公开(公告)号：US11958822B2

公开(公告)日：2024-04-16

申请号：US17965914

申请日：2022-10-14

申请人： CORSAIR PHARMA, INC.

发明人： Cyrus K. Becker ,  Meenakshi S. Venkatraman ,  Xiaoming Zhang ,  Jürg R. Pfister ,  Gwenaella Rescourio

IPC分类号： C07D321/00 ,  A61K9/00 ,  A61K9/70 ,  A61K31/165 ,  A61K31/216 ,  A61K31/341 ,  A61K31/365 ,  A61K45/06 ,  C07C59/72 ,  C07C69/712 ,  C07C69/734 ,  C07C69/74 ,  C07C69/96 ,  C07C219/16 ,  C07C235/20 ,  C07D207/08 ,  C07D211/60 ,  C07D257/06 ,  C07D263/24 ,  C07D263/26 ,  C07D265/30 ,  C07D295/088 ,  C07D295/145 ,  C07D307/20 ,  C07D317/34 ,  C07D317/40 ,  C07D453/02

CPC分类号： C07D321/00 ,  A61K9/0014 ,  A61K9/7023 ,  A61K31/165 ,  A61K31/216 ,  A61K31/341 ,  A61K31/365 ,  A61K45/06 ,  C07C59/72 ,  C07C69/712 ,  C07C69/734 ,  C07C69/74 ,  C07C69/96 ,  C07C219/16 ,  C07C235/20 ,  C07D207/08 ,  C07D211/60 ,  C07D257/06 ,  C07D263/24 ,  C07D263/26 ,  C07D265/30 ,  C07D295/088 ,  C07D295/145 ,  C07D307/20 ,  C07D317/34 ,  C07D317/40 ,  C07D453/02 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/42 ,  C07C2603/14

摘要： Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.

公开(公告)号：US20240117306A1

公开(公告)日：2024-04-11

申请号：US18323075

申请日：2023-05-24

申请人： CASSAVA SCIENCES, INC.

发明人： Hoau-Yan WANG ,  Lindsay BURNS BARBIER

IPC分类号： C12N5/079 ,  C07D205/04 ,  C07D207/08 ,  C07D211/14 ,  C07D211/74 ,  C07D217/04 ,  C07D265/30 ,  C07D265/36 ,  C07D277/02 ,  C07D277/04 ,  C07D279/12 ,  C07D295/08 ,  C07D295/088 ,  C07D471/10 ,  C07D491/04 ,  C07D491/056 ,  C07D498/10 ,  G01N33/50 ,  G01N33/68 ,  G01N33/94

CPC分类号： C12N5/0622 ,  C07D205/04 ,  C07D207/08 ,  C07D211/14 ,  C07D211/74 ,  C07D217/04 ,  C07D265/30 ,  C07D265/36 ,  C07D277/02 ,  C07D277/04 ,  C07D279/12 ,  C07D295/08 ,  C07D295/088 ,  C07D471/10 ,  C07D491/04 ,  C07D491/056 ,  C07D498/10 ,  G01N33/50 ,  G01N33/6896 ,  G01N33/94 ,  G01N2333/70571 ,  G01N2800/2821 ,  G01N2800/52

摘要： A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.

公开(公告)号：US11919874B2

公开(公告)日：2024-03-05

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 ,  A61K31/09 ,  A61K31/10 ,  A61K31/145 ,  A61K31/4164 ,  A61K31/5375 ,  A61K45/06 ,  C07C43/23 ,  C07C69/28 ,  C07C233/18 ,  C07C311/04 ,  C07C311/51 ,  C07C317/18 ,  C07C317/22 ,  C07C317/28 ,  C07D233/60

CPC分类号： C07D295/088 ,  A61K31/09 ,  A61K31/10 ,  A61K31/145 ,  A61K31/4164 ,  A61K31/5375 ,  A61K45/06 ,  C07C43/23 ,  C07C69/28 ,  C07C233/18 ,  C07C311/04 ,  C07C311/51 ,  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：US11779548B2

公开(公告)日：2023-10-10

申请号：US16871902

申请日：2020-05-11

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： Jie Li ,  Zilei Liu ,  Suhua Li ,  Peng Wu ,  K. Barry Sharpless

