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1. 发明专利

IL292466D0 Isoquinolinone derivatives, method for preparing the same, and pharmaceutical composition for preventing or treating poly(adp-ribose) polymerase-1-related diseases, comprising the same as active ingredient 未知
公开(公告)号：IL292466D0
公开(公告)日：2022-06-01
申请号：IL29246622
申请日：2022-04-25
申请人： DIGMBIO INC , KIM EUNHEE , PARK CHANGMIN , OH SEHWAN , KIM YOUNGHOON , LEE JUHEE , SEOL JAEHEE , SHIM AHRAM , KIM YOUNGGWAN , KOO TAE SUNG , JANG KI HONG
发明人： KIM EUNHEE , PARK CHANGMIN , OH SEHWAN , KIM YOUNGHOON , LEE JUHEE , SEOL JAEHEE , SHIM AHRAM , KIM YOUNGGWAN , KOO TAE-SUNG , JANG KI-HONG
IPC分类号： A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/55 , A61P27/02
摘要： The present invention relates to an isoquinolinone derivative, a preparation method therefor, and a pharmaceutical composition, comprising same as an active ingredient, for prevention or treatment of a poly(ADP-ribose)polymerase-1 (PARP-1)-associated disease. At a nano-molar concentration, the isoquinolinone derivative exhibits an excellent PARP-1 inhibition effect and, furthermore, an excellent cytoprotective effect (cell death preventing effect) against an eye disease or disorder, in detail, a retinal disease. Thus, a pharmaceutical composition comprising same as an active ingredient can be advantageously used for preventing or treating a PARP-1-associated disease, for example, an eye disease or disorder.

2. 发明专利

IL292466A Isoquinolinone derivatives, method for preparing the same, and pharmaceutical composition for preventing or treating poly(adp-ribose) polymerase-1-related diseases, comprising the same as active ingredient 未知
公开(公告)号：IL292466A
公开(公告)日：2022-06-01
申请号：IL29246622
申请日：2022-04-25
申请人： DIGMBIO INC , KIM EUNHEE , PARK CHANGMIN , OH SEHWAN , KIM YOUNGHOON , LEE JUHEE , SEOL JAEHEE , SHIM AHRAM , KIM YOUNGGWAN , KOO TAE SUNG , JANG KI HONG
发明人： KIM EUNHEE , PARK CHANGMIN , OH SEHWAN , KIM YOUNGHOON , LEE JUHEE , SEOL JAEHEE , SHIM AHRAM , KIM YOUNGGWAN , KOO TAE-SUNG , JANG KI-HONG
摘要： The present invention relates to isoquinolinone derivatives, a method for preparing the same, and a pharmaceutical composition for preventing or treating poly(ADP-ribose) polymerase-1 (PARP-1)-related diseases containing the same as an active ingredient. The isoquinolinone derivatives exhibit an excellent PARP-1 inhibitory effect at a concentration of nanomolar units, and further exhibit an excellent cytoprotective effect (apoptosis inhibitory effect) on ophthalmic diseases or disorders, specifically retinal disorders, and thus can be effectively used as a pharmaceutical composition for preventing or treating PARP-1-related diseases, for example, ophthalmic diseases or disorders, which contains the same as an active ingredient.

3. 发明申请

WO2008060557A2 EFFICIENT NUCLEAR DELIVERY OF ANTISENSE OLIGONUCLEOTIDES 审中-公开
标题翻译：反式寡核苷酸的有效核输送
公开(公告)号：WO2008060557A2
公开(公告)日：2008-05-22
申请号：PCT/US2007/023894
申请日：2007-11-14
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA , TEWARI, Manorama , KIM, Younghoon , DISCHER, Dennis
发明人： TEWARI, Manorama , KIM, Younghoon , DISCHER, Dennis
IPC分类号： A61K48/00
CPC分类号： C12N15/88 , A61K9/1273 , A61K48/00 , C12N15/111 , C12N2310/11 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2320/32 , C12N2310/3521
摘要： Provided is a biocompatible polyethylene oxide (PEO)-based polymersome system for the delivery of oligonucleotides, including antisense RNA, siRNA and RNAi, to a cell or tissue target, and method of use therefore, wherein the method comprises encapsulating the oligonucleotide in a biodegradable neutral, nano-transforming polymersome delivery vehicle and delivering the encapsulated oligonucleotide to the cell or tissue target in vitro or in vivo., particularly for treating a disease, such cancer or cellular hyperproliferation. The degradable polymersome, and the oligonucleotides stably encapsulated therein are taken up passively by cells and delivered into endolysosomes, wherein the polymersomes decompose at a known rate at a known pH, thereby releasing encapsulated oligonucleotides in a controlled manner within the cell and facilitating delivery of antisense oligonucleotide or siRNA or RNAi into the nucleus of the cell target.
摘要翻译：提供用于将寡核苷酸（包括反义RNA，siRNA和RNAi）递送至细胞或组织靶标的生物相容性聚环氧乙烷（PEO）基聚合物体系统及其使用方法，其中所述方法包括将寡核苷酸包封在可生物降解的中性纳米转化聚合物体递送载体中，并将包封的寡核苷酸体外或体内递送至细胞或组织靶标，特别是用于治疗疾病如癌症或细胞过度增殖。可降解聚合物囊泡和其中稳定包封的寡核苷酸被细胞被动吸收并递送到内溶酶体中，其中聚合物囊泡以已知的速率在已知pH下分解，从而以受控方式在细胞内释放包封的寡核苷酸并促进反义寡核苷酸或siRNA或RNAi进入细胞靶标的细胞核。

