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11. 发明授权

US06268338B1 Cyclohexapeptidyl amine compounds 失效
标题翻译：环己酰胺胺化合物
公开(公告)号：US06268338B1
公开(公告)日：2001-07-31
申请号：US08055996
申请日：1993-04-30
申请人： James M. Balkovec , Frances Aileen Bouffard , James F. Dropinski , Robert A. Zambias
发明人： James M. Balkovec , Frances Aileen Bouffard , James F. Dropinski , Robert A. Zambias
IPC分类号： A61K3800
CPC分类号： C07K7/56 , A61K38/00
摘要： Cyclohexapeptidyl amine compounds are disclosed of the formula: or its acid addition salt, wherein: R1 is H or OH; R2 is H or OH; R3 is QCnH2nNRVRVI, QCnH2nNRVRVIRVII+Y−, or Q(CH2)1-3CRVIIIRIXNHRX. R4 is H or OH; R5 is H, OH or CH3; R6 is H or CH3; RI is wherein Ra is C1-C10 alkyl; or (CH2)qNRbRc wherein Rb and Rc are independently H, C1-C10 alkyl or Rb and Rc taken together are wherein Rd is C1-C16 alkyl, phenyl or benzyl; RII is H, C1-4 alkyl or benzyl; RIII is H, C1-4 alkyl or benzyl; RIV is RII and RIII taken together as —(CH2)4— or —(CH2)5—; RV is H, C1-C4 alkyl or benzyl; RVI is H, C1-C4 alkyl or benzyl or RV and RVI together is —(CH2)4— or —(CH2)5—; RVII is H or C1-C4 alkyl; RVIII is H, (CH2)mH, (CH2)mOH, (CH2)mNH2 or COX wherein X is NH2, OH or O(CH2)mH; RIX is H, (CH2)mH, or together with RVIII is ═O (carbonyl); RX is H (except when RVIII and RIX are H, C(═NH)NH2, C(═NH)CH2)0-3H, CO(CH2)0-3H, CO(CH2)mNH2, (CH2)2-4OH or (CH2)2-4NH2; Q is O or S; Y is an anion of a pharmaceutically acceptable salt each m is independently an integer from 1 to 3, inclusive; n is an integer from 2 to 4, inclusive; p is an integer from 1 to 2, inclusive and q is an integer from 2 to 4, inclusive.
摘要翻译：公开了下式：或其酸加成盐的环己酰胺化合物，其中：R1是H或OH; R2是H或OH; R3是QCnH2nNRVRVI，QCnH2nNRVRVIRVII + Y-或Q（CH2）1-3CRVIIIRIXNHRX.R4是H 或OH; R 5是H，OH或CH 3; R 6是H或CH 3; R 1是其中R a是C 1 -C 10烷基; 或（CH 2）q NR b R c其中R b和R c独立地为H，C 1 -C 10烷基或R b和R c在一起，其中R 1为C 1 -C 16烷基，苯基或苄基; R II为H，C 1-4烷基或苄基; R III为H，Cl -4-烷基或苄基; RIV是RII和RIII，一起作为 - （CH 2）4 - 或 - （CH 2）5 - ; RV是H，C 1 -C 4烷基或苄基; R VI是H，C 1 -C 4烷基或苄基或 RV和RVI一起是 - （CH 2）4 - 或 - （CH 2）5; RVII是H或C 1 -C 4烷基; RVIII是H，（CH 2）m H，（CH 2）m OH，（CH 2）m NH 2或COX，其中X是NH 2 ，OH或O（CH 2）m H; RIX为H，（CH 2）m H或与RVIII一起为=（（羰基））; RX为H（除非当RVIII和RIX为H时，C（= NH）NH 2，C（ = NH）CH 2）0-3H，CO（CH 2）0-3H，CO（CH 2）m NH 2，（CH 2）2-4 OH或（CH 2）2-4 NH 2; Q为O或S; Y为药学上阴离子可接受的salteach m独立地为1〜3的整数，包括0和n; n为2〜4的整数，p为2〜4的整数，q为2〜4的整数。

12. 发明授权

US06030944A Cyclohexapeptidyl bisamine compounds 失效
标题翻译：环己酰肽双胺化合物
公开(公告)号：US06030944A
公开(公告)日：2000-02-29
申请号：US936558
申请日：1992-09-03
申请人： Frances Aileen Bouffard , James F. Dropinski , Robert A. Zambias
发明人： Frances Aileen Bouffard , James F. Dropinski , Robert A. Zambias
IPC分类号： A61K38/00 , A61P31/04 , A61P31/10 , C07K7/56 , C12P21/02 , C12P21/04 , C12R1/01 , C12R1/645 , A61K38/12 , C07K7/54
CPC分类号： C07K7/56 , A61K38/00
摘要： Certain bisamine compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for direct use in therapeutic compositions are described. A novel process for their preparation is also described.
摘要翻译：描述了具有环己基肽基核并且被发现具有适于直接用于治疗组合物的物理性质的抗生素活性的某些双胺化合物。还描述了其制备的新方法。

