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91. 发明授权

US11292767B2 Heterocyclic inhibitors of MCT4 有权
公开(公告)号：US11292767B2
公开(公告)日：2022-04-05
申请号：US16222949
申请日：2018-12-17
申请人： Vettore, LLC
发明人： Kenneth Mark Parnell , John McCall , Donna Romero
IPC分类号： C07D231/14 , C07D231/56 , A61P35/00 , C07D207/24 , C07C59/01 , C07D205/02 , C07D401/04 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07D213/12 , A61K45/06 , A61K31/415 , C07D403/06 , C07D405/06 , C07D405/14
摘要： Disclosed herein are compounds and compositions useful in the treatment of MCT4 mediated diseases, such as proliferative and inflammatory diseases, having the structure of Formula I: Methods of inhibition MCT4 activity in a human or animal subject are also provided.

92. 发明申请

US20220089572A1 NLRP3 MODULATORS 有权
公开(公告)号：US20220089572A1
公开(公告)日：2022-03-24
申请号：US17422512
申请日：2020-01-13
申请人： INNATE TUMOR IMMUNITY, INC.
发明人： Ashvinikumar V. Gavai , Derek J. Norris , Daniel O'MALLEY , Steven P. Seitz , Jay A. Markwalder , David K. Williams , Hua Gong , Scott Hunter Watterson , Christine M. Tarby
IPC分类号： C07D403/04 , C07D405/14 , C07D498/08 , C07D401/04 , C07D401/14 , C07D493/10 , C07D487/10 , C07D409/14 , C07D491/08 , C07D493/08 , A61P35/00
摘要： The present invention provides compounds of Formula (I):(I) wherein all of the variables are as defined herein. These compounds are modulators of NLRP3, which may be used as medicaments for the treatment of proliferative disorders, such as cancer in a subject (e.g., a human).

93. 发明申请

US20220087262A1 PESTICIDALLY ACTIVE PYRAZOLE DERIVATIVES 有权
公开(公告)号：US20220087262A1
公开(公告)日：2022-03-24
申请号：US17375490
申请日：2021-07-14
申请人： SYNGENTA PARTICIPATIONS AG
发明人： André JEANGUENAT , Myriem EL QACEMI , André STOLLER , Aurelien BIGOT , Denis GRIBKOV
IPC分类号： A01N43/56 , A01N43/80 , C07D401/14 , C07D403/04 , C07D413/02
摘要： A compound of formula (II) or formula (III) As defined herein.

94. 发明授权

US11279697B2 Aromatic derivative, preparation method for same, and medical applications thereof 有权
公开(公告)号：US11279697B2
公开(公告)日：2022-03-22
申请号：US16644919
申请日：2018-09-04
申请人： BIOARDIS LLC
发明人： Ning Shao , Ding Wang , Hongbin Yuan , Frank Kayser
IPC分类号： C07D413/10 , A61P35/04 , C07D231/12 , C07D231/38 , C07D231/54 , C07D403/04 , C07D403/10 , C07D471/04
摘要： An aromatic derivative as represented by formula (I), a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising same, a preparation method therefor, and uses of the aromatic derivative and the pharmaceutically acceptable salt thereof or the pharmaceutical composition comprising same in preparing a therapeutic agent, specifically an FGFR4 tyrosine kinase inhibitor, and in preparing a medicament for treating and/or preventing neoplastic and inflammatory diseases. The substituents of formula (I) are same as defined in the description.

95. 发明申请

US20220081437A1 HETEROARYL CARBOXAMIDE COMPOUNDS AS INHIBITORS OF RIPK2 有权
公开(公告)号：US20220081437A1
公开(公告)日：2022-03-17
申请号：US17409956
申请日：2021-08-24
申请人： Boehringer Ingelheim International GmbH
发明人： Pingrong LIU , Craig Andrew MILLER , Maolin YU , Zhonghua ZHANG , Sabine RUPPEL , Anil K. PADAYANA
IPC分类号： C07D471/04 , C07D231/12 , C07D403/04 , C07D401/04 , C07D417/04 , C07D417/14 , C07D487/04
摘要： The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes

