公开(公告)号：US4395412A

公开(公告)日：1983-07-26

申请号：US221622

申请日：1980-12-31

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Hiroyuki Imaizumi ,  Isamu Takakura ,  Hirokazu Ochiai ,  Takashi Yasuda ,  Hideo Taki ,  Masaru Tai ,  Yutaka Kodama

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Hiroyuki Imaizumi ,  Isamu Takakura ,  Hirokazu Ochiai ,  Takashi Yasuda ,  Hideo Taki ,  Masaru Tai ,  Yutaka Kodama

IPC: C07D295/20 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/57 ,  A61K31/545

CPC classification number: C07D295/20 ,  Y02P20/55

Abstract: A 7.alpha.-methoxycephalosporin represented by the general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents an organic group linked to the carbon atom through an oxygen or sulfur atom; R.sup.3 represents a lower alkyl group; n is 0, 1 or 2; A represents a hydrogen atom or a substituted or unsubstituted alkyl group; and B represents a substituted or unsubstituted alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl or heterocyclic group, and a salt thereof. These compounds have a broad antibacterial spectrum, high resistance to .beta.-lactamase produced from bacteria, and an effective antibacterial activity against clinical isolates of bacteria.

公开(公告)号：US4263292A

公开(公告)日：1981-04-21

申请号：US81835

申请日：1979-10-04

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Hiroyuki Imaizumi ,  Isamu Takakura ,  Hirokazu Ochiai ,  Takashi Yasuda ,  Hideo Taki ,  Masaru Tai ,  Yutaka Kodama

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Hiroyuki Imaizumi ,  Isamu Takakura ,  Hirokazu Ochiai ,  Takashi Yasuda ,  Hideo Taki ,  Masaru Tai ,  Yutaka Kodama

IPC: C07D241/08 ,  C07D295/20 ,  C07D501/57 ,  A61K31/545

CPC classification number: C07D241/08 ,  C07D295/20 ,  Y02P20/55

Abstract: A 7.alpha.-methoxycephalosporin represented by the general formula and a salt thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents an organic group linked to the carbon atoms through an oxygen or sulfur atom; R.sup.3 represents a lower alkyl group; n is 0, 1 or 2; A represents a hydrogen atom or a substituted or unsubstituted alkyl group; and B represents a substituted or unsubstituted alkyl group. These compounds have a broad antibacterial spectrum and high resistance to .beta.-lactamase produced from bacteria, and are well absorbed in a living body.

Abstract translation: 由通式表示的7α-甲氧头孢菌素及其盐：其中R 1表示氢原子或羧基保护基; R2表示通过氧或硫原子与碳原子连接的有机基团; R3表示低级烷基; n为0,1或2; A表示氢原子或取代或未取代的烷基; B表示取代或未取代的烷基。 这些化合物具有广泛的抗菌谱和对细菌产生的β-内酰胺酶的高抗性，并且在活体中被很好地吸收。

公开(公告)号：US4237280A

公开(公告)日：1980-12-02

申请号：US945346

申请日：1978-09-25

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Kaishu Momonoi ,  Isamu Takakura ,  Chiaki Kutani ,  Kiyoshi Tanaka ,  Kenshin Hayashi

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Kaishu Momonoi ,  Isamu Takakura ,  Chiaki Kutani ,  Kiyoshi Tanaka ,  Kenshin Hayashi

IPC: A61K31/54 ,  A61K31/545 ,  C07C20060101 ,  C07D20060101 ,  C07D501/04 ,  C07D501/12 ,  C07D501/36 ,  C07D501/46

CPC classification number: C07D501/36

Abstract: The N,N-dimethylacetamide adduct of 7-[D(-)-.alpha.-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-.alpha.-(4-hydroxyphenyl)acetamido]-3-[5-(1-methyl-1,2,3,4-tetrazolyl)thiomethyl]-.DELTA..sup.3 -cephem-4-carboxylic acid, a process for the production thereof, and a process for producing said acid and a pharmaceutically acceptable salt thereof through said adduct.

