公开(公告)号：US20180118762A1

公开(公告)日：2018-05-03

申请号：US15665506

申请日：2017-08-01

申请人： Millennium Pharmaceuticals, Inc.

发明人： Indu T. BHARATHAN ,  Chris BLACKBURN ,  Jeffrey P. CIAVARRI ,  Jouhara CHOUITAR ,  Courtney A. CULLIS ,  Natalie D'AMORE ,  Paul E. FLEMING ,  Kenneth M. GIGSTAD ,  Krista E. GIPSON ,  Mario GIRARD ,  Yongbo HU ,  Janice LEE ,  Gang LI ,  Mansoureh REZAEI ,  Michael D. SINTCHAK ,  Francois SOUCY ,  Stephen G. STROUD ,  Tricia J. VOS ,  Tzu-Tshin WONG ,  He XU ,  Tianlin XU ,  Yingchun YE

IPC分类号： C07D513/04 ,  A61K45/06 ,  A61K31/437 ,  C07D417/14 ,  A61K31/506 ,  C07D471/04 ,  C07D401/14 ,  A61K31/549 ,  C07D401/04 ,  A61K31/497 ,  A61K31/444

摘要： The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

公开(公告)号：US20170107579A1

公开(公告)日：2017-04-20

申请号：US15170328

申请日：2016-06-01

申请人： Millennium Pharmaceuticals, Inc.

发明人： Benjamin Stone AMIDON ,  James E. BROWNELL ,  James M. GAVIN ,  Erik M. KOENIG ,  Michael D. SINTCHAK ,  Peter G. SMITH

IPC分类号： C12Q1/68 ,  G01N33/574 ,  A61K31/519

CPC分类号： C12Q1/6886 ,  A61K31/519 ,  C07K16/40 ,  C12N9/0008 ,  C12N9/93 ,  C12Q1/25 ,  C12Q1/6883 ,  C12Q2600/106 ,  C12Q2600/156 ,  C12Q2600/158 ,  C12Y102/02 ,  C12Y603/02 ,  G01N33/5011 ,  G01N33/5023 ,  G01N33/573 ,  G01N33/574 ,  G01N33/57496 ,  G01N2333/9015 ,  G01N2333/90203 ,  G01N2500/04 ,  G01N2800/52

摘要： The invention provides isolated nucleic acids molecules, designated UBA3, UAE, or UBA6, or other E1 enzyme variant nucleic acid molecules, which encode novel E1 enzyme variant proteins. The invention also provides antisense nucleic acid molecules, recombinant expression vectors containing UBA3, UAE, or UBA6, or other E1 enzyme variant nucleic acid molecules, host cells into which the expression vectors have been introduced, and nonhuman transgenic animals in which a UBA3, UAE, or UBA6, or other E1 enzyme variant gene has been introduced or disrupted. The invention still further provides isolated UBA3, UAE, or UBA6, or other E1 enzyme variant proteins, fusion proteins, antigenic peptides and anti-UBA3, UAE, or UBA6, or other E1 enzyme variant antibodies. The invention provides methods to identify agents that inhibit UBA3, UAE, or UBA6, or other E1 enzyme variant expression or activity. Diagnostic and therapeutic methods utilizing compositions of the invention are also provided.

公开(公告)号：US20170073326A1

公开(公告)日：2017-03-16

申请号：US15347334

申请日：2016-11-09

申请人： Millennium Pharmaceuticals, Inc.

发明人： Indu T. BHARATHAN ,  Chris BLACKBURN ,  Jeffrey P. CIAVARRI ,  Jouhara CHOUITAR ,  Courtney A. CULLIS ,  Natalie D'AMORE ,  Paul E. FLEMING ,  Kenneth M. GIGSTAD ,  Krista E. GIPSON ,  Mario GIRARD ,  Yongbo HU ,  Janice LEE ,  Gang LI ,  Mansoureh REZAEI ,  Michael D. SINTCHAK ,  Francois SOUCY ,  Stephen G. STROUD ,  Tricia J. VOS ,  Tzu-Tshin WONG ,  He XU ,  Tianlin XU ,  Yingchun YE

IPC分类号： C07D401/04 ,  C07D401/14

CPC分类号： C07D513/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506 ,  A61K31/549 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D417/14 ,  C07D471/04 ,  A61K2300/00

摘要： The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

摘要翻译： 和其药学上可接受的盐，其中X，R 1，R 2，R 3，R 4，R 5，L 1，L 2，m和n如说明书中所述。 这样的化合物是VPS34的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。