公开(公告)号：US20100267709A1

公开(公告)日：2010-10-21

申请号：US12747030

申请日：2008-12-09

Applicant: Jonathan R. Young ,  Jongwon Lim ,  Michelle R. Machacek ,  Brandon Mitsuo Taoka ,  Ryan D. Otte

Inventor： Jonathan R. Young ,  Jongwon Lim ,  Michelle R. Machacek ,  Brandon Mitsuo Taoka ,  Ryan D. Otte

IPC: A61K31/437 ,  C07D471/04 ,  A61K31/506 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/541 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.

Abstract translation: 本发明提供抑制四种已知的哺乳动物JAK激酶（JAK1，JAK2，JAK3和TYK2）和PDK1的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过向需要治疗骨髓增生性疾病或癌症的患者施用化合物来抑制JAK1，JAK2，JAK3 TYK2和PDK1的活性的方法。

公开(公告)号：US20100048551A1

公开(公告)日：2010-02-25

申请号：US12085331

申请日：2006-11-17

Applicant: Jean-Francois Truchon ,  Nicolas Lachance ,  Cheuk Lau ,  Yves Leblanc ,  Christophe Mellon ,  Patrick Roy ,  Elise Isabel ,  Ryan D. Otte ,  Jonathan R. Young

Inventor： Jean-Francois Truchon ,  Nicolas Lachance ,  Cheuk Lau ,  Yves Leblanc ,  Christophe Mellon ,  Patrick Roy ,  Elise Isabel ,  Ryan D. Otte ,  Jonathan R. Young

IPC: A61K31/437 ,  A61K31/5377 ,  A61K31/4365 ,  C07D491/107 ,  C07D495/04 ,  C07D471/04 ,  A61P17/00 ,  A61K31/444 ,  A61P35/00 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P27/02 ,  A61P9/12 ,  A61P9/10 ,  A61P25/00

CPC classification number: C07D491/10 ,  C07D471/04

Abstract: The present invention provides inhibitors of kinases, specifically IκB kinases, JAK1, JAK2, JAK3 and TYK2. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting said kinase activity by administering the compound to a patient in need of treatment for myeloproliferative disorders, cancer or NF-κB-mediated diseases.

Abstract translation: 本发明提供激酶抑制剂，特别是I＆Kgr B激酶，JAK1，JAK2，JAK3和TYK2。 本发明还提供了包含这种抑制性化合物的组合物和通过将该化合物施用于需要治疗骨髓增生性疾病，癌症或NF-和κB介导的疾病的患者来抑制所述激酶活性的方法。

公开(公告)号：US07652058B2

公开(公告)日：2010-01-26

申请号：US11792514

申请日：2005-12-12

Applicant: Robert J. DeVita ,  Jinlong Jiang ,  Sander G. Mills ,  Jonathan R. Young

Inventor： Robert J. DeVita ,  Jinlong Jiang ,  Sander G. Mills ,  Jonathan R. Young

IPC: A61K31/407 ,  C07D491/052

CPC classification number: C07D491/04

Abstract: The present invention is directed to certain hydropyranopyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract translation: 本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的某些氢吡喃并吡咯烷化合物。本发明还涉及包含这些化合物作为活性成分的药物组合物和 使用化合物及其制剂治疗某些疾病，包括呕吐，尿失禁，抑郁和焦虑。

公开(公告)号：US20090131423A1

公开(公告)日：2009-05-21

申请号：US12083746

申请日：2006-10-18

Applicant: Christopher J. Dinsmore ,  Ana Esther Gabarda Ortega ,  Jongwon Lim ,  Michelle R. Machacek ,  Alan B. Northrup ,  Jonathan R. Young

Inventor： Christopher J. Dinsmore ,  Ana Esther Gabarda Ortega ,  Jongwon Lim ,  Michelle R. Machacek ,  Alan B. Northrup ,  Jonathan R. Young

IPC: A61K31/5377 ,  C07D471/04 ,  A61K31/4375 ,  A61K31/496 ,  A61P35/00 ,  C07D401/14 ,  C07D413/14

CPC classification number: C07D471/04

Abstract: The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract translation: 本发明涉及咪唑并[1,2-a]嘧啶衍生物，其可用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病，以及用于抑制受体酪氨酸激酶MET。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

公开(公告)号：US07015235B2

公开(公告)日：2006-03-21

申请号：US10468515

申请日：2002-02-25

Applicant: Mark T. Goulet ,  Ravi P. Nargund ,  Iyassu K. Sebhat ,  Feroze Ujjainwalla ,  Thomas F. Walsh ,  Daniel Warner ,  Zhixiong Ye ,  Jonathan R. Young ,  Raman K. Bakshi

