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1.发明授权
公开(公告)号：EP2702054B1
公开(公告)日：2018-10-24
申请号：EP12776252.4
申请日：2012-04-26
IPC分类号： C07D215/46 , A61K31/4709 , A61P29/00 , A61P35/00 , A61P33/06
CPC分类号： C07D215/46 , A61K31/4709 , A61K45/06 , A61P29/00 , A61P33/06 , A61P35/00 , C07D401/12 , C07D401/14 , Y02A50/411 , A61K31/4725 , A61K2300/00
摘要： The present invention relates to novel bisaminoquinoline compounds, pharmaceutical compositions comprising these novel compounds and methods for inhibiting autophagy in biological systems. Methods of treating cancer in patients in need using compounds and/or compositions according to the present invention alone or in combination with at least one additional anticancer agent represent additional aspects of the invention. Methods of treating disease states and/or conditions in which inhibition of autophagy plays a favorable treatment role including rheumatoid arthritis, malaria, antiphospholipid antibody syndrome, lupus, chronic urticaria and Sjogren's disease, with compounds according to the present invention represent additional aspects of the invention.
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公开(公告)号：EP3976039A1
公开(公告)日：2022-04-06
申请号：EP20815000.3
申请日：2020-05-24
IPC分类号： A61K31/473 , A61P35/00 , C07D219/12
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公开(公告)号：EP3471722A1
公开(公告)日：2019-04-24
申请号：EP17813776.6
申请日：2017-05-31
IPC分类号： A61K31/435 , C07D221/06
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4.发明公开COMPOSITIONS AND METHODS FOR INCREASING, OR PREVENTING OR REVERSING LOSS OF, SKIN PIGMENTATION IN A MAMMALIAN SUBJECT 审中-公开增加或防止或消除哺乳动物皮肤色素沉着损失的组合物和方法
公开(公告)号：EP3280702A1
公开(公告)日：2018-02-14
申请号：EP16777191.4
申请日：2016-04-06
CPC分类号： C07D405/04 , A61K8/49 , A61P17/00 , A61P17/06 , A61P17/14 , A61P17/16 , A61P17/18 , A61Q17/04 , A61Q19/02 , C07D221/16 , C07D491/048
摘要： The present invention includes compounds, compositions comprising the same, and methods using the compounds and/or compositions therein, for modulating skin pigmentation in a mammalian subject. In certain embodiments, the compounds of the invention treat or prevent skin disorders or diseases associated with hyperpigmentation in the subject. In other embodiments, the compounds of the invention act as antagonist to the non-canonical sex steroid hormone receptor GPRE1 and do not bind to a canonical nuclear estrogen receptor (ER). In yet other embodiments, the compounds of the invention comprise acts as agonists to the non-canonical sex steroid hormone receptor PAQR7 and do not bind to a canonical nuclear progesterone receptor (PR).
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公开(公告)号：EP4327879A2
公开(公告)日：2024-02-28
申请号：EP23205273.8
申请日：2017-05-31
IPC分类号： A61P35/00
摘要： The present invention includes compounds, compositions and methods that are useful for preventing or treating melanoma or any other Myc-expressing cancer in a subject. In certain embodiments, the compounds comprise estrogen (including estrogen derivatives or analogues), a selective GPER agonist and/or another small molecule G-protein coupled receptor (GPCR) agonist that increases cancer cell differentiation.
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公开(公告)号：EP4327879A3
公开(公告)日：2024-05-22
申请号：EP23205273.8
申请日：2017-05-31
IPC分类号： A61K31/473 , A61K39/395 , A61P35/00
CPC分类号： A61K45/06 , C07D221/16 , C07D491/08 , C07D221/22 , C07D405/04 , C07D409/04 , C07D491/056 , A61K39/3955 , C07K16/2818 , A61K2039/50520130101 , C07K2317/7620130101 , A61P35/00 , A61P35/02 , A61K38/15 , A61K31/473 , A61K2300/0020130101
摘要： The present invention includes compounds, compositions and methods that are useful for preventing or treating melanoma or any other Myc-expressing cancer in a subject. In certain embodiments, the compounds comprise estrogen (including estrogen derivatives or analogues), a selective GPER agonist and/or another small molecule G-protein coupled receptor (GPCR) agonist that increases cancer cell differentiation.
