公开(公告)号：US3840531A

公开(公告)日：1974-10-08

申请号：US23676472

申请日：1972-03-21

申请人： LILLY CO ELI

发明人： GREENE J

IPC分类号： C07D501/00 ,  A61K31/546 ,  C07D317/36 ,  C07D501/06 ,  C07D501/36 ,  C07D99/24

CPC分类号： C07D501/36 ,  C07D317/36

摘要： 1. A PROCESS FOR PREPARING A CEPHALOSPORIN OF THE FORMULA

2-(R-OOC-),3-((1-(H3C-)-TETRAZOL-5-YL)-S-CH2-),7-(H5C6-

CH(-OH)-CO-NH-)-2-CEPHEM

WHICH COMPRISES (1) REACTING A 7-ACYLAMIDO-3-ACTOXYMETHYL COMPOUND OF THE FORMULA

2-(R-OOC-),3-(H3C-COO-CH2-),7-(H-CO-NH-)-2-CEPHEM

IN WHICH R IS HYDROGEN OR A CARBOXY PROTECTING GROUP, WITH 1-METHYL-1H-TETRAZOLE-5-THIOL OR AN ALKALIM ALKALINE EARTH METAL OR AMMONIUM SALT THEREOF TO PRODUCE A 7ACYLAMIDO-3-(1 - METHYL-1H-TETRAZOLE-5-YLTHIOMETHYL) COMPOUND OF THE FORMULA

2-(R-OOC-),3-((1-(H3C-)-TETRAZOL-5-YL)-S-CH2-),7-(H-CO-

NH-)-2-CEPHEM

(2) CLEAVING THE 7-ACYLAMIDO-3-(1-METHYL-1H-TETRAZOL-5YLTHIOMETHYL) COMPOUND TO PRODUCE A 7-AMINO-3-(1-METHYL-1H-TETRAZOL-5-YLTHIOMETHYL) COMPOUND OF THE FORMULA

2-(R-OOC-),3-((1-(H3C-)-TETRAZOL-5-YL)-S-CH2-),7-(H2N-)-

2-CEPHEM

AND (3) ACYLATING THE RESULTING 7-AMINO COMPOUND WITH ANHYDRO-O-CARBOXYMANDELIC ACID HAVING THE FORMULA

2,4-DI(O=),5-(H5C6-)-1,3-DIOXOLANE

TO PRODUCE THE AFOREMENTIONED CEPHALOSPORIN.

公开(公告)号：US3813390A

公开(公告)日：1974-05-28

申请号：US28663072

申请日：1972-09-06

申请人： BRISTOL MYERS CO

发明人： NAITO T ,  OKUMURA J

IPC分类号： C07D501/18 ,  C07D501/36 ,  C07D99/24

CPC分类号： C07D501/36 ,  Y02P20/55

摘要： 7-(O-AMINOMETHYLPHENYLTHIOACETAMIDO) - 3 - (3 - HYDROXY-PYRIDAZIN-6-YLTHIOMETHYL))-3-CEPHEM - 4 - CARBOXYLIC ACID AND ITS NONTOXIC, PHARMACEUTICALLY ACCEPTABLE SALTS AND ESPECIALLY ITS DIMETHANESULFONATE DERIVATIVE ARE VALUABLE AS ANTIBACTERIAL AGENTS, AS NUTRITIONAL SUPPLEMENTS IN ANIMAL FEEDS AND AS THERAPEUTIC AGENTS IN POULTRY AND ANIMALS, INCLUDING MAN, AND ARE ESPECIALLY USEFUL IN THE TREATMENT OF INFECTIOUS DISEASES CAUSED BY MANY GRAMPOSITIIVE AND GRAM-NEGATIVE BACTERIA. 7-(O-AMINOMETHYLPHENYLTHIOACETAMIDO)-3-(3-HYDOXY-PYRIDAZIN - 6 - YLTHIOMETHYL)-3-CEPHEM-4-CARBOXYLIC ACID IS PREPARED, FOR EXAMPLE, BY TREATMENT OF 0*C. WITH TRIFLUOROACETIC ACID OF THE CORRESPONDING COMPOUND IN WHICH THE FREE AMINO GROUP IS PROTECTED WITH A TERT.-BUTOXYCARBONYL GROUP.

