公开(公告)号：US07612075B2

公开(公告)日：2009-11-03

申请号：US10628093

申请日：2003-07-25

Applicant: William R. Ewing ,  Michael R. Becker ,  Yong Mi Choi-Sledeski ,  Heinz W. Pauls ,  Wei He ,  Stephen M. Condon ,  Roderick S. Davis ,  Barbara A. Hanney ,  Alfred P. Spada ,  Christopher J. Burns ,  John Z. Jiang ,  Michael R. Myers ,  Wan F. Lau ,  Aiwen Li ,  Gregory B. Poli ,  Mark A. Bobko ,  Robert L. Morris ,  Joseph M. Karpinski ,  Timothy F. Gallagher ,  Kent W. Neuenschwander ,  Robert D. Groneberg ,  Jean-Francois Sabuco

Inventor： William R. Ewing ,  Michael R. Becker ,  Yong Mi Choi-Sledeski ,  Heinz W. Pauls ,  Wei He ,  Stephen M. Condon ,  Roderick S. Davis ,  Barbara A. Hanney ,  Alfred P. Spada ,  Christopher J. Burns ,  John Z. Jiang ,  Michael R. Myers ,  Wan F. Lau ,  Aiwen Li ,  Gregory B. Poli ,  Mark A. Bobko ,  Robert L. Morris ,  Joseph M. Karpinski ,  Timothy F. Gallagher ,  Kent W. Neuenschwander ,  Robert D. Groneberg ,  Jean-Francois Sabuco

IPC: A61K31/497 ,  C07D401/06

CPC classification number: C07D471/04 ,  C07D241/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D495/04

Abstract: This invention is directed to oxoazaheterocycyl compounds which inhibit Factor Xa, to oxoazaheterocycyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa.

Abstract translation: 本发明涉及将因子Xa，抑制因子Xa和因子IIa的含氮杂环化合物，包含这些化合物的药物组合物，可用于制备这些化合物的中间体，抑制因子Xa和直接抑制因子Xa的方法的含氮杂环化合物 同时直接抑制因子Xa和因子IIa的方法。

公开(公告)号：US06361773B1

公开(公告)日：2002-03-26

申请号：US08943353

申请日：1997-10-01

Applicant: John C. Lee ,  Jerry L. Adams ,  Timothy F. Gallagher ,  David W. Green ,  John Richard Heys ,  Peter C. McDonnell ,  Dean E. McNulty ,  Peter R. Young ,  James E. Strickler

Inventor： John C. Lee ,  Jerry L. Adams ,  Timothy F. Gallagher ,  David W. Green ,  John Richard Heys ,  Peter C. McDonnell ,  Dean E. McNulty ,  Peter R. Young ,  James E. Strickler

IPC: A61K39395

CPC classification number: C07K14/705 ,  A61K38/00 ,  C07K14/47 ,  C12N9/12

Abstract: This invention relates to drug binding proteins, to genes encoding same and to assays and methods for screening pharmaceuticals. More specifically, this invention relates to a Cytokine Suppressive Anti-Inflammatory Drug (CSAID) binding protein, to a gene encoding same and to assays and screens useful in the evaluation and characterization of drugs of this pharmacologic class.

Abstract translation: 本发明涉及药物结合蛋白，与编码该基因的基因以及用于筛选药物的测定和方法。 更具体地，本发明涉及细胞因子抑制性抗炎药（CSAID）结合蛋白，涉及编码该基因的基因以及可用于该药理学类药物的评估和表征的测定和筛选。

公开(公告)号：US5777097A

公开(公告)日：1998-07-07

申请号：US469421

申请日：1995-06-06

Applicant: John C. Lee ,  Jerry L. Adams ,  Timothy F. Gallagher ,  David W. Green ,  John Richard Heys ,  Peter C. McDonnell ,  Dean E. McNulty ,  Peter R. Young ,  James E. Strickler

Inventor： John C. Lee ,  Jerry L. Adams ,  Timothy F. Gallagher ,  David W. Green ,  John Richard Heys ,  Peter C. McDonnell ,  Dean E. McNulty ,  Peter R. Young ,  James E. Strickler

IPC: A01K67/027 ,  A61K38/00 ,  A61K39/395 ,  A61K48/00 ,  A61P29/00 ,  C07H21/04 ,  C07K14/47 ,  C07K14/705 ,  C07K14/715 ,  C07K16/24 ,  C12N1/19 ,  C12N1/21 ,  C12N9/12 ,  C12N15/09 ,  C12N15/12 ,  C12P21/02 ,  C12P21/08 ,  C12Q1/00 ,  C12Q1/68 ,  C12R1/19 ,  C12R1/865 ,  G01N33/53 ,  G01N33/566

CPC classification number: C07K14/705 ,  C07K14/47 ,  C12N9/12 ,  C12Q1/6876 ,  A61K38/00 ,  C12Q2600/136

Abstract: This invention relates to drug binding proteins, to genes encoding same and to assays and methods for screening pharmaceuticals. More specifically, this invention relates to a Cytokine Suppressive Anti-Inflammatory Drug (CSAID) binding protein, to a gene encoding same and to assays and screens useful in the evaluation and characterization of drugs of this pharmacologic class.

