65202-50-8Relevant articles and documents
HETEROARYL SUBSTITUTED 3-(1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE DERIVATIVES AND USES THEREOF
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Page/Page column 327-328, (2022/02/15)
The present disclosure provides a compound of Formula (I): (I), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein Rx and X1 are as defined herein, and methods of making and using same.
INHIBITOR COMPOUNDS
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Page/Page column 63; 85; 90-91, (2021/01/29)
The disclosure relates to heterocyclic compounds and methods for their preparation. The disclosure provides compounds that may have beneficial therapeutic activity in the treatment of a disease or condition mediated by excessive or otherwise undesirable Des1 and/or fibrotic activity.
METHODS OF MANUFACTURING A BIFUNCTIONAL COMPOUND, ULTRAPURE FORMS OF THE BIFUNCTIONAL COMPOUND, AND DOSAGE FORMS COMPRISING THE SAME
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Paragraph 0475-0476, (2021/11/20)
The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A: The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
Development of a Scalable Synthesis of the Small Molecule TGFβR1 Inhibitor BMS-986260
Vetrichelvan, Muthalagu,Rakshit, Souvik,Chandrasekaran, Sathishkumar,Chinnakalai, Karthikeyan,Darne, Chetan Padmakar,Doddalingappa, Dyamanna,Gopikumar, Indasi,Gupta, Anuradha,Gupta, Arun Kumar,Karmakar, Ananta,Lakshminarasimhan, Thirumalai,Leahy, David K.,Palani, Senthil,Radhakrishnan, Vignesh,Rampulla, Richard,Savarimuthu, Antony,Subramanian, Varadharajan,Velaparthi, Upender,Warrier, Jayakumar,Eastgate, Martin D.,Borzilleri, Robert M.,Mathur, Arvind,Vaidyanathan, Rajappa
, p. 1310 - 1320 (2020/07/24)
A scalable route to the small molecule TGFβR1 inhibitor BMS-986260 (1) was developed. This alternative approach circumvented the purification of intermediates by column chromatography and provided access to multikilogram quantities of the key intermediate
2-ARYLSULFONAMIDO-N-ARYLACETAMIDE DERIVATIZED STAT3 INHIBITORS
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Paragraph 00770; 00772; 00781; 00783, (2018/08/20)
The present disclosure provides pharmaceutical compositions comprising 2-arylsulfonamido-N-arylacetamide derivatized Stat3 inhibitors and certain pharmaceutically acceptable salts thereof, and methods of their use.
VINYL COMPOUNDS AS FGFR AND VEGFR INHIBITORS
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, (2018/06/23)
FGFR and VEGFR inhibitors are provided, and compounds represented by formula (1) or formula (II) as FGFR and VEGFR inhibitors, pharmaceutically acceptable salts or tautomers thereof are specifically disclosed.
Piperazine derivatives and their use as therapeutic agents
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, (2016/03/19)
Compounds for treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the compounds are of formula (I): where x y, W, V, R 2 , R 3 , R 4 , R 5 , R 6 , R 6a , R 7 , R 7a , R 8 , R 8a , R 9 and R 9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
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Page/Page column 49, (2015/12/08)
The present invention is directed to substituted five membered heteroaryl benzamide compounds compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
NOVEL COMPOUNDS FOR MODULATION OF ROR-GAMMA ACTIVITY
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Paragraph 00320, (2014/03/22)
The present invention relates to aryl sulfones and related compounds that are modulators of ROR-gamma receptors. The invention also provides pharmaceutical compositions comprising these modulators, and methods of modulating ROR-gamma receptors using them. Also provided are methods of using aryl sulfones and related compounds as modulators of ROR-gamma to treat ROR-gamma mediated diseases
CXCR7 ANTAGONISTS
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Paragraph 0333; 0334, (2014/06/23)
Compounds having formula I, or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient.
