公开(公告)号：US20130109670A1

公开(公告)日：2013-05-02

申请号：US13718928

申请日：2012-12-18

Applicant: PFIZER INC.

Inventor： Aranapakam Mudumbai VENKATESAN ,  Zecheng CHEN ,  Christoph Martin DEHNHARDT ,  Osvaldo DOS SANTOS ,  Efren Guillermo DELOS SANTOS ,  Arie ZASK ,  Jeroen Cunera VERHEIJEN ,  Joshua Aaron KAPLAN ,  David James RICHARD ,  Semiramis AYRAL-KALOUSTIAN ,  Tarek Suhayl MANSOUR ,  Ariamala GOPALSAMY ,  Kevin Joseph CURRAN ,  Mengxiao SHI

IPC: C07D498/08 ,  C07D491/113 ,  C07D413/14

CPC classification number: C07D401/12 ,  A61K31/5377 ,  A61K45/06 ,  C07D251/18 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  C07D451/06 ,  C07D453/02 ,  C07D491/113 ,  C07D498/08

Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.

公开(公告)号：US20130053386A1

公开(公告)日：2013-02-28

申请号：US13501628

申请日：2010-10-05

Applicant: William Colby Brown ,  Richard W. Heidebrecht ,  Jason Brubaker ,  Christian Fischer ,  John T. Hendrix ,  Elizabeth H. Kelley ,  Rachel N. MacCoss ,  Joey L. Methot ,  Thomas Miller ,  Karin M. Otte ,  Phieng Siliphaivanh ,  Thomas Reger ,  Peter D. Williams ,  Catherine M. Wiscount

Inventor： William Colby Brown ,  Richard W. Heidebrecht ,  Jason Brubaker ,  Christian Fischer ,  John T. Hendrix ,  Elizabeth H. Kelley ,  Rachel N. MacCoss ,  Joey L. Methot ,  Thomas Miller ,  Karin M. Otte ,  Phieng Siliphaivanh ,  Thomas Reger ,  Peter D. Williams ,  Catherine M. Wiscount

IPC: C07D231/20 ,  C07D403/12 ,  A61K31/4155 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/506 ,  C07D401/04 ,  C07D405/12 ,  C07D413/12 ,  A61K31/4245 ,  A61K31/422 ,  A61K31/5377 ,  C07D491/113 ,  A61K31/438 ,  A61K31/496 ,  C07D413/14 ,  A61P25/28 ,  A61K31/415

CPC classification number: C07D231/22 ,  C07D231/20 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D491/113

Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.

Abstract translation: 本发明包括一类新的二芳基醚衍生物，其抑制通过推定的γ-分泌酶处理APP，同时保留Notch信号通路，因此可用于治疗或预防阿尔茨海默病而不发展Notch抑制介导的胃肠道问题。 还包括药物组合物和使用方法。

公开(公告)号：US20120202795A1

公开(公告)日：2012-08-09

申请号：US13449711

申请日：2012-04-18

Applicant: Philip M. WEINTRAUB ,  Paul R. EASTWOOD ,  Shujaath MEHDI ,  David W. STEFANY ,  Kwon Yon MUSICK ,  Neil MOORCROFT ,  Sungtaek LIM ,  John Z. JIANG ,  Hartmut RUTTEN ,  Stefan PEUKERT ,  Uwe SCHWAHN

Inventor： Philip M. WEINTRAUB ,  Paul R. EASTWOOD ,  Shujaath MEHDI ,  David W. STEFANY ,  Kwon Yon MUSICK ,  Neil MOORCROFT ,  Sungtaek LIM ,  John Z. JIANG ,  Hartmut RUTTEN ,  Stefan PEUKERT ,  Uwe SCHWAHN

IPC: A61K31/4412 ,  C07D217/24 ,  C07D413/10 ,  C07D401/10 ,  C07D401/04 ,  C07D413/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D405/14 ,  A61K31/506 ,  C07D491/113 ,  C07D417/14 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/551 ,  A61K31/497 ,  A61P25/00 ,  A61P25/28 ,  A61P9/10 ,  A61P9/00 ,  A61K31/472 ,  A61K31/444 ,  C07D213/64

CPC classification number: C07D213/64 ,  C07D217/24 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/14

Abstract: The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R1, R2, R3 and R4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

Abstract translation: 本发明涉及一系列式I的2,3,5-取代吡啶酮衍生物：其中R，R 1，R 2，R 3和R 4如本文所定义。 本发明还涉及制备这些化合物的方法。 本发明的化合物是聚（腺苷5'-二磷酸核糖）聚合酶（PARP）的抑制剂，因此可用作药剂，特别是用于治疗和/或预防各种疾病，包括与中枢神经相关的疾病 系统和心血管疾病。

