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51. 发明授权

US4372864A Reagent for froth flotation of bituminous coal 失效
标题翻译：烟煤泡沫浮选试剂
公开(公告)号：US4372864A
公开(公告)日：1983-02-08
申请号：US860899
申请日：1977-12-15
申请人： James R. McCarthy
发明人： James R. McCarthy
IPC分类号： B03B9/00 , B03D1/002 , B03D1/012 , B03D1/02 , B03D1/00
CPC分类号： B03D1/02 , B03B9/005 , B03D1/002 , B03D1/006 , B03D1/018 , B03D2203/08
摘要： A reagent and a method for using the reagent for treating a solid material disposed in a liquid medium and having an oxygen-controlled surface condition. The reagent includes a liquid hydrocarbon, a reducing material and an activator material. The liquid hydrocarbon such as mineral oil has a specific gravity different from the specific gravity of the liquid medium. The reducing material such as phosphorous pentasulfide is present in an amount sufficient to establish a reducing environment around the solid material for breaking the oxygen control on the surface of the solid material. The activator material such as zinc thiophosphate is present in an amount sufficient to establish an electrostatic charge on the solid material after the oxygen-controlled surface condition has been broken. A more specific feature of the invention is directed to the method of flotation of extremely fine bituminous coal having an oxygen-controlled surface condition. The reagent is used in the conventional froth flotation equipment of the prior art.
摘要翻译：一种试剂和使用该试剂处理设置在液体介质中并具有氧控制表面状态的固体材料的方法。试剂包括液体烃，还原材料和活化剂材料。液体烃如矿物油的比重与液体介质的比重不同。诸如五硫化二磷的还原材料以足以在固体材料周围建立还原环境的量存在，以破坏固体材料表面上的氧气控制。催化剂材料如硫代磷酸锌存在的量足以在氧气受控表面状态被破坏之后在固体材料上形成静电电荷。本发明的更具体的特征涉及具有氧控制表面状态的极细煤烟的浮选方法。该试剂用于现有技术的常规泡沫浮选设备中。

52. 发明授权

US3972931A N,N'-Disubstituted benzamidines 失效
标题翻译： N，N {40-二取代苯甲酰胺
公开(公告)号：US3972931A
公开(公告)日：1976-08-03
申请号：US527989
申请日：1974-11-29
申请人： James R. McCarthy, Jr.
发明人： James R. McCarthy, Jr.
IPC分类号： A61K31/155 , C07C123/00
CPC分类号： A61K31/155
摘要： N,N'-Disubstituted benzamidine compounds such as N,N'-dimethyl-3,4-dichlorobenzamidine, and their pharmaceutically-acceptable salts are prepared by the reaction of a substituted phenylacetonitrile with an alkylamine and alkylammonium salt or alternatively, by reaction of the acetonitrile or corresponding N-alkylphenylacetamide with a trialkyloxonium fluoroborate followed by reaction with a primary alkylamine. The compounds have pharmacological activity as antidepressants and antianxiety or calming agents.
摘要翻译： N，N'-二取代的苄脒化合物如N，N'-二甲基-3,4-二氯苄脒及其药学上可接受的盐通过取代的苯基乙腈与烷基胺和烷基铵盐的反应制备，或者通过乙腈或相应的N-烷基苯基乙酰胺与三烷氧基氟硼酸盐接触，然后与伯烷基胺反应。这些化合物具有作为抗抑郁药和抗焦虑或镇定剂的药理活性。

53. 发明授权

US3969532A 1-Aryl-3-(2-hydroxyethyl) thioureas for treating depression 失效
标题翻译：用于治疗抑郁症的1-芳基-3-（2-羟乙基）硫脲
公开(公告)号：US3969532A
公开(公告)日：1976-07-13
申请号：US603831
申请日：1975-08-11
申请人： James R. McCarthy, Jr. , Don V. Wysong , Bobbie J. Allen
发明人： James R. McCarthy, Jr. , Don V. Wysong , Bobbie J. Allen
IPC分类号： C07C335/12 , C07C335/18 , A61K31/17
CPC分类号： C07C335/12 , C07C335/18
摘要： Certain 1-aryl-3-(2-hydroxyethyl)thioureas which are useful as antidepressants.
摘要翻译：可用作抗抑郁药的某些1-芳基-3-（2-羟乙基）硫脲。