96. 发明申请

US20220081412A1 QUINOLINYL-PYRAZINE-CARBOXAMIDE COMPOUNDS AND USES THEREOF 有权
公开(公告)号：US20220081412A1
公开(公告)日：2022-03-17
申请号：US17416876
申请日：2019-12-20
申请人： The Regents of the University of Michigan
发明人： Nouri Neamati , Joyeeta Roy
IPC分类号： C07D401/12 , C07D401/14 , C07D471/04 , C07D417/14 , C07D451/02 , C07D471/08 , C07D403/04 , C07D487/04 , C07D491/107 , C07D471/10 , C07D495/10 , C07D417/12
摘要： This invention is in the field of medicinal chemistry. In particular, the invention relates to anew class of small-molecules having a quinolinyl-pyrazine-carboxamide (or similar) structure which function as activators of the cholesterol biosynthesis pathway within cancer cells and/or immune cells, which function as activators of the cell cycle regulation pathway within cancer cells and/or immune cells, and which function as up-regulators of HMGCS1 protein expression within cancer cells and/or immune cells, and which function as effective therapeutic agents for treating, ameliorating, and preventing various forms of cancer and other inflammatory disease.

97. 发明授权

US11274093B2 Fused bicyclic benzoheteroaromatic compounds and methods of use thereof 有权
公开(公告)号：US11274093B2
公开(公告)日：2022-03-15
申请号：US16480211
申请日：2018-01-24
申请人： Araxes Pharma LLC
发明人： Liansheng Li , Jun Feng , Yuan Liu , Tao Wu , Pingda Ren , Yi Liu
IPC分类号： C07D403/04 , C07D403/12 , C07D403/14 , A61P35/04 , A61K9/00 , C07D401/12 , C07D401/14 , C07D471/04
摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (I) or a pharmaceutically acceptable salt, isotopic form, stereoisomer or prodrug thereof, wherein A, B, X, R1, R2a, R2b, R2c, L, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

98. 发明申请

US20220073470A1 INHIBITORS OF CGAS ACTIVITY AS THERAPEUTIC AGENTS 有权
公开(公告)号：US20220073470A1
公开(公告)日：2022-03-10
申请号：US17419837
申请日：2020-01-03
申请人： BELLBROOK LABS, LLC
发明人： Robert G. Lowery , Meera Kumar , Matthew Boxer , David Maloney , Susan Boyd
IPC分类号： C07D231/20 , C07C237/48 , C07D401/04 , C07D487/04 , C07D239/94 , C07D213/81 , A61P37/04 , C07D403/04
摘要： This disclosure relates to compounds, pharmaceutical compositions comprising them, and methods of using the compounds and compositions for treating or preventing inappropriate activation of a type I interferon (IFN) response in a subject in need thereof.

99. 发明申请

US20220071998A1 MODULATORS OF KV3 CHANNELS TO TREAT PAIN 有权
公开(公告)号：US20220071998A1
公开(公告)日：2022-03-10
申请号：US17472493
申请日：2021-09-10
申请人： Autifony Therapeutics Limited
发明人： Charles LARGE , Giuseppe ALVARO
IPC分类号： A61K31/506 , A61K31/4439 , A61K31/4196 , C07C43/315 , C07D307/94 , A61P29/02 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14
摘要： The present invention provides a modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels for use in the prophylaxis or treatment of pain. Modulators for use in the prophylaxis or treatment of pain include compounds of formula (I) or a pharmaceutically acceptable salt and/or solvate thereof and/or derivative thereof:

100. 发明授权

US11267803B2 Carbocyclic prolinamide derivatives 有权
公开(公告)号：US11267803B2
公开(公告)日：2022-03-08
申请号：US16734740
申请日：2020-01-06
申请人： ORION OPHTHALMOLOGY LLC
发明人： Robert Gomez , Jinyue Ding , Renata Marcella Oballa , David Andrew Powell
IPC分类号： C07D403/04 , C07D207/50 , C07D405/14 , C07D471/04 , C07D401/14 , C07D401/04 , C07D403/14
摘要： This invention is directed to novel carbocyclic prolinamide derivatives of Formula (I), and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention. The compounds of the invention are inhibitors of HTRA1. Thus, the compounds of the invention are useful in the prevention and treatment of a wide range of diseases mediated (in whole or in part) by HTRA1. The compounds of the invention are also useful for inhibiting HTRA1 protease activity in an eye or locus of an arthritis or related condition.

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