公开(公告)号：US20210179573A1

公开(公告)日：2021-06-17

申请号：US17188422

申请日：2021-03-01

申请人： Arbor Pharmaceuticals, LLC

发明人： Peter Virsik ,  David Wustrow ,  Thamil Annamalai ,  Suresh Manthati

IPC分类号： C07D295/185 ,  A61K31/40 ,  A61K31/27 ,  A61K31/5375 ,  C07C271/12 ,  C07D295/088 ,  C07D207/08 ,  A61K31/265 ,  C07C235/14 ,  C07C235/06

摘要： Improved methods of treating multiple sclerosis and/or psoriasis using prodrugs of methyl hydrogen fumarate are disclosed. The methods comprise administering certain prodrugs of methyl hydrogen fumarate. The methods are able to achieve high blood plasma concentrations of the active metabolite, methyl hydrogen fumarate, without causing significant gastrointestinal irritation. New prodrugs of methyl hydrogen fumarate are also disclosed.

公开(公告)号：US20210122758A1

公开(公告)日：2021-04-29

申请号：US16987581

申请日：2020-08-07

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-C10 aryl; 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：US10906867B2

公开(公告)日：2021-02-02

申请号：US16013048

申请日：2018-06-20

申请人： Novartis AG

发明人： Luis Brito ,  Delai Chen ,  Gabriel Grant Gamber ,  Andrew Geall ,  Kevin Love ,  Thomas Zabawa ,  Frederic Zecri

IPC分类号： C07C229/12 ,  C07C229/38 ,  C07D205/04 ,  C07D265/30 ,  C07D207/12 ,  C07D207/16 ,  C07D211/22 ,  C07D295/088 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D295/15 ,  C07C271/20 ,  C07C219/04 ,  A61K47/18 ,  A61K9/127 ,  A61K9/51 ,  A61K31/7105 ,  A61K31/713 ,  A61K39/12 ,  A61K39/39 ,  C07C271/22 ,  C07D211/06 ,  C07D211/34 ,  C07D211/44 ,  A61K39/00

摘要： This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L1, n and p are defined herein. The compounds of formula (X) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

公开(公告)号：US20200317628A1

公开(公告)日：2020-10-08

申请号：US16848061

申请日：2020-04-14

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：US10760052B2

公开(公告)日：2020-09-01

申请号：US16030494

申请日：2018-07-09

申请人： Pain Therapeutics, Inc.

发明人： Hoau-Yan Wang ,  Lindsay Burns Barbier

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

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：US20200062726A1

公开(公告)日：2020-02-27

申请号：US16569840

申请日：2019-09-13

申请人： CORSAIR PHARMA, INC.

发明人： Cyrus K. BECKER ,  Meenakshi S. VENKATRAMAN ,  Xiaoming ZHANG

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

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：US20200039943A1

公开(公告)日：2020-02-06

申请号：US16339285

申请日：2017-10-03

申请人： SIGILON THERAPEUTICS, INC.

发明人： Omid Veiseh ,  Richard Heidebrecht ,  Paul Kevin Wotton ,  Matthias Alexander Oberli ,  Robert James Miller

IPC分类号： C07D249/04 ,  A61P37/04 ,  A61P37/06 ,  A61K9/00 ,  A61K35/30 ,  C07K16/22 ,  A61K39/395 ,  C12N9/40 ,  A61K38/47 ,  A61K31/541 ,  C07D405/12 ,  A61K31/4192 ,  C07D295/088 ,  A61K31/54 ,  C07H15/26 ,  A61K31/7056 ,  C07F7/18 ,  A61K31/695 ,  C07D405/14 ,  C07D403/12 ,  C07D409/04

摘要： The present invention provides compounds, e.g., compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are implantable elements (e.g., devices and materials) comprising the same, as well as methods of use thereof, e.g., for treating or preventing a disease, disorder, or condition.

公开(公告)号：US10538532B2

公开(公告)日：2020-01-21

申请号：US16194608

申请日：2018-11-19

申请人： ENANTA PHARMACEUTICALS, INC.

发明人： Yao-Ling Qiu ,  Xuri Gao ,  Wei Li ,  Hui Cao ,  Meizhong Jin ,  Jorden Kass ,  Xiaowen Peng ,  Yat Sun Or

IPC分类号： C07D493/08 ,  A61K31/167 ,  A61K31/18 ,  A61K31/196 ,  A61K31/215 ,  A61K31/223 ,  A61K31/277 ,  A61K31/325 ,  A61K31/335 ,  A61K31/336 ,  A61K31/341 ,  A61K31/351 ,  A61K31/357 ,  A61K31/365 ,  A61K31/39 ,  A61K31/401 ,  A61K31/41 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/426 ,  A61K31/439 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4425 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/655 ,  C07B59/00 ,  C07C235/56 ,  C07C311/53 ,  C07C317/32 ,  C07C323/42 ,  C07D207/16 ,  C07D211/54 ,  C07D213/52 ,  C07D213/81 ,  C07D213/89 ,  C07D231/12 ,  C07D233/64 ,  C07D257/04 ,  C07D261/02 ,  C07D261/08 ,  C07D261/20 ,  C07D263/52 ,  C07D277/26 ,  C07D295/088 ,  C07D303/26 ,  C07D303/34 ,  C07D307/32 ,  C07D307/33 ,  C07D309/08 ,  C07D313/04 ,  C07D317/72 ,  C07D327/10 ,  C07D401/04 ,  C07D451/04 ,  C07D493/04 ,  C07C317/44 ,  C07C323/62

摘要： The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y-L-R  (I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

公开(公告)号：US10479804B2

公开(公告)日：2019-11-19

申请号：US16075547

申请日：2017-01-27

申请人： Gotion Inc.

发明人： Nicole Holub ,  Juergen Herbel

IPC分类号： C07C211/63 ,  C07F5/02 ,  C07D295/088

摘要： A process for preparing an ammonium or phosphonium borate salt KA containing a cation K and an anion A. The process includes providing a melt of a borate salt K1A, and adding a solution of an ammonium or phosphonium salt KA1 in a solvent or solvent mixture (i), wherein K is an organic ammonium or phosphonium cation, and A is a borate anion of formula (Ia) or (Ib).

公开(公告)号：US10450290B2

公开(公告)日：2019-10-22

申请号：US15811522

申请日：2017-11-13

申请人： Corsair Pharma Inc.

发明人： Cyrus K. Becker ,  Meenakshi S. Venkatraman ,  Xiaoming Zhang

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

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.