公开(公告)号：US20230021705A1

公开(公告)日：2023-01-26

申请号：US17723758

申请日：2022-04-19

申请人： Gilead Sciences, Inc.

发明人： Megan K. Armstrong ,  Gediminas J. Brizgys ,  James S. Cassidy ,  Elbert Chin ,  Chienhung Chou ,  Chao-I Hung ,  David W. Lin ,  Michael L. Mitchell ,  Ezra Roberts ,  Scott D. Schroeder ,  James G. Taylor ,  Rhiannon Thomas-Tran ,  Nathan E. Wright ,  Zheng-Yu Yang

IPC分类号： A61K31/5383 ,  C07D417/14 ,  C07D405/14 ,  C07D498/04 ,  C07D413/14 ,  C07D513/04 ,  C07D471/04 ,  C07D487/04 ,  C07D409/14 ,  C07D401/14 ,  C07D491/08 ,  C07D495/04 ,  A61K45/06 ,  A61K31/423 ,  A61K31/137 ,  A61K31/357 ,  A61K31/135 ,  A61K38/22 ,  A61K31/5375 ,  A61K31/4188 ,  A61K35/60 ,  A61K31/4439 ,  A61K31/437 ,  A61K31/519 ,  A61K31/4985 ,  A61K31/444 ,  A61K31/4995 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/4545 ,  C07D401/10 ,  A61K31/427 ,  A61K31/433 ,  C07D403/12

摘要： The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition in a human.

公开(公告)号：US20230015617A1

公开(公告)日：2023-01-19

申请号：US17470703

申请日：2021-09-09

申请人： KUDOS PHARMACEUTICALS LIMITED

发明人： Niall Morrison Barr Martin ,  Graeme Cameron Smith ,  Stephen Philip Jackson ,  Vincent M. Loh ,  Xiao-Ling Fan Cockcroft ,  Ian Timothy Williams Matthews ,  Keith Allan Menear ,  Frank Kerrigan ,  Alan Ashworth

IPC分类号： A61K31/502 ,  A61K31/00 ,  C07D237/32 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D491/04 ,  C07D403/10 ,  C07D495/04 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D403/14 ,  A61K31/506 ,  A61N5/10 ,  C07D243/08

摘要： Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.

公开(公告)号：US20230000851A1

公开(公告)日：2023-01-05

申请号：US17774239

申请日：2020-11-12

申请人： GREY WOLF THERAPEUTICS LIMITED

发明人： Martin QUIBELL ,  Michael SPARENBERG ,  Jason John SHIERS

IPC分类号： A61K31/451 ,  C07D211/28 ,  C07D257/04 ,  C07D207/09 ,  C07C311/21 ,  C07C317/34 ,  C07D211/34 ,  C07D401/10 ,  C07D417/10 ,  A61K31/41 ,  A61K31/40 ,  A61K31/196 ,  A61K31/277 ,  A61K31/454 ,  A61K35/15 ,  A61K39/00 ,  A61K39/395

摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, (I) wherein: Z is a group of formula: (II) wherein P and Q are each independently CR12R13; or one of P and Q is NR14 and the other is CR12R13; the group X—Y is —NHSO2— or —SO2NH—; R1 is H, CN or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, Cl and alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl, heteroaryl, SO2NR16R17, CONR10R11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; R9 is H or halo; and R10, R11, R12, R13, R14, R16 and R17 are each independently H or alkyl; R15 is selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; and m and n are each independently 0, 1, 2 or 3. Further aspects of the invention relate to such compounds for use in the field of immune-oncology and related applications.

公开(公告)号：US11542245B2

公开(公告)日：2023-01-03

申请号：US16980210

申请日：2019-03-08

申请人： Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

发明人： Julian Egger ,  Daniel Goetz ,  Michal Sowa

IPC分类号： C07D401/10

摘要： The present invention relates to a process for preparing 4-{[(2S)-2-{4-[5-chloro-2-(4-chloro-1H-1,2,3-triazol-1-yl)phenyl]-5-methoxy-2-oxopyridin-1(2H)-yl}butanoyl]amino}-2-fluorobenzamide (I) or 4-({(2S)-2-[4-{5-chloro-2-[4-(trifluoromethyl)-1H-1,2,3-triazol-1-yl]phenyl}-5-methoxy-2-oxopyridin-1(2H)-yl]butanoyl}amino)-2-fluorobenzamide (II) from 2,5-dimethoxypyridine (III), 1-(2-bromo-4-chlorophenyl)-4-chloro-1H-1,2,3-triazole (X-Cl) or 1-(2-bromo-4-chlorophenyl)-4-(trifluoromethyl)-1H-1,2,3-triazole (X-CF3), 4-amino-2-fluorbenzamide (XIII) and (2R)-2-aminobutanoic acid (XVII).

