公开(公告)号：WO2019110589A1

公开(公告)日：2019-06-13

申请号：PCT/EP2018/083491

申请日：2018-12-04

Applicant: F. HOFFMANN-LA ROCHE AG ,  HOFFMANN-LA ROCHE INC.

Inventor： ZHANG, Jitao David ,  HAN, Xingchun ,  YANG, Song ,  TRIYATNI, Miriam ,  LEONARD, Brian ,  WALLIER, Angelina ,  SCHMALER, Josephine ,  TURLEY, Daniel ,  TROPBERGER, Philipp ,  CROSET, Samuel

IPC: A61K31/4439 ,  A61K31/4985 ,  A61P31/20 ,  C12Q1/70

CPC classification number: A61K31/4985 ,  A61K31/4439 ,  A61P31/20 ,  C12Q1/707

Abstract: The present invention relates to novel therapeutic agents against hepatitis B virus (HBV) infection, particularly inhibitors of viral covalently closed circular DNA (cccDNA) which is the key barrier for HBV cure. Accordingly, the invention provides the pyrrolo[2,3-b]pyrazine compounds of formula (I), as described and defined herein, for use in the treatment of HBV infection. The compounds provided herein are highly potent against HBV infection and enable an improved therapy, particularly of chronic HBV infection and HBV rebound. The present invention further relates to a novel screening assay for the identification of therapeutic agents against HBV infection, particularly cccDNA inhibitors, which is performed in hepatocyte-like cells that recapitulate the complete HBV life cycle following infection with patient-derived HBV.

公开(公告)号：WO2019099203A1

公开(公告)日：2019-05-23

申请号：PCT/US2018/058576

申请日：2018-10-31

Applicant: HEPAGENE THERAPEUTICS, INC.

Inventor： XU, Xiaodong

IPC: C07D413/14 ,  A61K31/4439 ,  C07D417/14 ,  C07D487/08 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D413/14 ,  A61K31/4439 ,  A61P35/00 ,  A61P37/00 ,  C07D417/14 ,  C07D487/08

Abstract: The present technology is directed to compounds of formula (I), compositions thereof, and methods related to inhibition of ASKI. In particular, the present compounds and compositions may be used to treat ASKl-mediated disorders and conditions, including, e.g., fibrotic diseases and acute and chronic liver diseases, among others.

公开(公告)号：WO2019094798A1

公开(公告)日：2019-05-16

申请号：PCT/US2018/060133

申请日：2018-11-09

Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

Inventor： CHRISTIANO, Angela M.

IPC: A61K39/00 ,  A61K31/7105 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/506 ,  A61P17/14

CPC classification number: A61K8/64 ,  A61K8/606 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/7105 ,  A61K39/00 ,  A61P17/14 ,  A61Q7/00

Abstract: The presently disclosed subject matter relates, in certain embodiments, to compositions and methods for the inhibition of the Janus activated kinase-signal transducer and activator of transcription (JAK-STAT) pathway, and particularly inhibition of oncostatin (e.g. oncostatin M (OSM)), colony stimulating factor 1 receptor (CSF1R), interleukin-34 (IL-34), and/or trichophages, in order to induce or promote hair growth. In certain embodiments, the presently disclosed subject matter relates to topical treatments with small molecule inhibitors of the JAK-STAT pathway, and particularly small molecule inhibitors of oncostatin, CSF1R, IL-34, and/or trichophages, to induce or promote hair growth. Some embodiments are directed to treating hair loss disorders using inhibitors of oncostatin, CSF1R, IL-34 and/or trichophages. Embodiments also describe kits including inhibitors of oncostatin, CSF1R, IL-34 and/or trichophages.

