Patents by Inventor Michihiko Ochiai
Michihiko Ochiai has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
-
Patent number: 4514565Abstract: 3-Tertiary ammoniomethyl-7-beta-[alpha-(hydroxy or protected hydroxy)imino-alpha-(2-aminothiazol-4-yl)acetamido]-3-cephem-4-carboxylic acid, pharmaceutically acceptable salt or 4-carboxy ester is provided which is a broad spectrum antibiotic.Type: GrantFiled: June 24, 1983Date of Patent: April 30, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Taiiti Okada, Osami Aki, Akira Morimoto, Kenji Kawakita, Yoshihiro Matsushita
-
Patent number: 4510138Abstract: An antibacterial composition is provided consisting of a 7-[2-(2-aminothiazol)-4-yl)-2-(syn)-methoxyiminoacetamido]cephalosporin compound of the formula ##STR1## wherein R.sub.2 NH is amino or a protected amino group, n is an integer of 1 to 3 and R is a di-C.sub.1-3 alkylamino, carboxyl or sulfo group, or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: September 29, 1982Date of Patent: April 9, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Akira Morimoto, Yoshihiro Matsushita
-
Patent number: 4416817Abstract: Novel 3-methoxy-2-oxoazetidine derivatives, which are shown by the following formula ##STR1## wherein R.sub.1 is amino, acylated amino or protected amino, are of value as intermediates for the synthesis of useful compounds represented by the formula ##STR2## wherein R.sub.1 has the same meaning as defined above, as drugs in the treatment of bacterial infections.Type: GrantFiled: November 18, 1981Date of Patent: November 22, 1983Assignee: Takeda Chemical Industries, Ltd.Inventors: Taisuke Matsuo, Michihiko Ochiai
-
Patent number: 4380541Abstract: Novel 7-[2-(2-aminothiazol-4-yl)-2-(syn)-methoxyiminoacetamido]cephalosporanic acid derivatives of the formula: ##STR1## wherein R.sup.1 NH is an amino group which may optionally be protected, R.sup.2 is a halogen atom or a hydroxyl, thiol or amino group which may optionally be substituted; COOR is a carboxyl group which may optionally be esterified, and pharmaceutically acceptable salts thereof, have excellent antimicrobial activity against a broad spectrum of microorganisms including Gram-negative bacteria such as Escherichia coli, Serratia marcescens, Proteus rettgeri, Enterobacter cloacae, Citrobacter freundii. Thus, these compounds may be used as antibacterial agents for therapeutic purposes.Type: GrantFiled: February 14, 1978Date of Patent: April 19, 1983Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Akira Morimoto
-
Patent number: 4355160Abstract: The present invention is directed to a compound having antibacterial activity of the formula ##STR1## wherein R.sup.1 represents amino, protected amino, hydroxy or protected hydroxy;R.sup.4 represents heterocyclic thio wherein heterocyclic is a 5 to 6 membered hetero ring containing 1 to 4 hetero atoms from the group of oxygen, sulfur and nitrogen; andR.sup.5 is hydroxy or protected hydroxy, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 4, 1981Date of Patent: October 19, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Taiiti Okada, Osami Aki, Akira Morimoto, Kenji Kawakita, Yoshihiro Matsushita
-
Patent number: 4298607Abstract: A crystalline hemi-acid salt comprising one molecule of 7.beta.-[2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido]-3-[(1-methyl -1H-tetrazol-5-yl)thiomethyl]ceph-3-em-4-carboxylic acid and a half molecule of HCl and HBr, is endowed with a high stability and suitable for an active component of an antimicrobial composition.Type: GrantFiled: December 11, 1979Date of Patent: November 3, 1981Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Iwao Mikami, Michihiko Ochiai
-
Patent number: 4298606Abstract: Novel cephem compounds of the formula; ##STR1## wherein R.sup.1 represents amino or hydroxyl group which may be protected, R.sup.2 represents amino or hydroxyl group or a group convertible into these groups, R.sup.3 represents hydrogen or methoxy group or a group convertible into methoxy group, R.sup.4 represents hydrogen or a residue of a nucleophilic compound and R.sup.8 represents hydrogen or a halogen, or a pharmaceutically acceptable salt or ester thereof, have strong antibiotic properties against a wide variety of microorganisms including gram-positive bacteria as well as gram-negative ones, especially by oral administration and can be used as therapeutic agent for various bacterial infections of animals including human beings.Type: GrantFiled: August 28, 1979Date of Patent: November 3, 1981Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Taiiti Okada, Osami Aki, Akira Morimoto, Kenji Kawakita, Yoshihiro Matsushita
