公开(公告)号：US20100004455A1

公开(公告)日：2010-01-07

申请号：US12311315

申请日：2007-10-10

Applicant: Hirohito Oooka ,  Yasushi Shibata ,  Hiroki Inoue ,  Tsutomu Imagawa

Inventor： Hirohito Oooka ,  Yasushi Shibata ,  Hiroki Inoue ,  Tsutomu Imagawa

IPC: C07D221/02

CPC classification number: C07D221/22 ,  C07D221/24 ,  C07D491/113

Abstract: Provided is a method for producing a piperidin-4-one derivative useful as an intermediate for agricultural chemicals or pharmaceutical products. A piperidin-4-one derivative represented by formula (III-a) or formula (III-b) is produced by reacting a cyclic bis(aminol)ether compound represented by formula (I) and an acetone derivative represented by formula (II) in the presence of at least one substance selected from the group consisting of protonic acids, Lewis acids, acid halides and dialkyl sulfuric acids.

Abstract translation: 提供可用作农药或药品的中间体的哌啶-4-酮衍生物的制造方法。 由式（I-a）或式（III-b）表示的哌啶-4-酮衍生物通过式（I）表示的环状双（氨基醇）醚化合物与由式（II）表示的丙酮衍生物反应制备， 在至少一种选自质子酸，路易斯酸，酰卤和二烷基硫酸的物质存在下进行。

公开(公告)号：US20090264418A1

公开(公告)日：2009-10-22

申请号：US12493516

申请日：2009-06-29

Applicant: Matthias Nettekoven ,  Jean-Marc Plancher ,  Hans Richter ,  Olivier Roche ,  Sven Taylor

Inventor： Matthias Nettekoven ,  Jean-Marc Plancher ,  Hans Richter ,  Olivier Roche ,  Sven Taylor

IPC: A61K31/551 ,  C07D417/14 ,  A61K31/541 ,  C07D403/14 ,  A61K31/496 ,  C07D401/14 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/4545 ,  C07D243/08 ,  A61P3/04 ,  A61P25/00

CPC classification number: C07D401/06 ,  C07D209/42 ,  C07D401/14 ,  C07D403/06 ,  C07D405/12 ,  C07D487/04 ,  C07D491/113

Abstract: The present invention relates to compounds of formula I wherein G and R1 to R5 and R12 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

Abstract translation: 本发明涉及式I化合物，其中G和R 1至R 5和R 12如说明书和权利要求书中所定义，及其药学上可接受的盐。 该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

公开(公告)号：US20090054402A1

公开(公告)日：2009-02-26

申请号：US12104294

申请日：2008-04-16

Applicant: Xilu Wang ,  Xiaohong Song ,  Steven W. Elmore ,  Milan Bruncko ,  David J. Madar ,  Andrew J. Souers ,  Lisa A. Hasvold ,  Le Wang ,  Zhi-Fu Tao ,  Aaron R. Kunzer

Inventor： Xilu Wang ,  Xiaohong Song ,  Steven W. Elmore ,  Milan Bruncko ,  David J. Madar ,  Andrew J. Souers ,  Lisa A. Hasvold ,  Le Wang ,  Zhi-Fu Tao ,  Aaron R. Kunzer

IPC: A61K31/55 ,  C07D209/04 ,  A61K31/404 ,  C07D413/02 ,  A61K31/5377 ,  C07D401/02 ,  A61K31/4439 ,  C07D215/00 ,  A61K31/4709 ,  C07D403/02 ,  A61K31/496 ,  C07D413/14 ,  C07D265/36 ,  A61K31/538 ,  A61K31/517 ,  C07D417/02 ,  A61K31/541 ,  C07D223/16 ,  A61P43/00

CPC classification number: C07D209/42 ,  A61K31/5377 ,  C07D209/34 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D491/113

Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.

Abstract translation: 公开了抑制抗凋亡Mcl-1蛋白活性的化合物，含有该化合物的组合物，以及治疗涉及过表达或未调节的Mcl-1蛋白的疾病的方法。

公开(公告)号：US20090022689A1

公开(公告)日：2009-01-22

申请号：US12169906

申请日：2008-07-09

Applicant: Yat Sun Or ,  Lu Ying ,  Ce Wang ,  Yao-Ling Qiu

Inventor： Yat Sun Or ,  Lu Ying ,  Ce Wang ,  Yao-Ling Qiu

IPC: A61K31/407 ,  A61P31/12 ,  A61K38/21 ,  A61K39/00 ,  C07D491/20 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/422 ,  A61K31/4155

CPC classification number: C07D491/107 ,  A61K31/407 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K45/06 ,  C07D487/10 ,  C07D491/113 ,  C07D497/10 ,  C07D498/10 ,  A61K2300/00

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.

Abstract translation: 本发明公开了式（I）化合物或其药学上可接受的盐，酯或前药：其抑制含RNA病毒，特别是丙型肝炎病毒（HCV）。 因此，本发明的化合物干扰丙型肝炎病毒的生命周期，也可用作抗病毒剂。 本发明还涉及药物组合物，其包含用于给患有HCV感染的受试者施用的上述化合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的HCV感染的方法。 本发明涉及上文所示的新的抗病毒化合物，包含这些化合物的药物组合物，以及用于治疗或预防需要用所述化合物治疗的受试者中的病毒（特别是HCV）感染的方法。

公开(公告)号：US20080119460A1

公开(公告)日：2008-05-22

申请号：US11938514

申请日：2007-11-12

Applicant: Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

Inventor： Pier Giovanni Baraldi ,  Allan R. Moorman ,  Romeo Romagnoli

IPC: A61K31/551 ,  C07D333/20 ,  A61K31/381 ,  C07D403/06 ,  A61P25/02 ,  A61P9/00 ,  A61P25/00 ,  A61K31/496 ,  C07D491/113 ,  A61K31/438

CPC classification number: C07D491/113 ,  C07D333/36 ,  C07D409/06 ,  C07D409/12 ,  C07D487/10

Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.

