公开(公告)号：WO2020054825A1

公开(公告)日：2020-03-19

申请号：PCT/JP2019/035995

申请日：2019-09-13

申请人： キッセイ薬品工業株式会社

发明人： 滝川　靖 ,  河辺　佑介 ,  大津寄　悠 ,  中村　享資

IPC分类号： C07D473/18 ,  A61K31/522 ,  A61K31/5375 ,  A61K31/5377 ,  A61P1/04 ,  A61P43/00

摘要： 本発明は、プロリル水酸化酵素（PHDs）の阻害作用を有し、潰瘍性大腸炎等の炎症性腸疾患の治療剤として有用な新規化合物を提供することを課題とする。　本発明は、ヒポキサンチン化合物又はその薬理学的に許容される塩に関する。本発明の化合物又はその薬理学的に許容される塩は、プロリル水酸化酵素の阻害作用を有し、潰瘍性大腸炎等の炎症性腸疾患の治療剤等として有用である。一つの実施態様として、本発明は、ヒポキサンチン化合物又はその薬理学的に許容される塩、及び医薬品添加物を含む医薬組成物を患者に必要量を投与することを含む、炎症性腸疾患の治療方法に関する。

公开(公告)号：WO2020049536A1

公开(公告)日：2020-03-12

申请号：PCT/IB2019/057556

申请日：2019-09-07

申请人： JUBILANT GENERICS LIMITED

发明人： MEHTA, Kamal S ,  KUMAR, Dinesh ,  SRIVASTAVA, Saurabh ,  SINGH, Rakesh K ,  JHA, Amit

IPC分类号： C07D473/18 ,  A61K31/522

摘要： The present invention relates to a pharmaceutical composition comprising valacyclovir or its pharmaceutically acceptable salts thereof. Particularly, the oral pharmaceutical composition of this invention comprise of a powder for oral suspension or sprinkles encapsulated in capsule or a sachet. The formulation disclosed in the prior arts is difficult to taste mask as the said drug is strongly bitter in taste, however, the formulation of the present invention is expected to be taste-masked, wherein the formulation is free of ion exchange resin and also exhibit the desired pharmaceutical technical attributes.

公开(公告)号：WO2019221473A1

公开(公告)日：2019-11-21

申请号：PCT/KR2019/005753

申请日：2019-05-13

申请人： 씨제이헬스케어 주식회사

发明人： 이정환 ,  조영대 ,  강복기 ,  윤미영 ,  조근형

IPC分类号： A61K9/20 ,  A61K9/00 ,  A61K31/7034 ,  A61K31/522 ,  A61P3/10

摘要： 본 발명은 다파글리플로진, 이의 약학적으로 허용 가능한 염, 수화물 또는 용매화물; 리나글립틴, 이의 약학적으로 허용 가능한 염, 수화물 또는 용매화물; 및 부형제를 포함하는 약제학적 조성물 및 이의 제조방법에 대한 것으로, 제2형 당뇨병의 치료 효과를 향상시키고 부작용을 완화시켰으며, 각 단일 성분을 함유하는 제제와 동등한 용출률과 비임상 동등성을 확보하면서도 정제의 크기를 최소화 하고, 제품 품질의 안정성을 향상 시킴으로써 환자 복용 편의성 및 복약 순응도를 향상 시켜 효과적인 제2형 당뇨병 예방 또는 치료제로 유용하게 사용될 수 있는 장점을 나타낸다.

公开(公告)号：WO2019213151A1

公开(公告)日：2019-11-07

申请号：PCT/US2019/030023

申请日：2019-04-30

申请人： UNITY BIOTECHNOLOGY

发明人： BEAUSOLEIL, Anne-Marie ,  HUDSON, Ryan

IPC分类号： A61K31/496 ,  A61K31/5377 ,  A61K31/522 ,  A61K31/4545 ,  A61P27/02 ,  A61P9/10 ,  A61P19/02 ,  A61P11/00 ,  A61P35/00

摘要： This disclosure provides compounds with Bel inhibitory activity. Phosphonamidate compounds typically include a P -phenyl phosphonamidate moiety which is substituted with an N - aryl or /V-heteroaryl group. The P -phenyl phosphonamidate moiety may be optionally substituted at phosphorus with thio (=S) instead of oxo (=0), and/or with a thioxy group or a second amino group instead of an oxy group. One of the heteroatoms attached to phosphorus may be cyclically linked to the N-substituted nitrogen atom that is attached to the phosphorus to provide a heterocyclic ring. By incorporating such a cyclic constraint between two phosphorus substituents of the core linking moiety, a favorable binding conformation may be promoted in the compounds. Selected compounds promote apoptosis in senescent cells, and can be developed for treating senescent-related conditions, such as osteoarthritis, ophthalmic disease, pulmonary disease, and atherosclerosis. Selected compounds promote apoptosis in cancer cells, and can be developed as chemotherapeutic agents.

公开(公告)号：WO2019213076A1

公开(公告)日：2019-11-07

申请号：PCT/US2019/029909

申请日：2019-04-30

申请人： INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION ,  GACHON UNIVERSITY OF INDUSTRY-ACADEMIC COOPERATION FOUNDATION

发明人： CORSON, Timothy W. ,  SEO, Seung-Yong ,  LEE, Bit

IPC分类号： A61K31/522 ,  C07D487/04

摘要： The invention relates to a method of treatment of a patient with a ferrochelatase inhibitor, or a pharmaceutically acceptable salt thereof, or a derivative thereof. Also, the invention relates to a method of treatment of a patient with a ferrochelatase inhibitor that is a triazolopyrimidinone, or a derivative thereof, or a pharmaceutically acceptable salt thereof.

