公开(公告)号：US5300514A

公开(公告)日：1994-04-05

申请号：US33737

申请日：1993-03-18

Applicant: Raymond F. Brown ,  J. Jeffry Howbert ,  Karen L. Lobb ,  David A. Neel ,  Jon K. Reel ,  Beverley Greenwood

Inventor： Raymond F. Brown ,  J. Jeffry Howbert ,  Karen L. Lobb ,  David A. Neel ,  Jon K. Reel ,  Beverley Greenwood

IPC: C07D231/08 ,  C07D233/54 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D413/04 ,  C07D417/04 ,  A61K31/415

CPC classification number: C07D401/04 ,  C07D231/08 ,  C07D401/06 ,  C07D403/06 ,  C07D413/04 ,  C07D417/04

Abstract: Novel substituted pyrazolidinones have been found to exhibit significant binding to cholecystokinin (CCK) receptors and gastrin receptors in the brain and/or peripheral sites such as the pancreas, stomach, and ileum. The pyrazolidinones are CCK and gastrin receptor antagonists and find therapeutic application in the treatment of gastrointestinal disorders, central nervous system disorders and for appetite regulation in warm-blood vertebrates. Pharmaceutical formulations for such indications are described.

Abstract translation: 已经发现新的取代的吡唑烷酮在脑和/或外周位点如胰腺，胃和回肠中表现出与胆囊收缩素（CCK）受体和胃泌素受体的显着结合。 吡唑烷酮是CCK和胃泌素受体拮抗剂，可用于治疗胃肠道疾病，中枢神经系统疾病和用于温血脊椎动物食欲调节的治疗应用。 描述了用于这种适应症的药物制剂。

公开(公告)号：US5216026A

公开(公告)日：1993-06-01

申请号：US554218

申请日：1990-07-17

Applicant: J. Jeffry Howbert

Inventor： J. Jeffry Howbert

IPC: A61K31/18 ,  A61K31/64 ,  A61P35/00 ,  C07C311/55 ,  C07C311/56 ,  C07C323/67

CPC classification number: A61K31/64 ,  C07C311/55 ,  C07C311/56 ,  C07C323/67 ,  C07C2101/08 ,  C07C2101/14

Abstract: A method is provided for treating a susceptible neoplasm in mammals which comprises administering to a mammal in need of said treatment an effective amount for treating the neoplasm of the compound N-[[(4-chlorophenyl)amino]carbonyl]-1-butanesulfonamide or a pharmaceutically acceptable salt thereof, wherein said neoplasm is selected from the group consisting of ovarian, non-small cell lung, gastric, pancreatic, renal cell, breast, colorectal, small-cell lung, melanoma, head and neck, Kaposi's sarcoma, and rhabdomyosarcoma.

公开(公告)号：US08242106B2

公开(公告)日：2012-08-14

申请号：US12533596

申请日：2009-07-31

Applicant: J. Jeffry Howbert ,  Muralikrishna Duvvuri ,  Robert Hershberg ,  Gregory Dietsch

Inventor： J. Jeffry Howbert ,  Muralikrishna Duvvuri ,  Robert Hershberg ,  Gregory Dietsch

IPC: A61K31/55 ,  C07D223/16

CPC classification number: A61K31/55 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/19 ,  A61K31/724 ,  A61K47/40 ,  A61K47/48969 ,  A61K47/6951 ,  B82Y5/00 ,  C07D223/16 ,  C08B37/0012 ,  Y02A50/393

Abstract: The present invention is directed generally to stable formulations of a TLR agonist preferably a TLR7 or a TLR8 agonist, for use in the treatment of cancer, preferably solid tumors and lymphomas. Specifically, the present invention is directed to stable formulations of up to 50 mg/ml of a TLR agonist which comprise a cyclodextrin.

