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1. 发明专利

JP2002220395A PHOSPHONOCEPHEM COMPOUND 审中-公开
公开(公告)号：JP2002220395A
公开(公告)日：2002-08-09
申请号：JP2001243107
申请日：2001-08-10
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： ISHIKAWA TOMOYASU , HASHIGUCHI SHOHEI , IIZAWA YUJI
IPC分类号： A61K31/664 , A61P31/04 , C07F9/6561
摘要： PROBLEM TO BE SOLVED: To provide an antibacterial agent with enough satisfactory quality as a medicine. SOLUTION: Cephem compounds (especially their crystals) represented by formula (1) [wherein, X shows CH3COOH, CH3CH2COOH or CH3CN, and n is 0 to 5] are useful as the antibacterial agents (especially anti-MRSA agent), and have an excellent quality with high solid stability and with capability to be stably stored for a long term.

2. 发明专利

JP2001048893A PHOSPHONOCEPHEM DERIVATIVE, ITS PRODUCTION AND USE 失效
公开(公告)号：JP2001048893A
公开(公告)日：2001-02-20
申请号：JP2000206824
申请日：2000-07-04
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： ISHIKAWA TOMOYASU , HASHIGUCHI SHOHEI , IIZAWA YUJI
IPC分类号： C07D463/00 , A61K31/00 , A61K31/435 , A61K31/4353 , A61K31/535 , A61K31/5365 , A61K31/545 , A61K31/546 , A61K31/661 , A61K31/664 , A61P31/00 , A61P31/04 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/24 , C07D501/59 , C07D505/00 , C07D519/06 , C07F9/24 , C07F9/6561
摘要： PROBLEM TO BE SOLVED: To obtain a new phosphonocephem derivative having excellent solubility in water and useful as a medicine exhibiting excellent antibacterial action against a variety of Gram-positive and Gram-negative bacteria, especially methicillin-resistant staphylococci, etc. SOLUTION: The objective compound is expressed by formula I (R1 is phosphono or the life; R2 is H or a group bonded through C atom; Q and X are each N atom or CH; Y is S, O or the like; (n) is 0 or 1; and one of R3 and R4 is pyridinium and the other is H, a hydrocarbon group or the like), e.g. 7β-[2(Z)-ethoxyimino-2-(5-phosphonamino-1,2,4-thiadiazol-3-yl) acetamido]-3-[4-(1-methyl-4-pyridinio)-2-thiazolylthio]-3-cephem-4-car boxylate. The compound of formula I can be produced by reacting a compound of formula II with a carboxylic acid of formula III and optionally converting the group R1 into phosphino group. The compound of formula I has high solubility in water and is useful especially as an injection, etc.

3. 发明专利

JPH10265488A PHOSPHONOCEPHEM DERIVATIVE 失效
公开(公告)号：JPH10265488A
公开(公告)日：1998-10-06
申请号：JP7623497
申请日：1997-03-27
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： ISHIKAWA TOMOYASU , HASHIGUCHI SHOHEI , IIZAWA YUJI
IPC分类号： C07D501/56 , A61K31/66 , A61P31/04 , C07F9/44
摘要： PROBLEM TO BE SOLVED: To provide the subject new compound consisting of a specific phosphonocephem derivative, exhibiting antibacterial action on a wide variety of bacteria including methicillin resistant Staphylococcus aureus(MRSA), useful as an antibacterial agent, etc., such as an anti-MRSA agent and having excellent solubility in water. SOLUTION: This new cephem compound (ester or salt) is expressed by the formula I [R is a (protected)phosphono group; R is H or a group bonded through carbon atom; X is nitrogen atom or methine; (m) is 0 or 1; A is a (substituted) heterocyclic group containing quaternarized nitrogen atom bonded to carbon atom]. lt has excellent antibacterial action, stability and peroral absorbability and is useful e.g. as an antibacterial agent effective against methicillin resistant Staphylococcus aureus(MRSA) and bacteria of the genus Pseudomonas. The compound can be produced by reacting a cephem compound of the formula II with a carboxylic acid of the formula III [R is a (protected) phosphono group], its salt, its reactive derivative, etc., and optionally removing the protecting group from the reaction product.

