676371-64-5Relevant academic research and scientific papers
Large-Scale Synthesis and Modifications of Bicyclo[1.1.1]pentane-1,3-dicarboxylic Acid (BCP)
Ripenko, Vasyl,Vysochyn, Daniil,Klymov, Ivan,Zhersh, Serhii,Mykhailiuk, Pavel K.
, p. 14061 - 14068 (2021/07/20)
In flow photochemical addition of propellane to diacetyl allowed construction of the bicyclo[1.1.1]pentane (BCP) core in a 1 kg scale within 1 day. Haloform reaction of the formed diketone in batch afforded bicyclo[1.1.1]pentane-1,3-dicarboxylic acid in a
ANTI-HUMAN VISTA ANTIBODIES AND USE THEREOF
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Paragraph 442; 474, (2021/10/30)
The invention provides anti-VISTA antibody drug conjugates which may be used for targeted delivery of anti-inflammatory agents such as steroids to immune cells, e.g., myeloid cells. The invention also provides methods of using anti-VISTA antibody drug conjugates in the treatment of inflammatory and/or autoimmune conditions and/or for alleviating the toxicity of anti-inflammatory agents such as steroids.
Photochemical Formal (4 + 2)-Cycloaddition of Imine-Substituted Bicyclo[1.1.1]pentanes and Alkenes
Harmata, Alexander S.,Sowden, Madison J.,Spiller, Taylor E.,Stephenson, Corey R. J.
supporting information, p. 21223 - 21228 (2021/12/27)
Amines containing bridged bicyclic carbon skeletons are desirable building blocks for medicinal chemistry. Herein, we report the conversion of bicyclo[1.1.1]pentan-1-amines to a wide range of polysubstituted bicyclo[3.1.1]heptan-1-amines through a photochemical, formal (4 + 2)-cycloaddition of an intermediate imine diradical. To our knowledge, this is the first reported method to convert the bicyclo[1.1.1]pentane skeleton to the bicyclo[3.1.1]heptane skeleton. Hydrolysis of the imine products gives complex, sp3-rich primary amine building blocks.
HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Page/Page column 54; 55, (2019/01/17)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Paragraph 00121; 00122, (2019/05/30)
Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositons thereof, which are useful for treating a variety of conditions associated with methyl modifying enzymes.
NOVEL [1.1.1] BICYCLO COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS
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Page/Page column 40, (2019/11/12)
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
3-(5-AMINO-PYRAZIN-2-YL)-BENZENESULFONAMIDE DERIVATIVES AND RELATED COMPOUNDS AS PI3K-GAMMA KINASE INHIBITORS FOR TREATING E.G. CANCER
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, (2019/07/13)
This application relates to compounds of Formula (I) or pharmaceutically acceptable salts thereof, which are inhibitors of ΡΙ3Κ-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
PYRIMIDINE DERIVATIVES
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Page/Page column 26, (2019/06/11)
The invention provides new pyrimidine compounds having the general formula (I), wherein R1, R2, R3, n, and X are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
BICYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER
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Paragraph 00263, (2018/11/22)
The present disclosure is directed to novel compounds 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 cancer, including glioblastoma, bone cancer, head and neck cancer, melanoma, basal cell carcinoma, squamous cell carcinoma, adenocarcinoma, oral cancer, esophageal cancer, gastric cancer, intestinal cancer, colon cancer, bladder cancer, hepatocellular carcinoma, renal cell carcinoma, pancreatic cancer, ovarian cancer, cervical cancer, lung cancer, breast cancer, and prostate cancer. The compounds of the disclosure are selective antagonists of the EP4 receptor and useful treatment of various diseases that may be ameliorated with blockade of PGE2-mediated signaling.
ANALGESIC COMPOUNDS
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Paragraph 0252, (2018/12/13)
Disclosed herein are compounds of Formulae (la), (lb), (Ic), (Id), (le), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It), methods of synthesizing compounds of Formulae (la), (lb), (Ic), (Id), (le), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It), and methods of using compounds of Formulae (la), (lb), (Ic), (Id), (le), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It) as an analgesic.
