公开(公告)号：US12042541B2

公开(公告)日：2024-07-23

申请号：US18194540

申请日：2023-03-31

申请人： ARBUTUS BIOPHARMA CORPORATION

发明人： Muthiah Manoharan ,  Muthusamy Jayaraman ,  Kallanthottathil G. Rajeev ,  Laxman Eltepu ,  Steven Ansell ,  Jianxin Chen

IPC分类号： A61K47/44 ,  A61K9/127 ,  A61K31/7088 ,  A61K31/713 ,  A61K39/00 ,  A61K39/39 ,  A61K47/10 ,  A61K47/18 ,  A61K47/20 ,  A61K47/28 ,  C07C229/08 ,  C07C229/30 ,  C07C237/16 ,  C07C251/38 ,  C07C251/78 ,  C07C271/12 ,  C07C271/20 ,  C07C323/25 ,  C07D203/10 ,  C07D317/28 ,  C07D317/44 ,  C07D317/46 ,  C07D317/72 ,  C07D319/06 ,  C07D405/12 ,  C07D491/056 ,  C07D491/113 ,  C12N15/11 ,  C12N15/113

CPC分类号： A61K47/44 ,  A61K9/1272 ,  A61K31/7088 ,  A61K31/713 ,  A61K39/00 ,  A61K39/39 ,  A61K47/10 ,  A61K47/18 ,  A61K47/20 ,  A61K47/28 ,  C07C229/08 ,  C07C229/30 ,  C07C237/16 ,  C07C251/38 ,  C07C251/78 ,  C07C271/12 ,  C07C271/20 ,  C07C323/25 ,  C07D203/10 ,  C07D317/28 ,  C07D317/44 ,  C07D317/46 ,  C07D317/72 ,  C07D319/06 ,  C07D405/12 ,  C07D491/056 ,  C07D491/113 ,  C12N15/111 ,  C12N15/113 ,  A61K2039/55555 ,  A61K2039/55561 ,  C12N2310/14 ,  C12N2310/3515 ,  C12N2320/32 ,  Y02A50/30

摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure




wherein:



R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).

公开(公告)号：US20220388974A1

公开(公告)日：2022-12-08

申请号：US17749452

申请日：2022-05-20

申请人： Merck Sharp & Dohme LLC ,  Werthenstein Biopharma GMBH

发明人： Stephen M. Dalby ,  Clinton Scott Shultz ,  Chintal Desai ,  Joshua Lee ,  Zhiwei Chen ,  Jungchul Kim ,  Nastaran Salehi Marzijarani ,  Tao Wang ,  Eric M. Phillips ,  Patrick Larpent ,  Het P. Patel ,  Haiheng Guo ,  Xin Wang ,  Kangze Dai ,  Lu Chen ,  Teng Li ,  Taotao Lu ,  Jianjun Duan

IPC分类号： C07D317/72 ,  C07C317/14

摘要： The disclosure provides crystalline forms for certain synthetic intermediates for making belzutifan, a HIF-2α inhibitor, useful for the treatment of cancer. The disclosure also provides processes for isolating the crystalline forms.

公开(公告)号：US20220213051A1

公开(公告)日：2022-07-07

申请号：US17613983

申请日：2020-05-29

申请人： HYUNDAI PHARM CO., LTD.

发明人： Jeong Un HWANG ,  Jin Woong KIM ,  Kyu Hwan LEE ,  Eun Young KIM ,  Su Kyoung CHOI

IPC分类号： C07D317/72

摘要： The present invention relates to a novel crystal form of a 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method therefore and a pharmaceutical composition comprising same. A crystal form I of a compound of chemical formula 1, according to the present invention, exhibits more excellent physicochemical properties such as thermal stability, static electricity-inducing capability, compressibility, etc. compared to an amorphous form or a crystal form II, and thus is especially useful for preparation and long-term storage.

公开(公告)号：US20220091507A1

公开(公告)日：2022-03-24

申请号：US17543789

申请日：2021-12-07

申请人： JSR CORPORATION

发明人： Katsuaki NISHIKORI

IPC分类号： G03F7/039 ,  C08F220/18 ,  C07D327/04 ,  G03F7/038 ,  C07C309/12 ,  C07C309/06 ,  C07C381/12 ,  C07D317/72 ,  G03F7/004

摘要： A radiation-sensitive resin composition includes: a polymer which has a first structural unit including a phenolic hydroxyl group, and a second structural unit represented by formula (1); and a radiation-sensitive acid generating agent which has a compound represented by formula (2), R1 represents a hydrogen atom, or the like; R2 represents a hydrogen atom or the like; and R3 represents a divalent monocyclic alicyclic hydrocarbon group having 3 to 12 ring atoms. Ar1 represents a group obtained by removing (q+1) hydrogen atoms on an aromatic ring from an arene formed by condensation of at least two benzene rings; R4 represents a monovalent organic group having 1 to 20 carbon atoms; q is an integer of 0 to 7; and R5 represents a halogen atom, a hydroxy group, a nitro group, or a monovalent organic group having 1 to 20 carbon atoms, or the like.

