公开(公告)号：US20170088582A1

公开(公告)日：2017-03-30

申请号：US15312614

申请日：2015-05-19

Applicant: RQX PHARMACEUTICALS, INC. ,  GENENTECH, INC.

Inventor： Tucker Curran ROBERTS ,  Peter Andrew SMITH ,  Robert I. HIGUCHI ,  Prasuna PARASELLI ,  Philippe BERGERON ,  Michael F.T. KOEHLER ,  Huiyong HU ,  Jacob Bradley SCHWARZ ,  Cuong LY ,  James CRAWFORD

IPC: C07K5/103 ,  A61K38/07 ,  A61K38/06 ,  C07K7/06 ,  A61K38/08 ,  A61K45/06 ,  C07K5/083

CPC classification number: C07K5/101 ,  A61K31/395 ,  A61K31/407 ,  A61K31/4196 ,  A61K31/43 ,  A61K31/431 ,  A61K31/496 ,  A61K31/545 ,  A61K31/546 ,  A61K38/00 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K45/06 ,  C07K5/0202 ,  C07K5/0808 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/1008 ,  C07K5/1013 ,  C07K5/1019 ,  C07K7/06 ,  C07K7/08 ,  Y02A50/401 ,  Y02A50/47 ,  Y02A50/471 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/483 ,  A61K2300/00 ,  A61L2300/00

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

公开(公告)号：US20140080805A1

公开(公告)日：2014-03-20

申请号：US14088110

申请日：2013-11-22

Applicant: Genentech, Inc.

Inventor： Frederick COHEN ,  Vickie Hsiao-Wei TSUI ,  Cuong LY ,  John A. FLYGARE

IPC: C07D471/04 ,  C07D417/14 ,  C07D417/04

CPC classification number: C07D471/04 ,  C07D417/04 ,  C07D417/14

Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4′, R5, R6 and R6′ are as described herein.

Abstract translation: 本发明提供了可用作治疗恶性肿瘤的治疗剂的新的IAP抑制剂，其中化合物具有通式I：其中A，Q，X 1，X 2，Y，R 1，R 2，R 3，R 4，R 4'，R 5，R 6 和R6'如本文所述。