公开(公告)号：US09458177B2

公开(公告)日：2016-10-04

申请号：US14478523

申请日：2014-09-05

Applicant: Giorgio Caravatti ,  Robin Alec Fairhurst ,  Pascal Furet ,  Clive McCarthy ,  Heinrich Rueeger ,  Frank Hans Seiler ,  Frédéric Stauffer

Inventor： Giorgio Caravatti ,  Robin Alec Fairhurst ,  Pascal Furet ,  Clive McCarthy ,  Heinrich Rueeger ,  Frank Hans Seiler ,  Frédéric Stauffer

IPC: C07D403/04 ,  C07D498/04 ,  C07D413/14 ,  A61K31/5377 ,  A61K45/06

CPC classification number: C07D498/04 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/14

Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.

Abstract translation: 本发明涉及作为PI3K（磷脂酰肌醇-3-激酶）抑制剂的恶唑烷-2-酮取代的嘧啶化合物及其药物组合物，其制备方法和用于治疗依赖于 PI3K。

公开(公告)号：US20140378450A1

公开(公告)日：2014-12-25

申请号：US14478523

申请日：2014-09-05

Applicant: Giorgio CARAVATTI ,  Robin Alec FAIRHURST ,  Pascal FURET ,  Clive MCCARTHY ,  Heinrich RUEEGER ,  Frank Hans SEILER ,  Frédéric STAUFFER

Inventor： Giorgio CARAVATTI ,  Robin Alec FAIRHURST ,  Pascal FURET ,  Clive MCCARTHY ,  Heinrich RUEEGER ,  Frank Hans SEILER ,  Frédéric STAUFFER

IPC: C07D498/04 ,  A61K31/5377 ,  C07D413/14

CPC classification number: C07D498/04 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/14

Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.

Abstract translation: 本发明涉及作为PI3K（磷脂酰肌醇-3-激酶）抑制剂的恶唑烷-2-酮取代的嘧啶化合物及其药物组合物，其制备方法和用于治疗依赖于 PI3K。

公开(公告)号：US08822468B2

公开(公告)日：2014-09-02

申请号：US12396137

申请日：2009-03-02

Applicant: Pascal Furet ,  Clive McCarthy ,  Joseph Schoepfer ,  Carsten Spanka ,  Melanie Stang ,  Frederic Stauffer

Inventor： Pascal Furet ,  Clive McCarthy ,  Joseph Schoepfer ,  Carsten Spanka ,  Melanie Stang ,  Frederic Stauffer

IPC: C07D519/00 ,  C07D487/04 ,  A61K31/5025 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The invention relates to compounds of formula (I) and salts thereof wherein the substituents are as defined in the specification, the application of a compound of formula (I) in a process for the treatment of the human or animal body, in particular with regard to C-Met tyrosine kinase mediated disease; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner; processes for the preparation of a compound of formula (I).

Abstract translation: 本发明涉及式（I）化合物及其盐，其中取代基如本说明书中所定义，式（I）化合物在治疗人或动物体的方法中的应用，特别是关于 对C-Met酪氨酸激酶介导的疾病; 使用式（I）化合物制备用于治疗这些疾病的药物; 包含式（I）化合物的药物组合物，任选地在组合配偶体存在下; 制备式（I）化合物的方法。

公开(公告)号：US08466289B2

公开(公告)日：2013-06-18

申请号：US12938583

申请日：2010-11-03

Applicant: Mark G. Bock ,  Dinesh Chikkanna ,  Clive McCarthy ,  Henrik Moebitz ,  Chetan Pandit

Inventor： Mark G. Bock ,  Dinesh Chikkanna ,  Clive McCarthy ,  Henrik Moebitz ,  Chetan Pandit

IPC: C07D513/04 ,  C07D471/04 ,  C07D498/04 ,  A61K31/437 ,  A61K31/4355 ,  A61K31/4365

CPC classification number: C07D471/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention relates to compounds of Formula I where R1a, R1b, X, R2a, R2b, W, R3, R4, and R5 are as defined herein as well as pharmaceutically acceptable salts thereof. The compounds have been shown to act as MEK inhibitors which may be useful in the treatment of hyperproliferative diseases, like cancer and inflammation.