-
Patent number: 4278671Abstract: A 7-[2-(2-aminothiazol-4-yl)-2-(syn)-methoxyiminoacetamido] cephalosporin derivative of the formula; ##STR1## wherein R.sub.3 is hydrogen or a residue of a nucleophilic compound; R.sub.2 NH is an amino group which may optionally be protected, pharmaceutically acceptable salt or ester thereof, is found to have excellent anti-bacterial activity against a broad spectrum of bacteria inclusive of gram-negative bacteria such as Escherichia coli, Serratia marcescens, Proteus rettgeri, Enterobacter cloacae and Citrobacter freundii. Thus, this compound may be used for an antibacterial agent in therapeutical purposes.Type: GrantFiled: August 8, 1979Date of Patent: July 14, 1981Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Akira Morimoto, Yoshihiro Matsushita
-
Patent number: 4251657Abstract: A halogenoacetyl group is removed from a halogenoacetyl amino compound in a short period of reaction time by reacting the halogenoacetyl amino compound with an N-substituted dithiocarbamic acid or a salt thereof.Type: GrantFiled: December 5, 1978Date of Patent: February 17, 1981Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Akira Morimoto, Toshio Miyawaki
-
Patent number: 4205180Abstract: Novel cephem compounds of the formula; ##STR1## wherein R.sup.1 represents amino or hydroxyl group which may be protected, R.sup.2 represents amino or hydroxyl group or a group convertible into these groups, R.sup.3 represents hydrogen or methoxy group or a group convertible into methoxy group, R.sup.4 represents hydrogen or a residue of a nucleophilic compound and R.sup.8 represents hydrogen or a halogen, or a pharmaceutically acceptable salt or ester thereof, have strong antibiotic properties against a wide variety of microorganisms including gram-positive bacteria as well as gram-negative ones, especially by oral administration and can be used as therapeutic agent for various bacterial infections of animals including human beings.Type: GrantFiled: January 18, 1978Date of Patent: May 27, 1980Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Taiiti Okada, Osami Aki, Akira Morimoto, Kenji Kawakita, Yoshihiro Matsushita
-
Patent number: 4203899Abstract: Novel cephem compounds of the formula; ##STR1## wherein R.sup.1 represents amino or hydroxyl group which may be protected, R.sup.2 represents amino or hydroxyl group or a group convertible into these groups, R.sup.3 represents hydrogen or methoxy group or a group convertible into methoxy group, R.sup.4 represents hydrogen or a residue of a nucleophilic compound and R.sup.8 represents hydrogen or a halogen, or a pharmaceutically acceptable salt or ester thereof, have strong antibiotic properties against a wide variety of microorganisms including gram-positive bacteria as well as gram-negative ones, especially by oral administration and can be used as therapeutic agent for various bacterial infections of animals including human beings.Also disclosed are novel thiazolylacetic acid compounds of the formula: ##STR2## wherein R.sup.1 represents amino, protected amino, hydroxyl or protected hydroxyl, R.sup.Type: GrantFiled: April 17, 1978Date of Patent: May 20, 1980Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Taiiti Okada, Osami Aki, Akira Morimoto, Kenji Kawakita, Yoshihiro Matsushita
-
Patent number: 4197298Abstract: 7-[2-(2-aminothiazol-4-yl)-2-(syn)-methoxyiminoacetamido]cephalosporanic acid derivatives of the formula; ##STR1## wherein R.sup.1 NH is an amino group which may optionally be protected; COOR.sup.2 is a carboxyl group which may optionally be esterified; X is oxygen, sulfur or an imino group which may optionally be substituted; B is hydrogen or a hydroxyl, amino, thiol or hydrocarbon group which may optionally be substituted, or a salt thereof, are novel, .beta.-lactamase-resistant and low-toxicity compounds which display excellent activity against a broad spectrum of microorganisms including Gram-negative bacteria such as Escherichia coli, Serratia marcescens, Proteus rettgeri, Enterobacter cloacae, Citrobacter freundii. Thus, these compounds can be used for antibacterial agents in therapeutical purpose.Type: GrantFiled: February 14, 1978Date of Patent: April 8, 1980Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Akira Morimoto, Yoshihiro Matsushita
