公开(公告)号：US09624239B2

公开(公告)日：2017-04-18

申请号：US14009635

申请日：2012-04-03

申请人： Alain Laurent ,  Yannick Rose ,  Stephen Morris ,  James Jaquith

发明人： Alain Laurent ,  Yannick Rose ,  Stephen Morris ,  James Jaquith

IPC分类号： A61K31/519 ,  C07D487/04 ,  C07D491/147 ,  C07D495/14 ,  C12Q1/48 ,  C07D487/14 ,  C07K14/47 ,  C12N9/12

CPC分类号： C07D495/14 ,  C07D487/04 ,  C07D487/14 ,  C07D491/147 ,  C07K14/4703 ,  C12N9/1205 ,  C12Q1/485

摘要： The present invention relates to a novel family of inhibitors of protein kinases of Formula (1) wherein X is selected from CH2, O, S(0)n, or NR6; and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src, Btk and Lck protein kinase families.

公开(公告)号：US20160280711A1

公开(公告)日：2016-09-29

申请号：US15037923

申请日：2014-11-20

申请人： Pharmascience Inc.

发明人： Alain Laurent ,  Yannick Rose

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/506 ,  A61K45/06

CPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/506 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to a novel family of protein kinase inhibitors, more specifically the present invention is directed to inhibitors of the Tec or Src protein kinase families. The present invention also relates to the processes of preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative, inflammatory, autoimmune or infectious diseases, disorders, or conditions in which protein kinase activity is implicated.

摘要翻译： 本发明涉及一种新的蛋白激酶抑制剂家族，更具体地，本发明涉及Tec或Src蛋白激酶家族的抑制剂。 本发明还涉及这些化合物的制备方法，包含它们的药物组合物的用途，以及它们在治疗涉及蛋白激酶活性的增殖性，炎性，自身免疫性或感染性疾病，病症或病症中的用途。

公开(公告)号：US09365614B2

公开(公告)日：2016-06-14

申请号：US14285841

申请日：2014-05-23

申请人： Pharmascience Inc.

发明人： Alain Boudreault ,  James Jaquith ,  Patrick Bureau ,  John W. Gillard ,  Alain Laurent

IPC分类号： C07K7/06 ,  A61K31/40 ,  A61K38/00 ,  A61K38/08 ,  C07K5/087 ,  C07D207/14 ,  C07D207/16 ,  C07K5/083 ,  A61K31/4025 ,  A61K38/17

CPC分类号： C07K5/0812 ,  A61K31/40 ,  A61K31/4025 ,  A61K38/00 ,  A61K38/08 ,  A61K38/1761 ,  C07D207/14 ,  C07D207/16 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/081 ,  C07K7/06

摘要： A compound of Formula I or a salt thereof, methods for the preparation thereof, and related methods and compositions.

摘要翻译： 式I化合物或其盐，其制备方法，相关方法和组合物。

公开(公告)号：US20150250886A1

公开(公告)日：2015-09-10

申请号：US14431882

申请日：2013-09-30

申请人： PHARMASCIENCE INC.

发明人： Krishna Hari Bhandari ,  Naresh Talwar

IPC分类号： A61K47/26 ,  A61K31/485

CPC分类号： A61K47/26 ,  A61K9/205 ,  A61K31/135 ,  A61K31/137 ,  A61K31/4468 ,  A61K31/451 ,  A61K31/485 ,  A61K31/5513 ,  A61K36/888 ,  A61K2300/00

摘要： A modified release orally administrable abuse-deterrent pharmaceutical composition comprising: a therapeutically effective amount of an active pharmaceutical ingredient and konjac glucomannan. The active pharmaceutical ingredient can be selected from a number of compounds but is generally aimed to be a compound which is subject to widespread abuse such as opioids.

摘要翻译： 一种经口头给药的经口服给药的滥用药物组合物，其包含：治疗有效量的活性药物成分和魔芋葡甘露聚糖。 活性药物成分可以选自多种化合物，但通常旨在成为广泛滥用的化合物，例如阿片样物质。

公开(公告)号：US20130040892A1

公开(公告)日：2013-02-14

申请号：US13578574

申请日：2011-02-11

申请人： Alain Laurent ,  Melanie Proulx ,  Yannick Rose ,  Irina Denissova ,  Kenza Dairi ,  Scott Jarvis ,  James B. Jaquith

发明人： Alain Laurent ,  Melanie Proulx ,  Yannick Rose ,  Irina Denissova ,  Kenza Dairi ,  Scott Jarvis ,  James B. Jaquith

IPC分类号： A61K38/05 ,  C12N5/078 ,  C12N5/0787 ,  A61P29/00 ,  C07D471/04 ,  A61P35/00 ,  A61P37/00 ,  C12N5/071 ,  C07K5/062

CPC分类号： C07K5/06026 ,  A61K38/00 ,  C07K5/06034

摘要： A compound of Formula 1: (I) or salt thereof, as well as methods of making compounds of Formula 1, methods of using compounds of Formula 1 to treat proliferative disorders such as cancer, and related compounds, composition, and methods.