4. 发明申请

WO2011068288A1 AGENT FOR PREVENTION OR TREATMENT OF BENIGN PROSTATIC HYPERPLASIA COMPRISING A QUINAZOLINE DERIVATIVE 审中-公开
标题翻译：用于预防或治疗包含喹唑啉衍生物的BENIGN PROSTATIC HYPERPLASIA的药剂
公开(公告)号：WO2011068288A1
公开(公告)日：2011-06-09
申请号：PCT/KR2010/002240
申请日：2010-04-12
申请人： CHONG KUN DANG PHARMACEUTICAL CORP. , LEE, Sungsook , LEE, Jeakwang , CHOI, Hojin , KIM, Younghoon , LEE, Kyung Joo , MOON, Seungkee , KIM, Soojin , HA, Nina , KIM, Semi , HWANG, Inchang , KIM, Dalhyun , KANG, Sungkwon , LEE, Hongwoo , IM, Daisig , LEE, Seonwoo , KIM, Youngmin , LIM, Intaek , YU, Hosung
发明人： LEE, Sungsook , LEE, Jeakwang , CHOI, Hojin , KIM, Younghoon , LEE, Kyung Joo , MOON, Seungkee , KIM, Soojin , HA, Nina , KIM, Semi , HWANG, Inchang , KIM, Dalhyun , KANG, Sungkwon , LEE, Hongwoo , IM, Daisig , LEE, Seonwoo , KIM, Youngmin , LIM, Intaek , YU, Hosung
IPC分类号： A61K31/517 , A61P13/08 , A61K47/12
CPC分类号： A61K31/517
摘要： The present invention provides a prophylactic or therapeutic agent for benign prostatic hyperplasia (BPH) and accompanying lower urinary tract symptoms (LUTS), comprising a quinazoline derivative as an active ingredient. Further, the present invention provides a composition comprising a quinazoline derivative for use in the treatment or prevention of BPH and LUTS, and a method for preventing or treating BPH and LUTS, including administering an agent or a composition comprising a quinazoline derivative to a mammal including a human. The BPH prophylactic or therapeutic agent or composition ofthe present invention has excellent PDE5 inhibitory effects, exhibits low inhibitory activity on PDE6 and PDE11 at a dose exhibiting PDE5 inhibitory activity, thus providing less side effects, has a moderate blood half-life as compared to other PDE5 inhibitors and therefore can exert sufficient medicinal efficacy even with single administration/day without risk of drug accumulation,thus providing increased drug compliance and excellent metabolic stability.
摘要翻译：本发明提供了一种包含喹唑啉衍生物作为活性成分的良性前列腺增生（BPH）和伴随的下尿路症状（LUTS）的预防或治疗剂。此外，本发明提供了包含用于治疗或预防BPH和LUTS的喹唑啉衍生物的组合物，以及预防或治疗BPH和LUTS的方法，包括向哺乳动物施用包含喹唑啉衍生物的试剂或组合物，包括一个人。本发明的BPH预防或治疗剂或组合物具有优异的PDE5抑制作用，对PDE6和PDE11的抑制活性低，呈现PDE5抑制活性，因此具有较少的副作用，与其他药物相比具有适度的血液半衰期 PDE5抑制剂，因此即使在单次给药/天也可以发挥足够的药用效果，而没有药物积聚的风险，从而提供增加的药物依从性和优异的代谢稳定性。

5. 发明申请

WO2008060557A3 EFFICIENT NUCLEAR DELIVERY OF ANTISENSE OLIGONUCLEOTIDES 审中-公开
标题翻译：有效的核交付反义寡核苷酸
公开(公告)号：WO2008060557A3
公开(公告)日：2008-11-27
申请号：PCT/US2007023894
申请日：2007-11-14
申请人： UNIV PENNSYLVANIA , TEWARI MANORAMA , KIM YOUNGHOON , DISCHER DENNIS
发明人： TEWARI MANORAMA , KIM YOUNGHOON , DISCHER DENNIS
IPC分类号： A61K48/00
CPC分类号： C12N15/88 , A61K9/1273 , A61K48/00 , C12N15/111 , C12N2310/11 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2320/32 , C12N2310/3521
摘要： Provided is a biocompatible polyethylene oxide (PEO)-based polymersome system for the delivery of oligonucleotides, including antisense RNA, siRNA and RNAi, to a cell or tissue target, and method of use therefore, wherein the method comprises encapsulating the oligonucleotide in a biodegradable neutral, nano-transforming polymersome delivery vehicle and delivering the encapsulated oligonucleotide to the cell or tissue target in vitro or in vivo., particularly for treating a disease, such cancer or cellular hyperproliferation. The degradable polymersome, and the oligonucleotides stably encapsulated therein are taken up passively by cells and delivered into endolysosomes, wherein the polymersomes decompose at a known rate at a known pH, thereby releasing encapsulated oligonucleotides in a controlled manner within the cell and facilitating delivery of antisense oligonucleotide or siRNA or RNAi into the nucleus of the cell target.
摘要翻译：提供了一种用于向细胞或组织靶标递送包括反义RNA，siRNA和RNAi的寡核苷酸的生物相容性聚环氧乙烷（PEO）基聚合物体系，以及因此使用的方法，其中所述方法包括将寡核苷酸包封在可生物降解中性的纳米转化聚合物组递送载体，并将包封的寡核苷酸在体外或体内递送至细胞或组织靶，特别是用于治疗疾病，例如癌症或细胞过度增殖。稳定包被的可降解聚合物和寡核苷酸被细胞无源地吸收并递送到内溶体中，其中聚合物囊泡以已知的速率以已知的pH分解，从而以受控的方式在细胞内释放包封的寡核苷酸并促进反义寡核苷酸或siRNA或RNAi进入细胞靶的细胞核。

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