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1. 发明授权

US5684128A Process for preparing side chain derivatives of cyclohexapeptidyl lipopeptides 失效
标题翻译：制备环己肽基脂肽的侧链衍生物的方法
公开(公告)号：US5684128A
公开(公告)日：1997-11-04
申请号：US604135
申请日：1996-02-20
申请人： James M. Balkovec , Frances A. Bouffard , James F. Dropinski , Akinlolu A. Adefarati , Jan S. Tkacz
发明人： James M. Balkovec , Frances A. Bouffard , James F. Dropinski , Akinlolu A. Adefarati , Jan S. Tkacz
IPC分类号： C07K1/113 , A61K38/00 , C07K7/06 , C07K7/56 , C07K7/64
CPC分类号： C07K7/56 , A61K38/00 , Y10S930/27
摘要： An improved process for the preparation of side chain derivatives of cyclohexapeptidyl lipopeptides represented by the formula ##STR1## wherein R.sup.1 is fully defined, is disclosed.
摘要翻译：公开了制备由其中R1完全限定的式“IMAGE”（SEQ ID NO.1）表示的环己基肽基脂肽的侧链衍生物的改进方法。

2. 发明授权

US5516756A Aza cyclohexapeptide compounds 失效
标题翻译：氮杂环己肽化合物
公开(公告)号：US5516756A
公开(公告)日：1996-05-14
申请号：US333574
申请日：1994-10-31
申请人： James M. Balkovec , Frances A. Bouffard , James F. Dropinski
发明人： James M. Balkovec , Frances A. Bouffard , James F. Dropinski
IPC分类号： A61K38/00 , A61P31/04 , A61P31/10 , A61P31/12 , C07K7/54 , C07K7/56 , A61K38/12 , C07K7/52
CPC分类号： C07K7/56 , A61K38/00 , Y10S930/27
摘要： The present invention is directed to novel aza cyclohexapeptide compounds of the formula ##STR1## where all substituents are defined herein, which are useful as antifungal agents and for the treatment of Pneumocystis carinii infections. Compositions containing the compounds of the invention are also disclosed.
摘要翻译：本发明涉及式（I）的新型氮杂环己肽化合物，其中所有取代基均在本文中定义，其可用作抗真菌剂和用于治疗卡氏肺囊虫感染。还公开了含有本发明化合物的组合物。

3. 发明授权

US5854212A Cyclohexapeptidyl bisamine compound, compositions containing said compound and methods of use 失效
标题翻译：环己酰基双胺化合物，含有所述化合物的组合物和使用方法
公开(公告)号：US5854212A
公开(公告)日：1998-12-29
申请号：US738489
申请日：1996-10-23
申请人： James M. Balkovec , Frances A. Bouffard , James F. Dropinski
发明人： James M. Balkovec , Frances A. Bouffard , James F. Dropinski
IPC分类号： A61K38/00 , C07K7/56 , A61K38/12 , C07K7/64
CPC分类号： C07K7/56 , A61K38/00
摘要： A compound of the formula ##STR1## is disclosed which is useful for the treatment of fungal infections and for the treatment of infections caused by Pneumocystis carinii.
摘要翻译：公开了式（I）SEQ ID No.1的化合物，其可用于治疗真菌感染和治疗由卡氏肺囊虫引起的感染。

4. 发明授权

US5646245A Process for preparing side chain derivatives of cyclohexapeptidyl lipopeptides 失效
公开(公告)号：US5646245A
公开(公告)日：1997-07-08
申请号：US648741
申请日：1996-05-16
申请人： James M. Balkovec , Frances A. Bouffard , James F. Dropinski , Akinlolu A. Adefarati , Jan S. Tkacz
发明人： James M. Balkovec , Frances A. Bouffard , James F. Dropinski , Akinlolu A. Adefarati , Jan S. Tkacz
IPC分类号： C07K1/113 , A61K38/00 , C07K7/06 , C07K7/56 , C07K7/64 , A61K38/12
CPC分类号： C07K7/56 , A61K38/00 , Y10S930/27
摘要： An improved process for the preparation of side chain derivatives of cyclohexapeptidyl lipopeptides represented by the formula ##STR1## wherein R.sup.1 is fully defined, is disclosed.