54. 发明授权

US09206141B2 Processes for preparing linezolid 有权
标题翻译：制备利奈唑胺的方法
公开(公告)号：US09206141B2
公开(公告)日：2015-12-08
申请号：US13695211
申请日：2011-04-28
申请人： James R. McCarthy
发明人： James R. McCarthy
IPC分类号： C07D265/30 , C07D263/20
CPC分类号： C07D263/20
摘要： Processes and intermediates for preparing linezolid, and pharmaceutically acceptable salts thereof, are described herein.
摘要翻译：本文描述了制备利奈唑胺的方法和中间体及其药学上可接受的盐。

55. 发明授权

US06974808B2 CRF receptor antagonists and methods relating thereto 有权
标题翻译： CRF受体拮抗剂及其相关方法
公开(公告)号：US06974808B2
公开(公告)日：2005-12-13
申请号：US09995159
申请日：2001-11-27
申请人： James R. McCarthy
发明人： James R. McCarthy
IPC分类号： A61K31/4184 , A61K31/437 , A61K31/4375 , A61K31/5025 , A61K31/519 , A61K31/53 , A61P1/04 , A61P1/14 , A61P3/04 , A61P9/08 , A61P9/12 , A61P25/22 , A61P25/24 , A61P27/02 , A61P29/00 , C07D235/08 , C07D471/04 , C07D473/00 , C07D487/04
CPC分类号： C07D471/04 , C07D235/08 , C07D473/00 , C07D487/04
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.
摘要翻译：公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。

56. 发明授权

US06531475B1 CRF receptor antagonists and methods relating thereto 有权
标题翻译： CRF受体拮抗剂及其相关方法
公开(公告)号：US06531475B1
公开(公告)日：2003-03-11
申请号：US09574751
申请日：2000-05-18
申请人： Mustapha Haddach , Brian P. Dyck , Charles Q. Huang , Jodie Nelson , Zhiqiang Guo , James R. McCarthy
发明人： Mustapha Haddach , Brian P. Dyck , Charles Q. Huang , Jodie Nelson , Zhiqiang Guo , James R. McCarthy
IPC分类号： C07D47114
CPC分类号： C07D471/16 , C07D487/16
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein n, m, A, B, C, R, R1, R2 and Ar are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same
摘要翻译：公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。本发明的CRF受体拮抗剂具有以下结构：包括立体异构体及其药学上可接受的盐，其中n，m，A，B，C，R，R 1，R 2和Ar如本文所定义。还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法

57. 发明授权

US06482836B1 CRF antagonistic quino- and quinazolines 失效
标题翻译： CRF拮抗喹诺酮和喹唑啉
公开(公告)号：US06482836B1
公开(公告)日：2002-11-19
申请号：US09403393
申请日：1999-10-19
申请人： Charles Huang , Keith M. Wilcoxen , Chen Chen , Mustapha Haddach , James R. McCarthy
发明人： Charles Huang , Keith M. Wilcoxen , Chen Chen , Mustapha Haddach , James R. McCarthy
IPC分类号： A61K314706
CPC分类号： C07D215/233 , C07D215/12 , C07D215/36 , C07D215/42 , C07D239/94 , C07D401/04
摘要： This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR6R7, OR6 or SR7; R2 is hydrogen, C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is Ar1 or Het1; R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R6 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R7 is hydrogen, C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar2CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R6 and R7 taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group, optionally substituted with C1-6alkyl or C1-6alkyloxyC1-6alkyl; and Ar1 and Ar2 are each optionally substituted phenyl; and Het1 is optionally substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).
摘要翻译：本发明涉及包括立体异构体及其药学上可接受的酸加成盐形式的化合物，其中R 1是C 1-6烷基，NR 6 R 7，OR 6或SR 7; R2是氢，C1-6烷基，C1-6烷氧基或C1-6烷硫基; R3是Ar1或Het1; R 4和R 5各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，三氟甲基，氰基，硝基，氨基和单或二（C 1-6烷基）氨基; R6是氢，C1-6烷基，C1-6烷基磺酰基，C1-6烷基亚磺酰基或C1-6烷硫基; R 7是氢，C 1-8烷基，一或二（C 3-6环烷基）甲基，C 3-6环烷基，C 3-6烯基，羟基C 1-6烷基，C 1-6烷基羰氧基-C 1-6烷基或C 1-6烷氧基C 1-6烷基; R 6是C 1-8烷基，单或二（C 3-6环烷基） - 甲基，Ar 2 CH 2，C 1-6烷氧基C 1-6烷基，羟基C 1-6烷基，C 3-6烯基，噻吩基甲基，呋喃基甲基，C 1-6烷硫基C 1-6烷基，单或二 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基，C 1-6烷基羰基C 1-6烷基; 或R6和R7与它们所连接的氮原子一起可以形成任选被C 1-6烷基或C 1-6烷氧基C 1-6烷基取代的吡咯烷基，哌啶基，高哌啶基或吗啉基; Ar 1和Ar 2各自为任意取代的苯基; Het1是任选取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效的治疗来治疗与CRF过度分泌有关的疾病的方法，例如抑郁，焦虑，药物滥用