Abstract translation: 本发明涉及药物结合蛋白，与编码该基因的基因以及用于筛选药物的测定和方法。 更具体地，本发明涉及细胞因子抑制性抗炎药（CSAID）结合蛋白，涉及编码该基因的基因以及可用于该药理学类药物的评估和表征的测定和筛选。

公开(公告)号：US5023250A

公开(公告)日：1991-06-11

申请号：US398206

申请日：1989-08-24

Applicant: Jerry L. Adams ,  Timothy F. Gallagher ,  Ruth J. Mayer ,  Brian W. Metcalf

Inventor： Jerry L. Adams ,  Timothy F. Gallagher ,  Ruth J. Mayer ,  Brian W. Metcalf

IPC: C07J9/00 ,  C07J31/00 ,  C07J41/00 ,  C07J51/00

CPC classification number: C07J51/00 ,  C07J31/006 ,  C07J41/0094 ,  C07J9/00

Abstract: New 14.alpha.-carboxyalkyl sterols are regulators of HMG-CoA reductase and inhibitors of mammalian 14.alpha.-methyl demethylase and are useful in lowering serum cholesterol levels and treating fungal infections.

Abstract translation: 新的14α-羧甲基甾醇是HMG-CoA还原酶的调节剂和哺乳动物14α-甲基脱甲基酶的抑制剂，并且可用于降低血清胆固醇水平和治疗真菌感染。

公开(公告)号：US4663344A

公开(公告)日：1987-05-05

申请号：US710727

申请日：1985-03-11

Applicant: Philippe L. Durette ,  Bruce E. Witzel ,  Kathleen M. Rupprecht ,  Allan N. Tischler ,  Timothy F. Gallagher

Inventor： Philippe L. Durette ,  Bruce E. Witzel ,  Kathleen M. Rupprecht ,  Allan N. Tischler ,  Timothy F. Gallagher

IPC: C07D333/64 ,  C07D409/04 ,  C07D409/12 ,  A61K31/38 ,  A61K31/415

CPC classification number: C07D409/04 ,  C07D333/64 ,  C07D409/12

Abstract: 3-Hydroxybenzo[b]thiophene derivatives, such as 2-aralkyl, 2-alkyl and 2-alkenyl-3-hydroxybenzo[b]-thiophenes, were prepared by, among other methods, ring closure of 2-(2-carboxy-phenylthio)-.alpha.-substituted acetic acids. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory diseases and other prostaglandin and/or leukotriene mediated diseases.

Abstract translation: 3-羟基苯并[b]噻吩衍生物，例如2-芳烷基，2-烷基和2-烯基-3-羟基苯并[b]噻吩，通过其它方法制备2-（2-羧基 - 苯硫基）-α-取代的乙酸。 发现这些化合物可用于治疗疼痛，发热，炎症，关节炎病症，哮喘，过敏性疾病，皮肤疾病，心血管疾病，牛皮癣，炎性疾病和其他前列腺素和/或白三烯介导的疾病。

公开(公告)号：US07091204B2

公开(公告)日：2006-08-15

申请号：US10477067

申请日：2002-05-07

Applicant: Dashyant Dhanak ,  Timothy F. Gallagher ,  Steven D. Knight

Inventor： Dashyant Dhanak ,  Timothy F. Gallagher ,  Steven D. Knight

IPC: A61K31/404 ,  A61K31/495 ,  C07D239/02 ,  C07D207/04

CPC classification number: C07D207/12 ,  C07D333/34 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

Abstract translation: 本发明涉及磺酰胺，含有它们的药物组合物，以及它们作为尿素调节素II拮抗剂的用途。

公开(公告)号：US06849635B2

公开(公告)日：2005-02-01

申请号：US10477053

申请日：2002-05-07

Applicant: Dashyant Dhanak ,  Timothy F. Gallagher ,  Steven D. Knight ,  Stanley J. Schmidt

Inventor： Dashyant Dhanak ,  Timothy F. Gallagher ,  Steven D. Knight ,  Stanley J. Schmidt

IPC: C07D317/50 ,  A61K31/18 ,  A61K31/277 ,  A61K31/36 ,  A61K31/381 ,  A61K31/506 ,  A61P1/00 ,  A61P1/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P11/00 ,  A61P11/06 ,  A61P13/00 ,  A61P13/12 ,  A61P15/00 ,  A61P15/10 ,  A61P19/00 ,  A61P19/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P31/04 ,  A61P43/00 ,  C07C311/14 ,  C07C311/21 ,  C07C311/29 ,  C07D333/34 ,  C07D409/04 ,  A61K31/275 ,  A61K31/38

CPC classification number: C07D409/04 ,  C07C311/14 ,  C07C311/29 ,  C07D333/34

Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

Abstract translation: 本发明涉及磺酰胺，含有它们的药物组合物，以及它们作为尿素调节素II的拮抗剂的用途。

公开(公告)号：US06541505B1

公开(公告)日：2003-04-01

申请号：US09609103

申请日：2000-06-30

Applicant: William P. Dankulich ,  Daniel G. McGarry ,  Christopher Burns ,  Timothy F. Gallagher ,  Francis A. Volz

Inventor： William P. Dankulich ,  Daniel G. McGarry ,  Christopher Burns ,  Timothy F. Gallagher ,  Francis A. Volz

IPC: A61K31405

CPC classification number: C07D231/12 ,  C07D209/42 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.

