公开(公告)号：US11542450B2

公开(公告)日：2023-01-03

申请号：US16661822

申请日：2019-10-23

申请人： Thomas Daly

发明人： Thomas Daly

IPC分类号： C10L1/2387 ,  C10L1/233 ,  C10L1/26 ,  C10L1/24 ,  C10L1/222 ,  C07C205/15 ,  C07C205/40 ,  C07C215/08 ,  C07C217/08 ,  C07C217/28 ,  C07C217/48 ,  C07C219/06 ,  C07C219/22 ,  C07C229/12 ,  C07C229/22 ,  C07C309/14 ,  C07D213/74 ,  C07D295/088 ,  C07D295/15 ,  C07F9/09 ,  C07F9/38 ,  C07F9/58 ,  C09K3/00 ,  C10L1/10 ,  C10L1/22 ,  C10L1/238 ,  C11D1/66

摘要： Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

公开(公告)号：US11541029B2

公开(公告)日：2023-01-03

申请号：US13133021

申请日：2009-12-04

申请人： Chongxi Yu

发明人： Chongxi Yu

IPC分类号： C07C15/30 ,  C07C15/38 ,  A61K8/31 ,  A61K31/015 ,  A61K31/352 ,  C07D215/18 ,  A61K47/54 ,  C07D209/42 ,  C07D295/088 ,  C07D211/34 ,  C07D231/14 ,  C07D313/14 ,  C07D417/04 ,  C07D491/048 ,  C07D501/22 ,  C07D277/56 ,  C07D207/34

摘要： High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

公开(公告)号：US20220363666A1

公开(公告)日：2022-11-17

申请号：US17200743

申请日：2021-03-12

申请人： Black Diamond Therapeutics, Inc.

发明人： Alexander FLOHR ,  Alexander MAYWEG ,  George TRAINOR ,  David M. EPSTEIN ,  Matthew O'CONNOR ,  Elizabeth BUCK ,  Luca ARISTA

IPC分类号： C07D401/14 ,  C07D239/74 ,  C07D295/088 ,  C07D295/13 ,  C07D401/12 ,  C07D405/14 ,  C07D417/14 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/048 ,  C07D491/08 ,  C07D491/107

摘要： The present disclosure relates to new compounds or pharmaceutically acceptable salts or stereoisomers thereof of formula I as inhibitors of receptor tyrosine kinases (RTK), in particular extracellular mutants of ErbB-receptors. The present disclosure also relates to methods of preparation these compounds, compositions comprising these compounds, and methods of using them in the treatment of cancer in mammals (e.g. humans).

公开(公告)号：US20220356190A1

公开(公告)日：2022-11-10

申请号：US17547118

申请日：2021-12-09

申请人： Alkermes Pharma Ireland Limited

发明人： Tarek A. Zeidan ,  Scott Duncan ,  Christopher P. Hencken ,  Thomas Andrew Wynn ,  Carlos N. Sanrame

IPC分类号： C07D491/113 ,  A61K31/4015 ,  C07D207/40 ,  C07D207/12 ,  C07C229/12 ,  C07C229/18 ,  C07C317/18 ,  C07C317/28 ,  C07D207/408 ,  C07D211/92 ,  C07D295/088

摘要： The present invention provides compounds of formula (I), wherein:
R1 is unsubstituted C1-C6 alkyl;
La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and
R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10aryl;
or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.

公开(公告)号：US20220098162A1

公开(公告)日：2022-03-31

申请号：US17427629

申请日：2020-08-27

申请人： Henan Radiomedical Science and Technology Co., Ltd

发明人： Xuejun Xu ,  Yupo Yang ,  Zhengyan Yang

IPC分类号： C07D295/088

摘要： In view of the lack of anti-cancer targeted drugs in the prior art, the invention provides a naphthylamine compound and a biologically acceptable salt thereof, a preparation method thereof, and an application thereof. The naphthylamine compound and the biologically acceptable salt thereof provided by the invention can bind to protein sites related to tumor diseases in organisms through functional groups in the structure, and have hydrogen bonds and hydrophobic interactions with receptors, so as to achieve the purpose of inhibiting tumor cell proliferation.

公开(公告)号：US20210403432A1

公开(公告)日：2021-12-30

申请号：US17285413

申请日：2019-10-14

申请人： CK Biotech Inc.

发明人： Kang-Yell Choi ,  Seol Hwa Seo ,  Eunhwan Kim

IPC分类号： C07D215/38 ,  C07D487/04 ,  C07D471/04 ,  C07D207/44 ,  C07D513/04 ,  C07D239/42 ,  C07D498/04 ,  C07D209/40 ,  C07D217/16 ,  C07C229/36 ,  C07D309/38 ,  C07D311/30 ,  C07C237/48 ,  C07C39/215 ,  C07D295/088 ,  C07D487/22 ,  A61P3/04 ,  A61P3/10 ,  G01N33/68

摘要： Therapeutic compositions comprising one or more agents that inhibit CXXC5-DVL interface, and methods of administering those therapeutic compositions to model, treat, reduce resistance to treatment, prevent, and diagnose a condition/disease associated with a metabolic disease or a related clinical condition thereof, are disclosed.