公开(公告)号：US3812116A

公开(公告)日：1974-05-21

申请号：US15948571

申请日：1971-07-02

申请人： FUJISAWA PHARMACEUTICAL CO

发明人： TAKANO T ,  KARIYONE K ,  KURITA M ,  HASEGAWA M ,  YAZAWA H ,  NAKAMURA H

IPC分类号： C07D501/36 ,  C07D99/24

CPC分类号： C07D501/36

摘要： COMPOUNDS OF THE FORMULA

2-(M-OOC-),3-(R3-CH2-),7-(R2-O-CH(-R1)-CO-NH-)-2-CEPHEM

IN WHICH R1 IS HYDROGEN, LOWER ALKYL, ARYL, THIENYL OR FURYL, R2 IS ACYL CONTAINING MORE THAN ONE CARBON ATOM, R3 IS HYDROGEN, AZIDO OR HETEROCYCLIC THIO, AND M IS HYDROGEN OR A PHARMACEUTICALLY ACCEPTABLE, SUBSTANTIALLY NON-TOXIC CATION, HAVE STRONG ANTI-BACTERIAL ACTIVITY AND ARE ACTIVE ON ORAL ADMINISTERATION.

公开(公告)号：US3767667A

公开(公告)日：1973-10-23

申请号：US3767667D

申请日：1971-10-07

申请人： FUJISAWA PHARMACEUTICAL CO

发明人： KAMIYA T ,  SAITO Y

IPC分类号： C07D257/04 ,  C07D55/56

CPC分类号： C07D501/36 ,  C07D257/04

摘要： A PROCESS FOR PREPARING 1H-TETRAZOLE COMPOUNDS OF THE FORMULA:

1-R1,5-R2-1H-TETRAZOLE

WHEREIN R1 AND R2 ARE EACH HYDROGEN OR A POSSIBLE SUBSTITUENT, WHICH COMPRISES REACTING AN AMINE COMPOUND OF THE FORMULA:

R1-NH2

WHEREIN R1 IS AS DEFINED ABOVE, OR ITS SALT WITH AN ORTHOCARBOXYLIC ACID ESTER OF THE FORMULA:

R2C(OR3)3

WHEREIN R3 IS LOWER ALKYL AND R2 IS AS DEFINED ABOVE, AND A HYDRAZOIC ACID SALT.

公开(公告)号：US3757014A

公开(公告)日：1973-09-04

申请号：US3757014D

申请日：1971-05-07

申请人： BRISTOL MYERS CO

发明人： BRUCE L

IPC分类号： C07D271/10 ,  C07D271/113 ,  C07D501/36 ,  C07D99/24

CPC分类号： C07D271/113 ,  C07C243/00 ,  C07D501/36

摘要： 7-(D-(A-AMINO-A-PHENYLACETAMIDO))-3-(S-(5-HYDROXYMETHYL-1,3,4-OXADIAZOL-2 -YL)THIOMETHYL)-3-CEPHEM-4-CARBOXYLIC ACID AND ITS NONTOXIC, PHARMACEUTICALLY ACCEPTABLE SALTS ARE VALUABLE AS ANTIBACTERIAL AGENTS, AS NUTRITIONAL SUPPLEMENTS IN ANIMAL FEEDS AND AS THERAPEUTIC AGENTS IN POULTRY AND ANIMALS, INCLUDING MAN, AND ARE ESPECIALLY USEFUL IN THE TREATMENT, INCLUDING BY ORAL ADMINISTRATION, OF INFECTIOUS DISEASES CAUSED BY MANY GRAM-POSITIVE AND GRAM-NEGATIVE BACTERIA.