Abstract translation: 本发明一般涉及用于治疗癌症，优选实体瘤和淋巴瘤的TLR激动剂优选TLR7或TLR8激动剂的稳定制剂。 具体地，本发明涉及高达50mg / ml的包含环糊精的TLR激动剂的稳定制剂。

公开(公告)号：US07052846B2

公开(公告)日：2006-05-30

申请号：US10465524

申请日：2003-06-19

Applicant: Jeffrey Van Ness ,  John C Tabone ,  J Jeffry Howbert ,  John T Mulligan

Inventor： Jeffrey Van Ness ,  John C Tabone ,  J Jeffry Howbert ,  John T Mulligan

IPC: C12Q1/68 ,  C12P19/34 ,  C07H21/00 ,  C07H21/02

CPC classification number: C07H21/00 ,  C07B2200/11 ,  C12Q1/6825 ,  C12Q1/6846 ,  C12Q1/6872 ,  C40B40/00 ,  C12Q2563/149 ,  C12Q2563/113 ,  C12Q2563/167 ,  C12Q2525/191

Abstract: Tags and linkers specifically designed for a wide variety of nucleic acid reactions are disclosed, which are suitable for a wide variety of nucleic acid reactions wherein separation of nucleic acid molecules based upon size is required.

公开(公告)号：US06815212B2

公开(公告)日：2004-11-09

申请号：US10000467

申请日：2001-10-24

Applicant: Jeffrey Van Ness ,  John C. Tabone ,  J. Jeffry Howbert ,  John T. Mulligan

Inventor： Jeffrey Van Ness ,  John C. Tabone ,  J. Jeffry Howbert ,  John T. Mulligan

IPC: G01N2400

CPC classification number: C12Q1/6872 ,  Y10T436/24 ,  C12Q2563/167

Abstract: Methods are provided for detecting the binding of a first member to a second member of a ligand pair, comprising the steps of (a) combining a set of first tagged members with a biological sample which may contain one or more second members, under conditions, and for a time sufficient to permit binding of a first member to a second member, wherein said tag is correlative with a particular first member and detectable by non-fluorescent spectrometry, or potentiometry, (b) separating bound first and second members from unbound members, (c) cleaving the tag from the tagged first member, and (d) detecting the tag by non-fluorescent spectrometry, or potentiometry, and therefrom detecting the binding of the first member to the second member.

公开(公告)号：US06403577B1

公开(公告)日：2002-06-11

申请号：US08153847

申请日：1993-11-17

Applicant: Sung Y. Cho ,  Thomas A. Crowell ,  Bruce D. Gitter ,  Philip A. Hipskind ,  J. Jeffry Howbert ,  Joseph H. Krushinski, Jr. ,  Karen L. Lobb ,  Brian S. Muehl ,  James A. Nixon

Inventor： Sung Y. Cho ,  Thomas A. Crowell ,  Bruce D. Gitter ,  Philip A. Hipskind ,  J. Jeffry Howbert ,  Joseph H. Krushinski, Jr. ,  Karen L. Lobb ,  Brian S. Muehl ,  James A. Nixon

IPC: A61K3155

CPC classification number: C07D401/12 ,  C07C233/44 ,  C07C233/78 ,  C07C271/20 ,  C07D209/14 ,  C07D209/16 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14

Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.

Abstract translation: 本发明提供了一系列非肽基化合物，其可用于治疗或预防与超速激肽相关的生理障碍。 本发明还提供了治疗这些生理障碍的方法以及使用这些新化合物的药物制剂。

公开(公告)号：US6027890A

公开(公告)日：2000-02-22

申请号：US898501

申请日：1997-07-22

Applicant: Jeffrey Van Ness ,  John C. Tabone ,  J. Jeffry Howbert ,  John T. Mulligan

Inventor： Jeffrey Van Ness ,  John C. Tabone ,  J. Jeffry Howbert ,  John T. Mulligan

IPC: A01N43/04 ,  A61K38/00 ,  C07C69/74 ,  C12Q1/68 ,  G01N24/00 ,  G01N33/53 ,  G01N33/542

CPC classification number: C12Q1/6872 ,  Y10T436/24

Abstract: Methods are provided for detecting the binding of a first member to a second member of a ligand pair, comprising the steps of (a) combining a set of first tagged members with a biological sample which may contain one or more second members, under conditions, and for a time sufficient to permit binding of a first member to a second member, wherein said tag is correlative with a particular first member and detectable by non-fluorescent spectrometry, or potentiometry, (b) separating bound first and second members from unbound members, (c) cleaving the tag from the tagged first member, and (d) detecting the tag by non-fluorescent spectrometry, or potentiometry, and therefrom detecting the binding of the first member to the second member.

