公开(公告)号：US4981868A

公开(公告)日：1991-01-01

申请号：US384944

申请日：1989-07-25

申请人： James R. McCarthy ,  Donald P. Matthews ,  Charlotte L. Barney

发明人： James R. McCarthy ,  Donald P. Matthews ,  Charlotte L. Barney

IPC分类号： A61K31/05 ,  A61K31/047 ,  A61K31/085 ,  A61K31/38 ,  A61K31/381 ,  A61P9/12 ,  A61P43/00 ,  C07C17/00 ,  C07C25/24 ,  C07C37/62 ,  C07C39/373 ,  C07C41/22 ,  C07C43/225 ,  C07C391/02 ,  C07D333/12 ,  C07D333/28

CPC分类号： C07C39/373 ,  C07C391/02 ,  C07C43/225 ,  C07D333/28

摘要： This invention relates to novel 3-heteroaryl-2-fluoro-1-olefins and their pharmacological use as dopamine beta-hydroxylase DBH inhibitors in the treatment of DBH mediated conditions such as hypertension.

公开(公告)号：US4496725A

公开(公告)日：1985-01-29

申请号：US496800

申请日：1983-05-23

申请人： James R. McCarthy ,  Paul J. Widner

发明人： James R. McCarthy ,  Paul J. Widner

IPC分类号： A61K31/53 ,  A61P37/08 ,  C07D215/20 ,  C07D215/54 ,  C07D495/04 ,  C07D495/14 ,  C07D495/22 ,  C07D495/12

CPC分类号： C07D495/04 ,  C07D215/20 ,  C07D215/54 ,  C07D495/14

摘要： Substituted 1,2,3-triazino[4',5':4,5]thieno[2,3-b]quinolin-4(3H)-ones useful as antiallergic agents are described herein. The compounds are prepared by the reaction of an appropriate substituted 3-aminothieno[2,3-b]quinoline-2-carboxamide with sodium nitrite in an acid such as acetic acid.

摘要翻译： 本文描述了可用作抗过敏剂的取代的1,2,3-三嗪[4'，5'：4,5]噻吩并[2,3-b]喹啉-4（3H） - 酮。 通过在酸如乙酸中将适当的取代的3-氨基噻吩并[2,3-b]喹啉-2-甲酰胺与亚硝酸钠反应来制备化合物。

公开(公告)号：US4274949A

公开(公告)日：1981-06-23

申请号：US78591

申请日：1979-09-24

申请人： James R. McCarthy

发明人： James R. McCarthy

IPC分类号： B03B7/00 ,  B03D1/14

CPC分类号： B03B7/00 ,  B03D1/1462 ,  B03D1/1481

摘要： A froth separation apparatus is provided having a separation container of generally rectangular form having two spaced generally parallel vertical sides, two generally parallel ends and a bottom, an influent feed delivering a suspension of solids in liquid at spaced points along the top of the separation container, a reagent inlet into the influent feed in advance of the separation container, diagonal froth retention screen means extending across the separation container from end to end and from a line intermediate the top and bottom of one side wall to a line adjacent the bottom of the other side wall, froth creating means in the separation container above said screen means, a weir discharge means on the said other side wall at the bottom thereof adjacent the screen means line for removal of froth and outlet means at the bottom of said one side for tailings discharge.

摘要翻译： 提供了一种泡沫分离装置，其具有大致矩形形式的分离容器，其具有两个间隔开的大致平行的垂直侧面，两个大致平行的端部和底部，流入物料沿着分离容器的顶部的间隔点输送固体在液体中的悬浮液 ，在分离容器之前进入进水进料器的试剂入口，对角起泡保留筛网装置，其从一端到另一端延伸穿过分离容器，并且从一侧壁的顶部和底部延伸到邻近底部的管线 在所述筛网装置上方的分离容器中的另一侧壁，泡沫产生装置，在邻近筛网装置线的底部的所述另一侧壁上的堰排放装置，用于在所述一侧的底部移除泡沫和出口装置， 尾矿排放。

公开(公告)号：US4189444A

公开(公告)日：1980-02-19

申请号：US6143

申请日：1979-01-24

申请人： Albert Schuster ,  James R. McCarthy

发明人： Albert Schuster ,  James R. McCarthy

IPC分类号： C07C119/18

摘要： N,N.fwdarw.-disubstituted 2-naphthaleneethanimidamide is prepared by the conversion of a nitrile into the novel imido ester salt intermediate by alcoholysis followed by treatment of the intermediate with an alkylamine to give the product.