5. 发明授权

US5514651A Aza cyclohexapeptide compounds 失效
标题翻译：氮杂环己肽化合物
公开(公告)号：US5514651A
公开(公告)日：1996-05-07
申请号：US307978
申请日：1994-09-16
申请人： James M. Balkovec , Frances A. Bouffard , James F. Dropinski
发明人： James M. Balkovec , Frances A. Bouffard , James F. Dropinski
IPC分类号： A61K38/00 , C07K7/56 , A61K38/12 , C07K7/64
CPC分类号： C07K7/56 , A61K38/00 , Y10S930/27
摘要： The present invention relates to aza cyclohexapeptide compounds of the formula (Seq ID Nos. 1-10) ##STR1## which may be useful as antibiotics, antifungal agents and for the treatment of Pneumocystis carinii infections.
摘要翻译：本发明涉及式（Seq ID Nos.1-10）抗真菌剂和用于治疗卡氏肺囊虫感染的氮杂环己肽化合物。

6. 发明申请

US20110172225A1 ANTIFUNGAL AGENTS 有权
标题翻译：反真菌药
公开(公告)号：US20110172225A1
公开(公告)日：2011-07-14
申请号：US12680472
申请日：2008-09-25
申请人： James M. Balkovec , Phieng Siliphaivanh , Frances A. Bouffard , Roland A. Bouffard , Michael R. Peel , Weiming Fan , Ahmed Mamai , Sarah Dimick Gray
发明人： James M. Balkovec , Phieng Siliphaivanh , Frances A. Bouffard , Roland A. Bouffard , Michael R. Peel , Weiming Fan , Ahmed Mamai , Sarah Dimick Gray
IPC分类号： A61K31/5377 , C07D311/78 , C07D405/12 , C07D407/12 , C07D413/12 , C07D405/14 , A61K31/352 , A61K31/453 , A61K31/4025 , A61K31/422 , A61K31/4178 , A61K31/496 , A61K31/4545 , A61K31/454 , A61P31/10
CPC分类号： C07J71/0005
摘要： Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
摘要翻译：本文公开了enfumafungin的新型衍生物及其药学上可接受的盐，水合物和前药。还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这些化合物作为抗真菌剂和/或（1,3） - ＆bgr-D-葡聚糖合酶抑制剂的方法。所公开的化合物，其药学上可接受的盐，水合物和前药，以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。

7. 发明授权

US5514650A Aza cyclohexapeptide compounds 失效
标题翻译：氮杂环己肽化合物
公开(公告)号：US5514650A
公开(公告)日：1996-05-07
申请号：US298479
申请日：1994-08-29
申请人： James M. Balkovec , Regina M. Black , Frances A. Bouffard
发明人： James M. Balkovec , Regina M. Black , Frances A. Bouffard
IPC分类号： A61K38/00 , A61K38/08 , A61K38/12 , A61P31/00 , A61P31/04 , A61P31/10 , C07K7/06 , C07K7/54 , C07K7/56 , C07K7/64
CPC分类号： C07K7/56 , A61K38/00 , Y10S930/27
摘要： Ceretain aza cyclohexapeptide compounds have been found to have superior antibiotic properties. Novel processes for their preparation are also described.
摘要翻译：已经发现，谷类环己肽化合物具有优异的抗生素特性。还描述了其新型制备方法。

8. 发明授权

US08222255B2 Antifungal agents 有权
标题翻译：抗真菌剂
公开(公告)号：US08222255B2
公开(公告)日：2012-07-17
申请号：US12680472
申请日：2008-09-25
申请人： James M. Balkovec , Phieng Siliphaivanh , Frances A. Bouffard , Roland A. Bouffard, legal representative , Michael R. Peel , Weiming Fan , Ahmed Mamai , Sarah Dimick Gray
发明人： James M. Balkovec , Phieng Siliphaivanh , Frances A. Bouffard , Michael R. Peel , Weiming Fan , Ahmed Mamai , Sarah Dimick Gray
IPC分类号： C07D311/78 , C07D405/02 , A61K31/352 , A61K31/4025 , A61K31/4433 , A61K31/453 , A61K31/496 , A61K31/506 , A61K31/5355
CPC分类号： C07J71/0005
摘要： Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
摘要翻译：本文公开了enfumafungin的新型衍生物及其药学上可接受的盐，水合物和前药。还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这些化合物作为抗真菌剂和/或（1,3） - ＆bgr-D-葡聚糖合酶抑制剂的方法。所公开的化合物，其药学上可接受的盐，水合物和前药以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。