IPC分类号： A61K31/05 ,  A61K31/136 ,  C07C305/26 ,  C07K1/113 ,  C07K1/02 ,  A61K51/04 ,  A61K38/31 ,  A61K31/7048 ,  A61K31/70 ,  A61K31/655 ,  A61K31/65 ,  A61K31/56 ,  A61K31/5513 ,  A61K31/53 ,  A61K31/515 ,  A61K31/505 ,  A61K31/485 ,  A61K31/4745 ,  A61K31/473 ,  A61K31/4709 ,  A61K31/47 ,  A61K31/439 ,  A61K31/4353 ,  A61K31/4245 ,  A61K31/4168 ,  A61K31/407 ,  A61K31/4045 ,  A61K31/40 ,  A61K31/397 ,  A61K31/198 ,  A61K31/197 ,  A61K31/14 ,  C07K2/00 ,  C07D295/26 ,  C07D295/185 ,  C07D295/088 ,  C07D277/82 ,  A61K47/54 ,  C40B30/06 ,  C40B30/04 ,  C40B50/08 ,  C12N5/09 ,  C40B40/04

CPC分类号： A61K31/05 ,  A61K31/136 ,  A61K31/14 ,  A61K31/197 ,  A61K31/198 ,  A61K31/397 ,  A61K31/40 ,  A61K31/407 ,  A61K31/4045 ,  A61K31/4168 ,  A61K31/4245 ,  A61K31/439 ,  A61K31/4353 ,  A61K31/47 ,  A61K31/473 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/485 ,  A61K31/505 ,  A61K31/515 ,  A61K31/53 ,  A61K31/5513 ,  A61K31/56 ,  A61K31/65 ,  A61K31/655 ,  A61K31/70 ,  A61K31/7048 ,  A61K38/31 ,  A61K47/54 ,  A61K51/0497 ,  C07C305/26 ,  C07D277/82 ,  C07D295/088 ,  C07D295/185 ,  C07D295/26 ,  C07K1/02 ,  C07K1/1136 ,  C07K2/00 ,  C40B30/06 ,  C07C2601/14 ,  C07C2603/18 ,  C12N5/0693 ,  C12N2503/02 ,  C40B30/04 ,  C40B40/04 ,  C40B50/08 ,  G01N2500/00

摘要： A high-throughput screening methods for identifying candidate anticancer medicinal agents is described herein. The candidate anticancer medicinal agents are arylfluorosulfate compounds derived from phenolic compounds. The method involves in situ generation of the arylfluorosulfate compounds in multi-well plates by reaction of phenolic compounds in DMSO with a saturated solution of SO2F2 dissolved in a solvent such as acetonitrile, in the presence of an organic base, followed by reaction of generated fluoride ion with trimethylsilanol to form volatile trimethylsilyl fluoride. Solvents, organic base, and silyl compounds are then removed, in vacuo, to afford the arylfluorosulfate compounds suitable for biological screening in cancer cell lines without further purification.

公开(公告)号：US20230312479A1

公开(公告)日：2023-10-05

申请号：US18127215

申请日：2023-03-28

申请人： PeptiDream Inc.

发明人： Haruaki Kurasaki ,  Masatoshi Matsumoto ,  Ayumu Matsuda ,  Yutaka Kobayashi ,  Masahiko Kinebuchi ,  Tomoko Ashizawa ,  Katsuma Matsui ,  Motoki Murai ,  Masami Yamada

IPC分类号： C07D233/64 ,  C07C271/22 ,  C07C317/28 ,  C07D239/26 ,  C07D263/32 ,  C07D295/088 ,  C07D307/79 ,  C07D207/09 ,  C07D213/73 ,  C07C311/06

CPC分类号： C07D233/64 ,  C07C271/22 ,  C07C317/28 ,  C07D239/26 ,  C07D263/32 ,  C07D295/088 ,  C07D307/79 ,  C07D207/09 ,  C07D213/73 ,  C07C311/06 ,  C07B2200/07 ,  C07C2603/18

摘要： A novel amino acid derivative is provided, wherein the amino acid derivative is expected to improve binding affinity of polypeptides comprising the derivative therein.

公开(公告)号：US20230233516A1

公开(公告)日：2023-07-27

申请号：US18147171

申请日：2022-12-28

申请人： TECHFIELDS PHARMA CO., LTD

发明人： Chongxi Yu

IPC分类号： 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 ,  A61K8/31 ,  A61K31/015 ,  C07C15/30 ,  C07C15/38

CPC分类号： 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 ,  A61K8/31 ,  A61K31/015 ,  C07C15/30 ,  C07C15/38 ,  Y02A50/30

摘要： The invention provides compositions or pharmaceutical compositions of novel 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 and therefore render novel treatments. For example, HPCs of NSAIA have demonstrated indications such as treating hair loss and bold. 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：US20230201191A1

公开(公告)日：2023-06-29

申请号：US18162375

申请日：2023-01-31

申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. ,  UNIVERSITY OF CENTRAL FLORIDA RESEARCH FOUNDATION, INC.

