公开(公告)号：US20210171477A1

公开(公告)日：2021-06-10

申请号：US16632849

申请日：2018-07-23

申请人： NOVARTIS INFLAMMASOME RESEARCH, INC.

发明人： Luigi FRANCHI ,  Shomir GHOSH ,  Gary GLICK ,  Jason KATZ ,  Anthony William OPIPARI, Jr. ,  William ROUSH ,  Hans Martin SEIDEL ,  Dong-Ming SHEN ,  Shankar VENKATRAMAN ,  David Guenther WINKLER

IPC分类号： C07D277/36 ,  C07C307/06 ,  C07D307/64 ,  C07D333/34 ,  C07D263/46 ,  C07D213/71 ,  C07D231/18 ,  C07D487/04 ,  C07D215/36 ,  C07D317/62 ,  C07D307/79 ,  C07D239/26

摘要： In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured. The variables shown in Formula AA are as defined in the claims. The compounds of formula AA are NLRP3 activity modulators and, as such, can be used in the treatment of metabolic disorders (e.g. Type 2 diabetes, atherosclerosis, obesity or gout), a disease of the central nervous system (e.g. Alzheimer's disease, multiple sclerosis, Amyotrophic Lateral Sclerosis or Parkinson's disease), lung disease (e.g. asthma, COPD or pulmonary idiopathic fibrosis), liver disease (e.g. NASH syndrome, viral hepatitis or cirrhosis), pancreatic disease (e.g. acute pancreatitis or chronic pancreatitis), kidney disease (e.g. acute kidney injury or chronic kidney injury), intestinal disease (e.g. Crohn's disease or Ulcerative Colitis), skin disease (e.g. psoriasis), musculoskeletal disease (e.g. scleroderma), a vessel disorder (e.g. giant cell arteritis), a disorder of the bones (e.g. osteoarthritis, osteoporosis or osteopetrosis disorders), eye disease (e.g. glaucoma or macular degeneration), a disease caused by viral infection (e.g. HIV or AIDS), an autoimmune disease (e.g. Rheumatoid Arthritis, Systemic Lupus Erythematosus or Autoimmune Thyroiditis), cancer or aging.

公开(公告)号：US20210139445A1

公开(公告)日：2021-05-13

申请号：US17052937

申请日：2019-04-30

申请人： Semiconductor Energy Laboratory Co., Ltd.

发明人： Kyoko TAKEDA ,  Hiroshi KADOMA ,  Yusuke TAKITA ,  Tsunenori SUZUKI ,  Satoshi SEO

IPC分类号： C07D307/79 ,  H01L51/00

摘要： A novel organic compound is provided. Alternatively, an organic compound that exhibits light emission with favorable chromaticity is provided. Alternatively, an organic compound that exhibits blue light emission with favorable chromaticity is provided. Alternatively, a light-emitting device with favorable emission efficiency is provided. Alternatively, an organic compound having a high carrier-transport property is provided. Alternatively, an organic compound with favorable reliability is provided. An organic compound having at least one amino group in which any one of a substituted or unsubstituted dibenzofuranyl group, a substituted or unsubstituted dibenzothiophenyl group, and a substituted or unsubstituted carbazolyl group is bonded to any one of a substituted or unsubstituted naphthobisbenzofuran skeleton, a substituted or unsubstituted naphthobisbenzothiophene skeleton, and a substituted or unsubstituted naphthobenzothienobenzofuran skeleton is provided.

公开(公告)号：US20210087147A1

公开(公告)日：2021-03-25

申请号：US16635374

申请日：2018-07-31

申请人： Nodthera Limited

发明人： Mark G. BOCK ,  David HARRISON ,  Alan Paul WATT ,  Roderick Alan PORTER ,  Nicolas Felix Pierre BOUTARD ,  Charles-Henry Robert Yves FABRITIUS ,  Grzegorz Witold TOPOLNICKI ,  Oleksandr LEVENETS

IPC分类号： C07D231/12 ,  A61P37/06 ,  C07C271/30 ,  C07C263/10 ,  C07C209/36 ,  C07C201/14 ,  C07C45/68 ,  C07C271/28 ,  C07D307/79 ,  C07D213/55 ,  C07D233/60 ,  C07D231/14 ,  C07D241/12 ,  C07D237/08 ,  C07D249/08 ,  C07D239/26 ,  C07D409/12 ,  C07D493/04 ,  C07D309/12 ,  C07D241/24

摘要： The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as autoinflammatory and autoimmune diseases and cancers.

