公开(公告)号：US12098126B2

公开(公告)日：2024-09-24

申请号：US17821314

申请日：2022-08-22

申请人： Versitech Limited ,  Laboratory for Synthetic Chemistry and Chemical Biology Limited

发明人： Chi-Ming Che ,  Tingjie You

IPC分类号： C07D207/06 ,  B01J31/22 ,  C07D207/12 ,  C07D207/14 ,  C07D217/26 ,  C07D221/22 ,  C07D223/18 ,  C07D233/32 ,  C07D401/04 ,  C07D403/10 ,  C07D405/04 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/22

CPC分类号： C07D207/06 ,  B01J31/2295 ,  C07D207/12 ,  C07D207/14 ,  C07D217/26 ,  C07D221/22 ,  C07D223/18 ,  C07D233/32 ,  C07D401/04 ,  C07D403/10 ,  C07D405/04 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/22

摘要： Described herein is an iron(II)-phthalocyanine catalyzed C—H bond amination of alkyl azides. The catalyst is effective to produce intramolecular amination of saturated C—H bonds in moderate to excellent yields and the methods are tolerant of a wide scope of substrates. The methods described are useful for the synthesis of natural products derivatives and for the late-stage functionalization of pharmaceuticals.

公开(公告)号：US20230312520A1

公开(公告)日：2023-10-05

申请号：US18155528

申请日：2023-01-17

申请人： Arrakis Therapeutics, Inc.

发明人： Gnanasambandam KUMARAVEL ,  Jennifer C. PETTER ,  Jonathan Craig BLAIN ,  Donovan Noel CHIN ,  Chao FANG ,  Herschel MUKHERJEE ,  Neil KUBICA

IPC分类号： C07D401/14 ,  A61K47/54 ,  A61K47/68 ,  A61P25/28 ,  A61P43/00 ,  A61K9/00 ,  C07D495/04 ,  C12N15/115 ,  G01N33/50 ,  C07D401/12 ,  A61K31/522 ,  A61K39/395 ,  C12Q1/6816 ,  A61K31/65 ,  C07D217/26

CPC分类号： C07D401/14 ,  A61K47/545 ,  A61K47/6809 ,  A61P25/28 ,  A61P43/00 ,  A61K9/0019 ,  A61K9/0053 ,  C07D495/04 ,  C12N15/115 ,  G01N33/5008 ,  C07D401/12 ,  A61K31/522 ,  A61K39/395 ,  C12Q1/6816 ,  A61K31/65 ,  C07D217/26

摘要： The present invention relates to photoactivatable compounds and methods of use thereof for determining binding site and other structural information about RNA transcripts. The invention also provides methods of identifying RNA transcripts that bind compounds and are thus druggable, methods of screening drug candidates, and methods of determining drug binding sites and/or accessible or reactive sites on a target RNA.

公开(公告)号：US11679093B2

公开(公告)日：2023-06-20

申请号：US17251070

申请日：2019-06-11

申请人： THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE

发明人： Kambez Hajipouran Benam

IPC分类号： C07C257/18 ,  A61K31/167 ,  A61K31/472 ,  A61K31/4725 ,  C07D217/26 ,  C07D217/12 ,  A61K31/245 ,  A61K31/194 ,  A61K31/195 ,  A61K31/4166 ,  A61K31/42 ,  A61K31/422 ,  A61K45/06 ,  C07C279/18 ,  C07D233/70 ,  C07D261/08

CPC分类号： A61K31/245 ,  A61K31/167 ,  A61K31/194 ,  A61K31/195 ,  A61K31/4166 ,  A61K31/42 ,  A61K31/422 ,  A61K45/06 ,  C07C257/18 ,  C07C279/18 ,  C07D233/70 ,  C07D261/08

摘要： The present invention relates in certain aspects to the discovery of novel 2-naphthimidamide compounds that are capable of binding Type II Transmembrane Serine Proteases (TTSPs). In certain embodiments, the compounds of the invention can be used to treat or prevent Influenza A viral infection in a mammal.

