公开(公告)号：US20080118969A1

公开(公告)日：2008-05-22

申请号：US12021735

申请日：2008-01-29

申请人： Daniel Getman ,  Gary DeCrescenzo ,  John Freskos ,  Michael Vazquez ,  James Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David Brown ,  Joseph McDonald

发明人： Daniel Getman ,  Gary DeCrescenzo ,  John Freskos ,  Michael Vazquez ,  James Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David Brown ,  Joseph McDonald

IPC分类号： C12N7/06

CPC分类号： C07K5/06026 ,  A61K31/16 ,  A61K31/165 ,  A61K31/357 ,  A61K31/36 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K38/00 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06191

摘要： Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, compositions, and methods for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

摘要翻译： 选择的双氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。 本发明涉及这样的逆转录病毒蛋白酶抑制剂，更具体地涉及用于抑制逆转录病毒蛋白酶（例如人免疫缺陷病毒（HIV）蛋白酶），预防性逆转录病毒感染或逆转录病毒扩散的选择的新化合物，组合物和方法， 并治疗逆转录病毒感染。

公开(公告)号：US20060264483A1

公开(公告)日：2006-11-23

申请号：US11397055

申请日：2006-04-04

申请人： Daniel Getman ,  Gary DeCrescenzo ,  John Freskos ,  Michael Vazquez ,  James Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  Joseph McDonald

发明人： Daniel Getman ,  Gary DeCrescenzo ,  John Freskos ,  Michael Vazquez ,  James Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  Joseph McDonald

IPC分类号： A61K31/428 ,  A61K31/423 ,  A61K31/4184 ,  A61K31/343 ,  C07D417/02 ,  C07D277/62 ,  C07D263/60 ,  C07D235/04

CPC分类号： C07D263/56 ,  C07C317/44 ,  C07D215/36 ,  C07D217/02 ,  C07D217/04 ,  C07D235/30 ,  C07D235/32 ,  C07D249/20 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D307/82 ,  C07D311/58 ,  C07D317/62 ,  C07D319/18

摘要： Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

公开(公告)号：US20070037754A1

公开(公告)日：2007-02-15

申请号：US11501926

申请日：2006-08-10

申请人： Daniel Getman ,  Gary DeCrescenzo ,  John Freskos ,  Michael Vazquez ,  James Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David Brown ,  Joseph McDonald

发明人： Daniel Getman ,  Gary DeCrescenzo ,  John Freskos ,  Michael Vazquez ,  James Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David Brown ,  Joseph McDonald

IPC分类号： A61K38/04 ,  C07K5/04

CPC分类号： C07K5/06026 ,  A61K31/16 ,  A61K31/165 ,  A61K31/357 ,  A61K31/36 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K38/00 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06191

摘要： Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, compositions, and methods for inhibiting retroviral proteases, such as human inmmunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

摘要翻译： 选择的双氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。 本发明涉及这样的逆转录病毒蛋白酶抑制剂，更具体地涉及用于抑制逆转录病毒蛋白酶（例如人类免疫缺陷病毒（HIV）蛋白酶），预防性逆转录病毒感染或逆转录病毒扩散的选择的新化合物，组合物和方法， 并治疗逆转录病毒感染。

公开(公告)号：US20070004646A1

公开(公告)日：2007-01-04

申请号：US11450959

申请日：2006-06-12

申请人： Daniel Getman ,  Gary DeCrescenzo ,  John Freskos ,  Michael Vazquez ,  James Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David Brown ,  Joseph McDonald

发明人： Daniel Getman ,  Gary DeCrescenzo ,  John Freskos ,  Michael Vazquez ,  James Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David Brown ,  Joseph McDonald

IPC分类号： A61K38/04 ,  C07K5/04 ,  C07D403/02

CPC分类号： C07K5/021 ,  A61K38/00 ,  C07K5/06139 ,  C07K5/06165

摘要： Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, compositions, and methods for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

