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1. 发明公开

EP1182204A4 CRYSTALS OF CARBAPENEM DERIVATIVES AND PHARMACEUTICAL PREPARATIONS FOR INJECTION 有权
标题翻译： CRYSTAL CABAPENEMDERIVATE和药物制剂注射用
公开(公告)号：EP1182204A4
公开(公告)日：2002-10-30
申请号：EP00935544
申请日：2000-06-05
申请人： EISAI CO LTD
发明人： CHIBA HIROYUKI , TSUJII MASAHIKO , KOIWA ATSUSHI , SAKURAI SHIN , KAYANO AKIO , ISHIZUKA HIROYUKI , SAITO HIROYUKI , NAKAMURA TAIJU , KUSHIDA IKUO , SUZUKI YASUYUKI , YOSHIBA TAKAKO , ASHIZAWA KAZUHIDE , SAKURAI MASAHIRO , YAMAMOTO EIICHI
IPC分类号： A61K31/407 , A61P31/04 , C07D477/20 , A61K9/14 , A61K31/40
CPC分类号： C07D477/20 , A61K31/407
摘要： Crystals of mono- or tri-hydrates of hydrochlorides of carbapenem compounds useful as antibacterial agents, which are chemically stable and easy to purify; processes for the production of the crystals; and injectable powder preparations manufactured by packing the same. Specifically, crystals of monohydrates of hydrochlorides of carbapenem compounds which have powder X-ray diffraction patterns containing spacings (d) of 5.2, 4.3 and 4.0 Å and crystals of trihydrates of hydrochlorides of carbapenem compounds which have X-ray diffraction patterns containing spacings (d) of 9.0, 4.1 and 2.8 Å; processes for the production of the crystals; and injectable powder preparations manufactured by packing the same.

2. 发明公开

EP1201665A4 PROCESS FOR THE PREPARATION OF BASIC ANTIBIOTIC-INORGANIC ACID ADDITION SALTS AND INTERMEDIATE OXALATES 有权
标题翻译：用于生产抗生素与无机酸和碱加成盐，草酸盐中间体
公开(公告)号：EP1201665A4
公开(公告)日：2002-10-23
申请号：EP00948257
申请日：2000-07-27
申请人： EISAI CO LTD
发明人： KAYANO AKIO , CHIBA HIROYUKI , NAKAMURA TAIJU , SAKURAI SHIN , ISHIZUKA HIROYUKI , SAITO HIROYUKI , KOMATSU YUUKI , SASHO MANABU , SATO NOBUAKI , NEGI SHIGETO
IPC分类号： C07D477/02 , C07D477/08 , C07D477/20 , C07D499/68 , C07D501/22 , C07D501/36 , C07D501/46 , C07D463/00 , C07D499/00 , C07D501/00
CPC分类号： C07D477/20 , C07D477/02 , C07D477/08 , Y02P20/55
摘要： An industrially excellent novel process for the preparation of addition salts of basic antibiotics with inorganic acids (such as hydrochloric acid), by subjecting a basic antibiotic-oxalic acid addition salt (II) to salt-exchange with an inorganic acid salt (III) of an alkaline earth metal, wherein A is a basic antibiotic; R10 is a protected functional group to be used in organic synthesis; Ak-E is an alkaline earth metal; and B is an inorganic acid; carbapenem derivative-oxalic acid addition salts represented by general formula (II-I) and being useful as intermediates for the preparation of hydrochlorides of antimicrobial agents; and a process for preparing the same, (II-I) wherein A is a three- to seven-membered ring having at least one nitrogen atom; R1 is hydrogen or the like; R?2 and R5¿ are each hydrogen or a protecting group; R3 is a protecting group; R4 is hydrogen or the like; and R6 is hydrogen or the like.