公开(公告)号：US20230174530A1

公开(公告)日：2023-06-08

申请号：US17999001

申请日：2021-06-04

申请人： PATHIOS THERAPEUTICS LIMITED

发明人： Tom MCCARTHY ,  Gavin MILNE ,  Tobias MOECHEL ,  Alan NAYLOR

IPC分类号： C07D471/04 ,  C07D217/06 ,  C07D498/04 ,  C07D217/26 ,  C07D471/14 ,  C07D413/04 ,  C07D401/04 ,  C07D409/04

CPC分类号： C07D471/04 ,  C07D217/06 ,  C07D498/04 ,  C07D217/26 ,  C07D471/14 ,  C07D413/04 ,  C07D401/04 ,  C07D409/04

摘要： The present invention relates to a compound of formula (Ia), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring A is a 5- or 6-membered monocyclic aromatic or heteroaromatic ring, or a 9- or 10-membered bicyclic aromatic or heteroaromatic ring, each of which is optionally substituted with one or more substituents selected from F, Cl, Br, I, CN, alkoxy, NR11R11′, OH, SO2-alkyl, CO2-alkyl, alkyl, haloalkyl, aralkyl, aryl, and heteroaryl, and wherein said aryl and heteroaryl substituents are in turn optionally substituted with one or more substituents each independently selected from F, Cl, Br, I, CN, alkoxy, NR11R11′, OH, alkyl, haloalkyl, and aralkyl; Y and Z are each independently CR10R10′, wherein R10 and R10′ are each independently selected from H, F, alkyl, and haloalkyl; R1, R4, and R5 are each independently selected from H, F, Cl, Br, I and haloalkyl; R2 and R3 are each independently selected from H, F, Cl, Br, I, CN, and haloalkyl; wherein at least two of R2, R3 and R4 are other than H; and R11 and R11′ are each independently selected from H, alkyl, haloalkyl, COR12, and SO2R13, wherein R12 and R13 are both alkyl; wherein the compound is other than: N-(3,4-Dichlorophenyl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxamide; N-(3,4-Dichlorophenyl)-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxamide; N-(4-Chloro-3-(trifluoromethyl)phenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide; N-(3,4-dichlorophenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide; N-(3,4-Dichlorophenyl)-6,7-dihydroisoxazolo[4,5-c]pyridine-5(4H)-carboxamide; and N-(3,4-Dichlorophenyl)-4-methyl-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-carboxamide. Further aspects of the invention relate to such compounds for use in the field of immunooncology, immunology, and related applications.

公开(公告)号：US11647748B2

公开(公告)日：2023-05-16

申请号：US16918325

申请日：2020-07-01

申请人： MIGAL-GALILEE RESEARCH INSTITUTE LTD.

发明人： Itai Bloch ,  Elad Cohen ,  Rachel Amir ,  Maayan Gal

IPC分类号： C07D471/04 ,  C07D271/06 ,  A01N43/38 ,  A01N43/42 ,  A01N43/647 ,  A01N43/78 ,  A01N43/82 ,  A01N43/90 ,  C07D209/26 ,  C07D217/26 ,  C07D249/06 ,  C07D277/26

CPC分类号： A01N43/38 ,  A01N43/42 ,  A01N43/647 ,  A01N43/78 ,  A01N43/82 ,  A01N43/90 ,  C07D209/26 ,  C07D217/26 ,  C07D249/06 ,  C07D271/06 ,  C07D277/26 ,  C07D471/04

摘要： The present invention provides novel sulphonamide inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides for gardening, clearing waste ground, clearing industrial or constructions sites, clearing railways and railway embankments, pesticide, fungicide, agricultural plant stimulant or antimicrobial agent. Also provided is a method for the control of undesired vegetation or clearing areas from the undesired vegetation comprising applying to the locus of said undesired vegetation, to the undesired plants or to a habitat thereof, a herbicidally effective amount of the compound of the present invention.

公开(公告)号：US20230118751A1

公开(公告)日：2023-04-20

申请号：US17790500

申请日：2020-12-29

申请人： WUHAN LL SCIENCE AND TECHNOLOGY DEVELOPMENT CO., LTD.