Abstract translation: 本发明涉及其中R1a，R1b，X，R2a，R2b，W，R3，R4和R5如本文所定义的式I化合物及其药学上可接受的盐。 已经显示这些化合物作为MEK抑制剂，其可用于治疗过度增殖性疾病，如癌症和炎症。

公开(公告)号：US20120184561A1

公开(公告)日：2012-07-19

申请号：US13182182

申请日：2011-07-13

Applicant: Guido BOLD ,  Pascal FURET ,  Vito GUAGNANO ,  Clive McCARTHY ,  Andrea VAUPEL

Inventor： Guido BOLD ,  Pascal FURET ,  Vito GUAGNANO ,  Clive McCARTHY ,  Andrea VAUPEL

IPC: A61K31/496 ,  C07D471/04 ,  A61K31/437

CPC classification number: C07D235/06 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  C07D473/00

Abstract: The invention relates to compounds of the formula I, wherein the moieties R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, and salts thereof; as well as their use, methods of use for them and methods of their synthesis, and the like. The compounds are protein kinase inhibitors and can, inter alia, be used in the treatment of various proliferative diseases.

Abstract translation: 本发明涉及式I化合物，其中部分R1，R2，R3，R9，R10和Q和X，Y和Z如说明书中所定义，及其盐; 以及它们的使用，它们的使用方法及其合成方法等。 这些化合物是蛋白激酶抑制剂，尤其可用于治疗各种增殖性疾病。

公开(公告)号：US08039455B2

公开(公告)日：2011-10-18

申请号：US12159742

申请日：2006-12-28

Applicant: Claudia Betschart ,  Manuel Koller ,  Kurt Laumen ,  Andreas Lerchner ,  Rainer Machauer ,  Clive McCarthy ,  Marina Tintelnot-Blomley ,  Siem Jacob Veenstra

Inventor： Claudia Betschart ,  Manuel Koller ,  Kurt Laumen ,  Andreas Lerchner ,  Rainer Machauer ,  Clive McCarthy ,  Marina Tintelnot-Blomley ,  Siem Jacob Veenstra

IPC: C07D245/04 ,  A61K31/33

CPC classification number: C07D245/04 ,  C07D273/00

Abstract: The invention relates to novel macrocyclic compounds of the formula in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

Abstract translation: 本发明涉及下式的新型大环化合物，其中所有变量如本说明书中所定义，游离碱形式或酸加成盐形式，其制备方法，用作药物和包含它们的药物。

公开(公告)号：US08017608B2

公开(公告)日：2011-09-13

申请号：US10547691

申请日：2004-03-05

Applicant: Graham Charles Bloomfield ,  Ian Bruce ,  Catherine Leblanc ,  Mrinalini Sachin Oza ,  Lewis Whithead ,  Bernard Cuenoud ,  Thomas Hugo Keller ,  Louise Kirman ,  Clive McCarthy ,  Gaynor Elizabeth Woodward

Inventor： Graham Charles Bloomfield ,  Ian Bruce ,  Catherine Leblanc ,  Mrinalini Sachin Oza ,  Lewis Whithead ,  Bernard Cuenoud ,  Thomas Hugo Keller ,  Louise Kirman ,  Clive McCarthy ,  Gaynor Elizabeth Woodward

IPC: A61K31/5377 ,  A61K31/497 ,  A61K31/506 ,  A61K31/4523 ,  A61K31/41 ,  A61K31/426 ,  A61K31/427 ,  C07D413/02 ,  C07D401/02 ,  C07D403/02 ,  C07D285/12