3. 发明专利

CA2375601C CARBAPENEM COMPOUND CRYSTALS AND INJECTION PREPARATIONS 未知
公开(公告)号：CA2375601C
公开(公告)日：2008-07-29
申请号：CA2375601
申请日：2000-06-05
申请人： EISAI CO LTD
发明人： NAKAMURA TAIJU , KUSHIDA IKUO , CHIBA HIROYUKI , YOSHIBA TAKAKO , SUZUKI YASUYUKI , SAITO HIROYUKI , TSUJII MASAHIKO , ISHIZUKA HIROYUKI , SAKURAI MASAHIRO , YAMAMOTO EIICHI , ASHIZAWA KAZUHIDE , KAYANO AKIO , KOIWA ATSUSHI , SAKURAI SHIN
IPC分类号： C07D477/20 , A61K9/14 , A61K31/407 , A61P31/04
摘要： Crystals of mono- or tri-hydrates of hydrochlorides of carbapenem compounds useful as antibacterial agents, which are chemically stable and easy to purify; processes for the production of the crystals; and injectable powder preparations manufactured by packing the same. Specifically, crystals of monohydrates of hydrochlorides of carbapenem compounds which have powder X-ray diffraction patterns containing spacings (d) of 5.2, 4.3 and 4.0 .ANG. and crystals of trihydrates of hydrochlorides of carbapenem compounds which have X- ray diffraction patterns containing spacings (d) of 9.0, 4.1 and 2.8 .ANG.; processes for the production of the crystals; and injectable powder preparations manufactured by packing the same.

4. 发明专利

AT277930T 未知
公开(公告)号：AT277930T
公开(公告)日：2004-10-15
申请号：AT00948257
申请日：2000-07-27
申请人： EISAI CO LTD
发明人： KAYANO AKIO , CHIBA HIROYUKI , NAKAMURA TAIJU , SAKURAI SHIN , ISHIZUKA HIROYUKI , SAITO HIROYUKI , KOMATSU YUUKI , SASHO MANABU , SATO NOBUAKI , NEGI SHIGETO
IPC分类号： C07D477/02 , C07D477/08 , C07D477/20 , C07D499/68 , C07D501/22 , C07D501/36 , C07D501/46 , C07D463/00 , C07D499/00 , C07D501/00
摘要： The present invention provides: an industrially-excellent and novel process for producing a basic antibiotic.inorganic acid salt, for example, an excellent production process for producing a hydrochloride thereof industrially, that is, a production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: (wherein the ring A means the basic antibiotic; R means a protected functional group used in organic synthesis; Ak-E means the alkali earth metal; and B means the inorganic acid, respectively); a novel oxalate useful as a production intermediate for producing an antibiotic.hydrochloride industrially, that is, an oxalate (II-I) of a carbapenem compound represented by the following formula: (wherein the ring A represents a 3- to 7-membered ring having at least one nitrogen atom, and the ring A may be substituted with other than R ; R represents hydrogen or methyl group; R and R are the same as or different form each other and each represents hydrogen or a hydroxyl-protecting group; R represents a carboxyl-protecting group; R represents hydrogen, a lower alkyl group or an amino-protecting group; R represents (1) hydrogen, (2) an optionally protected hydroxyl group, carbamoyl, formimidoyl, acetoimidoyl or a lower alkyl group which may be substituted with a substituent represented by the formula: (wherein R and R are the same as or different from each other and each represents hydrogen, a lower alkyl group or an amino-protecting group) or (3) an amino-protecting group or an imino-protecting group; and m is 0 or 1); and a process for producing its.

5. 发明专利

DE60014390D1 未知
公开(公告)号：DE60014390D1
公开(公告)日：2004-11-04
申请号：DE60014390
申请日：2000-07-27
申请人： EISAI CO LTD
发明人： KAYANO AKIO , CHIBA HIROYUKI , NAKAMURA TAIJU , SAKURAI SHIN , ISHIZUKA HIROYUKI , SAITO HIROYUKI , KOMATSU YUUKI , SASHO MANABU , SATO NOBUAKI , NEGI SHIGETO
IPC分类号： C07D477/02 , C07D477/08 , C07D477/20 , C07D499/68 , C07D501/22 , C07D501/36 , C07D501/46 , C07D463/00 , C07D499/00 , C07D501/00
摘要： The present invention provides: an industrially-excellent and novel process for producing a basic antibiotic.inorganic acid salt, for example, an excellent production process for producing a hydrochloride thereof industrially, that is, a production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: (wherein the ring A means the basic antibiotic; R means a protected functional group used in organic synthesis; Ak-E means the alkali earth metal; and B means the inorganic acid, respectively); a novel oxalate useful as a production intermediate for producing an antibiotic.hydrochloride industrially, that is, an oxalate (II-I) of a carbapenem compound represented by the following formula: (wherein the ring A represents a 3- to 7-membered ring having at least one nitrogen atom, and the ring A may be substituted with other than R ; R represents hydrogen or methyl group; R and R are the same as or different form each other and each represents hydrogen or a hydroxyl-protecting group; R represents a carboxyl-protecting group; R represents hydrogen, a lower alkyl group or an amino-protecting group; R represents (1) hydrogen, (2) an optionally protected hydroxyl group, carbamoyl, formimidoyl, acetoimidoyl or a lower alkyl group which may be substituted with a substituent represented by the formula: (wherein R and R are the same as or different from each other and each represents hydrogen, a lower alkyl group or an amino-protecting group) or (3) an amino-protecting group or an imino-protecting group; and m is 0 or 1); and a process for producing its.