Abstract translation: 提供了用于检测第一成员与配体对的第二成员的结合的方法，其包括以下步骤：（a）在一些条件下，将一组第一标记成员与可包含一个或多个第二成员的生物样品组合， 并且足以允许第一构件与第二构件结合的时间，其中所述标签与特定第一构件相关并且可通过非荧光光谱法或电位法检测，（b）将结合的第一和第二构件与未结合的成员分离 ，（c）从标记的第一构件切割标签，以及（d）通过非荧光光谱法或电位法检测标签，从而检测第一构件与第二构件的结合。

公开(公告)号：US5663192A

公开(公告)日：1997-09-02

申请号：US326413

申请日：1994-10-20

Applicant: Robert F. Bruns, Jr. ,  Donald R. Gehlert ,  J. Jeffry Howbert ,  William H. W. Lunn

Inventor： Robert F. Bruns, Jr. ,  Donald R. Gehlert ,  J. Jeffry Howbert ,  William H. W. Lunn

IPC: A61K31/138 ,  A61K31/343 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/4453 ,  A61K31/4525 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/55 ,  A61K31/34 ,  A61K31/38

CPC classification number: A61K31/40 ,  A61K31/138 ,  A61K31/343 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/4453 ,  A61K31/4525 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/55

Abstract: This invention provides methods for treating or preventing a condition associated with an excess of neuropeptide Y which methods comprise administration of one or more substituted benzofurans, benzothiophenes or indoles.

Abstract translation: 本发明提供了治疗或预防与过量神经肽Y相关的病症的方法，该方法包括施用一种或多种取代的苯并呋喃，苯并噻吩或吲哚。

公开(公告)号：US5594028A

公开(公告)日：1997-01-14

申请号：US343056

申请日：1994-11-21

Applicant: Richard W. Harper ,  J. Jeffry Howbert ,  Gerald A. Poore ,  Brent J. Rieder ,  Eddie V. P. Tao ,  James A. Aikins

Inventor： Richard W. Harper ,  J. Jeffry Howbert ,  Gerald A. Poore ,  Brent J. Rieder ,  Eddie V. P. Tao ,  James A. Aikins

IPC: C07D209/08 ,  C07D263/56 ,  C07D307/79 ,  C07D311/58 ,  C07D317/62 ,  C07D319/18 ,  C07D333/54 ,  C07D333/72 ,  A61K31/36 ,  A61K31/18 ,  C07C311/16

CPC classification number: C07D263/56 ,  C07D209/08 ,  C07D307/79 ,  C07D311/58 ,  C07D317/62 ,  C07D319/18 ,  C07D333/54 ,  C07D333/72

Abstract: This invention provides certain sulfonamide derivatives, their pharmaceutical formulations, and their use in the treatment of susceptible neoplasms in mammals.

Abstract translation: 本发明提供某些磺酰胺衍生物，其药物制剂及其在哺乳动物易感性肿瘤治疗中的应用。

公开(公告)号：US5576337A

公开(公告)日：1996-11-19

申请号：US517316

申请日：1995-08-21

Applicant: Robert F. Bruns, Jr. ,  Donald R. Gehlert ,  J. Jeffry Howbert ,  William H. W. Lunn

Inventor： Robert F. Bruns, Jr. ,  Donald R. Gehlert ,  J. Jeffry Howbert ,  William H. W. Lunn

IPC: C07D333/56 ,  A61K31/38 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/445 ,  A61K31/4535 ,  A61K31/55 ,  A61P3/06 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  A61K31/40

CPC classification number: A61K31/4535 ,  A61K31/4025 ,  A61K31/55 ,  Y10S514/909

Abstract: A method of inhibiting the physiological disorder anxiety associated with an excess of neuropeptide Y or its symptoms comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

Abstract translation: 一种抑制与过量神经肽Y或其症状相关的生理障碍焦虑症的方法，包括向有需要的人施用有效量的具有式（I）的化合物，其中R 1和R 3独立地为氢， 图像>其中Ar是任选取代的苯基; R2选自吡咯烷，六亚甲基氨基和哌啶子基; 或其药学上可接受的盐的溶剂合物。