- TYK2 INHIBITORS AND USES THEREOF
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Described herein are compounds that are useful in treating a TYK2-mediated disorder. In some embodiments, the TYK2-mediated disorder is an autoimmune disorder, an inflammatory disorder, a proliferative disorder, an endocrine disorder, a neurological disorder, or a disorder associated with transplantation.
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Paragraph 00405
(2020/09/27)
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- POLYCYCLIC COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES
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The present disclosure relates to bifunctional compounds, ULM— L—PTM, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A- RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
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Paragraph 2065 2066
(2020/03/29)
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- NOVEL STING AGONISTS
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The present invention provides compounds of Formula I′: wherein , W, X, Y, Z, Z1, Z2, R1, R2, R3, R4 and R5 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.
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Paragraph 0795; 0799; 0800
(2020/05/14)
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- QUINAZOLINONES AS PARP14 INHIBITORS
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The present invention relates to quinazolinones and related compounds which are inhibitors of PARP14 and are useful, for example, in the treatment of cancer and inflammatory diseases.
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Paragraph 0319
(2019/07/10)
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- Novel CDK inhibitory compounds, preparation method thereof, pharmaceutical composition for use in preventing or treating CDK relating diseases containing the same as an active ingredient
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The present invention relates to a novel CDK inhibitory compound, a method for manufacturing the same, and a pharmaceutical composition for preventing or treating a CDK-related disease containing the compound as an active ingredient. The novel CDK inhibit
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Paragraph 0287-0290
(2018/10/24)
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- ISOXAZOLE DERIVATIVES FOR USE IN THE TREATMENT OF PULMONARY DISEASES AND DISORDERS
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The present disclosure features disclosed method of treating disorders such as COPD, bronchitis and/or asthma using disclosed compounds, optionally together with one or more additional active agents. Contemplated methods include administrating orally or by inhalation to a patient one or more disclosed compounds.
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Paragraph 0088
(2017/03/21)
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- COMPOUNDS, COMPOSITIONS, AND METHODS FOR INCREASING CFTR ACTIVITY
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The present disclosure is directed to disclosed compounds that increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.
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Paragraph 0143
(2016/07/27)
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- DERIVATIVES OF 3-HETEROARYLISOXAZOL-5-CARBOXYLIC AMIDE USEFUL FOR THE TREATMENT OF INTER ALIA CYSTIC FIBROSIS
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The present disclosure is based, in part, on the discovery that disclosed compounds can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.
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Paragraph 0119
(2016/07/27)
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- COMPOUNDS, COMPOSITIONS AND METHODS FOR INCREASING CFTR ACTIVITY
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The present disclosure features compounds such as those having the Formulae (Ila), (lIb), (lIc), (Ild), (IlIa), and (Illb), which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound, such as a compound of Formula (Ila), (lIb), (lIc), (lId), (IlIa), or (Illb).
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Paragraph 0129
(2016/11/07)
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- N-ACYLETHANOLAMINE HYDROLYZING ACID AMIDASE (NAAA) INHIBITORS AND THEIR USE THEREOF
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A compound is represented as Formula I, a tautomer thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. Compounds of Formula I are inhibitors of N-acylethanolamine hydrolyzing acid amidase (NAAA). The present technology is directed to compounds, compositions, and methods to inhibit N-acylethanolamine hydrolyzing acid amidase and to treat N-acylethanolamine hydrolyzing acid amidase mediated conditions in a subject.
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- Highly potent HCV NS4B inhibitors with activity against multiple genotypes
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The exploration of novel inhibitors of the HCV NS4B protein that are based on a 2-oxadiazoloquinoline scaffold is described. Optimization to incorporate activity across genotypes led to a potent new series with broad activity, of which inhibitor 1 displayed the following EC50 values: 1a, 0.08 nM; 1b, 0.10 nM; 2a, 3 nM; 2b, 0.6 nM, 3a, 3.7 nM; 4a, 0.9 nM; 6a, 3.1 nM.
- Phillips, Barton,Cai, Ruby,Delaney, William,Du, Zhimin,Ji, Mingzhe,Jin, Haolun,Lee, Johnny,Li, Jiayao,Niedziela-Majka, Anita,Mish, Michael,Pyun, Hyung-Jung,Saugier, Joe,Tirunagari, Neeraj,Wang, Jianhong,Yang, Huiling,Wu, Qiaoyin,Sheng, Chris,Zonte, Catalin
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supporting information
p. 2161 - 2166
(2014/04/03)
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- HETEROBICYCLIC COMPOUNDS
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Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.
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Paragraph 0644
(2013/09/12)
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- HETEROARYLOXYCARBOCYCLYL COMPOUNDS AS PDE10 INHIBITORS
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Heteroaryloxycarbocyclyl compounds of formula (I), and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive -compulsive disorder, and the like. Formula (I)
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Page/Page column 47
(2011/12/02)
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- Cyclobutane-derived diamines: Synthesis and molecular structure
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Cyclobutane diamines (i.e., cis- and trans-1,3-diaminocyclobutane, 6-amino-3-azaspiro[3.3]heptane, and 3,6-diaminospiro[3.3]heptane) are considered as promising sterically constrained diamine building blocks for drug discovery. An approach to the syntheses of their Boc-monoprotected derivatives has been developed aimed at the preparation of multigram amounts of the compounds. These novel synthetic schemes exploit classical malonate alkylation chemistry for the construction of cyclobutane rings. The conformational preferences of the cyclobutane diamine derivatives have been evaluated by X-ray diffraction and compared with the literature data on sterically constrained diamines, which are among the constituents of commercially available drugs.
- Radchenko, Dmytro S.,Pavlenko, Sergiy O.,Grygorenko, Oleksandr O.,Volochnyuk, Dmitriy M.,Shishkina, Svitlana V.,Shishkin, Oleg V.,Komarov, Igor V.
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experimental part
p. 5941 - 5952
(2010/11/04)
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