专利摘要:
The crystalline 2.5 hydrate of 7 beta -[2 min -(R)-2 min -(m-(methylsulfonamido)phenyl)-2 min -aminoacetamido]-3-Y# chloro-3-(1-carbadethiacephem)-4-carboxylic acid is an antibiotic with superior pharmaceutical elegance. Pharmaceutical formulations of the crystalline 2.5 hydrate are also described.
公开号:SU1750429A3
申请号:SU894613379
申请日:1989-02-02
公开日:1992-07-23
发明作者:Вейд Догерти Байрон
申请人:Эли Лилли Энд Компани (Фирма);
IPC主号:
专利说明:

(S
WITH
The invention relates to a method for the preparation of a new crystalline form of a cephalosporin antibiotic, namely, crystalline 2, 5, 1-carbatephalosporin, formula
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which is used in medicine.
The aim of the invention is the creation of a new crystalline form of cephalosporin, which has a higher stability in relative humidity conditions.
The designation used: LY- 2282J8 is the anhydrous form of compound I.
Example. 2.5 7/3 (2-) R (-2 -) hydrate (m-methylsulfonamido (phenyl) -2-aminoacetamino) -3-chloro-3/1-carba- (1-children) cephem / -4- carboxylic acid (2.5 hydrate LY-22823B).
Sample LY-228238 in an amount of 208 mg is dissolved in 1% acetic acid in water, and the resulting solution is freeze-dried. The solid is dissolved in 2 ml of water at j8 ° C. The solution makes it possible to stand at
but with
 but
room temperature for 16 hours. The resulting crystals are isolated by filtration and air dried to give the desired desired product. The product shows the powder X-ray diffraction pattern shown in the claims table.
Analysis for (H C1N406) 2.5 H2
Calculated,%: C, 41.85; H 4.96; N 11.48,
Found,%: C 41.56; H 4.86; N 11.31.
The Karl-Fisher analysis of other portions of the product obtained in a similar way confirms the presence of 2.5 mol of water per mole of LY-228238.
权利要求:
Claims (1)
[1]
Invention Formula
Method half crystalline 2, b hydrate of 1-carbacephalosporin of the formula
". and
o p-ci ch3-502-mn o Ton.
having the following x-ray diffraction properties measured for a powder under irradiation with a wavelength of 1,51.5405K K on a copper tube with a nickel filter (Cu: Ni) with the following values of interplanar distances d and relative intensities 1/1:
characterized in that the aqueous solution of 1% acetic acid containing the compound of the formula 1 is freeze-dried.
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同族专利:
公开号 | 公开日
DK49989D0|1989-02-03|
CN1034929A|1989-08-23|
NZ227842A|1990-12-21|
PT89612A|1989-10-04|
EP0327364A1|1989-08-09|
HUT49616A|1989-10-30|
AU615026B2|1991-09-19|
AU2961989A|1989-08-10|
HU204271B|1991-12-30|
KR890012960A|1989-09-20|
IL89150D0|1989-09-10|
JPH021489A|1990-01-05|
ZA89829B|1990-10-31|
DK49989A|1989-08-07|
引用文献:
公开号 | 申请日 | 公开日 | 申请人 | 专利标题

NO155548C|1979-02-10|1987-04-15|Kyowa Hakko Kogyo Kk|PROCEDURE FOR THE PREPARATION OF OPTICALLY ACTIVE CEPHALOSPORIN ANALOGS.|
JPS6348520B2|1979-11-14|1988-09-29|Kyowa Hakko Kogyo Kk|
ZA877398B|1986-10-03|1989-05-30|Lilly Co Eli|7-phenylglycine)1-carba-1-dethiacephalosporins|CA2002597C|1988-11-14|1999-03-23|Thomas M. Eckrich|Solvates of b-lactam antibiotic|
CA2002596A1|1988-11-14|1990-05-14|Thomas M. Eckrich|Hydrates of b-lactam antibiotic|
AU1234999A|1997-11-10|1999-05-31|Gist-Brocades B.V.|Crystallization of beta-lactam compounds|
US7378408B2|2001-11-30|2008-05-27|Pfizer Inc.|Methods of treatment and formulations of cephalosporin|
KR100933821B1|2002-11-05|2009-12-24|리도 케미칼 가부시키가이샤|Compound protecting against ultraviolet|
WO2011054182A1|2009-11-03|2011-05-12|Liu Li|Sodium transhinone iia sulfonate hydrate and preparation method and use thereof|
法律状态:
优先权:
申请号 | 申请日 | 专利标题
US15277788A| true| 1988-02-05|1988-02-05|
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