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    Oxazalidinone compounds and methods of preparation and use thereof
    1.
    发明授权
    Oxazalidinone compounds and methods of preparation and use thereof 失效
    恶唑烷酮化合物及其制备方法及用途

    公开(公告)号：US06743811B2

    公开(公告)日：2004-06-01

    申请号：US10183198

    申请日：2002-06-27

    申请人： Mikhail F. Gordeev ,  Gary W. Luehr ,  Dinesh V. Patel ,  Robert C. Gadwood

    发明人： Mikhail F. Gordeev ,  Gary W. Luehr ,  Dinesh V. Patel ,  Robert C. Gadwood

    IPC分类号： A61K31422

    CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

    摘要： Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.

    摘要翻译： 提供了恶唑烷酮及其合成方法。 还提供制备生物活性恶唑烷酮的方法以及包含恶唑烷酮的药学上可接受的组合物。 本文公开的恶唑烷酮可以容易地合成并用于各种应用中，包括用作抗微生物剂。 在一个实施方案中，提供了各种硫代酰胺甲基恶唑烷酮及其合成和使用的方法。

    Thiadiazolyl and oxadiazolyl phenyl oxazolidinone antibacterial agents
    2.
    发明授权
    Thiadiazolyl and oxadiazolyl phenyl oxazolidinone antibacterial agents 失效
    噻二唑基和恶二唑基苯基恶唑烷酮抗菌剂

    公开(公告)号：US5977373A

    公开(公告)日：1999-11-02

    申请号：US111995

    申请日：1998-07-08

    申请人： Robert C. Gadwood ,  Lisa Marie Thomasco ,  David John Anderson

    发明人： Robert C. Gadwood ,  Lisa Marie Thomasco ,  David John Anderson

    IPC分类号： A61K31/4245 ,  A61K31/433 ,  A61P31/04 ,  C07D413/10 ,  C07D417/10

    CPC分类号： C07D413/10 ,  C07D417/10

    摘要： The present invention provides thiadiazolyl and oxadiazolyl phenyl oxzolidinone compounds of formula I ##STR1## wherein Q is thiadiazolyl or oxadiazolyl; wherein X.sup.1 and X.sup.2 are independently hydrogen, fluorine or chlorine; andwherein R.sup.1 is, for example, --COCH.sub.3 or --COCH.sub.2 CH.sub.3.These compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive and gram-negative aerobic bacteria.

    摘要翻译： 本发明提供式I的噻二唑基和恶二唑基苯基唑烷酮化合物，其中Q是噻二唑基或恶二唑基; 其中X1和X2独立地为氢，氟或氯; 并且其中R 1是例如-COCH 3或-COCH 2 CH 3。 这些化合物是有用的抗微生物剂，对许多人类和兽医病原体有效，包括革兰氏阳性和革兰氏阴性的需氧细菌。

    Aminoaryl oxazolidinone N-oxides
    5.
    发明授权
    Aminoaryl oxazolidinone N-oxides 失效

    公开(公告)号：US06518427B1

    公开(公告)日：2003-02-11

    申请号：US09988077

    申请日：2001-06-28

    申请人： Robert C. Gadwood ,  Bharat V. Kamdar

    发明人： Robert C. Gadwood ,  Bharat V. Kamdar

    IPC分类号： A61K31495

    CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D491/08 ,  C07D491/10 ,  C07D495/08

    摘要： The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.

    Aminoaryl oxazolidinone N-oxides
    6.
    发明授权
    Aminoaryl oxazolidinone N-oxides 失效

    公开(公告)号：US06512112B2

    公开(公告)日：2003-01-28

    申请号：US09894019

    申请日：2001-06-28

    申请人： Robert C. Gadwood ,  Bharat V. Kamdar

    发明人： Robert C. Gadwood ,  Bharat V. Kamdar

    IPC分类号： C07D40300

    CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D491/08 ,  C07D491/10 ,  C07D495/08

    摘要： The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.

    Aminoaryl oxazolidinone N-oxides
    7.
    发明授权
    Aminoaryl oxazolidinone N-oxides 失效
    氨基芳基恶唑烷酮N-氧化物

    公开(公告)号：US06277985B1

    公开(公告)日：2001-08-21

    申请号：US08709998

    申请日：1996-09-09

    申请人： Robert C. Gadwood ,  Bharat V. Kamdar

    发明人： Robert C. Gadwood ,  Bharat V. Kamdar

    IPC分类号： C07D41310

    CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D491/08 ,  C07D491/10 ,  C07D495/08

    摘要： The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.

    摘要翻译： 本发明提供式I的氨基芳基恶唑烷酮N-氧化物化合物，其中变量如本文所定义。 这些化合物是非常水溶性的，其可用于制备这些化合物的药物制剂。 它们也在体内快速转化回母体胺，使得它们可用作母体胺的前药。 它们对许多人类和兽医病原体有效，包括革兰氏阳性好氧细菌，如多重耐药葡萄球菌，链球菌和肠球菌，以及厌氧生物，如拟杆菌属。 和梭菌属（Clostridia spp。） 物种和耐酸生物，如结核分枝杆菌，鸟分枝杆菌和分枝杆菌，以及生物体如支原体属（Mycoplasma spp）。

    Thiazolidinedione analogues for the treatment of metabolic diseases
    9.
    发明授权
    Thiazolidinedione analogues for the treatment of metabolic diseases 有权
    噻唑烷二酮类似物用于治疗代谢性疾病

    公开(公告)号：US08067450B2

    公开(公告)日：2011-11-29

    申请号：US12677541

    申请日：2008-09-15

    申请人： Gerard R. Colca ,  Robert C. Gadwood ,  Tim Parker

    发明人： Gerard R. Colca ,  Robert C. Gadwood ,  Tim Parker

    IPC分类号： A61K31/426 ,  C07D277/02

    CPC分类号： C07D277/34

    摘要： The present invention relates to thiazolidinedione analogues that are useful for treating hypertension, diabetes, and inflammatory diseases. Formula (I), wherein: each of R1 and R4 is independently selected from H, halo, aliphatic, and alkoxy, wherein the aliphatic and alkoxy are optionally substituted with 1-3 of halo; R2 is halo, hydroxy, or optionally substituted aliphatic, and R′2 is H, or R2 and R′2 together form oxo; R3 is H; and Ring A is a phenyl.

    摘要翻译： 本发明涉及可用于治疗高血压，糖尿病和炎性疾病的噻唑烷二酮类似物。 式（I），其中：R 1和R 4各自独立地选自H，卤素，脂族和烷氧基，其中脂族和烷氧基任选被1-3个卤素取代; R2是卤素，羟基或任选取代的脂族基，R'2是H，或R 2和R'2一起形成氧代; R3为H; 环A是苯基。