公开(公告)号：WO2018162928A1

公开(公告)日：2018-09-13

申请号：PCT/GB2018/050613

申请日：2018-03-09

Applicant: HELPERBY THERAPEUTICS LIMITED

Inventor： COATES, Anthony ,  HU, Yanmin

IPC: C07K7/62 ,  A61K38/12 ,  A61K31/05

CPC classification number: C07K7/62 ,  A61K31/05 ,  A61K31/137 ,  A61K31/138 ,  A61K31/336 ,  A61K31/395 ,  A61K31/407 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/545 ,  A61K31/704 ,  A61K31/7048 ,  A61K31/7072 ,  A61K38/12 ,  A61K45/06 ,  A61K2300/00

Abstract: The invention provides a method for restoring efficacy of an antibacterial agent, the method comprising (i) combining the antibacterial agent with a first antibiotic resistance breaker after a first time period; and (ii) combining the antibacterial agent with a second antibiotic resistance breaker after a second time period, wherein during each time period the efficacy of the antibacterial agent decreases due to increasing antibiotic resistance, and wherein each antibiotic resistance breaker at least partially restores the efficacy of the antibacterial agent relative to the end of the preceding time period. The first and second antibiotic resistance breakers have different mechanisms of action. Additionnally the invention provides the use of at least two antibiotic resistance breakers to prolong the efficacy of an antibacterial agent, wherein the at least two antibiotic resistance breakers have different mechanisms of action.

公开(公告)号：WO2018136843A1

公开(公告)日：2018-07-26

申请号：PCT/US2018/014595

申请日：2018-01-20

Applicant: UNIVERSITY OF KANSAS ,  UNIVERSITY OF FLORIDA

Inventor： ALDRICH, Jane ,  MUKHOPADHYAY, Archana ,  HANOLD, Laura E.

IPC: A61K38/00 ,  A61K38/07 ,  A61K38/12 ,  A61P35/00 ,  C07K5/10 ,  C07K5/12

Abstract: The present technology provides methods and medicaments useful for treating prostate cancer and breast cancer. Such methods include administering at least one of cyc/o [Phe-D-Pro-Phe-Trp] and cyc/o [Phe-D-Pro-Phe-D-Τrp] to a subject suffering from prostate cancer or breast cancer.

公开(公告)号：WO2018109042A3

公开(公告)日：2018-06-21

申请号：PCT/EP2017/082697

申请日：2017-12-13

Applicant: FERRING B.V.

Inventor： HENNINOT, Antoine ,  CARNEY, Daniel William

IPC: A61K38/12 ,  C07K5/12 ,  C07K7/54 ,  C07K7/56

Abstract: This disclosure relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof: Formula (I), in which n, R 1 , R 1 ', R 2 , R 3 , R 4 , R 4 ', and R 5 -R 14 are defined in the specification. The compounds of formula (I) can be used to treat bacterial infection.

公开(公告)号：WO2018109042A2

公开(公告)日：2018-06-21

申请号：PCT/EP2017/082697

申请日：2017-12-13

Applicant: FERRING B.V.

Inventor： HENNINOT, Antoine ,  CARNEY, Daniel William

IPC: A61K38/12 ,  C07K5/12 ,  C07K7/54 ,  C07K7/56

Abstract: This disclosure relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof: Formula (I), in which n, R 1 , R 1 ', R 2 , R 3 , R 4 , R 4 ', and R 5 -R 14 are defined in the specification. The compounds of formula (I) can be used to treat bacterial infection.