公开(公告)号：US20210403416A1

公开(公告)日：2021-12-30

申请号：US17251469

申请日：2019-06-13

申请人： Texas Tech University System

发明人： Susan E. Bergeson ,  Ted W. Reid ,  Mayank Shashtri ,  Peter Syapin ,  Phat Tran

IPC分类号： C07C237/26 ,  C07D317/72 ,  A61B5/00

摘要： The present invention includes novel molecules and methods for using the same to treat Alcohol Use Disorder (AUD), Substance Use Disorder (SUD), tobacco use, pain, or proinflammatory disorders comprising: identifying a subject in need of treatment for at least one of AUD, SUD, pain, or a proinflammatory disorder; and providing the subject with an effective amount of a modified minocycline to ameliorate or eliminate the AUD, SUD, pain, or proinflammatory disorder and that has reduced, or no, antimicrobial activity, wherein the modified tetracycline has a formula, e.g., or the modified doxycycline, minocycline, and tigecycline and their tautomerized structures, where the R-groups shown in the minocycline example above could be different combination of halogen, acetyl ester, methyl ester, and diacetal.

公开(公告)号：US20210139450A1

公开(公告)日：2021-05-13

申请号：US17047994

申请日：2019-04-15

申请人： Bayer Aktiengesellschaft

发明人： Albert SCHNATTERER ,  Michael DOCKNER ,  Peter BRUECHNER ,  Thomas HIMMLER

IPC分类号： C07D317/72 ,  C07D491/113

摘要： The present invention relates to a novel process for the esterification of N-acylated amino acids which contain an acid-labile keto protective group under alkaline conditions without using a polar aprotic solvent, in which the N-acylated amino acid with acid-labile keto protective group prepared in situ is esterified using an alkyl halide or a mono- or dialkyl ester of sulfuric acid.

公开(公告)号：US10934306B2

公开(公告)日：2021-03-02

申请号：US16715602

申请日：2019-12-16

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 ,  C07C317/44 ,  C07C323/62 ,  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

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：US20190352262A1

公开(公告)日：2019-11-21

申请号：US16475965

申请日：2018-02-01

申请人： YALE UNIVERSITY

发明人： Seth Herzon ,  Stephen K. Murphy ,  Mingshuo Zeng

IPC分类号： C07D209/96 ,  C07C69/675 ,  C07C49/573 ,  C07D317/72

摘要： The present invention is directed to novel pleuroniutilin antibiotic compounds, intermediates which are useful for making these novel amibioiic compounds and related methods and pharmaceutical compositions for treating pathogens, especially bacterial infections, including gram negative bacteria and synthesizing these compounds.

公开(公告)号：US10377732B2

公开(公告)日：2019-08-13

申请号：US15570781

申请日：2016-11-29

申请人： F.I.S.—Fabbrica Italiana Sintetici S.p.A.

发明人： Paolo Maragni ,  Massimo Verzini

IPC分类号： C07D309/14 ,  C07D317/28 ,  C07D317/72 ,  C07D303/36 ,  C07C271/16 ,  C07C309/73 ,  C07C233/18

摘要： The present invention relates to a process for preparing 3-amino tetrahydropyrans and, more particularly, to an improved method for synthesizing a 2,3,5-substituted tetrahydropyran derivative, intermediate being used in the preparation of dipeptidyl peptidase-IV enzyme inhibitors (DPP-4 inhibitors).

公开(公告)号：US20190055182A1

公开(公告)日：2019-02-21

申请号：US16166893

申请日：2018-10-22

申请人： California Institute of Technology

发明人： Brian M. Stoltz ,  Alexander N. Marziale ,  Robert A. Craig ,  Douglas Duquette ,  Kelly E. Kim ,  Marc Liniger ,  Yoshitaka Numajiri

IPC分类号： C07C45/65 ,  C07D211/94 ,  C07D223/10 ,  B01J31/04 ,  C07D317/72 ,  C07C49/647 ,  C07C49/683

摘要： This invention provides efficient and scalable enantioselective methods that yield 2-alkyl-2-allylcycloalkyanone compounds with quaternary stereogenic centers. Methods include the method for the preparation of a compound of formula (I): comprising treating a compound of formula (II) or (III): with a palladium (II) catalyst under alkylation conditions.