6. 发明专利

AT263767T 未知
公开(公告)号：AT263767T
公开(公告)日：2004-04-15
申请号：AT00935544
申请日：2000-06-05
申请人： EISAI CO LTD
发明人： CHIBA HIROYUKI , TSUJII MASAHIKO , KOIWA ATSUSHI , SAKURAI SHIN , KAYANO AKIO , KAMISUMACHI , ISHIZUKA HIROYUKI , SAITO HIROYUKI , NAKAMURA TAIJU , KUSHIDA IKUO , SUZUKI YASUYUKI , YOSHIBA TAKAKO , ASHIZAWA KAZUHIDE , SAKURAI MASAHIRO , YAMAMOTO EIICHI
IPC分类号： A61K31/407 , A61P31/04 , C07D477/20 , A61K9/14 , A61K31/40
摘要： The present invention provides carbapenem hydrochloride monohydrate and trihydrate crystals, which are chemically stable, easily purified and useful as antimicrobial agents, a process for producing them, and a powdery charged preparation for injection comprising them. That is, it provides carbapenem hydrochloride monohydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 5.2, 4.3 and 4.0 ANGSTROM , carbapenem hydrochloride trihydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 9.0, 4.1 and 2.8 ANGSTROM , a process for producing them, and a powdery charged preparation for injection comprising them.

7. 发明专利

AU5105100A Crystals of carbapenem derivatives and pharmaceutical preparations for injection 未知
公开(公告)号：AU5105100A
公开(公告)日：2000-12-28
申请号：AU5105100
申请日：2000-06-05
申请人： EISAI CO LTD
发明人： CHIBA HIROYUKI , TSUJII MASAHIKO , KOIWA ATSUSHI , SAKURAI SHIN , KAYANO AKIO , ISHIZUKA HIROYUKI , SAITO HIROYUKI , NAKAMURA TAIJU , KUSHIDA IKUO , SUZUKI YASUYUKI , YOSHIBA TAKAKO , ASHIZAWA KAZUHIDE , SAKURAI MASAHIRO , YAMAMOTO EIICHI
IPC分类号： A61K31/407 , A61P31/04 , C07D477/20 , A61K9/14
摘要： The present invention provides carbapenem hydrochloride monohydrate and trihydrate crystals, which are chemically stable, easily purified and useful as antimicrobial agents, a process for producing them, and a powdery charged preparation for injection comprising them. That is, it provides carbapenem hydrochloride monohydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 5.2, 4.3 and 4.0 ANGSTROM , carbapenem hydrochloride trihydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 9.0, 4.1 and 2.8 ANGSTROM , a process for producing them, and a powdery charged preparation for injection comprising them.

8. 发明专利

DE60009695T2 未知
公开(公告)号：DE60009695T2
公开(公告)日：2004-09-23
申请号：DE60009695
申请日：2000-06-05
申请人： EISAI CO LTD
发明人： CHIBA HIROYUKI , TSUJII MASAHIKO , KOIWA ATSUSHI , SAKURAI SHIN , KAYANO AKIO , ISHIZUKA HIROYUKI , SAITO HIROYUKI , NAKAMURA TAIJU , KUSHIDA IKUO , SUZUKI YASUYUKI , YOSHIBA TAKAKO , ASHIZAWA KAZUHIDE , SAKURAI MASAHIRO , YAMAMOTO EIICHI
IPC分类号： A61K31/407 , A61P31/04 , C07D477/20 , A61K9/14 , A61K31/40
摘要： The present invention provides carbapenem hydrochloride monohydrate and trihydrate crystals, which are chemically stable, easily purified and useful as antimicrobial agents, a process for producing them, and a powdery charged preparation for injection comprising them. That is, it provides carbapenem hydrochloride monohydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 5.2, 4.3 and 4.0 ANGSTROM , carbapenem hydrochloride trihydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 9.0, 4.1 and 2.8 ANGSTROM , a process for producing them, and a powdery charged preparation for injection comprising them.

