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公开(公告)号：US12064408B2
公开(公告)日：2024-08-20
申请号：US17326944
申请日：2021-05-21
发明人： Umut Ozcan , Joseph Majzoub , Ralph Mazitschek
IPC分类号： A61K31/198 , A61K31/19 , A61K31/192 , A61K31/194 , A61K31/195 , A61K38/22 , A61K45/06 , A61P3/04
CPC分类号： A61K31/198 , A61K31/19 , A61K31/192 , A61K31/194 , A61K31/195 , A61K38/2264 , A61K45/06 , A61P3/04 , A61K31/192 , A61K2300/00 , A61K31/194 , A61K2300/00 , A61K31/195 , A61K2300/00 , A61K31/198 , A61K2300/00 , A61K38/2264 , A61K2300/00
摘要： Pentacyclic triterpene weight loss agents are provided herein. Also provided are pharmaceutical formulations containing a therapeutically effective amount of one or more of the weight loss agents, or pharmaceutically acceptable salts or prodrugs thereof, in combination with one or more pharmaceutically acceptable excipients. The pharmaceutical formulations can be administered to a pre-obese, obese, or morbidly obese patient to induce weight loss, reduce body fat, reduce food intake, improve glucose homeostasis, prevent obesity, or a combination thereof. The weight loss agents can also be co-administered with leptin or a leptin analog.
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公开(公告)号：US20230341394A1
公开(公告)日：2023-10-26
申请号：US18020800
申请日：2021-08-16
申请人： DANA-FARBER CANCER INSTITUTE, INC. , THE GENERAL HOSPITAL CORPORATION , PRESIDENT AND FELLOWS OF HARVARD COLLEGE
发明人： Eric Fischer , Radoslaw Nowak , Hong Yue , Daan Overwijn , Ralph Mazitschek , Neil Connor Payne
IPC分类号： G01N33/569 , G01N33/542
CPC分类号： G01N33/56983 , G01N33/542 , G01N2333/165 , G01N2469/20
摘要： The present invention relates to a homogeneous, time resolved, Förster resonance energy transfer (TR-FRET)-based method for detection of SARS-CoV-2, SARS CoV-1, and MERS-CoV antibodies in a patient fluid sample.
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公开(公告)号：USRE49240E1
公开(公告)日：2022-10-11
申请号：US16815755
申请日：2020-03-11
IPC分类号： C07C237/40 , A61K31/167 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/455 , A61K31/4965 , A61K31/505 , A61K31/69 , A61K38/05 , A61K45/06 , C07C237/42 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24
摘要： The present invention relates to compounds which inhibit histone deacetylase activity and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to methods of treating and preventing hematological cell proliferative disorders, such as multiple myeloma, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
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公开(公告)号：US10696695B2
公开(公告)日：2020-06-30
申请号：US16017638
申请日：2018-06-25
IPC分类号： C07F5/02 , C07D257/08 , A61K51/04 , G01N33/534
摘要： This invention relates to water-soluble mono-alkoxy and mono-alkyne BODIPY derivatives, including methods for making the same. For examples, provided herein are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: is a BODIPY ligand system; X is a halogen; L is absent or a linker; and Z is selected from the group consisting of: a group reactive with a biologically active molecule and a detectable agent.
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5.发明申请公开(公告)号：US20190072562A1
公开(公告)日：2019-03-07
申请号：US16179177
申请日：2018-11-02
摘要： A multiphoton fluorescence anisotropy microscopy live cell imaging system and method to measure and map drug-target interaction in real time at subcellular resolution. Proposed modality enables a direct measurement of drug/target binding in vivo, high-resolution spatial and temporal mapping of bound and unbound drug distribution, and presents an versatile tool to enhance understanding of drug activity. Application of the system to measurement of intracellular target engagement of the chemotherapeutic Olaparib, a poly(ADP-ribose) polymerase inhibitor, in live cells and within a tumor in vivo.
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公开(公告)号：US09988343B2
公开(公告)日：2018-06-05
申请号：US15034276
申请日：2014-11-05
IPC分类号： A61K31/4406 , A61K31/167 , A61K31/69 , C07C237/40 , C07D213/82 , C07D241/24 , A61K38/05 , A61K45/06 , A61K31/4402 , A61K31/4409 , A61K31/455 , A61K31/4965 , A61K31/505 , C07D213/81 , C07D239/42 , C07C237/42
CPC分类号： C07C237/40 , A61K31/167 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/455 , A61K31/4965 , A61K31/505 , A61K31/69 , A61K38/05 , A61K45/06 , C07C237/42 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , A61K2300/00
摘要： The present invention relates to compounds which inhibit histone deacetylase activity and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to methods of treating and preventing hematological cell proliferative disorders, such as multiple myeloma, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
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公开(公告)号：US09968575B2
公开(公告)日：2018-05-15
申请号：US14431412
申请日：2013-09-26
发明人： Umut Ozcan , Joseph Majzoub , Ralph Mazitschek , Isin Cakir , Serkan Cabi
IPC分类号： C07C62/38 , A61K31/198 , A61K31/192 , A61K31/194 , A61K31/195 , A61K38/22 , A61K31/19 , A61K45/06
CPC分类号： A61K31/198 , A61K31/19 , A61K31/192 , A61K31/194 , A61K31/195 , A61K38/2264 , A61K45/06 , A61K2300/00
摘要： Pentacyclic triterpene weight loss agents are provided herein. Also provided are pharmaceutical formulations containing a therapeutically effective amount of one or more of the weight loss agents, or pharmaceutically acceptable salts or prodrugs thereof, in combination with one or more pharmaceutically acceptable excipients. The pharmaceutical formulations can be administered to a pre-obese, obese, or morbidly obese patient to induce weight loss, reduce body fat, reduce food intake, improve glucose homeostasis, prevent obesity, or a combination thereof. The weight loss agents can also be co-administered with leptin or a leptin analog.