公开(公告)号：WO2019066469A1

公开(公告)日：2019-04-04

申请号：PCT/KR2018/011386

申请日：2018-09-27

Applicant: 경북대학교 산학협력단 ,  경북대학교병원

Inventor： 김용림 ,  최순연 ,  오세현

IPC: A61K31/426 ,  A61K31/4439 ,  A23L33/10

CPC classification number: A23L33/10 ,  A61K31/426 ,  A61K31/4439

Abstract: 본 발명은 페북소스타트 (febuxostat) 또는 토피록소스타트 (topiroxostat)의 신규한 용도에 관한 것으로, 보다 상세하게는 페북소스타트, 토피록소스타트 및 이들의 약학적으로 허용 가능한 염으로 이루어진 군에서 선택되는 어느 하나 이상의 것을 유효성분으로 포함하는 암 전이 억제, 암의 예방 및 치료용 약학적 조성물에 대한 것이다. 페북소스타트 (febuxostat), 토피록소스타트 (topiroxostat)는 암의 전이를 특이적으로 억제하는 효과가 현저하여, 암 예방 및 치료를 위한 새로운 수단을 제공한다.

公开(公告)号：WO2019050890A1

公开(公告)日：2019-03-14

申请号：PCT/US2018/049463

申请日：2018-09-05

Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE

Inventor： ALTEROVITZ, Gil

IPC: A61K31/133 ,  A61K39/04 ,  A61K45/06 ,  C12N1/20 ,  G01N33/53 ,  G01N33/569

CPC classification number: A61K31/536 ,  A61K31/085 ,  A61K31/138 ,  A61K31/353 ,  A61K31/4045 ,  A61K31/4184 ,  A61K31/429 ,  A61K31/4422 ,  A61K31/4439 ,  A61K31/538 ,  A61K31/554 ,  A61K2300/00

Abstract: Provided herein are methods and compositions, including synergistic combinations, for the treatment of tuberculosis.

公开(公告)号：WO2019048851A1

公开(公告)日：2019-03-14

申请号：PCT/GB2018/052513

申请日：2018-09-05

Applicant: BENEVOLENTAI BIO LIMITED

Inventor： RICHARDSON, Peter ,  SHEPPARD, David

IPC: A61K31/404 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/4468 ,  A61K31/453 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/553 ,  A61P25/28 ,  A61K45/06

CPC classification number: A61K31/506 ,  A61K31/404 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/4468 ,  A61K31/453 ,  A61K31/454 ,  A61K31/496 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/553 ,  A61K45/06

Abstract: Methods for the prevention and treatment of neurodegenerative diseases, in particular motor neuron diseases such as amyotrophic lateral sclerosis (ALS), are described, as well as compositions and combined preparations for use in the methods. The methods comprise inhibiting CDK7 in the central nervous system of a subject in need of such prevention or treatment.

公开(公告)号：WO2019023815A1

公开(公告)日：2019-02-07

申请号：PCT/CL2018/050059

申请日：2018-07-30

Applicant: SERVICIOS CIENTÍFICOS NEUROINNOVATION LIMITADA

Inventor： MACCIONI BARAHONA, Ricardo ,  ROJO CASTILLO, Leonel ,  QUIÑONES SEPÚLVEDA, Luis

IPC: C07D413/12 ,  C07D417/12 ,  A61K31/4439 ,  A61K49/00

CPC classification number: A61K31/4439 ,  A61K49/00 ,  C07D413/12 ,  C07D417/12

Abstract: La presente invención corresponde a compuestos piridinmetilsulfinilbenzoxazoles y piridinmetilsulfinilbenzotiazoles, marcados 5 radiactivamente o con fluorescencia y sus composiciones, como biornarcadores especificos para el diagnóstico de enfermedades neurodegenerativas y patológicas involucradas con Ia proteína tau tales como AIzheimer y otras demencias. Conforme a Ia presente invención las técnicas donde se pueden emplear las moléculas descritas pueden ser: Tomografia Axial Computarizada 0 (CAT), resonancia magnetica nuclear (NMR), tanto estructural (sNMR) como funcional NMR (fNMR), tomografia computarizada de emisión de fotón único (SPECT) y Ia tomografia de emisión de positrones (PET). De esta forma Ia invención proporciona una herrarnienta farmacolóqicamente segura, con una elevada afinidad y selectividad por estructuras proteicas de proteína tau, lo cual 5 permite establecer una aplicación, método o uso de dichos agentes pare la identificación y diagnóstico de enfermedades neurodegenerativas, tau patologias, de preferencia enfermedad de Alzheirner.