-
Patent number: 4182868Abstract: A compound of the formula: ##STR1## wherein R.sup.2 is hydrogen or a halogen and R.sup.3 stands for methyl, acetoxymethyl, carbamoyloxymethyl, an alkoxymethyl, an alkylthiomethyl, 2-carboxy-1-ethenyl, or a heterocyclic thiomethyl, or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against Gram-negative bacteria including Escherichia coli, Proteus vulgaris, Pseudomonas aeruginosa, Serratia marcescense as well as Gram-positive ones including antibiotic resistant strains. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.Type: GrantFiled: May 6, 1977Date of Patent: January 8, 1980Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Akira Morimoto, Yoshihiro Matsushita, Osami Aki, Taiiti Okada, Kenji Kawakita
-
Patent number: 4145540Abstract: Cephem and penam compounds having a partial structure of formula (II): ##STR1## wherein R.sup.1 and R.sup.2, respectively, represent a hydrocarbon group which is attached to P, either directly or through an oxygen atom, and which may optionally be substituted, and R.sup.3 is a hydrocarbon residue, are useful as intermediates for synthetic penicillins and cephalosporins, which in turn are useful as antibiotics or intermediates for some other synthetic penicillins and cephalosporins having antibiotic activity. To the 6- or 7-amino group of these penam or cephem compounds an objective acyl group can be introduced to give 6- or 7-acyl amino compound in a good yield, without isomerization of 6.alpha.-or 7.alpha.-substituent OR.sup.3 of the penam or cephem compounds.Type: GrantFiled: July 26, 1976Date of Patent: March 20, 1979Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Akira Morimoto, Osami Aki, Taiiti Okada
-
Patent number: 4098888Abstract: Novel cephem compounds of the formula; ##STR1## wherein R.sup.1 represents amino or hydroxyl group which may be protected, R.sup.2 represents amino or hydroxyl group or a group convertible into these groups, R.sup.3 represents hydrogen or methoxy group or a group convertible into methoxy group, R.sup.4 represents hydrogen or a residue of a nucleophilic compound and R.sup.8 represents hydrogen or a halogen, or a pharmaceutically acceptable salt or ester thereof, have strong antibiotic properties against a wide variety of microorganisms including gram-positive bacteria as well as gram-negative ones, especially by oral administration and can be used as therapeutic agent for various bacterial infections of animals including human beings.Type: GrantFiled: December 19, 1975Date of Patent: July 4, 1978Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Taiiti Okada, Osami Aki, Akira Morimoto, Kenji Kawakita, Yoshihiro Matsushita
-
Patent number: 4008246Abstract: A compound of the formula: ##STR1## wherein R.sup.1 stands for a halogenoethoxycarbonylamino and R.sup.2 stands for hydrogen or a halogen, is an important intermediate for producing a cephalosporin derivative of the formula: ##STR2## wherein R.sup.3 stands for methyl, acetoxymethyl, carbamoyloxymethyl, an alkoxymethyl, an alkylthiomethyl, 2-carboxy-1-ethenyl, or a heterocyclic thiomethyl, R.sup.5 stands for hydrogen or methoxy and R.sup.2 has the same meaning as defined before, which is active against various pathogenic microorganisms even at a low concentration.Type: GrantFiled: August 8, 1975Date of Patent: February 15, 1977Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Akira Morimoto, Yoshihiro Matsushita, Taiiti Okada
-
Patent number: 4008227Abstract: A compound of the formula: ##STR1## wherein R.sup.1 represents mandeloyl or 2-(3-sydnone)-acetyl group and R.sup.2 represents a hydrogen atom, a halogen, an alkyl or an alkoxyl group, or a pharmaceutically accetable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria as well as gram-positive ones. Examples thereof include 7-[D-(-)-mandelamido]-3-[6'-(3'-methylpyridazinyl)-thio-methyl]-3-cephem-4 -carboxylic acid 2'-oxide, 7-[D-(-)-mandelamido]-3-[6'-(3'-methoxypyridazinyl)-thiomethyl]-3-cephem-4 -carboxylic acid 1'-oxide, and 7-[2'-(3'-sydnone)acetamido]-3-[6"-(3"-methylpyridazinyl)-thiomethyl]-3-ce phem-4-carboxylic acid 2"-oxide.Type: GrantFiled: June 25, 1974Date of Patent: February 15, 1977Assignee: Takeda Chemical Industries, Ltd.Inventors: Michihiko Ochiai, Osami Aki, Akira Morimoto, Taiiti Okada