.sub.1 -C.sub.4 alkylcarbonyl, hydroxycarbonyl, or C.sub.1 -C.sub.4 alkoxycarbonyl;pyridyl which may be substituted with halogen or C.sub.1 -C.sub.4 alkoxy;pyrimidyl;N-benzylazacyclohexyl; andR.sup.1 and R.sup.2 may form with the nitrogen atom attached thereto a ring structure as morpholino; thiomorpholino; piperazino which may be substituted with phenylcarbonyl, benzyl, or C.sub.1 -C.sub.4 alkyl;pyrrolidyl which may be substituted with hydroxycarbonyl or C.sub.1 -C.sub.4 alkoxycarbonyl; andpiperidino substituted with C.sub.1 -C.sub.4 alkyl, phenyl C.sub.1 -C.sub.4 alkyl, phenycarbonyl, or C.sub.1 -C.sub.4 alkoxycarbonyl;X is hydrogen; nitro; amino; or --OZ wherein Z is hydrogen; C.sub.1 -C.sub.4 alkyl; C.sub.2 -C.sub.4 alkenyl; benzyl which may be substituted with halogen, C.sub.1 -C.sub.4 alkyl, nitro, trifluoromethyl, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, or cyano; phenylcarbonylmethyl; pyridylmethyl; phenyl which may be substituted with nitro or halogen; pyridyl or pyrimidyl which may be substituted with nitro; phenylsulfonyl which may be substituted with C.sub.1 -C.sub.4 alkyl; or benzyloxycarbonyl which may be substituted with halogen;n is 4 to 10; andthe mark * indicates that the configuration of the carbon may be either one of D-configuration, L-configuration and DL-configuration or a pharmaceutical acceptable salt thereof.This phenylalanine derivative is effective as a proteinase inhibitor.

公开(公告)号：US4954512A

公开(公告)日：1990-09-04

申请号：US275193

申请日：1988-11-23

申请人： Katsunori Oguro ,  Hiroshi Nojima ,  Nobuyuki Hashizume ,  Norio Ohno ,  Taketoshi Naito

发明人： Katsunori Oguro ,  Hiroshi Nojima ,  Nobuyuki Hashizume ,  Norio Ohno ,  Taketoshi Naito

IPC分类号： A61K31/235 ,  A61K31/165 ,  A61K31/215 ,  A61K31/44 ,  A61K31/4406 ,  A61P1/04 ,  A61P43/00 ,  C07D211/62 ,  C07D213/75

CPC分类号： C07D213/75 ,  C07D211/62 ,  Y10S514/925 ,  Y10S514/926 ,  Y10S514/927

摘要： An anti-peptic ulcer composition containing, as an active ingredient, a therapeutically effective amount of a compound having the formula (I): ##STR1## wherein A represents H.sub.2 NCH.sub.2 --, ##STR2## B represents ##STR3## D and E each independently represent H, R,--R'CO.sub.2 R,--R'(OH)CO.sub.2 R, ##STR4## wherein X represents H, CONR.sub.2, CONHR, CONH.sub.2, CO.sub.2 H, CO.sub.2 R, or COR or --R'(CO.sub.2 R)--; R' represents a lower alkylene group and R represents a lower alkyl group; F represents H, ##STR5## or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

公开(公告)号：US4334108A

公开(公告)日：1982-06-08

申请号：US164147

申请日：1980-06-30

申请人： Katsuhiko Hashimoto ,  Hirohiko Nambu ,  Kazuhiro Watari ,  Kenichi Mizuno ,  Tadateru Murakami ,  Yutaka Matsuoka ,  Mitsutoshi Moriyama ,  Norio Ohno

发明人： Katsuhiko Hashimoto ,  Hirohiko Nambu ,  Kazuhiro Watari ,  Kenichi Mizuno ,  Tadateru Murakami ,  Yutaka Matsuoka ,  Mitsutoshi Moriyama ,  Norio Ohno

IPC分类号： C07C27/00 ,  B01J4/00 ,  B01J27/00 ,  C07C37/08 ,  C07C37/50 ,  C07C37/60 ,  C07C39/07 ,  C07C39/08 ,  C07C67/00

CPC分类号： B01J4/001 ,  C07C37/08 ,  Y02P20/52

摘要： Disclosed is a process for the preparation of phenols which comprises reacting an .alpha.-hydroxyalkyl-substituted aromatic compound and/or an .alpha.,.beta.-unsaturated alkyl-substituted aromatic compound with hydrogen peroxide in the presence of an acid catalyst, in which hydrogen peroxide is diluted with a diluent, especially acetone, so that the volume is at least 10 times the original volume, and the diluted hydrogen peroxide is supplied in a divided manner to at least two portions of a reaction vessel or the diluted hydrogen peroxide is scattered by sprinkling into the reaction vessel. According to a preferred embodiment, the diluted hydrogen peroxide is continuously supplied to the gas phase in the reaction vessel from a scattering device which is similar to but separate from a scattering device for supplying the starting aromatic compound, particularly, a product formed by oxidizing an isopropyl aromatic compound with molecular oxygen.According to this process, the efficiency of utilization of hydrogen peroxide is increased and a phenol of high quality can be obtained in a high yield with a high safety.

摘要翻译： 公开了一种制备酚的方法，其包括在酸催化剂存在下使α-羟基烷基取代的芳族化合物和/或α，β-不饱和烷基取代的芳族化合物与过氧化氢反应，其中过氧化氢是 用稀释剂，特别是丙酮稀释，使其体积为原始体积的至少10倍，稀释的过氧化氢以分开的方式供应至反应容器的至少两个部分，或者稀释的过氧化氢通过喷洒而分散 进入反应容器。 根据优选实施方案，将稀释的过氧化氢从反应容器中的气相连续地供给到与用于供给起始芳族化合物的散射装置相似但是分开的散射装置，特别是通过氧化 异丙基芳族化合物与分子氧。 根据该方法，提高了过氧化氢的利用效率，高安全性地获得了高质量的苯酚。

公开(公告)号：US4322567A

公开(公告)日：1982-03-30

申请号：US152155

申请日：1980-05-22

申请人： Fujihisa Matsunaga ,  Norio Ohno ,  Hirohiko Nambu

发明人： Fujihisa Matsunaga ,  Norio Ohno ,  Hirohiko Nambu

IPC分类号： B01J23/00 ,  C07B61/00 ,  C07C27/00 ,  C07C29/132 ,  C07C33/18 ,  C07C67/00 ,  C07C27/04 ,  C07C27/06

CPC分类号： C07C29/132

摘要： In a process for producing an aromatic alcohol by catalytic hydrogenation of at least one tertiary peroxide selected from the group consisting of tertiary aromatic hydroperoxides and tertiary aromatic peroxides in the presence of a palladium catalyst in a lower aliphatic alcohol solvent to form the corresponding alcohol; the improvement wherein said catalyst has a palladium metal surface area, determined by the CO chemisorption method, of up to about 200 m.sup.2 /g.multidot.Pd.

摘要翻译： 在钯催化剂存在下，在低级脂族醇溶剂中，通过至少一种选自叔芳基氢过氧化物和叔芳族过氧化物的三
次过氧化物的催化氢化生产芳香族醇的方法，形成相应的醇; 改进之处在于，所述催化剂具有通过CO化学吸附法确定的钯金属表面积高达约200m 2 / g×Pd。