摘要翻译： 选择的杂环羰基氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。 本发明涉及这样的逆转录病毒蛋白酶抑制剂，更具体地涉及用于抑制逆转录病毒蛋白酶（例如人免疫缺陷病毒（HIV）蛋白酶），预防性逆转录病毒感染或逆转录病毒扩散的选择的新化合物，组合物和方法， 并治疗逆转录病毒感染。

公开(公告)号：US20060189611A1

公开(公告)日：2006-08-24

申请号：US11337836

申请日：2006-01-24

申请人： Daniel Getman ,  Gary DeCrescenzo ,  John Freskos ,  Michael Vazquez ,  James Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David Brown ,  Joseph McDonald

发明人： Daniel Getman ,  Gary DeCrescenzo ,  John Freskos ,  Michael Vazquez ,  James Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David Brown ,  Joseph McDonald

IPC分类号： A61K31/5377 ,  A61K31/4025 ,  A61K31/40 ,  C07D413/02 ,  C07D405/02

CPC分类号： C07D307/79 ,  A61K38/00 ,  C07D235/30 ,  C07D277/62 ,  C07D295/15 ,  C07D311/58 ,  C07D317/62 ,  C07D319/18 ,  C07D339/06 ,  C07D405/12 ,  C07D405/14 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/0606 ,  C07K5/06069

摘要： Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

公开(公告)号：US20050227926A1

公开(公告)日：2005-10-13

申请号：US11036606

申请日：2005-01-18

申请人： Daniel Getman ,  Gary DeCrescenzo ,  John Freskos ,  Michael Vazquez ,  James Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David Brown ,  Joseph McDonald

发明人： Daniel Getman ,  Gary DeCrescenzo ,  John Freskos ,  Michael Vazquez ,  James Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David Brown ,  Joseph McDonald

IPC分类号： A61K38/00 ,  A61K38/04 ,  C07K5/04 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065

CPC分类号： C07K5/06026 ,  A61K38/00

摘要： Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

公开(公告)号：US06673822B2

公开(公告)日：2004-01-06

申请号：US10120791

申请日：2002-04-12

申请人： Daniel P Getman ,  Gary A DeCrescenzo ,  John N Freskos ,  Michael L Vazquez ,  James A Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David L Brown ,  Joseph J McDonald

发明人： Daniel P Getman ,  Gary A DeCrescenzo ,  John N Freskos ,  Michael L Vazquez ,  James A Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David L Brown ,  Joseph J McDonald

IPC分类号： A61K31428

CPC分类号： C07K5/021 ,  A61K38/00 ,  C07K5/06139 ,  C07K5/06165

摘要： Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

公开(公告)号：US06458785B1

公开(公告)日：2002-10-01

申请号：US09836443

申请日：2001-04-18

申请人： Daniel P Getman ,  Gary A. DeCrescenzo ,  John N. Freskos ,  Michael L. Vazquez ,  James A. Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David L. Brown ,  Joseph J. McDonald

发明人： Daniel P Getman ,  Gary A. DeCrescenzo ,  John N. Freskos ,  Michael L. Vazquez ,  James A. Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David L. Brown ,  Joseph J. McDonald

IPC分类号： A61K3154

CPC分类号： C07D307/79 ,  A61K38/00 ,  C07D235/30 ,  C07D277/62 ,  C07D295/15 ,  C07D311/58 ,  C07D317/62 ,  C07D319/18 ,  C07D339/06 ,  C07D405/12 ,  C07D405/14 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/0606 ,  C07K5/06069

摘要： Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

摘要翻译： 选择的氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。 本发明涉及逆转录病毒蛋白酶抑制剂，更具体地涉及选择的新化合物，用于抑制逆转录病毒蛋白酶如人免疫缺陷病毒（HIV）蛋白酶的组合物和方法，预防性地预防逆转录病毒感染或逆转录病毒的扩散，以及治疗 的逆转录病毒感染。

公开(公告)号：US6100423A

公开(公告)日：2000-08-08

申请号：US261822

申请日：1999-03-03

申请人： Joe T. Collins ,  Balekudru Devadas ,  Hwang-fun Lu ,  James W. Malecha ,  Julie Marion Miyashiro ,  Srinivasan Nagarajan ,  Joseph Gerace Rico ,  Thomas E. Rogers