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公开(公告)号：EP3856184A1
公开(公告)日：2021-08-04
申请号：EP19864249.8
申请日：2019-09-26
IPC分类号： A61K31/498 , A61P25/28 , C07D241/44
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8.发明公开
公开(公告)号：EP3848355A1
公开(公告)日：2021-07-14
申请号：EP21158586.4
申请日：2015-08-07
IPC分类号： C07D215/42 , C07D401/12 , C07D401/14 , A61K31/4706 , A61K31/4709 , A61P35/00 , A61P33/06 , A61P31/06 , A61P29/00 , A61P19/04 , C07D215/46 , A61K31/436 , A61K31/4375 , A61K31/4545 , A61K31/4745 , A61K31/4995 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/704 , A61K31/7056
摘要： The invention provides novel asymmetric and symmetric bisaminoquinolines and related compounds, methods of treatment and syntheses. The novel compounds exhibit effective anticancer activity and are useful in the treatment of a variety of autophagy-related disorders.
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9.发明公开DIMERIC QUINACRINE DERIVATIVES AS AUTOPHAGY INHIBITORS FOR CANCER THERAPY 审中-公开二甲基喹啉衍生物作为癌症治疗的自体抑制剂
公开(公告)号：EP3283463A1
公开(公告)日：2018-02-21
申请号：EP16780921.9
申请日：2016-04-26
IPC分类号： C07D219/12 , A61K31/473 , A61P35/00
CPC分类号： C07D219/12 , A61K31/473 , A61K31/7068 , A61K45/06 , A61P17/00 , A61P19/02 , A61P33/06 , A61P35/00 , A61P35/04 , A61P37/00 , Y02A50/411 , A61K2300/00
摘要： The invention provides dimeric quinacrine derivatives and related compounds and compositions, methods of treatment and syntheses. The novel compounds exhibit unexpected anticancer activity and are useful in the treatment of a variety of autophagy-related disorders.
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10.发明公开ASYMMETRIC BISAMINOQUINOLINES AND BISAMINOQUINOLINES WITH VARIED LINKERS AS AUTOPHAGY INHIBITORS FOR CANCER AND OTHER THERAPY 审中-公开不对称BISAMINOCHINOLINE和BISAMINOCHINOLINE具有不同于LINKERS AUTOPHAGIEINHIBITOREN癌症和其他疗法
公开(公告)号：EP3177595A1
公开(公告)日：2017-06-14
申请号：EP15830607.6
申请日：2015-08-07
IPC分类号： C07D215/42 , C07D401/12 , C07D401/14 , A61K31/4706 , A61K31/4709 , A61P35/00 , A61P33/06 , A61P31/06 , A61P29/00 , A61P19/04
CPC分类号： C07D215/46 , A61K31/436 , A61K31/4375 , A61K31/4545 , A61K31/4706 , A61K31/4709 , A61K31/4745 , A61K31/4995 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/704 , A61K31/7056 , C07D401/12 , Y02A50/411 , A61K2300/00
摘要： The invention provides novel asymmetric and symmetric bisaminoquinolmes and related compounds, methods of treatment and syntheses. The novel compounds exhibit effective anticancer activity and are useful in the treatment of a variety of autophagy-related disorders.
摘要翻译： 本发明提供了新颖的非对称和对称bisaminoquinolmes和相关的化合物，治疗和合成的方法。 所述的新化合物显示出有效的抗癌活性，并且在多种自噬相关病症的治疗中是有用的。
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