公开(公告)号：WO2019209811A1

公开(公告)日：2019-10-31

申请号：PCT/US2019/028697

申请日：2019-04-23

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： PURANDARE, Ashok V. ,  WAN, Honghe ,  HE, Liqi ,  GANGWAR, Sanjeev ,  POSY, Shoshana L. ,  POUDEL, Yam B. ,  SIVAPRAKASAM, Prasanna ,  CHOWDARI, Naidu S.

IPC分类号： C07D487/22 ,  A61K31/522

摘要： Compounds having a structure according to formula are modulators of TLR7 activity and can be used to treat conditions amenable to treatment by the modulation of TLR7 activity.

公开(公告)号：WO2019208805A1

公开(公告)日：2019-10-31

申请号：PCT/JP2019/018054

申请日：2019-04-26

申请人： 小野薬品工業株式会社

发明人： 有座　夕子

IPC分类号： A61K45/00 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/52 ,  A61K31/522 ,  A61P9/00 ,  A61P13/12 ,  A61P17/00 ,  A61P37/06 ,  A61P43/00

摘要： 本発明の課題は、有効な自己免疫疾患、なかでも天疱瘡、類天疱瘡、またはＡＮＣＡ関連血管炎の予防および／または治療剤を見出し、医薬品として提供することにある。　本発明に用いられるＢｔｋ阻害活性を有する化合物は、Ｂ細胞からの抗体産生抑制に加えて、好中球細胞外トラップ（ＮＥＴｓ：neutrophil extracellular traps）の形成を抑制するため、自己免疫疾患、なかでも天疱瘡、類天疱瘡、ネフローゼ症候群またはＡＮＣＡ関連血管炎の予防および／または治療に有用である。

公开(公告)号：WO2019183482A1

公开(公告)日：2019-09-26

申请号：PCT/US2019/023596

申请日：2019-03-22

申请人： THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM

发明人： SHAY, Jerry

IPC分类号： A61K31/7076 ,  A61K31/708 ,  A61K31/522 ,  A61P35/04

摘要： Brain tumors remain the leading cause of cancer-related deaths in children and often are associated with long-term sequelae among survivors of current therapies. Telomerase and telomeres play important roles in cancer, representing attractive therapeutic targets to treat children with poor-prognosis brain tumors such as diffuse intrinsic pontine glioma (DIPG), high-grade glioma (HGG) and high-risk medulloblastoma (MB). It has shown that DIPG, HGG and MB frequently express telomerase activity. It is now shown that the telomerase-dependent incorporation of 6-thio-2'deoxyguanosine (6-thio-dG), a telomerase substrate precursor analog, into telomeres leads to telomere dysfunction-induced foci (TIFs) along with extensive genomic DNA damage, cell growth inhibition and cell death of primary stem-like cells derived from patients with DIPG, HGG and MB. Importantly, the effect of 6-thio-dG is persistent even after drug withdrawal. Treatment with 6-thio-dG elicits a sequential activation of ATR and ATM pathways and induces G 2 /M arrest. In vivo , treatment of mice bearing MB xenografts with 6- thio-dG delays tumor growth, increases in-tumor TIFs and apoptosis. Furthermore, 6-thio-dG crosses the blood-brain barrier and specifically targets tumor cells in an orthotopic mouse model of DIPG. Together, these findings suggest that 6-thio-dG is a promising approach to treat therapy -resistant telomerase-positive pediatric brain tumors.

公开(公告)号：WO2019166432A1

公开(公告)日：2019-09-06

申请号：PCT/EP2019/054729

申请日：2019-02-26

申请人： F. HOFFMANN-LA ROCHE AG ,  HOFFMANN-LA ROCHE INC.

发明人： POESCHINGER, Thomas ,  RIES, Carola ,  SHEN, Hong ,  YUN, Hongying ,  HOVES, Sabine ,  HAGE, Carina

IPC分类号： A61K31/522 ,  A61P35/00

摘要： The present invention relates to compounds of formula (I), wherein R 1 , R 2 and R 3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, for (use in) the treatment and/or prophylaxis of liver cancer.

公开(公告)号：WO2019123482A8

公开(公告)日：2019-06-27

申请号：PCT/IN2018/050859

申请日：2018-12-19

申请人： IMPETIS BIOSCIENCES LTD.

发明人： MOOKHTIAR, Kasim ,  BASU, Sujay ,  ROUDURI, Sreekanth ,  MERU, Ashwin

IPC分类号： A61K31/519 ,  A61K31/522 ,  A61P35/00

摘要： The present disclosure discloses a pharmaceutical composition comprising compound of Formula I, Formula II, Formula III, Formula IV, and their pharmaceutically acceptable salts, analogs, tautomeric forms, stereoisomers, geometrical isomers, polymorphs, hydrates, solvates, metabolites, and prodrugs thereof, for the manufacture of a medicament for the treatment of a condition or disorder ameliorated by inhibition of the A 2A /A 2B receptor. It further discloses the use of the pharmaceutical composition of the present disclosure, for the preparation of a medicament for the treatment of a condition or disorder selected from prostate cancer, rectal cancer, renal cancer, ovarian cancer, endometrial cancer, thyroid cancer, pancreatic cancer, breast cancer, colon cancer, bladder cancer, brain cancer, glial cancer, melanoma cancer, pineal gland cancer, or lung cancer.