公开(公告)号：US11542238B2

公开(公告)日：2023-01-03

申请号：US15734525

申请日：2019-06-03

申请人： CORCEPT THERAPEUTICS INCORPORATED

发明人： Hazel Hunt ,  Damien Francis Philippe Crepin ,  Joseph Thomas Hill-Cousins ,  Thomas Matthew Baker ,  Lorna Duffy

IPC分类号： C07D239/54 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/10 ,  C07D417/04 ,  A61K31/50 ,  A61K31/505 ,  A61K31/513 ,  A61K47/20 ,  A61P1/16 ,  A61P25/18 ,  A61P35/00 ,  C07D401/08 ,  C07D403/08 ,  C07D405/08 ,  C07D417/08 ,  C07D471/04

摘要： The present invention provides a class of pyrimidinedione cyclohexenyl compounds and methods of using these compounds as glucocorticoid receptor modulators.

公开(公告)号：US11530182B2

公开(公告)日：2022-12-20

申请号：US17138346

申请日：2020-12-30

申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.

发明人： Srikumar Chellappan ,  Nicholas J. Lawrence ,  Sujeewa Ranatunga Mahanthe Mudiyanselage

IPC分类号： C07D211/60 ,  C07D401/06 ,  C07D401/12 ,  C07C237/22 ,  C07C251/24 ,  C07C255/57 ,  C07D211/34 ,  C07D211/96 ,  C07D233/92 ,  C07D241/04 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  A61K45/06

摘要： Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WW domain could prevent the induction of Sox2 and stemness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit sternness. Disclosed are compounds that affect the Yap1:Oct4 interaction.

公开(公告)号：US20220380319A1

公开(公告)日：2022-12-01

申请号：US17760864

申请日：2020-09-17

申请人： Bial - R&D Investments, S.A.

发明人： Renato T. Skerlj ,  Elyse Marie Josee Bourque ,  Soumya Ray ,  Peter T. Lansbury

IPC分类号： C07D235/04 ,  C07D235/26 ,  C07D401/10 ,  C07D403/10 ,  C07D471/04 ,  C07D401/12 ,  C07D417/10 ,  C07D405/12 ,  C07D487/04 ,  C07D471/08 ,  C07D491/08 ,  C07D491/107 ,  C07D403/12 ,  C07D417/12 ,  C07D498/04

摘要： The invention provides substituted benzimidazole carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.

公开(公告)号：US20220372016A1

公开(公告)日：2022-11-24

申请号：US17351935

申请日：2021-06-18

申请人： C4 Therapeutics, Inc.

发明人： Andrew J. Phillips ,  Christopher G. Nasveschuk ,  James A. Henderson ,  Katrina L. Jackson ,  Minsheng He ,  Yanke Liang ,  Mark E. Fitzgerald ,  Victoria Garza

IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D401/10 ,  C07D239/22

摘要： This invention provides pharmaceutical protein degraders and E3 ubiquitin ligase binders for therapeutic applications as described further herein.

公开(公告)号：US20220356166A1

公开(公告)日：2022-11-10

申请号：US17168574

申请日：2021-02-05

申请人： BioCryst Pharmaceuticals, Inc.

发明人： Pravin L. Kotian ,  Yarlagadda S. Babu ,  Weihe Zhang ,  Peng-Cheng Lu ,  Minwan Wu ,  Wei Lv ,  Trung Xuan Nguyen ,  Zhao Dang ,  Venkat R. Chintareddy ,  V. Satish Kumar ,  Krishnan Raman

IPC分类号： C07D401/10 ,  C07D209/12 ,  C07D261/20 ,  C07D307/80 ,  C07D333/64 ,  C07D401/12 ,  C07D405/10

摘要： Disclosed are compounds of formulae I and II, and pharmaceutically acceptable salts and prodrugs thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity.

公开(公告)号：US11472806B2

公开(公告)日：2022-10-18

申请号：US16612866

申请日：2018-05-14

申请人： Domain Therapeutics

发明人： Anne-Laure Blayo ,  Thomas Catelain ,  Ismet Dorange ,  Cédric Genet ,  Baptiste Manteau ,  Stanislas Mayer ,  Stephan Schann

IPC分类号： C07D471/14 ,  C07D223/18 ,  C07D401/10 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  G01N33/68

摘要： The present invention provides novel heterocyclic compounds of the general formula (I), including novel compounds of formula (Ia), and pharmaceutical compositions containing them. Moreover, the compounds of formula (I) or (Ia) and the pharmaceutical compositions containing them are provided for use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. The compounds of formula (I) or (Ia) can act as modulators of nervous system receptors sensitive to glutamate, in particular as modulators of metabotropic glutamate receptors (mGluRs), which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. The present invention further provides compounds of formula (I) or (Ia) that are modulators of metabotropic glutamate receptors (mGluRs), particularly positive allosteric modulators of mGluRs, and more specifically positive allosteric modulators of mGluR3.