公开(公告)号：US10947180B2

公开(公告)日：2021-03-16

申请号：US16679026

申请日：2019-11-08

申请人： vTv Therapeutics LLC

发明人： Per Sauerberg ,  Pavel Pihera ,  Zdenek Polivka ,  Miroslav Havranek ,  Ingrid Petterson ,  John Patrick Mogensen

IPC分类号： C07C69/736 ,  A61K31/5375 ,  A61K31/415 ,  C07C59/70 ,  C07C217/48 ,  C07C323/16 ,  C07C323/32 ,  C07D211/46 ,  C07D213/30 ,  C07D231/12 ,  C07D295/096 ,  C07D307/79 ,  C07D333/16 ,  C07D333/54 ,  C07D265/30 ,  C07D213/36 ,  C07D295/112 ,  C07D307/81 ,  C07D333/20 ,  A61K31/192 ,  A61K31/195 ,  A61K31/343 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/4402 ,  A61K31/445 ,  A61K31/495 ,  A61K31/5377

摘要： Phenoxy acetic acids and phenyl propionic acids and their use in improving mitochondrial energy output in a subject are provided herein. The present compounds are activators of PPARδ and may be useful for treating conditions mediated by the same.

公开(公告)号：US10772858B2

公开(公告)日：2020-09-15

申请号：US15570969

申请日：2016-05-02

申请人： GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION ,  Emory University

发明人： Binghe Wang ,  Erwin Van Meir ,  Jalisa Holmes Ferguson ,  Stefan Kaluz ,  Xingyue Ji

IPC分类号： A61K31/192 ,  A61K31/495 ,  A01N31/04 ,  A61K31/7068 ,  A61K31/536 ,  A61K31/435 ,  A61K31/175 ,  A61K31/17 ,  A61K31/475 ,  A61K31/166 ,  A61P35/00 ,  A61K31/085 ,  A61K31/09 ,  A61K31/341 ,  A61K31/343 ,  A61K31/351 ,  A61K31/352 ,  A61K31/357 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/421 ,  A61K31/436 ,  A61K31/443 ,  A61K31/444 ,  A61K31/445 ,  A61K31/5375 ,  A61K31/538 ,  A61K45/06 ,  C07C43/295 ,  C07D205/04 ,  C07D207/12 ,  C07D211/46 ,  C07D213/65 ,  C07D263/32 ,  C07D265/36 ,  C07D295/096 ,  C07D307/12 ,  C07D307/20 ,  C07D307/79 ,  C07D309/10 ,  C07D311/70 ,  C07D319/16 ,  C07D333/54 ,  C07D405/12 ,  C07D491/052

摘要： This disclosure relates to benzhydrol derivatives for managing conditions related to the Hypoxia Inducible Factor (HIF) pathway such as uses in treating cancer. In certain embodiment, the disclosure contemplates compounds and pharmaceutical compositions. In certain embodiment, the disclosure contemplates compounds disclosed herein as prodrugs, optionally substituted with one or more substituents, derivatives, or salts thereof.

公开(公告)号：US20200179385A1

公开(公告)日：2020-06-11

申请号：US16725709

申请日：2019-12-23

申请人： Autifony Therapeutics Limited

发明人： Giuseppe ALVARO ,  Agostino MARASCO

IPC分类号： A61K31/506 ,  A61K31/4439 ,  C07D317/46 ,  C07D405/14 ,  C07D307/94 ,  C07D307/79 ,  C07D413/14 ,  C07D405/12 ,  C07D413/12

摘要： The invention provides compounds of formula (I): Said compounds being modulators of Kv3 channels and of use in the prophylaxis or treatment of related disorders.

公开(公告)号：US10654820B2

公开(公告)日：2020-05-19

申请号：US16300303

申请日：2017-02-19

申请人： ZHEJIANG JINGXIN PHARMACEUTICAL CO., LTD.