公开(公告)号：US20120083557A1

公开(公告)日：2012-04-05

申请号：US13376849

申请日：2010-06-01

Applicant: Kai-Uwe Schoening

Inventor： Kai-Uwe Schoening

IPC: C08K5/3435 ,  C07D401/14 ,  C07D491/22 ,  C07D491/113 ,  C07D498/10 ,  C08L23/06 ,  C07D498/04 ,  C07D487/16 ,  C08K5/3492 ,  C08K5/3467 ,  C08K5/357 ,  C08L23/12 ,  C07D401/12 ,  C07D403/14

CPC classification number: C07D491/113 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D487/16 ,  C07D491/22 ,  C07D498/10 ,  C08K5/3435 ,  C08K5/353 ,  C08K2201/014

Abstract: The instant invention pertains to hindered amine compounds having at least two nitrogen atoms with different basicity. One part is substituted on the N-atom by alkoxy moieties and the other part is substituted on the N-atom by a hydroxy-alkyl moiety. These materials are particularly effective in stabilizing polymers, especially thermoplastic polyolefins, against the deleterious effects of oxidative, thermal and actinic radiation. The compounds are also particularly effective in stabilizing acid catalyzed and ambient cured coatings systems.

Abstract translation: 本发明涉及具有不同碱度的至少两个氮原子的受阻胺化合物。 一部分在N-原子上被烷氧基部分取代，另一部分在N-原子上被羟基 - 烷基部分取代。 这些材料在稳定聚合物，特别是热塑性聚烯烃方面特别有效，抵抗氧化，热和光化辐射的有害影响。 化合物在稳定酸催化和环境固化的涂料体系中也特别有效。

公开(公告)号：US20120040942A1

公开(公告)日：2012-02-16

申请号：US13202875

申请日：2010-02-24

Applicant: Martin Johansson ,  Viveca Thornqvist Otlner ,  Jorgen Toftered ,  David Wensbo ,  Maria Dalence

Inventor： Martin Johansson ,  Viveca Thornqvist Otlner ,  Jorgen Toftered ,  David Wensbo ,  Maria Dalence

IPC: A61K31/56 ,  A61K31/4375 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/541 ,  A61P11/06 ,  A61K31/5386 ,  C07D491/113 ,  A61K31/438 ,  A61P11/00 ,  A61P11/08 ,  C07D471/04 ,  C07D498/08

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.

Abstract translation: 本发明涉及具有通式（I）的新化合物，哪些化合物可用于治疗以支气管收缩为特征的疾病或疾病，例如， COPD和哮喘。

公开(公告)号：US20110152237A1

公开(公告)日：2011-06-23

申请号：US12936545

申请日：2010-08-26

Applicant: Pingyun Chen ,  Ricky Couch ,  Maosheng Duan ,  Richard Martin Grimes ,  Wieslaw Mieczyslaw Kazmierski ,  Beth Adams Norton ,  Matthew Tallant ,  Pingyun Chen ,  Ricky Couch ,  Maosheng Duan ,  Richard Martin Grimes ,  Wleslaw Mieczyslaw Kazmierski ,  Beth Adams Norton ,  Matthew Tallant

Inventor： Pingyun Chen ,  Ricky Couch ,  Maosheng Duan ,  Richard Martin Grimes ,  Wieslaw Mieczyslaw Kazmierski ,  Beth Adams Norton ,  Matthew Tallant ,  Pingyun Chen ,  Ricky Couch ,  Maosheng Duan ,  Richard Martin Grimes ,  Wleslaw Mieczyslaw Kazmierski ,  Beth Adams Norton ,  Matthew Tallant

IPC: A61K31/4178 ,  C07D491/113 ,  C07D495/10 ,  C07D491/107 ,  C07D403/14 ,  C07D471/10 ,  C07D487/10 ,  A61K31/438 ,  A61P31/12 ,  A61P31/14

CPC classification number: A61K31/4178 ,  A61K31/435 ,  A61K31/7056 ,  A61K38/21 ,  C07D403/12 ,  C07D403/14 ,  C07D471/10 ,  C07D487/10 ,  C07D487/20 ,  C07D491/10 ,  C07D491/107 ,  C07D491/113 ,  C07D495/10 ,  C07D519/00

Abstract: Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.

