公开(公告)号：US12122764B2

公开(公告)日：2024-10-22

申请号：US18069028

申请日：2022-12-20

申请人： Gilead Sciences, Inc.

发明人： Peter A. Blomgren ,  Zhimin Du ,  Musong Kim ,  Rhiannon Thomas-Tran ,  Michael T. Tudesco ,  Chandrasekar Venkataramani

IPC分类号： C07D401/14

CPC分类号： C07D401/14

摘要： The present disclosure relates to compounds that bind to and act as degraders of an IKAROS Family Zinc Finger (IKZF) protein, such as IKZF2 (Helios). The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding and degradation of an IKZF protein, such as IKZF2, including cancer.

公开(公告)号：US12102677B2

公开(公告)日：2024-10-01

申请号：US16877292

申请日：2020-05-18

申请人： Gilead Sciences, Inc.

发明人： Brian Moldt ,  Craig S. Pace

IPC分类号： A61K39/21 ,  A61K31/4745 ,  A61K31/519 ,  A61P31/18 ,  C07K16/10 ,  C12Q1/70

CPC分类号： A61K39/21 ,  A61K31/4745 ,  A61K31/519 ,  A61P31/18 ,  C07K16/1063 ,  C12Q1/703 ,  C07K2317/34 ,  C07K2317/76 ,  C07K2317/92 ,  C12Q2600/106 ,  C12Q2600/156

摘要： Provided are methods for identifying patient populations infected with HIV that can be targeted by antibodies that bind to HIV gp120 V3 glycan region.

公开(公告)号：US12091426B2

公开(公告)日：2024-09-17

申请号：US18054118

申请日：2022-11-09

申请人： Nurix Therapeutics, Inc. ,  Gilead Sciences, Inc.

发明人： John Buell ,  Frederick Cohen ,  Ryan Pemberton ,  Hunter P. Shunatona ,  Lan Wang ,  Mark Edward Zak

IPC分类号： C07D519/00

CPC分类号： C07D519/00

摘要： The present disclosure provides bifunctional compounds as HPK1 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by HPK1.

公开(公告)号：US12091420B2

公开(公告)日：2024-09-17

申请号：US18376159

申请日：2023-10-03

申请人： Gilead Sciences, Inc.

发明人： Stephen E. Ammann ,  Xinpei Cai ,  Eda Y. Canales ,  Weng K. Chang ,  Gregory F. Chin ,  Henok H. Kinfe ,  Jessica L. Mckinley ,  Michael R. Mish ,  Devan Naduthambi ,  Jason K. Perry ,  Kevin X. Rodriguez ,  Scott D. Schroeder ,  Christopher J. Swank ,  Joshua J. Van Veldhuizen

IPC分类号： C07D495/04 ,  C07D401/04 ,  C07D519/00

CPC分类号： C07D495/04 ,  C07D401/04 ,  C07D519/00

摘要： The present disclosure relates to compounds of Formula I:




and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, useful in the treatment of treating viral infections, for example, coronaviridae infections.

公开(公告)号：US20240269235A1

公开(公告)日：2024-08-15

申请号：US18540652

申请日：2023-12-14

申请人： Gilead Sciences, Inc.

发明人： Manuel Baca ,  Sarah A. Gilmore ,  Magdeleine S. Hung ,  Hassan Javanbakht ,  Manu Kanwar ,  Shahzada Khan ,  Prasenjit K. Mukherjee ,  Mark R. Nagel ,  Giuseppe Papalia ,  Danny W. Tam ,  Majlinda K. Thomas

IPC分类号： A61K38/20 ,  A61K38/00 ,  A61K39/395 ,  A61P31/20 ,  A61P35/00 ,  C07K14/55

CPC分类号： A61K38/2013 ,  A61K39/3955 ,  A61P31/20 ,  A61P35/00 ,  C07K14/55 ,  A61K38/00 ,  C07K2319/30

摘要： Provided are serum half-life extended-IL-2 variant (IL-2v) heterodimers having reduced binding to the IL2Rα (CD25) subunit. In particular, Fc-IL-2v heterodimers are provided and methods for making and using, e.g. for enhancing an immune response, e.g. in the prevention and treatment of viral infections and cancer.

公开(公告)号：US20240260553A1

公开(公告)日：2024-08-08

申请号：US18413972

申请日：2024-01-16

申请人： Gilead Sciences, Inc.

发明人： Daniel Rohrer ,  Peter Brams

IPC分类号： A01K67/0278 ,  C07K16/10 ,  C12N9/22 ,  C12N15/11

CPC分类号： A01K67/0278 ,  C07K16/1003 ,  C12N9/22 ,  C12N15/111 ,  A01K2217/072 ,  A01K2227/105 ,  A01K2267/01 ,  C07K2317/56 ,  C12N2310/20

摘要： Chimeric transgenic immunoglobulin (Ig) mice are provided that comprise an altered heavy chain locus in which endogenous mouse D and J segments have been deleted and a human heavy chain Ig transgene is inserted at that location such that the transgenic Ig mouse expresses an antibody repertoire that utilizes human VH and mouse VH in heavy chains, each linked to human DH and JH segments, leading to enhanced diversity. Methods of preparing and using the transgenic animals (e.g., to raise antibodies) are also provided.