发明人： Jun Lou ,  Yongkai Chen ,  Yihan Zhang ,  Xiaodan Guo ,  Lina Qian ,  Li Liu ,  Wei Peng ,  Fei Rong ,  Chaodong Wang

IPC分类号： C07D217/26 ,  C07D401/12 ,  C07D239/72 ,  C07D237/28 ,  C07D401/04

摘要： Disclosed is a fused ring compound and an application thereof. Disclosed is a fused ring compound represented by formula I, a pharmaceutically acceptable salt, a stereoisomer, a tautomer, an isotope compound, a crystal form, a nitrogen oxide, a solvate, or a solvate of the pharmaceutically acceptable salt thereof. The fused ring compound of the present invention has high P2X4 antagonistic activity, excellent selectivity, low toxicity and excellent metabolic stability.

公开(公告)号：US20230045929A1

公开(公告)日：2023-02-16

申请号：US17773197

申请日：2020-10-30

申请人： Cancer Research Technology Limited

发明人： Mairi SIME ,  Justin BOWER ,  Duncan MCARTHUR ,  Angelo PUGLIESE

IPC分类号： C07D217/26 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12

摘要： Provided are compounds of the Formula I, and salts and solvates thereof: (I) wherein R1, R2, R3, X1, X2, X3 and Z are defined in the specification. The compounds are inhibitors of salt-inducible kinase (SIK), particular SIK2, and are useful in therapy, particularly in the treatment of a proliferative disorder, a benign neoplasm, pathological angiogenesis, an inflammatory disease or condition, a musculoskeletal disease or condition, an autoimmune disease, a haematological disease or condition, a neurological disease or condition, a psychiatric disorder, or a metabolic disorder.

公开(公告)号：US11479561B2

公开(公告)日：2022-10-25

申请号：US16871532

申请日：2020-05-11

申请人： Cytokinetics, Incorporated

发明人： Ippei Sato ,  Takashi Kamikubo ,  Masanori Miura ,  Yuji Matsushima ,  Hiroaki Tanaka ,  Yasuhiro Shiina ,  Susumu Yamaki ,  Tomoyuki Saito ,  Hiroshi Kiyohara ,  Munemichi Ohe ,  Kayoko Mihara ,  Bradley Paul Morgan ,  Fady Malik ,  Scott Emile Collibee ,  Luke Ashcraft ,  Pu-Ping Lu ,  Jeffrey Michael Warrington ,  Marc Garard

IPC分类号： A61K31/4747 ,  A61K31/472 ,  C07D491/20 ,  C07D491/107 ,  C07D217/24 ,  C07D471/04 ,  C07D217/26 ,  C07D471/10 ,  A61P21/00

摘要： Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

公开(公告)号：US11465970B2

公开(公告)日：2022-10-11

申请号：US16772535

申请日：2018-12-14

申请人： Nanjing Cavendish Bio-Engineering Technology Co., Ltd. ,  Yongxiang Xu

发明人： Yongxiang Xu

IPC分类号： C07D217/26

摘要： The present application provides a method for synthesis of Roxadustat. A compound as represented by formula (VIII) is used as a raw material, and is reacted with phenol, a vinyl-containing ether, an acid, hydroxylamine, and then the product is reacted with glycine. In addition, the present application also provides intermediate compounds as represented by formula (IX), formula (XI), formula (XII), formula (IV), and formula (V) for synthesis of Roxadustat. Herein, details of the substituents involved in formula (VIII), formula (IX), formula (XI), and formula (XII) are stated in the description

公开(公告)号：US11420935B2

公开(公告)日：2022-08-23

申请号：US16849728

申请日：2020-04-15

申请人： Vivace Therapeutics, Inc.

发明人： Andrei W. Konradi ,  Tracy Tzu-Ling Tang Lin

IPC分类号： C07C235/66 ,  C07C311/51 ,  C07D217/24 ,  C07D217/26 ,  C07D401/12 ,  C07D213/40 ,  C07C255/24 ,  C07D333/70 ,  C07D305/08 ,  C07D305/06 ,  C07D241/12 ,  C07D233/64 ,  C07D257/04 ,  C07D213/73 ,  C07D213/61

摘要： Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating deseases, such as cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.