公开(公告)号：WO2018089648A3

公开(公告)日：2018-05-17

申请号：PCT/US2017/060881

申请日：2017-11-09

Applicant: OHIO STATE INNOVATION FOUNDATION

Inventor： PEI, Dehua ,  QIAN, Ziqing

IPC: A61K38/05 ,  A61K38/12 ,  A61K38/46

Abstract: Disclosed is a general, reversible bicyclization strategy to increase both the proteolytic stability and cell permeability of peptidyl drugs. A peptide drug is fused with a short cell-penetrating motif and converted into a conformationally constrained bicyclic structure through the formation of a pair of disulfide bonds. The resulting bicyclic peptide has greatly enhanced proteolytic stability as well as cell-permeability. Once inside the cell, the disulfide bonds are reduced to produce a linear, biologically active peptide. This strategy was applied to generate a cell-permeable bicyclic peptidyl inhibitor against the NEMO-IKK interaction.

公开(公告)号：WO2018089648A2

公开(公告)日：2018-05-17

申请号：PCT/US2017/060881

申请日：2017-11-09

Applicant: OHIO STATE INNOVATION FOUNDATION

Inventor： PEI, Dehua ,  QIAN, Ziqing

IPC: A61K38/12 ,  C07K7/50

Abstract: Disclosed is a general, reversible bicyclization strategy to increase both the proteolytic stability and cell permeability of peptidyl drugs. A peptide drug is fused with a short cell-penetrating motif and converted into a conformationally constrained bicyclic structure through the formation of a pair of disulfide bonds. The resulting bicyclic peptide has greatly enhanced proteolytic stability as well as cell-permeability. Once inside the cell, the disulfide bonds are reduced to produce a linear, biologically active peptide. This strategy was applied to generate a cell-permeable bicyclic peptidyl inhibitor against the NEMO-IKK interaction.

Abstract translation: 公开了增加肽基药物的蛋白水解稳定性和细胞渗透性的一般可逆双环化策略。 肽药物与短细胞穿透基序融合并通过形成一对二硫键而转化为构象受限的双环结构。 得到的双环肽极大地提高了蛋白水解稳定性以及细胞渗透性。 一旦进入细胞内，二硫键被还原以产生线性的生物活性肽。 该策略用于产生抗NEMO-IKK相互作用的细胞渗透性双环肽基抑制剂。

公开(公告)号：WO2018085574A2

公开(公告)日：2018-05-11

申请号：PCT/US2017/059770

申请日：2017-11-02

Applicant: WASHINGTON UNIVERSITY ,  DIPERSIO, John F. ,  KARPOVA, Darja

Inventor： DIPERSIO, John F. ,  KARPOVA, Darja

IPC: A61K38/16 ,  A61K38/12

CPC classification number: A61K38/19 ,  A61K31/395 ,  A61K31/4427 ,  A61K2300/00

Abstract: The present disclosure provides methods of treating a patient comprising administering an agent which interacts with a chemokine such as G-CSF, plerixafor, or Gro-β and VLA-4 inhibitors. These methods may be used in the treatment of a condition which requires the collection of hematopoietic stem cells for transfusions or in chemotherapy.

Abstract translation: 本公开提供了治疗患者的方法，其包括施用与趋化因子例如G-CSF，普乐沙福或Gro-β和VLA-4抑制剂相互作用的药剂。 这些方法可用于治疗需要收集造血干细胞进行输血或化疗的病症。

公开(公告)号：WO2018078008A1

公开(公告)日：2018-05-03

申请号：PCT/EP2017/077424

申请日：2017-10-26

Applicant: JANSSEN VACCINES & PREVENTION B.V.

Inventor： JURASZEK, Jaroslaw ,  VAN DONGEN, Maria ,  BRANDENBURG, Boerries

IPC: A61K38/10 ,  A61K38/12 ,  C07K14/47

Abstract: The present invention relates to novel compounds, in particular peptidic macrocyclic peptides, that are capable of binding to and/or neutralizing influenza viruses, in particular influenza A viruses comprising HA of the H1 subtype 1, and to pharmaceutical compositions comprising such compounds. The invention also relates to the use of the peptidomimetic 5 compounds in the diagnosis, prophylaxis and/or treatment of influenza virus infections.