公开(公告)号：US20210387957A1

公开(公告)日：2021-12-16

申请号：US17404589

申请日：2021-08-17

申请人： The University of British Columbia ,  Provincial Health Services Authority

发明人： Raymond J. Andersen ,  Marianne Dorothy Sadar ,  Kunzhong Jian ,  Nasrin R. Mawji ,  Jun Wang ,  Carmen Adriana Banuelos ,  Yu-Chi Yang

IPC分类号： C07D295/088 ,  C07C311/51 ,  C07C69/28 ,  C07C233/18 ,  C07C311/04 ,  A61K31/09 ,  A61K31/10 ,  A61K31/145 ,  A61K31/4164 ,  A61K31/5375 ,  A61K45/06 ,  C07C43/23 ,  C07C317/18 ,  C07C317/22 ,  C07C317/28 ,  C07D233/60

摘要： Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R11a, R11b, R11c, R11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

公开(公告)号：US20210371384A1

公开(公告)日：2021-12-02

申请号：US16962751

申请日：2019-01-30

申请人： The Regents of the University of California

发明人： Michael E. Jung ,  Xiaohong Chen ,  Cun-Yu Wang ,  Jiong Li ,  Jie Zheng

IPC分类号： C07D213/68 ,  C07D405/14 ,  C07D409/14 ,  C07D401/14 ,  C07D401/06 ,  C07D211/86 ,  C07D295/15 ,  C07C237/04 ,  C07C235/62 ,  C07D401/12 ,  C07D295/088 ,  C07D213/89 ,  C07C311/07 ,  A61P35/00

摘要： The present disclosure relates to compounds that are capable of modulating the WNT/Beta-Catenin pathway. The disclosure further relates to methods of treating colorectal cancer and other WNT/Beta-Catenin mediated cancers.

公开(公告)号：US11186564B2

公开(公告)日：2021-11-30

申请号：US16322278

申请日：2016-08-04

申请人： Sunovion Pharmaceuticals Inc.

发明人： Michele L. R. Heffernan ,  Larry Wendell Hardy ,  Scott P. Brown ,  Lee W. Herman

IPC分类号： C07D211/22 ,  C07D401/08 ,  C07D401/14 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D471/04 ,  C07D487/10 ,  C07D491/107 ,  C07D311/22 ,  C07D217/24 ,  C07D223/08 ,  C07D235/12 ,  C07D237/14 ,  C07D413/06 ,  C07D241/04 ,  C07D243/08 ,  C07D471/08 ,  C07D491/048 ,  C07D267/10 ,  C07D275/04 ,  C07D211/58 ,  C07D403/06 ,  C07D405/12 ,  A61P25/28 ,  C07D417/04 ,  A61P25/18 ,  C07D513/04 ,  C07D211/42 ,  C07D295/104 ,  C07D207/36 ,  C07D213/81 ,  C07D491/20 ,  C07D249/12 ,  C07D221/20 ,  C07D295/088 ,  C07D311/58 ,  C07D207/12 ,  C07D211/44 ,  C07D265/30 ,  C07D277/66 ,  C07D295/027 ,  C07D295/073 ,  C07D295/096 ,  C07D295/108 ,  C07D307/83 ,  C07D311/08 ,  C07D413/08 ,  C07D471/10

摘要： Compounds of formula I: are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disorders in a patient in need are also disclosed. Such disorders include depression, bipolar disorder, pain, schizophrenia, obsessive compulsive disorder, addiction, social disorder, attention deficit hyperactivity disorder, an anxiety disorder, autism, a cognitive impairment, or a neuropsychiatric symptom such as apathy, depression, anxiety, psychosis, aggression, agitation, impulse control disorders, and sleep disorders in neurological disorders such as Alzheimer's and Parkinson's diseases.

公开(公告)号：US20210323922A1

公开(公告)日：2021-10-21

申请号：US17098171

申请日：2020-11-13

申请人： Gilead Sciences, Inc.

发明人： Evangelos Aktoudianakis ,  Todd Appleby ,  Aesop Cho ,  Zhimin Du ,  Michael Graupe ,  Juan A. Guerrero ,  Salman Y. Jabri ,  Lateshkumar Thakorlal Lad ,  Paulo A. Machicao Tello ,  Jonathan William Medley ,  Samuel E. Metobo ,  Prasenjit Kumar Mukherjee ,  Devan Naduthambi ,  Gregory Notte ,  Eric Q. Parkhill ,  Barton W. Phillips ,  Scott Preston Simonovich ,  Neil H. Squires ,  Chandrasekar Venkataramani ,  Peiyuan Wang ,  William J. Watkins ,  Jie Xu ,  Kin Shing Yang ,  Christopher Allen Ziebenhaus

IPC分类号： C07D213/69 ,  A61K45/06 ,  A61K31/444 ,  C07D401/14 ,  A61K31/5377 ,  C07D213/85 ,  A61K31/44 ,  C07D213/30 ,  C07D295/088 ,  A61K31/4545 ,  C07D401/04 ,  A61K31/497 ,  C07D519/00 ,  C07D487/10 ,  C07D487/08 ,  C07D213/64 ,  C07D491/107 ,  C07D498/04 ,  C07D213/61 ,  C07D405/14

摘要： Compounds according to formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.