公开(公告)号：US3734907A

公开(公告)日：1973-05-22

申请号：US3734907D

申请日：1970-09-14

申请人： BRISTOL MYERS CO

发明人： CRAST L

IPC分类号： C07D501/36 ,  C07D99/24

CPC分类号： C07D501/36

摘要： 7 - (D - (A - AMINO-A-PHENYLACETAMIDO))-3-(5-METHYL1,3,4-OXADIAZOL-2-YLTHIOMETHYL)-3 -CEPHEM - 4 - CARBOXYLIC ACID AND ITS NONTOXIC, PHARMACEUTICALLY ACCEPTABLE SALTS ARE VALUABLE AS ANTIBACTERIAL AGENTS, AS NUTRITIONAL SUPPLEMENTS IN ANIMAL FEEDS AND AS THERAPEUTIC AGENTS IN POULTRY AND ANIMALS, INCLUDING MAN, AND ARE ESPECIALLY USEFUL IN THE TREATMENT, PARTICULARLY BY ORAL ADMINISTATION, OF INFECTIOUS DISEASES CAUSED BY MANY GRAM-POSITIVE AND GRAM-NEGATIVE BACTERIA.

公开(公告)号：US3563983A

公开(公告)日：1971-02-16

申请号：US3563983D

申请日：1967-10-31

申请人： FUJISAWA PHARMACEUTICAL CO

发明人： ATARASHI SUEO ,  HORIBE SUSUMU ,  MERA MASASHI ,  NAKAGAWA RITSUKO

IPC分类号： C07D501/36 ,  C07D99/24

CPC分类号： C07D501/36

摘要： THE COMPOUNDS OF THIS INVENTION ARE 3-(BENZENE-FUSED HETEROCYCLIC THIOL) SUBSTITUTED 7-SYDONONECCEPHALOSPORIN COMPOUNDS. THESE COMPOUNDS MAINFEST SIGNIFICANT ACTIVITY AGAINST A WIDE VARIETY OF MICROOGANISMS INCLUDING BOTH GRAM-POSITIVE AND GRAM-NEGATIVE BACTERIA, AND ALSO ARE EXCRETED IN BILE AT A HIGHER CONCENTRATION.

公开(公告)号：US3530123A

公开(公告)日：1970-09-22

申请号：US3530123D

申请日：1967-10-31

申请人： FUJISAWA PHARMACEUTICAL CO

发明人： TAKANO TADAYOSHI ,  HARADA HIROKICHI ,  KURITA MASARU ,  HASHIMOTO MASASHI ,  NIKAIDO HIROO

IPC分类号： C07D501/36 ,  C07D99/24

CPC分类号： C07D501/36 ,  C07D501/20 ,  C07D501/24 ,  C07D501/46

公开(公告)号：US3431259A

公开(公告)日：1969-03-04

申请号：US3431259D

申请日：1967-01-18

申请人： FUJISAWA PHARMACEUTICAL CO

发明人： HATTORI KIYOSHI ,  ATARASHI SUEO

IPC分类号： A61K20060101 ,  A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/36 ,  C07D93/08 ,  A61K27/00

CPC分类号： C07D501/36

公开(公告)号：US09834567B1

公开(公告)日：2017-12-05

申请号：US15687359

申请日：2017-08-25

申请人： TIANJIN UNIVERSITY ,  HAINAN LINGKANG PHARMACEUTICAL CO., LTD

发明人： Hongxun Hao ,  Linggang Tao ,  Fang He ,  Baohong Hou ,  Jingkang Wang ,  Jun Lv ,  Qiuxiang Yin ,  Yongli Wang ,  Junbo Gong ,  Chuang Xie ,  Ying Bao

IPC分类号： C07D501/36 ,  C07D501/12

CPC分类号： C07D501/36 ,  C07B2200/13 ,  C07D501/12

摘要： A novel crystalline form is defined by diffraction angle 2θ° of X-ray powder diffraction pattern and characteristic peak of differential scanning calorimetry (DSC). The novel crystalline form of Cefamandole Nafate is prepared as follows: adding Cefamandole Nafate in solid state to an organic solvent to form a suspension with a concentration of 0.04˜0.3 g/ml, stirring the suspension at 40˜50° C. for a period of time, and then cooling to 5˜15° C. at certain cooling rate, continuing to stir for a period of time, then suction filtrating the obtained suspension, the resulting filer cake is Cefamandole Nafate as wet product, which is dried to constant weight to provide the novel crystalline form of Cefamandole Nafate as final product.