摘要翻译： N，N'-二取代的2-萘甲酰亚胺酰胺是通过醇解将腈转化成新的酰亚胺酯盐中间体，然后用烷基胺处理中间体，得到产物。

公开(公告)号：US4086344A

公开(公告)日：1978-04-25

申请号：US722455

申请日：1976-09-13

申请人： James R. McCarthy ,  Jimmie L. Moore

发明人： James R. McCarthy ,  Jimmie L. Moore

IPC分类号： C07D498/18 ,  A61K31/505

CPC分类号： C07D498/18

摘要： N,15-Didehydro-15-deoxo-3,15-epi(methano(alkylimino))rifamycins which can exist in either the quinone or hydroquinone form, are prepared from the corresponding Mannich base derivatives by an acid-catalyzed dehydration reaction.

摘要翻译： 可以以醌或氢醌形式存在的N，15-二脱氢-15-脱氧-3,15-表（亚甲基（烷基亚氨基））利福霉素由相应的曼尼希碱衍生物通过酸催化脱水反应制备。

公开(公告)号：US20130053557A1

公开(公告)日：2013-02-28

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： C07D413/10 ,  C07C25/13 ,  C07D303/36 ,  C07D265/30 ,  C07D301/24

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。

公开(公告)号：US06610678B2

公开(公告)日：2003-08-26

申请号：US10266662

申请日：2002-10-08

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： A61K3133

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(C3-6cyclo-alkyl)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： 本发明涉及包括其立​​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; 通过施用有效的方法治疗与CRF分泌过高有关的疾病，如抑郁症，焦虑症，药物滥用

公开(公告)号：US06514982B1

公开(公告)日：2003-02-04

申请号：US09439840

申请日：1999-11-12

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： C07D48704

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

公开(公告)号：US6133276A

公开(公告)日：2000-10-17

申请号：US222374

申请日：1998-12-29

申请人： Jeffrey P. Whitten ,  James R. McCarthy ,  Zhengyu Liu ,  Charles Q. Huang ,  Philip E. Erickson ,  Dominic P. Behan

发明人： Jeffrey P. Whitten ,  James R. McCarthy ,  Zhengyu Liu ,  Charles Q. Huang ,  Philip E. Erickson ,  Dominic P. Behan

IPC分类号： A61K31/00 ,  A61K31/35 ,  A61K31/352 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4168 ,  A61K31/42 ,  A61K31/423 ,  A61K31/425 ,  A61K31/428 ,  A61K31/433 ,  A61K31/505 ,  A61K31/513 ,  A61P5/00 ,  A61P43/00 ,  C07D239/62 ,  C07D239/66 ,  C07D311/56 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D473/08 ,  C07D487/04 ,  A61K31/515

CPC分类号： C07D409/14 ,  C07D239/62 ,  C07D239/66 ,  C07D311/56 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D473/08 ,  C07D487/04

摘要： Ligand inhibitors for increasing levels of free corticotropin-releasing factor (CRF) in the brain are disclosed. Such ligand inhibitors cause release of CRF from the CRF/CRF-bind protein complex. Administration of the ligand inhibitors provide improvement in learning and memory, result in decreased food intake and/or provide treatment for diseases associated with low levels of CRF in the brain, notably Alzheimer's disease.

摘要翻译： 公开了用于增加脑中游离促皮质激素释放因子（CRF）水平的配体抑制剂。 这种配体抑制剂引起CRF / CRF结合蛋白复合物的CRF释放。 配体抑制剂的施用提供了学习和记忆的改善，导致食物摄取减少和/或提供与脑中低水平CRF相关疾病，特别是阿尔茨海默氏病的治疗。

公开(公告)号：US5830863A

公开(公告)日：1998-11-03

申请号：US764157

申请日：1996-12-13

申请人： Stephen H. Buck ,  Scott L. Harbeson ,  John L. Krstenansky ,  Chester F. Hassman, III ,  James R. McCarthy

发明人： Stephen H. Buck ,  Scott L. Harbeson ,  John L. Krstenansky ,  Chester F. Hassman, III ,  James R. McCarthy

IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K7/22

CPC分类号： C07K7/22 ,  C07K5/0207 ,  C07K5/0212 ,  A61K38/00 ,  Y10S514/826

摘要： Antagonists of neurokinin A which are derivatives of naturally occurring neurokinin A in which the amide bond connecting the two amino acids on the carboxy terminal end is modified are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.

摘要翻译： 描述了神经激肽A的拮抗剂，其是连接羧基末端上的两个氨基酸的酰胺键被修饰的天然存在的神经激肽A的衍生物。 使用常规竞争性结合和生物化学测定以及常规生理测试证实拮抗作用，并且还描述了在涉及神经激肽A的各种情况下使用这些衍生物。