公开(公告)号：US20080027058A1

公开(公告)日：2008-01-31

申请号：US11630224

申请日：2005-06-27

Applicant: Paul Coleman ,  Christopher Cox ,  Mark Fraley ,  George Hartman ,  John Schreier

Inventor： Paul Coleman ,  Christopher Cox ,  Mark Fraley ,  George Hartman ,  John Schreier

IPC: A61K31/4155 ,  A61K31/454 ,  A61K31/496 ,  A61P35/00 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06

CPC classification number: C07D231/12 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D487/08 ,  C07D491/107 ,  C07D491/113

Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

公开(公告)号：US20080027049A1

公开(公告)日：2008-01-31

申请号：US11828457

申请日：2007-07-26

Applicant: Gregory S. WELMAKER ,  Matthew A. WILSON ,  Geraldine R. McFARLANE ,  Joan E. SABALSKI ,  John A. BUTERA ,  Eugene J. Trybulski ,  David R. HERBST

Inventor： Gregory S. WELMAKER ,  Matthew A. WILSON ,  Geraldine R. McFARLANE ,  Joan E. SABALSKI ,  John A. BUTERA ,  Eugene J. Trybulski ,  David R. HERBST

IPC: A61K31/343 ,  A61K31/443 ,  A61K31/496 ,  A61K31/5377 ,  A61P1/00 ,  A61P25/00 ,  A61P3/00 ,  A61P9/00 ,  C07D307/91 ,  C07D405/12 ,  C07D411/12 ,  C07D491/107

CPC classification number: C07D307/91 ,  C07D307/93 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D491/113

Abstract: The present invention is directed to compounds of Formula I: that are potassium channel modulators and pharmaceutical compositions thereof. The present invention is further directed to methods of treatment using the compounds and pharmaceutical compositions of the invention. The present invention is still further directed to synthetic processes for producing the compounds of the invention.

Abstract translation: 本发明涉及式I化合物：其是钾通道调节剂及其药物组合物。 本发明还涉及使用本发明的化合物和药物组合物的治疗方法。 本发明还涉及用于制备本发明化合物的合成方法。

公开(公告)号：US07189854B2

公开(公告)日：2007-03-13

申请号：US11138793

申请日：2005-05-26

Applicant: Jagabandhu Das ,  Ping Chen ,  Derek J. Norris

Inventor： Jagabandhu Das ,  Ping Chen ,  Derek J. Norris

IPC: C07D401/00 ,  C07D233/44

CPC classification number: C07D277/56 ,  C07C233/65 ,  C07C237/40 ,  C07D213/81 ,  C07D213/82 ,  C07D231/38 ,  C07D233/90 ,  C07D239/42 ,  C07D263/48 ,  C07D409/12 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/113

Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.

Abstract translation: 新的环状化合物及其盐，含有这些化合物的药物组合物，以及使用这些化合物治疗蛋白质酪氨酸激酶相关疾病如免疫学和肿瘤学疾病的方法。

公开(公告)号：US07153856B2

公开(公告)日：2006-12-26

申请号：US11138942

申请日：2005-05-26

Applicant: Joel C. Barrish ,  John Wityak ,  Jagabandhu Das ,  Ping Chen ,  Derek J. Norris ,  Gary Schieven

Inventor： Joel C. Barrish ,  John Wityak ,  Jagabandhu Das ,  Ping Chen ,  Derek J. Norris ,  Gary Schieven

IPC: A61K31/497 ,  C07D241/02

CPC classification number: C07D277/56 ,  C07C233/65 ,  C07C237/40 ,  C07D213/81 ,  C07D213/82 ,  C07D231/38 ,  C07D233/90 ,  C07D239/42 ,  C07D263/48 ,  C07D409/12 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/113

Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.

公开(公告)号：US20060247300A1

公开(公告)日：2006-11-02

申请号：US11394388

申请日：2006-03-30

Applicant: Gregory Beatch ,  Bertrand Plouvier ,  Tao Sheng ,  Michael Walker ,  Richard Wall ,  Sandro Yong ,  Jeff Zhu ,  Alexander Zolotoy

Inventor： Gregory Beatch ,  Bertrand Plouvier ,  Tao Sheng ,  Michael Walker ,  Richard Wall ,  Sandro Yong ,  Jeff Zhu ,  Alexander Zolotoy

IPC: A61K31/4015 ,  C07D207/02

CPC classification number: C07D207/12 ,  C07D207/08 ,  C07D207/10 ,  C07D207/20 ,  C07D207/24 ,  C07D277/04 ,  C07D295/096 ,  C07D333/56 ,  C07D405/12 ,  C07D487/12 ,  C07D491/10 ,  C07D491/113

Abstract: Aminocyclohexyl ether compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses uses for the compounds and compositions, including the treatment of arrhythmia.

Abstract translation: 公开了氨基环己基醚化合物。 本发明的化合物可以掺入组合物和试剂盒中。 本发明还公开了化合物和组合物的用途，包括治疗心律失常。