Abstract translation: 7- [D（ - ） - α-（4-乙基-2,3-二氧代-1-哌嗪甲酰氨基）-α-（4-羟基苯基）乙酰氨基] -3- [5-（ 1-甲基-1,2,3,4-四唑基）硫基] - 三唑-3-头孢烯-4-羧酸，其制备方法，以及通过所述方法制备所述酸及其药学上可接受的盐的方法 加合物

公开(公告)号：US5858408A

公开(公告)日：1999-01-12

申请号：US765446

申请日：1997-01-17

Applicant: Sadao Sotani ,  Shosaku Kato ,  Yasuo Watanabe ,  Isamu Takakura

Inventor： Sadao Sotani ,  Shosaku Kato ,  Yasuo Watanabe ,  Isamu Takakura

IPC: A61K9/00 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5383 ,  A61K9/14

CPC classification number: A61K31/4375 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5383 ,  A61K9/006 ,  A61K9/0063

Abstract: The preent invention relates to a sustained-release oral ointment which comprises a hydrophobic ointment base, an adhesive substance, an aluminum compound and a drug. The ointment is useful as a sustained-release oral ointment which has applicability to an oral mucosa, particularly to a peridontal pocket, sustained-release properties to supply a drug to affected part over a long period of time while maintaining the concentration thereof at a sufficiently high level, and enhanced ratio of utilization of drug (the ratio of the total amount of drug released to affected part to the total amount of drug in the ointment applied).

Abstract translation: PCT No.PCT / JP94 / 01191 Sec。 371日期1997年1月17日 102（e）日期1997年1月17日PCT提交1994年7月20日PCT公布。 出版物WO96 / 02275 日期1996年2月1日本发明涉及一种缓释口服软膏，其包括疏水软膏基质，粘合剂物质，铝化合物和药物。 软膏可用作持续释放口服软膏，其适用于口腔粘膜，特别是适用于周围口袋，持续释放性能，以在长时间内将药物供应给受影响部位，同时将其浓度保持在足够的水平 高水平，提高药物使用比例（药物释放总量与受影响部位药物总量与药膏总量的比例）。

公开(公告)号：US4385178A

公开(公告)日：1983-05-24

申请号：US331900

申请日：1981-12-17

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Kaishu Momonoi ,  Isamu Takakura ,  Seietsu Kuroda ,  Kiyoshi Tanaka ,  Kenshin Hayashi ,  Bunei Nagahashi ,  Chiaki Kutani

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Kaishu Momonoi ,  Isamu Takakura ,  Seietsu Kuroda ,  Kiyoshi Tanaka ,  Kenshin Hayashi ,  Bunei Nagahashi ,  Chiaki Kutani

IPC: A61K20060101 ,  C07D20060101 ,  C07D501/04 ,  C07D501/14 ,  C07D501/16 ,  C07D501/18 ,  C07D501/36 ,  C07D501/60

CPC classification number: C07D501/04

Abstract: This disclosure relates to a novel process for producing 7-(substituted)amino-3-substituted thiomethyl cephem carboxylic acids which are intermediate products of cephalosporins being valuable antibacterial compounds for use in mammals including man.

公开(公告)号：US4321265A

公开(公告)日：1982-03-23

申请号：US117784

申请日：1980-02-01

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Hiroyuki Imaizumi ,  Isamu Takakura ,  Hirokazu Ochiai ,  Takashi Yasuda ,  Hideo Taki ,  Masaru Tai ,  Yutaka Kodama

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Hiroyuki Imaizumi ,  Isamu Takakura ,  Hirokazu Ochiai ,  Takashi Yasuda ,  Hideo Taki ,  Masaru Tai ,  Yutaka Kodama

IPC: C07D295/20 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/57

CPC classification number: C07D295/20 ,  Y02P20/55

Abstract: A 7.alpha.-methoxycephalosporin represented by the general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents an organic group linked to the carbon atom through an oxygen or sulfur atom; R.sup.3 represents a lower alkyl group; n is 0, 1 or 2; A represents a hydrogen atom or a substituted or unsubstituted alkyl group; and B represents a substituted or unsubstituted alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl or heterocyclic group, and a salt thereof. These compounds have a broad antibacterial spectrum, high resistance to .beta.-lactamase produced from bacteria, and an effective antibacterial activity against clinical isolates of bacteria.

Abstract translation: 由以下通式表示的7α-甲氧头孢菌素：其中R 1表示氢原子或羧基保护基; R2表示通过氧或硫原子与碳原子连接的有机基团; R3表示低级烷基; n为0,1或2; A表示氢原子或取代或未取代的烷基; B表示取代或未取代的烷基，环烷基，环烯基，环二烯基或杂环基，及其盐。 这些化合物具有广泛的抗菌谱，对细菌产生的β-内酰胺酶的高抗性，以及针对临床细菌分离株的有效抗菌活性。

公开(公告)号：US4200744A

公开(公告)日：1980-04-29

申请号：US845935

申请日：1977-10-27

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Hiroyuki Imaizumi ,  Isamu Takakura ,  Hirokazu Ochiai ,  Takashi Yasuda ,  Hideo Taki ,  Masuru Tai ,  Yutaka Kodama

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Hiroyuki Imaizumi ,  Isamu Takakura ,  Hirokazu Ochiai ,  Takashi Yasuda ,  Hideo Taki ,  Masuru Tai ,  Yutaka Kodama

IPC: C07D501/36 ,  C07D501/57

CPC classification number: C07D501/57

Abstract: Novel 7.alpha.-methoxy-cephalosporins and non-toxic salts thereof, which contain a di-oxo-piperazinyl-carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and methods for producing the same.