CPC classification number: C07D417/14 ,  C07D277/42 ,  C07D417/12

Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract translation: 游离或盐形式的式I化合物，其中R 1，R 2，R 3，R 4和R 5具有说明书中指出的含义，可用于治疗由磷脂酰肌醇3-激酶介导的疾病。 还描述了含有化合物的药物组合物和用于制备化合物的方法。

公开(公告)号：US20110124693A1

公开(公告)日：2011-05-26

申请号：US13020211

申请日：2011-02-03

Applicant: Graham Charles Bloomfield ,  Ian Bruce ,  Judy Fox Hayler ,  Catherine Leblanc ,  Darren Mark Le Grand ,  Clive McCarthy

Inventor： Graham Charles Bloomfield ,  Ian Bruce ,  Judy Fox Hayler ,  Catherine Leblanc ,  Darren Mark Le Grand ,  Clive McCarthy

IPC: A61K31/427 ,  A61P11/00 ,  A61P35/00 ,  A61P11/06 ,  A61P29/00 ,  A61P9/10 ,  A61P3/10 ,  A61P3/04 ,  A61P9/00 ,  A61P37/08 ,  A61P17/06

CPC classification number: C07D451/04 ,  C07D277/48 ,  C07D417/12 ,  C07D471/04

Abstract: Compounds of Formula I: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Abstract translation: 式I化合物：游离或盐形式，其中R a，R b，R 2，R 3，R 4和R 5具有说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的病症。 还描述了含有化合物的药物组合物和制备该化合物的方法。

公开(公告)号：US20110124624A1

公开(公告)日：2011-05-26

申请号：US13020247

申请日：2011-02-03

Applicant: Graham Charles Bloomfield ,  Ian Bruce ,  Judy Fox Hayler ,  Catherine LeBlanc ,  Darren Mark Le Grand ,  Clive McCarthy

Inventor： Graham Charles Bloomfield ,  Ian Bruce ,  Judy Fox Hayler ,  Catherine LeBlanc ,  Darren Mark Le Grand ,  Clive McCarthy

IPC: A61K31/426 ,  C07D417/12 ,  A61K31/4439 ,  C07D277/48 ,  A61K31/427 ,  A61K31/5377 ,  C07D451/04 ,  A61K31/46 ,  A61K31/496 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4245 ,  A61K31/433 ,  A61P17/06 ,  A61P35/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P29/00 ,  A61P37/06

CPC classification number: C07D451/04 ,  C07D277/48 ,  C07D417/12 ,  C07D471/04

Abstract: Compounds of Formula I: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Abstract translation: 式I化合物：游离或盐形式，其中R a，R b，R 2，R 3，R 4和R 5具有说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的病症。 还描述了含有化合物的药物组合物和制备该化合物的方法。

公开(公告)号：US20110039831A1

公开(公告)日：2011-02-17

申请号：US12849642

申请日：2010-08-03

Applicant: Pascal Furet ,  Clive McCarthy ,  Joseph Schoepfer ,  Stefan Stutz

Inventor： Pascal Furet ,  Clive McCarthy ,  Joseph Schoepfer ,  Stefan Stutz

IPC: A61K31/5025 ,  C07D487/04 ,  A61K31/551 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: The invention relates to compounds of formula (I) and salts thereof wherein the substituents are as defined in the specification, the application of a compound of formula (I) in a process for the treatment of the human or animal body, in particular with regard to C-Met tyrosine kinase mediated disease; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner; processes for the preparation of a compound of formula (I).

Abstract translation: 本发明涉及式（I）化合物及其盐，其中取代基如本说明书中所定义，式（I）化合物在治疗人或动物体的方法中的应用，特别是关于 对C-Met酪氨酸激酶介导的疾病; 使用式（I）化合物制备用于治疗这些疾病的药物; 包含式（I）化合物的药物组合物，任选地在组合配偶体存在下; 制备式（I）化合物的方法。