发明人： Joe T. Collins ,  Balekudru Devadas ,  Hwang-fun Lu ,  James W. Malecha ,  Julie Marion Miyashiro ,  Srinivasan Nagarajan ,  Joseph Gerace Rico ,  Thomas E. Rogers

IPC分类号： C07D239/14 ,  C07C229/00

CPC分类号： C07D239/14

摘要： The present invention is directed to compounds of the formula ##STR1## where R.sup.1 is BOC or H, R is H or lower alkyl; X and Y are the same or different halo atoms selected from the group consisting of Cl, Br or I and pharmaceutically acceptable salts and isomers thereof.

摘要翻译： 本发明涉及下式的化合物，其中R 1是BOC或H，R是H或低级烷基; X和Y是选自Cl，Br或I的相同或不同的卤原子及其药学上可接受的盐和异构体。

公开(公告)号：US5942600A

公开(公告)日：1999-08-24

申请号：US823101

申请日：1997-03-24

申请人： James A. Sikorski ,  Balekudru Devadas ,  Daniel P. Getman ,  David L. Brown ,  Srinivasan Nagarajan ,  Mark E. Zupec ,  Jeffrey I. Gordon

发明人： James A. Sikorski ,  Balekudru Devadas ,  Daniel P. Getman ,  David L. Brown ,  Srinivasan Nagarajan ,  Mark E. Zupec ,  Jeffrey I. Gordon

IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/083 ,  A61K38/06

CPC分类号： C07K5/06191 ,  C07K5/0606 ,  C07K5/081 ,  A61K38/00

摘要： Seryl-lysyl-based peptide and peptidomimetic compounds are described as inhibitors of the enzyme N-myristoyl transferase to provide selective control of the fungal organism Candida albicans. Peptidomimetic compounds of particular interest are those of the formula: ##STR1## wherein R.sup.1 is selected form aminoalkyl, p-aminoalkylphenylalkyl, imidazolylalkylphenylalkyl, 2-alkylimidazolylalkylphenylalkyl, benzimidazolylalkylphenylalkyl and 2-alkylbenzimidazolylalkylphenylalkyl; wherein R.sup.2 is selected from hydrido, alkyl, cycloalkyl, akenyl, alkynyl, haloalkyl, benzyl, alkylphenylalkyl, alkoxyphenylalkyl, halophenylalkyl, phenethyl, cycloalkylalkyl, halocycloalkylalkyl, alkylcycloalkylalkyl, alkoxycycloalkylalkyl and naphthylalkyl; wherein Y is selected from carboxylic acid, hydroxamic acid, phosphonic acid and tetrazolyl; or a pharmaceutically-acceptable salt, amide or ester thereof. Compounds of the formula are species-specific inhibitors of C. albicans with little effect on human NMT enzyme and thus would be useful in treating C. albicans fungal infections in humans.

摘要翻译： 基于丝氨酰赖氨酰的肽和拟肽化合物被描述为N-肉豆蔻酰转移酶的抑制剂，以提供真菌生物体白色念珠菌的选择性控制。 特别感兴趣的拟肽化合物是下式的化合物：其中R1选自氨基烷基，对氨基烷基苯基烷基，咪唑基烷基苯基烷基，2-烷基咪唑基烷基苯基烷基，苯并咪唑基烷基苯基烷基和2-烷基苯并咪唑基烷基苯基烷基; 烷基，环烷基，烯基，炔基，卤代烷基，苄基，烷基苯基烷基，烷氧基苯基烷基，卤代苯基烷基，苯乙基，环烷基烷基，卤代环烷基烷基，烷基环烷基烷基，烷氧基环烷基烷基和萘基烷基。 其中Y选自羧酸，异羟肟酸，膦酸和四唑基; 或其药学上可接受的盐，酰胺或酯。 式的化合物是白色念珠菌的物种特异性抑制剂，对人NMT酶几乎没有影响，因此可用于治疗人类白色念珠菌真菌感染。