Abstract translation: 公开了式III的化合物。 还公开了化合物的盐，包含化合物或盐的药物组合物，以及通过施用化合物或盐治疗HCV感染的方法。

公开(公告)号：US20110009391A1

公开(公告)日：2011-01-13

申请号：US12843124

申请日：2010-07-26

Applicant: Alain Jean BRAUN ,  Olivier CRESPIN ,  Claudie NAMANE ,  Eric NICOLAI ,  Francois PACQUET ,  Cecile PASCAL ,  Christophe PHILIPPO ,  Olivier VENIER

Inventor： Alain Jean BRAUN ,  Olivier CRESPIN ,  Claudie NAMANE ,  Eric NICOLAI ,  Francois PACQUET ,  Cecile PASCAL ,  Christophe PHILIPPO ,  Olivier VENIER

IPC: A61K31/4985 ,  C07D401/10 ,  C07D403/12 ,  C07D413/14 ,  C07D417/10 ,  C07D491/113 ,  C07D403/10 ,  C07C237/24 ,  C07C271/56 ,  C07C61/29 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61P3/10 ,  A61P3/04 ,  A61P9/00 ,  A61P9/12 ,  A61P9/10 ,  A61P25/28 ,  A61P27/06 ,  A61P31/00 ,  A61P1/16 ,  A61P37/00

CPC classification number: C07D239/26 ,  C07D241/44 ,  C07D401/10 ,  C07D401/12

Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application.

Abstract translation: 本发明涉及四氢喹喔啉脲衍生物，其制备及其治疗应用。

公开(公告)号：US20100305322A1

公开(公告)日：2010-12-02

申请号：US12854677

申请日：2010-08-11

Applicant: Peter Nesvadba ,  Lucienne Bugnon ,  Martin Von Büren

Inventor： Peter Nesvadba ,  Lucienne Bugnon ,  Martin Von Büren

IPC: C07D211/44 ,  C07D491/113

CPC classification number: C07D491/10 ,  C07B61/02 ,  C07D211/94

Abstract: The invention relates to a process for the preparation of secondary nitroxide radicals from their corresponding secondary amines by oxidation with an organic peracid, comprising the steps a) adding to a reaction vessel a secondary amine, optionally together with an organic solvent and in one batch a base selected from the group consisting of alkali metal, alkaline earth metal or ammonium bicarbonates and alkaline earth metal or ammonium carbonates or mixtures thereof in the form of a solid together with water or as an aqueous slurry; b) dosing a peracid under stirring to the reaction mixture in an amount of 1.0 to 2.5 mol per mol of secondary amine; and c) isolating the organic phase.

Abstract translation: 本发明涉及通过用有机过酸氧化从其相应的仲胺制备二级氮氧自由基的方法，包括以下步骤：a）向反应容器中加入仲胺，任选与有机溶剂一起加入一次 碱选自碱金属，碱土金属或碳酸氢铵，碱土金属或铵的碳酸盐或其混合物，其形式为水，或与水相混合; b）在搅拌下将过酸给予反应混合物，其量为每摩尔仲胺为1.0至2.5摩尔; 和c）分离有机相。

公开(公告)号：US20100216726A1

公开(公告)日：2010-08-26

申请号：US12712042

申请日：2010-02-24

Applicant: Kouki FUCHINO ,  R. Richard Goehring ,  Akira Matsumura ,  Bin Shao ,  Yoshiyuki Taoda ,  Naoki Tsuno ,  John William Frank Whitehead ,  Jiangchao Yao

Inventor： Kouki FUCHINO ,  R. Richard Goehring ,  Akira Matsumura ,  Bin Shao ,  Yoshiyuki Taoda ,  Naoki Tsuno ,  John William Frank Whitehead ,  Jiangchao Yao

IPC: A61K38/05 ,  C07D401/04 ,  A61K31/498 ,  A61P3/04 ,  A61P13/06 ,  A61P9/12 ,  A61P25/08 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P1/12 ,  C07D413/14 ,  A61K31/5377 ,  C07D471/04 ,  C07D491/113 ,  C07D451/14

CPC classification number: C07D451/14 ,  A61K31/498 ,  C07D401/04 ,  C07D401/14 ,  C07D451/04 ,  C07D471/08 ,  C07D471/14 ,  C07D487/04 ,  C07D498/08 ,  C07D519/00

Abstract: The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.

Abstract translation: 本发明涉及取代的喹喔啉型哌啶化合物，包含有效量的取代的喹喔啉型哌啶化合物的组合物和治疗或预防诸如疼痛的病症的方法，包括向有需要的动物施用有效量 的取代的喹喔啉型哌啶化合物。

公开(公告)号：US20100048599A1

公开(公告)日：2010-02-25

申请号：US12540300

申请日：2009-08-12

Applicant: GUOQING PAUL CHEN

Inventor： GUOQING PAUL CHEN

IPC: A61K31/4709 ,  C07D491/113 ,  C07D401/14 ,  A61P35/00

CPC classification number: A61K31/4709 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D491/113

Abstract: The present invention relates to compounds of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis, such as cancers associated with protein tyrosine kinases, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans.

Abstract translation: 本发明涉及式I化合物，其制备方法，含有它们作为活性成分的药物组合物，用于治疗与血管发生相关的疾病状态的方法，例如与蛋白酪氨酸激酶相关的癌症，其用作药物用途 在抑制热血动物如人类中抑制酪氨酸激酶的作用下降。