公开(公告)号：US10100064B2

公开(公告)日：2018-10-16

申请号：US15318483

申请日：2015-06-09

Applicant: Merck Sharp & Dohme Corp.

Inventor： Meredeth Ann McGowan ,  Kin Chiu Fong ,  Neville John Anthony ,  Hua Zhou ,  Jason D. Katz ,  Lihu Yang ,  Chaomin Li ,  Yuan Tian ,  Changwei Mu ,  Baijun Ye ,  Feng Shi ,  Xiaoli Zhao ,  Jianmin Fu ,  Yabin Li

IPC: C07D473/30 ,  C07D473/34 ,  C07D519/00 ,  A61K31/52

Abstract: The instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.

公开(公告)号：US11230547B2

公开(公告)日：2022-01-25

申请号：US16764448

申请日：2018-12-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： Meredeth A. McGowan ,  Jason D. Katz ,  Matthew Christopher ,  Hua Zhou ,  David James Witter ,  Chaomin Li ,  John Lampe ,  Joey L. Methot ,  Abdelghani A. Achab ,  Xavier Fradera ,  Shimin Xu

IPC: C07D487/08 ,  C07D519/00 ,  C07D403/14

Abstract: The instant invention provides compounds of formulas Ia and Ib which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.

公开(公告)号：US20180141947A1

公开(公告)日：2018-05-24

申请号：US15736510

申请日：2016-06-24

Applicant: Meredeth Ann MCGOWAN ,  Hua ZHOU ,  Jason D. KATZ ,  Lihu YANG ,  Joey L. METHOT ,  Kathryn Ann LIPFORD ,  Shimin XU ,  Ning FU ,  Guoquan XU ,  Deqian BIAN ,  Jianmin FU ,  Yabin LI ,  kin Chiu FONG ,  MERCK SHARP & DOHME CORP.

Inventor： Meredith Ann McGowan ,  Hua Zhou ,  Jason D. Katz ,  Lihu Yang ,  Joey L. Methot ,  Kathryn Ann Lipford ,  Shimin Xu ,  Ning Fu ,  Guoquan Xu ,  Deqian Bian ,  Jianmin Fu ,  Yabin Li ,  Kin Chiu Fong

IPC: C07D473/30 ,  C07D473/34 ,  C07D519/00 ,  C07D471/04 ,  A61P35/00 ,  A61P19/02 ,  A61P11/06 ,  A61P11/00 ,  A61P37/00 ,  A61P17/06 ,  A61P11/08

CPC classification number: C07D473/30 ,  A61K45/06 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P17/06 ,  A61P19/02 ,  A61P35/00 ,  A61P37/00 ,  C07D471/04 ,  C07D473/34 ,  C07D519/00

Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.

公开(公告)号：US20170114078A1

公开(公告)日：2017-04-27

申请号：US15318483

申请日：2015-06-09

Applicant: Meredeth Ann MCGOWAN ,  Kin Chiu FONG ,  Neville John ANTHONY ,  Hua ZHOU ,  Jason D. KATZ ,  Lihu YANG ,  Chaomin LI ,  Yuan TIAN ,  Changwei MU ,  Baijun YE ,  Feng SHI ,  Xiaoli ZHAO ,  Jianmin FU ,  Yabin LI ,  Merck Sharp & Dohme Corp.

Inventor： Meredeth Ann McGowan ,  Kin Chiu Fong ,  Neville John Anthony ,  Hua Zhou ,  Jason D. Katz ,  Lihu Yang ,  Chaomin Li ,  Yuan Tian ,  Changwei Mu ,  Baijun Ye ,  Feng Shi ,  Xiaoli Zhao ,  Jianmin Fu ,  Yabin Li

IPC: C07D519/00 ,  C07D473/30 ,  C07D473/34 ,  A61K31/52

CPC classification number: C07D519/00 ,  A61K31/52 ,  C07D473/30 ,  C07D473/34

Abstract: The instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.

公开(公告)号：US20160207926A1

公开(公告)日：2016-07-21

申请号：US14443314

申请日：2013-11-15

Applicant: Merck Sharp & Dohme Corp.

