公开(公告)号：US09096614B2

公开(公告)日：2015-08-04

申请号：US14357340

申请日：2012-11-08

Applicant: UCB Pharma S.A. ,  Katholieke Universiteit Leuven, K.U.Leuven R&D

Inventor： Daniel Christopher Brookings ,  Daniel James Ford ,  Richard Jeremy Franklin ,  Anant Ramrao Ghawalkar ,  Claire Louise Kulisa ,  Judi Charlotte Neuss ,  James Thomas Reuberson

IPC: C07D513/04 ,  C07D519/00 ,  A61K31/519 ,  A61P37/06

CPC classification number: C07D513/04 ,  A61K31/519 ,  C07D519/00

Abstract: A series of thiazolo[5,4-d]pyrimidine derivatives of formula (I) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof: (I) Q represents a group of formula (Qa), (Qb), (Qc), (Qd) or (Qe) are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.

Abstract translation: 一系列式（I）的噻唑并[5,4-d]嘧啶衍生物或其N-氧化物，或其药学上可接受的盐或溶剂化物：（I）Q表示式（Qa），（Qb） ，（Qc），（Qd）或（Qe）有利于治疗和/或预防各种人类疾病，包括炎症，自身免疫和肿瘤疾病; 病毒性疾病 和器官和细胞移植排斥反应。

公开(公告)号：US08604051B2

公开(公告)日：2013-12-10

申请号：US13760788

申请日：2013-02-06

Applicant: UCB Pharma S.A.

Inventor： Martin Clive Hutchings ,  Sarah Catherine Archibald ,  Daniel Christopher Brookings ,  Jeremy Martin Davis ,  James Andrew Johnson ,  Barry John Langham ,  Judi Charlotte Neuss

IPC: A61K31/44 ,  C07D513/02

CPC classification number: C07D495/04

Abstract: Novel processes for the preparation of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety and intermediates thereto are provided. The compounds prepared by the present processes may be useful, for example, as selective inhibitors of human MEK (MAPKK) enzymes, and are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.

Abstract translation: 提供了通过取代的苯胺基部分在2-位上被取代的噻吩并[2,3-b]吡啶衍生物的制备方法及其中间体。 通过本方法制备的化合物可用作例如人MEK（MAPKK）酶的选择性抑制剂，因此在医学中有益，例如在治疗炎症，自身免疫，心血管，增殖（包括肿瘤） 和伤害感受条件。 本方法可以提供改进的产率，化学或立体化学纯度，中间体和最终产物的制备和/或分离的容易程度，以及更具有工业上有用的反应条件和可加工性。

公开(公告)号：US20140315885A1

公开(公告)日：2014-10-23

申请号：US14357340

申请日：2012-11-08

Applicant: UCB Pharma S.A. ,  Katholieke Universiteit Leuven, K.U. Leuven R&D

Inventor： Daniel Christopher Brookings ,  Daniel James Ford ,  Richard Jeremy Franklin ,  Anant Ramrao Ghawalkar ,  Claire Louise Kulisa ,  Judi Charlotte Neuss ,  James Thomas Reuberson

IPC: C07D513/04 ,  C07D519/00

CPC classification number: C07D513/04 ,  A61K31/519 ,  C07D519/00

Abstract: A series of thiazolo[5,4-d]pyrimidine derivatives of formula (I) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof: (I) Q represents a group of formula (Qa), (Qb), (Qc), (Qd) or (Qe) are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.

Abstract translation: 一系列式（I）的噻唑并[5,4-d]嘧啶衍生物或其N-氧化物，或其药学上可接受的盐或溶剂化物：（I）Q表示式（Qa），（Qb） ，（Qc），（Qd）或（Qe）有利于治疗和/或预防各种人类疾病，包括炎症，自身免疫和肿瘤疾病; 病毒性疾病 和器官和细胞移植排斥反应。

公开(公告)号：US20130150573A1

公开(公告)日：2013-06-13

申请号：US13760788

申请日：2013-02-06

Applicant: UCB Pharma S.A.

Inventor： Clive Martin Hutchings ,  Sarah Catherine Archibald ,  Daniel Christopher Brookings ,  Jeremy Martin Davis ,  James Andrew Johnson ,  Barry John Langham ,  Judi Charlotte Neuss

IPC: C07D495/04

CPC classification number: C07D495/04

Abstract: Novel processes for the preparation of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety and intermediates thereto are provided. The compounds prepared by the present processes may be useful, for example, as selective inhibitors of human MEK (MAPKK) enzymes, and are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.

Abstract translation: 提供了通过取代的苯胺基部分在2-位上被取代的噻吩并[2,3-b]吡啶衍生物的制备方法及其中间体。 通过本方法制备的化合物可用作例如人MEK（MAPKK）酶的选择性抑制剂，因此在医学中有益，例如在治疗炎症，自身免疫，心血管，增殖（包括肿瘤） 和伤害感受条件。 本方法可以提供改进的产率，化学或立体化学纯度，中间体和最终产物的制备和/或分离的容易程度，以及更具有工业上有用的反应条件和可加工性。