摘要翻译： 式1化合物或其盐，以及制备式1化合物的方法，使用式1化合物治疗增殖性疾病如癌症的方法及其相关化合物，组合物和方法。

公开(公告)号：US20180117158A1

公开(公告)日：2018-05-03

申请号：US15855704

申请日：2017-12-27

申请人： Pharmascience Inc.

发明人： Krishna Hari Bhandari ,  Naresh Talwar

IPC分类号： A61K47/26 ,  A61K36/888 ,  A61K31/135 ,  A61K31/137 ,  A61K31/4468 ,  A61K9/20 ,  A61K31/485 ,  A61K31/5513 ,  A61K31/451

CPC分类号： A61K47/26 ,  A61K9/205 ,  A61K31/135 ,  A61K31/137 ,  A61K31/4468 ,  A61K31/451 ,  A61K31/485 ,  A61K31/5513 ,  A61K36/888 ,  A61K2300/00

摘要： A modified release orally administrable abuse-deterrent pharmaceutical composition comprising: a therapeutically effective amount of an active pharmaceutical ingredient and konjac glucomannan. The active pharmaceutical ingredient can be selected from a number of compounds but is generally aimed to be a compound which is subject to widespread abuse such as opioids.

公开(公告)号：US09795608B2

公开(公告)日：2017-10-24

申请号：US15262193

申请日：2016-09-12

申请人： PHARMASCIENCE, INC.

发明人： Alain Laurent ,  Yannick Rose

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/4162

CPC分类号： A61K31/519 ,  A61K31/4162 ,  C07D487/04

摘要： The present invention relates to a novel family of inhibitors of protein kinase of formula 1 and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src and Btk protein kinase families.

公开(公告)号：US20170158697A1

公开(公告)日：2017-06-08

申请号：US15039127

申请日：2014-11-26

申请人： Pharmascience Inc.

发明人： Alain Laurent ,  Yannick Rose

IPC分类号： C07D487/04 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/519

CPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  Y02A50/411

摘要： The present invention relates to a novel family of protein kinase inhibitors, more specifically the present invention is directed to inhibitors of the members of the Tec or Src protein kinase families. The present invention also relates to processes for the preparation of these compounds, to the pharmaceutical composition comprising them, and to their use in the treatment of proliferative, inflammatory, infectious or autoimmune diseases, disorder or condition in which protein kinase activity is implicated.

公开(公告)号：US08765681B2

公开(公告)日：2014-07-01

申请号：US13672637

申请日：2012-11-08

申请人： Pharmascience Inc.

发明人： Alain Boudreault ,  James Jaquith ,  Patrick Bureau ,  John W. Gillard ,  Alain Laurent

IPC分类号： A61K38/08 ,  A61K38/00 ,  A61K31/40 ,  A61K31/4025 ,  C07K7/06 ,  A61K38/17 ,  C07K5/083

CPC分类号： C07K5/0812 ,  A61K31/40 ,  A61K31/4025 ,  A61K38/00 ,  A61K38/08 ,  A61K38/1761 ,  C07D207/14 ,  C07D207/16 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/081 ,  C07K7/06

摘要： Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I or II or a salt thereof, in which R1, R2, R3, R100, R200, R300, A, A1, BG, Q and Q1 are substituents described herein. Also disclosed is the use of compounds of Formula I and II to treat proliferative disorders such as cancer.

摘要翻译： 公开了由式I或II表示的化合物或其盐的异构体，对映体，非对映异构体或互变异构体，其中R1，R2，R3，R100，R200，R300，A，A1，BG，Q和Q1是描述的取代基 这里。 还公开了使用式I和II的化合物来治疗增殖性疾病如癌症。

公开(公告)号：US20120195915A1

公开(公告)日：2012-08-02

申请号：US13425542

申请日：2012-03-21

申请人： Alain Laurent ,  Scott Jarvis ,  Patrick Bureau ,  Alain Boudreault ,  James Jaquith

发明人： Alain Laurent ,  Scott Jarvis ,  Patrick Bureau ,  Alain Boudreault ,  James Jaquith

IPC分类号： A61K38/08 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  C12N5/07 ,  A61K39/395

CPC分类号： G01N33/57484 ,  C07D207/09 ,  C07D207/16 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14 ,  C07D487/06 ,  C07D493/10 ,  C07K5/022 ,  C07K5/06026 ,  C07K5/06191 ,  G01N2333/4703 ,  G01N2333/70596 ,  G01N2500/02

摘要： Disclosed herein is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I: or a prodrug, or a pharmaceutically acceptable salt, or labeled with a detectable label or an affinity tag thereof; wherein R1, R1a, R100, R100a, R2, R200, W, B, and W1 are defined herein. Also disclosed are methods of using compounds of Formula I to treat proliferative disorders such as cancer.