4. 发明专利

JPH08337585A CEPHEM COMPOUND, ITS PRODUCTION AND ANTIMICROBIAL COMPOSITION 失效
公开(公告)号：JPH08337585A
公开(公告)日：1996-12-24
申请号：JP1299896
申请日：1996-01-29
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： MIYAKE AKIO , OKONOGI KENJI , ISHIKAWA TOMOYASU
IPC分类号： C07D519/06 , A61K31/545 , A61P31/04
摘要： PURPOSE: To obtain the subject new compound, a specific cephem compound, having a wide range of antimicrobial activity, presenting excellent antimicrobial action on methicillin-resistant Staphylococcus aureus(MRSA) and Pseudomonas bacteria, thus useful as e.g. an antimlcrobial agent. CONSTITUTION: This new cephem compound (ester, salt) is expressed by formula I [R is a (protected) amino; R is H car a group linked via a carbon atom; A is a substituted group of e.g. formula II (B is a six-membered aromatic heterocycle with one or two heteroatoms being N; R is a hydrocarbon)]. This compound has excellent antimicrobial effect on a wide range of Gram-positive and Gramnegative bacteria, esp. Staphylococcus aureus, MRSA and Pseudomonas bacteria, etc., therefore being useful as e.g. an antimicrobial agent. This compound is obtained by reaction of a 7-amino-3-cephem-4-carboxylic acid compound of formula III with a 1,2,4-thiadiazol-3-yl-3-iminoacetic acid derivative of formula IV.

5. 发明专利

JP2002187896A CEPHEM COMPOUND HAVING PHOSPHONO GROUP 审中-公开
公开(公告)号：JP2002187896A
公开(公告)日：2002-07-05
申请号：JP2001314306
申请日：2001-10-11
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： ISHIKAWA TOMOYASU , HASHIGUCHI SHOHEI , IIZAWA YUJI
IPC分类号： A61K31/664 , A61P31/04 , C07F9/6539 , C07F9/6561
摘要： PROBLEM TO BE SOLVED: To provide an anti-bacterial agent excellent in quality as a drug such as absorbability, solubility, purity, stability, preservability, handling easiness and the like, and well-content as a drug. SOLUTION: A compound represented by general formula I (n is from 0 to 5) or a salt thereof is disclosed.

6. 发明专利

JPH11255772A PHOSPHONOCEPHEM DERIVATIVE, ITS PRODUCTION AND USE THEREOF 失效
公开(公告)号：JPH11255772A
公开(公告)日：1999-09-21
申请号：JP35888798
申请日：1998-12-17
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： ISHIKAWA TOMOYASU , HASHIGUCHI SHOHEI , IIZAWA YUJI
IPC分类号： C07D463/00 , A61K31/00 , A61K31/435 , A61K31/4353 , A61K31/535 , A61K31/5365 , A61K31/545 , A61K31/546 , A61K31/661 , A61K31/664 , A61P31/00 , A61P31/04 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/24 , C07D501/59 , C07D505/00 , C07D519/06 , C07F9/24 , C07F9/6561
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound having a specific cationic group and a phosphonoamino-substituted five-membered cyclic group on a cephem skeleton, having water solubility, excellent antibacterial actions on (methicillin- resistant) Staphylococcus aureus, bacteria belonging to the genus Pseudomonas, or the like, and useful as an antibacterial agent. SOLUTION: A compound of formula I [R is phosphono group or the like; R is H or a binding group through one or more carbon atoms; Q and X are each N or CH; Y is S, O or CH2 ; (n) is 0 or 1; one of R and R is a (substituted) pyridinium and the other is H, a (substituted) hydrocarbon group or the like], its ester or salt thereof. For example, 7β-[2(Z)-ethoximino-2-(5- phophonoamino-1,2,4-thiadiazol-3-yl)acetamido]-3-[4-(1-methyl-4-pyridi nio)-2- thiazolylthio]-3-cephem-4-carboxylate. The compound of formula I is obtained by reacting a compound of formula II with a compound of formula III.

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