Abstract translation: 本发明涉及式I的（氨基亚氨基甲基或氨基甲基）苯并杂芳基化合物，其可用于通过将所述化合物与含有因子Xa的组合物组合来抑制因子Xa的活性。 本发明还涉及包含式I化合物的组合物，其制备方法，其用途，例如抑制凝血酶的形成或用于治疗患有或与生理学相关的疾病状态患者或受其影响的患者 有害的过量凝血酶。

公开(公告)号：US4760086A

公开(公告)日：1988-07-26

申请号：US705115

申请日：1985-02-27

Applicant: Allan N. Tischler ,  Bruce E. Witzel ,  Philippe L. Durette ,  Kathleen M. Rupprecht ,  Timothy F. Gallagher ,  Debra L. Allison ,  Marvin M. Goldenberg

Inventor： Allan N. Tischler ,  Bruce E. Witzel ,  Philippe L. Durette ,  Kathleen M. Rupprecht ,  Timothy F. Gallagher ,  Debra L. Allison ,  Marvin M. Goldenberg

IPC: C07C63/70 ,  C07D303/04 ,  C07D333/70 ,  C07D409/12 ,  A61K31/38 ,  C07D333/62

CPC classification number: C07D409/12 ,  A61K9/0048 ,  A61K9/0051 ,  C07C247/00 ,  C07D303/04 ,  C07D333/70

Abstract: N-Alkenyl-3-hydroxybenzo[b]thiophene-2-carboxamide derivatives have been prepared by:(1) treating a substituted 2-halobenzoate with thioacetamide followed by N-alkenylation with appropriate agents, such as aldehydes, ketones, enol ethers, epoxides, acetals or ketals;(2) treating a substituted thiosalicylate with an appropriately substituted haloacetamide, followed by dehydration; and(3) further synthetic modification of compounds prepared above.These compounds have been found to be effective inhibitors of both cyclooxygenase and lipoxygenase and thereby useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases, cardiovascular disorders, psoriasis, inflammatory bowel disease, glaucoma or other prostaglandins and/or leukotriene mediated diseases. Furthermore, these compounds have been found to exhibit cytoprotective activity which does not involve the inhibition of gastric acid secretion but can be used at relatively low dosages for increasing the resistance of gastro-intestinal mucosa to strong irritants.

Abstract translation: N-烯基-3-羟基苯并[b]噻吩-2-甲酰胺衍生物通过以下方法制备：（1）用硫代乙酰胺处理取代的2-卤代苯甲酸，然后用合适的试剂如醛，酮，烯醇醚， 环氧化物，缩醛或缩酮; （2）用适当取代的卤代乙酰胺处理取代的硫代水杨酸酯，然后脱水; 和（3）进一步合成上述制备的化合物。 已经发现这些化合物是环加氧酶和脂氧合酶的有效抑制剂，从而可用于治疗疼痛，发热，炎症，关节炎状况，哮喘，过敏性疾病，皮肤疾病，心血管疾病，牛皮癣，炎性肠病，青光眼或其他 前列腺素和/或白三烯介导的疾病。 此外，已经发现这些化合物具有不涉及抑制胃酸分泌的细胞保护活性，但可以以相对低的剂量使用以增加胃肠粘膜对强烈刺激物的抵抗力。

公开(公告)号：US4515722A

公开(公告)日：1985-05-07

申请号：US362632

申请日：1982-03-30

Applicant: Shu S. Yang ,  Thomas R. Beattie ,  Philippe L. Durette ,  Timothy F. Gallagher ,  Tsung-Ying Shen

Inventor： Shu S. Yang ,  Thomas R. Beattie ,  Philippe L. Durette ,  Timothy F. Gallagher ,  Tsung-Ying Shen

IPC: C07C43/192 ,  C07C43/196 ,  C07D493/10 ,  C07F9/117 ,  C07F9/40 ,  C07H15/18 ,  C07F9/10 ,  A61K31/66 ,  C07F9/08 ,  C07F9/113

CPC classification number: C07D493/10 ,  C07C43/192 ,  C07C43/196 ,  C07F9/117 ,  C07F9/4081 ,  C07H15/18 ,  Y02P20/55

Abstract: Phosphatidyl inositol analogs are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These phosphatidyl inositol analogs are prepared by condensation of a protected inositol with a substituted phosphonic or phosphorous acid followed by removal of protecting groups.

Abstract translation: 磷脂酰肌醇类似物被发现是有效的磷脂酶C抑制剂，从而有效的抗炎和止痛剂。 这些磷脂酰肌醇类似物通过将保护的肌醇与取代的膦酸或亚磷酸缩合，然后除去保护基来制备。