9. 发明授权

US5541160A Antifungal and anti-pneumocystis compounds, compositions containing such compounds, and methods of use 失效
标题翻译：抗真菌和抗肺囊虫化合物，含有这些化合物的组合物和使用方法
公开(公告)号：US5541160A
公开(公告)日：1996-07-30
申请号：US222157
申请日：1994-04-04
申请人： James M. Balkovec , Frances A. Bouffard , Regina M. Black
发明人： James M. Balkovec , Frances A. Bouffard , Regina M. Black
IPC分类号： A61K38/00 , C07K7/56 , C12P21/04
CPC分类号： C07K7/56 , A61K38/00
摘要： Compounds represented by the formula I (SEQ ID NO. 1) are disclosed: ##STR1## as well as pharmaceutically acceptable salts and hydrates thereof. R.sup.I represents C.sub.9 to C.sub.19 alkyl, C.sub.9 to C.sub.19 alkenyl, an aryl group which includes phenyl, biphenyl, naphthyl and terphenyl or a C.sub.1 to C.sub.12 alkyl, alkylamino, dialkylamino or alkoxyaryl group.R.sup.1, R.sup.2 and R.sup.4 independently represent H or --OH.R.sup.3 represents H, --OH, --O(CH.sub.2).sub.n NR.sup.V R.sup.VI, where R.sup.V and R.sup.VI independently represent H or C.sub.1-4 alkyl, or --O(CH.sub.2).sub.n NR.sup.V R.sup.VI R.sup.VII+ Y.sup.-, wherein R.sup.V and R.sup.VI are as defined above, R.sup.VII represents H or C.sub.1-4 alkyl, n is an integer of from 2-6 inclusive, and Y represents a counterion.R.sup.5 represents H, --CH.sub.3 or --OH;R.sup.6 represents H or --CH.sub.3 ;R.sup.7 represents H, --CH.sub.3, --CH.sub.2 C(.dbd.O)NH.sub.2, --(CH.sub.2).sub.2 NR.sup.V R.sup.VI or --(CH.sub.2).sub.2 NR.sup.V R.sup.VI R.sup.VII+ Y.sup.- with n, R.sup.V, R.sup.VI R.sup.VII and Y as defined above;and R.sup.8 represents --Cl, --Br, --I, --NO.sub.2, --N.sub.3, --(CH.sub.2).sub.0-4 NH.sub.2, --(CH.sub.2).sub.0-4 NH(C.sub.1-4 alkyl), --(CH.sub.2).sub.0-4 N(C.sub.1-4 alkyl).sub.2, --(CH.sub.2).sub.0-3 CH(.dbd.NOH), --NHC(.dbd.O)(CH.sub.2).sub.1-6 NH.sub.2 or --NHC(.dbd.O)(CH.sub.2).sub.1-6 NHC(.dbd.NH)(CH.sub.2).sub.0-3 H.Pharmaceutical compositions and methods of use are also disclosed.
摘要翻译：公开了由式I（SEQ ID NO.1）表示的化合物：其中药学上可接受的盐和水合物。 R 1表示C 9至C 19烷基，C 9至C 19烯基，包括苯基，联苯基，萘基和三联苯基或C 1至C 12烷基，烷基氨基，二烷基氨基或烷氧基芳基的芳基。 R1，R2和R4独立地表示H或-OH。 R3表示H，-OH，-O（CH2）nNRVRVI，其中RV和RVI独立地表示H或C1-4烷基或-O（CH2）nNRVRVIRVII + Y-，其中RV和RVI如上所定义，RVII表示H 或C 1-4烷基，n为2-6以下的整数，Y表示抗衡离子。 R5表示H，-CH3或-OH; R6代表H或-CH3; R 7表示H，-CH 3，-CH 2 C（= O）NH 2， - （CH 2）2 NRVRVI或 - （CH 2）2 NRVRVIRVII + Y-，其中n，RV，RVI RVII和Y定义如上; 并且R 8表示-Cl，-Br，-I，-NO 2，-N 3， - （CH 2）0-4NH 2， - （CH 2）0-4NH（C 1-4烷基）， - （CH 2）烷基）2， - （CH 2）0-3CH（= NOH），-NHC（= O）（CH 2）1-6 NH 2或-NHC（= O）（CH 2）1-6 NHC（= NH）（CH 2） -3H。还公开了药物组合物和使用方法。

10. 发明授权

US5378804A Aza cyclohexapeptide compounds 失效
标题翻译：氮杂环己肽化合物
公开(公告)号：US5378804A
公开(公告)日：1995-01-03
申请号：US32847
申请日：1993-03-16
申请人： James M. Balkovec , Regina M. Black , Frances A. Bouffard
发明人： James M. Balkovec , Regina M. Black , Frances A. Bouffard
IPC分类号： A61K38/00 , A61K38/08 , A61K38/12 , A61P31/00 , A61P31/04 , A61P31/10 , C07K7/06 , C07K7/54 , C07K7/56 , C07K7/64
CPC分类号： C07K7/56 , A61K38/00 , Y10S930/27
摘要： Aza cyclohexapeptide compounds are disclosed with a nitrogen attached to the cyclohexapeptide ring at the 5-carbon of the 4-hydroxyornithine component. Such compounds are represented by the formula: ##STR1## The compounds are disclosed as having antifungal, antiprotozoal and anti-Pneumocystis carinii activity.
摘要翻译：公开了在4-羟基鸟氨酸组分的5-碳上连接到环己肽环的氮的氮杂环己肽化合物。这些化合物由具有抗真菌，抗原生动物和抗卡氏肺囊虫活性的式S表示。

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