58. 发明授权

US06469166B2 Thiophenopyrimidines 有权
标题翻译：噻吩并嘧啶
公开(公告)号：US06469166B2
公开(公告)日：2002-10-22
申请号：US09896250
申请日：2001-06-29
申请人： Thomas R. Webb , Chen Chen , James R. McCarthy , Terence J. Moran
发明人： Thomas R. Webb , Chen Chen , James R. McCarthy , Terence J. Moran
IPC分类号： C07D49504
CPC分类号： C07D495/04
摘要： This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein X is S, SO or SO2; R1 is NR4R5 or OR5; R2 is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R4 is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R5 is C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar1CH2, C1-6alkyloxy-C1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of formula -Alk-O—CO-Ar1; or R4 and R5 taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; Ar is phenyl, substituted phenyl, pyridinyl or substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).
摘要翻译：本发明涉及包括立体异构体及其药学上可接受的酸加成盐形式的化合物，其中X是S，SO或SO 2; R1是NR4R5或OR5; R2是C1-6烷基，C1-6烷氧基或C1-6烷硫基; R3是氢，C1-6烷基，C1-6烷基磺酰基，C1-6烷基亚磺酰基或C1-6烷硫基; R4是氢，C1-6烷基，一或二（C3-6环烷基）甲基，C3-6环烷基，C3-6烯基，羟基C1-6烷基，C1-6烷基羰基氧基C 1-6烷基或C 1-6烷氧基C 1-6烷基; R5是C1-6烷基，单或二（C3-6环烷基）甲基，Ar1CH2，C1-6烷氧基-C 1-6烷基，羟基C 1-6烷基，C 3-6烯基，噻吩基甲基，呋喃基甲基，C 1-6烷硫基C 1-6烷基，吗啉基，单或二（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基，C 1-6烷基羰基C 1-6烷基，被咪唑基取代的C 1-6烷基; 或式-Alk-O-CO-Ar1基团; 或R 4和R 5与它们所连接的氮原子一起可以形成任选取代的吡咯烷基，哌啶基，高哌啶基或吗啉基; Ar是苯基，取代的苯基，吡啶基或取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。

59. 发明授权

US06218364B1 Fluorinated neurokinin A antagonists 失效
标题翻译：氟化神经激肽A拮抗剂
公开(公告)号：US06218364B1
公开(公告)日：2001-04-17
申请号：US08638407
申请日：1996-04-26
申请人： Scott L. Harbeson , James R. McCarthy
发明人： Scott L. Harbeson , James R. McCarthy
IPC分类号： A61K3800
CPC分类号： C07K5/0207 , A61K38/00 , C07K5/0212 , C07K7/22 , Y10S514/803
摘要： Peptide derivatives which are antagonists of neurokinin A. The derivatives have a modified peptide bond having a reduced amide and a fluorinated alkyl attached to the nitrogen atom of the modified peptide bond. For example, Asp-Ser-Phe-Val-Gly-Leu&PSgr;[CH2N(CH2CF3)]Leu(NH2).
摘要翻译：作为神经激肽A拮抗剂的肽衍生物。该衍生物具有修饰的肽键，其具有还原的酰胺和与修饰的肽键的氮原子连接的氟化烷基。例如，Asp-Ser-Phe-Val-Gly-Leu＆PSgr; [CH2N（CH2CF3）] Leu（NH2）。

60. 发明授权

US5607925A Treatment of carcinoma by administration of 2'-halomethylidenyl-2'-deoxynucleosides 失效
标题翻译：通过给予2'-卤代亚甲基-2'-脱氧核苷治疗癌症
公开(公告)号：US5607925A
公开(公告)日：1997-03-04
申请号：US333017
申请日：1994-11-01
申请人： Donald P. Matthews , Alan J. Bitonti , Michael L. Edwards , James R. McCarthy
发明人： Donald P. Matthews , Alan J. Bitonti , Michael L. Edwards , James R. McCarthy
IPC分类号： C07H19/06 , C07H19/16 , A61K31/70
CPC分类号： C07H19/06 , C07H19/16
摘要： This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
摘要翻译：本发明涉及某些新的2'-卤代亚甲基，2'-亚乙基和2'-乙炔基胞苷，尿苷和鸟苷衍生物及其组合物，其可用于治疗患有肿瘤或病毒疾病状态的患者。

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