公开(公告)号：KR860000083B1

公开(公告)日：1986-02-18

申请号：KR800001364

申请日：1980-04-01

Applicant: TAKEDA PHARMACEUTICAL IND CO L

Inventor： OKADA YOSHIYUKI ,  SATO YASUO

IPC: C07F9/547 ,  C10L5/14 ,  C07F9/65

公开(公告)号：KR810000861B1

公开(公告)日：1981-08-10

申请号：KR810002309

申请日：1981-06-25

Applicant: TAKEDA PHARMACEUTICAL

Inventor： MORIMOTO AKIRA ,  OCHIAI MICHIHIKO ,  MATSUSIDA YOSHIHIRO

IPC: C07D501/36

公开(公告)号：KR780000313B1

公开(公告)日：1978-08-16

申请号：KR740000752

申请日：1974-01-04

Applicant: TAKEDA PHARMACEUTICAL

Inventor： NAKAGAWA TATSUO ,  MISAKI MASARU ,  MORITAKA SINTAROU ,  TSUZIMOTO YUKISOU ,  TSUKENARI JUNKO

公开(公告)号：KR830001415B1

公开(公告)日：1983-07-25

申请号：KR770001971

申请日：1977-08-24

Applicant: TAKEDA PHARMACEUTICAL

Inventor： NAITO KENJO ,  TSUGAMURA KAZUO ,  SHINPO HARUO

IPC: C07D501/36

Abstract: The solid, storage stable cephalosporin salts I(X=Cl,Br; n=0-6) were prepd. by treating H2NCH2CH2NMe2 with CS2, conveting Me2NCH2CH2NHCS2H to its Me ester, and cyclizing the latter with NaN3 to the tetrazolethiol II. Reaction of the acetoxymethylcephem III with II, followed by treatment with 12N HCl gave 94% pure I(X=Cl, n=1). The MIC of stepilococus aureus FDA 209p and toxicity of mice were 0.39mcg/ml and CD 50>=20 g/kg, resp.

公开(公告)号：KR870001523B1

公开(公告)日：1987-08-22

申请号：KR820000373

申请日：1982-01-29

Applicant: TAKEDA PHARMACEUTICAL

Inventor： OKADA YOSHIYUKI ,  INOUE YOSHIHIRO ,  IWANAKA KOICHI

IPC: C07F9/6503 ,  A01N57/16 ,  C07F9/645 ,  C07F9/6506 ,  C07F9/6509 ,  C07F9/65 ,  C07F9/141

Abstract: 4-Pyrazolyl phosphates (I; R=alkyl; Y=alkyl-or halogensubstd. ph) are prepd. by the reaction of 4-hydroxypyrazole derivs. of formula(II) and phosphinic acid trialkylester. Thus, 99.7g phosphinic acid triethyl is reacted with 19.4g 1-(4-chlorophenyl)4-hydroxypyrazole at 160≦̸C for 7hr to give 31.7g 0-[1-(4chlorophenyl)-pyrazole-4-yl -0, 0- diethyl phosphinic acid ester.

公开(公告)号：KR810000862B1

公开(公告)日：1981-08-10

申请号：KR810002310

申请日：1981-06-25

Applicant: TAKEDA PHARMACEUTICAL

Inventor： MORIMOTO AKIRA ,  OCHIAI MICHIHIKO ,  MATSUSIDA YOSHIHIRO

IPC: C07D501/36

公开(公告)号：KR810000860B1

公开(公告)日：1981-08-10

申请号：KR770000897

申请日：1977-04-14

Applicant: TAKEDA PHARMACEUTICAL

Inventor： MORINOTO AKIRA ,  OCHIAI MICHIHIKO ,  MATSUSIDA YOSHIHIRO

IPC: C07D501/36

Abstract: Title compds. (I; R3 = H or nucleophilic residue; R2NH = NH2-protecting group) were prepd. by the reaction of II and III. Thus, 290 mg 7-amino-3-(N-chloroacetyl)carbamoyloxymethyl-3-cephem-4-carboxylic acid and 276 mg 2-(2-chloroacetamidothiazol-4-yl)-2-(syn)-methoxyiminoacetylchloride were reacted for 15 min with ice-cooling and for 2 hr at room temp. to give 402 mg 7-2-(2-chloroacetamidothiazol-4-yl)-2-(syn)-methoxymethyl-3-cephem-4-carboxylic acid.

公开(公告)号：KR810000493B1

公开(公告)日：1981-05-20

申请号：KR760000698

申请日：1976-03-23

Applicant: TAKEDA PHARMACEUTICAL

Inventor： SENDAI MIZZIUKI ,  TSUSIMA SUSMU ,  SIRAISI MISURU

IPC: C07D501/24

Abstract: A cephalosporin deriv. (I; R1 = H or acyl; R2 = residue of nucleophilic compd.) was prepd. by reaction of cephalosporanic acid ester (II; X = C6H5CH:, C6H4, CH3-CH-, -CH2CH2-) with nuclophilic compd. Formula II was obtained by acylation of 3-hydroxymethyl cephalosporanic acid with o-carboxymaleic anhydride or o-carboxysalicylic acid anhydride.

公开(公告)号：KR790000165B1

公开(公告)日：1979-03-24

申请号：KR740003197

申请日：1974-07-27

Applicant: TAKEDA PHARMACEUTICAL IND CO L

Inventor： MEKURO KANJI ,  KUADA YUTAKA ,  SATO YOSHIAKI ,  HUKONO TAKESHI

Abstract: Thie-o (2,3-b) pyridinecarboxylic acid derivs. (I; R1, R4, R5 = H, alkyl, R2 = H, alkyl, halogen and alkylene, producing alkyl-substituted or non-substituted 5 or 6 membered ring by binding R1 and R2), useful as broad spectrum antibiotic to gram positive and gram negative bacteria, and their salts were prepd. by cyclization of II (R1, R2 given, R3 = alkyl, Z = H, carboxyl), hydrolysis if needed, and alkylation of the resulting I'(R1, R2, R4 give-).

公开(公告)号：KR820000143B1

公开(公告)日：1982-02-20

申请号：KR780003706

申请日：1978-12-09

Applicant: TAKEDA PHARMACEUTICAL

Inventor： KATO M ,  TSUSIMA S ,  MATSUMOTO N

IPC: C07D501/18

Abstract: Title compds. II, as antibiotics with a broad spectrum activity, were prepd. by reaction of I (R1 = protected amino group) with acetylhalide or propionyl halide at -10≦̸C-50≦̸C, followed by conversion into the iminohalide, alcoholysis, and hydrolysis of the alkoxy imino compd. to I. (R2 = 3-oxobutyryl oxy group, 1-methyl-1H-tetrazol-5-yl thio group, or 1-(2-dimethyl amino ethyl)-1H-tetrazol-5-yl thio group).