13. 发明申请

US20130123237A1 NOVEL CYCLIC AZABENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS 有权
标题翻译：用作抗糖尿病药物的新型CYABAZABENZIMIDAZOLE衍生物
公开(公告)号：US20130123237A1
公开(公告)日：2013-05-16
申请号：US13812536
申请日：2012-02-23
申请人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
发明人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： A61K31/5377 , A61K31/437 , A61K31/4985 , A61K31/351 , A61K31/397 , A61K31/4412 , C07D471/04 , A61K31/496
CPC分类号： A61K31/5377 , A61K31/351 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/4412 , A61K31/496 , A61K31/4985 , A61K31/519 , A61K45/06 , C07D471/04 , C07D519/00 , A61K2300/00
摘要： Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译：结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制由AMPK激活的蛋白激酶介导的疾病。本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。

14. 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.

15. 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。

16. 发明授权

US08796258B2 Cyclic azabenzimidazole derivatives useful as anti-diabetic agents 有权
标题翻译：用作抗糖尿病药的环状氮杂苯并咪唑衍生物
公开(公告)号：US08796258B2
公开(公告)日：2014-08-05
申请号：US13812536
申请日：2012-02-23
申请人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
发明人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： A61K31/00 , C07D513/02
CPC分类号： A61K31/5377 , A61K31/351 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/4412 , A61K31/496 , A61K31/4985 , A61K31/519 , A61K45/06 , C07D471/04 , C07D519/00 , A61K2300/00
摘要： Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译：结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制由AMPK激活的蛋白激酶介导的疾病。本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。

17. 发明授权

US06908934B2 Therapeutic compounds for treating dyslipidemic conditions 失效
标题翻译：用于治疗血脂异常的治疗化合物
公开(公告)号：US06908934B2
公开(公告)日：2005-06-21
申请号：US10158679
申请日：2002-05-30
申请人： Alan D. Adams , Aileen Bouffard , James F. Dropinski , Clare E. Gutteridge , A. Brian Jones , Weiguo Lui , John George Ondeyka , Ali Shiafee , Sheo Bux Singh
发明人： Alan D. Adams , Aileen Bouffard , James F. Dropinski , Clare E. Gutteridge , A. Brian Jones , Weiguo Lui , John George Ondeyka , Ali Shiafee , Sheo Bux Singh
IPC分类号： A61K31/16 , A61K31/215 , A01N43/40 , A61K31/445
CPC分类号： A61K31/215 , A61K31/16
摘要： Compounds of Formula I and the pharmaceutically acceptable salts and esters thereof, wherein Z is selected from the group consisting of: (a) Formula Ia and (b) Formula Ib are novel LXR agonists and are useful in the treatment of dyslipidemic conditions particularly depressed levels of HDL cholesterol.
摘要翻译：式I化合物及其药学上可接受的盐和酯，其中Z选自：（a）式Ia和（b）式Ib是新型LXR激动剂，可用于治疗血脂异常，特别是抑郁水平的HDL胆固醇。

18. 发明授权

US5914313A 1-�4-hydroxy-5-aminoethyloxy-N.sup.2 -(10,12-dimethyl-1-oxotetradecyl)ornithine!-5-(3-hydroxyglutamine)-6-(3- hydroxyproline)echinocandin B, other aminoalkyl derivatives and salts thereof 失效
标题翻译： 1- [4-羟基-5-氨基乙氧基-N2-（10,12-二甲基-1-氧代十四烷基）鸟氨酸] -5-（3-羟基谷氨酰胺）-6-（3-羟基脯氨酸）棘白菌素B，其它氨基烷基衍生物和盐其中
公开(公告)号：US5914313A
公开(公告)日：1999-06-22
申请号：US5942
申请日：1993-01-15
申请人： Frances Aileen Bouffard , James F. Dropinski
发明人： Frances Aileen Bouffard , James F. Dropinski
IPC分类号： A61K38/00 , C07K7/56 , A61K38/12 , C07K7/50
CPC分类号： C07K7/56 , A61K38/00
摘要： A compound having the formula ##STR1## in which R.sub.1 is an aminoalkyl group and ##STR2## is an acyl group and salts thereof having high antibiotic activity and being substantially free of lytic activity are described.
摘要翻译：描述了具有下式的化合物，其中R 1是氨基烷基并且是酰基，并且其具有高抗生素活性和基本上没有裂解活性的盐。

19. 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。

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