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公开(公告)号：US20150284356A1
公开(公告)日：2015-10-08
申请号：US14408605
申请日：2013-06-21
申请人： Whatehead Institute for Biomedical Research , The General Hospital Corporation d/b/a Massachusetts General Hospital
IPC分类号： C07D311/08 , C07D263/57 , C07D213/75 , C07D277/64 , C07C233/29 , C07D213/643
CPC分类号： C07D311/08 , A61K45/06 , C07C233/29 , C07C235/24 , C07C235/38 , C07D213/643 , C07D213/75 , C07D263/57 , C07D263/58 , C07D277/64 , C07D277/82 , C07D311/16
摘要： The present invention provides compounds of Formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting fungal or parasitic growth. The compounds are useful as inhibitors of glycosylphosphatidylinositol (GPI)-anchor biosynthesis, in particular, as inhibitors of fungal Gwt1 activity. The present invention further provides methods of using the compounds described herein for treating fungal or parasitic infections. The compounds can also be used as biological probes to study the effects of inhibiting Gwt1 activity.
摘要翻译： 本发明提供式I化合物，其药学上可接受的盐及其药物组合物。 本发明的化合物可用于抑制真菌或寄生生长。 该化合物可用作糖基磷脂酰肌醇（GPI） - 锚定生物合成的抑制剂，特别是作为真菌Gwt1活性的抑制剂。 本发明还提供使用本文所述化合物治疗真菌或寄生虫感染的方法。 该化合物也可用作生物探针来研究抑制Gwt1活性的作用。
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9.发明申请HALOFUGINOL DERIVATIVES AND THEIR USE IN COSMETIC AND PHARMACEUTICAL COMPOSITIONS 审中-公开化学药物衍生物及其在化妆品和药物组合物中的应用公开(公告)号：US20150057297A1
公开(公告)日：2015-02-26
申请号：US14371934
申请日：2013-01-11
申请人： President and Fellows of Harvard College , The General Hospital Corporation d/b/a Massachusetts General Hospital
发明人： Malcolm Whitman , Tracy Keller , Ralph Mazitschek
IPC分类号： C07D401/06 , A61Q19/06 , A61Q19/00 , A61K8/49
CPC分类号： C07D401/06 , A61K8/4953 , A61K31/517 , A61K45/06 , A61Q19/00 , A61Q19/06 , Y02A50/411 , A61K2300/00
摘要： The present invention provides halofuginol, and derivatives and salts thereof, including diasteromerically enriched compositions thereof. The invention also provides pharmaceutical and cosmetic compositions thereof as well as methods for using halofuginol and derivatives thereof in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, malaria, ischemic damage, transplant rejection, neurodegenerative diseases, T-cell neoplasms, and cosmetic conditions.
摘要翻译： 本发明提供卤代吡喃醇及其衍生物和盐，包括非对映体富集的组合物。 本发明还提供了其药物和化妆品组合物以及使用卤氟丙醇及其衍生物治疗慢性炎性疾病，自身免疫性疾病，干眼症，纤维化，瘢痕形成，血管发生，病毒感染，疟疾，缺血性损伤，移植排斥， 神经变性疾病，T细胞肿瘤和美容条件。
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公开(公告)号：US11708353B2
公开(公告)日：2023-07-25
申请号：US16973080
申请日：2019-06-10
IPC分类号： C07D241/28 , C07D403/12 , C07D405/12 , A61P33/02 , C07D401/12 , C07D401/14
CPC分类号： C07D403/12 , A61P33/02 , C07D241/28 , C07D401/12 , C07D401/14 , C07D405/12
摘要： The present application provides compounds, such as compounds of Formula Ia, which are inhibitors of aminoacyl tRNA-synthetase (e.g., prolyl-tRNA-synthetase), and which are useful for treating disorders associated with aminoacyl tRNA-synthetase activity and/or expression. Pharmaceutical compositions comprising the compounds and methods of using the compounds are also provided.
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