发明人： SAID M. SEBTI ,  NICHOLAS J. LAWRENCE ,  JAMES TURKSON

IPC分类号： A61K31/495 ,  A61K33/243 ,  A61K33/24 ,  C07D295/088 ,  G01N33/50

CPC分类号： A61K31/495 ,  A61K33/243 ,  A61K33/24 ,  C07D295/088 ,  G01N33/5091

摘要： The subject invention concerns a compound and compositions having activity as an inhibitor of Stat3 protein and methods of using the compound and compositions. In one embodiment, a compound of the invention has the structure shown in formula I, formula II, or formula III. The subject invention also concerns methods of using the compounds and compositions of the invention.

公开(公告)号：US11679092B2

公开(公告)日：2023-06-20

申请号：US17365199

申请日：2021-07-01

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： C07C235/88 ,  A61K31/225 ,  C07D491/113 ,  C07C317/28 ,  C07D211/38 ,  C07D295/088 ,  C07D207/40 ,  C07D211/06 ,  C07D207/06 ,  C07D209/52 ,  C07C317/18 ,  C07C219/08 ,  C07C229/16 ,  C07C233/18 ,  C07C233/91

CPC分类号： A61K31/225 ,  C07C219/08 ,  C07C229/16 ,  C07C233/18 ,  C07C233/91 ,  C07C235/88 ,  C07C317/18 ,  C07C317/28 ,  C07D207/06 ,  C07D207/40 ,  C07D209/52 ,  C07D211/06 ,  C07D211/38 ,  C07D295/088 ,  C07D491/113

摘要： The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.

公开(公告)号：US11643657B2

公开(公告)日：2023-05-09

申请号：US16717986

申请日：2019-12-17

申请人： WAVE LIFE SCIENCES LTD.

发明人： David Charles Donnell Butler ,  Naoki Iwamoto ,  Meena ,  Nenad Svrzikapa ,  Gregory L. Verdine ,  Ivan Zlatev

IPC分类号： C12N15/113 ,  C07H21/00 ,  C07C317/28 ,  C07D295/088 ,  C12N15/11 ,  C12Q1/6876

CPC分类号： C12N15/113 ,  C07C317/28 ,  C07D295/088 ,  C07H21/00 ,  C12N15/11 ,  C12Q1/6876 ,  C12N15/111 ,  C12N2310/11 ,  C12N2310/14 ,  C12N2310/31 ,  C12N2310/315 ,  C12N2330/30

摘要： The present invention relates to chirally controlled oligonucleotides, chirally controlled oligonucleotide compositions, and the method of making and using the same. The invention specifically encompasses the identification of the source of certain problems with prior methodologies for preparing chiral oligonucleotides, including problems that prohibit preparation of fully chirally controlled compositions, particularly compositions comprising a plurality of oligonucleotide types. In some embodiments, the present invention provides chirally controlled oligonucleotide compositions. In some embodiments, the present invention provides methods of making chirally controlled oligonucleotides and chirally controlled oligonucleotide compositions.

公开(公告)号：US11623920B2

公开(公告)日：2023-04-11

申请号：US17751836

申请日：2022-05-24

申请人： Nuray Chemicals Private Limited

发明人： Ramasamy Venkatragavan ,  Erugu Balaiah ,  Paramanandam Senthilkumaran ,  Guttha Jayaprasad ,  Manniyam Kailasam Selvam ,  Noti Krishnareddy ,  Sorakka Pichandi Parthipan ,  Murugan Arunkumar ,  Palaniswamy Premkumar ,  Salamuthu Kaliraj ,  Shanmugam Arumugam ,  Singavarapu Ajay Madhukar ,  Raman Silambarasan ,  Saminathan Karthick ,  Kudumudi Jayaraman Parthiban ,  Ravi Silambarasan

IPC分类号： C07D295/088 ,  A61K9/16

摘要： The present disclosure relates to a process for preparing pitolisant hydrochloride of Formula-(I) and solid-state forms thereof.