Abstract translation: 本发明涉及新型化合物，特别是肽类大环肽，其能够结合和/或中和流感病毒，特别是包含H1亚​​型1的HA的流感A病毒，并且涉及 包含这些化合物的药物组合物 本发明还涉及拟肽化合物在诊断，预防和/或治疗流感病毒感染中的用途。

公开(公告)号：WO2017197390A1

公开(公告)日：2017-11-16

申请号：PCT/US2017/032669

申请日：2017-05-15

Applicant: SPERO POTENTIATOR, INC.

Inventor： COLEMAN, Scott ,  SHASTRI, Prathap N.

IPC: A61K38/12 ,  A61K38/14 ,  A61K45/06 ,  A61K31/351 ,  A61K31/407 ,  A61K31/46 ,  A61K31/496 ,  A61K31/575 ,  A61K31/7048 ,  A61K31/7052 ,  A61P31/04

CPC classification number: A61K38/12 ,  A61K9/0019 ,  A61K31/351 ,  A61K31/407 ,  A61K31/46 ,  A61K31/496 ,  A61K31/575 ,  A61K31/7048 ,  A61K31/7052 ,  A61K38/14 ,  A61K45/06 ,  A61P31/04 ,  Y02A50/473 ,  A61K2300/00

Abstract: This disclosure provides a method of treating a bacterial infection in a human patient comprising by administering a therapeutically effective dose of SPR741, a polymyxin analog, in combination with a therapeutically effective amount of an antibiotic other than SPR741. The disclosure establishes 100 mg to 500 mg of SPR741, administered 2 to 4 times daily as the effective amount of SPR741 for co-administration with a therapeutically effective amount of a second antibiotic. The disclosure also provides a method of treating a bacterial infection comprising administering 40 mg/ kg patient weight/ day or less and preferably 5 mg/ kg patient weight/ day or less of SPR741 in combination with a therapeutically effective amount of a second antibiotic.

Abstract translation: 本公开内容提供了治疗人类患者的细菌感染的方法，其包括通过施用治疗有效剂量的SPR741（多粘菌素类似物）与治疗有效量的除SPR741以外的抗生素组合。 本公开建立了100mg至500mg的SPR741，每日施用2至4次作为与治疗有效量的第二抗生素共同施用的SPR741的有效量。 本公开还提供了治疗细菌感染的方法，其包括与治疗有效量的第二抗生素组合施用40mg / kg患者体重/天或更少，优选5mg / kg患者体重/天或更少的SPR741。 / p>

公开(公告)号：WO2017197291A1

公开(公告)日：2017-11-16

申请号：PCT/US2017/032455

申请日：2017-05-12

Applicant: SPERO POTENTIATOR, INC.

Inventor： LISTER, Troy

IPC: A61K38/12 ,  A61K31/427 ,  A61K31/46 ,  A61K31/7048 ,  A61P31/04

CPC classification number: A61K38/12 ,  A61K9/0014 ,  A61K9/0019 ,  A61K31/427 ,  A61K31/439 ,  A61K31/46 ,  A61K31/7048 ,  A61P31/04 ,  Y02A50/473 ,  A61K2300/00

Abstract: This disclosure provides a method of potentiating the efficacy of certain antibiotics by administering a therapeutically effect amount of the antibiotic in combination with SPR741. In certain embodiments the antibiotic is retapamulin, telithromycin, or aztreonam. The disclosure also provides a method of treating a bacterial infection by administering SPR741 in combination with a second antibiotic and pharmaceutical compositions comprising SPR741 and a second antibiotic.

Abstract translation: 本公开内容提供了通过施用治疗有效量的抗生素与SPR741组合来增强某些抗生素的功效的方法。 在某些实施方案中，抗生素是瑞珠蛋白，泰利霉素或氨曲南。 本公开还提供了通过将SPR741与第二抗生素以及包含SPR741和第二抗生素的药物组合物联合给药来治疗细菌感染的方法。