9. 发明专利

HU0202283A2 PROCESS FOR THE PREPARATION OF BASIC ANTIBIOTIC-INORGANIC ACID ADDITION SALTS AND INTERMEDIATE OXALATES 未知
公开(公告)号：HU0202283A2
公开(公告)日：2002-10-28
申请号：HU0202283
申请日：2000-07-27
申请人： EISAI CO LTD
发明人： CHIBA HIROYUKI , ISHIZUKA HIROYUKI , KAYANO AKIO , KOMATSU YUUKI , NAKAMURA TAIJU , NEGI SHIGETO , SAITO HIROYUKI , SAKURAI SHIN , SASHO MANABU , SATO NOBUAKI
IPC分类号： C07D477/02 , C07D477/08 , C07D477/20 , C07D499/68 , C07D501/22 , C07D501/36 , C07D501/46
摘要： The present invention provides: an industrially-excellent and novel process for producing a basic antibiotic.inorganic acid salt, for example, an excellent production process for producing a hydrochloride thereof industrially, that is, a production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: (wherein the ring A means the basic antibiotic; R means a protected functional group used in organic synthesis; Ak-E means the alkali earth metal; and B means the inorganic acid, respectively); a novel oxalate useful as a production intermediate for producing an antibiotic.hydrochloride industrially, that is, an oxalate (II-I) of a carbapenem compound represented by the following formula: (wherein the ring A represents a 3- to 7-membered ring having at least one nitrogen atom, and the ring A may be substituted with other than R ; R represents hydrogen or methyl group; R and R are the same as or different form each other and each represents hydrogen or a hydroxyl-protecting group; R represents a carboxyl-protecting group; R represents hydrogen, a lower alkyl group or an amino-protecting group; R represents (1) hydrogen, (2) an optionally protected hydroxyl group, carbamoyl, formimidoyl, acetoimidoyl or a lower alkyl group which may be substituted with a substituent represented by the formula: (wherein R and R are the same as or different from each other and each represents hydrogen, a lower alkyl group or an amino-protecting group) or (3) an amino-protecting group or an imino-protecting group; and m is 0 or 1); and a process for producing its.

10. 发明专利

NO20020471D0 未知
公开(公告)号：NO20020471D0
公开(公告)日：2002-01-29
申请号：NO20020471
申请日：2002-01-29
申请人： EISAI CO LTD
发明人： KAYANO AKIO , CHIBA HIROYUKI , NAKAMURA TAIJU , SAKURAI SHIN , ISHIZUKA HIROYUKI , SAITO HIROYUKI , KOMATSU YUUKI , SASHO MANABU , SATO NOBUAKI , NEGI SHIGETO
IPC分类号： C07D477/02 , C07D477/08 , C07D477/20 , C07D499/68 , C07D501/22 , C07D501/36 , C07D501/46 , C07D
摘要： The present invention provides: an industrially-excellent and novel process for producing a basic antibiotic.inorganic acid salt, for example, an excellent production process for producing a hydrochloride thereof industrially, that is, a production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: (wherein the ring A means the basic antibiotic; R means a protected functional group used in organic synthesis; Ak-E means the alkali earth metal; and B means the inorganic acid, respectively); a novel oxalate useful as a production intermediate for producing an antibiotic.hydrochloride industrially, that is, an oxalate (II-I) of a carbapenem compound represented by the following formula: (wherein the ring A represents a 3- to 7-membered ring having at least one nitrogen atom, and the ring A may be substituted with other than R ; R represents hydrogen or methyl group; R and R are the same as or different form each other and each represents hydrogen or a hydroxyl-protecting group; R represents a carboxyl-protecting group; R represents hydrogen, a lower alkyl group or an amino-protecting group; R represents (1) hydrogen, (2) an optionally protected hydroxyl group, carbamoyl, formimidoyl, acetoimidoyl or a lower alkyl group which may be substituted with a substituent represented by the formula: (wherein R and R are the same as or different from each other and each represents hydrogen, a lower alkyl group or an amino-protecting group) or (3) an amino-protecting group or an imino-protecting group; and m is 0 or 1); and a process for producing its.

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