444607-92-5Relevant academic research and scientific papers
Stereospecific ring-expanding skeletal rearrangement of isoindoline to tetrahydroisoquinoline via a sequential aziridine ring formation/opening
Kobayashi, Kenichi,Endo, Ryusei,Honma, Yusuke,Kasahara, Emi,Saito, Haruka,Tanaka, Kosaku,Suzuki, Momoko,Kogen, Hiroshi
, p. 1239 - 1250 (2019/07/31)
A stereospecific skeletal rearrangement of isoindoline to tetrahydroisoquinoline was developed under Appel reaction conditions using a combination of PPh3 and CCl4. This reaction involves a sequential ring formation/opening of a labile aziridine and enables the construction of a quaternary carbon center, offering a highly useful method for accessing 3,3,4-trisubstituted tetrahydroisoquinolines.
BICYCLIC AZA COMPOUNDS AS MUSCARINIC M1 RECEPTOR AGONISTS.
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Page/Page column 88, (2015/09/22)
This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R1 , R2, R3 and R4 are as defined herein.
Synthesis of arylglycine and mandelic acid derivatives through carboxylations of α-amido and α-acetoxy stannanes with carbon dioxide
Mita, Tsuyoshi,Sugawara, Masumi,Hasegawa, Hiroyuki,Sato, Yoshihiro
, p. 2159 - 2168 (2012/06/01)
Incorporation reactions of carbon dioxide (CO2) with N-Boc-α-amido and α-acetoxy stannanes were developed using CsF as a mild tin activator. Monoprotected α-amido stannanes could be used, and the corresponding arylglycine derivatives were obtained in moderate-to-high yields under 1 MPa (10 atm) of CO2 pressure. α-Acetoxy stannanes also underwent carboxylation to afford mandelic acid derivatives in excellent yields under ambient CO2 pressure. Both transformations enabled the synthesis of α-tertiary and α-quaternary carboxylic acid derivatives. In addition, the chirality of (S)-N-tert-butylsulfonyl-α- amido stannanes was transferred with up to 90% inversion of configuration at 100 °C.
Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARδ agonists
Luckhurst, Christopher A.,Stein, Linda A.,Furber, Mark,Webb, Nicola,Ratcliffe, Marianne J.,Allenby, Gary,Botterell, Sara,Tomlinson, Wendy,Martin, Barrie,Walding, Andrew
scheme or table, p. 492 - 496 (2011/02/28)
Small molecule isoindoline and tetrahydroisoquinoline derivatives have been identified as selective agonists of human peroxisome proliferator-activated receptor δ (PPARδ. Compound 18 demonstrated efficacy in a biomarker for increased fatty acid oxidation,
AMIDE RESORCINOL COMPOUNDS
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Page/Page column 63, (2008/12/05)
The present invention is directed to amide resorcinol compounds and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as HSP-90 inhibitors.
AMIDE RESORCINOL COMPOUNDS
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Page/Page column 39; 82-83, (2008/06/13)
The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as HSP-90 inhibitors.
Piperidinyl-alpha-aminoamide modulators of chemokine receptor activity
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Page/Page column 20, (2010/02/14)
The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, W, X, Z, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
ACYL ISOINDOLINE DERIVATIVES AND ACYL ISOQUINOLINE DERIVATIVES AS ANTI-VIRAL AGENTS
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Page 41, (2010/02/09)
Anti-viral agents of Formula (I) wherein: R3 represents aryl or heteroaryl; R4 represents one or two substituents independently selected from hydrogen, C 1-6alkyl, halo, ORA , C(O)NRBR
N-arylsulfonyl aza-bicyclic derivatives as potent cell adhesion inhibitors
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, (2008/06/13)
Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
N-arylsulfonyl aryl aza-bicyclic derivatives as potent cell adhesion inhibitors
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, (2008/06/13)
Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