公开(公告)号：WO2019015559A1

公开(公告)日：2019-01-24

申请号：PCT/CN2018/095897

申请日：2018-07-17

Applicant: 南京圣和药业股份有限公司

Inventor： 王勇 ,  赵立文 ,  葛崇勋 ,  黄奕强 ,  曹陈 ,  李晴晴 ,  江宏 ,  韩伟 ,  张着伟 ,  张亚楠

IPC: C07D401/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/08 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/4725 ,  A61K31/444 ,  A61P25/28 ,  A61P29/00 ,  A61P9/00

CPC classification number: A61K31/427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/553 ,  A61P1/16 ,  A61P3/00 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12 ,  A61P11/00 ,  A61P13/12 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/08 ,  C07D498/04 ,  C07D498/08

Abstract: 本发明属于医药化学领域，涉及一类作为ASK抑制剂的杂环化合物及其应用，具体地，本发明提供式A所示的化合物或其异构体、药学上可接受的盐、溶剂化物、结晶或前药，它们的制备方法以及含有这些化合物的药物组合物和这些化合物或组合物用于治疗和/或预防细胞凋亡信号调节激酶1相关的疾病的用途。本发明的化合物具有优异的细胞凋亡信号调节激酶1抑制活性，非常有希望成为细胞凋亡信号调节激酶1相关疾病的治疗剂。

公开(公告)号：WO2018237249A1

公开(公告)日：2018-12-27

申请号：PCT/US2018/038964

申请日：2018-06-22

Applicant: BIOMIMETIX JV, LLC

Inventor： CRAPO, James D. ,  SILBERSTEIN, David S. ,  STONE, Kimberly C.

IPC: A61K31/409 ,  A61K31/555 ,  C07D487/22

CPC classification number: A61K31/409 ,  A61K9/0014 ,  A61K9/06 ,  A61K31/4439 ,  A61K47/06 ,  A61K47/10 ,  A61K47/38

Abstract: Described herein are methods, compositions, and kits for treating inflammatory skin conditions. In some embodiments, methods, compositions, and kits for topically administering MnTE-2-PyP 5+ to treat inflammatory skin conditions such as, e.g., atopic dermatitis, rosacea, acne, and/or plaque psoriasis. A composition of the present invention can include a meso-substituted metalloporphyrin, wherein the meso-substituted metalloporphyrin is Ames negative and optionally is present in the composition at a concentration of about 0.005% to about 1% by weight of the composition; water or an aqueous buffer solution; a hydrophobic base; a fatty alcohol; a polyhydric alcohol; a fatty acid ester; a surfactant; optionally a buffer and/or buffering agent; and optionally a preservative.

公开(公告)号：WO2018175537A1

公开(公告)日：2018-09-27

申请号：PCT/US2018/023497

申请日：2018-03-21

Applicant: DANA-FARBER CANCER INSTITUTE, INC. ,  THE SCRIPPS RESEARCH INSTITUTE ,  SCHREIBER, Stuart, L. ,  SCHILLING, Roger ,  NAG, Partha, Pratim ,  BITTKER, Joshua, A.

Inventor： SCHREIBER, Stuart, L. ,  SCHILLING, Roger ,  NAG, Partha, Pratim ,  BITTKER, Joshua, A. ,  PUIGSERVER, Pere ,  SHARABI, Kfir ,  KAMENECKA, Theodore ,  GRIFFIN, Patrick

IPC: A61K31/404 ,  A61K31/4045 ,  A61K31/405

CPC classification number: A61K45/06 ,  A61K31/138 ,  A61K31/381 ,  A61K31/40 ,  A61K31/404 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/497 ,  A61K31/519 ,  A61K31/55 ,  A61K2300/00

Abstract: The present invention provides compounds, pharmaceutical compositions and methods for treating and/or preventing a metabolic condition, such as diabetes.