Inventor： Abdelghani Abe Achab ,  Michael D. Altman ,  Yongqi Deng ,  Solomon Kattar ,  Jason D. Katz ,  Joey L. Methot ,  Hua Zhou ,  Meredeth McGowan ,  Matthew P. Christopher ,  Yudith Garcia ,  Neville John Anthony ,  Francesc Xavier Fradera Llinas ,  Liping Yang ,  Changwei Mu ,  Xiaona Wang ,  Feng Shi ,  Baijun Ye ,  Sixing Zhang ,  Xiaoli Zhao ,  Rong Zhang ,  Kin Chiu Fong ,  Xiansheng Leng

IPC: C07D487/04 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/52 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D473/34 ,  C07D519/00 ,  A61K2300/00

Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflamation, asthma, COPD and cancer.

Abstract translation: 本发明提供了作为PI3K-δ抑制剂的式I化合物，因此可用于治疗PI3K-δ介导的疾病如炎症，哮喘，COPD和癌症。

公开(公告)号：US20190119278A1

公开(公告)日：2019-04-25

申请号：US16089509

申请日：2017-03-24

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Abdelghani Abe Achab ,  Matthew P. Christopher ,  Francesc Xavier Fradera Llinas ,  Jason D. Katz ,  Joey L. Methot ,  Hua Zhou ,  Shimin Xu ,  Jianmin Fu ,  Ning Fu ,  Yabin Li ,  Xichao Wang

IPC: C07D473/00 ,  C07D519/00 ,  A61P35/00 ,  A61P37/02 ,  A61P11/06 ,  A61P19/02

Abstract: The instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.

公开(公告)号：US20150336948A1

公开(公告)日：2015-11-26

申请号：US14404208

申请日：2013-05-24

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael D. Altman ,  Christian Fischer ,  Jason D. Katz ,  Theresa M. Williams ,  Xu-Fang Zhang ,  Hua Zhou

IPC: C07D471/04 ,  C07D231/12

CPC classification number: C07D471/04 ,  C07B59/002 ,  C07B2200/05 ,  C07D231/12 ,  C07D471/08

Abstract: The present invention is directed to isotopically labeled biaryl urea compounds which possess high affinity to neurofibrillary tangles (NFTs), and thus are useful to determine the amount and distribution of NFTs in brain. The isotopically labeled biaryl urea compounds may also be useful as PET tracers and in competition assays to identify other compounds that may serve as PET tracers.

Abstract translation: 本发明涉及对神经原纤维缠结（NFT）具有高亲和力的同位素标记的联芳基脲化合物，因此可用于确定脑中NFT的量和分布。 同位素标记的联芳基脲化合物也可用作PET示踪剂，并用于竞争测定以鉴定可用作PET示踪剂的其它化合物。

公开(公告)号：US11179389B2

公开(公告)日：2021-11-23

申请号：US16764107

申请日：2018-12-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： Meredeth A. McGowan ,  Jason D. Katz ,  Hua Zhou ,  David James Witter ,  Chaomin Li ,  Kathryn A. Lipford ,  Joey L. Methot ,  Abdelghani A. Achab ,  Xavier Fradera ,  Shimin Xu ,  Jianmin Fu

IPC: A61K31/497 ,  C07D471/10 ,  C07D498/10 ,  C07D403/14 ,  C07D401/14 ,  C07D413/14 ,  A61K31/5386 ,  A61K31/5377 ,  C07D491/107

Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.

公开(公告)号：US10544147B2

公开(公告)日：2020-01-28

申请号：US16089509

申请日：2017-03-24

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Abdelghani Abe Achab ,  Matthew P. Christopher ,  Francesc Xavier Fradera Llinas ,  Jason D. Katz ,  Joey L. Methot ,  Hua Zhou ,  Shimin Xu ,  Jianmin Fu ,  Ning Fu ,  Yabin Li ,  Xichao Wang

IPC: C07D403/00 ,  C07D473/00 ,  A61P37/02 ,  A61P11/06 ,  A61P19/02 ,  A61P35/00 ,  C07D519/00

Abstract: The instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.

公开(公告)号：US10221178B2

公开(公告)日：2019-03-05

申请号：US15736510

申请日：2016-06-24

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Meredeth Ann McGowan ,  Hua Zhou ,  Jason D. Katz ,  Lihu Yang ,  Joey L. Methot ,  Kathryn Ann Lipford ,  Shimin Xu ,  Ning Fu ,  Guoquan Xu ,  Deqian Bian ,  Jianmin Fu ,  Yabin Li ,  Kin Chiu Fong

IPC: C07D473/30 ,  C07D473/34 ,  C07D471/04 ,  C07D519/00 ,  A61K45/06 ,  A61P37/00 ,  A61P17/06 ,  A61P11/06 ,  A61P11/08 ,  A61P11/00 ,  A61P35/00

Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.