Abstract translation: 新型7α-甲氧基头孢菌素及其无毒盐，其在分子中含有二 - 氧代 - 哌嗪基 - 羰基氨基。 这些化合物是用于包括人在内的哺乳动物的有价值的抗菌化合物。 本公开涉及这种化合物及其制备方法。

公开(公告)号：US4317907A

公开(公告)日：1982-03-02

申请号：US874637

申请日：1978-02-02

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Kaishu Momonoi ,  Isamu Takakura ,  Seietsu Kuroda ,  Kiyoshi Tanaka ,  Kenshin Hayashi ,  Bunei Nagahashi ,  Chiaki Kutani

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Kaishu Momonoi ,  Isamu Takakura ,  Seietsu Kuroda ,  Kiyoshi Tanaka ,  Kenshin Hayashi ,  Bunei Nagahashi ,  Chiaki Kutani

IPC: A61K20060101 ,  C07D20060101 ,  C07D501/04 ,  C07D501/14 ,  C07D501/16 ,  C07D501/18 ,  C07D501/36 ,  C07D501/60

CPC classification number: C07D501/04

Abstract: This disclosure relates to a novel process for producing 7-(substituted)amino-3-substituted thiomethyl cephem carboxylic acids which are intermediate products of cephalosporins being valuable antibacterial compounds for use in mammals including man.

Abstract translation: 本公开涉及一种用于生产7-（取代的）氨基-3-取代的硫代甲基头孢霉酸的新方法，其是头孢菌素的中间产物，其是用于包括人在内的哺乳动物的有价值的抗菌化合物。

公开(公告)号：US4312986A

公开(公告)日：1982-01-26

申请号：US54917

申请日：1979-07-05

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Kaishu Momonoi ,  Isamu Takakura ,  Seietsu Kuroda ,  Kiyoshi Tanaka ,  Kenshin Hayashi ,  Bunei Nagahashi ,  Chiaki Kutani

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Kaishu Momonoi ,  Isamu Takakura ,  Seietsu Kuroda ,  Kiyoshi Tanaka ,  Kenshin Hayashi ,  Bunei Nagahashi ,  Chiaki Kutani

IPC: A61K31/545 ,  A61K31/546 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/16 ,  C07D501/18 ,  C07D501/28 ,  C07D501/36 ,  C07D501/57 ,  C07D501/60

CPC classification number: C07D501/04 ,  C07D501/16 ,  C07D501/18

Abstract: This disclosure relates to a novel process for producing 7-(substituted)-amino-3-substituted thiomethyl-.DELTA..sup.3 -cephem-4-carboxylic acids which are intermediate products of cephalosporins being valuable antibacterial compounds for use in mammals including man.

Abstract translation: 本公开涉及一种用于生产7-（取代的） - 氨基-3-取代的硫代甲基-Detta 3-头孢烯-4-羧酸的新方法，其是头孢菌素的中间产物，其是用于包括人在内的哺乳动物的有价值的抗菌化合物。

公开(公告)号：US4304909A

公开(公告)日：1981-12-08

申请号：US69545

申请日：1979-08-24

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Kaishu Momonoi ,  Isamu Takakura ,  Chiaki Kutani ,  Kiyoshi Tanaka ,  Kenshin Hayashi

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Kaishu Momonoi ,  Isamu Takakura ,  Chiaki Kutani ,  Kiyoshi Tanaka ,  Kenshin Hayashi

IPC: A61K31/54 ,  A61K31/545 ,  C07C20060101 ,  C07D20060101 ,  C07D501/04 ,  C07D501/12 ,  C07D501/36 ,  C07D501/46

CPC classification number: C07D501/36

Abstract: The N,N-dimethylacetamide adduct of 7-[D(-)-.alpha.-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-.alpha.-(4-hydroxyphenyl)acetamido]-3-[5-(1-methyl-1,2,3,4-tetrazolyl)thiomethyl]-.DELTA..sup.3 -cephem-4-carboxylic acid, a process for the production thereof, and a process for producing said acid and a pharmaceutically acceptable salt thereof through said adduct.

Abstract translation: 7- [D（ - ） - α-（4-乙基-2,3-二氧代-1-哌嗪甲酰氨基）-α-（4-羟基苯基）乙酰氨基] -3- [5-（ 1-甲基-1,2,3,4-四唑基）硫基] - 三唑-3-头孢烯-4-羧酸，其制备方法，以及通过所述方法制备所述酸及其药学上可接受的盐的方法 加合物