发明人： Jianrong Zhu ,  Chunyong Peng ,  Hongban Zhong ,  Xiurong Hu

IPC分类号： C07D307/79 ,  A61K31/343 ,  B01D9/00 ,  A61P25/20

摘要： Crystal forms I and II of tasimelteon. Crystal form I: an X-ray powder diffraction spectrum using CuKα radiation and represented by a 2θ angle has diffraction peaks at least at 7.2°±0.2°, 7.9°±0.2°, 10.6°±0.2°, 14.4°±0.2°, 15.9°±0.2°, 17.3°±0.2°, 21.0°±0.2°, 23.2°±0.2°, and 24.4°±0.2°. Crystal form II: an X-ray powder diffraction spectrum using CuKα radiation and represented by a 2θ angle has diffraction peaks at least at 6.8°±0.2°, 12.1°±0.2°, 12.5°±0.2°, 13.1°±0.2°, 13.6°±0.2°, 13.8°±0.2°, 15.8°±0.2°, 17.0°±0.2°, 18.4°±0.2°, 20.8°±0.2°, 24.2°±0.2°, and 24.4°±0.2°. Crystal forms I and II of tasimelteon have advantages of excellent physicochemical property, good stability and solubility, and simple operation for preparation.

公开(公告)号：US20200049699A1

公开(公告)日：2020-02-13

申请号：US16437049

申请日：2019-06-11

申请人： Firmenich Incorporated

发明人： Xiaodong LI ,  Lena LUUKKONEN ,  Hong XU

IPC分类号： G01N33/543 ,  C07C233/65 ,  C07C235/54 ,  C07C275/30 ,  C07C275/34 ,  C07D307/84 ,  C07D317/68 ,  G01N33/566 ,  G01N33/74 ,  A23L27/20 ,  C07D263/56 ,  C07D213/81 ,  C07D213/85 ,  C07D215/48 ,  C07D217/06 ,  C07D231/14 ,  C07D333/24 ,  C07D333/38 ,  C07D401/04 ,  C07D409/12 ,  C07D417/12 ,  C07D261/18 ,  C07D271/12 ,  C07D275/03 ,  C07D209/08 ,  C07D277/64 ,  C07D209/42 ,  C07D285/135 ,  C07D213/40 ,  C07D307/52 ,  C07D307/68 ,  C07D307/79 ,  C07D307/82 ,  G01N33/50 ,  A23L2/56 ,  A61K8/49 ,  A61K8/55 ,  A61K47/22 ,  A61K47/24 ,  C07D405/12 ,  C07F9/655 ,  A23L27/00

摘要： The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units thereof. The present invention also relates to the use of hetero-oligomeric and chimeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.

公开(公告)号：US10471066B2

公开(公告)日：2019-11-12

申请号：US15817470

申请日：2017-11-20

申请人： vTv Therapeutics LLC

发明人： Per Sauerberg ,  Pavel Pihera ,  Zdenek Polivka ,  Miroslav Havranek ,  Ingrid Pettersson ,  John Patrick Mogensen

IPC分类号： A61K31/415 ,  A61K31/5375 ,  A61K31/5377 ,  C07C59/70 ,  C07C217/48 ,  C07C323/16 ,  C07C323/32 ,  C07D211/46 ,  C07D213/30 ,  C07D231/12 ,  C07D295/096 ,  C07D307/79 ,  C07D333/16 ,  C07D333/54 ,  C07D265/30 ,  C07D213/36 ,  C07D295/112 ,  C07D307/81 ,  C07D333/20 ,  A61K31/192 ,  A61K31/195 ,  A61K31/343 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/4402 ,  A61K31/445 ,  A61K31/495

摘要： Phenoxy acetic acids and phenyl propionic acids and their use in improving mitochondrial energy output in a subject are provided herein. The present compounds are activators of PPARδ and may be useful for treating conditions mediated by the same.

公开(公告)号：US20190315735A1

公开(公告)日：2019-10-17

申请号：US16455359

申请日：2019-06-27

申请人： Takeda Pharmaceutical Company Limited

发明人： Shigemitsu MATSUMOTO ,  Yasushi HATTORI ,  Masashi TOYOFUKU ,  Shinji MORIMOTO ,  Masaki DAINI ,  Takuto KOJIMA ,  Tomohiro KAKU ,  Mitsuhiro ITO

IPC分类号： C07D417/14 ,  C07D333/38 ,  C07D413/14 ,  C07D407/12 ,  C07D307/79 ,  C07D409/12 ,  C07D417/12 ,  C07D307/81 ,  C07D413/12 ,  C07D409/14 ,  C07D231/12 ,  C07D277/56 ,  C07D285/135 ,  C07D285/08 ,  C07D333/40 ,  C07D231/14 ,  C07D213/82

摘要： The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.