Inventor： Mark T. Goulet ,  Ravi P. Nargund ,  Iyassu K. Sebhat ,  Feroze Ujjainwalla ,  Thomas F. Walsh ,  Daniel Warner ,  Zhixiong Ye ,  Jonathan R. Young ,  Raman K. Bakshi

IPC: A61K31/445 ,  C07D211/06

CPC classification number: C07D491/08 ,  A61K31/445 ,  C07D211/62 ,  C07D211/64 ,  C07D401/06 ,  C07D401/14 ,  C07D413/06 ,  C07D413/14

Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Abstract translation: 某些新的4-取代N-酰化哌啶衍生物是人黑皮质素受体的激动剂，特别是人黑皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的活化反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。

公开(公告)号：US06622933B1

公开(公告)日：2003-09-23

申请号：US09855123

申请日：2001-05-14

Applicant: George A. Young ,  Jonathan R. Young

Inventor： George A. Young ,  Jonathan R. Young

IPC: A01G2502

CPC classification number: A01G25/02 ,  Y10T137/86413 ,  Y10T137/86445

Abstract: A lawn sprinkler system utilizes a master controller whose input is coupled to a water supply and whose output is coupled via pipe to a number of valves. The master controller is preprogrammed to supply water for a number of phases of operation, where the operation advances to a subsequent phase upon turning the supply of water off for a relatively short amount of time followed by turning the supply of water back on. Each of the valves includes an in-port and an out-port, where each valve cycles through each of the phases as controlled by the master controller. Each valve is setable/changeable to supply water to its respective out-port during a selected phase of operation.

Abstract translation: 草坪洒水系统利用主控制器，其输入端与水源相连，其输出通过管道耦合到多个阀门。 主控制器被预编程为多个操作阶段的水供水，其中在相当短的时间内关闭水源后，操作进入后续阶段，然后重新打开供水。 每个阀都包括入口和出口，每个阀循环通过主控制器控制的每个相。 每个阀门可设置/更换，以在选定的操作阶段向其各自的出口供水。

公开(公告)号：US6159975A

公开(公告)日：2000-12-12

申请号：US247240

申请日：1999-02-10

Applicant: Jonathan R. Young ,  Thomas F. Walsh ,  Mark T. Goulet ,  Michael H. Fisher

Inventor： Jonathan R. Young ,  Thomas F. Walsh ,  Mark T. Goulet ,  Michael H. Fisher

IPC: C07D519/00 ,  C07D401/12 ,  A61K31/407 ,  C07D215/06 ,  C07D471/04 ,  C07D487/06

CPC classification number: C07D519/00

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

公开(公告)号：US6110931A

公开(公告)日：2000-08-29

申请号：US276028

申请日：1999-03-25

Applicant: Thomas F. Walsh ,  Mark T. Goulet ,  Feroze Ujjainwalla ,  Jonathan R. Young

Inventor： Thomas F. Walsh ,  Mark T. Goulet ,  Feroze Ujjainwalla ,  Jonathan R. Young

IPC: A61P5/02 ,  C07D519/00 ,  A61K31/437 ,  A61K31/4375 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D519/00

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

公开(公告)号：US20140235641A1

公开(公告)日：2014-08-21

申请号：US14345982

申请日：2012-09-21

Applicant: Jason Brubaker ,  Joshua Close ,  Tony Siu ,  Graham Frank Smith ,  Luis E. Torres ,  Hyun Chong Woo ,  Jonathan R. Young ,  Zhongyong Wei ,  Feng Shi

Inventor： Jason Brubaker ,  Joshua Close ,  Tony Siu ,  Graham Frank Smith ,  Luis E. Torres ,  Hyun Chong Woo ,  Jonathan R. Young ,  Zhongyong Wei ,  Feng Shi

IPC: C07D401/04 ,  C07D405/14 ,  C07D409/04 ,  C07D417/14 ,  C07D405/04 ,  C07D413/14 ,  C07D401/14

CPC classification number: C07D405/08 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

Abstract translation: 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。

公开(公告)号：US08431569B2

公开(公告)日：2013-04-30

申请号：US12747030

申请日：2008-12-09

Applicant: Jonathan R. Young ,  Jongwon Lim ,  Michelle R. Machacek ,  Brandon Mitsuo Taoka ,  Ryan D. Otte

Inventor： Jonathan R. Young ,  Jongwon Lim ,  Michelle R. Machacek ,  Brandon Mitsuo Taoka ,  Ryan D. Otte

IPC: C07D487/02 ,  A61K31/503

CPC classification number: C07D471/04

Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.