公开(公告)号：US12053462B2

公开(公告)日：2024-08-06

申请号：US17379175

申请日：2021-07-19

申请人： Gilead Sciences, Inc.

发明人： Peter A. Blomgren ,  Taryn Campbell ,  Jayaraman Chandrasekhar ,  Christopher T. Clark ,  Julian A. Codelli ,  Kevin S. Currie ,  Jeffrey E. Kropf ,  Yasamin Moazami ,  Nicole Nava ,  Leena Patel ,  Stephane Perreault ,  Jason K. Perry ,  Kassandra F. Sedillo ,  Natalie Seeger ,  Kirk L. Stevens ,  Jennifer Anne Treiberg ,  Suet C. Yeung ,  Zhongdong Zhao

IPC分类号： C07D215/02 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5355 ,  A61K31/541 ,  A61K45/06 ,  C07D215/14 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D215/18 ,  C07D401/04 ,  C07D413/04 ,  C07D417/14 ,  C07D475/02 ,  C07D491/04 ,  C07D491/06 ,  C07D491/08 ,  C07D498/10 ,  C07D513/04

CPC分类号： A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5355 ,  A61K31/541 ,  A61K45/06 ,  C07D215/14 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D215/18 ,  C07D401/04 ,  C07D413/04 ,  C07D417/14 ,  C07D475/02 ,  C07D491/04 ,  C07D491/06 ,  C07D491/08 ,  C07D498/10 ,  C07D513/04

摘要： The present disclosure provides a compound of Formula (I):




or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

公开(公告)号：US20240254118A1

公开(公告)日：2024-08-01

申请号：US18391258

申请日：2023-12-20

申请人： Gilead Sciences, Inc.

发明人： Megan K. Armstrong ,  Elbert Chin ,  Chienhung Chou ,  Laurent P. Debien ,  Joshua D. Farr ,  Pancham Lal Gupta ,  Chao-I Hung ,  Michael L. Mitchell ,  Prasenjit K. Mukherjee ,  Shaina V. Nguyen ,  Gregory T. Notte ,  Daniel Roa ,  Adam J. Schrier ,  Zheng-Yu Yang

IPC分类号： C07D471/04 ,  A61K31/473 ,  A61K31/4741 ,  A61K31/4743 ,  A61K31/4745 ,  A61K31/4748 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  C07D401/12 ,  C07D491/048 ,  C07D513/04 ,  C07D519/00

CPC分类号： C07D471/04 ,  A61K31/473 ,  A61K31/4741 ,  A61K31/4743 ,  A61K31/4745 ,  A61K31/4748 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  C07D401/12 ,  C07D491/048 ,  C07D513/04 ,  C07D519/00

摘要： The present disclosure relates generally to compounds that inhibit PRMT5. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through inhibiting PRMT5. The disclosure further relates to the use of the compounds for the treatment of a disease or condition associated with chromosome 9p21 deletion or MTAP null. The disclosure further relates to the use of the compounds for the treatment of cancers.

公开(公告)号：US20240254104A1

公开(公告)日：2024-08-01

申请号：US18383128

申请日：2023-10-24

申请人： Gilead Sciences, Inc.

发明人： Bing Shi

IPC分类号： C07D401/14 ,  A61K45/06 ,  A61P31/18

CPC分类号： C07D401/14 ,  A61P31/18 ,  A61K45/06 ,  C07B2200/13

摘要： The present disclosure relates to pharmaceutically acceptable salts, cocrystals, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2- ((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-TH-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.

公开(公告)号：US12049461B2

公开(公告)日：2024-07-30

申请号：US16950654

申请日：2020-11-17

申请人： Gilead Sciences, Inc.

发明人： Ling-Jie Gao ,  Piet Andre Maurits Maria Herdewijn ,  Steven Cesar Alfons De Jonghe ,  William John Watkins ,  Lee Shun Chong

IPC分类号： A61K31/517 ,  A61K31/5375 ,  A61K31/5377 ,  A61P31/14 ,  C07D239/72 ,  C07D239/78 ,  C07D239/86 ,  C07D239/88 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04

CPC分类号： C07D413/04 ,  A61K31/517 ,  A61K31/5375 ,  A61K31/5377 ,  A61P31/14 ,  C07D239/72 ,  C07D239/78 ,  C07D239/86 ,  C07D239/88 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04

摘要： This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR′R″, C1-7alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.